thiophenes

Summary

Top Publications

  1. pmc Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes
    Julio Rosenstock
    Dallas Diabetes and Endocrine Center at Medical City, Dallas, Texas, USA
    Diabetes Care 35:1232-8. 2012
  2. pmc Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise
    K Stenlof
    Clinical Trial Center, Sahlgrenska University Hospital, Gothenburg, Sweden
    Diabetes Obes Metab 15:372-82. 2013
  3. ncbi Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin
    D Devineni
    Janssen Research and Development, LLC, Raritan, NJ 08869, USA
    Diabetes Obes Metab 14:539-45. 2012
  4. ncbi Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects
    S Sha
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ 08869, USA
    Diabetes Obes Metab 13:669-72. 2011
  5. pmc Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models
    Yin Liang
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Spring House, Pennsylvania, United States of America
    PLoS ONE 7:e30555. 2012
  6. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after hip arthroplasty
    Bengt I Eriksson
    Sahlgrenska University Hospital Ostra, Gothenburg, Sweden
    N Engl J Med 358:2765-75. 2008
  7. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty
    Michael R Lassen
    Nordsjaellands Hospital, Hørsholm, Denmark
    N Engl J Med 358:2776-86. 2008
  8. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty (RECORD4): a randomised trial
    Alexander G G Turpie
    McMaster University, Hamilton, Ontario L8L 2X2, Canada
    Lancet 373:1673-80. 2009
  9. ncbi Dual effect of strontium ranelate: stimulation of osteoblast differentiation and inhibition of osteoclast formation and resorption in vitro
    Edith Bonnelye
    Laboratoire de Génomique Fonctionelle de Lyon, Université de Lyon UMR5242, CNRS INRA ENS Université Lyon1 IFR 128 Biosciences Lyon Gerland, 46, Allee d Italie, 69007 Lyon, France
    Bone 42:129-38. 2008
  10. ncbi Prasugrel versus clopidogrel in patients with acute coronary syndromes
    Stephen D Wiviott
    Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    N Engl J Med 357:2001-15. 2007

Detail Information

Publications347 found, 100 shown here

  1. pmc Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes
    Julio Rosenstock
    Dallas Diabetes and Endocrine Center at Medical City, Dallas, Texas, USA
    Diabetes Care 35:1232-8. 2012
    ..To evaluate the effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, in type 2 diabetes mellitus inadequately controlled with metformin monotherapy...
  2. pmc Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise
    K Stenlof
    Clinical Trial Center, Sahlgrenska University Hospital, Gothenburg, Sweden
    Diabetes Obes Metab 15:372-82. 2013
    ..Canagliflozin is a sodium glucose co-transporter 2 inhibitor in development for type 2 diabetes mellitus (T2DM). The efficacy and safety of canagliflozin were evaluated in subjects with T2DM inadequately controlled with diet and exercise...
  3. ncbi Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin
    D Devineni
    Janssen Research and Development, LLC, Raritan, NJ 08869, USA
    Diabetes Obes Metab 14:539-45. 2012
    ..Canagliflozin is a sodium-glucose co-transporter 2 (SGLT2) inhibitor that is being investigated for the treatment of type 2 diabetes mellitus (T2DM)...
  4. ncbi Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects
    S Sha
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ 08869, USA
    Diabetes Obes Metab 13:669-72. 2011
    ..Canagliflozin was generally well tolerated; most adverse events were mild and no hypoglycaemia was reported. These results support further study of canagliflozin...
  5. pmc Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models
    Yin Liang
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Spring House, Pennsylvania, United States of America
    PLoS ONE 7:e30555. 2012
    ..Canagliflozin is a sodium glucose co-transporter (SGLT) 2 inhibitor in clinical development for the treatment of type 2 diabetes mellitus (T2DM)...
  6. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after hip arthroplasty
    Bengt I Eriksson
    Sahlgrenska University Hospital Ostra, Gothenburg, Sweden
    N Engl J Med 358:2765-75. 2008
    ..This phase 3 trial compared the efficacy and safety of rivaroxaban, an oral direct inhibitor of factor Xa, with those of enoxaparin for extended thromboprophylaxis in patients undergoing total hip arthroplasty...
  7. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty
    Michael R Lassen
    Nordsjaellands Hospital, Hørsholm, Denmark
    N Engl J Med 358:2776-86. 2008
    ..We investigated the efficacy of rivaroxaban, an orally active direct factor Xa inhibitor, in preventing venous thrombosis after total knee arthroplasty...
  8. ncbi Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty (RECORD4): a randomised trial
    Alexander G G Turpie
    McMaster University, Hamilton, Ontario L8L 2X2, Canada
    Lancet 373:1673-80. 2009
    ..We aimed to test the efficacy and safety of oral rivaroxaban for the prevention of venous thromboembolism after total knee arthroplasty...
  9. ncbi Dual effect of strontium ranelate: stimulation of osteoblast differentiation and inhibition of osteoclast formation and resorption in vitro
    Edith Bonnelye
    Laboratoire de Génomique Fonctionelle de Lyon, Université de Lyon UMR5242, CNRS INRA ENS Université Lyon1 IFR 128 Biosciences Lyon Gerland, 46, Allee d Italie, 69007 Lyon, France
    Bone 42:129-38. 2008
    ..It stimulates bone formation through its positive action on osteoblast differentiation and function, and decreases osteoclast differentiation as well as function by disrupting actin cytoskeleton organization...
  10. ncbi Prasugrel versus clopidogrel in patients with acute coronary syndromes
    Stephen D Wiviott
    Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    N Engl J Med 357:2001-15. 2007
    ..Dual-antiplatelet therapy with aspirin and a thienopyridine is a cornerstone of treatment to prevent thrombotic complications of acute coronary syndromes and percutaneous coronary intervention...
  11. ncbi Extended duration rivaroxaban versus short-term enoxaparin for the prevention of venous thromboembolism after total hip arthroplasty: a double-blind, randomised controlled trial
    Ajay K Kakkar
    Barts and the London School of Medicine and Dentistry, London, UK
    Lancet 372:31-9. 2008
    ..Our aim was to compare the use of rivaroxaban for extended thromboprophylaxis with short-term thromboprophylaxis with enoxaparin...
  12. ncbi AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
    Sonya D Zabludoff
    AstraZeneca R and D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
    Mol Cancer Ther 7:2955-66. 2008
    ....
  13. ncbi Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor
    Dagmar Kubitza
    Bayer HealthCare AG, Institute of Clinical Pharmocology, D 42096 Wuppertal, Germany
    Clin Pharmacol Ther 78:412-21. 2005
    ..The aim of this study was to investigate the safety, pharmacodynamics, and pharmacokinetics of BAY 59--7939, an oral, direct factor Xa inhibitor...
  14. ncbi Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939--an oral, direct Factor Xa inhibitor--after multiple dosing in healthy male subjects
    Dagmar Kubitza
    Institute of Clinical Pharmacology, Bayer HealthCare AG, 42096 Wuppertal, Germany
    Eur J Clin Pharmacol 61:873-80. 2005
    ....
  15. pmc Rotigotine effects on early morning motor function and sleep in Parkinson's disease: a double-blind, randomized, placebo-controlled study (RECOVER)
    Claudia Trenkwalder
    Department of Clinical Neurophysiology, University of Goettingen and Paracelsus Elena Klinik, Kassel, Germany
    Mov Disord 26:90-9. 2011
    ..Twenty-four-hour transdermal delivery of rotigotine to PD patients with early-morning motor dysfunction resulted in significant benefits in control of both motor function and nocturnal sleep disturbances...
  16. ncbi Dose-escalation study of the pharmacokinetics and pharmacodynamics of rivaroxaban in healthy elderly subjects
    Dagmar Kubitza
    Clinical Pharmacology, Bayer HealthCare AG, D 42096 Wuppertal, Germany
    Curr Med Res Opin 24:2757-65. 2008
    ..The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of rivaroxaban--a novel, oral, direct Factor Xa (FXa) inhibitor--in healthy elderly subjects...
  17. ncbi Assessment of laboratory assays to measure rivaroxaban--an oral, direct factor Xa inhibitor
    Meyer Michel Samama
    Hotel Dieu University Hospital, Paris, France 2Biomnis Laboratory, Ivry sur Seine, France
    Thromb Haemost 103:815-25. 2010
    ..Finally, all clotting and chromogenic assays showed a concentration-dependent effect induced by rivaroxaban...
  18. ncbi Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus
    Sumihiro Nomura
    Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 2 2 50 Kawagishi, Toda, Saitama, Japan
    J Med Chem 53:6355-60. 2010
    ..A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice...
  19. ncbi P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use
    Lars Wallentin
    Uppsala Clinical Research Centre, University Hospital, Uppsala SE 75185, Sweden
    Eur Heart J 30:1964-77. 2009
    ..The objectives of this systematic review are to summarize the pharmacokinetics, pharmacodynamics, and pharmacogenetics of the different P2Y(12) inhibitors and to discuss the clinical implications for treatment of patients...
  20. ncbi Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and
    Patricia L Podolin
    Respiratory and Inflammation Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406, USA
    J Pharmacol Exp Ther 312:373-81. 2005
    ..5 mg/kg, i.p., every other day. These results suggest that reduction of proinflammatory mediators and inhibition of antigen-induced T cell proliferation are mechanisms underlying the attenuation of CIA by the IKK-2 inhibitor, TPCA-1...
  21. ncbi Population pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor Xa inhibitor--in patients undergoing major orthopaedic surgery
    Wolfgang Mueck
    Clinical Pharmacology, Bayer HealthCare AG, Aprather Weg 18a, Wuppertal, Germany
    Clin Pharmacokinet 47:203-16. 2008
    ....
  22. ncbi Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist
    Barry G Shearer
    Research and Development, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Mol Endocrinol 22:523-9. 2008
    ..Here we describe the first report of a PPARbeta/delta small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPARbeta/delta...
  23. ncbi The clinical efficacy of a topical dorzolamide in the management of cystoid macular edema in patients with retinitis pigmentosa
    Yasuhiro Ikeda
    Department of Ophthalmology, Graduate School of Medical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Graefes Arch Clin Exp Ophthalmol 250:809-14. 2012
    ..The objective of this work was to evaluate the clinical efficacy of a topical dorzolamide (a carbonic anhydrase inhibitor) in CME associated with RP...
  24. ncbi Strontium ranelate inhibits key factors affecting bone remodeling in human osteoarthritic subchondral bone osteoblasts
    Steeve Kwan Tat
    Osteoarthritis Research Unit, University of Montreal Hospital Research Centre, Montreal, Quebec, Canada
    Bone 49:559-67. 2011
    ..In this study, we investigated in human OA subchondral bone osteoblasts the modulatory effect of strontium ranelate on the above key factors...
  25. ncbi Effects of the oral, direct factor xa inhibitor rivaroxaban on platelet-induced thrombin generation and prothrombinase activity
    Jochen Graff
    Pharmazentrum frankfurt ZAFES, Institute of Clinical Pharmacology, University Hospital, Frankfurt Main, Theodor Stern Kai 7, D 60590 Frankfurt am Main, Germany
    J Clin Pharmacol 47:1398-407. 2007
    ..Rivaroxaban strongly inhibits platelet-induced thrombin generation, after activation of either platelets or the coagulation pathway, even in the presence of minimal factor Xa inhibition in plasma...
  26. ncbi Rate of nuisance bleedings and impact on compliance to prasugrel in acute coronary syndromes
    Sebastien Armero
    Departement de Cardiologie, Hopital Universitaire Nord, Faculte de Medecine, Universite de la Mediterranee, Marseille, France
    Am J Cardiol 108:1710-3. 2011
    ..In conclusion, in the present study, minor bleedings were common during the first month after percutaneous coronary intervention and were significantly associated with prasugrel withdrawal...
  27. ncbi Rotigotine transdermal patch in early Parkinson's disease: a randomized, double-blind, controlled study versus placebo and ropinirole
    Nir Giladi
    Movement Disorders Unit, Department of Neurology, Tel Aviv Sourasky Medical Center, Sackler School of Medicine, Tel Aviv University, Tel Aviv, Israel
    Mov Disord 22:2398-404. 2007
    ..Application-site reactions were predominantly mild or moderate in intensity. In conclusion, the rotigotine transdermal patch represents an effective and safe option for the treatment of patients with early Parkinson's disease...
  28. pmc Rebalancing bone turnover in favour of formation with strontium ranelate: implications for bone strength
    J E Fonseca
    Rheumatology Research Unit, Instituto de Medicina Molecular, Edificio Egas Moniz, Faculdade de Medicina da Universidade de Lisboa, Av Professor Egas Moniz, 1649 028 Lisboa, Portugal
    Rheumatology (Oxford) 47:iv17-19. 2008
    ..The overall effect is a rebalanced bone turnover in favour of improved bone geometry, cortical thickness, trabecular bone morphology and intrinsic bone tissue quality, which translates into enhanced bone strength...
  29. ncbi Efficacy of pramipexole and transdermal rotigotine in advanced Parkinson's disease: a double-blind, double-dummy, randomised controlled trial
    Werner H Poewe
    Department of Neurology, Innsbruck Medical University, Innsbruck, Austria
    Lancet Neurol 6:513-20. 2007
    ....
  30. ncbi Prasugrel overcomes high on-clopidogrel platelet reactivity post-stenting more effectively than high-dose (150-mg) clopidogrel: the importance of CYP2C19*2 genotyping
    Dimitrios Alexopoulos
    Department of Cardiology, Patras University Hospital, Patras, Greece
    JACC Cardiovasc Interv 4:403-10. 2011
    ....
  31. ncbi High-affinity peroxisome proliferator-activated receptor β/δ-specific ligands with pure antagonistic or inverse agonistic properties
    Simone Naruhn
    Institute of Molecular Biology and Tumor Research IMT, Philipps University, Marburg, Germany
    Mol Pharmacol 80:828-38. 2011
    ..The possibility to differentially modulate specific functions of PPARβ/δ makes these novel compounds invaluable tools to advance our understanding of PPARβ/δ biology...
  32. ncbi Evaluation of vulvovaginal symptoms and Candida colonization in women with type 2 diabetes mellitus treated with canagliflozin, a sodium glucose co-transporter 2 inhibitor
    Paul Nyirjesy
    Department of Obstetrics and Gynecology, Drexel University College of Medicine, Philadelphia, PA 19102, USA
    Curr Med Res Opin 28:1173-8. 2012
    ..Vaginal Candida colonization and symptomatic vulvovaginal adverse events (VVAE) were assessed in females with T2DM treated with canagliflozin, a SGLT2 inhibitor...
  33. ncbi Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study
    Lindsay E Nicolle
    University of Manitoba, Winnipeg, Canada
    Curr Med Res Opin 28:1167-71. 2012
    ..To examine the effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor that lowers blood glucose by increasing urinary glucose excretion (UGE), on asymptomatic bacteriuria and urinary tract infections (UTIs)...
  34. ncbi Small organic probes as amyloid specific ligands--past and recent molecular scaffolds
    K Peter R Nilsson
    Department of Chemistry, IFM, Linkoping University, Linkoping, Sweden
    FEBS Lett 583:2593-9. 2009
    ..In this review, past and recent molecular scaffolds that have been utilized for the development of small organic amyloid imaging agents are discussed...
  35. pmc Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB
    Douglas Kojetin
    ACS Chem Biol 6:131-4. 2011
    ..Thus, SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions...
  36. ncbi Morbidity and Mortality After Stroke, Eprosartan Compared with Nitrendipine for Secondary Prevention: principal results of a prospective randomized controlled study (MOSES)
    Joachim Schrader
    Department of Internal Medicine, St Josefs Hospital, Cloppenburg, Germany
    Stroke 36:1218-26. 2005
    ..In hypertensive stroke patients, for the same level of blood pressure control, eprosartan will be more effective than nitrendipine in reducing cerebrovascular and cardiovascular morbidity and mortality...
  37. ncbi Strontium ranelate promotes osteoblastic cell replication through at least two different mechanisms
    Joseph Caverzasio
    Service of Bone Diseases, Department of Rehabilitation and Geriatrics, University Hospital of Geneva, CH 1211 Geneva 14, Switzerland
    Bone 42:1131-6. 2008
    ....
  38. ncbi Strontium ranelate does not stimulate bone formation in ovariectomized rats
    R K Fuchs
    Department of Anatomy and Cell Biology, Indiana University School of Medicine, Indianapolis, IN, USA
    Osteoporos Int 19:1331-41. 2008
    ..We evaluated the effects of SrR on the skeleton in ovariectomized (OVX) rats and evaluated the influence of dietary calcium...
  39. ncbi Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome
    Barbara Cool
    Department of Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Cell Metab 3:403-16. 2006
    ..These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome...
  40. ncbi Duloxetine: clinical pharmacokinetics and drug interactions
    Mary Pat Knadler
    Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    Clin Pharmacokinet 50:281-94. 2011
    ..While duloxetine is generally well tolerated, it is important to be knowledgeable about the potential for pharmacokinetic interactions between duloxetine and drugs that inhibit CYP1A2 or drugs that are metabolized by CYP2D6 enzymes...
  41. ncbi Strontium ranelate: a review of its use in the treatment of postmenopausal osteoporosis
    Emma D Deeks
    Adis, Auckland, New Zealand
    Drugs 70:733-59. 2010
    ..Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis...
  42. ncbi Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin
    Patrizia Diana
    Dipartimento Farmacochimico Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Bioorg Med Chem Lett 17:2342-6. 2007
    ....
  43. ncbi Dabigatran and rivaroxaban for prevention of venous thromboembolism--systematic review and adjusted indirect comparison
    Y K Loke
    School of Medicine, Health Policy and Practice, University of East Anglia, Norwich, UK
    J Clin Pharm Ther 36:111-24. 2011
    ..Dabigatran and rivaroxaban are new oral anticoagulants for thromboprophylaxis after elective orthopaedic surgery. We aimed to systematically compare their relative benefits and harms through meta-analysis, and adjusted indirect comparison...
  44. ncbi Bone material quality in transiliac bone biopsies of postmenopausal osteoporotic women after 3 years of strontium ranelate treatment
    Paul Roschger
    Ludwig Boltzmann Institute of Osteology at the Hanusch Hospital of WGKK and AUVA Trauma Centre Meidling, 4th Medical Department, Hanusch Hospital, 1140 Vienna, Austria
    J Bone Miner Res 25:891-900. 2010
    ..Taken together, these data provide evidence that the investigated bone quality determinants at tissue level were preserved in postmenopausal osteoporotic women after 3-year treatment with 2 g SrR per day plus calcium and vitamin D...
  45. pmc Potent induction of total cellular GSH and NQO1 as well as mitochondrial GSH by 3H-1,2-dithiole-3-thione in SH-SY5Y neuroblastoma cells and primary human neurons: protection against neurocytotoxicity elicited by dopamine, 6-hydroxydopamine, 4-hydroxy-2-no
    Zhenquan Jia
    Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, 2265 Kraft Drive, Blacksburg, VA 24060, USA
    Brain Res 1197:159-69. 2008
    ....
  46. ncbi Cost-effectiveness of rivaroxaban compared to warfarin for stroke prevention in atrial fibrillation
    Soyon Lee
    University of Connecticut School of Pharmacy, Storrs, CT, USA
    Am J Cardiol 110:845-51. 2012
    ..In conclusion, this Markov model suggests that rivaroxaban therapy may be a cost-effective alternative to adjusted-dose warfarin for stroke prevention in AF...
  47. ncbi Rivaroxaban compared with warfarin in patients with atrial fibrillation and previous stroke or transient ischaemic attack: a subgroup analysis of ROCKET AF
    Graeme J Hankey
    Stroke Unit, Department of Neurology, Royal Perth Hospital, Perth, Australia
    Lancet Neurol 11:315-22. 2012
    ..We aimed to investigate whether the efficacy and safety of rivaroxaban compared with warfarin is consistent among the subgroups of patients with and without previous stroke or transient ischaemic attack (TIA)...
  48. ncbi Advanced Parkinson disease treated with rotigotine transdermal system: PREFER Study
    Peter A LeWitt
    Clinical Neuroscience Center, Southfield, MI 48034, USA
    Neurology 68:1262-7. 2007
    ..In patients experiencing motor fluctuations, a major treatment challenge is the reduction of "off" time, particularly upon awakening. Rotigotine (Neupro) is a novel dopaminergic agonist with 24-hour transdermal delivery...
  49. ncbi Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer
    N Suh
    Department of Pharmacology, Dartmouth Medical School, Hanover, New Hampshire 03755, USA
    Cancer Res 61:8412-5. 2001
    ..Arzoxifene is devoid of the uterotrophic effects of tamoxifen, suggesting that, in contrast to tamoxifen, it is unlikely that the clinical use of arzoxifene will increase the risk of developing endometrial carcinoma...
  50. ncbi Evaluation of prasugrel compared with clopidogrel in patients with acute coronary syndromes: design and rationale for the TRial to assess Improvement in Therapeutic Outcomes by optimizing platelet InhibitioN with prasugrel Thrombolysis In Myocardial Infar
    Stephen D Wiviott
    TIMI Study Group, Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital, Boston, MA 02115, USA
    Am Heart J 152:627-35. 2006
    ..TRITON-TIMI 38 is designed to compare prasugrel with clopidogrel in moderate to high-risk patients with acute coronary syndrome (ACS)...
  51. ncbi Strontium ranelate treatment improves trabecular and cortical intrinsic bone tissue quality, a determinant of bone strength
    Patrick Ammann
    Division of Bone Diseases, WHO Collaborting Centre for Osteoporosis Prevention, Department of Rehabilitation and Geriatrics, University Hospitals, Geneva, Switzerland
    J Bone Miner Res 22:1419-25. 2007
    ....
  52. ncbi The effects of strontium ranelate on the risk of vertebral fracture in women with postmenopausal osteoporosis
    Pierre J Meunier
    Department of Rheumatology and Bone Diseases, Edouard Herriot Hospital, Lyons, France
    N Engl J Med 350:459-68. 2004
    ....
  53. ncbi Study design and rationale of a comparison of prasugrel and clopidogrel in medically managed patients with unstable angina/non-ST-segment elevation myocardial infarction: the TaRgeted platelet Inhibition to cLarify the Optimal strateGy to medicallY manage
    Chee Tang Chin
    Duke Clinical Research Institute, Durham, NC, USA
    Am Heart J 160:16-22.e1. 2010
    ....
  54. ncbi Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships
    Xiongyu Wu
    Department of Medicinal Chemistry, BMC, Uppsala University, P O Box 574, SE 751 23 Uppsala, Sweden
    J Med Chem 49:7160-8. 2006
    ..The butyloxyphenyl (56) and the propylthienyl (50) derivatives were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II...
  55. pmc Novel pentameric thiophene derivatives for in vitro and in vivo optical imaging of a plethora of protein aggregates in cerebral amyloidoses
    Andreas Aslund
    Department of Chemistry, IFM, Linkoping University, Sweden
    ACS Chem Biol 4:673-84. 2009
    ....
  56. ncbi Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay
    Yu Chen Barrett
    Bristol Myers Squibb, Princeton, New Jersey, USA
    Thromb Haemost 104:1263-71. 2010
    ..88-0.89) compared with PT/INR (r2 = 0.36) in patients undergoing VTE treatment suggested that anti-Xa activity was the better indicator of apixaban plasma concentrations...
  57. ncbi In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor
    E Perzborn
    Cardiovascular Research, Bayer HealthCare AG, Wuppertal, Germany
    J Thromb Haemost 3:514-21. 2005
    ..Bleeding times in rats and rabbits were not significantly affected at antithrombotic doses (3 mg kg(-1) p.o., AV shunt). Based on these results, BAY 59-7939 was selected for clinical development...
  58. ncbi Population pharmacokinetics and pharmacodynamics of once- and twice-daily rivaroxaban for the prevention of venous thromboembolism in patients undergoing total hip replacement
    Wolfgang Mueck
    Bayer HealthCare AG, Aprather Weg 18a, Wuppertal, Germany
    Thromb Haemost 100:453-61. 2008
    ....
  59. ncbi Body weight has limited influence on the safety, tolerability, pharmacokinetics, or pharmacodynamics of rivaroxaban (BAY 59-7939) in healthy subjects
    Dagmar Kubitza
    Clinical Pharmacology, Bayer HealthCare AG, Building 429, Aprather Weg 18a, Wuppertal, D 42096, Germany
    J Clin Pharmacol 47:218-26. 2007
    ..The area under the curve was unaffected by body weight or gender. No other clinically relevant differences were observed, suggesting that rivaroxaban is unlikely to require dose adjustment for body weight or gender...
  60. ncbi Effect of the dual peroxisome proliferator-activated receptor-alpha/gamma agonist aleglitazar on risk of cardiovascular disease in patients with type 2 diabetes (SYNCHRONY): a phase II, randomised, dose-ranging study
    Robert R Henry
    Department of Medicine, University of California at San Diego and VA San Diego Healthcare System, San Diego, CA 92161, USA
    Lancet 374:126-35. 2009
    ..The SYNCHRONY study aimed to establish the glucose-lowering and lipid-modifying effects, and safety profile, of the dual PPAR-alpha and PPAR-gamma agonist aleglitazar...
  61. ncbi Population model of the pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor xa inhibitor--in healthy subjects
    W Mueck
    Clinical Pharmacology, Pharmacometry, Bayer HealthCare AG, Wuppertal, Germany
    Int J Clin Pharmacol Ther 45:335-44. 2007
    ..This analysis aimed to define population models for the pharmacokinetics (PK) and pharmacodynamics (PD) ofrivaroxaban in healthy males...
  62. pmc Meta-analysis of duloxetine vs. pregabalin and gabapentin in the treatment of diabetic peripheral neuropathic pain
    Sibilia Quilici
    Health Economics and Outcomes Research, Uxbridge, UK
    BMC Neurol 9:6. 2009
    ..We conducted an indirect meta-analysis to compare the efficacy and tolerability of DLX with PGB and GBP in DPNP, using placebo as a common comparator...
  63. ncbi Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct factor Xa inhibitor, in healthy subjects
    Dagmar Kubitza
    Institute of Clinical Pharmacology, Bayer HealthCare AG, Wuppertal, Germany
    J Clin Pharmacol 46:549-58. 2006
    ..Time to maximum PT prolongation was delayed by 0.5 to 1.5 hours after food, with no relevant influence of food type. No significant difference in C(max) and AUC was observed with coadministration of BAY 59-7939 and ranitidine or antacid...
  64. ncbi Common polymorphisms of CYP2C19 and CYP2C9 affect the pharmacokinetic and pharmacodynamic response to clopidogrel but not prasugrel
    J T Brandt
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    J Thromb Haemost 5:2429-36. 2007
    ..The pharmacodynamic response to clopidogrel is more variable than the response to prasugrel, but the reasons for variation in response to clopidogrel are not well characterized...
  65. ncbi Oral, direct Factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement
    B I Eriksson
    Sahlgrenska University HospitalOstra, Gothenburg, Sweden
    J Thromb Haemost 4:121-8. 2006
    ..Joint replacement surgery is an appropriate model for dose-ranging studies investigating new anticoagulants...
  66. ncbi Effects of long-term strontium ranelate treatment on the risk of nonvertebral and vertebral fractures in postmenopausal osteoporosis: Results of a five-year, randomized, placebo-controlled trial
    Jean Yves Reginster
    University of Liege, Liege, Belgium
    Arthritis Rheum 58:1687-95. 2008
    ..This study was undertaken to assess the effect of strontium ranelate on nonvertebral and vertebral fractures in postmenopausal women with osteoporosis in a 5-year, double-blind, placebo-controlled trial...
  67. ncbi Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptor
    I Algaier
    Department of Pharmacology and Toxicology, University of Bonn, Bonn, Germany
    J Thromb Haemost 6:1908-14. 2008
    ..The P2Y(12) receptor plays a crucial role in platelet aggregation and is the target of platelet aggregation inhibitors, including the thienopyridine compound prasugrel...
  68. pmc A pharmacodynamic comparison of prasugrel vs. high-dose clopidogrel in patients with type 2 diabetes mellitus and coronary artery disease: results of the Optimizing anti-Platelet Therapy In diabetes MellitUS (OPTIMUS)-3 Trial
    Dominick J Angiolillo
    University of Florida College of Medicine Jacksonville, 655 W Eighth Street, Jacksonville, FL 32209, USA
    Eur Heart J 32:838-46. 2011
    ..The aim of this study was to perform serial pharmacodynamic assessments of prasugrel with high-dose clopidogrel in patients with DM...
  69. ncbi Cost-utility of long-term strontium ranelate treatment for postmenopausal osteoporotic women
    M Hiligsmann
    Department of Public Health, Epidemiology and Health Economics, University of Liege, Liege, Belgium
    Osteoporos Int 21:157-65. 2010
    ..The results of this study suggested that long-term treatment with strontium ranelate over 5 years is cost-effective compared to no treatment for postmenopausal osteoporotic women...
  70. ncbi Strontium ranelate reduces the risk of nonvertebral fractures in postmenopausal women with osteoporosis: Treatment of Peripheral Osteoporosis (TROPOS) study
    J Y Reginster
    Department of Epidemiology, Public Health and Health Economics, University of Liege, CHU Centre Ville, 45 Quai Godefroid Kurth, 4020 Liege, Belgium
    J Clin Endocrinol Metab 90:2816-22. 2005
    ....
  71. ncbi Solution-processed metallic conducting polymer films as transparent electrode of optoelectronic devices
    Yijie Xia
    Department of Materials and Engineering, National University of Singapore, Singapore
    Adv Mater 24:2436-40. 2012
    ..These PEDOT:PSS films with conductivity and transparency comparable to ITO can replace ITO as the transparent electrode of optoelectronic devices...
  72. pmc Inhibitors of the cellular trafficking of ricin
    Julien Barbier
    Laboratory of Molecular Toxinology and Biotechnology, Molecular engineering of proteins SIMOPRO, Life Sciences Division DSV, Institute of Biology and Technology Saclay, French Alternative Energies and Atomic Energy Commission CEA, F 91191 Gif sur Yvette, France
    Toxins (Basel) 4:15-27. 2012
    ....
  73. pmc Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase
    Mark D Rackham
    Department of Chemistry, Imperial College London, South Kensington Campus, London, SW7 2AZ, U K
    J Med Chem 56:371-5. 2013
    ..The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring...
  74. ncbi Duloxetine added to oral nonsteroidal anti-inflammatory drugs for treatment of knee pain due to osteoarthritis: results of a randomized, double-blind, placebo-controlled trial
    ELIJAH P FRAKES
    Eli Lilly and Company, Indianapolis, IN, USA
    Curr Med Res Opin 27:2361-72. 2011
    ..To determine the efficacy, tolerability, and safety of duloxetine when added to oral nonsteroidal anti-inflammatory drugs (NSAIDs) in patients with osteoarthritis (OA) of the knee with pain of moderate or greater severity...
  75. ncbi Prasugrel overcomes high on-clopidogrel platelet reactivity in chronic coronary artery disease patients more effectively than high dose (150 mg) clopidogrel
    Dimitrios Alexopoulos
    Department of Cardiology, Patras University Hospital Rio, Greece
    Am Heart J 162:733-9. 2011
    ..Strategies to optimize platelet inhibition in such patients are not clear...
  76. pmc Chemical structure of Retro-2, a compound that protects cells against ribosome-inactivating proteins
    Jewn Giew Park
    Computer Aided Molecular Design Laboratory, Mayo Clinic, Rochester, MN 55905, USA
    Sci Rep 2:631. 2012
    ..This calls for attention to (±)-2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one as a promising RIP inhibitor and for chemical characterization of drug leads obtained from high-throughput screens...
  77. ncbi Treatment of patients with early and advanced Parkinson's disease with rotigotine transdermal system: age-relationship to safety and tolerability
    Wolfgang Oertel
    Department of Neurology, Philipps Universitat, Baldingerstrasse, D 35043 Marburg, Germany
    Parkinsonism Relat Disord 19:37-42. 2013
    ..Data from more representative PD populations are required to fully assess potential risks of DA therapy in elderly patients...
  78. ncbi High compliance with rotigotine transdermal patch in the treatment of idiopathic Parkinson's disease
    Alfons Schnitzler
    Institute of Clinical Neuroscience and Medical Psychology, Heinrich Heine University, Universitatsstr 1, Dusseldorf, Germany
    Parkinsonism Relat Disord 16:513-6. 2010
    ..This open, prospective, non-interventional study investigated compliance with the patch under clinical practice conditions...
  79. pmc A spinal mechanism of action for duloxetine in a rat model of painful diabetic neuropathy
    T Mixcoatl-Zecuatl
    Department of Pathology, University of California, San Diego, La Jolla, CA 92093 0612, USA
    Br J Pharmacol 164:159-69. 2011
    ..This study was designed to clarify mechanisms responsible for the anti-allodynic effects of duloxetine in diabetes...
  80. pmc Rivaroxaban vs dabigatran for thromboprophylaxis after joint-replacement surgery: exploratory indirect comparison based on meta-analysis of pivotal clinical trials
    Vladimir Trkulja
    Department of Pharmacology, Zagreb University School of Medicine, Salata 11, 10000 Zagreb, Croatia
    Croat Med J 51:113-23. 2010
    ..To indirectly compare rivaroxaban and dabigatran for prevention of venous thromboembolism (VTE) after total hip or knee arthroplasty (THA, TKA) based on their pivotal efficacy/safety trials embracing a total of 20618 patients...
  81. ncbi Pharmacokinetics and pharmacodynamics of prasugrel, a thienopyridine P2Y12 inhibitor
    Paul P Dobesh
    College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198 6045, USA
    Pharmacotherapy 29:1089-102. 2009
    ..Thus, prasugrel has a pharmacokinetic and pharmacodynamic profile that compares favorably with those of existing antiplatelet agents...
  82. ncbi Prasugrel pharmacokinetics and pharmacodynamics in subjects with moderate renal impairment and end-stage renal disease
    D S Small
    Eli Lilly and Company, Indianapolis, IN, USA
    J Clin Pharm Ther 34:585-94. 2009
    ..The pharmacokinetic (PK) and pharmacodynamic (PD) responses to prasugrel were compared in three studies of healthy subjects vs. those with moderate or end-stage renal impairment...
  83. ncbi Ritonavir inhibits the two main prasugrel bioactivation pathways in vitro: a potential drug-drug interaction in HIV patients
    Youssef Daali
    Division of Clinical Pharmacology and Toxicology, Geneva University Hospitals, Geneva, Switzerland
    Metabolism 60:1584-9. 2011
    ..This finding suggests a potential significant drug-drug interaction between these two drugs...
  84. ncbi The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjects
    David S Small
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Eur J Clin Pharmacol 66:127-35. 2010
    ..We compared prasugrel pharmacokinetics, pharmacodynamics, and tolerability in healthy Chinese, Japanese, Korean and Caucasian subjects...
  85. ncbi Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency
    David R Anderson
    Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA
    Bioorg Med Chem Lett 19:4878-81. 2009
    ..Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors...
  86. ncbi Rotigotine transdermal patch for the treatment of Parkinson's disease and restless legs syndrome
    B Boroojerdi
    Schwarz BioSciences GmbH, UCB Pharma Group, Monheim, Germany
    Drugs Today (Barc) 46:483-505. 2010
    ..Overall, rotigotine transdermal patch has demonstrated favorable clinical efficacy and tolerability in the treatment of PD and RLS...
  87. ncbi Dose-dependent inhibition of human platelet aggregation by prasugrel and its interaction with aspirin in healthy subjects
    Joseph A Jakubowski
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Cardiovasc Pharmacol 49:167-73. 2007
    ..Within the limitations of the study, prasugrel was found to be well tolerated when dosed as LD followed by MD in the presence of ASA and provided greater platelet inhibition than ASA alone...
  88. ncbi Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability
    Yan Degenhardt
    Cancer Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Mol Cancer Ther 9:2079-89. 2010
    ....
  89. pmc Synthesis of a library of oligothiophenes and their utilization as fluorescent ligands for spectral assignment of protein aggregates
    Therése Klingstedt
    Department of Chemistry, Linkoping University, SE 581 83 Linkoping, Sweden
    Org Biomol Chem 9:8356-70. 2011
    ..Such LCOs will be highly useful for studying the underlying molecular events of protein aggregation diseases and could also be utilized for the development of novel diagnostic tools for these diseases...
  90. pmc Competitive enzymatic interactions determine the relative amounts of prostaglandins E2 and D2
    Rui Yu
    Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 S Wood Street, Chicago, IL 60612 7231, USA
    J Pharmacol Exp Ther 339:716-25. 2011
    ....
  91. ncbi Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency
    David R Anderson
    Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA
    Bioorg Med Chem Lett 19:4882-4. 2009
    ..The selectivity of the inhibitors can be rationalized by examination of X-ray crystal structures of inhibitors bound to MK2...
  92. ncbi A novel approach to control hyperglycemia in type 2 diabetes: sodium glucose co-transport (SGLT) inhibitors: systematic review and meta-analysis of randomized trials
    Giovanni Musso
    Gradenigo Hospital, Turin, Italy
    Ann Med 44:375-93. 2012
    ..Current treatment of hyperglycemia in type 2 diabetes (T2DM) is often ineffective and has unwanted effects. Therefore, novel antidiabetic drugs are under development...
  93. ncbi Return to theatre following total hip and knee replacement, before and after the introduction of rivaroxaban: a retrospective cohort study
    C D Jensen
    Wansbeck General Hospital, Woodhorn Lane, Ashington, Northumberland NE63 9JJ, UK
    J Bone Joint Surg Br 93:91-5. 2011
    ....
  94. ncbi Cost-effectiveness of prasugrel versus clopidogrel in patients with acute coronary syndromes and planned percutaneous coronary intervention: results from the trial to assess improvement in therapeutic outcomes by optimizing platelet inhibition with Prasug
    Elizabeth M Mahoney
    Saint Luke s Mid America Heart Institute, 4401 Wornall Rd, Kansas City, MO 64111, USA
    Circulation 121:71-9. 2010
    ..We evaluated the cost-effectiveness of prasugrel versus clopidogrel from the perspective of the US healthcare system by using data from TRITON-TIMI 38...
  95. ncbi How strontium ranelate, via opposite effects on bone resorption and formation, prevents osteoporosis
    P J Marie
    Laboratory of Osteoblast Biology and Pathology, INSERM, U606, Paris 75475, France
    Osteoporos Int 22:1659-67. 2011
    ....
  96. ncbi Intraocular pressure lowering, change of antiapoptotic molecule expression, and neuroretinal changes by dorzolamide 2%/timolol 0.5% combination in a chronic ocular hypertension rat model
    Hae Y Park
    Department of Ophthalmology and Visual Science, College of Medicine, St Mary s Hospital, The Catholic University of Korea, Seoul, Korea
    J Ocul Pharmacol Ther 24:563-71. 2008
    ..5% may have neuroprotective potential in the animal model, which is not mediated by Bcl-2 or Bcl-xL. The mechanism of neuroprotection by dorzolamide 2%/timolol 0.5% in chronic glaucoma models requires further investigation...
  97. pmc Is there adequate provision of venous thromboembolism prophylaxis following hip arthroplasty? An audit and international survey
    B A Rogers
    Adult Lower Extremity Reconstruction, Mount Sinai Hospital, Toronto, Canada
    Ann R Coll Surg Engl 92:668-72. 2010
    ....
  98. ncbi Prasugrel compared with high-dose clopidogrel in acute coronary syndrome. The randomised, double-blind ACAPULCO study
    Gilles Montalescot
    Institut de Cardiologie AP HP, INSERM U856 and Universite Paris 6, Hopital Pitie Salpetriere, Paris, France
    Thromb Haemost 103:213-23. 2010
    ..Thus, in ACS patients a prasugrel 10-mg MD regimen resulted in significantly greater platelet inhibition than clopidogrel at twice its approved MD or a 900-mg LD...
  99. ncbi Strontium ranelate effect in postmenopausal women with different clinical levels of osteoarthritis
    P Alexandersen
    Center for Clinical and Basic Research, Vejle, Denmark
    Climacteric 14:236-43. 2011
    ..Women were stratified according to reported symptoms of osteoarthritis and to the baseline levels of a cartilage degradation marker...
  100. ncbi Incidence of venous thromboembolism in users of strontium ranelate: an analysis of data from a prescription-event monitoring study in England
    Vicki Osborne
    Drug Safety Research Unit, Bursledon Hall, Southampton, UK
    Drug Saf 33:579-91. 2010
    ..Strontium ranelate is indicated for the treatment of postmenopausal osteoporosis. An association between strontium ranelate and venous thromboembolism (VTE) was identified in an analysis of phase III clinical trials...
  101. ncbi Population pharmacokinetic analyses to evaluate the influence of intrinsic and extrinsic factors on exposure of prasugrel active metabolite in TRITON-TIMI 38
    Rebecca E Wrishko
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Clin Pharmacol 49:984-98. 2009
    ..1%) was 30% (90% confidence interval [CI] 1.16-1.45) higher than exposure in patients > or =60 kg. Mean Pras-AM exposures for patients > or =75 years (10.5%) were 19% (90% CI: 1.11-1.28) higher compared with patients <75 years...

Research Grants68

  1. A General Synthetic Route to Glycosidase Inhibitors
    Aaron Aponick; Fiscal Year: 2006
    ....
  2. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..dihydropyrimidines, 2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and ..
  3. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2013
    ..and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to highly substituted ..
  4. CHEMICAL STUDIES OF NOVEL SULFUR CONTAINING ANTIBIOTICS
    Eloy Rodriguez; Fiscal Year: 1993
    ..bioactivity and mode of action of novel plant-derived dithiacyclohexadiene (1,2-dithiins) polyacetylenes, thiophenes and derivatives...
  5. Improving Outcomes in Pharmacotherapy of Social Phobia
    Mark Pollack; Fiscal Year: 2009
    ..It thus directly addresses a critical public health issue that adversely affects a substantial proportion of the population. ..
  6. D-Cycloserine Enhancement of Exposure in Social Phobia
    Mark H Pollack; Fiscal Year: 2010
    ..This study addresses an important public health issue by assessing an intervention that may lead to a more efficient and effective application of empirically based psychosocial interventions for the treatment of SAD. ..
  7. BUPROPION AS AN ADJUNCT TO THE NICOTINE PATCH PLUS CBT
    Maurizio Fava; Fiscal Year: 2003
    ....
  8. Phase I Trial of Safingol and Cisplatin
    Gary Schwartz; Fiscal Year: 2006
    ..conduct "proof of principle" biological assays to measure the degree of ceramide production and/or S1P inhibition, either of which may be predictive of clinical outcome or toxicity. ..
  9. FlaxSeed Lignan for Breast Cancer Chemoprevention
    CAROL FABIAN; Fiscal Year: 2007
    ..If positive, the results of this study will be critical to the design and implementation of a placebo-controlled Phase II prevention trial with Brevail and/or commercial flaxseed. [unreadable] [unreadable]..
  10. Impact of Trauma of Terroist Attack on Bipolar Patients
    Mark Pollack; Fiscal Year: 2003
    ..abstract_text> ..
  11. Phase II Study of Imatinib Mesylate in Patients with Inoperable Melanoma
    Gary K Schwartz; Fiscal Year: 2010
    ..Dose reductions are allowed in the setting of toxicity. Imaging studies will be performed on an every 6 week schedule. ..
  12. MR SPECTROSCOPIC IMAGING DURING METHADONE MAINTENANCE
    Mark Pollack; Fiscal Year: 2002
    ....
  13. Breast Cancer Prevention by Letrozole in High Risk Women
    Carol J Fabian; Fiscal Year: 2010
    ....
  14. Locomotion Control by Lumbar Spinal Cord Stimulation
    Changfeng Tai; Fiscal Year: 2008
    ..The proposed studies will not only improve our understanding of locomotion control in lumbar spinal cord but also benefit SCI patients. ..
  15. Extracellular Mechanisms For Thoracic Aortic Aneurysms
    John Ikonomidis; Fiscal Year: 2008
    ..abstract_text> ..
  16. Controlled Study of SAMe vs.Escitalopram in Major Depressive Disorder
    Maurizio Fava; Fiscal Year: 2008
    ..Secondary aims are to assess the acute effects of SAMe or escitalopram vs. placebo on remission rates, quality of life, and psychosocial functioning. ..
  17. High Throughput Radiation Biodosimetry
    Stephen Dertinger; Fiscal Year: 2007
    ..We propose to develop such a radiation biodosimetry assay based on the extremely high analysis rates that are possible with flow cytometry instrumentation. [unreadable] [unreadable] [unreadable]..
  18. PHYSIOLOGY OF ESTROGEN'S MOOD EFFECT IN MENOPAUSAL WOMEN
    Hadine Joffe; Fiscal Year: 2007
    ..Such training will lay the foundation for a career of clinical investigation into the physiology of perimenopausal depression and the impact of hot flushes on sleep, mood, and quality-of-life. ..
  19. FURANOCOUMARINS AND DRUGS EFFECT ON CYP3A4
    Paul Watkins; Fiscal Year: 2007
    ..abstract_text> ..
  20. Harvard Planning Grant for Institutional Clinical and Translational Science Award
    Daniel Singer; Fiscal Year: 2006
    ..We believe our planning process is specific, innovative yet disciplined, and should be robust. A full and competitive CTSA application will be produced in a timely manner. [unreadable] [unreadable] [unreadable]..
  21. Il-6 type cytokine protection from hyperoxic lung injury
    Aaron Waxman; Fiscal Year: 2007
    ..abstract_text> ..
  22. REVAMP Follow-Up
    Madhukar Trivedi; Fiscal Year: 2008
    ....
  23. Pharmacogenomics in Pulmonary Arterial Hypertension
    Raymond Benza; Fiscal Year: 2008
    ..PAH = pulmonary arterial hypertension PA = pulmonary artery PPH = primary pulmonary hypertension ..
  24. Can dynamic pupillography and/or spectral analysis of heart rate variability prov
    Solomon Tesfaye; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  25. Pelvic Floor Changes Before and After Birth
    REBECCA GLENN ROGERS; Fiscal Year: 2010
    ..This project will provide fundamental data to guide future decisions about labor interventions to prevent PF changes as well as data-based decisions regarding maternal request cesarean. ..
  26. Bone loss with aging occurs due to increased PPAR-g activity in marrow stem cells
    BEATA ANNA LECKA CZERNIK; Fiscal Year: 2010
    ..Completion of the above aims should enable us to determine the role of PPARg in this process and will allow designing therapeutic interventions that will selectively block PPARg anti-osteoblastic activity. ..
  27. Brain Cannabinoid Signaling: Selectivity and Adaptation
    Laura J Sim Selley; Fiscal Year: 2010
    ..This project will determine roles of specific signaling proteins in the effects of acute and long-term CB1R activation by THC and are relevant to cannabinoid therapeutics and drug abuse. ..
  28. Combining Antidepressants to Hasten Remission from Depression
    Jonathan W Stewart; Fiscal Year: 2010
    ....
  29. PROPHYLACTIC COGNITIVE THERAPY FOR DEPRESSION
    Michael E Thase; Fiscal Year: 2010
    ....
  30. NEW APPROACH TO ENDOTHELIAL CLEFT STRUCTURE
    Fitz Roy E Curry; Fiscal Year: 2010
    ..Our experiments evaluate the common mechanical properties of the endothelial glycocalyx that modulate water, solute, leukocyte, and red cell fluxes at the endothelial cell surface. ..
  31. Risks for Opioid Use and Abuse in Contrasting Chronic Pain Populations
    Mark Sullivan; Fiscal Year: 2009
    ....
  32. NEW AMINO-PROTECTING GROUPS AND COUPLING REAGENTS
    LOUIS CARPINO; Fiscal Year: 2009
    ..Microwave irradiation is expected to allow for the most efficient syntheses, especially with Bsmoc and HOAt-based chemistry. ..
  33. Rapid Screen for Genotoxicants, Chemoprotectors, and Radioprotectors
    Stephen Dertinger; Fiscal Year: 2008
    ..In addition, this assay can be used to investigate agents designed to ameliorate the effects of radiation exposure, e.g. biological response modifiers. [unreadable] [unreadable] [unreadable] [unreadable]..
  34. Effects of Nicotine on Human Cerebral Transmitters
    EDWARD DOMINO; Fiscal Year: 2008
    ..This research will provide direct proof of basic neuroscience studies, which indicate nicotine releases neurotransmitters such as dopamine and endogenous opioids. [unreadable] [unreadable] [unreadable]..
  35. PDE3 Inhibitors: Selective Blockers of Oocyte Maturation
    Jeffrey Jensen; Fiscal Year: 2007
    ..This approach is expected to provide a foundation for future Phase 1 trials of PDE3 inhibitors in humans. ..
  36. Pramipexole in Treatment-Resistant Depression
    Roy Perlis; Fiscal Year: 2007
    ..The proposed investigation and training program will provide critical skills, experience and data to aid the candidate in writing an R01 and becoming an independent investigator. ..
  37. Computerized Decision Support System for Depression
    Madhukar Trivedi; Fiscal Year: 2007
    ..Comparisons will be made between CDSS-D, PPA-D, and UC-D. [unreadable] [unreadable]..
  38. WHI Sex Hormone & Genetic Risk Factors for Hip Fracture
    Steven Cummings; Fiscal Year: 2005
    ..The proposed study is a very efficient approach to understanding the etiologies of hip fracture. ..
  39. AT2 Receptor Modulates Renal Angiotensin II Levels
    Helmy Siragy; Fiscal Year: 2005
    ..Data obtained from this proposal will lead to increased understanding of the pathophysiology of hypertension and development of novel therapies for its management. ..
  40. PPAR gamma-2 expression in marrow stroma during aging
    Beata Lecka Czernik; Fiscal Year: 2005
    ..Such intervention may slow down or even prevent age-related bone loss. ..
  41. Nocardia: A Novel Environmental Agent For Parkinsonism?
    Peter LeWitt; Fiscal Year: 2003
    ..These outcomes will be significant because they should add to our understanding of the neurodegenerative process in PD, and could lead to improved means of diagnosis and treatment for individuals with this disorder. ..
  42. The Angiotensin II-Induced JAK/STAT Pathway in Diabetes.
    Mario Marrero; Fiscal Year: 2005
    ..This area of research will provide new strategies and the potential for new therapeutics agents in the flight against diabetic complications. ..
  43. In vivo mutation assay based on pig-a locus
    Stephen Dertinger; Fiscal Year: 2004
    ....
  44. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  45. REACTIVE INTERMEDIATES OF CARCINOGENESIS OF PAHS
    KENNETH LAALI; Fiscal Year: 2004
    ..DNA binding and mammalian cell mutagenicity studies on the substituted and derivatized-PAHs proposed for stable ion work will enhance the available literature data on structure/reactivity relationships. ..
  46. VIRUS PHOTOINACTIVATION--DIMETHYLMETHYLENE BLUE IN RBC
    Stephen Wagner; Fiscal Year: 2004
    ..abstract_text> ..
  47. Measuring Cytogenetic Damage in Human Blood
    Stephen Dertinger; Fiscal Year: 2003
    ..abstract_text> ..
  48. IMPROVEMENT OF MEMBRANE BIOLOGY FACILITY
    FITZ ROY CURRY; Fiscal Year: 2002
    ..That project addressed other laboratory and basic infrastructure deficiencies in the same building that contains the subject laboratories in the current application. ..
  49. A CONSORTIUM TO INVESTIGATE HUMAN LONGEVITY AND FRAILTY
    Steven Cummings; Fiscal Year: 2002
    ..This Consortium will catalyze interactions between outstanding laboratory and clinical scientists that will lead to collaborative studies of the genetic determinants of longevity and frailty. ..
  50. GENERAL CLINICAL RESEARCH CENTERS ANNUAL MEETING
    Paul Watkins; Fiscal Year: 2006
    ..abstract_text> ..
  51. NICOTINE EFFECTS ON CEREBRAL BLOOD FLOW AND METABOLISM
    EDWARD DOMINO; Fiscal Year: 2001
    ..This could set the stage for the study of nicotine effects in persons with cofactors for smoking, such as attention deficit disorder or mood disorders. ..
  52. Treatment with Exercise Augmentation for Depression
    Madhukar Trivedi; Fiscal Year: 2006
    ....
  53. Chronic Thromboembolic Pulmonary Hypertension
    TIMOTHY MORRIS; Fiscal Year: 2006
    ..The fragments will be subjected to liquid chromatography-mass spectroscopy with data-dependent MS-2 data acquisition, followed by computer-assisted sequence analysis. ..
  54. Southeastern Michigan Parkinson's Disease Program
    Peter LeWitt; Fiscal Year: 2006
    ..This application also discusses concepts for three pharmacological agents that could be investigated in pilot studies and, if promising, in multicenter clinical trials for assessing neuroprotection. ..
  55. PULSE LOADED IV CLOMIPRAMINE IN UNRESPONSIVE OCD
    Lorrin Koran; Fiscal Year: 2001
    ..outcome can be predicted from baseline clinical information. (Throughout this revised grant application, revisions are indicated by bold type face, except that the new Introduction is in ordinary typeface). ..
  56. Angiotensin II Signaling in Diabetic Nephropathy
    Mario Marrero; Fiscal Year: 2006
    ..abstract_text> ..
  57. Pulmonary Hypertension Scientific Conference
    Michael McGoon; Fiscal Year: 2004
    ....
  58. Versatile Mutation Assay Platform
    Stephen Dertinger; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  59. Automation of the vitro Micronucleus Assay
    Stephen Dertinger; Fiscal Year: 2004
    ..abstract_text> ..
  60. OPTIMIZING MANAGEMENT OF TRANSIENT ISCHEMIC ATTACKS
    S Johnston; Fiscal Year: 2005
    ..This research will provide important results for clinicians and policy makers, and will foster the applicant's development as a health services researcher in cerebrovascular disease. ..
  61. Peripheral and Central Mechanism of Pain in Patients with Fibromyalgia
    ROLAND M STAUD; Fiscal Year: 2010
    ..Either way, we will provide evidence that will characterize the role of local anesthesia, placebo analgesia, or both. Thus patients with FM and other similar pain syndromes may strongly benefit from the results of our study. ..
  62. Efficacy of Acupuncture with PT for Knee Osteo-Arthritis
    John Farrar; Fiscal Year: 2005
    ..However, if the results are negative, then the addition of acupuncture to EPT should be generally curtailed. ..
  63. MECHANISM OF PAIN IN PATIENTS WITH FIBROMYALGIA SYNDROME
    Roland Staud; Fiscal Year: 2008
    ..In addition, our findings may contribute to the understanding of pain mechanisms related to other chronic pain disorders. ..
  64. Hereditary spastic paraplegia linked to chromosomes 8q
    Peter Hedera; Fiscal Year: 2006
    ..I will characterize the phenotype of transgenic animals. The study of a transgenic animal model will further enhance current state of knowledge about the pathophysiology of HSP and axonal degeneration. ..
  65. METHOD FOR THE ANALYSIS OF PAIN CLINICAL TRIALS
    John Farrar; Fiscal Year: 2001
    ..Over this time period, not only will adjunct does be varied upward or downward, depending on the complaint of side effect, whereas the opiod dose will be varied in response to pain complaint. ..
  66. TREATMENT REFRACTORY PANIC DISORDER
    Naomi Simon; Fiscal Year: 2004
    ..abstract_text> ..
  67. Genetic Predictors of Outcome in Acute MI
    Marc Sabatine; Fiscal Year: 2005
    ..Genomic control will be employed to detect and control for population stratification. Interaction terms will be incorporated into regression models to explore gene-environment and pharmacogenomic interactions. ..