Masahiko Hayakawa

Summary

Affiliation: Astellas Pharma Inc
Country: Japan

Publications

  1. ncbi Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem 14:6847-58. 2006
  2. ncbi Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Institute for Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem 15:403-12. 2007
  3. ncbi Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem Lett 17:2438-42. 2007
  4. ncbi Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki, Japan
    Bioorg Med Chem 15:5837-44. 2007
  5. ncbi Antihyperglycemic effects of ASP8497 in streptozotocin-nicotinamide induced diabetic rats: comparison with other dipeptidyl peptidase-IV inhibitors
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3, Toukoudai, Tuskuba, Ibaraki 300 2698, Japan
    Pharmacol Rep 61:899-908. 2009
  6. ncbi Antidiabetic effects of dipeptidyl peptidase-IV inhibitors and sulfonylureas in streptozotocin-nicotinamide-induced mildly diabetic mice
    Akiko Matsuyama-Yokono
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki 300 2698, Japan
    Metabolism 58:379-86. 2009
  7. ncbi Evaluation of the antidiabetic effects of dipeptidyl peptidase-IV inhibitor ASP8497 in streptozotocin-nicotinamide-induced mildly diabetic mice
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Japan
    Pharmacology 83:177-87. 2009
  8. ncbi Effects of the combination of dipeptidyl peptidase-IV inhibitor ASP8497 and antidiabetic drugs in streptozotocin-nicotinamide-induced mildly diabetic mice
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
    Eur J Pharmacol 605:170-6. 2009
  9. ncbi Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
    Bioorg Med Chem 17:3283-94. 2009
  10. ncbi Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba, Ibaraki 305 8585, Japan
    Eur J Med Chem 44:2533-43. 2009

Collaborators

Detail Information

Publications15

  1. ncbi Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem 14:6847-58. 2006
    ..58 microM. Moreover, 15e was found to be selective for p110alpha over other PI3K isoforms and protein kinases, making it the first example of a selective PI3K p110alpha inhibitor...
  2. ncbi Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Institute for Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem 15:403-12. 2007
    ..21microM, respectively, and suppressed tumor growth by 37% in a mouse HeLa xenograft model when dosed intraperitoneally at 25mg/kg. These results suggest that selective p110alpha inhibitors may have potential as cancer therapeutic agents...
  3. ncbi Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki 300 2698, Japan
    Bioorg Med Chem Lett 17:2438-42. 2007
    ..Furthermore, 10e showed anti-proliferative activity in various cell lines, including multi-drug resistant MCF7/ADR-res cells, and was effective against HeLa human cervical tumor xenografts in nude mice...
  4. ncbi Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors
    Masahiko Hayakawa
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Tokodai, Tsukuba, Ibaraki, Japan
    Bioorg Med Chem 15:5837-44. 2007
    ..26 nM, respectively; to the best of our knowledge, these compounds are the most potent PI3K p110alpha inhibitors reported to date. Compound 8c was also stable in solution and exhibited significant anti-tumor effectiveness in vivo...
  5. ncbi Antihyperglycemic effects of ASP8497 in streptozotocin-nicotinamide induced diabetic rats: comparison with other dipeptidyl peptidase-IV inhibitors
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3, Toukoudai, Tuskuba, Ibaraki 300 2698, Japan
    Pharmacol Rep 61:899-908. 2009
    ..This compound is expected to be useful as a therapeutic agent for impaired glucose tolerance and type 2 diabetes...
  6. ncbi Antidiabetic effects of dipeptidyl peptidase-IV inhibitors and sulfonylureas in streptozotocin-nicotinamide-induced mildly diabetic mice
    Akiko Matsuyama-Yokono
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki 300 2698, Japan
    Metabolism 58:379-86. 2009
    ....
  7. ncbi Evaluation of the antidiabetic effects of dipeptidyl peptidase-IV inhibitor ASP8497 in streptozotocin-nicotinamide-induced mildly diabetic mice
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Japan
    Pharmacology 83:177-87. 2009
    ..It is expected to be useful as a therapeutic agent for impaired glucose tolerance and type 2 diabetes...
  8. ncbi Effects of the combination of dipeptidyl peptidase-IV inhibitor ASP8497 and antidiabetic drugs in streptozotocin-nicotinamide-induced mildly diabetic mice
    Atsuo Tahara
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
    Eur J Pharmacol 605:170-6. 2009
    ..These profiles indicate that the combination of ASP8497 with existing antidiabetic drugs could be useful for correcting the postprandial hyperglycemia seen with type 2 diabetes...
  9. ncbi Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
    Bioorg Med Chem 17:3283-94. 2009
    ..28 microM and no agonistic activity for either the beta1- or beta2-AR. In addition, 21b showed significant hypoglycemic activity in a rodent diabetic model...
  10. ncbi Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba, Ibaraki 305 8585, Japan
    Eur J Med Chem 44:2533-43. 2009
    ..11 microM and no agonistic activity for either the beta1- or beta2-AR. In addition, 2f, 2u, and 2v showed significant hypoglycemic activity in a rodent diabetic model...
  11. ncbi Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan
    Chem Pharm Bull (Tokyo) 58:533-45. 2010
    ..In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model...
  12. ncbi Pharmacological profile of ASP8497, a novel, selective, and competitive dipeptidyl peptidase-IV inhibitor, in vitro and in vivo
    Yuka Someya
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3, Toukoudai, Tsukuba, Ibaraki 300 2698, Japan
    Naunyn Schmiedebergs Arch Pharmacol 377:209-17. 2008
    ..In contrast, ASP8497 did not cause hypoglycemia in fasted normal mice. These results indicate that ASP8497 is a potent, competitive, and selective DPP-IV inhibitor with antihyperglycemic activity...
  13. ncbi ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity
    Akiko Matsuyama-Yokono
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3 Toukoudai, Tuskuba, Ibaraki 300 2698, Japan
    Biochem Pharmacol 76:98-107. 2008
    ..These present preclinical studies indicate that ASP8497 is a novel selective DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes...
  14. ncbi Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists
    Tatsuya Maruyama
    Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba, Ibaraki 305 8585, Japan
    Bioorg Med Chem 17:5510-9. 2009
    ..10 and 0.16 microM, respectively, and no agonistic activity for either the beta1- or beta2-AR. In addition, they showed significant hypoglycemic activity in a rodent diabetic model...
  15. ncbi Chronic inhibition of dipeptidyl peptidase-IV with ASP8497 improved the HbA(1c) level, glucose intolerance, and lipid parameter level in streptozotocin-nicotinamide-induced diabetic mice
    Akiko Matsuyama-Yokono
    Drug Discovery Research, Astellas Pharma Inc, 5 2 3, Toukoudai, Tsukuba, Ibaraki, Japan
    Naunyn Schmiedebergs Arch Pharmacol 379:191-9. 2009
    ..It is therefore suggested that ASP8497 may be a potential agent for the treatment of type 2 diabetes...