WO1998054093A1 - Novel angiogenesis inhibitors - Google Patents
Novel angiogenesis inhibitors Download PDFInfo
- Publication number
- WO1998054093A1 WO1998054093A1 PCT/US1998/010590 US9810590W WO9854093A1 WO 1998054093 A1 WO1998054093 A1 WO 1998054093A1 US 9810590 W US9810590 W US 9810590W WO 9854093 A1 WO9854093 A1 WO 9854093A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pyrimidine
- pyrazolo
- pyridyl
- compound
- alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Definitions
- R 4 is H, Cj.io a] ky ⁇ , C 3 - 6 cycloalkyl, C 5 . 10 aryl, C 5 . 10 heteroaryl, C 3 . 10 heterocyclyl, C ⁇ - 6 alkoxyNR 7 R 8 , N0 2 , OH, -NH 2 or C 5 . 10 heteroaryl, said alkyl, aryl, heteroaryl and heterocyclyl being optionally substituted with from one to three members selected from R a ; and all other variables are as described above.
- VEGF receptor kinase activity is measured by inco ⁇ oration of radio-labeled phosphate into polyglutamic acid, tyrosine, 4: 1 (pEY) substrate.
- the phosphorylated pEY product is trapped onto a filter membrane and the incoporation of radio- labeled phosphate quantified by scintillation counting.
- KDR (Terman, B.I. et al. Oncogene (1991) vol. 6, pp. 1677-1683.) and Flt-1 (Shibuya, M. et al. Oncogene (1990) vol. 5, pp. 519- 524) were cloned as glutathione S-transferase (GST) gene fusion proteins. This was accomplished by cloning the cytoplasmic domain of the KDR kinase as an in frame fusion at the carboxy terminus of the GST gene.
- GST glutathione S-transferase
Priority Applications (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98923719A EP0984692A4 (en) | 1997-05-30 | 1998-05-26 | ANGIOGENESIS INHIBITORS |
| AU75944/98A AU734009B2 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
| US09/424,132 US6380203B1 (en) | 1998-01-14 | 1998-05-26 | Angiogenesis inhibitors |
| CA002291709A CA2291709A1 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
| JP50079099A JP2002501532A (ja) | 1997-05-30 | 1998-05-26 | 新規血管形成阻害薬 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4807697P | 1997-05-30 | 1997-05-30 | |
| US60/048,076 | 1997-05-30 | ||
| GB9800681.0 | 1998-01-14 | ||
| GBGB9800681.0A GB9800681D0 (en) | 1998-01-14 | 1998-01-14 | Novel angiogenesis inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1998054093A1 true WO1998054093A1 (en) | 1998-12-03 |
Family
ID=26312935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1998/010590 WO1998054093A1 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP0984692A4 (ja) |
| JP (1) | JP2002501532A (ja) |
| AU (1) | AU734009B2 (ja) |
| CA (1) | CA2291709A1 (ja) |
| WO (1) | WO1998054093A1 (ja) |
Cited By (159)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1109555A1 (en) * | 1998-08-31 | 2001-06-27 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| EP1147107A1 (en) * | 1999-01-20 | 2001-10-24 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| EP1161433A1 (en) * | 1999-03-11 | 2001-12-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| WO2002040485A1 (fr) * | 2000-11-17 | 2002-05-23 | Ishihara Sangyo Kaisha, Ltd. | Medicaments preventifs ou therapeutiques contre le diabete, contenant des composes a heterocycle fusionne ou leurs sels |
| WO2003051886A1 (en) * | 2001-12-17 | 2003-06-26 | Smithkline Beecham Corporation | Pyrazolopyridazine derivatives |
| US6593326B1 (en) | 1998-12-24 | 2003-07-15 | Astrazeneca Ab | 2,4-diamino pyrimidine compounds having anti-cell proliferative activity |
| US6632820B1 (en) | 1998-08-29 | 2003-10-14 | Astrazeneca Ab | Pyrimidine compounds |
| US6649608B2 (en) | 2000-03-01 | 2003-11-18 | Astrazeneca Ab | 2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents |
| US6649759B2 (en) | 2000-03-30 | 2003-11-18 | Pfizer Inc. | Neuropeptide Y antagonists |
| US6670368B1 (en) | 1999-04-06 | 2003-12-30 | Astrazeneca Ab | Pyrimidine compounds with pharmaceutical activity |
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| US6716831B1 (en) | 1999-03-06 | 2004-04-06 | Astrazeneca Ab | 2,4-diamino-pyrimidine deprivatives having anti-cell proliferative activity |
| WO2004087707A1 (en) * | 2003-03-31 | 2004-10-14 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
| US6833456B2 (en) | 2002-03-01 | 2004-12-21 | Agouron Pharmaceuticals, Inc. | Indolyl-urea derivatives of thienopyridines useful as antiangiogenic agents, and methods for their use |
| US6838464B2 (en) | 2000-03-01 | 2005-01-04 | Astrazeneca Ab | 2,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineaoplastic agents |
| US6844341B2 (en) | 2001-02-17 | 2005-01-18 | Astrazeneca Ab | Pyrimidine derivatives for inhibition of cell proliferation |
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| CA2291709A1 (en) | 1998-12-03 |
| AU7594498A (en) | 1998-12-30 |
| EP0984692A4 (en) | 2001-02-21 |
| JP2002501532A (ja) | 2002-01-15 |
| AU734009B2 (en) | 2001-05-31 |
| EP0984692A1 (en) | 2000-03-15 |
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