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
Abstract
Description
Claims
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP50079099A JP2002501532A (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
US09/424,132 US6380203B1 (en) | 1998-01-14 | 1998-05-26 | Angiogenesis inhibitors |
AU75944/98A AU734009B2 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
CA002291709A CA2291709A1 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
EP98923719A EP0984692A4 (en) | 1997-05-30 | 1998-05-26 | Novel angiogenesis inhibitors |
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 (en) |
JP (1) | JP2002501532A (en) |
AU (1) | AU734009B2 (en) |
CA (1) | CA2291709A1 (en) |
WO (1) | WO1998054093A1 (en) |
Cited By (159)
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EP1109555A1 (en) * | 1998-08-31 | 2001-06-27 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
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