发明名称 SUBSTITUTED INDAZOLE DERIVATIVES AND THEIR USE AS PHOSPHODIESTERASE (PDE) TYPE IV AND TUMOR NECROSIS FACTOR (TNF) INHIBITORS
摘要 1. A compound of the formula I or a pharmaceutically acceptable salt thereof, wherein: R is cyclopentyl or cyclohexyl; R1 is C1-C2 alkyl, and R2 is a grouping selected from the group, consisting from the groupings of formulas from (1.1) to (1.12) 2. The compound of Claim 1 wherein R2 is a grouping of formula (l.1). 3. The compound of Claim 1 wherein R2 is a grouping of formula (l.10). 4. The compound of Claim 1 wherein R2 is a grouping of formula (l.6). 5. The compound of Claim 1 wherein R2 is a grouping of formula (l.5). 6. The compound of Claim 1 wherein R2 is a grouping of formula (l.3). 7. The compound of Claim 1, selected from the group consisting of: racemic 4-(1-cyclopentyl-3-ethyl-1H-indazol-6-yl)-pyrrolidine-2-one; (+)-4-(1-cyclopentyl-3-ethyl-1H-indazol-6-yl)-pyrrolidine-2-one; (-)4-(1-cyclopentyl-3-ethyl-1H-indazol-6-yl)-pyrrolidine-2-one; and pharmaceutically acceptable salts of said compounds. 8. The compound of Claim 1 selected from the group consisting of: racemic 4-(1-cyclohexyl-3-ethyl-1H-indazol-6-yl)-pyrrolidine-2-one; (+)-4-(1-cyclohexyl-3-ethyl-1H-indazol-6-yl)-pyrrolidine-2-one; (-)-4-(1-cyclohexyl-3-ethyl-lH-indazol-6-yl)-pyrrolidine-2-one; and pharmaceutically acceptable salts of said compounds. 9. The compound of Claim 1 wherein R is cyclopentyl. 10. The compound of Claim 1 wherein R is cyclohexyl. 11. The compound of Claim 1 wherein R1 is ethyl. 12. A pharmaceutical composition for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal comprising a therapeutically-effective amount of the compound of Claim 1 and a pharmaceutically acceptable carrier. 13. A method for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal which comprises administering to said mammal a therapeutically-effective amount of the compound of Claim 1.
申请公布号 EA002274(B1) 申请公布日期 2002.02.28
申请号 EA19980001047 申请日期 1997.06.02
申请人 PFIZER INC. 发明人 MARFAT, ANTHONY
分类号 A61K31/00;A61K31/415;A61K31/416;A61K31/4178;A61K31/506;A61P1/00;A61P3/00;A61P11/00;A61P13/00;A61P17/00;A61P19/00;A61P25/04;A61P29/00;A61P31/00;A61P35/00;A61P43/00;C07D403/04 主分类号 A61K31/00
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