发明名称 Indazole derivatives as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) for treating asthma, arthritis, bronchitis, CNS disorders
摘要 The compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein it further relates to pharmaceutical compositions containing, and methods of using for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. Wherein; R is H, C1-9alkyl, -(CH2)m(5 to 10 membered heterocyclyl) wherein m is 0 to 2, (C1-6alkoxy)C1-8alkyl, C2-8alkenyl, or -(Z1)b(Z2)c(C8-10aryl) wherein b and c are independently 0 or 1, Z1 is C1-6alkylene or C2-6alkenylene, and Z2 is 0, S, SO2, or NR12, and wherein said R groups are optionally substituted by 1 to 3 substituents independently selected from the group consisting of halo, hydroxy, C1-5alkyl, C2-5alkenyl, C1-6alkoxy, trifluoromethyl, nitro, -CO2R12, -C(O)NR12R13, -NR12R13 and -SO2NR12R13; R1 is H, C1-9alkyl, C2-3alkenyl, or phenyl, wherein said alkyl, alkenyl and phenyl R, groups are optionally substituted by I to 3 substituents independently selected from the group consisting of methyl, ethyl, trifluoromethyl, and halo; R2 is R18, -C(O)NR12(CHR12)mC(O)NR12O(CH2)q(C8-10) aryl), -C(=NR32)NH(CH2)p(C8-10aryl), -C(O)NR12(CHR12)mC(O)NR12(CH2)pOR12, -C(O)NR12(CHR12)mS(C1-4alkyl), -C(=NOC(O)R25)R26, -CR17R18CHR20NR9SO2(CH2)pA, -CR17R18CHR28NR9P(O)(OR12)C(O)(C1-4alkyl), -CR17R18CHR26NR9P(O)(C1-4alkoxy)2, -Z3-R7, or -(CR17R18)mNR10(C(O))qR10 wherein p is 0 to 2, m is 1 to 6, and q is 1 or 2; or R2 is wherein in said formulas (la)-(li), the structures of formulas (If) and (Ig) are attached to formula I at carbons 5, 6, or 7 of said formulas (If) and (Ig), the dashed line in formulas (Ic) and (Id) indicates a single bond or double bond, except Re is absent in formulas (Ic) and (Id) where said dashed line indicates a double bond, n is 0 to 2, p is 0 to 6, and m is 0 or 1;
申请公布号 NZ334213(A) 申请公布日期 2000.08.25
申请号 NZ19970334213 申请日期 1997.08.25
申请人 PFIZER INC 发明人 MARFAT, ANTHONY
分类号 A61K31/00;A61K31/415;A61K31/416;A61K31/44;A61K31/4427;A61K31/4433;A61K31/4439;A61K31/4709;A61K31/505;A61K31/506;A61P1/00;A61P1/04;A61P3/00;A61P3/10;A61P11/00;A61P11/06;A61P11/08;A61P17/00;A61P17/06;A61P19/00;A61P19/02;A61P25/00;A61P27/16;A61P29/00;A61P31/18;A61P35/00;A61P37/08;A61P43/00;C07D231/56;C07D401/06;C07D401/12;C07D403/06;C07D403/12;C07D409/04;(IPC1-7):A61K31/44 主分类号 A61K31/00
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