申请人:Janssen Pharmaceutica N.V.
公开号:US20030199473A1
公开(公告)日:2003-10-23
This invention concerns the compounds of formula
1
the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R
1
and R
2
are each independently selected from hydrogen; hydroxy; amino; optionally substituted C
1-6
alkyl; C
1-6
alkyloxy; C
1-6
alkylcarbonyl; C
1-6
alkyloxycarbonyl; Ar
1
; mono- or di(C
1-6
alkyl)amino; mono- or di(C
1-6
alkyl)aminocarbonyl; dihydro-2(3H)-furanone; or R
1
and R
2
taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C
1-6
alkyl)aminoC
1-4
alkylidene; R
3
is hydrogen, Ar
1
, C
1-6
alkylcarbonyl, C
1-6
alkyl, C
1-6
alkyloxycarbonyl, C
1-6
alkyl substituted with C
1-6
alkyloxycarbonyl; and R
4
, R
5
, R
6
, R
7
and R
8
are each independently selected from hydrogen, halo, C
1-6
alkyl, C
1-6
alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C
1-10
alkyl; C
3-10
alkenyl; C
3-10
alkynyl; C
3-7
cycloalkyl; Ar
1
is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
本发明涉及公式1的化合物,其药学上可接受的酸盐加成物和立体化学异构体,其中R1和R2各自独立地选择氢; 羟基; 氨基; 可选取代的C1-6烷基; C1-6烷氧基; C1-6烷基羰基; C1-6烷氧羰基; Ar1; 单或双(C1-6烷基)氨基; 单或双(C1-6烷基)氨基羰基; 二氢-2(3H)-呋喃酮; 或R1和R2共同形成吡咯烷基,哌啶基,吗啉基,偶氮基或单或双(C1-6烷基)氨基C1-4烷基亚甲基; R3为氢,Ar1,C1-6烷基羰基,C1-6烷基,C1-6烷氧羰基,C1-6烷基取代C1-6烷氧羰基; R4,R5,R6,R7和R8各自独立地选择氢,卤素,C1-6烷基,C1-6烷氧基,氰基,氨基羰基,硝基,氨基,三卤甲基或三卤甲氧基; L是可选取代的C1-10烷基; C3-10烯基; C3-10炔基; C3-7环烷基; Ar1是可选取代的苯基; 用于制造治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。它还涉及公式(I)化合物的一个子组成的新化合物,它们的制备和包含它们的组合物。