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A process for the preparation of novel therapeutically useful 5- (2,5-disubstituted phenyl) -1,3-dialkyl-1,6-dihydro-7H-pyrazolo 4,3-d pyrimidin-7-one.
A process for the preparation of novel therapeutically useful 5- (2,5-disubstituted phenyl) -1,3-dialkyl-1,6-dihydro-7H-pyrazolo 4,3-d pyrimidin-7-one.
Compounds of formula: CHEM and pharmaceutically acceptable salts thereof, wherein R1 is H; C1-C3 alkyl optionally substituted with one or more fluoro substituents; or C3-C5 cycloalkyl; R2 is H, or C1-C6 alkyl optionally susbtituted with one or more fluoro subtituents or with C3-C6 cycloalkyl; R3 is C1-C6 alkyl optionally substituted with one or more fluoro substituents or with C3-C6 cycloalkyl; C3-C5 cycloalkyl; C3-C6 alkenyl; or C3-C6 alkynyl; R4 is C1-C4 alkyl optionally substituted with OH, NR5R6, CN, CONR5R6 or CO2R7; C2-C4 alkenyl optionally substituted with CN, CONR5R6 or CO2R7; C2-C4 alkanoyl optionally substituted with NR5R6; hydroxy C2-C4 alkyl optionally susbtituted with NR5R6; (C2-C3 alkoxy)C1-C2 alkyl optionally substituted with OH or NR5R6; CONR5R6; CO2R7; halo; NR5R6; NHSO2NR5R6; NHSO2R8; or phenyl or heterocyclyl either of which is optionally substituted with methyl; R5 and R6 are each independently H or C1-C4 alkyl, or together with the nitrogen atom to which they are attached from a pyrrolidinyl, piperidino, morpholino, 4-(NR9)-piperazinyl or imidazoyl group wherein said group is optionally substituted with methyl or hydroxy; R7 is H or C1-C4 alkyl; R8 is C1-C3 alkyl optionally substituted with NR5R6; and R9 is H; C1-C3 alkyl optionally substituted with phenyl; hydroxy C2-C3 alkyl; or C1-C4 alkanoyl; are selective cGMP PDE inhibitors useful in the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.
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机译:式:的化合物及其药学上可接受的盐,其中R 1为H;任选地被一个或多个氟取代基取代的C 1 -C 3烷基;或C3-C5环烷基;或R 2是H,或任选地被一个或多个氟取代基或被C3-C6环烷基取代的C1-C6烷基; R 3是任选地被一个或多个氟取代基或被C3-C6环烷基取代的C1-C6烷基; C3-C5环烷基; C3-C6烯基;或C3-C6炔基;或R 4为任选地被OH,NR 5 R 6,CN,CONR 5 R 6或CO 2 R 7取代的C 1 -C 4烷基;任选地被CN,CONR 5 R 6或CO 2 R 7取代的C 2 -C 4烯基;任选被NR 5 R 6取代的C 2 -C 4烷酰基;任选被NR 5 R 6取代的羟基C 2 -C 4烷基; (C 2 -C 3烷氧基)C 1 -C 2烷基,其任选地被OH或NR 5 R 6取代; CONR <5> R <6>; CO 2 R 7;光环; NR 5 R 6; NHSO 2 NR 5 R 6; NHSO 2 R 8;苯基或杂环基,其任选被甲基取代; R 5和R 6各自独立地为H或C 1 -C 4烷基,或与它们所连接的氮原子一起由吡咯烷基,哌啶子基,吗啉代,4-(NR 9)-哌嗪基或咪唑基连接其中所述基团任选地被甲基或羟基取代的基团; R 7为H或C1-C4烷基; R 8为任选被NR 5 R 6取代的C 1 -C 3烷基; R 9为H;任选地被苯基取代的C1-C3烷基;羟基C2-C3烷基;或C1-C4烷酰基;或是选择性cGMP PDE抑制剂,可用于治疗心血管疾病,如心绞痛,高血压,心力衰竭和动脉粥样硬化。
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