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    • 1. 发明授权
    • N-substituted 9-alkyladenines
    • N-取代的9-烷基腺嘌呤
    • US5670501A
    • 1997-09-23
    • US299992
    • 1994-09-01
    • James V. PeckRonald J. WysockiIbrahim M. UwaydahNoel J. Cusack
    • James V. PeckRonald J. WysockiIbrahim M. UwaydahNoel J. Cusack
    • A61K31/52A61P7/10A61P9/00A61P13/02A61P15/00A61P25/02C07D473/34A61K31/535C07D317/72
    • C07D473/34
    • Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.2 cannot be H or halogen; and pharmaceutically-acceptable salts thereof. These compounds are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to facilitate recovery from coma, to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrhythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.
    • 其中R 1为C 1至C 4直链或支链烷基的式(ⅩⅧ)表示的光学活性或外消旋化合物; R2选自H,-OR1,-SR1,-NH(R1),-N(R4)(R5),氨基羰基,卤素和-CN,其中R4和R5独立地为C1-C6直链 或支链烷基,或一起形成3-至7-元杂环烷基取代基,这种选自氧,氮和硫的杂原子,任选地包括另外的杂原子,其选自氮,氧和 硫; R3是环戊基或:其中R'和R“独立地是H,= O,-OH或-NH 2,条件是R'和R”可以一起形成如下结构:R3: 其中R“是-OH或-NH 2; 并且进一步的条件是当R 3是环戊基或降冰片基时,则R 2不能是H或卤素; 及其药学上可接受的盐。 这些化合物可用作利尿剂,抗急性或慢性肾功能衰竭的肾脏保护剂,以及促进从昏迷恢复的药剂,以改善由除颤或心肺复苏引起的治疗结果,通过防止复苏后心动过缓,缓慢心律失常和心脏停搏恢复 心脏停搏手术后的心脏功能,治疗或预防间歇性跛行。
    • 2. 发明授权
    • Substituted 9-alkyladenines
    • 取代的9-烷基腺嘌呤
    • US5981524A
    • 1999-11-09
    • US904553
    • 1997-08-04
    • James V. PeckRonald J. WysockiIbrahim M. UwaydahNoel J. Cusack
    • James V. PeckRonald J. WysockiIbrahim M. UwaydahNoel J. Cusack
    • A61K31/52A61P7/10A61P9/00A61P13/02A61P15/00A61P25/02C07D473/34A61K31/535C07D317/72
    • C07D473/34
    • Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.2 cannot be H or halogen; and pharmaceutically-acceptable salts thereof.These compounds are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to facilitate recovery from coma, to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrhythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.
    • 由下式表示的光学活性或外消旋化合物,其中R 1为C 1至C 4直链或支链烷基; R2选自H,-OR1,-SR1,-NH(R1),-N(R4)(R5),氨基羰基,卤素和-CN,其中R4和R5独立地为C1-C6直链 或支链烷基,或一起形成3-至7-元杂环烷基取代基,该杂原子选自氧,氮和硫,任选地包括另外的杂原子,其选自氮,氧和 硫; R 3是环戊基或:其中R'和R“独立地是H,= O,-OH或-NH 2,条件是R'和R”可以一起形成如下R3的结构:其中R' “是-OH或-NH 2; 并且进一步的条件是当R 3是环戊基或降冰片基时,则R 2不能是H或卤素; 及其药学上可接受的盐。 这些化合物可用作利尿剂,抗急性或慢性肾功能衰竭的肾脏保护剂,以及促进从昏迷恢复的药剂,以改善由除颤或心肺复苏引起的治疗结果,通过防止复苏后心动过缓,缓慢心律失常和心脏停搏恢复 心脏停搏手术后的心脏功能,治疗或预防间歇性跛行。