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    • 97. 发明授权
    • Ethynyl-alanine aryl/alkylsulfonyl-terminated amino-diol compounds for
treatment of hypertension
    • 用于治疗高血压的乙炔基 - 丙氨酸芳基/烷基磺酰基封端的氨基二醇化合物
    • US5314920A
    • 1994-05-24
    • US916447
    • 1992-07-20
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • C07C317/44A61K31/16
    • C07C317/44C07C2101/02C07C2101/14
    • Compounds characterized generally as ethynyl alanine aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl-containing moeity; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
    • 通常表示乙炔基丙氨酸芳基/烷基磺酰基封端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是下式的化合物,其中R 1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘基甲基和氯萘基甲基 ; 其中R2选自氢,甲基,乙基和苯基; 其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,氟萘基甲基和氯萘基甲基; 其中R5是炔丙基或含炔丙基的摩尔; 其中R 7为环己基甲基; 并且其中R8选自正丙基,异丁基,环丙基,环丙基甲基,烯丙基和乙烯基。
    • 99. 发明授权
    • Aryloxyphenylpropylamines and their calcium overload blocking
compositions and methods of use
    • 丙烯酰氧基苯基丙胺及其钙超载阻断组合物及其使用方法
    • US5310756A
    • 1994-05-10
    • US898060
    • 1992-06-12
    • Palle JakobsenJorgen Drejer
    • Palle JakobsenJorgen Drejer
    • A61K31/135A61K31/275A61K31/357A61K31/36A61P9/10A61P21/02A61P25/04A61P25/06A61P25/08C07C213/02C07C217/48C07C217/72C07C253/30C07C255/59C07D317/64C07D521/00C07C255/50
    • C07C217/72C07C217/48C07C255/59C07D317/64C07C2101/02C07C2102/10
    • Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1- -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy- or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano; orR.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.The novel compounds are useful in the treatment of anoxia, migraine, ischemia, epilepsy, traumatic injury and neurode-generative diseases.
    • 具有式(I)的新型芳氧基苯基丙胺其中X为H,氰基,卤素,卤代烷基,C 1-6 - 烷氧基,C 1 - 烷基,C 1-5 - 烷酰基,C 3-5 - 亚烷基,芳氧基或芳烷氧基, R 3为任选被一个或多个氰基,卤代C 1-6烷基,C 1-6 - 烷氧基,C 1-6 - 烯基,三氟甲基,C 3-5 - 亚烷基, 芳氧基或芳烷氧基; 且R 1和R 2独立地为C 1-10 - 烷基,C 3-7 - 环烷基,C 2-10 - 烯基,C 3-6 - 环烷基-C 1-5 - 烷基,任选被C 1-5 - 烷氧基或氰基取代; 或者R 1和R 2可以与药学上可接受的酸一起形成碳环和其盐,条件是R 1不是C 3-7 - 环烷基,可以是直链,支链或环状的C 1-10 - 烷基或链烯基,未取代的 或被C 1-4 - 烷氧基,芳氧基或环烷基或环烷基烷基取代,当X为H且R 2为甲基时。 新型化合物可用于治疗缺氧,偏头痛,局部缺血,癫痫,创伤性损伤和神经发生疾病。