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标题翻译：具有金属蛋白酶抑制活性的肽衍生物

公开(公告)号：WO1995035307A1

公开(公告)日：1995-12-28

申请号：PCT/EP1995002100

申请日：1995-06-02

申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , NORCINI, Gabriele , BOTTA, Daniela , ROMAGNANO, Stefano , SANTANGELO, Francesco

发明人： ZAMBON GROUP S.P.A.

IPC分类号： C07K05/02

CPC分类号： C07K5/022 , A61K38/00

摘要： Compounds of formula (I) wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, nitro groups, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R1 is a hydrogen atom, a straigth or branched C1-C6 alkyl or an arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a biphenyl, a naphthyl or a 5- or 6-membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R2 is a straigth or branched C1-C6 alkyl optionally substituted by one or more substituents selected among amino, mono- or di-(C1-C6)alkylamino or aminocarbonyl groups, mono or di-(C1-C6)-alkylaminocarbonyl groups, an arylalkyl, an arylcarbonylaminoalkyl, an arylaminocarbonylalkyl or an arylalkylaminocarbonylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety, the aryl being optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; X is a single bond or an -N(R3)- group wherein R3 is a hydrogen atom or a straight or C1-C4 alkyl group; the carbon atoms marked with an asterisk are asymmetric carbon atoms; and their pharmaceutically acceptable salts, are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

摘要翻译：式（I）化合物其中R是任选被一个或多个选自卤素原子，硝基，羟基，烷氧基，烷基，硫代烷基或具有1至6个碳原子的烷氧基羰基的一个或多个取代基取代的联苯基烷基部分中的原子，含有一个或多个氟原子的C 1 -C 3烷基，羧基，氨基或氨基羰基，酰氨基，氨基磺酰基，烷基部分中具有1至6个碳原子的单或二烷基氨基，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; R 1是烷基部分中的氢原子，直链或支链的C 1 -C 6烷基或具有1至6个碳原子的芳基烷基，其中芳基是苯基，联苯基，萘基或5或6元芳族具有一个或两个选自氮，氧和硫的杂原子的杂环，任选地被一个或多个选自具有1-6个碳原子的卤素原子，羟基，烷氧基，烷基，硫代烷基或烷氧基羰基中的相同或不同的取代基取代在烷基部分中，含有一个或多个氟原子，羧基，硝基，氨基或氨基羰基的C 1 -C 3烷基，酰氨基，氨基磺酰基，具有1至6个碳原子的单或二烷基氨基烷基部分，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; R 2是任选被一个或多个选自氨基，单 - 或二 - （C 1 -C 6）烷基氨基或氨基羰基，单或二 - （C 1 -C 6） - 烷基氨基羰基的取代基取代的直链或支链C 1 -C 6烷基，芳基烷基，芳基羰基氨基烷基，芳基氨基羰基烷基或在烷基部分具有1至6个碳原子的芳基烷基氨基羰基烷基，芳基任选被一个或多个相同或不同的取代基取代，选自卤素原子，羟基，烷氧基，烷基，在烷基部分具有1至6个碳原子的硫代烷基或烷氧基羰基，含有一个或多个氟原子的C 1 -C 3烷基，羧基，硝基，氨基或氨基羰基，酰氨基，氨基磺酰基，单或二在烷基部分具有1至6个碳原子的 - 烷基氨基，在烷基部分具有1至6个碳原子的单 - 或二 - 烷基氨基羰基; X是单键或-N（R3） - 基，其中R3是氢原子或直链或C1-C4烷基; 标有星号的碳原子是不对称碳原子; 及其药学上可接受的盐。式（I）化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

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