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    • 11. 发明授权
      US5739123A Phosphinic acid derivatives with metallopeptidase inhibitory activity 失效
    • Phosphinic acid derivatives with metallopeptidase inhibitory activity
    • US5739123A
    • 1998-04-14
    • US750035
    • 1996-11-27
    • Gabriele Norcini , Daniela Botta , Francesco Santangelo , Gabriele Morazzoni
    • Gabriele Norcini , Daniela Botta , Francesco Santangelo , Gabriele Morazzoni
    • A61K31/66 , A61P9/00 , A61P43/00 , C07F9/30
    • C07F9/301
    • Compounds of formula (I), ##STR1## wherein R is a biphenyl group 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, C.sub.1 -C.sub.3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom, a straight or branched C.sub.1 -C.sub.6 alkyl group or an arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a biphenyl, a napthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted with 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, C.sub.1 -C.sub.3 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; R.sub.2 is a straight or branched C.sub.1 -C.sub.6 alkyl group, optionally containing one or more fluorine atoms or one or more --NH-- groups, an arylalkyl, an arylcarbonylaminoalkyl, an arylalkylcarbonylaminoalkyl or an arylaminocarbonylalkyl group having from 1 to 6 carbon atoms and optionally one or more --NH-- groups 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, C.sub.1 -C.sub.3 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; m is 0 or 1; X is a hydrogen or fluorine atom; the carbon atom marked with an asterisk is an asymmetric carbon atom; 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 12. 发明授权
      US5760285A Phosphonyldipeptides useful in the treatment of cardiovascular diseases 失效
    • Phosphonyldipeptides useful in the treatment of cardiovascular diseases
    • 可用于治疗心血管疾病的膦酰二肽
    • US5760285A
    • 1998-06-02
    • US702701
    • 1996-09-13
    • Gabriele Norcini , Gabriele Morazzoni , Francesco Santangelo
    • Gabriele Norcini , Gabriele Morazzoni , Francesco Santangelo
    • A61K38/00 , C07K5/06 , C07F9/22 , A01N57/36
    • C07K5/06191 , A61K38/00
    • Compounds of formula (II) ##STR1## wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl or thioalkyl groups having from 1 to 6 carbon atoms in the alkyl moiety, carboxylic groups, nitro groups, amino, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 allyl; R.sub.2 is a straight or branched C.sub.1 -C.sub.6 alkyl or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a naphthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted as above indicated for the R substituent; R.sub.3 is a straight or branched C.sub.1 -C.sub.6 alkyl, optionally containing one or more fluorine atoms, or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety; the carbon atoms marked with an asterisk are asymmetric carbon atoms; and their pharmaceutically acceptable salts, are described. The compounds of formula (II) are useful in the treatment of cardiovascular diseases.
    • PCT No.PCT / EP95 / 01322 Sec。 371日期1996年9月13日 102（e）1996年9月13日PCT PCT 1995年4月11日PCT公布。 WO95 / 28417 PCT出版物 日期：1995年10月26日化学式（II）其中R是任选被一个或多个选自卤素原子，羟基，烷氧基，烷基或硫代烷基中的一个或多个相同或不同的取代基取代的联苯基 在烷基部分具有1至6个碳原子，在烷基部分具有1至6个碳原子的羧基，硝基，氨基，一或二烷基氨基; R1是氢原子或直链或支链C1-C4烯丙基; R2是直链或支链的C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基，其中芳基是苯基，萘基或具有一个或两个选自氮， 氧和硫，任选地被如上述R取代基所取代; R3是任选地含有一个或多个氟原子的直链或支链C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基; 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（II）的化合物可用于治疗心血管疾病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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