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    • 3. 发明申请
    • PHOSPHONYLDIPEPTIDES USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISEASES
    • 用于治疗心血管疾病的磷酰胆碱
    • WO1995028417A1
    • 1995-10-26
    • PCT/EP1995001322
    • 1995-04-11
    • ZAMBON GROUP S.P.A.NORCINI, GabrieleMORAZZONI, GabrieleSANTANGELO, Francesco
    • ZAMBON GROUP S.P.A.
    • C07K05/06
    • C07K5/06191A61K38/00
    • Compounds of formula (II) 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; R1 is a hydrogen atom or a straight or branched C1-C4 alkyl; R2 is a straight or branched C1-C6 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; R3 is a straight or branched C1-C6 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.
    • 式(II)化合物其中R是任选被一个或多个选自在烷基部分中具有1至6个碳原子的卤素原子,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 ,羧基,硝基,氨基,在烷基部分具有1至6个碳原子的一或二烷基氨基; R1是氢原子或直链或支链C 1 -C 4烷基; 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。