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    • 37. 发明授权
    • Azabenzimidazole derivatives which are thromboxane receptor antagonists
    • 作为血栓素受体拮抗剂的偶氮苯并咪唑衍生物
    • US5124336A
    • 1992-06-23
    • US650732
    • 1991-02-05
    • Nicole Bru-MagniezEric NicolaiJean-Marie Teulon
    • Nicole Bru-MagniezEric NicolaiJean-Marie Teulon
    • A61K31/415A61K31/4184A61K31/44A61P9/00A61P9/10A61P9/12A61P11/00A61P13/02A61P15/00A61P25/04A61P37/06A61P37/08A61P43/00C07D235/06C07D235/16C07D235/28C07D471/04C07F9/6506C07F9/6561
    • C07D471/04C07D235/16C07D235/28C07F9/65068C07F9/6561
    • The present invention relates to the derivatives of the formula ##STR1## in which: A is an aromatic ring or a nitrogen heterocycle;X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are independently a hydrogen atom, a halogen atom, a lower alkyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, an alkoxy radical, an alkylthio radical, a sulfone group, SO.sub.2 -lower alkyl, a sulfoxide group, SO-lower alkyl, a trifluoromethyl group, a nitro group, a hydroxyl group, a methylene alcohol radical or a group COOR', in which R' is a hydrogen or a lower alkyl; X.sub.3 and X.sub.4 can also form a naphthalene with the phenyl;B is CR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being a hydrogen atom, a lower alkyl or a C.sub.3 -C.sub.7 cycloalkyl radical, or the sulfur atom;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, a lower alkyl radical or a C.sub.3 -C.sub.7 cycloalkyl radical; CR.sub.1 R.sub.2 or CR.sub.3 R.sub.4 can form with B, when the latter is CR.sub.5 R.sub.6, a cycloalkyl or a cycloalkene having 3 to 7 carbon atoms; R.sub.1 R.sub.2 and R.sub.3 R.sub.4 can also form a ring having 3 to 7 carbon atoms;n is an integer from 1 to 4 and can be 0 if R.sub.1 and R.sub.2 are other than hydrogen; andD is a chemical group which can be: COOR.sub.7, R.sub.7 being the hydrogen atom, a lower alky radical or a C.sub.3 -C.sub.7 cycloalkyl radical, CONH-R.sub.8, R.sub.8 being the hydrogen atom, a lower alkyl radical or a C.sub.3 -C.sub.7 cycloalkyl radical, or CN,and to their addition salts. The compounds are thromboxane antagonist receptors.
    • 本发明涉及式(I)的衍生物,其中:A是芳环或氮杂环; X 1,X 2,X 3和X 4独立地为氢原子,卤素原子,低级烷基,C 3 -C 7环烷基,烷氧基,烷硫基,砜基,SO 2 - 低级烷基,亚砜基, SO - 低级烷基,三氟甲基,硝基,羟基,亚甲基基团或COOR'基团,其中R'为氢或低级烷基; X3和X4也可以与苯基形成萘; B是CR5R6,R5和R6是氢原子,低级烷基或C3-C7环烷基或硫原子; R1,R2,R3和R4独立地为氢原子,低级烷基或C3-C7环烷基; CR1R2或CR3R4可与B形成,当后者为CR5R6时,可以具有3-7个碳原子的环烷基或环烯烃; R1R2和R3R4也可以形成具有3至7个碳原子的环; n为1〜4的整数,如果R 1和R 2不是氢,则为0; D为化学基团,可以是:COOR7,R7是氢原子,低级烷基或C3-C7环烷基,CONH-R8,R8是氢原子,低级烷基或C3-C7环烷基 自由基或CN,以及它们的加成盐。 化合物是血栓素拮抗剂受体。