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31 条记录 (耗时 0.035 秒)

    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    11.
    发明申请
    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权

    公开(公告)号：US20120135958A1

    公开(公告)日：2012-05-31

    申请号：US13386827

    申请日：2010-07-23

    申请人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    发明人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    IPC分类号： A61K31/695 ,  A61K31/498 ,  C07D417/14 ,  C07F7/10 ,  C07D401/14 ,  C07D401/04 ,  A61P37/04 ,  A61P3/04 ,  A61P3/10 ,  A61P3/00 ,  A61P9/10 ,  A61P9/12 ,  A61P27/02 ,  A61P25/00 ,  A61P19/10 ,  A61P9/00 ,  A61P1/16 ,  A61P17/02 ,  A61P31/00 ,  A61K31/541

    CPC分类号： C07D401/10 ,  C07D401/12

    摘要： The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —SO2-alkyl, SO2—NR6R7, —NR6—COOR5, —NR6—COR5, or —CO—NR6-alkyl-OR5 group; R5, R6, and R7 are a hydrogen, or an alkyl or alkyl-phenyl group; and R8 is an alkyl, alkyl-Si(alkyl)3, —SO2-alkyl-Si(alkyl)3, phenyl, alkoxy-imino group, or alkyl-cycloalkyl group optionally substituted by one or more halogen atoms or one or more hydroxyl or hydroxyl-alkyl groups; or R8 and R9, together with the carbon atoms to which they are bonded, form a cycloalkyl group optionally substituted by one or more halogen atoms or one or more carboxy groups; and R9 is a hydrogen atom or an alkyl group; with the proviso that, when R8 is an alkyl group, it is bonded onto the Ar2 silicon atom. The invention also relates to a method for preparing same and to the therapeutic use thereof.

    Azabenzimidazole derivatives which are thromboxane receptor antagonists
    12.
    发明授权
    Azabenzimidazole derivatives which are thromboxane receptor antagonists 失效
    作为血栓素受体拮抗剂的偶氮苯并咪唑衍生物

    公开(公告)号：US5124336A

    公开(公告)日：1992-06-23

    申请号：US650732

    申请日：1991-02-05

    申请人： Nicole Bru-Magniez ,  Eric Nicolai ,  Jean-Marie Teulon

    发明人： Nicole Bru-Magniez ,  Eric Nicolai ,  Jean-Marie Teulon

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/44 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D235/06 ,  C07D235/16 ,  C07D235/28 ,  C07D471/04 ,  C07F9/6506 ,  C07F9/6561

    CPC分类号： C07D471/04 ,  C07D235/16 ,  C07D235/28 ,  C07F9/65068 ,  C07F9/6561

    摘要： 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.

    摘要翻译： 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。