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    Azabenzimidazole derivatives which are thromboxane receptor antagonists
    5.
    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。

    Noval benzimidazole and azabenzimiazole derivatives which are thromboxane receptor antagonists, their methods of preparation and pharmaceutical compositions in which they are present
    8.
    发明授权
    Noval benzimidazole and azabenzimiazole derivatives which are thromboxane receptor antagonists, their methods of preparation and pharmaceutical compositions in which they are present 失效
    作为血栓烷受体拮抗剂的Noval苯并咪唑和氮杂苯并噻唑衍生物，其制备方法及其存在的药物组合物

    公开(公告)号：US5021443A

    公开(公告)日：1991-06-04

    申请号：US493880

    申请日：1990-03-15

    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, an alkoxy radical, an alkylthio radical, a sulfone group, a sulfoxide group, 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 or a lower alkyl, or the sulfur atom;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom or a lower alkyl 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 6 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 or a lower alkyl, CONH--R.sub.8, R.sub.8 being the hydrogen atom or a lower alkyl, CN, ##STR2## R.sub.9 being the hydrogen atom or a lower alkyl, or NHSO.sub.2 CF.sub.3, and to their addition salts.

    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，烷氧基，烷硫基，砜基，亚砜基，三氟甲基，硝基，羟基， 亚甲基醇基或COOR'基团，其中R'是氢或低级烷基; X3和X4也可以与苯基形成萘; B是CR5R6，R5和R6是氢原子或低级烷基或硫原子; R1，R2，R3和R4独立地是氢原子或低级烷基; 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6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; 并且D是可以是：COOR7，R7是氢原子或低级烷基，CONH-R8，R8是氢原子或低级烷基的化学基团，CN，R9是氢原子或低级烷基 ，或NHSO 2 CF 3，以及它们的加成盐。

    Process for the preparation of monoesters or diesters of-9,10-endoethano-9,10-dihydroanthracene-11,11-dicarboxylic acid and for the preparation of symmetrical or asymmetrical methylidenemalonates
    9.
    发明授权
    Process for the preparation of monoesters or diesters of-9,10-endoethano-9,10-dihydroanthracene-11,11-dicarboxylic acid and for the preparation of symmetrical or asymmetrical methylidenemalonates 失效
    制备-9,10-内联乙醇基-9,10-二氢蒽-10,11,11-二羧酸的单酯或二酯的方法，用于制备对称或不对称的亚甲基亚氨基三

    公开(公告)号：US4931584A

    公开(公告)日：1990-06-05

    申请号：US162573

    申请日：1988-03-01

    申请人： Nicole Bru-Magniez ,  Christian De Cock ,  Jacques Poupaert ,  Jean-Luc De Keyser ,  Pierre Dumont

    发明人： Nicole Bru-Magniez ,  Christian De Cock ,  Jacques Poupaert ,  Jean-Luc De Keyser ,  Pierre Dumont

    IPC分类号： C07D303/16 ,  B01J31/04 ,  C07B61/00 ,  C07C67/00 ,  C07C67/343 ,  C07C69/38 ,  C07C69/593 ,  C07C69/73 ,  C07C69/732 ,  C07C69/753 ,  C07C253/00 ,  C07C255/52

    CPC分类号： C07C69/38

    摘要： The invention relates to novel monoesters and diesters of 9,10-endoethano-9,10-dihydroanthracene-11,11-dicarboxylic acid.These novel monoesters and diesters correspond to the following structural chemical formula (II): ##STR1## in which R.sup.1 and R.sup.2 are identical or different and can represent H, an alkali metal or alkaline earth metal atom, a linear or branched alkyl group having from 1 to 6 carbon atoms, an alicyclic group having from 3 to 6 carbon atoms, an alkenyl group having from 2 to 6 carbon atoms, defined in their cis or trans variety, or an alkynyl group having from 2 to 6 carbon atoms, the said groups optionally being substituted by one or more functional groups such as ether, epoxide, halogeno, cyano, ester, aldehyde, ketone, aryl etc., where R.sup.1 and R.sup.2 cannot be H or ethyl simultaneously. These addition products constitute valuable intermediates for the preparation of methylidenemalonates in high yields and with a high purity.

    摘要翻译： 本发明涉及9,10-内联乙醛-9,10-二氢蒽-11,11-二羧酸的新型单酯和二酯。 这些新型单酯和二酯对应于以下结构化学式（II）：其中R 1和R 2相同或不同并可以表示H，碱金属或碱土金属原子，直链或支链烷基 具有1至6个碳原子的基团，具有3至6个碳原子的脂环族基团，具有2至6个碳原子的烯基，其顺式或反式变体中定义，或具有2至6个碳原子的炔基 所述基团任选被一个或多个官能团如醚，环氧化物，卤代，氰基，酯，醛，酮，芳基等所取代，其中R1和R2不能同时为H或乙基。 这些加成产物构成用于以高产率和高纯度制备亚甲基亚氨基三甲酸酯的有价值的中间体。