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    Thiophene compounds
    1.
    再颁专利
    Thiophene compounds 失效
    噻吩化合物

    公开(公告)号：USRE37078E1

    公开(公告)日：2001-02-27

    申请号：US09368343

    申请日：1999-08-03

    申请人： Michel Wierzbicki ,  Frédéric Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frédéric Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    IPC分类号： A61K3138

    CPC分类号： C07D333/24

    摘要： The invention relates to thiophene compounds of formula: wherein: X1, X2, Y1 and Y2, which are identical or different, each represents hydrogen or halogen, (C1-C5)-alkyl or alkoxy, or trifluoromethyl, X1 and Y1, which are identical or different, each represents C1-C5 alkoxy, X2 and Y2 each represents hydrogen, R1 represents hydrogen or (C1-C5)-alkyl, A represents a straight (C1-C5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C1-C5)-alkyl, and R2 represents hydrogen, (C1-C6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

    摘要翻译： 本发明涉及下式的噻吩化合物：其中：相同或不同的X1，X2，Y1和Y2各自表示氢或卤素，其中： X1和Y1， 它们相同或不同，各自表示C1-C5烷氧基，X2和Y2各自表示氢，R1表示氢或（C1-C5） - 烷基，A表示直链 （C 1 -C 5） - 烃链，其中每个碳原子任选被（C 1 -C 5） - 烷基单取代或二取代，R 2表示氢，（C 1 -C 6） - 烷基，环己基或苄基; 本发明的产品可以用作抗炎剂。

    New thiophene compounds as intermediates
    2.
    发明授权
    New thiophene compounds as intermediates 失效
    新噻吩化合物作为中间体

    公开(公告)号：US5175294A

    公开(公告)日：1992-12-29

    申请号：US740075

    申请日：1991-08-05

    申请人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Martine Brisset ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Martine Brisset ,  Charles Tordjman

    IPC分类号： C07D333/20 ,  C07D333/24

    CPC分类号： C07D333/20 ,  C07D333/24

    摘要： New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: ##STR2## in which: X, n, a, b, c, R.sub.1, R.sub.2, R and R' are as above defined.

    摘要翻译： 新的具有下式的噻吩化合物：其中：X表示氢，卤素，C 1 -C 5烷基或烷氧基或二烷基氨基; n表示1或2; a表示2〜6的整数， b表示2或3; c表示1或2，并且b + c = 4; R1和R2表示氢或（C1-C5）烷基，或与它们所键合的碳原子一起形成含有3至6个碳原子的烃环; 并且R和R'表示氢或（C1-C5）烷基，或与它们所键合的氮原子一起形成任选地含有氧原子的五价或六价杂环或本身可被取代的第二氮原子; 及其生理上可耐受的盐。 本发明的产品可以治疗特别用于治疗以组织损失为特征的病理学。 作为上述化合物I的合成中使用的新的中间产物，下式的酰胺如下：其中：X，n，a，b，c，R 1，R 2，R和R'如上所定义。

    Thiophene compounds
    3.
    发明授权
    Thiophene compounds 失效
    噻吩化合物

    公开(公告)号：US5705525A

    公开(公告)日：1998-01-06

    申请号：US605537

    申请日：1996-02-22

    申请人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Charles Tordjman

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P1/00 ,  A61P17/00 ,  A61P29/00 ,  C07D333/24 ,  C07D333/16 ,  C07D333/20

    CPC分类号： C07D333/24

    摘要： The invention relates to thiophene compounds of formula: ##STR1## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents hydrogen or halogen, (C.sub.1 -C.sub.5)-alkyl or alkoxy, or trifluoromethyl, R.sub.1 represents hydrogen or (C.sub.1 -C.sub.5)-alkyl, A represents a straight (C.sub.1 -C.sub.5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C.sub.1 -C.sub.5)-alkyl, and R.sub.2 represents hydrogen, (C.sub.1 -C.sub.6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

    摘要翻译： 本发明涉及下式的噻吩化合物：其中：X 1，X 2，Y 1和Y 2相同或不同，各自表示氢或卤素，（C 1 -C 5） - 烷基或烷氧基或三氟甲基，R 1表示氢 或（C 1 -C 5） - 烷基，A表示直链（C 1 -C 5） - 烃链，其中每个碳原子任选被（C 1 -C 5） - 烷基单取代或二取代，并且R 2表示氢，（ C 1 -C 6） - 烷基，环己基或苄基; 及其生理上可耐受的盐。 本发明的产品可以用作抗炎剂。

    Thiophene compounds, compositions and use
    4.
    发明授权
    Thiophene compounds, compositions and use 失效
    噻吩化合物，组成和用途

    公开(公告)号：US5061704A

    公开(公告)日：1991-10-29

    申请号：US617501

    申请日：1990-11-23

    申请人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Martine Brisset ,  Charles Tordjman

    发明人： Michel Wierzbicki ,  Frederic Sauveur ,  Jacqueline Bonnet ,  Martine Brisset ,  Charles Tordjman

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P3/00 ,  A61P43/00 ,  C07D333/20 ,  C07D333/24

    CPC分类号： C07D333/24 ,  C07D333/20

    摘要： 1. New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.2. As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: ##STR2## in which: X, n, a, b, c, R.sub.1, R.sub.2, R and R' are as above defined.

    摘要翻译： 1.下式的新噻吩化合物：其中：X表示氢，卤素，C 1 -C 5烷基或烷氧基或二烷基氨基; n表示1或2; a表示2〜6的整数， b表示2或3; c表示1或2，并且b + c = 4; R1和R2表示氢或（C1-C5）烷基，或与它们所键合的碳原子一起形成含有3至6个碳原子的烃环; 并且R和R'表示氢或（C1-C5）烷基，或与它们所键合的氮原子一起形成任选地含有氧原子的五价或六价杂环或本身可被取代的第二氮原子; 及其生理上可耐受的盐。 本发明的产品可以治疗特别用于治疗以组织损失为特征的病理学。 2.作为合成上述化合物I的新中间体产物，下式的酰胺如下：其中：X，n，a，b，c，R1，R2，R和R'如上所述 定义