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35 条记录 (耗时 0.035 秒)

    Perhydroisoindole derivatives as antagonists of substance P
    2.
    发明授权
    Perhydroisoindole derivatives as antagonists of substance P 失效
    全氟异吲哚衍生物作为P物质的拮抗剂

    公开(公告)号：US5484804A

    公开(公告)日：1996-01-16

    申请号：US313121

    申请日：1994-10-11

    申请人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    发明人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    IPC分类号： C07D405/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/02 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D209/44 ,  C07D403/06 ,  C07D409/06 ,  C07D401/06

    CPC分类号： C07D403/06 ,  C07D209/44 ,  C07D409/06

    摘要： This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.

    摘要翻译： PCT No。PTC / FR93 / 00352 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。 公开号WO93 / 21155 本发明涉及通式（I）的新型全氢异吲哚衍生物，其中基团R是任选被卤素原子或甲基取代的2-或3-取代的苯基; R1是任选取代的苯基，环己二烯基，萘基，茚基或任选取代的杂环基; R2是H，卤素，OH，烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基，烷硫基，酰氧基，羧基，任选取代的烷氧基羰基，苄氧羰基，氨基或酰氨基; R3是任选的2-取代的苯基; 当R 5为H或R 4和R 5为OH或R 4和R 5一起形成键时，R 4为OH或氟; 异构形式及其混合物; 任选的盐; 及其制备。 新型衍生物作为P物质拮抗剂是特别有用的。

    Perhydroisoindole derivatives and preparation
    4.
    发明授权
    Perhydroisoindole derivatives and preparation 失效
    全氢异吲哚衍生物及其制备方法

    公开(公告)号：US5463077A

    公开(公告)日：1995-10-31

    申请号：US313120

    申请日：1994-10-11

    申请人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    发明人： Daniel Achard ,  Serge Grisoni ,  Jean-Luc Malleron ,  Jean-Francois Peyronel ,  Michel Tabart

    IPC分类号： C07D209/44 ,  C07D403/06 ,  C07D409/06 ,  C07D209/04

    CPC分类号： C07D403/06 ,  C07D209/44 ,  C07D409/06 ,  Y02P20/55

    摘要： This ivention relates to novel perhydroisoindole derivatives having formula (I), ##STR1## wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R' is a phenyl radical optionally 2-substituted by a C.sub.1-2 alkylk or alkyloxy radical, R" is a fluorine atom or a hydroxy radical, and R'" is a hydrogen atom, or else R' and R'" are hydroxy radicals, or R" and R'" together form a bond, and R.sup.o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.

    摘要翻译： PCT No.PCT / FR93 / 00351 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。 出版物WO93 / 21154 日本公开日1993年10月28日。本说明书涉及具有式（I），其中符号R相同或不同的式（I）的新型全氢异吲哚衍生物是任选被2-或3-取代的苯基 卤素原子或甲基，R'是任选被C 1-2烷基或烷氧基取代的苯基，R“是氟原子或羟基，R”'是氢原子，或 其中R'和R“'是羟基，或者R”和R“'一起形成键，而Ro是氢原子或保护基; 其盐适用; 及其制备。 这些产品是用于制备具有P物质拮抗剂活性的衍生物的合成中间体。

    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them
    6.
    发明授权
    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效

    公开(公告)号：US5021420A

    公开(公告)日：1991-06-04

    申请号：US375934

    申请日：1989-07-06

    申请人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    发明人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P43/00 ,  C07D275/06 ,  C07D417/00 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    CPC分类号： C07D275/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    8.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US06841562B2

    公开(公告)日：2005-01-11

    申请号：US10659095

    申请日：2003-09-10

    申请人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61P31/04 ,  C07D211/60 ,  C07D401/06 ,  C07D409/14 ,  A61K31/44 ,  C07D215/12 ,  C07D215/18

    CPC分类号： C07D401/06 ,  C07D211/60 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中R 1a是氢，卤素，羟基，氨基，烷基氨基，二烷基氨基，羟基氨基，烷氧基氨基或烷基烷氧基氨基，R 1b是氢，或者R 1a和R 1b形成氧代，R 2是羧基，羧甲基或羟甲基， 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基，或与任选被卤素或三氟甲基取代的环烷硫基（3至7个成员）或与杂芳硫基（ 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基或R3是被苯基或杂芳基取代的炔丙基，被苯基或杂芳基取代 R4是烷基，烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基，其各种异构体形式，分别或混合物，和 它们的盐，它们的制备方法和中间体以及含有它们的组合物。 这些新型衍生物是有效的抗菌剂。