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1. 发明公开

EP0839133A1 DERIVES DE 4,9-ETHANO-BANZO(f)ISOINDOLE COMME INHIBITEURS DE FARNESYL TRANSFERASE 失效
标题翻译： 4,9-乙烯基（F）葡萄糖醛酸转运酶抑制剂
公开(公告)号：EP0839133A1
公开(公告)日：1998-05-06
申请号：EP96924952.0
申请日：1996-07-08
申请人： RHONE-POULENC RORER S.A.
发明人： COMMERCON, Alain , LEBRUN, Alain , MAILLIET, Patrick , PEYRONEL, Jean-François , SOUNIGO, Fabienne , TRUCHON, Alain , ZUCCO, Martine
IPC分类号： C07D409 , A61K31 , A61P35 , A61P43 , C07D209 , C07D277 , C07D417 , C07F9
CPC分类号： C07D209/72 , C07F9/5728
摘要： Novel products of general formula (I), preparation thereof and pharmaceutical compositions containing said products are disclosed. In general formula (I), R is a radical of general formula -(CH2)m-X1-(CH2)n-Z, where X1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH2 radicals being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR4, where R4 is alkyl, or CON(R5)(R6), where R5 is hydrogen or alkyl and R6 is hydrogen or optionally substituted alkyl, or else R5 is hydrogen or alkyl and R6 is hydroxy, optionally substituted alkyloxy or amino, or PO(OR7)2, where R7 is hydrogen or alkyl; or a radical -NH-CO-T where T is hydrogen or optionally substituted alkyl; or else a radical (a); R1 and R2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R1 and R2 in ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted heteroatoms, or R1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R2 is thioalkyl; R3 is hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or -NH-, -CO-, methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of general formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.

2. 发明授权

EP0635003B1 DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA SUBSTANCE P 有权转让
标题翻译： PERHYDROISOINDOLE衍生物作为P物质拮抗剂
公开(公告)号：EP0635003B1
公开(公告)日：1998-06-17
申请号：EP93909005.6
申请日：1993-04-08
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , GRISONI, Serge , MALLERON, Jean-Luc , PEYRONEL, Jean-François , TABART, Michel
IPC分类号： C07D209/44 , A61K31/40 , C07D409/06
CPC分类号： C07D403/06 , C07D209/44 , C07D409/06

3. 发明公开

EP0794944A1 DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA SUBSTANCE P 失效
标题翻译： DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA物质P
公开(公告)号：EP0794944A1
公开(公告)日：1997-09-17
申请号：EP95941161.0
申请日：1995-11-29
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , PEYRONEL, Jean-François , TABART, Michel
IPC分类号： A61K31 , A61P1 , A61P9 , A61P11 , A61P25 , A61P27 , A61P29 , A61P43 , C07D209 , C07D401 , C07D409
CPC分类号： C07D401/06 , C07D209/44 , C07D409/06
摘要： New perhydroinsoindole having the general formula (I) wherein R1 is optionally substituted phenyl or is cyclohexadienyl, naphtyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is phenyl optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF3, and R4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N3 or -NHCN, and the radicals R which are similar or different represent H, alkyl or phenyl, in their isomer forms having the structure (Ia) or mixtures thereof, optionally their salts when they exist and preparation thereof. The new derivatives of the invention are particularly useful as antagonists of substance P.
摘要翻译：具有通式（I）的新的全氢异吲哚：其中R 1是任选取代的苯基或是环己二烯基，萘基，茚基或单环或多环杂环基，饱和或不饱和的5至9℃和任选取代的，R 2是H或卤素，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，烷氧基羰基，二烷基氨基酰氧基羰基，苄氧基羰基，氨基或酰氨基，R3是在-2位任选被基团烷基或烷氧基1或2C或OH或F取代的苯基，（Ia）的异构体形式中，R4是含有被卤素或CN，N3或-NHCN取代的1或2C的烷基，且相同或不同的基团R表示H，烷基或苯基，或它们的混合物，当它们存在时其任选的盐及其制备。本发明的新衍生物作为物质P的拮抗剂特别有用。

4. 发明公开

EP0586490A1 NOUVEAUX DERIVES DE PERHYDROISOINDOLE, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 失效
标题翻译：新PERHYDROISOINDOLDERIVATE，生产和药物含。
公开(公告)号：EP0586490A1
公开(公告)日：1994-03-16
申请号：EP92911474.0
申请日：1992-05-15
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , GRISONI, Serge , HANESSIAN, Stephen , MOUTONNIER, Claude , PEYRONEL, Jean-François , TABART, Michel , TRUCHON, Alain
IPC分类号： A61K31 , A61P43 , C07D209 , C07D403 , C07D405 , C07D409
CPC分类号： C07D209/44
摘要： Nouveaux dérivés de perhydroisoindole de formule générale (I) dans laquelle les radicaux R sont des atomes d'hydrogène ou forment ensemble une liaison, les symboles R' sont des radicaux phényle pouvant être substitués par un atome d'halogène ou un radical méthyle en position 2 ou 3, X est un atome d'oxygène ou un radical NH, R1 est phényle éventuellement substitué, cyclohexadiényle, naphtyle, ou hétérocyclyle, R2 est H, halogène, OH, alcoyle, aminoalcoyle, alcoylaminoalcoyle, dialcoylaminoalcoyle, alcoyloxy, alcoythio, acyloxy, carboxy, alcoyloxycarbonyle éventuellement substitué, benzyloxycarbonyle, amino ou acylamino, R3 est halogène ou OH et R4 est H ou halogène si R3 est halogène sous leurs formes isomères ou leurs mélanges, éventuellement leurs sels lorsqu'ils existent et leur préparation. Les nouveaux dérivés selon l'invention sont particulièrement intéressants comme antagonistes de la substance P.

5. 发明授权

EP0839133B1 DERIVES DE 4,9-ETHANO-BENZO(f)ISOINDOLE COMME INHIBITEURS DE FARNESYL TRANSFERASE 失效
标题翻译： 4,9-乙酸苄酯（F）葡萄糖醛酸转运酶抑制剂
公开(公告)号：EP0839133B1
公开(公告)日：1999-10-06
申请号：EP96924952.3
申请日：1996-07-08
申请人： RHONE-POULENC RORER S.A.
发明人： COMMERCON, Alain , LEBRUN, Alain , MAILLIET, Patrick , PEYRONEL, Jean-François , SOUNIGO, Fabienne , TRUCHON, Alain , ZUCCO, Martine
IPC分类号： C07D209/72 , A61K31/40 , C07D403/06 , C07D401/06 , C07F9/572 , C07D405/12 , C07D409/12 , C07D401/12 , C07D417/12
CPC分类号： C07D209/72 , C07F9/5728

6. 发明授权

EP0693059B1 DERIVES DE PERHYDROISOINDOLE, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 失效
标题翻译： Perhydroisoindole衍生物，生产和YOU BEHALTENDE制药摘要
公开(公告)号：EP0693059B1
公开(公告)日：1997-03-12
申请号：EP94912582.7
申请日：1994-04-01
申请人： RHONE-POULENC RORER S.A.
发明人： CRESPO, André , FARDIN, Véronique , GUILLAUME, Jean-Marc , MALLERON, Jean-Luc , PEYRONEL, Jean-François
IPC分类号： C07D209/44 , C07D403/06 , C07D403/10 , A61K31/40
CPC分类号： C07D403/06 , C07D209/44
摘要： Perhydroisoindole derivatives of general formula (I), wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.

7. 发明公开

EP0693059A1 PERHYDROISOINDOLE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 失效
标题翻译： Perhydroisoindole衍生物，生产和YOU BEHALTENDE制药摘要
公开(公告)号：EP0693059A1
公开(公告)日：1996-01-24
申请号：EP94912582.0
申请日：1994-04-01
申请人： RHONE-POULENC RORER S.A.
发明人： CRESPO, André , FARDIN, Véronique , GUILLAUME, Jean-Marc , MALLERON, Jean-Luc , PEYRONEL, Jean-François
IPC分类号： A61K31 , A61P1 , A61P9 , A61P11 , A61P13 , A61P15 , A61P25 , A61P29 , A61P43 , C07D209 , C07D403
CPC分类号： C07D403/06 , C07D209/44
摘要： Perhydroisoindole derivatives of general formula (I), wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.

8. 发明公开

EP0635002A1 NOUVEAUX DERIVES DE PERHYDROISOINDOLE, ET LEUR PREPARATION 失效
标题翻译： NOUVEAUX DERIVES DE PERHYDROISOINDOLE，ET LEUR PREPARATION
公开(公告)号：EP0635002A1
公开(公告)日：1995-01-25
申请号：EP93909004.0
申请日：1993-04-08
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , GRISONI, Serge , MALLERON, Jean-Luc , PEYRONEL, Jean-François , TABART, Michel
IPC分类号： C07D209 , C07D403 , C07D409
CPC分类号： C07D403/06 , C07D209/44 , C07D409/06 , Y02P20/55
摘要： Novel perhydroisoindole derivatives having formula (I), 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 C1-2 alkyl 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° is a hydrogen atom or a protective radical; salts thereof wherever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.
摘要翻译：具有式（I）的新的全氢异吲哚衍生物，其中符号R相同或不同，是任选地被卤素原子或甲基取代的2-或3-取代的苯基，R'是任选地被2-取代的苯基由C1-2烷基或烷氧基组成，R'为氟原子或羟基，R“'为氢原子，或者R'和R”'为羟基，或者R'和R' ''一起形成键，并且R 0是氢原子或保护基; 任何适用的盐; 和其制备。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。

9. 发明公开

EP0587673A1 NOUVEAUX DERIVES DU THIOPYRANOPYRROLE ET LEUR PREPARATION 失效
标题翻译：新THIOPYRANOPYRROLE及其制备方法。
公开(公告)号：EP0587673A1
公开(公告)日：1994-03-23
申请号：EP92911607.0
申请日：1992-05-15
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , MOUTONNIER, Claude , PEYRONEL, Jean-François , TABART, Michel , TRUCHON, Alain
IPC分类号： A61K31 , A61P9 , A61P25 , A61P29 , A61P37 , C07D495
CPC分类号： C07D495/04
摘要： Nouveaux dérivés de thiopyranopyrrole de formule générale (I) dans laquelle R est hydrogène, allyle ou un radical de structure: -CRaRbRc dans laquelle Ra et Rb sont des atomes d'hydrogène ou des radicaux phényle éventuellement substitutés (par halogène, alcoyle, alcoyloxy ou nitro), et Rc est défini comme Ra et Rb ou représente un radical alcoyle ou alcoyloxyalcoyle, l'un au moins de Ra, Rb et Rc étant un radical phényle substitué ou non, et n = 0 à 2, sous leurs formes stéréoisomères et leurs mélanges, éventuellement leurs sels lorsqu'ils existent et leur préparation. Les nouveaux dérivés selon l'invention sont particulièrement intéressants comme intermédiaires de synthèse.

10. 发明公开

EP0966473A1 THIAZOLOBENZOHETEROCYCLES, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
标题翻译： THIAZOLOBENZOHETERORINGE，生产和药物含有它们的
公开(公告)号：EP0966473A1
公开(公告)日：1999-12-29
申请号：EP98912552.0
申请日：1998-02-26
申请人： RHONE-POULENC RORER S.A.
发明人： HARDY, Jean-Claude , BOUQUEREL, Jean , NEMECEK, Patrick , ALOUP, Jean-Claude , MIGNANI, Serge , PEYRONEL, Jean-François
IPC分类号： C07D215 , A61K31 , A61P9 , A61P25 , A61P43 , C07D241 , C07D265 , C07D279 , C07D293 , C07D401 , C07D498 , C07D513 , C07D517
CPC分类号： C07D513/06
摘要： The invention concerns compounds of formula (I) in which R1 represents a sulphur or selenium atom, R2 represents hydrogen or alkyl, -R3-R4-R5- represents a chain of formula -CH2-CH2-CH2-, -CH(R7)-CH2-CH2-, -CH2-CH2-CH(R8)-, -CH2-CH(R9)-CH2-, -CH2-CH2-S-, -CH2-CH2-SO-, -CH2-CH2-SO2-, -CH2-CH2-Se-, -CH2-CH2-O-, -CH2-CH2-CO-, -CH2-CH2-N(R10)-, -CH2-CO-N(R10)-, -CH2-CF2-CH2-, -CH2-CF2-CH(OH)-, -CH2-CH(R13)-S-, -CH2-CH(R13)-SO-, or -CH2-CH(R13)-SO2-, R6 represents a polyfluoroalkyl, polyfluoroalcoxy or polyfluoroalkylthio radical, R7 represents alkyl, -CH2OH, -CH2-SO2-alk or -CH2-NR11R12, R8 represents alkyl, hydroxy, -CH2OH, -NR11R12, -CH2-NR11R12, -S-alk, -SO-alk, -SO2-alk, thienyl, furyl, phenyl, or phenyl substituted, R9 represents alkyl or -CH2OH, R10 represents hydrogen or alkyl, R11 represents hydrogen or alkyl, -CO-alk or -CO-CF3, R12 represents hydrogen or alkyl, or R11 and R12 form with the nitrogen atom to which they are bound a heterocyclic compound, R13 represents alkyl or -CH2OH, their salts, their methods of preparation, medicines containing them and the intermediates.

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