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1. 发明申请

WO03008407A3 PHENYLSULFONYL-1,3-DIHYDRO-2H-INDOLE-2-ONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：苯磺酰基-1,3-二氢-2H-吲哚-2-酮衍生物的制备及其治疗用途
公开(公告)号：WO03008407A3
公开(公告)日：2003-10-16
申请号：PCT/FR0202500
申请日：2002-07-15
申请人： SANOFI SYNTHELABO , DI MALTA ALAIN , GARCIA GEORGES , ROUX RICHARD , SCHOENTJES BRUNO , SERRADEIL-LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
发明人： DI MALTA ALAIN , GARCIA GEORGES , ROUX RICHARD , SCHOENTJES BRUNO , SERRADEIL-LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
IPC分类号： A61K20060101 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/503 , A61K31/506 , A61K31/55 , A61K31/551 , A61P20060101 , A61P1/04 , A61P1/08 , A61P1/12 , A61P1/14 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P3/12 , A61P5/24 , A61P5/38 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P15/00 , A61P15/04 , A61P15/10 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P21/02 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P27/06 , A61P27/12 , A61P29/00 , A61P29/02 , A61P31/00 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07D20060101 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention concerns compounds of formula (I), as well as their addition salts with acids or organic salts, their solvates and/or hydrate(s), exhibiting affinity and selectivity for arginine-vasopressin V>1b 1a
摘要翻译：本发明涉及式（I）化合物以及它们与酸或有机盐，它们的溶剂合物和/或水合物的加成盐，它们对精氨酸 - 加压素V> 1b受体和/或对于卵胞质受体，此外，对于某些化合物，对V> 1a <受体具有亲和力。本发明还涉及制备它们的方法，可用于制备它们的式（IV）的中间体化合物，含有它们的药物组合物以及它们用于制备药物的用途。

2. 发明申请

WO0155130A3 NOVEL 1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES AND THEIR USE AS LIGANDS FOR V1B AND V1A ARGININE-VASOPRESSIN RECEPTORS 审中-公开
标题翻译：新的1,3-二氢-2H-吲哚-2-酮衍生物及其作为V1B和V1A亚氨基血管紧张素受体的配体使用
公开(公告)号：WO0155130A3
公开(公告)日：2002-03-14
申请号：PCT/FR0100226
申请日：2001-01-24
申请人： SANOFI SYNTHELABO , ROUX RICHARD , SERRADEIL LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
发明人： ROUX RICHARD , SERRADEIL-LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
IPC分类号： A61K20060101 , A61K31/404 , A61K31/405 , A61K31/496 , A61K31/5377 , A61P20060101 , A61P1/00 , A61P1/18 , A61P3/06 , A61P3/08 , A61P5/38 , A61P5/50 , A61P7/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/02 , A61P15/04 , A61P15/12 , A61P17/06 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D207/12 , C07D209/04 , C07D209/34 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14
CPC分类号： C07D403/04 , A61K31/405 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The invention concerns compounds of formula (I) and their possible salts with mineral or organic acids, their solvates and/or hydrates, having affinity and selectivity for V1b receptor or for both V1b and V1a arginine-vasopressin receptors. The invention also concerns their preparation method, intermediate compounds of formula (II) used in their preparation, pharmaceutical compositions containing them for use in preparing medicines.
摘要翻译：本发明涉及式（I）化合物及其与矿物或有机酸，它们的溶剂化物和/或水合物的可能的盐，对V1b受体或V1b和V1a精氨酸 - 加压素受体具有亲和力和选择性。本发明还涉及它们的制备方法，其制备中使用的式（II）的中间体化合物，含有它们用于制备药物的药物组合物。

3. 发明申请

WO0164668A2 NOVEL 1,3-DIHYDRO-2H-INDOL-2-ONE, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新的1,3-二氢-2H-吲哚-2-酮，制备方法和含有其的药物组合物
公开(公告)号：WO0164668A2
公开(公告)日：2001-09-07
申请号：PCT/FR0100509
申请日：2001-02-22
申请人： SANOFI SYNTHELABO , SERRADEIL LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
发明人： SERRADEIL-LE GAL CLAUDINE , TONNERRE BERNARD , WAGNON JEAN
IPC分类号： A61K31/4725 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/12 , A61P35/00 , C07D209/42 , C07D401/04 , C07D403/04 , A61K31/404 , A61K31/472
CPC分类号： C07D401/04 , C07D209/42 , C07D403/04
摘要： The invention concerns compounds of formula (I) and their solvates and/or hydrates, having affinity and selectivity for V1b or for both V1b and V1a arginine-vasopressin receptors. The invention also concerns a method for preparing them, intermediate compounds of formula (II) useful for preparing them, pharmaceutical compositions containing them, and their use for preparing medicines.
摘要翻译：本发明涉及式（I）化合物及其溶剂化物和/或水合物，对V1b或V1b和V1a精氨酸 - 加压素受体具有亲和力和选择性。本发明还涉及制备它们的方法，用于制备它们的式（II）的中间体化合物，含有它们的药物组合物及其制备药物的用途。

4. 发明申请

WO0155134A2 NOVEL 1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新型1,3-二氢-2H-吲哚-2-酮衍生物，制备方法和含有它们的药物组合物
公开(公告)号：WO0155134A2
公开(公告)日：2001-08-02
申请号：PCT/FR0100228
申请日：2001-01-24
申请人： SANOFI SYNTHELABO , SCHOENTJES BRUNO , SERRADEIL LE GAL CLAUDINE , WAGNON JEAN
发明人： SCHOENTJES BRUNO , SERRADEIL-LE GAL CLAUDINE , WAGNON JEAN
IPC分类号： A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/08 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/04 , A61P43/00 , C07D413/04
CPC分类号： C07D413/04
摘要： The invention concerns compounds of formula (I), and their solvates and/or hydrates, having affinity and selectivity for V1b receptors or for both V1b and V1a arginine-vasopressin receptors. The invention also concerns their method of preparation, intermediate compounds of formula (II) used for preparing them, pharmaceutical compositions containing them and their use for preparing medicines.
摘要翻译：本发明涉及式（I）化合物及其溶剂合物和/或水合物，对V1b受体或V1b和V1a精氨酸 - 加压素受体具有亲和力和选择性。本发明还涉及它们的制备方法，用于制备它们的式（II）的中间体化合物，含有它们的药物组合物及其制备药物的用途。

5. 发明申请

WO2004009585A2 ACYLOXYPYRROLIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：乙酰吡咯烷酮衍生物，其制备和治疗用途
公开(公告)号：WO2004009585A2
公开(公告)日：2004-01-29
申请号：PCT/FR0302262
申请日：2003-07-17
申请人： SANOFI SYNTHELABO , AULOMBARD ALAIN , GARCIA GEORGES , PRADINES ANTOINE , SERRADEIL-LE GAL CLAUDINE , WAGNON JEAN
发明人： AULOMBARD ALAIN , GARCIA GEORGES , PRADINES ANTOINE , SERRADEIL-LE GAL CLAUDINE , WAGNON JEAN
IPC分类号： A61K31/404 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/10 , A61P13/12 , A61P25/20 , A61P25/22 , A61P25/24 , A61P35/00 , C07D403/04
CPC分类号： C07D403/04
摘要： The invention concerns acyloxypyrrolidine derivatives of general formula (I), wherein: R1 represents a hydrogen atom, a C1-C6 alkyl, a C3-C6 cycloalkyl, a -CH2CH2COOH group or a -NR2R3 group; R2 and R3 each independently represent a hydrogen atom or a C1-C6 alkyl. The invention also concerns a method for preparing said derivatives and their therapeutic use.
摘要翻译：本发明涉及通式（I）的酰氧基吡咯烷衍生物，其中：R1表示氢原子，C1-C6烷基，C3-C6环烷基，-CH2CH2COOH基或-NR2R3基; R2和R3各自独立地表示氢原子或C1-C6烷基。本发明还涉及制备所述衍生物及其治疗用途的方法。

6. 发明申请

WO2007071840A3 COMPOUNDS BASED ON FOUR AROMATIC RINGS, PREPARATION AND USES THEREOF 审中-公开
标题翻译：基于四种芳香环的化合物，其制备和用途
公开(公告)号：WO2007071840A3
公开(公告)日：2007-08-09
申请号：PCT/FR2006002773
申请日：2006-12-18
申请人： CEREP , BOTEZ IULIANA , NICOLAI ERIC , GOURLAOUEN NELLY , DAVID-BASEI CHRISTELLE , BALAVOINE FABRICE , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
发明人： BOTEZ IULIANA , NICOLAI ERIC , GOURLAOUEN NELLY , DAVID-BASEI CHRISTELLE , BALAVOINE FABRICE , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
IPC分类号： C07D471/04 , A61K31/431 , A61K31/4439 , A61P3/00 , A61P9/00 , C07D401/06 , C07D401/14 , C07D403/12 , C07D413/06 , C07D413/12 , C07D417/14
CPC分类号： C07D401/06 , C07D207/335 , C07D209/08 , C07D209/14 , C07D211/46 , C07D231/12 , C07D401/14 , C07D403/06 , C07D405/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/113
摘要： The present invention relates to novel compounds, to the preparation thereof and to uses, in particular therapeutic uses, thereof. It relates more particularly to derived compounds which have at least four aromatic rings, to the preparation thereof and to uses thereof, in particular in the field of human or animal health. These compounds have in particular a certain affinity for neuropeptide Y, NPY, biological receptors, and more particularly for NPY Y1 receptors, present in the central and peripheral nervous systems. The compounds according to the invention are preferably NPY antagonists, and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also relates to pharmaceutical compositions comprising such compounds, to the preparation thereof and to uses thereof, and also to methods of treatment using said compounds.
摘要翻译：本发明涉及新化合物，其制备和用途，特别是其治疗用途。本发明更具体地涉及具有至少四个芳香环的衍生化合物，其制备及其用途，特别是在人类或动物健康领域。这些化合物对神经肽Y，NPY，生物受体特别是对中枢和外周神经系统中存在的NPY Y1受体具有特定的亲和力。根据本发明的化合物优选为NPY拮抗剂，因此可以用于任何涉及NPY的病症的治疗或预防性治疗。本发明还涉及包含此类化合物的药物组合物，其制备方法及其用途，以及使用所述化合物的治疗方法。

7. 发明申请

WO2008087278A3 5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY AS SELECTIVE LIGANDS OF V2 VASOPRESSIN RECEPTORS 审中-公开
标题翻译： 5-烷基-L-吲哚-2-酮衍生物，其制备方法及其在治疗中的应用作为V2 VASOPRESSIN受体的选择性配体
公开(公告)号：WO2008087278A3
公开(公告)日：2008-09-18
申请号：PCT/FR2007002028
申请日：2007-12-10
申请人： SANOFI AVENTIS , FOULON LOIC , ROCHARD PIERRICK , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
发明人： FOULON LOIC , ROCHARD PIERRICK , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
IPC分类号： C07D209/34 , A61K31/404 , C07D401/12 , C07D403/10 , C07D403/12 , C07D487/04
CPC分类号： C07D209/34 , C07D401/12 , C07D403/10 , C07D403/12 , C07D487/04
摘要： The invention relates to compounds of the formula (I) in which: R 0 is (C 1 -C 4 )alkyl, mono or polyfluoro-(C 1 C 4 )alkyl, cyclopropyl or -CH2- cyclopropyl, (C 2 -C 4 )alkenyl or (C 2 -C 4 )alkynyl; R 1 is H, (C 1 -C 5 )alkyl, mono or polyfluoro-(C 1 C 5 )alkyl, hydroxy-(C 2 -C 5 )alkyl, -(CH 2 )m-(C 3 -C 5 )cycloalkyl; Z 1 is H or halogen, (C 1 C 4 )alkyl, mono or polyfluoro-(C- 1 -C 4 )alkyl, (C 1 - C 4 )alkoxy, mono or PoIy[IuOrO-(C 1 -C 4 )Alkoxy, cyclopropyl or -CH 2 -yclopropyle, optionally substituted; Z 2 is a halogen atom or a T 1 W group, in which T 1 is a -(CH 2 ) n - group, and W is one or more of H, (C 1 - C 4 )alkyl, mono or polyfluoro-(C- 1 -C 4 )alkyl or cyclopropyl optionally substituted, or W is -C(O)OR 19 , or W is -C(O)NR 6 R 7 , or W is a -NR 8 C(O)R 9 group, or W is -NR 10 R 11 , or W is a -OR 12 group; R 4 is (CrC4)alkyl, mono or polyfluoro-(C 1 C 4 )alkyl, OH, (C 1 - C 4 )alkoxy, (C2-C4) alkenyl, nitro, COORCl, benzyloxy, or R 4 is - C(O)NR 13 R 14 , or R 4 is -NR 15 R 16 , or R 4 is -NR 17 C(O)R 18 ; R 3 and R 5 are H or halogen, (CrC4)alkyl, mono or polyfluoro-(CrC4)alkyl, (C 1 - C 4 )alkoxy or mono or polyfluoro-(C 1 C 4 )alkoxy; m = 0, 1 or 2; n = 0 or 1; said compounds being in their base, hydrate or solvate state, in the form of cis/trans isomers, or mixtures thereof. The invention also relates to a method for the preparation of the compounds of the formula (I) and to the use thereof in therapy.
摘要翻译：本发明涉及式（I）的化合物，其中：R 0是（C 1 -C 4 -C 4）烷基，单或多氟 - （C 1 -C 4）烷基，环丙基或-CH 2 - 环丙基，（C 2 -C 4）烷基，（C 1 -C 4））烯基或（C 1 -C 2 -C 4）炔基; R 1是H，（C 1 -C 5）烷基，单或多氟 - （C 1 -C 1）烷基，烷基，羟基 - （C 2 -C 5 -C 5）烷基， - （CH 2 CH 2）m - （C _{3 -C _{5 ）环烷基; Z 1是H或卤素，（C 1 -C 4）烷基，单或多氟 - （C 1 -C 12）（C 1 -C 4）烷基，（C 1 -C 4）烷基，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，环丙基或-CH 2 - 环丙基，任选取代的; Z 2是卤素原子或T 1 W基团，其中T 1是 - （CH 2/2）），W是H，（C 1 -C 4）烷基，单或多氟（（C 1 -C 4）任选取代的C 1 -C 6烷基或环丙基，或W是-C（O）OR 19，或W是-C （O）NR 6 R 7或W是-NR 8 C（O）R 9基团，或W是-NR 10 R 11，或W是-OR 12基团; R 4是（C 1 -C 4）烷基，单或多氟 - （C 1 -C 4）C 4烷基，OH，（C 1 H 4）（C 2 -C 4）烷基，（C 2 -C 4）烯基，硝基，COORCl，苄氧基或R 4是-C（O）NR 13 R 14或R 4是-NR 15 R 16，或R 14， 4是-NR 17 C（O）R 18; R 3和R 5是H或卤素，（C 1 -C 4）烷基，单或多氟 - （C 1 -C 4）烷基，（C 1 -C 4）（C 1 -C 4）烷氧基或单或多氟 - （C 1 -C 4）烷氧基; m = 0,1或2; n = 0或1; 所述化合物是其顺式/反式异构体形式的其碱，水合物或溶剂合物状态，或其混合物。本发明还涉及制备式（I）化合物的方法及其在治疗中的用途。}}

8. 发明申请

WO2007088276A3 SULFONAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF 审中-公开
标题翻译：磺酰胺衍生物及其制备和治疗应用
公开(公告)号：WO2007088276A3
公开(公告)日：2007-10-25
申请号：PCT/FR2007000182
申请日：2007-02-01
申请人： SANOFI AVENTIS , COURTEMANCHE GILLES , DESPEYROUX PIERRE , FONTAINE EVELYNE , ROCHARD PIERRICK , SERRADEIL-LE GAL CLAUDINE , VON ROEDERN ERICH
发明人： COURTEMANCHE GILLES , DESPEYROUX PIERRE , FONTAINE EVELYNE , ROCHARD PIERRICK , SERRADEIL-LE GAL CLAUDINE , VON ROEDERN ERICH
IPC分类号： C07C311/21 , A61K31/18 , C07C311/29
CPC分类号： C07C311/29 , C07B2200/07 , C07D295/13
摘要： The invention concerns sulfonamide derivatives of general formula (I), wherein: Ar 1 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl group; T represents a -(CH 2 ) n or a group (A); Ar 2 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl group; Ar 3 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl; R represents a hydrogen or a (C 1 -C 4 ) alkyl; R' represents an optionally substituted (C 1 -C 4 ) alkyl; a carboxylic acid, a (C 1 -C 4 ) carboxylate, an optionally substituted carboxamide; in base, acid addition salt, hydrate or solvate form, or in enantiomeric, diastereoisomeric, rotameric, atropoisomeric forms or mixtures thereof. The invention also concerns the preparation method as well as the therapeutic use of the compounds of formula (I).
摘要翻译：本发明涉及通式（I）的磺酰胺衍生物，其中：Ar 1表示任选被一个或几个基团取代的芳基，任选取代的杂环基; T表示一个 - （CH _{）_{n 或一个组（A）; Ar 2表示任选被一个或几个基团取代的芳基，任选取代的杂环基; Ar 3表示任选被一个或几个基团取代的芳基，任选取代的杂环基; R代表氢或（C 1 -C 4）烷基; R'表示任选取代的（C 1 -C 4）烷基; 羧酸，（C 1 -C 4）羧酸酯，任选取代的羧酰胺; 碱加成盐，水合物或溶剂化物形式，或以对映异构体，非对映异构体，旋转异构体，阻转异构体形式或其混合物存在。本发明还涉及式（I）化合物的制备方法以及治疗用途。}}

9. 发明申请

WO2006108965A2 NPY ANTAGONISTS, PREPARATION AND USE 审中-公开
标题翻译： NPY拮抗剂，制备和使用
公开(公告)号：WO2006108965A2
公开(公告)日：2006-10-19
申请号：PCT/FR2006000829
申请日：2006-04-14
申请人： CEREP , BOTEZ IULIANA , DAVID-BASEI CHRISTELLE , GOURLAOUEN NELLY , NICOLAI ERIC , BALAVOINE FABRICE , VALETTE GERARD , SERRADEIL-LE GAL CLAUDINE
发明人： BOTEZ IULIANA , DAVID-BASEI CHRISTELLE , GOURLAOUEN NELLY , NICOLAI ERIC , BALAVOINE FABRICE , VALETTE GERARD , SERRADEIL-LE GAL CLAUDINE
CPC分类号： C07D295/088 , C07D211/42 , C07D211/46 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D453/06 , C07D471/08
摘要： The invention relates to novel compounds, to the preparation and use thereof, in particular therapeutic. Said invention particularly relates to derived compounds comprising at least two aromatic cycles, to the preparation and use thereof, mainly for human and animal health care. Said compounds exhibit an affinity to biological receptors Y and NPY of a neuropeptide Y which are present in the central and peripheral nervous systems. The inventive compounds are preferably embodied in the form NPY antagonists, and more particularly in the form of NPY Y1 subtype antagonists and, whereby are usable in therapeutic or prophylactic treatment all NPY involving disorders. Pharmaceutical compositions comprising said compounds, the preparation and the use thereof and treating methods using said compounds are also disclosed.
摘要翻译：本发明涉及新化合物，其制备和用途，特别是治疗剂。所述发明特别涉及包含至少两个芳族循环的衍生化合物，其制备和用途主要用于人和动物保健。所述化合物对存在于中枢和外周神经系统中的神经肽Y的生物受体Y和NPY表现出亲和力。本发明化合物优选以NPY拮抗剂形式，更具体地以NPY Y1亚型拮抗剂的形式实施，由此可用于治疗或预防性治疗所有涉及疾病的NPY。还公开了包含所述化合物的药物组合物，其制备及其用途和使用所述化合物的治疗方法。

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