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1.发明授权Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use 失效苯磺酰基-1,3-二氢-2h-吲哚-2-酮衍生物，其制备及其治疗用途公开(公告)号：US07119086B2
公开(公告)日：2006-10-10
申请号：US10484370
申请日：2002-07-15
申请人： Alain Di Malta , Georges Garcia , Richard Roux , Bruno Schoentjes , Claudine Serradeil-Le Gal , Bernard Tonnerre , Jean Wagnon
发明人： Alain Di Malta , Georges Garcia , Richard Roux , Bruno Schoentjes , Claudine Serradeil-Le Gal , Bernard Tonnerre , Jean Wagnon
IPC分类号： A61K31/496 , A61K31/551 , C07D401/14 , C07D417/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors.The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要翻译： 本发明涉及下式的化合物：以及其与矿物或有机酸及其盐的溶剂合物和/或水合物的盐，对精氨酸 - 加压素V 1b受体具有亲和力和选择性， /或对于可待因受体，以及对于某些化合物，对V 1a受体的亲和力。 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及其用于制备药用产品的用途。
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2.发明授权1,3-dihydro-2H-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them 有权1,3-二氢-2H-吲哚-2-酮衍生物，其制备方法和含有它们的药物组合物公开(公告)号：US07297692B2
公开(公告)日：2007-11-20
申请号：US11462062
申请日：2006-08-03
IPC分类号： A61K31/5377 , A61K31/404 , C07D209/04 , C07D403/04
CPC分类号： C07D403/04 , A61K31/405 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要翻译： 本发明涉及下式的化合物及其与矿物或有机酸及其溶剂化物和/或水合物的可能的盐，其对V 1b受体具有亲和力和选择性， 精氨酸 - 加压素的V 1b 1b和V 1a 1a受体都是精氨酸 - 加压素的受体。 本发明还涉及制备它们的方法，可用于制备它们的中间式式（II）化合物，含有它们的药物组合物及其用于制备药用产品的用途。
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3.发明申请NOVEL 1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权新型1,3-二氢-2H-吲哚-2-酮衍生物，其制备方法和含有它们的药物组合物公开(公告)号：US20070004703A1
公开(公告)日：2007-01-04
申请号：US11462062
申请日：2006-08-03
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/405
CPC分类号： C07D403/04 , A61K31/405 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要翻译： 本发明涉及下式的化合物及其与矿物或有机酸及其溶剂化物和/或水合物的可能的盐，其对V 1b受体具有亲和力和选择性， 精氨酸 - 加压素的V 1b 1b和V 1a 1a受体都是精氨酸 - 加压素的受体。 本发明还涉及制备它们的方法，可用于制备它们的中间式式（II）化合物，含有它们的药物组合物及其用于制备药用产品的用途。
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4.发明授权1,3-dihydro-2h-indol-2-one derivatives and their use as ligands for V1b and V1a arginine-vasopressin receptors 有权1,3-二氢-2h吲哚-2-酮衍生物及其作为V1b和V1a精氨酸 - 加压素受体配体的用途公开(公告)号：US06730695B2
公开(公告)日：2004-05-04
申请号：US10182048
申请日：2002-07-24
IPC分类号： A61K31404
CPC分类号： C07D403/04 , A61K31/405 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要翻译： 本发明涉及下式的化合物及其与矿物或有机酸及其溶剂合物和/或水合物的可能盐，其对V1b受体或对于精氨酸的V1b和V1a受体具有亲和性和选择性 - 加压素。本发明还涉及制备它们的方法，可用于制备它们的中间体式（II）化合物，含有它们的药物组合物及其用于制备药用产品的用途。
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5.发明授权1,3-dihydro-2H-indol-2-one derivatives, preparation method and pharmaceutical composition containing them 失效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：US06624164B2
公开(公告)日：2003-09-23
申请号：US10182638
申请日：2002-11-25
IPC分类号： A61K315377
CPC分类号： C07D413/04
摘要： The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting affinity for the arginine-vasopressin V1b receptors or for both V1b and V1a receptors. The invention also relates to their process of preparation, to the intermediate compounds of formula (II) of use for their preparation, to the pharmaceutical compositions comprising them and to their use for the preparation of medicaments.
摘要翻译： 本发明涉及下式的化合物及其对精氨酸 - 加压素V1b受体或V1b和V1a受体表现出亲和力的溶剂合物和/或水合物。本发明还涉及其制备方法，其中式（II ）用于制备它们的药物组合物及其用于制备药物的用途。
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6.发明授权1,3-dihydro-2h-indol-2-one, preparation method and pharmaceutical compositions containing same 失效1,3-二氢-2H-吲哚-2-酮，制备方法和含有它们的药物组合物公开(公告)号：US06596732B2
公开(公告)日：2003-07-22
申请号：US10203730
申请日：2002-08-12
IPC分类号： C07D40104
CPC分类号： C07D401/04 , C07D209/42 , C07D403/04
摘要： The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting an affinity and a selectivity for arginine-vasopressin V1b receptors or for both V1b and V1a receptors.
摘要翻译： 本发明涉及下式的化合物及其对精氨酸 - 加压素V1b受体或V1b和V1a受体表现出亲和力和选择性的溶剂合物和/或水合物。
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7.发明申请Acyloxypyrrolidine derivatives, preparation thereof and application thereof in therapeutic 失效环氧嘧啶衍生物，其制备方法及其在治疗中的应用公开(公告)号：US20050192335A1
公开(公告)日：2005-09-01
申请号：US11038384
申请日：2005-01-19
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 , A61K31/405 , C07D43/02
CPC分类号： C07D403/04
摘要： The invention relates to acyloxypyrrolidine derivatives of general formula (I): in which: R1 represents a hydrogen atom, a (C1-C6)alkyl, a (C3-C6)cycloalkyl, a group —CH2CH2COOH or a group —NR2R3; R2 and R3 each represent, independently, a hydrogen atom or a (C1-C6)alkyl. Also disclosed and claimed are the method of preparation of the compounds of the invention and their application in therapeutics.
摘要翻译： 本发明涉及通式（I）的酰氧基吡咯烷衍生物：其中：R 1表示氢原子，（C 1 -C 6 -C 6亚烷基） 烷基，（C 3 -C 6 -C 6）环烷基，基团-CH 2 CH 2 COOH 或基团-NR 2 R 3; R 2和R 3各自独立地表示氢原子或（C 1 -C 6 -C 6）烷基， 烷基。 还公开并要求保护的是本发明化合物的制备方法及其在治疗中的应用。
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8.发明申请Novel 1,3-dihydro-2H-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them 失效新的1,3-二氢-2H-吲哚-2-酮衍生物，其制备方法和含有它们的药物组合物公开(公告)号：US20050176770A1
公开(公告)日：2005-08-11
申请号：US11064896
申请日：2005-02-24
IPC分类号： A61K31/404 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P5/10 , A61P5/24 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/06 , A61P19/02 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06 , A61P27/12 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/04 , C07D401/04 , C07D403/04 , C07D405/14 , A61K31/454 , C07D43/02
CPC分类号： C07D401/04 , C07D403/04 , C07D405/14
摘要： The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the V1b receptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要翻译： 本发明涉及以下化合物：并且对V 1 B 1 N 2受体具有亲和力和选择性，并且对V 1b和V N 2 >精氨酸 - 加压素受体1a> 1a。 本发明还涉及制备它们的方法，可用于制备它们的式（II）中间体化合物，含有它们的药物组合物及其用于制备药用产品的用途。
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9.发明授权Acyloxypyrrolidine derivatives, preparation thereof and application thereof in therapeutic 失效环氧嘧啶衍生物，其制备方法及其在治疗中的应用公开(公告)号：US07202267B2
公开(公告)日：2007-04-10
申请号：US11038384
申请日：2005-01-19
IPC分类号： A61K31/404 , C07D403/04
CPC分类号： C07D403/04
摘要： The invention relates to acyloxypyrrolidine derivatives of general formula (I): in which: R1 represents a hydrogen atom, a (C1–C6)alkyl, a (C3–C6)cycloalkyl, a group —CH2CH2COOH or a group —NR2R3; R2 and R3 each represent, independently, a hydrogen atom or a (C1–C6)alkyl. Also disclosed and claimed are the method of preparation of the compounds of the invention and their application in therapeutics.
摘要翻译： 本发明涉及通式（I）的酰氧基吡咯烷衍生物：
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10.发明授权1,3-dihydro-2H-indol-2-one derivatives, method for preparing same and pharmaceutical compositions containing them 失效1,3-二氢-2H-吲哚-2-酮衍生物，其制备方法和含有它们的药物组合物公开(公告)号：US06864277B2
公开(公告)日：2005-03-08
申请号：US10311435
申请日：2001-06-19
IPC分类号： A61K31/404 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P5/10 , A61P5/24 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/06 , A61P19/02 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06 , A61P27/12 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/04 , C07D401/04 , C07D403/04 , C07D405/14 , A61K31/4015
CPC分类号： C07D401/04 , C07D403/04 , C07D405/14
摘要： The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the Vreceptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要翻译： 本发明涉及式VI化合物及其溶剂合物和/或其水合物，对VIb受体或精氨酸加压素的V1b和V1a受体均具有亲和性和选择性。本发明还涉及其制备方法， 可用于制备它们的式（II）的中间体化合物，含有它们的药物组合物及其用于制备药用产品的用途。
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