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1.发明申请NOVEL 3-AMINOALKYL-1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 有权新型3-氨基-1,3-二氢-2H-吲哚-2-酮衍生物，其制备方法及其治疗方法公开(公告)号：US20110059955A1
公开(公告)日：2011-03-10
申请号：US12858976
申请日：2010-08-18
IPC分类号： A61K31/551 , C07D401/06 , A61K31/454 , C07D403/02 , A61K31/404 , A61K31/496 , C07D209/04 , C07D413/06 , A61K31/5377 , C07D471/08 , A61P9/12 , A61P9/00 , A61P11/00 , A61P25/00 , A61P35/00 , A61P1/00
CPC分类号： C07D209/34
摘要： The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application.The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification.These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.
摘要翻译： 本发明涉及新的3-氨基烷基-1,3-二氢-2H-吲哚-2-酮衍生物及其制备方法及其治疗应用。 本发明的化合物对应于式（I）：其中变量如说明书中所述。 这些化合物对人类精氨酸 - 加压素（AVP）V1a受体表现出强烈的亲和力和高选择性，另外一些化合物对AVP V1b受体也表现出强烈的亲合力。
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2.发明申请5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY 审中-公开5-烷基-2-吲哚-2-酮衍生物，其制备方法及其在治疗中的应用公开(公告)号：US20100069384A1
公开(公告)日：2010-03-18
申请号：US12483782
申请日：2009-06-12
IPC分类号： A61K31/5377 , A61K31/4439 , A61K31/404 , C07D413/10 , C07D401/10 , C07D209/34 , A61P9/04 , A61P25/22 , A61P25/24 , A61P3/10
CPC分类号： C07D209/34 , C07D401/12 , C07D403/10 , C07D403/12 , C07D487/04
摘要： The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.
摘要翻译： 本发明涉及5-烷氧基 - 二氢吲哚-2-酮的衍生物，其制备方法及其治疗应用。 这些新型衍生物对加压素（“V2受体”）的V2受体具有亲和性和选择性，因此可构成药物组合物的活性成分。
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3.发明申请Novel Indolin-2-one Derivatives, Their Preparation and the Pharmaceutical Compositions Comprising Them 审中-公开新型二氢吲哚-2-酮衍生物及其制备方法及药物组合物公开(公告)号：US20070203184A1
公开(公告)日：2007-08-30
申请号：US11744003
申请日：2007-05-03
IPC分类号： A61K31/4015 , A61K31/454
CPC分类号： C07D401/04 , A61K31/4015 , A61K31/454 , C07D209/34 , C07D209/38 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12
摘要： The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.
摘要翻译： 本发明涉及新颖的式（I）的二氢吲哚-2-酮衍生物：制备方法和包含它们的药物组合物。 这些化合物对催产素受体具有亲和力。
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![1,3-DIHYDRO-2H-PYRROLO[3,2-b]PYRIDIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USES THEREOF](/abs-image/US/2011/03/24/US20110071160A1/abs.jpg.150x150.jpg)
4.发明申请1,3-DIHYDRO-2H-PYRROLO[3,2-b]PYRIDIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USES THEREOF 有权1,3-二氢-2H-吡喃并[3,2-b]吡啶-2-酮衍生物，其制备方法及其治疗用途公开(公告)号：US20110071160A1
公开(公告)日：2011-03-24
申请号：US12905287
申请日：2010-10-15
IPC分类号： A61K31/496 , C07D471/04 , A61K31/437 , A61P15/06 , A61P15/00 , A61P15/08 , A61P13/06 , A61P9/12 , A61P25/00 , A61P3/10
CPC分类号： C07D471/04
摘要： The subject matter of the present invention are compounds corresponding to formula (I): in which: X is an unsubstituted or substituted divalent (C1-C5)alkylene radical; R1 is an —NR8R9 group; or an unsubstituted or substituted piperidin-3-yl or piperidin-4-yl radical; R2 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R3 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group; and R5 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group.
摘要翻译： 本发明的主题是对应于式（I）的化合物：其中：X是未取代或取代的二价（C1-C5）亚烷基; R1是-NR8R9基团; 或未取代或取代的哌啶-3-基或哌啶-4-基; R2是氢原子，卤素原子，Alk基团或OAlk基团; R3是氢原子，卤素原子，Alk基团或OAlk基团; R4是氢原子，卤素原子，Alk基团，羟基或OAlk基团; R5为氢原子，卤原子，Alk基，羟基或OAlk基。
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5.发明申请公开(公告)号：US20090054439A1
公开(公告)日：2009-02-26
申请号：US12183487
申请日：2008-07-31
申请人： Gilles COURTEMANCHE , Pierre DESPEYROUX , Evelyne FONTAINE , Pierrick ROCHARD , Claudine SERRADEIL-LE GAL , Erich Von Roedern
发明人： Gilles COURTEMANCHE , Pierre DESPEYROUX , Evelyne FONTAINE , Pierrick ROCHARD , Claudine SERRADEIL-LE GAL , Erich Von Roedern
IPC分类号： A61K31/5375 , C07C311/29 , C07D265/30 , A61K31/18
CPC分类号： C07C311/29 , C07B2200/07 , C07D295/13
摘要： The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R, R′ and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.
摘要翻译： 本发明涉及式（I）化合物：其中Ar1，Ar2，Ar3，R，R'和T如本文所定义，其制备，药物组合物和用作食欲肽2受体拮抗剂。
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6.发明申请3-SPIROINDOLIN-2-ONE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF 审中-公开3-SPIROINDOLIN-2-ONE衍生物，其制备和治疗用途公开(公告)号：US20070191367A1
公开(公告)日：2007-08-16
申请号：US11682988
申请日：2007-03-07
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D209/96
摘要： The subject of the present invention is a compound of formula (I): in the base, hydrate or solvate state, in the form of cis/trans isomers or of mixtures thereof, preparation and therapeutic use thereof.
摘要翻译： 本发明的主题是式（I）的化合物：在碱，水合物或溶剂化状态下，以顺式/反式异构体或其混合物的形式，其制备和治疗用途。
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公开(公告)号：US20090275580A1
公开(公告)日：2009-11-05
申请号：US12504278
申请日：2009-07-16
IPC分类号： A61K31/5377 , C07D413/12 , A61P25/00 , A61P9/00 , A61P27/02
CPC分类号： C07D209/96
摘要： The subject of the present invention is a compound of formula (I): in the base, hydrate or solvate state, in the form of cis/trans isomers or of mixtures thereof, preparation and therapeutic use thereof.
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公开(公告)号：US20070191359A1
公开(公告)日：2007-08-16
申请号：US11682991
申请日：2007-03-07
IPC分类号： A61K31/5355 , C07D413/02
CPC分类号： C07D209/96
摘要： The subject of the present invention is a compound of formula (I): in the base, hydrate or solvate state, in the form of cis/trans isomers or of mixtures thereof, preparation and therapeutic use thereof.
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9.发明申请公开(公告)号：US20070185136A1
公开(公告)日：2007-08-09
申请号：US11670586
申请日：2007-02-02
申请人： Gilles COURTEMANCHE , Pierre DESPEYROUX , Evelyne FONTAINE , Pierrick ROCHARD , Claudine SERRADEIL-LE GAL
发明人： Gilles COURTEMANCHE , Pierre DESPEYROUX , Evelyne FONTAINE , Pierrick ROCHARD , Claudine SERRADEIL-LE GAL
IPC分类号： A61K31/506 , A61K31/4709 , A61K31/4433 , A61K31/427 , A61K31/381
CPC分类号： C07D213/42 , C07C311/21 , C07C311/29 , C07C311/44 , C07D217/06 , C07D233/64 , C07D257/04 , C07D271/06 , C07D277/28 , C07D317/62 , C07D319/18 , C07D333/20
摘要： Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.
摘要翻译： 公开了具有本文所定义的通式（I）的化合物，其制备方法及其用于预防或治疗涉及食欲肽2受体相关功能障碍的任何疾病，例如肥胖，食欲或味觉障碍，包括恶病质， 厌食和贪食症，糖尿病，代谢综合征，呕吐和恶心，抑郁和焦虑，瘾，情绪和行为障碍，精神分裂症，睡眠障碍，不宁腿综合征，记忆学习障碍，性和心理性功能障碍，疼痛，内脏或神经性疼痛，痛觉过敏 ，异常性疼痛，消化系统疾病，肠易激综合征，神经元脱色，缺血性或出血性发作，库欣氏病，吉兰巴利综合征，强直性营养不良，尿失禁，甲状腺功能亢进，垂体功能障碍，高血压或低血压。
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