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1. 发明授权

US08362067B2 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译： 3-氨基烷基-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：US08362067B2
公开(公告)日：2013-01-29
申请号：US12858976
申请日：2010-08-18
申请人： Loïc Foulon , Laurent Goullieux , Brigitte Pouzet , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Loïc Foulon , Laurent Goullieux , Brigitte Pouzet , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： C07D209/46 , C07D403/00 , A01N43/38 , A61K31/40
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。

2. 发明授权

US06673790B1 Indolin-2-one derivatives, preparation and their use as ocytocin receptor ligands 失效
标题翻译：二氢吲哚-2-酮衍生物，制备及其作为细胞毒素受体配体的用途
公开(公告)号：US06673790B1
公开(公告)日：2004-01-06
申请号：US10240483
申请日：2002-10-02
申请人： Loïc Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gérard Valette
发明人： Loïc Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gérard Valette
IPC分类号： A61P510
CPC分类号： C07D401/04 , 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：本发明涉及式（I）的新的二氢吲哚-2-酮衍生物：制备物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。

3. 发明授权

US07488743B2 Indolin-2-one pyridine derivatives, preparation and therapeutic use thereof 有权
标题翻译：二氢吲哚-2-酮吡啶衍生物，其制备和治疗用途
公开(公告)号：US07488743B2
公开(公告)日：2009-02-10
申请号：US11686977
申请日：2007-03-16
申请人： Loïc Foulon , Claudine Serradeil-Le Gal , Gérard Valette
发明人： Loïc Foulon , Claudine Serradeil-Le Gal , Gérard Valette
IPC分类号： A61K31/4439 , C07D401/14
CPC分类号： C07D401/12
摘要： The disclosure concerns indolin-2-one pyridine compounds of general formula (I): wherein R0, R1, R2, R3, R4, Z and B have the meanings given in the description, and pharmaceutically acceptable salts thereof; and also pharmaceutical compositions comprising, processes for making and methods of using said compounds.
摘要翻译：本发明涉及通式（I）的二氢吲哚-2-酮吡啶化合物：其中R 0，R 1，R 2，R 3，R 4，Z和B具有本说明书中给出的含义及其药学上可接受的盐; 以及包含其制备方法和使用所述化合物的方法的药物组合物。

4. 发明申请

US20070185166A1 Indolin-2-one Pyridine Derivatives, Preparation And Therapeutic Use Thereof 有权
标题翻译：二氢吲哚-2-酮吡啶衍生物，其制备和治疗用途
公开(公告)号：US20070185166A1
公开(公告)日：2007-08-09
申请号：US11686977
申请日：2007-03-16
申请人： Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： A61K31/4439 , C07D403/02
CPC分类号： C07D401/12
摘要： The disclosure concerns indolin-2-one pyridine compounds of general formula (I): wherein R0, R1, R2, R3, R4, Z and B have the meanings given in the description, and pharmaceutically acceptable salts thereof; and also pharmaceutical compositions comprising, processes for making and methods of using said compounds.
摘要翻译：本公开涉及通式（I）的二氢吲哚-2-酮吡啶化合物：其中R 0，R 1，R 2，R 2， R 3，R 4，Z和B具有说明书中给出的含义及其药学上可接受的盐; 以及包含其制备方法和使用所述化合物的方法的药物组合物。

5. 发明授权

US6090818A Indolin-2-one derivatives, method for preparing them and pharmaceutical compositions containing them 有权
标题翻译：二氢吲哚-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：US6090818A
公开(公告)日：2000-07-18
申请号：US331007
申请日：1999-06-14
申请人： Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： C07D491/107 , A61K31/404 , A61K31/407 , A61K31/454 , A61K31/5377 , A61P1/16 , A61P7/00 , A61P9/00 , A61P25/00 , A61P27/02 , A61P43/00 , C07D209/96 , C07D401/12 , C07D491/10 , C07D213/04 , A61K31/395 , C07D209/10
CPC分类号： C07D401/12 , C07D209/96 , C07D491/10
摘要： The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them. These compounds have an excellent affinity for vasopressin and/or oxytocin ##STR1##
摘要翻译： PCT No.PCT / FR97 / 02270 Sec。 371日期1999年6月14日第 102（e）1999年6月14日PCT 1997年12月11日PCT PCT。第WO98 / 25901号公报日期1998年6月18日本发明涉及式（I）化合物，其制备方法和含有它们的药物组合物。这些化合物对加压素和/或催产素具有极好的亲和力

6. 发明授权

US5994350A 3-spiro-indolin-2-one derivatives as vasopressin and/or oxytocin receptor ligands 失效
标题翻译： 3-螺 - 二氢吲哚-2-酮衍生物作为加压素和/或催产素受体配体
公开(公告)号：US5994350A
公开(公告)日：1999-11-30
申请号：US51900
申请日：1998-04-17
申请人： Loic Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Loic Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： C07D209/54 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/541 , A61K45/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/04 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P25/34 , A61P27/02 , A61P27/06 , A61P27/12 , A61P35/00 , A61P43/00 , C07D209/96 , C07D401/12 , C07D403/12 , C07D413/12 , C07D209/06
CPC分类号： C07D401/12 , C07D209/96 , C07D403/12
摘要： The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.
摘要翻译： PCT No.PCT / FR96 / 01666 Sec。 371日期：1998年4月17日 102（e）日期1998年4月17日PCT 1996年10月24日PCT公布。第WO97 / 15556号公报日期1997年5月1日本发明的主题是下式的二氢吲哚-2-酮衍生物：其中：W表示-CH 2 - 或-SO 2 - 基; Cy形式与其键合的碳一起是非芳族的，饱和的或不饱和的C 3 -C 12烃环，其任选地被一个或多个（C 1 -C 7）烷基缩合或取代，所述基团取代相同的碳原子一次或多次，或由C 3 -C 6螺环烷基取代; T表示任选地被（C 3 -C 6）亚环烷基中断的（C 1 -C 4）亚烷基，所述亚烷基任选地被（C 1 -C 3）烷基在同一个碳原子上被一次或多次取代; 或者T表示直接键; Z特别表示氨基; R 1和R 2以及R 3和R 4是氢或取代基，例如卤素，烷基等。

7. 发明申请

US20090233910A1 Npy antagonists, preparation and uses 审中-公开
标题翻译： Npy拮抗剂，制剂和用途
公开(公告)号：US20090233910A1
公开(公告)日：2009-09-17
申请号：US11918470
申请日：2006-04-14
申请人： Iuliana Botez , Christelle David-Basei , Nelly Gourlaouen , Eric Nicolai , Fabrice Balavoine , Gerard Valette , Claudine Serradeil-Le Gal
发明人： Iuliana Botez , Christelle David-Basei , Nelly Gourlaouen , Eric Nicolai , Fabrice Balavoine , Gerard Valette , Claudine Serradeil-Le Gal
IPC分类号： A61K31/551 , C07D243/08 , A61P25/02
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 present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
摘要翻译：本发明涉及新化合物，其制备及其用途，特别是治疗用途。更具体地说，它涉及具有至少两个芳族周期的衍生化合物，它们的制备及其用途，特别是在人或动物健康领域。这些化合物对存在于中枢和周围神经系统中的神经肽Y，NPY的生物受体具有亲和力。本发明的化合物优选为NPY拮抗剂，更优选为亚型NPY Y1的拮抗剂，因此可用于治疗或预防性治疗涉及NPY的任何疾病。本发明还涉及含有所述化合物的药物组合物，其制备及其用途，以及使用所述化合物的治疗方法。

8. 发明授权

US08324214B2 1,3-dihydro-2H-pyrrolo[3,2-bpyridin-2-one derivatives, preparation thereof and therapeutic uses thereof 有权
标题翻译： 1,3-二氢-2H-吡咯并[3,2-b]吡啶-2-酮衍生物，其制备及其治疗用途
公开(公告)号：US08324214B2
公开(公告)日：2012-12-04
申请号：US12905287
申请日：2010-10-15
申请人： Cedric Couturier , Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Cedric Couturier , Loic Foulon , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： A61K31/496 , A61K31/437 , C07D471/04 , 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; RI 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; RI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。

9. 发明授权

US5506258A Compounds bearing sulphamoyl and amidino radicals, their preparation process and pharmaceutical compositions containing them 失效
标题翻译：带有氨磺酰基和脒基的化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5506258A
公开(公告)日：1996-04-09
申请号：US195281
申请日：1994-02-14
申请人： Bernard Christophe , Loic Foulon , Alain Pellet , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Bernard Christophe , Loic Foulon , Alain Pellet , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： A61K31/16 , A61K31/155 , A61K31/18 , A61K38/00 , A61P9/00 , A61P25/00 , C07C311/18 , C07D215/36 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/078 , A61K31/40 , C07D295/192
CPC分类号： C07K5/06078 , C07K5/06139 , A61K38/00
摘要： The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted;Ar.sub.2 represents a phenyl or thienyl optionally substituted;R.sub.1, R.sub.2 and R'.sub.2 are independently of each other, H or (C.sub.1 -C.sub.4)alkyl;R.sub.1 represents nothing and N is attached to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond; or R.sub.1 or R.sub.2 is attached to Ar.sub.2 and represents a (C.sub.1 -C.sub.3)alkylene;R.sub.3 and R.sub.4, which are identical or different, represent H, (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached, a (C.sub.5 -C.sub.7) saturated heterocycle selected from pyrrolidine, piperidine and hexahydroazepine;Z.sub.1 represents a (C.sub.1 -C.sub.12)alkylene, optionally interrupted or extended by a (C.sub.5 -C.sub.7)cycloalkyl or phenyl;Q.sub.1 represents methyl, amino, alkoxycarbonylamino, alkylamino, dialkylamino, a (C.sub.5 -C.sub.7) saturated heterocyclic amino group, amidino, alkylamidino, guanidino, alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy, alkoxy, (C.sub.2 -C.sub.8)alkoxycarbonyl, amino(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkylamino or carbamoyl, or phenyl optionally substituted;Q.sub.2 represents H or alkyl;Q.sub.3 represents H or (C.sub.1 -C.sub.4)alkyl;or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent a (C.sub.2) or (C.sub.3)alkylene, whereas Z.sub.1 represents nothing, in the form of pure enantiomers or mixtures thereof in any proportions, as well as their salts with acids.These compounds have an affinity for the biological receptors of neuropeptides Y (NPY), which are present in the central and peripheral nervous system.
摘要翻译：本发明的主题是其中Ar 1表示任选取代的萘基，苯基，喹啉基或异喹啉的式I化合物（I） Ar2表示任选取代的苯基或噻吩基; R 1，R 2和R'2彼此独立地为H或（C 1 -C 4）烷基; R1不表示，N与Ar2连接，任选地R 2和R'2形成双键; 或者R 1或R 2与Ar 2相连，表示（C1-C3）亚烷基; R3和R4相同或不同，代表H，（C1-C4）烷基或与其连接的氮原子一起形成选自吡咯烷，哌啶和六氢氮杂的（C5-C7）饱和杂环; Z1表示（C 1 -C 12）亚烷基，任选地被（C 5 -C 7）环烷基或苯基中断或延伸; Q1代表甲基，氨基，烷氧基羰基氨基，烷基氨基，二烷基氨基，（C5-C7）饱和杂环氨基，脒基，烷基脒基，胍基，烷基胍基，吡啶基，咪唑基，嘧啶基，吲哚基，羟基，烷氧基，（C2-C8）烷氧基羰基，氨基（C 1 -C 4）烷基-N-（C 1 -C 4）烷基氨基或氨基甲酰基或任选取代的苯基; Q2表示H或烷基; Q3表示H或（C1-C4）烷基; 或Q 1和Q 3连接以形成杂环并且一起表示（C 2）或（C 3）亚烷基，而Z 1不以任何比例的纯对映异构体或其混合物的形式以及它们与酸的盐形式表示。这些化合物对存在于中枢和外周神经系统中的神经肽Y（NPY）的生物受体具有亲和力。

10. 发明授权

US6046341A 3-spiro-indolin-2-one derivatives 有权
标题翻译： 3-螺 - 二氢吲哚-2-酮衍生物
公开(公告)号：US6046341A
公开(公告)日：2000-04-04
申请号：US417190
申请日：1999-10-12
申请人： Loic Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gerard Valette
发明人： Loic Foulon , Georges Garcia , Claudine Serradeil-Le Gal , Gerard Valette
IPC分类号： C07D209/54 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/541 , A61K45/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/04 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P25/34 , A61P27/02 , A61P27/06 , A61P27/12 , A61P35/00 , A61P43/00 , C07D209/96 , C07D401/12 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D209/96 , C07D403/12
摘要： The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.
摘要翻译：本发明的主题是下式的二氢吲哚-2-酮衍生物：其中：W表示-CH 2 - 或-SO 2 - 基; Cy形式与其键合的碳一起是非芳族的，饱和的或不饱和的C 3 -C 12烃环，其任选地被一个或多个（C 1 -C 7）烷基缩合或取代，所述基团取代相同的碳原子一次或多次，或由C 3 -C 6螺环烷基取代; T表示任选地被（C 3 -C 6）亚环烷基中断的（C 1 -C 4）亚烷基，所述亚烷基任选地被（C 1 -C 3）烷基在同一个碳原子上被一次或多次取代; 或者T表示直接键; Z特别表示氨基; R 1和R 2以及R 3和R 4是氢或取代基，例如卤素，烷基等。

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