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41. 发明授权

US07247731B2 Ligands for metals and improved metal-catalyzed processes based thereon 有权
标题翻译：金属配体和基于其的改进的金属催化方法
公开(公告)号：US07247731B2
公开(公告)日：2007-07-24
申请号：US11229043
申请日：2005-09-16
申请人： Stephen L. Buchwald , David W. Old , John P. Wolfe , Michael Palucki , Ken Kamikawa
发明人： Stephen L. Buchwald , David W. Old , John P. Wolfe , Michael Palucki , Ken Kamikawa
IPC分类号： C07D211/70 , C07F7/04 , C07F9/02
CPC分类号： C07C1/26 , C07C1/321 , C07C17/16 , C07C17/263 , C07C29/32 , C07C29/38 , C07C37/18 , C07C41/30 , C07C45/68 , C07C45/71 , C07C49/675 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/08 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2531/24 , C07C2531/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C15/14 , C07C35/21 , C07C33/24 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C35/08
摘要： One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
摘要翻译：本发明的一个方面涉及用于过渡金属的新配体。本发明的第二方面涉及包含这些配体的催化剂在过渡金属催化的碳 - 杂原子和碳 - 碳键形成反应中的用途。本发明方法提供了过渡金属催化反应的许多特征的改进，包括合适底物的范围，反应条件和效率。

42. 发明申请

US20070049596A1 Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) 有权
标题翻译：药物组合物作为二肽基肽酶-IV（DPP-IV）的抑制剂
公开(公告)号：US20070049596A1
公开(公告)日：2007-03-01
申请号：US11510451
申请日：2006-08-25
申请人： Zhonghua Pei , Thomas Geldern , David Madar , Xiaofeng Li , Fatima Basha , Hong Yong , Kenton Longenecker , Bradley Backes , Andrew Judd , Matthew Mulhern , Kent Stewart
发明人： Zhonghua Pei , Thomas Geldern , David Madar , Xiaofeng Li , Fatima Basha , Hong Yong , Kenton Longenecker , Bradley Backes , Andrew Judd , Matthew Mulhern , Kent Stewart
IPC分类号： A61K31/498 , A61K31/495 , A61K31/445 , A61K31/47 , A61K31/277
CPC分类号： C07C211/48 , C07C211/40 , C07C217/52 , C07C217/54 , C07C217/74 , C07C217/84 , C07C217/86 , C07C225/22 , C07C229/42 , C07C229/48 , C07C229/60 , C07C233/43 , C07C233/78 , C07C235/46 , C07C237/24 , C07C237/30 , C07C237/42 , C07C255/54 , C07C255/58 , C07C311/22 , C07C311/36 , C07C317/22 , C07C317/36 , C07C2601/14 , C07C2601/16 , C07D207/16 , C07D209/08 , C07D209/48 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/64 , C07D213/68 , C07D213/74 , C07D213/82 , C07D217/04 , C07D263/56 , C07D263/60 , C07D277/04 , C07D277/64 , C07D295/135 , C07D295/185 , C07D295/205 , C07D317/66 , C07D319/18 , C07D333/34 , C07D333/38 , C07D409/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II, as well as hyperglycemia, metabolic syndrome, hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.
摘要翻译：本发明涉及抑制二肽基肽酶IV（DPP-IV）的化合物，其可用于预防或治疗糖尿病，特别是II型糖尿病，以及高血糖症，代谢综合征，高胰岛素血症，肥胖症，动脉粥样硬化，各种免疫调节疾病，和其他疾病。

43. 发明授权

US07141312B2 Organic electroluminescent device based on 2,5-diaminoterephthalic acid derivatives 失效
标题翻译：基于2,5-二氨基对苯二甲酸衍生物的有机电致发光器件
公开(公告)号：US07141312B2
公开(公告)日：2006-11-28
申请号：US10784149
申请日：2004-02-20
申请人： Andreas Richter , Jens Schöenewerk , Gerhard Diener
发明人： Andreas Richter , Jens Schöenewerk , Gerhard Diener
IPC分类号： H01L51/54 , H05B33/14 , C09K11/06
CPC分类号： H01L51/0059 , C07C229/62 , C07C255/58 , C07C2601/14 , C07C2603/42 , C07D209/08 , C07D213/74 , C07D239/42 , C07D295/135 , C07D295/192 , C07D317/66 , C07D455/04 , H01L51/0053 , H01L51/006 , H01L51/0081 , H01L51/5012 , H01L2251/308 , Y10S428/917
摘要： The application relates to an organic electroluminescent device which contains 2,5 diaminoterephthalic acid derivatives of formula 1a as emitter substances in one or several emitter layers in a pure or doped manner. The ring A is a triple unsaturated benzene ring wherein R4′ and R8′ are equal to zero or ring A is a double unsaturated ring respectively provided with a double bond in the 1,2 position and 4,5-position, and wherein R10 is a nitrile radical —CN or a radical C(═X1)—X2R1; R11 is a nitrile radical —CN or a radical —C(═X3)—X4R5, X1 and X3 are oxygen, sulphur or imino, X2 and X4 are oxygen, sulphur or optionally substituted amino, R1 to R8, R4′ and R8′ are H, C1–C20-alkyl, aryl, heteroaryl, R4 and R8 can also be halogen, nitro, cyanogen or amino, R2 to R4, R6–R8, R4′ and R8′ can also be trifluoromethyl or pentafluorophenyl, wherein certain radicals can form a saturated or unsaturated ring. The novel devices are characterized by narrow emission bands, low driver voltages, high photometric efficiency and high thermal stability within a broad spectral range.
摘要翻译：本申请涉及一种有机电致发光器件，其以纯或掺杂的方式在一个或多个发射极层中含有2.5个式Ia的二氨基对苯二甲酸衍生物作为发射体物质。环A是三不饱和苯环，其中R 4'和R 8'等于零或环A是分别具有双键的双不饱和环 1,2位和4,5位，其中R 10是腈基-CN或基团C（-X 1 -OR） - X 2＆lt; 1＆lt; 1＆gt; R 11是腈基-CN或-C（-X 3 O）-X 4 R 5 O X 1，X 3和X 3是氧，硫或亚氨基，X 2和X 4是氧，硫或任选取代的氨基，R 1至R 8，R 4'和R 8'是H， C 1 -C 20烷基，芳基，杂芳基，R 4和R 8也可以是卤素，硝基，氰基或氨基，R 2至 R 4，R 6，R 8，R 4，R 8和R 8， >也可以是三氟甲基或五氟苯基，其中某些基团可以形成饱和或不饱和的环。新颖的器件的特征在于窄的发射带，低的驱动电压，高的光度效率和宽的光谱范围内的高的热稳定性。

44. 发明申请

US20060069255A1 Novel aryl ureido benzoic acid derivatives and their use 失效
标题翻译：新型芳基脲基苯甲酸衍生物及其用途
公开(公告)号：US20060069255A1
公开(公告)日：2006-03-30
申请号：US10535683
申请日：2003-11-10
申请人： Jon Valgeirsson , Elsebet Nielsen , Dan Peters
发明人： Jon Valgeirsson , Elsebet Nielsen , Dan Peters
IPC分类号： C07D271/06 , C07D211/82
CPC分类号： C07D213/75 , C07C275/42 , C07C309/51 , C07C2603/18 , C07D209/40 , C07D231/56 , C07D257/04 , C07D271/07 , C07D317/66 , C07D333/36
摘要： This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.
摘要翻译：本发明涉及可用作离子型GluR5受体的选择性和非竞争性拮抗剂的新型芳基脲基苯甲酸衍生物。由于其生物学活性，本发明的芳基脲基衍生物被认为可用于治疗对天冬氨酸或谷氨酸受体的调节有反应的疾病。此外，本发明提供了根据本发明使用的化合物，以及包含化合物的药物组合物，以及治疗对天冬氨酸或谷氨酸受体的调节作用的疾病或病症或病症的方法。

45. 发明申请

US20060020131A1 Inhibitors of histone deacetylase 失效
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20060020131A1
公开(公告)日：2006-01-26
申请号：US10531406
申请日：2003-10-16
申请人： Stephane Raeppel , Frederic Gaudette , Isabelle Paquin , Arkadii Vaisburg , Daniel Delorme
发明人： Stephane Raeppel , Frederic Gaudette , Isabelle Paquin , Arkadii Vaisburg , Daniel Delorme
IPC分类号： C07D265/30 , C07D403/04
CPC分类号： C07C311/19 , C07C233/80 , C07C235/84 , C07C237/40 , C07C2601/02 , C07C2601/08 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/74 , C07D239/47 , C07D249/14 , C07D277/82 , C07D295/155 , C07D295/185 , C07D317/66 , C07D401/12
摘要： The invention provides compoods and methods for treating cell proliferative-diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.
摘要翻译：本发明提供了治疗细胞增殖性疾病的综合症和方法。本发明提供组蛋白脱乙酰酶酶活性的新抑制剂，包含抑制剂和药学上可接受的载体，赋形剂或稀释剂的化合物的组合物，以及在体外和治疗上使用该化合物抑制细胞增殖的方法。

46. 发明申请

US20050267126A1 Compounds derived from aryl carbamates, preparation thereof and uses of same 审中-公开
标题翻译：衍生自芳基氨基甲酸酯的化合物，其制备及其用途
公开(公告)号：US20050267126A1
公开(公告)日：2005-12-01
申请号：US10524875
申请日：2003-08-22
申请人： Magali Maillet , Laurent Saniere , Eric Nicolai , Dominique Potin , Michel Langlois
发明人： Magali Maillet , Laurent Saniere , Eric Nicolai , Dominique Potin , Michel Langlois
IPC分类号： A61P1/00 , A61P9/00 , A61P9/06 , A61P13/00 , A61P15/00 , A61P25/00 , C07D207/09 , C07D207/16 , C07D207/34 , C07D207/40 , C07D207/416 , C07D209/18 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/78 , C07D213/69 , C07D213/74 , C07D213/82 , C07D215/48 , C07D215/54 , C07D239/38 , C07D241/20 , C07D241/24 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/215 , C07D307/14 , C07D307/24 , C07D317/66 , C07D317/68 , C07D333/20 , C07D333/38 , C07D401/04 , C07D521/00 , A61K31/496 , C07D43/02
CPC分类号： C07D207/416 , C07D207/09 , C07D207/16 , C07D207/34 , C07D209/18 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/78 , C07D213/69 , C07D213/74 , C07D213/82 , C07D215/48 , C07D215/54 , C07D231/12 , C07D233/56 , C07D239/38 , C07D241/20 , C07D241/24 , C07D249/08 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/215 , C07D307/14 , C07D307/24 , C07D317/66 , C07D317/68 , C07D333/20 , C07D333/38 , C07D401/04
摘要： The invention concerns novel compounds, preparation and uses of same, particularly therapeutic. More particularly, the invention concerns compounds derived from arylcarbamates, preparation and uses of same, particularly in the field of human or animal health. The inventive compounds are preferably ligands of serotoninergic 5-HT4 receptors, and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, preparation and uses thereof, and treatment methods using said compounds.
摘要翻译：本发明涉及新型化合物，其制备和用途，特别是治疗性的。更具体地，本发明涉及衍生自芳基氨基甲酸酯的化合物，其制备方法及其用途，特别是在人或动物健康领域。本发明化合物优选为5-羟色胺能5-HT 4受体的配体，因此可用于治疗或预防性治疗涉及5-HT4受体的任何疾病。本发明还涉及包含这些化合物的药物组合物，其制备和用途以及使用所述化合物的治疗方法。

47. 发明授权

US06962929B2 Pentafluorobenzenesulfonamides and analogs 失效
标题翻译：五氟苯磺酰胺和类似物
公开(公告)号：US06962929B2
公开(公告)日：2005-11-08
申请号：US10270259
申请日：2002-10-11
申请人： John A. Flygare , Julio Cesar Medina , Bei Shan , David Louis Clark , Terry J. Rosen
发明人： John A. Flygare , Julio Cesar Medina , Bei Shan , David Louis Clark , Terry J. Rosen
IPC分类号： C07D295/12 , A61K31/165 , A61K31/18 , A61K31/255 , A61K31/357 , A61K31/36 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/44 , A61K31/47 , A61K31/5375 , A61P35/00 , C07C309/73 , C07C311/21 , C07C313/04 , C07C313/06 , C07C323/49 , C07D209/08 , C07D213/76 , C07D231/56 , C07D295/135 , C07D317/66 , C07D319/18 , C07K14/00 , C07K14/47 , A61K31/38 , A61K31/34
CPC分类号： C07K14/47 , A61K31/18 , A61K31/255 , A61K31/357 , A61K31/36 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/44 , A61K31/47 , A61K31/5375 , C07C309/73 , C07C311/21 , C07C313/06 , C07C323/49 , C07D209/08 , C07D213/76 , C07D231/56 , C07D295/135 , C07D317/66 , C07D319/18 , Y02A50/411
摘要： The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents. The compositions include compounds of the general formula I:
摘要翻译：本发明提供了与新的五氟苯基磺酰胺衍生物和类似物有关的方法和组合物及其作为药理活性剂的用途。该组合物特别用作治疗疾病状态，特别是癌症，血管再狭窄，微生物感染和牛皮癣的药理作用，或作为用于开发这种药物的铅化合物。组合物包括通式I的化合物：

48. 发明授权

US06867310B1 Arylation and vinylation of activated carbons 有权
标题翻译：活性炭的酰化和乙烯化
公开(公告)号：US06867310B1
公开(公告)日：2005-03-15
申请号：US09239024
申请日：1999-01-27
申请人： Stephen L. Buchwald , John P. Wolfe , Jens Ahman , Malisa Troutman , Michael Palucki , Ken Kamikawa , Andre Chieffi
发明人： Stephen L. Buchwald , John P. Wolfe , Jens Ahman , Malisa Troutman , Michael Palucki , Ken Kamikawa , Andre Chieffi
IPC分类号： C07C1/26 , C07C17/26 , C07C41/16 , C07C45/68 , C07C45/71 , C07C67/31 , C07C205/04 , C07C205/06 , C07C209/10 , C07C209/18 , C07C211/48 , C07C211/55 , C07C211/59 , C07C213/02 , C07C213/08 , C07C217/40 , C07C217/84 , C07C217/92 , C07C221/00 , C07C225/12 , C07C225/22 , C07C227/08 , C07C227/18 , C07C229/36 , C07C229/60 , C07C231/12 , C07C233/07 , C07C235/46 , C07C249/02 , C07C249/16 , C07C251/24 , C07C251/86 , C07C253/30 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/02 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/18 , C07F9/48 , C07F9/50 , C07F9/572 , C07F9/653 , C07F9/6547 , C07F9/6571 , C07F15/00 , C07D317/44
CPC分类号： C07D213/74 , C07C1/26 , C07C17/263 , C07C45/68 , C07C45/71 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/657 , C07C49/755 , C07C49/215 , C07C49/245 , C07C49/782 , C07C49/683 , C07C49/213 , C07C49/84 , C07C49/255 , C07C47/575 , C07C49/67 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C205/04 , C07C205/06
摘要： The present invention provides transition-metal-catalyst-based methods for the arylation and vinylation of activated methyl, methylene, and methine carbons with aryl halides, vinyl halides, and the like. The methods of the invention provide several improvements over existing methods, including the ability to synthesize efficiently and under mild conditions α-aryl and α-vinyl products from a wide range of starting materials, including ketones, esters, hydrazones, and imines. Furthermore, the methods of the invention may be used in an asymmetric sense, i.e. to produce enantiomerically-enriched chiral α-aryl and α-vinyl products.
摘要翻译：本发明提供了基于过渡金属催化剂的方法，用于芳基卤化物，卤代乙烯等的活化的甲基，亚甲基和次甲基碳的芳基化和乙烯基化的方法。本发明的方法相对于现有方法提供了若干改进，包括在温和条件下有效合成α-芳基和α-乙烯基产物的能力，所述α-芳基和α-乙烯基产物包括酮，酯，腙和亚胺。此外，本发明的方法可以以不对称方式使用，即产生对映异构体富集的手性α-芳基和α-乙烯基产物。

49. 发明申请

US20050009871A1 Ubiquitin ligase inhibitors 有权
标题翻译：泛素连接酶抑制剂
公开(公告)号：US20050009871A1
公开(公告)日：2005-01-13
申请号：US10858537
申请日：2004-06-01
申请人： Usha Ramesh , Gary Look , Rajinder Singh , Sarkiz Issakani
发明人： Usha Ramesh , Gary Look , Rajinder Singh , Sarkiz Issakani
IPC分类号： C07C233/75 , C07C275/34 , C07C311/21 , C07C311/29 , C07C311/48 , C07C311/51 , C07C311/64 , C07C317/34 , C07C323/49 , C07C335/42 , C07D207/16 , C07D207/26 , C07D207/32 , C07D207/325 , C07D209/08 , C07D211/46 , C07D211/58 , C07D213/42 , C07D213/64 , C07D213/76 , C07D213/78 , C07D215/40 , C07D217/02 , C07D231/56 , C07D235/30 , C07D239/34 , C07D239/42 , C07D261/16 , C07D265/36 , C07D295/13 , C07D295/26 , C07D307/14 , C07D307/91 , C07D317/66 , C07D319/20 , C07D333/36 , C07D401/12 , A61K31/4545 , C07
CPC分类号： C07C323/49 , C07C233/75 , C07C275/34 , C07C311/21 , C07C311/29 , C07C311/48 , C07C311/51 , C07C311/64 , C07C317/34 , C07C335/42 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07D207/16 , C07D207/26 , C07D207/325 , C07D209/08 , C07D211/46 , C07D211/58 , C07D213/42 , C07D213/64 , C07D213/76 , C07D213/78 , C07D215/40 , C07D217/02 , C07D231/56 , C07D235/30 , C07D239/34 , C07D239/42 , C07D261/16 , C07D265/36 , C07D295/13 , C07D295/26 , C07D307/14 , C07D307/91 , C07D317/66 , C07D319/20 , C07D333/36 , C07D401/12
摘要： This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.
摘要翻译：本发明描述了可用作泛素连接酶抑制剂的化合物。本发明的化合物可用作涉及泛素化的生物体的生物化学途径的抑制剂。本发明还提供了包含本发明所述化合物用于治疗需要抑制泛素连接酶的病症的药物组合物。此外，本发明提供了抑制细胞泛素化的方法，包括使需要泛素化抑制的细胞与根据本发明的化合物接触。

50. 发明申请

US20040180964A1 NPY Y5 antagonist 失效
公开(公告)号：US20040180964A1
公开(公告)日：2004-09-16
申请号：US10747359
申请日：2003-12-30
申请人： Shionogi & Co.
发明人： Yasuyuki Kawanishi , Hideyuki Takenaka , Kohji Hanasaki , Tetsuo Okada
IPC分类号： A61K031/18
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1 wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof

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