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111. 发明申请

US20120136002A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20120136002A1
公开(公告)日：2012-05-31
申请号：US13321078
申请日：2010-05-18
申请人： Rajeev Goswami , Anil Kumar Vuppala , Ramesh Veludandi , Ramesh Sistla , Chakshusmathi Ghadiyaram , Muralidhara Ramachandra
发明人： Rajeev Goswami , Anil Kumar Vuppala , Ramesh Veludandi , Ramesh Sistla , Chakshusmathi Ghadiyaram , Muralidhara Ramachandra
IPC分类号： A61K31/44 , C07D401/12 , A61K31/4709 , A61K31/4545 , C07D213/82 , C07C311/47 , A61K31/175 , C07C257/18 , C07D401/06 , A61K31/496 , C07D211/60 , A61K31/445 , C07D295/192 , A61K31/495 , C07D215/08 , A61K31/47 , C07D217/06 , A61K31/472 , C07D295/205 , C07D213/72 , A61K31/277 , A61K31/245 , C07D235/30 , A61K31/4184 , A61P35/00 , C07D213/69
CPC分类号： C07C311/47 , C07C235/62 , C07C257/18 , C07C259/18 , C07C309/51 , C07C311/21 , C07D211/26 , C07D211/58 , C07D213/61 , C07D213/68 , C07D213/73 , C07D213/75 , C07D213/76 , C07D213/78 , C07D213/82 , C07D215/08 , C07D217/06 , C07D295/104 , C07D401/06
摘要： A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
摘要翻译：公开了其中R 1至R 15，P 1，P 2，A，B和Q如权利要求中所定义并且其药学上可接受的盐和酯的式（I）化合物。式（I）化合物具有作为脱氧酶抑制剂的用途，并且可用于治疗依赖于脱氧酶的条件，特别是癌症。

112. 发明授权

US07807693B2 Substituted prolinamides, manufacturing, and the use thereof as medicaments 有权
标题翻译：取代的脯氨酰胺，制造及其作为药物的用途
公开(公告)号：US07807693B2
公开(公告)日：2010-10-05
申请号：US11749204
申请日：2007-05-16
申请人： Kai Gerlach , Georg Dahmann , Herbert Nar , Roland Pfau , Henning Priepke , Annette Schuler-Metz , Wolfgang Wienen
发明人： Kai Gerlach , Georg Dahmann , Herbert Nar , Roland Pfau , Henning Priepke , Annette Schuler-Metz , Wolfgang Wienen
IPC分类号： A61K31/4725 , A61K31/4025 , C07D217/00 , C07D217/06 , C07D207/08 , C07D207/12
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04
摘要： The present invention relates to new substituted prolinamides of general formula (I) wherein D, L, E, G, J, M, R3, R4, R5 and R13 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures, and the salts thereof.
摘要翻译：本发明涉及通式（I）的新的取代的脯氨酸酰胺，其中D，L，E，G，J，M，R 3，R 4，R 5和R 13如说明书中所定义，互变异构体，对映异构体，非对映异构体，混合物及其盐。

113. 发明申请

US20100094014A1 EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：激素氨基酸受体拮抗剂
公开(公告)号：US20100094014A1
公开(公告)日：2010-04-15
申请号：US12574201
申请日：2009-10-06
申请人： Jose Antonio Martinez-Perez , Thomas Michael Wilson
发明人： Jose Antonio Martinez-Perez , Thomas Michael Wilson
IPC分类号： C07D217/06
CPC分类号： C07D401/12 , C07D217/26 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).
摘要翻译：本发明提供式（I）和式（I（a））的新化合物或其药学上可接受的盐; 治疗神经系统疾病和神经变性疾病，特别是疼痛和偏头痛的方法，包括施用式（I）或式（I（a））的化合物; 和制备式（I）或式（I（a））的化合物的方法。

115. 发明申请

US20050197362A1 Preventives/remedies for urinary disturbance 失效
标题翻译：预防/治疗尿路障碍
公开(公告)号：US20050197362A1
公开(公告)日：2005-09-08
申请号：US10935646
申请日：2004-09-08
申请人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
发明人： Yuji Ishihara , Yuji Ishichi , Takayuki Doi , Hiroshi Nagabukuro , Naoyuki Kanzaki , Motoki Ikeuchi
IPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61P13/00 , A61P13/08 , A61P43/00 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/22 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06
CPC分类号： A61K31/00 , A61K31/138 , A61K31/40 , A61K31/445 , A61K31/473 , A61K31/549 , A61K31/55 , A61K31/553 , C07C233/41 , C07C311/07 , C07C311/08 , C07C311/37 , C07C2602/08 , C07D209/08 , C07D209/14 , C07D209/48 , C07D211/32 , C07D215/227 , C07D217/04 , C07D217/06 , C07D217/08 , C07D223/16 , C07D235/26 , C07D239/80 , C07D265/36 , C07D285/14 , C07D285/22 , C07D307/78 , C07D307/79 , C07D311/58 , C07D319/18 , C07D333/22 , C07D471/06 , C07D513/06 , G01N2333/91215
摘要： Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要翻译：含有具有乙酰胆碱酯酶抑制作用的化合物和α1拮抗作用的化合物的预防/补救措施，其显示出改善膀胱尿功能的优异效果（即，改善尿流率和排尿效率的效果）而不影响尿压或血压。

116. 发明申请

US20050148584A1 Novel substituted diamine derivatives useful as motilin antagonists 有权
标题翻译：新颖的取代二胺衍生物可用作胃动素拮抗剂
公开(公告)号：US20050148584A1
公开(公告)日：2005-07-07
申请号：US11066202
申请日：2005-02-25
申请人： Sigmond Johnson , Ralph Rivero
发明人： Sigmond Johnson , Ralph Rivero
IPC分类号： C07D295/04 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K45/00 , A61P1/00 , A61P1/04 , A61P3/04 , A61P43/00 , C07C233/25 , C07C233/75 , C07C233/78 , C07D207/08 , C07D207/26 , C07D207/27 , C07D209/48 , C07D209/54 , C07D209/66 , C07D211/40 , C07D213/40 , C07D213/89 , C07D217/06 , C07D295/092 , C07D295/13 , C07D295/18 , C07D295/185 , C07D307/68 , C07D333/20 , C07D471/08 , C07D413/02 , A61K31/537 , A61K31/5377
CPC分类号： C07C233/25 , C07C233/75 , C07D207/08 , C07D207/27 , C07D209/48 , C07D209/54 , C07D209/66 , C07D211/40 , C07D213/40 , C07D213/74 , C07D213/89 , C07D217/06 , C07D221/04 , C07D295/088 , C07D295/13 , C07D295/185 , C07D307/68 , C07D333/20 , C07D471/08
摘要： The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.
摘要翻译：本发明涉及下式的新的取代二胺衍生物：其中R 1，R 2，R 3，R 4， X 1，X 1，X 2，X 3，X 4，A，Y和n分别为说明书中描述的含有它们的药物组合物和其制造中使用的中间体。更具体地，本发明的化合物是可用于治疗相关病症和障碍的胃动素受体拮抗剂，例如胃肠反流障碍，进食障碍导致肥胖症和肠易激综合征。

117. 发明申请

US20050124652A1 Guanidino compounds 审中-公开
标题翻译：胍基化合物
公开(公告)号：US20050124652A1
公开(公告)日：2005-06-09
申请号：US10503392
申请日：2003-02-03
申请人： Rustum Boyce , Daniel Chu
发明人： Rustum Boyce , Daniel Chu
IPC分类号： A61P3/04 , A61P3/10 , C07D209/08 , C07D215/08 , C07D217/06 , C07D217/14 , C07D221/10 , C07D223/16 , C07D401/04 , C07D401/06 , A61K31/47 , A61K31/165 , A61K31/198 , A61K31/277
CPC分类号： C07D209/08 , C07D215/08 , C07D217/06 , C07D217/14 , C07D221/10 , C07D223/16 , C07D401/04 , C07D401/06
摘要： A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.
摘要翻译：提供了能够作为MC4-R激动剂的各种含有胍基的小分子。化合物具有本文提供的各种结构。该化合物可用于治疗MC4-R介导的疾病，并且可以配制成药物制剂和组合物。

118. 发明申请

US20050032790A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20050032790A1
公开(公告)日：2005-02-10
申请号：US10923010
申请日：2004-08-23
申请人： John Liebeschuetz , Amanda Lyons , Christopher Murray , Andrew Rimmer , Stephen Young , Nicholas Camp , Stuart Jones , Phillip Morgan , William Wylie , Simon Richards , John Masters , Michael Wiley
发明人： John Liebeschuetz , Amanda Lyons , Christopher Murray , Andrew Rimmer , Stephen Young , Nicholas Camp , Stuart Jones , Phillip Morgan , William Wylie , Simon Richards , John Masters , Michael Wiley
IPC分类号： C07C237/36 , C07C255/60 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D487/04 , A61K31/54 , A61K31/19 , A61K31/40 , A61K31/445 , A61K31/497
CPC分类号： C07D401/14 , C04B35/632 , C07C237/36 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D487/04
摘要： Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
摘要翻译：其中R2，X，L，Y，Cy，Lp，D和n如说明书中所定义的式（I）化合物是用作抗血栓形成剂的丝氨酸蛋白酶抑制剂。

119. 发明申请

US20050004164A1 2-Cyanopropanoic acid amide and ester derivatives and methods of their use 审中-公开
标题翻译： 2-氰基丙酸酰胺和酯衍生物及其使用方法
公开(公告)号：US20050004164A1
公开(公告)日：2005-01-06
申请号：US10833678
申请日：2004-04-28
申请人： Thomas Caggiano , Antony Brazzale , William Moore , Callain Kim
发明人： Thomas Caggiano , Antony Brazzale , William Moore , Callain Kim
IPC分类号： A61K20060101 , A61K31/277 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/496 , A61P29/00 , C07C255/19 , C07C255/41 , C07C323/62 , C07D205/04 , C07D209/08 , C07D211/18 , C07D211/34 , C07D211/82 , C07D213/74 , C07D215/00 , C07D215/14 , C07D217/06 , C07D217/16 , C07D295/185 , C07D295/192 , C07D401/04
CPC分类号： C07C323/62 , C07C255/41 , C07C2601/14 , C07D211/34 , C07D215/14 , C07D295/192 , C07D401/04
摘要： This invention provides compounds of formula I or a pharmaceutically acceptable salt thereof that are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐，其可用于治疗疾病的炎性成分，并且特别可用于治疗动脉粥样硬化，心肌梗塞，充血性心力衰竭，炎性肠病，关节炎，II型糖尿病，和自身免疫性疾病如多发性硬化和风湿性关节炎。

120. 发明申请

US20020040002A1 Hydroxamic acids substituted by heterocycles useful for inhibition of tumor necrosis factor 审中-公开
标题翻译：被用于抑制肿瘤坏死因子的杂环取代的羟氨酸
公开(公告)号：US20020040002A1
公开(公告)日：2002-04-04
申请号：US09814119
申请日：2001-03-22
申请人： ZENECA LIMITED
发明人： Thomas Geoffrey Colerick Bird
IPC分类号： A61K038/05 , C07D239/72 , C07D235/04 , C07D217/06 , C07D215/38
CPC分类号： C07D215/227 , C07D209/38 , C07D215/14 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/64
摘要： 1 Compounds of formula (I), wherein: n is 1 to 6; Het is a nitrogen containing ring fused to the benzene ring on two adjacent carbon atoms to form a bicyclic ring system which ring system may be optionally substituted; R1 is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, aryl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R2 is C1-6alkyl, C2-6alkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R3 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R4 is hydrogen or C1-6alkyl; or R3 and R4 together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R1-R4, is optionally substituted; and pharmceutically acceptable salts and in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumour Necrosis Factor and/or one or more matrix metalloproteinase enzymes. Compositions containing them and their preparation are also described.
摘要翻译：式（I）化合物，其中n为1至6; Het是与两个相邻碳原子上的苯环稠合的含氮环，形成环系统可以任选取代的双环体系; R 1是氢，C 1-8烷基，C 2-6烯基，C 2-6炔基，C 3-8环烷基，芳基，杂芳基，杂环基，芳基C 1-6烷基，杂芳基C 1-6烷基，杂环基C 1-6烷基或C 3-8环烷基C 1-6烷基; R 2是C 1-6烷基，C 2-6烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或天然存在的氨基酸的侧链; R 3是氢，C 1-6烷基，C 3-8环烷基，C 4-8环烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或杂环基C 1-6烷基; R4是氢或C1-6烷基; 或R 3和R 4与它们所连接的氮原子一起形成杂环; 其中R 1 -R 4中的任何基团或环任选被取代; 和药学上可接受的盐和其体内可水解的酯被描述为产生肿瘤坏死因子和/或一种或多种基质金属蛋白酶的抑制剂。还描述了含有它们的组合物及其制备方法

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