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公开(公告)号:US20060009471A1
公开(公告)日:2006-01-12
申请号:US11159724
申请日:2005-06-23
申请人: Wenqing Yao , Meizhong Xu , Colin Zhang , Konstantinos Agrios , Brian Metcalf , Jincong Zhuo
发明人: Wenqing Yao , Meizhong Xu , Colin Zhang , Konstantinos Agrios , Brian Metcalf , Jincong Zhuo
IPC分类号: A61K31/495 , A61K31/4747 , A61K31/407 , C07D471/10 , C07D491/10
CPC分类号: C07D207/08 , C07D207/06 , C07D209/54 , C07D211/16 , C07D211/22 , C07D211/52 , C07D217/06 , C07D217/16 , C07D221/20 , C07D241/04 , C07D295/108 , C07D295/185 , C07D401/04 , C07D491/04 , C07D491/10 , C07D495/04
摘要: The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
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公开(公告)号:US20060004041A1
公开(公告)日:2006-01-05
申请号:US11120502
申请日:2005-05-03
申请人: Christopher Cummings , David Lowe , William Ripka
发明人: Christopher Cummings , David Lowe , William Ripka
IPC分类号: A61K31/4709 , C07D43/02 , C07D41/02
CPC分类号: C07D217/02 , A61K31/47 , C07D217/06 , C07D217/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要: The present invention relates to a class of small molecule hydroxamic acid compounds capable of inhibiting histone deacetylases (HDACs). The present invention also relates to methods of preparation of hydroxamic acid HDAC inhibitor compounds of the invention, which are N-substituted-1,2,3,4-tetrahydroisoquinoline hydroxamic acid derivatives, and their incorporation into pharmaceutical compositions and methods of administration. The present invention also relates to N-substituted-1,2,3,4-tetrahydroisoquinoline hydroxamic acid derivatives, which may be prepared as a hydroxamic acid HDAC inhibitor compound library that can be utilized in screening methods known in the art.
摘要翻译: 本发明涉及能抑制组蛋白脱乙酰酶(HDAC)的一类小分子异羟肟酸化合物。 本发明还涉及本发明的异羟肟酸HDAC抑制剂化合物的制备方法,它们是N-取代-1,2,3,4-四氢异喹啉异羟肟酸衍生物,以及它们掺入药物组合物和给药方法中。 本发明还涉及可以用于本领域已知的筛选方法中的异羟肟酸HDAC抑制剂化合物文库的N-取代-1,2,3,4-四氢异喹啉异羟肟酸衍生物。
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公开(公告)号:US20050215587A1
公开(公告)日:2005-09-29
申请号:US11126309
申请日:2005-05-11
IPC分类号: C07C237/36 , C07C237/42 , C07C255/60 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D233/54 , C07D235/06 , C07D241/24 , C07D273/00 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/64 , C07D277/68 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/79 , C07D317/68 , C07D333/36 , C07D333/38 , C07D333/60 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/12 , C07D487/04 , A61K31/4709 , A61K31/404 , A61K31/4178 , A61K31/427 , A61K31/4439
CPC分类号: C07D217/04 , C07B2200/07 , C07C237/36 , C07C237/42 , 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 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/06 , C07D231/56 , C07D233/64 , C07D235/06 , C07D241/24 , C07D273/00 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/64 , C07D277/68 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/79 , C07D317/68 , C07D333/36 , C07D333/38 , C07D333/60 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/12 , C07D487/04
摘要: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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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。
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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。
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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。
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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。
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公开(公告)号:US20040254193A1
公开(公告)日:2004-12-16
申请号:US10852726
申请日:2004-05-24
申请人: Pfizer Inc
发明人: John Lowe III
IPC分类号: A61K031/496 , C07D43/02
CPC分类号: C07D217/06
摘要: The present invention relates to compounds of formula I 1 wherein X and Y are as defined in the specification, and to pharmaceutical compositions comprising the compound of formula I and a pharmaceutically effective carrier; and to a method useful in treating or preventing in mammals, including humans, a disorder or condition selected from the group consisting of anxiety, depression, dysthymia, major depressive disorder, migraine, post-traumatic stress disorder, avoidant personality disorder, borderline personality disorder and phobias.
摘要翻译: 本发明涉及式I化合物,其中X和Y如说明书中所定义,以及包含式I化合物和药学上有效载体的药物组合物; 以及可用于治疗或预防哺乳动物(包括人),选自焦虑,抑郁,精神抑郁,重度抑郁障碍,偏头痛,创伤后应激障碍,避孕人格障碍,边缘人格障碍 和恐惧症。
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公开(公告)号:US20040158076A1
公开(公告)日:2004-08-12
申请号:US10772678
申请日:2004-02-04
申请人: Genentech, Inc.
IPC分类号: C07D211/82
CPC分类号: C07D213/75 , C07C233/87 , C07C271/22 , C07C271/44 , C07C271/48 , C07C271/54 , C07C271/56 , C07C271/58 , C07C311/06 , C07C311/09 , C07C311/58 , C07C323/43 , C07C323/59 , C07D207/16 , C07D207/22 , C07D207/28 , C07D211/46 , C07D211/60 , C07D211/62 , C07D215/36 , C07D217/06 , C07D217/14 , C07D217/22 , C07D231/16 , C07D235/06 , C07D235/26 , C07D249/18 , C07D277/12 , C07D277/56 , C07D295/205 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/72 , C07D471/10
摘要: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
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公开(公告)号:US20040158062A1
公开(公告)日:2004-08-12
申请号:US10775001
申请日:2004-02-09
申请人: Pfizer Inc
IPC分类号: C07D279/12 , C07D277/28 , C07D263/02
CPC分类号: C07D239/26 , C07D213/57 , C07D217/06 , C07D401/14
摘要: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds are useful in the treatment of benign prostatic hyperplasia.
摘要翻译: 本发明涉及可用于治疗的喹唑啉化合物的新方法。 更具体地,这些化合物可用于治疗良性前列腺增生。
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