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公开(公告)号:US07750160B2
公开(公告)日:2010-07-06
申请号:US10989824
申请日:2004-11-15
申请人: Zdravko V. Milanov , Hitesh K. Patel , Robert M. Grotzfeld , Shamal A. Mehta , Andiliy G. Lai , David J. Lockhart
发明人: Zdravko V. Milanov , Hitesh K. Patel , Robert M. Grotzfeld , Shamal A. Mehta , Andiliy G. Lai , David J. Lockhart
IPC分类号: C07D221/04 , C07D471/04 , C07D413/12 , C07D261/14 , C07D277/20 , C07D277/32 , C07D513/14 , A61K31/47 , A61K31/4375 , A61K31/422 , A61K31/4353 , A61K31/426 , A61K31/4402 , A61K31/4412 , A61K31/443 , A61K31/429
CPC分类号: C07D231/12 , A61K31/42 , C07D231/40 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/04 , C07D513/04 , Y02A50/401 , Y02A50/411
摘要: The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
摘要翻译: 本发明提供用于治疗由各种激酶介导的病症的方法和组合物,其中使用尿素化合物的衍生物。 本发明还提供了使用化合物和/或组合物治疗受试者中各种疾病和不需要的病症的方法。
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公开(公告)号:US20100144741A1
公开(公告)日:2010-06-10
申请号:US12515521
申请日:2007-11-22
申请人: Mathias Frederiksen , Rainer Martin Luond , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Bernard Lucien Roy , Heinrich Rueeger
发明人: Mathias Frederiksen , Rainer Martin Luond , Clive McCarthy , Henrik Moebitz , Jean-Michel Rondeau , Bernard Lucien Roy , Heinrich Rueeger
IPC分类号: A61K31/4402 , C07D401/02 , C07D239/42 , C07C233/40 , C07D213/72 , C07D405/10 , C07D237/20 , C07D487/04 , A61K31/505 , A61K31/506 , A61K31/4418 , A61K31/50 , A61K31/5025 , A61P25/00
CPC分类号: C07D401/12 , C07C233/40 , C07C2601/02 , C07D213/74 , C07D231/38 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/52 , C07D261/14 , C07D487/04
摘要: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译: 本发明涉及以游离碱形式或以酸加成盐形式的式(I)的新型环状化合物,其制备方法,其用作药物和包含它们的药物。
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公开(公告)号:US20100081644A1
公开(公告)日:2010-04-01
申请号:US12564132
申请日:2009-09-22
申请人: Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
发明人: Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
IPC分类号: A61K31/4196 , C07D413/12 , A61K31/422 , C07D417/12 , A61K31/41 , A61K31/454 , C07D249/14
CPC分类号: C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译: 公开了式(I)的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂,拮抗剂或反向激动剂,并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。
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公开(公告)号:US20100075984A1
公开(公告)日:2010-03-25
申请号:US12161391
申请日:2007-01-18
申请人: José Hidalgo Rodríguez , Juan Lorenzo Catena Ruiz , Isabel Masip Masip , Maria del Carmen Serra Comas , Oscar Rey Puiggrós , Carmen Lagunas Arnal , Carolina Salcedo Roca , Dolors Balsa López
发明人: José Hidalgo Rodríguez , Juan Lorenzo Catena Ruiz , Isabel Masip Masip , Maria del Carmen Serra Comas , Oscar Rey Puiggrós , Carmen Lagunas Arnal , Carolina Salcedo Roca , Dolors Balsa López
IPC分类号: A61K31/497 , C07D413/10
CPC分类号: C07D261/14 , C07D413/12 , C07D413/14 , C07D471/04
摘要: Compounds of formula (I), and their pharmaceutically acceptable salts and solvates, wherein X represents —O—, —NH—, —S—, —NHC(═O)— or —NHC(═S)—; R1 represents —H or a hydrocarbon chain; R2 represents —H, alkoxy, amino, a hydrocarbon chain or a radical of a cycle; R3 represents —H, a hydrocarbon chain or a radical of a cycle; R4 represents —H or a hydrocarbon chain; alternatively R3 and R4 form together a cycle; R5 and R6 represent —H or halogen, and R7 represents —H, a hydrocarbon chain or heteroaryl, are useful against bacterial infections in animals, including humans.
摘要翻译: 式(I)化合物及其药学上可接受的盐和溶剂化物,其中X表示-O-,-NH-,-S-,-NHC(= O) - 或-NHC(= S) - )。 R1表示-H或烃链; R2表示-H,烷氧基,氨基,烃链或一个环的基团; R3表示-H,烃链或一个环的基团; R4表示-H或烃链; 或者R3和R4一起形成一个循环; R5和R6表示-H或卤素,R7表示-H,烃链或杂芳基,可用于包括人在内的动物的细菌感染。
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公开(公告)号:US20100035898A1
公开(公告)日:2010-02-11
申请号:US12462318
申请日:2009-07-31
申请人: David Beattie , Anny-Odile Colson , Andrew James Culshaw , Lisa Sharp , Emily Stanley , Lilya Sviridenko
发明人: David Beattie , Anny-Odile Colson , Andrew James Culshaw , Lisa Sharp , Emily Stanley , Lilya Sviridenko
IPC分类号: A61K31/519 , A61K31/437 , A61K31/44 , A61K31/425 , C07D487/00 , C07D471/02 , C07D401/12 , C07D277/04
CPC分类号: A61K31/5377 , A61K31/166 , A61K31/415 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K45/06 , C07C233/79 , C07C255/58 , C07C311/39 , C07C317/28 , C07C2601/14 , C07D209/08 , C07D213/74 , C07D213/82 , C07D213/84 , C07D215/38 , C07D231/12 , C07D231/16 , C07D231/38 , C07D231/56 , C07D233/61 , C07D233/64 , C07D239/42 , C07D249/12 , C07D249/14 , C07D257/04 , C07D257/06 , C07D261/14 , C07D277/04 , C07D277/42 , C07D295/135 , C07D401/04 , C07D401/12 , C07D403/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
摘要翻译: 描述了可用作促肾上腺皮质激素释放因子(CRF1)受体拮抗剂的环己基酰胺衍生物。
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公开(公告)号:US07652021B2
公开(公告)日:2010-01-26
申请号:US11364154
申请日:2006-02-28
申请人: Peter Aranyi , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Zoltan Kapui , Edit Susan , Tibor Szabo , Katalin Urban-Szabo , Marton Varga
发明人: Peter Aranyi , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Zoltan Kapui , Edit Susan , Tibor Szabo , Katalin Urban-Szabo , Marton Varga
IPC分类号: C07D403/12 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/506 , A61K31/33 , A61K31/41 , A61P3/10
CPC分类号: C04B35/632 , C07D207/16 , C07D213/74 , C07D215/38 , C07D221/22 , C07D231/38 , C07D241/20 , C07D253/06 , C07D261/14 , C07D277/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07D471/04
摘要: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).
摘要翻译: 本发明涉及具有二肽基肽酶IV酶抑制活性的通式(I)的新型化合物,其药物组合物,使用所述化合物的方法,其制备方法和通式(II),(IV)的中间体) ,(V),(VII),(VIII)和(IX)。
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公开(公告)号:US20100016304A1
公开(公告)日:2010-01-21
申请号:US12448549
申请日:2007-12-21
申请人: Yasumichi Fukuda , Yoshikazu Asahina , Ayako Nakamura , Kenji Fujita , Tomohiro Ide , Fumiyoshi Kobayashi , Shinji Kobayashi , Kanji Komatsu , Masanori Yamamoto
发明人: Yasumichi Fukuda , Yoshikazu Asahina , Ayako Nakamura , Kenji Fujita , Tomohiro Ide , Fumiyoshi Kobayashi , Shinji Kobayashi , Kanji Komatsu , Masanori Yamamoto
IPC分类号: A61K31/5377 , C07D263/14 , A61K31/421 , A61K31/426 , C07D277/28 , C07D513/04 , A61K31/4365 , C07D417/12 , A61P3/10
CPC分类号: C07C317/44 , C07C2601/08 , C07D213/75 , C07D213/80 , C07D215/38 , C07D217/22 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/28 , C07D241/44 , C07D261/14 , C07D263/48 , C07D275/02 , C07D277/20 , C07D277/46 , C07D277/82 , C07D285/08 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
摘要翻译: 由下式(1)表示的化合物:(其中由*表示的碳原子为R构型; R 1和R 2各自独立地为氢原子,卤素原子,氨基,羟基,羟基氨基 基团,硝基,氰基,氨磺酰基,C1-C6烷基,C1-C6烷氧基,C1-C6烷基硫烷基,C1-C6烷基亚磺酰基或C1-C6烷基磺酰基;以及 A是取代或未取代的杂芳基)或其药学上可接受的盐。
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公开(公告)号:US20090275537A1
公开(公告)日:2009-11-05
申请号:US12228421
申请日:2008-08-11
申请人: Xiangping Qian , Chihyuan (Grace) Chuang , Pu-Ping Lu , Bing Yao , Qing (Kevin) Lu , Hong Jiang , Wenyue Wang , Bradley P. Morgan , David J. Morgans, JR.
发明人: Xiangping Qian , Chihyuan (Grace) Chuang , Pu-Ping Lu , Bing Yao , Qing (Kevin) Lu , Hong Jiang , Wenyue Wang , Bradley P. Morgan , David J. Morgans, JR.
IPC分类号: A61K31/675 , C07D217/22 , A61K31/47 , A61K31/496 , A61K31/44 , A61K31/4375 , A61K31/4985 , A61P11/06 , A61P25/00 , A61P21/00 , A61P1/00 , A61P9/12 , C07D487/02 , C07D471/02 , C07D213/02 , C07D401/02 , C07F9/06
CPC分类号: C07H21/04 , C07D213/75 , C07D217/22 , C07D261/14 , C07D277/82 , C07D401/12 , C07D471/04 , C07D487/04
摘要: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
摘要翻译: 描述了调节平滑肌肌球蛋白和/或非肌肉肌球蛋白的化学实体,治疗与平滑肌肌球蛋白和/或非肌肉肌球蛋白相关的疾病和病症的药物组合物和方法。
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公开(公告)号:US20090263472A1
公开(公告)日:2009-10-22
申请号:US12300026
申请日:2007-05-23
IPC分类号: A61K9/127 , C07D403/04 , A61K31/506 , A61K38/06 , C07K5/097 , A61K9/12 , A61K9/48 , A61K9/28 , A61P9/00
CPC分类号: C07D239/52 , C07D209/20 , C07D239/34 , C07D239/60 , C07D261/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/06 , C07D413/12 , C07D417/04 , C07K5/0821
摘要: Endothelin receptor antagonist nitroderivatives of general formula (I): having an improved pharmacological activity compared with their parent compounds. They can be employed for treating or preventing endothelial-related disorders, renal, pulmonary, cardiac and vascular diseases, and inflammatory processes.
摘要翻译: 通式(I)的内皮素受体拮抗剂硝基衍生物:与其母体化合物相比具有改善的药理活性。 它们可用于治疗或预防内皮相关疾病,肾,肺,心脏和血管疾病以及炎性过程。
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公开(公告)号:US20090137570A1
公开(公告)日:2009-05-28
申请号:US12361287
申请日:2009-01-28
申请人: Hong LIU , Arnab K. CHATTERJEE , David C. TULLY , Phillip B. ALPER , Badry BURSULAYA , Jianhua GUO , David H. WOODMANSEE , Daniel MUTNICK , Donald S. KARANEWSKY , Yun HE
发明人: Hong LIU , Arnab K. CHATTERJEE , David C. TULLY , Phillip B. ALPER , Badry BURSULAYA , Jianhua GUO , David H. WOODMANSEE , Daniel MUTNICK , Donald S. KARANEWSKY , Yun HE
IPC分类号: A61K31/5377 , C07D413/12 , C07D295/145 , C07D413/14 , C07D279/12 , C07D241/04 , C07D417/12 , A61K31/454 , A61K31/404 , A61K31/495 , C07D403/12 , C07D401/12 , C07D209/08 , A61K31/541 , A61K31/54
CPC分类号: C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
摘要翻译: 本发明提供了选择性抑制组织蛋白酶S的化合物,组合物和方法。在优选的方面,组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。
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