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31. 发明申请

WO2003086398A1 AMINOCARBONYL SUBSTITUTED PYRIDINES, PYRIDAZINES, PYRIMIDINES, PYRAZINES AND TRIAZINES HAVING ANTIANGIOGENIC ACTIVITY 审中-公开
标题翻译：氨基羰基取代的吡啶类，吡咯烷酮，吡咯烷酮，具有抗生素活性的吡啶类和三嗪类
公开(公告)号：WO2003086398A1
公开(公告)日：2003-10-23
申请号：PCT/US2003/011066
申请日：2003-04-03
申请人： ABBOTT LABORATORIES
发明人： HAVIV, Fortuna , BRADLEY, Michael, F. , HENKIN, Jack , DINGES, Jürgen , SAUER, Daryl, R. , KOLACZKOWSKI, Lawrence , VASUDEVAN, Anil , PARK, David, C.
IPC分类号： A61K31/455
CPC分类号： C07D213/81 , A61K31/4439 , A61K31/4545 , A61K31/4747 , A61K31/496 , A61K31/541 , A61K31/551 , C07D213/82 , C07D239/28 , C07D241/24 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/10
摘要： Compounds having the formula (I) are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds. A is selected from the group consisting of pyridine, pyridine N-oxide, pyridazine, pyrimidine. pyrazine, and triazine; R 1 and R 2 , together with the nitrogen atom to which they are attached, form a five - to eight - membered ring containing an additional zero to two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; wherein the ring can be optionally substituted with one, two, or three substituents independently selected from the group consisting of alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, amino, aminocarbonyl, aryl, arylalkoxycarbonyl, wylalkyl, carboxy, formyl, haloalkyl, heterocycle, (heterocycle)alkyl, hydroxy, hydroxyalkoxyalkyl, hydroxyalkyl, and spiroheterocycle; R 3 at each occurance is independently selected from the group consisting 'of alkenyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, alkylsulfanyl, amino, aminocarbonyl, aryl, arylalkyl, aryloxy, cyano, cyanoalkyl, cyanoalkyl, (cycloalkyl)alkyl, halo, haloalkyl, heterocycle, hydroxy, hydroxyalkyl, and nitro; X is selected from the group consisting of O, S, and CH 2 ; and m is 0-4.
摘要翻译：具有式（I）的化合物是血管发生抑制剂。还公开了含有化合物的组合物，制备化合物的方法和使用该化合物的治疗方法。 A选自吡啶，吡啶N-氧化物，哒嗪，嘧啶。吡嗪和三嗪; R 1和R 2与它们所连接的氮原子一起形成含有另外的0至2个选自氮，氧和硫的杂原子的五元至八元环; 其中所述环可以任选被一个，两个或三个独立地选自烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，氨基，氨基羰基，芳基，芳基烷氧基羰基，二烷基，羧基，甲酰基，卤代烷基，杂环，（杂环）烷基，羟基，羟基烷氧基烷基，羟烷基和螺杂环; R 3各自独立地选自：烯基，烷氧基，烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，烷基硫烷基，氨基，氨基羰基，芳基，芳烷基，芳氧基，氰基，氰基烷基，氰基烷基，（环烷基）烷基，卤素，卤代烷基，杂环，羟基，羟基烷基和硝基; X选自O，S和CH 2; m为0-4。

32. 发明申请

WO01035951A2 ARYL NITRONE THERAPEUTICS AND METHODS FOR TREATING INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译： ARYL NITRONE THERAPEUTICS AND METHODS FOR TRAIS INFLAMMATORY BOWEL DISEASE
公开(公告)号：WO01035951A2
公开(公告)日：2001-05-25
申请号：PCT/US2000/031018
申请日：2000-11-13
IPC分类号： A61K31/15 , A61K31/24 , A61K31/4747 , A61K31/00
CPC分类号： A61K31/4747 , A61K31/15 , A61K31/24
摘要： Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.
摘要翻译：公开了使用芳基硝酮化合物治疗或预防炎症性肠病（IBD）的方法。也公开了可用于治疗或预防IBD的含有芳基硝酮化合物的药物组合物。

33. 发明申请

WO00056918A1 METHOD FOR SCREENING CYSTEINE PROTEASE INHIBITOR 审中-公开
标题翻译：筛选CYSTEINE PROTEASE抑制剂的方法
公开(公告)号：WO00056918A1
公开(公告)日：2000-09-28
申请号：PCT/JP2000/001662
申请日：2000-03-17
IPC分类号： A61K31/438 , A61K31/4747 , A61P43/00 , C07D235/20 , C07D497/20 , C07D497/22 , C12Q1/37 , C12N9/99
CPC分类号： C07D235/20 , A61K31/438 , A61K31/4747 , C12Q1/37 , G01N2333/8139 , G01N2333/96466 , G01N2500/00
摘要： A method for screening a cysteine protease inhibitor potentiating the cysteine protease inhibitory activity in the presence of polyvalent metal ions which comprises treating cysteine protease with a test compound in the presence of polyvalent metal ions occurring in vivo; and medicinal compositions for treating apoptosis-associated diseases which contain as the active ingredient a cysteine protease inhibitor potentiating the cysteine protease inhibitory activity in the presence of polyvalent metal ions occurring in vivo.
摘要翻译：一种筛选半胱氨酸蛋白酶抑制剂的方法，其在多价金属离子存在下增强半胱氨酸蛋白酶抑制活性，其包括在体内发生多价金属离子存在下用受试化合物处理半胱氨酸蛋白酶; 以及用于治疗凋亡相关疾病的药物组合物，其含有作为活性成分的半胱氨酸蛋白酶抑制剂，其在体内发生的多价金属离子存在下增强半胱氨酸蛋白酶抑制活性。

34. 发明申请

WO0004012A8 COMPOUNDS SPECIFIC FOR THE HUMAN alpha 1d ADRENERGIC RECEPTOR AND USES THEREOF 审中-公开
标题翻译：对人α1d肾上腺素能受体特异的化合物及其用途
公开(公告)号：WO0004012A8
公开(公告)日：2000-09-14
申请号：PCT/US9916101
申请日：1999-07-16
申请人： SYNAPTIC PHARMA CORP , KONKEL MICHAEL , WETZEL JOHN M , NOBLE STEWART , GLUCHOWSKI CHARLES , CRAIG DOUGLAS A
发明人： KONKEL MICHAEL , WETZEL JOHN M , NOBLE STEWART , GLUCHOWSKI CHARLES , CRAIG DOUGLAS A
IPC分类号： C07D295/06 , A61K31/00 , A61K31/438 , A61K31/4747 , A61K31/495 , A61K31/496 , A61P9/12 , A61P13/00 , A61P43/00 , C07D221/20 , C07D295/08 , C07D401/06 , A61K31/45 , C07D403/06
CPC分类号： A61K31/495 , A61K31/00 , A61K31/4747 , A61K31/496
摘要： This invention is directed towards a method of inhibiting activation of a human alpha 1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human alpha 1d adrenergic receptor. This invention provides for a compound which binds selectively to a human alpha 1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human alpha 1d adrenergic receptor which comprises administering to the subject an amount of the above defined compound to treat the disease.
摘要翻译：本发明涉及抑制人α1肾上腺素能受体活化的方法，该方法包括使该受体与化合物接触以抑制该受体的活化，其中该化合物选择性结合人α1肾上腺素能受体。本发明提供了选择性结合人α1肾上腺素能受体的化合物。本发明还提供了包含治疗有效量的上述定义的化合物和药学上可接受的载体的药物组合物。本发明进一步提供了治疗患有对人α1d肾上腺素能受体的拮抗作用易受治疗的疾病的受试者的方法，该方法包括给予受试者一定量的上述定义的化合物以治疗疾病。

35. 发明申请

WO00004012A1 COMPOUNDS SPECIFIC FOR THE HUMAN alpha 1d ADRENERGIC RECEPTOR AND USES THEREOF 审中-公开
标题翻译：人类α1dADRENERGIC受体的特异性化合物及其用途
公开(公告)号：WO00004012A1
公开(公告)日：2000-01-27
申请号：PCT/US1999/016101
申请日：1999-07-16
IPC分类号： C07D295/06 , A61K31/00 , A61K31/438 , A61K31/4747 , A61K31/495 , A61K31/496 , A61P9/12 , A61P13/00 , A61P43/00 , C07D221/20 , C07D295/08 , C07D401/06 , A61K31/45 , C07D403/06
CPC分类号： A61K31/495 , A61K31/00 , A61K31/4747 , A61K31/496
摘要： This invention is directed towards a method of inhibiting activation of a human alpha 1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human alpha 1d adrenergic receptor. This invention provides for a compound which binds selectively to a human alpha 1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human alpha 1d adrenergic receptor which comprises administering to the subject an amount of the above defined compound to treat the disease.
摘要翻译：本发明涉及抑制人α1D肾上腺素能受体活化的方法，其包括使受体与化合物接触以抑制受体活化，其中所述化合物选择性结合人α1D肾上腺素能受体。本发明提供了选择性结合人α1d肾上腺素能受体的化合物。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。本发明进一步提供了一种治疗患有易患有人α1D肾上腺素能受体拮抗作用的疾病的受试者的方法，该方法包括向受试者施用一定量的上述限定化合物以治疗该疾病。

36. 发明申请

WO2014037751A1 PHARMACOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：药物活性化合物
公开(公告)号：WO2014037751A1
公开(公告)日：2014-03-13
申请号：PCT/GB2013/052361
申请日：2013-09-09
申请人： CANCER RESEARCH TECHNOLOGY LIMITED
发明人： HOELDER, Swen , BLAGG, Julian , CHEUNG, Jack , ATRASH, Butrus , SHELDRAKE, Peter
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D401/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/107 , A61P35/00 , A61K31/472 , A61K31/4375 , A61K31/4985 , A61K31/506 , A61K31/496
CPC分类号： A61K31/4725 , A61K31/4375 , A61K31/4747 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K31/541 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/107
摘要： The present invention relates to compounds of formula (II) wherein X, Y, R 2 , R 3 , R 4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及其中X，Y，R2，R3，R4和Ar全部如本文所定义的式（II）化合物。已知本发明的化合物通过与Mps1激酶本身的相互作用直接或间接地抑制单轴1（Mps1，也称为TTK）激酶的主轴检查点功能。特别地，本发明涉及这些化合物作为治疗和/或预防增殖性疾病如癌症的治疗剂的用途。本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。

37. 发明申请

WO2008060621A2 AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为化学受体拮抗剂的氨基吡啶
公开(公告)号：WO2008060621A2
公开(公告)日：2008-05-22
申请号：PCT/US2007024076
申请日：2007-11-16
申请人： ABBOTT LAB , GEORGE DAWN M , DIXON RICHARD W , FRIEDMAN MICHAEL , HOBSON ADRIAN , LI BIQIN , WANG LU , WU XIAOYUN , WISHART NEIL
发明人： GEORGE DAWN M , DIXON RICHARD W , FRIEDMAN MICHAEL , HOBSON ADRIAN , LI BIQIN , WANG LU , WU XIAOYUN , WISHART NEIL
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/438 , A61K31/454 , C07D401/04
CPC分类号： A61K31/454 , A61K31/437 , A61K31/438 , A61K31/4545 , A61K31/4709 , A61K31/4747 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , A61K31/553 , C07D207/14 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D487/14
摘要： The present invention is directed to novel aminopyrrolidines of formula I, pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译：本发明涉及式I的新型氨基吡咯烷，其药学上可接受的盐，其代谢物，其异构体，其立体异构体或其前体药物，其中变量如本文所定义。式（I）化合物可用作趋化因子受体拮抗剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如癌症。

38. 发明申请

WO2008019070A3 PHARMACEUTICAL COMPOSITIONS OF TROSPIUM FOR TREATING SMOOTH MUSCLE HYPERACTIVITY DISORDERS 审中-公开
标题翻译：用于治疗平滑肌肉超敏性疾病的药物的药物组合物
公开(公告)号：WO2008019070A3
公开(公告)日：2008-04-24
申请号：PCT/US2007017353
申请日：2007-08-03
申请人： VERSI EBRAHIM
发明人： VERSI EBRAHIM
IPC分类号： A61K31/44
CPC分类号： A61K31/4747
摘要： Pharmaceutical compositions and methods are disclosed using trospium and/or its metabolites, and pro-drugs with antimuscarinic smooth muscle relaxant properties, administered as a subcutaneous injection, implant or other depot preparation for the treatment of urinary incontinence, and other smooth muscle hyperactivity disorders thus avoiding the poor bioavailability of oral administration.
摘要翻译：公开了药物组合物和方法，其使用鳟鱼和/或其代谢物，以及具有抗毒蕈碱性平滑肌松弛剂性质的前药，作为皮下注射，植入物或其它用于治疗尿失禁的贮库制剂以及其它平滑肌多动障碍避免口服给药的生物利用度差。

39. 发明申请

WO2007106792A2 METHODS FOR TREATING SARCOPENIA WITH A GROWTH HORMONE SECRETAGOGUE 审中-公开
标题翻译：用生长激素秘密处理恐怖症的方法
公开(公告)号：WO2007106792A2
公开(公告)日：2007-09-20
申请号：PCT/US2007/063841
申请日：2007-03-13
申请人： THORNER, Michael O.
发明人： THORNER, Michael O.
IPC分类号： A61K31/4747
CPC分类号： A61K31/4747 , A61K31/00 , A61K31/438 , A61K31/454
摘要： The present invention relates to methods for treating sarcopenia with a growth hormone secretagogue.
摘要翻译：本发明涉及用生长激素促分泌素治疗肌肉减少症的方法。

40. 发明申请

WO2004110368A3 COMBINATION THERAPY FOR THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译：治疗高血压的联合治疗
公开(公告)号：WO2004110368A3
公开(公告)日：2006-07-20
申请号：PCT/US2004017090
申请日：2004-06-02
申请人： MERCK & CO INC , FONG TUNG M , ERONDU NGOZI E , MACNEIL DOUGLAS J , MCINTYRE JAMES H , VAN DER PLOEG LEONARDUS H T
发明人： FONG TUNG M , ERONDU NGOZI E , MACNEIL DOUGLAS J , MCINTYRE JAMES H , VAN DER PLOEG LEONARDUS H T
IPC分类号： A61K38/17 , A61K20060101 , A61K31/155 , A61K31/353
CPC分类号： A61K31/4747 , A61K31/155 , A61K31/352 , A61K31/353 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compositions comprising an anti-obesity agent and an anti-hypertensive agent useful for the treatment of hypertension, hypertension associated with obesity, and hypertension-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.
摘要翻译：本发明涉及包含用于治疗高血压，与肥胖相关的高血压和高血压相关疾病的抗肥胖剂和抗高血压剂的组合物。本发明还涉及通过给予本发明的组合物来治疗或预防有需要的受试者中肥胖和肥胖相关疾病的方法。本发明进一步提供可用于实施这些方法的药物组合物，药物和试剂盒。

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