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51. 发明申请

US20030181496A1 Pyrrole derivatives 失效
标题翻译：吡咯衍生物
公开(公告)号：US20030181496A1
公开(公告)日：2003-09-25
申请号：US10352067
申请日：2003-01-28
发明人： Teruhisa Tokunaga , William Ewan Hume , Makoto Kitoh , Ryu Nagata
IPC分类号： A61K031/425 , A61K031/4178 , A61K031/416 , A61K031/415 , A61K031/4025 , C07D417/02 , C07D43/02 , C07D49/02
CPC分类号： C07D207/33 , C07D207/333 , C07D401/06 , C07D403/06 , C07D471/04
摘要： Pyrrole derivatives represented by the following formula: 1 wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is nullCOnull, nullSO2null, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W2 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
摘要翻译：由下式表示的吡咯衍生物：其中环Z是任选取代的吡咯环等; W 2是-CO - ， - SO 2 - ，任选取代的C 1 -C 4亚烷基等; Ar 2是任选取代的芳基等; W 2和Ar 1表示以下（1）和（2）：（1）W 1是任选取代的C 1 -C 4亚烷基等; Ar 1是具有1-4个氮原子的任选取代的双环杂芳基作为成环原子：（2）W 1是任选取代的C 2 -C 5亚烷基，任选取代的C 2 -C 5亚烯基等; 并且Ar 1是在相对于W 1的结合位置的邻位或间位被羧基，烷氧基羰基等取代的芳基或单环杂芳基，或其药学上可接受的盐这些化合物可用作药物如用于器官或组织的纤维化抑制剂。

52. 发明申请

US20030119886A1 Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
公开(公告)号：US20030119886A1
公开(公告)日：2003-06-26
申请号：US10254701
申请日：2002-09-25
申请人： Pharmacia Corporation
发明人： John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas , Hwang-Fun Lu
IPC分类号： A61K031/44 , A61K031/426 , A61K031/425 , A61K031/421 , A61K031/42 , A61K031/4172 , A61K031/415 , A61K031/381 , A61K031/277 , A61K031/34 , A61K031/165
CPC分类号： C07D231/12 , C07D263/32
摘要： This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

53. 发明申请

US20030060482A1 Urease inhibitors 审中-公开
标题翻译：尿素酶抑制剂
公开(公告)号：US20030060482A1
公开(公告)日：2003-03-27
申请号：US10220803
申请日：2002-09-05
发明人： Masahiro Kajiwara
IPC分类号： C07D498/02 , A61K031/4745 , A61K031/425 , C07D275/04
CPC分类号： C07D275/04 , A61K31/428 , A61K31/437 , C07D513/04
摘要： A urease inhibitor and an anti-Helicobacter pylori agent, which contain, as an active ingredient, an isothiazole derivative represented by the general formula (1): 1 wherein R1 represents a hydrogen atom or an amino group, R2 represents a hydrogen atom, a lower alkyl group, or an acetyl group, and X represents a carbon atom or a nitrogen atom. These drugs are effective to prevent and treat gastrointestinal diseases caused by urease of Helicobacter pylori, such as chronic gastritis and gastroduodenal ulcer.
摘要翻译：脲酶抑制剂和抗幽门螺杆菌试剂，其含有通式（1）表示的异噻唑衍生物作为有效成分：其中R1表示氢原子或氨基，R2表示氢原子，低级烷基或乙酰基，X表示碳原子或氮原子。这些药物有效预防和治疗幽门螺杆菌脲酶引起的胃肠道疾病，如慢性胃炎和胃十二指肠溃疡。

54. 发明申请

US20030035835A1 Sustained-release form of administration containing tramadol saccharinate 失效
标题翻译：含有曲马多糖精的缓释形式
公开(公告)号：US20030035835A1
公开(公告)日：2003-02-20
申请号：US10084248
申请日：2002-02-28
发明人： Johannes Bartholomaeus , Heinrich Kugelmann , Iris Ziegler
IPC分类号： A61K031/425 , A61K009/22
CPC分类号： C07D275/06 , A61K9/0056 , A61K9/0058 , A61K9/0095 , A61K9/1652 , A61K9/2054 , A61K9/2081 , A61K9/2846 , A61K9/5015 , A61K9/5026 , A61K9/5047 , A61K31/135 , A61K31/137 , A61K31/19 , A61K31/195 , A61K31/205 , A61K31/428 , A61K31/54 , A61K31/60 , C07C217/74 , C07C307/02 , C07C2601/14 , C07D291/06 , A61K2300/00
摘要： Disclosed herein is sustained-release formulations of tramadol comprising tramadol saccharinate coated with at least one sustained-release coating. The sustained release formulations may also contain tramadol in non-sustained release form, and other pharmaceutically acceptable excipients. Also disclosed are methods of preparation of and methods of treatment using the inventive formulations.
摘要翻译：本文公开了包含用至少一种缓释涂层涂覆的曲马多糖精酸盐的曲马多缓释制剂。持续释放制剂还可以含有非持续释放形式的曲马多和其它药学上可接受的赋形剂。还公开了使用本发明制剂的制备方法和治疗方法。

55. 发明申请

US20020164266A1 Microbicidal mixtures 审中-公开
标题翻译：杀菌剂混合物
公开(公告)号：US20020164266A1
公开(公告)日：2002-11-07
申请号：US10096557
申请日：2002-03-13
发明人： Peter Wachtler , Martin Kugler
IPC分类号： A61K031/425 , A61K031/045
CPC分类号： A01N43/80 , A01N35/08 , A01N2300/00
摘要： The invention relates to synergistic mixtures of methyl-2H-isothiazol-3-one and 2-bromo-2-nitropropanediol for controlling microorganisms in industrial materials.
摘要翻译：本发明涉及甲基-2H-异噻唑-3-酮和2-溴-2-硝基丙二醇的协同混合物，用于控制工业材料中的微生物。

56. 发明申请

US20020091142A1 Alpha4beta1 and alpha4beta7 integrin inhibitors 审中-公开
标题翻译： Alpha4beta1和alpha4beta7整合素抑制剂
公开(公告)号：US20020091142A1
公开(公告)日：2002-07-11
申请号：US09803303
申请日：2001-03-09
发明人： Nigel Graham Cooke , Michael Lloyd Sabio
IPC分类号： C07F007/10 , C07D213/81 , A61K031/44 , A61K031/425
CPC分类号： C07D213/82 , A61K31/425 , A61K31/44 , C07D207/48 , C07D213/65 , C07D277/06 , C07D295/192 , C07F7/081
摘要： Compounds of the formula I 1 as defined and their pharmaceutically acceptable salts are inhibitors of null4null1 and/or null4null7 integrins, and are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of transplant rejection and inflammatory and autoimmune diseases.
摘要翻译：定义的式I化合物及其药学上可接受的盐是α4β1和/或α4β7整联蛋白的抑制剂，并且可用于抑制细胞粘附和治疗或预防性治疗移植排斥反应和炎性和自身免疫性疾病。

57. 发明申请

US20020040043A1 Amidino derivatives and their use as thrombin inhibitors 失效
标题翻译：脒衍生物及其作为凝血酶抑制剂的用途
公开(公告)号：US20020040043A1
公开(公告)日：2002-04-04
申请号：US09839609
申请日：2001-04-23
发明人： Thomas Antonsson
IPC分类号： A61K031/425 , A61K031/4162 , A61K031/381 , A61K031/277
CPC分类号： C07D333/34 , C07C309/73 , C07C311/21 , C07C311/29 , C07C323/60 , C07D233/84 , C07D261/16 , C07F9/5304
摘要： There is provided compounds of formula I, 1 wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译：提供式I化合物，其中R 1，R 2，R 3，Y，n和B具有在描述中给出的含义，其可用作胰蛋白酶样蛋白酶如凝血酶的竞争性抑制剂，特别是用于治疗条件需要抑制凝血酶（如血栓形成）或作为抗凝剂。

58. 发明申请

US20020013352A1 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：US20020013352A1
公开(公告)日：2002-01-31
申请号：US09829767
申请日：2001-04-10
发明人： Sigmond G. Johnson , Ralph A. Rivero
IPC分类号： A61K031/425 , A61K031/40 , A61K031/18 , A61K031/165 , A61K031/4025
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 1 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型取代的二胺衍生物：其中R1，R2，R3，R4，X1，X2，X3，X4，A，Y和n如说明书中所述，含有它们的药物组合物和其中使用的中间体制造。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。

59. 发明申请

US20010034359A1 Albumin-binding compounds that prevent nonenzymatic glycation and that may be used for treatment of glycation-related pathologies 有权
标题翻译：抑制非酶糖基化并可用于治疗糖基化相关病理学的白蛋白结合化合物
公开(公告)号：US20010034359A1
公开(公告)日：2001-10-25
申请号：US09817940
申请日：2001-03-27
发明人： Margo P. Cohen
IPC分类号： A61K031/425
CPC分类号： A61K31/192 , A61K31/196 , A61K31/40 , A61K31/405 , A61K31/5415 , C07C229/42
摘要： The present invention is directed to compositions that inhibit the nonenzymatic glycation of albumin, as well as methods of using compounds that inhibit albumin glycation for the treatment of glycation-related pathologies.
摘要翻译：本发明涉及抑制白蛋白的非酶糖基化的组合物，以及使用抑制白蛋白糖基化的化合物治疗糖基化相关病理学的方法。

60. 发明申请

US20010020034A1 Isothiazole derivatives useful as anticancer agents 有权
标题翻译：异噻唑衍生物可用作抗癌剂
公开(公告)号：US20010020034A1
公开(公告)日：2001-09-06
申请号：US09803296
申请日：2001-03-09
发明人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
IPC分类号： A61K031/425 , A61K031/496 , A61K031/5377
CPC分类号： C07D275/03 , C07C33/46 , C07C327/58 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of the formula 1 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂化物，其中X1，R1，R2和R3如本文所定义。本发明还涉及含有上述化合物的药物组合物和通过施用上述化合物治疗哺乳动物过度增殖性疾病的方法。

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