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1. 发明申请

US20040224999A1 Use of angiotensin II receptor antagonists for treating acute myocardial infarction 失效
公开(公告)号：US20040224999A1
公开(公告)日：2004-11-11
申请号：US10859776
申请日：2004-06-03
发明人： Jessica M. Mann , Pascale Oddou , Eric Michel Neuhart
IPC分类号： A61K031/41
CPC分类号： A61K31/4174 , A61K31/00 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/4709
摘要： The invention relates to the use of an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of acute MI and for the secondary prevention of acute MI.

2. 发明申请

US20040176425A1 Cycloalkyl containing anilide ligands for the thyroid receptor 审中-公开
标题翻译：含有甲苯受体的酰苯胺配体的环烷基
公开(公告)号：US20040176425A1
公开(公告)日：2004-09-09
申请号：US10764118
申请日：2004-01-23
发明人： William N. Washburn , Wei Meng
IPC分类号： A61K031/44 , A61K031/41 , A61K031/195 , A61K031/277
CPC分类号： C07C233/60 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： Novel thyroid receptor ligands are provided having the general formula I 1 wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式I的新型甲状腺受体配体，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10和R 11如本文所定义。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

3. 发明申请

US20040157902A1 Integrin antagonists 审中-公开
标题翻译：整合素拮抗剂
公开(公告)号：US20040157902A1
公开(公告)日：2004-08-12
申请号：US10479060
申请日：2003-11-26
发明人： Wolfgang Stnullhle , Alfred Jonczyk , Oliver Schadt , Simon Goodman
IPC分类号： A61K031/41 , A61K031/325
CPC分类号： C07D213/74 , C07D401/12
摘要： Novel biphenyl derivatives of the general formula (I), in which A, X, R1, R1null, R1null, R2 R2null, R2null and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel inhibitors of integrin receptors, in particular of the nullvnull3, nullvnull5 and/or nullvnull6 integrin receptors. The novel compounds can be used as medicaments. 1
摘要翻译：通式（I）的新型联苯衍生物，其中A，X，R 1，R 1，R“1”，R 2“R 2'，R 2” >和n如专利权利要求1中所定义，其立体异构体和其生理学上可接受的盐或溶剂化物是整合素受体的新型抑制剂，特别是alphavbeta3，alphavbeta5和/或alphavbeta6整联蛋白受体。新型化合物可用作药物。

4. 发明申请

US20040048909A1 Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US20040048909A1
公开(公告)日：2004-03-11
申请号：US10451408
申请日：2003-06-23
发明人： Takayuki Namiki , Kenichi Kishii , Masaki Mitani , Masashi Tamai , Naoki Hiyama , Makoto Kimura , Satoshi Ichinomiya
IPC分类号： A61K031/41 , A61K031/175 , A61K031/18 , A61K031/165
CPC分类号： C07D257/04 , C07C275/30 , C07C311/09 , C07C311/60
摘要： Biphenyl derivatives represented by the following formula (1): 1 wherein R1 represents a C5-7 alkyl group, R2 represents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, R3 represents a tetrazolyl group, nullNHCOCF3, nullNHSO2CF3 or nullSO2NHCONHR4 in which R4 represents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a C1-4 alkylene group or nullSO2NHnull, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.
摘要翻译：由下式（1）表示的联苯衍生物：其中R 1表示C 5-7烷基，R 2表示取代或未取代的芳族烃或环烷基，R 3表示四唑基， NHCOCF3，-NHSO2CF3或-SO2NHCONHR4，其中R 4表示取代或未取代的芳族烃基，Z表示单键，C1-4亚烷基或-SO2NH-，及其盐类; 和ACAT抑制剂和含有它们作为活性成分的药物。根据本发明的化合物具有优异的ACAT抑制活性，并且可用作通过增强ACAT活性（例如高胆固醇血症，动脉粥样硬化等）而引起的疾病的预防剂和/或治疗剂。

5. 发明申请

US20030187043A1 SUBSTITUTED N-BENZOYL-N'(TETRAZOLYLPHENYL)-UREAS AND THEIR USE AS PEST CONTROL AGENTS 失效
标题翻译：取代的N-苯甲酰基-N'（四氢噻吩基） - 和它们作为病虫害控制剂使用
公开(公告)号：US20030187043A1
公开(公告)日：2003-10-02
申请号：US10275829
申请日：2002-11-08
发明人： Fritz Maurer , Christoph Erdelen
IPC分类号： C07D261/20 , A61K031/41
CPC分类号： C07D257/04 , A01N47/34 , C07D405/04 , C07D405/06
摘要： The present invention relates to new substituted N-benzoyl-Nnull-(tetrazolylphenyl)-ureas of the formula (I) 1 in which R1, R2, R3, R4 and n are as stated in the description, to processes for their preparation, and to their use as pesticides.
摘要翻译：本发明涉及式（I）的新的取代的N-苯甲酰基-N' - （四唑基苯基） - 脲，其中R 1，R 2，R 3，R 4和n分别为在说明书中说明了它们的制备过程及其作为农药的用途。

6. 发明申请

US20030176479A1 Use of selective EP4 receptor agonists for the treatment of liver failure, loss of patency of the ductus arteriosus, glaucoma or ocular hypertension 审中-公开
标题翻译：使用选择性EP4受体激动剂治疗肝功能衰竭，动脉导管未闭，青光眼或高眼压
公开(公告)号：US20030176479A1
公开(公告)日：2003-09-18
申请号：US10386324
申请日：2003-03-11
发明人： Kimberly O. Cameron , Bruce A. Lefker
IPC分类号： A61K031/41 , A61K031/4015
CPC分类号： A61K31/4025 , A61K31/40 , A61K31/41
摘要： The present invention is directed to methods for treating liver failure, loss of patency of the ductus arteriosus, glaucoma or ocular hypertension, comprising administering to the patient in need thereof a therapeutically effective amount of a selective EP4 receptor agonist of the Formulae 1 wherein the variables A, B, Q, nullU, and R2 for Formula l; and the variables Ar, nullM, nullN, R, W, and Z for Formula II are as defined in the specification.
摘要翻译：本发明涉及用于治疗肝衰竭，动脉导管未闭，青光眼或高眼压的通畅性的方法，包括向需要的患者施用治疗有效量的式的选择性EP4受体激动剂，其中变量A ，B，Q，= U和R2; 并且式II中的变量Ar，= M，= N，R，W和Z如说明书中所定义。

7. 发明申请

US20030171406A1 Medicinal compositions containing propenone derivatives 审中-公开
标题翻译：含有丙烯酮衍生物的药物组合物
公开(公告)号：US20030171406A1
公开(公告)日：2003-09-11
申请号：US10296475
申请日：2002-11-25
发明人： Akihiko Sato
IPC分类号： A61K031/4439 , A61K031/427 , A61K031/422 , A61K031/4196 , A61K031/41
CPC分类号： C07D405/06 , A61K31/165 , A61K31/341 , A61K31/41 , A61K31/4155 , A61K31/4196 , A61K31/443 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/499 , A61K31/506 , A61K31/513 , A61K31/522 , A61K31/551 , A61K31/5517 , A61K31/675 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： A combination of an integrate inhibitor with an anti-retrovirus active substance and medical compositions containing the same as the active ingredients are found.
摘要翻译：发现整合抑制剂与抗逆转录病毒活性物质的组合以及含有与活性成分相同的药物组合物。

8. 发明申请

US20030153537A1 Reducing tetracycline resistance in living cells 失效
标题翻译：减少活细胞中四环素的耐药性
公开(公告)号：US20030153537A1
公开(公告)日：2003-08-14
申请号：US09504697
申请日：2000-02-16
发明人： Stuart B. Levy
IPC分类号： A61K031/65 , A61K031/41
CPC分类号： C07D295/13 , A61K31/65 , C07C237/26 , C07C323/29 , C07C2601/08 , A61K2300/00
摘要： The present invention provides an improved methodology by which therapeutically to overcome resistance to tetracycline in living cells including bacteria, parasites, fungi, and rickettsiae. The methodology employs a blocking agent such as C5 ester derivatives, or 6-deoxy 13-(substituted mercapto) derivatives of tetracycline, in combination with other tetracycline-type antibiotics as a synergistic combination of compositions to be administered simultaneously, sequentially or concurrently. In another embodiment, certain novel compositions are provided which may be administered alone against, for example, a sensitive or resistant strain of gram positive bacteria such as S. aureus and E. faecalis. The concomitantly administered compositions effectively overcome the tetracycline resistant mechanisms present such that the cell is effectively converted from a tetracycline-resistant state to a tetracycline-sensitive state.
摘要翻译：本发明提供了一种改进的方法，其通过其治疗来克服包括细菌，寄生虫，真菌和立克次体在内的活细胞中对四环素的抗性。该方法采用封闭剂如C5酯衍生物或四环素的6-脱氧13-（取代的巯基）衍生物与其他四环素型抗生素组合，作为同时，顺序或同时施用的组合物的协同组合。在另一个实施方案中，提供某些新的组合物，其可以针对例如革兰氏阳性细菌如金黄色葡萄球菌和粪肠球菌的敏感或抗性菌株单独施用。伴随施用的组合物有效克服存在的四环素抗性机制，使得细胞有效地从四环素抗性状态转变为四环素敏感状态。

9. 发明申请

US20030130324A1 METHOD FOR PREVENTING OR CONTROLLING CATARACT 无效
标题翻译：用于防止或控制CATARACT的方法
公开(公告)号：US20030130324A1
公开(公告)日：2003-07-10
申请号：US08648092
申请日：1996-06-21
发明人： JOHNSTON W. MCAVOY , CORAL G. CHAMBERLAIN
IPC分类号： A61K031/41
CPC分类号： C07K16/22 , A61K38/39 , A61K38/57
摘要： The present invention relates to a method for preventing or controlling pathological changes which occur in association with cataract formation in the mammalian eye by reducing the amount of or inhibiting the action of transforming growth factor-beta(TGFnull). The invention also relates to the use of inhibitors of TGFnull to prevent or minimise nullaftercataractnull.
摘要翻译：本发明涉及通过减少转化生长因子-β（TGFβ）的作用量或抑制转化生长因子-β（TGFβ）的作用来预防或控制与哺乳动物眼睛白内障形成有关的病理变化的方法。本发明还涉及TGFbeta抑制剂用于预防或最小化“后药”的用途。

10. 发明申请

US20030092685A1 Compounds, compositions and methods for treating or preventing pneumovirus infection and associated diseases 审中-公开
公开(公告)号：US20030092685A1
公开(公告)日：2003-05-15
申请号：US10280528
申请日：2002-10-25
发明人： Theodore J. Nitz , Daniel C. Pevear
IPC分类号： A61K031/65 , A61K031/55 , A61K031/553 , A61K031/554 , A61K031/426 , A61K031/4196 , A61K031/41
CPC分类号： C07D257/04 , C07D249/14 , C07D257/06 , C07D261/08 , C07D277/24
摘要： Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.

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