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21. 发明申请

US20040224994A1 Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives 有权
标题翻译：杀虫剂（二卤代丙烯基）苯基烷基取代的二氢苯并呋喃和二氢苯并吡喃衍生物
公开(公告)号：US20040224994A1
公开(公告)日：2004-11-11
申请号：US10832624
申请日：2004-04-27
发明人： George Theodoridis , Edward J. Barron , Dominic P. Suarez , Y. Larry Zhang , Ping Ding , David M. Roush , Stephen F. Donovan , Frank J. Zawacki , Walter H. Yeager , John W. Lyga , Daniel H. Cohen
IPC分类号： A61K031/427 , A61K031/4245 , A61K031/42 , C07D417/02 , C07D413/02
CPC分类号： A01N43/30 , A01N43/32 , A01N43/40 , A01N43/60 , A01N47/16 , C07D211/22 , C07D307/79 , C07D307/83 , C07D311/04 , C07D401/04 , C07D495/10
摘要： Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. 1 wherein x and y are integers independently selected from 0 or 1; and B is a bridging group*null(CR16R17)qnull(CR18R19)rnull(CR20R21)snullLtnull(CR22R23)unull(CR24R25)vnull(CR26R27)wnull,where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.
摘要翻译：公开了杀虫（二卤代丙烯基）苯基烷基取代的二氢苯并呋喃和式I的二氢苯并吡喃衍生物。这些化合物在一系列昆虫害虫中提供了意想不到的杀虫活性，并结合所需的物理性质，包括改善的光稳定性。其中x和y是独立地选自0或1的整数; 并且B是桥连基团* - （CR 16 R 17）q - （CR 18 R 19）r - （CR 20 R 21）s -Lt-（CR 22）（R 25 R 25）） - （CR 26 R 27）w - ，其中星号表示在A处的连接; q，r，s，u，v和w是独立地选自0,1和2的整数; 并且t是选自0和1的整数。本文完全描述了A，D，E，G，M，R至R 11和R 16至R 27。此外，还公开了包含杀虫有效量的至少一种式I化合物的组合物和通过将所述组合物施用于存在昆虫或预期存在的场所来控制昆虫的方法。

22. 发明申请

US20040220241A1 Substituted biphenyl derivatives 失效
标题翻译：取代的联苯衍生物
公开(公告)号：US20040220241A1
公开(公告)日：2004-11-04
申请号：US10239397
申请日：2003-01-14
发明人： Horst Juraszyk , Dieter Dorsch , Werner Mederski , Christos Tsaklakidis , Christopher Barnes , Johannes Gleitz
IPC分类号： A61K031/4245 , C07D271/12
CPC分类号： C07C317/40 , C07C257/18 , Y02P20/55
摘要： The invention relates to compounds of the formula I 1 in which R1, R2, R3, R4 and X have the meaning indicated in the text. The compounds act as inhibitors of factors Xa and VIIa and can therefore be employed for the control and prevention of thromboembolic conditions such as thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
摘要翻译：本发明涉及其中R 1，R 2，R 3，R 4和X具有本文所示含义的式I化合物。这些化合物作为因子Xa和VIIa的抑制剂，因此可用于控制和预防血栓栓塞症状如血栓形成，心肌梗塞，动脉硬化，炎症，中风，心绞痛，血管成形术后的再狭窄和间歇性跛行。

23. 发明申请

US20040220239A1 Inhibitors of serine protease activity methods and compositions for treatment of nitric oxide-induced clinical conditions 审中-公开
公开(公告)号：US20040220239A1
公开(公告)日：2004-11-04
申请号：US10669251
申请日：2003-09-25
发明人： Leland Shapiro
IPC分类号： A61K031/433 , A61K031/4245
CPC分类号： A61K38/57 , A61K31/00 , A61K31/4245 , Y02A50/411
摘要： A novel method of treating and preventing diseases is provided. In particular, compositions and methods of blocking diseases associated with aberrant levels of nitric oxide and facilitated by a serine proteolytic (SP) activity are disclosed, which consist of administering to a subject a therapeutically effective amount of a compound having a serine protease inhibitory activity. Among effective compounds are null1-antitrypsin and synthetic drugs mimicking some or all of the actions of null1-antitrypsin.

24. 发明申请

US20040198778A1 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US20040198778A1
公开(公告)日：2004-10-07
申请号：US10810517
申请日：2004-03-26
申请人： Wyeth
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K031/433 , A61K031/4245 , A61K031/4196
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), 1 are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; nnull1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when YnullC, or substituted diene fused to Y when YnullC; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，CON或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; n = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

25. 发明申请

US20040034072A1 Aza-amino acid derivatives (factor Xa inhibitors 15) 失效
标题翻译：氮杂氨基酸衍生物（因子Xa抑制剂15）
公开(公告)号：US20040034072A1
公开(公告)日：2004-02-19
申请号：US10362050
申请日：2003-08-04
发明人： Werner Mederski , Horst Juraszyk , Dieter Dorsch , Christos Tsaklakidis , Johannes Gleiltz , Christopher Barnes
IPC分类号： A61K031/4245 , A61K031/195
CPC分类号： C07D213/30 , C07C311/47 , C07C317/42 , C07C333/04 , C07C2601/14 , C07D211/46 , C07D257/04 , C07D295/088 , C07D317/40
摘要： The invention relates to semicarbazides of the general formula I 1 where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
摘要翻译：本发明涉及通式I的氨基脲，其中R 1，R 2，R 3，R 4和I具有权利要求1所示的含义。式I化合物可用作特别是用于控制和预防血栓形成障碍如血栓形成，心肌梗塞，动脉硬化，炎症，中风，心绞痛，血管成形术后再狭窄和间歇性跛行的药物活性化合物。

26. 发明申请

US20040034060A1 Pharmacologic inhibition of Myc function 有权
标题翻译：药理学抑制Myc功能
公开(公告)号：US20040034060A1
公开(公告)日：2004-02-19
申请号：US10459769
申请日：2003-06-12
发明人： Edward V. Prochownik , Christine Giap , John S. Lazo , Xiaoying Yin
IPC分类号： A61K031/445 , A61K031/427 , A61K031/4245 , A61K031/137
CPC分类号： A61K31/137 , A61K31/135 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/427 , A61K31/445
摘要： The c-Myc oncoprotein, a helix-loop-helix-leucine zipper (HLH-ZIP) transcription factor, is frequently deregulated in human cancers. All known functions of c-Myc, including those pertaining to transformation, require that it heterodimerize with another HLH-ZIP protein, Max. Using a high throughput yeast-based assay, we identified seven low molecular weight substances that inhibit c-Myc-Max association. Each compound also prevented this interaction in vitro and inhibited the growth of c-Myc-expressing fibroblasts, although not of fibroblasts lacking c-Myc. Finally, short-term exposure of c-Myc over expressing fibroblasts to several of the compounds markedly reduced their in vivo tumorigenicity. These studies suggest that yeast-based assays can be used to identify inhibitors of protein-protein interactions and that these frequently function in mammalian cells. The signature specificities of each of the c-Myc-Max compounds identified here further suggest synergistic in vivo function.
摘要翻译：螺旋 - 环 - 螺旋 - 亮氨酸拉链（HLH-ZIP）转录因子的c-Myc癌蛋白在人类癌症中经常被放松。 c-Myc的所有已知功能，包括与转化有关的功能，都要求其与另一种HLH-ZIP蛋白Max，使用高通量的基于酵母的测定法，我们确定了七种抑制c-Myc-Max结合的低分子量物质。每种化合物在体外也阻止了这种相互作用，并且抑制了表达c-Myc的成纤维细胞的生长，尽管不是缺乏c-Myc的成纤维细胞。最后，c-Myc对几种化合物的表达成纤维细胞的短期暴露显着降低了其体内致瘤性。这些研究表明，基于酵母的测定可用于鉴定蛋白质 - 蛋白质相互作用的抑制剂，并且这些测定在哺乳动物细胞中经常起作用。此处鉴定的每种c-Myc-Max化合物的特征特征进一步表明协同的体内功能。

27. 发明申请

US20030220376A1 Methods for treating carbonic anhydrase mediated disorders 审中-公开
标题翻译：治疗碳酸酐酶介导的疾病的方法
公开(公告)号：US20030220376A1
公开(公告)日：2003-11-27
申请号：US10367384
申请日：2003-02-14
申请人： Pharmacia Corporation
发明人： Jaime L. Masferrer , Janet M. O'Neal
IPC分类号： A61K031/41 , A61K031/429 , A61K031/4245 , A61K031/426 , A61K031/421 , A61K031/4196 , A61K031/4192
CPC分类号： A61K31/18 , A61K31/415 , A61K31/4188 , A61K31/42 , A61K31/4965 , A61K31/635 , A61K45/06 , A61K2300/00
摘要： The current invention provides methods to treat or prevent carbonic anhydrase mediated diseases or disorders. The method generally comprises administering a tricyclic compound having a sulfonamide group to a subject wherein the compound inhibits carbonic anhydrase.
摘要翻译：本发明提供了治疗或预防碳酸酐酶介导的疾病或病症的方法。该方法通常包括向受试者施用具有磺酰胺基团的三环化合物，其中所述化合物抑制碳酸酐酶。

28. 发明申请

US20030212012A1 Pharmaceutically active pyrrolidine derivatives 失效
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US20030212012A1
公开(公告)日：2003-11-13
申请号：US10239912
申请日：2003-02-10
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Mattias Schwarz , Russell Thomas , Antony Baxter
IPC分类号： A61K031/7052 , A61K031/53 , A61K031/4439 , A61K031/4245 , A61K031/427 , A61K031/422 , A61K031/4184 , A61K031/4196 , C07D417/14 , C07D413/14 , C07D43/14
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula (I). Said 1 compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of null(CnullO)null, null(CnullO)nullOnull, nullC(nullNH)null, null(CnullO)nullNHnull, null(CnullS)nullNH, nullSO22null, nullSO2NHnull, nullCH2null,B is either a group null(CnullO)nullNR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式（I）的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法，其中X选自CR 6 R 7，NOR 6，NNR 6 R 7; A选自 - （C = O） - ， - （C = O）-O-，-C（= NH） - ， - （C = O）-NH-， - （C = S） -NH，-SO 2 - ， - SO 2 NH - ， - CH 2 - ，B为基团 - （C = O）-NR 8 R 9，或表示具有式（a）的杂环残基，其中Q为NR10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

29. 发明申请

US20030203945A1 Heterocyclic derivatives useful as pharmaceutical agents 审中-公开
标题翻译：用作药剂的杂环衍生物
公开(公告)号：US20030203945A1
公开(公告)日：2003-10-30
申请号：US10429349
申请日：2003-05-05
发明人： David Clive Blakemore , Justin Stephen Bryans , Sophie Caroline Williams
IPC分类号： A61K031/433 , A61K031/41 , A61K031/4245
CPC分类号： C07D291/04 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K45/06 , A61K47/545 , A61K47/555 , C07D257/04 , C07D271/07 , C07D285/08
摘要： This invention relates to novel heterocyclic derivatives of the formula (VII), (VIII) or (IX) 1 in which P, Q, R1-R6, m and n are as defined in the specification, and to pharmaceutically acceptable salts thereof. The compounds and pharmaceutical compositions containing them are useful in the treatment of a range of disorders including epilepsy, faintness attacks, hypokinesia, cranial disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases and gastrointestinal disorders, especially irritable bowel syndrome.
摘要翻译：本发明涉及式（VII），（VIII）或（IX）的新型杂环衍生物，其中P，Q，R 1 -R 6，m和n如说明书中所定义，其可接受的盐。含有它们的化合物和药物组合物可用于治疗一系列疾病，包括癫痫，微弱发作，运动功能减退，颅内障碍，抑郁症，焦虑症，恐慌症，疼痛，神经病理学疾病，炎性疾病和胃肠道疾病，特别是肠易激综合征。

30. 发明申请

US20030187038A1 Fibrinogen-lowering agents 审中-公开
标题翻译：纤维蛋白原降低剂
公开(公告)号：US20030187038A1
公开(公告)日：2003-10-02
申请号：US10344719
申请日：2003-02-14
发明人： Yoshimi Imura , Masao Hirakata
IPC分类号： A61K031/4245 , A61K031/4184
CPC分类号： A61K31/4184
摘要： We offer a fibrinogen-lowering agent comprising a compound having an angiotensin II antagonistic activity, a prodrug thereof, or a salt thereof. Because of having an excellent effect of lowering fibrinogen, the above fibrinogen-lowering agent is useful as a prophylactic or therapeutic agent for various diseases caused by hyperfibrionogenemia, etc.
摘要翻译：我们提供一种纤维蛋白降低剂，其包含具有血管紧张素II拮抗活性的化合物，其前药或其盐。由于具有降低纤维蛋白原的优异效果，因此上述纤维蛋白原降低剂可用作高纤维蛋白原血症等引起的各种疾病的预防或治疗剂。

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