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31. 发明申请

US20090005344A1 Compounds and Methods of Use Thereof 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：US20090005344A1
公开(公告)日：2009-01-01
申请号：US11718277
申请日：2005-10-27
申请人： James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
发明人： James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
IPC分类号： A61K31/4184 , A61K31/381 , A61P43/00 , A61P29/00 , A61P19/02 , A61P17/06 , A61P19/08 , A61P11/06
CPC分类号： C07F5/025 , C07D235/18 , C07D417/04
摘要： Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译：描述了咪唑和苯并咪唑硼酸化合物，其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

32. 发明授权

US5310927A Benzofuran derivatives 失效
标题翻译：苯并呋喃衍生物
公开(公告)号：US5310927A
公开(公告)日：1994-05-10
申请号：US883164
申请日：1992-05-15
申请人： Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , Duncan B. Judd
发明人： Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , Duncan B. Judd
IPC分类号： A61K31/415 , A61K31/665 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D307/82 , C07D405/06 , C07D405/14 , C07F9/655 , C07D407/12 , A61K31/41 , C07D
CPC分类号： C07D307/82 , C07D405/06 , C07D405/14
摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinR.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, fluoroC.sub.1-6 alkyl, C.sub.1-6 alkoxy, --CHO, --CO.sub.2 H or --COR.sup.2 ;Ar represents the group ##STR2## Het represents an N-linked imidazolyl group optionally substituted by one, two or three substituents.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译：本发明提供式（I）化合物：其溶剂合物或代谢不稳定的酯，其中R 1表示氢原子或卤素原子或选自C 1-6烷基，C 2-6烯基，氟C 1-6烷基，C 1-6烷氧基， CHO，-CO 2 H或-COR 2; Ar表示组 Het表示任选被一个，两个或三个取代基取代的N-连接的咪唑基。该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

33. 发明授权

US5302589A Heterocyclic inhibitors of 5-.alpha.-testosterone reductase 失效
标题翻译： 5-α-睾酮还原酶的杂环抑制剂
公开(公告)号：US5302589A
公开(公告)日：1994-04-12
申请号：US927091
申请日：1992-08-07
申请人： Stephen V. Frye , David Middlemiss , Francis G. Fang
发明人： Stephen V. Frye , David Middlemiss , Francis G. Fang
IPC分类号： C07D471/06 , A61K31/435
CPC分类号： C07D471/06
摘要： The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 arei) independently, hydrogen or lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl orii) taken together with the linking nitrogen to form a 4 to 8 atom heterocyclic group, ##STR3## wherein; Y represents O, CH.sub.2, --N.dbd., NH or N(lower alkyl) optionally substituted with one or more lower alkyl groups;Ar is an aromatic group of 6 to 12 carbons;R.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N-- --CH.dbd.N-- or --N.dbd.CH--;n and m are independently 0, 1 or 2;and pharmaceutically acceptable salts thereof;their preparation, medical use and pharmaceutical formulations.
摘要翻译：本发明涉及式（I）的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮：其中R 1和R 2独立地是氢或低级烷基，带有R1和R2的碳之间的键是单键或双键，或ii）一起形成-CH 2 - 基以形成环丙烷环，并且具有R 1和R 2的碳之间的键是单键; X为，其中R 5，R 6，R 7和R 8独立地为氢或低级烷基，p和q独立地为0或1; R3为低级烷基，低级烯基，低级环烷基，低级烷氧基，硫代吡啶基，金刚烷基，-NR9R10或-Ar-NR9R10，其中R9和R10为i）独立地为氢或低级烷基，低级烯基，低级炔基，低级环烷基，，金刚烷基，芳基，苄基，二苯甲基，降冰片基或ii）与连接氮一起形成4至8个原子的杂环基，其中; Y表示任选被一个或多个低级烷基取代的O，CH 2，-N =，NH或N（低级烷基） Ar为6〜12个碳原子的芳香族基团; R4是氢或甲基; Z是-O - ， - NH - ， - N（低级烷基），-S - ， - SO - ， - SO 2，-CH 2 CH 2 - ， - CH = CH-，CO，CO 2， CH = N-或-N = CH-; n和m独立地为0,1或2; 及其药学上可接受的盐; 其制剂，医疗用途和药物配方。

34. 发明授权

US5252593A Pyrazole containing benzofuran derivatives and pharmaceutical compositions 失效
标题翻译：吡唑含有苯并呋喃衍生物和药物组合物
公开(公告)号：US5252593A
公开(公告)日：1993-10-12
申请号：US883380
申请日：1992-05-15
申请人： Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , Colin D. Eldred , John G. Montana , Pritom Shah , Stephen P. Watson
发明人： Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , Colin D. Eldred , John G. Montana , Pritom Shah , Stephen P. Watson
IPC分类号： A61K31/415 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/18 , A61P25/28 , C07D405/06 , C07D405/14 , A61K31/41 , C07D405/02
CPC分类号： C07D405/06 , C07D405/14
摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

35. 发明申请

US20140350019A1 ANILINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION 有权
标题翻译：苯胺衍生物，其制备及其治疗应用
公开(公告)号：US20140350019A1
公开(公告)日：2014-11-27
申请号：US14344925
申请日：2012-09-07
申请人： John Feutrill , Caroline Leriche , David Middlemiss
发明人： John Feutrill , Caroline Leriche , David Middlemiss
IPC分类号： C07C217/84 , C07C255/57 , C07C215/76 , C07C255/58 , C07C237/30 , C07D295/088 , C07C235/20 , C07C213/02 , C07C213/08 , C07C253/30 , A61K45/06 , A61K31/196 , A61K31/277 , A61K31/216 , A61K31/5375 , A61K31/165 , C07C63/72
CPC分类号： C07C217/84 , A61K9/0014 , A61K9/0048 , A61K31/165 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/5375 , A61K45/06 , C07C63/72 , C07C65/105 , C07C65/24 , C07C213/02 , C07C213/08 , C07C215/76 , C07C233/75 , C07C235/20 , C07C235/56 , C07C237/30 , C07C253/30 , C07C255/57 , C07C255/58 , C07C255/59 , C07D295/088
摘要： The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
摘要翻译：本发明涉及式（I）的苯胺衍生物，其制备及其治疗应用，例如治疗青光眼：式（I），R 1a表示H，卤素，（C 1 -C 6）烷基或CN ; R 1b表示H，卤素或（C 1 -C 6）烷基; R1c表示H或（C1-C6）烷基; R 2表示H，卤素，OH，O-（C 1 -C 6）烷基或（C 1 -C 6）烷基; R 3表示H，卤素，（C 1 -C 6）烷基，OH，O-（C 1 -C 6）烷基，CONH 2或CN; R 4表示H，卤素或（C 1 -C 6）烷基; R5表示H或F：R7表示H或F; R8表示H或F; R9表示H或（C1-C6）烷基或其一种对映异构体。

36. 发明授权

US08865699B2 Amino triazoles as PI3K inhibitors 有权
标题翻译：氨基三唑作为PI3K抑制剂
公开(公告)号：US08865699B2
公开(公告)日：2014-10-21
申请号：US12744940
申请日：2008-11-21
申请人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
发明人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中X，T1和R1至R3具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及生产和用作药物。

37. 发明授权

US08314257B2 Treatment of CRTH2-mediated diseases and conditions 有权
公开(公告)号：US08314257B2
公开(公告)日：2012-11-20
申请号：US12232447
申请日：2008-09-17
申请人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
发明人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要： The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

38. 发明授权

US08198314B2 Treatment of CRTH2-mediated diseases and conditions 有权
公开(公告)号：US08198314B2
公开(公告)日：2012-06-12
申请号：US12232446
申请日：2008-09-17
申请人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
发明人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要： The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

39. 发明授权

US08163931B2 Treatment of CRTH2-mediated diseases and conditions 有权
公开(公告)号：US08163931B2
公开(公告)日：2012-04-24
申请号：US12232444
申请日：2008-09-17
申请人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
发明人： David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
IPC分类号： C07D215/38
CPC分类号： C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要： The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

40. 发明申请

US20120041195A1 Heterocyclic compounds 审中-公开
标题翻译：杂环化合物
公开(公告)号：US20120041195A1
公开(公告)日：2012-02-16
申请号：US13201165
申请日：2010-02-09
申请人： Caroline Leriche , Eric Auclair , Jacques Le Roux , David Middlemiss
发明人： Caroline Leriche , Eric Auclair , Jacques Le Roux , David Middlemiss
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted triazolopyridine compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder. In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.
摘要翻译：本发明涉及某些新化合物，其制备方法和用于治疗或改善激酶介导的病症的方法。更具体地，本发明涉及可用作选择性激酶抑制剂的取代的三唑并吡啶化合物，用于制备这些化合物的方法和用于治疗或改善激酶介导的病症的方法。特别地，所述方法涉及治疗或改善包括心血管疾病，糖尿病，糖尿病相关疾病，炎性疾病，免疫学疾病，癌症和眼睛疾病如视网膜病变或黄斑变性或其他玻璃体视网膜疾病的激酶介导的疾病，以及类似。

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