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31. 发明授权

US07094911B2 Biphenyl and biphenyl-analogous compounds as integrin antagonists 失效
标题翻译：联苯和联苯类似物作为整联蛋白拮抗剂
公开(公告)号：US07094911B2
公开(公告)日：2006-08-22
申请号：US10285073
申请日：2002-10-31
申请人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
发明人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号： C07D333/24 , C07D333/36 , C07D409/06 , A61K31/38 , A61P19/10
CPC分类号： C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要翻译：本发明涉及联苯和联苯类似物，其作为药物组合物的制备和用途，作为整联蛋白拮抗剂，特别涉及用于治疗和预防癌症，动脉硬化，再狭窄，溶骨性疾病如骨质疏松和眼科疾病根据本发明的化合物具有式（1）其中R 1，R 2，U，V，A，B，W，R 3， SUP，C和R 4具有如权利要求中所定义的含义。

32. 发明授权

US07074934B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：US07074934B2
公开(公告)日：2006-07-11
申请号：US10296245
申请日：2001-06-12
申请人： Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
发明人： Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
IPC分类号： C07D211/08 , C07D211/20 , C07D333/56 , C07C233/00 , A61K31/445
CPC分类号： C07D417/12 , A61K31/165 , A61K31/277 , A61K31/381 , A61K31/426 , C07C237/22 , C07C255/58 , C07C271/22 , C07C271/66 , C07C2601/08 , C07D209/08 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/55 , C07D215/38 , C07D233/24 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/54 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/46 , C07D317/60 , C07D333/38 , C07D333/60 , C07D333/66 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D409/06 , C07D417/06
摘要： Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
摘要翻译：其中R 2，X，L，Y，Cy，Lp，D和n如说明书中所定义的式（I）化合物是用作抗血栓形成剂的丝氨酸蛋白酶抑制剂。

33. 发明申请

US20060142357A1 Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 失效
标题翻译： 11-β-羟基类固醇脱氢酶1型抑制剂
公开(公告)号：US20060142357A1
公开(公告)日：2006-06-29
申请号：US11135662
申请日：2005-05-24
申请人： Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher Fotsch , Aiwen Li , Guolin Cai , Randall Hungate , Chester Yuan , Christopher Tegley , David Jean , Nianhe Han , Qi Huang , Qingyian Liu , Michael Bartberger , George Moniz , Matthew Frizzle
发明人： Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric Bercot , Christopher Fotsch , Aiwen Li , Guolin Cai , Randall Hungate , Chester Yuan , Christopher Tegley , David Jean , Nianhe Han , Qi Huang , Qingyian Liu , Michael Bartberger , George Moniz , Matthew Frizzle
IPC分类号： A61K31/426 , A61K31/421 , C07D277/04 , C07D263/04
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1804
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R 1，R 2，R 2， 3，R 4，R 5，R 6，R 7，X和Z分别为以及包含该化合物的药物组合物的使用方法，以及该化合物用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的病症和用于制备作用于人的药物的方法 11-β-羟基类固醇脱氢酶1型酶。

34. 发明授权

US07026334B1 Thiazolidine compounds and pharmaceutical compositions exhibiting thrombopoietin receptor agonism 失效
标题翻译：噻唑烷化合物和显示血小板生成素受体激动作用的药物组合物
公开(公告)号：US07026334B1
公开(公告)日：2006-04-11
申请号：US10048008
申请日：2000-07-24
申请人： Hiroshi Takemoto , Masami Takayama , Takeshi Shiota
发明人： Hiroshi Takemoto , Masami Takayama , Takeshi Shiota
IPC分类号： A61K31/427 , C07D417/12
CPC分类号： C07D277/20 , C07D277/54 , C07D277/82 , C07D417/12 , C07D417/14
摘要： Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: wherein X1 is optionally substituted heteroaryl or the like; Y1 is —NRACO— (CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted arylene or the like; and A1 is a ring represented by general formula (II) or (III):
摘要翻译：含有作为活性成分的通式（I）化合物，其前体药物，它们的药学上可接受的盐或它们的溶剂合物并且表现出血小板生成素受体激动剂的药物组合物：其中X 1是任选取代的杂芳基等; Y 1是-NR A - （CH 2）2 - 或其类似物（其中R A是氢等等）; Z 1是任选取代的亚芳基等; 和A 1是由通式（II）或（III）表示的环：

35. 发明申请

US20060069037A1 Peptide-containing alpha-ketoamide cysteine and serine protease inhibitors 审中-公开
公开(公告)号：US20060069037A1
公开(公告)日：2006-03-30
申请号：US11273850
申请日：2005-11-15
申请人： Sankar Chatterjee , John Mallamo , Ron Bihovsky , Gregory Wells
发明人： Sankar Chatterjee , John Mallamo , Ron Bihovsky , Gregory Wells
IPC分类号： A61K38/05 , A61K38/04 , C07K5/06 , C07K5/04
CPC分类号： C07D207/08 , C07C311/06 , C07C311/46 , C07C311/48 , C07D207/20 , C07D207/48 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D235/06 , C07D239/42 , C07D275/06 , C07D277/40 , C07D277/54 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07K5/0202 , C07K5/06069
摘要： This invention relates to peptide-containing α-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.

36. 发明申请

US20060014794A1 CXCR1 and CXCR2 chemokine antagonists 失效
标题翻译： CXCR1和CXCR2趋化因子拮抗剂
公开(公告)号：US20060014794A1
公开(公告)日：2006-01-19
申请号：US11126977
申请日：2005-05-11
申请人： Jianhua Chao , Arthur Taveras , Cynthia Aki , Daniel Lundell , Jay Fine , Tony Priestley , Angelo Reggiani
发明人： Jianhua Chao , Arthur Taveras , Cynthia Aki , Daniel Lundell , Jay Fine , Tony Priestley , Angelo Reggiani
IPC分类号： A61K31/454
CPC分类号： C07D333/36 , C07D207/34 , C07D207/36 , C07D231/38 , C07D231/46 , C07D275/03 , C07D277/54 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12
摘要： The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.
摘要翻译：本发明涉及具有式（1）的通式结构的化合物：可用于治疗，预防或改善CXCR1或CXCR2趋化因子介导的疾病。

37. 发明授权

US06956045B2 Thiazolyl inhibitors of Tec family tyrosine kinases 有权
公开(公告)号：US06956045B2
公开(公告)日：2005-10-18
申请号：US10641876
申请日：2003-08-15
申请人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch, III
发明人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch, III
IPC分类号： C07D277/20 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D277/32 , C07D277/46 , C07D277/54 , C07D417/12 , C07D417/14 , C07D491/10 , C07D491/107 , A61K31/454 , C07D417/10
CPC分类号： C07D417/12 , C07D277/46 , C07D277/54 , C07D417/14 , C07D491/10
摘要： Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.

38. 发明申请

US20040235916A1 Thiazolyl amides and their use as antiviral drugs 审中-公开
标题翻译：噻唑酰胺及其作为抗病毒药物的用途
公开(公告)号：US20040235916A1
公开(公告)日：2004-11-25
申请号：US10481672
申请日：2003-12-19
发明人： Rudolf Schohe-Loop , Ulrich Betz , Rudiger Fischer , Martin Hendrix , Gerald Kleymann , Judith Baumeister , Wolfgang Bender , Peter Eckenberg , Gabriele Handke-Erguden , Kerstin Henninger , Axel Jensen , Jorg Keldenich , Udo Schneider , Olaf Weber
IPC分类号： A61K031/427 , A61K031/426 , C07D417/02 , C07D277/38
CPC分类号： C07D417/12 , C07D277/54
摘要： The invention relates to the novel compounds of formula (I), to a method for producing the same and to their use as drugs, especially as antiviral drugs.
摘要翻译：本发明涉及式（I）的新型化合物，其制备方法及其作为药物，特别是作为抗病毒药物的用途。

39. 发明授权

US06605629B1 Neurotrophin production secretion promoting agent 有权
标题翻译：神经营养蛋白生成分泌促进剂
公开(公告)号：US06605629B1
公开(公告)日：2003-08-12
申请号：US09868304
申请日：2001-06-29
申请人： Yu Momose , Katsuhito Murase
发明人： Yu Momose , Katsuhito Murase
IPC分类号： C07D41312
CPC分类号： C07D263/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/38 , C07D263/46 , C07D263/48 , C07D277/32 , C07D277/40 , C07D277/54 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14
摘要： A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.
摘要翻译：一种神经营养因子产生/分泌促进剂，其包含下式的唑衍生物：其中R1表示卤素原子，可任意取代的杂环基，可任选被取代的羟基，可任选被取代的硫醇基，或可任选被取代的氨基; A表示可任选被取代的酰基，可任选被取代的杂环基，可任意取代的羟基或可任意被酯化或酰胺化的羧基; B表示可任选被取代的芳族基团; X表示可任选被取代的氧原子，硫原子或氮原子; Y表示二价烃基或杂环基，或其盐; 其可用作预防或治疗神经病的药剂。

40. 发明申请

US20030114649A1 5,5-Disubstituted thiazolidine derivative pesticides 失效
标题翻译： 5,5-二取代噻唑烷衍生物农药
公开(公告)号：US20030114649A1
公开(公告)日：2003-06-19
申请号：US10241625
申请日：2002-09-11
申请人： Nippon Soda Co., Ltd.
发明人： Isao Iwataki , Vladimir F. Rudchenko , Thomas Kurz , Charles R. Semer IV , Thomas A. Kucharek , Detlef Geffken
IPC分类号： C07H017/02 , C07D417/02 , C07D277/14
CPC分类号： C07D277/50 , C07D277/42 , C07D277/54
摘要： Fungicidal 5,5-disubstituted thiazolidine derivatives are provided having the formula; 1 wherein R1 is selected from the group consisting of C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 cycloalkyl, and optionally substituted phenyl; R2 is phenyl substituted by An; A is each independently selected from the group consisting of H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkenyloxy, C1-C6 alkynyloxy, nitro, optionally substituted amino, C1-C6 alkylthio, C1-C6 alkoxycarbonyl, phenoxy, phenyl, optionally substituted pyridyl, optionally substituted thienyl, and optionally substituted furyl; n is 0-5; X is O; Y is selected from the group consisting of O, S, NnullOH, optionally substituted arylimino, optionally substituted alkylimino, optionally substituted carbamoyloxyimino, optionally substituted sulfamoyloxyimino, optionally substituted aroyloxyimino, optionally substituted alkoxycarbonyloxyimino, optionally substituted alkylhydrazono, optionally substituted phenylhydrazono, and alkylsulfenyl; and Z is optionally substituted phenylamino.
摘要翻译：提供具有下式的杀真菌的5,5-二取代的噻唑烷衍生物：其中R 1选自C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6环烷基和任选取代的苯基; R2是被An取代的苯基; A各自独立地选自H，卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6烯氧基，C 1 -C 6炔氧基，硝基，任选取代的氨基，C 1 -C 6烷硫基， C 1 -C 6烷氧基羰基，苯氧基，苯基，任选取代的吡啶基，任选取代的噻吩基和任选取代的呋喃基; n为0-5; X是O; Y选自O，S，N-OH，任选取代的芳基亚氨基，任选取代的烷基亚氨基，任选取代的氨基甲酰氧基亚氨基，任选取代的氨磺酰氧基亚氨基，任选取代的芳酰氧基亚氨基，任选取代的烷氧基羰基氧亚氨基，任选取代的烷基亚肼基，任选取代的苯基亚肼基， ; Z是任选取代的苯基氨基。

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