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71. 发明申请

US20060223804A1 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US20060223804A1
公开(公告)日：2006-10-05
申请号：US11172289
申请日：2005-06-30
申请人： Sapna Shah , Neng-Yang Shih , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Wrobleski , Ashwin Rao , Cheng Wang
发明人： Sapna Shah , Neng-Yang Shih , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Wrobleski , Ashwin Rao , Cheng Wang
IPC分类号： A61K31/53 , A61K31/454 , C07D413/02 , C07D403/02
CPC分类号： C07D401/04 , A61K31/4178 , A61K31/451 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/573 , A61K45/06 , C07D211/56 , C07D211/60 , C07D211/66 , C07D211/76 , C07D413/04 , C07D417/04 , C07D498/20
摘要： A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
摘要翻译：具有式I所示的一般结构的化合物或其药学上可接受的盐和/或溶剂合物可用于治疗由NK 1受体介导的疾病或病症，例如各种生理疾病，症状或疾病，包括呕吐，抑郁，焦虑和咳嗽。

72. 发明授权

US07067539B2 Cannabinoid receptor ligands 失效
公开(公告)号：US07067539B2
公开(公告)日：2006-06-27
申请号：US10214897
申请日：2002-08-07
申请人： Joseph A. Kozlowski , Neng-Yang Shih , Brian J. Lavey , Razia K. Rizvi , Bandarpalle B. Shankar , James M. Spitler , Ling Tong , Ronald L. Wolin , Michael K. Wong
发明人： Joseph A. Kozlowski , Neng-Yang Shih , Brian J. Lavey , Razia K. Rizvi , Bandarpalle B. Shankar , James M. Spitler , Ling Tong , Ronald L. Wolin , Michael K. Wong
IPC分类号： A61K31/444 , A61K31/435 , C07D213/70 , C07D213/71 , C07D213/89
CPC分类号： C07D213/70 , C07C31/24 , C07C317/22 , C07C317/32 , C07C317/36 , C07C317/44 , C07C323/41 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/36 , C07D233/42 , C07D233/84 , C07D239/38 , C07D307/64 , C07D333/20 , C07D333/34 , C07D333/38
摘要： The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

73. 发明授权

US07049320B2 NK1 antagonists 有权
公开(公告)号：US07049320B2
公开(公告)日：2006-05-23
申请号：US10321687
申请日：2002-12-17
申请人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
发明人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
IPC分类号： A61K31/44 , C07D221/20
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

74. 发明申请

US20060106062A1 Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
标题翻译：用作PDE4抑制剂的取代的2-喹啉基 - 恶唑
公开(公告)号：US20060106062A1
公开(公告)日：2006-05-18
申请号：US11130359
申请日：2005-05-16
申请人： Rongze Kuang , David Blythin , Neng-Yang Shih , Ho-Jane Shue , Xiao Chen , Jianhua Cao , Danlin Gu , Ying Huang , John Schwerdt , Pauline Ting , Shing-Chun Wong , Li Xiao
发明人： Rongze Kuang , David Blythin , Neng-Yang Shih , Ho-Jane Shue , Xiao Chen , Jianhua Cao , Danlin Gu , Ying Huang , John Schwerdt , Pauline Ting , Shing-Chun Wong , Li Xiao
IPC分类号： A61K31/4709 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D405/14 , C07D401/04 , C07D405/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.
摘要翻译：本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

75. 发明申请

US20060100228A1 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US20060100228A1
公开(公告)日：2006-05-11
申请号：US11157510
申请日：2005-06-21
申请人： Bandarpalle Shankar , Eric Gilbert , Razia Rizvi , Chunli Huang , Joseph Kozlowski , Stuart McCombie , Neng-Yang Shih
发明人： Bandarpalle Shankar , Eric Gilbert , Razia Rizvi , Chunli Huang , Joseph Kozlowski , Stuart McCombie , Neng-Yang Shih
IPC分类号： A61K31/4747 , A61K31/46 , A61K31/405 , C07D455/02 , C07D403/02
CPC分类号： C07D221/20 , C07D209/52 , C07D401/12 , C07D471/08
摘要： Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
摘要翻译：式I化合物和/或其药学上可接受的盐，溶剂化物或前药，或含有这些化合物的药物组合物表现出抗炎和免疫调节活性，并且可有效治疗癌症和炎症，免疫调节或呼吸系统疾病或病症。

76. 发明申请

US20060063843A1 Compounds for the treatment of inflammatory disorders 失效
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US20060063843A1
公开(公告)日：2006-03-23
申请号：US11255130
申请日：2005-10-20
申请人： Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人： Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号： A61K31/66 , A61K31/165
CPC分类号： C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）的化合物：

77. 发明申请

US20050282861A1 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US20050282861A1
公开(公告)日：2005-12-22
申请号：US11197979
申请日：2005-08-05
申请人： Richard Friary , Joseph Kozlowski , Bandarpalle Shankar , Michael Wong , Guowei Zhou , Brian Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youhen Shu
发明人： Richard Friary , Joseph Kozlowski , Bandarpalle Shankar , Michael Wong , Guowei Zhou , Brian Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youhen Shu
IPC分类号： A61K31/445 , A61K31/4535 , A61K31/454 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/08 , C07D211/26 , C07D211/96 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
CPC分类号： C07D401/12 , C07D211/26 , C07D211/96 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.
摘要翻译：公开了具有抗炎和免疫调节活性的式I化合物或化合物的药学上可接受的盐。还公开了含有所述化合物的药物组合物。

78. 发明授权

US06878732B2 NK1 antagonists 失效
标题翻译： NK1拮抗剂
公开(公告)号：US06878732B2
公开(公告)日：2005-04-12
申请号：US10386577
申请日：2003-03-12
申请人： Michelle Laci Wrobleski , Gregory A. Reichard , Neng-Yang Shih , Dong Xiao
发明人： Michelle Laci Wrobleski , Gregory A. Reichard , Neng-Yang Shih , Dong Xiao
IPC分类号： A61K31/075 , A61K31/122 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/17 , A61K31/196 , A61K31/27 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/423 , A61K31/4453 , A61K31/498 , A61K31/5375 , A61K31/538 , A61K31/573 , A61K45/00 , A61P1/00 , A61P1/08 , A61P3/04 , A61P11/00 , A61P11/14 , A61P13/00 , A61P13/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/32 , A61P25/36 , A61P43/00 , C07C43/174 , C07C43/178 , C07C49/753 , C07C215/42 , C07C217/52 , C07C229/48 , C07C233/23 , C07C233/39 , C07C237/04 , C07C237/08 , C07C237/20 , C07C237/24 , C07C239/12 , C07C251/42 , C07C251/44 , C07C251/50 , C07C271/22 , C07C271/24 , C07C271/34 , C07C275/26 , C07D205/12 , C07D207/26 , C07D207/27 , C07D209/54 , C07D235/02 , C07D241/38 , C07D249/12 , C07D253/06 , C07D263/52 , C07D265/34 , C07D295/18 , C07D295/185 , C07D295/20 , C07D295/215 , C07D403/06 , C07J7/00 , A61K31/415 , C07D233/02 , C07D233/04
CPC分类号： C07D207/27 , C07C43/1747 , C07C43/1788 , C07C49/753 , C07C217/52 , C07C229/48 , C07C233/23 , C07C237/04 , C07C237/20 , C07C239/12 , C07C251/44 , C07C271/22 , C07C271/24 , C07C271/34 , C07C275/26 , C07C2601/04 , C07D205/12 , C07D209/54 , C07D235/02 , C07D241/38 , C07D253/06 , C07D263/52 , C07D265/34 , C07D295/185 , C07D295/215
摘要： A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough:
摘要翻译：具有式（I）的NK1拮抗剂，具有本文定义的变量，其可用于治疗许多障碍，包括呕吐，抑郁，焦虑和咳嗽：

79. 发明授权

US5945428A Substituted oximes, hydrazones and olefins as neurokinin antagonists 失效
标题翻译：取代的肟，腙和烯烃作为神经激肽拮抗剂
公开(公告)号：US5945428A
公开(公告)日：1999-08-31
申请号：US960724
申请日：1997-10-30
申请人： Neng-Yang Shih , Gregory A. Reichard , Robert G. Aslanian
发明人： Neng-Yang Shih , Gregory A. Reichard , Robert G. Aslanian
IPC分类号： C07D471/10 , A61K31/44 , C07D221/00
CPC分类号： C07D471/10
摘要： Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3;b, d and e are independently 0, 1 or 2;R is H, C.sub.1-6 alkyl, --OH or C.sub.2 -C.sub.6 hydroxyalkyl;A is an optionally substituted oxime, hydrazone or olefin;X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)-- --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.1)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl;Q is --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6, phenyl, naphthyl or heteroaryl;R.sup.6a, R.sup.7a, R.sup.8a, R.sup.9a, R.sup.6 and R.sup.7 are H, C.sub.1-6 alkyl, C.sub.2 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; or R.sup.6 and R.sup.7, together with the nitrogen to which they are attached, form a ring;R.sup.9a is R.sup.6 or --OR.sup.6 ; andZ is spiro-substituted piperidinyl or substituted piperazinyl wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中：a为0,1,2或3; b，d和e独立地为0,1或2; R为H，C 1-6烷基，-OH或C 2 -C 6羟基烷基; A是任选取代的肟，腙或烯烃; X是键，-C（O） - ， - O - ， - NR 6 - ， - S（O）e - ， - N（R 6）C（O） - ， - OC（O）NR6-， - OC（= S）NR6-，-N（R6）C（= S）O-，-C（= NOR1） - ， - S（O）（R 6）S（O）2 - ， - N（R 6）C（O）O-或-OC（O） - ; T是H，苯偶酰亚氨基，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; Q是-SR 6，-N（R 6）（R 7），-OR 6，苯基，萘基或杂芳基; R6a，R7a，R8a，R9a，R6和R7是H，C1-6烷基，C2-C6羟基烷基，C1-C6烷氧基-C1-C6烷基，苯基或苄基; 或R 6和R 7与它们所连接的氮一起形成环; R9a为R6或-OR6; Z是螺取代的哌啶基或取代的哌嗪基，其中芳基，杂环烷基，杂芳基，环烷基和桥连的环烷基任选被取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，炎性疾病和胃肠道疾病的方法，以及包含所述化合物的药物组合物。

80. 发明授权

US5932596A Imidazoylalkyl substituted with a six membered nitrogen containing nitrogen containing heterocyclic ring 失效
标题翻译：用含六价氮的含氮杂环取代的咪唑烷基
公开(公告)号：US5932596A
公开(公告)日：1999-08-03
申请号：US457352
申请日：1995-06-01
申请人： Neng-Yang Shih , Michael J. Green
发明人： Neng-Yang Shih , Michael J. Green
IPC分类号： C07D401/06 , A61K31/445
CPC分类号： C07D401/06
摘要： Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0.Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula 1.0 to a patient in need of such treatment.
摘要翻译：公开了式1.0的化合物或其药学上可接受的盐或溶剂化物。还公开了包含药学上可接受的载体和有效量的式1.0化合物的药物组合物。进一步公开的是治疗过敏（例如哮喘），炎症，高血压，升高的眼内压（例如青光眼）的方法，降低眼内压的方法，睡眠障碍，超低运动性和酸性分泌的状态胃肠道，中枢神经系统的低血压和多动症（例如，激动和抑郁）和其他CNS疾病（例如阿尔茨海默病，精神分裂症和偏头痛），包括向有需要的患者施用有效量的式1.0化合物这样的治疗。

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