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1. 发明申请

US20060069269A1 Novel indazolone derivatives useful as 11b-HSD1 inhibitors 失效
标题翻译：用作11b-HSD1抑制剂的新型吲唑酮衍生物
公开(公告)号：US20060069269A1
公开(公告)日：2006-03-30
申请号：US11235375
申请日：2005-09-26
申请人： Kurt Amrein , Jianping Cai , Robert Goodnow , Daniel Hunziker , Bernd Kuhn , Alexander Mayweg , Werner Neidhart
发明人： Kurt Amrein , Jianping Cai , Robert Goodnow , Daniel Hunziker , Bernd Kuhn , Alexander Mayweg , Werner Neidhart
IPC分类号： C07D231/56
CPC分类号： C07D231/56 , C07D401/06 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R7 have the significances given in the description and claims can be used in the form of pharmaceutical compositions.
摘要翻译：式（I）化合物

2. 发明申请

US20050089936A1 Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid amides 审中-公开
标题翻译： 3-芳基-1H-吲哚-2-羧酸酰胺的组合文库
公开(公告)号：US20050089936A1
公开(公告)日：2005-04-28
申请号：US10957161
申请日：2004-10-01
申请人： Jianping Cai , Robert Goodnow
发明人： Jianping Cai , Robert Goodnow
IPC分类号： A61K31/405 , A61K31/4745 , C07D209/04 , C07D209/42 , C07D471/02 , G01N33/53
CPC分类号： C07D209/42 , C07D209/04
摘要： Combinatorial libraries that contain various different 4,5-fused-3-substituted-2-pyrrocarboxylic amides for screening pharmacological activity and methods of synthesizing said libraries.
摘要翻译：包含用于筛选药理学活性的各种不同的4,5-稠合-3-取代-2-吡咯羧酰胺的组合文库以及合成所述文库的方法。

3. 发明申请

US20070049632A1 Pyrazolones as inhibitors of 11B-hydroxysteroid dehydrogenase 失效
标题翻译：吡唑啉酮作为11B-羟基类固醇脱氢酶的抑制剂
公开(公告)号：US20070049632A1
公开(公告)日：2007-03-01
申请号：US11507080
申请日：2006-08-18
申请人： Bruce Banner , Joseph Bilotta , Nader Fotouhi , Paul Gillespie , Robert Goodnow , Matthew Hamilton , Nancy-Ellen Haynes , Agnieszka Kowalczyk , Alexander Mayweg , Michael Myers , Sherrie Pietranico-Cole , Nathan Scott , Kshitij Thakkar , Jefferson Tilley
发明人： Bruce Banner , Joseph Bilotta , Nader Fotouhi , Paul Gillespie , Robert Goodnow , Matthew Hamilton , Nancy-Ellen Haynes , Agnieszka Kowalczyk , Alexander Mayweg , Michael Myers , Sherrie Pietranico-Cole , Nathan Scott , Kshitij Thakkar , Jefferson Tilley
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07D231/54
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
摘要翻译：本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。

4. 发明申请

US20050089935A1 Combinatorial library of 3-aryl-1h-indole-2-carboxylic acid 失效
标题翻译： 3-芳基-1h-吲哚-2-羧酸的组合文库
公开(公告)号：US20050089935A1
公开(公告)日：2005-04-28
申请号：US10957159
申请日：2004-10-01
申请人： Jianping Cai , Robert Goodnow
发明人： Jianping Cai , Robert Goodnow
IPC分类号： A61K31/405 , A61K31/4745 , C07B61/00 , C07D209/42 , C07D471/02 , G01N33/53
CPC分类号： C07D209/42 , C07B2200/11 , C40B40/04
摘要： Combinatorial libraries that contains various different 4, 5 fused 3-substituted-2-pyrrolocarboxylic acids for screening pharmacological activity and methods of synthesizing said libraries.
摘要翻译：包含各种不同的4,5-稠合的3-取代-2-吡咯羧酸用于筛选药理活性的组合文库和合成所述文库的方法。

5. 发明申请

US20060292638A1 Sequence #115 as a target for identifying weight modulating compounds 审中-公开
标题翻译：序号＃115作为鉴别重量调节化合物的靶标
公开(公告)号：US20060292638A1
公开(公告)日：2006-12-28
申请号：US11514392
申请日：2006-09-01
申请人： Robert Goodnow , David Mark , Mitchell Martin , James Rosinski
发明人： Robert Goodnow , David Mark , Mitchell Martin , James Rosinski
IPC分类号： G01N33/53
CPC分类号： G01N33/566 , G01N33/6893 , G01N2333/726 , G01N2500/00 , G01N2500/02 , G01N2500/04 , G01N2500/10 , G01N2500/20
摘要： Sequence #115, a G protein-coupled receptor, has been identified as a target for identifying weight modulating compounds. Compounds that modulate sequence #115 may be useful for the treatment of obesity and cachexia. Cell-based and cell-free assays are described to identify compounds which bind to and/or activate or inhibit the activity of sequence #115.
摘要翻译：序列＃115，G蛋白偶联受体，已被鉴定为鉴定重量调节化合物的靶标。调节序列＃115的化合物可用于治疗肥胖症和恶病质。描述基于细胞和无细胞的测定来鉴定结合和/或激活或抑制序列＃115的活性的化合物。

6. 发明申请

US20060122256A1 Biaryloxymethylarenecarboxylic acids as glycogen synthase activators 失效
标题翻译：作为糖原合成酶活化剂的生物芳氧基甲基羧酸
公开(公告)号：US20060122256A1
公开(公告)日：2006-06-08
申请号：US11283925
申请日：2005-11-21
申请人： Paul Gillespie , Robert Goodnow , Jefferson Tilley
发明人： Paul Gillespie , Robert Goodnow , Jefferson Tilley
IPC分类号： A61K31/381 , A61K31/34 , A61K31/192
CPC分类号： C07C65/24 , C07C51/09 , C07D213/30 , C07D213/61 , C07D213/64 , C07D213/79 , C07D215/06 , C07D215/14 , C07D231/12 , C07D261/08 , C07D277/56 , C07D307/42 , C07D317/54 , C07D319/08 , C07D333/16 , C07D401/12 , C07D409/12 , C07D417/12 , C07C59/66
摘要： The present invention relates to compounds of formula (I) wherein Ar, Ar2, R2, R3, R4, m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
摘要翻译：本发明涉及式（I）的化合物，其中Ar，Ar 2，R 2，R 3，R 4， m，p和s如说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与糖原合成酶如糖尿病的活化相关的疾病。

7. 发明申请

US20060223852A1 Pyrazoles 失效
标题翻译：吡唑
公开(公告)号：US20060223852A1
公开(公告)日：2006-10-05
申请号：US11395763
申请日：2006-03-31
申请人： Paul Gillespie , Robert Goodnow , Qiang Zhang
发明人： Paul Gillespie , Robert Goodnow , Qiang Zhang
IPC分类号： A61K31/4709 , A61K31/454 , C07D409/14
CPC分类号： C07D401/06 , C07D231/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
摘要翻译：本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。

8. 发明申请

US20060199816A1 Aryl sulfonyl piperidines 审中-公开
标题翻译：芳基磺酰基哌啶
公开(公告)号：US20060199816A1
公开(公告)日：2006-09-07
申请号：US11365053
申请日：2006-03-01
申请人： Paul Gillespie , Robert Goodnow , Agnieszka Kowalczyk , Sung-Sau So , Qiang Zhang
发明人： Paul Gillespie , Robert Goodnow , Agnieszka Kowalczyk , Sung-Sau So , Qiang Zhang
IPC分类号： A61K31/538 , A61K31/4709 , A61K31/453 , A61K31/445
CPC分类号： C07D211/96 , A61K31/445 , A61K31/453 , A61K31/4709 , A61K31/538 , C07D401/06 , C07D401/12 , C07D409/12 , C07D409/14 , C07D487/08
摘要： Provided herein are compounds of the formula (1): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
摘要翻译：本文提供了式（1）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。

9. 发明授权

US6001824A Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same 失效
标题翻译：丁酰基 - 酪氨酰基精胺，其类似物及其制备和使用方法
公开(公告)号：US6001824A
公开(公告)日：1999-12-14
申请号：US376924
申请日：1995-01-23
申请人： Koji Nakanishi , Danwen Huang , Seok-Ki Choi , Aristotle Kalivretenos , Robert Goodnow
发明人： Koji Nakanishi , Danwen Huang , Seok-Ki Choi , Aristotle Kalivretenos , Robert Goodnow
IPC分类号： C07C237/22 , C07C245/18 , C07C247/16 , C07C247/18 , C07C279/14 , A61K31/655
CPC分类号： C07C279/14 , C07C237/22 , C07C245/18 , C07C247/16 , C07C247/18
摘要： The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R.sub.2 is a 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R.sub.3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an a alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl) aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl, (trifluoromethyl)aminoacetyl or D- or L-arginyl group bonded through the .alpha.-carbonyl moiety thereof; R.sub.4 is H, or a linear or branched chain alkyl group; wherein R.sub.5, R.sub.6 and R.sub.7 are independently the same or different and are H, a linear or branched chain alkyl group, an aryl group or an arylalkyl group; wherein n, j and t are each 0 or 1; wherein m, o, p, q, r and s are independently the same or different and are 0, 1 or 2; wherein r+s and m+o are each equal to 2; wherein, if j is 0, p+q is 2; wherein, if j is 1, then p is 1, q is 0 and R.sub.6 is H; and wherein * denotes a D or L configuration. The invention also provides a method of synthesizing the compound. Another aspect of the invention concerns a method of treating a subject afflicted by a disorder associated with binding of an etiological agent to a glutamate receptor.
摘要翻译：本发明提供具有以下结构的化合物：其中R1是饱和或不饱和的直链或支链烷基或胆甾烷基; 其中R2是2-吲哚基，3-吲哚基，4-吲哚基，5-吲哚基，4-羟基苯基，4-（芳基烷氧基）苯基，3,4-二卤代苯基，4-羟基-3,5-二卤代苯基，4-叠氮基苯基或4-卤代苯基; 其中R 3为H，直链或支链烷基或烯基，或苯基，2-叠氮基苯基，3-叠氮基苯基，4-叠氮基苯基或链烯基酰基，3-氨基-3-丁基丙基，N- [N- （N- {4-叠氮基苯甲酰基}氨基丙基）氨基丙基]，顺式或反式肉桂基，2-氨基-2 - [（4'-叠氮基苯基）乙酰基，（三氟甲基）氨基乙酰基或D-或L-精氨酰基其α-羰基部分; R4是H或直链或支链烷基; 其中R5，R6和R7独立地相同或不同，为H，直链或支链烷基，芳基或芳基烷基; 其中n，j和t各自为0或1; 其中m，o，p，q，r和s独立地相同或不同，为0,1或2; 其中r + s和m + o各自等于2; 其中，如果j是0，p + q是2; 其中，如果j为1，则p为1，q为0且R6为H; 并且其中*表示D或L构型。本发明还提供了一种合成化合物的方法。本发明的另一方面涉及一种治疗受病原体与谷氨酸受体的结合相关疾病的受试者的治疗方法。

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