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31. 发明授权

US08450355B2 Compounds for the treatment of inflammatory diseases 有权
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US08450355B2
公开(公告)日：2013-05-28
申请号：US13120730
申请日：2009-09-22
申请人： Michael K. C. Wong , Wensheng Yu , Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , Joseph A. Kozlowski , Seong Heon Kim , Guowei Zhou , De-Yi Yang , Razia K. Rizvi , Lei Chen , Aneta Maria Kosinzki , Kristin E. Rosner , Luke Fire , Judson E. Richard , Dansu Li
发明人： Michael K. C. Wong , Wensheng Yu , Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , Joseph A. Kozlowski , Seong Heon Kim , Guowei Zhou , De-Yi Yang , Razia K. Rizvi , Lei Chen , Aneta Maria Kosinzki , Kristin E. Rosner , Luke Fire , Judson E. Richard , Dansu Li
IPC分类号： A61K31/4166 , A61K31/4178 , C07D233/02
CPC分类号： C07D405/14 , C07D403/06 , C07D403/14 , C07D491/048
摘要： This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α combinations thereof.
摘要翻译：本发明涉及如本文定义的式（I） - （IX）：或其药学上可接受的盐，溶剂合物或酯的化合物，其可用于治疗由MMP，ADAM，TACE介导的疾病或病症，聚集蛋白聚糖酶，其TNF-α组合。

32. 发明申请

US20110288054A1 COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS 有权
标题翻译：用于治疗炎症性疾病的化合物
公开(公告)号：US20110288054A1
公开(公告)日：2011-11-24
申请号：US13120728
申请日：2009-09-22
申请人： Bandarpalle B. Shankar , Seong Heon Kim , Wensheng Yu , Ling Tong , Michael K.C. Wong , Brian J. Lavey , Joseph A. Kozlowski , Lei Chen , Razia K. Rizvi , Aneta Maria Kosinski , De-Yi Yang , Guowei Zhou , Kristen E. Rosner , Luke Fire , Judson E. Richard , Dansu Li
发明人： Bandarpalle B. Shankar , Seong Heon Kim , Wensheng Yu , Ling Tong , Michael K.C. Wong , Brian J. Lavey , Joseph A. Kozlowski , Lei Chen , Razia K. Rizvi , Aneta Maria Kosinski , De-Yi Yang , Guowei Zhou , Kristen E. Rosner , Luke Fire , Judson E. Richard , Dansu Li
IPC分类号： A61K31/675 , A61K31/4355 , A61K31/5377 , A61K31/496 , C07F9/6561 , A61K31/4178 , C07D403/14 , C07D403/06 , A61K31/513 , C07D405/14 , A61K31/4741 , C07D401/14 , A61K31/4439 , A61P29/00 , C07D491/048
CPC分类号： C07D403/14 , C07D403/06 , C07D405/14 , C07D491/048
摘要： This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
摘要翻译：本发明涉及本文所述的式（I）化合物或其药学上可接受的盐，溶剂化物或酯，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-或介导的疾病或病症其组合。

33. 发明授权

US07645774B2 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US07645774B2
公开(公告)日：2010-01-12
申请号：US11197979
申请日：2005-08-05
申请人： Richard J. Friary , Joseph A. Kozlowski , Bandarpalle B. Shankar , Michael K. C. Wong , Guowei Zhou , Brian J. Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youheng Shu
发明人： Richard J. Friary , Joseph A. Kozlowski , Bandarpalle B. Shankar , Michael K. C. Wong , Guowei Zhou , Brian J. Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youheng Shu
IPC分类号： A61K31/445 , C07D211/26
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。

34. 发明授权

US07071213B2 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US07071213B2
公开(公告)日：2006-07-04
申请号：US10292778
申请日：2002-11-12
申请人： Richard J. Friary , Joseph A. Kozlowski , Bandarpalle B. Shankar , Michael K. C. Wong , Guowei Zhou , Brian J. Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youheng Shu
发明人： Richard J. Friary , Joseph A. Kozlowski , Bandarpalle B. Shankar , Michael K. C. Wong , Guowei Zhou , Brian J. Lavey , Neng-Yang Shih , Ling Tong , Lei Chen , Youheng Shu
IPC分类号： A61K31/445 , C07D401/12
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。

35. 发明授权

US08361959B2 Spiro-imidazolone derivatives as glucagon receptor antagonists 有权
标题翻译：螺 - 咪唑啉酮衍生物作为胰高血糖素受体拮抗剂
公开(公告)号：US08361959B2
公开(公告)日：2013-01-29
申请号：US13121725
申请日：2009-09-30
申请人： Andrew Stamford , Michael W. Miller , Duane Eugene DeMong , William J. Greenlee , Joseph A. Kozlowski , Brian J. Lavey , Michael K. C. Wong , Wensheng Yu , Xing Dai , De-Yi Yang , Guowei Zhou
发明人： Andrew Stamford , Michael W. Miller , Duane Eugene DeMong , William J. Greenlee , Joseph A. Kozlowski , Brian J. Lavey , Michael K. C. Wong , Wensheng Yu , Xing Dai , De-Yi Yang , Guowei Zhou
IPC分类号： A61F7/10 , A61K31/4184 , C07D235/02
CPC分类号： C07D235/02 , A61K31/4184 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K2300/00
摘要： The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：（I）其中环A，环B，R 1，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，和涉及使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之有关的病症的方法。

36. 发明申请

US20110178007A1 SPIRO-IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS 有权
标题翻译： SPIRO-IMIDAZOLONE衍生物作为GLUCAGON受体拮抗剂
公开(公告)号：US20110178007A1
公开(公告)日：2011-07-21
申请号：US13121725
申请日：2009-09-30
申请人： Andrew Stamford , Michael W Miller , Duane Eugene Demong , William J Greenlee , Joseph A Kozlowski , Brian J Lavey , Michael K.C. Wong , Wensheng Yu , Xing Dai , De-Yi Yang , Guowei Zhou
发明人： Andrew Stamford , Michael W Miller , Duane Eugene Demong , William J Greenlee , Joseph A Kozlowski , Brian J Lavey , Michael K.C. Wong , Wensheng Yu , Xing Dai , De-Yi Yang , Guowei Zhou
IPC分类号： A61K31/4184 , C07D235/02 , C07D403/12 , C07D491/107 , A61K31/4188 , C07D401/14 , A61K31/4439 , C07F7/10 , A61K31/695 , C07D405/14 , C07D405/04 , A61K31/4709 , A61K38/28 , A61K38/16 , A61K38/22 , A61K31/7034 , A61K31/70 , A61K31/7048 , A61P3/10
CPC分类号： C07D235/02 , A61K31/4184 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K2300/00
摘要： The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：（I）其中环A，环B，R 1，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，和涉及使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之有关的病症的方法。

37. 发明申请

US20130012434A1 NOVEL SPIRO IMIDAZOLONES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂，组合物及其使用方法的新型SPIRO咪唑烷
公开(公告)号：US20130012434A1
公开(公告)日：2013-01-10
申请号：US13636244
申请日：2011-03-22
申请人： Michael K. Wong , Brian J. Lavey , Wensheng Yu , Joseph A. Kozlowski , Duanc E. DeMong , Xing Dai , Andrew W. Stamford , Michael W. Miller , Guowei Zhou , De-Yi Yang , William J. Greenlee
发明人： Michael K. Wong , Brian J. Lavey , Wensheng Yu , Joseph A. Kozlowski , Duanc E. DeMong , Xing Dai , Andrew W. Stamford , Michael W. Miller , Guowei Zhou , De-Yi Yang , William J. Greenlee
IPC分类号： A61K31/4184 , C07D235/02 , C07D471/10 , A61K31/438 , C07F7/10 , A61K31/695 , C07D491/107 , C07D487/10 , A61K31/4188 , C07D403/14 , A61K31/497 , A61K31/506 , C07D487/04 , A61K31/4985 , A61K38/28 , A61P3/10 , A61K38/17 , A61K38/26 , A61K31/7034 , A61K31/7048 , A61P3/04 , A61P3/06 , A61P9/10 , C07D403/12
CPC分类号： C07D403/12 , C07D233/70 , C07D401/10 , C07D405/10 , C07F7/0812
摘要： The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：其中环A，环B，R 1，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，以及使用该化合物作为胰高血糖素受体拮抗剂，并用于治疗或预防2型糖尿病及与此有关的病症。

38. 发明申请

US20130012493A1 NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂，组合物及其使用方法的新型SPIRO咪达唑仑衍生物
公开(公告)号：US20130012493A1
公开(公告)日：2013-01-10
申请号：US13636276
申请日：2011-03-22
申请人： He Zhao , Ping Chen , Peishan Lin , Peng Dai , Jason Louis Davis , Duane E. DeMong , Michael W. Miller , Xing Dai , Michael K. Wong , Brian J. Lavey , Wensheng Yu , Guowei Zhou , Andrew W. Stamford , Joseph A. Kozlowski , William J. Greenlee
发明人： He Zhao , Ping Chen , Peishan Lin , Peng Dai , Jason Louis Davis , Duane E. DeMong , Michael W. Miller , Xing Dai , Michael K. Wong , Brian J. Lavey , Wensheng Yu , Guowei Zhou , Andrew W. Stamford , Joseph A. Kozlowski , William J. Greenlee
IPC分类号： A61K31/454 , A61P3/10 , C07D403/12 , A61K31/4178 , A61K31/5386 , A61K31/55 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D498/08 , C07D401/14 , C07D403/14
CPC分类号： C07D403/12 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14 , C07D491/08 , C07D498/08
摘要： The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及通式（I）的化合物：其中环A，环B，G，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，和涉及使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之有关的病症的方法。

39. 发明授权

US5530125A Synthesis of .alpha.-substituted-aryl ethylamines 失效
标题翻译： α-取代的芳基乙胺的合成
公开(公告)号：US5530125A
公开(公告)日：1996-06-25
申请号：US290894
申请日：1994-08-19
申请人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
发明人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
IPC分类号： C07D217/24 , A61K31/55 , A61P25/00 , A61P25/18 , B01J31/24 , C07B61/00 , C07C231/12 , C07D209/34 , C07D213/56 , C07D223/16 , C07D225/06 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/24 , C07D491/056
CPC分类号： C07D223/16
摘要： A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.
摘要翻译： PCT No.PCT / US93 / 01425 Sec。 371日期：1994年8月19日 102（e）日期1994年8月19日PCT提交1993年2月23日PCT公布。公开号WO93 / 16997 日期：1993年9月2日。一种制备α-取代芳基乙酰胺的新方法，其中取代基是芳基或1-烯基或1-环烯基，其中氮原子不携带氢原子包括芳基乙酰胺在α-碳原子上具有一个或两个氢原子，其中氮原子不携带氢原子，在惰性非质子有机溶剂中具有强碱，随后与零价过渡金属催化剂反应，然后与式 R4-X，其中R4选自芳族基团，1-烯基和1-环烯基，X是特定的离去基团，特别是三氟甲磺酸酯基团。 α-取代的芳基乙酰胺可用作制备（通过还原）具有药理活性的α-取代的芳基乙胺，例如1-取代-2,3,4,5-四氢-1H-3-苯并氮杂的中间体。其中1-取代基R4是1-（1-环烯基）的某些苯并氮杂是新的。

40. 发明授权

US5241065A 2,3,4,5-tetrahydro-1H-3-benzazepines having anti-psychotic activity 失效
标题翻译：具有抗肌动蛋白活性的2,3,4,5-四氢-1H-苯并嗪
公开(公告)号：US5241065A
公开(公告)日：1993-08-31
申请号：US841603
申请日：1992-02-25
申请人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
发明人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
IPC分类号： C07D217/24 , A61K31/55 , A61P25/00 , A61P25/18 , B01J31/24 , C07B61/00 , C07C231/12 , C07D209/34 , C07D213/56 , C07D223/16 , C07D225/06 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/24 , C07D491/056
CPC分类号： C07D223/16
摘要： A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.
摘要翻译：用于制备α-取代的芳基乙酰胺的新方法，其中取代基是芳基或1-烯基或1-环烯基，其中氮原子不携带氢原子包括具有一个或两个氢原子的芳基乙酰胺与其中氮原子不携带氢原子，在惰性非质子有机溶剂中具有强碱，然后与零价过渡金属催化剂反应，然后与式R 4 -X的化合物反应，其中R 4为选自芳族基团，1-烯基和1-环烯基，X是特定的离去基团，特别是三氟甲磺酸酯基团。 α-取代的芳基乙酰胺可用作制备（通过还原）具有药理活性的α-取代的芳基乙胺，例如1-取代-2,3,4,5-四氢-1H-3-苯并氮杂的中间体。其中1-取代基R4是1-（1-环烯基）的某些苯并氮杂是新的。

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