专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 发明授权

US5889006A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5889006A
公开(公告)日：1999-03-30
申请号：US700628
申请日：1996-08-08
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02 , C07D403/02 , C07D403/14
CPC分类号： C07D405/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物）其中R，R 1，R 2，R 3，R 4，R 21，R 27 R28，X，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱性拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

4. 发明授权

US6043255A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US6043255A
公开(公告)日：2000-03-28
申请号：US266079
申请日：1999-03-10
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02
CPC分类号： C07D405/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

5. 发明授权

US5440033A Indolyl-, pyrrolyl- and pyrazolyl substituted benzazepines 失效
标题翻译：吲哚基，吡咯基和吡唑基取代的苯并氮杂
公开(公告)号：US5440033A
公开(公告)日：1995-08-08
申请号：US149411
申请日：1993-11-09
申请人： Joel G. Berger , Joseph A. Kozlowski , Wei Chang
发明人： Joel G. Berger , Joseph A. Kozlowski , Wei Chang
IPC分类号： C07D403/04 , C07D521/00 , A61K31/55
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/04
摘要： Disclosed herein are compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein Ar, R, X, and Y are as described herein are described. The compounds are useful for treating psychoses and depression and for providing analgesia. Compositions containing the compounds and methods for producing the compounds are also disclosed.
摘要翻译：本文公开了式I化合物及其药学上可接受的盐，其中Ar，R，X和Y如本文所述。该化合物可用于治疗精神病和抑郁症并提供止痛。还公开了含有化合物的组合物和用于制备化合物的方法。

6. 发明授权

US08178553B2 Compounds for the treatment of inflammatory disorders 有权
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US08178553B2
公开(公告)日：2012-05-15
申请号：US12690633
申请日：2010-01-20
申请人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Shankar B. Bandarpalle , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Aneta Maria Kosinski , Seong-Heon Kim , De-Yi Yang , Razia K. Rizvi
发明人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Shankar B. Bandarpalle , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Aneta Maria Kosinski , Seong-Heon Kim , De-Yi Yang , Razia K. Rizvi
IPC分类号： A61K31/4178 , A61K31/437 , A61K31/4439 , A61P3/00 , A61P29/00 , A61P11/00 , C07D491/048 , C07D471/04 , C07D401/14 , C07D403/06
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
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, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症。

7. 发明申请

US20120010181A1 COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS 失效
标题翻译：用于治疗炎症性疾病的化合物
公开(公告)号：US20120010181A1
公开(公告)日：2012-01-12
申请号：US13127952
申请日：2009-11-09
申请人： Joseph A. Kozlowski , Wensheng Yu , Michael K.C. Wong , Seong Heon Kim , Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , De-Yi Yang , Robert Feltz , Aneta Maria Kosinski , Guowei Zhou , Razia K. Rizvi , Chaoyang Dai , Luke Fire , Vinay Girijavallabhan , Dansu Li , Janeta Popovici-Muller , Judson E. Richard , Kristen E. Rosner , M. Arshad Siddiqui , Liping Yang
发明人： Joseph A. Kozlowski , Wensheng Yu , Michael K.C. Wong , Seong Heon Kim , Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , De-Yi Yang , Robert Feltz , Aneta Maria Kosinski , Guowei Zhou , Razia K. Rizvi , Chaoyang Dai , Luke Fire , Vinay Girijavallabhan , Dansu Li , Janeta Popovici-Muller , Judson E. Richard , Kristen E. Rosner , M. Arshad Siddiqui , Liping Yang
IPC分类号： A61K31/4178 , C07D401/14 , C07D491/052 , C07D413/14 , C07D417/14 , C07D403/14 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/436 , A61K31/5377 , A61K31/541 , A61K31/551 , A61P29/00 , A61P19/02 , A61P1/02 , A61P35/00 , A61P35/04 , A61P25/00 , A61P27/06 , A61P1/00 , A61P17/06 , A61P9/00 , A61P31/18 , A61P31/04 , C07D403/06
CPC分类号： C07D403/14
摘要： This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer 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：本发明涉及式（I）的化合物：（化学式应该插在这里，它以纸的形式出现）（I）或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚蛋白聚糖蛋白聚糖酶，TNF-或其组合介导的疾病或病症。

8. 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。

9. 发明申请

US20090156586A1 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：US20090156586A1
公开(公告)日：2009-06-18
申请号：US12364845
申请日：2009-02-03
申请人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Bandarpalle B. Shankar , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong Heon Kim
发明人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Bandarpalle B. Shankar , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong Heon Kim
IPC分类号： A61K31/4178 , C07D403/06 , C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14 , C07D413/14 , A61K31/427 , A61K31/517 , A61K31/54 , A61K31/5377 , A61K31/4725 , A61K31/4709 , A61K31/4439 , A61K31/506
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
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, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症。

10. 发明申请

US20090111803A1 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：US20090111803A1
公开(公告)日：2009-04-30
申请号：US12338353
申请日：2008-12-18
申请人： Wensheng Yu , Ling Tong , Lei Chen , Joseph A. Kozlowski , Brian J. Lavey , Neng-Yang Shih , Vincent S. Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael K.C. Wong , De-Yi Yang , Seong Heon Kim , Bandarpalle B. Shankat
发明人： Wensheng Yu , Ling Tong , Lei Chen , Joseph A. Kozlowski , Brian J. Lavey , Neng-Yang Shih , Vincent S. Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael K.C. Wong , De-Yi Yang , Seong Heon Kim , Bandarpalle B. Shankat
IPC分类号： A61K31/5377 , C07D233/02 , A61K31/4178 , C07D403/02 , C07D277/20 , A61K31/426 , C07D401/14 , A61K31/4709 , A61P19/02 , A61P37/00 , A61P9/00 , A61P29/00 , A61K31/4545 , C07D215/00 , A61K31/4439 , C07D403/14 , A61K31/506 , A61K31/497 , C07D413/14
CPC分类号： C07D401/14 , C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14
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, ADAMs, TACE, TNF—or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，TNF-或其组合介导的疾病或病症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式