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公开(公告)号：US20190352294A1
公开(公告)日：2019-11-21
申请号：US16461849
申请日：2017-11-13
Applicant: Ashwin RAO , Brian Alexander MCKITTRICK , Matthew LOMBARDO , Jacqueline D. HICKS , Amy Bittner MCCRACKEN , Hong Dong CHU , Sung-Sau SO , Peter ORTH , Zhicai WU , Ping LAN , John S. DEBENHAM , Brent R. WHITEHEAD , Jerry A. TAYLOR , Zhongxiang SUN , Revathi Reddy KATIPALLY , Jonathan E. GABLE , Markus K. DAHLGREN , Sathesh P. BHAT , Merck Sharp & Dohme Corp.
Inventor： Ashwin U. Rao , Brian Alexander McKittrick , Matthew Lombardo , Jacqueline D. Hicks , Amy Bittner McCracken , Hong Dong Chu , Sung-Sau So , Peter Orth , Zhicai Wu , Ping Lan , John S. Debenham , Brent R. Whitehead , Jerry A. Taylor , Zhongxiang Sun , Revathi Reddy Katipally , Jonathan E. Gable , Markus K. Dahlgren , Sathesh P. Bhat
IPC: C07D413/14 , C07D495/04 , A61P7/02
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
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公开(公告)号：US20120190696A1
公开(公告)日：2012-07-26
申请号：US13499135
申请日：2010-10-01
Applicant: Gerald W. Shipps, JR. , Clifford C. Cheng , Xioahua Huang , Abdelghani Achab , Peter Orth , Johannes H. Voigt
Inventor： Gerald W. Shipps, JR. , Clifford C. Cheng , Xioahua Huang , Abdelghani Achab , Peter Orth , Johannes H. Voigt
IPC: A61K31/519 , A61P9/00 , A61P3/00 , A61P3/10 , A61P3/04 , C07D487/04 , A61P3/06
CPC classification number: A61K31/54 , A61K45/06 , A61K2300/00
Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below:
Abstract translation: 本发明涉及作为脂肪酸结合蛋白（FABP）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关疾病的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：
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公开(公告)号：US20120122837A1
公开(公告)日：2012-05-17
申请号：US13242426
申请日：2011-09-23
Applicant: CLIFFORD CHENG , GERALD W. SHIPPS, JR. , XIAOHUA HUANG , YING HUANG , NING SHAO , ASHWIN RAO , ANANDAN PALANI , PETER ORTH , JOHANNES H. VOIGT , ROBERT J. HERR , LANA MICHELE ROSSITER , QI ZENG , XIANFENG SUN
Inventor： CLIFFORD CHENG , GERALD W. SHIPPS, JR. , XIAOHUA HUANG , YING HUANG , NING SHAO , ASHWIN RAO , ANANDAN PALANI , PETER ORTH , JOHANNES H. VOIGT , ROBERT J. HERR , LANA MICHELE ROSSITER , QI ZENG , XIANFENG SUN
IPC: A61K31/498 , A61K31/5377 , A61K31/4709 , C07D413/06 , A61K31/506 , C07D471/04 , C07D403/06 , C07D401/14 , A61K31/4985 , C07D403/14 , C07D241/44 , A61P3/04 , A61P3/10 , A61P9/10 , A61P3/06 , A61K31/55
CPC classification number: C07D403/06 , C07D241/44 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/06
Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
Abstract translation: 本发明涉及作为脂肪酸结合蛋白（“FABP”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关的化合物的用途 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量减低或空腹血糖受损。
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公开(公告)号：US07824897B2
公开(公告)日：2010-11-02
申请号：US12702760
申请日：2010-02-09
Applicant: Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey O. Strickland
Inventor： Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey O. Strickland
CPC classification number: C12N9/6489 , C07K2299/00
Abstract: The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.
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公开(公告)号：US07687527B2
公开(公告)日：2010-03-30
申请号：US12338425
申请日：2008-12-18
Applicant: 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. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Umar Faruk Mansoor , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li
Inventor： 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. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Umar Faruk Mansoor , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li
IPC: A61K31/415 , A61K31/425
CPC classification number: C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D491/04 , C07D495/04
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物，酯或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖酶，TNF-或组合介导的疾病或病症 其中。
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Patent Agency Ranking
公开(公告)号：US20090137586A1
公开(公告)日：2009-05-28
申请号：US12338445
申请日：2008-12-18
Applicant: 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. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Aneta M. Micula , Robert Feltz
Inventor： 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. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Aneta M. Micula , Robert Feltz
IPC: A61K31/5377 , C07D491/048 , A61K31/4355 , C07D413/14 , A61P1/00 , C07D403/06 , A61K31/4178
CPC classification number: C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D491/04 , C07D495/04
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物，酯或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖酶，TNF-或组合介导的疾病或病症 其中。
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7.发明授权Methods for identifying modified tumor necrosis factor-alpha converting enzyme inhibitors 失效鉴定修饰的肿瘤坏死因子-α转化酶抑制剂的方法公开(公告)号：US07529628B2
公开(公告)日：2009-05-05
申请号：US11582710
申请日：2006-10-18
Applicant: Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey O. Strickland
Inventor： Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey O. Strickland
CPC classification number: C12N9/6489 , C07K2299/00
Abstract: The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.
Abstract translation: 本发明公开了一种修饰的肿瘤坏死因子-α转化酶（TACE）催化结构域，其与天然TACE催化结构域不同，在高蛋白浓度下是稳定的。 本发明还公开了用多种抑制剂在蛋白质 - 配体复合物中产生修饰的TACE蛋白的晶体的方法。 此外，本发明公开了使用获得的蛋白质，晶体和/或三维结构来鉴定可调节TACE的酶活性的化合物的方法。
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8.发明授权Crystalline form of an n231 mutant catalytic domain of ADAM33 and methods of use thereof 失效ADAM33的n231突变体催化结构域的结晶形式及其使用方法公开(公告)号：US07285408B2
公开(公告)日：2007-10-23
申请号：US10741208
申请日：2003-12-19
Applicant: Peter Orth , Paul Reichert , Vincent S. Madison , Wenyan Wang , Jun Zou
Inventor： Peter Orth , Paul Reichert , Vincent S. Madison , Wenyan Wang , Jun Zou
CPC classification number: C12N9/6489 , A61K38/00 , C07K2299/00 , Y02A90/26
Abstract: The present invention discloses purified polypeptides that comprise an active human ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human ADAM33 catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human ADAM33. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human ADAM33 in structure based drug design to identify compounds that can modulate the enzymatic activity of human ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the human ADAMS33 catalytic domain.
Abstract translation: 本发明公开了包含活性人ADAM33催化结构域的纯化多肽。 此外，本发明公开了编码本发明多肽的核酸。 本发明还公开了生长包含活性人ADAM33催化结构域的多肽的X射线衍射晶体的方法。 本发明还公开了人ADAM33的催化结构域的结晶形式。 此外，本发明公开了在基于结构的药物设计中使用人ADAM33的X射线衍射晶体的方法来鉴定可以调节人ADAM33的酶活性的化合物。 本发明还公开了通过施用治疗量的人ADAMS33催化结构域来治疗呼吸系统疾病的方法。
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公开(公告)号：US20060276506A1
公开(公告)日：2006-12-07
申请号：US11333663
申请日：2006-01-17
Applicant: Wensheng Yu , Ling Tong , Lei Chen , Joseph Kozlowski , Brian Lavey , Neng-Yang Shih , Vincent Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael Wong , De-Yi Yang , Seong Kim , Bandarpalle Shankar , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Umar Mansoor , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li
Inventor： Wensheng Yu , Ling Tong , Lei Chen , Joseph Kozlowski , Brian Lavey , Neng-Yang Shih , Vincent Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael Wong , De-Yi Yang , Seong Kim , Bandarpalle Shankar , M. Siddiqui , Kristin Rosner , Chaoyang Dai , Umar Mansoor , Janeta Popovici-Muller , Vinay Girijavallabhan , Dansu Li
IPC: A61K31/4709 , A61K31/4245 , A61K31/4178 , C07D413/14 , C07D403/02
CPC classification number: C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D491/04 , C07D495/04
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
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10.发明授权Modified tumor necrosis factor-alpha converting enzyme and methods of use thereof 失效改良型肿瘤坏死因子-α转化酶及其使用方法公开(公告)号：US07138264B1
公开(公告)日：2006-11-21
申请号：US10444257
申请日：2003-05-21
Applicant: Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey Strickland
Inventor： Brian M. Beyer , Richard N. Ingram , Peter Orth , Corey Strickland
CPC classification number: C12N9/6489 , C07K2299/00
Abstract: The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.
Abstract translation: 本发明公开了一种修饰的肿瘤坏死因子-α转化酶（TACE）催化结构域，其与天然TACE催化结构域不同，在高蛋白浓度下是稳定的。 本发明还公开了用多种抑制剂在蛋白质 - 配体复合物中产生修饰的TACE蛋白的晶体的方法。 此外，本发明公开了使用获得的蛋白质，晶体和/或三维结构来鉴定可调节TACE的酶活性的化合物的方法。
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