Patents by Inventor Gaifa Lai
Gaifa Lai has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8829036Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 14, 2012Date of Patent: September 9, 2014Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Inc.Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Patent number: 8691833Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 8, 2012Date of Patent: April 8, 2014Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Inc.Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X.E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Patent number: 8691831Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 9, 2012Date of Patent: April 8, 2014Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120276118Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 14, 2012Publication date: November 1, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X.E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120231017Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: ZHAONING ZHU, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mozzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Sainoz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120231018Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mozzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20110213029Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: ApplicationFiled: May 6, 2011Publication date: September 1, 2011Applicants: Schering Corporation, Pharmacopeia Drug DiscoveryInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, JR., Laura L. Rokosz, Gaifa Lai, James P. Jakway, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
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Patent number: 7964646Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: August 8, 2006Date of Patent: June 21, 2011Assignees: Schering Corporation, Pharmacopeia Drug DiscoveryInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Jr., Laura L. Rokosz, Gaifa Lai
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Patent number: 7763609Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: February 23, 2007Date of Patent: July 27, 2010Assignees: Schering Corporation, Pharmacopeia, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Patent number: 7691856Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.Type: GrantFiled: January 9, 2007Date of Patent: April 6, 2010Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Arthur G. Taveras, Jianhua Chao, Purakkattle J. Biju, Younong Yu, Cynthia J. Aki, J. Robert Merritt, Ge Li, John J. Baldwin, Gaifa Lai, Minglang Wu, Evan A. Hecker
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Patent number: 7671212Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.Type: GrantFiled: December 20, 2004Date of Patent: March 2, 2010Assignee: Schering CorporationInventors: Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Junying Zheng, Purakkattle J. Biju, Younong Yu, Jianhua Chao, Gaifa Lai, Minglang Wu
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Publication number: 20090306079Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: ApplicationFiled: January 13, 2009Publication date: December 10, 2009Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, JR., Laura L. Rokosz, Gaifa Lai, James P. Jakway, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
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Publication number: 20090281075Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed.Type: ApplicationFiled: November 7, 2008Publication date: November 12, 2009Applicant: PHARMACOPEIA, INC.Inventors: Andrew L. Roughton, Yajing Rong, Koc-Kan Ho, Michael J. Ohlmeyer, David Diller, Ray Jui-Hsiang Chan, Gaifa Lai
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Publication number: 20080200445Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula 1.Type: ApplicationFiled: February 23, 2007Publication date: August 21, 2008Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan Ye, Johannes Voigt, Corey Strickland, Elizabeth Smith, Andrew Stamford, William Greenlee, Robert Mazzola, John Caldwell, Jared Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy Le, Kurt Saionz, Suresh Babu, Rachael Hunter, Michelle Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20080045489Abstract: Disclosed are novel cyclobutenedione Compounds 1 to 18 comprising a cyclobutenedione ring, a substituted phenyl ring, and a —CH(C2H5)-furan moiety. The phenyl ring and the —CH(C2H5)-furan moiety are each bound to the cyclobutenedione ring through a —NH— moiety. Also disclosed are methods of treating chemokine mediated diseases (e.g., cancer, COPD, acute and chronic inflammatory disorders, psoriasis, cystic fibrosis, and asthma) using the novel Compounds 1 to 18.Type: ApplicationFiled: July 5, 2007Publication date: February 21, 2008Inventors: Jianhua Chao, Michael Czarniecki, Zhenmin He, Gaifa Lai, J. Merritt
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Publication number: 20070264230Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.Type: ApplicationFiled: January 9, 2007Publication date: November 15, 2007Inventors: Arthur Taveras, Jianhua Chao, Purakkattle Biju, Younong Yu, Jay Fine, William Hipkin, Cynthia Aki, J. Merritt, Ge Li, John Baldwin, Gaifa Lai, Minglang Wu, Evan Hecker
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Publication number: 20070021494Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: ApplicationFiled: August 8, 2006Publication date: January 25, 2007Inventors: Arthur Taveras, Cynthia Aki, Richard Bond, Jianping Chao, Michael Dwyer, Johan Ferreira, Jianhua Chao, Younong Yu, John Baldwin, Bernd Kaiser, Ge Li, J. Merritt, Purakkattle Biju, Kingsley Nelson, Laura Rokosz, Gaifa Lai, James Jakway, Minglang Wu, Evan Hecker, Daniel Lundell, Jay Fine
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Patent number: 7132445Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: July 30, 2003Date of Patent: November 7, 2006Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Jr., Laura L. Rokosz, James P. Jakway, Gaifa Lai, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
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Publication number: 20060025453Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.Type: ApplicationFiled: December 20, 2004Publication date: February 2, 2006Inventors: Arthur Taveras, J. Merritt, John Baldwin, Junying Zheng, Purakkattle Biju, Younong Yu, Jianhua Chao, Jay Fine, Daniel Lundell, Tony Priestley, Angelo Reggiani, Gaifa Lai, Minglang Wu
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Publication number: 20040186142Abstract: Disclosed are novel compounds of the formula: 1Type: ApplicationFiled: October 7, 2003Publication date: September 23, 2004Applicant: Schering Corporation Pharmacopeia, Inc.Inventors: Arthur G. Taveras, Jianhua Chao, Purakkattle J. Biju, Younong Yu, Jay S. Fine, William Hipkin, Cynthia J. Aki, J. Robert Merritt, Ge Li, John J. Baldwin, Gaifa Lai, Minglang Wu, Evan A. Hecker