Patents by Inventor Heping Wu
Heping Wu 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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Publication number: 20240092760Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.Type: ApplicationFiled: June 13, 2023Publication date: March 21, 2024Inventors: Jian QIU, Qi WEI, Matt TSCHANTZ, Heping SHI, Youtong WU, Huiling TAN, Lijun SUN, Chuo CHEN, Zhijian CHEN
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Publication number: 20240076297Abstract: The present invention provides compounds of the structural Formula (I), and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.Type: ApplicationFiled: July 22, 2021Publication date: March 7, 2024Applicant: Merck Sharp & Dohme LLCInventors: Amjad Ali, Jared N. Cumming, Manuel De Lera Ruiz, Duane DeMong, Thomas H. Graham, Elisabeth T. Hennessy, Joseph M. Kelly, Rongze Kuang, Michael Man-Chu Lo, Umar Faruk Mansoor, Jesus Moreno, Uma Swaminathan, Heping Wu, Yingchun Ye, Younong Yu
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Publication number: 20230322785Abstract: The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.Type: ApplicationFiled: July 21, 2022Publication date: October 12, 2023Applicant: Merck Sharp & Dohme LLCInventors: Amjad Ali, Christopher W. Boyce, Jared N. Cumming, Duane DeMong, Thomas H. Graham, Subrahmanyam Gudipati, Andrew J. Hoover, Xianhai Huang, Rongze Kuang, Jae-Hun Kim, Joseph M. Kelly, Yeon-Hee Lim, Michael Man-Chu Lo, Jesus Moreno, Jing Su, Heping Wu, Dong Xiao, Younong Yu, Xiaohong Zhu
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Patent number: 11332492Abstract: This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers.Type: GrantFiled: August 28, 2019Date of Patent: May 17, 2022Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Jian Liu, Heping Wu, Linghang Zhuang, Suxing Liu, Rumin Zhang, Feng He, Weikang Tao
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Publication number: 20220135539Abstract: This application discloses RAF inhibitors of the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of various disorders related to the excessive RAF activity, including cancers.Type: ApplicationFiled: November 2, 2021Publication date: May 5, 2022Inventors: Peng Zhao, Heping Wu, Linghang Zhuang, Yu Zhou, Suxing Liu, Jian Liu
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Publication number: 20220002267Abstract: Compounds of formula (I) useful as tyrosine kinase 2 (Tyk2) inhibitors, pharmaceutical compositions containing these compounds, methods of using the pharmaceutical compositions in the treatment of various disorders related to the regulation of Tyk2 activity, and methods of preparing these compounds are disclosed.Type: ApplicationFiled: June 24, 2021Publication date: January 6, 2022Inventors: Linghang Zhuang, Jian Liu, Heping Wu, Puhui Li, Yu Zhou, Suxing Liu
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Publication number: 20210253621Abstract: This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers.Type: ApplicationFiled: August 28, 2019Publication date: August 19, 2021Inventors: Jian Liu, Heping Wu, Linghang Zhuang, Suxing Liu, Rumin Zhang, Feng He, Weikang Tao
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Patent number: 11046714Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.Type: GrantFiled: August 25, 2014Date of Patent: June 29, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Ali Amjad, Gioconda V. Gallo, Timothy J. Henderson, Rongze Kuang, Yeon-Hee Lim, Michael Man-Chu Lo, Edward Metzger, Manuel de Lera Ruiz, Andrew Stamford, Paul Tempest, Brent Whitehead, Heping Wu
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Publication number: 20210053973Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: “Z” and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.Type: ApplicationFiled: December 10, 2018Publication date: February 25, 2021Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad ALI, Yeon-Hee LIM, Gioconda V. GALLO-ETIENNE, Joseph Michael KELLY, Michael BERLIN, Pauline TING, Jayaram R. TAGAT, Dong XIAO, Rongze KUANG, Heping WU, Hongwu WANG
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Patent number: 10822338Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.Type: GrantFiled: July 5, 2016Date of Patent: November 3, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu Lo, Pauline C. Ting, Andrew W. Stamford, Paul Tempest
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Patent number: 10472347Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.Type: GrantFiled: November 13, 2015Date of Patent: November 12, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Rongze Kuang, Pauline Ting, Amjad Ali, Heping Wu, Michael Berlin, Andrew Stamford, Hongwu Wang, Gang Zhou, David Kim, Qiaolin Deng, Yeon-Hee Lim, Younong Yu
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Publication number: 20180362530Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.Type: ApplicationFiled: July 5, 2016Publication date: December 20, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu LO, Pauline C. Ting, Andrew W. Stamford, Paul Tempest
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Patent number: 10138212Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.Type: GrantFiled: February 1, 2016Date of Patent: November 27, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Rongze Kuang, Yeon-Hee Lim, Michael Man-Chu Lo, Pauline C. Ting, Purakkattle Biju, Manuel de Lera Ruiz, Sylvia J. Degrado, Alexander L. Tung, Timothy J. Henderson, Liwu Hong, Jae-Hun Kim, Dong Won-Shik Kim, Joe Lee, Jie Wu, Heping Wu, Yushi Xiao, Tao Yu, Gang Zhou, Xiaohong Zhu, Kevin D. McCormick, Jayaram R. Tagat, Dong Xiao, Tanweer Khan, Jianhua Cao, Michael Berlin, Yonglian Zhang
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Publication number: 20180327385Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.Type: ApplicationFiled: November 13, 2015Publication date: November 15, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Rongze KUANG, Pauline Ting, Amjad Ali, Heping Wu, Michael Berlin, Andrew Stamford, Hongwu Wang, Gang Zhou, David Kim, Qiaolin Deng, Yeon-Hee Lim, Younong Yu
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Patent number: 10093683Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: GrantFiled: April 21, 2015Date of Patent: October 9, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Yeon-Hee Lim, Zhuyan Guo, Amjad Ali, Scott D. Edmondson, Weiguo Liu, Gioconda V. Gallo-Etienne, Heping Wu, Ying-Duo Gao, Andrew W. Stamford, Younong Yu, Nancy J. Kevin, Rajan Anand, Deyou Sha, Santhosh F. Neelamkavil, Zahid Hussain, Puneet Kumar, Remond Moningka, Joseph L. Duffy, Jiayi Xu, Yu Jiang, Anjan Chakrabarti, Hiroki Sone
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Patent number: 10081617Abstract: 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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: GrantFiled: April 11, 2016Date of Patent: September 25, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Eric Mertz, Scott D. Edmondson, Sung-Sau So, Wanying Sun, Weiguo Liu, Santhosh F. Neelamkavil, Ying-Duo Gao, Alan Hruza, Yi Zang, Amjad Ali, Rudrajit Mal, Jiafang He, Rongze Kuang, Heping Wu, Anthony K. Ogawa, Andrew F. Nolting
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Patent number: 10011615Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.Type: GrantFiled: February 2, 2017Date of Patent: July 3, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
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Publication number: 20180079743Abstract: 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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: ApplicationFiled: April 11, 2016Publication date: March 22, 2018Applicant: MERCK SHARP & DOHME CORP.Inventors: Eric Mertz, Scott D. Edmondson, Sung-Sau So, Wanying Sun, Weiguo Liu, Santhosh F. Neelamkavil, Ying-Duo Gao, Alan Hruza, Yi Zang, Amjad Ali, Rudrajit Mal, Jiafang He, Rongze Kuang, Heping Wu, Anthony K. Ogawa, Andrew F. Nolting
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Publication number: 20180037554Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.Type: ApplicationFiled: February 1, 2016Publication date: February 8, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Rongze Kuang, Yeon-Hee Lim, Michael Man-Chu Lo, Pauline C. Ting, Purakkattle Biju, Manuel de Lera Ruiz, Sylvia J. Degrado, Alexander L. Tung, Timothy J. Henderson, Liwu Hong, Jae-Hun Kim, Dong Won-Shik Kim, Joe Lee, Jie Wu, Heping Wu, Yushi Xiao, Tao Yu, Gang Zhou, Xiaohong Zhu, Kevin D. McCormick, Jayaram R. Tagat, Dong Xiao, Tanweer Khan, Jianhua Cao, Michael Berlin, Yonglian Zhang
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Patent number: 9868727Abstract: 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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: GrantFiled: July 23, 2015Date of Patent: January 16, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Sung-Sau So, Anthony K. Ogawa, Rongze Kuang, Heping Wu, Amjad Ali, Ying-Duo Gao, Yu Jiang, Chunsing Li, Tingting Yu