Patents by Inventor Alexander Pasternak
Alexander Pasternak 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: 20190144432Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.Type: ApplicationFiled: January 10, 2019Publication date: May 16, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
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Patent number: 10227331Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.Type: GrantFiled: June 24, 2016Date of Patent: March 12, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, David Hunter, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu, Yunfeng Bai, Zhixiang Zheng, Xu Zhang
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Patent number: 10221163Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.Type: GrantFiled: June 24, 2016Date of Patent: March 5, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
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Patent number: 10208064Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: July 9, 2015Date of Patent: February 19, 2019Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinlong Jiang, Shuzhi Dong, Xin Gu, Takao Suzuki, Joseph P. Vacca, Zhifa Pu, Shouning Xu
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Patent number: 10160751Abstract: The present invention provides compounds of Formula (I); and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: February 8, 2016Date of Patent: December 25, 2018Inventors: Alexander Pasternak, Jessica Frie, Shuzhi Dong, Takao Suzuki, Shouning Xu
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Publication number: 20180244656Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.Type: ApplicationFiled: June 24, 2016Publication date: August 30, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu
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Publication number: 20180179190Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.Type: ApplicationFiled: June 24, 2016Publication date: June 28, 2018Applicant: Marck Sharp & Dohme Corp.Inventors: Frank Bennett, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Xin Gu, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Yuhua Huang, David Hunter, Dexi Yang, Katherine Young, Li Xiao, Zhibo Zhang, Jianmin Fu, Yunfeng Bai, Zhixiang Zheng, Xu Zhang
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Patent number: 9951052Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: October 27, 2014Date of Patent: April 24, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Haifeng Tang, Jessica Frie, Ronald Dale Ferguson, Zhiqiang Guo, Zhi-Cai Shi, Brian Cato, Qinghong Fu
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Patent number: 9926317Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: July 9, 2015Date of Patent: March 27, 2018Assignee: Merck Sharp Dohme Corp.Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinglong Jiang, Shuzhi Dong, Xin Gu
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Publication number: 20180016263Abstract: The present invention provides compounds of Formula (I); and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: ApplicationFiled: February 8, 2016Publication date: January 18, 2018Inventors: Alexander Pasternak, Jessica Frie, Shuzhi Dong, Takao Suzuki, Shouning Xu
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Patent number: 9850245Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: October 26, 2015Date of Patent: December 26, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Fa-Xiang Ding, Shuzhi Dong, Jinlong Jiang, Haifeng Tang, Xin Gu, Reynalda K. DeJesus, Jessica Frie, Qinghong Fu, Takao Suzuki, Zhifa Pu
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Patent number: 9839629Abstract: Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: December 19, 2014Date of Patent: December 12, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Shuzhi Dong, Alexander Pasternak, Xin Gu, Qinghong Fu, Jinlong Jiang, Fa-Xiang Ding, Haifeng Tang, Reynalda K. DeJesus, Takao Suzuki
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Patent number: 9839642Abstract: The present invention relates to compounds of formula I that are metallo-?-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with ?-lactam antibiotics for overcoming resistance.Type: GrantFiled: May 4, 2015Date of Patent: December 12, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Haifeng Tang, Shu-Wei Yang, Mihir Mandal, Jing Su, Guoqing Li, Weidong Pan, Haiqun Tang, Reynalda DeJesus, Jianping Pan, William Hagmann, Fa-Xiang Ding, Li Xiao, Alexander Pasternak, Yuhua Huang, Shuzhi Dong, Dexi Yang
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Patent number: 9777002Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: GrantFiled: November 22, 2013Date of Patent: October 3, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Shawn P. Walsh, Brian Cato, Jessica L. Frie, Dooseop Kim, Alexander Pasternak, Zhi-Cai Shi
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Publication number: 20170275302Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: ApplicationFiled: October 9, 2015Publication date: September 28, 2017Inventors: Alexander Pasternak, Barbara Pio, Harry Chobanian, Zhi-Cai Shi, Shuzhi Dong, Yan Guo, Shawn P. Walsh, Zhiqiang Guo, Ronald D. Ferguson II, Brian Cato
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Publication number: 20170275283Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: ApplicationFiled: October 26, 2015Publication date: September 28, 2017Inventors: Alexander Pasternak, Fa-Xiang Ding, Shuzhi Dong, Jinlong Jiang, Haifeng Tang, Xin Gu, Reynalda K. DeJesus, Jessica Frie, Qinghong Fu, Takao Suzuki, Zhifa Pu
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Publication number: 20170275298Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: ApplicationFiled: October 26, 2015Publication date: September 28, 2017Inventors: Alexander Pasternak, Shuzhi Dong, Xin Gu, Jinlong Jiang, Zhi-Cai Shi, Shawn P. Walsh, Zhicai Wu, Yang Yu, Ronald Ferguson, II, Zhiqiang Guo, Jessica Frie, Takao Suzuki, Timothy A. Blizzard, Qinghong Fu, Kelsey F. Vangelder
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Patent number: 9765074Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: March 10, 2014Date of Patent: September 19, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Fa-Xiang Ding, Shuzhi Dong, Dipshikha Biswas, Haifeng Tang, Jinlong Jiang, Cangming Yang, Xin Gu
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Patent number: 9751881Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: July 28, 2014Date of Patent: September 5, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Haifeng Tang, Barbara Pio, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Ronald Dale Ferguson, II, Zack Zhiqiang Guo, Harry Chobanian, Jessica Frie, Yan Guo, Zhicai Wu, Yang Yu, Ming Wang
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Patent number: 9718808Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: GrantFiled: January 5, 2015Date of Patent: August 1, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Dipshikha Biswas, Fa-Xiang Ding, Shuzhi Dong, Xin Gu, Jinlong Jiang, Alexander Pasternak, Takao Suzuki, Joseph Vacca, Shouning Xu