Patents by Inventor Michael Berlin
Michael Berlin 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).
-
Publication number: 20200085793Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of ?-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: August 20, 2019Publication date: March 19, 2020Inventors: Andrew P. Crew, Hanqing Dong, Michael Berlin, Steven M. Sparks
-
Publication number: 20200055825Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.Type: ApplicationFiled: October 17, 2019Publication date: February 20, 2020Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Xin Chen, Yimin Qian, Kurt Zimmermann, Craig M. Crews, Michael Berlin, Lawrence Snyder
-
Publication number: 20200038378Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: October 1, 2019Publication date: February 6, 2020Inventors: ANDREW P. CREW, Jing Wang, Michael Berlin, Peter Dragovich, Huifen Chen, Leanna Staben
-
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
-
Publication number: 20190315732Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: April 4, 2019Publication date: October 17, 2019Inventors: Andrew P. Crew, Keith R. Hornberger, Jing Wang, Hanging Dong, Michael Berlin, Craig M. Crews
-
Publication number: 20190300521Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: April 1, 2019Publication date: October 3, 2019Inventors: Andrew P. Crew, Jing Wang, Michael Berlin, Peter Dragovich, Huifen Chen, Leanna Staben
-
Publication number: 20180346461Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.Type: ApplicationFiled: July 27, 2018Publication date: December 6, 2018Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Xin Chen, Yimin Qian, Kurt Zimmermann, Craig M. Crews, Michael Berlin, Lawrence Snyder
-
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
-
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
-
Publication number: 20180228907Abstract: The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.Type: ApplicationFiled: April 13, 2018Publication date: August 16, 2018Inventors: Andrew P. Crew, Craig M. Crews, Hanqing Dong, Keith R. Hornberger, Jing Wang, Yimin Qian, Kurt Zimmermann, Michael Berlin, Lawrence B. Snyder
-
Publication number: 20180215731Abstract: The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.Type: ApplicationFiled: January 31, 2018Publication date: August 2, 2018Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Keith R. Homberger, Yimin Qian, Lawrence B. Snyder, Jing Wang, Kurt Zimmermann
-
Publication number: 20180193314Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 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: June 6, 2016Publication date: July 12, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Junying Zheng, Walter Won, Michael Berlin, Pauline Ting, Guoqing Li, Dong Xiao, Hongwu Wang, Robert Aslanian
-
Publication number: 20180193470Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: December 22, 2017Publication date: July 12, 2018Inventors: Andrew P. Crew, Kurt Zimmermann, Jing Wang, Michael Berlin, Hanqing Dong, Alexey Ishchenko, Yimin Qian, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
-
Publication number: 20180177750Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: December 21, 2017Publication date: June 28, 2018Inventors: Andrew P. Crew, Lawrence B. Snyder, Jing Wang, Hanqing Dong, Yimin Qian, Michael Berlin
-
Publication number: 20180125821Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: November 1, 2017Publication date: May 10, 2018Inventors: Andrew P. Crew, Michael Berlin, John J. Flanagan, Hanqing Dong, Alexey Ishchenko
-
Publication number: 20180099940Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.Type: ApplicationFiled: October 11, 2017Publication date: April 12, 2018Inventors: Andrew P. Crew, Keith R. Hornberger, Lawrence B. Snyder, Kurt Zimmermann, Jing Wang, Michael Berlin, Craig M. Crews, Hanqing Dong
-
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
-
Patent number: 9676780Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” 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: December 20, 2013Date of Patent: June 13, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Michael Berlin, Pauline Ting, Gang Zhou, Tao Yu, Christopher Boyce, Joseph Michael Kelly, Jayaram R. Tagat, Junying Zheng, Xianhai Huang, Wei Zhou, Jae-Hun Kim, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Rajan Anand, Qiaolin Deng
-
Patent number: 9642746Abstract: Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.Type: GrantFiled: February 26, 2014Date of Patent: May 9, 2017Inventor: Michael Berlin
-
Publication number: 20170119579Abstract: Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.Type: ApplicationFiled: February 26, 2014Publication date: May 4, 2017Inventor: Michael Berlin