Patents by Inventor Yongxin Han
Yongxin Han 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: 12291538Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: GrantFiled: May 3, 2023Date of Patent: May 6, 2025Assignee: Merck Sharp & Dohme LLCInventors: Indu Bharathan, Symon Gathiaka, Yongxin Han, Xiaoshen Ma, Ryan D. Otte, David L. Sloman, Thomas H. Graham, Timothy Henderson, Elisabeth Hennessy, Anandan Palani
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Publication number: 20250120961Abstract: Disclosed are p53 modulators represented by the following structural formula I: The variables in structural formula I are described herein. Also disclosed are method of treating cancer in a subject with the disclosed p53 modulators, particularly cancers with dysfunctional p53.Type: ApplicationFiled: June 27, 2024Publication date: April 17, 2025Inventors: David Belanger, Yongxin Han, Jeffrey Hale, Daniel F. Ortwine, Aysegul Ozen, Matthew Hurley, Kamran Haider, Mark E. Fitzgerald, Michael Hale
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Patent number: 12275729Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: October 29, 2018Date of Patent: April 15, 2025Assignee: Merck Sharp & Dohme LLCInventors: Yongqi Deng, Abdelghani Achab, David Jonathan Bennett, Indu Bharathan, Xavier Fradera, Craig Gibeau, Yongxin Han, Derun Li, Kun Liu, Qinglin Pu, Sulagna Sanyal, David Sloman, Wensheng Yu, Hongjun Zhang
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Patent number: 12264134Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: November 25, 2019Date of Patent: April 1, 2025Assignee: Merck Sharp & Dohme LLCInventors: Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Xianhai Huang, Joseph Kozlowski, Guoqing Li, Theodore A. Martinot, Alexander Pasternak, Andreas Verras, Li Xiao, Feng Ye, Wensheng Yu, Rui Zhang
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Patent number: 12264139Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Nonalcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.Type: GrantFiled: June 10, 2021Date of Patent: April 1, 2025Assignee: Merck Sharp & Dohme LLCInventors: Yongxin Han, Jongwon Lim, Satyanarayana Tummanapalli, Phieng Siliphaivanh, Kerrie Spencer
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Patent number: 12157727Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: June 8, 2020Date of Patent: December 3, 2024Assignee: Merck Sharp & Dohme LLCInventors: Yongxin Han, Yongqi Deng, Hua Zhou, Meredeth A. McGowan, Hongjun Zhang, Wensheng Yu, Brett A. Hopkins, Xavier Fradera, Nunzio Sciammetta
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Patent number: 12152019Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: October 11, 2019Date of Patent: November 26, 2024Assignee: Merck Sharp & Dohme LLCInventors: Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Jongwon Lim, Theodore A. Martinot, Alexander Pasternak, Li Xiao, Wensheng Yu
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Patent number: 12091405Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: October 28, 2019Date of Patent: September 17, 2024Assignee: Merck Sharp & Dohme LLCInventors: Dane Clausen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Guoqing Li, Theodore A. Martinot, Alexander Pasternak, David Sloman, Li Xiao, Wensheng Yu, Rui Zhang
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Patent number: 12065438Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: November 1, 2019Date of Patent: August 20, 2024Assignee: Merck Sharp & Dohme LLCInventors: Yongxin Han, David Jonathan Bennett, Indu Bharathan, Liangqin Guo, Brett A. Hopkins, Xianhai Huang, Derun Li, Min Lu, Alexander Pasternak, David L. Sloman, Hongjun Zhang, Hua Zhou
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Publication number: 20240262842Abstract: Compounds of Formula (I) or (Ia) or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or (Ia) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: April 27, 2022Publication date: August 8, 2024Inventors: Kazuaki SHIBATA, Hiroki Asakura, Kei AKEMOTO, Toshihiro SAKAMOTO, Hitomi KONDO, Tomohiro YAMAMOTO, Risako MIURA, Patrick SCHÖPF, Juan DEL POZO, George Madalin GIAMBUSU, Thomas H. GRAHAM, Yongxin HAN, Elisabeth T. HENNESSY, Anandan PALANI, Michael RYAN, David L. Sloman, Steven HOWARD
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Publication number: 20240246968Abstract: Compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: April 27, 2022Publication date: July 25, 2024Inventors: Kazuaki SHIBATA, Hitomi KONDO, Tomohiro YAMAMOTO, Toshihiro SAKAMOTO, Hiroki ASAKURA, Kei AKEMOTO, Risako MIURA, Tetsuya SUGIMOTO, Juan DEL POZO, George Madalin GIAMBUSU, Thomas H. GRAHAM, Yongxin HAN, Elisabeth T. HENNESSY, Shuhei KAWAMURA, Michael RYAN
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Publication number: 20240239788Abstract: Compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: April 15, 2022Publication date: July 18, 2024Inventors: David L. Sloman, Gianni Chessari, Patrick Schöpf, Steven Howard, Yuichi Kawai, Kazuaki Shibata, Hiroki Asakura, Takao Uno, Takeshi Sagara, Masayuki Nakamura, Yu Kobayakawa, David Jonathan Bennett, Indu Bharathan, Thomas H. Graham, Yongxin Han, Zahid Hussain, Xiaoshen Ma, Mihir Mandal, Ryan D. Otte, Anandan Palani, Uma Swaminathan, Mycah Uehling, Yingchun Ye, Ryan Chau, Alec H. Christian, Symon Gathiaka, Timothy J. Henderson, Elisabeth T. Hennessy, Andrew J. Hoover, Shuhei Kawamura, Igri Kolaj, Thomas W. Lyons, Matthew J. Mitcheltree, Aaron Sather
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Patent number: 11992489Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: August 12, 2019Date of Patent: May 28, 2024Assignee: Merck Sharp & Dohme LLCInventors: Dane Clausen, Xavier Fradera, Yongxin Han, Alexander Pasternak, Li Xiao, Hongjun Zhang
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Publication number: 20240124478Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, CS, R2, and R3 are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: November 23, 2021Publication date: April 18, 2024Inventors: Yongxin Han, Elisabeth Hennessy, Andrew J. Hoover, Jesus Moreno, David L. Sloman, Uma Swaminathan, Yingchun Ye
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Publication number: 20240083913Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, CY, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: May 3, 2023Publication date: March 14, 2024Inventors: Indu Bharathan, Symon Gathiaka, Yongxin Han, Xiaoshen Ma, Ryan D. Otte, David L. Sloman, Thomas H. Graham, Timothy Henderson, Elisabeth Hennessy, Anandan Palani
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Publication number: 20240043448Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: May 3, 2023Publication date: February 8, 2024Inventors: Indu Bharathan, Symon Gathiaka, Yongxin Han, Xiaoshen Ma, Ryan D. Otte, David L. Sloman, Thomas H. Graham, Timothy Henderson, Elisabeth Hennessy, Anandan Palani
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Publication number: 20230416266Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, CA, R1, R2a, and R2b are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: ApplicationFiled: November 23, 2021Publication date: December 28, 2023Inventors: Yongxin Han, Elisabeth Hennessy, Andrew J. Hoover, Jesus Moreno, Uma Swaminathan
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Patent number: 11697657Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.Type: GrantFiled: October 27, 2020Date of Patent: July 11, 2023Assignee: Merck Sharp & Dohme LLCInventors: Indu Bharathan, Symon Gathiaka, Yongxin Han, Xiaoshen Ma, Ryan D. Otte, David L. Sloman, Thomas H. Graham, Timothy Henderson, Elisabeth Hennessy, Anandan Palani
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Aryl and heteroaryl ether derivatives as liver X receptor beta agonists, compositions, and their use
Patent number: 11655216Abstract: In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.Type: GrantFiled: October 9, 2017Date of Patent: May 23, 2023Assignee: Merck Sharp & Dohme LLCInventors: Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu, Bin Zhu -
Publication number: 20230008022Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: ApplicationFiled: November 25, 2019Publication date: January 12, 2023Applicant: Merck Sharp & Dohme Corp.Inventors: Dane Clausen, Ping Chen, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Xianhai Huang, Joseph Kozlowski, Guoqing Li, Theodore A. Martinot, Alexander Pasternak, Andreas Verras, Li Xiao, Feng Ye, Wensheng Yu, Rui Zhang