Patents Examined by Kahsay Habte
  • Patent number: 10851088
    Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: December 1, 2020
    Assignee: Denali Therapeutics Inc.
    Inventors: Travis Remarchuk, Anantha Sudhakar
  • Patent number: 10844073
    Abstract: Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer).
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: November 24, 2020
    Assignee: President and Fellows of Harvard College
    Inventors: Jung Hwa Lee, Yoshito Kishi, Ayumi Osawa, Zhanjie Li
  • Patent number: 10836764
    Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: November 17, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
  • Patent number: 10829460
    Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, L, X, W, Y1, Y2, Y3, and Y4 are described herein, useful as inhibitors of zinc-dependent histone deacetylases (HDACs) and in the treatment of diseases or disorders associated with HDACs.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: November 10, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Jennifer R. Thomason, Mary-Margaret Zablocki, Bingsong Han, Nicholas Barczak, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair
  • Patent number: 10829500
    Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: November 10, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Andreas Kuglstatter, Ulrike Obst Sander, Jens-Uwe Peters, Mark Rogers-Evans, Thomas Woltering, Christian Schnider, Roger Wermuth
  • Patent number: 10821115
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: February 6, 2020
    Date of Patent: November 3, 2020
    Assignee: AMGEN INC.
    Inventors: Paul E. Harrington, Kate Ashton, Sean P. Brown, Matthew R. Kaller, Todd J. Kohn, Brian Alan Lanman, Kexue Li, Yunxiao Li, Jonathan D. Low, Ana Elena Minatti, Alexander J. Pickrell, Markian M. Stec, Joshua Taygerly
  • Patent number: 10822327
    Abstract: A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: November 3, 2020
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Tao Liu, Jia Li, Yongzhou Hu, Yubo Zhou, Xiaowu Dong, Anhui Gao, Pinrao Song, Peipei Wang, Lexian Tong, Xiaobei Hu, Mingbo Su
  • Patent number: 10816552
    Abstract: A compound of formula (I): as described herein and methods and uses thereof as for mass tagging a biosensor or biologically active material.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: October 27, 2020
    Assignees: The Governing Council of the University of Toronto, University Health Network
    Inventors: Mark Nitz, Landon J. Edgar, Bradly G. Wouters, David Hedley, Lisa M. Willis, Matthew A. Lumba, Hanuel Park, Ravi N. Vellanki
  • Patent number: 10815251
    Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl or alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: October 27, 2020
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Patent number: 10807987
    Abstract: The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, pain, behavioral and psychological symptoms of dementia and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.
    Type: Grant
    Filed: March 27, 2019
    Date of Patent: October 20, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yuya Oguro, Shigemitsu Matsumoto, Takeshi Wakabayashi, Norihito Tokunaga, Taku Kamei, Mitsuhiro Ito, Satoshi Mikami, Masaki Seto, Shinji Morimoto, Shinji Nakamura, Sachie Takashima, Masataka Murakami, Masaki Daini, Makoto Kamata, Minoru Nakamura, Yasufumi Wada, Hiroyuki Kakei, Kazuaki Takami, Taisuke Tawaraishi, Jumpei Aida, Kouichi Iwanaga, Satoshi Yamamoto
  • Patent number: 10800773
    Abstract: Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: October 13, 2020
    Assignee: Integral Health, Inc.
    Inventors: Brian Raimundo, Elena S. Koltun, John Griffin, Eric Stangeland
  • Patent number: 10800748
    Abstract: The present invention provides an improved process for the manufacture (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to said salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: October 13, 2020
    Assignee: INKE, S.A.
    Inventors: Enric Capdevila Urbaneja, Juan Huguet Clotet, Pere Dalmases Barjoan
  • Patent number: 10800771
    Abstract: The present invention is related to an improved process for the preparation of dasatinib anhydrous crystalline Neat form N-6 with high purity and high yield. The present invention also relates to purification of dasatinib crystalline Neat form N-6.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: October 13, 2020
    Assignee: NATCO PHARMA LIMITED
    Inventors: Durga Prasad Konakanchi, Buchappa Gongalla, Uma Naresh Babu Kotra, Srinivasulu Sakkani, Dharmender Ragidi, Kotayyababu Sikha, Venkaiah Chowdary Nannapaneni
  • Patent number: 10792651
    Abstract: This invention relates generally to olefin metathesis catalyst compounds, to the preparation of such compounds, compositions comprising such compounds, methods of using such compounds, articles of manufacture comprising such compounds, and the use of such compounds in the metathesis of olefins and olefin compounds. The invention has utility in the fields of catalysts, organic synthesis, polymer chemistry, and industrial and fine chemicals industry.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: October 6, 2020
    Assignees: Umicore AG & Co. KG, California Institute of Technology
    Inventors: Adam M. Johns, Jessica R. Herron, Richard L. Pederson, Bryan A. Fiamengo, Jennifer A. Beerman, Tzu-Pin Lin, Crystal K. Chu, Robert H. Grubbs
  • Patent number: 10787571
    Abstract: The present invention pertains to: an oxidation color developable compound that is represented by general formula (1), that has excellent solubility in water, and that is less affected by a substance coexisting in a sample; and an oxidation color development reagent using the oxidation color developable compound. In general formula (I), R1, R2, R3, and R4 each represent a straight-chain or branched alkyl group having 1-6 carbon atoms, X represents a hydrophilic functional group, and L represents —(CH2)j— (j represents an integer of 2-10), —(CH2CH2O)k— (k represents an integer of 1-10), or —(CH2)m—Z—(CH2)n— (m and n each independently represent an integer of 1-10, and Z represents —N+(CH3)2—, —CONH—, —NHCO—, —COO—, —OCO—, —NHCOO—, —OCONH—, —NHCONH—, and —(CH2NHCO)q—).
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: September 29, 2020
    Assignee: DOJINDO LABORATORIES
    Inventors: Masaki Murai, Chiaki Matsumoto, Ryo Sakamoto, Nobuyuki Ozeki, Munetaka Ishiyama
  • Patent number: 10787454
    Abstract: The invention provides substituted imidazo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-imidazo[1,5-a]pyrimidine-8-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: September 29, 2020
    Assignee: BIAL—BioTech Investments, Inc.
    Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury, William J. Greenlee, Andrew C. Good
  • Patent number: 10781191
    Abstract: Improved processes for producing high purity acesulfame potassium. In one embodiment, the process comprises the steps of contacting a solvent, e.g., dichloromethane, and a cyclizing agent, e.g., sulfur trioxide, to form a cyclizing agent composition and reacting an acetoacetamide salt with the cyclizing agent in the composition to form a cyclic sulfur trioxide adduct. The contact time is less than 60 minutes. The process also comprises forming from the cyclic sulfur trioxide adduct composition a finished acesulfame potassium composition comprising non-chlorinated, e.g., non-chlorinated, acesulfame potassium and less than 35 wppm 5-halo acesulfame potassium, preferably less than 5 wppm.
    Type: Grant
    Filed: November 15, 2019
    Date of Patent: September 22, 2020
    Assignee: Celanese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10781190
    Abstract: A process for producing acesulfame potassium, the process comprising the steps of providing a cyclizing agent composition comprising a cyclizing agent and a solvent and having an initial temperature, cooling the cyclizing agent composition to form a cooled cyclizing agent composition having a cooled temperature less than 35° C., reacting an acetoacetamide salt with the cyclizing agent in the cooled cyclizing agent composition to form a cyclic sulfur trioxide adduct composition comprising cyclic sulfur trioxide adduct; and, forming from the cyclic sulfur trioxide adduct in the cyclic sulfur trioxide adduct composition the finished acesulfame potassium composition comprising non-chlorinated acesulfame potassium and less than 39 wppm 5-chloro-acesulfame potassium. The cooled temperature is at least 2° C. less than the initial temperature.
    Type: Grant
    Filed: November 15, 2019
    Date of Patent: September 22, 2020
    Assignee: Celanese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10781205
    Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: September 22, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Linda N. Casillas, John David Harling, Afjal Hussain Miah, Mark David Rackham, Ian Edward David Smith
  • Patent number: 10781209
    Abstract: The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: September 22, 2020
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Thomas P. Maduskuie, Jr., Nikoo Falahatpisheh