Abstract: The present disclosure provides a method of preparing a compound of Formula I, wherein R1 is C1-C4 alkyl; R2 is C1-C4 alkyl; and R3 is selected from the group consisting of C1-C6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess.
Type:
Grant
Filed:
February 11, 2020
Date of Patent:
September 19, 2023
Assignee:
Dracen Pharmaceuticals, Inc.
Inventors:
Jon Philip Lawson, Robert Christian Wild, Yiyang Shao, Jinxiao Chu, Jinchao Weng, Pavel Majer
Abstract: Provided herein are methods of treating a nervous system injury, such as a central nervous system injury and/or a peripheral nervous system injury, and methods for treating an injured neuron using glycopyrrolate, mexiletine, or a mixture thereof.
Abstract: The disclosure provides methods of treating a patient having primary hyperoxaluria or idiopathic hyperoxaluria comprising administering a therapeutically effective amound of compound of the formula and pharmaceutically acceptable salts, solvates, and hydrates thereof to the patient. The variables, e.g. ring A, n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful inhibiting the conversion of glyoxylate to oxalate. When administered to a patient having a disease or disorder associated with elevated oxalate levels, such as PH type 1, type 2, or type 3 or idiopathic hyperoxaluria the compounds prevent or substantially reduce the amount and buildup of oxalate the patient's kidneys, bladder, urinary tract and other parts of the patient's body.
Type:
Grant
Filed:
May 17, 2021
Date of Patent:
September 12, 2023
Assignees:
VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Inventors:
Matthew Hall, Daniel J. Urban, John Knight, Ross Holmes, Kyle David Wood, Alex Waterson, Victor M. Darley-Usmar, Leonard M. Neckers
Abstract: The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.
Type:
Grant
Filed:
January 26, 2022
Date of Patent:
September 12, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Gediminas Brizgys, Eda Canales, Chienhung Chou, Michael Graupe, Jiayao Li, Roland D. Saito, Scott D. Schroeder, Winston C. Tse, Qiaoyin Wu, Jennifer R. Zhang
Abstract: The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with a serotonin 5-HT2 receptor.
Abstract: The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
Type:
Grant
Filed:
November 29, 2021
Date of Patent:
August 29, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Peter A. Blomgren, Kevin S. Currie, Christian Gege, Jeffrey E. Kropf, Jianjun Xu
Abstract: The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.
Abstract: The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X?Y—Z, X—Y?Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.
Abstract: Provided is a pharmaceutical composition which contains pemafibrate, a salt thereof or a solvate thereof and has excellent stability. A pharmaceutical composition is provided containing pemafibrate, a salt thereof or a solvate thereof and having a moisture content of 2.4 mass % or less.
Abstract: Provided herein is a method for treating a monocarboxylate transporter MCT4-mediated disorder in a subject in need thereof. The method comprises the step of administering to the subject a compound of structural Formula I and/or a salt thereof. The treatment of the monocarboxylate transporter MCT4-mediated disorder may inhibit activity of MCT4, or a mutant thereof, sometimes with at least a 100-fold selectivity for MCT4 over MCT1.
Abstract: In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I?) forms.
Type:
Grant
Filed:
December 14, 2021
Date of Patent:
August 8, 2023
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Adam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi, Gene Timothy Fass, Michael Simeone, R. Michael Baldwin, David L. Bourdet
Abstract: The present invention relates to a blend for prevention, mitigation, or treatment of schizophrenia, the blend containing a carbamate compound of chemical formula 1, or a pharmaceutically acceptable salt, solvate, or hydrate thereof and, more specifically, to a blend and a pharmaceutical composition each containing a carbamate compound of chemical formula 1 and aripiprazole, and to a use thereof for treating schizophrenia.
Type:
Grant
Filed:
August 9, 2021
Date of Patent:
August 8, 2023
Assignee:
SK BIOPHARMACEUTICALS CO., LTD.
Inventors:
Chan Mi Joung, Sun Gwan Hwang, Ji Won Lee, Young Koo Jang
Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, Darier's disease, scleroderma, cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
Type:
Grant
Filed:
December 30, 2020
Date of Patent:
August 1, 2023
Assignee:
BioSplice Therapeutics, Inc.
Inventors:
Sunil Kumar Kc, Chi Ching Mak, Gopi Kumar Mittapalli, Brian Joseph Hofilena, Brian Walter Eastman, Jianguo Cao, Chandramouli Chiruta, Venkataiah Bollu
Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are disclosed to be inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Type:
Grant
Filed:
November 15, 2021
Date of Patent:
July 25, 2023
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
Abstract: The present disclosure relates to a composition having a structure that includes where R1 includes at least one of hydrogen, carbon, and/or fluorine, and includes a covalent bond. In some embodiments of the present disclosure, R1 may include at least one of hydrogen, fluorine, a carboxyl group, a hydroxyl group, an alkoxy group, and/or a hydrocarbon chain. In some embodiments of the present disclosure, the composition may be derived from at least one of In some embodiments of the present disclosure, at least a portion of the composition may be bioderived.
Abstract: Disclosed are compounds of formula I: as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Type:
Grant
Filed:
December 7, 2021
Date of Patent:
July 25, 2023
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.
Type:
Grant
Filed:
October 8, 2021
Date of Patent:
July 25, 2023
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Debra Jane Wallace, Fenger Zhou, Yuguang Wang, Takashi Nakai, Vishnu Vardhan Reddy Karnati, Wayne C. Schairer, William Kissel, Song Xue, Ahmad Hashash
Abstract: An anti-freezing composition according to an embodiment of the present disclosure includes at least one of a compound represented by Formula 1 and a compound represented by Formula 2. An anti-freezing composition according to another embodiment of the present disclosure includes a peptide consisting of amino acids having different chirality, thereby having an excellent effect of inhibiting ice formation or ice recrystallization.
Type:
Grant
Filed:
July 1, 2022
Date of Patent:
July 11, 2023
Assignee:
GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY
Abstract: Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.
Type:
Grant
Filed:
November 15, 2021
Date of Patent:
July 4, 2023
Assignee:
Northwestern University
Inventors:
Karl A. Scheidt, Ansoo Lee, Richard C. Betori