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: 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: 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: 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
Abstract: There is provided an alkali metal salt of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide and formulations thereof. This salt finds particular utility in the treatment or prevention of a disorder or condition ameliorated by the activation of AMPK.
Abstract: The present invention relates to a pharmaceutical composition for the prevention or treatment of solid cancers or blood cancers such as acute leukemia or chronic leukemia, including, as an active ingredient, a 1,2-naphthoquinone derivative compound or a pharmaceutically acceptable salt thereof, wherein the 1,2-naphthoquinone derivative compound has excellent effects in killing cancer cells of various solid cancers, acute leukemia, and chronic leukemia, and thus, can be useful as a pharmaceutical composition for the prevention or treatment of cancer, in particular, solid cancers, acute leukemia, or chronic leukemia.
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
June 27, 2023
Assignee:
YUNGJIN PHARM. CO., LTD.
Inventors:
Ki Ryang Kweon, Jun Young Heo, Min Ho Shong, Jeong Su Han, Min Jeong Ryu
Abstract: An object of the present invention is to provide a novel plant growth inhibiting agent and a plant growth inhibiting method using the same. The plant growth inhibiting agent of the present invention comprises, as an active ingredient, a compound represented by the following formula (I?) and/or a salt thereof. In the formula (I?), R1a represents a substituted or unsubstituted C1 to C20 alkyl group, a substituted or unsubstituted C6 to C14 aryl group, a substituted or unsubstituted C3 to C13 heteroaryl group, or the like; R2 represents a substituted or unsubstituted C1 to C20 alkylene group, a substituted or unsubstituted C6 to C14 arylene group, or the like; R3a represents OH, a substituted or unsubstituted C1 to C6 alkoxy group, or the like; X represents an oxygen atom; Y represents a substituent; q represents any integer of 0 to 3; n represents 0 or 1; and m represents 0 or 1.
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
June 27, 2023
Assignees:
National University Corporation Kumamoto University, Nippon Soda Co., Utd.
Inventors:
Hayato Ishikawa, Tokio Tani, Shinichiro Sawa, Takashi Ishida, Yusuke Fukushima, Jun Inagaki
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 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 9, 2021
Date of Patent:
June 27, 2023
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
Abstract: The invention relates to functionalised dioxaborolane or dioxaborinane derivatives of formula (I), wherein R1 is covalently bonded to the boron atom by a carbon atom; one of R2, R3, R?3 or R4 is a radical of formula —X; or one of R1, R2, R3, R?3 or R4 is a radical of formula —X; and X is a functionalised radical. The invention relates to the method for preparing same and the uses thereof.
Type:
Grant
Filed:
January 6, 2022
Date of Patent:
June 20, 2023
Assignees:
ECOLE SUPERIEURE DE PHYSIQUE ET DE CHIMIE INDUSTRIELLES DE LA VILLE DE PARIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract: Disclosed crystalline Siponimod fumaric acid, solid state forms (polymorphs) thereof, processes for preparation thereof and pharmaceutical compositions thereof.
Type:
Grant
Filed:
January 22, 2019
Date of Patent:
June 13, 2023
Assignee:
TEVA PHARMACEUTICALS INTERNATIONAL GMBH
Inventors:
Marisa Martinelli, Pavel Kolesa, Maurizio Paiocchi, Matteo Toso, Roberta Volonté, Piero Paravidino
Abstract: Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.
Type:
Grant
Filed:
April 29, 2022
Date of Patent:
June 13, 2023
Assignee:
Massachusetts Institute of Technology
Inventors:
Ronald T. Raines, Brian Gold, Jesus M. Dones, Nile S. Abularrage, Brian James Graham
Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.
Type:
Grant
Filed:
April 25, 2022
Date of Patent:
June 13, 2023
Assignees:
Georgetown University, The Board of Regents of the University of Oklahoma
Inventors:
Milton L. Brown, Yali Kong, Courtney Houchen, Sripathi M. Sureban, Parthasarathy Chandrakesan
Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Type:
Grant
Filed:
May 15, 2019
Date of Patent:
May 30, 2023
Assignee:
VIVACE THERAPEUTICS, INC.
Inventors:
Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.
Type:
Grant
Filed:
August 9, 2021
Date of Patent:
May 9, 2023
Inventors:
Hina Siddiqui, Muhammad Iqbal Choudhary, Atia-tul- Wahab, Atta-ur- Rahman, Fazila Rizvi, Sheeba Wajid