Abstract: Provided herein are compounds that inhibit pKal, a serine protease whose activity is responsible for proteolytically cleaving kininogen and generating the potent vasodilator and pro-inflammatory peptide bradykinin, which can lead to painful and debilitating inflammatory attacks (e.g., edema). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating pKal-related diseases and disorders (e.g., edema) with the compounds in a subject, by administering the compounds and/or compositions described herein.
Type:
Grant
Filed:
August 3, 2018
Date of Patent:
November 9, 2021
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Jeremy Travins, Thomas Miller, Nikolaos Papaioannou
Abstract: The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Type:
Grant
Filed:
December 12, 2019
Date of Patent:
November 9, 2021
Assignee:
YUHAN CORPORATION
Inventors:
Tae Dong Han, Hee Jae Tak, Eun Kyung Kim, Eui Chul Lee, Sol Park, Hyok Jun Cho, Cheol Hee Lim, So Young Kim, Hyun Ho Choi, Da Na Jeong, Na Yeon Yang, Na Ry Ha
Abstract: A compound of the general formula (I). The compounds of formula I are useful for treatment of a cardiac disease, disorder or condition in a mammal.
Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoletic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Abstract: An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
Inventors:
John J. Acton, III, Jianming Bao, Qiaolin Deng, Melissa Egbertson, Ronald Ferguson, II, Xiaolei Gao, Scott Timothy Harrison, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Zhaoyang Meng, Meng Na, Michael T. Rudd, Oleg Selyutin, David M. Tellers, Ling Tong, Fengqi Zhang
Abstract: The invention provides compounds of formula (I), stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof: (I) wherein A1 to A6 and R1 to R4 are as defined herein. Such compounds are suitable for use in the treatment or prevention of diseases or conditions which are mediated by the activation of lactate dehydrogenase A (LDHA), for example cancer.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
October 12, 2021
Assignee:
ARCTIC PHARMA AS
Inventors:
Jo Klaveness, Bora Sieng, Steffi Lundvall, Claudia Alejandra Bøen, Kathrin Hnida
Abstract: Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
Type:
Grant
Filed:
April 10, 2020
Date of Patent:
September 21, 2021
Assignees:
THE SCRIPPS RESEARCH INSTITUTE, BLACKTHORN THERAPEUTICS, INC.
Inventors:
Edward Roberts, Miguel A. Guerrero, Mariangela Urbano, Hugh Rosen, Robert M. Jones, Candace Mae Laxamana, Xianrui Zhao, Eric Douglas Turtle
Abstract: The invention relates to a compound chosen from the compounds of formula (I) below, the optical and geometrical isomers thereof and the tautomers thereof, and also the addition salts thereof with an acid or a base, and the solvates thereof: (I). The invention also relates to the use of these particular compounds and the compositions for dyeing keratin fibers.
Abstract: 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.
Abstract: 1-Phenylacetyl-8-aminohexahydro-2H-pyrano[3,4-b]pyrazines of formula are disclosed. The compounds are kappa ligands and are useful to treat drug dependency, pruritus, pain, and inflammation.
Type:
Grant
Filed:
December 7, 2018
Date of Patent:
August 17, 2021
Assignee:
The Rockefeller University
Inventors:
Mary Jeanne Kreek, Amy Ripka, Brian Reed, Eduardo Butelman
Abstract: The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Type:
Grant
Filed:
December 12, 2019
Date of Patent:
August 17, 2021
Assignee:
YUHAN CORPORATION
Inventors:
Tae Dong Han, Hee Jae Tak, Eun Kyung Kim, Dong Hoon Kim, Su Bin Choi, Sol Park, Hyun Ho Choi, Tae Wang Kim, Mi Kyeong Ju, Na Ry Ha
Abstract: The present invention concerns the tetrahydrate form of the compound: (3S)-4-{4-[3-(3-methylpiperidin-1-yl)propoxy]phenyl}pyridine 1-oxide, dihydrochloride, its process of preparation and therapeutical uses thereof.
Type:
Grant
Filed:
March 20, 2018
Date of Patent:
August 3, 2021
Assignee:
BIOPROJET
Inventors:
Marc Capet, Jeanne-Marie Lecomte, Jean-Charles Schwartz
Abstract: Provided are a compound represented by the following formula I; a novel photoreactive compound that can be used in nucleic acid photoreaction techniques by a photoreactive crosslinking agent comprising the compound; and a photoreactive crosslinking agent in which the photoreactive compound is used.
Type:
Grant
Filed:
July 19, 2018
Date of Patent:
August 3, 2021
Assignees:
JAPAN ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY, NICCA CHEMICAL CO., LTD.
Abstract: Disclosed herein are a compound of formula (I) and a preparation method and uses thereof. The compound shows a good inhibitory activity against ROCK, providing a new medicinal strategy to clinically treat the diseases associated with abnormal ROCK activity.
Type:
Grant
Filed:
December 16, 2019
Date of Patent:
August 3, 2021
Assignee:
HITGEN INC.
Inventors:
Jin Li, Dengyou Zhang, Jingchao Feng, Wei Liao, Li Lin, Si Li
Abstract: Disclosed are a compound as shown in general formula I, a pharmaceutically acceptable salt, an isomer or a mixture thereof, and a solvate, a polymorph, a stable isotope derivative or a prodrug thereof. The compound of the present disclosure has comparatively strong PARP inhibitory activity and can be used for treating diseases associated with PARP, such as cancers and inflammatory diseases.
Abstract: The present technology provides compounds according to Formulas (I), (II), or (III) useful in inhibiting an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus in a cell and/or treating subjects suffering from an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus.
Type:
Grant
Filed:
September 22, 2016
Date of Patent:
July 13, 2021
Assignee:
The Regents of the University of California
Inventors:
Paul Krogstad, Michael E. Jung, Jun Zuo, Yanpeng Xing
Abstract: The invention provides compositions and methods for intrathecal administration of the compound MCOPPB or a pharmaceutically acceptable salt thereof for treating pain, such as neuropathic pain suffered by an adult human.
Type:
Grant
Filed:
October 1, 2019
Date of Patent:
June 29, 2021
Assignee:
Centrexion Therapeutics Corporation
Inventors:
James N. Campbell, Barton Harley Manning
Abstract: The present invention provides an agent containing an orotic acid derivative that has high solubility in solvent and has superior physiological activity. The agent of the present invention is a melanin production inhibitor, whitening agent, fibroblast activator, collagen and/or elastin production promoter or wrinkle ameliorant containing as an active ingredient thereof an orotic acid derivative represented by the following general formula (1) or a salt thereof. In formula (1), R preferably represents a side chain of glutamic acid, glycine, histidine or aspartic acid. [In formula (1), R represents a side chain of a naturally-occurring amino acid and R may form, together with a nitrogen atom adjacent thereto through a single carbon atom, a hetero ring.