Abstract: The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
Abstract: Various embodiments of this invention are directed to pharmaceutical compositions and methods for treating disease. The compositions of such embodiments include dicarboxylic acid compounds containing electron withdrawing groups, alkyl esters of dicarboxylic acids containing electron withdrawing groups, or compounds of Formulae I to X. The methods of various embodiments include administering an effective amount of any of these pharmaceutical compositions to a patient in need of treatment.
Type:
Grant
Filed:
March 2, 2017
Date of Patent:
August 25, 2020
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Bruce A. Freeman, Francisco J. Schopfer
Abstract: Disclosed are compounds having formulae I and II or pharmaceutically acceptable salts or hydrates thereof, a preparation method thereof and pharmaceutical compositions thereof. The compounds having formulae I and II possesses an isocitrate dehydrogenase 2 (IDH2) inhibitory activity and are capable of treating IDH2 mutation-induced cancers.
Type:
Grant
Filed:
July 29, 2016
Date of Patent:
August 18, 2020
Assignees:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
Abstract: The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Type:
Grant
Filed:
September 14, 2018
Date of Patent:
August 11, 2020
Assignee:
Aduro BioTech Inc.
Inventors:
Chudi Obioma Ndubaku, George Edwin Katibah, Tucker Curran Roberts, Leonard Sung, Stephane Ciblat, Franck Raeppel, Vu Linh Ly, Yeeman K. Ramtohul, Taras Rybak, Mariam Zaky, Laura Gillard, Hossein Ismaili
Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Type:
Grant
Filed:
July 6, 2017
Date of Patent:
August 4, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Zilun Hu, Cailan Wang, Mimi L. Quan, Peter W. Glunz
Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Type:
Grant
Filed:
March 12, 2019
Date of Patent:
August 4, 2020
Assignee:
Shire Human Genetic Therapies, Inc.
Inventors:
Nikolaos Papaioannou, Sarah Jocelyn Fink, Thomas Allen Miller, Gerald Wayne Shipps, Jr., Jeremy Mark Travins, David Edward Ehmann, Alastair Rae, John Mark Ellard
Abstract: [Problem] To provide a compound useful as an MC4 receptor agonist. [Means for Solution] The present inventors studied MC4 receptor agonists, and have found that a piperazine derivative has an MC4 receptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.
Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
Type:
Grant
Filed:
April 5, 2019
Date of Patent:
July 14, 2020
Assignee:
Prelude Therapeutics Incorporated
Inventors:
Juan Luengo, Hong Lin, Michael Hawkins, Rupa Shetty, Philip Pitis, Gisela Saborit Villarroya
Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.
Type:
Grant
Filed:
March 1, 2019
Date of Patent:
July 7, 2020
Assignee:
Janssen BioPharma, Inc.
Inventors:
Robert Than Hendricks, Leonid Beigelman, David Bernard Smith, Antitsa Dimitrova Stoycheva
Abstract: The present invention provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of A?42 oligomers in a subject. It further provides a method of reducing formation of or disrupting A?42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition.
Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Type:
Grant
Filed:
May 4, 2017
Date of Patent:
June 30, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
David K. Williams, Weifang Shan, James Aaron Balog
Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.
Type:
Grant
Filed:
January 18, 2019
Date of Patent:
June 30, 2020
Assignee:
Kadmon Corporation, LLC
Inventors:
Masha V. Poyurovsky, Ji-In Kim, Kevin G. Liu, Alexandra Zanin-Zhorov
Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.
Type:
Grant
Filed:
December 12, 2018
Date of Patent:
June 23, 2020
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Yat Sun Or, Jun Ma, Guoqiang Wang, Xuechao Xing, Ruichao Shen, Bin Wang
Abstract: Disclosed are a novel pyrimidine derivative compound, a pharmaceutically acceptable salt thereof, a method for preparing the compound and a pharmaceutical use of the compound as an anticancer agent or a therapeutic agent for degenerative brain diseases. Specifically, the novel pyrimidine derivative compound has excellent inhibitory activities against kinase enzymes such as ARK5/NUAK1, ACK1, FLT3, JAK1, JAK2 and JAK2 (V617F) and thus is useful for treating and preventing leukemia, ovarian cancer, breast cancer, non-small cell carcinoma, colorectal cancer, glioma, and brain protein abnormalities such as Alzheimer's disease, progressive supranuclear palsy and frontotemporal dementia, that is, degenerative diseases caused by Tau deposition.
Type:
Grant
Filed:
March 22, 2019
Date of Patent:
June 16, 2020
Assignee:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
Inventors:
So Ha Lee, Kyung Ho Yoo, Eun Joo Roh, Tae Bo Sim, Tae Young Kim, Jae Ho Kim
Abstract: Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
Abstract: Disclosed are a benzazepine derivative, a preparation method, a pharmaceutical composition and the use thereof. A compound as shown in formula (I) of the present invention, and an isomer, a prodrug, a stable isotope derivative or a pharmaceutically acceptable salt thereof have the following structure. The benzazepine derivative of the present invention has a good regulation effect on the TLR family and the related signaling pathway, and in particular, has a good regulation effect on TLR8, can effectively treat, relieve and/or prevent various diseases mediated by TLR family and the TLR-related signaling pathway, and in particular, can effectively treat, relieve and/or prevent various diseases mediated by TLR8, such as cancers, autoimmune diseases, infections, inflammations, transplantation rejections, graft-versus-host diseases, etc.
Type:
Grant
Filed:
May 4, 2017
Date of Patent:
June 2, 2020
Assignee:
SHANGHAI DE NOVO PHARMATECH CO., LTD.
Inventors:
Daxin Gao, Yuxun Wang, Shoujun Chen, Heping Yang
Abstract: This invention discloses the use of aza-tryptanthrin derivatives as an IDO1 and/or TDO inhibitors, and the derivatives are represented by the general Formula (I). The compounds represented by the Formula (I) have inhibitory effects on indoleamine-2,3-dioxygenase 1 (IDO1) and/or tryptophan-2,3-dioxygenase (TDO), and can be used for treating diseases having the pathological features of IDO1 and/or TDO-mediated tryptophan metabolism, including but not limited to tumors, autoimmune disease, infectious diseases, Alzheimer's disease, depression, anxiety.
Abstract: The present disclosure provides pyrimidine compounds of Formula 1 and uses thereof for example, for the potential treatment of diseases associated with P2X purinergic receptors. In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the potential treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
Type:
Grant
Filed:
March 20, 2017
Date of Patent:
May 26, 2020
Assignee:
Afferent Pharmaceuticals, Inc.
Inventors:
Ronald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
Abstract: A compound has a guanidine skeleton that inhibits the protease activity of MALT1 and exerts a therapeutic or prophylactic effect on autoimmune disease such as psoriasis or allergic disease such as atopic dermatitis. The guanidine derivative is typified by the following formula or a pharmacologically acceptable salt thereof.
Abstract: The invention relates to compounds of formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, R4a, R4b and R5 are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
Type:
Grant
Filed:
December 14, 2018
Date of Patent:
May 19, 2020
Assignee:
Genentech, Inc.
Inventors:
James John Crawford, Aleksandr Kolesnikov, Jianwen A. Feng