Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
Type:
Grant
Filed:
August 24, 2015
Date of Patent:
September 11, 2018
Inventors:
Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
Abstract: The invention provides compounds of formula (I) that inhibit PDI, for use in methods to treat or prevent a disease or condition in a subject that would benefit by inhibition of PDI.
Type:
Grant
Filed:
June 26, 2017
Date of Patent:
September 4, 2018
Assignees:
Beth Israel Deaconess Medical Center, Inc., The Broad Institute, Inc.
Inventors:
Robert Flaumenhaft, Partha Pratim Nag, Tatiana Pilyugina, Jun Pu, Sivaraman Dandapani, Benito Munoz, Chris Dockendorff
Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Type:
Grant
Filed:
March 19, 2014
Date of Patent:
August 28, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Christopher F. Thompson, Danielle Falcone, Wei Deng, Luis Torres, Hongbo Zeng, Yunfeng Bai, Jianmin Fu, Norman Kong, Yumei Liu, Zhixiang Zheng, Mark E. Scott
Abstract: The present invention provides a crystal of 6-arylamino pyridone carboxamide compound and a preparation method thereof. The crystal is obtained by dissolving 6-(2-chloro-4-iodophenylamino)-N-(2-hydroxylethyoxyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-carboxamide in an aprotic polar solvent and adding a second solvent thereto. The crystallization method has the advantage of simple and convenient operations, and is beneficial to an industrial production. The resulting crystal has the advantage a high purity and good stability, and is benefit to the manufacture and storage of a medicament containing the same.
Type:
Grant
Filed:
August 5, 2015
Date of Patent:
July 17, 2018
Assignees:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Centaurus Biopharma Co., Ltd.
Inventors:
Lulu Wang, Xiquan Zhang, Fei Liu, Yizhong Zhu, Chao Gao, Song Tang, Bo Zhu, Jianqiu Tang
Abstract: A compound of formula (I) or a salt thereof wherein R1 represents a hydrogen atom, a methyl group or a ethyl group R2 represents a hydrogen atom or a fluorine atom R3 represents a hydrogen atom, a methyl group or an ethyl group.
Type:
Grant
Filed:
March 26, 2014
Date of Patent:
July 17, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Niall Andrew Anderson, Brendan John Fallon, John Martin Pritchard
Abstract: The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer.
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Grant
Filed:
May 19, 2015
Date of Patent:
June 19, 2018
Assignee:
Merck Sharp & Dohme
Inventors:
Tesfaye Biftu, Purakkattle Biju, Timothy A. Blizzard, Zhengxia Chen, Matthew J. Clements, Mingxiang Cui, Jessica L. Frie, William K. Hagmann, Bin Hu, Hubert Josien, Anilkumar G. Nair, Christopher W. Plummer, Cheng Zhu
Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
Type:
Grant
Filed:
December 15, 2016
Date of Patent:
June 19, 2018
Assignee:
Incyte Corporation
Inventors:
Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
Type:
Grant
Filed:
March 31, 2017
Date of Patent:
June 5, 2018
Assignee:
Amygdala Neurosciences, Inc.
Inventors:
Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G Strickley, Chandrasekar Venkataramani, Jeff Zablocki
Abstract: The present invention relates to a novel catalytic hydrogenation of substituted 2-methyl cyanopyridyl derivatives, in particular 3-chloro-5-(trifluoromethyl)pyridin-2-yl]acetonitrile [=Py-CN] to substituted 2-ethylaminopyridine derivatives, in particular 2-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]ethanamine [=Py-ethanamine] or salts thereof in the presence of metal catalysts, in particular palladium catalysts.
Type:
Grant
Filed:
November 11, 2014
Date of Patent:
June 5, 2018
Assignee:
BAYER CROPSCIENCE AKTIENGESELLSCHAFT
Inventors:
Wahed Ahmed Moradi, Thomas Himmler, Thomas Norbert Mueller, Albert Schnatterer, Guenter Schlegel
Abstract: The present invention aims to provide a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid with high purity, and a method for producing its derivative. The present invention provides a method for producing a cis-5-hydroxy-2-piperidinecarboxylic acid derivative, which method comprises a step of converting cis-5-hydroxy-2-piperidinecarboxylic acid into a compound(s) of Formula (1) and/or Formula (2) (wherein R1 represents a protective group for an amino group, and R2 represents a C1-C6 alkyl group), and a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid.
Abstract: Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.
Type:
Grant
Filed:
October 14, 2016
Date of Patent:
May 29, 2018
Assignee:
AMGEN INC.
Inventors:
David Bauer, Matthew Bio, Melanie Cooke, Katrina W. Copeland, Matthew Peterson, Michele Potashman, Roman Shimanovich, Helming Tan
Abstract: Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.
Type:
Grant
Filed:
May 26, 2017
Date of Patent:
May 22, 2018
Assignee:
Celgene Corporation
Inventors:
G. Patrick Stahly, David Jonaitis, Ho-Wah Hui, Kevin J. Klopfer
Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, tautomers, stereoisomers, solvates, hydrates, polymorphs, and compositions thereof. Also provided are methods and kits involving the inventive compounds for treating proliferative diseases (e.g., cancers (e.g., breast cancer, prostate cancer, lung cancer, and ovarian cancer), benign neoplasms, angiogenesis, inflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound of the invention may enhance the anti-tumor immune response by inhibiting or eliminating the immune suppression mediated by immune suppressor myeloid cells (MDSCs), inducing apoptosis, and/or inhibit or down-regulate proteins (e.g., epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), estrogen receptor (ER), X-linked inhibitor of apoptosis protein (XIAP), and heat shock protein 90 (Hsp90)) in the subject.
Type:
Grant
Filed:
July 10, 2013
Date of Patent:
May 15, 2018
Assignees:
Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
Inventors:
Kenneth C. Anderson, Teru Hideshima, Ralph Mazitschek, Gullu Gorgun
Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Type:
Grant
Filed:
October 19, 2012
Date of Patent:
May 1, 2018
Assignee:
GLAXOSMITHKLINE LLC
Inventors:
Rebecca L. Casaubon, Radha Narayan, Christopher Oalmann, Chi B. Vu
Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Type:
Grant
Filed:
March 19, 2014
Date of Patent:
May 1, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew Lloyd Childers, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Michelle Martinez, Danielle Falcone, Luis Torres, Yongqi Deng, Ravi Kurukulasuriya, Hongbo Zeng, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
Abstract: The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates: wherein R, R? and X are as described in the specification.
Type:
Grant
Filed:
December 2, 2014
Date of Patent:
April 24, 2018
Assignee:
UNICHEM LABORATORIES LIMITED
Inventors:
Dhananjay G. Sathe, Arijit Das, Yogesh Subhash Patil, Nilesh L. Bonde, Ankush Sampat Kekan
Abstract: The present invention relates to novel piperidine derivatives, stereoisomers thereof or pharmaceutically acceptable salts thereof; methods for preparing the compound; and pharmaceutical compositions comprising the compound. The novel piperidine derivatives, according to the present invention, having an effect as GPR119 agonist can be used for treatment of metabolic disorders, including diabetes mellitus (especially type II) and related disorders.
Type:
Grant
Filed:
June 11, 2013
Date of Patent:
April 17, 2018
Assignee:
CHONG KUN DANG PHARMACEUTICAL CORP.
Inventors:
ChangSik Lee, TaegSu Jang, DaeKyu Choi, MooSung Ko, DoHoon Kim, SoYoung Kim, JaeKi Min, WooSik Kim, YoungTae Lim