Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
Type:
Grant
Filed:
October 5, 2015
Date of Patent:
November 7, 2017
Assignee:
3-V Biosciences, Inc.
Inventors:
Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
Abstract: A compound which is the hydrobromide salt of N-{4-chloro-2-hydroxy-3-[(3S)-3-piperidinylsulfonyl]phenyl}-N?-(3-fluoro-2-methylphenyl)urea, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments.
Abstract: The present invention provides a compound represented by the formula (Ia) as a novel cationic lipid that forms a lipid particle and also provides a lipid particle comprising the compound. The present invention further provides a nucleic acid lipid particle containing the lipid particle, and a pharmaceutical composition containing the nucleic acid lipid particle as an active ingredient.
Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
Type:
Grant
Filed:
June 7, 2016
Date of Patent:
October 31, 2017
Assignee:
Amgen Inc.
Inventors:
Matthew Bio, Sebastien Caille, Brian Cochran, Yuanqing Fang, Brian M. Fox, Brian S. Lucas, Lawrence R. McGee, Filisaty Vounatsos, Sean H. Wiedemann, Sarah Wortman
Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-B signaling are described. In particular, the compositions and methods are useful for reducing or eliminating the pathologies associated with Alzheimer's disease. The compositions include urea derivatives containing a piperidine, piperidinium, or a piperidin-4-yl methyl; cycloalkyl, aryl, and fluorobenzyl moieties.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
October 24, 2017
Inventors:
Mary Jean Tanga, Laura Ellen Downs Beaulieu, Anton Wyss-Coray, Carol Green, Hui Zhang, Jian Luo
Abstract: The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1?) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
Type:
Grant
Filed:
April 2, 2015
Date of Patent:
October 17, 2017
Assignee:
ELECTROPHORETICS LIMITED
Inventors:
Joseph M. Sheridan, Jonathan R. Heal, William D. O. Hamilton, Ian H. Pike
Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
Type:
Grant
Filed:
April 16, 2013
Date of Patent:
October 17, 2017
Assignees:
Case Western Reserve University, Board of Regents of the University of Texas System, University of Kentucky Research Foundation
Inventors:
Sanford Markowitz, James K. V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
Type:
Grant
Filed:
April 13, 2015
Date of Patent:
September 26, 2017
Assignee:
Exelixis, Inc.
Inventors:
Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava
Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
Type:
Grant
Filed:
August 10, 2015
Date of Patent:
September 26, 2017
Assignee:
BAYER CROPSCIENCE AG
Inventors:
Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Stefan Hillebrand, Juergen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
Abstract: The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1?) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
Type:
Grant
Filed:
September 1, 2015
Date of Patent:
September 19, 2017
Assignee:
ELECTROPHORETICS LIMITED
Inventors:
Joseph M. Sheridan, Jonathan R. Heal, William D. O. Hamilton, Ian H. Pike
Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent for the prophylaxis or treatment of diabetes mellitus are provided.
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Grant
Filed:
March 12, 2014
Date of Patent:
August 29, 2017
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Andrew Cook, Alexandre Côté, Les A. Dakin, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
March 12, 2014
Date of Patent:
August 22, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, Kyle J. Eastman, Kyle E. Parcella
Abstract: A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
Abstract: There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of the invention.
Type:
Grant
Filed:
November 18, 2014
Date of Patent:
August 22, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kyoung S. Kim, Liping Zhang, Ashok Vinayak Purandare, Steven P. Seitz
Abstract: The invention relates to the use of substituted benzamide derivatives of Formula I: Wherein: A1 and A2 are —N or —CH, so that if A1 is —N, then A2 is —CH and If A2 is —N, then A1 is —CH; R is a hydrogen atom, or represents branched or unbranched —(C1-C3)-alkyl, —(C1-C3)-alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen or hydroxyl, —(C1-C3)—O—(C1-C3), —(C1-C3)—O—(C1-C3), wherein one, two or three hydrogen atoms may be substituted by a halogen, or R is a group wherein R3 and R4 both together or independently are halogen, hydroxyl, —(C1-C3)alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen or hydroxyl, —O—(C1-C3)-alkyl, —O—(C1-C3)-alkyl, wherein one, two or three hydrogen atoms may be substituted by a halogen, —O—(C1-C3)—O—(C1-C3), —O—(C1-C3)—O—(C1-C3), wherein one, two or three hydrogen atoms may be substituted by a halogen; R1 and R2 both together or independently are halogen, hydroxyl, —(C1-C3)-alkyl, —(C1-C3C)-alkyl, wherein one, two or three hydrog
Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
Type:
Grant
Filed:
August 29, 2014
Date of Patent:
August 8, 2017
Assignee:
Ambit Biosciences Corporation
Inventors:
Mark W. Holladay, Gang Liu, Martin W. Rowbottom
Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
Abstract: A composition for controlling pests includes a compound represented by the formula (1) or N-oxide thereof: and 4-oxo-4-[(2-phenylethyl)amino]-butyric acid. A method for controlling pests has a step of applying to plants, plant seeds, bulbs, or soil where plants grow an effective amount of the composition for controlling pests. The composition for controlling pests and the method for controlling pests exhibit excellent controlling efficacy on pest.