Abstract: The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.
Type:
Grant
Filed:
November 11, 2016
Date of Patent:
November 7, 2017
Assignee:
Janssen Pharmaceutica NV
Inventors:
Diego Fernando Domenico Broggini, Vit Lellek, Susanne Lochner, Neelakandha S. Mani, Adrian Maurer, Daniel J. Pippel, Lana K. Young
Abstract: The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.
Type:
Grant
Filed:
March 18, 2016
Date of Patent:
October 31, 2017
Assignee:
Novartis AG
Inventors:
Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Bo Han, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Franck Mallet, Julie Martz, Can Wang, Jing Xiong, Xianglin Zhao
Abstract: Provided is a novel compound which has an excellent A? aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents —CH2—, —O—, —S—, or —NH—; R1 and R2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group.
Type:
Grant
Filed:
December 9, 2014
Date of Patent:
October 24, 2017
Assignee:
JAPAN SCIENCE AND TECHNOLOGY AGENCY
Inventors:
Motomu Kanai, Yohei Soma, Tadamasa Arai, Takushi Araya
Abstract: A condensed cyclic compound and an organic light-emitting device, the compound being represented by Formula 1: (A1)a1-(L1)b1-(A2)a2??<Formula 1> wherein, in Formula 1, A1 is a group represented by Formula 2-1, below, a1 is 1, 2, or 3, and, when a1 is 2 or greater, two or more A1s are identical to or different from each other, A2 is a group represented by Formula 2-2, below, a2 is 1, 2, or 3, and, when a2 is 2 or greater, two or more A2s are identical to or different from each other,
Type:
Grant
Filed:
June 4, 2015
Date of Patent:
October 17, 2017
Assignee:
SAMSUNG DISPLAY CO., LTD.
Inventors:
Dongwoo Shin, Seulong Kim, Younsun Kim, Jungsub Lee, Naoyuki Ito
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof (Formula (I)) in which m, X, R1, R2, R3 and R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
August 7, 2014
Date of Patent:
October 17, 2017
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Sarah Bousba, Anne Goldby, Kerry Jenkins, Natasha Kinsella, Martin Teall
Abstract: The present invention concerns a method for preparing certain steroidal derivatives alkylated in position 6, comprising a step of alkylating the corresponding compound halogenated in position 6 with an organometallic alkylating agent.
Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
October 10, 2017
Assignee:
Wisconsin Alumi Research Foundation
Inventors:
Jennifer Schomaker, Luke Boralsky, John Hershberger, Jared Rigoli, Christopher S. Adams
Abstract: Myeloperoxidase inhibitor, pharmaceutical compositions containing the inhibitor and the use of the inhibitor to treat, for example, cardiovascular conditions.
Abstract: The invention relates to the compounds of formula I and formula Ia or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of formula I or formula Ia; and methods for treating or preventing epilepsy, seizures and convulsions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, seizures and convulsions.
Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
Type:
Grant
Filed:
July 27, 2015
Date of Patent:
September 19, 2017
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher F. Claiborne, Lloyd J. Payne, Richard J. Boyce, Todd B. Sells, Stephen G. Stroud, Stuart Travers, Tricia J. Vos, Gabriel S. Weatherhead
Abstract: The invention described herein pertains to processes and intermediates for preparing indole containing pharmaceuticals, particularly to processes and intermediates for preparing selective estrogen receptor modulators, such as bazedoxifene.
Type:
Grant
Filed:
May 13, 2014
Date of Patent:
September 5, 2017
Assignee:
Indiana University Research and Technology Corporation
Abstract: The present invention pertains to a method for producing an optically active compound which includes a step for reducing an imino group of an imine compound or a step for reducing an unsaturated bond of a heterocyclic compound, while in the presence of hydrogen gas as a hydrogen donor and one or more types of complexes selected from a group consisting of a complex represented by general formula (1), a complex represented by general formula (2), a complex represented by general formula (3), and a complex represented by general formula (4) (the general formulas (1)-(4) are as stipulated by claim 1).
Abstract: Novel phenazine derivatives, methods for their preparation and their medical use, in particular as anti-neoplastic agents and anti-infective agents, are provided. Novel methods for the preparation of iodinin and myxin are also provided.
Type:
Grant
Filed:
November 3, 2014
Date of Patent:
August 29, 2017
Assignees:
Universitetet I Oslo, Bergen Teknologioverføring AS, Université Claude Bernard Lyon 1
Inventors:
Stein Ove Døskeland, Pål Rongved, Lars Herfindal, Marc Le Borgne, Elvar Örn Viktorsson, Ove Alexander Høgmoen Åstrand
Abstract: The present invention provides a compound of formula (I) or the salt thereof: wherein R is at least one selected from the group consisting of unsubstituted C1-4 alkyl, C1-4 alkyl substituted by C6-18 aryl or —OR1, and —C(?O)Z. The compound is a type-S protein kinase inhibitor, which binds to an ATP-binding site and a substrate-recognition site of a protein kinase simultaneously. The present invention further provides a pharmaceutical composition, which includes a compound of formula (I) or a salt and a pharmaceutically acceptable carrier thereof. The present invention further provides a use of a compound of formula (I) or a salt thereof, which is for the manufacture of a protein kinase inhibitor as a drug.
Type:
Grant
Filed:
January 16, 2015
Date of Patent:
August 22, 2017
Assignee:
National Chiao Tung University
Inventors:
Jinn-Moon Yang, Kai-Cheng Hsu, Tzu-Ying Sung, Shen Rong Lin, Yun-Ming Wang, Kuang-Mei Hsu, Hsin-Ping Lin, Wan-Chun Liu
Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
Type:
Grant
Filed:
June 20, 2014
Date of Patent:
August 22, 2017
Assignee:
Karyopharm Therapeutics Inc.
Inventors:
Erkan Baloglu, Sharon Shacham, Dilara McCauley, Trinayan Kashyap, William Senapedis, Yosef Landesman, Gali Golan, Ori Kalid, Sharon Shechter
Abstract: The invention relates to the compounds of formula I and formula IA or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I and formula IA; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, Myotonia congenita and post-traumatic stress disorder.
Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.
Type:
Grant
Filed:
July 12, 2016
Date of Patent:
August 22, 2017
Assignee:
JANSSEN PHARMACEUTICA N.V.
Inventors:
Brett D. Allison, Bryan James Branstetter, J. Guy Breitenbucher, Michael D. Hack, Natalie A. Hawryluk, Alec D. Lebsack, Kelly J. McClure, Jeffrey E. Merit
Abstract: A thiazole compound represented by Formula (1): wherein R1 represents a C1-C4 alkyl group optionally having one or more fluorine atoms, R2 represents a hydrogen atom etc., R3 and R4 are the same or different and each represents a hydrogen atom etc., Ar represents a phenyl group optionally having one or more atoms or groups selected from the group A etc., and n represents 1 or 2 has excellent control activity against pests.
Abstract: Described are ROR? modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.
Type:
Grant
Filed:
September 18, 2014
Date of Patent:
August 8, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
T. G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Zhonghui Lu, David S. Weinstein