Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
Type:
Grant
Filed:
May 9, 2013
Date of Patent:
September 13, 2016
Assignee:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventors:
Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
Abstract: The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.
Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
August 30, 2016
Assignee:
Proximagen Limited
Inventors:
Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
Abstract: The invention provides a method of changing a ratio of 68 to 64 kDa protein of MRJP3 in a royal jelly, a method of producing a royal jelly comprising MRJP3 having a changed ratio of 68 to 64 kDa protein relative to a control royal jelly and the royal jelly produced thereform. Also provided is a method of promoting the growth of the larva of a queen bee comprising feeding the larva of the queen bee a royal jelly of the invention. Further provided is a method of producing bee larva, pupa and queen bees with sizes larger than normal.
Abstract: Provided are compositions, methods of making the compositions, and methods of using the compositions. The compositions can be provided as pharmaceutical preparations for use in disease treatment, such as cancer therapy. The compositions include novel pharmaceutical preparations which contain effective concentrations of a chemical compound. One compound used is 10H-1,3-Dioxolo[4,5-g]pyrano[3?,4?:6,7]indolizino[1,2-b]quinoline-8,11(7H,12H)-dione, 7-ethyl-7-hydroxy-, (S)-. The invention also provides methodologies for preparing pharmaceutical preparations for use in intravenous and oral pharmaceutical preparations that contain drug compounds that are difficult to dissolve in water.
Abstract: A method for making the compound is set forth utilizing the starting material
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
August 2, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.
Type:
Grant
Filed:
November 21, 2014
Date of Patent:
July 26, 2016
Assignee:
Genentech, Inc.
Inventors:
Frederick Cohen, Malcolm Huestis, Cuong Ly, Snahel Patel, Michael Siu, Xianrui Zhao
Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
Abstract: The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.
Type:
Grant
Filed:
October 23, 2013
Date of Patent:
June 28, 2016
Assignee:
YUHAN CORPORATION
Inventors:
Chan-Sun Park, Young-Hwan Kim, Gyu-Jin Lee, Youn Hur, Eun-Hye Jung, Hee-Jae Tak, Seung-Yub Shin, Ho-Jin Lee, Chun-Ho Lee, Koo-Yeon Lee
Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
Type:
Grant
Filed:
April 9, 2012
Date of Patent:
June 7, 2016
Assignee:
SPHAERA PHARMA PTE. LTD
Inventors:
Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
Abstract: Compositions and methods related to the removal of acidic gas. In particular, the present disclosure relates to a composition and method for the removal of acidic gas from a gas mixture using a solvent comprising a blend of piperazine and at least one diamine or triamine.
Type:
Grant
Filed:
July 18, 2014
Date of Patent:
April 26, 2016
Assignee:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Gary Rochelle, Omkar Namjoshi, Le Li, Yang Du, Thu Nguyen
Abstract: The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4?-acetoxy-2?-benzoyloxy-5?,20-epoxy-1?-hydroxy-7?,10?-dimethoxy-9-oxo-11-taxen-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.
Type:
Grant
Filed:
June 11, 2014
Date of Patent:
April 12, 2016
Assignee:
AVENTIS PHARMA S.A.
Inventors:
Eric Didier, Nicolas Tremaudeux, Lionel Zaske
Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.
Type:
Grant
Filed:
February 24, 2014
Date of Patent:
April 5, 2016
Assignee:
Phyton Holdings, LLC
Inventors:
James H. Johnson, T. G. Sambandam, Barry J. Hand, Christopher D. Howe, Roland R. Franke, Brian A. Bucher, John S. Juchum, Rex T. Gallagher, Marc A. Plante, Edward M. Desimone, III, Dong S. Yang
Abstract: Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation.
Type:
Grant
Filed:
November 23, 2012
Date of Patent:
March 29, 2016
Assignee:
THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, & THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIV. TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
Inventors:
David George Lloyd, Darren Fayne, Mary Jane Meegan, Miriam Carr, Gemma Karena Kinsella, Laura Caboni, Wiliam Nicholas Jagoe, Billy Egan, Fernando Blanco, D. Clive Williams
Abstract: The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
Abstract: The present invention relates to a new process for the preparation of 6-hydroxy-5-arylbicyclo[2.2.2]octan-2-one compounds of the formula (II); which may subsequently be further transformed to compounds of the formula (I): The present invention further relates to novel compounds as such, which compounds are useful intermediates in the above process.
Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.