Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or arterial flutter.
Type:
Grant
Filed:
August 10, 2015
Date of Patent:
March 21, 2017
Assignee:
SANOFI
Inventors:
Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler, Josef Pernerstorfer, Joachim Brendel
Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
Type:
Grant
Filed:
August 4, 2015
Date of Patent:
March 14, 2017
Assignee:
Rhodes Technologies
Inventors:
Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
Abstract: The invention provides compounds of formula Ia, Ib and Ic: and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
Type:
Grant
Filed:
March 8, 2016
Date of Patent:
March 14, 2017
Assignees:
Rutgers, The State University of New Jersey, Provid Pharmaceuticals Inc.
Inventors:
Richard H. Ebright, Yon W. Ebright, Juan Shen, James Bacci, Anne-Cecile Hiebel, William Solvibile, Christopher Self, Gary Olson
Abstract: Embodiments of the present disclosure provide for a method of making an alkylene carbonate, catalysts, methods of converting CO2 to an alkylene carbonate, and the like.
Type:
Grant
Filed:
July 8, 2014
Date of Patent:
March 7, 2017
Assignee:
KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGY
Inventors:
Valerio D'Elia, Jeremie D. A. Pelletier, Jean-Marie Basset
Abstract: The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
Type:
Grant
Filed:
June 6, 2014
Date of Patent:
March 7, 2017
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Volker Schulze, Hans-Georg Lerchen, Donald Bierer, Antje Margret Wengner, Gerhard Siemeister, Philip Lienau, Ursula Krenz, Dirk Kosemund, Detlef Stöckigt, Michael Brüning, Ulrich Lücking, Ildikó Terebesi
Abstract: The present invention relates to Coix seed oil extracted from Semen Coicis, pharmaceutical preparations thereof, and the use thereof in the treatment of tumors and inflammation. Specifically, the Coix seed oil contains 5 diglyceride and 8 triglyceride ingredients in the following mass percentages: 1,3-diolein 0.40-0.58%, 1-linolein-3-olein 0.91-1.31%, 1,2-diolein 0.24-0.35%, 1-olein-2-linolein 0.66-0.95%, 1,2-dilinolein 0.33-0.47%, trilinolein 4.87-6.99%, 1-olein-2,3-dilinolein 13.00-18.69%, 1-palmitin-2,3-dilinolein 5.25-7.54%, 1,3-diolein-2-linolein 13.23-19.02%, 1-palmitin-2-linolein-3-olein 10.26-14.75%, 1,3-dipalmitin-2-linolein 2.28-3.28%, triolein 14.44-20.76% and 1-palmitin-2,3-diolein 8.06-11.58%.
Abstract: Provided is a method for continuously producing a cyclic carbonate, by which generation of a glycol in a reaction for synthesizing a cyclic carbonate is suppressed, and a cyclic carbonate having a high purity can be efficiently obtained even by simple purification. A method for continuously producing a cyclic carbonate, including filling a catalyst in a fixed-bed tube reactor, and continuously feeding carbon dioxide and an epoxide to the fixed-bed tube reactor to thereby bringing the carbon dioxide and the epoxide into contact with the catalyst, while continuously withdrawing the reaction liquid in the fixed-bed tube reactor, wherein the method includes a pre-treatment step in which a pre-treatment liquid containing a cyclic carbonate is brought into contact with the catalyst before feeding the carbon dioxide and the epoxide to the fixed-bed tube reactor, and the generated glycol is removed out of the system.
Type:
Grant
Filed:
July 18, 2014
Date of Patent:
March 7, 2017
Assignees:
MARUZEN PETROCHEMICAL CO., LTD., National Institute of Advanced Industrial Science and Technology
Abstract: Described herein is the surprising discovery that ketone bodies protect cell and tissues from ionizing radiation. Based on this finding, methods of protecting animal tissue and cells from damage caused by radiation exposure are disclosed which include, contacting the tissue with a therapeutically effective amount of an agent including at least one ketone ester, thereby protecting the tissue from radiation damage. Ketone esters can be used to minimize, reduce and/or prevent tissue damage following intentional and accidental radiation exposure, as well as increasing the therapeutic efficacy of radiation therapies by protecting non-target tissue from incidental radiation damage.
Type:
Grant
Filed:
November 5, 2013
Date of Patent:
February 28, 2017
Assignees:
TDELTAS, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Abstract: Disclosed herein are methods for treating a human subject having a disease associated with an increased level of apoptosis using a nitroxide. Further disclosed are methods for treating a human subject in need of a reduced expression level of a gene associated with the apoptosis pathway using a nitroxide.
Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
February 21, 2017
Assignee:
Heptares Therapeutics Limited
Inventors:
Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
Abstract: The invention relates to the use of compounds corresponding to formula (I), or a pharmaceutically acceptable salt thereof, for preparing a medicament for the treatment of bladder cancer.
Abstract: Novel methods and systems for producing a substantially pure d-threo stereoisomer of methylphenidate or a salt thereof are provided. In particular, methods and systems for producing d-threo-methylphenidate hydrochloride in pure stereoisomeric form from d-threo-ritalinic acid hydrochloride using diazomethane are described. The described methods can be performed on a large scale, and thus provide d-threo methylphenidate or a salt thereof, and particularly the hydrochloride salt of d-threo-methylphenidate, in stereoisomerically pure form and in large quantities from a single batch reaction. Also described are novel compositions of d-threo methylphenidate hydrochloride.
Type:
Grant
Filed:
December 4, 2015
Date of Patent:
February 21, 2017
Assignee:
AMPAC Fine Chemicals LLC
Inventors:
Aslam Malik, Francis Hempenstall, Nicholas Duda, Ali Suleman
Abstract: Whole exome sequencing of 12 tumor-normal DNA pairs, RNAseq analysis and targeted deep sequencing identified new genetic alterations in PTCL transformation. These analyses identified highly recurrent epigenetic factor mutations in TET2, DN-MT3A and IDH2 as well as a new highly prevalent RHOA p.Gly17Val (NM_001664) mutation present in 22/35 (67%) of angioimmunoblastic T-cell lymphomas (AITL) and in 8/44 (18%) not otherwise specified PTCL (PTCL NOS) samples. Mechanistically, the RHOA Gly17Val protein interferes with RHOA signaling in biochemical and cellular assays, an effect potentially mediated by the sequestration of activated Guanine Exchange Factor (GEF) proteins. In addition, new and recurrent, genetic defects are described including mutations in FYN, ATM, B2M and CD58 implicating SRC signaling, impaired DNA damage response and escape from immune surveillance mechanisms in the pathogenesis of PTCL.
Type:
Grant
Filed:
June 3, 2014
Date of Patent:
February 21, 2017
Assignee:
The Trustees of Columbia University in the City of New York
Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula I.
Type:
Grant
Filed:
February 18, 2016
Date of Patent:
February 21, 2017
Assignee:
REGENTS OF THE UNIVERSITY OF MINNESOTA
Inventors:
Venkatram R. Mereddy, Lester R. Drewes, Mohammad Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
Abstract: The present invention relates to a compound having a 2,6-difluorophenylether structure useful as organic electronic materials, pharmaceuticals and agrochemicals, and in particular, liquid crystal display device materials. Provided are a compound represented by general formula (1): and a liquid crystal composition containing the compound and a liquid crystal display device that uses the liquid crystal composition. Since the compound represented by general formula (1) is used as a component of a liquid crystal composition, a liquid crystal composition that exhibits low viscosity and a liquid crystal phase over a wide temperature range can be obtained. Thus, the compound is particularly useful as a component of a liquid crystal composition for high-response-speed liquid crystal display devices.
Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
Type:
Grant
Filed:
October 6, 2015
Date of Patent:
February 21, 2017
Assignee:
Flatley Discovery Lab
Inventors:
Bridget M. Cole, Richard A. Nugent, Paul T. Smith, Jr.
Abstract: The turgidity of potato tubers and other root vegetables is improved, maintained, or restored and/or the greening of potato tubers is delayed, prevented or inhibited and/or internal diseases caused by fungi and bacteria are prevented or treated by the application of one or more ?,?-unsaturated aliphatic aldehydes and ketones, C3 to C14 aliphatic aldehydes and ketones, and/or C3 to C7 saturated or unsaturated primary and secondary aliphatic alcohols.
Abstract: The present invention provides compounds of general formula 1 useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
Type:
Grant
Filed:
January 19, 2016
Date of Patent:
February 7, 2017
Assignee:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH