Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
Type:
Grant
Filed:
August 12, 2011
Date of Patent:
August 5, 2014
Assignee:
Janssen Pharmaceutica NV
Inventors:
Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
Type:
Grant
Filed:
June 18, 2013
Date of Patent:
July 8, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Frank Himmelsbach, Birgit Jung, Ralf Lotz
Abstract: A process is described for the preparation of s-triazine derivatives of the formula in which R is a C1-C12-alkyl radical, by reacting a cyanuric acid halide with a p-aminobenzoic acid ester, which comprises a C6-C12-alkyl radical as radical of the ester alcohol, in a molar ratio of 1:3 to 1:5 in a xylene isomer mixture as solvent. 10 The process is characterized in that the solvent is used in amounts of from 0.6 to 2.1 mol/l.
Abstract: The present disclosure provides isotopically substituted compounds of the formula (II): wherein T, U, V, W, X, Y, Z, R0, R3, R4, R5 and R6 are as defined in the detailed description. The method for detection and quantification using the same is also disclosed.
Type:
Grant
Filed:
January 9, 2012
Date of Patent:
July 1, 2014
Assignee:
Purdue Research Foundation
Inventors:
Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
Abstract: The invention relates to compounds corresponding to formula (I): in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.
Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.
Type:
Grant
Filed:
March 27, 2013
Date of Patent:
June 17, 2014
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
Steven C. Zimmerman, Chun-Ho Wong, Paul J. Hergenrother, Jessie Peh
Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
Type:
Grant
Filed:
April 3, 2013
Date of Patent:
June 10, 2014
Assignee:
Roche Palo Alto LLC
Inventors:
Henrietta Dehmlow, Shawn David Erickson, Patrizio Mattei, Hans Richter
Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
Type:
Grant
Filed:
November 30, 2012
Date of Patent:
June 3, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
Type:
Grant
Filed:
September 10, 2013
Date of Patent:
May 27, 2014
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
May 20, 2014
Assignee:
Novartis AG
Inventors:
Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Brian Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
Abstract: The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
July 1, 2011
Date of Patent:
April 29, 2014
Assignee:
Merck Patent GmbH
Inventors:
Bayard R. Huck, Constantin Neagu, Reinaldo Jones, Lizbeth Celeste DeSelm, Yufang Xiao, Srinivasa R. Karra, Ruoxi Lan, Igor Mochalkin, Amanda E. Sutton, Thomas E. Richardson
Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
December 3, 2012
Date of Patent:
April 15, 2014
Assignee:
Vanderbilt University
Inventors:
Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Yiu-Yin Cheung
Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
December 1, 2011
Date of Patent:
April 8, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Type:
Grant
Filed:
June 14, 2013
Date of Patent:
April 8, 2014
Assignee:
Amgen Inc.
Inventors:
Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.