Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
Type:
Grant
Filed:
March 26, 2012
Date of Patent:
February 11, 2014
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
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:
December 3, 2012
Date of Patent:
February 4, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 20, 2013
Date of Patent:
February 4, 2014
Assignee:
Eli Lilly and Company
Inventors:
Maria-Jesus Blanco-Pillado, Matthew Joseph Fisher, Steven Lee Kuklish, Tatiana Natali Vetman
Abstract: This invention provides the methods of separation and identification of a novel type of piperidine flavan alkaloids from an African herbal tea, the leaves of Combretum micranthum commonly known as kinkeliba, and the procedures for preparing the total piperidine flavan alkaloids (TPFA). In particular, this invention relates to the use of the plant extract that may contain TPFA as anti-diabetic agents in treatment of metabolic disorders and other applications related to this new chemical structure and derivatives thereof.
Abstract: The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
Type:
Grant
Filed:
October 28, 2010
Date of Patent:
January 21, 2014
Assignee:
Janssen Pharmaceutica NV
Inventors:
Michael H. Parker, Dennis J. Hlasta, Yifang Huang, Allen B. Reitz, Edward C. Lawson, Carsten Schubert, Eric Strobel, Brett A. Tounge, Kimberly White, Michael P. Winters, Shyamali Ghosh
Abstract: The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
Type:
Grant
Filed:
March 22, 2012
Date of Patent:
January 21, 2014
Assignee:
Sanofi-Aventis U.S. LLC
Inventors:
Nakyen Choy, John J. Shay, Jr., Adam W. Sledeski
Abstract: Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R5, R6 and R13 are defined herein.
Type:
Grant
Filed:
March 31, 2009
Date of Patent:
January 21, 2014
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Shoujun Chen, Jun Jiang, Lijun Sun, Keizo Koya
Abstract: The present invention provides an improved process for the synthesis of nebivolol or its pharmaceutically acceptable salts, more particularly hydrochloride salt of formula (I). The present invention further provides a new Form T1 of nebivolol and its pharmaceutically acceptable salts. The present invention also provides pharmaceutical compositions and process for the preparation of a solid oral dosage form of nebivolol hydrochloride of formula (I), without the use of wetting agent, and optionally using binder and/or disintegrant.
Abstract: The present invention is directed to AHCY inhibitors of formula (I): which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.
Type:
Grant
Filed:
August 31, 2009
Date of Patent:
January 14, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Antonella Converso, Timothy J. Hartingh, Mark E. Fraley
Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.
Type:
Grant
Filed:
November 9, 2012
Date of Patent:
January 7, 2014
Assignees:
The Regents of the University of California, The University of Connecticut
Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alkyl groups, and optionally having hydroxyl and/or alkoxyl groups substituents.
Type:
Grant
Filed:
July 6, 2012
Date of Patent:
December 31, 2013
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Helen E. Blackwell, Matthew D. Bowman, Jennifer C. O'Neill, Joseph R. Stringer
Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
December 17, 2013
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
Type:
Grant
Filed:
October 12, 2012
Date of Patent:
December 10, 2013
Assignee:
Hoffman-La Roche Inc.
Inventors:
Pascal Dott, Steven Paul Hanlon, Stefan Hildbrand, Hans Iding, Andrew Thomas, Pius Waldmeier
Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.
Abstract: The present invention provides an improved process for the synthesis of nebivolol or its pharmaceutically acceptable salts, more particularly hydrochloride salt of formula (I). The present invention further provides a new Form T1 of nebivolol and its pharmaceutically acceptable salts. The present invention also provides pharmaceutical compositions and process for the preparation of a solid oral dosage form of nebivolol hydrochloride of formula (I), without the use of wetting agent, and optionally using binder and/or disintegrant.
Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Grant
Filed:
February 27, 2012
Date of Patent:
December 3, 2013
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
December 3, 2013
Assignee:
Akebia Therapeutics, Inc.
Inventors:
Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
Type:
Grant
Filed:
November 24, 2009
Date of Patent:
December 3, 2013
Assignee:
Janssen Pharmaceutica NV
Inventors:
J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Seierstad