Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,
Type:
Grant
Filed:
March 13, 2015
Date of Patent:
April 5, 2016
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
Abstract: The present invention relates to a process for the preparation of d-threo-ritalinic acid salt thereof. More particularly, the present invention relates a process for the preparation of d-threo-ritalinic acid salt via novel organic salts of intermediate thereof.
Abstract: An improved process or method of synthesis of carfentanil and other potent opioid analgesics of the N-alkyl 4-substituted 4-piperdinylamide class which can be used as morphine substitutes.
Type:
Grant
Filed:
May 23, 2014
Date of Patent:
March 8, 2016
Assignee:
The United States of America as Represented by the Secretary of the Army
Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
March 31, 2014
Date of Patent:
March 8, 2016
Assignee:
GRÜNENTHAL GMBH
Inventors:
Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Type:
Grant
Filed:
July 2, 2014
Date of Patent:
February 23, 2016
Assignees:
Janssen Pharmaceuticals, Inc., Addex Pharma SA
Inventors:
Hassan Julien Imogai, Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MacDonald, Shriley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Patrick Finn, Gagik Melikyan
Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
Type:
Grant
Filed:
March 3, 2015
Date of Patent:
February 16, 2016
Assignee:
THESAN PHARMACEUTICALS, INC.
Inventors:
Stephen D. Barrett, James B. Kramer, Mark L. Boys, Huifen Chen
Abstract: A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.
Type:
Grant
Filed:
July 19, 2007
Date of Patent:
February 16, 2016
Assignee:
AbbVie Inc.
Inventors:
Todd S. McDermott, Seble H. Wagaw, Kenneth M. Engstrom, Jorge Gandarilla, Albert Kruger, Michael J. Rozema, Michael G. Fickes, Steven J. Wittenberger, Lakshmi Bhagavatula, Thomas B. Borchardt
Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
Type:
Grant
Filed:
February 18, 2015
Date of Patent:
February 2, 2016
Assignee:
AstraZeneca AB
Inventors:
Robert Bruce Diebold, Thomas Woodrow Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh
Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
Type:
Grant
Filed:
November 25, 2014
Date of Patent:
February 2, 2016
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Sabine Axt, Timothy J. Church, Viengkham Malathong
Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X and G are each as defined in the description, and agrochemically active salts, metal complexes and N-oxides thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
Type:
Grant
Filed:
September 12, 2014
Date of Patent:
February 2, 2016
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Tomoki Tsuchiya, Pierre Wasnaire, Jurgen Benting, Daniela Portz, Ulrike Wachendorff-Neumann, Stefan Hillebrand
Abstract: One aspect of the invention relates to compounds, compositions and methods for treating oxidative stress and/or hypertension. In certain embodiments, the invention relates to a mixture of tempol and an angiotensin receptor blocker (ARB) and the use of said mixture to treat oxidative stress and/or hypertension. In certain embodiments, the invention relates to a tempol/ARB adduct and the use of said adduct to treat oxidative stress and/or hypertension.
Type:
Grant
Filed:
September 17, 2010
Date of Patent:
January 12, 2016
Assignee:
Georgetown University
Inventors:
Milton L. Brown, Yali Kong, Christopher Stuart Wilcox
Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
Abstract: The present application describes modulators of chemokine receptor activity of formula I or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
Type:
Grant
Filed:
October 1, 2014
Date of Patent:
December 29, 2015
Assignee:
Bristol-Myers Squibb Company
Inventors:
T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
July 18, 2014
Date of Patent:
December 22, 2015
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Grant
Filed:
April 26, 2013
Date of Patent:
December 22, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
Abstract: The present invention relates to a novel polymorphic form of Fexofenadine hydrochloride, to a process for preparing it, to pharmaceutical compositions containing it, as well as its use. The invention also relates to intermediates useful for the preparation of Fexofenadine hydrochloride, antihistamine drug used in the treatment of allergy symptoms.
Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.
Type:
Grant
Filed:
June 11, 2014
Date of Patent:
December 15, 2015
Assignees:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN, VANDERBILT UNIVERSITY
Inventors:
Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter