Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.
Abstract: The invention relates to substituted amidine compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amidine compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted amidine compounds. The substituted amidine compounds of the present invention are defined by the following formula I: wherein A1 to A4, B1 to B3, R1 to R3, (R4)p, (R5)q, X and Y are defined as in the description.
Type:
Grant
Filed:
December 14, 2009
Date of Patent:
January 21, 2014
Assignee:
BASF SE
Inventors:
Florian Kaiser, Karsten Koerber, Matthias Pohlman, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Wolfgang von Deyn, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Cecille Ebuenga
Abstract: The present invention relates to amino-4-methyl imidazoles and pharmaceutically-acceptable salts thereof. The compound may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
Type:
Grant
Filed:
October 15, 2007
Date of Patent:
November 19, 2013
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
Type:
Grant
Filed:
October 20, 2010
Date of Patent:
February 26, 2013
Assignee:
FAB Pharma S.A.S.
Inventors:
Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
Abstract: The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
November 1, 2011
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Jochen Goerlitzer, Heiner Glombik, Eugen Falk, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
Abstract: Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.
Type:
Grant
Filed:
December 4, 2009
Date of Patent:
August 2, 2011
Assignee:
Galderma Research & Development
Inventors:
Jean Guy Boiteau, Corinne Millois Barbuis, Karine Bouquet
Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.
Type:
Grant
Filed:
June 17, 2008
Date of Patent:
May 17, 2011
Assignee:
3M Innovative Properties Company
Inventors:
Karl E. Benson, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. I. Moore, Rahul Shah
Abstract: Methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase I? activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.
Type:
Grant
Filed:
November 12, 2008
Date of Patent:
April 12, 2011
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William Arthur Metz, Jr., Fa-Xiang Ding
Abstract: Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Type:
Grant
Filed:
June 13, 2006
Date of Patent:
February 15, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingwu Duan, Zhonghui Lu, David S. Weinstein, Bin Jiang
Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
July 1, 2009
Date of Patent:
December 7, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Nicole Zimmermann, Peter D. J. Grootenhuis, Mehdi Michel Djamel Numa, Dean Stamos, Corey Don Anderson, Tara Whitney
Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Grant
Filed:
May 16, 2006
Date of Patent:
April 14, 2009
Assignee:
Kalypsys Inc.
Inventors:
James W. Malecha, Sergio G. Duron, Andrew K. Lindstrom
Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Grant
Filed:
October 25, 2005
Date of Patent:
February 24, 2009
Assignee:
Kalypsys, Inc
Inventors:
Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
Abstract: This invention generally relates to the derivatives of 1-substituted-3-pyrroli dines having the structure of Formula (I): The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.
Type:
Grant
Filed:
December 23, 2002
Date of Patent:
December 16, 2008
Assignee:
Ranbaxy Laboratories Limited
Inventors:
Anita Mehta, Jang Bahadur Gupta, Pakala Kumara Savithru Sarma
Abstract: Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.
Type:
Grant
Filed:
April 25, 2003
Date of Patent:
December 9, 2008
Assignee:
Gilead Sciences, Inc.
Inventors:
James M. Chen, Xiaowu Chen, Choung U. Kim, William A. Lee, Christopher P. Lee, Peter H. Nelson, James D. Tario, Lianhong Xu
Abstract: The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-?-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.
Type:
Grant
Filed:
July 19, 2004
Date of Patent:
December 9, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
David H Igo, Paul R Johnson, Daniel E Patterson, Amarjit Sab Randhawa
Abstract: Novel phosphonate compounds are provided including a phosphonoglyoxylamide ester, an ?-keto phosphonophosphinate ester, a carbonylbisphosphonate analog of a nucleotide, and a diazomethylenebisphosphonate analog of a nucleotide, as well as methods of making synthetically and medically useful ?-keto phosphonate compounds.
Type:
Grant
Filed:
July 30, 2002
Date of Patent:
December 9, 2008
Assignee:
University of Southern California
Inventors:
Charles E. McKenna, Boris A. Kashemirov, Patricia I. Bonaz-Krause
Abstract: The present invention provides a VDAC regulator comprising a compound represented by the formula (I): wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group; a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of Down's syndrome and the like.
Type:
Grant
Filed:
March 13, 2003
Date of Patent:
December 9, 2008
Assignees:
Takeda Pharmaceutical Company Limited, Tokyo Institute of Technology