Abstract: A class of novel 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 (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd 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:
January 12, 2006
Date of Patent:
January 5, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
T. G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
Abstract: The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.
Type:
Grant
Filed:
November 25, 2005
Date of Patent:
December 22, 2009
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
José Ignacio Andrés-Gil, José Manuel Bartolomé-Nebreda, Manuel Jesus Alcázar-Vaca, Maria de las Mercedes Garcia-Martin, Antonius Adrianus Hendrikus Petrus Megens
Abstract: The invention relates to 5-(oximinoalkyl- and hydrazonalkyl-amino)pyrazole derivatives of formula (I) or salts thereof: formula (I), wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
Type:
Grant
Filed:
December 22, 2006
Date of Patent:
December 1, 2009
Assignee:
Merial Limited
Inventors:
David Chou, Werner Knauf, Michael Maier, Friederike Lochhaas, Karl Seeger
Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
Type:
Grant
Filed:
December 21, 2006
Date of Patent:
November 24, 2009
Assignees:
Zealand Pharma A/S, Wyeth
Inventors:
Bjarne Due Larsen, Jørgen Søberg Petersen, Ketil Jørgen Haugan, John A. Butera, James K. Hennan, Edward H. Kerns, Evgueni L. Piatnitski
Abstract: The present invention provides compounds of formula (I) wherein A is (1), (2), (3), (4), (5), (6) or (7) and wherein R1, R7, y and Ar1 are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.
Type:
Grant
Filed:
May 19, 2005
Date of Patent:
November 10, 2009
Assignee:
Eli Lilly and Company
Inventors:
John Richard Harris, Barry Peter Clark, Peter Thaddeus Gallagher, Maria Ann Whatton
Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
October 11, 2005
Date of Patent:
November 3, 2009
Assignee:
Amgen Inc.
Inventors:
Toshihiro Aya, Guolin Cai, Jian J. Chen, Derin D'Amico, Thomas Nguyen, Wenyuan Qian
Abstract: The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
Type:
Grant
Filed:
May 24, 2004
Date of Patent:
November 3, 2009
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Martin Eberle, Philipp Ermert, Daniel Obrecht, Frank Lach, Anatol Luther, Felix Bachmann, Allessandro Strebel
Abstract: The present invention relates to thiazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.
Type:
Grant
Filed:
June 27, 2005
Date of Patent:
October 6, 2009
Assignee:
deCODE genetics ehf
Inventors:
Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof wherein m, n, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
Type:
Grant
Filed:
July 12, 2006
Date of Patent:
September 1, 2009
Assignee:
Roche Palo Alto LLC
Inventors:
Timothy Owens, Steven Sethofer, Keith Adrian Walker, Shu Hai Zhao
Abstract: The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene -5,4?-imidazol]-5?(1?H)-one compound of formula I Also provided are methods and compositions for the inhibition of ?-secretase (BACE) and the treatment of ?-amyloid deposits and neurofibrillary tangles.
Type:
Grant
Filed:
February 23, 2007
Date of Patent:
September 1, 2009
Assignee:
Wyeth
Inventors:
Dominick Anthony Quagliato, Patrick Michael Andrae, Yi Fan
Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.
Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
Type:
Grant
Filed:
January 23, 2004
Date of Patent:
August 11, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
Abstract: A salt of the compound N-{2-tert-butyl-1-[(4,4-difluorocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide, which is an ethanesulphonic acid salt, a sulphuric acid salt, an ethane disulphonic acid salt, a hydrochloric acid salt, a hydrobromic acid salt, a phosphoric acid salt, an acetic acid salt, a fumaric acid salt, a maleic acid salt, a tartaric acid salt, a citric acid salt, a methanesulphonic acid salt, or a p-toluenesulphonic acid salt of said compound.
Abstract: This invention provides compounds of Formula (I), N-oxides and suitable salts thereof, wherein A and B are independently O or S; each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; K is, together with the two contiguous linking carbon atoms, a 5- or 6-membered heteroaromatic ring optionally substituted with 1 to 3 R4; and R1 R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I), an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).
Type:
Grant
Filed:
June 21, 2005
Date of Patent:
July 14, 2009
Assignee:
E.I. du Pont de Nemours and Company
Inventors:
Gary David Annis, Bruce Lawrence Finkelstein
Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
Type:
Grant
Filed:
August 5, 2003
Date of Patent:
July 14, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
Abstract: The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors. Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
March 21, 2006
Date of Patent:
June 30, 2009
Assignee:
Merck Frosst Canada Ltd.
Inventors:
Marc Blouin, Erich L. Grimm, Yves Gareau, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Richard Friesen
Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.