Abstract: Disclosed are CRTH2 inhibitors represented by Structural Formula (I): The values for the variables of Structural Formula (I) are provided herein.
Type:
Grant
Filed:
February 23, 2006
Date of Patent:
May 31, 2011
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Jeremy D. Little, Shomir Ghosh, Sean Harrison, Amy M. Elder, Christelle C. Renou, Kenneth G. Carson
Abstract: The invention relates to compounds of formula (I): wherein Ra, R1, Ar, L, A, W, Y, and Z are as defined in the disclosure; to compositions containing them; and to the preparation and use thereof, in particular as anticancer agents.
Type:
Grant
Filed:
October 11, 2007
Date of Patent:
May 24, 2011
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Michel Tabart, Eric Bacque, Frank Halley, Baptiste Ronan, Pascal Desmazeau, Fabrice Viviani, Catherine Souaille
Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
August 26, 2008
Date of Patent:
May 24, 2011
Assignee:
Theravance, Inc.
Inventors:
Daisuke Roland Saito, Daniel D. Long, John R. Jacobsen
Abstract: Novel thienopyridine derivatives of the formula (I), in which R1, R2, R3 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
Abstract: The present invention is directed to novel cyclopropanated macrocyclic ketone and lactone compounds of the general formula: wherein X is an atom or a functional group selected from the group consisting of O, N, S, R—CH, and CH2; wherein R is a C1-C3 alkyl group; wherein Y and W independently represent is a linear or branched alkyl or alkenyl group, optionally substituted, consisting of less than 10 and preferably less than 7 carbon atoms; and wherein O is an oxygen atom, and the use of these novel compounds in creating fragrances and scents in items such as perfumes, colognes, and personal care products.
Type:
Grant
Filed:
December 5, 2008
Date of Patent:
May 17, 2011
Assignee:
International Flavors & Fragrances Inc.
Inventors:
Anubhav P. S. Narula, Edward Mark Arruda, Franc T. Schiet
Abstract: The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-? activity.
Type:
Grant
Filed:
November 16, 2007
Date of Patent:
May 17, 2011
Assignee:
Millenium Pharmaceuticals, Inc.
Inventors:
Anjali Pandey, Robert M. Scarborough, Meenakshi S. Venkatraman
Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and 6,7,8,9-tetrahydroimidazonaphthyridines) with a sulfide-, sulfinyl-, or sulfonyl-containing ether substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
Type:
Grant
Filed:
December 3, 2004
Date of Patent:
May 10, 2011
Assignee:
3M Innovative Properties Company
Inventors:
Matthew R. Radmer, William H. Moser, Joan T. Moseman, Joseph F. Dellaria, Jr.
Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Type:
Grant
Filed:
August 30, 2007
Date of Patent:
May 10, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Andreas D. Christ, Rainer E. Martin, Peter Mohr
Abstract: Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
Abstract: Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
Type:
Grant
Filed:
July 20, 2005
Date of Patent:
April 26, 2011
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rajashekhar Betageri, Thomas A. Gilmore, Daniel Kuzmich, John Robert Proudfoot, David S. Thomson
Abstract: This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor.
Abstract: The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.
Abstract: The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
Abstract: The present invention relates to the compound of the formula To methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
April 5, 2011
Assignee:
Schering Corporation
Inventors:
Pauline C. Ting, Joe F. Lee, Kung-I Feng, Michael R. Reeder, Scott T. Trzaska, Man Zhu, Chen Mao, Dimitar L. Filipov, Dimitrios N. Zarkadas
Abstract: Compounds of the formula: wherein: n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCl, 5-OMe; 2,4-diCl; 3,4,5-tri-OMe; 2-Cl, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCl, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 16, 2008
Date of Patent:
April 5, 2011
Assignee:
Wyeth LLC
Inventors:
Frank Boschelli, Jennifer M. Golas, Kim T. Arndt
Abstract: The present invention is related to a compound of formula (I) wherein R1, R2, R3 and R4 are as defined herein, or an addition salt of an acid thereof, the pharmaceutical composition and preparation thereof, and the therapeutic use thereof in the treatment or the prevention of diseases involving Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
March 29, 2011
Assignee:
Sanofi-Aventis
Inventors:
Antonio Almario Garcia, Patrick Lardenois, Anne Olivier
Abstract: This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.
Type:
Grant
Filed:
June 1, 2004
Date of Patent:
March 29, 2011
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Usha V. Ramesh, Gary Charles Look, Rajinder Singh, Sarkiz D. Issakani
Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
Type:
Grant
Filed:
June 3, 2005
Date of Patent:
March 29, 2011
Assignee:
Merck Patent GmbH
Inventors:
Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Dirk Finsinger, Wolfgang Staehle, Christiane Amendt, Ulrich Emde, Frank Zenke
Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
Type:
Grant
Filed:
May 21, 2010
Date of Patent:
May 17, 2011
Assignee:
Wyeth Holdings Corporation
Inventors:
Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Philip Frost