Abstract: Compounds of the formula (I), in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
January 7, 2014
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
Type:
Grant
Filed:
June 2, 2011
Date of Patent:
January 7, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
Abstract: The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
Type:
Grant
Filed:
November 15, 2011
Date of Patent:
December 24, 2013
Assignee:
Acetylon Pharmaceuticals, Inc.
Inventors:
John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.
Type:
Grant
Filed:
December 15, 2009
Date of Patent:
December 17, 2013
Assignee:
Novartis AG
Inventors:
Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy
Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
March 24, 2009
Date of Patent:
December 10, 2013
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
September 17, 2010
Date of Patent:
December 3, 2013
Assignee:
Vanderbilt University
Inventors:
P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds and/or their pharmaceutically acceptable salts may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
Type:
Grant
Filed:
June 15, 2010
Date of Patent:
November 19, 2013
Assignee:
Cephalon, Inc.
Inventors:
Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
Abstract: Novel acid addition salts of 6-{2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy}-3-ethoxy-1,2-benzisoxazole of following formula are disclosed, particularly a crystalline form of a bis-dihydrogenphosphate salt: Such compounds have particular advantages with regard to treatment of picornaviruses. Related pharmaceutical compositions and methods of treating a picornavirus infection are also disclosed.
Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
April 29, 2008
Date of Patent:
November 12, 2013
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
Abstract: The present invention aims to provide a novel SCD inhibitor. The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.
Abstract: A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.
Type:
Grant
Filed:
December 23, 2011
Date of Patent:
October 29, 2013
Assignees:
Gilead Sciences, Inc., K.U. Leuven Research & Development
Inventors:
Eric D. Dowdy, Kenneth M. Kent, Norma J. Tom, Vahid Zia
Abstract: A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.
Type:
Grant
Filed:
July 6, 2007
Date of Patent:
October 29, 2013
Assignees:
Gilead Sciences, Inc., K.U. Leuven Research & Development
Inventors:
Steven S. Bondy, Terrence C. Dahl, David A. Oare, Reza Oliyai, Winston C. Tse, Vahid Zia
Abstract: The present disclosure provides pyridine urea compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, V and W are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
Type:
Grant
Filed:
December 6, 2011
Date of Patent:
October 22, 2013
Assignee:
Confluence Life Sciences, Inc.
Inventors:
Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas, Susan L. Hockerman
Abstract: A method for producing a 3-(substituted oxy)-4-pyridazinol compound represented by the following general formula (I): comprising reacting a compound represented by the following general formula (III): with a compound represented by the following general formula (IV): MO—R2??(IV). The compound represented by the general formula (I) can be reacted with a compound represented by the following general formula (VI): to provide a compound of general formula (V): Each of the groups in the formulas is defined. The compounds of general formulas (I) and (V) can be obtained in a high yield and with high selectivity at a low cost, and therefore various functional and active substances can be advantageously synthesized using the compounds as a medicine, an agricultural chemical, a functional material, or an intermediate thereof.
Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
Type:
Grant
Filed:
March 1, 2010
Date of Patent:
October 1, 2013
Assignee:
IRM LLC
Inventors:
Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.
Abstract: The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:
Type:
Grant
Filed:
March 13, 2008
Date of Patent:
September 17, 2013
Assignee:
Novartis AG
Inventors:
Miao Dai, Feng He, Rishi Kumar Jain, Rajesh Karki, Joseph Kelleher, III, John Lei, Luis Llamas, Michael A. Mcewan, Karen Miller-Moslin, Lawrence Bias Perez, Stefan Peukert, Naeem Yusuff
Abstract: A pyridazinone compound represented by formula (I) wherein R1 represents a C1-6 alkyl group or a (C1-6 alkyloxy) C1-6 alkyl group, R2 and R3 represent hydrogen or a C1-6 alkyl group, W represents halogen, etc., Z1 represents a C1-6 alkyl group, Z2 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, etc., and n represents 0, 1, 2, 3 or 4, has a weed-controlling effect and an arthropod-controlling effect.
Abstract: The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or trifluoromethyl; R4 is pyrrolidinyl, morpholinyl or pyridyl, amino or dimethylamino; R5 is trifluoromethyl or methylsulfonyl; R6 is hydrogen or methyl; and R7, R8, R9, R10 and R11 are independently hydrogen fluoro, cyano, chloro, methyl, trifluoromethyl, trifluoromethoxy or methylsulfonyl, provided that at least two of R7, R8, R9, R10 and R11 are hydrogen useful in the treatment of cancer.
Type:
Grant
Filed:
November 5, 2009
Date of Patent:
August 13, 2013
Assignee:
Eli Lilly and Company
Inventors:
Jolie Anne Bastian, Julia Marie Clay, Jeffrey Daniel Cohen, Philip Arthur Hipskind, Karen Lynn Lobb, Daniel Jon Sall, Michelle Lee Thompson, Takako Wilson (nee Takakuwa)