Abstract: The present invention relates to mono-sulfate and hemi-sulfate salts of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine, to crystalline and amorphous forms thereof and to their use in pharmaceutical formulations.
Type:
Grant
Filed:
October 14, 2011
Date of Patent:
December 11, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thomas Cleary, Alexander Glomme, Olaf Grassmann, Shan-Ming Kuang, Roland Meier, Doreen Miller, Regina Moog, Franziska E. Rohrer, Jason Yang
Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
Type:
Grant
Filed:
August 31, 2009
Date of Patent:
December 11, 2012
Assignee:
Novartis AG
Inventors:
Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
Abstract: The present invention is directed to solid forms of the Raf kinase inhibitor 1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine, as well as compositions thereof and uses of the same.
Type:
Grant
Filed:
February 28, 2008
Date of Patent:
December 4, 2012
Assignee:
Novartis AG
Inventors:
Ahmad Hashash, Kangwen L. Lin, Augustus O. Okhamafe
Abstract: The present invention relates to a defined crystalline modification of the compound of the formula (I), to processes for its preparation and to its use in agrochemical preparations.
Type:
Grant
Filed:
September 18, 2007
Date of Patent:
December 4, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Britta Olenik, Peter Jeschke, Robert Velten, Bernd Gallenkamp, Wolfgang Joerges, Ronald Vermeer, Leonardo Pitta
Abstract: A crystal of dexlansoprazole and sorbitol. The crystal is a co-crystal or a salt thereof of dexlansoprazole and sorbitol. There is also a method for making the co-crystal or salt thereof.
Abstract: The invention discloses a compound of general formula (I) and a process for preparing this compound. The invention discloses a fungicidal composition comprising a compound of general formula (I) and a method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
November 23, 2011
Date of Patent:
November 27, 2012
Assignee:
Bayer SAS
Inventors:
Pierre-Yves Coqueron, Philippe Desbordes, Darren James Mansfield, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Alain Villier, Pierre Genix
Abstract: Process for the preparation of crystalline anhydrous (R)-2-[[[3-methyl-4-(2,2,2-trifluoroetoxy)-2-piridyl]methyl]sulphinyl]benzimidazole (dexlansoprazole).
Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.
Abstract: Saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines=compounds corresponding to formula (I), wherein the various substituents have the meaning provided in the description, and pharmaceutical formulations containing these compounds and methods for producing these compounds and related pharmaceutical formulation, and to methods for treating or inhibiting pain, depression and/or anxiety states.
Type:
Grant
Filed:
December 22, 2006
Date of Patent:
October 2, 2012
Assignee:
Gruenenthal GmbH
Inventors:
Bernd Sundermann, Hagen-Heinrich Hennies, Klaus Schiene, Petra Bloms-Funke, Werner Englberger, Sven Frormann, Derek Saunders
Abstract: Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.
Type:
Grant
Filed:
October 5, 2011
Date of Patent:
October 2, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jeremy Green, Jingrong Cao, Upul Keerthi Bandarage, Jon H. Come, Craig Marhefka
Abstract: Object Provided are ?-form crystal, ?-form crystal, and ?-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance. Means for Resolution A solving means includes ?-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150° C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2?(°), and the like.
Abstract: The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
September 25, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y. S. Lam
Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
Type:
Grant
Filed:
July 22, 2009
Date of Patent:
September 25, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
Abstract: Disclosed is a process for producing compound C represented by formula C: wherein R? represents straight chain, branched chain, or cyclic C2-6 alkylcarbonyl, wherein R1b is used as a protective group for hydroxyl at the 7-position of compound C.
Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
Type:
Grant
Filed:
June 24, 2011
Date of Patent:
September 4, 2012
Assignee:
Schering Corporation
Inventors:
George G. Wu, Anantha Sudhakar, Tao Wang, Ji Xie, Frank X. Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia Zavialov, Hoa N. Nguyen, Ngiap Kie. Lim
Abstract: A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.
Abstract: The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
Type:
Grant
Filed:
April 15, 2006
Date of Patent:
August 28, 2012
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Ingo Flamme, Jens-Kerim Ergüden, Felix Oehme, Kai Thede, Gunter Karig, Alexander Kuhl, Hanno Wild, Joachim Schuhmacher, Peter Kolkhof, Lars Bärfacker, Joachim Hütter
Abstract: The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent. The present invention also relates to novel crystalline omeprazole sodium form E and crystalline omeprazole sodium form F as well to the processes for their preparation as well, both with considerably low levels of residual solvents. Omeprazole sodium form A and both novel crystalline forms omeprazole sodium form E and form F are useful for the treatment of gastrointestinal disorders.
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
August 21, 2012
Assignee:
Lek Pharmaceuticals d.d.
Inventors:
Lidija Vranicar Savanovic, Zoran Ham, Janez Rzen
Abstract: The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.