Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/332)
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Publication number: 20110245242Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R10 and L1, L2, E1, E2, E3, Y and Z have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hille, Kerstin Ilgö, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Arnd Voerste, Peter Dahmen, Rurth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano
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Publication number: 20110230497Abstract: The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.Type: ApplicationFiled: November 2, 2009Publication date: September 22, 2011Applicant: H. Lundbeck A/SInventors: John Matthew Peterson, Chien-An Chen, Bin Chen, Lingyun Wu, Michael Lloyd Sabio
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Publication number: 20110230507Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: September 22, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, John Keily
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Publication number: 20110218208Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20110212965Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: ApplicationFiled: May 11, 2011Publication date: September 1, 2011Applicant: METHYLGENE INC.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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Publication number: 20110212939Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: September 1, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Philip Graham Clarke, Graham John Dawson, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Thomas Martin Krulle, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Patent number: 8008312Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor, and in particular to inhibit viral entry of certain viruses. Certain compounds in particular can reduce entry of immunodeficiency virus (HIV) into a cell while not reducing the capacity of stem cells to proliferate, and therefore can be useful for long term treatment regimes. The compounds are useful in particular in the treatment or prevention of HIV infections.Type: GrantFiled: January 9, 2006Date of Patent: August 30, 2011Assignee: Emory UniversityInventors: Hyunsuk Shim, Dennis C. Liotta, James P. Snyder, Weiqiang Zhan, Zhongxing Liang
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Patent number: 8008037Abstract: A chemistry matrix for use in determining the concentration of an analyte in a biological fluid includes a glucose dehydrogenase, nicotinamide adenine dinucleotide, an alkylphenazine quaternary salt, and/or a nitrosoaniline. The chemistry matrix is used with an electrochemical biosensor to determine the concentration of an analyte after a reaction occurs within the biosensor, at which time an analysis is completed to determine the concentration. A method of determining the concentration of an analyte using the chemistry matrix of glucose dehydrogenase, nicotinamide adenine dinucleotide, an alkylphenazine quaternary salt, and/or a nitrosoaniline is another aspect that is described. The method also further features test times of five seconds or less. Methods utilizing the new chemistry matrix can readily determine an analyte such as blood glucose at concentrations of from about 20-600 mg/dL at a pH of from about 6.5 to about 8.5.Type: GrantFiled: March 27, 2008Date of Patent: August 30, 2011Assignee: Roche Diagnostics Operations, Inc.Inventors: Christopher D. Wilsey, Mitali Ghoshal, Herbert Wieder
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Patent number: 8003655Abstract: The invention relates to substituted sulphoximines according to the general formula (I): in which A, E, G, X, R1, R2, R3, R4, R5, R6, R7, R8, m, p, q, are given in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted sulphoximines, to methods of preparing said substituted sulphoximines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.Type: GrantFiled: July 11, 2007Date of Patent: August 23, 2011Assignee: Bayer Schering Pharma AGInventors: Ingo Hartung, Georg Kettschau, Hans Briem, Karl-Heinz Thierauch, Ulrich Luecking, Ulf Boemer, Martin Krueger
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Patent number: 8003789Abstract: This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halType: GrantFiled: October 31, 2007Date of Patent: August 23, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries
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Publication number: 20110201580Abstract: The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.Type: ApplicationFiled: February 4, 2011Publication date: August 18, 2011Applicant: Chiesi Farmaceutici S.p.A.Inventors: Eleonora GHIDINI, Andrea RIZZI, Andrea VIRDIS, Fabio RANCATI, Anna RENCUROSI
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Publication number: 20110201606Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising themType: ApplicationFiled: April 27, 2011Publication date: August 18, 2011Applicant: Novartis AGInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
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Publication number: 20110196147Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: April 4, 2011Publication date: August 11, 2011Inventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110190499Abstract: The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.Type: ApplicationFiled: August 10, 2010Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter LINZ, Gerd KRAEMER, Sabrina KUSSEROW, Juergen SCHNAUBELT
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Publication number: 20110172204Abstract: A compound of the formula: wherein: R1 represents C1-6 alkyl or H; Y represents —NR2R3 as depicted in formula (B), or a ring of formula (A) wherein a represents the point of attachment to the pyrimidinyl ring; R2 represents C1-4alkyl substituted by C1-3 alkoxy; R3 represents C1-4 alkyl; W represents —(CH2)n—; W1 represents —(CH2)p—; n represents 1 or 2 or 3; p represents 1 or 2; R4 represents C1-4 alkoxy, C1-6 alkyl or halogen; and R5 represents halogen or H, provided that, when R4 represents halogen, R5 is not H, or a pharmaceutically acceptable salt thereof. The compounds of the invention have been found to modulate the histamine H3 receptor.Type: ApplicationFiled: January 7, 2011Publication date: July 14, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Parminder Kaur Pooni, Kevin John Merchant, William John Buffham
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Publication number: 20110166137Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: July 7, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
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Publication number: 20110166155Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: January 6, 2011Publication date: July 7, 2011Inventors: Bradford VAN WAGENEN, Radhakrishnan UKKIRAMAPANDIAN, Joshua CLAYTON, Ian EGLE, James R. EMPFIELD, Methvin ISAAC, Fupeng MA, Abdelmalik SLASSI, Gary STEELMAN, Rebecca URBANEK, Sally WALSH
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Publication number: 20110166117Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 30, 2010Publication date: July 7, 2011Inventors: Roger Bonnert, Stephen Brough, Andrew Davies, Timothy Luker, Thomas McInally, Ian Millichip, Garry Pairaudeau, Anil Patel, Rukhsana Rasul, Stephen Thom
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Publication number: 20110160455Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: ApplicationFiled: September 23, 2010Publication date: June 30, 2011Applicant: AstraZeneca UK Ltd.Inventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Patent number: 7968707Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 27, 2007Date of Patent: June 28, 2011Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Publication number: 20110152236Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.Type: ApplicationFiled: August 13, 2009Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
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Publication number: 20110150833Abstract: Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: June 23, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Yen Ting Chen, Yan Yin, Hampton Sessions, Michael P. Smolinski, Lei Yao, Bo Wang, Bozena Frackowiak-Wojtasek
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Publication number: 20110152235Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20110144081Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Publication number: 20110135604Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Anthony Casarez, Mingzhe Ji, Choung U. Kim, Xiaoning C. Sheng, Qiaoyin Wu
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Patent number: 7951803Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: GrantFiled: March 9, 2007Date of Patent: May 31, 2011Assignee: Pharmacopeia, LLCInventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
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Publication number: 20110124669Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).Type: ApplicationFiled: February 4, 2011Publication date: May 26, 2011Applicant: SARcode CorporationInventors: Wang Shen, Kenneth Barr, Johan D. Oslob, Min Zhong
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Publication number: 20110124647Abstract: The present invention relates to novel derivatives of substituted benzylamines, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 28, 2008Publication date: May 26, 2011Applicant: Bayer CropScience AGInventors: Christian Arnold, Ulrich Görgens, Hans-Georg Schwarz, Graham Holmwood, Roland Andree, Olga Malsam, Otto Schallner, Eva-Marie Franken, Horst-Peter Antonicek, Stefan Werner
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Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
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Publication number: 20110105532Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20110105543Abstract: This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R1, R2, R3, R4 and R5. independently of each other, represent hydrogen, halo, tri-fluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkoxy, alkyl, amino or sulfamoyl; or R1 and R2, together with the phenyl ring to which they are attached form an indolyl ring or a benzo-dioxolyl ring; and R3, R4 and R5 are as defined above; and R6 represents amino or nitro, which are found to be modulators of the nicotinic acetylcholine receptors.Type: ApplicationFiled: March 9, 2009Publication date: May 5, 2011Applicant: NeuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
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Publication number: 20110105324Abstract: What is described are compounds of the formula (I) in which the respective substituents have the meanings given in the description. The compounds of the formula (I) can be used as herbicides and plant growth regulators.Type: ApplicationFiled: April 11, 2009Publication date: May 5, 2011Applicant: BAYER CROPSCIENCE AGInventors: Christoph Hugh Rosinger, Dieter Feucht, Klaus-Helmut Mueller, Isolde Haeuser-Hahn, Jan Dittgen, Ernst Rudolf Gesing, Christian Waldraff
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Publication number: 20110098313Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.Type: ApplicationFiled: October 20, 2010Publication date: April 28, 2011Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 7932246Abstract: Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N? or —C?; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.Type: GrantFiled: May 15, 2006Date of Patent: April 26, 2011Assignee: Chroma Therapeutics Ltd.Inventors: David Festus Charles Moffat, Sanjay Ratilal Patel, Francesca Ann Mazzei, Andrew James Belfield, Sandra Van Meurs
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Patent number: 7932387Abstract: Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] (also known as rosuvastatin) calcium salt and hydrates can exist in new crystal forms B and C. These crystal forms provide a higher diversity on crystalline materials to optimize manufacture, formulation and biological efficiency.Type: GrantFiled: January 23, 2006Date of Patent: April 26, 2011Assignee: BASF SEInventors: Fritz Blatter, Paul Adriaan Van Der Schaaf, Martin Szelagiewicz
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Publication number: 20110092526Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.Type: ApplicationFiled: October 19, 2010Publication date: April 21, 2011Applicant: ASTRAZENECA ABInventors: Stuart Norman Lile Bennett, Frederick Woolf Goldberg, Andrew Leach, Paul Robert Owen Whittamore, Pernilla Sörme
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Patent number: 7919618Abstract: Novel methods of synthesizing piperazines, piperidines and related compounds are disclosed, as are compounds useful for their preparation.Type: GrantFiled: August 2, 2007Date of Patent: April 5, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hugh Alfred Burgoon, Jr., Ramanaiah C. Kanamarlapudi, Wenxue Wu
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Publication number: 20110077403Abstract: The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.Type: ApplicationFiled: March 19, 2009Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Adil Duran, Stefan Goepper, Joerg Halmer, Michael Konrad
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Publication number: 20110071134Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:Type: ApplicationFiled: April 26, 2010Publication date: March 24, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Zhan Shi, Brendan S. Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
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Patent number: 7906511Abstract: The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a salt thereof is provided. In the formula, the ring X represents: R1 and R2 independently represent a hydrogen atom, an alkyl group, an aryl group, an aromatic heterocyclic group or the like; R3 represents a hydrogen atom, a halogen atom, a hydroxy group, an alkoxy group, an aryloxy group, an alkyl group, an aryl group, an amino group, an alkylamino group or the like; A1 represents a sulfur atom or the like; and A2 represents an alkylene group.Type: GrantFiled: March 31, 2006Date of Patent: March 15, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Publication number: 20110053912Abstract: A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.Type: ApplicationFiled: March 29, 2010Publication date: March 3, 2011Applicant: Astellas Pharma Inc.Inventors: Yuji Matsushima, Hirokazu Kubota, Hisao Hamaguchi, Yoshinori Okamoto, Takeshi Hondo, Fusako Nishigaki
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Publication number: 20110053901Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.Type: ApplicationFiled: February 13, 2009Publication date: March 3, 2011Applicants: SIGNUM BIOSCIENCES, INC., Signum Biosciences, Inc.Inventors: Seung-Yub Lee, Michael Voronkov, Peter Wolanin
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Patent number: 7897627Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: GrantFiled: December 15, 2008Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20110028501Abstract: Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 26, 2009Publication date: February 3, 2011Inventors: Harold B Wood, Jason W. Szewczyk, Yong Huang, Alan D. Adams
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Patent number: 7879860Abstract: The invention relates to the delta and epsilon crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide (the compound of formula I, see below), certain processes for their preparation, pharmaceutical compositions containing these crystal forms, and their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.Type: GrantFiled: August 24, 2006Date of Patent: February 1, 2011Assignee: Novartis AGInventor: Michael Mutz