The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
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Patent number: 8748603Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.Type: GrantFiled: July 12, 2011Date of Patent: June 10, 2014Assignee: AstraZeneca ABInventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
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Publication number: 20140148430Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: November 26, 2012Publication date: May 29, 2014Applicant: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
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Patent number: 8735579Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: GrantFiled: August 26, 2009Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
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Publication number: 20140141099Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Inventors: Julian Golec, John Pollard, James Westcott, Hayley Binch, Michael Mortimore, Daniel Robinson
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Publication number: 20140128570Abstract: The present invention relates to ?-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.Type: ApplicationFiled: April 6, 2012Publication date: May 8, 2014Inventors: Danith H. Ly, Srinivas Rapireddy, Bichismita Sahu
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Patent number: 8703781Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.Type: GrantFiled: October 15, 2010Date of Patent: April 22, 2014Assignee: GlaxoSmithKline LLCInventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
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Publication number: 20140107139Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.Type: ApplicationFiled: June 7, 2012Publication date: April 17, 2014Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
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Publication number: 20140094604Abstract: The present invention is related to new intermediates and processes for preparing Ticagrelor disclosed in this patent application.Type: ApplicationFiled: April 6, 2012Publication date: April 3, 2014Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Vinod Kumar Kansal, Dhirenkumar Mistry, Sanjay Vasoya, Ghanshyam Pandey, Amlt Taneja, Pramond Kadappa, Jiri Stohandl, Jaroslay Frantisek
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Publication number: 20140079636Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: March 15, 2013Publication date: March 20, 2014Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140081023Abstract: 2-Amino-5,8-dialkoxy[1,2,4]-triazolo[1,5-c]pyrimidines are manufactured from 4-chloro-2,5-dialkoxypyrimidines in a process that avoids hydrazine and cyanogen halide.Type: ApplicationFiled: September 10, 2013Publication date: March 20, 2014Applicant: DOW AGROSCIENCES LLCInventors: Douglas C. Bland, Gary Roth, Craig Bott, Christopher T. Hamilton, Joseph Neuman
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Patent number: 8673926Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.Type: GrantFiled: February 14, 2013Date of Patent: March 18, 2014Assignee: University of Georgia Research Foundation, Inc.Inventor: Chung K. Chu
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Publication number: 20140073651Abstract: The invention relates to benzamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: February 21, 2012Publication date: March 13, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Mark Murphy, Dorte Renneberg
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Patent number: 8653267Abstract: The present invention discloses a co-crystal compound of optical devices. The co-crystal compound is crystallized out with hydrogen bonding by a temperature fluctuation method after mixing small organic molecules without optoelectronic properties and organic molecules having heterocyclic rings with optoelectronic properties. The photoluminescence (PL) intensity of this hydrogen-bonded co-crystal compound according to the present invention can vary with a variety of the small organic molecules without optoelectronic properties, so as to modulate the PL intensity.Type: GrantFiled: May 11, 2010Date of Patent: February 18, 2014Assignee: National Central UniversityInventors: Tu Lee, Pu-Yun Wang
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Publication number: 20140045862Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.Type: ApplicationFiled: January 31, 2013Publication date: February 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventor: Daiichi Sankyo Company, Limited
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Publication number: 20140046062Abstract: The present invention relates to improved process for the preparation of lamivudine or emtricitabine. Thus, (1?R,2?S,5?R)-menthyl-5(R,S)-acetoxy-[1,3]-oxathiolane-2(R)-carboxylate is reacted with N-propinoyl cytosine in hexamethyl disilazane and then added trityl perchlorate to obtain a solid containing (1?R,2?S,5?R)-menthyl-5S-(N-4?-propionylcytosin-1?-yl)-[1,3]-oxathiolane-2R-carboxylate. The solid obtained above is reacted with methane sulfonic acid to obtain (2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-[1,3]-oxathiolane-2-carboxylic acid, 2S-isopropyl-5R-methyl-1R-cyclohexyl ester. The above compound is reduced with sodium borohydride to obtain lamivudine.Type: ApplicationFiled: January 8, 2010Publication date: February 13, 2014Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna
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Publication number: 20140037754Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: January 9, 2013Publication date: February 6, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Patent number: 8637535Abstract: Solid phases of (?)-cis-FTC, which are designated herein as amorphous (?)-FTC and Forms II and III (?)-cis-FTC) are provided that can be distinguished from Form I (?)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.Type: GrantFiled: June 9, 2009Date of Patent: January 28, 2014Assignees: Gilead Sciences, Inc., Abbvie, Inc.Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
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Publication number: 20140024616Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: September 19, 2013Publication date: January 23, 2014Applicant: DOW AGROSCIENCES LLCInventors: Timothy Boebel, Kristy Bryan, Carla J.R. Klittich, Beth Lorsbach, Timothy P. Martin, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, W. John Owen
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Publication number: 20140011824Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: Dow Agrosciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Patent number: 8618103Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 9, 2010Date of Patent: December 31, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
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Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20130336883Abstract: The invention provides compounds that bind to deoxycytidine kinase (dCK) and compositions including pharmaceutically acceptable compositions containing the compounds. The compounds are useful in treating diseases and disorders where dCK activity is implicated such as cancer and immune disorders. The compounds also find use in clinical methodologies including positron emission tomography (PET) imaging.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Caius G. Radu, Hsiang-I Liao, Nagichettiar Satyamurthy, Johannes Czernin, Jennifer M. Murphy, David A. Nathanson
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Patent number: 8609864Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: GrantFiled: January 7, 2010Date of Patent: December 17, 2013Assignee: Purdue Pharmaceutical Products, L.P.Inventors: Yu Chen, Yi Chen
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Patent number: 8604192Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: GrantFiled: September 23, 2009Date of Patent: December 10, 2013Assignee: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Eric E. Swayze
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Publication number: 20130317220Abstract: Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.Type: ApplicationFiled: December 16, 2011Publication date: November 28, 2013Applicant: Actavis Group Ptc EhfInventors: Vignesh Nair, Nikhil Trivedi, Anil Shahaji Khile, Nitin Sharadchandra Pradhan
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Publication number: 20130310403Abstract: The present invention relates to a fluoro-homoneplanocin A, its nucleoside derivative, and synthetic methods. The novel fluoro-homoneplanocin A and its nucleoside derivative in the present invention have an effect on cancer prevention or treatment, and therefore can be used as anticancer drugs.Type: ApplicationFiled: April 11, 2013Publication date: November 21, 2013Applicant: EWHA UNIVERSITY - INDUSTRY COLABORATION FOUNDATIONInventor: EWHA UNIVERSITY - INDUSTRY COLLABORATION FOUNDATION
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Patent number: 8586600Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: May 31, 2012Date of Patent: November 19, 2013Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter
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Publication number: 20130296562Abstract: The present invention relates to a stereoselective glycosylation for the preparation of 1,3-oxathiolane nucleoside in high yield and high optical purity. The invention specifically relates to a process of the preparation of Lamivudine and Emtricitabine using zirconium (IV) chloride (ZrCl4) as a catalyst in glycosylation.Type: ApplicationFiled: January 10, 2012Publication date: November 7, 2013Applicant: LUPIN LIMITEDInventors: Bhairab Nath Roy, Girij Pal Singh, Dhananjai Srivastava, Umesh Parasharam Aher, Sudhakar Uttam Patil
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Patent number: 8575342Abstract: Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C?C—C?C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.Type: GrantFiled: September 29, 2005Date of Patent: November 5, 2013Assignee: Tibotech Pharmaceuticals Ltd.Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Patent number: 8575338Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: GrantFiled: April 8, 2009Date of Patent: November 5, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasuyuki Tsuzuki, Miki Hirai
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Patent number: 8557833Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: September 30, 2010Date of Patent: October 15, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Alistair Rutherford
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Patent number: 8552020Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: August 5, 2010Date of Patent: October 8, 2013Assignee: Dow AgroSciences, LLC.Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20130252943Abstract: In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive 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: ApplicationFiled: February 27, 2013Publication date: September 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, María Luz Martín-Martín
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Publication number: 20130252941Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: F. Hoffmann-La Roche AGInventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
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Patent number: 8518885Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.Type: GrantFiled: July 16, 2008Date of Patent: August 27, 2013Assignees: Georgia Tech Research Corporation, Emory UniversityInventors: James C. Powers, Jonathan D. Glass, Asli Ovat, Zhaozhao Li
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Publication number: 20130196993Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 1, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck
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Patent number: 8492390Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.Type: GrantFiled: December 23, 2011Date of Patent: July 23, 2013Assignee: Santaris Pharma A/SInventors: Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Patent number: 8481554Abstract: The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also relate to the combination of lamivudine and other Anti-HIV agents. Thus, for example, the present invention provides a stable tablet formulation comprising lamivudine, isomalt, crospovidone, calcium stearate and opadry white.Type: GrantFiled: May 27, 2009Date of Patent: July 9, 2013Assignee: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Male Srinivas Reddy, Pothireddy Venkateswar Reddy, Muppidi Vanaja Kumari
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Patent number: 8470839Abstract: This present disclosure is related to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: August 5, 2010Date of Patent: June 25, 2013Assignee: Dow Agrosciences, LLC.Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20130158002Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: February 28, 2011Publication date: June 20, 2013Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
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Publication number: 20130158056Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: September 26, 2011Publication date: June 20, 2013Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
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Publication number: 20130143876Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 3, 2012Publication date: June 6, 2013Inventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Bernd NOSSE
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Patent number: 8455507Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: October 13, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: John Studley, Stephen Young
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Publication number: 20130123241Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Patent number: 8431588Abstract: Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, —C(?O)R5, or —C(?O)CHR6—NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, —C(?O)CHR5, or —C(?O)CHR6—NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl; or R8 and R8? combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.Type: GrantFiled: July 1, 2009Date of Patent: April 30, 2013Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck
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Patent number: 8410123Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: GrantFiled: December 23, 2011Date of Patent: April 2, 2013Assignee: AstraZeneca ABInventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20130079343Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: November 24, 2012Publication date: March 28, 2013Applicant: Korea Institute of Science and TechnologyInventor: Korea Institute of Science and Technology
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Publication number: 20130072681Abstract: The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 25, 2011Publication date: March 21, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Prakash Bhimaji Kshirsagar, Satish Manohar Bhoge, Santosh Richhariya, Kaptan Singh
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Patent number: 8399655Abstract: There is provided a method for resolving a compound of formula III, in the cis configuration: There is also provided a process for producing optically active compound of formula I or II: wherein: R1, R2, R3 are as defined herein, the method and process involving the production, recovery and conversion of diastereomeric salts.Type: GrantFiled: June 22, 2011Date of Patent: March 19, 2013Assignee: SHIRE Canada Inc.Inventors: Alex Cimpoia, Joana R. Simion