Ring Sulfur In The Bicyclo Ring System Patents (Class 546/114)
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Publication number: 20130035355Abstract: The present invention relates to Prasugrel or a pharmaceutically acceptable salt thereof, compositions containing said active ingredient as well as pharmaceutical compositions containing said active ingredient or a composition containing said active ingredient. The present invention further relates to methods for the preparation of the novel compositions.Type: ApplicationFiled: February 10, 2011Publication date: February 7, 2013Applicant: ratiopharm GmbHInventors: Sandra Brueck, Jana Paetz
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Publication number: 20130035332Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one 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: April 25, 2011Publication date: February 7, 2013Inventors: Mark E. Layton, Michael J. Kelly
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Publication number: 20130035356Abstract: An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, and method for producing the same.Type: ApplicationFiled: September 19, 2012Publication date: February 7, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130030014Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 11, 2012Publication date: January 31, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Publication number: 20130030183Abstract: The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-?-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.Type: ApplicationFiled: December 21, 2010Publication date: January 31, 2013Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Márta Porcs-Makkay, Tamás Gregor, Balázs Volk, Gábor Németh, József Barkóczy, Bálint Nyulasi, Tibor Mezei, György Ruzsics, Angéla Pandur, Erika Szilágyi, Kálmán Nagy, Péter Slégel, Enikö Molnár, Jözsef Debreczeni
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Publication number: 20130029971Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 5, 2011Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20130029984Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130023555Abstract: 4-Amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide which inhibits protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved aqueous solubility profile, compositions containing 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide and methods of treating diseases using 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide are disclosed.Type: ApplicationFiled: July 18, 2012Publication date: January 24, 2013Applicant: Abbott LaboratoriesInventors: Michael R. Michaelides, Michael L. Curtin, James H. Holms, Douglas H. Steinman
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Patent number: 8357804Abstract: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: GrantFiled: June 9, 2011Date of Patent: January 22, 2013Assignee: AbbVie Inc.Inventors: Geoff G. Z. Zhang, Paul J. Brackemeyer, Ahmad Y. Sheikh
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Patent number: 8357684Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: March 2, 2011Date of Patent: January 22, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
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Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8350037Abstract: A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: GrantFiled: January 22, 2010Date of Patent: January 8, 2013Assignee: UCB Pharma, S.A.Inventors: James Andrew Johnson, Daniel Christopher Brookings, Martin Clive Hutchings, Barry John Langham, Judi Charlotte Neuss
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Publication number: 20130005979Abstract: This invention relates to a novel thienopyridine derivative represented by formula (1), which is useful as an organic semiconductor device, such as an organic thin film transistor element, and the invention also relates to method for producing the thienopyridine derivative represented by formula (1):Type: ApplicationFiled: March 14, 2011Publication date: January 3, 2013Applicants: Kuraray Co. Ltd., Hiroshima UniversityInventors: Joji Ohshita, Yutaka Harima, Takashi Sugioka, Koichi Kanehira
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Publication number: 20130005762Abstract: The invention relates to the composition and use of a medicament comprising a fixed dose combination of droloxifene and clopidogrel.Type: ApplicationFiled: December 1, 2010Publication date: January 3, 2013Applicant: TCP Innovations LimitedInventor: David John Grainger
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Publication number: 20130005705Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: June 27, 2012Publication date: January 3, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
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Publication number: 20130005701Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: January 27, 2012Publication date: January 3, 2013Applicant: Bayer Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Patent number: 8343382Abstract: A method for altering the electronic and optical properties of a chemical compound having a band gap and a framework that includes ?-delocalized electrons. The method includes complexing a Lewis acid to a basic site within the framework to form a Lewis acid adduct having a band gap that differs from the band gap of the chemical compound. The ?max of the Lewis acid adduct can be shifted to a longer wavelength in comparison to the ?max of the chemical compound. In various versions, the chemical compound can be a conjugated oligomer, a conjugated polymer, or a small molecule comprising a conjugated ?-electron system. Electronic devices that include Lewis acid adducts are also provided.Type: GrantFiled: May 24, 2010Date of Patent: January 1, 2013Assignee: The Regents of the University of CaliforniaInventors: Guillermo C. Bazan, Gregory C. Welch, Robert Coffin, Jeff Peet
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Patent number: 8343997Abstract: Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: December 18, 2009Date of Patent: January 1, 2013Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Christopher Oalmann, Jeremy S. Disch, Pui Yee Ng, Robert Perni
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Publication number: 20120330018Abstract: The object of the present invention is a process for preparing the 2-acetoxy-5-(2-fluor-?-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]pyridine (prasugrel) of the formula (I). The process starts form crystalline 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI). Further objects of the present invention are two novel crystalline forms of 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI) and the use thereof for preparing the compound of the formula (V) and process preparing thereof.Type: ApplicationFiled: December 21, 2010Publication date: December 27, 2012Applicant: Egis Gyogyszergyar Nyilvanosan Mukodo ReszvenytarsasagInventors: Márta Porcs-Makkay, Balázs Volk, Tamás Gregor, József Barkóczy, Tibor Mezei, Judit Broda, Bálint Nyulasi, György Ruzsics, Enikõ Molnár, József Debreczeni, Kálmán Nagy, Angéla Pandur, Zsuzsanna Szent-Királlyi
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Publication number: 20120329763Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: March 23, 2012Publication date: December 27, 2012Inventors: Ashok KUMAR, Satish Rajanikant SOUDAGAR, Nellithanath Thankachen BYJU, Gaurav SAHAL, Arpana Prashant MATHUR, Sanjay Pandurang GAWADE, Dinesh Kanji BHADRA, Devki MOJE
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120329762Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.Type: ApplicationFiled: January 6, 2012Publication date: December 27, 2012Inventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki Moje
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Publication number: 20120316148Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
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Patent number: 8329907Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: March 9, 2010Date of Patent: December 11, 2012Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
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Patent number: 8329920Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: GrantFiled: May 26, 2011Date of Patent: December 11, 2012Assignee: Pfizer Inc.Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Patent number: 8329726Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: December 8, 2011Date of Patent: December 11, 2012Assignee: MethylGene Inc.Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Ljubomir Isakovic, Marie-Claude Granger, Naomy Bernstein
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Publication number: 20120309783Abstract: Compounds that inhibit protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved safety profile due to low CYP3A4 inhibition, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: August 14, 2012Publication date: December 6, 2012Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, Robin Frey, Michael Curtin
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Publication number: 20120302524Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: ApplicationFiled: December 28, 2010Publication date: November 29, 2012Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTUREInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20120302547Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.Type: ApplicationFiled: August 8, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Macklin Brian Arnold, Yen Dao, Kevin Matthew Gardinier, David Joseph Garmene, Steven James Green, Erik James Hembre, Jianliang Lu
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120289471Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: ApplicationFiled: April 18, 2012Publication date: November 15, 2012Applicant: SIGNATURE R&D HOLDINGS, LLCInventor: V. Ravi Chandran
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Publication number: 20120289702Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Publication number: 20120289497Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20120277212Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.Type: ApplicationFiled: October 29, 2010Publication date: November 1, 2012Applicants: PRESTWICK CHEMICAL, INC., DOMAIN THERAPEUTICSInventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen
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Publication number: 20120270868Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: October 17, 2011Publication date: October 25, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
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Publication number: 20120264739Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.Type: ApplicationFiled: December 30, 2010Publication date: October 18, 2012Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20120258955Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.Type: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: JANSSEN PHARMACEUTICA NVInventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
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Patent number: 8283360Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: December 18, 2009Date of Patent: October 9, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
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Patent number: 8283359Abstract: A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: GrantFiled: July 30, 2008Date of Patent: October 9, 2012Assignee: UCB Pharma S.A.Inventors: Martin Clive Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Publication number: 20120252805Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase II enzyme.Type: ApplicationFiled: December 16, 2010Publication date: October 4, 2012Inventors: Deborah Chen, Kiew Ching Lee, Lamont Roscoe Terrel
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Publication number: 20120253040Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: ApplicationFiled: December 14, 2010Publication date: October 4, 2012Applicant: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Publication number: 20120252800Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.Type: ApplicationFiled: December 16, 2010Publication date: October 4, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Gregor James MacDonald, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Joaquin Pastor-Fernández
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Publication number: 20120252837Abstract: The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.Type: ApplicationFiled: May 8, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, André Malanda
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Publication number: 20120245149Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
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Patent number: 8273736Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 20, 2009Date of Patent: September 25, 2012Assignee: Abbott LaboratoriesInventors: Patrick Betschmann, Andrew F. Burchat, David J. Calderwood, Michael L. Curtin, Steven K. Davidsen, Heather M. Davis, Robin R. Frey, Howard R. Heyman, Gavin C. Hirst, Peter Hrnciar, Michael R. Michaelides, Melanie A. Muckey, Kelly D. Mullen, Paul Rafferty, Carol K. Wada
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Publication number: 20120238599Abstract: The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.Type: ApplicationFiled: March 19, 2012Publication date: September 20, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Gilnam Lee, Han Won Cho, Eun Jin Song, Hye Sun Jeon, Min Jeong Kim, Jeongbeob Seo, Albert Charles Gyorkos, Suk Young Cho
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Publication number: 20120232274Abstract: An improved process for preparing crystalline form-1 of (S)-methyl 2-(2-chlorophenyl)-2-{6,7-dihydrothieno[3,2-c]pyridine-5(4H)-yl}acetate bisulfate (clopidogrel bisulfate) of formula I is provided The preparation comprises the straight conversion of an uncyclized material of (S)-methyl 2-[2-(thiophen-2-yl)ethylamino]-2-(2-chlorophenyl) acetate hydrochloride into clopidogrel bisulfate crystalline form-1 without any degradation of clopidogrel baseType: ApplicationFiled: March 22, 2010Publication date: September 13, 2012Applicant: PHARMAZELL GMBHInventors: Wolfgang Burger, Omprakash Gudaparthi, Konda Srinivasa Reddy, Suneel K. Kumar, Venkata P. Ramana