Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Publication number: 20130012535Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation.Type: ApplicationFiled: August 22, 2012Publication date: January 10, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Taro Kanamaru, Shinichiro Tajiri
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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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Patent number: 8349817Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.Type: GrantFiled: December 22, 2009Date of Patent: January 8, 2013Assignee: CoNCERT Pharmaceuticals, Inc.Inventors: Rose A. Persichetti, Julie F. Liu, Craig E. Masse, Scott L. Harbeson
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Publication number: 20130005763Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of a drug in the lower gastrointestinal tract, and thereby provide a sustained-release solid preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release solid preparation containing (A) a pharmacologically active drug, (B) carboxyvinyl polymer, (C) povidone, and (D) carmellose sodium, xanthan gum, or sodium carboxymethyl starch.Type: ApplicationFiled: August 22, 2012Publication date: January 3, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Taro Kanamaru, Shinichiro Tajiri
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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: 20130004550Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D50) of 40 ?m or smaller, (C) a cellulose derivative, and (D) a saccharide or a nonionic water-soluble polymer followed by molding.Type: ApplicationFiled: August 22, 2012Publication date: January 3, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Taro Kanamaru, Shinichiro Tajiri, Sachiko Fukui, Kazuhiro Yoshida
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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: 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: 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: 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: 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: 20120329774Abstract: 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: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: UCB Pharma S.A.Inventors: Clive Martin 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: 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: 20120323310Abstract: The present invention is directed to a drug eluting stent system, including: a stent; a tocopherol agent coupled to the stent; wherein the stent is adapted to elute the tocopherol agent into a surrounding lumenal wall tissue when implanted along the lumen within a body of a patient.Type: ApplicationFiled: January 24, 2012Publication date: December 20, 2012Applicant: CELONOVA BIOSCIENCES, INC.Inventors: James W. Larrick, James C. Peacock, III
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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: 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: 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: 20120270886Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, and n are as described herein.Type: ApplicationFiled: July 5, 2012Publication date: October 25, 2012Inventors: Michael F. T. Koehler, Lewis Gazzard, Vickie Hsiao-Wei Tsui
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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: 20120264692Abstract: The present invention is based on the discovery of genetic polymorphisms that are associated with venous thrombosis. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.Type: ApplicationFiled: October 11, 2011Publication date: October 18, 2012Applicants: Leiden University Medical Center (LUMC) Acting on Behalf of Academic Hospital Leiden (AZL), CELERA CORPORATIONInventors: Lance BARE, James J. DEVLIN, Frits R. ROSENDAAL, Pieter H. REITSMA, Irene D. BEZEMER
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Publication number: 20120264721Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of an phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Julie F. Liu, Rose A. Persichetti
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Publication number: 20120264708Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.Type: ApplicationFiled: April 27, 2012Publication date: October 18, 2012Inventors: Claire Mitchell, Alan Laties
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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: 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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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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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: 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: 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: 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: 20120245166Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.Type: ApplicationFiled: October 14, 2010Publication date: September 27, 2012Applicant: Southern Research InstituteInventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
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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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Patent number: 8268862Abstract: Provided herein are novel sirtuin-modulating compounds 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: January 24, 2011Date of Patent: September 18, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Patent number: 8263772Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): 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: GrantFiled: June 8, 2007Date of Patent: September 11, 2012Assignee: 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: 8263773Abstract: Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.Type: GrantFiled: June 24, 2009Date of Patent: September 11, 2012Assignee: Richter Gedeon Nyrt.Inventors: Istvan Gyertyan, Katalin Nogradi, Ottilia Elekes, Monika Vastag, Amrita Agnes Bobok, Katalin Saghy
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Publication number: 20120225887Abstract: Compounds are provided for use with glucokinase that comprise the formula: 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: April 10, 2012Publication date: September 6, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20120225857Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Publication number: 20120220569Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 30, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomohiro Ohashi, Zenyu Shiokawa, Yuta Tanaka, Satoshi Sasaki
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Patent number: 8252931Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: GrantFiled: September 28, 2006Date of Patent: August 28, 2012Assignee: Novartis AGInventors: Gregory Raymond Bebernitz, Louise Kirman
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Patent number: 8247557Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3?, R4, R4?, R5, R6, R6? and n are as described herein.Type: GrantFiled: December 19, 2006Date of Patent: August 21, 2012Assignee: Genentech, Inc.Inventors: Michael F. T. Koehler, Lewis Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20120208813Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.Type: ApplicationFiled: February 28, 2012Publication date: August 16, 2012Inventors: Natsuki ISHIZUKA, Takashi SASATANI, Yoshiharu HIRAMATSU, Masanao INAGAKI, Masahide ODAN, Hiroshi HASHIZUMI, Susumu MITSUMORI, Yasuhiko FUJII, Yoshikazu FUKUI, Hideaki WATANABE, Jun SATO