Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
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Publication number: 20140038951Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: January 15, 2013Publication date: February 6, 2014Applicant: OMEROS CORPORATIONInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler
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Patent number: 8642643Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: December 18, 2008Date of Patent: February 4, 2014Assignee: SanofiInventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter, Raymond Kosley
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Patent number: 8642644Abstract: The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.Type: GrantFiled: July 29, 2009Date of Patent: February 4, 2014Assignee: Duke UniversityInventors: Eric J. Toone, David L. Epstein, Pratap Challa, Phillip W. Snyder, Xin Chen, Mitchell A. deLong
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Publication number: 20140031405Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; X is methine or nitrogen; A is R5 is hydrogen, halogen, —?—C1-C6alkyl, —?—C3-C7cycloalkyl or -?-aryl; R6 is hydrogen, halogen, —?—C1-C6alkyl, —?—C3-C7cycloalkyl or -?-aryl; and agrochemically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/enantiorners/tautorriers and N-oxides of those compounds are suitable for use as microbiocides.Type: ApplicationFiled: February 16, 2012Publication date: January 30, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Harald Walter, Daniel Stierli
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Publication number: 20140024587Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: ApplicationFiled: September 23, 2013Publication date: January 23, 2014Applicant: Duke UniversityInventors: Mitchell A. deLong, John M. McIver, Robert S. Youngquist
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Publication number: 20140024608Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: March 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Publication number: 20140018385Abstract: Pharmaceutical compositions and methods for inhibiting cell growth, modulating function of PCNA, treating prostate cancer, and enhancing PCNA trimer formation are disclosed.Type: ApplicationFiled: September 8, 2011Publication date: January 16, 2014Applicant: UNIVERSITY OF CINCINNATIInventors: Zhongyun Dong, Matthew Wortman, Zonqing Tan, Kelsey Dillehay
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Publication number: 20140005187Abstract: The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.Type: ApplicationFiled: December 22, 2011Publication date: January 2, 2014Applicant: The Curators of the University of MissouriInventors: Salman M. Hyder, Yayun Liang, Xiaoqin Zou, Sam Z. Grinter, Sheng-you Huang
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Publication number: 20130345164Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.Type: ApplicationFiled: April 21, 2011Publication date: December 26, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
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Patent number: 8598224Abstract: The present invention relates to thiophene containing compounds of formula (I) wherein m, n, p, q, r, s, R1, R2, and R3 are as defined in the description. Included also are pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions.Type: GrantFiled: December 14, 2010Date of Patent: December 3, 2013Assignee: AbbVie Inc.Inventors: Derek W Nelson, Jennifer M Frost
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Publication number: 20130316985Abstract: A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein.Type: ApplicationFiled: May 20, 2013Publication date: November 28, 2013Applicant: Corning IncorporatedInventors: Huayun Deng, Ye Fang
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Publication number: 20130310254Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.Type: ApplicationFiled: November 24, 2011Publication date: November 21, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
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Patent number: 8586603Abstract: The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.Type: GrantFiled: December 20, 2010Date of Patent: November 19, 2013Inventors: Peter Gmeiner, Miriam Ruberg, Harald Hüebner
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Publication number: 20130302422Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: May 22, 2013Publication date: November 14, 2013Applicants: KT & G CORPORATION, MAZENCE INC.Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
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Publication number: 20130289083Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprisType: ApplicationFiled: March 13, 2013Publication date: October 31, 2013Inventor: NewLink Genetics Corporation
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Publication number: 20130289057Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.Type: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Patent number: 8569325Abstract: A method for the prevention of diseases caused by thrombus or embolus. The method is to separately administer 2-acetoxy-5-(?-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, in their pharmacologically effective amounts, to a warm-blooded animal.Type: GrantFiled: January 3, 2008Date of Patent: October 29, 2013Assignees: Daiichi Sankyo Company, Limited, Ube Industries, Ltd.Inventors: Fumitoshi Asai, Atsuhiro Sugidachi, Taketoshi Ogawa, Teruhiko Inoue
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Patent number: 8552032Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: October 8, 2013Assignee: Janssen Pharmaceutica NVInventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
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Publication number: 20130261130Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: October 3, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
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Publication number: 20130253022Abstract: Pharmaceutical compositions of the invention include fluorinated sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, Parkinson's disease, Huntington's disease, heavy metal toxicity and any neurodegenerative disease involving glutamate toxicity.Type: ApplicationFiled: November 18, 2011Publication date: September 26, 2013Applicants: FOX CHASE CHEMICAL DIVERSITY CENTER, INC., ADVANCED NEURAL DYNAMICS, INC.Inventors: Garry Robert Smith, Douglas E. Brenneman, Allen B. Reitz, Yan Zhang, Yanming Du
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Publication number: 20130252964Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.Type: ApplicationFiled: January 18, 2013Publication date: September 26, 2013Applicant: PolyMedix, Inc.Inventors: Richard W. Scott, Katie Freeman, Haizhong Tang, Gill Diamond
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Publication number: 20130245025Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130245064Abstract: The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein R1 is phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, R2 is hydrogen or methyl, and R3 and R4 have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: September 19, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Piero Paravidino
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Publication number: 20130237547Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: March 28, 2013Publication date: September 12, 2013Applicant: Janssen Pharmaceutica, NVInventor: Jay M. Matthews
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Patent number: 8530512Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present and when x=0, W is not phenyl.Type: GrantFiled: December 20, 2010Date of Patent: September 10, 2013Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski, Ranjit Verma, Leah Defoe
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Patent number: 8524763Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: September 22, 2009Date of Patent: September 3, 2013Assignee: Calcimedica, Inc.Inventor: Jeffrey P. Whitten
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI -
Publication number: 20130217759Abstract: The invention provides sulphonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: October 12, 2011Publication date: August 22, 2013Applicant: Zafgen Inc.Inventors: Robert Zahler, Hazel Joan Dyke, Thomas David Pallin, Susan Mary Cramp
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Publication number: 20130210904Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.Type: ApplicationFiled: August 15, 2012Publication date: August 15, 2013Inventors: Jeremy E. Wulff, Michael G. Brant, Jeremy W. Mason, Caleb M. Bromba, Martin J. Boulanger
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Patent number: 8501961Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.Type: GrantFiled: July 8, 2009Date of Patent: August 6, 2013Assignee: Purdue Research FoundationInventor: Arun K. Ghosh
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
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Publication number: 20130165505Abstract: Administration of certain 1-phenylalkanecarboxylic acid derivatives is useful for improving Cognitive Function; treating Cognitive Impairment, in particular Mild Cognitive Impairment; and preventing and/or reducing the risk of developing Alzheimer's Disease in a cognitively normal subject.Type: ApplicationFiled: December 21, 2012Publication date: June 27, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8470872Abstract: Disclosed herein are compounds of Formula I as disclosed herein, methods of modulating the activity of an estrogen receptor and methods of treating a disorder associated with estrogen receptors.Type: GrantFiled: December 14, 2011Date of Patent: June 25, 2013Assignee: Acadia Pharmaceuticals Inc.Inventors: Roger Olsson, Lene Hyldtoft, Magnus Gustafsson, Brigitte Winther Lund
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Publication number: 20130143765Abstract: Provided herein are methods for identifying compounds that are inhibitors of a calcium-activated chloride channel. Aminothiophene and aminothiazole compounds, and compositions comprising these compounds, described herein that inhibit efflux of chloride through a calcium-activated chloride channel are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased chloride and fluid secretion, for example, secretory diarrhea.Type: ApplicationFiled: August 31, 2012Publication date: June 6, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Ricardo De La Fuente Gonzalez
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Publication number: 20130142858Abstract: Drug delivery devices comprising a non-bioabsorbable polymer structure configured to support a composition comprising an active agent. The devices include a plurality of portions fused together and a recess configured to support the composition. At least one of the portions includes an impermeable polymer and at least one other portion includes a rate-limiting water-permeable polymer. The rate-limiting water-permeable polymer allows for transportation of the active agent to an exterior of the device.Type: ApplicationFiled: May 17, 2011Publication date: June 6, 2013Applicant: Aerie Pharmaceuticals, Inc.Inventors: Casey Kopczynski, Cheng-Wen Lin, Chris Sutay
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Patent number: 8450502Abstract: Provided is a pharmaceutical composition for inhibiting angiogenesis, comprising a therapeutically effective amount of a compound represented by Formula 1: (I) wherein R1 through R13 and X are as defined in the specification. Compounds used as an active ingredient in the pharmaceutical composition of the present invention bind to QP-C to provide effective prevention of angiogenesis and can be effectively used for prevention and/or treatment of angiogenesis-related diseases or disorders. Further, the active compounds of the present invention inhibit biological functions of QP-C, which consequently leads to inhibition of angiogenic responses without the risk of cellular apoptosis, thus significantly improving safety of the drug.Type: GrantFiled: January 30, 2009Date of Patent: May 28, 2013Assignee: Industry-Academic Cooperation Foundation Yonsei UniversityInventors: Ho Jeong Kwon, Hye Jin Jung
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8445530Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: October 1, 2012Date of Patent: May 21, 2013Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Publication number: 20130123263Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 10, 2013Publication date: May 16, 2013Applicants: F. HOFFMANN - LA ROCHE AG, GENENTECH, INC.Inventors: GENENTECH, INC., F. HOFFMANN - LA ROCHE AG
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Patent number: 8440713Abstract: A [1]benzothieno[3,2-b][1]benzothiophene compound expressed by General Formula (I): General Formula (I) where X and Y are each independently a hydrogen atom; a halogen atom; or a functional group having a straight or branched aliphatic alkyl group optionally having a halogen atom, a functional group having an alicyclic alkyl group optionally having a halogen atom, a functional group having a straight or branched aliphatic alkenyl group optionally having a halogen atom, a functional group having an alicyclic alkenyl group optionally having a halogen atom, a functional group having a carboxyl group, or a functional group having a thiol group, as a partial structure; and X and Y are the same or each independently different, provided that at least one of X and Y has a straight or branched aliphatic alkenyl group, an alicyclic alkenyl group, a carboxyl group or a thiol group, as a partial structure.Type: GrantFiled: April 15, 2009Date of Patent: May 14, 2013Assignee: Ricoh Company, Ltd.Inventors: Daisuke Goto, Masafumi Torii, Tamotsu Horiuchi, Tamotsu Aruga, Hiroshi Ikuno, Toshiya Sagisaka, Satoshi Yamamoto, Takeshi Orito, Masataka Mohri, Takashi Okada, Takuji Kato, Shinji Matsumoto
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Patent number: 8436041Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica, NVInventor: Jay M. Matthews
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Publication number: 20130109677Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: December 3, 2010Publication date: May 2, 2013Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, John Emmerson Campbell, Michael Charles Hewitt, Una Campbell, Taleen G. Hanania
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Publication number: 20130101667Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: ApplicationFiled: October 24, 2012Publication date: April 25, 2013Applicant: ENDO PHARMACEUTICALS, INC.Inventor: Endo Pharmaceuticals, Inc.
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Patent number: 8415347Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: GrantFiled: August 5, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
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Publication number: 20130085174Abstract: The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.Type: ApplicationFiled: April 30, 2012Publication date: April 4, 2013Inventor: Christos C. Zouboulis
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Patent number: 8404703Abstract: A combination of 2-acetoxy-5-(?-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.Type: GrantFiled: September 13, 2006Date of Patent: March 26, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Fumitoshi Asai, Atsuhiro Sugidachi, Taketoshi Ogawa, Teruhiko Inoue
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Publication number: 20130072473Abstract: The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: May 9, 2012Publication date: March 21, 2013Inventors: Bradley Tait, Noel A. Powell, Matthew Cullen