C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
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Publication number: 20140045911Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.Type: ApplicationFiled: July 18, 2013Publication date: February 13, 2014Applicants: THESAN PHARMACEUTICALS, INC.Inventors: Jin LI, Nicole Lee Kolosko
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Patent number: 8648109Abstract: Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described.Type: GrantFiled: January 22, 2013Date of Patent: February 11, 2014Assignee: Warner-Lambert Company LLCInventors: Jason Albert Leonard, Jonathan Mark Miller
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Patent number: 8642576Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: GrantFiled: August 29, 2012Date of Patent: February 4, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Patent number: 8642640Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.Type: GrantFiled: October 7, 2009Date of Patent: February 4, 2014Assignees: Exelixis, Inc., Daiichi Sankyo Company, LimitedInventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Hiroyuki Tsuruoka, Kazumasa Aoki, Masatoshi Honzumi, Yusuke Asoh, Keiji Saito, Tsuyoshi Homma
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Patent number: 8637567Abstract: This invention provides compounds, compositions and methods for treating a cognitive disorder or memory disorder in animals that result from aging or other neurodegenerative condition. In particular, compounds of this invention can stimulate neural cell growth, increased amounts of cells containing a key enzyme needed for production of the cholinergic neurotransmitter, and can improve memory and cognitive function in animals who have experienced a loss of memory or cognitive function.Type: GrantFiled: October 13, 2010Date of Patent: January 28, 2014Assignee: Neuren Pharmaceuticals Ltd.Inventors: Peter David Gluckman, Jian Guan, Mary-Anne Woodnorth, Margaret Anne Brimble
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Patent number: 8637576Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.Type: GrantFiled: October 20, 2009Date of Patent: January 28, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Michael R. Degraffenreid, Xiao He, Lisa D. Julian, Dustin L. McMinn, Daqing Sun, Yosup Rew, Xuelei Yan
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Patent number: 8637572Abstract: Disclosed is a novel composition which has an effect on promoting production of collagen. The composition has high photostability and is free from side effects such as those of retinoids. Specifically disclosed is a composition for promoting collagen production which contains one or more compounds selected from the group consisting of D-aspartic acid, D-alanine, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving skin a condition. The skin condition may include but is not limited to photoaging and/or wrinkles. The composition may be used for an external preparation for the skin or food. The composition may be a composition for promoting type I collagen production.Type: GrantFiled: September 27, 2010Date of Patent: January 28, 2014Assignee: Shiseido Company, Ltd.Inventors: Yutaka Ashida, Yosuke Tojo, Shoichiro Shimada, Chieko Mizumoto, Masashi Mita
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Publication number: 20140024647Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 18, 2012Publication date: January 23, 2014Inventor: Akira Yukimasa
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Publication number: 20140024696Abstract: [Object] A prophylactic or therapeutic agent for a cardiovascular disease is provided. [Means for Resolution] An atropisomer of a compound represented by the following general formula (I): (wherein R1 is a C1-C3 alkyl group or a hydroxy-C1-C3 alkyl group; and R2 is a hydrogen atom or a C1-C3 alkoxy group).Type: ApplicationFiled: July 30, 2013Publication date: January 23, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Hiroyuki Tsuruoka, Noriyuki Hayashi, Juri Yoshida, Yusuke Asoh
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Publication number: 20140024700Abstract: The present invention provides methods for evaluating or monitoring the efficacy of a therapeutic intervention for treating a cardiac disorder. Such methods comprise measuring or detecting the level of at least one miRNA in a biological sample from a patient receiving the therapeutic intervention and comparing the level to the level of said at least one miRNA in a control sample, wherein the measured level of said at least one miRNA is indicative of the therapeutic efficacy of the therapeutic intervention. Methods of predicting or assessing the severity or progression of heart failure in a patient by measuring one or more miRNAs in a biological sample from the patient are also disclosed.Type: ApplicationFiled: December 15, 2011Publication date: January 23, 2014Applicant: miRagen Therapeutics, Inc.Inventors: Eva Van Rooij, Brent Dickinson, Anita Seto
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Publication number: 20140024639Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
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Publication number: 20140023615Abstract: The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.Type: ApplicationFiled: March 29, 2012Publication date: January 23, 2014Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Stephen I-Hong Hsu
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Publication number: 20140017308Abstract: Compositions comprising a fatty acid oil mixture, at least one free fatty acid, and at least one statin or pharmaceutically acceptable salt, hydrate, solvate, or complex thereof, and uses thereof are disclosed. Further disclosed are preconcentrates capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution.Type: ApplicationFiled: September 8, 2011Publication date: January 16, 2014Applicant: Pronova Biopharma Norge ASInventors: Svein Olaf Hustvedt, Gunnar Berge, Preben Houlberg Olesen, Anette Müllertz
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Publication number: 20140011850Abstract: A method of improving cognitive function or treating cognitive dysfunction is provided. The method is based on activating a kainate receptor or a glutamate GluR6 receptor by kainate or a glutamate GluR6 receptor activator such as an agonist. Additionally, a method of enhancing a learning ability by activating a kainate receptor such as the glutamate GluR6 receptor via kainate or a glutamate GluR6 receptor activator such as an agonist is provided.Type: ApplicationFiled: June 26, 2013Publication date: January 9, 2014Inventors: Edi Barkai, Dietmar Schmitz
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Publication number: 20140004186Abstract: Preconcentrates comprising a fatty acid oil mixture, at least one surfactant, and at least one statin or pharmaceutically acceptable salt, hydrate, solvate, or complex thereof, and methods and uses thereof are disclosed. The preconcentrates are capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution.Type: ApplicationFiled: September 8, 2011Publication date: January 2, 2014Applicant: Pronova Biopharma Norge ASInventors: Svein Olaf Hustvedt, Preben Houlberg OLesen, Gunnar Berge, Jo Erik Johnsrud Klaveness
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Publication number: 20140004082Abstract: A method for treating core binding factor (CBF) leukemia in a subject, comprising administering to a subject having CBF leukemia a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, that inhibits CBF? and RUNX1 binding in the subject, thereby treating the CBF leukemia.Type: ApplicationFiled: March 15, 2012Publication date: January 2, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Pu Liu, Wei Zheng, Juan Marugan, Noel T. Southall, Lea Cunningham
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Publication number: 20140005151Abstract: Administering water-soluble or dispersible synthetic analogs or derivatives of astaxanthin, lutein, zeaxanthin, or lycophyll and/or other carotenoids to a subject may reduce some of the adverse effects of inflammation in a body organ or tissue. The analogs or derivatives may be incorporated into pharmaceutical, over-the-counter, or nutraceutical preparations. Administration of the analogs or derivatives described herein may reduce deposition of inflammatory mediators such as C-reactive protein, complement system proteins or the membrane attack complex (MAC) in tissues. Reduced deposition of these molecules in tissues may reduce cell damage and/or lysis in the tissues.Type: ApplicationFiled: June 19, 2013Publication date: January 2, 2014Inventor: Samuel F. Lockwood
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Publication number: 20130344167Abstract: The present invention relates to a galenic composition suitable for administration to a non-human animal, including at least the following three components: one or more active principles; an agent for accelerating delitescence; an agent for delaying delitescence, wherein the agent for accelerating delitescence an the agent for delaying delitescence are integrated in the composition so as to form a matrix with the controlled release of the active principle(s). The invention also relates to the uses of said compositions, as well as to a method for measuring the in vitro delitescence thereof.Type: ApplicationFiled: November 27, 2011Publication date: December 26, 2013Applicant: VETALIS SARLInventors: Laurent Chery, Jean-Pierre Wajda-Dubos
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Patent number: 8614205Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.Type: GrantFiled: June 2, 2012Date of Patent: December 24, 2013Inventors: Richard D Wood, William Welsh
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Publication number: 20130337031Abstract: The present disclosure is drawn to topical formulations, transdermal systems, and related methods. In one embodiment, a topical formulation is provided that includes a local anesthetic, a first compound, and a second compound. The first compound and second compound are different and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate.Type: ApplicationFiled: March 8, 2013Publication date: December 19, 2013Applicant: Nuvo Research Inc.Inventor: Nuvo Research Inc.
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Publication number: 20130336902Abstract: A personal care composition is disclosed comprising a di-amido gellant, wherein the di-amido gellant has a formula: wherein R1 and R2 are aminofunctional end-groups which may be the same or different, and L is a linking moiety of molecular weight from 14 to 500 g/mol. The personal care composition may take a variety of forms such as a leave-on composition or an emulsion and/or may comprise one or more actives or agents.Type: ApplicationFiled: June 13, 2012Publication date: December 19, 2013Inventors: SUSANA FERNANDEZ PRIETO, JOHAN SMETS, BEATRIU ESCUDER GIL, JUAN FELIPE MIRAVET CELADES, VICENT JOSEP NEBOT CARDA, PAUL ROBERT TANNER
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Publication number: 20130337022Abstract: A pH responsive and mucoadhesive pharmaceutical dosage form for the release of a pharmaceutically active agent is described. The dosage form includes a mucoadhesive layer for site-specific mucoadhesion, a water-insoluble outer layer, and an intermediate layer including one or more pharmaceutically active agents for site-specific delivery. The different membranous layers perform different functions in order to create a drug delivery system which is able to deliver a drug to a specific site, for a particular period of time and with a specific drug release pattern. The dosage form can have two or more intermediate layers, each layer comprising an active agent. The mucoadhesive layer can also include an active agents. The dosage form is preferably an oral or buccal delivery form for release of the active agent into the gastro intestinal tract. The intermediate layer can be an electrospun fibrous membrane layer containing the active agent.Type: ApplicationFiled: November 28, 2011Publication date: December 19, 2013Applicant: UNIVERSITY OF THE WITWATERSRAND, JOHANNESBURGInventors: Viness Pillay, Rubina Perveen Shaikh, Yahya Essop Choonara, Lisa Claire Du Toit
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Patent number: 8609649Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: GrantFiled: March 20, 2008Date of Patent: December 17, 2013Assignee: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R. P. Novak
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Publication number: 20130331394Abstract: Methods of identifying new treatments for schizophrenia, and the use of the same.Type: ApplicationFiled: June 11, 2013Publication date: December 12, 2013Inventor: Peter Siekmeier
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Publication number: 20130331427Abstract: The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.Type: ApplicationFiled: October 25, 2012Publication date: December 12, 2013Applicant: Blanchette Rockefeller Neuroscience InstituteInventor: Blanchette Rockefeller Neuroscience Institute
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Publication number: 20130331387Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.Type: ApplicationFiled: February 22, 2012Publication date: December 12, 2013Applicant: Lupin LimitedInventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130331411Abstract: The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.Type: ApplicationFiled: September 23, 2011Publication date: December 12, 2013Applicants: BETH ISRAEL DEACONESS MEDICAL CENTER, THE BROAD INSTITUTE, INC.Inventors: Chris Dockendorff, Robert Flaumenhaft, Lawrence MacPherson
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Publication number: 20130324556Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.Type: ApplicationFiled: January 27, 2012Publication date: December 5, 2013Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
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Publication number: 20130324531Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: May 29, 2013Publication date: December 5, 2013Applicant: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
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Publication number: 20130324539Abstract: Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed.Type: ApplicationFiled: May 30, 2013Publication date: December 5, 2013Inventors: Peter A. Virsik, David J. Wustrow, Thamil Annamalai
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Patent number: 8597666Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.Type: GrantFiled: October 28, 2011Date of Patent: December 3, 2013Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Ilan Zalit, Fanny Leska, Mali Kadosh, Dorit Marco, Yonit Messer-Triger
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Publication number: 20130316995Abstract: The invention relates to fatty acid statin conjugates and fatty acid FXR agonist conjugates; compositions comprising an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate.Type: ApplicationFiled: May 1, 2013Publication date: November 28, 2013Applicant: Catabasis Pharmaceuticals, Inc.Inventor: Catabasis Pharmaceuticals, Inc.
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Patent number: 8592454Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: GrantFiled: September 18, 2009Date of Patent: November 26, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
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Patent number: 8592452Abstract: A compound represented by the formula (I) wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R6, R7 and R8, R1 is an electron-withdrawing group, R2, R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R6 is a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R7 is a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or R6 and R7 optionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), and R8 is a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygType: GrantFiled: August 1, 2006Date of Patent: November 26, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Atsushi Hasuoka
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Publication number: 20130310437Abstract: The present invention relates to the use of a combination of glycine, proline, and optionally a natural or synthetic viscosity-controlling polymer, and/or lysine and/or leucine, to prepare a composition for the treatment of osteoarthritis.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: PROFESSIONAL DIETETICS S.R.L.Inventors: Franco CONTI, Francesco Saverio DIOGUARDI
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Publication number: 20130310419Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.Type: ApplicationFiled: January 31, 2012Publication date: November 21, 2013Applicant: LUPIN LIMITEDInventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 8586618Abstract: The present invention provides a compound of formula I and a compound of formula II, methods of use and formulations thereof.Type: GrantFiled: October 8, 2007Date of Patent: November 19, 2013Assignee: Biosignal LimitedInventors: Naresh Kumar, George Iskander
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Patent number: 8586623Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: November 19, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Patent number: 8586622Abstract: Disclosed is a novel composition which has a function of stimulating production of laminin-332. The composition is stable and safe, and can be used routinely. Specifically disclosed is a laminin-332 production stimulating composition which contains one or more compounds selected from the group consisting of D-alanine, D-hydroxyproline, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving a skin condition. The skin condition may include, but is not limited to a photoaging, wrinkles, a rough skin, fine wrinkles and a dry skin. The composition may be used for an external preparation for the skin or a food.Type: GrantFiled: May 14, 2010Date of Patent: November 19, 2013Assignee: Shiseido Company, Ltd.Inventors: Yosuke Tojo, Jun-ichi Hosoi, Kayo Matsumoto
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Publication number: 20130303530Abstract: The present invention provides methods and compositions for treating chronic pelvic pain syndrome. In particular, the present invention provides methods and compositions for treating chronic pelvic pain syndrome with an agent that targets MCP-1, MIP-1?, or the CCR-2 receptor.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Applicant: Northwestern UniversityInventors: Anthony J. Schaeffer, David Klumpp, Praveen Thumbikat
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Publication number: 20130303547Abstract: This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Brian E. Green, David D. Anderson, Todd D. Bosse, Curt S. Cooper, Larry L. Klein, Allan C. Krueger, Daniel P. Larson, Dachun Liu, Keith F. McDaniel, Christopher E. Motter, John K. Pratt, Todd W. Rockway, Teresa A. Rosenberg, Ming C. Yeung, Hui-Ju Chen, Jason P. Shanley
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Publication number: 20130303466Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: November 14, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
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Publication number: 20130303558Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with vascular diseases such as stroke. In particular, the present invention relates to genetic polymorphisms that have utility for such uses as predicting disease risk or predicting an individual's response to a treatment such as statins, including groups of polymorphisms that may be used as a signature marker set for such uses, as well as 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 19, 2012Publication date: November 14, 2013Inventors: May LUKE, James J. DEVLIN
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Publication number: 20130296279Abstract: The invention in one embodiment is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to a composition comprising the compound of formula I or a pharmaceutically acceptable salt, and methods of treating the indications listed herein.Type: ApplicationFiled: May 10, 2013Publication date: November 7, 2013Inventor: Adam Morgan
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Publication number: 20130295173Abstract: The present disclosure provides pharmaceutical compositions of statins and polyunsaturated fatty acids (PUFAs), in which the statins are dissolved in the PUFAs, the PUFA species being present substantially in the free acid form. Also provided are oral unit dosage forms of the disclosed pharmaceutical compositions and methods of treating blood lipid disorders using the compositions and oral unit dosage forms.Type: ApplicationFiled: May 7, 2013Publication date: November 7, 2013Inventors: Bernardus N M MACHIELSE, Timothy J. Maines, Bharat M. Mehta, Michael H. Davidson
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Publication number: 20130295185Abstract: A novel BH3 ?-helical mimetic, BH3-M6, which binds to Bcl-XL and prevents its binding to fluorescently-labeled Bak-BH3 peptide in vitro with an IC50 value of 734 nM is presented herein. BH3-M6 is a pan-Bcl-2 antagonist that inhibits the binding of Bcl-XL, Bcl-2 and Mcl-1 to multi-domain Bax or Bak, or BH3-only Bim or Bad in a cell-free system and in intact human cancer cells, freeing up pro-apoptotic proteins to induce apoptosis. BH3-M6-induced apoptosis is caspase- and Bax-dependent. Furthermore, human cancer cells with high Bcl-2 or Bcl-XL levels are more sensitive to BH3-M6-induced cell death, suggesting that this compound can overcome drug resistance due to Bcl-2 or Bcl-XL overexpression. The pan-Bcl-2 inhibitor BH3-M6 may be encapsulated in a micelle to provide a more bioavailable therapeutic agent. Specifically, the BH3-M6 compound may be encapsulated within a micelle comprising a multiblock copolymer according to the methods described herein.Type: ApplicationFiled: July 12, 2013Publication date: November 7, 2013Inventors: Said M. Sebti, Andrew D. Hamilton, Kevin Sill, Adam Carie
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Patent number: 8575197Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.Type: GrantFiled: September 24, 2009Date of Patent: November 5, 2013Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
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Patent number: 8575191Abstract: The present invention provides methods of treating non-small cell lung cancer by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound in combination with a therapeutically effective amount of an epidermal growth factor tyrosine kinase inhibitor.Type: GrantFiled: August 31, 2011Date of Patent: November 5, 2013Assignee: ArQule, Inc.Inventors: Yinpu Chen, Edward G. Garmey, Brian Schwartz
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Publication number: 20130287758Abstract: An injectable amino-acid composition acts naturally to fuel collagen synthesis, which retards aging and helps to clear cellular decay while accelerating the cell division that promotes healthy, younger looking skin. The amino-acid composition includes carnosine. The composition is injected into the dermis of patients. The composition can be used in conjunction with botulinum toxin and fillers to enhance their effectiveness and extend their usefulness.Type: ApplicationFiled: April 1, 2013Publication date: October 31, 2013Inventor: Donna M. Tozzi