C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
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Patent number: 9573883Abstract: Disclosed are salts, such as nitrates, of acetyl-L-carnitine and propionyl-L-carnitine and methods of making the compounds.Type: GrantFiled: December 15, 2014Date of Patent: February 21, 2017Assignee: ThermoLife International, LLCInventors: Ronald Kramer, Alexander Nikolaidis
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Patent number: 9522931Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.Type: GrantFiled: May 18, 2012Date of Patent: December 20, 2016Assignee: Janssen Pharmaceutica NVInventors: Kenneth M. Wells, Ronald K. Russell, Xun Li, Shawn Branum, Derek A. Beauchamp, Sumihiro Nomura, Yosuke Matsumura
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Patent number: 9487505Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: September 25, 2013Date of Patent: November 8, 2016Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
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Patent number: 9422335Abstract: The present invention provides modified TLR2 ligands useful for modulating inflammatory responses. In particular, the ligands comprise (a) a fatty acid di- or tri-linoleate and (b) a GM1-binding peptide. The linoleate provides the anti-inflammatory function, while the GM1-binding peptide facilitates endocytosis.Type: GrantFiled: August 30, 2012Date of Patent: August 23, 2016Assignee: UTI Limited PartnershipInventors: Elizabeth M. Long, Stephen M. Robbins, Paul Kubes, Ela Kolaczkowska
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Patent number: 9387234Abstract: A method is provided for increasing trafficking of endothelial progenitor cells to an ischemic myocardium in a subject's heart comprising administering to the subject's heart an amount of Stromal-Derived Factor-1 (SDF-1).Type: GrantFiled: July 10, 2013Date of Patent: July 12, 2016Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventor: Silviu Itescu
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Patent number: 9346814Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.Type: GrantFiled: January 17, 2013Date of Patent: May 24, 2016Assignees: Universiteit Antwerp, Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Patent number: 9340500Abstract: 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: GrantFiled: April 18, 2012Date of Patent: May 17, 2016Assignee: SHIONOGI & CO., LTD.Inventor: Akira Yukimasa
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Patent number: 9226965Abstract: A method and composition for treating, preventing or ameliorating heart failure, cardiac hypertrophy, and/or myocardial dysfunction includes administering a therapeutically effective amount of a HDAC inhibitor, such as phenylbutyrate, in combination with an ACE inhibitor, such as captopril.Type: GrantFiled: October 3, 2008Date of Patent: January 5, 2016Assignee: U.S. DEPARTMENT OF VETERANS AFFAIRSInventors: Wesley W. Brooks, Oscar H.L. Bing
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Patent number: 9198896Abstract: A pharmaceutical composition and treatment method to reduce the proliferation of cancerous or tumor cells, in which the combined active agents are methylglyoxal, ascorbic acid, creatine and melatonin.Type: GrantFiled: August 18, 2010Date of Patent: December 1, 2015Assignee: NATIONAL RESEARCH DEVELOPMENT CORPORATIONInventor: Manju Ray
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Patent number: 9198942Abstract: A bioactive compound obtained from A. cinnamomea mycelium is prepared. The A. cinnamomea mycelium is solid-state cultivated. The bioactive compound is 2,3,6-trimethoxy-4-methylphenol and is called Leader 1. Leader 1 effectively suppresses movement, migration and invasion of lung cancer cells. Leader 1 achieves the effect of anti-metastasis and shows excellent resistance to physiological activity and mechanism on cancer metastasis.Type: GrantFiled: August 18, 2014Date of Patent: December 1, 2015Assignee: TAIWAN LEADER BIOTECH CORP.Inventors: Chin-Chung Lin, Jong-Tar Kuo, Ching-Chun Chen, Jent-turn Lee, Yu-Yen Lin
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Patent number: 9067884Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: GrantFiled: July 2, 2014Date of Patent: June 30, 2015Assignee: Synta Pharmaceuticals Corp.Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20150147309Abstract: The present invention relates to an allosteric non-inhibitory chaperone of the lysosomal acid alpha-glucosidase (GAA) for use in the treatment of a pathological condition characterized by a deficiency of the lysosomal acid alpha-glucosidase (GAA), to pharmaceutical composition thereof, to a method for increasing the activity of GAA in a subject and to a method for identifying an allosteric non-inhibitory chaperone for GAA.Type: ApplicationFiled: June 6, 2013Publication date: May 28, 2015Inventors: Giancarlo Parenti, Caterina Porto, Marco Moracci, Maria Carmina Ferrara, Beatrice Cobucci-Ponzano, Generoso Andria
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Publication number: 20150148335Abstract: The invention relates to a liquid formulation comprising propylene glycol and an effective amount of an inodilator, an angiotensin converting enzyme inhibitor, or a combination of an inodilator and an angiotensin converting enzyme inhibitor and to use of the formulation for treating cardiac disease and/or hypertension.Type: ApplicationFiled: May 17, 2013Publication date: May 28, 2015Inventors: Nicholas Bova, Stephen Page, Giuseppe Pippia
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Publication number: 20150147396Abstract: Nanoparticles are provided that comprise S-nitrosothiol (SNO) groups covalently bonded to the nanoparticles and/or S-nitrosothiol containing molecules encapsulated within the nanoparticles, as well as methods of making and using the nanoparticles. The invention also provides methods of preparing nanoparticles comprising Snitrosothiol (SNO) groups covalently bonded to the nanoparticles, where the methods comprise a) providing a buffer solution comprising chitosan, polyethylene glycol, nitrite, glucose, and hydrolyzed 3-mercaptopropyltrimethoxysilane (MPTS); b) adding hydrolyzed tetramethoxysilane (TMOS) to the buffer solution to produce a sol-gel; and c) lyophilizing and ball milling the sol-gel to produce nanoparticles of a desired size.Type: ApplicationFiled: May 1, 2013Publication date: May 28, 2015Inventors: Parimala Nacharaju, Chaim Tuckman-Vernon, Adam J. Friedman, Pedro Cabrales, Joel M. Friedman
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Publication number: 20150148360Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.Type: ApplicationFiled: July 19, 2013Publication date: May 28, 2015Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
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Patent number: 9040575Abstract: 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: GrantFiled: July 22, 2013Date of Patent: May 26, 2015Assignee: PROFESSIONAL DIETETICS, S.R.L.Inventors: Franco Conti, Francesco Saverio Dioguardi
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Patent number: 9034913Abstract: Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.Type: GrantFiled: September 11, 2006Date of Patent: May 19, 2015Assignee: Pfizer Inc.Inventors: Renuka D. Reddy, Evgenyi Shalaev, Ravi M. Shanker, Carl B. Ziegler
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Patent number: 9029406Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.Type: GrantFiled: March 12, 2012Date of Patent: May 12, 2015Assignee: Seattle Genetics, IncInventors: Hans-Georg Lerchen, Sherif El Sheikh, Beatrix Stelte-Ludwig, Joachim Schuhmacher, Mark Gnoth
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Publication number: 20150126575Abstract: There is provided a new dosage regimen for Compound A which maximizes anti-tumor activity while maintaining acceptable toxicity levels.Type: ApplicationFiled: January 14, 2015Publication date: May 7, 2015Inventors: Kelli Glenn, Brian Higgins, Gwen Nichols, Kathryn Packman
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Publication number: 20150126486Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Atsushi NAGANAWA, Kensuke KUSUMI, Kazuhiro OTSUKI, Tetsuya SEKIGUCHI, Akito KAKUUCHI, Koji SHINOZAKI, Hiroshi YAMAMOTO, Shigeyuki NONAKA
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Publication number: 20150119414Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.Type: ApplicationFiled: January 2, 2015Publication date: April 30, 2015Applicant: PIVOTAL THERAPEUTICS INC.Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar Ahmad SHAIKH, Jason YANTHA, Valerie B. SCHINI-KERTH
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Patent number: 9018237Abstract: The present disclosure relates to compositions for and methods of improving wound healing, including compositions for and methods of treating chronic wounds, and compositions for the inhibition and treatment of necrosis and extended quiescence that result in cellular necrosis instead of normal proliferation. The methods for wound healing administer one or more compositions including hydroxytyrosol and oleuropein with cells derived from umbilical cord blood.Type: GrantFiled: July 11, 2014Date of Patent: April 28, 2015Inventor: Darlene E. McCord
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Patent number: 9018206Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: September 12, 2012Date of Patent: April 28, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150111749Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.Type: ApplicationFiled: December 31, 2014Publication date: April 23, 2015Inventors: Huazhang Huang, Ratnakar Asolkar
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Patent number: 9012454Abstract: This document provides methods and materials related to treating mammals (e.g., humans) having a sexual dysfunction that is refractory to treatment with a PDE V inhibitor. For example, methods and materials related to the use of an ACE inhibitor and/or an angiotensin II receptor blocker with a PDE V inhibitor to treat mammals having a sexual dysfunction (e.g., erective dysfunction) that is unresponsive to treatment with a PDE V inhibitor are provided.Type: GrantFiled: December 8, 2006Date of Patent: April 21, 2015Assignee: Mayo Foundation for Medical Education and ResearchInventor: Frank V. Brozovich
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Publication number: 20150105392Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20150104504Abstract: 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: April 16, 2015Inventors: Bernardus Machielse, Timothy J. Maines, Michael H. Davidson, Bharat M. Mehta
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Publication number: 20150105378Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20150105436Abstract: Methods for regulating glucagon release and of treating hypoglycemia, and for screening drug candidates for heating hypoglycemia. The methods are useful for treating diabetes melititus and screening drug candidates for potential efficacy.Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: Per-Olof Berggren, Alejandro Caicedo, Over Cabrera
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Patent number: 9006249Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: June 7, 2012Date of Patent: April 14, 2015Assignee: Novartis AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Patent number: 9006283Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.Type: GrantFiled: July 12, 2007Date of Patent: April 14, 2015Assignee: Acumen Pharmaceuticals, Inc.Inventors: Grant A. Krafft, Todd Pray, William F. Goure
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Publication number: 20150099786Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150094322Abstract: Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventor: Susanne Riel
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Publication number: 20150094323Abstract: Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are provided.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventor: Susanne Riel
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Publication number: 20150087626Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.Type: ApplicationFiled: July 4, 2011Publication date: March 26, 2015Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Publication number: 20150086624Abstract: A pharmaceutical composition in multilayer-coated form including an omega-3 fatty acid or an alkyl ester thereof and a statin-based drug, and more particularly, a pharmaceutical composition for oral administration including: (a) a gelatin capsule core containing an omega-3 fatty acid or an alkyl ester thereof; (b) a first coating layer formed by coating, on the gelatin capsule core, hydroxypropyl methylcellulose and a copolymer of butyl methacrylate, (2-demethylaminoeethyl) methacrylate, and methyl methacrylate at a weight ratio of 1:2:1; and (c) a second coating layer formed by coating, on the first coating layer, a coating solution containing a statin-based drug.Type: ApplicationFiled: May 21, 2013Publication date: March 26, 2015Applicant: KUHNIL PHARM. CO., LTD.Inventors: Jae-Pyoung Cho, Pung-Sok Lee, Seul-A Lee, Min-Ho Jeong, Mase Lee
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Patent number: 8987322Abstract: The present invention relates to formulations comprising therapeutically effective amounts of at least one acid-stable, carrier-mediated transport statin, at least one poorly water-soluble, carrier-mediated transport statin, or at least one large molecular weight, carrier-mediated transport statin, such as atorvastatin and rosuvastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to exhibit a controlled-release of a therapeutic amount of the statin in the small intestine, thereby limiting systemic exposure of the statin and maximizing liver-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.Type: GrantFiled: October 19, 2004Date of Patent: March 24, 2015Assignee: Circ Pharma Research and Development LimitedInventors: Jackie Butler, John Devane, Paul Stark
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Patent number: 8987306Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: GrantFiled: September 24, 2009Date of Patent: March 24, 2015Assignee: The Trustees Of The University of PennsylvaniaInventors: William F. DeGrado, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
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Publication number: 20150079170Abstract: The present invention relates to novel tablet dosage forms and methods of preparing these forms, which can be used for different classes of pharmaceutical active ingredients posing stability issues in a single unit system. The dosage form includes a first layer, which includes a tablet of one or more active pharmaceutical ingredients, which is inlayed in the first layer along with other pharmaceutically acceptable excipients, and a second layer that includes one or more active pharmaceutical ingredients optionally with other pharmaceutically acceptable excipients.Type: ApplicationFiled: September 13, 2013Publication date: March 19, 2015Inventors: Girish Kumar JAIN, Ramakant GUNDU, Rahul DABRE
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Patent number: 8980868Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.Type: GrantFiled: July 30, 2010Date of Patent: March 17, 2015Assignee: Thar Pharmaceuticals, Inc.Inventors: Mazen Hanna, Ning Shan, Miranda Cheney, David Weyna
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Patent number: 8980936Abstract: 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: GrantFiled: July 18, 2013Date of Patent: March 17, 2015Assignee: Thesan Pharmaceuticals, Inc.Inventors: Jin Li, Nicole Lee Kolosko
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Publication number: 20150073032Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.Type: ApplicationFiled: September 8, 2014Publication date: March 12, 2015Inventor: Andre CHOLLET
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Publication number: 20150072003Abstract: The present invention relates to a hygroscopic matrix based composition, a process for the preparation thereof and its use in the treatment of diseases.Type: ApplicationFiled: October 28, 2014Publication date: March 12, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Eric Garcia, Nicole Kaiser, Joerg Kriese, Susanne Meier, Thomas Meyer, Susanne Page
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Publication number: 20150065553Abstract: The present invention is directed to statin formulations having improved solubility and/or stability and methods for the same.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Leo PAVLIV, Andrew VILA
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Patent number: 8969397Abstract: Disclosed herein are systems and methods for contributing to the local treatment of pain. More specifically, the disclosed systems and methods contribute to the local treatment pain by inhibiting the NF?B family of transcription factors.Type: GrantFiled: February 5, 2010Date of Patent: March 3, 2015Assignee: Warsaw Orthopedic, Inc.Inventors: Eric N. Burright, Lisa L. Shafer, Bill McKay, John Zanella
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Publication number: 20150056138Abstract: The invention features compounds and methods relating to hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters useful for diagnostic purposes. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention include radiolabeled inhibitors that can be used in research or clinical applications (e.g., for the treatment of cancer or ischemia-related central nervous system injury).Type: ApplicationFiled: October 15, 2014Publication date: February 26, 2015Inventor: Stephanie Lynn Martinelli
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Publication number: 20150057328Abstract: The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.Type: ApplicationFiled: October 31, 2014Publication date: February 26, 2015Inventors: Christoph BOSS, Christine BROTSCHI, John GATFIELD, Markus GUDE, Bibia HEIDMANN, Thierry SIFFERLEN, Jodi T. WILLIAMS
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Publication number: 20150051235Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: October 21, 2014Publication date: February 19, 2015Applicant: Infirst Healthcare LimitedInventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
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Publication number: 20150051247Abstract: Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.Type: ApplicationFiled: August 16, 2012Publication date: February 19, 2015Inventor: Samy O. Meroueh
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Patent number: 8957000Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.Type: GrantFiled: June 17, 2013Date of Patent: February 17, 2015Assignee: Marrone Bio Innovations, Inc.Inventors: Huazhang Huang, Ratnakar Asolkar