Additional Hetero Ring Patents (Class 514/422)
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Publication number: 20140186328Abstract: The present invention provides neuroprotective polyphenol compounds, which can be synthetic analogs of fisetin, baicalein or chlorogenic acid, that maintain neuroprotective, anti-inflammatory, glutathione promoting, and/or antioxidant properties. The neuroprotective polyphenol compounds are useful for promoting, enhancing and/or increasing neuron protection, growth and/or regeneration. The polyphenol compounds further find use for increasing and or maintaining intracellular glutathione (GSH) levels. The polyphenol compounds are also useful for treating, preventing, mitigating and/or delaying neurodegenerative conditions, including diabetes, Parkinson's disease, Huntington's disease, Alzheimer's disease, non-Alzheimer's dementias, multiple sclerosis, traumatic brain injury, spinal cord injury or ALS.Type: ApplicationFiled: February 5, 2014Publication date: July 3, 2014Applicant: Salk Institute for Biological StudiesInventors: David R. Schubert, Pamela A. Maher, Chandramouli Chiruta
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Publication number: 20140186278Abstract: An anhydrous multiphase gel system consisting of an outer lipid matrix and an inner phase gelled by means of a polymer is described, which can be obtained by a) Melting the lipid phase with the formation of a liquid lipid phase, b) Mixing and homogenizing polymers or polymer blends capable of swelling with the formation of a polymer phase to be dispersed, c) Combining the polymer phase with the liquid lipid phase and homogenizing the phases, and d) Cold stirring the phase mixture until a solid gel-like mixed structure of the entire system is formed. The anhydrous multiphase gel system is particularly suitable for taking up difficulty soluble active substances in high concentration and for providing topical and transdermal applications. The described system is called an EDRS, “Entrapped Drug Reservoir System”.Type: ApplicationFiled: September 19, 2013Publication date: July 3, 2014Inventor: Patrick Franke
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Publication number: 20140186329Abstract: The present invention provides methods of use of polyphenol compounds for treating, preventing, mitigating and delaying ischemia or a condition where ischemia occurs. In one embodiment, the method comprises providing a polyphenol analog; and administering the polyphenol analog to a subject to treat ischemia or a condition where ischemia occurs. Various embodiments of the present invention are useful for the treatment of patients having, or at risk for, any of (1) ischemic stroke, (2) hemorrhagic stroke, (3) cardiovascular disease, (4) ischemia related spinal cord injury, (5) ischemia in diabetic patients, or (6) embolic stroke. For example, use of the polyphenol compounds can maintain glutathione levels in the patient.Type: ApplicationFiled: February 6, 2014Publication date: July 3, 2014Inventors: Paul A. Lapchak, David R. Schubert, Pamela A. Maher, Chandramouli Chiruta
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Publication number: 20140187546Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.Type: ApplicationFiled: January 2, 2014Publication date: July 3, 2014Applicant: Rutgers, The State University of New JerseyInventors: Longqin Hu, Amrik Sahota
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Patent number: 8765681Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.Type: GrantFiled: November 8, 2012Date of Patent: July 1, 2014Assignee: Pharmascience Inc.Inventors: Alain Boudreault, James Jaquith, Patrick Bureau, John W. Gillard, Alain Laurent
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Publication number: 20140178447Abstract: Disclosed herein are methods and compositions for rendering medical devices and other surfaces biofilm resistant by the use of a coating composition comprising a combination of one or more antimicrobial agent, one or more anti-inflammatory agent, optionally a releasing agent, optionally decandediol, and a lubricious matrix system comprising a biomedical polymer. In certain embodiments said coating composition is adhered to the device or surface by a coating comprising urethane and silicone adhesives.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Inventors: Shanta M. Modak, Ronald Citron, Santoshkumar Dongre, Nayana Baiju, Arnab Kumar Ghosh
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Publication number: 20140179753Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: March 5, 2014Publication date: June 26, 2014Applicant: Simpson Biotech Co., Ltd.Inventors: Masao HATTORI, Ali EL-HALAWANY, Megumi MIZUNO, Chia-Chin SHEU
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Publication number: 20140179752Abstract: The specification discloses compositions and methods for treating a soft tissue defect of an individual.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Allergan, Inc.Inventors: Dennis E. Van Epps, Guan-Liang Jiang, Wha Bin Im
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Publication number: 20140179661Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.Type: ApplicationFiled: April 8, 2012Publication date: June 26, 2014Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
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Publication number: 20140171481Abstract: The present invention features solid compositions comprising amorphous Compound I. For instance, Compound I may be formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.Type: ApplicationFiled: February 14, 2014Publication date: June 19, 2014Inventors: Bernd Liepold, Tina Jung, Peter H?lig, Rudolf Schroeder, Nancy E. Sever, Justin S. Lafountaine, Brent D. Sinclair, Yi Gao, Jianwei Wu
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Patent number: 8754117Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.Type: GrantFiled: January 28, 2013Date of Patent: June 17, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, Jianguo Ma
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Patent number: 8754095Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: SanofiInventor: Zhongli Gao
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Publication number: 20140163025Abstract: The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: December 2, 2013Publication date: June 12, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Sara FRATTINI, Elke LANGKOPF, Holger WAGNER
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Patent number: 8748476Abstract: The invention provides the use of darifenacin, or a pharmaceutically acceptable derivative thereof, in the manufacture of a medicament for the reduction of urgency in patients suffering from overactive bladder.Type: GrantFiled: March 4, 2009Date of Patent: June 10, 2014Assignee: Warner Chilcott Company, LLCInventors: Enrico Colli, Paul Quinn, Dzelal Serdarevic, Larence Howard Skillern
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Patent number: 8748470Abstract: The present invention concerns methods and compositions for the inhibition or reduction of the primary tumor and metastasis by inhibition of fatty acid binding proteins.Type: GrantFiled: March 16, 2012Date of Patent: June 10, 2014Assignee: The University of ChicagoInventors: Ernst Lengyel, Kristin Nieman, Hilary Kenny
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Publication number: 20140155447Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20140155382Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
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Patent number: 8742135Abstract: A compound having a structure expressed by the following Structural Formula (1), tautomers thereof, or salts of the compound or the tautomers.Type: GrantFiled: October 21, 2011Date of Patent: June 3, 2014Assignee: Microbial Chemistry Research FoundationInventors: Masayuki Igarashi, Ryuichi Sawa, Yoshiko Homma
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Patent number: 8735385Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: May 27, 2014Assignee: SanofiInventor: Zhongli Gao
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Patent number: 8734831Abstract: A method for manufacturing a porous ceramic scaffold having an organic/inorganic hybrid coating layer containing a bioactive factor includes (a) forming a porous ceramic scaffold; (b) mixing a silica xerogel and a physiologically active organic substance in a volumetric ratio ranging from 30:70 to 90:10 and treating by a sol gel method to prepare an organic/inorganic hybrid composite solution; (c) adding a bioactive factor to the organic/inorganic hybrid composite solution and agitating until gelation occurs; and (d) coating the porous ceramic scaffold with the organic/inorganic composite containing the bioactive factor added thereto. In accordance with the method, the porous ceramic scaffold may be uniformly coated with the organic/inorganic hybrid composite while maintaining an open pore structure, and stably discharge the bioactive factor over a long period of time.Type: GrantFiled: April 15, 2011Date of Patent: May 27, 2014Assignee: SNU R&DB FoundationInventors: Hyoun-Ee Kim, Shin-Hee Jun, Eun-Jung Lee
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Publication number: 20140142067Abstract: The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto.Type: ApplicationFiled: November 12, 2013Publication date: May 22, 2014Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITYInventors: Aviv GAZIT, Shimon SLAVIN, Esther PRIEL, Sara YITZCHAK
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Publication number: 20140142159Abstract: The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a diastereoisomer thereof for use in the treatment of cancers associated with human papillomavirus. The present invention also relates to the pharmaceutical compositions containing the compounds of Formula (I) for the treatment of cancers associated with human papillomavirus.Type: ApplicationFiled: June 22, 2012Publication date: May 22, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Swati Ajay Piramal, Muralidhara Padigaru, Veena R Agarwal, Gandhali Ashwin Deshpande
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Publication number: 20140142082Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: PHENEX PHARMACEUTICALS AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Publication number: 20140142042Abstract: A combination of a prostaglandin EP4 agonist and an effective amount of: a prostaglandin EP2 agonist, a skin growth factor, a small peptide, a small inhibitory RNA targeting excess chronic inflammation or fibrosis, a cytokine with beneficial anti-inflammatory activity, an adenosine A2a receptor agonist, an anti-oxidant, or a combination thereof, may be used to treat skin wounds or scars.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Applicant: Allergan, Inc.Inventors: Guang L. Jiang, Robert M. Burk, Wha-Bin Im, Larry A. Wheeler
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Publication number: 20140140997Abstract: Provided are methods for treating or reducing the likelihood of developing a retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline. These methods require the administration of at least one agent that specifically binds to CD11a and/or CD18, or ICAM-1, and/or decreases or prevents the binding of LFA-1 (CD11a/CD18 heterodimer) to ICAM-1. Also provided are veterinary compositions and methods of identifying candidate agents useful for treating or reducing retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline.Type: ApplicationFiled: June 15, 2012Publication date: May 22, 2014Applicant: CytoDyn Inc.Inventor: Richard Trauger
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Patent number: 8729075Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: GrantFiled: February 7, 2013Date of Patent: May 20, 2014Assignee: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas Natoli
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Patent number: 8729068Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: GrantFiled: October 26, 2012Date of Patent: May 20, 2014Assignee: Astellas Pharma Inc.Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Patent number: 8729063Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: December 20, 2012Date of Patent: May 20, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Publication number: 20140135373Abstract: Compound with formula (I), wherein R? and R? represent a hydrogen atom, a monovalent radical with formula (IIa), or a monovalent radical with formula (IIb), it being understood that at least one of the R? or R? radicals does not represent a hydrogen atom and that when the R? and R? radicals do not represent a hydrogen atom, R? and R? are identical; method for preparing and using in cosmetics and as a drug.Type: ApplicationFiled: May 24, 2012Publication date: May 15, 2014Applicant: SOCIETE D'EXPLOITATION DE PROUITS POUR LES INDUSTRIES CHMIQUES SEPPICInventors: Andre Benattar, Laetitia Cattuzzato, Sandy Dumont, Stephanie Garcel, Jerome Guilbot, Sebastien Kkerverdo, Herve Rolland
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Publication number: 20140135322Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.Type: ApplicationFiled: July 13, 2012Publication date: May 15, 2014Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
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Publication number: 20140135310Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.Type: ApplicationFiled: June 29, 2012Publication date: May 15, 2014Applicant: Adamed Sp. z o.o.Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
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Publication number: 20140135385Abstract: This invention relates to methods of treating T-cell mediated diseases or disorders in human or animal subjects, such as autoimmune diseases and chronic graft versus host disease in humans and animals. In particular, the methods comprise administering to the human or animal patient a pharmaceutical composition comprising a ryanodine receptor inhibitor.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Applicant: The Regents of the University of CaliforniaInventor: Alla F. Fomina
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Publication number: 20140128436Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: November 8, 2013Publication date: May 8, 2014Applicant: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20140128358Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: October 3, 2011Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Berthon
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Patent number: 8716180Abstract: The present invention provides a method of reducing mycotoxin contamination of a plant and/or harvested plant material, said method comprising treating plant propagation material with one or more fungicides, germinating or growing said plant propagation material to produce a plant, and harvesting plant material from said plant.Type: GrantFiled: June 28, 2006Date of Patent: May 6, 2014Assignee: Syngenta Crop Protection LLCInventors: Edmond Sztor, Pascal Poels, Michael Oostendorp, Franz Brandl
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Patent number: 8716327Abstract: The disclosure provides methods for treating fatty liver disease and associated conditions by inhibiting the synthesis of glucosphingolipids, as exemplified by the use of glucosylceramide synthase substrate analogs.Type: GrantFiled: May 9, 2007Date of Patent: May 6, 2014Assignee: Genzyme CorporationInventors: Hongmei Zhao, Nelson S. Yew, Seng H. Cheng, Canwen Jiang, Cynthia Marie Arbeeny
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Publication number: 20140121260Abstract: The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: MedWell Laboratories Ltd.Inventors: Taher NASSAR, Raiyn Nureldin, Rayan Anwar
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Patent number: 8709434Abstract: Phycobilins are disclosed to have prodrug activity as inhibitors of NADPH oxidase activity and are disclosed to be useful in the prophylaxis and/or treatment of medical conditions associated with or linked to an NADPH oxidase activity. Compositions containing phycobilins are described which facilitate the administration of phycobilins.Type: GrantFiled: November 13, 2007Date of Patent: April 29, 2014Assignee: PCB Associates, Inc.Inventors: Mark Fredrick McCarty, Sheldon Saul Hendler, David Michael Rorvik, Toyoshi Inoguchi
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SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF SQUAMOUS CELL CARCINOMA OF HEAD AND NECK
Publication number: 20140112918Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.Type: ApplicationFiled: May 30, 2012Publication date: April 24, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy -
Publication number: 20140112882Abstract: Methods for use of a composition comprising agents that increase pancreatic interleukin-22 production in the treatment of pancreatic inflammatory disorders including pancreatitis-associated acute lung injury.Type: ApplicationFiled: October 8, 2013Publication date: April 24, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Aida Habtezion, Jing Xue
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Patent number: 8703184Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent.Type: GrantFiled: March 20, 2013Date of Patent: April 22, 2014Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Patent number: 8703649Abstract: The present invention relates to formulation comprising at least (i) two pesticidal compounds A and B dissolved in a lactic acid ester and wherein a) both A and B have melting points below 900 C b) both A and B are selected from the following list: pyraclos-trobin, metalaxyl, mefenoxam, trifloxystrobin, imazalil, pro-chloraz and ipconazole with the proviso that A is different from B (ii) at least one pesticidal compound C present in solid particles, and having a melting point of 900 C and above, and to their use as seed treatment formulation as well as their use for plant protection, including seed and crop protection.Type: GrantFiled: July 20, 2010Date of Patent: April 22, 2014Assignee: BASF SEInventors: Rafel Israels, Katharine Klamczynski, Marco Kuhns, Ulf Schlotterbeck
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8703810Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: GrantFiled: June 8, 2011Date of Patent: April 22, 2014Assignee: Seragon Pharmaceuticals, Inc.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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Publication number: 20140107123Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: ApplicationFiled: August 5, 2013Publication date: April 17, 2014Applicant: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Publication number: 20140107095Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: SERAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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Patent number: 8697723Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.Type: GrantFiled: June 14, 2013Date of Patent: April 15, 2014Assignee: Orion CorporationInventors: David Din Belle, Patrik Holm, Arto Karljalainen, Arto Tolvanen, Gerd Wohlfahrt, Petteri Rummakko
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Patent number: 8697870Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: November 19, 2008Date of Patent: April 15, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20140100211Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8691235Abstract: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: GrantFiled: April 5, 2010Date of Patent: April 8, 2014Assignee: Poly-Med, Inc.Inventors: Shalaby W Shalaby, David Ingram, Georgios T Hilas, Sheila Nagatomi