At Imidazole Ring Carbon Patents (Class 514/400)
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Publication number: 20140364379Abstract: Ophthalmic products and related methods are described herein. These methods include a stabilizing composition comprising a therapeutically active agent which is separated from a liquid vehicle composition by a barrier. The barrier may be removed to allow the two compositions to mix to provide an ophthalmically acceptable liquid comprising the therapeutically active agent.Type: ApplicationFiled: July 26, 2012Publication date: December 11, 2014Applicant: Allergan Inc.Inventors: Anuradha V. Gore, Sai Shankar, Sukhon Likitiersuang, Chetan P. Pujara, Sesha Neervanna
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Publication number: 20140357587Abstract: The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.Type: ApplicationFiled: October 9, 2012Publication date: December 4, 2014Inventors: Vladimir Evgenievich Nebolsin, Lyudmila Vasilievna Kolobukhina
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Publication number: 20140357673Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: July 31, 2014Publication date: December 4, 2014Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey William Perry, Roderick Joseph Sorenson, Mary Xuan Dziem O'Riordan, Yafei Jin
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Patent number: 8901106Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: GrantFiled: March 26, 2012Date of Patent: December 2, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ellen K. Kick, Michael J. Hageman, Victor R. Guarino, Ching-Chiang Su, Chenkou Wei, Jayakumar S. Warrier, Satheesh Nair
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Publication number: 20140343112Abstract: The present invention encompasses an amino acid composition for recovery of muscle strength and function.Type: ApplicationFiled: November 19, 2012Publication date: November 20, 2014Inventors: Arny Ferrando, Robert R. Wolfe
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Publication number: 20140343000Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: July 24, 2014Publication date: November 20, 2014Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
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Patent number: 8889725Abstract: An ant bait which contains an active substance having insecticidal activity and a sugar syrup is described.Type: GrantFiled: March 8, 2007Date of Patent: November 18, 2014Assignee: Bayer Cropscience AGInventors: Volker Gutsmann, Thomas Böcker, Günther Nentwig, Justin McBeath, Jeffery Einam
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Publication number: 20140335036Abstract: A hair care composition having from about from about 0.025% to about 0.25% by weight of the composition of histidine. The hair care composition further includes a gel matrix phase. The gel matrix has from about 0.1% to about 20% of one or more high melting point fatty compounds, from about 0.1% to about 10% of a C22 cationic surfactant system, and at least about 20% of an aqueous carrier, by weight of said hair care composition. The present invention may further comprise a deposition polymer.Type: ApplicationFiled: May 6, 2014Publication date: November 13, 2014Applicant: The Procter & Gamble CompanyInventors: Jennifer Mary Marsh, Toshiyuki Iwata, Phan Shean Lim
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Patent number: 8883180Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: August 29, 2013Date of Patent: November 11, 2014Assignee: Bayer Intellectual Property GmbHInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140329815Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Publication number: 20140323501Abstract: Immune-modulators of formula (I) below are prepared: A pharmaceutical composition contains the immune-modulators. The pharmaceutical composition is used as a drug, especially as an immune-modulating drug. The compound can be used in treatment of immune disorders and for immune suppression. Thus, for example, the compound can be used in treating hypo-immunity, rejection after organ transplantation and auto-immune disease.Type: ApplicationFiled: July 5, 2012Publication date: October 30, 2014Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCESInventors: Weijuan Han, Haijing Zhang, Xiaojian Wang, Jing Jin, Gang Li, Yi Zhang, Qiong Xiao, Wanqi Zhou, Xiaoguang Chen, Dali Yin
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Publication number: 20140322247Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.Type: ApplicationFiled: March 13, 2014Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
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Publication number: 20140315961Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
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Publication number: 20140315945Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140314850Abstract: The present application relates to functionalized nanodiamonds, to complexes comprising a functionalized nanodiamond reversibly bound to a nucleic acid and to compositions comprising such functionalized nanodiamonds and complexes. In particular, the functionalized nanodiamonds comprise at least one naturally occurring basic amino acid, or analogs or derivatives thereof, covalently linked to a nanodiamond. The present application also includes methods and uses of the complexes and compositions, for example for delivering a nucleic acid to a cell.Type: ApplicationFiled: April 17, 2014Publication date: October 23, 2014Applicant: University of SaskatchewanInventors: Ildiko Badea, Ronald Verrall, Jackson M. Chitanda, Randeep Kaur, Saniya Alwani
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Publication number: 20140309195Abstract: Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing.Type: ApplicationFiled: January 8, 2014Publication date: October 16, 2014Applicant: INTERNATIONAL STEM CELL CORPORATIONInventors: Rodolfo Gonzalez, Maxim Poustovoitov, Ruslan Semechkin
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Publication number: 20140309268Abstract: Several embodiments provided herein relate to histamine dosing regimens are and uses of such regimens in the restoration of histamine balance in subjects suffering from, for example, histapenia and/or histadelia. Several embodiments also relate to the use of histamine dosing regimens for the treatment and/or prevention of migraine headaches.Type: ApplicationFiled: June 25, 2014Publication date: October 16, 2014Inventor: Cristian Arnou
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Patent number: 8859604Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: GrantFiled: February 3, 2014Date of Patent: October 14, 2014Assignee: Furiex Pharmaceuticals, Inc.Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Publication number: 20140303099Abstract: Compositions and methods for improving cardiovascular health, especially in the elderly, by delivering a selection of essential amino acids selected from the group of histidine, isoleucine, leucine, valine, lysine, methionine, phenylalanine, threonine, and arginine, which may be supplemented with a low glycemic carbohydrate and/or a medium chain fatty acid.Type: ApplicationFiled: April 14, 2014Publication date: October 9, 2014Applicant: Energy Light, LLCInventors: Robert Wolfe, John P. Troup, Nicolaas ("Mick") Emile Paulas Deutz
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Publication number: 20140302069Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.Type: ApplicationFiled: November 7, 2012Publication date: October 9, 2014Inventors: David Fairlie, Robert C. Reid
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Publication number: 20140301998Abstract: Disclosed is a cosmetic or dermatological formulation comprising a) at least one polyol in a concentration of from 0.1 to 20% by weight, based on the total weight of the formulation, and b) at least one diol selected from 2-methyl-1,3-propanediol, pentanediol, and hexanediol, in a concentration of from 0.1 to 25% by weight, based on the total weight of the formulation.Type: ApplicationFiled: June 2, 2014Publication date: October 9, 2014Applicant: BEIERSDORF AGInventors: Rainer KROPKE, Jens NIELSEN, Kathrin WOLTER
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Publication number: 20140287988Abstract: Provided herein are compositions, which include an active pharmaceutical ingredient and macrogol 15 hydroxystearate, and methods for using the same for treating diseases or disorder.Type: ApplicationFiled: December 9, 2013Publication date: September 25, 2014Applicant: ALLERGAN, INC.Inventors: ANURADHA V. GORE, KEVIN S. WARNER, CHETAN P. PUJARA, RICHARD S. GRAHAM, AJAY P. PARASHAR, MU-LAN LEE, ROBERT S. JORDAN, SUKHON LIKITLERSUANG
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Publication number: 20140271955Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicants: The Scripps Research Institute, The California Institute for Biomedical ResearchInventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
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Publication number: 20140271854Abstract: Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Applicant: FURIEX PHARMACEUTICALSInventors: Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
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Publication number: 20140271604Abstract: Polymorphic forms of histone deacetylase inhibitors (HDAC) and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns, solubility, stability and other properties.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventor: STEFAN PRONIUK
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Patent number: 8835480Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.Type: GrantFiled: April 22, 2008Date of Patent: September 16, 2014Assignee: California Institute of TechnologyInventors: Peter B. Dervan, Nicholas G. Nickols
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Publication number: 20140256779Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: Jannsen Pharmaceutica, N.V.Inventors: Henry J. Breslin, Chaozhong Cai, Wei He, Robert W. Kavash
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Publication number: 20140256743Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicants: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
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Compounds, compositions and methods for the treatment of beta-amyloid diseases and synucleinopathies
Patent number: 8829198Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: October 3, 2008Date of Patent: September 9, 2014Assignee: Proteotech IncInventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow, Lesley Larsen -
Patent number: 8829004Abstract: The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. According to the present invention inhibitors of the nitric oxide dioxygenase or arginase can be used for the manufacture of a medicament for the treatment of cancer. The present invention further provides a method for identifying compounds which can be used for the treatment of cancer, wherein the method allows to specifically identify compounds which induce apoptosis through the ROS signaling pathway. The present invention also provides a kit for identifying compounds which induce tumor apoptosis by inactivating a catalase on the tumor cell surface.Type: GrantFiled: September 27, 2012Date of Patent: September 9, 2014Assignee: Universitaetsklinikum FreiburgInventor: Georg Bauer
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Publication number: 20140243362Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.Type: ApplicationFiled: September 25, 2012Publication date: August 28, 2014Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
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Patent number: 8815924Abstract: Novel heterocyclic compounds of the formula (I), in which R1, D, W, T and T? have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: April 4, 2005Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20140234306Abstract: A method for treating an autism spectrum condition includes administering an effective dose of a TNF-? inhibiting agent to a person having an autism spectrum condition or pervasive development disorder and at least one of elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum, as compared to normal conditions; and lowering at least one of the elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum. A TNF-? inhibiting agent includes at least one of Lenalinomide; Thalidomide; L-Carnosine; Infliximab; Etanercept; a stem cell preparation; derivatives thereof, isomers thereof, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Inventor: Michael Chez
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Publication number: 20140228419Abstract: The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.Type: ApplicationFiled: September 18, 2012Publication date: August 14, 2014Applicant: DoubleHill GmbHInventors: Jochen Kalbe, Olaf Hansen
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Publication number: 20140228296Abstract: The present invention relates to the discovery that an increased fraction of albumin is carbamylated in patients suffering from kidney disease (e.g., end-stage renal disease) and that the fraction of carbamylated albumin is also correlated with increased disease severity, particularly risk of mortality. The present invention also relates to the discovery that free amino acids can reduce carbamylation of albumin. Based on these discoveries the present invention provides diagnostic and prognostic methods for patients suffering from, or suspected of suffering from kidney disease. The invention also provides methods for treating kidney disease by administration of a compound or composition that reduced protein carbamylation, such as free amino acids or dipeptides.Type: ApplicationFiled: July 13, 2012Publication date: August 14, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventors: Anders H. Berg, S. Ananth Karumanchi, Ravi I. Thadhani
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Patent number: 8802128Abstract: Biocompatible intraocular implant systems are formulated for discontinuous or intermittent release of therapeutic levels of a therapeutic agent (such as a steroid) to minimize development of side effects associated with continuous or long term use of such agent. The implant system may comprise one or more implant, and preferably, although not necessarily, also contains an auxiliary agent having an activity effective to lessen at least one side effect associated with said therapeutic agent compared to the use of an otherwise identical implant system lacking said auxiliary agent. The implants containing the therapeutic agent and auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the ocular side effects otherwise accompanying the use of such therapeutic agent.Type: GrantFiled: July 21, 2006Date of Patent: August 12, 2014Assignee: Allergan, Inc.Inventors: Michael R. Robinson, Scott M. Whitcup
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Publication number: 20140221444Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: FURIEX PHARMACEUTICALS, INC.Inventors: Luigi Anzalone, Frank J. Villani, Chrisptoher A. Teleha, Penina Feibush, Barry Fegely
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Publication number: 20140221337Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.Type: ApplicationFiled: February 6, 2014Publication date: August 7, 2014Applicant: Xention LimitedInventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
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Publication number: 20140212362Abstract: Compositions containing imidazole-based compounds, and optionally, colloidal oatmeal, for the treatment, prevention, and management of symptoms, conditions, diseases, and disorders of the skin. Also, methods for the treatment, prevention, and management of symptoms, conditions, diseases, and disorders of the skin using compositions containing imidazole-based compounds, and optionally, colloidal oatmeal.Type: ApplicationFiled: March 31, 2014Publication date: July 31, 2014Applicant: THERACEUTIX, LLCInventor: Douglas A. Pippin
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Patent number: 8791102Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: GrantFiled: October 16, 2009Date of Patent: July 29, 2014Assignee: Exelixis, Inc.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20140206736Abstract: Composition comprising leucine, isoleucine, valine, threonine and lysine for use in prophylactic and/or therapeutic treatment of renal disorders in a subject, preferably an elderly subject.Type: ApplicationFiled: March 26, 2014Publication date: July 24, 2014Applicant: DETERMINANTS OF METABOLISM RESEARCH LABORATORY S.R.L.Inventors: Franco CONTI, Francesco Saverio DIOGUARDI
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Publication number: 20140206651Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: ApplicationFiled: March 24, 2014Publication date: July 24, 2014Applicant: Pfizer Inc.Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
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Publication number: 20140200251Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.Type: ApplicationFiled: September 13, 2013Publication date: July 17, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Douglas E. Raines, Stuart A. Forman, Keith W. Miller, Syed Shaukat Husain, Joseph F. Cotten
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Publication number: 20140200516Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II; aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Applicant: ABBOTT LABORATORIESInventor: Harry A. DUGGER, III
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Patent number: 8772336Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: October 11, 2012Date of Patent: July 8, 2014Assignees: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
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Patent number: 8765798Abstract: Dipeptide compounds containing a histidine residue proved to have interesting blocking activity on secondary products from lipid oxidative stress, in particular on unsaturated aldehydes such as malondialdehyde and hydroxynonenal, which are known to contribute to the inset of quite a number of chronic pathologies such as neurodegenerative, inflammatory chronic, cardiovascular diseases, diabetes complications and cataract.Type: GrantFiled: June 15, 2007Date of Patent: July 1, 2014Assignee: Flamma S.p.A.Inventors: Gianpaolo Negrisoli, Renato Canevotti
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Publication number: 20140178458Abstract: A medicinal skin protection composition is disclosed with an active ingredient combination that specifically serves to care for aging skin that is exposed to difficult environmental conditions. The active ingredient combination obligatorily includes the components almond oil, linseed oil fatty acids, amino acids, and creatine. The medicinal skin protection composition can be used for aging skin in the form of creams, lotions etc., and also for a variety of incontinence articles, such as sanitary towels or nappies.Type: ApplicationFiled: August 10, 2012Publication date: June 26, 2014Applicants: Evonik Industries AG, Paul Hartmann AGInventors: Hans Smola, Marina Kagan-Hoper, Thomas Mangen, Petra Allef, Eckhard Heisler
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Publication number: 20140178349Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: December 16, 2013Publication date: June 26, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
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Publication number: 20140163009Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.Type: ApplicationFiled: January 23, 2012Publication date: June 12, 2014Applicant: CHDI FoundationInventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
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Publication number: 20140163081Abstract: Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: November 21, 2013Publication date: June 12, 2014Applicants: Exelixis Patent Company LLC, BRISTOL-MYERS SQUIBB COMPANYInventors: Brett B. Busch, William C. Stevens, JR., Ellen K. Kick, Haiying Zhang, Venkataiah Bollu, Richard Martin, Raju Mohan