Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
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Publication number: 20140038987Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.Type: ApplicationFiled: October 8, 2013Publication date: February 6, 2014Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
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Patent number: 8642577Abstract: The present application provides methods and compositions for combination therapy with antiviral compounds for the treatment of poxvirus infections, such as orthopox virus infections. In one embodiment, a method of treatment of a poxvirus infection is provided that comprises administering to a host in need thereof cidofovir, cyclic cidofovir, or a salt, ester, or prodrug thereof in combination or alternation with at least a second anti-poxvirus agent. The second anti-poxvirus agent is, for example, a biologic, such as a pegylated interferon.Type: GrantFiled: April 10, 2006Date of Patent: February 4, 2014Assignee: Chimerix, Inc.Inventors: Merrick R. Almond, George R. Painter
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Publication number: 20140031208Abstract: The present invention relates to the use of dithiine-tetracarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-tetracarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.Type: ApplicationFiled: April 10, 2012Publication date: January 30, 2014Applicant: BASF SEInventors: Bernd Mueller, Nadege Boudet, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Richard Riggs, Ian Robert Craig, Jurith Montag, Egon Haden
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Patent number: 8637682Abstract: The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E2 (PGE2), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.Type: GrantFiled: May 11, 2009Date of Patent: January 28, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Isabella Coletta, Patrizia Dragone, Guido Furlotti, Barbara Garofalo, Angelo Guglielmotti, Giorgina Mangano, Caterina Maugeri
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Patent number: 8637080Abstract: The present invention provides a simple and improved rupturing controlled release device that is capable of providing a controlled release of active agent contained in the core first through a preformed passageway and then through an in situ formed second passageway into an environment of use in a standardized release profile manner. The rupturing controlled release device comprises a core comprising at least one drug and at least one osmopolymer, a semipermeable membrane enclosing the core and having at least one preformed passageway there through, wherein the semipermeable membrane ruptures during use to form a second passageway in the semipermeable membrane at a location spaced away from the preformed passageway, and a release-controlling subcoat between the core and the semipermeable membrane.Type: GrantFiled: June 25, 2008Date of Patent: January 28, 2014Assignee: Osmotica Kereskedelmi és Szolgáltató, KFTInventors: Ana C. Pastini, Joaquina Faour, Juan A. Vergez, Marcelo A. Ricci, Gustavo A. Fischbein
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Publication number: 20140024641Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.Type: ApplicationFiled: January 7, 2013Publication date: January 23, 2014Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
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Publication number: 20140010866Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: December 29, 2011Publication date: January 9, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20140005246Abstract: The present invention relates to the use of known dithiine-tetracarboximides as bird repellent.Type: ApplicationFiled: March 8, 2012Publication date: January 2, 2014Applicant: BAYER Intellectual Property GmbHInventor: Thomas Seitz
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Patent number: 8618156Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: GrantFiled: July 6, 2012Date of Patent: December 31, 2013Assignee: Gruenenthal GmbHInventors: Michael Gruss, Stefan Kluge, Stefan Pruehs
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Publication number: 20130345231Abstract: The invention described herein pertains to anticancer therapeutic agents that exhibit preferential cytotoxicity to malignant cells that express a cancer specific isoform of proliferating cell nuclear antigen (caPCNA) compared to cytotoxicity to comparable non-malignant cells, pharmaceutical compositions comprising the agents, and their use in cancer therapy.Type: ApplicationFiled: March 21, 2012Publication date: December 26, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Robert J. Hickey, Linda H. Malkas
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Patent number: 8614245Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: GrantFiled: January 8, 2013Date of Patent: December 24, 2013Assignee: Gruenenthal GmbHInventors: Michael Gruss, Stefan Kluge, Stefan Pruehs
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Publication number: 20130338207Abstract: The methods and compositions disclosed herein relate to using carbazole, and derivatives thereof to modify a signaling activity such as epidermal growth factor receptor (EGFR) signalling, and angiogenesis activity, in a cell.Type: ApplicationFiled: July 31, 2013Publication date: December 19, 2013Inventor: Jack L. Arbiser
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Publication number: 20130338143Abstract: Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety.Type: ApplicationFiled: November 15, 2011Publication date: December 19, 2013Applicant: Neuroderm, Ltd.Inventors: Oron Yacoby-Zeevi, Mara Nemas, Eduardo Zawozink
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Publication number: 20130331424Abstract: Described herein are antimicrobial compounds identified via a high-throughput inhibitor screen of the in vitro activity of MipZ, which is an ATPase that regulates division site placement in Caulobacter crescentus. The compounds and their analogs are active against bacterial membranes and thus represent a novel class of antimicrobial compounds. The antimicrobial compounds are effective against both actively growing bacterial cells as well as bacterial cells in the stationary phase. The antimicrobial compounds are also effective against bacteria in biofilms.Type: ApplicationFiled: June 10, 2013Publication date: December 12, 2013Inventors: Douglas Benjamin Weibel, Ye Jin Eun, Marie Hazel Foss, Katherine Ann Hurley
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Patent number: 8604074Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: GrantFiled: January 11, 2010Date of Patent: December 10, 2013Assignee: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20130302282Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: October 21, 2011Publication date: November 14, 2013Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Patent number: 8580841Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia): and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.Type: GrantFiled: July 22, 2009Date of Patent: November 12, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M Jones, Daniel J Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V Moody, Xiuwen Zhu, Scott Stirn
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Publication number: 20130295025Abstract: The chronic use of p-adrenergic inverse agonists such as nadolol, carvedilol, and ICI-118,551 provides an improved method for the treatment of mucus hypersecretion in subjects with such mucus hypersecretion. One aspect of a method according to the present invention is a method of preventing or controlling mucus hypersecretion in the respiratory tract comprising administering a therapeutically effective quantity of a p-adrenergic inverse agonist to a subject with mucus hypersecretion or at risk of mucus hypersecretion. The invention further encompasses pharmaceutical compositions comprising the p-adrenergic inverse agonist and the additional compound.Type: ApplicationFiled: January 9, 2012Publication date: November 7, 2013Applicant: INVION LIMITEDInventors: Richard A. Bond, Mitchell Glass
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Publication number: 20130295145Abstract: The present invention relates to stable pharmaceutical compositions comprising nano size droplets of etodolac or salts thereof along with other pharmaceutically acceptable excipients. These compositions exhibit greater permeability, and improved bioavailability leading to enhanced therapeutic activity. The invention also relates to processes for the preparation of such compositions.Type: ApplicationFiled: October 18, 2011Publication date: November 7, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Sunilendu Bhushan Roy, Jay Shantilal Kothari, Shafiq Sheikh, Jitendra Dasharathlal Patel, Jinesh Suresh Pancholi
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Publication number: 20130296167Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: ApplicationFiled: April 17, 2013Publication date: November 7, 2013Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
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Publication number: 20130296315Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: March 11, 2013Publication date: November 7, 2013Inventor: Bayer CropScience AG
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Patent number: 8568756Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: GrantFiled: June 2, 2009Date of Patent: October 29, 2013Assignee: The Trustees of Princeton UniversityInventors: Bonnie Bassler, Lee Swem
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Publication number: 20130281484Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: April 22, 2013Publication date: October 24, 2013Inventors: Alan Kozikowski, Kyle Vincent Butler, Jay Hans Kalin
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Publication number: 20130281462Abstract: Disclosed herein are compounds (for example, diamidine derivatives and prodrugs) and methods of use thereof, for example in treating muscular dystrophy (DM) or disease caused by a toxic RNA in a subject. In some embodiments, the methods include administering an effective amount of one of more of the disclosed compounds to a subject to treat or inhibit DM or a disease caused by or associated with toxic RNA, such as DM1, DM2, spinocerebellar ataxia type 8 (SCA8), fragile X tremor ataxia syndrome (FXTAS), or Huntington disease-like 2 (HLD2). In some examples, the methods include selecting a subject for treatment, for example selecting a subject with DM1, DM2, SCA8, FXTAS, or HLD2.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Applicants: University of OregonInventor: State of Oregon, acting by and through the State Board of Higher Education, on behalf of the University of Oregon
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Patent number: 8563038Abstract: Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.Type: GrantFiled: June 24, 2010Date of Patent: October 22, 2013Assignee: Egalet Ltd.Inventors: Christine Andersen, Karsten Lindhardt, Jan Martin Oevergaard, Louise Inoka Lyhne-Iversen, Martin Rex Olsen, Anne-Mette Haahr, Pernille Kristine Hoeyrup Hemmingsen
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Patent number: 8563591Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each inType: GrantFiled: August 26, 2005Date of Patent: October 22, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
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Publication number: 20130274248Abstract: [PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.Type: ApplicationFiled: May 31, 2013Publication date: October 17, 2013Inventors: Kazuei Igarashi, Hiromitsu Takayama
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Publication number: 20130267511Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: June 3, 2013Publication date: October 10, 2013Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Vendeville, Origene Nyanguile
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Publication number: 20130261137Abstract: The present invention relates to, inter alia, an anti-microtubule agent for use in a method of treating a subject having a latent virus, the method comprising: administering the anti-microtubule agent and an anti-viral agent to the subject.Type: ApplicationFiled: September 9, 2011Publication date: October 3, 2013Applicant: ULC BUSINESS PLCInventors: Edward Hiu Fung Tsao, Paul Kellam, Richard Gareth Jenner
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Patent number: 8546382Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.Type: GrantFiled: April 15, 2010Date of Patent: October 1, 2013Assignee: Children's Medical Center CorporationInventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
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Publication number: 20130252964Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.Type: ApplicationFiled: January 18, 2013Publication date: September 26, 2013Applicant: PolyMedix, Inc.Inventors: Richard W. Scott, Katie Freeman, Haizhong Tang, Gill Diamond
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Patent number: 8541462Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.Type: GrantFiled: January 25, 2012Date of Patent: September 24, 2013Assignee: AEterna Zentaris GmbHInventors: Tilmann Schuster, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
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Publication number: 20130231311Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
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Publication number: 20130231360Abstract: The present disclosure is directed to compounds of Formula (I) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.Type: ApplicationFiled: April 21, 2011Publication date: September 5, 2013Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.Inventors: Jonathan Higgins, Debasis Patnaik, Natalia Ulyanova, Ross L. Stein, Jun Xian, Marcie Glicksman, Gregory D. Cuny
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Patent number: 8524916Abstract: The present invention relates to novel dithiinetetra(thio)carboximides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.Type: GrantFiled: September 3, 2011Date of Patent: September 3, 2013Assignee: Bayer CropScience AGInventors: Thomas Himmler, Thomas Seitz, Ulrike Wachendorff-Neumann
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Publication number: 20130224151Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors alone or in combination for the treatment or prevention of abdominal, visceral or pelvic pain. Also described herein are pharmaceutical compositions comprising a FAAH inhibitor, alone or in combination with an additional therapeutic agent for the treatment of abdominal, visceral or pelvic pain.Type: ApplicationFiled: March 31, 2011Publication date: August 29, 2013Applicants: UNITED STATES OF AMERICA, IRONWOOD PHARMACEUTICALS, INCInventors: James Philip Pearson, Mark G. Currie, Yvette Tache, Muriel Larauche
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Patent number: 8519154Abstract: The present invention relates to a method for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising administering to the patient suffering from asthma and COPD an effective dose of carbazole derivatives or salt thereof, optionally along with pharmaceutically acceptable excipients. Structural formula of the compounds of general formula 1 useful as phosphodiesterase-4 (PDE-4) enzyme inhibitors, inhibitor for signalling molecule for the treatment of asthma and asthma related diseases is given below: wherein R1=H or OCH3; R2?CH3 or CHO; R3?H or OCH3; R4?H or OCH3 Herbal route for the isolation of compound of general formula 1 from the bark of plant Murraya Koenigii and chemical route for the preparation of such compounds from basic compounds such as vanillin is also reported.Type: GrantFiled: February 3, 2012Date of Patent: August 27, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Sibabrata Mukhopadhyay, Mumu Chakraborty, Tulika Mukherjee, Arun Bandyopadhyay, Dipak Kar, Tanima Banerjee, Aditya Konar, Debaprasad Jana, Siddhartha Roy, Santu Bandyopadhyay, Balram Ghosh, Mabalirajan Ulaganathan, Rakesh Kamal Johri, Subhash Chander Sharma, Gurdarshan Singh, Bholanath Paul, Vasanta Madhava Sharma Gangavaram, Jhillu Singh Yadav, Radha Krishna Palakodety
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Publication number: 20130217673Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.Type: ApplicationFiled: February 22, 2012Publication date: August 22, 2013Applicant: Warsaw Orthopedic, IncInventor: Jared T. Wilsey
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Patent number: 8513292Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.Type: GrantFiled: June 19, 2008Date of Patent: August 20, 2013Assignee: ArQule, Inc.Inventors: Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
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Publication number: 20130202553Abstract: Methods, processes, uses, and pharmaceutical compositions are provided herein for mobilizing hematopoietic progenitor cells and/or cancer stem cells from bone marrow into peripheral blood, comprising the administration of an effective amount of an inhibitor of GTPases, such as a Cdc-42 specific inhibitor alone or in combination with one or more additional agents. Specifically, methods are disclosed for mobilizing hematopoietic stem cells into a subject's peripheral blood. In particular, embodiments of the method involve specific inhibition of the Cdc42 GTPase to increase the numbers of hematopoietic stem cells into a subject's peripheral blood of a subject.Type: ApplicationFiled: February 21, 2013Publication date: August 8, 2013Applicant: CHILDREN'S HOSPITAL MEDICAL CENTERInventor: Children's Hospital Medical Center
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Patent number: 8501959Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: June 23, 2009Date of Patent: August 6, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Brian Andrew Stearns, Yen Pham Truong
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Publication number: 20130196965Abstract: The invention relates to a compound of formula (I) wherein A, B, D and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: January 10, 2013Publication date: August 1, 2013Applicant: HOFFMANN-LA ROCHE INC.Inventor: HOFFMANN-LA ROCHE INC.
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Publication number: 20130190339Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: December 10, 2012Publication date: July 25, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents of the University of Texas System
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Publication number: 20130190273Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: February 19, 2013Publication date: July 25, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
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Patent number: 8492426Abstract: A method of treating diabetes by administering Carvedilol in patients and diabetes mellitus. This method of treatment will eliminate the need for insulin and other blood sugar controlling agents in hypertensive patients with Type II diabetes mellitus, and will significantly reduce the required dosage of insulin and eliminate the need for other blood controlling agents in patients with Type I diabetes mellitus. This method will also delay and/or prevent the progression of non-insulin dependent Type II diabetes mellitus to insulin-dependent Type II diabetes mellitus. Moreover, this method has been shown to preserve improve insulin receptor sensitivity such that patient's HbA1c level reaches and is maintained at or near 7% or less.Type: GrantFiled: July 12, 2012Date of Patent: July 23, 2013Inventor: Anis Ahmad
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Publication number: 20130184301Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: January 14, 2013Publication date: July 18, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents of the University of Texas System
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Publication number: 20130184307Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: ApplicationFiled: March 6, 2013Publication date: July 18, 2013Applicant: Arena Pharmaceuticals, Inc.Inventor: Arena Pharmaceuticals, Inc.
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Publication number: 20130184271Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: February 19, 2013Publication date: July 18, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM