Ring Oxygen In The Bicyclo Ring System Patents (Class 514/302)
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Patent number: 8058289Abstract: The present invention is related to pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: October 18, 2010Date of Patent: November 15, 2011Assignee: Merck Serono SAInventors: Thomas Rueckle, Anna Quattropani, Vincent Pomel, Jerome Dorbais, David Covini, Alexander Bischoff
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Patent number: 8053574Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: GrantFiled: July 16, 2008Date of Patent: November 8, 2011Assignee: Novartis AGInventors: Ian Bruce, Darren Mark Legrand, James Dale, Thomas Anthony Hunt
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Publication number: 20110269753Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.Type: ApplicationFiled: January 21, 2010Publication date: November 3, 2011Applicant: ORCHID RESEARCH LABORATORIES LTD.Inventors: Gopalan Balasubramanian, Sukunath Narayanan, Ganapavarapu Veera Raghava Sharma, Lavanya Andiappan, Shridhar Narayanan, Sanjeev Saxena, Sridharan Rajagopal, Santosh Lolaknath Vishwakarma, Saravanan Thirunavukkarasu
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Patent number: 8048879Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compound corresponding to formula I, methods for producing them, to medicaments containing these compounds, the use of these compounds for producing medicaments and related treatment methodsType: GrantFiled: April 5, 2006Date of Patent: November 1, 2011Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann, Jörg Holenz, HagenHeinrich Hennies
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Publication number: 20110263529Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 27, 2011Inventors: Ruo Xu, John W. Clader
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Publication number: 20110263596Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20110263617Abstract: The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.Type: ApplicationFiled: September 8, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael Mark, Peter Eickelmann, Gerd Luippold, Leo Thomas
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Publication number: 20110263562Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.Type: ApplicationFiled: April 26, 2011Publication date: October 27, 2011Inventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
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Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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Patent number: 8039481Abstract: The present invention includes novel derivatives of bicyclic tetrahydrofuran imino acids of formula I, processes for their preparation, and uses thereof as medicaments. The compounds are suitable for use in the therapy and prophylaxis of diseases which are associated with an increased matrix metalloproteinase activity.Type: GrantFiled: July 13, 2007Date of Patent: October 18, 2011Assignee: Sanofi-AventisInventors: Manfred Schudok, Hans Matter, Armin Hofmeister
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Publication number: 20110250142Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing hypertension and complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and a second antihypertensive agent (preferably a calcium antagonist, an ACE inhibitor, or an angiotensin II receptor antagonist) for treating and/or preventing hypertension and complications in patients with diabetes and/or metabolic syndrome.Type: ApplicationFiled: March 1, 2011Publication date: October 13, 2011Inventors: Benson M. Fong, Glen V. Cornett
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Publication number: 20110251211Abstract: A method for treating a subject having an inflammatory or auto-immune disease with a substituted isoxazolo pyridinone. Also, a method for administering a substituted isoxazolo pyridinone to a cell to retain or increase glucocorticoid receptor transrepression activity with only minimal glucocorticoid receptor transactivation activity.Type: ApplicationFiled: January 13, 2010Publication date: October 13, 2011Inventors: Huaqiang Eric Xu, Yong Xu, Yuanzheng He
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Publication number: 20110245259Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: ApplicationFiled: December 11, 2009Publication date: October 6, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110230502Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: ApplicationFiled: March 18, 2011Publication date: September 22, 2011Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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Publication number: 20110230497Abstract: The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.Type: ApplicationFiled: November 2, 2009Publication date: September 22, 2011Applicant: H. Lundbeck A/SInventors: John Matthew Peterson, Chien-An Chen, Bin Chen, Lingyun Wu, Michael Lloyd Sabio
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Patent number: 8022084Abstract: The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.Type: GrantFiled: January 26, 2006Date of Patent: September 20, 2011Assignee: H. Lundbeck A/SInventors: Daniel J. Kumke, Jerry A. Murry, Bryon L. Simmons, Feng Xu
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Patent number: 8022057Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: November 7, 2008Date of Patent: September 20, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Toufike Kanouni, Michael B. Wallace
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Publication number: 20110224196Abstract: This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from obstructive sleep apnea syndrome (OSAS). Treatment of OSAS is effected by administering a carbonic anhydrase inhibitor to the patient in combination with at least one additional active agent. Examples of additional active agents include modafinil, eszopiclone, zolpidem, zaleplon, and phentermine.Type: ApplicationFiled: January 7, 2011Publication date: September 15, 2011Applicant: Vivus, Inc.Inventors: Leland F. Wilson, Peter Tam, Thomas Najarian, Charles H. Bowden
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Publication number: 20110212031Abstract: The present invention relates to novel MAO-B binding compounds and methods for measuring effects of the compounds, by measuring changes of MAO-B levels in living patients. More specifically, the present invention relates to use of the compounds of this invention as therapeutic agents for inhibition of MAO-B activity as well as a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study MAO-B levels in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel MAO-B binding compounds as diagnostic, as we a therapeutic, agents. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds.Type: ApplicationFiled: October 21, 2009Publication date: September 1, 2011Inventors: Cyrille Sur, David L. Williams
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Publication number: 20110212970Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: September 1, 2011Applicant: CALCIMEDICA, INC.Inventors: GONUL VELICELEBI, KENNETH A. STAUDERMAN, JEFFREY P. WHITTEN, YAZHONG PEI, JIANGUO CAO, ZHIJUN WANG, EVAN ROGERS, BRIAN DYCK, JONATHAN GREY
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Publication number: 20110212941Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: ApplicationFiled: November 3, 2009Publication date: September 1, 2011Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Patent number: 7999107Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia.Type: GrantFiled: January 16, 2008Date of Patent: August 16, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: John S. Debenham, Jeffrey J. Hale, Pei Huo, Christina B. Madsen-Duggan, Thomas F. Walsh, Lin Yan
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Patent number: 7994191Abstract: The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.Type: GrantFiled: December 2, 2009Date of Patent: August 9, 2011Assignee: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Michael J. Grogan, Martin Tremblay
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110190334Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.Type: ApplicationFiled: November 3, 2010Publication date: August 4, 2011Applicant: NOVARTIS AGInventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
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Publication number: 20110178120Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: AMBRILIA BIOPHARMA, INC.Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
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Publication number: 20110152225Abstract: Rosiglitazone, 5-ASA or structurally analogous Compounds according to the general formula (I): or Compounds according to the general formula (Ia): For the induction of CAMP expression in tissues having PPAR-gamma receptors. Such tissues include epithelia or mucosae tissue having PPAR-gamma receptors and of particular interest is CAMP expression in the gut.Type: ApplicationFiled: February 27, 2008Publication date: June 23, 2011Inventors: Sergio Baroni, Pierre Desreumaux, Salvatore Bellinvia
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Publication number: 20110150864Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110144086Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.Type: ApplicationFiled: July 15, 2009Publication date: June 16, 2011Applicant: The United States of America, as represented by the Secretary, Dept of Health and Human ServiceInventors: Sanjay A. Desai, Ajay D. Pillai
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Publication number: 20110130387Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 29, 2010Publication date: June 2, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Publication number: 20110112137Abstract: Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided.Type: ApplicationFiled: February 23, 2009Publication date: May 12, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan, John W. Erickson
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Publication number: 20110098237Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
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Publication number: 20110086833Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: May 27, 2009Publication date: April 14, 2011Inventors: Sergey V. Paushkin, Nikolai Naryshkin, Charles Romfo, Ellen Welch
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Publication number: 20110085985Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: May 28, 2009Publication date: April 14, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Publication number: 20110082171Abstract: Provided is the use of an agonist of a GABAA receptor for use in the prevention, reduction or inhibition of scarring formed on healing of a wound. Also provided is a method of preventing, reducing or inhibiting scarring formed on healing of a wound, in which a therapeutically effective amount of an agonist of a GABAA receptor is administered to a patient in need of such prevention, reduction or inhibition. The GABAA receptor agonist used may be an agonist specific to the GABAA receptor, such as Gaboxadol (7-tetra hydroisoxazolo[5,4-c]pyridin-3-ol), or a pharmaceutically acceptable salt thereof. The scarring to be prevented, reduced or inhibited may be scarring formed on healing of a wound of the dermis.Type: ApplicationFiled: June 2, 2009Publication date: April 7, 2011Applicant: Renovo LimitedInventors: Mark William James Ferguson, Nicholas Occleston, Sharon O'Kane, Kerry Nield, Nick Goldspink
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Publication number: 20110082132Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH?CH—E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.Type: ApplicationFiled: June 2, 2009Publication date: April 7, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110077239Abstract: A medicament for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the production of such a medicament, and a method for the treatment of such phantom phenomenaType: ApplicationFiled: June 18, 2010Publication date: March 31, 2011Inventors: Marlies Knipper, Lukas Ruettiger, Bernhard Schick, Julia Dlugaiczyk
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Publication number: 20110077154Abstract: The present invention relates to pyridin-4-ylmethyl sulfonamides of formula I wherein Het, Ra, Rc, Rf, m, n, p, R, A and Y are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.Type: ApplicationFiled: May 20, 2009Publication date: March 31, 2011Applicant: BASF SEInventors: Alice Glaettli, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Marianna Vrettou
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Patent number: 7915417Abstract: Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.Type: GrantFiled: August 11, 2008Date of Patent: March 29, 2011Assignee: Washington UniversityInventors: Scott J. Hultgren, Jerome S. Pinkner, Fredrik Almqvist, Nils Pemberton, Veronica Aberg, Andreas Larsson
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Publication number: 20110071111Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome.Type: ApplicationFiled: July 15, 2010Publication date: March 24, 2011Inventors: Benson M. Fong, Glenn V. Cornett
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Publication number: 20110052536Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of treating HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: September 18, 2008Publication date: March 3, 2011Inventors: Shirit Einav, Jeffrey S. Glenn, Robert McDowell, Wenjin Yang, Hadas Dvory-Sobol
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Patent number: 7897615Abstract: The present invention provides previous methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.Type: GrantFiled: October 2, 2007Date of Patent: March 1, 2011Assignee: Chugai Sciyaku Kabushiki KaishaInventors: Mark D. Kafka, Mark E. Wilson, Anna Russell, Gary D. Lopaschuk, Jason R. Dyck
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Publication number: 20110046175Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20110046176Abstract: Furanopyridine cannabinoid analog compounds of the formula I are disclosed. The compounds are useful to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20110039883Abstract: The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I wherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Hubert Heuer, Norbert Tennagels
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Publication number: 20110039843Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko Iwakoshi, Ippei Uemura