The Six-membered Hetero Rings Are Bonded Directly To Each Other Patents (Class 514/334)
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Patent number: 8129416Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: GrantFiled: May 21, 2007Date of Patent: March 6, 2012Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Laurence Clary, Corinne Millois Barbuis
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Patent number: 8114895Abstract: The present invention relates to an isolated bioactive molecule Caerulomycin A, derivatives and analogs thereof as effective immunosuppressive agents. The immunosuppressive property of the compound is targeted in particular against the lymphocytes, CD4+ T cells, CD8+ T cells and B cells and in the production of IL-4 and IFN-? and antibodies. The compound operates through a mechanism by downregulating the expression of activation marker CD28 and upregulating the immunosuppressive marker CTLA-4. Caerulomycin A has previously been isolated from Streptomyces caeruleus and found to have useful antifungal activity. Prior to the present invention however, this compound had not been determined to have immunomodulatory activity.Type: GrantFiled: September 12, 2006Date of Patent: February 14, 2012Assignee: Council of Science and Industrial ResearchInventors: Arvind Kumar Singla, Javed Naim Agrewala, Rakesh Mulraj Vohra, Ravinder Singh Jolly
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Patent number: 8110579Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: GrantFiled: February 11, 2009Date of Patent: February 7, 2012Assignee: Sanofi-AventisInventors: Jean-Michel Altenburger, Valerie Fossey, Philip Janiak, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres
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Publication number: 20120014917Abstract: The invention relates to methods of treating patients infected with human immunodeficiency virus (HIV) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicants: University of Minnesota, INTERMUNE, INC.Inventors: Karl Kossen, Timothy Schacker, Ashley T. Haase
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Patent number: 8097628Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.Type: GrantFiled: May 21, 2009Date of Patent: January 17, 2012Assignee: Glaxo Group LimitedInventors: Carlos Alemparte-Gallardo, Christopher Barfoot, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Alan Joseph Hennessy, Neil David Pearson, Modesto Jesus Remuinan-Blanco
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Patent number: 8093269Abstract: The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.Type: GrantFiled: June 7, 2006Date of Patent: January 10, 2012Assignee: University of Florida Research FoundationInventors: William R. Kem, Ferenc Soti
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Publication number: 20110301140Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are 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 orexin receptors are involved.Type: ApplicationFiled: August 4, 2011Publication date: December 8, 2011Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
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Patent number: 8067441Abstract: The present invention relates to the use of Collismycin and derivatives thereof as inhibitors of oxidative stress in cells and their use for the preparation of medicaments for the treatment of oxidative stress-induced diseases or conditions, especially neurodegenerative diseases, such as Alzheimer's Disease and Parkinson's Disease.Type: GrantFiled: July 28, 2006Date of Patent: November 29, 2011Assignees: Neuropharma, S.A., Instituto Biomar, S.A.Inventors: Ana Martinez Gil, Paola Usan Egea, Miguel Medina Padilla, Esther Garcia Palomero, Julia Perez Baz, Rosa Isabel Fernandez Chimeno, Antonio Medarde Fernandez, Librada Maria Canedo Hernandez, Francisco Romero Millan, Ana Castro Morera, Mercedes Alonso Cascon, Jorge Sanchez Quesada
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Publication number: 20110288129Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: July 8, 2011Publication date: November 24, 2011Applicant: ABBOTT LABORATORIESInventors: Anil Vasudevan, Brian S. Brown, Jerome F. Daanen, Arthur R. Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark A. Matulenko
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Patent number: 8058272Abstract: The present disclosure relates to XIAP inhibitor compound of the formula I:Type: GrantFiled: December 7, 2007Date of Patent: November 15, 2011Assignee: Novartis AGInventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20110269666Abstract: A method for treating septic hypotension, including administering at least one alpha-2 agonist or other sympatholytic, and at least one vasopressor. The alpha-2 agonist may be clonidine or dexmedetomidine, and the sympaholytic may be rilmelidine, monoxidine, alpha-methyldopa and alpha-methylparatyrosine. The vasopressor may be noradrenaline, adrenaline, vasopressin, angiotensin and phenylephrine. The method can include intravenous infusion of the patient with at least one inotrope such as dobutamine and phosphodiesterase inhibitors. Suitable inotropes include amrinone and milrinone. In a preferred embodiment, the alpha-2 agonist and the vasopressor are simultaneously administered. Also disclosed is a composition for treating septic shock hypotension which includes at least one alpha-2 agonist and at least one vasopressor.Type: ApplicationFiled: June 24, 2011Publication date: November 3, 2011Inventor: Luc QUINTIN
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Publication number: 20110263615Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.Type: ApplicationFiled: July 8, 2011Publication date: October 27, 2011Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Woltering
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Publication number: 20110257199Abstract: Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.Type: ApplicationFiled: June 17, 2011Publication date: October 20, 2011Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa, Laixing Hu
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Publication number: 20110251208Abstract: The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca2+- sensitizing agent or a pharmaceutically acceptable derivative thereof for the treatment of a patient suffering from hypertrophic cardiomyopathy (HCM). According to another aspect the present invention relates to the use of a PDE III inhibitor and/or Ca2+-sensitizing agent for the preparation of a medicament for the treatment of a patient suffering from HCM.Type: ApplicationFiled: November 23, 2009Publication date: October 13, 2011Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Juergen Daemmgen, Olaf Joens
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Publication number: 20110251144Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject at least one compound selected from the group consisting of those set forth in Table 1, Table 2, Table 3, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: September 16, 2009Publication date: October 13, 2011Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20110251162Abstract: The present subject matter relates to pathogenesis of MRSA. Specifically, the present disclosures identifies the pro-inflammatory properties of PVL as the cause of MRSA. Viewed from this new perspective, the present subject matter achieves novel methods and apparatus for treating MRSA infection in a subject involving the administration of an anti-inflammatory drug to the subject. Furthermore the present subject matter teaches methods and apparatus for treating a Panton-Valetine leukocidin associated infection in a subject involving the administration of an anti-inflammatory drug to the subject.Type: ApplicationFiled: September 25, 2009Publication date: October 13, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: George Y. Liu, Ching Wen Tseng
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Publication number: 20110245286Abstract: Methods of inhibiting release of a proinflammatory cytokine from a macrophage are provided. The methods comprise treating the macrophage with a cholinergic agonist in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from the macrophage, wherein the cholinergic agonist is selective for an ?7 nicotinic receptor. Methods for inhibiting an inflammatory cytokine cascade in a patient are also provided. The methods comprise treating the patient with a cholinergic agonist in an amount sufficient to inhibit the inflammatory cytokine cascade, wherein the cholinergic agonist is selective for an ?7 nicotinic receptor. Methods for determining whether a compound is a cholinergic agonist reactive with an ?7 nicotinic receptor are also provided. The methods comprise determining whether the compound inhibits release of a proinflammatory cytokine from a mammalian cell.Type: ApplicationFiled: February 1, 2011Publication date: October 6, 2011Applicant: THE FEINSTEIN INSTITUTE FOR MEDICAL RESEARCHInventors: KEVIN J. TRACEY, HONG WANG
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Publication number: 20110237627Abstract: Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.Type: ApplicationFiled: March 23, 2010Publication date: September 29, 2011Applicant: ROCK CREEK PHARMACEUTICALS, INC.Inventors: Tom Thomas Puthiaparampil, Thomas Kanathkunn David, Muppala Sarveswara Raju
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Publication number: 20110237525Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.Type: ApplicationFiled: June 18, 2010Publication date: September 29, 2011Inventors: Boyd E. Haley, Niladri Narayan Gupta
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Publication number: 20110230483Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: March 14, 2011Publication date: September 22, 2011Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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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: 20110212945Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: ApplicationFiled: August 8, 2008Publication date: September 1, 2011Applicant: ALMIRALL, S.A.Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
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Publication number: 20110201591Abstract: The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are 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 orexin receptors are involved.Type: ApplicationFiled: October 26, 2009Publication date: August 18, 2011Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mamio Christa Mattern, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
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Publication number: 20110201602Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: ApplicationFiled: November 22, 2010Publication date: August 18, 2011Applicant: Amgen Inc.Inventors: Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Stuart C. CHAFFEE, Paul TEMPEST, Phillip R. OLIVIERI, Rebecca E. JOHNSON, Brian K. ALBRECHT, Vinod F. PATEL, Victor J. CEE, Joseph L. KIM, Steven BELLON, Xiaotian ZHU, Yuan CHENG, Ning XI, Karina ROMERO, Hanh Nho NGUYEN, Holly L. DEAK
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Patent number: 7998982Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: August 8, 2008Date of Patent: August 16, 2011Assignee: Abbott LaboratoriesInventors: Anil Vasudevan, Brian S. Brown, Jerome F. Daanen, Arthur R. Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark A. Matulenko
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Patent number: 7994199Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.Type: GrantFiled: March 16, 2010Date of Patent: August 9, 2011Assignee: Memory Pharmaceuticals CorporationInventors: Brian Herbert, Wenge Xie, Truc Minh Nguyen, Allen T Hopper, Ashok Tehim
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Publication number: 20110190206Abstract: Embodiments of the invention are directed to methods of treating reperfusion or resuscitation injury in an individual in need of such treatment, comprising the step of administering to the individual who has had, having, or is at immediate risk of having an ischemic event an amount of a composition comprising a protein kinase A (PKA) activator and a ?1-adrenergic receptor antagonist sufficient to reduce reperfusion injury to an ischemic tissue.Type: ApplicationFiled: June 12, 2009Publication date: August 4, 2011Inventors: Ming-He Huang, Kenichi Fujise, Barry F. Uretsky
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Publication number: 20110158983Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.Type: ApplicationFiled: March 5, 2009Publication date: June 30, 2011Inventors: Newell Bascomb, John Maki, Fredric S. Young
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Publication number: 20110152324Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.Type: ApplicationFiled: February 16, 2010Publication date: June 23, 2011Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Qun Sun, Laykea Tafesse
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Publication number: 20110151035Abstract: A smoking cessation aid is in the form of a lozenge containing powdered tobacco and a therapeutically effective amount of a silver salt. In another embodiment, a lozenge contains nicotine and a therapeutically effective amount of a silver salt. In yet another embodiment, a lozenge contains (i) at least one of anatabine, anabasine, and nornicotine, and (ii) a therapeutically effective amount of a silver salt.Type: ApplicationFiled: December 13, 2010Publication date: June 23, 2011Applicant: ROCK CREEK PHARMACEUTICALS, INC.Inventor: Curtis Wright, IV
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Publication number: 20110151024Abstract: The present invention relates to compositions and methods for preventing migraines. The migraine prophylaxis composition is a single dosage form comprising at least one form of elemental magnesium and at least one NSAID. The prophylaxis composition, comprising at least one form of elemental magnesium and a therapeutically effective concentration of acetylsalicylic acid may also provide cardiac protection and prevent cardiovascular diseases.Type: ApplicationFiled: March 1, 2011Publication date: June 23, 2011Inventor: Alexander Mauskop
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Publication number: 20110136833Abstract: The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: August 3, 2009Publication date: June 9, 2011Applicant: Shinogi & Co., Ltd.Inventors: Hidenori Mikamiyama, Chiyou NI, Bin Shao, Laykea Tafesse
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Publication number: 20110130390Abstract: The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders.Type: ApplicationFiled: January 3, 2011Publication date: June 2, 2011Inventor: Norbert Müller
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Publication number: 20110130380Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.Type: ApplicationFiled: September 2, 2010Publication date: June 2, 2011Inventors: Paul A. Barsanti, Cheng Hu, Xianming Jin, Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton
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Publication number: 20110118316Abstract: The invention relates to a method for the treatment or prevention of diseases or conditions associated with vascular endothelium dysfunction or liver injury comprising the administration to a patient in a need of such treatment or prevention of a therapeutically or prophylactically effective amount of a compound selected from the group consisting of: wherein R represents hydrogen atom, CH3, OH, pyridyl (C5H4N), 1-methylpyridyl (C5H4N—CH3) or pyridyl substituted with hydroxy group ((OH)C5H3N), and X represents a physiologically acceptable counterion.Type: ApplicationFiled: January 21, 2011Publication date: May 19, 2011Applicant: TRIGENDO sp. z o.o.Inventors: Andrzej MARCINEK, Stefan Chlopicki, Jerzy Gebicki, Jan Adamus
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Publication number: 20110112064Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are 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 T-type calcium channels are involved.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20110112128Abstract: A method of treating ileus in a subject by administering to the subject an effective amount of a pharmacological agent that increases the activity of cholinergic receptor in a subject. Examples of pharmacological agents are brain muscarinic agonist, cholinergic agonist or cholinesterase inhibitor. The methods of the present invention can be used to treat ileus caused by abdominal surgery, or administration of narcotics or chemotherapeutic agents such as during cancer chemotherapy.Type: ApplicationFiled: July 20, 2010Publication date: May 12, 2011Inventors: Kevin J. Tracey, Mitchell P. Fink
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Patent number: 7939549Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).Type: GrantFiled: February 27, 2009Date of Patent: May 10, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Satoshi Nagato, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito
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Patent number: 7939548Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: July 31, 2007Date of Patent: May 10, 2011Assignee: Cytokinetics, Inc.Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
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Publication number: 20110092544Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein each W and Y is independently CH2, O, C(?O), S(?O)n, NR8 or a direct bond; R4 is H, halogen, cyano, hydroxy, C1-C2 alkyl, C1-C2 haloalkyl, C2 alkenyl, C2 haloalkenyl or C2 alkynyl; m is an integer selected from 0, 1, 2, 3, 4 and 5; and R1, R2, R3, R5, R8 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: June 18, 2009Publication date: April 21, 2011Applicant: E.I. DU PONT DE nemours and companyInventor: Bruce Lawrence Finkelstein
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Publication number: 20110091574Abstract: Methods of treating adenocarcinoma cells such as NSCLC cells are disclosed that depend upon the level of functionally active LKB1 expressed in the cancer cells being treated. In one embodiment, the cancer cells express functionally active LKB1 and the method comprises contacting those cells with a LKB1-stimulating amount of a COX-2-specific inhibitor in combination with an inhibiting amount of a specific inhibitor of mTOR. In another embodiment, the cancer cells express about 25 percent or less of the normal, functional LKB1 expressed by non-transformed cells of the same type are contacted with a growth inhibiting amount of an agent that inhibits cellular metabolism and induces energetic stress.Type: ApplicationFiled: February 13, 2009Publication date: April 21, 2011Applicant: Catholic Healthcare WestInventors: Landon J. Inge, Keith D. Coon
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Publication number: 20110092456Abstract: The present invention shows that cilostazol, a phosphodiesterase 3 inhibitor has additional beneficial effects to atorvastatin on myocardial remodeling by inducing and preserving eNOS phosphorylation. The present invention demonstrates a cardioprotective effect of Cilostazol indicating the therapeutic potency of this drug. In addition, the present invention demonstrates that the additional effect of Cilostazol and atorvastatin therapy against ischemia injury is due to the augmentation of phosphatodylicositol 3-kinase/AKT (PI3-/AKT), PKA and p-eNOS signaling.Type: ApplicationFiled: October 19, 2009Publication date: April 21, 2011Inventor: Yochai Birnbaum
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Publication number: 20110082134Abstract: The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.Type: ApplicationFiled: November 12, 2010Publication date: April 7, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. JONES, Graeme SEMPLE, Beatriz FIORAVANTI, Guilherme PEREIRA, Imelda CALDERON, Jane Laguerta UY, Kameshwari DUVVURI, Jin Sun Karoline CHOI, Yifeng XIONG, Vibha DAVE, Mihai D. AZIMIOARA
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Publication number: 20110070189Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: September 21, 2010Publication date: March 24, 2011Inventors: Jim Li, Javier de Vincente Fidalgo, Ryan Craig Schoenfield, Francisco Xavier Talamas
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Publication number: 20110071192Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: ApplicationFiled: September 21, 2010Publication date: March 24, 2011Applicant: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20110052694Abstract: Described herein are microneedle drug delivery systems comprising a pharmaceutical compositions comprising pharmaceutically active agents (e.g., cannabidiol and prodrugs of cannabidiol) and microneedle arrays suitable for local and systemic delivery of the active agent to a mammal. Also described herein are methods of using a microneedle transdermal or topical drug delivery systems comprising pharmaceutical compositions, comprising cannabidiol and prodrugs of cannabidiol, and microneedle arrays in the treatment disease, including pancreatitis and pancreatic cancer.Type: ApplicationFiled: August 31, 2010Publication date: March 3, 2011Applicant: ALLTRANZ INC.Inventors: Audra Lynn Stinchcomb, Stan Lee Banks, Miroslaw Jerzy Golinski, Jeffery Lynn Howard, Dana Carmel Hammell
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Publication number: 20110045076Abstract: Intravaginal drug delivery devices, including intravaginal rings, are provided herein. The devices comprise a polyether urethane composition and a pharmaceutically effective amount of at least one vaginally administrable drug homogeneously distributed throughout the polyether urethane. The devices are capable of exhibiting a substantially zero order release profile of drug over extended periods of time. Also disclosed are methods for making the devices and methods of using the devices to prevent or treat a biological condition.Type: ApplicationFiled: January 23, 2009Publication date: February 24, 2011Inventors: Patrick F. Kiser, Kavita Gupta
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Publication number: 20110028460Abstract: It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.Type: ApplicationFiled: August 2, 2010Publication date: February 3, 2011Inventors: Edward T. Kisak, John M. Newsam, Dominic King-Smith, Pankaj Karande, Samir Mitragotri
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel