Divalent Chalcogen Or Acyclic Nitrogen Double Bonded At 2-position, Or Tautomeric Equivalent Patents (Class 514/392)
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Publication number: 20120316198Abstract: Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed.Type: ApplicationFiled: December 3, 2010Publication date: December 13, 2012Applicant: The United States of American, as Represented by the Secretary, Dept. of Health and Human ServicesInventors: Adrian Wiestner, Yihong Ye, Qiuyan Wang, William C. Trenkle, Bidhan A. Shinkre
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Publication number: 20120309744Abstract: The invention encompasses dosing regimens in which a subject is administered menatetrenone over a period of time to establish initial therapeutic baseline blood concentration of the menatetrenone followed by a maintenance therapy to maintain therapeutic blood concentrations. In other embodiments, the invention encompasses methods of treating hepatocellular adenocarcinoma in a subject in need thereof comprising administering to a subject a therapeutically effective dosing regimen of menatetrenone.Type: ApplicationFiled: June 1, 2011Publication date: December 6, 2012Applicant: NBI Pharmaceuticals, Inc.Inventors: John NEUSTADT, Steve PIECZENIK
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Publication number: 20120309777Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.Type: ApplicationFiled: February 16, 2011Publication date: December 6, 2012Applicant: UNIVERSITE LAVALInventors: René C. Gaudreault, Sébastien Fortin
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Publication number: 20120283302Abstract: A SCCA-1 production inhibitor, comprising as an active ingredient, at least one carboxamide derivative selected from the group consisting of compounds represented by the following formula (I): wherein X is CR5 or N, R1, R4 and R5 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, R2 and R3 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, or each represents a group —(CH2)n—, wherein n represents an integer of 1 or 2, and may form a 5- to 6-membered ring together with the atoms to which they are bonded and with the carbonyl group, allantoin, and salts thereof.Type: ApplicationFiled: April 28, 2010Publication date: November 8, 2012Applicant: SHISEIDO COMPANY, LTDInventors: Maki Kaneko, Takuya Hiruma, Masaru Suetsugu, Chika Katagiri, Toshii Iida, Tomoko Onodera
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Publication number: 20120283303Abstract: The present invention relates to the use of N-aminoimidazole or N-aminoimidazole thione derivatives as cytoprotective compounds in vitro and in vivo and for the treatment or prevention of cell death mediated disorders and/or GSK-3 mediated disorders or processes.Type: ApplicationFiled: April 30, 2012Publication date: November 8, 2012Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENTInventors: Christophe Pannecouque, Wim Robberecht, Miguel Stevens
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Publication number: 20120277235Abstract: A composition comprising at least one physiologically tolerated film forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.Type: ApplicationFiled: March 30, 2012Publication date: November 1, 2012Inventors: Karl Theodor Kraemer, Manfred Bohn
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Publication number: 20120269864Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: June 11, 2012Publication date: October 25, 2012Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
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Publication number: 20120270916Abstract: Compositions for the topical or transdermal treatment of neuropathy. More particularly, transdermal or topical compositions including a combination of ingredients that provide a surprising degree of effective relief from the symptoms of peripheral neuropathy are described.Type: ApplicationFiled: March 16, 2012Publication date: October 25, 2012Applicant: TARAXOS INC.Inventor: Richard Wolicki
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Publication number: 20120270902Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: ApplicationFiled: February 13, 2012Publication date: October 25, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Martin Neitzel, Jennifer Marugg
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Patent number: 8283363Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: November 5, 2010Date of Patent: October 9, 2012Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20120245191Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: March 19, 2012Publication date: September 27, 2012Inventors: Daniel Hunziker, Werner Neidhart
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Publication number: 20120238610Abstract: Treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. The use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune and inflammatory diseases associated with TLR3 as well as TLR4 and/or TLR3/TLR4 cellular signaling in association with related pathologies is disclosed. Methods of treating a subject having a disease or condition associated with abnormal TLR-3 as well as TLR-4 and/or TLR3/TLR4 cellular signaling in association with related pathologies are also disclosed. The present disclosure also relates to the treatment of autoimmune-inflammatory pathologies and chemokine and cytokine-mediated diseases associated with TLR overexpression and signaling.Type: ApplicationFiled: February 9, 2012Publication date: September 20, 2012Inventors: Leonard D. Kohn, Norikazu Harii, Uruguaysito Benavides-Peratta, Mariana Gonzalez-Murguiondo, Christopher J. Lewis, Douglas J. Goetz
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Publication number: 20120238607Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 21, 2012Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulf BRÜGGEMEIER, Chantal FÜRSTNER, Volker GEISS, Joerg KELDENICH, Armin KERN, Martina DELBECK, Peter KOLKHOF, Axel KRETSCHMER, Elisabeth POOK, Carsten SCHMECK, Hubert TRÜBEL
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Patent number: 8268875Abstract: Methods for treating carpal tunnel syndrome and tarsal tunnel syndrome in a subject involve providing an effective amount of an anti-cytokine agent at or near inflammation in the carpal or tarsal tunnel. Anti-cytokine agents, such as, TNF-a inhibitors, NF-?B inhibitors, IL-1 inhibitors, IL-6 inhibitors, IL-8 inhibitors, IL-12 inhibitors, IL-15 inhibitors, IL-10, Interferon-gamma (IFN-gamma) act to prevent further inflammation initiated by cytokine factors. One embodiment includes, adding with the anti-cytokine agent one or more of an antibiotic or analgesic. Delivery of the anti-cytokine agent may be provided to the inflamed tissue of the carpal or tarsal tunnel by injection, implantation, or a transdermal patch. These agents, individually or in combination, directly address the underlying inflammation that causes the discomfort, pain, and restricted movement associated with carpal and tarsal tunnel syndrome.Type: GrantFiled: November 16, 2010Date of Patent: September 18, 2012Assignee: Warsaw Orthopedic, Inc.Inventor: John M. Zanella
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Patent number: 8263624Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: GrantFiled: May 25, 2007Date of Patent: September 11, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
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Publication number: 20120225917Abstract: The present invention provides a pest control composition having an excellent controlling effect on pests, which comprises a combination of an ester compound represented by the formula (1): and a cyclic compound represented by the formula (2a) and/or a cyclic compound represented by the formula (2b).Type: ApplicationFiled: November 19, 2010Publication date: September 6, 2012Inventors: Masahiro Yamada, Yoshito Tanaka
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Publication number: 20120196911Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are used to activate alpha2 adrenergic receptors. The compounds of Formula 1 are incorporated in pharmaceutical compositions and are used as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors.Type: ApplicationFiled: April 16, 2012Publication date: August 2, 2012Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler, John R. Cappiello
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Publication number: 20120196824Abstract: The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.Type: ApplicationFiled: October 8, 2010Publication date: August 2, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Tomofumi Setsuta, Maki Seki, Hiroshi Iwasaki, Minoru Tanaka
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Publication number: 20120190719Abstract: Disclosed herein is a method of treating compulsive disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist.Type: ApplicationFiled: August 26, 2010Publication date: July 26, 2012Applicant: ALLERGAN, INC.Inventors: Daniel W. Gil, John E. Donello, Lauren M.B. Luhrs
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Publication number: 20120183481Abstract: A heparanase activity inhibitor comprising, as an active ingredient, a cyclic carboxamide derivative represented by formula (I): wherein n is an integer of 1 to 3, R1 is hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl, X is —CH2— or a group represented by —N(R2)—, and R2 is hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl, or a salt thereof.Type: ApplicationFiled: September 29, 2010Publication date: July 19, 2012Inventors: Shunsuke Iriyama, Hirotada Fukunishi, Masaru Suetsugu, Satoshi Amano
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Publication number: 20120177656Abstract: Methods for regulating the formation of a sulfilimine crosslink in a subject by administering a sulfilimine crosslink modulator are disclosed The sulfilimine modulator may inhibit or create a sulfilimine crosslink and maybe useful for treating a disease, such as cancer The sulfilimine crosslink may be between two or more peptidesType: ApplicationFiled: June 11, 2010Publication date: July 12, 2012Inventors: Billy G. Hudson, Roberto Vanacore, Gautam Bhave, Vadim Pedchenko
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Patent number: 8217063Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 15, 2008Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Patent number: 8217069Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: GrantFiled: April 16, 2008Date of Patent: July 10, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Publication number: 20120165380Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, acute, neuropathic and chronic.Type: ApplicationFiled: October 17, 2011Publication date: June 28, 2012Applicant: ALLERGAN, INC.Inventors: Daniel W. Gil, John E. Donello, Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha
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Publication number: 20120156244Abstract: Pharmaceutical compositions for the treatment of nasal congestion, wherein the pharmaceutical compositions comprise low concentrations of a super-selective subclass of selective ?-2 adrenergic receptor agonists. Methods of using the compositions for the treatment of nasal congestion, cerebrovascular disease or systemic conditions, and as delivery vehicles to deliver other active agents to treat systemic or cerebrovascular diseases or conditions.Type: ApplicationFiled: February 27, 2012Publication date: June 21, 2012Applicant: ALPHA SYNERGY DEVELOPMENT INC.Inventor: Gerald Horn
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Publication number: 20120156259Abstract: The present invention relates to biodegradable polyethylene glycol based water-insoluble hydrogels comprising backbone moieties which are interconnected by hydrolytically degradable bonds, the backbone moieties further comprising reactive functional groups, wherein the water-insoluble hydrogel is further characterized in that the ratio between the time period for the complete degradation of the hydrogel by hydrolysis of the degradable bonds into water-soluble degradation products comprising one or more backbone moieties and the time period for the release of the first 10 mol-% of water-soluble degradation products comprising one or more backbone moieties based on the total amount of backbone moieties in the hydrogel is greater than 1 and equal to or less than 2. The invention further relates to conjugates of such hydrogels with ligands or ligating groups, prodrugs and pharmaceutical compositions as well as their use in a medicament.Type: ApplicationFiled: July 30, 2010Publication date: June 21, 2012Applicant: ASCENDIS PHARMA A/SInventors: Harald Rau, Ulrich Hersel, Mathias Krusch, Dirk Vetter, Tobias Voigt
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Patent number: 8202895Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 18, 2010Date of Patent: June 19, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiβ, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
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Publication number: 20120149702Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Publication number: 20120141391Abstract: The present invention relates to the use of creatine compounds such as, for example, creatine, creatine phosphate or analogs of creatine, such as creatine-pyruvate, creatine-ascorbate, cyclocreatine, 3 guanidinopropionic acid, guanidinoacetate, homocyclocreatine, guanidino benzoates as energy generating systems and antioxidants for preservation of skin against adverse aging effects and damage secondary to insults such as harmful sun radiations, stress and fatigue. The creatine compounds which can be used in the present method include (1) creatine, creatine phosphate and analogs of these compounds which can act as substrates or substrate analogs for creatine kinase; (2) molecules that mimic the biological activity of creatine (3) molecules that modulate the creatine kinase system.Type: ApplicationFiled: June 29, 2011Publication date: June 7, 2012Applicant: AVICENA GROUP, INC.Inventor: Rima Kaddurah-Daouk
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Publication number: 20120141611Abstract: In one embodiment, a composition containing ergothioneine and/or synthesized l-ergothioneine and one or more compounds selected from the group consisting of vitamin B-12, glucosamine sulfate, calcium ascorbate, turmeric extract, black pepper extract, hyaluronic acid, collagen, glycosaminoglycans, cat's claw extract, acai berry; and white willow bark extract is provided to a mammal to improve a variety of health related factors, including but not limited to brain health, joint health, eye health, mitondchorial optimization/improvement and reduction of inflammation and pain in a mammal.Type: ApplicationFiled: December 5, 2011Publication date: June 7, 2012Inventors: Bernard Martin Landes, Michael A. Finamore
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Patent number: 8193227Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: December 10, 2004Date of Patent: June 5, 2012Assignee: Abbott LaboratoriesInventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20120136035Abstract: Disclosed herein is 4-(1-(3-(hydroxymethyl)-2-methylphenyl)ethyl)-1H-imidazole-2(3H)-thione and methods of using the compound to treat chronic pain.Type: ApplicationFiled: February 12, 2010Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventor: Daniel W. Gil
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Patent number: 8178571Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are used to activate alpha2 adrenergic receptors. The compounds of Formula 1 are incorporated in pharmaceutical compositions and are used as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors.Type: GrantFiled: August 3, 2010Date of Patent: May 15, 2012Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael Garst, Larry A. Wheeler, John R. Cappiello
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Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20120093947Abstract: A method of treating a reactive airway disease in a subject comprising administering at least one peroxidase inhibitor in association with administration of at least one ?-agonist.Type: ApplicationFiled: March 1, 2010Publication date: April 19, 2012Applicants: UNITED STATES DEPARTMENT OF VETERANS AFFAIRS, UNIVERSITY OF CINCINNATIInventors: Bradley E. Britigan, Krzysztof J. Reszka, Dennis W. McGraw
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Publication number: 20120088665Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) sulfur-containing triazole compounds I as described in the application, and 2) a fungicidal compound II, where the compounds II of component 2 are selected from among the compounds described in the application, and to the use of the fungicidal mixtures for controlling phytopathogenic fungi and to compositions comprising them.Type: ApplicationFiled: June 11, 2010Publication date: April 12, 2012Applicant: BASF SEInventors: Jochen Dietz, Thomas Grote, Egon Haden, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Wassilios Grammenos
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Publication number: 20120083443Abstract: The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCS treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCS. Likewise, RBCS of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCS. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release RBCS. Thus the invention is directed to compositions and methods for improving ATP release by RBCS, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.Type: ApplicationFiled: November 22, 2011Publication date: April 5, 2012Applicant: SAINT LOUIS UNIVERSITYInventors: Randy S. Sprague, Madelyn Stumpf
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Publication number: 20120083501Abstract: The invention provides novel tricyclic compounds of Formula I? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.Type: ApplicationFiled: September 23, 2011Publication date: April 5, 2012Inventors: Kevin W. Hunt, Tony P. Tang, Allen A. Thomas
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Publication number: 20120083500Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Li CHEN, Michael Patrick DILLON, Lichun FENG, Minmin YANG
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Patent number: 8129423Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: October 12, 2007Date of Patent: March 6, 2012Assignee: Hoffman-La Roche Inc.Inventors: Jean Ackermann, Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart, Tadakatsu Takahashi
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Publication number: 20120040940Abstract: The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related peripheral neuropathies. More particularly, the invention relates to combined therapies for treating said disease by affecting simultaneously muscarinic receptor signaling and thyroid hormone pathway in a subject.Type: ApplicationFiled: June 17, 2009Publication date: February 16, 2012Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Nathalie Cholet
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Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
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Publication number: 20110301105Abstract: We have discovered that p63 inhibition results in increased cellular proliferation. We have also performed a screen for agents capable of increasing cellular proliferation, (e.g., of stem cells such as skin-derived precursors (SKPs)). The invention therefore invention provides compositions, methods, and kits for increasing proliferation of cells, using compounds that decrease p63 expression or activity or using the compounds described herein. The invention also features methods of using these compounds for increasing hair growth, improving skin health, or promoting skin repair in a subject.Type: ApplicationFiled: March 30, 2011Publication date: December 8, 2011Applicant: The Hospital for Sick ChildrenInventors: Freda Miller, David Kaplan, Kristen Smith, Maryline Paris, Sibel Naska
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Patent number: 8071635Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.Type: GrantFiled: February 16, 2008Date of Patent: December 6, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Patent number: 8063086Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.Type: GrantFiled: October 17, 2007Date of Patent: November 22, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Todd M. Heidelbaugh, Daniel W. Gil, Michael E. Garst, Larry A. Wheeler
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Patent number: 8063087Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.Type: GrantFiled: July 25, 2008Date of Patent: November 22, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gill, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
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Patent number: 8063088Abstract: The invention is concerned with novel imidazolidine derivatives of formula (I) wherein R1 to R3, A, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: June 4, 2009Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Publication number: 20110269717Abstract: The instant invention describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: November 30, 2010Publication date: November 3, 2011Applicant: BrainCells Inc.Inventors: Carrolee BARLOW, Todd A. Carter, Kai Treuner, Kym I. Lorrain, Corey R. Seehus