Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/245)
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Patent number: 8513162Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.Type: GrantFiled: December 24, 2009Date of Patent: August 20, 2013Assignee: Sumitomo Chemical Company, LimitedInventor: Hiromasa Mitsudera
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Publication number: 20130203738Abstract: The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g.Type: ApplicationFiled: February 9, 2011Publication date: August 8, 2013Applicants: NAGOYA CITY UNIVERSITY, NAGASAKI UNIVERSITYInventors: Yoshifumi Nishimura, Aritaka Nagadoi, Yuuka Hirao, Yoshio Goshima, Naoya Yamashita, Naoki Miyata, Takayoshi Suzuki, Ryuta Hiraishi, Hiroshi Ueda
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Patent number: 8501775Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).Type: GrantFiled: May 9, 2008Date of Patent: August 6, 2013Assignee: SALTIGO GmbHInventors: Achim Harder, Georg von Samson-Himmlstjerna, Bernd-Wieland Kruger, Heinz Melhorn, Jurgen Schmidt
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Publication number: 20130178457Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).Type: ApplicationFiled: July 5, 2012Publication date: July 11, 2013Applicant: LUPIN LIMITEDInventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Patent number: 8481541Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: March 3, 2011Date of Patent: July 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
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Publication number: 20130172385Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).Type: ApplicationFiled: May 9, 2008Publication date: July 4, 2013Applicant: LANXESS DEUTSCHLAND GMBHInventors: Achim Harder, Georg von Samson-Himmlstjerna, Bernd-Wieland Kruger, Heinz Mehlhorn, Jurgen Schmidt
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Publication number: 20130165658Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.Type: ApplicationFiled: June 9, 2011Publication date: June 27, 2013Inventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
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Publication number: 20130144057Abstract: (Meth)acrylic acid ester, which contains one or more partial structures each represented by the following formula 1 in a molecule thereof, wherein the partial structure is a urethane structure which does not have a hydrogen atom directly bonded to a nitrogen atom of the following formula 1: where the nitrogen atom is not bonded to a hydrogen atom.Type: ApplicationFiled: November 28, 2012Publication date: June 6, 2013Inventor: Mitsunobu MORITA
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Publication number: 20130116192Abstract: N-(aminoacyl)-amino compound, represented by the following formula Wherein R1 denotes hydrogen, low alkyl or carbonyl, and N1 denotes an NH group and R2 denotes hydrogen or low alkylphenyl or aralkyl or imidazoalkyl or indolylalkyl, R1 and R2 together may complete a pyrrolidine or piperidine or thiazolidine ring and R3 denotes hydrogen or methyl or low alkyl and R4 denotes hydrogen or alkyl or the group remaining on exclusion of R4 from the formula and Z is a straight chain or branched alkylene, which may contain up to 3 carbon atoms. and R5 is nitrogen or sulphur or oxygen or salts thereof and ester compounds, characterised in that A is an ester or amino acid or alternatively sodium or a potassium salt of arginate and/or of ornithate and/or of aspharaginate.Type: ApplicationFiled: March 30, 2011Publication date: May 9, 2013Inventor: Gosbert Weth
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Publication number: 20130095376Abstract: An electrode active material for a secondary battery includes a radical compound represented by formula (1): (wherein at least one of R1 to R6 is a protic hydrophilic group); and an alkali metal or an alkaline earth metal.Type: ApplicationFiled: October 15, 2012Publication date: April 18, 2013Applicant: CANON KABUSHIKI KAISHAInventor: CANON KABUSHIKI KAISHA
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Patent number: 8404689Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: GrantFiled: March 2, 2011Date of Patent: March 26, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Patent number: 8404719Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: December 12, 2011Date of Patent: March 26, 2013Assignee: AbbVie Inc.Inventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
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Patent number: 8394801Abstract: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.Type: GrantFiled: March 25, 2010Date of Patent: March 12, 2013Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Tilmann Schuster, Emmanuel Polymeropoulos, Michael Czech, Eckhard Claus
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Publication number: 20130012699Abstract: The present invention relates to a carbon dioxide absorbent, an ionic liquid obtained by reacting amide and an organic acid and a method of using the same. The amidium-based ionic liquid of the present invention has excellent CO2 absorption capability, which is hardly reduced even with repeated use, is easy to synthesize and has low manufacturing cost thus being useful as a CO2 absorbent.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicants: Kia Motors Corporation, Hyundai Motor CompanyInventors: Seok Jin Choi, Jelliarko Palgunadi, Je Eun Kang, Hoon Sik Kim, Sung Yeup Chung
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Patent number: 8349923Abstract: The present invention relates to a novel method of flame retarding a polymeric substrate by adding a small but efficient amount of a synergistic mixture of at least one sterically hindered N-alkoxyamine (NOR), at least a metal salt of hypophosphorous (phosphinic) acid and at least one organo-halogen flame retardant. A further aspect of the invention is the flame retardant composition itself and together with a polymer. The present invention also relates to polymeric articles (e.g. moldings, films, fibers, etc.) that are stabilized against light, heat and oxygen and made flame retardant by incorporation of at least one sterically hindered N-alkoxy amine, at least a metal salt of hypophosphorous acid (phosphinic acid) and at least one organo-halogen flame retardant.Type: GrantFiled: December 12, 2008Date of Patent: January 8, 2013Assignee: BASF SEInventor: Michael Roth
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Patent number: 8343968Abstract: The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: GrantFiled: May 23, 2008Date of Patent: January 1, 2013Assignee: Merck Canada Inc.Inventors: Tom Yao-Hsiang Wu, Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Erich I. Grimm, Sebastien Laliberte, Austin Chen
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Patent number: 8338142Abstract: The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.Type: GrantFiled: February 18, 2008Date of Patent: December 25, 2012Assignee: Kaneka CorporationInventors: Kohei Mori, Masutoshi Nojiri, Akira Nishiyama, Naoaki Taoka
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Patent number: 8309596Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 8309579Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 28, 2011Date of Patent: November 13, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Jerome Gonzalez
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Patent number: 8309553Abstract: The invention relates to anhydrous crystalline orvepitant maleate (Form 1), pharmaceutical formulations comprising the same, its use in therapy and processes for preparing the same, wherein orvepitant is as shown in formula (I).Type: GrantFiled: April 9, 2009Date of Patent: November 13, 2012Assignee: Glaxo Group LimitedInventors: Stefania Beato, Franco Sartor, Ian Philip Steeples
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Publication number: 20120264941Abstract: The present invention concerns a method for the synthesis of glycerol dithiocarbamates or bis-dithiocarbamates (GDTCs) in which a reaction medium comprising (1) a carbonate selected from diethyl carbonate, dimethyl carbonate and ethylene or propylene carbonate associated with a glycerol type polyol in the presence of a basic catalyst or (2) a cyclic carbonate comprising five ring members, in a solvent medium, is supplemented with a primary or secondary amine in the presence of carbon disulphide, and the GDTC formed is recovered. In particular, a glycerol type polyol is brought into the presence of diethyl carbonate in the presence of a catalyst, then a primary or secondary amine is added to the reaction medium in the presence of carbon disulphide, and the GDTC formed is recovered. The invention can be used for one-step synthesis of glycerol dithiocarbamates directly from glycerol as the starting material and solvent.Type: ApplicationFiled: December 21, 2010Publication date: October 18, 2012Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Francois Jerome, Rodolphe De Sousa, Joel Barrault, Yannick Pouilloux
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Patent number: 8283383Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 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: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Patent number: 8283466Abstract: Catalytic processes for preparing caprolactam, pipecolinic acid, and their derivatives, from lysine or alpha-amino-epsilon-caprolactam starting materials, and products produced thereby. A process for preparing caprolactam or a derivative thereof, the process comprising contacting a reactant comprising lysine or alpha aminocaprolactam with a catalyst and a gas comprising hydrogen gas, in the presence of a solvent. The catalyst may be provided on a support material, such as a transition metal.Type: GrantFiled: February 20, 2008Date of Patent: October 9, 2012Assignee: Board of Trustees of Michigan State UniversityInventor: John W. Frost
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Publication number: 20120228151Abstract: An extraction component enabling the concurrent recovery of gold and/or palladium selectively from a hydrochloric acid media containing the base metals and other contaminants. The disclosed extractant disclosed eliminates the conventional multi-step process for such extraction by providing for an extraction method which uses a single solvent extraction reagent. Further enhancing the conventional multi step process, the conventional scrubbing stage is eliminated by a single stripping stage. The resulting solutions can be obtained from leaching many types of material such as copper anode slimes, the treatment of scrap such as electronic circuit boards and plating effluents, PGM, or refractory gold ores.Type: ApplicationFiled: March 7, 2011Publication date: September 13, 2012Inventors: Loghman Moradi, Hiwa Salimi, Mohammad Piltan, Issa Yavari
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Patent number: 8258156Abstract: The invention provides compounds, 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: GrantFiled: May 23, 2011Date of Patent: September 4, 2012Assignee: IRM LLCInventors: Phillip B. Alper, Mihai Azimioara, Christopher N. Cow, Robert Epple, Pierre-Yves Michellys, Victor Nikulin
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Publication number: 20120220577Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: ApplicationFiled: June 4, 2010Publication date: August 30, 2012Inventors: Markus Henrich, Angela Hansen, Jens Nagel, Valerjans Kauss, Jevgenijs Rozhkovs, Ginta Grunsteine, Dina Trifanova
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Publication number: 20120214996Abstract: Dibenzylidene and heterobenzylideneacetone derivatives, related 4-piperidones, related 4-thiopyranones and the corresponding sulfinyl- and sulfonyl-analogues for their use for prophylaxis or treatment of trypanosomiasis and leishmaniasis.Type: ApplicationFiled: September 20, 2010Publication date: August 23, 2012Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Elisabeth Davioud-Charvet, Ingrid Nicole Wenzel, Thomas J.J. Muller, Gilles Hanquet, Don Antoine Lanfranchi, Frederic Leroux, Thibault Gendron
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Publication number: 20120184438Abstract: This invention relates to agrochemical compositions comprising a benzamide compound of formula (I) where R1 is fluoro, methoxy or C1-4 alkyl; R2 and R3 are each independently optionally substituted C1-6 alkyl or optionally substituted C2-6 alkenyl; or R3 is hydrogen and R3 is optionally substituted C5-8 alkyl or optionally substituted C4-6 alkenyl or optionally substituted benzyl; or R2 and R3 and the nitrogen atom to which they are both attached together form an optionally substituted 5-, 6- or 7-membered ring, which ring optionally contains at least one further heteroatom selected from O, N and S; to the use of those benzamide compounds as solvents; to certain novel compounds of formula (I); and to a process for preparing those novel compounds.Type: ApplicationFiled: July 15, 2010Publication date: July 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Gordon Alistair Bell, David Stock, Jeffrey Steven Wailes
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Publication number: 20120178732Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 6, 2011Publication date: July 12, 2012Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120148952Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.Type: ApplicationFiled: January 17, 2012Publication date: June 14, 2012Applicant: JSR CorporationInventors: Kazuo NAKAHARA, Mitsuo SATO
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Publication number: 20120149860Abstract: A compound represented by the following formula (a): CH2?CR1—CONJ-CKR2—(CH2)n—COO-Q1-Rf1??(a) is provided. This compound is capable of forming a polymer having an oil repellency equivalent to polymers containing a polyfluoroalkyl group containing at least 8 carbon atoms, although the polyfluoroalkyl group contains up to 6 carbon atoms. In the formula, R1 is hydrogen atom or methyl group, R2 is hydrogen atom or a group represented by —(CH2)m—COO-Q2-Rf2 (r), n and m are independently an integer of 0 to 4, Rf1 and Rf2 are independently a polyfluoroalkyl group or a polyfluoroether group containing 1 to 6 carbon atoms, Q1 and Q2 are independently single bond or a divalent linkage group, J is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, K is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, and j and k are independently single bond or an alkylene group containing 1 to 3 carbon atoms with the proviso that j and k are not simultaneously single bond.Type: ApplicationFiled: August 17, 2010Publication date: June 14, 2012Applicant: AGC SEIMI CHEMICAL CO.,LTD.Inventors: Fusae Ishiwata, Ryo Hirabayashi, Hirotaka Shimizu
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Patent number: 8188290Abstract: The present invention relates to a new and useful process for preparing N,N-substituted carbamoyl halides from secondary amines, carbon dioxide, trialkylsilyl chloride and a halogenating agent.Type: GrantFiled: October 26, 2006Date of Patent: May 29, 2012Assignee: Glaxo Group LimitedInventors: Ilaria Bientinesi, Zadeo Cimarosti, Giuseppe Guercio, Corinne Leroi, Alcide Perboni
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Patent number: 8188289Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.Type: GrantFiled: March 13, 2007Date of Patent: May 29, 2012Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless
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Patent number: 8183255Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: February 4, 2008Date of Patent: May 22, 2012Assignee: Pfizer, Inc.Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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Publication number: 20120123128Abstract: Optically active nipecotamide can be produced by a method for producing optically active nipecotamide comprising: a step of reacting nipecotamide with optically active lactic acid to prepare a mixture of diastereomer salts and then allowing one diastereomer salt in the mixture of the diastereomer salts to precipitate; a step of collecting the precipitated diastereomer salt; and, a step of treating the collected diastereomer salt with a base to cause optically active nipecotamide to release.Type: ApplicationFiled: July 7, 2010Publication date: May 17, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yosuke Watanabe, Yutaka Ohtani
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Publication number: 20120101039Abstract: A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: April 26, 2012Applicant: LEO PHARMA A/SInventors: Jef Fenscholdt, Thomas Høyer, Xifu Liang, Sophie Elisabeth Havez
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Patent number: 8163926Abstract: The present invention relates to a process for the manufacture of a compound of the Formula IIa: wherein R is a suitable sulphonate ester; from a (C1-C6)alkyl-4-piperidinecarboxylate compound of the Formula III:Type: GrantFiled: September 27, 2006Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Jorgen Blixt, Michael David Golden, Philip John Hogan, David Michael Glanville Martin, Francis Joseph Montgomery, Zakariya Patel, John David Pittam, George Joseph Sependa, Christopher John Squire, Nicholas Cartwright Alexander Wright
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Patent number: 8163898Abstract: [PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.Type: GrantFiled: September 12, 2008Date of Patent: April 24, 2012Assignee: MSD K. K.Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
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Publication number: 20120083509Abstract: What are described are insect- and mite-repellent compositions comprising at least 2 enantiomers selected from the group of 1-[(S)-sec-butyloxycarbonyl]-2-(S)-(2-hydroxyethyl)piperidine (referred to hereinafter as S,S), 1-[(R)-sec-butyloxycarbonyl]-2-(R)-(+)-(2-hydroxyethyl) piperidine (referred to hereinafter as R,R), 1-[(S)-sec-butoxycarbonyl]-2-(R)-(+)-(2-hydroxyethyl) piperidine (referred to hereinafter as S,R), 1-[(R)-sec-butyloxycarbonyl]-2-(S)-(+)-(2-hydroxyethyl) piperidine (referred to hereinafter as R,S), excluding the racemate mixture thereof, a process for preparation thereof and the use thereof in insect- and mite-repellent formulations.Type: ApplicationFiled: June 8, 2011Publication date: April 5, 2012Applicant: SALTIGO GMBHInventors: Burkhard KOCH, Andreas JOB, Nikolaus Müller
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Publication number: 20120077711Abstract: The present invention provides compounds and libraries of compounds having formula (I): wherein L, n, S and A are defined generally and subsets herein. These compounds and libraries of compounds are useful generally in the drug discovery process.Type: ApplicationFiled: May 26, 2011Publication date: March 29, 2012Applicant: SUNESIS PHARMACEUTICALS, INC.Inventors: Andrew C. Braisted, Daniel A. Erlanson, Jeffrey W. Jacobs
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Publication number: 20120065230Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: March 21, 2011Publication date: March 15, 2012Applicant: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Patent number: 8129384Abstract: This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals.Type: GrantFiled: October 9, 2009Date of Patent: March 6, 2012Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, David Amantini, Sandro Belvedere
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Publication number: 20120046317Abstract: The present invention relates to a new class of heterocyclic compounds and pharmaceutically acceptable salts thereof, process for preparing the same, pharmaceutical composition containing these compounds and to their use in treatment of diseases caused due to formation and accumulation of AGEs (Advanced Glycation end products). The compounds of the present invention are useful for the treatment of diabetic and aging-related complications caused by formation and accumulation of AGEs, such as neuropathy, nephropathy, microangiopathy, retinopathy, hypertension, heart failure, atherosclerosis, Alzheimer's disease & dermatological disorders.Type: ApplicationFiled: May 6, 2010Publication date: February 23, 2012Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ramesh Chandra Gupta, Manish Patel, Jignesh Kotecha, Sachin Latad, Jaya Abraham, Sanjay Srivastava, Milin Rode, Shailesh Deshpande, Anita Chaudhary, Amit Kumar Kesarwani
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Publication number: 20120041025Abstract: Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.Type: ApplicationFiled: February 19, 2010Publication date: February 16, 2012Inventor: Sampath Parthasarathy
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Publication number: 20120029021Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: January 17, 2011Publication date: February 2, 2012Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITYInventors: Yong Ba, Errol V. Mathias
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Patent number: 8071604Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: November 8, 2007Date of Patent: December 6, 2011Assignees: Cephalon France, Cephalon, Inc.Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110275612Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.Type: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
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Patent number: 8053438Abstract: Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: November 16, 2009Date of Patent: November 8, 2011Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz