Plural Rings In Acid Moiety Patents (Class 560/27)
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Patent number: 8507715Abstract: An optically active ?-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which: nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL.Type: GrantFiled: June 22, 2011Date of Patent: August 13, 2013Assignee: National University Corporation Nagoya UniversityInventors: Kazuaki Ishihara, Manabu Hatano, Takahiro Horibe
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Publication number: 20130197234Abstract: The present invention relates to methods for producing an optically active amine compound via a highly enantioselective hydrogenation reaction of an imine compound, wherein the imine compound is hydrogenated using a ruthenium metal complex having high catalytic activity and represented by Formula (1) RuXYAB??(1) such as RuBr2[(S,S)-xylskewphos][(S,S)-dpen].Type: ApplicationFiled: February 1, 2013Publication date: August 1, 2013Applicants: National University Corporation Hokkaido University, Kanto Kagaku Kabushiki KaishaInventors: Kanto Kagaku Kabushiki Kaisha, National University Corporation Hokkaido University
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Patent number: 8492499Abstract: The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups with b) one or more compounds of the formula (I) Y—(XH)n??(I) with the proviso that at least 50% of the free isocyanate groups of component a) are reacted with the compounds of the formula (I) to give an intermediate which contains uretdione groups, and subsequently the intermediate is reacted with c) one or more compounds of the general formula (II) Z—NHRm??(II) with the proviso that all free NCO groups optionally still present and at least 20% of uretdione groups originally used are reacted with Z—(NHR)m. The invention further relates to the use of the addition compounds as dispersants and dispersion stabilizers, and to a process for preparing them.Type: GrantFiled: March 20, 2007Date of Patent: July 23, 2013Assignee: BYK-Chemie GmbHInventors: Karlheinz Haubennestel, Stefan Moessmer, Wolfgang Pritschins, Thomas Launag
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130184279Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.Type: ApplicationFiled: December 18, 2012Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130172295Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosedType: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130158275Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: August 22, 2011Publication date: June 20, 2013Applicant: NOVARTIS AGInventors: David Hook, Bernhard Riss, Jianguang Zhou, Yunzhong Li, Erhard Bappert
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Publication number: 20130158285Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: August 22, 2011Publication date: June 20, 2013Applicant: NOVARTIS AGInventors: David Hook, Jianguang Zhou, Yunzhong Li
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Publication number: 20130158261Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: TaiMed Biologics, Inc.Inventor: TaiMed Biologics, Inc.
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Publication number: 20130137720Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.Type: ApplicationFiled: November 30, 2012Publication date: May 30, 2013Applicant: The Regents of the University of Colorado, a body corporatedInventors: Xiang Wang, Wenqing Xu
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Patent number: 8450477Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.Type: GrantFiled: September 15, 2008Date of Patent: May 28, 2013Assignee: Basilea Pharmaceutica A.G.Inventors: Marc Muller, Xiaoping Wu, Lin Xu
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Patent number: 8449890Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-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: GrantFiled: February 16, 2012Date of Patent: May 28, 2013Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20130131164Abstract: The invention relates to retigabine with improved color quality, and to processes for preparing the same. In addition, the invention relates to a process for drying wet retigabine. Also, the invention relates to stabilized or substantially stabilized retigabine in solid state, or a mixture or pharmaceutical formulation comprising the same. Further, the invention also relates to an improved process for preparing retigabine.Type: ApplicationFiled: February 18, 2011Publication date: May 23, 2013Applicant: MEDICHEM, S.A.Inventors: Ernesto Duran Lopez, Jordi Bosch I Lladó, Judit Serra Miralles
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Publication number: 20130116318Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:Type: ApplicationFiled: December 1, 2010Publication date: May 9, 2013Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20130109751Abstract: The present invention relates to the use of LSD-1 enzyme inhibitors in the osteogenic differentiation of cells capable to differentiate into osteoblasts, especially mesenchymal stem cells, adult stem cells, and cells with osteogenic potentialType: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: MESOGENICS S.R.L.Inventor: MESOGENICS S.R.L.
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Publication number: 20130096092Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.Type: ApplicationFiled: June 10, 2011Publication date: April 18, 2013Applicants: Health and Human ServicesInventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8420850Abstract: The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.Type: GrantFiled: May 9, 2011Date of Patent: April 16, 2013Assignee: Iberhospitex, S.AInventors: Lluis Duocastella Codina, Maria Molina, Ofir Arad, Jose Ignacio Borrell Bilbao, David Sanchez Garcia, Sofia Henriette Petterson Salom
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Patent number: 8404885Abstract: A high adhesive acrylate monomer has a specific chemistry figure. This monomer may be easily prepared in a simplified way, and various linkers may be used between L-DOPA and an acrylate group attached to a tail of L-DOPA, so molecular weight and size of the entire material may be easily controlled. Also, various kinds of acrylate to be combined to a isocyanate compound used as a linker may be selected, so various molecules may be easily composed.Type: GrantFiled: December 3, 2008Date of Patent: March 26, 2013Assignee: LG Chem, Ltd.Inventors: Woo-Sung Kim, Jee-Seon Kim, Ja-Young Han
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Publication number: 20130066101Abstract: The invention relates to a process for producing a compound according to formula (i) or salt thereof, wherein R1 and R1? are independently hydrogen or an amine protecting group and R2 is a carboxyl group or an ester group, comprising reacting a compound according to formula (ii) or salt thereof, wherein R1, R1? and R2 are defined as above, with hydrogen in the presence of a transition metal catalyst and a chiral ligand, wherein the transition metal is selected from group 7, 8 or 9 of the periodic table. Furthermore, the invention relates to products obtainable by said process and to their use in the production of NEP inhibitors. Moreover, the invention relates to the use of transition metal catalyst in the preparation of NEP inhibitors or prodrugs thereof.Type: ApplicationFiled: October 26, 2012Publication date: March 14, 2013Applicant: NOVARTIS AGInventor: Novartis AG
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Publication number: 20130041173Abstract: Modified diamond particles for use in chromatography with a desired functional group at the diamond surface, formed from reaction of hydroxyl groups at diamond surfaces with a reactive molecule.Type: ApplicationFiled: June 18, 2012Publication date: February 14, 2013Inventors: Matthew R. Linford, David Scott Jensen, Landon Andrew Wiest
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Patent number: 8362300Abstract: The present invention provides addition compounds, which suitable as dispersants and as dispersion stabilizers, and to the salts of the said compounds. The invention further provides processes for preparing these addition compounds, to their use as dispersants and dispersion stabilizers for organic and inorganic pigments and also fillers in organic and aqueous systems, and to pulverous or fibrous solids coated with such dispersants and intended for incorporation into liquid systems.Type: GrantFiled: May 6, 2005Date of Patent: January 29, 2013Assignee: BYK-Chemie GmbHInventors: Wolfgang Pritschins, Udo Krappe, Karlheinz Haubennestel, Andrea Esser
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Publication number: 20120330038Abstract: A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds.Type: ApplicationFiled: March 8, 2011Publication date: December 27, 2012Applicants: API Corporation, National University Corporation TOHOKU UNIVERSITYInventors: Masahiro Terada, Norie Momiyama, Tohru Konno
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Publication number: 20120289710Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a g-amino-d-biphenyl-a-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: January 21, 2011Publication date: November 15, 2012Inventors: David Hook, Jianguang Zhou, Yunzhong Li
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Publication number: 20120238582Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER hAFTUNGInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Publication number: 20120225937Abstract: The present invention relates to salts of 2-(2-((4-(((4-chlorophenyl)(phenyl)-carbamoyloxy)methyl)cyclohexyl)methoxy)acetamido)ethanesulfonic acid (Compound 1) and crystalline forms, solvates and hydrates thereof. The present invention further relates to processes and intermediates useful in the preparation of Compound I and salts, solvates and hydrates thereof.Type: ApplicationFiled: September 21, 2010Publication date: September 6, 2012Applicant: Arena Pharmaceuticals, Inc.Inventors: Anthony C. Blackburn, Sagar Raj Shakya, John A. DeMattei, Tsung-Hsun Chuang
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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: 20120213807Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-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, Cameron Smith
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Publication number: 20120202854Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: April 17, 2012Publication date: August 9, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: George Doherty, Adam Cook
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Patent number: 8236983Abstract: The present invention includes methods of making and methods of using peptidomimetics compositions that mimic ?-helical BH3 sequences in cells. The peptidomimetics can be used to mimic ?-helical BH3 sequences and kill cancer cells.Type: GrantFiled: January 13, 2009Date of Patent: August 7, 2012Assignee: Board of Regents, The University of Texas SystemInventor: Jung-Mo Ahn
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Publication number: 20120189546Abstract: This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: July 9, 2010Publication date: July 26, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Keith Graham, Heribert Schmitt-Willich, Dominic Franck
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Publication number: 20120178957Abstract: The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin.Type: ApplicationFiled: September 25, 2010Publication date: July 12, 2012Inventors: Guoliang Zhu, Jian Zhang, Lljun Yang, Qingdan Yao, Jie Ying
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Patent number: 8217075Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkType: GrantFiled: January 27, 2009Date of Patent: July 10, 2012Assignee: OroxcellInventors: Jean Pachot, Christophe Dini, Alexis Denis
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Patent number: 8217050Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: GrantFiled: November 5, 2007Date of Patent: July 10, 2012Assignee: Chroma Therapeutics LimitedInventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
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Publication number: 20120172426Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.Type: ApplicationFiled: July 1, 2011Publication date: July 5, 2012Applicant: REVIVA PHARMACEUTICALS, INC.Inventors: Laxminarayan Bhat, Kouacou Adiey
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Publication number: 20120157386Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Cameron SMITH, Melissa FLEURY, Roland GENDRON, Ryan HUDSON, Adam D. HUGHES
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Publication number: 20120157383Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
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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: 20120142916Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: December 21, 2011Publication date: June 7, 2012Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murtidhar Waykole
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Patent number: 8173829Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.Type: GrantFiled: March 31, 2010Date of Patent: May 8, 2012Assignee: Sunovion Pharmaceuticals Inc.Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
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Patent number: 8158814Abstract: An object of the present invention is to provide insecticides having high effectiveness.Type: GrantFiled: August 23, 2004Date of Patent: April 17, 2012Assignee: Mitsui Chemicals, Inc.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara
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Patent number: 8148567Abstract: An object of the present invention is to provide a process for producing a urethane (meth)acrylate safely with good productivity, and for achieving the object, the invention provides a process for continuously producing a urethane (meth)acrylate, containing causing a mixed liquid of a compound (A) having a hydroxyl group and a (meth)acryloyl group and a compound (B) having an isocyanate group to pass continuously and densely through a tubular microchannel formed in a heat-conducting reaction device, and reacting the hydroxyl group of the compound (A) with the isocyanate group of the compound (B), in which the tubular microchannel in the reaction device has a space size making a fluid cross-sectional area, through which the mixed liquid passes densely, of from 0.1 to 4.0 mm2, and the process contains heating the heat-conducting reaction device to a temperature of from 100 to 250° C.Type: GrantFiled: March 12, 2009Date of Patent: April 3, 2012Assignee: DIC CorporationInventors: Fumihiko Ishiyama, Takeshi Hizawa, Hideki Watanabe
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Publication number: 20120059055Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 15, 2011Publication date: March 8, 2012Applicant: PANMIRA PHARMACEUTICALS, LLCInventors: John Howard HUTCHINSON, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang
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Publication number: 20120053238Abstract: The invention relates to solid retigabine in non-crystalline form together with a surface stabiliser in the form of a stable intermediate. In the intermediate of the invention, retigabine is preferably present in amorphous form or in the form of a solid solution. The invention further relates to processes for the production of retigabine in a solid, non-crystalline form and to pharmaceutical formulations containing solid, non-crystalline retigabine.Type: ApplicationFiled: March 17, 2010Publication date: March 1, 2012Applicant: ratiopharm GmbHInventors: Jana Paetz, Katrin Rimkus
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Publication number: 20120046255Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 14, 2008Publication date: February 23, 2012Applicant: THE UNIVERSITY OF MELBOURNE of ROYAL PARADE PARKVILLEInventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Tomasz Bilski
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Publication number: 20120024382Abstract: The invention relates to novel polyaromatic and polyheteroaromatic compounds and derivatives thereof. The compounds display high solubility in organic solvents. A further aspect of the invention relates to the use of the novel compounds in the fabrication of organic film based heterojunction devices. In one form the devices display high conversion efficiencies in solar cell applications.Type: ApplicationFiled: November 27, 2009Publication date: February 2, 2012Applicants: THE UNIVERSITY OF ULM, THE UNIVERSITY OF MELBOURNEInventors: Andrew Holmes, David Jones, Wing Ho Wallace Wong, Chang Qi Ma, Peter Baeuerle
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Publication number: 20120010403Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Inventor: Keigo TANAKA
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Publication number: 20120010401Abstract: An industrially advantageous method for producing a 1,5-benzodiazepine compound is provided. A compound (5) is obtained according to the reaction scheme shown below, and this compound is used as an intermediate.Type: ApplicationFiled: March 29, 2010Publication date: January 12, 2012Applicant: Zeria Pharmaceutical Co., Ltd.Inventor: Masaru Terauchi
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Patent number: 8053590Abstract: The invention relates to a method for producing enantiomers form of 2,3-diaminopropionic acid derivatives of formula (I) by asymmetric hydrogenation from compounds of formula (II).Type: GrantFiled: April 6, 2009Date of Patent: November 8, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joerg Rieke-Zapp, Guenter Billen