Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
August 26, 2010
Date of Patent:
September 30, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
Abstract: A phosphate-containing nanoparticle delivery vehicle includes nanoparticle, an active ingredient, and a phosphodiester moiety connecting the nanoparticle and the active ingredient and forms a prodrug. The nanoparticle delivery vehicle achieves the function of increasing hydrophilicity of the active ingredient and specificity against tumor cells. Advantages of the nanoparticle material include biocompatibility, magnetism and/or controllable drug release.
Type:
Grant
Filed:
July 13, 2012
Date of Patent:
September 30, 2014
Assignee:
National Cheng-Kung University
Inventors:
Jih Ru Hwu, Yu-Sern Lin, Chen-Sheng Yeh, Dar-Bin Shieh, Wu-Chou Su
Abstract: The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
Abstract: The present invention relates to a process for the preparation of carbapenem compound of Formula (I), wherein P1 is hydrogen or a carboxyl protecting group, P3 is hydrogen or a hydroxyl protecting group, R1 is C1-3 alkyl, and A is selected from a group consisting of a) Formula (II), b) Formula (III), c) Formula (IV), d) Formula (V), e) Formula (VI), f) Formula (VII), wherein P2 is hydrogen or an amino protecting group, R2 and R3 may be same or different and are hydrogen, C1-5 alkyl, optionally substituted aryl, or optionally substituted heteroaryl, and X1 is O or S, or its stereoisomers, or salts thereof.
Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Type:
Grant
Filed:
February 26, 2008
Date of Patent:
September 16, 2014
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
Abstract: This invention belongs to the chemical-pharmaceutical field. New compounds of pterocarpanquinone family presented in formula (I) according to this invention are capable to be activated by reduction generating alkylating species intracellularly. It presents selective cytotoxic effects particularly on mammalian human and nonhuman cells that divide constantly and are useful in treating diseases and dysfunctions related to the phenomenon of undesired cell proliferation. Such compounds are also effective for the treatment of diseases or dysfunctions related to high levels of TNF-? in human and nonhuman mammals.
Type:
Grant
Filed:
November 5, 2009
Date of Patent:
September 16, 2014
Assignee:
Universidade Federal Do Rio de Janeiro
Inventors:
Alcides Jose Monteiro Da Silva, Vivian Mary Barral Dold Rumjanek, Bartira Rossi Bergmann, Eduardo Salustiano Jesus Dos Santos, Paulo Roberto Ribeiro Costa, Chaquip Daher Netto, Wallace Pacienza Lima, Eduardo Caio Torres Dos Santos, Moises Clemente Marinho Cavalcante, Sergio Henrique Seabra, Ingred Goretti Rica
Abstract: The present invention relates to a type of norcantharidin analogues and a method to synthesis such norcantharidin analogues by transition metal-catalyzed alkynylation of 7-oxabenzonorbornadienes. The present invention also relates to the use of such norcantharidin analogues in manufacture of a medicament for the treatment of cancer tumors.
Type:
Grant
Filed:
December 28, 2012
Date of Patent:
September 16, 2014
Assignees:
Hong Kong Baptist University, Yunnan University of Nationalities
Inventors:
Albert Sun-Chi Chan, Baomin Fan, Jun Wang, Chengyuan Lin, Chao Huang, Qingjing Yang, Jianbin Xu, Zhaoxiang Bian, Aiping Lu, Jun Hu
Abstract: The present invention relates to a process for the preparation of olopatadine and, more particularly, to an improved method of synthesizing olopatadine which comprises reacting a dibenz[b,e]oxepin-11-one derivative of formula (III) and a suitable reagent under Witting condition, and to the intermediate 11-[(Z)-3-(dimethylamino)-propylidene]-6-11-dihydrodibenz[b,e]-oxepin-2-acet-amide p-toluensulfonate salt.
Type:
Grant
Filed:
February 1, 2010
Date of Patent:
September 16, 2014
Assignee:
Zach System S.p.A
Inventors:
Alberto Guidi, Filippo Chiarello, Gianmauro Orru', Massimo Verzini, Livius Cotarca, Jean-Claude Kizirian, Elisenda Trepat Guixer, Francisco Marquillas Olondriz
Abstract: A phosphate-containing nanoparticle delivery vehicle includes a nanoparticle, an active ingredient, and a phosphodiester moiety connecting the nanoparticle and the active ingredient and forms a prodrug. The nanoparticle delivery vehicle achieves the function of increasing hydrophilicity of the active ingredient and specificity against tumor cells. Advantages of the nanoparticle material include biocompatibility, magnetism and/or controllable drug release.
Type:
Grant
Filed:
July 13, 2012
Date of Patent:
September 9, 2014
Assignee:
National Cheng-Kung University
Inventors:
Jih Ru Hwu, Yu-Sern Lin, Chen-Sheng Yeh, Dar-Bin Shieh, Wu-Chou Su
Abstract: A process for making a cyclic compounds such as cyclic acetal or cyclic ketones by feeding aldehyde or ketone compounds and polyhydroxyl compounds to a reaction zone at a molar ratio of polyhydroxyl compounds to aldehyde or ketone compounds of at least 3:1, reacting these compounds in the presence of a solid acid such as an acidic ion exchange resin, to generate a liquid reaction mixture without separating water from the reaction mixture as it is being formed in the reaction mixture, withdrawing the liquid reaction mixture from the reaction zone as a liquid product stream, and feeding the liquid reaction product stream to a distillation column to separate cyclic acetal compounds from unreacted polyhydroxyl compounds, and optionally recycling back the unreacted polyhydroxyl compounds to the reaction zone. The process produces cyclic acetal compounds in yields of at least 90% with long catalyst life. The process is also suitable to make cyclic ketals from ketone compounds.
Type:
Grant
Filed:
June 24, 2011
Date of Patent:
September 9, 2014
Assignee:
Eastman Chemical Company
Inventors:
Daniel Latham Terrill, Brian David McMurray, Damon Ray Billodeaux, James Lon Little, Adam Scott Howard
Abstract: A method of modulating the flavor of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavor-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.
Type:
Grant
Filed:
June 24, 2010
Date of Patent:
August 26, 2014
Assignee:
Givaudan S.A.
Inventors:
Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
Abstract: The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents C1-4 alkyl-, C1-4 alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
Abstract: Disclosed is a method of producing an optically active fluorinated oxetane, which can be an important pharmaceutical or agricultural intermediate, by reaction of a fluorinated ?-keto ester with an acyl alkenyl ether in the presence of a transition metal complex with an optically active ligand. This method utilizes a catalytic asymmetric synthesis process and does not require a stoichiometric amount of chiral source. It is thus possible to dramatically reduce the amount of use of the asymmetric catalyst especially when the reaction is performed at a high concentration of substrate (with the use of a small amount of reaction solvent) or in the absence of a reaction solvent (under neat conditions). Further, the target optically active fluorinated oxetane can be obtained with high yield and with very high optical purity. The product contains almost no difficult-to-separate impurity and shows high chemical purity.
Type:
Grant
Filed:
February 22, 2010
Date of Patent:
August 19, 2014
Assignees:
Central Glass Company, Limited, Tokyo Institute of Technology
Abstract: A method for industrially preparing a nitrogen substituted 6-amino-5,6,7,8-tetrahydronaphthol includes reacting a nitrogen substituted amino-5,6,7,8-tetrahydronaphthol compound of formula (II) with a 2-substituted ethyl sulfonate compound of formula (III) under an alkaline condition and in the presence of a sulfite.
Type:
Grant
Filed:
June 21, 2012
Date of Patent:
August 19, 2014
Assignee:
Shan Dong Luye Pharmaceutical Co., Ltd.
Inventors:
Qingguo Meng, Mina Yang, Tao Wang, Qilin Wang, Jun Li, Zheng Ruan
Abstract: The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.
Type:
Grant
Filed:
June 13, 2011
Date of Patent:
August 19, 2014
Assignee:
Dipharma Francis S.r.l.
Inventors:
Emanuele Attolino, Mario Michieletti, Davide Rossi, Pietro Allegrini
Abstract: The invention relates to a process for the manufacture of epichlorohydrin (“ECH”) by catalytic oxidation of allyl chloride (“AC”) with an oxidant wherein the catalytic oxidation is performed in an aqueous reaction medium, wherein a water-soluble manganese complex is used as oxidation catalyst, followed by the isolation of epichlorohydrin.
Abstract: The present invention relates to a process of preparing a taxoid (X) by reacting a protected baccatin derivative (B) with a ?-lactam (C) in the presence of one or more Lewis acids and a base agent. The present invention also relates to a process of preparing the protected baccatin derivative (B) from a baccatin derivative (A) comprising a protection reaction catalyzed by one or more Lewis acids with an optional base agent.
Abstract: The invention provides novel derivatives of cyclopamine having the following formula:
Type:
Grant
Filed:
August 27, 2008
Date of Patent:
July 22, 2014
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
Type:
Grant
Filed:
June 28, 2011
Date of Patent:
July 22, 2014
Assignee:
GFV, LLC
Inventors:
John K. Thottathil, Raymond P. Warrell, Jr.