Oxy In Acid Moiety Patents (Class 560/53)
  • Patent number: 11135318
    Abstract: Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: October 5, 2021
    Assignee: The General Hospital Corporation
    Inventors: Chongzhao Ran, Anna Moore, Jian Yang
  • Patent number: 9598338
    Abstract: The subject invention pertains to myricanol derivatives, therapeutic compositions, and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau.
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: March 21, 2017
    Assignees: UNIVERSITY OF SOUTH FLORIDA, THE DEPARTMENT OF VETERANS AFFAIRS
    Inventors: Chad Dickey, Umesh Jinwal, Laurent Calcul, Bill J. Baker, Matthew Lebar
  • Patent number: 9399635
    Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: July 26, 2016
    Assignee: GREEN TECH CO., LTD.
    Inventors: Hachiro Sugimoto, Michiaki Okuda, Takashi Takahashi, Ichiro Hijikuro, Hidetaka Suzuki, Shinichi Nakayama
  • Publication number: 20150119576
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Manabu YAOSAKA, Tomohisa UTSUNOMIYA, Yuji MORIYAMA, Tomohiro MATSUMOTO, Kazutaka MATOBA
  • Publication number: 20150087705
    Abstract: Disclosed herein are compounds, compositions and methods for preventing and treating diseases such as intracerebral hemorrhage, cancer, or conditions associated with damaged cells, activated lymphocytes, or microbial products. The disclosed compounds are curcumin analogs. The curcumin analogs possess anti-inflammatory and antioxidant properties, which in part, reduce AP-1 and NF-?B activity.
    Type: Application
    Filed: September 22, 2014
    Publication date: March 26, 2015
    Inventors: Cargill H. Alleyne, JR., Krishnan M. Dhandapani, Ken Wen, MingLiang Ma, WenJing Hu
  • Patent number: 8975434
    Abstract: In order to provide a novel method for producing a cyclopentanone compound, the present invention is a method for producing a cyclopentanone compound represented by the formula (I). The method includes the steps of: substituting the group represented by Y by a hydrogen atom by allowing a compound represented by the formula (III) or an intermediate compound obtained from the compound represented by the formula (III) to react with a catalyst or a halogenating agent; and substituting, by hydrogen atoms, (i) the group or the atom represented by Z1 and (ii) the group or the atom represented by Z2, by reducing the compound represented by the formula (III) or the intermediate compound obtained from the compound represented by the formula (III).
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: March 10, 2015
    Assignee: Kureha Corporation
    Inventor: Hisashi Kanno
  • Publication number: 20150051410
    Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 19, 2015
    Applicant: CHIROGATE INTERNATIONAL INC.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
  • Publication number: 20150025255
    Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 22, 2015
    Applicant: Lung Biotechnology Inc.
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
  • Patent number: 8895624
    Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: November 25, 2014
    Assignee: Haoma Medica Ltd.
    Inventors: Stephen Hodges, Robin Soper
  • Publication number: 20140323664
    Abstract: Substituted phenacyl molecules are provided and employed to create molecules and polymers/copolymers that exhibit photoresponsiveness. In some instances, the substituted phenacyl molecule is incorporated into the polymer/copolymer backbone, and photoirradiation of the polymer/copolymer causes the substituted phenacyl group to break down and the polymer/copolymer to undergo degradation. In other instances, the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone. In yet other instances the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and a drug or polymer additive is linked to the photoresponsive substituted phenacyl group such that photoirradiation releases the drug or additive. In yet other embodiments the substituted phenacyl molecules extend as a side chain from the polymer/copolymer backbone, and serve to link the polymer/copolymer to another polymer/copolymer backbone, and photoirradiation breaks the links.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 30, 2014
    Inventors: Abraham Joy, Shuangyi Sun
  • Publication number: 20140256004
    Abstract: The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Sanjay Naik, Maruti Ghagare, Sandip Vasant Chikhalikar
  • Publication number: 20140221394
    Abstract: The invention provides an acid addition salt of a compound of the formula (1). Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
    Type: Application
    Filed: January 7, 2014
    Publication date: August 7, 2014
    Applicant: Astex Therapeutic Ltd.
    Inventors: Martyn Frederickson, John Francis Lyons, Neil Thomas Thompson, Mladen Vinkovic, Brian John Williams, Andrew James Woodhead, Alison Jo-Anne Woolford
  • Patent number: 8796459
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 5, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20140213794
    Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 31, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Nobuyuki ARAKI, Toru YAMAZAKI, Nobuyuki KUSANO, Eiyu IMAI, Hisashi KANNO, Masaru MORI, Taiji MIYAKE
  • Patent number: 8785494
    Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: July 22, 2014
    Assignee: LEO-Pharma A/S
    Inventor: Bjarne Nørremark
  • Publication number: 20140200352
    Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Nobuyuki ARAKI, Toru YAMAZAKI, Nobuyuki KUSANO, Eiyu IMAI, Hisashi KANNO, Masaru MORI, Taiji MIYAKE
  • Patent number: 8703991
    Abstract: A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: April 22, 2014
    Assignee: Wellstat Therapeutics Corporation
    Inventors: David D. Wirth, Richard Hudspeth
  • Publication number: 20140107372
    Abstract: In order to provide a novel method for producing a cyclopentanone compound, the present invention is a method for producing a cyclopentanone compound represented by the formula (I). The method includes the steps of: substituting the group represented by Y by a hydrogen atom by allowing a compound represented by the formula (III) or an intermediate compound obtained from the compound represented by the formula (III) to react with a catalyst or a halogenating agent; and substituting, by hydrogen atoms, (i) the group or the atom represented by Z1 and (ii) the group or the atom represented by Z2, by reducing the compound represented by the formula (III) or the intermediate compound obtained from the compound represented by the formula (III).
    Type: Application
    Filed: June 4, 2012
    Publication date: April 17, 2014
    Applicant: KUREHA CORPORATION
    Inventor: Hisashi Kanno
  • Publication number: 20140094613
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 3, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki MURASE, Toshihito KUMAGAI, Hisaya WADA, Hisahide TANIMOTO, Koumei OHTA, Yoshihiro KIMURA
  • Publication number: 20140046086
    Abstract: The present invention provides efficient, economical and environmental friendly methods for synthesis of prostaglandin analogs including tafluprost and intermediates thereof. The invention involves a selective oxidation using in situ boronate ester protection and a unique crystallization method to remove the undesired isomers of fluorinated intermediates.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: Scinopharm (Changshu) Pharmaceuticals, Ltd.
    Inventor: Wen-Hsien Wen
  • Publication number: 20140039194
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: August 1, 2013
    Publication date: February 6, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Dominika PCION, Carrie TOMASI, Mark Charles WHITCOMB, Eric D. DOWDY, Wenyi FU, Patricia MACLEOD
  • Publication number: 20130330286
    Abstract: An inhibitor of endothelin action or a skin-whitening agent, comprising a compound represented by Formula (1) or a salt thereof as an active ingredient. wherein in Formula (1), R1 represents a formyl group or an alkyl group having 1 to 4 carbon atom(s), and R2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atom(s).
    Type: Application
    Filed: November 24, 2011
    Publication date: December 12, 2013
    Applicant: Kao Corporation
    Inventors: Tsuyoshi Ohba, Daiki Murase, Mitsuru Sugiyama
  • Patent number: 8586776
    Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: November 19, 2013
    Assignee: FibroStatin, S.L.
    Inventors: Juan Saus, Santos Fustero, Juan F. Sanz-Cervera, Enrique Perez-Paya, Raul Blasco, Francisco Revert-Ros, Fernando Revert
  • Publication number: 20130296599
    Abstract: The invention provides novel phenylglyoxylic acid derivatives, which may be useful as intermediates for preparing stereoisomerically enriched drug compounds. The invention also provides methods of making phenylglyoxylic acid derivatives, and uses of phenylglyoxylic acid derivatives.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Dharma Rao Polisetti, Kalpathy Santhosh, Muralidhar Bondlela, Robert Carl Andrews, Thomas Scott Yokum, Eugene Campian, Rajashaker Kache
  • Publication number: 20130296422
    Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
    Type: Application
    Filed: November 1, 2011
    Publication date: November 7, 2013
    Applicant: ARIGEN PHARMACEUTICALS, INC.
    Inventors: Hiroyuki Saimoto, Kiyoshi Kita, Yoshisada Yabu, Masaichi Yamamoto
  • Publication number: 20130281705
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventor: Shalini SHARMA
  • Publication number: 20130259850
    Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I or a pharmaceutically acceptable salt thereof. In Formula I m is 0, 1, 2, 3 or 4; n is 0 or 1; m+n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are —CH2CH2—. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms.
    Type: Application
    Filed: May 9, 2013
    Publication date: October 3, 2013
    Applicant: WELLSTAT THERAPEUTICS CORPORATION
    Inventors: James Dennen O'NEIL, Michael K. BAMAT, Reid W. von BORSTEL, Shalini SHARMA, Ramachandran ARUDCHANDRAN
  • Patent number: 8492452
    Abstract: A polymerizable photoinitiator is represented by Formula (I): wherein R1, R2 and R3 are independently selected from the group consisting of a hydrogen, an optionally substituted alkyl group and an optionally substituted aryl group or R1 and R3 represent the necessary atoms to form a five to eight membered ring; p, w, y and z are all integers with y representing a value 1 to 6; p representing the sum of w and z; p representing a value of 1 to 6; w=1 to (p?z) and z=0 to (p?w); L represents an optionally substituted (p+y)-valent linking group comprising 1 to 14 carbon atoms; A represents a radically polymerizable group selected from the group consisting of an acrylate group, a methacrylate group, a styrene group, an acryl amide group, a methacryl amide group, a maleate group, a fumarate group, an itaconate group, a vinyl ether group, an allyl ether group, an allyl ester group and a vinyl ester group; and X represents a photoinitiating moiety including at least one group capable of initiating a free radical p
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: July 23, 2013
    Assignee: Agfa Graphics NV
    Inventors: Johan Loccufier, Luc Van Maele, Jaymes Van Luppen, Roland Claes
  • Publication number: 20130131372
    Abstract: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.
    Type: Application
    Filed: May 16, 2011
    Publication date: May 23, 2013
    Applicant: GENFIT
    Inventors: Karine Bertrand, Alice Roudot, Patrice Rool
  • Publication number: 20130116437
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: September 14, 2012
    Publication date: May 9, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20130030050
    Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.
    Type: Application
    Filed: December 22, 2010
    Publication date: January 31, 2013
    Applicant: Haoma Medica Limited
    Inventors: Stephen Hodges, Robin Soper
  • Patent number: 8338637
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: December 25, 2012
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120302638
    Abstract: Esters of 4,5-disubstituted-oxy-2-methyl-3,6-dioxo-cyclohexa-1,4-dienyl alkyl acids were prepared chemically and/or enzymatically. Depending upon the ester, improved melanocyte cytotoxicity was achieved. Improved cytotoxicity characteristics are consistent with ester analogs being more physiologically compatible and less irritating to skin than their corresponding acids.
    Type: Application
    Filed: August 8, 2012
    Publication date: November 29, 2012
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: Michael Fitzpatrick Wempe, Liu Deng, Stephanie Kay Clendennen, Neil Warren Boaz
  • Publication number: 20120289735
    Abstract: A bis(formylphenyl) compound expressed by general formula (2) is useful as a photo-sensitive resist material:
    Type: Application
    Filed: July 20, 2012
    Publication date: November 15, 2012
    Applicant: HONSHU CHEMICAL INDUSTRY CO., LTD.
    Inventors: Akira YOSHITOMO, Tatsuya IWAI
  • Patent number: 8288580
    Abstract: A benzophenone compound is represented by the following formula (I): (A)n-X—(B)m??(I) wherein X is an organic moiety having (n+m) valence, (n+m) being an integer ranging from 1 to 4; A is B is R is H or a methyl group; n is the number of A bonded to X and is an integer ranging from 1 to 4; and m is the number of B bonded to X and is an integer ranging from 0 to 3.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: October 16, 2012
    Assignee: Double Bond Chemical Ind. Co., Ltd.
    Inventors: Jimmy Liu, Kuei-Ta Chen, I-Ling Chen
  • Publication number: 20120238763
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: November 18, 2010
    Publication date: September 20, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura
  • Publication number: 20120232286
    Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.
    Type: Application
    Filed: December 7, 2010
    Publication date: September 13, 2012
    Applicant: KUREHA CORPORATION
    Inventors: Nobuyuki Araki, Toru Yamazaki, Nobuyuki Kusano, Eiyu Imai, Hisashi Kanno, Masaru Mori, Taiji Miyake
  • Publication number: 20120230925
    Abstract: Disclosed is the use of benzotropolone derivatives of formula (1), wherein R1, R2 and R7 independently from each other are hydrogen; C1-C3alkyl; or COR8; R3 is hydrogen; or COOR9 R4 is hydrogen; or C1-C3alkyl; R5 is hydrogen; hydroxy; C1-C3-alkoxy; or -0-(CO)—R10; R6 is hydrogen; C1-C3alkyl; or COR8; or R5 and R6 together may form a five or six membered ring; or R6 and R7 together form a five or six membered ring; and R8, R9, R10 independently of each other are C1-C30alkyl; for protecting body-care and household products from photolytic and oxidative degradation.
    Type: Application
    Filed: October 5, 2010
    Publication date: September 13, 2012
    Applicant: BASF SE
    Inventors: Barbara Wagner, Oliver Reich, Alexander Mantler, Reinhold Öhrlein, Walter Fischer, Albert Schneider
  • Publication number: 20120213758
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 23, 2012
    Applicant: DeCODE Genetics enf
    Inventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
  • Publication number: 20120149707
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Application
    Filed: April 21, 2011
    Publication date: June 14, 2012
    Applicant: OSCOTEC INC.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Patent number: 8198323
    Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.
    Type: Grant
    Filed: April 12, 2010
    Date of Patent: June 12, 2012
    Assignees: The University of North Carolina at Chapel Hill, The University of Rochester Medical Center, Androscience Corporation
    Inventors: Kuo-Hsiung Lee, Li Lin, Charles C-Y Shih, Ching-Yuan Su, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang
  • Publication number: 20120142934
    Abstract: A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.
    Type: Application
    Filed: March 10, 2011
    Publication date: June 7, 2012
    Inventors: Chien-Hong CHENG, Jaganathan Karthikeyan, Pang-Chi Huang
  • Publication number: 20120130090
    Abstract: A trifluoromethylthiophenium derivative salt useful as synthetic intermediates for pharmaceuticals and agrochemicals, a method for producing the same, and a method for producing trifluoromethyl-containing compounds using the same are provided. An S-(trifluoromethyl)-benzo[b]thiophenium derivative salt is represented by the following general formula (1): wherein R1, R2, R3, and R4 are each independently a hydrogen atom, a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a methoxy group, an ethoxy group, a linear, branched, or cyclic alkyloxy group having 3 to 10 carbon atoms, a fluorine atom, a chlorine atom, a bromine atom, a nitro group, or a cyano group, R5 is a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a phenyl group, or a substituted phenyl group, and X? represents an anion.
    Type: Application
    Filed: July 13, 2010
    Publication date: May 24, 2012
    Inventors: Norio Shibata, Takumi Kagawa
  • Publication number: 20120129931
    Abstract: This invention relates to caffeic acid derivatives and improving viability of neuronal cells by contacting neuronal cells by caffeic acid derivatives as shown in the specification.
    Type: Application
    Filed: November 15, 2011
    Publication date: May 24, 2012
    Applicant: ChemiGen
    Inventors: Junyi Liu, Yangsheng Du
  • Publication number: 20120129926
    Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: May 24, 2012
    Applicant: LEO PHARMA A/S
    Inventor: Bjarne Nørremark
  • Publication number: 20120108839
    Abstract: The present invention relates to a process for preparing a prostaglandin derivative and an intermediate therefor. In accordance with the present invention, the prostaglandin F (PGF) derivative can be efficiently prepared with high purity by removing the protecting group of a protected prostaglandin E (PGE) derivative obtained from conjugate addition and then stereoselectively reducing the ketone group on the cyclopentanone ring of the PGE derivative.
    Type: Application
    Filed: March 11, 2010
    Publication date: May 3, 2012
    Applicant: YONSUNG FINE CHEMICAL CO., LTD.
    Inventors: Changyoung Oh, Kee Young Lee, Yong Hyun Kim, Jae Eun Joo
  • Publication number: 20120095051
    Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: May 14, 2010
    Publication date: April 19, 2012
    Inventors: Francis Johnson, Lorne Golub
  • Patent number: 8153801
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: April 10, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Steven Pfeiffer
  • Publication number: 20120065179
    Abstract: There is provided a prodrug of a pharmaceutically active agent, such prodrug comprising a beta-keto carboxylic acid, a beta-keto carboxylic acid salt or a beta-keto carboxylic acid ester functional group, a pharmaceutical composition comprising the prodrug, and to the use of the prodrug or composition for treatment of a mammalian subject suffering from a condition which can be cured or alleviated by administration of the pharmaceutically active agent. There is further provided a method of inhibiting decarboxylation of a compound comprising a beta-keto carboxylic acid or a salt thereof with a monovalent cation, characterized in that a dry salt of the beta-keto carboxylic acid with a divalent or polyvalent cation is prepared.
    Type: Application
    Filed: April 13, 2010
    Publication date: March 15, 2012
    Applicant: YKI, Ytemiska Institutet AB
    Inventor: Martin Andersson
  • Publication number: 20120029107
    Abstract: The invention pertains to novel oligofunctional photoinitiators of the formula (1) or (1A). R1 and R2 are methyl or together are —(CH2)5—; and n is 2 or 3, and the solvent in (1A) is water or an organic solvent; and their use in photopolymerizable compositions, in particular inks.
    Type: Application
    Filed: March 19, 2010
    Publication date: February 2, 2012
    Applicant: BASF SE
    Inventors: Ulrich Berens, Jean-Luc Birbaum, Katia Studer