Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
  • Publication number: 20100248313
    Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
    Type: Application
    Filed: December 18, 2008
    Publication date: September 30, 2010
    Inventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
  • Publication number: 20100249085
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Application
    Filed: May 8, 2008
    Publication date: September 30, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • Publication number: 20100239551
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
    Type: Application
    Filed: January 4, 2008
    Publication date: September 23, 2010
    Applicant: IRM LLC
    Inventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Badry Bursulaya
  • Patent number: 7799927
    Abstract: An indolestyryl compound. The indolestyryl compound has formula (I): wherein Z1 comprises benzene, naphthalene, or heterocyclic ring containing O, S, or N, R2 comprises H, halogen atoms, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, sulfuric ester, amide, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R3, R4, R5, and R6 comprise H, alkyl, aralkyl, or heterocyclic ring containing O, S, or N, R7 and R8 comprise H or alkyl, R10 comprises H, alkyl, halogen atoms, nitro, hydroxyl, amino, ester, or substituted or non-substituted sulfonyl, W comprises carbon or nitrogen, Y comprises carbon, oxygen, sulfur, selenium, —NR, or —C(CH3)2, m is 1˜3, and X1 comprises an anionic group or an anionic organometallic complex, wherein R3 and R4 are joined to a nitrogen atom or R5 and R6 are joined together to form a ring, and R bonded to nitrogen is C1-5 alkyl.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: September 21, 2010
    Assignee: Industrial Technology Research Institute
    Inventors: Shin-Shin Wang, Chien-Wen Chen, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Wen-Yih Liao, Chien-Liang Huang, Tzuan-Ren Jeng, Ching-Yu Hsieh, An-Tse Lee
  • Publication number: 20100233116
    Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: August 13, 2007
    Publication date: September 16, 2010
    Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
  • Publication number: 20100221764
    Abstract: The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.
    Type: Application
    Filed: May 29, 2008
    Publication date: September 2, 2010
    Applicant: BIOMERIEUX
    Inventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
  • Publication number: 20100221215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 9, 2010
    Publication date: September 2, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20100197686
    Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
    Type: Application
    Filed: March 21, 2008
    Publication date: August 5, 2010
    Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventors: Chengguo Xing, Jignesh Doshi
  • Patent number: 7767701
    Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: August 3, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: Masaichi Hasegawa, Jun Tang, Hideyuki Sato
  • Patent number: 7750021
    Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 6, 2010
    Assignee: IRM LLC
    Inventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
  • Publication number: 20100168179
    Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.
    Type: Application
    Filed: March 11, 2010
    Publication date: July 1, 2010
    Inventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann, Jens Hoffmann, Rosemarie Lichtner
  • Patent number: 7745377
    Abstract: The invention provides peptide synthons having protected functional groups for attachment of desired moieties (e.g. functional molecules or probes). Also provided are peptide conjugates prepared from such synthons, and synthon and conjugate preparation methods including procedures for identifying the optimum probe attachment site. Biosensors are provided having environmentally sensitive dyes that can locate specific biomolecules within living cells and detect chemical and physiological changes in those biomolecules as the living cell is moving, metabolizing and reacting to its environment. Methods are included for detecting GTP activation of a Rho GTPase protein using polypeptide biosensors. When the biosensor binds GTP-activated Rho GTPase protein, the environmentally sensitive dye emits a signal of a different lifetime, intensity or wavelength than when not bound.
    Type: Grant
    Filed: May 5, 2005
    Date of Patent: June 29, 2010
    Assignee: The Scripps Research Institute
    Inventors: Klaus M. Hahn, Alexei Toutchkine, Rajeev Muthyala, Vadim Kraynov, Steven J. Bark, Dennis R. Burton, Chester Chamberlain
  • Patent number: 7745632
    Abstract: A cyanine compound represented by the general formula (I), (VI) or (VII): wherein ring-A1 is an optionally substituted benzene or naphthalene ring; B is a group represented by the general formula (II) or (III); R1 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or an aryl group having 6 to 30 carbon atoms; R2 is a substituent represented by the general formula (IV); and Y1 is a hydrogen atom, an organic group having 1 to 30 carbon atoms, or a substituent represented by the general formula (IV): wherein ring-A2 is the same as the ring-A1 in the general formula (I); Y4 and Y5 each are independently the same as Y1 in the general formula (I); X2 is the same as X1 in the general formula (I); R10 is the same as R1 in the general formula (I); R11 is the same as R2 in the general formula (I); R23 and R24 are the same as R21 and R22 in the formulas (II) and (III); n is an integer of 0 to 6; the polymethine chain may have a subst
    Type: Grant
    Filed: April 4, 2006
    Date of Patent: June 29, 2010
    Assignee: Adeka Corporation
    Inventors: Yohei Aoyama, Koichi Shigeno
  • Patent number: 7741343
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: June 22, 2010
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7741327
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: June 22, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, John A Brinkman, Stuart Hayden, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
  • Patent number: 7741316
    Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: June 22, 2010
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 7737166
    Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: June 15, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
  • Patent number: 7718646
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: May 18, 2010
    Assignee: Sanofi-Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20100120839
    Abstract: There is provided compounds of formula I, wherein R1, R2, A1, A2, A3 and A4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
    Type: Application
    Filed: April 21, 2008
    Publication date: May 13, 2010
    Inventors: Kiyo No, Andrei Sanin, Gasse Kromann
  • Publication number: 20100121062
    Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
    Type: Application
    Filed: September 25, 2009
    Publication date: May 13, 2010
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
  • Publication number: 20100113460
    Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: Givaudan SA
    Inventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
  • Publication number: 20100099682
    Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.
    Type: Application
    Filed: September 17, 2009
    Publication date: April 22, 2010
    Inventors: Ralf GLATTHAR, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
  • Publication number: 20100093707
    Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.
    Type: Application
    Filed: December 17, 2009
    Publication date: April 15, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
  • Publication number: 20100060155
    Abstract: Disclosed is a novel organic semiconductor material which has a twisted quaterphenylene skeleton as a central unit and simultaneously possesses a skeleton having an electron-transporting property and a skeleton having a hole-transporting property at the terminals of the quaterphenylene skeleton. Specifically, the organic semiconductor material has a [1,1?:2?,1?:2?,1??]quaterphenyl-4-4??-diyl group, and one of the terminals of the [1,1?:2?,1?:2?,1??]quaterphenyl-4-4??-diyl group is bonded to a skeleton having an electron-transporting property such as a benzoxazole group or an oxadiazole group. A skeleton having a hole-transporting property such as diarylamino group is introduced at the other terminal. This structure allows the formation of a compound having a bipolar property, a high molecular weight, an excellent thermal stability, a large band gap, and high triplet excitation energy.
    Type: Application
    Filed: September 4, 2009
    Publication date: March 11, 2010
    Inventors: Satoshi Seo, Sachiko Kawakami, Hiroko Nomura, Nobuharu Ohsawa
  • Publication number: 20100035947
    Abstract: A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for Solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].
    Type: Application
    Filed: April 11, 2008
    Publication date: February 11, 2010
    Inventors: Yoshitaka Nakamura, Masayuki Murakami, Makoto Yamaoka, Masakazu Wakayama, Kazuhiro Umeo
  • Patent number: 7659296
    Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds of Formula (I) wherein the variables R, R?, RP, RP3, LP1, LP2, ZP, RB, RB?, LXB and ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and methods of use.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: February 9, 2010
    Assignee: Eli Lilly and Company
    Inventors: Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee
  • Publication number: 20100029720
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
    Type: Application
    Filed: September 9, 2009
    Publication date: February 4, 2010
    Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
  • Patent number: 7652125
    Abstract: A resin composition having high heat resistance and low dielectric constant after heat treatment, a varnish thereof and a semiconductor device using the same are provided by a resin composition including a compound having a structure represented by the general formula (1): wherein, “Ar” is an aromatic group; “a” is 0 or 1; R11 is an organic group having one or more carbon atoms and at least one is a group having an alicyclic structure; when “q” is an integer of 2 or more, R11s may be the same or different from each other; at least one of R1 to R5 and at least one of R6 to R10 on respective benzene rings are Ar-binding sites or R11-binding sites and the others of R1 to R5 and R6 to R10 are each hydrogen, a group having an alicyclic structure, an organic group having 1 to 10 carbon atoms, a hydroxyl group or a carboxyl group; when “a” is 0, at least one of R1 to R5 and R6 to R10 is a group having an alicyclic structure; “q” is an integer of 1 or more; and “X” is any of —O—, —NHCO—, —COHN—, —COO— and —OCO—.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: January 26, 2010
    Assignee: Sumitomo Bakelite Company, Ltd.
    Inventors: Takashi Enoki, Atsushi Izumi, Yumiko Yamamoto, Takahiro Harada
  • Publication number: 20100015054
    Abstract: Disclosed are reactive polyfluoro benzoxazole polymethine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which X is selected from the group consisting of —O—, —S— and at least one of groups R1 and R2 is the group -L-Rx or -L-Rp, where L is a linking group, Rx is a group suitable for covalent attachment of the dye to a component and Rp is a component; and at least one of groups R3, R4, R5, R6, R7, R8, R9 and R10 comprises fluorine. The use of polymethine dyes substituted by fluorine and having additional substitution by sulphonic acid groups, for labelling biological target molecules results in a labelled product in which there is reduced dye-dye aggregation and improved photostability, compared with cyanine dyes having no such substitutions.
    Type: Application
    Filed: October 4, 2007
    Publication date: January 21, 2010
    Applicant: GE HEALTHCARE UK LIMITED
    Inventor: Najeeb Said
  • Publication number: 20100004271
    Abstract: The invention provides Compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, wherein R3, R4, G, Y, W and R5 are as defined in the specification. The invention also provides the use of such Compounds in the treatment or Prophylaxis of a condition associated with a disease or disorder associated with thyroid receptor activity.
    Type: Application
    Filed: July 4, 2006
    Publication date: January 7, 2010
    Applicant: KARO BIO AB
    Inventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Lofstedt, Aiping Cheng, Thomas Fredrik Hansson, Edouard Zamaratski
  • Publication number: 20100003445
    Abstract: Disclosed is a cyanine compound represented by general formula (I) below. Also disclosed are an optical filter using the compound and an optical recording material.
    Type: Application
    Filed: March 28, 2008
    Publication date: January 7, 2010
    Applicant: ADEKA CORPORATION
    Inventors: Toru Yano, Mitsuhiro Okada, Koichi Shigeno
  • Publication number: 20090318445
    Abstract: The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.
    Type: Application
    Filed: December 28, 2006
    Publication date: December 24, 2009
    Applicants: NORVARTIS AG, NOVARTIS PHARMA GMBH
    Inventors: Arkadius Pichota, Jeyaraj Duraiswamy, Zheng Yin, Thomas Hugo Keller, Mark Schreiber
  • Publication number: 20090305410
    Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.
    Type: Application
    Filed: December 12, 2008
    Publication date: December 10, 2009
    Applicant: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung, Hye Eun Hoover
  • Publication number: 20090306078
    Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.
    Type: Application
    Filed: July 3, 2007
    Publication date: December 10, 2009
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Jung Joon Lee, Jeong-Hyung Lee, Kyeong Lee, Young-Soo Hong, B.K. Shanthaveerappa, Yinlan Jin, Jin Hwan Kim, Xuejun Jin
  • Patent number: 7625929
    Abstract: The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl Group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: December 1, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
  • Patent number: 7625923
    Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: December 1, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alexandra Nirschl, James C. Sutton, Lawrence Hamann, Tammy Wang, Yan Zou, Chongqing Sun
  • Patent number: 7625758
    Abstract: Protein dyes whose molecular structure is that of a coumarin moiety coupled to a quaternary ammonium heterocycle through a vinyl or polyvinyl linkage demonstrate the ability to associate with proteins in a non-covalent, non-specific manner at low pH, where the associated form displays a significantly higher fluorescence emission than the unassociated form. This makes the dyes useful as selective labels for proteins at the low pH and eliminates the need for the removal of extraneous components from the medium in which the proteins reside prior to detection.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: December 1, 2009
    Inventor: Thomas R. Berkelman
  • Patent number: 7622460
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: November 24, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20090281279
    Abstract: Disclosed are analogues of trimethine cyanine dyes, which are useful for importing fluorescent properties to target materials by covalent and non-covalent association.
    Type: Application
    Filed: May 15, 2007
    Publication date: November 12, 2009
    Applicant: Carnegie Mellon University
    Inventors: Alan S. Waggoner, Ratnakar B. Mujumdar
  • Publication number: 20090281131
    Abstract: The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-?).
    Type: Application
    Filed: September 10, 2007
    Publication date: November 12, 2009
    Inventors: Balasubramanian Gopalan, Dhamjewar Ravi, Shrikant Havale, Swamy Keshavapura Hosamane Sreedhara
  • Publication number: 20090274632
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: August 19, 2008
    Publication date: November 5, 2009
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Publication number: 20090258917
    Abstract: There is provided the use of a compound of formula I, wherein Y, W1 to W4, Z1 to Z4 and R have meanings given in the description, and pharmaceutically-acceptable salts thereof, for the manufacture of a medicament for the treatment of a disease in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
    Type: Application
    Filed: October 12, 2006
    Publication date: October 15, 2009
    Inventors: Benjamin Pelcman, Kristofer Olofsson, Wesley Schaal, Ivars Kalvins, Martins Katkevics, Vita Ozola, Edgars Suna
  • Publication number: 20090253762
    Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
    Type: Application
    Filed: September 8, 2008
    Publication date: October 8, 2009
    Inventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
  • Patent number: 7595343
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: September 29, 2009
    Assignee: MethylGene, Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Publication number: 20090239841
    Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
    Type: Application
    Filed: October 24, 2005
    Publication date: September 24, 2009
    Inventors: Alan J. Hutchison, Jun Yuan
  • Patent number: 7592343
    Abstract: Compounds of formula (Ia): where x, y, G, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, are disclosed, as well as pharmaceutical compositions comprising the compounds. These compounds and pharmaceutical compositions are useful in treating SCD-mediated diseases or conditions.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: September 22, 2009
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vandna Raina, Serguei Sviridov, Vishnumurthy Kodumuru, Nagasree Chakka, Shifeng Liu, Shaoyi Sun, Duanjie Hou
  • Publication number: 20090221593
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidin
    Type: Application
    Filed: August 18, 2006
    Publication date: September 3, 2009
    Inventors: Giorgio Bonanomi, Romano Di Fabio, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
  • Publication number: 20090211038
    Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.
    Type: Application
    Filed: September 19, 2008
    Publication date: August 27, 2009
    Inventors: Andrew GREAVES, Nicolas DAUBRESSE
  • Patent number: 7579478
    Abstract: The present invention provides processes for the purification of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol. The processes include recrystallizing the compound from a solution comprising acetone and acetonitrile; treating the crude purified product with a clarifying agent in a solution comprising ethyl acetate, and precipitating or triturating the compound from a mixed solvent system.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: August 25, 2009
    Assignee: Wyeth
    Inventor: Silvio Iera
  • Publication number: 20090203904
    Abstract: Compositions are provided that include an electron donor and a sensitizing compound. More specifically, the electron donor is an arylsulfinate salt. Methods of polymerization are also provided that can be used to prepare polymeric material from a photopolymerizable composition that includes ethylenically unsaturated monomers and a photoinitiator system. The photoinitiator system includes an electron donor and a sensitizing compound.
    Type: Application
    Filed: April 23, 2009
    Publication date: August 13, 2009
    Inventors: Rajdeep S. Kalgutkar, Michael C. Palazzotto