Chalcogen Attached Directly To The Additional Hetero Ring By Nonionic Bonding Patents (Class 546/283.1)
  • Patent number: 9861104
    Abstract: The present invention relates to a method for producing an aqueous suspension concentrate formulation and novel suspension concentrate formulations of the compound of formula I. The method comprises: a) providing an aqueous slurry of coarse particles of the compound of the formula I, where the compound of the formula I is at least partially present in its crystalline form B, which, in an X-ray powder diffractogram at 25° C. and Cu-K? radiation, shows at least three, preferably at least four, in particular at least 5 or at least 7 or at least 9 or all of the following reflexes, given as 2? values: 8.0±0.2°, 9.5±0.2°, 10.7±0.2°, 11.0±0.2°, 11.2±0.2°, 11.7±0.2°, 14.2±0.2°, 15.6±0.2°, 16.5±0.2°, 17.7±0.2°, 21.5±0.2°; b) comminuting the coarse particles in the slurry of the compound of formula I, which is at least partially present in its form B, in the presence of the at least one surfactant.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 9, 2018
    Assignee: BASF SE
    Inventors: Torsten Knieriem, Tiziana Chiodo, Christopher Koradin, Tanja Weber, Walter Weishaar
  • Patent number: 9598428
    Abstract: The present invention relates to a method for preparing the pyripyropene compound of the formula (I) which method comprises the following steps: i) subjecting a pyripyropene compound of formula Pyripyropene A to an alkaline hydrolysis to yield a 1,7,11 -trideacetylpyripyropene A, ii) reacting 1,7,11-trideacetylpyripyropene A obtained in step i) with cyclopropane carbonyl chloride to yield a raw product containing the pyripyropene compound of formula (I); iii) subjecting the raw product of step ii) to crystallization to yield a crystalline pyripyropene compound of formula (I) and a mother liquor; and iv) recycling the mother liquor or a pyripyropene compound containing fraction thereof to the alkaline hydrolysis of step i).
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: March 21, 2017
    Assignee: BASF SE
    Inventors: Melanie Bonnekessel, Wolfgang Reichert, Ralf Hoock, Thomas Kaeding, Christopher Koradin, Andreas Pletsch, Manfred Ehresmann, Hartwig Schroeder
  • Patent number: 9023837
    Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: May 5, 2015
    Assignee: Colby Pharmaceutical Company
    Inventors: Hirak S. Basu, David A. Zarling, George Wilding, Farideh Mehraein-Ghomi, Dawn R. Church
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Patent number: 8975263
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: March 10, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shigeo Yamanoi, Katsuji Kagechika, Tsuyoshi Soneda, Yuichi Ochiai, Hidenori Namiki, Fuminao Doi, Madoka Hoshino, Shoko Yoshida
  • Publication number: 20150056166
    Abstract: The present invention relates to flavone derivatives and to compositions containing one or more of these flavone derivatives. The present invention further relates to flavone derivatives or compositions for use in the treatment and/or prevention of a viral infection, and to a method of preventing or treating these infections.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 26, 2015
    Inventors: Thomas Pietschmann, Sibylle Haid, Juliane Gentzsch, Christina Grethe, Elisabeth Davioud-Charvet, Don Antoine Lanfranchi, Mourad Elhabiri, Xavier Benlloch-Martin
  • Patent number: 8952003
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Patent number: 8853414
    Abstract: Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: October 7, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Yoshimasa Fukuda, Takashi Ando, Kimihiko Goto, Nozomu Nakanishi, Takashi Watanabe, Kenichi Kurihara, Nobuto Minowa, Masaaki Mitomi
  • Patent number: 8853413
    Abstract: Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: October 7, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Yoshimasa Fukuda, Takashi Ando, Kimihiko Goto, Nozomu Nakanishi, Takashi Watanabe, Kenichi Kurihara, Nobuto Minowa, Masaaki Mitomi
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140227302
    Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: September 4, 2012
    Publication date: August 14, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett
  • Publication number: 20140219960
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 7, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Publication number: 20140213786
    Abstract: The present invention provides a novel method for producing a compound represented by general formula (VII) below or a pharmaceutically acceptable salt thereof or a synthetic intermediate thereof: wherein R2 represents a hydrogen atom or a halogen atom, Rc represents a C1-6 alkyl group, X represents a group selected from a heteroaryl group etc., R11 represents an atom or group selected from a hydrogen atom, a halogen atom, a C1-6 alkyl group, etc., R16 and R17 each independently represent an atom or group selected from a hydrogen atom, a C1-6 alkyl group, etc., and R15 represents a hydrogen atom or a C1-6 alkyl group.
    Type: Application
    Filed: September 5, 2012
    Publication date: July 31, 2014
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Masatoshi Murakata, Takuma Ikeda, Takahiro Ichige
  • Patent number: 8791263
    Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: July 29, 2014
    Assignee: Osaka University
    Inventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
  • Patent number: 8759529
    Abstract: A process for producing compound C represented by formula C is disclosed: wherein R? represents substituent groups as described herein. The process can produce pyripyropene derivatives that have acyloxy groups at the 1- and 11-positions and a hydroxyl group at the 7-position and are useful as insect pest control agents at a high yield.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: June 24, 2014
    Assignee: BASF SE
    Inventors: Kimihiko Goto, Kazumi Yamamoto, Masayo Sakai, Masaaki Mitomi, Takashi Ando
  • Publication number: 20140148480
    Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.
    Type: Application
    Filed: January 15, 2014
    Publication date: May 29, 2014
    Applicant: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6)
    Inventors: Michele REBOUD-RAVAUX, Chahrazade YERROUM-EL AMRI, Xiao TAN, Lixian QIN, Maurice PAGANO, Alain HOVNANIAN, Laetitia FURIO, Bernard PIROTTE
  • Publication number: 20140105920
    Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 17, 2014
    Inventor: David Sherris
  • Publication number: 20140057950
    Abstract: The present invention relates to compounds of the general formula (I) which show a specific activity against cancer cell lines, the use of these compounds for prophylaxis and treatment of cancer as well as to pharmaceutical compositions containing at least one compound of general formula (I).
    Type: Application
    Filed: December 22, 2011
    Publication date: February 27, 2014
    Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DE WISSENSCHAFTEN E.V.
    Inventors: Mathias Christmann, Lea Radtke, Herbert Waldmann, Matthieu Willot, Slava Ziegler, Hongyan Sun
  • Publication number: 20140045778
    Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:
    Type: Application
    Filed: January 3, 2013
    Publication date: February 13, 2014
    Applicants: THE KITASATO INSTITUTE, MEIJI SEIKA PHARMA CO., LTD.
    Inventors: MEIJI SEIKA PHARMA CO., LTD., THE KITASATO INSTITUTE
  • Publication number: 20140024639
    Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • Publication number: 20130303544
    Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.
    Type: Application
    Filed: December 21, 2011
    Publication date: November 14, 2013
    Applicant: BEIJING SHENOGEN PHARMA GROUP LTD.
    Inventors: Hongxia Ding, Kun Meng, Jin Li
  • Publication number: 20130231325
    Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I: which are ALDH-2 inhibitors, useful for treating a patient in need thereof, for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.
    Type: Application
    Filed: August 30, 2012
    Publication date: September 5, 2013
    Applicant: Gilead Sciences. Inc.
    Inventors: Michael Graupe, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 8519128
    Abstract: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: August 27, 2013
    Assignee: The Kitasato Institute
    Inventors: Hiroshi Tomoda, Tohru Nagamitsu, Satoshi Omura
  • Publication number: 20130210772
    Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.
    Type: Application
    Filed: April 15, 2011
    Publication date: August 15, 2013
    Applicant: COLBY PHARMACEUTICAL COMPANY
    Inventors: Hirak S. Basu, David A. Zarling, George Wilding, Farideh Mehraein-Ghomi, Dawn R. Church
  • Publication number: 20130190360
    Abstract: Pesticidal composition containing a pyripyropene insecticide and an adjuvant The present invention relates to a compositions comprising a pyripyropene pesticide of the formula (I) or (II) as defined below and an adjuvant. The present invention relates also to methods of preparing and applying such compositions, as well as several uses thereof, and finally seeds, comprising said composition. The invention also relates to an aqueous pesticide formulation comprising a pesticide compound of the formula I as defined in claim 1 in the form of fine particles suspended in an aqueous liquid.
    Type: Application
    Filed: September 13, 2011
    Publication date: July 25, 2013
    Applicant: BASF SE
    Inventors: Wen Xu, Paul Neese, William Maurice Fletcher, Douglas D. Anspaugh, Heidi Emilia Saxell, Cedric Dieleman, Walter Weishaar, Paul Ch. Kierkus, Kara Benton, Rainer Berghaus, Tatjana Levy
  • Patent number: 8476313
    Abstract: Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 2, 2013
    Assignee: The Ohio State University Research Foundation
    Inventors: Robert W. Brueggemeier, Young-Woo Kim, John C. Hackett
  • Publication number: 20130157375
    Abstract: In one aspect, there is provided a fluorescent iron-binding compound bound to a solid phase. Also provided is a method for detecting non-transferrin bound iron in a sample, comprising contacting the sample with a fluorescent iron-binding compound bound to a solid phase and detecting a fluorescent signal derived from the fluorescent iron-binding compound bound to the solid phase, wherein the fluorescent signal is indicative of non-transferrin bound iron levels in the sample. Further provided is use of a fluorescent iron-binding compound bound to a solid phase to detect non-transferrin bound iron in a sample.
    Type: Application
    Filed: April 27, 2011
    Publication date: June 20, 2013
    Applicants: LONDON SCHOOL OF HYGIENE AND TROPICAL MEDICINE, KING'S COLLEGE LONDON
    Inventors: Robert Hider, Yongmin Ma, Ulrich Schaible, Maria Podinovskaia
  • Publication number: 20130129757
    Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferat
    Type: Application
    Filed: January 11, 2013
    Publication date: May 23, 2013
    Applicant: Immunolight, LLC
    Inventor: Immunolight, LLC
  • Publication number: 20130131091
    Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Yoshimasa Fukuda, Nozomu Nakanishi, Masato Tani, Nobuto Minowa, Masaaki Mitomi, Satoshi Omura, Toshiaki Sunazuka, Hiroshi Tomoda
  • Publication number: 20130131429
    Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferat
    Type: Application
    Filed: January 11, 2013
    Publication date: May 23, 2013
    Applicant: lmmunolight, LLC
    Inventor: lmmunolight, LLC
  • Publication number: 20130116247
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 9, 2013
    Applicant: MANNKIND CORPORATION
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Publication number: 20130085163
    Abstract: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —13—O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.
    Type: Application
    Filed: March 25, 2011
    Publication date: April 4, 2013
    Applicant: SCHOOL JURIDICAL PERSON KITASATO INSTITUTE
    Inventors: Hiroshi Tomoda, Tohru Nagamitsu, Daisuke Matsuda, Taichi Ohshiro, Masaki Ohtawa, Satoshi Omura
  • Patent number: 8410109
    Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: April 2, 2013
    Assignee: Resverlogix Corp.
    Inventors: Norman C. W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
  • Publication number: 20130060042
    Abstract: Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.
    Type: Application
    Filed: November 10, 2010
    Publication date: March 7, 2013
    Inventors: Yoshimasa Fukuda, Takashi Ando, Kimihiko Goto, Nozomu Nakanishi, Takashi Watanabe, Kenichi Kurihara, Nobuto Minowa, Masaaki Mitomi
  • Publication number: 20130045935
    Abstract: This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.
    Type: Application
    Filed: May 3, 2011
    Publication date: February 21, 2013
    Inventors: Tak-Hang Chan, Larry Ming-Cheung Chow, Kin-Fai Chan, Iris Lai King Wong
  • Patent number: 8372866
    Abstract: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: February 12, 2013
    Assignee: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Sabrina Pucci, Roberto Artusi, Gianfranco Caselli, Marco Lanza, Laura Mennuni, Francesco Makovec, Lucio Claudio Rovati, Stefania Mazza
  • Publication number: 20120330022
    Abstract: There is provided a method for producing a pyripyropene derivative represented by the following formula A by an enzyme method. The production method of the present invention allows for production of a pyripyropene derivative under simpler conditions and in shorter steps. [wherein R represents a linear, branched or cyclic C2-6 alkylcarbonyl group (when the alkyl moiety of this group is branched or cyclic, C3-6 alkyl carbonyl group)].
    Type: Application
    Filed: January 19, 2011
    Publication date: December 27, 2012
    Inventors: Kentaro Yamamoto, Mariko Tsuchida, Kazuhiko Oyama, Kimihiko Goto, Masaaki Mitomi
  • Publication number: 20120328661
    Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: October 20, 2010
    Publication date: December 27, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
  • Publication number: 20120330021
    Abstract: A process for producing compound C represented by formula C is disclosed: wherein R? represents substituent groups as described herein. The process can produce pyripyropene derivatives that have acyloxy groups at the 1- and 11-positions and a hydroxyl group at the 7-position and are useful as insect pest control agents at a high yield.
    Type: Application
    Filed: August 13, 2012
    Publication date: December 27, 2012
    Inventors: Kimihiko Goto, Kazumi Yamamoto, Masayo Sakai, Masaaki Mitomi, Takashi Ando
  • Publication number: 20120295920
    Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
    Type: Application
    Filed: December 10, 2010
    Publication date: November 22, 2012
    Inventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
  • Publication number: 20120264736
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Application
    Filed: October 6, 2011
    Publication date: October 18, 2012
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • Publication number: 20120252745
    Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.
    Type: Application
    Filed: February 19, 2010
    Publication date: October 4, 2012
    Inventors: Brian S. J. Blagg, Huiping Zhao, Alison Catherine Donnelly
  • Patent number: 8263778
    Abstract: Disclosed is a process for producing compound C represented by formula C: wherein R? represents straight chain, branched chain, or cyclic C2-6 alkylcarbonyl, wherein R1b is used as a protective group for hydroxyl at the 7-position of compound C.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: September 11, 2012
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Kimihiko Goto, Kazumi Yamamoto, Masayo Sakai, Masaaki Mitomi, Takashi Ando
  • Publication number: 20120172399
    Abstract: This invention relates to new compounds that can serve as hypoxia mimetics. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one of these compounds.
    Type: Application
    Filed: July 14, 2010
    Publication date: July 5, 2012
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Hong Cao, Yinxiang Wang, Fenlai Tan, Yunyan Hu
  • Publication number: 20120172348
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 22, 2010
    Publication date: July 5, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Patent number: 8202890
    Abstract: Disclosed is a compound usable as a pest control agent and has excellent pest control activity. A compound represented by formula (I) has excellent pest control activity. The compound or an agriculturally or horticulturally acceptable salt thereof is thus useful as a pest control agent.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: June 19, 2012
    Assignees: Meiji Seika Pharma Co., Ltd., The Kitasato Institute
    Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Satoshi Omura, Toshiaki Sunazuka
  • Publication number: 20120122810
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Publication number: 20120046470
    Abstract: Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.
    Type: Application
    Filed: May 12, 2010
    Publication date: February 23, 2012
    Inventors: Yoshimasa Fukuda, Takashi Ando, Kimihiko Goto, Nozomu Nakanishi, Takashi Watanabe, Kenichi Kurihara, Nobuto Minowa, Masaaki Mitomi
  • Publication number: 20110262482
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Applicant: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard