Carbocyclic Ring Containing Patents (Class 546/322)
  • Patent number: 10370334
    Abstract: Provided are an inositol nicotinate crystalline form A and a preparation method therefor. The X-ray powder diffraction analysis, obtained by using Cu-K? ray measurement, of the inositol nicotinate crystalline form A has obvious characteristic diffraction peaks at least at 2? values, expressed in degrees, of 7.05, 7.41, 9.74, 17.80, 19.86, 23.57, 25.48 and 26.20 with an error range of +/?0.2°. The preparation method is one of or a mixed crystallization method of two or more of an evaporation crystallization method, a cooling crystallization method or an anti-solvent crystallization method. The process thereof is simple and easy to operate, and has more selectivity; the inositol nicotinate crystalline form A can be prepared by various methods, and the prepared product has a good crystallization degree and high chemical stability; and the inositol nicotinate crystalline form A prepared by the present method does not have the problem that a residual solvent is out-of-limit.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: August 6, 2019
    Assignee: WEIFANG SHENGYU PHARMA CO., LTD.
    Inventors: Liwei Zhu, Xuefeng Mei, Jianrong Wang
  • Patent number: 9376388
    Abstract: Provided herein are fluoropicolinoyl fluorides and processes for their preparation. In some embodiments, provided herein is a process for the preparation of 5-fluoro-6-aryl-picolinoyl fluorides from chloropicolinoyl chlorides.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: June 28, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: James M. Renga, Yang Cheng, Joseck M. Muhuhi, David E. Podhorez, Gary A. Roth, Scott P. West, Gregory T. Whiteker, Yuanming Zhu
  • Publication number: 20150025247
    Abstract: Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 22, 2015
    Inventors: Liu DENG, Neil Warren BOAZ, Sabine DELAIRE
  • Publication number: 20140364457
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Publication number: 20140274905
    Abstract: The present invention generally relates to methods of modulating Cav1.2 channels and Cav1.2 channel activators.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Duke University
    Inventors: Geoffrey S. Pitt, Adam S. Barnett, Xinhe Yin
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Patent number: 8686184
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20130338199
    Abstract: The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (A?42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease, Huntington's disease, multiple sclerosis, amytrophic lateral sclerosis and ischemic stroke.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Uday Saxena, Venkateswarlu Akella
  • Publication number: 20130224657
    Abstract: The present invention provides an acid generator generates a sulfonic acid represented by the following general formula (1) in response to high-energy beam or heat: To provide a novel acid generator which is suitably used as an acid generator for a resist composition, which solves the problems of LER and a depth of focus and can be effectively and widely used particularly without degradation of a resolution, a chemically amplified resist composition using the same, and a patterning process.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 29, 2013
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventor: SHIN-ETSU CHEMICAL CO., LTD.
  • Publication number: 20130102641
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: December 13, 2012
    Publication date: April 25, 2013
    Applicant: XENOPORT, INC.
    Inventor: XENOPORT, INC.
  • Publication number: 20130040389
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 14, 2013
    Applicant: Intrexon Coporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20120308588
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20120301552
    Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: November 29, 2012
    Applicant: JAPAN TOBACCO INC.
    Inventors: Yuko Shinagawa, Teruhiko Inoue, Toshihiro Kiguchi, Taku Ikenogami, Naoki Ogawa, Kenji Fukuda, Takashi Nakagawa, Masanori Shindo, Yuki Soejima
  • Publication number: 20120190861
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Publication number: 20120145238
    Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.
    Type: Application
    Filed: August 27, 2010
    Publication date: June 14, 2012
    Applicant: BASF SE
    Inventors: Junichi Tanabe, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi
  • Publication number: 20120135975
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.
    Type: Application
    Filed: May 14, 2007
    Publication date: May 31, 2012
    Applicant: MERCK & CO., INC.
    Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
  • Publication number: 20120035224
    Abstract: The invention relates to compounds derived from betulin, and to the use thereof in plant pest control, particularly as antifeedants for butterfly larvae, beetles and snails. Further, the invention relates to novel betulin derivatives and methods for the production thereof either directly from betulin, or via intermediates derived therefrom.
    Type: Application
    Filed: June 1, 2007
    Publication date: February 9, 2012
    Applicant: Valtion teknillinen tutkimuskeskus
    Inventors: Sami Alakurtti, Jari Yli-Kauhaluoma, Taru Mäkelä, Salem Koskimies, Pia Bergström, Heikki Hokkanen, Ingeborg Menzler-Hokkanen
  • Publication number: 20120029198
    Abstract: Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.
    Type: Application
    Filed: December 22, 2010
    Publication date: February 2, 2012
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: Liu Deng, Neil Warren Boaz
  • Publication number: 20120022227
    Abstract: The present invention relates to reagents and methods for [18F]-fluorination of biomolecules, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).
    Type: Application
    Filed: March 22, 2010
    Publication date: January 26, 2012
    Inventors: Dag Erlend Olberg, Arukwe Joseph Maduabuchi
  • Patent number: 8093274
    Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of GGTase I. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: January 10, 2012
    Assignee: The Regents of the University of California
    Inventors: Fuyuhiko Tamanoi, Ohyun Kwon, Masaru Watanabe, Hannah Fiji
  • Publication number: 20110233477
    Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methine dyes.
    Type: Application
    Filed: March 28, 2011
    Publication date: September 29, 2011
    Applicant: BASF SE
    Inventors: Hiroshi Yamamoto, Shinji Nakamichi, Junichi Tanabe, Ryuichi Takahashi, Hitoshi Yamato
  • Publication number: 20110213157
    Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)—CO— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)— (R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2— (R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.
    Type: Application
    Filed: August 14, 2008
    Publication date: September 1, 2011
    Applicant: RESEARCH FOUNDATION ITSUU LABORATORY
    Inventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
  • Publication number: 20110178138
    Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.
    Type: Application
    Filed: July 28, 2008
    Publication date: July 21, 2011
    Applicant: The Regents of the University of California
    Inventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hanna Fiji, Masaru Watanabe
  • Publication number: 20110097347
    Abstract: The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (A?42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease and ischemic stroke.
    Type: Application
    Filed: July 9, 2009
    Publication date: April 28, 2011
    Inventors: Uday Saxena, Venkateswarulu Akella
  • Publication number: 20110092544
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein each W and Y is independently CH2, O, C(?O), S(?O)n, NR8 or a direct bond; R4 is H, halogen, cyano, hydroxy, C1-C2 alkyl, C1-C2 haloalkyl, C2 alkenyl, C2 haloalkenyl or C2 alkynyl; m is an integer selected from 0, 1, 2, 3, 4 and 5; and R1, R2, R3, R5, R8 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: June 18, 2009
    Publication date: April 21, 2011
    Applicant: E.I. DU PONT DE nemours and company
    Inventor: Bruce Lawrence Finkelstein
  • Patent number: 7893263
    Abstract: This invention relates to novel corosolic acid analogs of the formula I, wherein R1, R2, R3, R4 and R5 are described herein. These compounds exhibit good hypoglycemic and 5-lipoxygenase inhibitory activities. They also inhibit tumour growth. Pharmaceutical compositions containing known adjutants and the title compounds are also within the scope of this invention.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: February 22, 2011
    Assignee: Laila Nutraceuticals
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Venkateswarlu Somepalli, Venkateswara Rao Chirravuri
  • Patent number: 7893270
    Abstract: The present invention relates to a process for the preparation of compounds of formula (I), wherein the substituents are as defined in claim 1, by reacting a compound of formula (II), with a bromine or chlorine source to form a compound of formula (III), wherein X is chlorine or bromine; reacting that compound with water to form the compound of formula (IV), converting that compound, using a compound of formula (V), wherein M+ is the hydrogen cation or an alkali metal ion, alkaline earth metal ion or ammonium ion, into the compound of formula (VI), and treating that compound with a cyanide source in the presence of a base.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: February 22, 2011
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: David Anthony Jackson, Andrew Edmunds, Martin Charles Bowden, Ben Brockbank
  • Publication number: 20110039851
    Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
    Type: Application
    Filed: October 14, 2008
    Publication date: February 17, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
  • Publication number: 20110021571
    Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
    Type: Application
    Filed: September 16, 2010
    Publication date: January 27, 2011
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, Fenmei Yao, Maria J. Ludwikow, Thu Phan, Ge Peng
  • Publication number: 20100317854
    Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
    Type: Application
    Filed: August 23, 2010
    Publication date: December 16, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
  • Publication number: 20100305166
    Abstract: A compound of formula (I) or salts thereof, wherein R1, R2, R3, R4, n and X are as defined in the specification; a process for preparing such compounds, a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Application
    Filed: October 30, 2008
    Publication date: December 2, 2010
    Inventors: Alessandra Gaiba, Susan Roomans, Martin Edward Swarbrick
  • Publication number: 20100298138
    Abstract: The present invention relates to the use of aminoazoline and urea derivatives for com-bating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds and to specific azoline and urea derivatives.
    Type: Application
    Filed: May 23, 2008
    Publication date: November 25, 2010
    Applicant: BASF SE
    Inventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
  • Publication number: 20100210837
    Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin.
    Type: Application
    Filed: April 18, 2008
    Publication date: August 19, 2010
    Inventor: Taifo Mahmud
  • Patent number: 7741346
    Abstract: An object of the present invention is to find new pharmacological actions of urea compounds having structure represented by the general formula [1]. The urea compounds having the structure represented by the general formula [1] have excellent angiogenesis inhibitory actions. [wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantylalkyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfur].
    Type: Grant
    Filed: November 29, 2002
    Date of Patent: June 22, 2010
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hidehito Matsuoka, Kazuo Nishimura, Hisayuki Seike, Hiroyuki Aono, Masaaki Murai
  • Publication number: 20100113770
    Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group r
    Type: Application
    Filed: October 14, 2009
    Publication date: May 6, 2010
    Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.
    Inventors: Susumu MUTO, Akiko ITAI
  • Publication number: 20100063114
    Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of GGTase I. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.
    Type: Application
    Filed: March 22, 2007
    Publication date: March 11, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Fuyuhiko Tamanoi, Ohyun Kwon, Masaru Watanabe, Hannah Fiji
  • Patent number: 7674827
    Abstract: Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds for combating animal pests The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: March 9, 2010
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
  • Publication number: 20100004459
    Abstract: The present invention is to provide the compounds useful as a treating or preventing agent for gout and hyperuricemia which are 2-phenylnicotinic acid derivatives having a uric acid lowering action due to an excellent xanthine oxidase inhibitory action. Since the 2-phenylnicotinic acid derivatives of the present invention exhibit a uric acid lowering action due to an excellent xanthine oxidase inhibitory action and also hypolipemic action, their utility is very high as a treating or preventive agent for gout and hyperuricemia which are often accompanied by hyperlipemia as a complication.
    Type: Application
    Filed: December 12, 2007
    Publication date: January 7, 2010
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Nobuo Menjo, Tomohiro Ookubo, Taisuke Hasegawa, Kazuhito Furukawa, Akihiro Fujita
  • Publication number: 20090318509
    Abstract: Provided are compounds of formula (I) and other compounds. Also provided are pharmaceutical compositions comprising these compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal, and methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock.
    Type: Application
    Filed: June 4, 2007
    Publication date: December 24, 2009
    Inventor: Yousef Al-Abed
  • Patent number: 7629471
    Abstract: Ascochlorin or an analog or derivative thereof and a compound having a primary amino group are mixed and reacted with each other in the presence/absence of a basic catalyst to synthesize a novel imino compound. The novel imino compound thus synthesized is a ligand capable of activating nuclear receptor superfamily such as retinoid orphan receptor (RXR), peroxisome proliferator-activated receptor (PPAR) and steroid receptor (PXR), and shows an effect of promoting the transcription of a drug-metabolizing enzyme CYP7A1. The imino compound has a therapeutic effect on diseases such as lifestyle-related diseases, chronic inflammation and cancers.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: December 8, 2009
    Assignee: NRL Pharma, Inc.
    Inventors: Takeshi Kitahara, Hidenori Watanabe, Kunio Ando
  • Publication number: 20090197924
    Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alk
    Type: Application
    Filed: January 27, 2009
    Publication date: August 6, 2009
    Applicants: Oroxcell, Alexis Denis
    Inventors: Jean Pachot, Christophe Dini, Alexis Denis
  • Publication number: 20090137558
    Abstract: The present invention relates to substituted pyridine compounds of Formula (I) and derivatives thereof, and to a process for preparing these substituted pyridines. The invention also relates to the use of the substituted pyridines as intermediates in the production of pharmaceutical, chemical and agro-chemical products.
    Type: Application
    Filed: December 1, 2005
    Publication date: May 28, 2009
    Applicant: PEAKDALE MOLECULAR LIMITED
    Inventors: Raymond Fisher, Andrew Lund
  • Publication number: 20090023786
    Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: April 5, 2005
    Publication date: January 22, 2009
    Applicant: Alton Pharma, Inc.
    Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
  • Publication number: 20080312286
    Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: July 26, 2005
    Publication date: December 18, 2008
    Inventors: Anthony B. Pinkerton, Jean-Michel Vernier, Rowena Cube, John Hutchinson, Celine Bonnefous, Theodore Kamenecka
  • Publication number: 20080234305
    Abstract: The invention relates to novel tetrahydropyridine derivatives and use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
    Type: Application
    Filed: October 5, 2004
    Publication date: September 25, 2008
    Inventors: Olivier Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
  • Publication number: 20080139816
    Abstract: The present invention relates to a process for the preparation of compounds of formula (I), wherein the substituents are as defined in claim 1, by reacting a compound of formula (II), with a bromine or chlorine source to form a compound of formula (III), wherein X is chlorine or bromine; reacting that compound with water to form the compound of formula (IV), converting that compound, using a compound of formula (V), wherein M+ is the hydrogen cation or an alkali metal ion, alkaline earth metal ion or ammonium ion, into the compound of formula (VI), and treating that compound with a cyanide source in the presence of a base.
    Type: Application
    Filed: April 29, 2005
    Publication date: June 12, 2008
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: David Anthony Jackson, Andrew Edmunds, Martin Charles Bowden, Ben Brockbank
  • Patent number: 7335673
    Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: February 26, 2008
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
  • Patent number: 7320993
    Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: January 22, 2008
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Patent number: 7232821
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: June 19, 2007
    Assignee: Glaxo Group Limited
    Inventors: Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Xiao Qing Lewell, Alan Naylor, Riccardo Novelli