Halogen Attached Directly Or Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/302)
  • Publication number: 20150045378
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Patent number: 8946434
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 3, 2015
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Patent number: 8840866
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: September 23, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20140256549
    Abstract: The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 11, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventor: David A. Morgenstern
  • Publication number: 20140228310
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Publication number: 20140228219
    Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.
    Type: Application
    Filed: May 29, 2012
    Publication date: August 14, 2014
    Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
  • Publication number: 20140121187
    Abstract: Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 1, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Ihl Young Choi, Hae Soo Kim, Pil Ho Kim, Soo Bong Han, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Patent number: 8618102
    Abstract: The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Georgia B. McGaughey, Anthony J. Roecker, John D. Schreier
  • Publication number: 20130331382
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: December 12, 2013
    Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Publication number: 20130303541
    Abstract: The present invention discloses an aryloxy dihalopropenyl ether compound with the structure shown as general formula (I), of which the group definitions can be seen in the specification. The present invention also discloses the use of the compound with general formula (I) as an insecticide in the agricultural field and an insecticidal composition using the compound with general formula (I) as an active component.
    Type: Application
    Filed: March 28, 2012
    Publication date: November 14, 2013
    Applicants: Shenyang Research Institute Of Chemical Industry Co., Ltd., SINOCHEM CORPORATION
    Inventors: Changling Liu, Jichun Yang, Xiuhui Chang, Miao Li, KeKe Li, Qiao Wu, Yuquan Song
  • Publication number: 20130202573
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Publication number: 20130203727
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
    Type: Application
    Filed: July 1, 2011
    Publication date: August 8, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
  • Patent number: 8461183
    Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: June 11, 2013
    Assignee: Genfit
    Inventors: Christophe Masson, Karine Caumont-Bertrand
  • Publication number: 20130129624
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Application
    Filed: January 7, 2013
    Publication date: May 23, 2013
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20130089502
    Abstract: A functional PET imaging method is disclosed for differentiation between bilateral hyperplasia and unilateral adenoma comprising (1) introducing a radioactively labelled CYP11 B2 (aldosterone synthase) inhibitor which binds selectively to CYP11 B2 (aldosterone synthase) relative to CYP11 B1 (11?-hydroxylase) into a mammal with adrenal glands and (2) conducting positron emission tomography (PET) in the region of the adrenal glands to obtain a functional PET image of the adrenal glands. Also disclosed are radioactive tracer compounds suitable for use in this method, precursors for making the same, and a process for making the radioactive tracer compounds capable of being conducted as a rapid one-pot reaction.
    Type: Application
    Filed: June 1, 2011
    Publication date: April 11, 2013
    Applicants: UNIVERSITAT DES SAARLANDES, JULIUS-MAXIMILIANS-UNIVERSITAT
    Inventors: Bruno Allolio, Stefanie Hahner, Andreas Schirbel, Rolf Hartmann, Christina Zimmer
  • Publication number: 20130045869
    Abstract: Complexes of herbicidal carboxylic acids and amine-containing polymers or oligomers are provided. These herbicidal complexes are useful for controlling unwanted plant growth. The herbicidal complexes have low solubility in water, low volatility relative to commercial compositions of the corresponding herbicidal carboxylic acids, and offer similar or improved herbicidal performance when compared to existing salts of the herbicidal carboxylic acids.
    Type: Application
    Filed: August 15, 2012
    Publication date: February 21, 2013
    Applicant: Dow AgroSciences LLC
    Inventors: Lei Liu, Hong Zhang, Alex Kennedy, Holger Tank, David G. Ouse, James M. Gifford, Min Zhao
  • Publication number: 20130023663
    Abstract: The present invention relates to stilbene and quinine compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis- or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BBOC amino acid esters are formed with the phenolic hydroxyl at the 3 -position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior stilbenes.
    Type: Application
    Filed: August 17, 2012
    Publication date: January 24, 2013
    Inventors: John Anthony Hadfield, Alan Thomson McGown, Stephen Patrick Mayalap, Edwar John Land, Ian Hamblett, Keira Gaukroger, Nicholas James Lawrence, Lucy Annette Hepworth, John Butler
  • Publication number: 20130005767
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120258924
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Applicant: INTERMUNE, INC.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • Patent number: 8273773
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 25, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
  • Patent number: 8227490
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 24, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20120178705
    Abstract: Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of ?-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells.
    Type: Application
    Filed: January 5, 2012
    Publication date: July 12, 2012
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventor: Pi-Hui LIANG
  • Publication number: 20120156212
    Abstract: The present invention relates to compounds as novel thymidylate synthase inhibitors, novel strategies to treat or prevent neoplasia in a subject, methods and compositions thereof.
    Type: Application
    Filed: May 29, 2010
    Publication date: June 21, 2012
    Inventors: David A. Ostrov, Carmen J. Allegra
  • Publication number: 20120021912
    Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: January 18, 2010
    Publication date: January 26, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20120009480
    Abstract: The electrolyte solution for a lithium ion secondary battery according to the present invention contains a nonaqueous solvent, a lithium salt and a compound represented by the general formula (Z) shown below. Thereby, a lithium ion secondary battery having high battery characteristics and simultaneously achieving a high safety as well can be provided. R—SO2—Ar1—O—R1??(Z) wherein Ar1 denotes a substituted or nonsubstituted divalent aromatic group having 5 to 30 atoms of the nucleus(es); R1 denotes a saturated or unsaturated monovalent hydrocarbon group having 1 to 20 carbon atoms; and R denotes a saturated or unsaturated monovalent hydrocarbon group having a perfluoroalkyl group and having 2 to 22 carbon atoms.
    Type: Application
    Filed: August 8, 2011
    Publication date: January 12, 2012
    Applicants: YAMAGUCHI UNIVERSITY, ASAHI KASEI E-MATERIALS CORPORATION
    Inventors: Asami OHASHI, Yoshiyuki ISHII, Hiroaki OKAMOTO, Yuki MORITA
  • Publication number: 20120004166
    Abstract: The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • Publication number: 20120004187
    Abstract: The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives, and to the physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, A and X are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • Publication number: 20110319449
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Application
    Filed: March 9, 2010
    Publication date: December 29, 2011
    Inventors: Saleem Ahmad, William N. Washburn, Andres S. Hernandez, Jeffrey A. Robl, Khehyong Ngu, Zhenghua Wang
  • Publication number: 20110281898
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Roger Victor Bonnert, Anil Patel, Stephen Thom
  • Publication number: 20110237791
    Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
    Type: Application
    Filed: April 6, 2011
    Publication date: September 29, 2011
    Applicants: TAISHO PHARMACEUTICAL CO., LTD, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takanori KAWAGUCHI, Kengo WATATANI, Keiko FUSEGI, Masahiro BOHNO, Hajime ASANUMA, Shoichi KURODA, Yudai IMAI, Tomomichi CHONAN, Nagaaki SATO, Shigeru TOKITA, Shigetada SASAKO, Takumi OKADA, Keishi HAYASHI, Shin ITOH, Noriko SAITO, Rui JIBIKI, Seishi ISHIYAMA, Hirofumi OTA
  • Patent number: 8013001
    Abstract: Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Christopher D. Bayne, Alan T. Johnson, Shao Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Jr., Haixia Wang, Yinong Xie
  • Patent number: 7998986
    Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: August 16, 2011
    Assignee: Exelixis Patent Company LLC
    Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Ronald C. Griffith
  • Publication number: 20110193022
    Abstract: Provided is a liquid crystal compound having general physical properties necessary for a compound, stability to heat, light or the like, a wide liquid crystal phase temperature range, a high clearing point, an excellent compatibility with other liquid crystal compounds, a large refractive index anisotropy and a large dielectric anisotropy. Provided are a liquid crystal composition including the liquid crystal compound, and a liquid crystal display device containing the liquid crystal composition. The compound is represented by formula (1): wherein, for example, R1 is alkyl having 1 to 20 carbons; at least one of the rings A1 to A6 is pyrimidine-2,5-diyl or pyridine-2,5-diyl and the others are 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z6 are a single bond; L1 to L4 is hydrogen or halogen; X1 is hydrogen, halogen, —C?N or alkyl having 1 to 10 carbons; and l, m, n, o, p and q are 0 or 1 and l+m+n+o+p+q=3.
    Type: Application
    Filed: October 14, 2009
    Publication date: August 11, 2011
    Applicants: JNC CORPORATION, CHISSO PETROCHEMICAL CORPORATION
    Inventors: Hiroyuki Tanaka, Kouki Sagou
  • Publication number: 20110195993
    Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
    Type: Application
    Filed: May 26, 2009
    Publication date: August 11, 2011
    Inventors: Christophe Masson, Karine Caumont-Bertrand
  • Publication number: 20110190227
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists Of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: August 4, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns, Jeffrey Roger Roppe
  • Patent number: 7981909
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: July 19, 2011
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20110166157
    Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: March 11, 2011
    Publication date: July 7, 2011
    Applicant: ALBIREO AB
    Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Per Olof Sjögren
  • Publication number: 20110144347
    Abstract: Provided is a process for the epimerization of the cis isomer of atovaquone, atovaquone intermediates and isomeric mixtures thereof into their corresponding trans-isomers resulting in higher yield of pure atovaquone.
    Type: Application
    Filed: June 30, 2008
    Publication date: June 16, 2011
    Applicant: CHEMAGIS LTD.
    Inventors: Fuqiang Zhu, Michel Bekhazi
  • Publication number: 20110112151
    Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than
    Type: Application
    Filed: February 25, 2009
    Publication date: May 12, 2011
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter
  • Publication number: 20110053974
    Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 3, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
  • Publication number: 20100298367
    Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
    Type: Application
    Filed: March 4, 2009
    Publication date: November 25, 2010
    Inventors: Sean P. Brown, Paul J. Dransfield, Jonathan Houze, Todd J. Kohn, Jiwen Liu, Julio Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Ming Yu, Liusheng Zhu
  • Publication number: 20100286206
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: September 12, 2008
    Publication date: November 11, 2010
    Applicants: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC., ADDEX PHARMA, S.A.
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James Macdonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
  • Publication number: 20100256199
    Abstract: The present invention relates to a polymorphic form of the compound 3-chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, methods of preparing it, pharmaceutical compositions and medicaments containing the same, and use of such polymorph, compositions and medicaments in the treatment or prevention of a condition caused by certain parasitic infections such as malaria, and in particular a condition caused by infection by Plasmodium falciparum
    Type: Application
    Filed: November 27, 2008
    Publication date: October 7, 2010
    Inventors: Pingyun Y. Chem, Ricky Couch
  • Publication number: 20100249139
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20100204256
    Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.
    Type: Application
    Filed: February 5, 2010
    Publication date: August 12, 2010
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Elisabetta Armani, Maurizio Delcanale
  • Publication number: 20100179137
    Abstract: [Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.
    Type: Application
    Filed: June 6, 2008
    Publication date: July 15, 2010
    Inventors: Takashi Kamikubo, Fukushi Hirayama, Masanori Miura, Yuriko Komiya, Takao Okuda, Keisuke Maki