Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/462)
  • Patent number: 9840511
    Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV: formula (I).
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: December 12, 2017
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow
  • Patent number: 9421208
    Abstract: Described herein are combinations of ACK inhibitors and HDAC inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: August 23, 2016
    Assignee: Pharmacyclics LLC
    Inventor: Sriram Balasubramanian
  • Patent number: 9382225
    Abstract: The present invention relates to a method of reducing a C—O bond to the corresponding C—H bond in a substrate which could be a benzylic alcohol, allylic alcohol, ester, or ether or an ether bond beta to a hydroxyl group or alpha to a carbonyl group.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: July 5, 2016
    Assignee: Kat2Biz AB
    Inventors: Joseph Samec, Anna Lundstedt, Supaporn Sawadjoon
  • Patent number: 9315482
    Abstract: The invention relates to compounds of formula (I) for use in the prevention and/or treatment of viral infections: Wherein X, Y, Z, T, R1a and R1b are as defined in claim 1.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: April 19, 2016
    Assignees: Institut Pasteur, Centre National de la Recherche Scientifique, Institut Curie
    Inventors: Pierre-Olivier Vidalain, Marianne Lucas-Hourani, Frédéric Tangy, Hélène Munier-Lehmann, Daniel Dauzonne
  • Patent number: 9181514
    Abstract: The present invention is directed to novel fragrance compounds and their unexpected advantageous use in improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the compounds, wherein the compounds are represented by the following formula: wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen and methyl; and R4 is a C1-C3 alkyl group.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: November 10, 2015
    Assignee: International Flavors & Fragrances, Inc.
    Inventors: Anthony T. Levorse, Jr., Nicole L. Giffin, Robert P. Belko, Michael G. Monteleone
  • Patent number: 9040727
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: May 26, 2015
    Assignees: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-Think Pharmaceutical Co., Ltd., Sinopharm A-Think Medical and Pharmaceutical Research & Development (Beijing) Co., Ltd.
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Patent number: 8975277
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf
  • Publication number: 20150057238
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
  • Publication number: 20150057207
    Abstract: The present invention relates to novel compounds and their use as fragrance materials.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Inventors: Benjamin Amorelli, Edward Mark Arruda, Robert P. Belko, Tingwei Cai, Adam P. Closson, Nicole L. Giffin, Gary J. Mertz, Michael G. Monteleone
  • Patent number: 8952185
    Abstract: Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: February 10, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mitsuhisa Yamano, Mitsutaka Goto, Takahiro Konishi
  • Patent number: 8927594
    Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: January 6, 2015
    Assignees: National Sun Yat-Sen University, National Museum of Marine Biology & Aquarium
    Inventors: Jyh-Horng Sheu, Wei-Hsien Wang, Zhi-Hong Wen, Bo-Wei Chen, Ping-Jyun Sung
  • Publication number: 20140336102
    Abstract: The present invention is directed to novel diethyl-methyl-hexahydro-isobenzofuran compounds and a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of these novel compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: November 13, 2014
    Inventors: Adam P. Closson, Ryan D. Oesterle, Nicole L. Giffin, Michael G. Monteleone
  • Publication number: 20140336376
    Abstract: Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. In the formula, Ar is an aromatic carbocyclic ring or a heterocyclic ring; and Ar2 is represented by any one of the following rings and the like.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 13, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tadakiyo NAKAGAWA, Kayo Matsumoto, Sen Takeshita, Tomomi Yoshida, Munetaka Tokumasu, Hiroki Inoue, Kaori Kobayashi
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Publication number: 20140296120
    Abstract: The present invention is directed to novel fragrance compounds and their unexpected advantageous use in improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the compounds, wherein the compounds are represented by the following formula: wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen and methyl; and R4 is a C1-C3 alkyl group.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Anthony T. Levorse, JR., Nicole L. Giffin, Robert P. Belko, Michael G. Monteleone
  • Patent number: 8835659
    Abstract: The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: September 16, 2014
    Assignees: Ikerchem, S.L., Universidad del Pais Vasco
    Inventors: Fernando Pedro Cossio Mora, Leire Lidia Arias Echeverría, Yosu Ion Vara Zalazar, Eneko Aldaba Arévalo, Eider San Sebastián Larzabal, Aizpea Zubia Olascoaga
  • Patent number: 8809376
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: August 19, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Stefan Peters
  • Patent number: 8703966
    Abstract: A method of catalytic oxidative coupling for the formation of hetero-coupled bis-arenes. The method includes placing a solvent, an arene compound, and a catalyst in a reactor having a oxidant atmosphere such that hetero-coupled bis-arenes are formed.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: April 22, 2014
    Assignee: Board of Governors for Higher Education, State of Rhode Island and Providence Plantations
    Inventor: Brenton DeBoef
  • Publication number: 20140107139
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: June 7, 2012
    Publication date: April 17, 2014
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
  • Patent number: 8669271
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: March 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Niklas Heine, Elke Langkopf, Bernd Nosse
  • Patent number: 8642585
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • Publication number: 20140024671
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 23, 2014
    Inventors: Michael EISSENSTAT, Dehui DUAN
  • Publication number: 20130345444
    Abstract: Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like.
    Type: Application
    Filed: February 16, 2012
    Publication date: December 26, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Mitsuhisa Yamano, Mitsutaka Goto, Takeshi Kajiwara, Hiroyuki Maeda, Takahiro Konishi, Misayo Sera, Yuichiro Kondo, Seiji Yamasaki
  • Publication number: 20130345445
    Abstract: The present invention relates to a method of reducing a C—O bond to the corresponding C—H bond in a substrate which could be a benzylic alcohol, allylic alcohol, ester, or ether or an ether bond beta to a hydroxyl group or alpha to a carbonyl group.
    Type: Application
    Filed: March 8, 2012
    Publication date: December 26, 2013
    Applicant: KAT2BIZ AB
    Inventors: Joseph Samec, Anna Lundstedt, Supaporn Sawadjoon
  • Patent number: 8608977
    Abstract: The present invention relates to compounds of the general formula I in which the variables are each defined as follows: W is a (Y4-T2-)s(Y3-A2-)tY2—Z2 moiety, Z1, Z2 are each independently unreactive radicals as defined more specifically in the description or reactive radicals through which polymerization can be brought about, A1, A2 are each independently spacers as defined more specifically in the description, Y1 to Y5 are linking units as defined more specifically in the description, Y6 is a chemical single bond or —CO—, T1, T2 are each independently, as defined more specifically in the description, divalent saturated or unsaturated, optionally substituted and optionally fused iso- or heterocyclic radicals, Q is substituents as defined more specifically in the description, r, t are each independently 0 or 1, s is 0, 1, 2 or 3 and q is 0, 1, 2, 3 or 4.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: December 17, 2013
    Assignee: BASF SE
    Inventors: Olivier Enger, Markus Hoffmann, Jochen Brill, Stephan Maurer, Bernd Ziegler
  • Patent number: 8603357
    Abstract: The present inventions to provide a novel polymerizable chiral compound (chiral agent) having high helical twisting power, a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound, a liquid crystal polymer, and an optically anisotropic body.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: December 10, 2013
    Assignee: Zeon Corporation
    Inventors: Kei Sakamoto, Kentaro Tamura
  • Patent number: 8598374
    Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: December 3, 2013
    Assignee: Metabolex, Inc.
    Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Fayek Nashashibi, Xin Chen, Phuongly Pham
  • Publication number: 20130316938
    Abstract: Provided is class of compounds of formula (I) wherein X, R1, R2 and R3 have the same meaning as given in the specification capable of releasing fragrant compounds in a controlled manner into the surroundings.
    Type: Application
    Filed: December 23, 2011
    Publication date: November 28, 2013
    Applicant: GIVAUDAN S.A.
    Inventors: Corinne Baumgartner, Felix Flachsmann, Philip Kraft
  • Publication number: 20130289074
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: April 24, 2013
    Publication date: October 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Matthias ECKHARDT, Elke LANGKOPF, Stefan PETERS
  • Publication number: 20130281453
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 24, 2013
    Applicant: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
  • Patent number: 8558017
    Abstract: Chiral ruthenium catalysts comprising salen and alkenyl ligands are provided for stereoselective cyclopropanation, and methods of cyclopropanation are provided. The chiral ruthenium catalyst is prepared in situ by combining an alkenyl ligand, a deprotonated chiral salen ligand, and a ruthenium (II) metal. A preferred catalyst is prepared in situ by combining 2,3-dihydro-4-venylbenzofuran,deprotonated 1,2-cyclohexanediamino-N,N?-bis(3,5-di-t-butyl-salicylidene) and RuCl2(p-cymene)]2.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: October 15, 2013
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: David E. Pereira, Wade Aumiller, Raymond Dagger
  • Publication number: 20130267510
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2011
    Publication date: October 10, 2013
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
  • Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130237571
    Abstract: The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
    Type: Application
    Filed: July 20, 2011
    Publication date: September 12, 2013
    Applicant: Conexios Life Sciences PVT. LTD.
    Inventors: Jagannath Madanahalli Ranganath Rao, Nagarajan Arumugam, Mohd Mudabbir Ansari, Chandrasekhas Gudla, Shanmugam Pachiyappan, Manivannan Ramalingam, Jenson George, George Fernanda Arul, Kenchegowda Bommegowda, Y, Sathesh Kumar Angupillai, Ramamoorthy Kottamalai, Pradeep Jidugu, Shivanageshwara Rao, D
  • Publication number: 20130237536
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 8518302
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula I wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: August 27, 2013
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Publication number: 20130217704
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 22, 2013
    Inventor: Sequoia Pharmaceuticals, Inc.
  • Publication number: 20130203688
    Abstract: The present document describes a nutraceutical or cosmeceutical composition for the prophylaxis of an ailment comprising a therapeutically effective amount of a sugar plant syrup filtration residue in association with a pharmaceutically acceptable carrier. The present document also describes a nutraceutical or cosmeceutical composition for improving health condition of skin. The present document describes a method of producing a sugar plant syrup-derived product; wherein the improvement is characterized in the step of: collecting a sugar plant syrup residue during the production of sugar or syrup to produce a syrup-derived by-product.
    Type: Application
    Filed: August 19, 2011
    Publication date: August 8, 2013
    Applicant: FÉDÉRATION DES PRODUCTEURS ACÉRI-COLES DU QUÉBEC
    Inventors: Julie Barbeau, Geneviève Béland
  • Publication number: 20130158261
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: TaiMed Biologics, Inc.
    Inventor: TaiMed Biologics, Inc.
  • Patent number: 8460583
    Abstract: There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO2, P, PO, PO2, and SiR2; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R1 through R10 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO3R2, —OPO3R2, or CN.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: June 11, 2013
    Assignee: E I du Pont de Nemours and Company
    Inventors: Hong Meng, Dengfu Wang
  • Publication number: 20130131351
    Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
    Type: Application
    Filed: October 5, 2012
    Publication date: May 23, 2013
    Applicant: Metabolex, Inc.
    Inventor: Metabolex, Inc.
  • Patent number: 8410293
    Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 2, 2013
    Assignee: BASF SE
    Inventors: Klaus Ebel, Bernhard Brunner, Christoph Stock, Ralf Pelzer
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20130029846
    Abstract: The present invention relates to the use of bicyclic amidine compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to novel bicyclic amidines and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: March 28, 2011
    Publication date: January 31, 2013
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
  • Publication number: 20130023662
    Abstract: Chiral ruthenium catalysts comprising salen and alkenyl ligands are provided for stereoselective cyclopropanation, and methods of cyclopropanation are provided. The chiral ruthenium catalyst is prepared in situ by combining an alkenyl ligand, a deprotonated chiral salen ligand, and a ruthenium (II) metal. A preferred catalyst is prepared in situ by combining 2,3-dihydro-4-venylbenzofuran, deprotonated 1,2-cyclohexanediamino-N,N?-bis(3,5-di-t-butyl-salicylidene) and RuCl2(p-cymene)]2.
    Type: Application
    Filed: December 12, 2011
    Publication date: January 24, 2013
    Applicant: VANDA PHARMECEUTICALS INC.
    Inventors: David E. Pereira, Wade Aumiller, Raymond Dagger
  • Publication number: 20130005994
    Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.
    Type: Application
    Filed: June 28, 2012
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Klaus Ebel, Bernhard Brunner, Christoph Stock, Ralf Pelzer
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Publication number: 20120316230
    Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.
    Type: Application
    Filed: February 15, 2012
    Publication date: December 13, 2012
    Inventors: Giancarlo Naccari, Sergio Baroni
  • 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
  • Patent number: 8309600
    Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: November 13, 2012
    Assignee: Metabolex Inc.
    Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen