The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/187)
  • Publication number: 20150133451
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 14, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki TAKAMI, Yusuke TOMINARI, Zenyu SHIOKAWA, Akito SHIBUYA, Yusuke SASAKI, Tony GIBSON, Terufumi TAKAGI
  • Publication number: 20150111933
    Abstract: The present invention relates to deuterated thiazolidinone analogues as agonists for follicle stimulating hormone receptor and their use for treating fertility disorders.
    Type: Application
    Filed: January 24, 2013
    Publication date: April 23, 2015
    Applicant: Merck Patent GmbH
    Inventors: Henry Yu, Marianne Donnelly
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150031733
    Abstract: The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.
    Type: Application
    Filed: April 26, 2013
    Publication date: January 29, 2015
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuya Yoshimoto, Teruki Takahashi, Daisuke Oohira, Shuhei Azuma
  • Patent number: 8940900
    Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
  • Publication number: 20140243366
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • 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: 20140128383
    Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Applicant: LABORATOIRE BIODIM
    Inventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
  • Publication number: 20140128499
    Abstract: A rubber composition for the manufacture of tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more thiazole compounds chosen from compounds having the following formula (I): Certain specific thiazole derivatives are described.
    Type: Application
    Filed: April 16, 2012
    Publication date: May 8, 2014
    Applicants: MICHELIN RECHERCHE ET TECHNIQUE S.A., COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN
    Inventors: Anne Veyland, Nicolas Seeboth
  • Publication number: 20140102540
    Abstract: A dye, having a structure represented by formula (1A): wherein A represents a group of atoms necessary for forming a ring together with the carbon-nitrogen bond; at least one of Y1A and Y2A represents an acidic group, in which when they each represent an acidic group, they may be the same as or different from each other, or when only one of them represents an acidic group, the other represents an electron-withdrawing group; D represents a group to give a dye; n represents an integer of 1 or greater; L represents a single bond or a divalent linking group; and Y3A represents an acidic group.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Katsumi KOBAYASHI, Keizo KIMURA, Tatsuya SUSUKI, Hirotaka SATOU, Yukio TANI
  • Publication number: 20140107153
    Abstract: Disclosed herein is a stable compound having a structure: therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: December 13, 2013
    Publication date: April 17, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello, Michael E. Garst
  • Patent number: 8680339
    Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: March 25, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140030223
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
  • Publication number: 20130316906
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: October 28, 2011
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
  • Patent number: 8569302
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: October 29, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
  • Publication number: 20130237573
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
  • Patent number: 8497382
    Abstract: A compound represented by the formula (I) wherein R1 and R2 are each a hydrogen atom, an alkyl group and the like, R3 is a hydrogen atom, an alkyl group and the like, R4 is a hydrogen atom, an alkyl group and the like, m is an integer of 0 to 3, X is a bond, an oxygen atom or a sulfur atom, Y is a carbonyl group, a hydroxymethylene group and the like, and Z is a halogen atom, an alkyl group, an aryl group, a heteroaryl group and the like, or a pharmaceutically acceptable salt thereof has a superior PPAR? agonist action and a lipid-lowering action, and is useful as a prophylactic or therapeutic drug for hyperlipidemia and the like.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: July 30, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventor: Naoko Ando
  • Publication number: 20130184318
    Abstract: The present invention provides methods of determining the effect of test agents on the compliance of trabecular meshwork (TM) tissue, at the level of the extracellular matrix (ECM) and/or cells within the TM. Agents that modulate (e.g., increase or decrease) compliance of the TM tissue find use. Agents that increase the compliance of ECM and TM cells within the TM find use in the treatment and prevention of eye disorders characterized by high intraocular pressure, e.g., glaucoma.
    Type: Application
    Filed: April 28, 2011
    Publication date: July 18, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Paul Russell, Christopher J. Murphy
  • Patent number: 8450304
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: May 28, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
  • Publication number: 20120295920
    Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
    Type: Application
    Filed: December 10, 2010
    Publication date: November 22, 2012
    Inventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
  • Publication number: 20120196838
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
  • Publication number: 20120129893
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: January 12, 2012
    Publication date: May 24, 2012
    Inventors: Jacques DUMAS, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Wendy Lee, Aniko Redman, Robert Sibley, Joel Renick
  • Publication number: 20120122780
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and 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: May 20, 2010
    Publication date: May 17, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet
  • Publication number: 20120028800
    Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: January 25, 2010
    Publication date: February 2, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20110319416
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Application
    Filed: January 28, 2010
    Publication date: December 29, 2011
    Applicant: EMORY UNIVERSITY
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Cara Mosley, Timothy M. Acker, Sommer Zimmerman
  • Publication number: 20110257379
    Abstract: A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Inventor: Hsin-Hsien Wu
  • Publication number: 20110237630
    Abstract: A compound represented by the formula (I) wherein R1 and R2 are each a hydrogen atom, an alkyl group and the like, R3 is a hydrogen atom, an alkyl group and the like, R4 is a hydrogen atom, an alkyl group and the like, m is an integer of 0 to 3, X is a bond, an oxygen atom or a sulfur atom, Y is a carbonyl group, a hydroxymethylene group and the like, and Z is a halogen atom, an alkyl group, an aryl group, a heteroaryl group and the like, or a pharmaceutically acceptable salt thereof has a superior PPAR? agonist action and a lipid-lowering action, and is useful as a prophylactic or therapeutic drug for hyperlipidemia and the like.
    Type: Application
    Filed: December 1, 2009
    Publication date: September 29, 2011
    Inventor: Naoko Ando
  • Patent number: 8026370
    Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: September 27, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
  • Publication number: 20110230521
    Abstract: Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: May 1, 2009
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Christian Harcken, Thomas Wai-Ho Lee, Pingrong Liu, John Lord, CAN Mao, Wang Mao, Brain Christopher Raudenbush, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer
  • Patent number: 8003678
    Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: August 23, 2011
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Publication number: 20110201616
    Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
    Type: Application
    Filed: June 22, 2009
    Publication date: August 18, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
  • 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
  • Publication number: 20110178092
    Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: December 19, 2007
    Publication date: July 21, 2011
    Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
  • Publication number: 20110136880
    Abstract: Latrunculin derivatives are disclosed, as are anti-invasive and cytotoxic uses for latrunculins and latrunculin derivatives, and semisyntheses of latrunculin derivatives. The latrunculins and latrunculin derivatives are useful, for example, in treating cancers.
    Type: Application
    Filed: December 6, 2010
    Publication date: June 9, 2011
    Inventors: Khalid El Sayed, Mohammad Khanfar
  • Publication number: 20110105488
    Abstract: The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.
    Type: Application
    Filed: March 20, 2009
    Publication date: May 5, 2011
    Applicant: Chlorion Pharma, Inc.
    Inventors: Giorgio Attardo, Sasmita Tripathy
  • Publication number: 20110071175
    Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: December 12, 2008
    Publication date: March 24, 2011
    Inventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara A. Vitabile-Woo, Mathias Domostoj
  • Publication number: 20110034450
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: April 6, 2009
    Publication date: February 10, 2011
    Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFT
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20110034507
    Abstract: The present invention relates to farnesoid X receptors (FXR, NR1H4). FXR is a member of the nuclear receptor class of ligand-activate transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same. Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome.
    Type: Application
    Filed: June 13, 2008
    Publication date: February 10, 2011
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Adwoa Akwabi-Ameyaw, David Norman Deaton, Robert Blount McFadyen, Frank Navas, III
  • Patent number: 7879892
    Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: February 1, 2011
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
  • Publication number: 20110020278
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: July 19, 2010
    Publication date: January 27, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
  • Publication number: 20100279868
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.
    Type: Application
    Filed: June 26, 2008
    Publication date: November 4, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Stephane Andre Marie Jeanmart, Christopher John Mathews, Steve Smith, John Benjamin Taylor, Mangala Govenkar
  • Publication number: 20100273739
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Publication number: 20100273724
    Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.
    Type: Application
    Filed: July 7, 2010
    Publication date: October 28, 2010
    Applicant: CARDIOME PHARMA CORP.
    Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M.C. Plouvier, Aregahegn S. Yifru
  • Publication number: 20100267688
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: April 15, 2010
    Publication date: October 21, 2010
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
  • Publication number: 20100222326
    Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 24, 2008
    Publication date: September 2, 2010
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
  • Patent number: 7786119
    Abstract: This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R1, R2, R3, R4, R5, LB, L and DM are defined herein, including isolated enantiomeric and diastereomeric isomers thereof, and mixtures thereof. Pharmaceutical compositions and methods of use are also disclosed.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: August 31, 2010
    Assignee: Cardiome Pharma Corp.
    Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M. C. Plouvier, Aregahegn S. Yifru
  • Publication number: 20100210524
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Application
    Filed: July 21, 2008
    Publication date: August 19, 2010
    Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
  • Publication number: 20100197917
    Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.
    Type: Application
    Filed: March 18, 2010
    Publication date: August 5, 2010
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
  • Publication number: 20100137371
    Abstract: The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
    Type: Application
    Filed: August 8, 2006
    Publication date: June 3, 2010
    Inventors: Carl Berthelette, Claude Dufresne, Lianhai Li, zhaoyin Wang