Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
  • Publication number: 20140142074
    Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
  • Publication number: 20140142105
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: NOVARTIS AG
    Inventors: Christina Hebach, Emilie Joly, Joerg Kallen, James Gilbert Ternois, Marina Tintelnot-Blomley
  • Patent number: 8729271
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 20, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
  • Patent number: 8729104
    Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: May 20, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Ihor E. Kopka, Bing Li, Anthony K. Ogawa, Feroze Ujjainwalla
  • Patent number: 8729105
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: May 20, 2014
    Assignee: Hoffmann La-Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Patent number: 8729103
    Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: May 20, 2014
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar
  • Patent number: 8729107
    Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: May 20, 2014
    Assignee: Purdue Research Foundation
    Inventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
  • Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • Publication number: 20140135364
    Abstract: Pesticidal compositions and their uses are disclosed.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
  • Publication number: 20140134262
    Abstract: The present invention provides a compound of Formula I: for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride level; wherein R1, X1, R7, R5, C, L and p are defined herein. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride levels.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 15, 2014
    Inventors: Yoshie Arai, Margaret Elizabeth Brousseau, Jessie Gu, Tomoko Hayashi, Hironobu Mitani, Muneto Mogi, Kazuhiko Nonomura, Ken Yamada
  • Publication number: 20140135329
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 15, 2014
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20140128363
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140128427
    Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
  • Publication number: 20140128397
    Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 8, 2014
    Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
  • Publication number: 20140120147
    Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: NOVARTIS AG
    Inventors: Steve NANCHEN, Noelle GAUVRY, Thomas GOEBEL
  • Publication number: 20140121194
    Abstract: There is provided a method for controlling an animal ectoparasite having excellent controlling effects. The method for controlling an ectoparasite of dogs comprises orally administering an ectoparasite-controlling agent comprising as an active ingredient an isoxazoline compound represented by formula (I): wherein X1 represents a halogen atom or a C1-C3 haloalkyl, X2 represents a hydrogen atom, a halogen atom or a C1-C3 haloalkyl, X3 represents a hydrogen atom or a halogen atom, Q represents, for example, Q1, A1 represents R11—C(?O)—N(R12)—N(R13)—, R11—C(?O)—N(R12)—CH2— or R11—C(?O)—N(R12)—, and R10 represents a hydrogen atom, a halogen atom or a C1-C3 alkyl group, to a dog in a period from 30 minutes immediately before the start of feeding to 120 minutes after the end of feeding.
    Type: Application
    Filed: October 17, 2013
    Publication date: May 1, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kaori IKARI, Naonobu NISHIGUCHI
  • Patent number: 8710231
    Abstract: There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1? and casein kinase 1?. In addition, the present inhibitor inhibits casein kinase 1? and casein kinase 1?, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1? or casein kinase 1? is associated. There is further provided a pharmaceutical agent useful for the treatment of, particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1? and casein kinase 1? comprising, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom which is fluorine, chlorine, bromine or iodine.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: April 29, 2014
    Assignees: Pharmadesign, Inc., NB Health Laboratory Co., Ltd.
    Inventors: Masako Okamoto, Kiyoshi Takayama
  • Patent number: 8710083
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: April 29, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Zhi-Qiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
  • Patent number: 8710084
    Abstract: The present invention provide a tetrazolyl oxime derivative represented by formula (1) (in formula (1), X represents a halogen atom or the like, n1 represents an integer of 0 to 5, A represents a tetrazolyl group, Het represents a group represented by formula (4) or the like, in formula (4), R represents a halogen atom or the like, n2 represents an integer of 0 to 3, Z represents a group represented by formula (a), in formula (a), R50-R53 represents a hydrogen atom or the like, n3 represents an integer of 0 to 2, n4 represents 1 or 2, n5 represents 0 or 1) or salt thereof, and a plant disease control agent containing the same as an active ingredient.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: April 29, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
  • Patent number: 8710055
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: April 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Steffen Steurer
  • Publication number: 20140113931
    Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 24, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20140107057
    Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140107056
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 8697715
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: April 15, 2014
    Assignees: Array BioPharma, Inc., Genentech, Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Patent number: 8697732
    Abstract: The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: April 15, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
  • Patent number: 8697704
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: April 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
  • Patent number: 8697733
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: April 15, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20140100108
    Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.
    Type: Application
    Filed: March 26, 2012
    Publication date: April 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
  • Publication number: 20140100226
    Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
    Type: Application
    Filed: December 12, 2013
    Publication date: April 10, 2014
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru OKADA, Masaya KATO, Norifumi SATO, Tetsuyuki UNO, Hideki KITAGAKI, Junpei HARUTA, Hidetaka HIYAMA, Tomonori SHIBATA
  • Patent number: 8691821
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 8, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • Publication number: 20140094462
    Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 3, 2014
    Inventors: Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye
  • Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Publication number: 20140088071
    Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: November 2, 2011
    Publication date: March 27, 2014
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
  • Publication number: 20140088148
    Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.
    Type: Application
    Filed: April 4, 2012
    Publication date: March 27, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith
  • Publication number: 20140087943
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.
    Type: Application
    Filed: September 24, 2013
    Publication date: March 27, 2014
    Applicant: BASF SE
    Inventors: Karsten KOERBER, Florian KAISER, Juergen LANGEWALD
  • Patent number: 8680269
    Abstract: The present invention concerns novel heteroaryl-N-aryl thiosemicarbazones and their use in pest control, as insecticides and aca?cides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: March 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
  • Publication number: 20140079667
    Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 20, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Patent number: 8673911
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: March 18, 2014
    Assignee: MethylGene Inc.
    Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
  • Patent number: 8674109
    Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: March 18, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
  • Patent number: 8673941
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • Publication number: 20140073634
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 13, 2014
    Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
    Inventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
  • Publication number: 20140073650
    Abstract: Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e.
    Type: Application
    Filed: September 24, 2013
    Publication date: March 13, 2014
    Applicant: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Harshani R. Lawrence, Said M. Sebti, Sevil Ozcan
  • Publication number: 20140066424
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 6, 2014
    Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
    Inventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
  • Publication number: 20140066483
    Abstract: Disclosed herein is a method of upregulating regulatory T-cells, and treating diseases that would benefit from such upregulation, by administering an alpha 2 receptor agonist.
    Type: Application
    Filed: November 4, 2013
    Publication date: March 6, 2014
    Applicant: Allergan, Inc.
    Inventors: Daniel W. Gil, John E. Donello, Veena Viswanath, Lauren M.B. Luhrs
  • Publication number: 20140057919
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: Pfizer Inc.
    Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
  • Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140057952
    Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 27, 2014
    Applicant: ALLERGAN, INC.
    Inventors: WENKUI K. FANG, Liming Wang, Evelyn G. Corpuz, Ken Chow, WhaBin Im
  • Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • Publication number: 20140057892
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD) heart failure, ischemia, and anemia.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: Akebia Therapeutics, Inc.
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon