Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
  • Publication number: 20140057920
    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, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140057951
    Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
    Type: Application
    Filed: February 19, 2013
    Publication date: February 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: Bayer Intellectual Property GmbH
  • Patent number: 8658675
    Abstract: The invention relates to pyridine derivatives of Formula (I), wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: February 25, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
  • Patent number: 8658659
    Abstract: The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: February 25, 2014
    Assignees: AB Science, Centre National de la Recherche Scientifique (CNRS), Institut Curie
    Inventors: David Grierson, Abdellah Benjahad, Alain Moussy, Martine Croisy
  • Patent number: 8658661
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to 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: Grant
    Filed: August 12, 2011
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, John D. Huber, Ho Yin Lo, Pui Leng Loke, Weimin Liu, Tina Marie Morwick, Alan Olague, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20140051575
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Application
    Filed: March 30, 2012
    Publication date: February 20, 2014
    Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Anne-Sophie Rebstock, Ulrike Wachendorff-Neumann
  • Patent number: 8653062
    Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Publication number: 20140045900
    Abstract: A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.
    Type: Application
    Filed: October 12, 2011
    Publication date: February 13, 2014
    Applicant: Bial-Portela & CA, S.A.
    Inventors: Patricio Manuel Vieira Araujo Soares Da Silva, Teresa Lucia Silva Pereira Nunes, Lyndon Christopher Wright, Pedro Nuno Leal Palma, David Alexander Learmonth
  • Publication number: 20140045800
    Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Application
    Filed: February 4, 2013
    Publication date: February 13, 2014
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20140045902
    Abstract: The present invention relates to a compound of formula 1 or 2 wherein R1 represents straight-chain or branched C2-C8 alkyl, C2-C8 alkenyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group, or C2-C4 alkynyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group; and R2 represents hydroxyl, C1-C6 alkyl, C1-C6 alkylcarbonyl, di(C1-C6-alkyl)aminomethyl, C3-C6 heterocyclylmethyl or arylaminomethyl, wherein the aryl group is optionally substituted by at least one substituent selected from the group consisting of halogens and C1-C6 alkoxy as well as associated pharmaceutical compositions and uses of the compound or composition in therapy, in particular for the treatment of a disorder or a disease susceptible to inhibition of COX-2.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: KING SAUD UNIVERSITY
    Inventors: Fars K. Alanazi, Awwad A. Radwan, Ibrahim A. Alsarra
  • Publication number: 20140045795
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 13, 2014
    Applicant: SYNTA PHARMACEUTICALS CORPORATION
    Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
  • Patent number: 8648081
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: February 11, 2014
    Assignee: Eli Lilly and Company
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Publication number: 20140039009
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 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: Application
    Filed: October 15, 2013
    Publication date: February 6, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhiqiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Publication number: 20140039013
    Abstract: The present invention provide chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit host targeting functions in insects such as mosquitoes. Method of employing such agents, and articles incorporating the same, are also provided.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 6, 2014
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Patrick L. Jones
  • Publication number: 20140038821
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Publication number: 20140031310
    Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising combinations of beneficial ingredients that in alternative embodiments are serviceable as therapies or palliatives for treating, preventing or improving conditions, states and disease symptoms involving the use of targeted protein kinase inhibitors such as Multi-Kinase Inhibitors (MKIs) or Epidermal Growth Factor Receptor (EGFR) Inhibitors (EGFRIs), or the use of other oral oncolytics, such as capcitabine or erlotinib, known to be associated with drug-induced dermatological toxicity, e.g.
    Type: Application
    Filed: January 18, 2012
    Publication date: January 30, 2014
    Inventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
  • Publication number: 20140031335
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 30, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee Lee, Jung Taek Oh, JaeKwang Lee, JaeWon Lee, Suyeal Bae, Nina Ha, Sera Lee
  • Publication number: 20140031353
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Application
    Filed: January 30, 2011
    Publication date: January 30, 2014
    Applicant: CUREGENIX, INC.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Publication number: 20140031374
    Abstract: The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear ?-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
    Type: Application
    Filed: December 8, 2011
    Publication date: January 30, 2014
    Applicant: OSLO University Hospital, HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss, Andrey Edward Voronkov
  • Patent number: 8637674
    Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: January 28, 2014
    Assignee: EWHA University-Industry Collaboration Foundation
    Inventors: Yun Soo Bae, Jee Hyun Lee, Mi Sun Seo, Soo Young Lee, Sun Choi, Kee In Lee, Hye Rin Bin
  • Patent number: 8637559
    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: Grant
    Filed: November 14, 2006
    Date of Patent: January 28, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata
  • Publication number: 20140024639
    Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • Publication number: 20140024649
    Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
    Type: Application
    Filed: October 10, 2011
    Publication date: January 23, 2014
    Applicants: Auckland UniServices Limited, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
  • Publication number: 20140024682
    Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 23, 2014
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel V. A. Soares da Silva
  • Publication number: 20140024665
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: June 5, 2013
    Publication date: January 23, 2014
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20140024648
    Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Application
    Filed: March 6, 2012
    Publication date: January 23, 2014
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Marjo Pihlavisto, David Smith, Auni Juhakoski, Ferenc Fulop, Laszlo Lazar, Istvan Szatmari, Ferenc Miklos, Zsolt Szakonyi, Lorand Kiss, Marta Palko
  • Patent number: 8633222
    Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: January 21, 2014
    Assignee: Targacept, Inc.
    Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve, Craig Harrison Miller
  • Patent number: 8633134
    Abstract: The invention relates to substituted amidine compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amidine compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted amidine compounds. The substituted amidine compounds of the present invention are defined by the following formula I: wherein A1 to A4, B1 to B3, R1 to R3, (R4)p, (R5)q, X and Y are defined as in the description.
    Type: Grant
    Filed: December 14, 2009
    Date of Patent: January 21, 2014
    Assignee: BASF SE
    Inventors: Florian Kaiser, Karsten Koerber, Matthias Pohlman, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Wolfgang von Deyn, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Cecille Ebuenga
  • Patent number: 8629165
    Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: January 14, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Patent number: 8623875
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: January 7, 2014
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Publication number: 20140005229
    Abstract: Provided is a fungicidal aqueous suspension composition for agriculture and horticulture, comprising: a component (A) in the form of a specific oxime compound, salt thereof or N-oxide thereof, a component (B) in the form of at least one type of compound selected from the group consisting of a polyoxyalkylene alkyl ether, polyoxyalkylene fatty acid ester, polyoxyalkylene sorbitan fatty acid ester and silicone-based surfactant, and a component (C) in the form of at least one type of compound selected from the group consisting of a nonionic surfactant and anionic surfactant other than component (B).
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Applicant: NIPPON SODA CO., LTD
    Inventors: Rieko Nakamura, Tomoyuki Saiga, Satoshi Fujii
  • Publication number: 20140005212
    Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 2, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
  • Publication number: 20140005230
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Application
    Filed: March 13, 2012
    Publication date: January 2, 2014
    Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8618137
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5, A, W, X, G, Z, J and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 31, 2013
    Assignee: E I du Pont de Nemours and Company
    Inventor: Robert James Pasteris
  • Patent number: 8618112
    Abstract: Novel crystalline salts of 3-[4-(3-ethanesulfonyl-propyl)-bicyclo[2.2.2]oct-1-yl]-4-methyl-5-(2-trifluoromethyl-phenyl)-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph E. Lynch, Yuri Y. Bereznitski, Frederick T. Mattrey, John L. Leazer, Jr., Russell R. Ferlita, Jinchu Liu, Jungjun Yin, Robert M. Wenslow, Jr.
  • Patent number: 8618304
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: December 31, 2013
    Assignee: Sanofi
    Inventors: Josef Pernerstorfer, Heinz-Werner Kleemann, Matthias Schaefer, Alena Safarova, Marcel Patek
  • Patent number: 8618139
    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: Grant
    Filed: November 11, 2011
    Date of Patent: December 31, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Publication number: 20130345241
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
    Type: Application
    Filed: August 30, 2013
    Publication date: December 26, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
  • Publication number: 20130345193
    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: August 23, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130345221
    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 vertebrates.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: NOVARTIS AG
    Inventors: Noëlle Gauvry, Steve Nanchen
  • Patent number: 8614233
    Abstract: A compound of Formula, (I) or Formula: (II).
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: December 24, 2013
    Assignee: Universite de Montreal
    Inventors: Christophe Pardin, Jeffrey W. Keillor, William D. Lubell
  • Patent number: 8614217
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: December 24, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Publication number: 20130338112
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: August 1, 2013
    Publication date: December 19, 2013
    Inventors: Zachary Demko, Christopher Borella, Shoujun Chen, Lijun Sun
  • Publication number: 20130338195
    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: Application
    Filed: June 20, 2013
    Publication date: December 19, 2013
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20130338196
    Abstract: Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 19, 2013
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20130338155
    Abstract: The present invention relates to compounds that inhibit the activity of Hsp90 and methods of using these compounds for treating or preventing infection.
    Type: Application
    Filed: June 4, 2013
    Publication date: December 19, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: Weiwen Ying
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20130331416
    Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.
    Type: Application
    Filed: July 25, 2013
    Publication date: December 12, 2013
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares da Silva