1,2-oxazoles (including Hydrogenated) Patents (Class 546/272.1)
-
Publication number: 20120196861Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
-
Publication number: 20120196905Abstract: Methods and small molecule compounds for smoking and CNS disease harm reduction are provided.Type: ApplicationFiled: August 5, 2011Publication date: August 2, 2012Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventor: John R. CASHMAN
-
Patent number: 8231888Abstract: 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: GrantFiled: June 9, 2011Date of Patent: July 31, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
-
Patent number: 8227461Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 23, 2010Date of Patent: July 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20120184538Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 10, 2012Publication date: July 19, 2012Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
-
Patent number: 8222246Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: March 29, 2010Date of Patent: July 17, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
-
Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
-
Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
-
Patent number: 8207203Abstract: This invention offers isoxazole derivatives represented by the following formula (I) in which R1 and R2 each stands for hydrogen, lower alkyl, amino and the like; R3 stands for substituted or unsubstituted aryl or hetero aryl; R4 stands for hydrogen or lower alkyl; R5 stands for substituted or unsubstituted phenyl, furyl and the like; and Y stands for —CH2—, —CO—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.Type: GrantFiled: June 26, 2007Date of Patent: June 26, 2012Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Koichi Hasumi, Shuji Ohta, Takahisa Saito, Shuichiro Sato, Jun-ya Kato, Jun Sato, Hiroyuki Suzuki, Hajime Asano, Mami Okada, Yasuhiro Matsumoto, Kazuhiko Shirota
-
Publication number: 20120157386Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Cameron SMITH, Melissa FLEURY, Roland GENDRON, Ryan HUDSON, Adam D. HUGHES
-
Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
-
Publication number: 20120149706Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Inventors: Jacques DUMAS, Uday KHIRE, Timothy B. Lowinger, Holger PAULSEN, Bernd RIEDL, Willian J. SCOTT, Roger A. SMITH, Jill WOOD, Holia HATOUM-MOKDAD, Wendy LEE, Aniko REDMAN, Jeffrey JOHNSON, Robert SIBLEY
-
Publication number: 20120142666Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: June 8, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
-
Publication number: 20120142691Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: August 4, 2010Publication date: June 7, 2012Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
-
Publication number: 20120142677Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
-
Patent number: 8193221Abstract: A compound of formula (I) wherein A1, A2, A3, A4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: GrantFiled: October 13, 2008Date of Patent: June 5, 2012Assignee: Syngenta Crop Protection LLCInventors: Werner Zambach, Peter Renold
-
Patent number: 8193192Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: GrantFiled: August 29, 2007Date of Patent: June 5, 2012Assignee: Phenex Pharmaceuticals AGInventors: Claus Kremoser, Ulrich Deuschle, Ulrich Abel, Andreas Schulz
-
Publication number: 20120136026Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 31, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
-
Patent number: 8188119Abstract: The present invention provides an antifungal agent which has excellent antifungal action, and which is also excellent in terms of its properties, and in particular its solubility in water and safety. The present invention discloses a compound represented by the following formula (I) or a salt thereof. wherein R1, R2, R3, R4, A, X, Y, and Z are defined in the specification.Type: GrantFiled: October 6, 2009Date of Patent: May 29, 2012Assignee: Eisai R&D Management Co., LtdInventor: Keigo Tanaka
-
Publication number: 20120121727Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
-
Publication number: 20120101105Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.Type: ApplicationFiled: May 31, 2010Publication date: April 26, 2012Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
-
Patent number: 8163728Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: April 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20120094830Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: ApplicationFiled: December 14, 2011Publication date: April 19, 2012Applicant: BAYER CROPSCIENCE AGInventors: Bernd ALIG, Rüdiger FISCHER, Christian FUNKE, Ernst Rudolf F. GESING, Achim HENSE, Olga MALSAM, Mark Wilhelm DREWES, Ulrich GÖRGENS, Tetsuya MURATA, Katsuaki WADA, Christian ARNOLD, Erich SANWALD
-
Publication number: 20120095039Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.Type: ApplicationFiled: November 21, 2011Publication date: April 19, 2012Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
-
Publication number: 20120094980Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
-
Publication number: 20120094993Abstract: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, 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 dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: October 7, 2011Publication date: April 19, 2012Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
-
Publication number: 20120094837Abstract: The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.Type: ApplicationFiled: July 15, 2011Publication date: April 19, 2012Applicant: Bayer Crop Science AGInventors: Friedrich August MÜHLTHAU, Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Markus HEIL, Achim HENSE, Joachim KLUTH, Adeline KÖHLER, Eva-Maria FRANKEN, Olga MALSAM, Arnd VOERSTE, Peter JESCHKE, Angela BECKER, Peter LÖSEL, Yoshitaka SATO
-
Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
-
Patent number: 8158657Abstract: An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability.Type: GrantFiled: February 12, 2010Date of Patent: April 17, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Keigo Tanaka, Satoshi Inoue, Norio Murai, Masayuki Matsukura, Kazutaka Nakamoto, Shuji Shirotori, Shinya Abe
-
Publication number: 20120083475Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.Type: ApplicationFiled: June 11, 2010Publication date: April 5, 2012Inventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
-
Publication number: 20120071481Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: ApplicationFiled: February 2, 2010Publication date: March 22, 2012Inventors: Ronald Palin, Paul David Ratcliffe, Steven G. Kultgen, Koc-Kan Ho, Andrew Laird Roughton
-
Publication number: 20120065212Abstract: 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: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
-
Publication number: 20120064121Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Shoujun Chen
-
Patent number: 8134007Abstract: The present invention relates to compounds of the formula (I): and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: GrantFiled: May 2, 2008Date of Patent: March 13, 2012Assignee: Pfizer Inc.Inventors: Sharanjeet Kaur Bagal, Karl Richard Gibson, Mark Ian Kemp, Cedric Poinsard, Blanda Luzia Stammen, Stephen Martin Denton, Melanie Susanne Glossop
-
Publication number: 20120059171Abstract: The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) which are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I) wherein R1 to R5, R8 and R9 are described as in the description. The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.Type: ApplicationFiled: April 29, 2010Publication date: March 8, 2012Applicant: BASF SEInventors: Michael Rack, Karsten Koerber, Florian Kaiser
-
Publication number: 20120053051Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from 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, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22, —S(O)pR25 or —S(O)(?NR28)R29; and R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.Type: ApplicationFiled: February 28, 2011Publication date: March 1, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
-
Publication number: 20120035122Abstract: This invention recites isoxazoline substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in mammals and birds. R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.Type: ApplicationFiled: August 4, 2011Publication date: February 9, 2012Inventors: Valerie A. Vaillancourt, Nathan Anthony Logan Chubb, Michael Curtis, William Howson, Graham M. Kyne, Sanjay Menon, Susan M. K. Sheehan, Donald J. Skalitzky, John A. Wendt
-
Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
-
Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
-
Publication number: 20120015980Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: January 19, 2012Applicant: BAYER CROPSCIENCE AGInventors: Rüdiger FISCHER, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christian Funke, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Tetsuya Murata
-
Publication number: 20120015946Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 18, 2010Publication date: January 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
-
Publication number: 20120010199Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
-
Patent number: 8093394Abstract: The invention relates to new compounds of 5-thioxilose, preferably derivatives of the 5-thioxilopyranose type, and to a method for preparing the same and their use as the active ingredient of drugs mainly intended for treating or inhibiting thrombosis or heart failure or thromboembolic diseases.Type: GrantFiled: March 26, 2009Date of Patent: January 10, 2012Assignee: Laboratoires Fournier S.A.Inventors: Véronique Barberousse, Didier Thomas, Michel Bondoux
-
Patent number: 8084473Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof.Type: GrantFiled: April 23, 2008Date of Patent: December 27, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel, legal representative
-
Publication number: 20110312963Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPDType: ApplicationFiled: December 11, 2009Publication date: December 22, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
-
Publication number: 20110313152Abstract: 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: ApplicationFiled: February 26, 2010Publication date: December 22, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
-
Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
-
Publication number: 20110306592Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z 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: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
-
Publication number: 20110301205Abstract: The present invention relates to isoxazole compounds of formula (I) having fungicidal activity, to agricultural compositions comprising them, and to the use of said compounds and compositions in agriculture for the control of microbial pests, particularly fungal pests, on plants.Type: ApplicationFiled: December 11, 2009Publication date: December 8, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Shy-Fuh Lee, Ulrich Johannes Haas, Micah Gliedt