Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
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Patent number: 8735579Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: GrantFiled: August 26, 2009Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
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Patent number: 8735396Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.Type: GrantFiled: May 22, 2013Date of Patent: May 27, 2014Assignee: Pfizer Inc.Inventors: Jeffrey Allen Pfefferkorn, Anthony Lai Ling
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Patent number: 8735412Abstract: The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.Type: GrantFiled: October 9, 2009Date of Patent: May 27, 2014Assignee: Bayer Intellectual Property GmbHInventors: Ulrich Lücking, Rolf Jautelat, Gerhard Siemeister, Julia Schulze, Philip Lienau
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Publication number: 20140141977Abstract: The invention relates to suspension concentrates comprising a) one or more pesticides that are solid at room temperature, b) one or more specific copolymers, c) one or more additional auxiliary substances as applicable and d) one or more solvents. The copolymers b) comprise structural units of formula (I), wherein A stands for C2-C4-alkyls, B stands for a C2-C4-alkyl different from A, R stands for hydrogen or methyl, m is a number from 1 to 500, n is a number from 1 to 500, the sum of m+n is equal to 2 to 1000 and P stands for H or for a specific other concluding group, and structural units derived from specific ethylenic, unsaturated monomers that comprise an aromatic group, and structural units derived from specific ethylenic, unsaturated monomers that comprise aliphatic hydrocarbon residue. The suspension concentrates according to the invention are advantageously suitable for use as pesticides.Type: ApplicationFiled: March 10, 2012Publication date: May 22, 2014Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Andreas Wacker, Carsten Schaefer, Alexander Woerndale, Robert Milbradt
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Patent number: 8729091Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: February 15, 2013Date of Patent: May 20, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Publication number: 20140135216Abstract: The present invention relates to pesticidal mixtures 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 fungicide. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: May 30, 2012Publication date: May 15, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140135353Abstract: A crystalline sodium salt of a compound of formula I (INN: Raltegravir) or a hydrate/solvate thereof is disclosed as well as a process for obtaining the same.Type: ApplicationFiled: April 27, 2012Publication date: May 15, 2014Applicant: SANDOZ AGInventors: Fritz Blatter, Katharina Reichenbächer, Robert Ziegert, Josef Wieser, Johannes Ludescher
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Patent number: 8722722Abstract: The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.Type: GrantFiled: December 7, 2012Date of Patent: May 13, 2014Assignee: Teva Pharmaceutical Industries LtdInventors: Ana Kwokal, Lilach Hedvati, Revital Burstein, Adi Yeori, Rinat Moshkovits-Kaptsan
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Patent number: 8722883Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: GrantFiled: March 15, 2013Date of Patent: May 13, 2014Assignee: AstraZeneca ABInventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Cherylin Francis Preston, Jeffrey Paul Stonehouse, Neal Michael Smith
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Patent number: 8722882Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.Type: GrantFiled: December 21, 2009Date of Patent: May 13, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Andrew Stamford, Jinsong Hao, Charles Lee Jayne, Yan Xia
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Publication number: 20140128365Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.Type: ApplicationFiled: November 2, 2012Publication date: May 8, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
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Publication number: 20140128345Abstract: Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release.Type: ApplicationFiled: November 6, 2013Publication date: May 8, 2014Applicant: UNIVERSITY OF WASHINGTONInventors: Kim A. Woodrow, Cameron Ball, Anna Blakney, Emily Krogstad, Huarong Nie
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Publication number: 20140128367Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: June 14, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
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Patent number: 8710053Abstract: A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more QoI compounds selected from group (A) consisting of dimoxystrobin, azoxystrobin, fluoxastrobin, pyraclostrobin, kresoxim-methyl, picoxystrobin, trifloxystrobin and N-methyl-alpha-methoxyimino-2-[(2,5-dimethylphenoxy)methyl]phenylacetamide is provided by the present invention, and this composition has excellent effect for controlling a plant disease.Type: GrantFiled: April 25, 2011Date of Patent: April 29, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
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Publication number: 20140113899Abstract: An agro-horticultural agent of the present invention is intended to provide an agro-horticultural agent capable of providing, with a smaller spray amount, the same effect as compared to a conventional agro-horticultural agent. The agro-horticultural agent of the present invention includes a plurality of active ingredients and one of the plurality of active ingredients is an azole derivative represented by the following general formula (I); where: Ra and Rb each represent a predetermined hydrocarbon group and at least one of Ra and Rb has a chlorine atom or a bromine atom substituted for a hydrogen atom; Y represents a chlorine atom or a fluorine atom; and m represents 0 or 1.Type: ApplicationFiled: June 6, 2012Publication date: April 24, 2014Applicant: KUREHA CORPORATIONInventors: Hideaki Tateishi, Nobuyuki Araki, Toru Yamazaki, Taiji Miyake, Keiichi Sudo, Hisashi Kanno
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Publication number: 20140113895Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 8703649Abstract: The present invention relates to formulation comprising at least (i) two pesticidal compounds A and B dissolved in a lactic acid ester and wherein a) both A and B have melting points below 900 C b) both A and B are selected from the following list: pyraclos-trobin, metalaxyl, mefenoxam, trifloxystrobin, imazalil, pro-chloraz and ipconazole with the proviso that A is different from B (ii) at least one pesticidal compound C present in solid particles, and having a melting point of 900 C and above, and to their use as seed treatment formulation as well as their use for plant protection, including seed and crop protection.Type: GrantFiled: July 20, 2010Date of Patent: April 22, 2014Assignee: BASF SEInventors: Rafel Israels, Katharine Klamczynski, Marco Kuhns, Ulf Schlotterbeck
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Publication number: 20140107112Abstract: The present invention relates to compositions for controlling plant pests, which contain the compound of the formula (I) in a mixture with fungicidally active compounds, except for cyclopropylcarboxamide derivatives and azolylmethylcycloalkanes.Type: ApplicationFiled: December 13, 2013Publication date: April 17, 2014Applicant: Bayer Intellectual Property GmbHInventors: Christoph ERDELEN, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Krämer
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Publication number: 20140100231Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
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Publication number: 20140100107Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I), (B) an inhibitor of the respiratory chain at complex I or II and (C1) an inhibitor of the ergosterol biosynthesis, in particular an azole compound, or (C2) an inhibitor of the respiratory chain at complex III, in particular a strobilurin compound. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: ApplicationFiled: March 28, 2012Publication date: April 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrike Wachendorff-Neumann, Ingo Wetcholowsky, Anton Kraus, Thomas Seitz, Jose Augusto Geraldes
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Patent number: 8691573Abstract: The present invention relates compounds for stabilizing cells and methods of their use.Type: GrantFiled: December 3, 2009Date of Patent: April 8, 2014Assignee: The Scripps Research InstituteInventors: Yue Xu, Sheng Ding
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Publication number: 20140094478Abstract: The present invention relates to a composition and tablet comprising raltegravir and to a process for the preparation of such tablet.Type: ApplicationFiled: May 29, 2012Publication date: April 3, 2014Applicant: ratiopharm GmbHInventors: Daniela Stumm, Dominique Meergans
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Patent number: 8686155Abstract: 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: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Patent number: 8685990Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.Type: GrantFiled: July 25, 2013Date of Patent: April 1, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Haiyan Bian, Peter J. Connolly, Gilles Bignan, Chaozhong Cai, Scott L. Dax, Bart L. DeCorte, Shu-Chen Lin, Li Liu, Mark J. Macielag, Philip M. Pitis, Yue-Mei Zhang, Bin Zhu, Wei He
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Patent number: 8685984Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: GrantFiled: July 5, 2013Date of Patent: April 1, 2014Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Patent number: 8685969Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.Type: GrantFiled: June 16, 2011Date of Patent: April 1, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
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Patent number: 8685989Abstract: Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of of 0 to 5; X and Y are each a connected bond, a cycloalkyl group, or —CO—; and Q is a hydrogen atom or a phenyl group.Type: GrantFiled: May 29, 2012Date of Patent: April 1, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Patent number: 8685972Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: July 31, 2009Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
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Patent number: 8686143Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: October 25, 2011Date of Patent: April 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Publication number: 20140088124Abstract: Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.Type: ApplicationFiled: June 1, 2012Publication date: March 27, 2014Inventors: Robert J. DeVita, QingMei Hong, Zhong Lai, Kevin D. Dykstra, Yang Yu, Jian Liu, Donald M. Sperbeck, Tianying Jian, Deodial Guiadeen, Ginger Xu-qiang Yang, Zhicai Wu, Shuwen He, Pauline C. Ting, Robert Aslanian, Jeffrey T. Kuethe, James Balkovec, Rongze Kuang, Gang Zhou, Heping Wu
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Patent number: 8680106Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.Type: GrantFiled: July 5, 2013Date of Patent: March 25, 2014Assignee: AbbVic Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Publication number: 20140079666Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 5, 2012Publication date: March 20, 2014Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventors: Thomas R. Webb, Vincent A. Boyd
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Publication number: 20140080780Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Inventor: Benjamin WOLOZIN
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Publication number: 20140073636Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.Type: ApplicationFiled: April 30, 2013Publication date: March 13, 2014Applicant: TAKEDA GMBHInventor: Ulrich KAUTZ
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Publication number: 20140073651Abstract: The invention relates to benzamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: February 21, 2012Publication date: March 13, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Mark Murphy, Dorte Renneberg
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Patent number: 8669254Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 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: GrantFiled: December 8, 2011Date of Patent: March 11, 2014Assignee: Hoffman-La Roche Inc.Inventors: Paul Hebeisen, Stephan Roever
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Publication number: 20140066407Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.Type: ApplicationFiled: November 8, 2013Publication date: March 6, 2014Applicant: Bayer Intellectual Property GmbHInventors: DUTZMANN Stefan, STENZEL Klaus, JAUTELAT Manfred
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Publication number: 20140066422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: ApplicationFiled: February 13, 2013Publication date: March 6, 2014Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Patent number: 8664226Abstract: Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPAR? activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.Type: GrantFiled: April 16, 2010Date of Patent: March 4, 2014Assignee: Kowa Company, Ltd.Inventors: Toru Miura, Kazuhiro Onogi, Seiichi Sato, Junya Tagashira, Gen Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Patent number: 8664235Abstract: The present invention relates to a method of combating animal pests which comprises contacting the animal pests, their habit, breeding ground, food supply, plant, seed, soil, area, material or environment in which the animal pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from animal attack or infestation with a pesticidally effective amount of at least one 6-halogeno[1,2,4]triazolo[1,5-a]-pyrimidine of the general formula (I), wherein X, R1, R2, R3 and R4 are as defined in claim 1 and/or the agriculturally useful salts thereof.Type: GrantFiled: September 10, 2004Date of Patent: March 4, 2014Assignee: Merial LimitedInventors: Ernst Baumann, Thomas Grote, Frank Schieweck, Wolfgang von Deyn, Norbert Götz, Michael Hofmann, Markus Kordes, Michael Puhl, Michael Rack, Thomas Schmidt, Toni Bucci, Henry Van Tuyl Cotter, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Publication number: 20140057919Abstract: 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: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Applicant: Pfizer Inc.Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
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Publication number: 20140057921Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.Type: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Applicant: NOVARTIS AGInventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY
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Publication number: 20140057915Abstract: There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: August 16, 2013Publication date: February 27, 2014Applicants: TOPIVERT PHARMA LIMITED, RESPIVERT LIMITEDInventors: CLAIRE ANNE MARIE CARIOU, CATHERINE ELISABETH CHARRON, EUAN ALEXANDER FRASER FORDYCE, MATTHEW COLIN THOR FYFE, DANIEL HAMZA, KAZUHIRO ITO, JOHN KING-UNDERWOOD, PETER JOHN MURRAY, STUART THOMAS ONIONS, STEPHEN MALCOLM THOM, HAYLEY TEGAN ANGELA WATSON, JONATHAN GARETH WILLIAMS
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Publication number: 20140057893Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.Type: ApplicationFiled: April 5, 2012Publication date: February 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Publication number: 20140051714Abstract: The present invention relates to the GPR119 agonist, 4-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yloxy)-5-fluoro-6-(2-methyl-6-(methylsulfonyl)pyridin-3-yloxy)pyrimidine (Compound 1): and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing the secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 20, 2012Publication date: February 20, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventor: Robert M. Jones
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Publication number: 20140051703Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.Type: ApplicationFiled: April 11, 2013Publication date: February 20, 2014Applicant: Cytopia Research Pty Ltd.Inventors: David Gerard BOURKE, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
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Patent number: 8653068Abstract: A compound or its pharmaceutically acceptable salt, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: GrantFiled: October 30, 2009Date of Patent: February 18, 2014Assignee: Pain Therapeutics, Inc.Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 8653002Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.Type: GrantFiled: August 26, 2010Date of Patent: February 18, 2014Assignee: BASF SEInventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
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Publication number: 20140045848Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.Type: ApplicationFiled: April 11, 2013Publication date: February 13, 2014Applicant: Cytopia Research Pty Ltd.Inventors: David Gerard Bourke, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
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Publication number: 20140038950Abstract: An anti-fungal treatment for trees and bushes. Included are all methods of delivery of active ingredients, including foliar and trunk spraying application, granular soil surface, soil drench, soil injection, and trunk injection. The chemical combination includes a group 3 fungicide like propiconazole, that is, a systemic with curative and protective action, that works via the demethylation of C-14 during ergosterol biosynthesis. The combination also includes a group 11 fungicide like Azoxystrobin, or Fluoxastrobin for which their biochemical mode of action is inhibition of electron transport. The combined efficacy of there two classes of chemicals is reduced spreading of the fungus and increased killing of fungus. It has also been found that these chemicals used individually on trees and bushes, have unexpected benefits.Type: ApplicationFiled: September 8, 2013Publication date: February 6, 2014Inventor: NORMAN J. HELIE