Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
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Patent number: 8569322Abstract: Lamivudine oxalate, preparation method and crystalline forms thereof are disclosed. A preparation method of Lamivudine is also disclosed.Type: GrantFiled: December 23, 2010Date of Patent: October 29, 2013Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.Inventors: Yanlong Liu, Fei Liu, Xiquan Zhang
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Patent number: 8569319Abstract: Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.Type: GrantFiled: April 29, 2011Date of Patent: October 29, 2013Assignee: Deciphera Pharmaceuticals, LLSInventors: Daniel L. Flynn, Michael D. Kaufman
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Patent number: 8569336Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: October 29, 2013Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K. C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20130281428Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.Type: ApplicationFiled: January 30, 2013Publication date: October 24, 2013Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
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Patent number: 8563715Abstract: [Problem] To provide a prophylactic/therapeutic agent against, for example, nerve diseases and the like such as ischemic brain disease and neurodegenerative disease, or a prophylactic/therapeutic agent against diseases against which antioxidant action is effective, as a cell protecting agent, in particular as an inhibitor of brain cell damage or brain cell death.Type: GrantFiled: March 31, 2009Date of Patent: October 22, 2013Assignee: Zenyaku Kogyo KabushikikaishaInventors: Takeshi Nagata, Toshiaki Suzuki, Akira Yoshimura, Naoto Tadano, Toshiyuki Matsuno, Hideki Satoh, Kenichi Saitoh, Soichi Ohta
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Publication number: 20130274261Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.Type: ApplicationFiled: March 18, 2013Publication date: October 17, 2013Inventor: Arthur T. SANDS
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Publication number: 20130274253Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.Type: ApplicationFiled: December 22, 2011Publication date: October 17, 2013Applicant: SANOFIInventors: Maurice Brollo, Jean-Christophe Carry, Victor Certal, Eric Didier, Gilles Doerflinger, Youssef EL Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Laurent Schio, Fabienne Thompson
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Patent number: 8557850Abstract: The present invention provides a plant disease control agent containing at least one of tetrazoyloxime dirivatives and salts thereof, and at least one selected from the group consisting of fosetyl, propamocarb, basic copper chloride, chlorothalonil, manzeb, cymoxanil, folpet, iminoctadine, cyazofamid, metalaxyl, fludioxonil, tebuconazole, prothioconazole, thiamethoxam, azoxystrobin and salts thereof.Type: GrantFiled: March 24, 2009Date of Patent: October 15, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Ichirou Urihara, Atsunori Isshiki, Hiroyasu Hosokawa, Tomoyuki Saiga
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Publication number: 20130267415Abstract: 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 one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl, 3,5-dichloro-4-fluoro-phenyl, or 3,5-bis-trifluoromethylphenyl; R4 is methyl or chlorine; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; and wherein component B is an insecticide. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest a combination of components A and B.Type: ApplicationFiled: December 15, 2011Publication date: October 10, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
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Publication number: 20130267513Abstract: A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; -0-C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl and halogen, wherein said C1-6-alkyl, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independType: ApplicationFiled: May 16, 2011Publication date: October 10, 2013Inventors: Brayn Chan, Anthony Estrada, Zachary Sweeney, Edward Giles Mciver, Stephen Lewis
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Publication number: 20130267545Abstract: A method of improving the growth of plants such as corn, soybean, wheat, or rice is provided by reducing the incidence of one or more fungal infections. The method comprises the step of applying a foliar treatment composition at least once to established plants, wherein the treatment composition comprises effective amounts of active ingredients prothioconazole, trifloxystrobin, and azoxystrobin.Type: ApplicationFiled: June 15, 2011Publication date: October 10, 2013Applicant: BAYER CROPSCIENCE LPInventors: Randy Allen Myers, James Bloomberg, James Alan Hopkins
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Patent number: 8551912Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of Formula (I) wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.Type: GrantFiled: April 23, 2008Date of Patent: October 8, 2013Assignee: Syngenta Crop Protection LLCInventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
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Patent number: 8552021Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(?O)R6 or —C(?O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.Type: GrantFiled: September 29, 2010Date of Patent: October 8, 2013Assignees: Janssen Products, L.P., Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Michael Pelcman, Bengt Christian Sund, Horst Jurgen Wahling, Pedro Manuel Passos Pinho, Anna Winqvist, Karl Magnus Nilsson
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Patent number: 8552019Abstract: The instant invention provides for compounds of formula A that inhibit PDK1 activity: The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: November 24, 2009Date of Patent: October 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin A. Keenan, Alan B. Northrup
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Publication number: 20130261069Abstract: The present invention provides pesticidal mixtures comprising a component A, a component B and a component C, wherein component A is a compound of formula (I) wherein one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl; R4 is methyl; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; component B is a compound selected from Sedaxane, Fludioxonil, Metalaxyl, Mefenoxam, Cyprodinil, Azoxystrobin, Tebuconazole, Difenoconazole, Thiabendazole, Fluopyram, Penflufen, N-[9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide and Fuxapyroxad; or component B is a compound selected from Tefluthrin, Lambda-cyhalothrin, Abamectin, Spinosad, Spinetoram, Chlorpyrifos, ThiType: ApplicationFiled: June 9, 2011Publication date: October 3, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ana Dutton, Jerome Yves Cassayre, Ulrich Johannes Haas
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Patent number: 8546411Abstract: The present invention relates to novel crystalline polymorphic and amorphous forms of the compound methyl (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.Type: GrantFiled: August 7, 2008Date of Patent: October 1, 2013Assignee: Makhteshim Chemical Works Ltd.Inventors: Sharona Zamir, Inna Faktorovitch
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Publication number: 20130252972Abstract: The present invention relates to a compound of formula I: (I) wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.Type: ApplicationFiled: July 19, 2011Publication date: September 26, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wendeborn
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130252980Abstract: The present invention relates to novel GPR 119 agonists of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: October 5, 2011Publication date: September 26, 2013Applicant: Cadila Healthcare LimitedInventors: Harikishore Pingali, Pandurang Zaware
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Publication number: 20130252981Abstract: A pyrimidine compound of the formula (1): wherein: R1 represents hydrogen, and the like; R2 represents hydrogen, and the like; R3 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; R4 and R5 are represent a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; X represents nitrogen, and the like; Y represents nitrogen, and the like; and Z represents oxygen or —NR8— wherein R8 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like. The compound has a superior activity of controlling pests.Type: ApplicationFiled: November 30, 2011Publication date: September 26, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura
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Publication number: 20130252982Abstract: Suggested are alkoxylation products of 2-isopropyl-5-methyl-hexan-1-ol in which AO stands for an ethylene oxide, propylene oxide or butylenes oxide unit or their mixtures and n denominates an integer of from 1 to 100.Type: ApplicationFiled: November 10, 2011Publication date: September 26, 2013Applicant: COGNIS IP MANAGEMENT GMBHInventors: Stefan Busch, Ingo Fleute-Schlachter, Sandra Mack, Eike Ulf Mahnke, Anja Wick
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Publication number: 20130252898Abstract: The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1-associated biomarker in a biological sample is also disclosed.Type: ApplicationFiled: May 30, 2013Publication date: September 26, 2013Applicant: Morehouse School Of MedicineInventors: Gale W. Newman, Barbara A. Jacob-Mungin, Chamberlain Obialo
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Publication number: 20130252963Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Yun Jin, Zehong Wan, Qing Zhang
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Patent number: 8541575Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: July 23, 2009Date of Patent: September 24, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Chiara Marchionni, Michele Modugno
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Patent number: 8541432Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.Type: GrantFiled: September 13, 2012Date of Patent: September 24, 2013Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
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Patent number: 8541431Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: September 24, 2013Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Patent number: 8541423Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.Type: GrantFiled: April 11, 2012Date of Patent: September 24, 2013Assignee: Hydra Biosciences, Inc.Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mandel-Brehm
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Patent number: 8541402Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: May 3, 2012Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Patent number: 8541433Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.Type: GrantFiled: February 19, 2009Date of Patent: September 24, 2013Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Martine Clozel, Urs Regenass
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Publication number: 20130247250Abstract: The present invention is directed to methods of increasing the environmental stress tolerance of a plant, to methods of improving the quality and/or yield of a plant crop, to methods of application of agrochemicals having a physiological effect on a plant in the plant irrigation water, and to crops produced using said methods.Type: ApplicationFiled: June 3, 2011Publication date: September 19, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ulrich Johannes Haas, Christophe Weider, Ronald Zeun, Albert Bassi, Daniel Perkins
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Publication number: 20130245050Abstract: The present invention relates to the use of N-phenylethylpyrazole carboxamide derivatives or salts thereof for extended shelf life and storage stability of fruits and vegetables, to a method for extending shelf life or fruits and vegetables by applying N-phenylethylpyrazole carboxamide derivatives or salts thereof to the crops prior to the harvest of the fruits or vegetables.Type: ApplicationFiled: August 15, 2011Publication date: September 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Heiko Rieck, Dominique Steiger, Peter Howard Davies, Sylvain Tafforeau, Lorianne Fought, George Hauley Musson, IV, Luk De Maeyer, Gilbert Labourdette, Helen Lachaise, Sebastian Hoffmann
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Publication number: 20130243754Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: December 20, 2012Publication date: September 19, 2013Applicant: TARGEGEN, INC.Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
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Patent number: 8536138Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.Type: GrantFiled: December 5, 2011Date of Patent: September 17, 2013Assignee: Vivus, Inc.Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Patent number: 8536089Abstract: The invention relates to fungicidal compositions comprising as active ingredient a combination of components A) and B) as defined in the patent claims, to a method of controlling phytopathogenic diseases on crop plants using such a compositions and to a method of protecting natural substances of vegetable and/or animal origin and/or their processed forms using such a composition.Type: GrantFiled: August 11, 2005Date of Patent: September 17, 2013Assignee: Syngenta Crop Protection LLCInventors: Harald Walter, Urs Neuenschwander, Ronald Zeun, Josef Ehrenfreund, Hans Tobler, Camilla Corsi, Clemens Lamberth
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Patent number: 8530488Abstract: The present invention relates to novel crystalline forms of bosentan and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said crystalline forms and use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris.Type: GrantFiled: October 24, 2008Date of Patent: September 10, 2013Assignee: Generics [UK] LimitedInventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Prakash Bansode, Dattatraya Shinde, Sunanda Phadtare
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Patent number: 8530489Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 22, 2012Date of Patent: September 10, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
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Patent number: 8524723Abstract: The present invention relates to novel crystalline polymorphic and amorphous forms of the compound methyl (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.Type: GrantFiled: December 6, 2012Date of Patent: September 3, 2013Assignee: Makhteshim Chemical Works Ltd.Inventors: Sharona Zamir, Inna Faktorovitch
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Publication number: 20130225583Abstract: The present invention is directed to substituted amino-triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 17, 2011Publication date: August 29, 2013Inventors: Gerald W. Shipps, JR., Berengere Sauvagnat, Jack Bracken, William T. McElroy, Christopher D. Cox, Ginny Ho, Georgia Mcgaughey
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Publication number: 20130224147Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: January 10, 2013Publication date: August 29, 2013Applicant: Idenix Pharmaceuticals, Inc.Inventor: Idenix Pharmaceuticals, Inc.
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Publication number: 20130225617Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: January 31, 2013Publication date: August 29, 2013Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDInventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
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Publication number: 20130225619Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Publication number: 20130216498Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: December 23, 2010Publication date: August 22, 2013Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
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Publication number: 20130217688Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: May 2, 2013Publication date: August 22, 2013Applicant: Celgene Avilomics Research, Inc.Inventor: Celgene Avilomics Research, Inc.
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Patent number: 8513244Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 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 process and intermediates for preparing such compounds.Type: GrantFiled: May 18, 2012Date of Patent: August 20, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Adam D. Hughes
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Patent number: 8513239Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.Type: GrantFiled: October 9, 2008Date of Patent: August 20, 2013Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Jianping Cai, Xin-Jie Chu, Hongju Li, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 8513271Abstract: 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: October 28, 2010Date of Patent: August 20, 2013Assignee: 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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Publication number: 20130210832Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.Type: ApplicationFiled: May 17, 2011Publication date: August 15, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl McConnell, Harald Engelhardt, Christiane Kofink
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Publication number: 20130203727Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Publication number: 20130202573Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: August 8, 2013Applicant: Ardea Biosciences, Inc.Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
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Publication number: 20130203601Abstract: Stabilized liquid agrochemical compositions are provided that comprise flowable, aqueous dispersion concentrates comprising a) a continuous aqueous liquid phase; b) at least one dispersed, solid phase comprising a dispersion of polymer particles having a mean particle size of at least one micron, wherein the outside surfaces of the particles comprise a colloidal solid material and wherein the particles have at least one agrochemically active ingredient distributed therein, optionally a non-porous particulate mineral that acts as a diffusion barrier to slow the release of the active ingredient, and optionally at least one non-cross-linkable mobile chemical such that the extraction of this chemical from the disperse phase renders it porous in a manner that allows the active ingredient to diffuse out. The colloidal solid is used to stabilize the polymenzable resin in an emulsion state during preparation.Type: ApplicationFiled: June 7, 2011Publication date: August 8, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jeffrey David Fowler, Sejong Kim