Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
  • Patent number: 8569322
    Abstract: Lamivudine oxalate, preparation method and crystalline forms thereof are disclosed. A preparation method of Lamivudine is also disclosed.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: October 29, 2013
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Yanlong Liu, Fei Liu, Xiquan Zhang
  • Patent number: 8569319
    Abstract: 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: Grant
    Filed: April 29, 2011
    Date of Patent: October 29, 2013
    Assignee: Deciphera Pharmaceuticals, LLS
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Patent number: 8569336
    Abstract: 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: Grant
    Filed: November 9, 2009
    Date of Patent: October 29, 2013
    Inventors: 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
  • Publication number: 20130281428
    Abstract: 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: Application
    Filed: January 30, 2013
    Publication date: October 24, 2013
    Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
  • Patent number: 8563715
    Abstract: [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: Grant
    Filed: March 31, 2009
    Date of Patent: October 22, 2013
    Assignee: Zenyaku Kogyo Kabushikikaisha
    Inventors: Takeshi Nagata, Toshiaki Suzuki, Akira Yoshimura, Naoto Tadano, Toshiyuki Matsuno, Hideki Satoh, Kenichi Saitoh, Soichi Ohta
  • Publication number: 20130274261
    Abstract: 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: Application
    Filed: March 18, 2013
    Publication date: October 17, 2013
    Inventor: Arthur T. SANDS
  • Publication number: 20130274253
    Abstract: 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: Application
    Filed: December 22, 2011
    Publication date: October 17, 2013
    Applicant: SANOFI
    Inventors: 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
  • Patent number: 8557850
    Abstract: 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: Grant
    Filed: March 24, 2009
    Date of Patent: October 15, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Ichirou Urihara, Atsunori Isshiki, Hiroyasu Hosokawa, Tomoyuki Saiga
  • Publication number: 20130267415
    Abstract: 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: Application
    Filed: December 15, 2011
    Publication date: October 10, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
  • Publication number: 20130267513
    Abstract: 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 independ
    Type: Application
    Filed: May 16, 2011
    Publication date: October 10, 2013
    Inventors: Brayn Chan, Anthony Estrada, Zachary Sweeney, Edward Giles Mciver, Stephen Lewis
  • Publication number: 20130267545
    Abstract: 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: Application
    Filed: June 15, 2011
    Publication date: October 10, 2013
    Applicant: BAYER CROPSCIENCE LP
    Inventors: Randy Allen Myers, James Bloomberg, James Alan Hopkins
  • Patent number: 8551912
    Abstract: 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: Grant
    Filed: April 23, 2008
    Date of Patent: October 8, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
  • Patent number: 8552021
    Abstract: 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: Grant
    Filed: September 29, 2010
    Date of Patent: October 8, 2013
    Assignees: Janssen Products, L.P., Medivir AB
    Inventors: 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
  • Patent number: 8552019
    Abstract: 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: Grant
    Filed: November 24, 2009
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin A. Keenan, Alan B. Northrup
  • Publication number: 20130261069
    Abstract: 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, Thi
    Type: Application
    Filed: June 9, 2011
    Publication date: October 3, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Ana Dutton, Jerome Yves Cassayre, Ulrich Johannes Haas
  • Patent number: 8546411
    Abstract: 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: Grant
    Filed: August 7, 2008
    Date of Patent: October 1, 2013
    Assignee: Makhteshim Chemical Works Ltd.
    Inventors: Sharona Zamir, Inna Faktorovitch
  • Publication number: 20130252972
    Abstract: 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: Application
    Filed: July 19, 2011
    Publication date: September 26, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wendeborn
  • Publication number: 20130252937
    Abstract: 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: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Publication number: 20130252980
    Abstract: 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: Application
    Filed: October 5, 2011
    Publication date: September 26, 2013
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pandurang Zaware
  • Publication number: 20130252981
    Abstract: 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: Application
    Filed: November 30, 2011
    Publication date: September 26, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura
  • Publication number: 20130252982
    Abstract: 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: Application
    Filed: November 10, 2011
    Publication date: September 26, 2013
    Applicant: COGNIS IP MANAGEMENT GMBH
    Inventors: Stefan Busch, Ingo Fleute-Schlachter, Sandra Mack, Eike Ulf Mahnke, Anja Wick
  • Publication number: 20130252898
    Abstract: 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: Application
    Filed: May 30, 2013
    Publication date: September 26, 2013
    Applicant: Morehouse School Of Medicine
    Inventors: Gale W. Newman, Barbara A. Jacob-Mungin, Chamberlain Obialo
  • Publication number: 20130252963
    Abstract: 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: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • Patent number: 8541575
    Abstract: 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: Grant
    Filed: July 23, 2009
    Date of Patent: September 24, 2013
    Assignee: 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
  • Patent number: 8541432
    Abstract: 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: Grant
    Filed: September 13, 2012
    Date of Patent: September 24, 2013
    Assignee: Novartis AG
    Inventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
  • Patent number: 8541431
    Abstract: 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: Grant
    Filed: May 19, 2009
    Date of Patent: September 24, 2013
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
  • Patent number: 8541423
    Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: September 24, 2013
    Assignee: Hydra Biosciences, Inc.
    Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mandel-Brehm
  • Patent number: 8541402
    Abstract: 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: Grant
    Filed: May 3, 2012
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Patent number: 8541433
    Abstract: 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: Grant
    Filed: February 19, 2009
    Date of Patent: September 24, 2013
    Assignee: Actelion Pharmaceuticals, Ltd.
    Inventors: Martine Clozel, Urs Regenass
  • Publication number: 20130247250
    Abstract: 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: Application
    Filed: June 3, 2011
    Publication date: September 19, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Ulrich Johannes Haas, Christophe Weider, Ronald Zeun, Albert Bassi, Daniel Perkins
  • Publication number: 20130245050
    Abstract: 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: Application
    Filed: August 15, 2011
    Publication date: September 19, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Heiko Rieck, Dominique Steiger, Peter Howard Davies, Sylvain Tafforeau, Lorianne Fought, George Hauley Musson, IV, Luk De Maeyer, Gilbert Labourdette, Helen Lachaise, Sebastian Hoffmann
  • Publication number: 20130243754
    Abstract: 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: Application
    Filed: December 20, 2012
    Publication date: September 19, 2013
    Applicant: TARGEGEN, INC.
    Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
  • Patent number: 8536138
    Abstract: 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: Grant
    Filed: December 5, 2011
    Date of Patent: September 17, 2013
    Assignee: Vivus, Inc.
    Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
  • Patent number: 8536089
    Abstract: 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: Grant
    Filed: August 11, 2005
    Date of Patent: September 17, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Harald Walter, Urs Neuenschwander, Ronald Zeun, Josef Ehrenfreund, Hans Tobler, Camilla Corsi, Clemens Lamberth
  • Patent number: 8530488
    Abstract: 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: Grant
    Filed: October 24, 2008
    Date of Patent: September 10, 2013
    Assignee: Generics [UK] Limited
    Inventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Prakash Bansode, Dattatraya Shinde, Sunanda Phadtare
  • Patent number: 8530489
    Abstract: 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: Grant
    Filed: May 22, 2012
    Date of Patent: September 10, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Patent number: 8524723
    Abstract: 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: Grant
    Filed: December 6, 2012
    Date of Patent: September 3, 2013
    Assignee: Makhteshim Chemical Works Ltd.
    Inventors: Sharona Zamir, Inna Faktorovitch
  • Publication number: 20130225583
    Abstract: 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: Application
    Filed: October 17, 2011
    Publication date: August 29, 2013
    Inventors: Gerald W. Shipps, JR., Berengere Sauvagnat, Jack Bracken, William T. McElroy, Christopher D. Cox, Ginny Ho, Georgia Mcgaughey
  • Publication number: 20130224147
    Abstract: 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: Application
    Filed: January 10, 2013
    Publication date: August 29, 2013
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventor: Idenix Pharmaceuticals, Inc.
  • Publication number: 20130225617
    Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: January 31, 2013
    Publication date: August 29, 2013
    Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
    Inventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
  • Publication number: 20130225619
    Abstract: 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: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130216498
    Abstract: 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: Application
    Filed: December 23, 2010
    Publication date: August 22, 2013
    Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
  • Publication number: 20130217688
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: May 2, 2013
    Publication date: August 22, 2013
    Applicant: Celgene Avilomics Research, Inc.
    Inventor: Celgene Avilomics Research, Inc.
  • Patent number: 8513244
    Abstract: 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: Grant
    Filed: May 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8513239
    Abstract: 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: Grant
    Filed: October 9, 2008
    Date of Patent: August 20, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Jianping Cai, Xin-Jie Chu, Hongju Li, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
  • Patent number: 8513271
    Abstract: 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: Grant
    Filed: October 28, 2010
    Date of Patent: August 20, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: 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
  • Publication number: 20130210832
    Abstract: 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: Application
    Filed: May 17, 2011
    Publication date: August 15, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Darryl McConnell, Harald Engelhardt, Christiane Kofink
  • Publication number: 20130203727
    Abstract: 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: Application
    Filed: July 1, 2011
    Publication date: August 8, 2013
    Applicant: 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
  • Publication number: 20130202573
    Abstract: 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: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Publication number: 20130203601
    Abstract: 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: Application
    Filed: June 7, 2011
    Publication date: August 8, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jeffrey David Fowler, Sejong Kim