Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Patent number: 8822464Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: November 26, 2012Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Publication number: 20140243273Abstract: The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I.Type: ApplicationFiled: May 7, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Irina Nikolaevna Kadiyala, Shahla Jamzad, Thomas Carl Hoock, Lori Kell Taylor, Kathryn Lea Sewell
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Publication number: 20140235442Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Inventors: Heike HUNGENBERG, Gilbert LABOURDETTE, Albert SCHIRRING, Burkhard SCHUETZ, Anne SUTY-HEINZE, Wolfgang THIELERT, Martin VAUPEL
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Publication number: 20140228338Abstract: The topical ophthalmic use of certain 2,4-diamino-substituted 1,3-triazines for preventing or alleviating ocular pain in patients is disclosed. Topcial ocular pharmaceutical composition are also disclosed.Type: ApplicationFiled: February 13, 2014Publication date: August 14, 2014Applicant: Novartis AGInventors: Martha E. Gadd, Peter G. Klimko, Karen C. David, Kenneth C. Appell, Mark R. Hellberg
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Publication number: 20140227260Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Auspex Pharmaceuticals, Inc.Inventor: Chengzhi Zhang
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Patent number: 8795701Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.Type: GrantFiled: April 8, 2008Date of Patent: August 5, 2014Assignee: Bayer CropScience AGInventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
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Patent number: 8796449Abstract: Novel s-triazine compounds are disclosed that have a formula represented by the following: L1, L2, L3, R1, R2, R3, R4, R5a, R5b, and R5c are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, where microbial infection is either a direct cause or a related condition.Type: GrantFiled: March 17, 2011Date of Patent: August 5, 2014Assignee: New York UniversityInventor: Neville Robert Kallenbach
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Patent number: 8791115Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitizers.Type: GrantFiled: December 18, 2006Date of Patent: July 29, 2014Assignee: Poxel SASInventors: Gérard Moinet, Daniel Cravo, Didier Mesangeau
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Patent number: 8791049Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.Type: GrantFiled: December 13, 2010Date of Patent: July 29, 2014Assignee: Gowan Co.Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
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Publication number: 20140206633Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.Type: ApplicationFiled: February 3, 2011Publication date: July 24, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
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Patent number: 8778835Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: July 5, 2007Date of Patent: July 15, 2014Assignee: Bayer Cropscience AGInventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
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Patent number: 8778836Abstract: This invention relates to a new herbicidal composition comprising desmedipham and optionally phenmedipham and/or ethofumesate.Type: GrantFiled: April 25, 2013Date of Patent: July 15, 2014Assignee: Bayer Cropscience LPInventor: David A. Long
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Patent number: 8778837Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: November 27, 2008Date of Patent: July 15, 2014Assignee: Bayer CropScience AGInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140194429Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.Type: ApplicationFiled: March 13, 2013Publication date: July 10, 2014Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
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Publication number: 20140193519Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.Type: ApplicationFiled: August 2, 2013Publication date: July 10, 2014Applicant: ZIOPHARM ONCOLOGY, INC.Inventors: Barbara P. Wallner, Brian Eric Schwartz, Philip B. Komarnitsky, Gerald Bacher, Bernhard Kutscher, Gerhard Raab
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Patent number: 8765944Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: August 16, 2011Date of Patent: July 1, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Li-Qiang Sun, Eric Mull, Qian Zhao, Tao Wang, Zhongxing Zhang, Paul Michael Scola
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Publication number: 20140179637Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.Type: ApplicationFiled: December 21, 2013Publication date: June 26, 2014Applicants: The Research Foundation for The State University of New York, Northwestern UniversityInventors: Jonathan Leis, Carol Carter
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Publication number: 20140179662Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.Type: ApplicationFiled: March 1, 2012Publication date: June 26, 2014Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBHInventors: Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
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Publication number: 20140179697Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: December 23, 2013Publication date: June 26, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20140171430Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: April 20, 2012Publication date: June 19, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
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Patent number: 8754084Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.Type: GrantFiled: March 27, 2013Date of Patent: June 17, 2014Assignee: The Board of Trustees of the University of IllinoisInventors: Steven C. Zimmerman, Chun-Ho Wong, Paul J. Hergenrother, Jessie Peh
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Publication number: 20140161845Abstract: The present invention provides non-peptide compounds of formula (I) wherein: X is —(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is —(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORa, —SRa, —S(O)2NRbRc, —NRbRc, —NRaCORd, —C(O)Ra, —C(O)ORa, and —C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g.Type: ApplicationFiled: July 20, 2012Publication date: June 12, 2014Applicant: University of Louisville Research Foundation Inc.Inventors: Donald R. Demuth, Frederick A. Luzzio
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Patent number: 8748411Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: GrantFiled: May 5, 2006Date of Patent: June 10, 2014Assignee: Centro de Ingenieria Genetica y BiotechnologiaInventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
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Publication number: 20140155379Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: December 20, 2013Publication date: June 5, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Publication number: 20140155263Abstract: Fungicidal mixtures comprising, as active components, 1) azolopyrimidinylamines of the formula I, in which the substituents are as defined in the description and 2) at least one active compound II selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates and other active compounds selected from the group consisting of guanidines, antibiotics, sulfur-containing heterocyclyl compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, growth retardants and cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine; in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I with active compounds II and the use of the compound I with active compounds II for preparing such mixtures, and also compositions comprising these mixtures.Type: ApplicationFiled: February 10, 2014Publication date: June 5, 2014Applicant: BASF SEInventors: Christine Beck, Matthias NIEDENBRÜCK, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo HÜNGER
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Patent number: 8742101Abstract: This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.Type: GrantFiled: November 13, 2008Date of Patent: June 3, 2014Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Richard Storer, Gilles Gosselin, David Dukhan, Frederic Leroy
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Publication number: 20140141972Abstract: This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: E I DU PONT NEMOURS AND COMPANYInventors: RICHARD ALAN BERGER, Isaac Billy Annan, George Philip Lahm, John Lindsey Flexner, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140140973Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140135335Abstract: Compounds of Formula I, including pharmaceutically acceptable salts, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:Type: ApplicationFiled: November 7, 2013Publication date: May 15, 2014Inventors: TAO WANG, Zhiwei Yin, Paul Michael Scola
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Publication number: 20140135281Abstract: The present invention relates to methods and compositions comprising cyromazine for the control of bee mites and for the reduction of bee mite infestations, such as the control and reduction of infestations of parasitic bee mites, such as Varroa destructor in bee, preferably honey bee, colonies, and to the treatment of varroatosis in bees.Type: ApplicationFiled: May 14, 2012Publication date: May 15, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventor: Andre Fougeroux
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Publication number: 20140134130Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:Type: ApplicationFiled: November 7, 2013Publication date: May 15, 2014Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
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Patent number: 8722674Abstract: Disclosed herein are a 1,3,5-triazine-2,4,6-triamine compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for preventing or treating metabolic syndromes, diabetes, or cancers with deletion of P53 gene, which comprises the same.Type: GrantFiled: August 28, 2008Date of Patent: May 13, 2014Assignee: Hanall Biopharma Co., Ltd.Inventors: Hyae Gyeong Cheon, Kwang-Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong-Cheol Lee, Sung Wuk Kim, Sung Soo Jun
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Patent number: 8722071Abstract: The present invention provides polymer microcapsules of biocide, useful for preparing coating materials such as interior and exterior paints, which comprises of an active agent biocide and an encapsulating polymer. Microcapsules described in this invention are prepared by dispersing an organic phase containing an active agent either in dissolved state or dispersed state in a polymer solution using a low boiling point solvent, in an aqueous phase containing an emulsifying agent; agitating the emulsion at 800-1200 resolution per minute for 3-5 hours at 25 -27° C. to evaporate the low boiling point solvent and thus to permit the formation of the microcapsules; separating the microcapsules, washing with water and drying the microcapsules at temperature between 25-35° C.Type: GrantFiled: February 27, 2006Date of Patent: May 13, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Shukla Parshuram Gajanan, Swaminathan Sivaram
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Patent number: 8716301Abstract: A method is provided herein to increase an immune response to an antigen. The method includes administering an agent that inhibits extracellular adenosine or inhibits adenosine receptors. Also disclosed are methods to increase the efficacy of a vaccine and to increase an immune response to a tumor antigen or immune cell-mediated tumor destruction.Type: GrantFiled: December 2, 2011Date of Patent: May 6, 2014Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Michail V. Sitkovsky, Akio Ohta
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Publication number: 20140113900Abstract: The present application relates to novel substituted imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: May 2, 2012Publication date: April 24, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexander Straub, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
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Publication number: 20140100230Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.Type: ApplicationFiled: December 10, 2013Publication date: April 10, 2014Applicant: HYDRA BIOSCIENCES, INC.Inventors: Jayhong A. Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
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Publication number: 20140094448Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: September 13, 2013Publication date: April 3, 2014Applicant: SENHWA BIOSCIENCES, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas Raffaele, Suchitra Ravula, David M. Ryckman
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Patent number: 8685976Abstract: The subject invention discloses an agent for promoting cell adhesion to a support, comprising a dispirotripiperazine derivative represented by Formula I below or a salt thereof; a method for promoting cell adhesion to a support comprising adding the dispirotripiperazine derivative represented by Formula I below or a salt thereof to a culture medium, or applying the same to a support; and an agonist of a heparin sulfate that comprises the dispirotripiperazine derivative represented by Formula I below or a salt thereof, and that promotes cell adhesion and/or cell growth.Type: GrantFiled: June 16, 2009Date of Patent: April 1, 2014Assignee: Kyoto UniversityInventors: Motonari Uesugi, Sayumi Yamazoe
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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Publication number: 20140088109Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin -1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney
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Publication number: 20140088099Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: November 20, 2013Publication date: March 27, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Pingda REN, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Publication number: 20140073632Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of screening for CFTR corrector compounds are also described herein. The methods of screening include contacting a cell that endogenously expresses a CFTR mutation with the compound to be screened and detecting a rescue of halide efflux from the cell.Type: ApplicationFiled: May 17, 2012Publication date: March 13, 2014Applicants: THE UAB RESEARCH FOUNDATION, DISCOVERYBIOMED INC.Inventors: Erik M. Schwiebert, James F. Collawn, Zsuzsa Bebok
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Publication number: 20140066430Abstract: 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: ApplicationFiled: October 3, 2013Publication date: March 6, 2014Applicant: Amgen Inc.Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
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Publication number: 20140066434Abstract: The invention discloses methods and compositions for treating or preventing Parkinson's disease by administering a compound of Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: April 6, 2012Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: William C. Shakespeare
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Publication number: 20140050786Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitisers.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: POXEL SASInventors: Gerard MOINET, Daniel CRAVO, Didier MESANGEAU
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Publication number: 20140051676Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.Type: ApplicationFiled: October 15, 2013Publication date: February 20, 2014Applicant: NOVARTIS AGInventors: Oliver BARKER, Jonathan Mark BENTLY, Mark Gary BOCK, Thomas CAIN, Praful CHOVATIA, Jennifer Ruth DOD, Florence EUSTACHE, Laura GLEAVE, Jonathan HARGRAVE, Alexander HEIFETZ, Richard LAW, Ali RAOOF, David WILLOWS
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Publication number: 20140045852Abstract: The present invention relates to substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).Type: ApplicationFiled: April 18, 2012Publication date: February 13, 2014Applicants: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Lücking, Rolf Bohlmann, Arne Scholz, Gerhard Siemeister, Mark Jean Gnoth, Ulf Bomer, Gerd Rühter, Carsten Schultz-Fademrecht, Dirk Kosemund, Philip Lienau
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Publication number: 20140045826Abstract: The invention discloses methods and compositions for treating or preventing neurodegenerative disease by administering a compound of Formula I: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: April 6, 2012Publication date: February 13, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: William C. Shakespeare, Frank G. Haluska
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Publication number: 20140038968Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: October 17, 2012Publication date: February 6, 2014Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz