1,3,5-triazine Ring Patents (Class 544/113)
  • Publication number: 20130150365
    Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Application
    Filed: February 6, 2013
    Publication date: June 13, 2013
    Applicant: Vestaron Corporation
    Inventor: Vestaron Corporation
  • Patent number: 8461158
    Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: June 11, 2013
    Assignee: Pathway Therapeutics Inc.
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Publication number: 20130143883
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: January 4, 2013
    Publication date: June 6, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130137635
    Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.
    Type: Application
    Filed: February 9, 2011
    Publication date: May 30, 2013
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventor: Arthur Thomas Sands
  • Publication number: 20130129813
    Abstract: Compositions and methods for tissue-specific targeted delivery of therapeutic agents through the use of tissue-specific peptidomimetic ligands are disclosed herein. The ligand comprises a composition of formula A-scaffold-A? and one or more hydrophobic anchors covalently linked to the scaffold. The A and A? compounds linked to the scaffold comprise monovalent peptidomimetic compounds wherein each monovalent peptidomimetic compound is selected from the group consisting of fragments IKs, GKs, IDs, GSs, GTs, VSs, TKs, KTs, ARs, KIs, KEs, AEs, GRs, YSs, IRs, and morpholino.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 23, 2013
    Applicant: GRADALIS, INC.
    Inventor: Nancy Smyth Templeton
  • Publication number: 20130131057
    Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: May 13, 2011
    Publication date: May 23, 2013
    Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO
    Inventors: Joaquin Pastor Fernández, Sonia Martínez Gonzalez, Antonlo Rodriguez Hergueta, Francisco Javier Ramos Lima, Rosa Maria Alvarez Escobar, Ana Isabel Higueras Hernandez
  • Patent number: 8445486
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: May 21, 2013
    Assignee: Wyeth LLC
    Inventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo Dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
  • Publication number: 20130109670
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 2, 2013
    Applicant: PFIZER INC.
    Inventor: PFIZER INC.
  • Patent number: 8415340
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: April 9, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Peiying Liu, Mark D. Wittman, David R. Langley
  • Publication number: 20130079303
    Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Application
    Filed: November 19, 2012
    Publication date: March 28, 2013
    Applicant: AMGEN INC.
    Inventor: Amgen Inc.
  • Publication number: 20130079345
    Abstract: 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: Application
    Filed: March 20, 2011
    Publication date: March 28, 2013
    Applicants: BAYER INTELLECTUAL PROPERTY GMBH, LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Peter Nussbaumer, Gerd Ruhter, Carsten Schultz-Fademrecht, Ulrich Lucking, Axel Choidas, Bert Klebl
  • Patent number: 8404765
    Abstract: The present invention relates to polypiperidine compounds capable of conferring to polymeric materials, particularly polyolefins, a high stability against photodegradation and oxidative action of air, which belong to the HALS category and have the following general formula (I) in which x can be zero or 1; y is between 1 and 10; m and n, which may be different or equal to each other, range from 2 to 8; A represents a NPiR1 group or a NR2R3 group; and Pi represents the group of formula (II) wherein R1 is selected from the group consisting of H, C1-C4 straight-chain and branched-chain alkyl groups; R2 and R3 can be the same or different and are selected in the group consisting of H, C1-C8 straight-chain and branched-chain alkyl groups, cyclic alkyl groups having from 5 to 12 carbon atoms, or form together with the nitrogen atom a heterocyclic ring having from 5 to 7 members, comprising other heteroatoms such as O, R4 is selected from the group consisting of H, C1-C4 straight-chain and branched-
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: March 26, 2013
    Assignee: 3V Sigma S.p.A.
    Inventors: Luca Bemporad, Ferruccio Berte, Carlo Seccomandi
  • Publication number: 20130040912
    Abstract: The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: UNIVERSITY OF BASEL
    Inventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
  • Publication number: 20130029982
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: July 18, 2012
    Publication date: January 31, 2013
    Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Publication number: 20130023497
    Abstract: The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: June 7, 2010
    Publication date: January 24, 2013
    Inventors: Chunlin Tao, Qinwei Wang, Tulay Polat, Laxman Nallan, Neil Desai
  • Publication number: 20130005723
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: June 6, 2012
    Publication date: January 3, 2013
    Inventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo Dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
  • Publication number: 20120329699
    Abstract: Novel compounds based on diaminostilbene are provided. The compounds conform to the general structures The compounds are useful as optical brighteners. Compositions, such as laundry compositions, containing such compounds are also provided.
    Type: Application
    Filed: September 4, 2012
    Publication date: December 27, 2012
    Applicant: MILLIKEN & COMPANY
    Inventors: Robert L. Mahaffey, Eduardo Torres, Dominick J. Valenti, Patrick D. Moore, Leland G. Close, JR.
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Publication number: 20120277233
    Abstract: The invention provides pyridyl-triazine derivatives to inhibit the hedgehog signaling pathway and the use of such compounds in the treatment of hyperproliferative diseases and angiogenisis mediated diseases.
    Type: Application
    Filed: June 8, 2010
    Publication date: November 1, 2012
    Applicant: California Capital Equity, LLC
    Inventors: Chunlin Tao, Hongna Han, Xiaowen Sun, Neil Desai
  • Publication number: 20120252802
    Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.
    Type: Application
    Filed: March 27, 2012
    Publication date: October 4, 2012
    Applicant: Pathway Therapeutics Inc.
    Inventors: S. David Brown, David J. Matthews
  • Publication number: 20120238576
    Abstract: The present invention comprises inter alia compounds as shown in formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 7, 2010
    Publication date: September 20, 2012
    Applicant: CALIFORNIA CAPITAL EQUITY, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Laxman Nallan, Tulay Polat, Lukasz Koroniak, Neil Desai
  • Publication number: 20120238577
    Abstract: Disclosed are compounds for inhibiting prostaglandin transporter (PGT) activity, pharmaceuticals compositions including the compounds, and methods of treating subjects using the compounds.
    Type: Application
    Filed: September 20, 2010
    Publication date: September 20, 2012
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Victor L. Schuster, Yuling Chi, Andrew S. Wasmuth, Richard S. Pottorf, Gary L. Olson
  • Patent number: 8262945
    Abstract: Photochromic compositions are disclosed comprising a polymeric material, a photochromic dye, a hydroxyphenyl triazine UV absorber and, optionally, a further light stabilizer selected from the sterically hindered amines. These systems provide a reversible photochromic effect and show improved light stabilization and color fastness.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Mara Destro, Dario Lazzari, Dirk Simon, Manuele Vitali
  • Publication number: 20120213729
    Abstract: 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: Application
    Filed: August 16, 2011
    Publication date: August 23, 2012
    Inventors: Li-Qiang Sun, Eric Mull, Qian Zhao, Tao Wang, Zhongxing Zhang, Paul Michael Scola
  • Publication number: 20120202814
    Abstract: The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4:
    Type: Application
    Filed: October 4, 2010
    Publication date: August 9, 2012
    Applicants: UNIVERSITÀ DEGLI STUDI DI SIENA, CONSIGLIO NAZIONALE DELLE RICERCHE
    Inventors: Marco Radi, Maurizio Botta, Federico Falchi, Giovanni Maga, Fausto Baldanti, Stefania Paolucci
  • Publication number: 20120202776
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: May 21, 2009
    Publication date: August 9, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Publication number: 20120196860
    Abstract: The invention provides Triazine derivatives and further provides methods of using these compounds to modulate protein kinases and for treating diseases and conditions mediated by protein kinases.
    Type: Application
    Filed: June 9, 2010
    Publication date: August 2, 2012
    Applicant: CALIFORNIA CAPITAL EQUITY, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Laxman Nallan, Tulay Polat, David Ho, Neil Desai
  • Publication number: 20120190682
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 26, 2012
    Inventors: Erwin Goetschi, Synese Jolidon, Thomas Luebbers
  • Patent number: 8227463
    Abstract: [Problems] The object is to improve the absorbability of a heterocyclic compound including s-triazine and a pyrimidine derivative in vitro. [Means for Solving Problems] Disclosed is, for example, an amorphous body of a heterocyclic compound as represented by the general formula (I) [wherein each of R's and others is as defined in the description] including s-triazine and a pyrimidine derivative, or a hydrate, a solvate or a pharmaceutically acceptable salt of the heterocyclic compound. Also disclosed is a process for producing the amorphous body. Further disclosed are: a solid dispersion comprising the amorphous body; and a medicinal preparation comprising the solid dispersion.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: July 24, 2012
    Assignee: Zenyaku Kogyo Kabushiki Kaisha
    Inventors: Tadaaki Sugama, Nobuhiro Ishihara, Yoshiharu Tanaka, Masayuki Takahashi, Shinichi Yaguchi, Tetsuo Watanabe
  • Patent number: 8217036
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: July 10, 2012
    Assignee: Wyeth LLC
    Inventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo Dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
  • Publication number: 20120172361
    Abstract: Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: June 7, 2010
    Publication date: July 5, 2012
    Applicant: CALIFORNIA CAPITAL EQUITY, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Tulay Polat, Laxman Nallan, David Ho, Neil Desai
  • Publication number: 20120165309
    Abstract: [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3K?-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided [Means for Solution] It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3K?-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, etc.), hematologic tumor (leukemia etc.
    Type: Application
    Filed: February 10, 2010
    Publication date: June 28, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
  • Patent number: 8188273
    Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.
    Type: Grant
    Filed: October 19, 2011
    Date of Patent: May 29, 2012
    Assignee: Dow AgroSciences, LLC.
    Inventors: Noormohamed M. Niyaz, Katherine A. Guenthenspberger, Ricky Hunter, Annette Vitale Brown, Jaime S. Nugent
  • Publication number: 20120071594
    Abstract: Compounds consisting of an oligomer or a polymer of a 1,3,5-triazine derivative, having the general formula I: and a solvent-free process for the production of the compounds of Formula I as well as the use of the self-extinguishing oligomeric or polymeric compounds as flame retardants and light stabilizers in thermoplastic polymers such as polypropylene or regenerated cellulose or polyester.
    Type: Application
    Filed: October 12, 2011
    Publication date: March 22, 2012
    Applicant: MCA Technologies GmbH
    Inventor: Bansi Lal Kaul
  • Publication number: 20120053167
    Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Application
    Filed: March 2, 2010
    Publication date: March 1, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
  • Publication number: 20120040837
    Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.
    Type: Application
    Filed: October 19, 2011
    Publication date: February 16, 2012
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Katherine A. Guenthenspberger, Ricky Hunter, Annette V. Brown, Jaime S. Nugent
  • Publication number: 20120022066
    Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Application
    Filed: July 20, 2011
    Publication date: January 26, 2012
    Applicant: Vestaron Corporation
    Inventors: Robert M. Kennedy, Bruce A. Steinbaugh
  • Publication number: 20120009151
    Abstract: Disclosed herein are novel triazines and related compounds, the synthesis thereof, and compositions, including pharmaceutical compositions, comprising the novel triazines and related compounds. Such novel triazines and related compounds function to inhibit or block entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
    Type: Application
    Filed: December 19, 2008
    Publication date: January 12, 2012
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Amy Qi Han, Glen A. Coburn, Kathleen P. Provoncha, Yakov Rotshteyn
  • Publication number: 20110319400
    Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.
    Type: Application
    Filed: June 27, 2011
    Publication date: December 29, 2011
    Inventors: Christopher M. Flores, Paul R. Wade
  • Publication number: 20110319414
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.
    Type: Application
    Filed: February 10, 2010
    Publication date: December 29, 2011
    Inventors: Hiroyuki Kai, Takayuki Kameyama, Tsuyoshi Hasegawa, MIho Oohara, Yukio Tada, Takeshi Endoh
  • Patent number: 8067588
    Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.
    Type: Grant
    Filed: September 26, 2008
    Date of Patent: November 29, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Noormohamed M. Niyaz, Katherine A. Guenthenspberger, Ricky Hunter, Annette V. Brown, Jaime S. Nugent
  • Publication number: 20110275762
    Abstract: The invention relates to novel therapeutic agents and diagnostic probes. The invention also relates to phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor triazine-, pyrimidine- and pyridine-based compounds? Formula (I), their stereoisomers, geometric isomers, tautomers, solvates, metabolites, N-oxide derivatives, pharmaceutically acceptable salts, and prodrugs thereof compositions of the new compounds; either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, for treating disorders mediated by lipid kinases. •Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 10, 2009
    Publication date: November 10, 2011
    Applicant: UNIVERSITY OF BASEL
    Inventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
  • Publication number: 20110275635
    Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.
    Type: Application
    Filed: January 8, 2010
    Publication date: November 10, 2011
    Applicant: THE UAB RESEARCH FOUNDATION
    Inventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
  • Patent number: 8039469
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: October 18, 2011
    Assignee: Wyeth LLC
    Inventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
  • Publication number: 20110237587
    Abstract: 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: Application
    Filed: August 28, 2008
    Publication date: September 29, 2011
    Applicants: HANALL PHARMACEUTICAL COMPANY, LTD, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Hyae Gyeong Cheon, Kwang-Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong-Cheol Lee, Sung Wuk Kim, Sung Soo Jun
  • Publication number: 20110218188
    Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: November 12, 2009
    Publication date: September 8, 2011
    Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Publication number: 20110207926
    Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.
    Type: Application
    Filed: August 24, 2009
    Publication date: August 25, 2011
    Applicant: HAMARI CHEMICALS, LTD.
    Inventors: Shirou Maeda, Akihisa Maeda
  • Publication number: 20110190264
    Abstract: The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.
    Type: Application
    Filed: April 3, 2009
    Publication date: August 4, 2011
    Applicant: IRM LLC
    Inventors: Tao Jiang, Pierre-Yves Michellys, Truc Ngoc Nguyen, Wei Pei, Baogen Wu, Xuefeng Zhu
  • Publication number: 20110183954
    Abstract: The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: December 17, 2009
    Publication date: July 28, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Lynsie Almeida, Claudio Edmundo Chuaqui, Stephanos Loannidis, Bo Peng, Mei Su
  • Publication number: 20110152240
    Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.
    Type: Application
    Filed: November 15, 2010
    Publication date: June 23, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas B. Raffaele, Suchitra Ravula, David M. Ryckman