1,3,5-triazine Ring Patents (Class 544/113)
  • Patent number: 9951040
    Abstract: The present invention describes heterocyclic compounds of general Formula 1 and their method of preparation thereof. The present invention describes general Formula 1 which inhibits phosphoinositide 3-kinase (PI3K) and can be used as the anticancer agents.
    Type: Grant
    Filed: November 17, 2015
    Date of Patent: April 24, 2018
    Assignee: Council of Scientific and Industrial Research
    Inventors: Thanusha Thatikonda, Suresh Kumar, Umed Singh, Priya Mahajan, Girish Mahajan, Amit Nargotra, Fayaz Malik, Dilip Manikrao Mondhe, Ram Asrey Vishwakarma, Parvinder Pal Singh
  • Patent number: 9938234
    Abstract: Provided herein are compounds and compositions useful in increasing PPAR? activity. The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: April 10, 2018
    Assignees: Salk Institute for Biological Studies, Mitobridge, Inc.
    Inventors: Ronald M. Evans, Michael Downes, Thomas J. Baiga, Joseph P. Noel, Emi Kanakubo Embler, Weiwei Fan, John F. W. Keana, Mark G. Bock, Arthur F. Kluge, Mike A. Patane
  • Patent number: 9567345
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]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 pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: February 14, 2017
    Assignee: Lead Discovery Center GmbH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Patent number: 9175011
    Abstract: The invention relates to compounds of formula (I) wherein m, n, R1, T0 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds as well as methods of treating mTOR related diseases.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: November 3, 2015
    Assignee: CELLZONE LIMITED
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150126510
    Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
    Type: Application
    Filed: March 18, 2013
    Publication date: May 7, 2015
    Applicants: Universiteit Antwerpen, Shakturana CV
    Inventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
  • Publication number: 20150126506
    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: January 8, 2015
    Publication date: May 7, 2015
    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: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150111873
    Abstract: Pyrazolo[1,5-a][1,3,5]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 pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 23, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
  • Publication number: 20150065705
    Abstract: There is provided a novel triazinone compound that has an excellent T-type voltage-dependent calcium channel inhibitory activity and is specifically useful for treatment of pain. A compound of Formula (I), a tautomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof: where each substituent is defined in detail in the description or claims, for example R1 is H or C1-6 alkoxy, etc., each of L1 and L2 is independently a single bond or NR2, etc., L3 is C1-6 alkylene, etc., A is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc., B is C3-11 cycloalkylene, etc., D is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Inventors: Noriko Saito, Jun Egi, Hiroshi Nagai, Megumi Ueno, Yusuke Shintani, Yusuke Inaba, Michiaki Adachi, Yuichi Hirai, Takeshi Kawazu, Koichi Yasutake, Daiki Takahashi
  • Publication number: 20150057395
    Abstract: Compounds consisting of an oligomer or a polymer of a 1,3,5-triazine derivative, having the general formula I: wherein: X is selected from: or X is a heterocyclic radical containing in the ring at least one nitrogen atom which radical is linked to the triazine ring through one of such nitrogen atoms, R2 is alkyl or cycloalkyl, R1 is a divalent radical of piperazine of the formula or R2 is a divalent radical according to the formula or R2 is a radical according to the formula Y n is an integer from 2 to 30, inclusive, m is an integer from 2 to 6, inclusive, p is an integer from 2 to 12, inclusive, and X1=OH, NH2 or X whereby X and X1 may be the same or different, and, X2=H or is a C1-C4 alkyl group, 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 31, 2014
    Publication date: February 26, 2015
    Inventor: Bansi Lal Kaul
  • Publication number: 20150045365
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: August 6, 2014
    Publication date: February 12, 2015
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
  • Publication number: 20150025057
    Abstract: 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: Application
    Filed: October 8, 2014
    Publication date: January 22, 2015
    Applicant: NOVARTIS AG
    Inventors: 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
  • Publication number: 20150018329
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]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 pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 15, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Publication number: 20150018328
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
  • Publication number: 20150011752
    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: September 4, 2014
    Publication date: January 8, 2015
    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: 20150011751
    Abstract: To provide a novel triazine derivative represented by the following formula (I): A triazine derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, a substituted or unsubstituted heterocyclic fused ring, or a substituted or unsubstituted alkynyl group, R2 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group, R3 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic ring, or a substituted or unsubstituted heterocyclic fused ring, R4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, or a halogen atom, and R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, or R1 and R5 may be combined to form a saturated or unsaturate
    Type: Application
    Filed: March 7, 2013
    Publication date: January 8, 2015
    Inventors: Wataru Kawahata, Tokiko Asami, Masaaki Sawa, Yuko Asamitsu, Takayuki Irie, Takahiro Miyake, Takao Kiyoi
  • Publication number: 20140378443
    Abstract: The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.
    Type: Application
    Filed: June 20, 2014
    Publication date: December 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20140378438
    Abstract: The invention relates to compounds of formula (I) wherein m, n, R1, T0 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds as well as methods of treating mTOR related diseases.
    Type: Application
    Filed: September 21, 2012
    Publication date: December 25, 2014
    Applicant: CELLZOME LIMITED
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
  • Patent number: 8912180
    Abstract: Provided is a novel compound which is an agent for treating rejection reactions in various organ transplantations, allergy diseases, autoimmune diseases, and hematologic tumor, and 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). The provided compound has a PI3K? selective inhibitory action, an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action, including an activation inhibitory action.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: December 16, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Fumie Takahashi, Sunao Imada, Toru Asano, Yoshihiro Kozuki, Junko Maeda, Koji Kato, Hidehiko Fukahori, Masahiko Shiwaku
  • Publication number: 20140343061
    Abstract: The present invention relates to compounds corresponding to formula (I) in which: —R1 represents a substituted phenyl; —R2 represents: —a substituted phenyl; —a heteroaromatic group, the said group being unsubstituted or substituted one or more times; —R3 represents a group Alk; —R4 represents a hydrogen atom or a (C1-C4)alkyl; —R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; —or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; —R6 represents a group —COOAlk, a group —CONH2 or a group —NHSO2Alk; —Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use.
    Type: Application
    Filed: December 11, 2012
    Publication date: November 20, 2014
    Inventors: Joelle Arnaud, Martine Artiaga, Francis Barth, Laurent Hortala, Serge Martinez, Pascale Roux
  • Publication number: 20140303167
    Abstract: The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
    Type: Application
    Filed: August 22, 2012
    Publication date: October 9, 2014
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Patent number: 8835629
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: September 16, 2014
    Assignee: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard
  • Publication number: 20140255386
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: July 24, 2012
    Publication date: September 11, 2014
    Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTE
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Publication number: 20140249128
    Abstract: The present disclosure provides substituted triazine carboxamides of Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, E, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 4, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Dawit Tadesse, Jianming Yu
  • Publication number: 20140213784
    Abstract: The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 31, 2014
    Applicant: SANDOZ AG
    Inventors: Hubert Sturm, Kerstin Knepper
  • Patent number: 8772287
    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: June 10, 2013
    Date of Patent: July 8, 2014
    Assignee: VetDC, Inc.
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Publication number: 20140179662
    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 1, 2012
    Publication date: June 26, 2014
    Applicants: LEAD DISCOVERY CENTER GMBH, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
  • Patent number: 8748421
    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: July 25, 2013
    Date of Patent: June 10, 2014
    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: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • Publication number: 20140134130
    Abstract: 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: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Publication number: 20140088103
    Abstract: Provided herein are (fused ring arylamino and heterocyclylamino) 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: March 27, 2014
    Applicant: MEI PHARMA, INC.
    Inventors: S. David Brown, David J. Matthews
  • Publication number: 20140088102
    Abstract: Provided herein are (alpha-substituted cycloalkylamino or heterocyclylamino) 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: March 27, 2014
    Applicant: MEI PHARMA, INC.
    Inventors: S. David Brown, David J. Matthews
  • Publication number: 20140066406
    Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD PHARMACEUTICALS, INC.
  • Publication number: 20140051676
    Abstract: 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: Application
    Filed: October 15, 2013
    Publication date: February 20, 2014
    Applicant: NOVARTIS AG
    Inventors: 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
  • Publication number: 20130317217
    Abstract: For the separation, removal, isolation, purification, characterisation, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—CI or C—CN; Y is O, S or NR2; Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or ?-phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.
    Type: Application
    Filed: July 30, 2013
    Publication date: November 28, 2013
    Applicant: PROMETIC BIOSCIENCES LTD
    Inventors: JASON RICHARD BETLEY, JAMES CHRISTOPHER PEARSON, BEN MARTIN BEACOM, TADEUSZ ANTONI PODGORSKI, ROBERT WILLIAM PANNELL
  • Publication number: 20130315865
    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: July 25, 2013
    Publication date: November 28, 2013
    Applicant: PFIZER INC.
    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: 20130303516
    Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
    Type: Application
    Filed: January 25, 2012
    Publication date: November 14, 2013
    Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
  • Patent number: 8575159
    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: December 18, 2012
    Date of Patent: November 5, 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: 20130289016
    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: Application
    Filed: June 10, 2013
    Publication date: October 31, 2013
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Publication number: 20130261119
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or pro-drug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: October 27, 2011
    Publication date: October 3, 2013
    Applicant: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
  • Patent number: 8512421
    Abstract: A polyurethane derivative and a composition thereof are disclosed. The polyurethane derivative of the present invention has a structure of formula (I). The polyurethane derivative and the composition thereof can be used for increasing light fastness.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Everlight Chemical Industrial Corporation
    Inventors: Hsin-Ying Lu, Sheue-Rong Lee, Tzu-Heng Ko, Hsiang-Lin Chiang, Der-Gun Chou
  • Publication number: 20130203904
    Abstract: The present invention relates to polypiperidine compounds of polymeric type which are capable of conferring to the polymeric materials, particularly to polyolefins, a high stability against photodegradation and oxidative action of air, belong to the HALS category and have general formula (I): wherein p is from 3 to 20; n is from 2 to 12; R and R1, which are the same or different, are selected in the group consisting of hydrogen, linear and branched C1-C12 alkyl groups, alkenyl groups having 3 to 8 carbon atoms and aralkyl groups having 7 to 19 carbon atoms; X and X1, which are the same or different, are selected in the group consisting oxygen and groups of formula (II) wherein R2 is selected in the group consisting of hydrogen, linear and branched C1-C12 alkyl groups, cycloalkyl groups having, 5 to 12 carbon atoms and aralkyl groups having 7 to 12 carbon atoms; A represents a —(CH2)a— group wherein a is from 2 to 12, with the proviso that a is different from n; Z is selected in the group consist
    Type: Application
    Filed: October 27, 2011
    Publication date: August 8, 2013
    Applicant: 3V SIGMA S.P.A.
    Inventors: Francesco Maestri, Simone Del Sordo, Ferruccio Berte
  • Publication number: 20130203758
    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: February 4, 2013
    Publication date: August 8, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130190287
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 25, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC.
    Inventor: AGIOS PHARMACEUTICALS, INC.
  • Patent number: 8486939
    Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, 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: July 6, 2010
    Date of Patent: July 16, 2013
    Assignee: Pathway Therapeutics Inc.
    Inventors: Gordon William Rewcastle, Kit Yee Tsang, Swarnalatha Akuratiya Gamage, Anna Claire Giddens
  • Publication number: 20130172317
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Rj are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstituted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: July 4, 2013
    Inventors: Hiroyuki Kai, Takayuki Kameyama, Tohru Horiguchi, Kentaro Asahi, Takeshi Endoh, Yasuhiko Fujii, Takuya Shintani, Ken'ichiroh Nakamura, Sae Jikihara, Tsuyoshi Hasegawa, Miho Oohara, Yukio Tada, Toshikatsu Maki, Akira Iida
  • Publication number: 20130158000
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventor: BAYER INTELLECTUAL PROPERTY GmbH
  • 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