1,3,5-triazine Ring Patents (Class 544/113)
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1,3,5 -triazine based PI3K inhibitors as anticancer agents and a process for the preparation thereof
Patent number: 9951040Abstract: 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: GrantFiled: November 17, 2015Date of Patent: April 24, 2018Assignee: Council of Scientific and Industrial ResearchInventors: 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: 9938234Abstract: 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: GrantFiled: October 2, 2015Date of Patent: April 10, 2018Assignees: 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
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Patent number: 9567345Abstract: 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: GrantFiled: March 1, 2013Date of Patent: February 14, 2017Assignee: Lead Discovery Center GmbHInventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
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Patent number: 9175011Abstract: 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: GrantFiled: September 21, 2012Date of Patent: November 3, 2015Assignee: CELLZONE LIMITEDInventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
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Patent number: 9040558Abstract: 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: GrantFiled: December 28, 2005Date of Patent: May 26, 2015Assignee: 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
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Publication number: 20150126510Abstract: 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: ApplicationFiled: March 18, 2013Publication date: May 7, 2015Applicants: Universiteit Antwerpen, Shakturana CVInventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
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Publication number: 20150126506Abstract: 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: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: 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
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Publication number: 20150111873Abstract: 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: ApplicationFiled: March 1, 2013Publication date: April 23, 2015Applicant: LEAD DISCOVERY CENTER GMBHInventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch, Gerd Rühter, Carsten Schultz-Fademrecht, Peter Nussbaumer
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Publication number: 20150065705Abstract: 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: ApplicationFiled: March 29, 2013Publication date: March 5, 2015Inventors: Noriko Saito, Jun Egi, Hiroshi Nagai, Megumi Ueno, Yusuke Shintani, Yusuke Inaba, Michiaki Adachi, Yuichi Hirai, Takeshi Kawazu, Koichi Yasutake, Daiki Takahashi
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Publication number: 20150057395Abstract: 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: ApplicationFiled: October 31, 2014Publication date: February 26, 2015Inventor: Bansi Lal Kaul
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Publication number: 20150045365Abstract: 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: ApplicationFiled: August 6, 2014Publication date: February 12, 2015Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
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Publication number: 20150025057Abstract: 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 8, 2014Publication date: January 22, 2015Applicant: 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: 20150018328Abstract: 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: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Applicant: AGIOS PHARMACEUTICALS, INCInventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
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Publication number: 20150018329Abstract: 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: ApplicationFiled: March 1, 2013Publication date: January 15, 2015Applicant: LEAD DISCOVERY CENTER GMBHInventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
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Publication number: 20150011752Abstract: 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: ApplicationFiled: September 4, 2014Publication date: January 8, 2015Inventors: 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
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Publication number: 20150011751Abstract: 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 unsaturateType: ApplicationFiled: March 7, 2013Publication date: January 8, 2015Inventors: Wataru Kawahata, Tokiko Asami, Masaaki Sawa, Yuko Asamitsu, Takayuki Irie, Takahiro Miyake, Takao Kiyoi
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Publication number: 20140378438Abstract: 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: ApplicationFiled: September 21, 2012Publication date: December 25, 2014Applicant: CELLZOME LIMITEDInventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Mihiro Sunose, Adeline Morel, Laura Convery, Rita Adrego
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Publication number: 20140378443Abstract: 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: ApplicationFiled: June 20, 2014Publication date: December 25, 2014Inventors: William L. Jorgensen, Karen S. Anderson
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Patent number: 8912180Abstract: 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: GrantFiled: February 8, 2013Date of Patent: December 16, 2014Assignee: Astellas Pharma Inc.Inventors: Fumie Takahashi, Sunao Imada, Toru Asano, Yoshihiro Kozuki, Junko Maeda, Koji Kato, Hidehiko Fukahori, Masahiko Shiwaku
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Publication number: 20140343061Abstract: 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: ApplicationFiled: December 11, 2012Publication date: November 20, 2014Inventors: Joelle Arnaud, Martine Artiaga, Francis Barth, Laurent Hortala, Serge Martinez, Pascale Roux
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Publication number: 20140303167Abstract: 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: ApplicationFiled: August 22, 2012Publication date: October 9, 2014Applicant: LEAD DISCOVERY CENTER GMBHInventors: Axel Choidas, Bert Klebl, Peter Habenberger, Jan Eickhoff, Roman Thomas, Johannes Heuckmann
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Publication number: 20140275024Abstract: 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: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
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Patent number: 8835629Abstract: 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: GrantFiled: October 27, 2011Date of Patent: September 16, 2014Assignee: The Walter and Eliza Hall Institute of Medical ResearchInventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard
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Publication number: 20140255386Abstract: 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: ApplicationFiled: July 24, 2012Publication date: September 11, 2014Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTEInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20140249128Abstract: 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: ApplicationFiled: February 26, 2014Publication date: September 4, 2014Applicant: Purdue Pharma L.P.Inventors: Dawit Tadesse, Jianming Yu
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Publication number: 20140213784Abstract: 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: ApplicationFiled: April 11, 2012Publication date: July 31, 2014Applicant: SANDOZ AGInventors: Hubert Sturm, Kerstin Knepper
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Patent number: 8772287Abstract: 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: GrantFiled: June 10, 2013Date of Patent: July 8, 2014Assignee: VetDC, Inc.Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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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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Patent number: 8748421Abstract: 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: GrantFiled: July 25, 2013Date of Patent: June 10, 2014Assignee: Wyeth LLCInventors: 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
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Publication number: 20140134235Abstract: 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: ApplicationFiled: October 14, 2013Publication date: May 15, 2014Applicant: 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
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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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Publication number: 20140088102Abstract: 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: ApplicationFiled: March 27, 2012Publication date: March 27, 2014Applicant: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Publication number: 20140088103Abstract: 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: ApplicationFiled: March 27, 2012Publication date: March 27, 2014Applicant: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Publication number: 20140066406Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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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: 20130315865Abstract: 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: ApplicationFiled: July 25, 2013Publication date: November 28, 2013Applicant: 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
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Publication number: 20130317217Abstract: 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: ApplicationFiled: July 30, 2013Publication date: November 28, 2013Applicant: PROMETIC BIOSCIENCES LTDInventors: JASON RICHARD BETLEY, JAMES CHRISTOPHER PEARSON, BEN MARTIN BEACOM, TADEUSZ ANTONI PODGORSKI, ROBERT WILLIAM PANNELL
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Publication number: 20130303516Abstract: 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: ApplicationFiled: January 25, 2012Publication date: November 14, 2013Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
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Patent number: 8575159Abstract: 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: GrantFiled: December 18, 2012Date of Patent: November 5, 2013Assignee: Wyeth LLCInventors: 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
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Publication number: 20130289016Abstract: 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: ApplicationFiled: June 10, 2013Publication date: October 31, 2013Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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Publication number: 20130261119Abstract: 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: ApplicationFiled: October 27, 2011Publication date: October 3, 2013Applicant: The Walter and Eliza Hall Institute of Medical ResearchInventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
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Patent number: 8512421Abstract: 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: GrantFiled: September 18, 2012Date of Patent: August 20, 2013Assignee: Everlight Chemical Industrial CorporationInventors: Hsin-Ying Lu, Sheue-Rong Lee, Tzu-Heng Ko, Hsiang-Lin Chiang, Der-Gun Chou
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Publication number: 20130203904Abstract: 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 consistType: ApplicationFiled: October 27, 2011Publication date: August 8, 2013Applicant: 3V SIGMA S.P.A.Inventors: Francesco Maestri, Simone Del Sordo, Ferruccio Berte
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Publication number: 20130203758Abstract: 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: ApplicationFiled: February 4, 2013Publication date: August 8, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130190287Abstract: 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: ApplicationFiled: January 7, 2013Publication date: July 25, 2013Applicant: AGIOS PHARMACEUTICALS, INC.Inventor: AGIOS PHARMACEUTICALS, INC.
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Patent number: 8486939Abstract: 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: GrantFiled: July 6, 2010Date of Patent: July 16, 2013Assignee: Pathway Therapeutics Inc.Inventors: Gordon William Rewcastle, Kit Yee Tsang, Swarnalatha Akuratiya Gamage, Anna Claire Giddens
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Publication number: 20130172317Abstract: 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: ApplicationFiled: August 9, 2011Publication date: July 4, 2013Inventors: 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
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Publication number: 20130158000Abstract: 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: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventor: BAYER INTELLECTUAL PROPERTY GmbH
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Publication number: 20130150364Abstract: [Problem] A novel and excellent compound which is useful as an agent for preventing and/or 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). [Means for Solution] The present inventors have investigated a compound having 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 have found that the heterocyclic compound of the present invention has a PI3K? selective inhibitory action and/or and IL-2 production inhibitory action and/or a B cell proliferation inhibitory action (including an activation inhibitory action), thereby completing the present invention.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.