Polycyclo Ring System Having The Asymmetrical Triazine Ring As One Of The Cyclos Patents (Class 544/183)
  • Patent number: 10329295
    Abstract: The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: March 7, 2016
    Date of Patent: June 25, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Michael D. Altman, Jason D. Brubaker, Craig R. Gibeau
  • Patent number: 10294241
    Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: May 21, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventor: Makoto Kawai
  • Patent number: 10000496
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDGFR are described herein.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: June 19, 2018
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Kevin J. Wilson, Yulian Zhang
  • Patent number: 9994575
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: June 12, 2018
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Patent number: 9944651
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: April 17, 2018
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Patent number: 9598416
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[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: Grant
    Filed: December 11, 2012
    Date of Patent: March 21, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marie-Pierre Collin, Dirk Brohm, Mélanie Héroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Patent number: 9475815
    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: Grant
    Filed: February 20, 2013
    Date of Patent: October 25, 2016
    Assignee: BAYER INTELLETUAL PROPERTY GMBH
    Inventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Voehringer, Niels Lindner
  • Patent number: 9469638
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: October 18, 2016
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Patent number: 9403834
    Abstract: A compound of formula (I), wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: August 2, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Srinivasu Pothukanuri
  • Patent number: 9388189
    Abstract: New pyrrolotriazinone derivatives having the chemical structure of Formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: July 12, 2016
    Assignee: Almirall, S.A.
    Inventors: Montserrat Erra Sola, Marta Carrascal Riera, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Francisco Javier Bernal Anchuela, Lluis Miquel Pages Santacana, Marta Mir Cepeda, Gaspar Casals Coll, Maria Begoña Hernandez Olasagarre
  • Patent number: 9340547
    Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: May 17, 2016
    Assignee: Almirall, S.A.
    Inventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Taltavull Moll, Montserrat Erra Sola
  • Patent number: 9206184
    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: Grant
    Filed: December 14, 2012
    Date of Patent: December 8, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer
  • Patent number: 9050345
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: June 9, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Kavitha Govindrajulu, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • Patent number: 9040691
    Abstract: This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), 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 angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: May 26, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Klar, Verena Vöhringer, Joachim Telser, Mario Lobell, Frank Süβmeier, Volkhart Min-Jian Li, Michael Böttger, Stefan Golz, Dieter Lang, Karl-Heinz Schlemmer, Thomas Schlange, Andreas Schall, Wenlang Fu
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Patent number: 9034485
    Abstract: The present invention relates to compounds of the formula (1) and to the use thereof in organic electronic devices, and to organic electronic devices which comprise compounds of the formula (1), preferably as hole-transport materials and/or as emitting materials.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: May 19, 2015
    Assignee: Merck Patent GmbH
    Inventors: Arne Buesing, Holger Heil, Philipp Stoessel, Amir Hossain Parham, Rocco Fortte, Jonas Valentin Kroeber
  • Publication number: 20150133453
    Abstract: Compounds of the formula I in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: April 6, 2013
    Publication date: May 14, 2015
    Applicant: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller
  • Publication number: 20150111887
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 23, 2015
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Publication number: 20150111854
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 23, 2015
    Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
  • Publication number: 20150099752
    Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
    Type: Application
    Filed: April 26, 2012
    Publication date: April 9, 2015
    Applicant: ALMIRALL, SA
    Inventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Tal Tavul Moll, Montserat Eraa Sola
  • Publication number: 20150094309
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 2, 2015
    Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
  • Patent number: 8987441
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
  • Publication number: 20150080371
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[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 11, 2012
    Publication date: March 19, 2015
    Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150031876
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Application
    Filed: September 5, 2014
    Publication date: January 29, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Publication number: 20150031676
    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: February 20, 2013
    Publication date: January 29, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Patent number: 8940412
    Abstract: An organic electroluminescence device and a material for producing the organic electroluminescence device. The organic electroluminescence device includes an organic thin film layer between a cathode and an anode, the organic thin film layer including one or more layers, in which the organic thin film layer includes one or more light emitting layers and at least one of the light emitting layers includes a phosphorescent material and a host material. The host material has an essential structure in which a naphthalene ring is bonded to a fluorene skeleton, dibenzofuran skeleton, or dibenzothiophene skeleton. The organic electroluminescence device is a phosphorescent device having high efficiency and long lifetime.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 27, 2015
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yoriyuki Takashima, Toshihiro Iwakuma, Toshinari Ogiwara, Chishio Hosokawa, Mitsunori Ito
  • Patent number: 8937175
    Abstract: The invention relates to novel compounds as ligands for transition metal complexes and materials made thereof that can be used, for example, as emitters in organic light-emitting electrochemical cells (OLEECs). According to the invention, non-fluorinated electron-poor emitter materials are disclosed for the first time that can be used in organic light-emitting electrochemical cells.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: January 20, 2015
    Assignee: Osram GmbH
    Inventors: Andreas Kanitz, Daniel Stark
  • Patent number: 8927710
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: January 6, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20140378305
    Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Patent number: 8916598
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: December 23, 2014
    Assignee: Proteotech Inc
    Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow
  • Publication number: 20140336173
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, 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 10, 2012
    Publication date: November 13, 2014
    Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
  • Patent number: 8865623
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140256719
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Kavitha Govindrajulu, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • Patent number: 8829185
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: September 9, 2014
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Steven Magnuson, Barton Phillips, Yamin Wang, Tindy Li, Kyle Parcella, Jason Newcom, Harold C. E. Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Kristen M. Allegue, Zhen Liu
  • Patent number: 8815417
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: August 26, 2014
    Assignee: Samsung Display Co., Ltd.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
  • Patent number: 8802675
    Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
    Type: Grant
    Filed: January 31, 2010
    Date of Patent: August 12, 2014
    Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.
    Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
  • Publication number: 20140221377
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
  • Publication number: 20140221333
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 19, 2012
    Publication date: August 7, 2014
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Patent number: 8791257
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jay A. Markwalder, Brian E. Fink, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Steven P. Seitz
  • Patent number: 8778893
    Abstract: The present invention is directed to metabolites of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of cancer.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: July 15, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jiachang Gong, Lisa J. Christopher, Vinod Kumar Arora
  • Patent number: 8765754
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: July 1, 2014
    Assignee: Locus Pharmaceuticals, Inc.
    Inventors: Zenon Konteatis, Kristofer Moffett, Younghee Lee, Wenchun Chao, Dora Do-York Wong
  • Patent number: 8754211
    Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishnan Sridhar
  • Publication number: 20140163033
    Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
    Type: Application
    Filed: April 26, 2012
    Publication date: June 12, 2014
    Applicant: ALMIRALL, SA
    Inventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Tal Tavul Moll, Montserat Eraa Sola
  • Publication number: 20140148459
    Abstract: This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and pounds.
    Type: Application
    Filed: September 26, 2011
    Publication date: May 29, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Manoj Kumar Khera, Ajay Soni, Jitendra Sattigeri, Viswajanani Sattigeri, Biswajit Das, Ian A. Cliffe, Pradip Kumar Bhatnagar, Abdul Rehman Abdul Rauf, Arpita Musib, Subham Saha, Neeraj Kumar Yadav, Sabir Ahammed, Ranadheer R. Reddy, Abhijit Ray, Punit Srivastava, Sunanda Ghosh Dastidar
  • Patent number: 8716473
    Abstract: The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O?); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: May 6, 2014
    Assignee: Sentinel Oncology Limited
    Inventors: Robert George Boyle, David Winter Walker
  • Patent number: 8715621
    Abstract: The present invention provides a variety of radicals, which are useful as polarizing compounds. Exemplary radicals are represented by compounds of Structural Formulae (I), (II), (III) and (IV) as described herein.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 6, 2014
    Assignee: Massachusetts Institute of Technology
    Inventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
  • Patent number: 8710261
    Abstract: The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5R?, —NHC(?O)OR4, —NHSO2R4, C(?Y)NR4R5, C(?O)OR6 [wherein Y is oxygen or sulphur], OR5, —O(C?O)NR4R5, O-acyl, S(O)mR4, —SO2N(R4)2, cyano, amidino or guanidino [wherein R4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R5 is hydrogen or R4; Rx is R4 or —SO2N(R4)2 and R6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4, —OC(?O)NR4R5, O-acyl, NH2, NR4R5, —NHC(?Y)R4, —NHC(?Y)NR5Rx, —NHC(?O)OR4, —NHSO2R4, and to processes for t
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: April 29, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Venkata P. Palle, Viswajanani Jitendra Sattigeri, Manoj Kumar Khera, Sreedhara Rao Voleti, Abhijit Ray, Sunanda G. Dastidar
  • Patent number: 8691818
    Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic infl
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: April 8, 2014
    Assignee: University Of Greenwich
    Inventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
  • Patent number: 8691981
    Abstract: Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: April 8, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Roxana Schlam, Alicia Tee Fuay Ng, Chenkou Wei