Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Bicyclo Ring System Patents (Class 514/264.11)
  • Patent number: 10253029
    Abstract: The disclosure includes compounds of Formula (I) wherein Warhead1, Warhead2, R3, R4, R5, R6, R7, R8, Q, A, B, p, q, Z1, Z2, Z3, and Z4 are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: April 9, 2019
    Assignee: Newave Pharmaceutical Inc.
    Inventors: Yi Chen, Yan Lou
  • Patent number: 10233160
    Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: March 19, 2019
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Ruoxi Lan, Justin Potnick, Lizbeth Celeste DeSelm, Mark W. Cronin, Jr., Constantin Neagu, Xiaoling Chen, Roch Boivin, Theresa L. Johnson, Andreas Goutopoulos
  • Patent number: 10221154
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: March 5, 2019
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Patent number: 10000490
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: June 19, 2018
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Chandrasekhar V. Miduturu
  • Patent number: 9980942
    Abstract: The present invention relates generally to methods and pharmaceutical compositions for rejuvenating hematopoietic stem cells and progenitor cells from blood, intestinal tissue and dermal tissue by administration of at least one inhibitor of a GT-Pase, such as Cdc42 GTPase.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: May 29, 2018
    Assignees: CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITAET ULM
    Inventors: Hartmut Geiger, Maria Carolina Florian, Yi Zheng
  • Patent number: 9914730
    Abstract: The present application provides azaquinazoline compounds as defined herein. This application further describes compositions comprising the same. These azaquinazoline compounds and their salts have atypical protein kinase C (“aPKC”) inhibitory activity, and may be used to treat proliferative disorders.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: March 13, 2018
    Assignee: Cancer Research Technology Limited
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J Dugan, Katherine M. Fowler, Robert L Hudkins, Eugen F. Mesaros, Nathaniel J. T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Patent number: 9718815
    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: Grant
    Filed: January 8, 2015
    Date of Patent: August 1, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 9662333
    Abstract: A tetrahydropyridopyrimidine compound represented by formula (I) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition including the tetrahydropyridopyrimidine compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier:
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: May 30, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
  • Patent number: 9629925
    Abstract: The present disclosure relates to immunoglobulins and immunoglobulin conjugates with reduced oligomerization and efficient labeling and compositions, methods of generating such immunoglobulins and immunoglobulin conjugates and methods of using such immunoglobulin conjugates particularly in the treatment and prevention of disease.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: April 25, 2017
    Assignees: Novartis AG, Massachusetts Institute of Technology
    Inventors: Naresh Chennamsetty, Bernhard Helk, Veysel Kayser, Bernhardt Trout, Vladimir Voynov
  • Patent number: 9630963
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: April 25, 2017
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Kenneth Albert Brameld, Erik Verner
  • Patent number: 9440968
    Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: September 13, 2016
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Ruoxi Lan, Justin Potnick, Lizbeth Celeste Deselm, Mark W. Cronin, Jr., Constantin Neagu, Xiaoling Chen, Roch Boivin, Theresa L. Johnson, Andreas Goutopoulos
  • Patent number: 9409900
    Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: August 9, 2016
    Assignees: FUJIAN HAIXI PHARMACEUTICALS, INC., BETTA PHARMACUETICALS CO., LTD.
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
  • Patent number: 9334267
    Abstract: This invention provides compounds of Formula I: (Formula I should be inserted here) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula I; and use of a compound of Formula I for treating specified cancers.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: May 10, 2016
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
  • Patent number: 9266857
    Abstract: This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: February 23, 2016
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Patent number: 9180129
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: November 10, 2015
    Assignee: NOVARTIS AG
    Inventors: Tona M. Gilmer, Rakesh Kumar
  • Patent number: 9133192
    Abstract: This invention relates to piperidino-pyhmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: September 15, 2015
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Mourad Daoubi Khamlichi
  • Patent number: 9045485
    Abstract: This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2 and R3 are as defined herein, and their use as pharmaceuticals.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: June 2, 2015
    Assignee: CONVERGENCE PHARMACEUTICALS LIMITED
    Inventors: David R. Witty, David Norton, Jason Paul Tierney, Ghislaine Lorthioir, Mairi Sime, Karen Louise Philpott
  • 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: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20150119392
    Abstract: This invention provides compounds of Formula I: (Formula I should be inserted here) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula I; and use of a compound of Formula I for treating specified cancers.
    Type: Application
    Filed: March 5, 2013
    Publication date: April 30, 2015
    Inventors: Daniel L. Flynn, Michael D. Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Publication number: 20150087627
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.
    Type: Application
    Filed: April 15, 2014
    Publication date: March 26, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • Publication number: 20150086543
    Abstract: The present invention provides methods of predicting response to a cancer therapy based on the methylation status of the ERBB2 gene. One aspect of the invention provides a method of predicting response to an EGFR inhibitor therapy based on the methylation status of the ERBB2 gene.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 26, 2015
    Applicant: GENENTECH, INC.
    Inventors: Thomas E. Januario, David Shames
  • Patent number: 8975250
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 10, 2015
    Assignee: SANOFI
    Inventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
  • Publication number: 20150064238
    Abstract: The invention provides a method for enhancing the delivery of an anti-platelet drug for the treatment of acute stroke, comprising delivering a composition comprising an anti-platelet drug and a vehicle that can reduce the binding rate of plasma proteins, so that the anti-platelet drug can achieve the effect of treating acute stroke at a low dose. By use of the neuro-protective efficacy of anti-platelet drug, the invention allows the drug to release slowly to the site of treatment by combining anti-platelet drugs with a vehicle that can reduce the binding rate of plasma proteins to effectively reduce the dose of the anti-platelet drug and consequently reduce the side effects such as hypotension caused by, administration of a high dose of the anti-platelet drugs. The invention also provides a pharmaceutical composition for enhancing treatment of acute stroke and a method for treating acute stroke using the pharmaceutical composition of the invention.
    Type: Application
    Filed: July 28, 2014
    Publication date: March 5, 2015
    Inventor: Jen Cheng Lin
  • Patent number: 8969363
    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: Grant
    Filed: July 18, 2012
    Date of Patent: March 3, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Patent number: 8952018
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: February 10, 2015
    Assignee: GlaxosmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Publication number: 20150031693
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.
    Type: Application
    Filed: November 2, 2012
    Publication date: January 29, 2015
    Applicant: AFRAXIS HOLDINGS, INC.
    Inventors: John C. Mckew, Wenwei Huang, David Campbell, Sergio G. Durön, Mark Behnke, Min Shen
  • Publication number: 20150031672
    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: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150031674
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: GENENTECH, INC.
    Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
  • Publication number: 20150025090
    Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
  • Publication number: 20140378481
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 25, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Publication number: 20140377285
    Abstract: The present invention provides for methods and pharmaceutical compositions for treating disorders using treatment regimens involving multiple agents. In one aspect, a method of treatment is provided resulting in reduced toxicity and/or synergistic effect by administration according to a described dosing schedule.
    Type: Application
    Filed: November 8, 2012
    Publication date: December 25, 2014
    Inventors: Yi Liu, Shunyou Wang, Matthew R. Janes, Lucy Lan, Pingda Ren, Christian Rommel
  • Patent number: 8912203
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: December 16, 2014
    Assignee: Afraxis Holdings, Inc.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • Publication number: 20140364430
    Abstract: Provided herein are PAK inhibitors.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Jay LICHTER, David CAMPBELL, Benedikt VOLLRATH, Sergio G. DURÓN
  • Patent number: 8901137
    Abstract: The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: December 2, 2014
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Wolfgang M. Korn, Olga K. Mirzoeva
  • Publication number: 20140350031
    Abstract: This invention relates to piperidino-pyhmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Application
    Filed: February 7, 2013
    Publication date: November 27, 2014
    Inventors: David Craig Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Mourad Daoubi Khamlichi
  • Publication number: 20140350020
    Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 5, 2011
    Publication date: November 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
  • Patent number: 8889696
    Abstract: Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: November 18, 2014
    Assignee: Temple University—Of The Commonwealth System Of Higher Education
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 8877763
    Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: November 4, 2014
    Assignees: Genosco, Oscotec, Inc.
    Inventors: Hong Woo Kim, Hee Kyu Lee, Ho-Juhn Song, Jaekyoo Lee, Jong Sung Koh, Jung-Ho Kim, Se Won Kim, In Yong Lee
  • Publication number: 20140323477
    Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders using such compounds.
    Type: Application
    Filed: April 30, 2014
    Publication date: October 30, 2014
    Applicant: GENENTECH, INC.
    Inventors: James J. CRAWFORD, Wendy LEE, Joachim RUDOLPH
  • Publication number: 20140323478
    Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Application
    Filed: April 30, 2014
    Publication date: October 30, 2014
    Applicant: AFRAXIS HOLDINGS, INC.
    Inventors: Sergio DURÓN, David CAMPBELL, Chudi NDUBAKU, Joachim RUDOLPH
  • Publication number: 20140323464
    Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.
    Type: Application
    Filed: May 16, 2012
    Publication date: October 30, 2014
    Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
  • Patent number: 8859545
    Abstract: Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, respiratory conditions, and others.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Evotec AG
    Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
  • Publication number: 20140302012
    Abstract: The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of Formula (I): in combination with one or both of bendamustine and rituximab.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 9, 2014
    Applicants: Sanofi, Exelixis, Inc.
    Inventors: Arthur DeCillis, Joanne Lager, Tal Zaks
  • Publication number: 20140296233
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicants: Sanofi, Celgene Avilomics Research, Inc.
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
  • Publication number: 20140296265
    Abstract: The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I:
    Type: Application
    Filed: April 27, 2012
    Publication date: October 2, 2014
    Applicants: Sanofi, Exelixis, Inc.
    Inventors: Arthur DeCillis, Joanne Lager, Tal Zaks
  • Patent number: 8846656
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: September 30, 2014
    Assignee: Novartis AG
    Inventors: Christopher Michael Adams, Veronique Darsigny, Alec Nathanson Flyer, Christine Fang Gelin, Timothy Brian Hurley, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Erik Meredith, Chang Rao, Michael H. Serrano-Wu, Catherine Fooks Solovay