Bicyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/253)
  • Patent number: 10125127
    Abstract: A compound having formula I is useful for treating a neurodegenerative disease: R1 is an C1-12 organyl group; is a C1-12 heterocyclic ring system containing 5 to 12 ring atoms and up to three heteroatoms individually selected from the group consisting of N, O, S, and Se; R2 are C1-12 organyl groups; R7, R8 are each independently, hydrogen (H), hydroxyl, oxo (i.e., carbonyl), C1-8 alkyl, C1-8 alkoxyl, C2-8 alkenyl, C2-10 alkynyl, C5-7 cycloalkyl, C5-7 cycloalkenyl, halo, C1-4 aldehyde, or —NR4q where R4 is H, C1-8 alkyl, C2-8 alkenyl, C4-8 cycloalkyl, C4-8 cycloalkenyl, or C6-10 aryl; o is 0, 1, 2, 3, or 4; A is a C6-12 aryl group, C5-12 heteroaryl group, or an optionally substituted 3-hydroxypyridin-4(1H)-one; p is an integer from 1 to 6; and Zm is absent or a divalent linking moiety; and m is an integer representing the number of time Z is repeated.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: November 13, 2018
    Assignee: WAYNE STATE UNIVERSITY
    Inventor: Aloke K. Dutta
  • Patent number: 10047060
    Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: August 14, 2018
    Assignee: Gilead Calistoga LLC
    Inventors: Stacy Bremner, Jerry Evarts, Keiko Sujino, Duong Tran, Dragos Vizitiu
  • Patent number: 9878992
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: January 30, 2018
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Patent number: 9688662
    Abstract: The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: June 27, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ian Stansfield, Yannick Aime Eddy Ligny, Nathalie Claudie Isabelle Amblard, Matthias Luc Aime Versele
  • Patent number: 9670166
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: June 6, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Gnamm, Thorsten Oost, Stefan Peters, Holger Hoesch, Uwe Joerg Ries
  • Patent number: 9585884
    Abstract: The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: March 7, 2017
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 9493459
    Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: November 15, 2016
    Assignee: AMGEN INC.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
  • Patent number: 9421213
    Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: August 23, 2016
    Assignee: AstraZeneca AB
    Inventors: Kevin Michael Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
  • Patent number: 9409886
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: August 9, 2016
    Assignees: ARRAY BIOPHARMA INC., GENENTECH, INC.
    Inventors: Josef Bencsik, James F. Blake, James M. Graham, Martin F. Hentemann, Nicholas C. Kallan, Ian S. Mitchell, Stephen T. Schlachter, Keith L. Spencer, Dengming Xiao, Rui Xu, Mike Welch, Jun Liang, Brian S. Safina
  • Patent number: 9359340
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: June 7, 2016
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Leivers, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • Patent number: 9345705
    Abstract: The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: May 24, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stuart Denham Shumway, Carlo Toniatti, Brian Scott Roberts, Melissa M. Martin
  • Patent number: 9320739
    Abstract: Compositions of 1-(3-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-3-(5-(1,1,1, -trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: April 26, 2016
    Assignee: Ambit Biosciences Corporation
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • Patent number: 9309204
    Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: April 12, 2016
    Assignees: ARRAY BIOPHARMA INC., GENENTECH, INC.
    Inventors: Jonathan W. Lane, Travis Remarchuk, Sagar Shakya, Keith L. Spencer, Peter J. Stengel
  • Patent number: 9303040
    Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: April 5, 2016
    Assignee: ARRAY BIOPHARMA INC.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik
  • Patent number: 9290459
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: March 22, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Gnamm, Thorsten Oost, Stefan Peters, Holger Hoesch, Uwe Joerg Ries
  • Patent number: 9115093
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: August 25, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Gnamm, Thorsten Oost, Stefan Peters, Klaus Rudolf
  • Patent number: 9096542
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: August 4, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Patent number: 9062026
    Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: June 23, 2015
    Assignee: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, Francesco Parlati, David Wustrow
  • Patent number: 9029383
    Abstract: Methods for treating and/or preventing skin ulcers are provided featuring administration of pharmaceutical compositions comprising inhibitors of activity or expression Of Lp-PLA2 protein to patients subject to or at risk of developing skin ulcers.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: May 12, 2015
    Assignee: The Trustees Of The University of Pennsylvania
    Inventors: Robert Wilensky, Damir Hamamdzic, Harrilla Profka
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Patent number: 9018218
    Abstract: The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) can be used in the prevention of plants diseases caused by a plurality of pathogenic bacteria such as oomycota, basidiomycota, ascomycota, and fungi imperfecti, and due to these compounds have good bioactivity, which make them have very good effects at very low doses, especially more effective to powdery mildew of wheat. Therefore, the present invention relates to the use of the compounds having general formula I as fungicides, both in agriculture and other fields.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: April 28, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Baoshan Chai, Zhinian Li, Xufeng Sun, Zhonggang Shan
  • Publication number: 20150105407
    Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventor: Aleem Gangjee
  • Patent number: 9006251
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 14, 2015
    Assignee: Janssen Pharamceutica NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20150099881
    Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
    Type: Application
    Filed: May 17, 2013
    Publication date: April 9, 2015
    Applicant: Genetech, Inc.
    Inventors: Jonathan W. Lane, Travis Remarchuk, Sagar Shakya, Keith L. Spencer, Peter J. Stengel
  • Publication number: 20150099880
    Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
    Type: Application
    Filed: May 17, 2013
    Publication date: April 9, 2015
    Applicant: Genetech, Inc.
    Inventors: Srinivasan Babu, Francis Gosselin, Yingqing Ran, Travis Remarchuk, Scott J. Savage, Jeffrey Stults, Herbert Yajima
  • Patent number: 8999997
    Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: April 7, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
  • Patent number: 8993541
    Abstract: There are disclosed aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: March 31, 2015
    Assignee: Syntrix Biosystems, Inc.
    Inventors: Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
  • Patent number: 8969555
    Abstract: The present invention provides compounds of the Formula I: wherein X is a bond or CH2; R is selected from the group consisting of R1 and R2 are each independently selected from the group consisting of CH and N; R3 is H or CH3; R4 is H or CH3; L is selected from the group consisting of —O(CH2)3—, —C(O)NH(CH2)2—, —CH2C(O)NH(CH2)2—, —(CH2)3N(C(O)CH3)CH2—, —(CH2)2N(C(O)CH3)CH2—, —(CH2)3NH—, (CH2)2OCH2—, —(CH2)4—, —(CH2)2NHCH2—, —(CH2)3O—, and —CH2O(CH2)2—; or a pharmaceutically acceptable salt thereof. Compounds of this invention are autotaxin inhibitors.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: March 3, 2015
    Assignee: Eli Lilly and Company
    Inventors: Thomas James Beauchamp, Yen Dao, Spencer Brian Jones, Bryan Hurst Norman, Lance Allen Pfeifer
  • Patent number: 8962633
    Abstract: The present invention provides compostions and methods useful for treating and preventing metabolic bone diseases and disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing metabolic bone diseases and disorders such as, for example osteoporosis, osteopenia and osteopenia related diseases and abnormal bone marrow.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: February 24, 2015
    Assignee: Thomas Jefferson University
    Inventors: Yi Shi, Theresa Freeman
  • Publication number: 20150031709
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 29, 2015
    Applicant: SUNOVION PHARMACEUTICALS, INC.
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
  • Patent number: 8933084
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: January 13, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8916704
    Abstract: The dihydroquinone derivatives of piperidine and piperazine are 7-piperazinyl and 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones that exhibit D2 and 5-HT1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: where X is carbon or nitrogen and R is a group selected from a through f having the formula: or a pharmaceutically acceptable salt thereof. The piperazine compounds are prepared by condensing 4-bromo-2-nitro-benzonitrile with 1-Boc-piperazine (1-tert-butoxycarbonyl-piperazine) to form an intermediate that is converted to a piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: December 23, 2014
    Assignees: King Fahd University of Petroleum and Minerals, King Abdulaziz City for Science and Technology
    Inventor: Nisar Ullah
  • Patent number: 8907086
    Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
  • Publication number: 20140357644
    Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: August 12, 2014
    Publication date: December 4, 2014
    Inventors: Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith Lee Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang
  • Patent number: 8901132
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: December 2, 2014
    Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Publication number: 20140349996
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
  • Patent number: 8895747
    Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 25, 2014
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt
  • Publication number: 20140309244
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, A, X, D1, D2 and Y3 are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: September 23, 2011
    Publication date: October 16, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato, Clara Massol
  • Patent number: 8859566
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 14, 2014
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20140303188
    Abstract: The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III, and 5,6-saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: April 3, 2014
    Publication date: October 9, 2014
    Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT
    Inventor: Aleem Gangjee
  • Patent number: 8853199
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: October 7, 2014
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • Patent number: 8853216
    Abstract: The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: October 7, 2014
    Assignees: Array BioPharma, Inc., Genentech, Inc.
    Inventors: Josef Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith L. Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang, James Graham
  • Patent number: 8846681
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: September 30, 2014
    Assignees: Array BioPharma, Inc., Genentech, Inc.
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlachter, Anna L. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
  • Publication number: 20140288100
    Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.
    Type: Application
    Filed: September 23, 2011
    Publication date: September 25, 2014
    Applicants: University of Utah Research Foundation, The United States of American, as Represented by the Decretary, Department of Health and Human
    Inventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
  • Patent number: 8841311
    Abstract: The present invention relates to sulphone-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.
    Type: Grant
    Filed: July 18, 2009
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Bernd Buchmann, Dirk Kosemund, Duy Nguyen, Arne Von Bonin
  • Patent number: 8835434
    Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: September 16, 2014
    Assignees: Array Biopharma, Inc., Genentech, Inc.
    Inventors: Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith Lee Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang
  • Publication number: 20140256691
    Abstract: The invention provides a combination of a) a compound of Formula (Ia): or a pharmaceutically acceptable salt thereof, and b) abiraterone or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer.
    Type: Application
    Filed: March 30, 2012
    Publication date: September 11, 2014
    Applicant: GENENTECH, INC.
    Inventors: Michelle Nannini, Deepak Sampath