At 2-position And At 4- Or 6-position Patents (Class 544/309)
  • Patent number: 9873673
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: January 23, 2018
    Assignee: Pfizer Inc.
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Patent number: 9732045
    Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 15, 2017
    Assignee: AbbVie Inc.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 9656970
    Abstract: Provided are 5-(trifluoromethyl)pyrimidine derivatives useful as intermediates for pharmaceuticals and agrochemicals and as intermediates for electronic materials and methods for producing the same. 2,4-dichloro-5-(trifluoromethyl)pyrimidine is reacted with 2,2,2-trifluoroethanol, benzyl alcohol, or benzenethiol to obtain the intended 2-(2,2,2-trifluoroethoxy)-4-chloro-5-(trifluoromethyl)pyrimidine, 2-benzyloxy-4-chloro-5-(trifluoromethyl)pyrimidine, 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine, or 2-chloro-4-phenylthio-5-(trifluoromethyl)pyrimidine.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: May 23, 2017
    Assignee: TOSOH F-TECH, INC.
    Inventors: Takumi Kagawa, Daiki Shigehiro, Kosuke Kawada
  • Patent number: 9540334
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: January 10, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 9499493
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: November 22, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 9434698
    Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: September 6, 2016
    Assignee: ABBVIE INC.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 9120958
    Abstract: An adhesive may be formulated with a functional component that reacts in the presence of ultraviolet light with a neighboring functional component to form a nonreversible bond therebetween. The functional component may include at least one —C?C— functional group that is able to undergo dimerization with a neighboring component. A method for making the adhesive includes covalently bonding the functional component to a support polymer, wherein the functional component may be covalently bonded to the support polymer by a linking molecule. A kit containing the adhesive and an ultraviolet light source is also provided.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: September 1, 2015
    Assignee: Empire Technology Development LLC
    Inventor: Glen Leon Brizius
  • Patent number: 9040550
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: May 26, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Publication number: 20150065532
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Patent number: 8895737
    Abstract: This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: November 25, 2014
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 8853397
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: October 7, 2014
    Assignee: Rigel Pharmacuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8841447
    Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: September 23, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 8841314
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: September 23, 2014
    Assignee: Pfizer Inc.
    Inventors: David Hepworth, Roger B. Ruggeri
  • Patent number: 8835449
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: September 16, 2014
    Assignee: Pfizer Inc.
    Inventors: Edward L. Conn, David Hepworth, Roger B. Ruggeri
  • Patent number: 8822685
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8748443
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: June 10, 2014
    Assignee: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Patent number: 8735579
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: May 27, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
  • Publication number: 20140135497
    Abstract: This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients.
    Type: Application
    Filed: November 5, 2013
    Publication date: May 15, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Li Liu, Deniz Akalay, Weitong Dong, Jianqing Feng, Christian Wolfgang Hemp, Jun Lu, Le Xie, Jinsong Yang
  • Publication number: 20140128272
    Abstract: Provided are a method for retaining in a dormant state a cancer tissue-derived cell mass that can reflect accurately the in vivo behavior of cancer cells, and an evaluation method for examining the sensitivity to various treatments including a drug sensitivity test by using a cancer tissue-derived cell mass in such a dormant state. The cancer tissue-derived cell mass is prepared from an individual. Such a cancer tissue-derived cell mass is cultured in vitro under the conditions of hypoxia and low levels of growth factors. Furthermore, a treatment with a drug, etc. is applied in vitro to the cancer tissue-derived cell mass in the dormant state so that evaluation is achieved by examination of its proliferation state, determination of life and death, and analysis of signals.
    Type: Application
    Filed: February 15, 2013
    Publication date: May 8, 2014
    Inventor: Masahiro Inoue
  • Patent number: 8685973
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Patent number: 8604192
    Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: December 10, 2013
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Patent number: 8604193
    Abstract: Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: December 10, 2013
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Stacey Heumann, Christopher M. Levins, Steven Pfeiffer, Donald Tang
  • Patent number: 8501238
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: August 6, 2013
    Assignee: AbbVie Inc.
    Inventors: Charles A. Flentge, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
  • Patent number: 8481731
    Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.
    Type: Grant
    Filed: June 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences, Inc.
    Inventors: Joe A. Tran, Chen Chen
  • Patent number: 8455639
    Abstract: The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: June 4, 2013
    Assignee: Sandoz AG
    Inventors: Johannes Ludescher, Josef Wieser, Gerhard Laus
  • Patent number: 8410266
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: April 2, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
  • Publication number: 20130072486
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: March 16, 2012
    Publication date: March 21, 2013
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Patent number: 8372973
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
  • Patent number: 8362247
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: January 29, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz
  • Patent number: 8334295
    Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: December 18, 2012
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Hongyan Guo, Choung U. Kim, Ill Y. Lee, Michael L. Mitchell, Gerry Rhodes, Jong C. Son, Lianhong Xu
  • Patent number: 8329900
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: December 11, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
  • Patent number: 8318756
    Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: November 27, 2012
    Assignee: Adherex Technologies, Inc.
    Inventors: Thomas Spector, William Paul Peters, Donald W. Kufe, Brian Huber
  • Patent number: 8288539
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: October 16, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
  • Patent number: 8278316
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 2, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • Patent number: 8242129
    Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: August 14, 2012
    Assignee: Exelixis, Inc.
    Inventors: Amy L. Tsuhako, Naing Aay, S. David Brown, Wai Ki Vicky Chan, Hongwang Du, Ping Huang, Brian Kane, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Michael Pack, Wei Xu, Peiwen Zhou
  • Patent number: 8236952
    Abstract: The present invention describes compounds produced from an orotic acid molecule and an amino acid molecule. The compounds being in the form of amino acid orotate compounds bound by an amide linkage and produced by one of two disclosed methods; 1) reacting orotic acid or derivatives thereof with a thionyl halide, and then combining the acyl halide with an amino acid in the presence of dichloromethane and a DMAP catalyst; or 2) protecting the carboxylic acid of an amino acid and then combining the amino acid with a DCC activated orotic acid, followed by removal of the carboxylic acid protecting group. The resulting amino acid orotate amide has an enhanced stability in solution as compared to a related ester. In addition, specific benefits are conferred by the particular amino acid used to form the compounds in addition to, and separate from, the orotate substituent.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: August 7, 2012
    Assignee: Northern Innovations Holding Corp.
    Inventors: Joseph MacDougall, Shan Chaudhuri
  • Patent number: 8232275
    Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: July 31, 2012
    Assignees: Wayne State University, The Regents of the University of Michigan
    Inventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
  • Patent number: 8193198
    Abstract: Disclosed are uracil compounds represented by Formula 1, a method for preparing the compounds, and a herbicide including the same as an active ingredient: wherein R1, R2, R3, R4, R5, X, Y, Z and W are the same as defined in the detailed description.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: June 5, 2012
    Assignees: Korea Research Institute of Chemical Technology, Dongbu HiTek Co., Ltd.
    Inventors: Young Kwan Ko, Kun Hoe Chung, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo, Dae Whang Kim, Tae Joon Kim, In Young Choi, Young Kwon Kim, Tae Hyun Oh, Jun Hyuk Choi, Mee Young Seok, Kyung Sung Kim, Bong Jin Chung
  • Patent number: 8188104
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flengte, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
  • Patent number: 8188275
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: May 29, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
  • Patent number: 8173663
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: May 8, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
  • Patent number: 8148525
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: April 3, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sasha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8084605
    Abstract: Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: wherein the Compound I is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: December 27, 2011
    Inventors: Ron C. Kelly, Lien H. Koztecki
  • Patent number: 8076302
    Abstract: A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents: [wherein R represents a nitrogen-containing heterocyclic ring which may have any one of a C1-C3 alkyl group or a C1-C3 alkoxy group as a substituent, or a C1-C6 alkyl group which has one primary amino group as a substituent].
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: December 13, 2011
    Assignee: aRigen Pharmaceuticals, Inc.
    Inventors: Haruhiko Machida, Masaichi Yamamoto
  • Patent number: 8017620
    Abstract: Deoxyuridine derivatives of the formula where R1 is H or various substituents; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(?O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH, —OH; R11 is H, F, —CH3, —CH2NH2, —CH2OH, CH(OH)CH3, CH(NH2)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: September 13, 2011
    Assignee: Medivir AB
    Inventors: Ian Gilbert, Corinne Nguyen, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska, Gian Filippo Ruda
  • Publication number: 20110196149
    Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 11, 2011
    Applicant: GE HEALTHCARE LIMITED
    Inventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
  • Patent number: 7994183
    Abstract: The present invention provides a solid preparation containing 2[[6-[(3R)-3-amino-1 -piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active ingredient. Specifically, the present invention provides a solid preparation containing a granule composed of compound (A) or a salt thereof and an additive (excluding microcrystalline cellulose) and a tablet containing (a) a granule containing compound (A) or a salt thereof and microcrystalline cellulose, and (b) a tableting aid containing magnesium stearate and microcrystalline cellulose.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: August 9, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yusuke Murakawa, Miyuki Hohokabe
  • Publication number: 20110178059
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 21, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad ALI, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
  • Publication number: 20110166096
    Abstract: Disclosed are uracil derivatives of the formula (I): wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in particular together with a cytostatic agent for suppressing or reducing resistance building up on cytostatic treatment.
    Type: Application
    Filed: June 25, 2009
    Publication date: July 7, 2011
    Applicant: RESPROTECT GMBH
    Inventors: Rudolf Fahrig, Kurt Eger, Martin Führer, Nicole Heinze, Matthias Klemm, Jörg-Christian Heinrich
  • Patent number: 7968559
    Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: June 28, 2011
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang