Polycyclo Ring System Having A 1,3,5-triazine As One Of The Cyclos Patents (Class 514/246)
  • Patent number: 10201543
    Abstract: Provided are crystalline forms of 2-Methyl-1-[(4-[6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol mesylate useful for treating cancer and methods of treating cancer, comprising administering to a subject in need thereof said compound.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: February 12, 2019
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Stefan Kluge
  • Patent number: 10125136
    Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: November 13, 2018
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
  • Patent number: 10118903
    Abstract: In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: November 6, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Patrick M. Woster, Craig J. Kutz
  • Patent number: 9868743
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: January 16, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Eric Gillis, Paul Michael Scola
  • Patent number: 9545445
    Abstract: The present invention relates to a therapeutic drug or a preventive drug for hypertension or high-normal blood pressure, comprising (a) and (b) as active ingredients: (a) a 2-phenylthiazole compound represented by formula (I) or a pharmaceutically acceptable salt thereof; (b) at least one compound or a pharmaceutically acceptable salt thereof selected from the group consisting of calcium antagonists, renin-angiotensin system inhibitors, diuretics, sympatholytic agents, vasodilators, and medicinally acceptable salts of these. The present invention also relates to a therapeutic method or a preventive method for hypertension or high-normal blood pressure, comprising administering the above (a) and (b) in amounts effective for treating or preventing hypertension or high-normal blood pressure.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 17, 2017
    Assignee: Teijin Pharma Limited
    Inventors: Takashi Shirakura, Mizuho Tamura, Yoshimasa Takahashi, Ippei Kuwahara
  • Patent number: 9192551
    Abstract: A kit for protecting keratin materials against UV radiation above 280 nm, including at least two different compositions, at least one compound (X), at least one compound (Y), and at least one hydrophobic screening system including (i) at least one hydrophobic organic sunscreen agent (A) absorbing UV radiation of 320-400 nm and at least one hydrophobic organic sunscreen agent (B) absorbing UV radiation of 280-320 nm, and optionally an inorganic sunscreen (D); (ii) at least one hydrophobic organic sunscreen (C) absorbing UV radiation of 280-400 nm, and optionally an inorganic sunscreen (D); or (iii) at least one hydrophobic organic sunscreen (A) absorbing UV radiation of 320-400 nm and either at least one hydrophobic organic sunscreen (C) absorbing UV radiation of 280-400 nm, or at least one inorganic sunscreen (D); at least one of compounds (X) and (Y) being a silicone compound.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: November 24, 2015
    Assignee: L'OREAL
    Inventors: Anne-Laure Gaudry, Martin Josso, Cécile Boschet
  • Patent number: 9000156
    Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: April 7, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Shibata, Tsutomu Imagawa
  • Patent number: 8980893
    Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: March 17, 2015
    Assignee: Merial, Inc.
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Publication number: 20150025079
    Abstract: Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventor: Bei Yin
  • Patent number: 8906920
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney
  • Publication number: 20140323503
    Abstract: The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 30, 2014
    Inventors: Charles Stuart Hoffman, Ozge Ceyhan
  • Publication number: 20140275092
    Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange
  • Publication number: 20140271606
    Abstract: Methods of treating bleeding disorders, such as bleeding diseases such as hemophilia, by administering adenosine 2a receptor and/or adenosine 2b receptor antagonists to subjects in need thereof are disclosed. In some embodiments, the methods further include administration of the antagonist with one or more of Factor VIII, Factor IX and Factor XI to treat the bleeding disorder.
    Type: Application
    Filed: February 13, 2014
    Publication date: September 18, 2014
    Inventor: Derek Sim
  • Patent number: 8791115
    Abstract: The present invention relates to combinations of triazine derivatives and of insulin sensitizers.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: July 29, 2014
    Assignee: Poxel SAS
    Inventors: Gérard Moinet, Daniel Cravo, Didier Mesangeau
  • Patent number: 8691982
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, where R1 is a (C1-C6)alkyl or (C3-C6)cycloalkyl group; R2 is a (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkenyl, (C1-C6)fluoroalkyl, (C1-C3)fluoroalkoxy, or (C1-C6)alkoxy(C1-C6)alkyl group, substituted: (i) with one to three hydroxyl groups, or (ii) with an NRaRb group, where Ra and Rb are independently a hydrogen atom or a (C1-C3)alkyl group; or a pyrrolidinylmethyl group substituted with one to three hydroxyl groups; R9 is the same as R2 or hydrogen; the R2 and R9 groups independently being substitutable with an —OCOR3 group, where R3 is a natural or unnatural amino acid derivative or a piperidyl group; alternatively, R2 and R9 together form a heterocyclic compound; X and Y are independently a substitutable phenyl or heteroaryl group, the heteroaryl group being a thienyl, pyridyl, pyrimidinyl, thiazolyl, pyrrolyl, or furanyl group; and R6 is a hydrogen or a (C1-C3)alkyl group.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: April 8, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite Paris Descartes, Universite Claude Bernard Lyon 1, Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Laurent Meijer, Hervé Galons, Benoit Joseph, Florence Popowycz, Nassima Oumata
  • Publication number: 20140045779
    Abstract: This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof.
    Type: Application
    Filed: August 29, 2011
    Publication date: February 13, 2014
    Inventor: Lifeng Xu
  • Patent number: 8618101
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 31, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney
  • Patent number: 8586584
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: November 19, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Annapurna Pendri, Zhongxing Zhang, Weixu Zhai, Guo Li, Samuel Gerritz, Paul Michael Scola, Li-Qiang Sun, Qian Zhao, Eric Mull
  • Publication number: 20130302417
    Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 14, 2013
    Inventors: Bret Berner, Sui Yuen Eddie Hou
  • Publication number: 20130273037
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 17, 2013
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • Publication number: 20130267502
    Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
  • Patent number: 8551994
    Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—Cl or C—CN; Y is O, S or NR2; 0 Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or &bgr; -phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.
    Type: Grant
    Filed: May 9, 2006
    Date of Patent: October 8, 2013
    Assignee: Prometic Biosciences Ltd
    Inventors: Jason Richard Betley, James Christopher Pearson, Ben Martin Beacom, Tadeusz Antoni Podgorski, Robert William Pannell
  • Patent number: 8518931
    Abstract: The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: August 27, 2013
    Assignee: IRM LLC
    Inventors: Tao Jiang, Pierre-Yves Michellys, Truc Ngoc Nguyen, Wei Pei, Baogen Wu, Xuefeng Zhu
  • Publication number: 20130143886
    Abstract: The present invention relates to methods of preserving or increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. The present invention also relates to methods of increasing renal function in a subject in need thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.
    Type: Application
    Filed: January 30, 2013
    Publication date: June 6, 2013
    Applicant: Takeda Pharmaceuticals U.S.A., Inc.
    Inventor: Takeda Pharmaceuticals U.S.A., Inc.
  • Patent number: 8389570
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: March 5, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Patent number: 8383812
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: February 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney, Victor W. Rosso, Jun Li
  • Patent number: 8367823
    Abstract: The present invention includes methods, articles, compositions and colorant dyes and pigments that include biocidal N-halamine dye composition having two or more heterocyclic ring structures attached to one or more N-halamine groups, wherein one or more halogens associate with the one or more one or more N-halamine groups to affect biocidal activity.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: February 5, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Yuyu Sun, Jie Luo
  • Patent number: 8334382
    Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: December 18, 2012
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
  • Patent number: 8231888
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: July 31, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Patent number: 8182795
    Abstract: An oil-in-water emulsified sunscreen cosmetic which contains: (A) Containing the following three types of surfactants (A-1)-(A-3); (A-1) A POE stearic ester having a POE mole number of 20-120; (A-2) sorbitan tristearate; and (A-3) glyceryl stearate having a HLB of 5-8; (B) bis-ethylhexyloxyphenolmethoxyphenyltriazine and/or tert-butylmethoxybenzoylmethane, oil soluble ultraviolet absorbents, solid at room temperatures; (C) ethylhexyl methoxycinnamate and/or octocrylene, oil soluble ultraviolet absorbents, liquid at room temperature; (D) phenylbenzimidazolesulfonic acid, a water soluble ultraviolet absorbent; and (E) a higher alcohol having 14-24 carbon atoms.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: May 22, 2012
    Assignee: Shiseido Co., Ltd.
    Inventors: Yoshihito Takakura, Kazuaki Suzuki, Takayuki Omura
  • Publication number: 20120065207
    Abstract: The present disclosure relates to a method of treating hyperuricemia in a patient that also suffers from a second disease state requiring treatment with theophylline, wherein the patient receives concomitant treatment with a xanthine oxidoreductase inhibitor and theophylline without resulting in theophylline toxicity to the patient and without substantial adjustments to the manufacturer's recommended dosage of theophylline.
    Type: Application
    Filed: October 27, 2011
    Publication date: March 15, 2012
    Applicant: Takeda Pharmaceuticals North America, Inc.
    Inventors: Lhanoo Gunawardhana, Max Tsai, Himanshu Naik
  • Publication number: 20120065165
    Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.
    Type: Application
    Filed: November 2, 2009
    Publication date: March 15, 2012
    Applicant: ARGINETIX, INC
    Inventors: Simon E. Aspland, Dan E. Berkowitz, Trinity Bivalacqua, Hunter Champion
  • Publication number: 20120059010
    Abstract: The invention provides ?-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.
    Type: Application
    Filed: March 28, 2011
    Publication date: March 8, 2012
    Applicant: Institute for Chemical Genomics
    Inventors: Michael Kahn, Masakatsu Eguchi
  • Patent number: 8124650
    Abstract: Antitumor combinations comprising a taxane and at least one epidophllotoxin for treating neoplastic diseases are described.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: February 28, 2012
    Assignee: Aventis Pharma S.A.
    Inventor: Marie-Christine Bissery
  • Patent number: 8110682
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, —C(O)—, or —C(R3?)(R4?)—; X is —N(R1)— or —C(R6)(R7)—; Y is —S(O)2—, —C(?O)—, —PO(OR9) or —C(R6?R7?)—; is a single or double bond and R, R1, R2, R3, R4, R3?, R4?, R5, R6, R6?, R7 and R7? are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: February 7, 2012
    Assignee: Schering Corporation
    Inventors: Brian McKittrick, Zhaoning Zhu, Andrew Stamford, Elizabeth M. Smith
  • Patent number: 8101652
    Abstract: Antitumor combinations comprising a taxane and at least one antimetabolite for treating neoplastic diseases are described.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: January 24, 2012
    Assignee: Aventis Pharma S.A.
    Inventor: Marie-Christine Bissery
  • Patent number: 7998960
    Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of plasminogen or a protein that is a plasminogen analogue, an affinity adsorbent is used that is a compound of formula (II) wherein one X is N and the other is N, C—Cl or C—CN; A is a support matrix, optionally linked to the triazine ring by a spacer; Z is O, S or N—R and R is H, C1-6 alkyl, C1-6 hydroxyalkyl, benzyl or &bgr;-phenylethyl; B is an optionally substituted hydrocarbon linkage containing from 1 to 10 carbon atoms; D is H, OH or a primary amino, secondary amino, tertiary amino, quaternary ammonium, imidazole, guanidino or amidino group; or B-D is —CHCOOH—(CH2)3-4—NH2; and q is 2 to 6.
    Type: Grant
    Filed: May 9, 2006
    Date of Patent: August 16, 2011
    Assignee: Prometic Biosciences Ltd.
    Inventors: Jason Richard Betley, James Christopher Pearson, Claudia Hildegard Kuhn, Baldev Singh Baines
  • Patent number: 7964204
    Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: June 21, 2011
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Publication number: 20110108493
    Abstract: Provided are biocidal compositions comprising 2,2-dibromo-3-nitrilopropionamide and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water containing systems.
    Type: Application
    Filed: June 18, 2010
    Publication date: May 12, 2011
    Inventors: Bei Yin, Michael V. Enzien, Donald J. Love
  • Publication number: 20110086858
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: October 14, 2010
    Publication date: April 14, 2011
    Inventors: Tao Wang, Annapurna Pendri, Zhongxing Zhang, Weixu Zhai, Guo Li, Samuel Gerritz, Paul Michael Scola, Li-Qiang Sun, Qian Zhao, Eric Mull
  • Patent number: 7915257
    Abstract: The present invention relates to the use of specific derivatives of triazinetriones for controlling coccidioses in livestock, especially pigs.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: March 29, 2011
    Assignee: Bayer Animal Health GmbH
    Inventors: Gisela Greif, Iris Heep, Hans-Christian Mundt
  • Publication number: 20110046142
    Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.
    Type: Application
    Filed: June 11, 2008
    Publication date: February 24, 2011
    Applicant: Northeastern University
    Inventors: Kim Lewis, Gabriele Casadei
  • Publication number: 20100331310
    Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.
    Type: Application
    Filed: February 9, 2009
    Publication date: December 30, 2010
    Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noboru Yamamoto
  • Patent number: 7855206
    Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds 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: November 9, 2007
    Date of Patent: December 21, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason M. Cox, Hong Dong
  • Publication number: 20100311756
    Abstract: The present invention relates to methods for reducing the progression of at least one of cardiac hypertrophy, cardiac remodeling or left ventricular dysfunction following a cardiac insult in a subject in need of treatment thereof. Moreover, the present invention also relates to methods of delaying the onset of heart failure symptoms or reducing the incidence of cardiovascular events following a cardiac insult in a subject in need of treatment thereof.
    Type: Application
    Filed: January 19, 2010
    Publication date: December 9, 2010
    Applicant: TAKEDA PHARMACEUTICALS NORTH AMERICA, INC.
    Inventors: Lin Zhao, Robert Hamlin, Yingjie Chen
  • Patent number: 7834014
    Abstract: The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease. In one embodiment, the invention features a compound of formula (I).
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: November 16, 2010
    Assignee: Biogen Idec MA Inc.
    Inventors: Hairuo Peng, Gang Yao, Russell C. Petter, Gnanasambandam Kumaravel
  • Patent number: 7816365
    Abstract: Disclosed are compounds of formula (I), which are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and which can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: November 5, 2004
    Date of Patent: October 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Guenter Hoelzemann, Wilfried Rautenberg
  • Publication number: 20100249138
    Abstract: A method for treating or preventing a host mammal that exhibits aversive signs and symptoms present during protracted abstinence or extended discontinuation syndromes as seen after cessation of compulsive activity, behaviors, or substance use is disclosed. That method comprises administering to a host mammal in need a pharmaceutical composition containing an aversive sign and symptom lessening amount a compound of Formula I or a pharmaceutically acceptable salt thereof dissolved or dispersed in a physiologically acceptable diluent, and repeating the administration as needed, wherein W, X, Y and Z, R1 and Ar are defined within. Data are provided in rats as host mammals using behavioral models dependent on the CRF1 system: defensive burying, alcohol dependence, cocaine dependence and nicotine dependence. A contemplated method also is useful for inhibiting relapse of such a behavior.
    Type: Application
    Filed: September 12, 2008
    Publication date: September 30, 2010
    Inventors: George F. Koob, Eric P. Zorrilla, Barbara Mason, Kim Janda, Peter Wirsching
  • Patent number: 7750005
    Abstract: The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: July 6, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Stefanie Flohr, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Pavel Safar, James Spoonamore, Martin Smrcina
  • Patent number: 7713972
    Abstract: The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotriazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.
    Type: Grant
    Filed: June 11, 2004
    Date of Patent: May 11, 2010
    Assignee: Asubio Pharma Co., Ltd.
    Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi