5-position Is Unsubstituted Or Alkyl Substituted Only Patents (Class 544/312)
  • Patent number: 7745458
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: June 29, 2010
    Assignee: Glaxo Group Limited
    Inventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
  • Patent number: 7732602
    Abstract: The present invention relates to an herbicide composition comprising, as active ingredients, a uracil compound represented by the following formula (I): wherein Z represents halogen or cyano; A represents oxygen, sulfur or NH; R1 represents hydroxyl, C1-C7 alkoxy or others, and R2 represents hydrogen or methyl, and one or more organophosphorus compounds selected from the group consisting of N-(phosphonomethyl)glycine, agriculturally acceptable salts of Glyphosate and ammonium DL-homoalanine-4-yl(methyl)phosphinate; and a method for controlling weeds which comprises applying an effective amount of said herbicide composition to weeds. According to the invention, particularly weeds in orchards, cornfields, soybean fields, cotton fields and non-crop lands can be effectively controlled.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 8, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Nobuaki Mito, Shinsuke Shibuya
  • Publication number: 20100136127
    Abstract: The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.
    Type: Application
    Filed: July 16, 2008
    Publication date: June 3, 2010
    Inventors: Kazumichi Yamamoto, Hiroyoshi Koyama
  • Publication number: 20100113413
    Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.
    Type: Application
    Filed: January 5, 2010
    Publication date: May 6, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Qing Dong, Stephen W. Kaldor
  • Patent number: 7678796
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 16, 2010
    Assignee: AstraZeneca AB
    Inventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
  • Publication number: 20100035905
    Abstract: The present invention relates to hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]-sulfonyl]benzamide. The invention also relates to a process for the preparation of these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I.
    Type: Application
    Filed: October 12, 2007
    Publication date: February 11, 2010
    Inventors: Thomas Schmidt, Joachim Gebhardt, Sandra Löhr, Michael Keil, Jan Hendrik Wevers, Peter Erk, Heidi Emilia Saxell, Gerhard Hamprecht, Guido Mayer, Bernd Wolf, Gerhard Cox, Alfred Michel, Werner Seitz, Cyrill Zagar, Robert Reinhard, Bernd Sievernich
  • Patent number: 7652051
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Publication number: 20100004445
    Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 7, 2010
    Applicant: PGxHealth, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert Thompson
  • Publication number: 20090306379
    Abstract: Compositions comprising Compound I, wherein the Compound I is present in one or more polymorphic forms. Also provided are kits and articles of manufacture with compositions comprising one or more polymorphs of Compound I, and methods of using the compositions to treat various diseases.
    Type: Application
    Filed: August 5, 2009
    Publication date: December 10, 2009
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Mark Andres, Keith Lorimer
  • Patent number: 7598379
    Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: October 6, 2009
    Assignee: PGx Health, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Publication number: 20090240027
    Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
    Type: Application
    Filed: November 19, 2008
    Publication date: September 24, 2009
    Inventors: Eric Marsault, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Sylvie Beaubien, Luc Ouellet, Carl St-Louis, Sophie Beauchemin
  • Publication number: 20090221618
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is ; and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Application
    Filed: August 18, 2006
    Publication date: September 3, 2009
    Inventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Publication number: 20090186912
    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: Application
    Filed: September 17, 2008
    Publication date: July 23, 2009
    Applicant: 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
  • Publication number: 20090176784
    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: Application
    Filed: September 17, 2008
    Publication date: July 9, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Pamela L. Donner, John T. Randolph, Allan C. Krueger, David A. Betebenner, Douglas K. Hutchinson, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, John E. Hengeveld, Rodger F. Henry, Xiaochun Lou, Geoff G.Z. Zhang
  • Publication number: 20090156812
    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: Application
    Filed: December 18, 2007
    Publication date: June 18, 2009
    Applicant: IOVATE T. & P. INC.
    Inventors: Joseph MacDougall, Shan Chaudhuri
  • Publication number: 20090156575
    Abstract: The invention provides compounds of general formula wherein A, B, p, w, x, y, and z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: September 4, 2006
    Publication date: June 18, 2009
    Inventors: Lena Borjesson, Henrik Johansson, Anna Kristoffersson, Igor Shamovsky, Marco Skrinjar, Stephen Connolly, Tero Linnanen
  • Publication number: 20090137802
    Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: January 28, 2009
    Publication date: May 28, 2009
    Inventors: Elfatih Elzein, Rao Kalla, Tim Marquart, Jeff Zablocki, Xiaofen Li
  • Patent number: 7521396
    Abstract: The invention relates to compounds of the formula (I) in which Q, R1, R2, R3, R4, R5, R6, R7 are as defined in the disclosure, to processes for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: April 21, 2009
    Assignee: Bayer CropScience AG
    Inventors: Hans-Georg Schwarz, Roland Andree, Dorothee Hoischen, Joachim Kluth, Karl-Heinz Linker, Anton Vidal-Ferran, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 7495006
    Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: February 24, 2009
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Shuli Mao, Michael Hager
  • Publication number: 20080293941
    Abstract: The present invention relates to a process for preparing 1-alkyl-3-phenyluracils of the formula I where the variables R1 to R7 are as defined in the description by reacting 3-phenyluracils of the formula II and alkylating agents of the formula III R1-L1 ??III, with one another, wherein during the entire reaction the pH is kept in a range from 1 to 6 by adding base a little at a time.
    Type: Application
    Filed: May 18, 2006
    Publication date: November 27, 2008
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Joachim Gebhardt, Sandra Lohr, Michael Keil, Thomas Schmidt, Jan Hendrik Wevers, Helmut Zech, Rudolf Haberler
  • Publication number: 20080287476
    Abstract: Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.
    Type: Application
    Filed: March 12, 2008
    Publication date: November 20, 2008
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Ronald J. Christopher, Paul Covington, Atsushi Ogawa
  • Publication number: 20080280931
    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: Application
    Filed: November 29, 2007
    Publication date: November 13, 2008
    Inventors: Ron C. Kelly, Lien H. Koztecki
  • Publication number: 20080227798
    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: Application
    Filed: November 29, 2007
    Publication date: September 18, 2008
    Inventors: Ron C. KELLY, Lien H. Koztecki
  • Patent number: 7407914
    Abstract: The present invention relates to an herbicide composition comprising, as active ingredients, a uracil compound represented by the following formula (I): wherein Z represents halogen or cyano; A represents oxygen, sulfur or NH; R1 represents hydroxyl, C1-C7 alkoxy or others, and R2 represents hydrogen or methyl, and one or more compounds selected from the group consisting of N-(7-fluoro-3,4-dihydro-3-oxo-4-prop-2-ynyl-2H-1,4-benzoxazin-6-yl)cyclohex-1-ene-1,2-dicarboxamide and N-[2,4-dichloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,4-triazol-1-yl]phenyl]methanesulfonamide; and a method for controlling weeds which comprises applying an effective amounts of said herbicide composition to weeds. According to the invention, particularly weeds in orchards, soybean fields and non-crop lands can be effectively controlled.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: August 5, 2008
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Nobuaki Mito, Shinsuke Shibuya
  • Publication number: 20080161562
    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: Application
    Filed: October 30, 2007
    Publication date: July 3, 2008
    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: 7358359
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: April 15, 2008
    Assignee: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman
  • Patent number: 7304070
    Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: December 4, 2007
    Assignee: CV Therapeutics, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Patent number: 7205260
    Abstract: The present invention relates to an herbicide composition comprising, as active ingredients, a uracil compound represented by the following formula (I): wherein Z represents halogen or cyano; A represents oxygen, sulfur or NH; R1 represents hydroxyl, C1–C7 alkoxy or others, and R2 represents hydrogen or methyl, and one or more compounds selected from the group consisting of N-(7-fluoro-3,4-dihydro-3-oxo-4-prop-2-ynyl-2H-1,4-benzoxazin-6-yl)cyclohex-1-ene-1,2-dicarboxamide and N-[2,4-dichloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,4-triazol-1-yl]phenyl]methanesulfonamide; and a method for controlling weeds which comprises applying an effective amounts of said herbicide composition to weeds. According to the invention, particularly weeds in orchards, soybean fields and non-crop lands can be effectively controlled.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: April 17, 2007
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Nobuaki Mito, Shinsuke Shibuya
  • Patent number: 7202252
    Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.
    Type: Grant
    Filed: February 17, 2004
    Date of Patent: April 10, 2007
    Assignee: Endacea, Inc.
    Inventors: Constance Neely Wilson, John J. Partridge
  • Patent number: 7179896
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: February 20, 2007
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 7135475
    Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: November 14, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
  • Patent number: 7125993
    Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: October 24, 2006
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Rao Kalla, Tim Marquart, Jeff Zablocki, Xiaofen Li
  • Patent number: 7115544
    Abstract: A plant growth regulator for cotton harvest, which contains as an active ingredient, a compound of formula (I): wherein X is CH or nitrogen; Z is halogen; A is oxygen, sulfur, or NH; R1 is hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl}C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl}C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: October 3, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 7109243
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: September 19, 2006
    Assignee: IRM LLC
    Inventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
  • Patent number: 7034156
    Abstract: The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which R1 is hydrogen, cyano, nitro or halogen, R2 is cyano, nitro, halogen or optionally substituted alkyl or alkoxy, R3 is hydrogen, hydroxyl, mercapto, amino, hydroxyamino, hydrazino, halogen, or one of the radicals —R6, -Q-R6, —NH—R6, —NH—O—R6, —NH—SO2—R6, —N(SO2—R6)2, —CQ1-R6, —CQ1-Q2-R6, —CQ1-NH—R6, -Q2-CQ1-R6, —NH—CQ1-R6, —N(SO2—R6)(CQ1-R6), -Q2-CQ1-Q2-R6, —NH—CQ1-Q2-R6 or -Q2-CQ1-NH—R6, where Q is O, S, SO or SO2, Q1 and Q2 are each independently oxygen or sulphur and R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R4 is hydrogen, halogen or optionally substituted alkyl, and R5 is fluorine- and/or chlorine-substituted alkyl, as intermediates for the 1-amino-3-phenyluracil derivatives, and to a process f
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: April 25, 2006
    Assignee: Bayer CropScience AG
    Inventors: Jörn Stölting, Dorothee Hoischen, Roland Andree, Karl-Heinz Linker, Holger Weintritt, Heinz-Jürgen Wroblowsky
  • Patent number: 7022851
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein R1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: April 4, 2006
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee
  • Patent number: 7015230
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: March 21, 2006
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Darin E. Jones, Melvin L. Rueppel
  • Patent number: 7001910
    Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: February 21, 2006
    Assignee: Vita-Invest S.A.
    Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
  • Patent number: 6969766
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: November 29, 2005
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 6939965
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: September 6, 2005
    Assignees: Gilead Sciences, Inc., Emory University
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, José D. Soria, Marcos Sznaidman
  • Patent number: 6936602
    Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 30, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
  • Patent number: 6911450
    Abstract: The invention relates to a compound having general formula (I): wherein n is equal to 3; R1 is an ethyl or isopropyl group; each of the R2 groups is independently of each other a hydrogen atom, a C1-C3 alkyl group or a halogen atom; one of the R3 and R4 groups represents a hydrogen atom while the other of the R3 and R4 groups represents an OH or OR5 group, where R5 can be a C2-C7 acyl group, an alkyl(C1-C6)animo-carbonyl group, an aralkyl(C1-C6)aminocarbonyl optionally substituted on the aryl, an arylcarbonyl group optionally substituted or a heteroarylaminocarbonyl group. Said compound is particularly suitable as an antiviral agent and especially as an anti-HIV-1 agent.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: June 28, 2005
    Assignees: Universite de Geneve, Mayoly Spindler
    Inventor: Jean M. J. Tronchet
  • Patent number: 6900222
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6852717
    Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 8, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
  • Patent number: 6815398
    Abstract: Novel substituted phenyluracils of the general formula (I) in which n represents 0, 1 or 2, R1 represents hydrogen, amino or optionally substituted alkyl, R2 represents carboxyl, cyano, carbamoyl, thiocarbamoyl or in each case optionally substituted alkyl or alkoxycarbonyl, X represents hydroxyl, mercapto, amino, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylcarbonyloxy, alkoxycarbonyloxy, alkylaminocarbonyloxy, dialkylaminocarbonyloxy, phenylcarbonyloxy, alkylcarbonylamino, alkoxycarbonylamino, alkylsulphonylamino, alkenyl, alkenyloxy, alkenyloxycarbonyl, alkinyl, alkinyloxy or alkinyloxycarbonyl, where in the case that n is greater than 1, X in the individual possible compounds may also have meanings other than those given.
    Type: Grant
    Filed: May 7, 2002
    Date of Patent: November 9, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Hans-Georg Schwarz, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
  • Patent number: 6800590
    Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture. The compound has the following structure: wherein, D or E is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl or C1-C4 haloalkoxy; R1 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy; R2 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 carbamyl, C1-C4 alkoxycarbonyl, C1-C4 haloalkyl, cyano, nitro, carboxy or its alkali metal, alkali earth metal and organoammonium salts, C1-C4 alkylamido, C1-C4 haloalkylamido, heterocyclic amido, benzamido or substituted benzamido, benzo or substituted benzo compounds; R3 is hydrogen, C1-C4 alkanoyl, C1-C4 haloalkanoyl, benzoyl or C1-C4 alkoxyacetyl; X is CH or N; n=1-3.
    Type: Grant
    Filed: April 9, 2003
    Date of Patent: October 5, 2004
    Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Zheijiang Chemical Industry Research Institute
    Inventors: Long Lü, Jie Chen, Jun Wu, Wen Ling, Lisheng Mao, Mingzhi Li, Xian Cai, Weili Peng, Yong Wu, Shenggan Wu, Hongjun Wang, Guochao Wang, Hu Cui, Shidong Han, Weilian Qiu, Yonghua Wang
  • Patent number: RE39056
    Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: April 4, 2006
    Assignee: Merck & Co, Inc.
    Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman
  • Patent number: RE39263
    Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: September 5, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
  • Patent number: RE39590
    Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: April 24, 2007
    Assignee: ISK Americas Incorporated
    Inventors: Sandeep Gupta, Shao-Yong Wu, Masamitsu Tsukamoto, David A. Pulman, Bai-Ping Ying