Purine Containing (including Hydrogenated) Patents (Class 544/228)
  • Patent number: 7977343
    Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: July 12, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
  • Patent number: 7741318
    Abstract: Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: June 22, 2010
    Assignee: Schering Corporation
    Inventors: Martin C. Clasby, Samuel Chackalamannil, Bernard R. Neustadt, Xiaobang Gao
  • Patent number: 6919449
    Abstract: The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III) by photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: July 19, 2005
    Assignee: Orchid Chemicals and Pharmaceuticals Limited
    Inventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Pratik Ramesh Sathe, Sivakumaran Sundaravadivelan, Praveen Nagesh Ganesh
  • Patent number: 6734143
    Abstract: The present invention provides 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: May 11, 2004
    Assignee: Dow AgroSciences LLC
    Inventors: Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M. Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
  • Patent number: 6531484
    Abstract: Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & co., Inc.
    Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
  • Patent number: 6136827
    Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: October 24, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Sander G. Mills, Bryan Oates
  • Patent number: 5955501
    Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 21, 1999
    Assignee: Procyon Pharmaceuticals, Inc.
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 5770591
    Abstract: A bis(platinum) complex having the structure: ##STR1## wherein X, Y, Z, X', Y', and Z' are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, dicarboxylate, substituted dicarboxylate primary or secondary amine, sulfoxide, phosphine, pyridine-type nitrogen and the like; preferably, there is at least one Pt-anion bond on each Pt molecule; and A is a diamine or polyamine.Complexes of trans geometry ?PtX.sub.2 (L)(L')! where at least L is a planar ligand such as pyridine but preferably quinoline and L' may be amine, sulfoxide or substituted sulfoxide and X is a chloride, nitrate or carboxylate.A process for obtaining bis(platinum) complexes where the two platinum coordination spheres may contain different ligands in each sphere and where the geometry of each platinum coordination sphere may be the same or different.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: June 23, 1998
    Assignee: The University of Vermont and State Agricultural College
    Inventor: Nicholas Farrell
  • Patent number: 5728691
    Abstract: Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are described. These compounds possess antibacterial, growth promoting and probiotic activity.
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: March 17, 1998
    Assignees: Laboratorios Aranda S.A. De C.V., Judith Marcia Arrieta Munguia
    Inventor: Miguel Angel Corpi Constantino
  • Patent number: 5506243
    Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: April 9, 1996
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
  • Patent number: 5484763
    Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: January 16, 1996
    Assignee: American Cyanamid Company
    Inventor: Peter J. Wepplo
  • Patent number: 4716232
    Abstract: 1-(Vinyl phosphonate adduct) pyrazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: December 29, 1987
    Assignee: Eli Lilly and Company
    Inventor: Robert J. Ternansky
  • Patent number: 4388326
    Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.
    Type: Grant
    Filed: May 7, 1980
    Date of Patent: June 14, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone