Exactly Five Ring Nitrogens In The Bicyclo Ring System (e.g., Triazolo[4,5-d]pyrimidine, Etc.) Patents (Class 514/261.1)
  • Patent number: 6645965
    Abstract: Nitric acid salts with medicines having an antihypertensive activity.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: November 11, 2003
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Publication number: 20030199517
    Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of
    Type: Application
    Filed: May 23, 2003
    Publication date: October 23, 2003
    Applicant: Wolf-Georg Forssmann
    Inventors: Wolf-Georg Forssmann, Christian Georg Steif, Michael Carsten Truss, Stefan Uckert, Udo Jonas
  • Publication number: 20030199526
    Abstract: The present invention provides a compound of formula (I): 1
    Type: Application
    Filed: December 9, 2002
    Publication date: October 23, 2003
    Inventors: Deborah Choquette, Robert J. Davies, Marion W. Wannamaker
  • Publication number: 20030181469
    Abstract: The invention provides new forms of a chemical compound of formula (I). The invention relates to forms fo a chemical compound (I), in particular to crystalline and amorphous forms, more particularly four crystalline forms and an amorphous form. The invention further relates to processes for the preparation of such forms, to pharmaceutical compositions comprising the compound in crystalline and/or amorphous form and to therapeutic use of such forms.
    Type: Application
    Filed: December 2, 2002
    Publication date: September 25, 2003
    Inventors: Martin Bohlin, Steve Cosgrove, Bo Lassen
  • Patent number: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Publication number: 20030158184
    Abstract: The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.
    Type: Application
    Filed: December 21, 2001
    Publication date: August 21, 2003
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Publication number: 20030144305
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: December 20, 2002
    Publication date: July 31, 2003
    Applicant: AstraZeneca AB
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Publication number: 20030144235
    Abstract: Compounds represented by the formula 1: 1
    Type: Application
    Filed: September 9, 2002
    Publication date: July 31, 2003
    Inventors: John A. Secrist, Kamal N. Tiwari, John A. Montgomery
  • Patent number: 6599907
    Abstract: A method of treating cystic fibrosis in a patient comprising: administering to said patient an effective amount of a type V cyclic nucleotide phosphodisterase inhibitor, wherein said inhibitor is a compound of formula (I):  wherein A is a five- or six-membered ring containing one or more N atoms, X is a substituent of formula (II):  wherein R1 represents C1-4 alkyl, and X is positioned at either or both of the 2-position and/or the 8-position in (I).
    Type: Grant
    Filed: December 26, 2001
    Date of Patent: July 29, 2003
    Assignee: University of Wales College of Medicine
    Inventors: Robert Leslie Dormer, Margaret Ann McPherson
  • Publication number: 20030139427
    Abstract: This invention pertains to compounds which specifically bind to the adenosine A1, A2a, and A3 receptors and the use of these compounds to treat a disease associated with the A1, A2a, and A3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
    Type: Application
    Filed: August 23, 2002
    Publication date: July 24, 2003
    Applicant: OSI Pharmaceuticals Inc.
    Inventors: Arlindo L. Castelhano, Bryan McKibben
  • Publication number: 20030109484
    Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Application
    Filed: June 6, 2002
    Publication date: June 12, 2003
    Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
  • Publication number: 20030087873
    Abstract: The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug.
    Type: Application
    Filed: October 18, 2001
    Publication date: May 8, 2003
    Inventors: Lieven Stuyver, Kyoichi Watanabe
  • Publication number: 20030078275
    Abstract: This invention describes novel pyrazole compounds of formula IIa: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: April 24, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M.C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
  • Publication number: 20030069237
    Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
    Type: Application
    Filed: April 26, 2002
    Publication date: April 10, 2003
    Inventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
  • Publication number: 20030060431
    Abstract: Nucleoside analogues or base analogues having structure (1), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.
    Type: Application
    Filed: September 3, 2002
    Publication date: March 27, 2003
    Inventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
  • Patent number: 6525056
    Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: February 25, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
  • Patent number: 6489333
    Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: December 3, 2002
    Assignee: Bristol - Meyers Squibb Pharma Company
    Inventors: William J. Pitts, Prabhakar K. Jadhav
  • Publication number: 20020165202
    Abstract: Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.
    Type: Application
    Filed: September 13, 2001
    Publication date: November 7, 2002
    Applicant: The Regents of the University of California
    Inventors: Dennis A. Carson, Howard Cottam
  • Publication number: 20020123629
    Abstract: The invention provides a compound of formula I 1
    Type: Application
    Filed: February 15, 2002
    Publication date: September 5, 2002
    Inventor: Bernhard Peter Neumann
  • Publication number: 20020058635
    Abstract: Novel purine L-nucleoside compounds are disclosed, in which both the purine rings and the sugar are either modified, functionalized, or both. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Th1 and Th2.
    Type: Application
    Filed: October 30, 2001
    Publication date: May 16, 2002
    Inventor: Devron R. Averett