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:
September 18, 2003
Publication date:
April 1, 2004
Applicant:
Merrell Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Michael L. Edwards, Donald P. Matthews
Abstract: The invention provides [1,2,3]-triazolo[4,5-d]pyrimidine analogue compounds of formula (I)
The invention is also directed to pharmaceutical compositions containing the compounds, processes for the preparation of the compounds and methods of treatment employing the compounds.
Abstract: The invention provides novel substituted cyclopentane compounds, their use as medicaments, compositions containing them and processes for their preparation.
Abstract: The invention provides novel 1,2,3-triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
Type:
Application
Filed:
April 24, 2003
Publication date:
February 5, 2004
Inventors:
Roger Brown, Simon Guile, Garry Pairaudeau, Brian Springthorpe
Abstract: The present invention provides compounds of Formula (I) wherein Q1, Q2, Q3, Q4, Y1, Y2, and Z are as defined in the description, and pharmaceutically acceptable salts thereof, and C1-C8 alkyl esters thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of Formula (I) and their pharmaceuticalyl acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.
Type:
Application
Filed:
February 21, 2003
Publication date:
January 22, 2004
Inventors:
Joseph Armand Picard, William Howard Roark, Drago Robert Sliskovic
Abstract: The invention features 2,7-disubstituted purines and their isosteres such as the corresponding 3-deazapurines and 3-deaza-8-azapurines. The compounds disclosed herein have potent anti-microbial, e.g., anti-bacterial and anti-mycoplasmal properties. The compounds described herein inhibit DNA polymerase IIIC and DNA polymerase IIIE species; the compounds thus inhibit the growth of bacteria and mycoplasmata. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial or mycoplasmal infections, e.g., in eukaryotic cell cultures, animals, or humans.
Type:
Application
Filed:
February 10, 2003
Publication date:
January 22, 2004
Inventors:
George E. Wright, Wei-Chu Xu, Neal C. Brown
Abstract: A method for the identification and treatment of pathogenic microorganism infections by inhibiting one or more enzymes in a metabolic pathway by inhibiting the conversion of substrate to produce the penultimate or ultimate product particularly by inhibiting the activity of one or more of the enzymes in the pathway, and compounds and pharmaceutical compositions for inhibiting infections of pathogenic microorganisms by inhibiting such enzymes.
Abstract: The use of a composition that elevates intracellular levels of cyclic nucleotide cyclases in combination with phosphodiesterase inhibitors and cell grafts to restore function after CNS injury.
Type:
Application
Filed:
February 7, 2003
Publication date:
November 27, 2003
Inventors:
Mary Bartlett Bunge, Damien Daniel Pearse
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
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
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
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.
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
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
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.
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
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.
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
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
Applicant:
NYCOMED AMERSHAM PLC
Inventors:
Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
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
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.
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
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.