Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful 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 preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Application
Filed:
August 21, 2003
Publication date:
February 19, 2004
Inventors:
Neville J Anthony, Robert P. Gomez, Steven D. Young, Melissa S, Egbertson, John S. Wai, Jennifer J. Bennett
Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: 1
Type:
Application
Filed:
July 18, 2002
Publication date:
February 5, 2004
Applicant:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.
Type:
Application
Filed:
May 23, 2003
Publication date:
January 29, 2004
Applicant:
CHIRON CORPORATION
Inventors:
Rustum S. Boyce, Natalia Aurrecoechea, Daniel Chu, Aaron Smith
Abstract: The current invention discloses useful bicyclic and tricyclic amidino derivative compounds, pharmaceutical compositions containing these novel compounds, and to their use as nitric oxide synthase inhibitors.
Type:
Application
Filed:
October 7, 2002
Publication date:
January 29, 2004
Inventors:
Donald W. Hansen, E. Ann Hallinan, Alok K. Awasthi, Suzanne Metz, Jeffrey A. Scholten, Jeffery S. Snyder, Mihaly V. Toth, Ronald Keith Webber
Abstract: The invention relates to novel triazolotriazinones of the general formula (I), to a method for their production and to the pharmaceutical use thereof.
Type:
Grant
Filed:
October 21, 2002
Date of Patent:
January 27, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
Abstract: This invention relates to bicyclic heterocycles that inhibit cyclin-dependent kinase or tyrosine kinase enzymes, or both, and as such are useful to treat cell proliferative disorders such as angiogenesis, atherosclerosis, restenosis, and cancer as well as immunological disorders such as asthma, rheumatoid arthritis, autoimmune diabetes, and graft rejection associated with transplant surgery in mammals.
Type:
Grant
Filed:
October 3, 2001
Date of Patent:
January 27, 2004
Assignee:
Warner-Lambert Company
Inventors:
James Bernard Kramer, Howard Daniel Hollis Showalter
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.
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: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.
Abstract: A subject of the invention is the compounds of formula
in which
Y represents a hydrogen atom or a fluorine atom,
n represents an integer comprised between 1 and 8,
Z represents a hydrogen atom or the remainder of a carboxylic acid, optionally substituted on the heterocycle by one or more alkyl, alkenyl, alkynyl, O-alkyl, O-alkenyl, O-alkynyl, S-alkyl, S-alkenyl, S-alkynyl radicals containing up to 8 carbon atoms, one or more OH, NH2, C═N, NO2, CF3 radicals or one or more aryl radicals containing up to 14 carbon atoms or heteroaryl radicals containing one or more nitrogen oxygen or sulphur atoms, the aryl or heteroaryl radicals themselves being able to be substituted as well as their addition salts with acids,
The products of formula (I) have antibiotic properties.
Abstract: The present invention is related to oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
Type:
Application
Filed:
February 27, 2003
Publication date:
December 4, 2003
Inventors:
Philip Anthony Harris, Robert Walton McNutt, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Robert Peel, Edgar Raymond Wood
Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for thee &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.
Type:
Application
Filed:
June 17, 2003
Publication date:
November 20, 2003
Inventors:
William Robert Carling, David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
Abstract: The invention relates to novel triazolotriazinones of the general formula (I), to a method for their production and to the pharmaceutical use thereof.
Type:
Application
Filed:
October 21, 2002
Publication date:
November 13, 2003
Inventors:
Ulrich Niewohner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
Abstract: The invention relates to compounds of the formula (I): wherein: ring C is 9 or 10-membered bicyclic heteroaromatic group containing at least one nitrogen atom in the ring attached to Z and optionally containing a further 1-3 heteroatoms, selected independently from O, S, and N, with the proviso that ring C is not a quinazoline, quinoline or cinnoline group; either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—; or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, NH—, —S—, CH2— or a direct substituents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 2; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, hydroxy, halogeno, C1-4alkyl, or any other value as defined herein; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the
Abstract: Organic compounds having the structure I are provided where the variables have the values described herein.
Type:
Application
Filed:
July 2, 2002
Publication date:
November 6, 2003
Applicant:
Chiron Corporation
Inventors:
Paul A. Renhowe, Cynthia M. Shafer, Christopher McBride, Joel Benjamin Silver, Sabina Pecchi, Timothy D. Machajewski, William R. McCrea, Daniel J. Poon, Teresa Thomas
Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diamine compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
November 4, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Kevin Richard Guertin, Lina Quattrocchio Setti
Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
Abstract: The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Application
Filed:
January 15, 2003
Publication date:
October 23, 2003
Applicant:
SUGEN, INC.
Inventors:
Peng Cho Tang, Todd Anthony Miller, Li Sun, Ngoc My Tran, Asaad Nematalla, Anh Thi Nguyen
Abstract: The present invention relates to novel imidazoly 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Application
Filed:
February 25, 2003
Publication date:
October 9, 2003
Applicant:
SUGEN, INC.
Inventors:
Peng Cho Tang, Li Sun, Gerald McMahon, G. Davis Harris
Abstract: The present invention is directed to novel benzimidazole derivatives that possess antibacterial activity. The invention also is directed to compositions including the benzimidazole derivatives, and methods for using the same.
Type:
Application
Filed:
February 6, 2002
Publication date:
October 2, 2003
Inventors:
Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
Abstract: Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): 1
Type:
Application
Filed:
November 6, 2002
Publication date:
October 2, 2003
Inventors:
Jollie Duaine Godfrey, John Hynes, Alaric J. Dyckman, Katerina Leftheris, Zhongping Shi, Stephen T. Wrobleski, Wendel William Doubleday, John A. Grosso
Abstract: Triazinoindole derivatives are useful in the prophylaxis and treatment of pestivirus infections and diseases associated with pestivirus infections.
Type:
Application
Filed:
February 5, 2003
Publication date:
September 18, 2003
Inventors:
Daniel C. Pevear, Theodore J. Nitz, Martin Seipel
Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.
Type:
Grant
Filed:
July 15, 2002
Date of Patent:
September 9, 2003
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
William Robert Carling, David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.
Type:
Application
Filed:
November 8, 2002
Publication date:
August 21, 2003
Applicant:
NEUROGEN CORPORATION
Inventors:
Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
Abstract: A class of substituted 1,2,4-triazolo[4,3-]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
Type:
Grant
Filed:
February 19, 2002
Date of Patent:
August 19, 2003
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
William Robert Carling, Alexander Richard Guiblin, Kevin William Moore, Christopher Richard Moyes, Michael Rowley, Leslie Joseph Street
Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
October 23, 2001
Publication date:
August 14, 2003
Inventors:
Francesco G. Salituro, Guy W. Bemis, Susanne Wilke, Jeremy Green, Jingrong Cao, Huai Gao, Edmund Martin Harrington
Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diamine compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B.
Type:
Application
Filed:
December 10, 2002
Publication date:
August 14, 2003
Inventors:
Kevin Richard Guertin, Lina Quattrocchio Setti
Abstract: The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
Type:
Application
Filed:
May 30, 2002
Publication date:
July 24, 2003
Inventors:
Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Ulrich Niewohner, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J. Cuthbert, Mary F. Fitzgerald, Graham Sturton
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
Abstract: Novel tricyclic compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling. The compounds have the following formulas
where R1, R2 and R3 are defined in the written description of the invention.
Type:
Grant
Filed:
November 29, 2000
Date of Patent:
July 1, 2003
Assignee:
Cell Therapeutics, Inc.
Inventors:
Baoqing Gong, J. Peter Klein, Michael Coon
Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.
Type:
Application
Filed:
August 28, 2002
Publication date:
June 26, 2003
Applicant:
Pfizer Inc.
Inventors:
Brian Thomas O'Neill, Jotham Wadsworth Coe, Christopher J. O'Donnell
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure:
including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, R6, X and Y are as defined herein.
Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
Type:
Application
Filed:
July 3, 2002
Publication date:
June 19, 2003
Applicant:
Axys Pharmaceuticals, Inc.
Inventors:
Huiyong Hu, John Hendrix, Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, David Sperandio, Wendy Young, Steve Torkelson
Abstract: The present invention relates to new substituted imidazotriazinones, processes for their preparation, and their use for the production of medicaments, in particular for improving perception, concentration power, learning power and/or memory power.
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
June 3, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ulrich Niewöhner, Dagmar Schauss, Martin Hendrix, Gerhard König, Frank-Gerhard Böss, Franz-Josef Van Der Staay, Rudy Schreiber, Karl-Heinz Schlemmer, Rolf Grosser
Abstract: The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof.