Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
The nitrogen is bonded directly at 4- or 6-position (Class 544/317)
  • Novel crystals of 1,3,4-oxadiazole derivatives, process for producing the crystals and medicines containing the same as the active ingredient
    Publication number: 20040023998
    Abstract: Type-2 crystals of 2-[5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidyl]-N-[1 -(2-[5-t-butyl-1,3,4-oxadiazolyl]carbonyl)-2-(R,S)-methylpropyl]acetamide represented by formula (I), a process for producing the same, and a pharmaceutical agent containing the same as an active ingredient.
    Type: Application
    Filed: August 4, 2003
    Publication date: February 5, 2004
    Inventors: Tsutomu Kojima, Kazuyuki Ohmoto
  • 1-H-3-arylpirrolidine-2,4-dione derivatives
    Publication number: 20040019061
    Abstract: The invention concerns 1-H-3-arylpyrrolidine-2,4-dione derivatives of formula (I), 1
    Type: Application
    Filed: July 3, 2002
    Publication date: January 29, 2004
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann
  • 2,5-substituted pyrimidine derivatives-CCR-3 receptor antagonists
    Publication number: 20040014775
    Abstract: This invention relates to certain pyrimidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Application
    Filed: July 1, 2003
    Publication date: January 22, 2004
    Inventors: Daisy Joe Du Bois, Long Mao, Daniel Harry Rogers, John Patrick Williams
  • Dihydropyrimidines and uses thereof
    Patent number: 6680323
    Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: January 20, 2004
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
  • Calcilytic compounds
    Publication number: 20040009980
    Abstract: Novel phosphate esters compounds and methods of using them as calcilytic compounds are provided.
    Type: Application
    Filed: April 24, 2003
    Publication date: January 15, 2004
    Inventors: Pradip Bhatnagar, Joelle L. Burgess, James F. Callahan, Maria A. Lago
  • Pyrimidine derivatives
    Publication number: 20040006068
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Application
    Filed: January 24, 2003
    Publication date: January 8, 2004
    Applicant: Tularik Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents
    Publication number: 20030236258
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: January 14, 2003
    Publication date: December 25, 2003
    Applicant: Pfizer Inc.
    Inventors: Kristin M. Lundy, Hengmiao Cheng, Subas M. Sakya, Jin Li, Martha L. Minich, Chikara Uchida
  • Thioether substituted imidazoquinolines
    Patent number: 6667312
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: December 23, 2003
    Assignee: 3M Innovative Properties Company
    Inventors: Jason D. Bonk, Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
  • Caspase inhibitors and uses thereof
    Publication number: 20030232846
    Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors.
    Type: Application
    Filed: June 10, 2002
    Publication date: December 18, 2003
    Inventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
  • Pyrazole compositions
    Publication number: 20030232848
    Abstract: Compounds of formulae (IA) and (IB): 1
    Type: Application
    Filed: April 2, 2003
    Publication date: December 18, 2003
    Applicant: Pfizer Inc.
    Inventors: Bernard Joseph Banks, Nathan Anthony Logan, James John Eshelby, Darren John Schulz
  • 2-pyrimidinyloxy-n-aryl-benzylamine derivatives,their processes and uses
    Publication number: 20030220198
    Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture.
    Type: Application
    Filed: April 9, 2003
    Publication date: November 27, 2003
    Inventors: Long L, 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
  • Heterocyclic arylsulfonamidobenzylic compounds
    Publication number: 20030220339
    Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.
    Type: Application
    Filed: January 29, 2003
    Publication date: November 27, 2003
    Applicant: Tularik Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • 5-lipoxygenase inhibitors: (2-azinylamino) quinone derivatives
    Patent number: 6653311
    Abstract: We have synthesized a series of new derivatives of (2-azinylamino) quinone, that have the general formula shown below. Several compounds of this new series of derivatives have been shown to be inhibitors of 5-lipoxygenase, with minimal or no effect on cycloxygenase-1 and 2-(COX-1 and COX-2) activity. where: A is N, CH, or, CCl; B is N, CH, CCH3, or Cph; X is H, Cl, Br, or I; Y is H, or CH3; R1 is H, CH3, OCH3, or Ph; and R2 is H, CH3, OCH3, or Ph; or R1—R2 is (CH═CH)2; and R3 is H or CH3.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: November 25, 2003
    Assignees: Board of Supervisors of Louisiana State University, Agricultural and Mechanical College
    Inventors: Nicholas G. Bazan, Carlos Sunkel, Julio Alvarez Builla-G.
  • Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
    Patent number: 6649622
    Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 18, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard Sulsky, Jeffrey A. Robl
  • Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals
    Publication number: 20030212070
    Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1
    Type: Application
    Filed: August 14, 2002
    Publication date: November 13, 2003
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel
  • &agr;v&bgr;3 integrin inhibitors
    Patent number: 6645991
    Abstract: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: November 11, 2003
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Oliver Schadt, Simon Goodman
  • Quinuclidine acrylamides
    Patent number: 6642246
    Abstract: Compounds of formula I wherein A represents: and R, R1, R2, R3 and R4 are as defined in the specification, pharmaceutically-cceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: November 4, 2003
    Assignee: Astrazeneca AB
    Inventor: Richard Schmiesing
  • Kinase inhibitors
    Publication number: 20030199511
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: December 12, 2002
    Publication date: October 23, 2003
    Inventors: Qun Li, Keith W. Woods, Gui-Dong Zhu, John P. Fischer, Jianchun Gong, Tongmei Li, Virajkumar Gandhi, Sheela A. Thomas, Garrick K. Packard, Xiaohong Song, Jason N. Abrams, Robert B. Diebold, Jurgen Dinges, Charles W. Hutchins, Vincent S. Stoll, Saul H. Rosenberg, Vincent L. Giranda
  • 2,4-substituted pyrrolidine derivatives-CCR-3 receptor antagonists
    Publication number: 20030199532
    Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Application
    Filed: February 18, 2003
    Publication date: October 23, 2003
    Inventors: Denis John Kertesz, Michael Garret Roepel
  • Crystalline pharmaceutical
    Publication number: 20030191313
    Abstract: New crystalline forms of lopinavir are disclosed.
    Type: Application
    Filed: March 12, 2003
    Publication date: October 9, 2003
    Inventors: Daniel A. Dickman, Sanjay Chemburkar, James J. Fort, Rodger F. Henry, David Lechuga-Ballesteros, Yuping Niu, William Porter
  • Pyridyl sulfone derivatives
    Publication number: 20030186968
    Abstract: The invention provides compounds of the formula 1
    Type: Application
    Filed: February 20, 2003
    Publication date: October 2, 2003
    Inventors: Ruth E. Tenbrink, Steven W. Kortum
  • Preparation of triazoles by organometallic addition to ketones and intermediates therefor
    Publication number: 20030181720
    Abstract: The invention provides a process for the preparation of a compound of the formula: 1
    Type: Application
    Filed: February 19, 2003
    Publication date: September 25, 2003
    Inventors: Michael Butters, Alan John Pettman, Julie Ann Harrison
  • Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
    Patent number: 6624180
    Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
    Type: Grant
    Filed: November 20, 2001
    Date of Patent: September 23, 2003
    Assignee: Pharmacia Corporation
    Inventors: Michael J. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Rondald K. Webber
  • Tetrahydroquinoline analogues as muscarinic agonists
    Publication number: 20030176418
    Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Application
    Filed: December 23, 2002
    Publication date: September 18, 2003
    Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
  • Pyrimidinonesulfamoylureas`
    Publication number: 20030171368
    Abstract: The disclosure is directed to compounds of the formula (I) 1
    Type: Application
    Filed: February 6, 2002
    Publication date: September 11, 2003
    Inventors: Werner Seitz, Andreas Kling, Herve Geneste, Thomas Subkowski, Claudia Graef, Wilfried Hornberger
  • Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands
    Publication number: 20030171380
    Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): 1
    Type: Application
    Filed: May 14, 2002
    Publication date: September 11, 2003
    Inventors: Argyrios G. Arvanitis, Paul J. Gilligan, Richard A. Hartz
  • Aspartic protease inhibitors
    Patent number: 6613764
    Abstract: The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen. R7 and R8 are H or alkyl, R1 and R2 are H or alkyl, and R3 is a non-aromatic substituent. Substituent A is OH, NH2, or SH. Substituents B and B1 include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R′ together with the nitrogen to which they are bonded, and/or B′ and R2 together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 2, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Ramnarayan S. Randad, John W. Erickson, Michael A. Eissenstat, Lucyna Lubkowska
  • Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
    Publication number: 20030162787
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: October 23, 2002
    Publication date: August 28, 2003
    Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
  • Aryloxy substituted pyrimidine imidazole compounds
    Patent number: 6610695
    Abstract: Novel 2,4,5-triaryl substituted imidazole compounds and compositions for use in therapy of CSBP/RK/p38 mediated diseases.
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: August 26, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Dennis Lee, Scott A. Long
  • Phenylalanine derivatives
    Patent number: 6610710
    Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: August 26, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Chieko Ejima, Mitsuhiko Kojima, Eiji Nakanishi, Hiroyuki Izawa, Yuko Satake, Nobuyasu Suzuki, Manabu Suzuki, Masahiro Murata
  • Crystalline pharmaceutical
    Patent number: 6608198
    Abstract: New crystalline forms of lopinavir are disclosed.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: August 19, 2003
    Assignee: Abbott Laboratories
    Inventors: Daniel A. Dickman, Sanjay Chemburkar, James J. Fort, Rodger F. Henry, David Lechuga-Ballesteros, Yuping Niu, William Porter
  • Inhibitors of phospholipase enzymes
    Publication number: 20030153751
    Abstract: Novel compounds are disclosed which inhibit the activity of phospholipase enzymes in a mammal, particularly cytosolic phospholipase A2. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.
    Type: Application
    Filed: May 8, 2002
    Publication date: August 14, 2003
    Applicant: American Home Products Corporation
    Inventors: Jasbir S. Seehra, Neelu Kaila, John C. McKew, Frank Lovering, Jean E. Bemis, YiBin Xiang
  • Imidazol derivatives as raf kinase inhibitors
    Publication number: 20030153588
    Abstract: Compounds of formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6-alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except for hydrogen may be optionally substituted; R2 and R3 independently represent optionally substituted C1-6-alkyl, or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted C3-7cycloalkyl or C3-7cycloalkenyl ring; or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted 5 to 7-membered heterocyclyl ring containing up to 3 heteroatoms selected from N, O, S.
    Type: Application
    Filed: January 7, 2003
    Publication date: August 14, 2003
    Inventors: Jon Graham Steadman, Andrew Kenneth Takle
  • Heterocyclo-alkylsulfonyl pyrazoles
    Publication number: 20030149026
    Abstract: The present invention relates to heterocyclo alkylsulfonyl pyrazoles of the formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: August 7, 2003
    Inventors: Subas M. Sayka, Martha L. Minich
  • 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones useful for inhibition of farnesyl-protein transferase
    Publication number: 20030149063
    Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-,5- (arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras- oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
    Type: Application
    Filed: August 23, 2002
    Publication date: August 7, 2003
    Applicant: American Cyanamid Company
    Inventors: Joseph William Epstein, Semiramis Ayral-Kaloustian, Gary Harold Birnberg, Edward James Salaski, Gloria Jean Macewan, Katherine Cheung
  • Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
    Patent number: 6600044
    Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: July 29, 2003
    Assignee: Brantford Chemicals Inc.
    Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
  • Substituted 1,3-diaryl-2-pyrid-2-yl-3-(pyrid-2-ylamino)propanol derivatives, process for their preparation, pharmaceuticals comprising these compounds and their use
    Patent number: 6596728
    Abstract: Substituted 1,3-diaryl-2-pyridin-2-yl-3-(pyridin-2-ylamino)propanol derivatives of the formula (I), and salts thereof, in which the radicals have the meanings given in the specification, and physiologically tolerated salts thereof and processes for their preparation are described. The compounds are suitable, for example, as hypolipidemic agents.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: July 22, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Reinhard Kirsch, Alfons Enhsen, Heiner Glombik, Werner Kramer, Eugen Falk
  • Synthesis of heteroarylamine intermediate compounds
    Publication number: 20030135046
    Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
    Type: Application
    Filed: December 6, 2002
    Publication date: July 17, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Nathan K. Yee
  • Method and structure for inhibiting activity of serine elastases
    Publication number: 20030134856
    Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors.
    Type: Application
    Filed: December 23, 2002
    Publication date: July 17, 2003
    Inventor: John C. Cheronis
  • 5-Heteroatom-substituted pyrazoles
    Publication number: 20030134858
    Abstract: The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: July 17, 2003
    Inventors: Martha L. Minich, Subas M. Sakya, Andrei Shavnya, Kristin Lundy DeMello
  • Inhibitors of glycogen synthase kinase 3
    Publication number: 20030130289
    Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Application
    Filed: December 3, 2002
    Publication date: July 10, 2003
    Applicant: Chiron Corporation
    Inventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
  • Tyrosine kinase inhibitors
    Patent number: 6586424
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: July 1, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, George D. Hartman, Peter J. Manley
  • Tyrosine kinase inhibitors
    Patent number: 6586423
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: July 1, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, George D. Hartman, Peter J. Manley, Randall W. Hungate, Leonard Rodman
  • Heterocyclo-alkylsulfonyl pyrazoles as anti-inflammatory/analgesic agents
    Publication number: 20030119836
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: July 2, 2002
    Publication date: June 26, 2003
    Inventors: Subas M. Sakya, Bryson Rast
  • Compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 6583139
    Abstract: Disclosed as compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: June 24, 2003
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Reinhardt Bernhard Baudy, Dimitrios Sarantakis
  • HIV REPLICATION INHIBITING PYRIMIDINES
    Publication number: 20030114472
    Abstract: This invention concerns the use of compounds of formula 1
    Type: Application
    Filed: November 1, 1999
    Publication date: June 19, 2003
    Inventors: BART DE CORTE, MARC RENE DE JONGE, JAN HEERES, CHIH YUNG HO, PAUL ADRIAAN JAN JANSSEN, ROBERT W. KAVASH, LUCIEN MARIA HENRICUS KOYMANS, MICHAEL JOSEPH KUKLA, DONALD WILLIAM LUDOVICI, KOEN JEANNE ALFONS VAN AKEN
  • Substituted azoles
    Patent number: 6579874
    Abstract: Compounds of formula I wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of bone metabolism, e.g. osteoporosis.
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: June 17, 2003
    Assignee: Novartis AG
    Inventors: Lászlo Révész, Achim Schlapbach
  • Benzocycloalkylenylamine derivatives as muscarinic receptor antagonists
    Publication number: 20030109524
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: November 6, 2002
    Publication date: June 12, 2003
    Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
  • Pyrrole substituted 2-indolinone protein kinase inhibitors
    Patent number: 6573293
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts 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: Grant
    Filed: February 15, 2001
    Date of Patent: June 3, 2003
    Assignees: Sugen, Inc., Pharmacia & Upjohn Co.
    Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
  • Pyrazoles
    Patent number: 6573270
    Abstract: Compounds of formulae (IA) and (IB): wherein R1, R2, R3, Ar1 and X are as defined above, are endothelin antagonists. The compounds are therefore useful in the treatment of a variety of conditions mediated by endothelin, such as restenosis, renal failure and systemic and pulmonary hypertension.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: June 3, 2003
    Assignee: Pfizer Inc.
    Inventors: Bernard Joseph Banks, Nathan Anthony Logan Chubb, James John Eshelby, Darren John Schulz