Six-membered Ring Consisting Of One Nitrogen And Five Carbons (e.g., Pyridine, Etc.) Patents (Class 544/124)
The additional six-membered hetero ring is one of the cyclos in a polycyclo ring system (Class 544/125)
Piperidine ring (Class 544/129)
Double bonded divalent chalcogen containing (Class 544/131)
  • Pyridine and pyrimidine derivatives
    Publication number: 20030216382
    Abstract: The present invention provides compounds of formula (I) 1
    Type: Application
    Filed: February 10, 2003
    Publication date: November 20, 2003
    Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
  • Farnesyltransferase inhibitors
    Publication number: 20030216441
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: May 10, 2002
    Publication date: November 20, 2003
    Inventors: Stephen L. Gwaltney, Lissa T.J. Nelson, Stephen J. O'Connor, Hing L. Sham, Gerard M. Sullivan, Weibo Wang
  • Antithrombotic amides
    Publication number: 20030212069
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Application
    Filed: March 5, 2003
    Publication date: November 13, 2003
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pineiro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents
    Publication number: 20030207882
    Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents, L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.
    Type: Application
    Filed: May 2, 2003
    Publication date: November 6, 2003
    Applicant: ZENECA LIMITED
    Inventors: Andrew Stocker, John Preston, Michael James Smithers
  • &agr;1b-adrenergic receptor antagonists
    Patent number: 6642228
    Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: November 4, 2003
    Assignee: Toray Industries, Inc.
    Inventors: Ryoji Hayashi, Eiji Ohmori, Masafumi Isogaya, Mitsuhiro Moriwaki, Hiroki Kumagai
  • Novel substituted diamine derivatives useful as motlin antagonists
    Publication number: 20030203906
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula 1
    Type: Application
    Filed: November 8, 2002
    Publication date: October 30, 2003
    Inventors: Sigmong G. Johnson, Ralph A. Rivero
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6638930
    Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: October 28, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Gyrase inhibitors and uses thereof
    Patent number: 6632809
    Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: October 14, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
  • Hydroxyformamidine derivatives and medicines containing the same
    Publication number: 20030186979
    Abstract: Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided.
    Type: Application
    Filed: December 12, 2002
    Publication date: October 2, 2003
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Amide derivatives
    Publication number: 20030186966
    Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Application
    Filed: January 29, 2003
    Publication date: October 2, 2003
    Applicant: ASTRAZENECA AB
    Inventor: Dearg S. Brown
  • Sulphonamide derivatives
    Publication number: 20030171350
    Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 12, 2002
    Publication date: September 11, 2003
    Inventors: MacKlin Brian Arnold, David Michael Bender, Andrew Hendley Fray, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
    Patent number: 6617339
    Abstract: Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: September 9, 2003
    Assignee: Syngenta Limited
    Inventor: Michael Barry Gravestock
  • Substituted pyrazoles as p38 kinase inhibitors
    Patent number: 6617324
    Abstract: A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: September 9, 2003
    Assignee: G. D. Searle & Company
    Inventors: Ashok S. Naraian, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xi, Ish K. Khanna, Yi Yu
  • Pyridinylimidazoles
    Publication number: 20030166633
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2 and R3 represent various functional groups, and one of X1 and X2 is N and the other is NR10; and their use as pharmaceuticals.
    Type: Application
    Filed: October 29, 2002
    Publication date: September 4, 2003
    Inventors: Laramie Mary Gaster, Michael Stewart Hadley, John David Harling, Frank Peter Harrington, Jag Paul Heer, Thomas Daniel Heightman, Andrew Hele Payne
  • Novel oxazolidinone derivatives and a process for the preparation thereof
    Publication number: 20030166620
    Abstract: The present invention relates to novel oxazolidinone derivatives, their pharmaceutically acceptable salts and a process for the preparation thereof. More particularly, the present invention relates to oxazolidinone derivatives having pyridine or pyrimidine moeity substituted by heterocycle and heteroaromaticcycle at 4-position of phenyl ring. The compounds of the present invention have wide antibacterial spectrum, superior antibacterial activity and low toxicity, such that the compound of this invention can be used as an antibacterial agent.
    Type: Application
    Filed: November 27, 2002
    Publication date: September 4, 2003
    Inventors: Jae-Gul Lee, Won-Bin Leem, Jong-Hwan Cho, Sung-Hak Choi, Jong-Jin Lee, Sang-Kuk Park, Tae-Hoo Lee, Dong-Goo Kim, Hyun-Jung Sung
  • Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
    Publication number: 20030166644
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Application
    Filed: December 13, 2002
    Publication date: September 4, 2003
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Inhibitors of p38
    Patent number: 6608060
    Abstract: The present invention relates to inhibitors of p38, 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: Grant
    Filed: June 14, 1999
    Date of Patent: August 19, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
  • NK-1 receptor active amine oxide prodrugs
    Publication number: 20030149039
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Application
    Filed: January 7, 2003
    Publication date: August 7, 2003
    Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Synthesis for heteroarylamine compounds
    Patent number: 6603000
    Abstract: Disclosed is a novel method of producing heteroaryl amines of the formula(I): wherein X, Y and Z are described herein, the heteroarylamines are useful in the production of heteroaryl ureas which are key component in pharmaceutically active compounds possessing a heteroaryl urea group.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: August 5, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Nathan Yee, Suresh R. Kapadia, Jinhua J. Song
  • Inhibitors of Src and other protein kinases
    Publication number: 20030144309
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: May 16, 2002
    Publication date: July 31, 2003
    Inventor: Young Choon-Moon
  • Pyridone substituted benzothiazole derivatives
    Patent number: 6599901
    Abstract: The present invention relates to compounds of the formula wherein R is as defined herewithin. The compounds of formula I have a good affinity to the A2A receptor and therefore they may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, aniticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: July 29, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
  • Substituted pyridine or piperidine compounds
    Publication number: 20030139408
    Abstract: The invention relates to a compound of formula (I): 1
    Type: Application
    Filed: November 27, 2002
    Publication date: July 24, 2003
    Inventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cecile Lebrun, Daniel-Henri Caignard, Pierre Renard
  • Arthropodicidal carboxanilides
    Publication number: 20030139397
    Abstract: Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form —CH2—, —CH2CH2—, —O—, —S—, —S(O)—, —S(O)2—, —NR8—, —OCH2—, —SCH2—, —N(R8)CH2—, substituted —CH2— and substituted —CH2CH2—, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N═CR11R12, OR7, COR13, CO2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)1R15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R9
    Type: Application
    Filed: August 28, 2002
    Publication date: July 24, 2003
    Inventor: David Walter Piotrowski
  • 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
  • Synthesis of heteroarylamine intermediate compounds
    Patent number: 6593471
    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: Grant
    Filed: December 6, 2001
    Date of Patent: July 15, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
  • Piperadinyl-substituted pyridylalkane, alkene and alkine carboxamides
    Patent number: 6593344
    Abstract: The invention relates to new piperidinyl-substituted pyridyl carboxamides of the general formula (I), wherein the structure element E has meanings (E1) or (E2) and whereby the heterocyclic ring can optionally have a double bond. These substances have especially high cytostatic activities and pronounced immunosuppressive properties which make them suitable for therapeutic treatment in broad tumor spectrum.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: July 15, 2003
    Assignee: Klinge Pharma GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Heteroaromatic substituted amides with antagonistic activity to neurokinin 1 receptors
    Publication number: 20030130508
    Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.
    Type: Application
    Filed: October 29, 2002
    Publication date: July 10, 2003
    Inventors: Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Synthesis of heteroarylamine intermediate compounds
    Patent number: 6590099
    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: Grant
    Filed: December 6, 2001
    Date of Patent: July 8, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
  • 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
  • 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
  • N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
    Publication number: 20030119811
    Abstract: Compounds represented by Formula (I): 1
    Type: Application
    Filed: April 2, 2002
    Publication date: June 26, 2003
    Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
  • Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
    Patent number: 6583282
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: June 24, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • 3-substituted piperidines comprising urea functionality, and methods of use thereof
    Publication number: 20030114436
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
    Type: Application
    Filed: November 5, 2002
    Publication date: June 19, 2003
    Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
  • Process for preparing substituted pyridines
    Publication number: 20030114670
    Abstract: A process for preparing a compound of the formula 1
    Type: Application
    Filed: December 12, 2002
    Publication date: June 19, 2003
    Inventors: Robert L. Dow, Steven R. Schneider
  • 3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
    Patent number: 6579873
    Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein R1, R2, Ar1 and HetAr2 are as described in the specification.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: June 17, 2003
    Assignee: Pharmacia Corporation
    Inventors: Ashok Anantanarayan, Michael Clare, Lifeng Geng, Gunnar J. Hanson, Richard A. Partis, Michael A. Stealey, Richard M. Weier
  • Compounds and compositions as protease inhibitors
    Patent number: 6576630
    Abstract: The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: June 10, 2003
    Assignee: AXYS Pharmaceuticals, Inc.
    Inventors: John O. Link, Arnold J. Martelli, Valeri Martichonok, John W. Patterson, Oliver L. Saunders, Sheila Zipfel
  • MCH antagonists and their use in the treatment of obesity
    Publication number: 20030105094
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: March 19, 2002
    Publication date: June 5, 2003
    Applicant: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • 6-Methylnicotinamide derivatives as antiviral agents
    Publication number: 20030092709
    Abstract: The present invention relates to novel 6-methylnicotinamide derivatives and their pharmaceutically acceptable salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. The 6-methylnicotinamide derivatives of the present invention exhibit their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV) and Hepatitis C virus (HCV), such that they can be used for hepatitis B, hepatitis C and acquired immune deficiency syndrome (AIDS).
    Type: Application
    Filed: October 10, 2002
    Publication date: May 15, 2003
    Inventors: Sung-June Yoon, Sang-Wook Lee, Jin-Soo Lee, Nam-Doo Kim, Geun-Hyung Lee, Hak-Dong Lee, Jong-Woo Kim, Sang-Jin Park, Hee-Jeong Park
  • Substituted 3-pyridyl-4-arylpyrroles, and related therapeutic and prophylactic methods
    Patent number: 6562843
    Abstract: This invention provides novel substituted 3-pyridyl-4-arylpyrroles, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing TNF-&agr; production and/or p38 activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: May 13, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventor: James L. Bullington
  • Tricyclic compound
    Patent number: 6562817
    Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: May 13, 2003
    Assignee: Shionogi & Co., Ltd.
    Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
  • Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
    Patent number: 6555539
    Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: April 29, 2003
    Assignee: Agouron Pharmaceuticals
    Inventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace
  • Novel substituted aryl hydroxamic acids as metalloproteinase inhibitors
    Publication number: 20030073682
    Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: 1
    Type: Application
    Filed: April 3, 2002
    Publication date: April 17, 2003
    Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
  • Nitrogen containing heteroaromatics as factor Xa inhibitors
    Patent number: 6548512
    Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
  • Substituted imidazoles having anti-cancer and cytokine inhibitory activity
    Patent number: 6548520
    Abstract: The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
    Type: Grant
    Filed: March 3, 2001
    Date of Patent: April 15, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Susan B. Dillon, Sandra D. Griego, Dennis Lee
  • Il-8 receptor antagonists
    Publication number: 20030055248
    Abstract: This invention relates to novel compounds and compositions thereof useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: October 7, 2002
    Publication date: March 20, 2003
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Methods of using novel compounds as neuro-protective agents
    Publication number: 20030050311
    Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
    Type: Application
    Filed: September 3, 2002
    Publication date: March 13, 2003
    Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
  • Process for preparation of 2-phenyl acetic acid derivatives
    Patent number: 6531597
    Abstract: The present invention is a process for the preparation of a compound of formula The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabienne Hoffmann-Emery, Michelangelo Scalone, Paul Spurr
  • Compounds useful as reversible inhibitors of cysteine proteases
    Patent number: 6525052
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: February 25, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
  • Novel synthesis for heteroarylamine compounds
    Publication number: 20030028017
    Abstract: Disclosed is a novel method of producing heteroaryl amines of the formula(I): 1
    Type: Application
    Filed: July 11, 2001
    Publication date: February 6, 2003
    Inventors: Nathan Yee, Suresh R. Kapadia, Jinhua J. Song
  • Process for the synthesis of gonadotropin releasing hormone antagonists
    Publication number: 20030013876
    Abstract: The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, 1
    Type: Application
    Filed: April 5, 2002
    Publication date: January 16, 2003
    Inventors: John Y. L. Chung, Roger N. Farr, Guy R. Humphrey