Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/304)
Sulfur and acyclic nitrogen bonded directly to the same carbon (Class 546/305)
Plural acyclic nitrogens bonded directly to the same carbon or single bonded directly to each other (Class 546/306)
Plural nitrogens attached directly to the six-membered hetero ring by nonionic bonding (Class 546/307)
Acyclic nitrogen bonded directly to a -c(=x)- group, wherein x is chalcogen (Class 546/309)
Having -c(=x)-, wherein x is chalcogen, bonded directly to the six-membered hetero ring (Class 546/310)
The nitrogen bonded additionally only to hydrogen (Class 546/311)
Chalcogen attached indirectly to the six-membered hetero ring by nonionic bonding (Class 546/312)
  • Photographic processing composition containing heterocycle combination and method of forming image
    Publication number: 20030054298
    Abstract: A photographic processing composition for silver halide color photographic lightsensitive material, comprising at least one compound represented by the formula (I):
    Type: Application
    Filed: March 29, 2002
    Publication date: March 20, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Makoto Suzuki, Yasufumi Nakai, Yoshiharu Yabuki
  • Novel cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
    Publication number: 20030050314
    Abstract: There are described cycloalkyl derivatives of the formula (I)
    Type: Application
    Filed: May 10, 2002
    Publication date: March 13, 2003
    Applicant: Aventis Pharma S.A.
    Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
  • Pyridine compounds and their pharmaceutical use
    Patent number: 6521643
    Abstract: A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: February 18, 2003
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaki Tomishima, Kazuhiko Take
  • Process
    Patent number: 6518432
    Abstract: The invention relates to a novel process for the preparation of certain pharmaceutically active pyridyl compounds.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: February 11, 2003
    Assignee: AstraZeneca AB
    Inventor: Melvyn E. Giles
  • HIV integrase inhibitors
    Publication number: 20030027847
    Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula 1
    Type: Application
    Filed: June 18, 2001
    Publication date: February 6, 2003
    Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
  • (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Publication number: 20030027826
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CERP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: December 12, 2001
    Publication date: February 6, 2003
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Chiral catalysts for asymmetric acylation and related transformations
    Publication number: 20030017942
    Abstract: A chiral catalyst comprising a 3,4-disubstituted pyridine, or a salt, N functionalized derivative, dimer or oligomer thereof, wherein the 3-substituent is substantially hindered from rotation about the bond (sp2-sp2 biaryl axis) linking it to pyridine and the 4-substituent is an aliphatic or aromatic amine linked by a single bond to the pyridine, the pyridine nitrogen being functionalized or unfunctionalized, preferably comprising a compound of formula I 1
    Type: Application
    Filed: May 30, 2002
    Publication date: January 23, 2003
    Inventors: Alan Christopher Spivey, Tomasz Slawomir Fekner
  • Advanced glycation end-product intermediaries and post-amadori inhibition
    Publication number: 20030013746
    Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.
    Type: Application
    Filed: August 8, 2002
    Publication date: January 16, 2003
    Applicant: University of Kansas Medical Center.
    Inventors: Billy G. Hudson, Parvin Todd, Raja Gabriel Khalifah, Aaron Ashley Booth
  • Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
    Patent number: 6495574
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: December 17, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Compounds and methods for the inhibition of the expression of VCAM-1
    Publication number: 20020177717
    Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
    Type: Application
    Filed: January 30, 2002
    Publication date: November 28, 2002
    Inventor: Patricia K. Somers
  • N-(aryl)-2-arylethenesulfonamides and therapeutic uses thereof
    Publication number: 20020165412
    Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.
    Type: Application
    Filed: February 28, 2002
    Publication date: November 7, 2002
    Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
  • Inhibitors of glycogen synthase kinase 3
    Publication number: 20020156087
    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 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: September 6, 2001
    Publication date: October 24, 2002
    Inventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Kirk Johnson, Keith B. Pfister, Savithri Ramurthy, Lynn Seely, Allan S. Wagman, Manjo Desai, Barry H. Levine
  • Novel herbicides
    Publication number: 20020156285
    Abstract: Compounds of formula 1 1
    Type: Application
    Filed: January 31, 2002
    Publication date: October 24, 2002
    Inventors: Walter Kunz, Kurt Nebel
  • Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6458803
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • N- heterocyclic inhibitors of TNF-alpha expression
    Publication number: 20020137747
    Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.
    Type: Application
    Filed: June 26, 2001
    Publication date: September 26, 2002
    Inventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
  • Process for a carbon-carbon coupling reaction of aryl halides with olefins by heterogeneous catalysts
    Publication number: 20020128478
    Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.
    Type: Application
    Filed: March 4, 2002
    Publication date: September 12, 2002
    Inventors: Shane W. Krska, Thorsten S. Rosner, Yongkui Sun
  • Processes for preparing pesticidal intermediates
    Publication number: 20020128485
    Abstract: The present invention relates to processes for the preparation of a compound of the formula 1
    Type: Application
    Filed: April 12, 2002
    Publication date: September 12, 2002
    Inventor: Jean-Erick Ancel
  • Propanolamine derivatives
    Publication number: 20020120148
    Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: 1
    Type: Application
    Filed: February 14, 2002
    Publication date: August 29, 2002
    Applicant: Fujisawa Pharmaceutical Co. Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • 2-methoxyimino-2- (pyridinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
    Publication number: 20020115865
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Application
    Filed: January 30, 2002
    Publication date: August 22, 2002
    Inventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmit
  • Cyanoguanidines as cell proliferation inhibitors
    Publication number: 20020107400
    Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, 1
    Type: Application
    Filed: February 4, 2002
    Publication date: August 8, 2002
    Applicant: Leo Pharmaceutical Products Ltd. A/S
    Inventors: Charlotte Schou Hunneche, Erik Rytter Ottosen
  • Phenylserine derivatives as integrin antagonists
    Publication number: 20020095050
    Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.
    Type: Application
    Filed: June 12, 2001
    Publication date: July 18, 2002
    Inventor: Andrea Vaupel
  • Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists
    Patent number: 6420558
    Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: July 16, 2002
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Minoru Ishikawa, Shoichi Murakami, Mikio Yamamoto, Dai Kubota, Mitsugu Hachisu, Kiyoaki Katano, Keiichi Ajito
  • 4-phenyl-pyridine derivatives
    Publication number: 20020091265
    Abstract: The present invention relates to compounds of the general formula 1
    Type: Application
    Filed: July 10, 2001
    Publication date: July 11, 2002
    Inventors: Michael Bos, Quirico Branca, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Dermal anesthetic agents
    Patent number: 6413987
    Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Substituted pyridine compounds useful for controlling chemical synaptic transmission
    Publication number: 20020058646
    Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.
    Type: Application
    Filed: February 1, 2001
    Publication date: May 16, 2002
    Inventors: Nan-Horng Lin, Liming Dong
  • Naphthalene derivatives
    Publication number: 20020058811
    Abstract: Compounds of formula (1) where R1 is of formulae (II), (III), or (IV), or (V); R2 is —R4, —O—R4, —O—S(O)2—R4, —NR4R5, R4—(CH2)b—NH(C═X)—(CH2)c—, R4—(CH2)b—O(C—O)NH—(CH2)c—(C═O)NH—, R4—(C═O)NH—(C═O)NH—, —(CH2)b—NH(C═X)—(CH2)c—R4, R4—(CH2)b—O(C═O)CH2)c—, —(CH2)b—O(C═O)—(CH2)c—R4, —NH(C═X)NH—R4, R4—O(C═O)O—, —O(C═O)NH—R4, R4—O(C═O)NH—, —(CH2)b—(C═O)—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C═O)—NR4, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae —R4, —R4R5, &md
    Type: Application
    Filed: December 3, 2001
    Publication date: May 16, 2002
    Inventors: Bertrand L. Chenard, John E. Macor, Barbara E. Segelstein
  • Substituted urea compounds useful in pain management
    Patent number: 6387949
    Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: May 14, 2002
    Assignee: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Vlad Gregor, Niklas Plobeck, Edward Roberts, Eric Sun
  • Process for making 3-amino-2-chloro-4-methylpyridine
    Publication number: 20020052507
    Abstract: A method for making 3-amino-2-chloro-4-methylpyridine, as shown in Scheme 12, below.
    Type: Application
    Filed: September 12, 2001
    Publication date: May 2, 2002
    Inventor: Bernard Franklin Gupton
  • Water-soluble rhodamine dye peptide conjugates
    Patent number: 6372907
    Abstract: The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: April 16, 2002
    Assignee: Apptera Corporation
    Inventors: Linda G. Lee, Ronald J. Graham, William E. Werner, Elana Swartzman, Lily Lu
  • Supernucleophilic 4-substituted-pyridine catalysts, and processes useful for preparing same
    Patent number: 6369230
    Abstract: A process of preparing 4-substituted pyridine compounds via pyridine betaine compounds.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: April 9, 2002
    Assignee: Reilly Industries, Inc.
    Inventors: Joe W. Curtis, Marudai Balasubramanian, Joel R. Calvin, Eric F. V. Scriven, Charles R. Hopper, Ramiah Murugan, L. Mark Huckstep
  • Substituted 4-phenyl-pyridine compounds with activity as antagonists of neurokinin 1 receptors
    Publication number: 20020040040
    Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
    Type: Application
    Filed: August 3, 2001
    Publication date: April 4, 2002
    Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Enamine derivatives
    Publication number: 20020037909
    Abstract: Enamine derivatives of formula (1) are described: 1
    Type: Application
    Filed: April 16, 2001
    Publication date: March 28, 2002
    Inventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
  • Cycloalkenyl substituted compounds
    Patent number: 6362193
    Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: March 26, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ravi Garigipati
  • Solid phase synthesis of heterocycles
    Patent number: 6362009
    Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: March 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Benito Munoz, Chixu Chen
  • Pharmaceutical compositions for prevention and treatment of central nervous system disorders
    Publication number: 20020032206
    Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.
    Type: Application
    Filed: October 9, 2001
    Publication date: March 14, 2002
    Inventors: William Scott Caldwell, Gary Maurice Dull, Garyland Page Dobson
  • Branched alkoxy-subsituted 2-aminopyridines
    Publication number: 20020022642
    Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula 1
    Type: Application
    Filed: September 20, 2001
    Publication date: February 21, 2002
    Inventor: John Adams Lowe
  • Corticotropin releasing factor antagonists
    Publication number: 20020016328
    Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae 1
    Type: Application
    Filed: January 17, 2001
    Publication date: February 7, 2002
    Inventor: Yuhpyng L. Chen
  • IL-8 receptor antagonists
    Patent number: 6335352
    Abstract: Novel compounds useful in the treatment of Interleukin-8 mediated diseases, and methods of using them are disclosed.
    Type: Grant
    Filed: February 4, 1999
    Date of Patent: January 1, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Deborah Lynn Bryan, John Gerald Gleason, Katherine L. Widdowson
  • Substituted 3,3-diamino-2-propenenitriles, their preparation and use
    Publication number: 20010056188
    Abstract: Disclosed are substituted cyanoenamines, compositions containing these compounds, and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.
    Type: Application
    Filed: March 16, 2001
    Publication date: December 27, 2001
    Inventors: John Bondo Hansen, Tina Moller Tagmose, John Patrick Mogensen, Florencio Zaragoza Dorwald, Anker Steen Jorgensen
  • Aromatic amine derivatives having NOS inhibiting action
    Patent number: 6331553
    Abstract: Compounds represented by the general formula (1): (where R1 and R2 are typically a hydrogen atom; R3 and R4 are typically a hydrogen atom or a lower alkyl group; R5 is typically a hydrogen atom; X1, X2, X3 and X4 are typically a hydrogen atom or a lower alkoxy group; A is typically an optionally substituted pyridine ring; m and n are each 0 or 1) have an NOS inhibiting activity and are useful as therapeutics of cerebrovascular diseases and other pharmaceuticals.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: December 18, 2001
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Toru Esaki, Toshihiko Makino, Yoshikazu Nishimura, Toshiaki Nagafuji
  • Heterocyclic protease inhibitors
    Patent number: 6326492
    Abstract: Described are compounds of the Formula VII: wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: December 4, 2001
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Aihua Wang, Tianbao Lu, Bruce E. Tomczuk, Richard M. Soll, John Spurlino, Roger Bone
  • Diagnostic reagent for complications associated with diabetes or renal failure
    Patent number: 6323038
    Abstract: In view of the situation of the prior art, the present invention specifies the structure of a late-stage product of Mailard reaction in vivo having a close relation with various tissue disorders, and provides a diagnostic reagent for complications associated with diabetes or renal failure, containing the above compound as a main component.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: November 27, 2001
    Assignee: Asai Germanium Research Institute Co., Ltd.
    Inventors: Tomoko Oya, Hiroyuki Kobayashi, Mitsuo Akiba, Norihiro Kakimoto, Yasujiro Morimitsu, Toshihiko Osawa
  • Modulators of p38 MAP kinase
    Publication number: 20010044440
    Abstract: Compounds of formula I are effective modulators of p38 MAP kinase.
    Type: Application
    Filed: February 23, 2001
    Publication date: November 22, 2001
    Inventors: David J. Morgans, Silke Thode, Dongxu Sun
  • Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
    Publication number: 20010044536
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: 1
    Type: Application
    Filed: May 4, 2001
    Publication date: November 22, 2001
    Inventor: Gary B. Phillips
  • Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
    Publication number: 20010044537
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: 1
    Type: Application
    Filed: May 4, 2001
    Publication date: November 22, 2001
    Applicant: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Process for preparing 2-phenyl-3-aminopyridine, substituted phenyl derivatives, thereof, and salts thereof
    Patent number: 6316632
    Abstract: A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: November 13, 2001
    Assignee: Pfizer Inc
    Inventors: Tamim F. Braish, Stephane Caron, Michael James Castaldi
  • &agr;-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
    Patent number: 6313150
    Abstract: An &agr;-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R1 represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR2 (R2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: November 6, 2001
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshikazu Ohtsuka, Takami Murashi, Shinji Suzuki, Michio Masuko, Hideyuki Takenaka
  • Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    Patent number: 6313302
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
    Publication number: 20010031874
    Abstract: The present invention provides compounds of Formula I shown below.
    Type: Application
    Filed: May 15, 2001
    Publication date: October 18, 2001
    Inventors: David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
  • Tetrapartate prodrugs
    Publication number: 20010031873
    Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided 1
    Type: Application
    Filed: January 12, 2001
    Publication date: October 18, 2001
    Inventors: Richard B. Greenwald, Hong Zhao