Thiomorpholines (i.e., Fully Hydrogenated 1,4-thiazines) Patents (Class 544/59)
  • Patent number: 6680317
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: January 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Publication number: 20040010143
    Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
    Type: Application
    Filed: February 20, 2003
    Publication date: January 15, 2004
    Applicants: G.D. Searle & Co., Pharmacia Corporation (Monsanto Company)
    Inventors: Deborah E. Bertenshaw, Daniel P. Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
  • Publication number: 20040006225
    Abstract: Process for removing a residual fragment of a chiral auxiliary from a diastereomeric compound with formula (2) 1
    Type: Application
    Filed: November 26, 2002
    Publication date: January 8, 2004
    Inventors: Marcelles Sluis Van Der, Quirinus Bernardus Broxterman, Ben Lange De
  • Patent number: 6673803
    Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: January 6, 2004
    Assignee: Zeneca Limited
    Inventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
  • Publication number: 20030236253
    Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.
    Type: Application
    Filed: March 14, 2003
    Publication date: December 25, 2003
    Applicant: Gruenenthal GmbH
    Inventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
  • Publication number: 20030232815
    Abstract: The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the growth or regeneration of neuronal cells. In part, the invention provides compounds that interact with or bind to a cyclophilin and compounds that have activity towards neuronal cells. Methods for using the compounds, such as administering them to cells or animals or using them to treat neurodegenerative conditions, are specifically included.
    Type: Application
    Filed: June 11, 2003
    Publication date: December 18, 2003
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Mark Vaal, Chi Choi, Ling Wei
  • Publication number: 20030232806
    Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).
    Type: Application
    Filed: May 6, 2003
    Publication date: December 18, 2003
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takuya Seko, Masashi Kato
  • Publication number: 20030232811
    Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
    Type: Application
    Filed: January 31, 2003
    Publication date: December 18, 2003
    Applicant: TEIJIN LIMITED
    Inventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
  • Publication number: 20030232985
    Abstract: This invention relates to novel succinoylamino heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 18, 2003
    Inventors: Lorin A. Thompson, Padmaja Kasireddy
  • Publication number: 20030232742
    Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP&agr;, and the drug released by the enzymatic activity of FAP&agr; is cytotoxic or cytostatic under physiological conditions.
    Type: Application
    Filed: November 9, 2001
    Publication date: December 18, 2003
    Inventors: Stefan Peters, Dietmar Leipert, Christian Eickmeier, John Edward Park, Martin Lenter, Pilar Garin-Chesa, Juergen Mack
  • Publication number: 20030225071
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: June 11, 2002
    Publication date: December 4, 2003
    Inventors: Stacie S. Canan Koch, Therese N. Alexander, Mark Barvian, Gary Bolton, Fredrick E. Boyer, Benjamin J. Burke, Tod Holler, Tanya M. Jewell, Vara Prasad Josyula, David J. Kucera, Maria A. Linton, Jeffrey J. Machak, Lennert J. Mitchell, Sean T. Murphy, Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Michael Melnick
  • Publication number: 20030224940
    Abstract: The invention relates to novel pesticidally active &agr;-sulfin and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the specification, and R8 is either hydrogen, (a), (b), (c), (d) or (e) wherein R11, R12, R13, R15 and R17 are each independently hydrogen or C1-C4 alkyl, R13 is C4-C12 alkyl, C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R16 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR18R19— or —NR2O—, wherein R18, R19 and R20 independently of each other are hydrogen or C1-C4 alkyl. The novel compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
    Type: Application
    Filed: May 6, 2003
    Publication date: December 4, 2003
    Inventors: Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
  • Publication number: 20030216375
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: September 17, 2002
    Publication date: November 20, 2003
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Publication number: 20030216370
    Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.
    Type: Application
    Filed: April 10, 2003
    Publication date: November 20, 2003
    Inventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen
  • Publication number: 20030212062
    Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, 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: Application
    Filed: March 11, 2003
    Publication date: November 13, 2003
    Applicant: Synaptic Pharmaceutical Corporation
    Inventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
  • Publication number: 20030212056
    Abstract: The present application describes novel &bgr;-sulfone derivatives of formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: November 13, 2003
    Inventors: Jingwu Duan, Gregory R. Ott
  • Publication number: 20030212049
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: February 27, 2003
    Publication date: November 13, 2003
    Applicant: Wyeth
    Inventors: Jeremy I. Levin, James Ming Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Publication number: 20030208067
    Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: May 28, 2002
    Publication date: November 6, 2003
    Inventors: Sheldon Xiaodong Cao, David Paul Dumas, Xiaohua Chen, Jae Young Yang
  • Publication number: 20030208068
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Application
    Filed: March 13, 2003
    Publication date: November 6, 2003
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Publication number: 20030207871
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: February 19, 2003
    Publication date: November 6, 2003
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Publication number: 20030199698
    Abstract: Novel compounds of the formula I 1
    Type: Application
    Filed: May 16, 2003
    Publication date: October 23, 2003
    Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
  • Publication number: 20030191189
    Abstract: Compounds of Formula I are disclosed which are useful as fungicides 1
    Type: Application
    Filed: November 25, 2002
    Publication date: October 9, 2003
    Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
  • Publication number: 20030191118
    Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.
    Type: Application
    Filed: November 4, 2002
    Publication date: October 9, 2003
    Applicant: Tanabe Seiyaku Co., Ltd.
    Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
  • Publication number: 20030187295
    Abstract: The invention relates to a method for the production of &OHgr;-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2=chlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.
    Type: Application
    Filed: November 8, 2002
    Publication date: October 2, 2003
    Inventors: Volker Schaefer, Wolfgang Knoll, Alexander Schmitt, Christoph Huettner
  • Patent number: 6627627
    Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: September 30, 2003
    Assignee: Pfizer Inc.
    Inventor: Harry Ralph Howard
  • Publication number: 20030181442
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: November 27, 2001
    Publication date: September 25, 2003
    Applicant: BAYER CORPORATION
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Publication number: 20030181441
    Abstract: A compound of the formula 1
    Type: Application
    Filed: August 12, 1999
    Publication date: September 25, 2003
    Inventors: KIM MCCLURE, MARK C. NOE, MICHAEL A. LETAVIC, LOUIS S. CHUPAK
  • Publication number: 20030181443
    Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): 1
    Type: Application
    Filed: May 6, 2003
    Publication date: September 25, 2003
    Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
  • Patent number: 6624171
    Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: September 23, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
  • Publication number: 20030171579
    Abstract: The invention relates to novel compounds of formula (I), wherein R, R1 and R2 have the meaning as cited claim 1. According to the invention, the compounds are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis post-angioplasty, intermittent claudication, tumours, tumour related illnesses and/or tumour metastases.
    Type: Application
    Filed: January 27, 2003
    Publication date: September 11, 2003
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Publication number: 20030171349
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
    Type: Application
    Filed: February 28, 2003
    Publication date: September 11, 2003
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
  • Publication number: 20030171352
    Abstract: The present invention relates to compounds of the formula I 1
    Type: Application
    Filed: January 24, 2003
    Publication date: September 11, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
  • Publication number: 20030168192
    Abstract: Compounds of formula (1) containing sterically hindered groups, polymers thereof and the use of these polymers in papermaking processes and dewatering processes.
    Type: Application
    Filed: March 19, 2003
    Publication date: September 11, 2003
    Inventor: Amjad Mohmood Mohammed
  • Publication number: 20030166643
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1
    Type: Application
    Filed: December 11, 2002
    Publication date: September 4, 2003
    Applicant: Wyeth
    Inventors: Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Leo M. Albert
  • 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
  • Publication number: 20030158186
    Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: December 20, 2002
    Publication date: August 21, 2003
    Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Bradley Paul Morgan, Han-Jie Zhou, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans,
  • Publication number: 20030158180
    Abstract: A compound having the general formula (Ia) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Application
    Filed: October 3, 2002
    Publication date: August 21, 2003
    Inventor: Peter Bernstein
  • Publication number: 20030153559
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Application
    Filed: November 20, 2002
    Publication date: August 14, 2003
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
  • Publication number: 20030152600
    Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.
    Type: Application
    Filed: December 6, 2002
    Publication date: August 14, 2003
    Inventors: Maria Dalko, Yann Mahe, Lionel Breton
  • Publication number: 20030149015
    Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula 1
    Type: Application
    Filed: December 10, 2002
    Publication date: August 7, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
  • Publication number: 20030149021
    Abstract: In accordance with the present invention, there is provided a new class of compounds, i.e., mono(dithio)carbamate esters of piperazine and analogs thereof, with or without substituents. Also provided are methods for the preparation of invention compounds and the pharmaceutical use thereof in the treatment of a variety of pathological conditions, especially for the treatment of cancers. A lead compound has shown good anticancer activity with low toxicity.
    Type: Application
    Filed: May 28, 2002
    Publication date: August 7, 2003
    Applicant: Medinox, Inc.
    Inventors: Runtao Li, Tieming Cheng, Jingrong Cui, Tingmin Wang
  • Publication number: 20030149020
    Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
    Type: Application
    Filed: May 13, 2002
    Publication date: August 7, 2003
    Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
  • Publication number: 20030144277
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: September 18, 2002
    Publication date: July 31, 2003
    Inventor: George V. DeLucca
  • Publication number: 20030144276
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1
    Type: Application
    Filed: January 6, 2003
    Publication date: July 31, 2003
    Applicant: Eisai Co. Ltd.
    Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
  • Publication number: 20030144505
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: 1
    Type: Application
    Filed: January 16, 2003
    Publication date: July 31, 2003
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
  • Publication number: 20030139401
    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: Application
    Filed: November 20, 2001
    Publication date: July 24, 2003
    Applicant: Pharmacia Corporation
    Inventors: Michael S. 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, Ronald K. Webber
  • Publication number: 20030134849
    Abstract: A compound of formula (I) in which R1 is halo, lower alkoxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted heterecyclic group or optionally substituted lower alkynyl, R2 is amidated carboxy, R3 is hydrogen or acyl, Ar is aryl or heterocyclic group, X is thia, sulfinyl or sulfonyl, Y and Z are each lower alkylene, m and n are each an integer of 0 to 2, and a salt thereof, useful as inhibitors of matrix metalloproteinases (MMP) or the production of tumor necrosis factor &agr; (TNF &agr;).
    Type: Application
    Filed: August 19, 2002
    Publication date: July 17, 2003
    Inventors: Masahiro Neya, Hitoshi Yamazaki, Kazuhiko Ohne, Yuki Sawada, Tsuyoshi Mizutani, Yoshimasa Imamura, Noriko Mukai
  • Publication number: 20030134827
    Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1
    Type: Application
    Filed: March 12, 2002
    Publication date: July 17, 2003
    Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie
  • Publication number: 20030130256
    Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: February 5, 2003
    Publication date: July 10, 2003
    Inventors: David Lauffer, Michael Mullican, Brian Ledford
  • Publication number: 20030125548
    Abstract: A method for identifying molecules and designing novel pharmaceuticals is disclosed. The disclosed method of novel pharmaceutical design identifies a novel chemical group that triggers a mechanism of action for an identified reaction, thereby avoiding the various structural complexities associated with the application of the structure-based drug design. Additionally, examples of potential therapeutics identified by the mechanism based drug design method are provided.
    Type: Application
    Filed: September 13, 2002
    Publication date: July 3, 2003
    Inventors: Dorit Arad, Arthur P Bollon, David c Young, Bradley W Poland, Andrew S Peek