ATE193304T1 - Inhibitoren der menschlichen neutrophilenelastase - Google Patents

Inhibitoren der menschlichen neutrophilenelastase

Info

Publication number
ATE193304T1
ATE193304T1 AT95940031T AT95940031T ATE193304T1 AT E193304 T1 ATE193304 T1 AT E193304T1 AT 95940031 T AT95940031 T AT 95940031T AT 95940031 T AT95940031 T AT 95940031T AT E193304 T1 ATE193304 T1 AT E193304T1
Authority
AT
Austria
Prior art keywords
inhibitors
elastasis
human neutrophil
elastase
human
Prior art date
Application number
AT95940031T
Other languages
English (en)
Inventor
Albert Gyorkos
Lyle W Spruce
Original Assignee
Cortech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cortech Inc filed Critical Cortech Inc
Application granted granted Critical
Publication of ATE193304T1 publication Critical patent/ATE193304T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
AT95940031T 1994-11-21 1995-11-17 Inhibitoren der menschlichen neutrophilenelastase ATE193304T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/345,820 US5618792A (en) 1994-11-21 1994-11-21 Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
PCT/US1995/014989 WO1996016080A1 (en) 1994-11-21 1995-11-17 Human neutrophil elastase inhibitors

Publications (1)

Publication Number Publication Date
ATE193304T1 true ATE193304T1 (de) 2000-06-15

Family

ID=23356635

Family Applications (1)

Application Number Title Priority Date Filing Date
AT95940031T ATE193304T1 (de) 1994-11-21 1995-11-17 Inhibitoren der menschlichen neutrophilenelastase

Country Status (17)

Country Link
US (8) US5618792A (de)
EP (1) EP0793674B1 (de)
JP (1) JPH10511933A (de)
KR (1) KR100369665B1 (de)
CN (1) CN1170414A (de)
AT (1) ATE193304T1 (de)
AU (1) AU687285B2 (de)
CA (1) CA2205198C (de)
DE (1) DE69517196T2 (de)
DK (1) DK0793674T3 (de)
ES (1) ES2145936T3 (de)
GR (1) GR3034208T3 (de)
IL (1) IL116078A (de)
PT (1) PT793674E (de)
TW (1) TW474924B (de)
WO (1) WO1996016080A1 (de)
ZA (1) ZA959819B (de)

Families Citing this family (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6001814A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors
US6100238A (en) * 1994-11-21 2000-08-08 Cortech Inc. Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors
US6150334A (en) * 1994-11-21 2000-11-21 Cortech, Inc. Serine protease inhibitors-tripeptoid analogs
US6001811A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors--N-substituted derivatives
US6015791A (en) * 1994-11-21 2000-01-18 Cortech Inc. Serine protease inhibitors-cycloheptane derivatives
US20020119985A1 (en) * 1994-11-21 2002-08-29 Albert Gyorkos Serine protease inhibitors
US6159938A (en) * 1994-11-21 2000-12-12 Cortech, Inc. Serine protease inhibitors comprising α-keto heterocycles
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US6001813A (en) * 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
US5998379A (en) * 1994-11-21 1999-12-07 Cortech Inc. Serine protease inhibitors-proline analogs
MY113488A (en) * 1995-01-27 2002-03-30 Novo Nordisk As Compounds with growth hormone releasing properties
WO1997046514A1 (en) * 1996-05-31 1997-12-11 Novartis Ag Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues
TR199901681T2 (xx) 1996-12-06 2000-03-21 Cortech, Inc. Serin proteas inhibit�rleri.
US6635632B1 (en) * 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US5773430A (en) * 1997-03-13 1998-06-30 Research Foundation Of State University Of New York Serine proteinase inhibitory activity by hydrophobic tetracycline
AR012374A1 (es) * 1997-04-15 2000-10-18 Smithkline Beecham Corp Inhibidores de proteasas, composiones farmaceuticas y usos para la preparacion de medicamentos.
US6004933A (en) * 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
AU9664198A (en) * 1997-09-26 1999-04-23 Eli Lilly And Company Method for the treatment of cystic fibrosis
AU746582B2 (en) * 1997-10-23 2002-05-02 Southern Research Institute Activating C1-secretion
US6656910B2 (en) 1997-12-04 2003-12-02 Cortech, Inc. Serine protease inhibitors
US6610748B1 (en) * 1998-02-24 2003-08-26 Fujisawa Pharmaceutical Co., Ltd. Preventives/remedies for skin aging
US6162791A (en) * 1998-03-02 2000-12-19 Apotex Inc. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes
IL139187A0 (en) * 1998-04-23 2001-11-25 Cortech Inc Cysteine protease inhibitors
KR20010078724A (ko) * 1998-06-03 2001-08-21 존 더블류. 갈루치 2세 세린 프로테아제 저해제로서의 인돌 및테트라히드로이소퀴놀린을 함유하는 α-케토 옥사디아졸
US6255453B1 (en) * 1998-06-03 2001-07-03 Cortech, Inc. Peptoid and nonpeptoid containing alpha-keto oxadiazoles as serine protease inhibitors
EP1114822A3 (de) * 1998-06-03 2002-11-13 Cortech Inc. Alpha-Keto-oxadiazole enthaltende Indole und Tetrahydroisochinoline zur Verwendung als Serin-Protease-Hemmer
DZ2815A1 (fr) * 1998-06-12 2003-12-01 Smithkline Beecham Corp Inhibiteurs de protéase.
US6958330B1 (en) * 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related compounds
AUPP508798A0 (en) * 1998-08-05 1998-08-27 Biotech Australia Pty Limited Method of treating psoriasis
EP1105412A1 (de) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitoren bestehend aus alpha-keto heterozyklischen verbindungen
US6576654B1 (en) 1998-09-23 2003-06-10 Eli Lilly And Company Method for the treatment of cystic fibrosis
WO2000032620A1 (en) 1998-12-02 2000-06-08 Merck Frosst Canada & Co. Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
US6849605B1 (en) * 1999-03-05 2005-02-01 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
AU3731400A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
AU3864000A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of herpes viruses
WO2000051623A2 (en) 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
WO2000055145A1 (en) 1999-03-12 2000-09-21 Ono Pharmaceutical Co., Ltd. 1,3,4-oxadiazole derivatives and process for producing the same
US20040176358A1 (en) * 1999-04-30 2004-09-09 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US20060025388A1 (en) * 1999-04-30 2006-02-02 Glick Gary D Compositions and methods relating to novel compounds and targets thereof
US7276348B2 (en) * 1999-04-30 2007-10-02 Regents Of The University Of Michigan Compositions and methods relating to F1F0-ATPase inhibitors and targets thereof
US20030119029A1 (en) * 1999-04-30 2003-06-26 Regents Of The University Of Michigan Compositions and methods relating to novel benzodiazepine compounds and targets thereof
MXPA01011052A (es) 1999-04-30 2002-11-22 Univ Michigan Aplicaciones terapeuticas de benzodiazepinas pro-apoctoticas.
US7144880B2 (en) 1999-04-30 2006-12-05 Regents Of The University Of Michigan Compositions relating to novel compounds and targets thereof
US20050113460A1 (en) * 1999-04-30 2005-05-26 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6867217B1 (en) * 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) * 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6908919B2 (en) * 1999-05-19 2005-06-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6906068B1 (en) 1999-05-19 2005-06-14 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4 - triazinones useful as anticoagulants
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
CA2375229A1 (en) * 1999-06-17 2000-12-28 Source Precision Medicine, Inc. Method and compounds for inhibiting activity of serine elastases
CA2376961A1 (en) * 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
AR026748A1 (es) * 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
US6448278B2 (en) * 1999-12-23 2002-09-10 Pfizer Inc. Procollagen C-proteinase inhibitors
WO2001068605A1 (en) * 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
AU2001251315A1 (en) * 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
EP1274676A2 (de) * 2000-04-17 2003-01-15 Pharmacia Corporation Polycyclische aryl- und heteroaryl- substuierte 1,4-chinone zur selektiven hemmung des blutgerinnungsprozesses
WO2001087851A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
CA2416248A1 (en) 2000-07-18 2002-01-24 Neurogen Corporation 5-substituted 2-aryl-4-pyrimidinones
WO2002026229A1 (en) * 2000-09-29 2002-04-04 Ono Pharmaceutical Co., Ltd. Airway mucus secretion inhibitors
AU2001292306A1 (en) * 2000-09-29 2002-04-08 Ono Pharmaceutical Co. Ltd. Remedies for inflammatory bowel diseases
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
CA2430037A1 (en) 2000-11-20 2002-05-30 Michael S. South Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
AU2001297611A1 (en) 2000-12-29 2002-08-19 Celltech R And D, Inc. Pharmaceutical uses and synthesis of diketopiperazines
US6645993B2 (en) * 2001-03-30 2003-11-11 Warner-Lambert Company 3-heterocyclylpropanohydroxamic acid PCP inhibitors
US20030236257A1 (en) * 2001-04-04 2003-12-25 South Michael S. Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the cogulation cascade
ATE445400T1 (de) * 2001-05-25 2009-10-15 Bristol Myers Squibb Co Hydantion-derivate als hemmer von matrix- metalloproteinasen
WO2003006014A1 (en) * 2001-07-10 2003-01-23 Ono Pharmaceutical Co., Ltd. Medicine comprising combination of five-membered heterocyclic compound and drug compensating for or enhancing its activity
CA2462647A1 (en) * 2001-10-03 2003-04-10 Michael S. South 6-membered unsaturated heterocyclic compounds useful for selective inhibition of the coagulation cascade
BR0213092A (pt) * 2001-10-03 2004-10-19 Pharmacia Corp Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação
US20040082585A1 (en) * 2001-10-03 2004-04-29 Pharmacia Corporation Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
MXPA04003170A (es) * 2001-10-03 2004-07-08 Pharmacia Corp Compuestos policiclicos, sustituidos, provisto de 5 miembros, utiles para la inhibicion selectiva de la cascada de coagulacion.
EP1456225A2 (de) * 2001-11-14 2004-09-15 Geneprot, Inc. Erweiterte native chemische ligation von drei oder mehreren peptidfragmenten
US20040068113A1 (en) * 2001-11-20 2004-04-08 South Michael S. Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
WO2003047740A2 (en) * 2001-12-05 2003-06-12 California Institute Of Technology ENANTIOSELECTIVE TRANSFORMATION OF α,β-UNSATURATED KETONES USING CHIRAL ORGANIC CATALYSTS
CA2369540C (en) * 2001-12-31 2013-10-01 Blackberry Limited Method and apparatus for computing a shared secret key
WO2003074450A2 (en) * 2002-02-28 2003-09-12 The University Of Tennessee Research Corporation Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
US20040018984A1 (en) * 2002-07-17 2004-01-29 Mizuo Miyazaki Methods for preventing adhesion formation using protease inhibitors
TW200418791A (en) * 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
US20040220242A1 (en) * 2003-05-02 2004-11-04 Leland Shapiro Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide induced clinical conditions
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
US7059806B2 (en) * 2003-08-21 2006-06-13 Trangsrud Julian P Hole former for an invert
DK2520654T3 (en) * 2003-08-26 2017-05-01 Univ Colorado Regents Inhibitors of serine protease activity and their use in methods and compositions for the treatment of bacterial infections
ATE483708T1 (de) 2004-03-08 2010-10-15 Prosidion Ltd Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
US20050272723A1 (en) * 2004-04-27 2005-12-08 The Regents Of The University Of Michigan Methods and compositions for treating diseases and conditions associated with mitochondrial function
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US20060052369A1 (en) * 2004-09-07 2006-03-09 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
JP2008528448A (ja) * 2005-01-03 2008-07-31 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 新規化合物に関連する組成物および方法、ならびにその標的
CA2611031A1 (en) 2005-06-01 2007-05-10 The Regents Of The University Of Michigan Unsolvated benzodiazepine compositions and methods
US20070105844A1 (en) * 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
CA2779041A1 (en) 2005-11-01 2007-05-10 The Regents Of The University Of Michigan Novel 1,4-benzodiazepine-2,5-diones with therapeutic properties
US20080124303A1 (en) * 2005-12-12 2008-05-29 Cavit Sciences, Inc Methods and compositions for treatment of viral infections
US7759338B2 (en) * 2006-04-27 2010-07-20 The Regents Of The University Of Michigan Soluble 1,4 benzodiazepine compounds and stable salts thereof
EP2027143A2 (de) * 2006-05-23 2009-02-25 Irm Llc Verbindungen und zusammensetzungen als kanalaktivierende protease-hemmer
JP5264716B2 (ja) 2006-06-09 2013-08-14 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 化合物およびその標的に関連する組成物および方法
CA2677487A1 (en) 2007-02-09 2008-08-14 Irm Llc Compounds and compositions as channel activating protease inhibitors
KR101131238B1 (ko) 2007-02-09 2012-03-30 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
CA2677485A1 (en) * 2007-02-09 2008-08-14 Irm Llc Compounds and compositions as channel activating protease inhibitors
JP5383513B2 (ja) 2007-03-09 2014-01-08 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 化合物およびその標的に関連する組成物ならびに方法
BRPI0811204A8 (pt) * 2007-05-10 2015-09-22 Bristol Myers Squibb Co Tetra-hidroibenzo-1,4-diazepinas substituídas por arila e heteroarila e uso das mesmas para bloquear a recaptação de norepinefrina, dopamina e serotonina
NZ583689A (en) 2007-09-14 2012-04-27 Univ Michigan F1f0-atpase inhibitors and related methods
NZ584842A (en) 2007-11-06 2012-06-29 Univ Michigan Benzodiazepinone compounds useful in the treatment of skin conditions, in particular, psoriasis
US20090156509A1 (en) * 2007-12-12 2009-06-18 Accuthera, Inc. Tri-peptide Inhibitors of Serine Elastases
AU2009291632B2 (en) 2008-09-11 2013-04-04 The Regents Of The University Of Michigan Aryl guanidine F1F0-ATPase inhibitors and related methods
WO2010121164A2 (en) 2009-04-17 2010-10-21 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
JP2013505258A (ja) 2009-09-18 2013-02-14 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン ベンゾジアゼピノン化合物およびそれを使用する治療方法
JP5856064B2 (ja) 2009-11-17 2016-02-09 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療特性を有する1,4−ベンゾジアゼピン−2,5−ジオンおよび関連化合物
US9126978B2 (en) 2009-11-17 2015-09-08 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
MY159958A (en) * 2009-12-18 2017-02-15 Idenix Pharmaceuticals Inc 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors
EP3628327A1 (de) 2011-06-24 2020-04-01 The Regents of the University of Colorado, A Body Corporate Zusammensetzungen, verfahren und verwendung für alpha-1-antitrypsin-fusionsmoleküle
US20130101664A1 (en) 2011-08-18 2013-04-25 Donald W. Kufe Muc1 ligand traps for use in treating cancers
KR20140137347A (ko) 2012-01-10 2014-12-02 더 리젠츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코포레이트 알파-1 안티트립신 융합 분자용 조성물, 방법 및 용도
RU2670982C2 (ru) 2013-05-08 2018-10-29 Киссеи Фармасьютикал Ко., Лтд. ПРОИЗВОДНЫЕ α-ЗАМЕЩЕННОГО ГЛИЦИНАМИДА
AU2020349353A1 (en) 2019-09-17 2022-04-14 Duke University Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
HUE064089T2 (hu) 2020-04-16 2024-02-28 Mereo Biopharma 4 Ltd Alvelesztat neutrofil elasztáz inhibitort alkalmazó módszerek alfa-1-antitripszin hiány által közvetített légzõszervi megbetegedés kezelésére
AU2022373971A1 (en) 2021-10-20 2024-04-04 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis
CN119431269B (zh) * 2024-10-10 2026-03-24 浙江工业大学 一种由1,2-二酰肼类化合物合成1,3,4-恶二唑类化合物的方法

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB397073A (en) * 1932-06-09 1933-08-17 Solex Improvements in carburettors for internal combustion engines
GB1397073A (en) * 1971-05-19 1975-06-11 Glaxo Lab Ltd 1,2,4-oxadizoles
US4338453A (en) * 1980-09-17 1982-07-06 The Upjohn Company Aminoalkyl-1,2,4-triazoles
US5055450A (en) * 1985-01-22 1991-10-08 Ici Americas Inc. Peptide derivatives
GB8809316D0 (en) * 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
EP0376012A3 (de) * 1988-12-27 1992-05-06 American Cyanamid Company Renin-Hemmer
KR920701200A (ko) * 1990-03-30 1992-08-11 미즈노 시게루 신규의 4h-3,1-벤조옥사진-4-온 유도체
GB9216272D0 (en) * 1991-08-15 1992-09-09 Ici Plc Substituted heterocycles
ZA926185B (en) * 1991-08-22 1993-03-01 Merrell Dow Pharma Novel orally-active elastase inhibitors.
GB9307555D0 (en) * 1992-04-16 1993-06-02 Zeneca Ltd Heterocyclic compounds
FR2694295B1 (fr) * 1992-07-28 1994-09-02 Adir Nouveaux peptides dérivés de trifluoromethylcetones, leur procéde de préparation et les compositions pharmaceutiques qui les contiennent.
US5550139A (en) * 1994-01-03 1996-08-27 The Wichita State University Serine protease inhibitors
GB9402680D0 (en) * 1994-02-11 1994-04-06 Zeneca Ltd Pyrrolidine derivatives
AU690986B2 (en) * 1994-06-02 1998-05-07 Merrell Pharmaceuticals Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase

Also Published As

Publication number Publication date
IL116078A0 (en) 1996-01-31
KR100369665B1 (ko) 2003-04-11
EP0793674A1 (de) 1997-09-10
JPH10511933A (ja) 1998-11-17
CN1170414A (zh) 1998-01-14
US6037325A (en) 2000-03-14
WO1996016080A1 (en) 1996-05-30
AU4164696A (en) 1996-06-17
US5861380A (en) 1999-01-19
PT793674E (pt) 2000-11-30
US5618792A (en) 1997-04-08
IL116078A (en) 1999-12-31
ES2145936T3 (es) 2000-07-16
EP0793674B1 (de) 2000-05-24
TW474924B (en) 2002-02-01
GR3034208T3 (en) 2000-11-30
DK0793674T3 (da) 2000-08-14
US5891852A (en) 1999-04-06
US5874585A (en) 1999-02-23
CA2205198A1 (en) 1996-05-30
ZA959819B (en) 1996-05-30
DE69517196T2 (de) 2001-02-01
AU687285B2 (en) 1998-02-19
US5807829A (en) 1998-09-15
CA2205198C (en) 2002-06-04
DE69517196D1 (de) 2000-06-29
US5869455A (en) 1999-02-09
US5801148A (en) 1998-09-01

Similar Documents

Publication Publication Date Title
DE69517196D1 (de) Inhibitoren der menschlichen neutrophilenelastase
WO1998024806A3 (en) Substituted oxadiazole, thiadiazole and triazole serine protease inhibitors
NO934218D0 (no) Inhibitorer av cathepsin G og elastase for forhindring avbindevevsnedbrytning
TR199901191T2 (xx) Benzamidoaldehitlerin sistein proteaz� inhibit�r� olarak kullan�m�.
MY122696A (en) Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases.
DK1029921T3 (da) Serpinresistent t-PA, mutanter, gener
CY1108610T1 (el) Πεπτιδια της il-2 και παραγωγα αυτων και χρηση αυτων ως θεραπευτικοι παραγοντες
BR0215405A (pt) Composições e processos de uso de collajolie
MY113489A (en) Reversible protease inhibitors
TR199800773T2 (xx) Trombin inhibit�rleri.
TR199902751T2 (xx) Proteaz inhibit�rleri.
ATE261969T1 (de) Pyrrolopyrrolone als inhibitoren von neutrophiler elastase
EE200000138A (et) Pürrolopürrolooni derivaadid neutrofiili elastaasi inhibiitoritena
MY128261A (en) New substituted azetidinones as anti-inflammatory and antidegenerative agents
HUT76926A (hu) Új elasztáz inhibitorok
BG103789A (en) Fungicidal compositions
EE200000137A (et) Pürrolopürrolooni derivaadid neutrofiili elastaasi inhibiitoritena
WO1998020034A3 (en) Novel serine protease inhibitor nucleic acid molecules, proteins and uses thereof
FI951078A0 (fi) Retrovirusinfektion inhibitio
ATE192443T1 (de) Dithiazoldioxide und ihre verwendung als mikrobizide
BR9713684A (pt) Inibidores de serina protease
IT1305242B1 (it) Preparatore di mazzi di pelli.

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee