DK0793674T3 - Inhibitorer af human neutrofil elastase - Google Patents

Inhibitorer af human neutrofil elastase

Info

Publication number
DK0793674T3
DK0793674T3 DK95940031T DK95940031T DK0793674T3 DK 0793674 T3 DK0793674 T3 DK 0793674T3 DK 95940031 T DK95940031 T DK 95940031T DK 95940031 T DK95940031 T DK 95940031T DK 0793674 T3 DK0793674 T3 DK 0793674T3
Authority
DK
Denmark
Prior art keywords
inhibitors
neutrophil elastase
human neutrophil
elastase
thiadiazole
Prior art date
Application number
DK95940031T
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 DK0793674T3 publication Critical patent/DK0793674T3/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12Cyclic peptides with only normal peptide bonds in the ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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)
DK95940031T 1994-11-21 1995-11-17 Inhibitorer af human neutrofil elastase DK0793674T3 (da)

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
DK0793674T3 true DK0793674T3 (da) 2000-08-14

Family

ID=23356635

Family Applications (1)

Application Number Title Priority Date Filing Date
DK95940031T DK0793674T3 (da) 1994-11-21 1995-11-17 Inhibitorer af human neutrofil elastase

Country Status (17)

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

Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6001813A (en) * 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
US6150334A (en) * 1994-11-21 2000-11-21 Cortech, Inc. Serine protease inhibitors-tripeptoid analogs
US6015791A (en) * 1994-11-21 2000-01-18 Cortech Inc. Serine protease inhibitors-cycloheptane derivatives
US5998379A (en) * 1994-11-21 1999-12-07 Cortech Inc. Serine protease inhibitors-proline analogs
US20020119985A1 (en) 1994-11-21 2002-08-29 Albert Gyorkos Serine protease inhibitors
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
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
US6159938A (en) * 1994-11-21 2000-12-12 Cortech, Inc. Serine protease inhibitors comprising α-keto heterocycles
US6001811A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors--N-substituted derivatives
EP0805816B1 (en) * 1995-01-27 2004-07-28 Novo Nordisk A/S Compounds with growth hormone releasing properties
AU2959397A (en) * 1996-05-31 1998-01-05 Novartis Ag Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues
NZ336046A (en) * 1996-12-06 2000-10-27 Cortech Inc Serine protease inhibitors containing substituted oxadiazole, thiadiazole and triazole peptide derivatives
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
JP2001517707A (ja) * 1997-09-26 2001-10-09 イーライ・リリー・アンド・カンパニー 嚢胞性繊維症の処置方法
US6251930B1 (en) 1997-10-23 2001-06-26 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
EP1089752A4 (en) * 1998-06-03 2002-01-02 Cortech Inc ALPHA-KETO OXADIAZOLE AS A SERINE PROTEASE INHIBITOR
EP1114822A3 (en) * 1998-06-03 2002-11-13 Cortech Inc. Indoles and tetrahydroisoquinolines containing alpha-keto oxadiazoles as serine protease inhibitors
EP1093368A4 (en) * 1998-06-03 2002-11-13 Cortech Inc ALPHA KETOOXADIAZOLES CONTAINING INDOL AND TETRAHYDROISOQUINOLINE AS SERINE PROTEASE INHIBITORS
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 (en) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
US6576654B1 (en) 1998-09-23 2003-06-10 Eli Lilly And Company Method for the treatment of cystic fibrosis
AU764860B2 (en) 1998-12-02 2003-09-04 Merck Frosst Canada & Co. Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
AU3731400A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
WO2000051625A1 (en) * 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of herpes viruses
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
US6489308B1 (en) 1999-03-05 2002-12-03 Trustees Of University Of Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric-oxide-induced clinical conditions
TW482763B (en) 1999-03-12 2002-04-11 Ono Pharmaceutical Co 1,3,4-oxadiazole derivatives and a process for preparing 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
US7572788B2 (en) 1999-04-30 2009-08-11 The Regents Of The University Of Michigan Compositions and methods 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
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
EP1398033B1 (en) * 1999-04-30 2009-06-17 The Regents Of The University Of Michigan Use of benzodiazepines for treating autoimmune diseases, inflammations, neoplasies, viral infections and atherosclerosis
US20060025388A1 (en) * 1999-04-30 2006-02-02 Glick Gary D Compositions and methods relating to novel compounds 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
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils 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
US6750342B1 (en) * 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
US6908919B2 (en) * 1999-05-19 2005-06-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6664255B1 (en) * 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6569876B1 (en) 1999-06-17 2003-05-27 John C. Cheronis Method and structure for inhibiting activity of serine elastases
AU6371900A (en) * 1999-07-26 2001-02-13 Du Pont Pharmaceuticals 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
AU2001243598A1 (en) * 2000-03-13 2001-09-24 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
EP1268428A2 (en) * 2000-04-05 2003-01-02 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
DE60108948T2 (de) 2000-04-05 2005-11-03 Pharmacia Corp. Polyzyclisch aryl und heteroaryl substituierte 4-pyronen verwendbar als selektive hemmung von dem koagulationsprozess
US20040171616A9 (en) * 2000-04-17 2004-09-02 South Michael S. Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
AU2001222501A1 (en) * 2000-05-18 2001-11-26 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
JPWO2002026229A1 (ja) * 2000-09-29 2004-02-05 小野薬品工業株式会社 気道粘液分泌抑制剤
US20030212115A1 (en) * 2000-09-29 2003-11-13 Yasushi Hirota Remedies for inflammatory bowel diseases
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
JP2004517074A (ja) 2000-11-20 2004-06-10 ファルマシア・コーポレーション 凝血カスケードを選択的に阻害するのに有用な置換された多環アリールおよびヘテロアリールピリジン類
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
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
ES2333412T3 (es) * 2001-05-25 2010-02-22 Bristol-Myers Squibb Company Derivados de hidantoina como inhibidores de metaloproteinasas de matriz.
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
EP1438292A1 (en) * 2001-10-03 2004-07-21 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
CA2462645A1 (en) * 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
EP1448534A1 (en) * 2001-10-03 2004-08-25 Pharmacia Corporation 6-membered unsaturated heterocyclic compounds useful for selective inhibition ofthe coagulation cascade
US20040082585A1 (en) * 2001-10-03 2004-04-29 Pharmacia Corporation Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
US7884182B2 (en) * 2001-11-14 2011-02-08 Amylin Pharmaceuticals, Inc. Chemical peptide ligation with three or more components
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
US7592463B2 (en) * 2001-12-05 2009-09-22 California Institute Of Technology Enantioselective transformation of α,β-unsaturated ketones using chiral organic catalysts
CA2369540C (en) * 2001-12-31 2013-10-01 Certicom Corp. Method and apparatus for computing a shared secret key
AU2003217304A1 (en) * 2002-02-28 2003-09-16 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
PL2520654T3 (pl) 2003-08-26 2017-08-31 The Regents Of The University Of Colorado, A Body Corporate Inhibitory aktywności proteazy serynowej i ich zastosowanie w sposobach i kompozycjach do leczenia zakażeń bakteryjnych
US7884112B2 (en) 2004-03-08 2011-02-08 Stuart Edward Bradley Pyrrolopyridine-2-carboxylic acid hydrazides
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
JP2008521873A (ja) 2004-12-02 2008-06-26 プロシディオン・リミテッド ピロロピリジン−2−カルボン酸アミド類
WO2006074358A1 (en) * 2005-01-03 2006-07-13 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
EP1893218A4 (en) 2005-06-01 2011-01-12 Univ Michigan NON-SOLVATED BENZODIAZEPINE PREPARATIONS AND METHODS
US20070105844A1 (en) * 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
CA2628193C (en) 2005-11-01 2012-08-14 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
WO2007137080A2 (en) * 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
MX2008015488A (es) 2006-06-09 2009-02-12 Univ Michigan Composiciones y metodos relacionados con compuestos novedosos y objetivos de los mismos.
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
WO2008112553A1 (en) 2007-03-09 2008-09-18 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
EA017249B8 (ru) * 2007-05-10 2013-01-30 Олбани Молекьюлар Рисерч, Инк. Арил- и гетероарилзамещенные тетрагидробензо-1,4-диазепины и их применение для блокирования обратного захвата норэпинефрина, допамина и серотонина
MX2010002732A (es) 2007-09-14 2010-06-02 Univ Michigan Inhibidores de f1f0-atpasa y metodos relacionados.
RU2010122902A (ru) 2007-11-06 2011-12-20 Дзе Риджентс оф дзе Юниверсити оф Мичиган (US) Бензодиапениноновые соединения, применимые в лечении кожных состояний
US20090156509A1 (en) * 2007-12-12 2009-06-18 Accuthera, Inc. Tri-peptide Inhibitors of Serine Elastases
WO2010030891A2 (en) 2008-09-11 2010-03-18 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
WO2011062766A2 (en) 2009-11-17 2011-05-26 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
EP2501387B1 (en) 2009-11-17 2016-07-27 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 (en) 2011-06-24 2020-04-01 The Regents of the University of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
US20130101664A1 (en) 2011-08-18 2013-04-25 Donald W. Kufe Muc1 ligand traps for use in treating cancers
EP2802653A4 (en) 2012-01-10 2015-09-02 Univ Colorado Regents ALPHA-1 ANTITRYPSIN FUSION MOLECULE COMPOSITIONS, METHODS AND USES THEREOF
BR112015028075A2 (pt) 2013-05-08 2017-07-25 Kissei Pharmaceutical derivado de glicinamida alfa-substituída
CA3154761A1 (en) 2019-09-17 2021-03-25 Mereo Biopharma 4 Limited Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
US20230190723A1 (en) 2020-04-16 2023-06-22 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
CA3234399A1 (en) 2021-10-20 2023-04-27 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

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 (en) * 1988-12-27 1992-05-06 American Cyanamid Company Renin inhibitors
CA2056453A1 (en) * 1990-03-30 1991-10-01 Koji Kobayashi 4h-3, 1-benzoxazin-4-one derivative
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
EP0763055B1 (en) * 1994-06-02 1999-11-03 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
ES2145936T3 (es) 2000-07-16
US5874585A (en) 1999-02-23
US5801148A (en) 1998-09-01
US6037325A (en) 2000-03-14
ZA959819B (en) 1996-05-30
PT793674E (pt) 2000-11-30
CA2205198A1 (en) 1996-05-30
US5618792A (en) 1997-04-08
DE69517196T2 (de) 2001-02-01
EP0793674A1 (en) 1997-09-10
US5807829A (en) 1998-09-15
EP0793674B1 (en) 2000-05-24
WO1996016080A1 (en) 1996-05-30
CN1170414A (zh) 1998-01-14
AU687285B2 (en) 1998-02-19
KR100369665B1 (ko) 2003-04-11
IL116078A0 (en) 1996-01-31
CA2205198C (en) 2002-06-04
US5861380A (en) 1999-01-19
US5869455A (en) 1999-02-09
US5891852A (en) 1999-04-06
AU4164696A (en) 1996-06-17
DE69517196D1 (de) 2000-06-29
TW474924B (en) 2002-02-01
ATE193304T1 (de) 2000-06-15
JPH10511933A (ja) 1998-11-17
GR3034208T3 (en) 2000-11-30
IL116078A (en) 1999-12-31

Similar Documents

Publication Publication Date Title
DK0793674T3 (da) Inhibitorer af human neutrofil elastase
TR199901191T2 (xx) Benzamidoaldehitlerin sistein proteaz� inhibit�r� olarak kullan�m�.
WO1998024806A3 (en) Substituted oxadiazole, thiadiazole and triazole serine protease inhibitors
MY122696A (en) Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases.
DK0587799T3 (da) Inhibitorer af cathepsin G og elastase til forebyggelse af bindevævsnedbrydning
TR199800773T2 (xx) Trombin inhibit�rleri.
BG104885A (en) Novel heterocyclically substituted amides with cysteine protease-inhibiting effect
MXPA03006224A (es) Inhibidores de cruzipaina y otras proteasas de cisteina.
AP2000001761A0 (en) Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase.
ATE246708T1 (de) Elatase-inhibitoren
EE200000137A (et) Pürrolopürrolooni derivaadid neutrofiili elastaasi inhibiitoritena
DK0666755T3 (da) Inhibering af HIV-infektion
BR9611904A (pt) Dioxidos de ditiazol
CA2109516A1 (en) Inhibitors of cathepsin g and elastase for preventing connective tissue degradation
DK1194158T3 (da) Anvendelse af UK 114-proteiner til hæmning af organtransplantatafstödning
IT1305242B1 (it) Preparatore di mazzi di pelli.
BR9713684A (pt) Inibidores de serina protease
KR970052165U (ko) 압축기의 방진메스