ES2145936T3 - Inhibidores de elastasa neutrofila humana. - Google Patents

Inhibidores de elastasa neutrofila humana.

Info

Publication number
ES2145936T3
ES2145936T3 ES95940031T ES95940031T ES2145936T3 ES 2145936 T3 ES2145936 T3 ES 2145936T3 ES 95940031 T ES95940031 T ES 95940031T ES 95940031 T ES95940031 T ES 95940031T ES 2145936 T3 ES2145936 T3 ES 2145936T3
Authority
ES
Spain
Prior art keywords
human
neutrophila
elastase inhibitors
elastase
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES95940031T
Other languages
English (en)
Inventor
Albert Gyorkos
Lyle W Spruce
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cortech Inc
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 ES2145936T3 publication Critical patent/ES2145936T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Peptides Or Proteins (AREA)

Abstract

LA PRESENTE INVENCION, SE REFIERE A CIERTOS PEPTOIDES DE OXADIAZOL, TIADIAZOL Y TRIAZOL SUSTITUIDOS, QUE SON UTILES COMO INHIBIDORES DE SERINA PROTEASAS, INCLUYENDO LA ELASTASA DE NEUTROFILOS HUMANOS, CONOCIDA TAMBIEN COMO ELASTASA DE LEUCOCITOS HUMANOS.
ES95940031T 1994-11-21 1995-11-17 Inhibidores de elastasa neutrofila humana. Expired - Lifetime ES2145936T3 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ES2145936T3 true ES2145936T3 (es) 2000-07-16

Family

ID=23356635

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95940031T Expired - Lifetime ES2145936T3 (es) 1994-11-21 1995-11-17 Inhibidores de elastasa neutrofila humana.

Country Status (17)

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

Families Citing this family (125)

* 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
US6159938A (en) * 1994-11-21 2000-12-12 Cortech, Inc. Serine protease inhibitors comprising α-keto heterocycles
US6001814A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors
US20020119985A1 (en) 1994-11-21 2002-08-29 Albert Gyorkos Serine protease inhibitors
US6100238A (en) * 1994-11-21 2000-08-08 Cortech Inc. Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as 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
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
US6001811A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors--N-substituted derivatives
CZ238197A3 (en) * 1995-01-27 1997-12-17 Novo Nordisk As Growth hormone formation stimulating compounds
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
AU734615B2 (en) * 1996-12-06 2001-06-21 Cortech, Inc. Serine protease inhibitors
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
CA2304482A1 (en) * 1997-09-26 1999-04-08 Eli Lilly And Company Method for the treatment of cystic fibrosis
EP1032410A1 (en) * 1997-10-23 2000-09-06 Southern Research Institute Activating c1?- secretion
US6656910B2 (en) 1997-12-04 2003-12-02 Cortech, Inc. Serine protease inhibitors
WO1999043352A1 (en) * 1998-02-24 1999-09-02 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
NZ507696A (en) * 1998-04-23 2003-10-31 Cortech Inc Triazole, oxadiazole and thiadiazole derivatives useful as cysteine protease inhibitors
EP1114822A3 (en) * 1998-06-03 2002-11-13 Cortech Inc. Indoles and tetrahydroisoquinolines containing alpha-keto oxadiazoles as serine protease inhibitors
KR20010078725A (ko) * 1998-06-03 2001-08-21 존 더블류. 갈루치 2세 세린 프로테아제 저해제로서의 펩토이드 및 비펩토이드를함유하는 알파-케토 옥사디아졸
JP2004517028A (ja) * 1998-06-03 2004-06-10 コーテック インコーポレーテッド セリンプロテアーゼ阻害剤としてのα−ケトオキサジアゾール類含有インドールおよびテトラヒドロイソキノリン
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
JP2002531464A (ja) 1998-12-02 2002-09-24 メルク フロスト カナダ アンド カンパニー カスパーゼ−3阻害薬としてのγ−ケト酸テトラペプチド類
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
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
WO2000055145A1 (en) 1999-03-12 2000-09-21 Ono Pharmaceutical Co., Ltd. 1,3,4-oxadiazole derivatives and process for producing the same
US7144880B2 (en) 1999-04-30 2006-12-05 Regents Of The University Of Michigan Compositions 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
ATE433752T1 (de) 1999-04-30 2009-07-15 Univ Michigan Verwendung von benzodiazepinen zur behandlung von autoimmunischen krankheiten, entzündungen, neoplasien, viralen infektionen und atherosklerosis
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
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
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
US6664255B1 (en) * 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones 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
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6458952B1 (en) * 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils 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
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
JP2003502442A (ja) * 1999-06-17 2003-01-21 ソース・プリシジョン・メディシン・インク セリンエラスターゼの活性を阻害する方法及び化合物
EP1206449A1 (en) * 1999-07-26 2002-05-22 Bristol-Myers Squibb 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
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
WO2001077079A2 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
CA2405561A1 (en) * 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
JP2004501077A (ja) * 2000-04-17 2004-01-15 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換1,4−キノン
AU2001222501A1 (en) * 2000-05-18 2001-11-26 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
EP1301490A2 (en) * 2000-07-18 2003-04-16 Neurogen Corporation 5-substituted 2-aryl-4-pyrimidinones
US20030212115A1 (en) * 2000-09-29 2003-11-13 Yasushi Hirota Remedies for inflammatory bowel diseases
CA2423945A1 (en) * 2000-09-29 2003-03-27 Atsushi Nagai Restrainers of airway mucus secretion
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
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
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
WO2002062797A2 (en) * 2000-12-29 2002-08-15 Celltech R & 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
JP2004535411A (ja) * 2001-05-25 2004-11-25 ブリストルーマイヤーズ スクイブ カンパニー マトリックスメタロプロテナーゼ及び/またはTNF−α転換酵素(TACE)の阻害剤としてのヒダントイン及び関連複素環化合物
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
US20040082585A1 (en) * 2001-10-03 2004-04-29 Pharmacia Corporation Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
CA2462647A1 (en) * 2001-10-03 2003-04-10 Michael S. South 6-membered unsaturated 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
BR0213092A (pt) * 2001-10-03 2004-10-19 Pharmacia Corp Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação
WO2003042235A2 (en) * 2001-11-14 2003-05-22 Geneprot, Inc. Extended native chemical ligation of three or more peptide fragments
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
EP1461320B1 (en) * 2001-12-05 2008-04-09 California Institute Of Technology Enantioselective transformation of alfa,beta-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
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
ES2353309T3 (es) 2004-03-08 2011-03-01 Prosidion Ltd. Hidrazidas del ácido pirrolopiridin-2-carboxílico como inhibidores de glucógeno fosforilasa.
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
WO2007053193A2 (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
NZ568254A (en) 2005-11-01 2011-06-30 Univ Michigan 1,4-Benzodiazepine-2,5-diones for regulating cell death and treating autoimmune diseases
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
US7951823B2 (en) * 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors
EP2418206A3 (en) 2006-06-09 2012-06-27 The Regents of the University of Michigan Benzodiazepine derivatives useful in the treatment of autoimmune disorders
EP2117541A1 (en) * 2007-02-09 2009-11-18 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
KR20090108131A (ko) 2007-02-09 2009-10-14 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
CA2680017C (en) 2007-03-09 2013-11-12 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
CA2685860A1 (en) * 2007-05-10 2008-11-20 Amr Technology, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
CN101855203B (zh) 2007-09-14 2014-03-19 密执安州立大学董事会 F1f0-atp合成酶抑制剂以及相关的方法
UA99839C2 (ru) 2007-11-06 2012-10-10 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Бензодиазепиноновые соединения, применяемые при лечении кожных состояний
US20090156509A1 (en) * 2007-12-12 2009-06-18 Accuthera, Inc. Tri-peptide Inhibitors of Serine Elastases
EP2352724B1 (en) 2008-09-11 2015-04-22 The Regents of the University of Michigan Aryl guanidine f1f0-atpase inhibitors and their medical use
US8604023B2 (en) 2009-04-17 2013-12-10 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
WO2011035124A1 (en) 2009-09-18 2011-03-24 The Regents Of The University Of Michigan Benzodiazepinone compounds and methods of treatment using same
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
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
SG181797A1 (en) * 2009-12-18 2012-07-30 Idenix Pharmaceuticals Inc 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors
KR20200044138A (ko) 2011-06-24 2020-04-28 더 리젠츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코포레이트 알파-1 안티트립신 융합 분자용 조성물, 방법 및 용도
US20130101664A1 (en) 2011-08-18 2013-04-25 Donald W. Kufe Muc1 ligand traps for use in treating cancers
JP2015504675A (ja) 2012-01-10 2015-02-16 ザ リージェンツ オブ ザ ユニバーシティ オブ コロラド,ア ボディー コーポレイトTHE REGENTS OF THE UNIVERSITY OF COLORADO,a body corporate アルファ−1アンチトリプシン融合分子の組成物、方法、及び使用
CN105263901B (zh) 2013-05-08 2017-06-23 橘生药品工业株式会社 α‑取代甘氨酰胺衍生物
WO2021053058A1 (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
LT4106757T (lt) 2020-04-16 2023-11-10 Mereo Biopharma 4 Limited Neutrofilų elastazės inhibitoriaus alvelestato panaudojimas kvėpavimo sistemos ligų, nulemtų alfa-1 antitripsino nepakankamumo, gydymui
JP2024540952A (ja) 2021-10-20 2024-11-06 メレオ バイオファーマ 4 リミテッド 線維化の治療における使用のための好中球エラスターゼ阻害剤
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 (en) * 1988-12-27 1992-05-06 American Cyanamid Company Renin inhibitors
US5204462A (en) * 1990-03-30 1993-04-20 Japan Tobacco, Inc. 4h-3,1-benzoxazin-4-one derivative
GB9216272D0 (en) * 1991-08-15 1992-09-09 Ici Plc Substituted heterocycles
AU655831B2 (en) * 1991-08-22 1995-01-12 Merrell Pharmaceuticals Inc. 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
DK0763055T3 (da) * 1994-06-02 2000-05-08 Merrell Pharma Inc Perflouralkylketon-inhibitorer af elastase og fremgangsmåde til fremstilling deraf
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
EP0793674B1 (en) 2000-05-24
AU687285B2 (en) 1998-02-19
US5874585A (en) 1999-02-23
PT793674E (pt) 2000-11-30
US5807829A (en) 1998-09-15
DE69517196D1 (de) 2000-06-29
DE69517196T2 (de) 2001-02-01
KR100369665B1 (ko) 2003-04-11
IL116078A0 (en) 1996-01-31
JPH10511933A (ja) 1998-11-17
WO1996016080A1 (en) 1996-05-30
US5618792A (en) 1997-04-08
CA2205198C (en) 2002-06-04
CN1170414A (zh) 1998-01-14
TW474924B (en) 2002-02-01
CA2205198A1 (en) 1996-05-30
AU4164696A (en) 1996-06-17
GR3034208T3 (en) 2000-11-30
US6037325A (en) 2000-03-14
ATE193304T1 (de) 2000-06-15
IL116078A (en) 1999-12-31
DK0793674T3 (da) 2000-08-14
US5801148A (en) 1998-09-01
US5869455A (en) 1999-02-09
EP0793674A1 (en) 1997-09-10
ZA959819B (en) 1996-05-30
US5891852A (en) 1999-04-06
US5861380A (en) 1999-01-19

Similar Documents

Publication Publication Date Title
DK0793674T3 (da) Inhibitorer af human neutrofil elastase
HN1997000012A (es) Derivados de triazol utiles en terapia.
HN1997000126A (es) Derivados de indazol
HN1997000099A (es) Inhibidores de metaloproteasas matriciales basados en
HN1998000132A (es) Combinaciones terapeuticas
HN1999000155A (es) 4-carboxiamino-2-metil-1,2,3,4-tetrahidroquinolinas
HN1999000154A (es) 1,2,3,4 tetrahidroquinolinas 2 sustituidas 4 - carboxiamino sustituidas.
HN1998000124A (es) Terapia de combinacion
HN1998000086A (es) Derivados de 9 - desofo - 9 aza - 9a - homoeritromicina a - c - 4 sustituidos.
HN1999000125A (es) Nuevos derivados sustituidos del pirazol
HN1997000097A (es) Piridinas condensadas con heterociclicos
TR200103270T2 (tr) Serin proteas inhibitörleri
HN1998003689A (es) Azetidinas
IS5590A (is) Bensoxasínón/bensóþíasínón notuð sem serínprótínkljúfatálmar
DE59910457D1 (de) Isomalt als wirkstoff enthaltendes erkältungsmittel
ES2150660T3 (es) Bata quirurgica.
ATA144997A (de) Gewebekleber
HN1997000094A (es) Variante de apratinina con propiedades mejoradas
NO975534D0 (no) Imidazo-£1,5|-pyridin-avledete serinproteaseinhibitorer
BR9713684A (pt) Inibidores de serina protease
HN1999000038A (es) Nuevos compuestos fungicidas
IT1305242B1 (it) Preparatore di mazzi di pelli.
ES2185042T3 (es) Inhibidores de la trombina.
NO954451D0 (no) Undertöy, samt innleggsåle
HN1997000100A (es) Pirazoles parasiticidas

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 793674

Country of ref document: ES