HUP0100669A2 - Szerin proteázokat gátló peptidszármazékok és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Szerin proteázokat gátló peptidszármazékok és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0100669A2
HUP0100669A2 HU0100669A HUP0100669A HUP0100669A2 HU P0100669 A2 HUP0100669 A2 HU P0100669A2 HU 0100669 A HU0100669 A HU 0100669A HU P0100669 A HUP0100669 A HU P0100669A HU P0100669 A2 HUP0100669 A2 HU P0100669A2
Authority
HU
Hungary
Prior art keywords
serine protease
pharmaceutical compositions
protease inhibitors
peptide derivatives
organic group
Prior art date
Application number
HU0100669A
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
Priority claimed from US08/771,317 external-priority patent/US5801148A/en
Priority claimed from US08/985,056 external-priority patent/US5998379A/en
Priority claimed from US08/984,884 external-priority patent/US6001811A/en
Priority claimed from US08/985,201 external-priority patent/US6150334A/en
Priority claimed from US08/984,881 external-priority patent/US6015791A/en
Application filed by Cortech, Inc. filed Critical Cortech, Inc.
Publication of HUP0100669A2 publication Critical patent/HUP0100669A2/hu
Publication of HUP0100669A3 publication Critical patent/HUP0100669A3/hu

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    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

A találmány az (I) általános képletű vegyületekre vonatkozik, ahol aképletben X jelentése oxigénatom, és Y jelentése nitrogénatom; R1jelentése szerves csoport, R2 és R3 jelentése egymástól függetlenülhidrogénatom vagy szerves csoport, A jelentése kovalens kötés, -C(O)-,-NHC(O)-, -S(O)2-, -NH- -S(O)2-, -OC(O)- vagy -C- képletű csoport, R4jelentése hidrogénatom vagy szerves csoport. A találmány tárgykörébetartozik továbbá egy vagy több fenti vegyületet tartalmazó gyógyászatikészítmény és e vegyületek alkalmazása szerin proteáz gátlásáraszolgáló gyógyászati készítmény előállítására. Ó
HU0100669A 1996-12-06 1997-12-05 Peptide derivatives as serine protease inhibitors, their use and pharmaceutical compositions comprising thereof HUP0100669A3 (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US08/771,317 US5801148A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-proline analogs
US08/761,313 US5869455A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-N-substituted derivatives
US08/760,916 US5861380A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-keto and di-keto containing ring systems
US08/762,381 US5891852A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-cycloheptane derivatives
US08/761,190 US5807829A (en) 1994-11-21 1996-12-06 Serine protease inhibitor--tripeptoid analogs
US98529897A 1997-12-04 1997-12-04
US08/985,056 US5998379A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-proline analogs
US08/984,884 US6001811A (en) 1994-11-21 1997-12-04 Serine protease inhibitors--N-substituted derivatives
US08/985,201 US6150334A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-tripeptoid analogs
US08/984,881 US6015791A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-cycloheptane derivatives
PCT/US1997/021636 WO1998024806A2 (en) 1996-12-06 1997-12-05 Substituted oxadiazole, thiadiazole and triazole serine protease inhibitors

Publications (2)

Publication Number Publication Date
HUP0100669A2 true HUP0100669A2 (hu) 2001-08-28
HUP0100669A3 HUP0100669A3 (en) 2001-12-28

Family

ID=27581319

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100669A HUP0100669A3 (en) 1996-12-06 1997-12-05 Peptide derivatives as serine protease inhibitors, their use and pharmaceutical compositions comprising thereof

Country Status (11)

Country Link
EP (1) EP0954526A2 (hu)
JP (1) JP3220169B2 (hu)
CN (1) CN1247542A (hu)
AU (1) AU734615B2 (hu)
CA (1) CA2272548A1 (hu)
HU (1) HUP0100669A3 (hu)
NO (1) NO992734L (hu)
NZ (1) NZ336046A (hu)
RU (1) RU2217436C2 (hu)
TR (2) TR200103270T2 (hu)
WO (1) WO1998024806A2 (hu)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6004933A (en) * 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
US6656910B2 (en) * 1997-12-04 2003-12-02 Cortech, Inc. Serine protease inhibitors
JP2003535022A (ja) * 1998-06-03 2003-11-25 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アルファー‐ケトオキサジアゾール含有ペプトイド及び非ペプトイド
EP1105412A1 (en) * 1998-08-17 2001-06-13 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
FR2782997A1 (fr) * 1998-09-08 2000-03-10 Hoechst Marion Roussel Inc Nouveaux derives de la benzodiazepinone, procede de preparation et intermediaires de ce procede, application a titre de medicaments et compositions pharmaceutiques les renfermant
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
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
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
AU3719100A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
RU2001124908A (ru) * 1999-03-12 2004-02-27 Оно Фармасьютикал Ко. Лтд. (Jp) Производные 1,3,4-оксадиазола и способ их получения
AU5625900A (en) * 1999-06-17 2001-01-09 Cortech, Inc. Method and compounds for inhibiting activity of serine elastases
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
NZ517962A (en) * 1999-09-27 2003-11-28 Ono Pharmaceutical Co Pyrimidine derivatives, process for preparing the derivatives and drugs containing the same as the active ingredient
US20030087831A1 (en) * 1999-12-03 2003-05-08 Kazuyuki Ohmoto 1,3,4-Oxadiazolin-2-one derivatives and drugs containing these derivatives as the active ingredient
US6797720B2 (en) 1999-12-03 2004-09-28 Ono Pharmaceutical Co., Ltd. 1,3,4-oxadiazoline derivative and an agent comprising its derivative as active ingredient
EP1253144A4 (en) * 2000-02-03 2003-02-12 Ono Pharmaceutical Co 1,3,4-OXADIAZOLE DERIVATIVES AND A METHOD FOR THE PRODUCTION THEREOF
KR20020072302A (ko) * 2000-02-03 2002-09-14 오노 야꾸힝 고교 가부시키가이샤 1,3,4-옥사디아졸 유도체 및 그 제조 방법
WO2002014310A1 (fr) * 2000-08-10 2002-02-21 Ono Pharmaceutical Co., Ltd. 2-[5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidyl]-n-[1-(2-[5-t-butyl-1,3,4-oxadiazolyl]carbonyl)-2-(r,s)-methylpropyl]acetamide chlorhydrate
US20040023998A1 (en) * 2000-09-08 2004-02-05 Tsutomu Kojima Novel crystals of 1,3,4-oxadiazole derivatives, process for producing the crystals and medicines containing the same as the active ingredient
AU2001292305A1 (en) * 2000-09-29 2002-04-08 Ono Pharmaceutical Co. Ltd. Airway mucus secretion inhibitors
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
EP1404704B9 (en) * 2001-07-11 2008-02-20 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
IL148924A (en) * 2002-03-26 2015-06-30 Mor Research Applic Ltd Use of substances that inhibit intracellular elastase activity in the preparation of a drug for the treatment and / or prevention of necrosis of cells and related diseases
EP3192872A1 (en) 2003-08-26 2017-07-19 The Regents of the University of Colorado, a body corporate Inhibitors of serine protease activity and their use in methods and compositions for treatment of bacterial infections
US7358368B2 (en) 2003-11-04 2008-04-15 Ajinomoto Co., Inc. Azlactone compound and method for preparation thereof
AU2007253819B2 (en) 2006-05-23 2011-02-17 Irm Llc Compounds and compositions as channel activating protease inhibitors
TWI389899B (zh) * 2006-08-08 2013-03-21 Msd Oss Bv 具口服活性之凝血酶抑制劑
EP2117537A1 (en) 2007-02-09 2009-11-18 Irm Llc Compounds and compositions as channel activating protease inhibitors
JP5268120B2 (ja) * 2007-05-22 2013-08-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンゾイミダゾロンキマーゼ阻害薬
US9938353B2 (en) 2011-06-24 2018-04-10 The Regents Of The University Of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
CA2896951A1 (en) 2012-01-10 2013-07-18 The Regents Of The University Of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
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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
AU734615B2 (en) 2001-06-21
JP2001507679A (ja) 2001-06-12
WO1998024806A2 (en) 1998-06-11
CA2272548A1 (en) 1998-06-11
RU2217436C2 (ru) 2003-11-27
CN1247542A (zh) 2000-03-15
NO992734D0 (no) 1999-06-04
TR200103270T2 (tr) 2003-03-21
AU5589498A (en) 1998-06-29
NZ336046A (en) 2000-10-27
EP0954526A2 (en) 1999-11-10
HUP0100669A3 (en) 2001-12-28
JP3220169B2 (ja) 2001-10-22
NO992734L (no) 1999-08-02
TR199901681T2 (xx) 2000-03-21
WO1998024806B1 (en) 1999-05-20
WO1998024806A3 (en) 1998-10-15

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