TR199901681T2 - Serin proteas inhibit�rleri. - Google Patents

Serin proteas inhibit�rleri.

Info

Publication number
TR199901681T2
TR199901681T2 TR1999/01681T TR9901681T TR199901681T2 TR 199901681 T2 TR199901681 T2 TR 199901681T2 TR 1999/01681 T TR1999/01681 T TR 1999/01681T TR 9901681 T TR9901681 T TR 9901681T TR 199901681 T2 TR199901681 T2 TR 199901681T2
Authority
TR
Turkey
Prior art keywords
protease inhibitors
serine protease
serine
thiadiazole
inhibitors
Prior art date
Application number
TR1999/01681T
Other languages
English (en)
Turkish (tr)
Inventor
Gyorkos Albert
Lyle Spruce W.
Original Assignee
Cortech, Inc.
Gyorkos Albert
Lyle Spruce W.
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 US08/984,884 external-priority patent/US6001811A/en
Priority claimed from US08/985,056 external-priority patent/US5998379A/en
Priority claimed from US08/984,881 external-priority patent/US6015791A/en
Priority claimed from US08/985,201 external-priority patent/US6150334A/en
Application filed by Cortech, Inc., Gyorkos Albert, Lyle Spruce W. filed Critical Cortech, Inc.
Publication of TR199901681T2 publication Critical patent/TR199901681T2/xx

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
    • 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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
TR1999/01681T 1996-12-06 1997-12-05 Serin proteas inhibit�rleri. TR199901681T2 (xx)

Applications Claiming Priority (10)

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
US08/761,190 US5807829A (en) 1994-11-21 1996-12-06 Serine protease inhibitor--tripeptoid analogs
US08/762,381 US5891852A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-cycloheptane derivatives
US08/760,916 US5861380A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-keto and di-keto containing ring systems
US98529897A 1997-12-04 1997-12-04
US08/984,884 US6001811A (en) 1994-11-21 1997-12-04 Serine protease inhibitors--N-substituted derivatives
US08/985,056 US5998379A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-proline analogs
US08/984,881 US6015791A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-cycloheptane derivatives
US08/985,201 US6150334A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-tripeptoid analogs

Publications (1)

Publication Number Publication Date
TR199901681T2 true TR199901681T2 (xx) 2000-03-21

Family

ID=27581319

Family Applications (2)

Application Number Title Priority Date Filing Date
TR1999/01681T TR199901681T2 (xx) 1996-12-06 1997-12-05 Serin proteas inhibit�rleri.
TR2001/03270T TR200103270T2 (tr) 1996-12-06 1997-12-05 Serin proteas inhibitörleri

Family Applications After (1)

Application Number Title Priority Date Filing Date
TR2001/03270T TR200103270T2 (tr) 1996-12-06 1997-12-05 Serin proteas inhibitörleri

Country Status (11)

Country Link
EP (1) EP0954526A2 (ja)
JP (1) JP3220169B2 (ja)
CN (1) CN1247542A (ja)
AU (1) AU734615B2 (ja)
CA (1) CA2272548A1 (ja)
HU (1) HUP0100669A3 (ja)
NO (1) NO992734L (ja)
NZ (1) NZ336046A (ja)
RU (1) RU2217436C2 (ja)
TR (2) TR199901681T2 (ja)
WO (1) WO1998024806A2 (ja)

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
EP1089752A4 (en) * 1998-06-03 2002-01-02 Cortech Inc ALPHA-KETO OXADIAZOLE AS A SERINE PROTEASE INHIBITOR
WO2000009542A1 (en) * 1998-08-17 2000-02-24 Cortech, Inc. SERINE PROTEASE INHIBITORS COMPRISING α-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
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
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
WO2000052034A2 (en) * 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
CA2367418A1 (en) * 1999-03-12 2000-09-21 Ono Pharmaceutical Co., Ltd. 1,3,4-oxadiazole derivatives and process for producing the same
AU5625900A (en) 1999-06-17 2001-01-09 Cortech, Inc. Method and compounds for inhibiting activity of serine elastases
WO2001007407A1 (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
CA2385292A1 (en) * 1999-09-27 2001-04-05 Tsutomu Kojima Pyrimidine compounds, processes for the preparation thereof and pharmaceutical compositions comprising the compounds as active ingredient
EP1234834A4 (en) * 1999-12-03 2003-01-29 Ono Pharmaceutical Co 1,3,4-OXADIAZOLINE-2-ONE DERIVATIVES AND MEDICINAL PRODUCTS CONTAINING SUCH DERIVATIVES USEFUL AS 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
KR20020072303A (ko) * 2000-02-03 2002-09-14 오노 야꾸힝 고교 가부시키가이샤 1,3,4-옥사디아졸 유도체 및 그 제조 방법
EP1253143A4 (en) * 2000-02-03 2003-03-26 Ono Pharmaceutical Co 1,3,4-OXADIAZOLE DERIVATIVES AND A METHOD FOR THE PRODUCTION THEREOF
AU2001277736A1 (en) * 2000-08-10 2002-02-25 Ono Pharmaceutical Co. Ltd. 2-(5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidyl)-n-(1-(2-( -t-butyl-1,3,4-oxadiazolyl)carbonyl)-2-(r,s)-methylpropyl) acetamide hydrochloride
EP1318150A4 (en) * 2000-09-08 2004-04-14 Ono Pharmaceutical Co NEW CRYSTALS OF 1,3,4-OXADIAZOLE DERIVATIVES, METHOD FOR THE PRODUCTION OF THE CRYSTALS AND THE MEDICINAL PRODUCTS CONTAINING THEM AS AN ACTIVE SUBSTANCE
CA2423945A1 (en) * 2000-09-29 2003-03-27 Atsushi Nagai Restrainers of airway mucus secretion
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
KR100926244B1 (ko) * 2001-07-11 2009-11-12 버텍스 파마슈티칼스 인코포레이티드 브릿지된 바이사이클릭 세린 프로테아제 억제제
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
CA2536918A1 (en) 2003-08-26 2005-03-03 Leland Shapiro Compositions of, and methods for, alpha-1 antitrypsin fc fusion molecules
EP1533306A1 (en) 2003-11-04 2005-05-25 Ajinomoto Co., Inc. Azlactone compound and method for preparation thereof
RU2419626C2 (ru) 2006-05-23 2011-05-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
TWI389899B (zh) * 2006-08-08 2013-03-21 Msd Oss Bv 具口服活性之凝血酶抑制劑
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
US9150556B2 (en) 2007-05-22 2015-10-06 Boehringer Ingelheim International Gmbh Benzimidazolone chymase inhibitors
AU2012272636A1 (en) 2011-06-24 2013-05-02 Advent Bio Holdings Llc Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
AU2013202648B2 (en) 2012-01-10 2016-05-19 Konkuk University Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
US9458092B2 (en) * 2013-05-08 2016-10-04 Kissei Pharmaceutical Co., Ltd. α-Substituted glycinamide derivative
JP2017523213A (ja) * 2014-08-06 2017-08-17 ノバルティス アーゲー 抗菌薬としてのキノロン誘導体

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9216272D0 (en) * 1991-08-15 1992-09-09 Ici Plc Substituted heterocycles
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.
CA2189526C (en) * 1994-06-02 2001-02-27 William A. Metz, Jr. 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
NO992734D0 (no) 1999-06-04
RU2217436C2 (ru) 2003-11-27
JP3220169B2 (ja) 2001-10-22
EP0954526A2 (en) 1999-11-10
NO992734L (no) 1999-08-02
JP2001507679A (ja) 2001-06-12
NZ336046A (en) 2000-10-27
CN1247542A (zh) 2000-03-15
HUP0100669A3 (en) 2001-12-28
WO1998024806B1 (en) 1999-05-20
CA2272548A1 (en) 1998-06-11
AU5589498A (en) 1998-06-29
WO1998024806A3 (en) 1998-10-15
WO1998024806A2 (en) 1998-06-11
AU734615B2 (en) 2001-06-21
HUP0100669A2 (hu) 2001-08-28
TR200103270T2 (tr) 2003-03-21

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