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TR200103270T2 - Serin proteas inhibitörleri - Google Patents

Serin proteas inhibitörleri

Info

Publication number
TR200103270T2
TR200103270T2 TR2001/03270T TR200103270T TR200103270T2 TR 200103270 T2 TR200103270 T2 TR 200103270T2 TR 2001/03270 T TR2001/03270 T TR 2001/03270T TR 200103270 T TR200103270 T TR 200103270T TR 200103270 T2 TR200103270 T2 TR 200103270T2
Authority
TR
Turkey
Prior art keywords
serine
inhibitors
proteas inhibitors
serine proteas
thiadisole
Prior art date
Application number
TR2001/03270T
Other languages
English (en)
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 US08/760,916 external-priority patent/US5861380A/en
Priority claimed from US08/985,056 external-priority patent/US5998379A/en
Priority claimed from US08/985,201 external-priority patent/US6150334A/en
Priority claimed from US08/984,884 external-priority patent/US6001811A/en
Priority claimed from US08/984,881 external-priority patent/US6015791A/en
Application filed by Cortech, Inc., Gyorkos Albert, Lyle Spruce W. filed Critical Cortech, Inc.
Publication of TR200103270T2 publication Critical patent/TR200103270T2/tr

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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)
  • 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

Mevcut bulus: serin proteas inhibitörleri için faydali olan sübstitüsyonlu okzadiazol, tiyadizol triazol peptoidleri ile igilidir.
TR2001/03270T 1996-12-06 1997-12-05 Serin proteas inhibitörleri TR200103270T2 (tr)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US08/760,916 US5861380A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-keto and di-keto containing ring systems
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
US08/761,313 US5869455A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-N-substituted derivatives
US08/771,317 US5801148A (en) 1994-11-21 1996-12-06 Serine protease inhibitors-proline analogs
US98529897A 1997-12-04 1997-12-04
US08/985,056 US5998379A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-proline analogs
US08/985,201 US6150334A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-tripeptoid analogs
US08/984,884 US6001811A (en) 1994-11-21 1997-12-04 Serine protease inhibitors--N-substituted derivatives
US08/984,881 US6015791A (en) 1994-11-21 1997-12-04 Serine protease inhibitors-cycloheptane derivatives

Publications (1)

Publication Number Publication Date
TR200103270T2 true TR200103270T2 (tr) 2003-03-21

Family

ID=27581319

Family Applications (2)

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

Family Applications After (1)

Application Number Title Priority Date Filing Date
TR1999/01681T TR199901681T2 (tr) 1996-12-06 1997-12-05 Serin proteas inhibitörleri.

Country Status (11)

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

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
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
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
AU3511500A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
US7704958B1 (en) 1999-03-05 2010-04-27 Bio Holding, Inc. Methods and compositions for inhibiting apoptosis using serine protease inhibitors
RU2001124908A (ru) * 1999-03-12 2004-02-27 Оно Фармасьютикал Ко. Лтд. (Jp) Производные 1,3,4-оксадиазола и способ их получения
US6569876B1 (en) 1999-06-17 2003-05-27 John C. Cheronis Method and structure 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
EP1219608A4 (en) * 1999-09-27 2003-01-08 Ono Pharmaceutical Co PYRIMID DERIVATIVES, METHOD FOR PRODUCING THE DERIVATIVES AND MEDICINES CONTAINING IT AS THE ACTIVE COMPONENT
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
AU1556601A (en) * 1999-12-03 2001-06-12 Ono Pharmaceutical Co. Ltd. 1,3,4-oxadiazolin-2-one derivatives and drugs containing these derivatives as the active ingredient
WO2001057004A1 (fr) * 2000-02-03 2001-08-09 Ono Pharmaceutical Co., Ltd. Derives de 1,3,4-oxadiazole et leur procede de production
KR20020072302A (ko) * 2000-02-03 2002-09-14 오노 야꾸힝 고교 가부시키가이샤 1,3,4-옥사디아졸 유도체 및 그 제조 방법
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
CA2421499A1 (en) * 2000-09-08 2003-03-06 Ono Pharmaceutical Co., Ltd. Novel crystals of 1,3,4-oxadiazole derivative, process for producing the same and pharmaceutical agent containing the same as active ingredient
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
CN100402549C (zh) * 2001-07-11 2008-07-16 沃泰克斯药物股份有限公司 桥连二环的丝氨酸蛋白酶抑制剂
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
WO2005019434A2 (en) 2003-08-26 2005-03-03 The Regents Of The University Of Colorado, A Body Corporate Serine protease inhibitors 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
CN101600428A (zh) 2007-02-09 2009-12-09 Irm责任有限公司 作为通道活化蛋白酶抑制剂的化合物和组合物
ATE518840T1 (de) 2007-05-22 2011-08-15 Boehringer Ingelheim Int Benzimidazolonchymasehemmer
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
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
CA2911037A1 (en) * 2013-05-08 2014-11-13 Hideaki Hirasawa .alpha.-substituted glycinamide derivative
WO2016020836A1 (en) * 2014-08-06 2016-02-11 Novartis Ag Quinolone derivatives as antibacterials

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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.
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
RU2217436C2 (ru) 2003-11-27
AU734615B2 (en) 2001-06-21
NO992734D0 (no) 1999-06-04
NZ336046A (en) 2000-10-27
EP0954526A2 (en) 1999-11-10
WO1998024806A3 (en) 1998-10-15
TR199901681T2 (tr) 2000-03-21
CN1247542A (zh) 2000-03-15
JP3220169B2 (ja) 2001-10-22
JP2001507679A (ja) 2001-06-12
WO1998024806B1 (en) 1999-05-20
HUP0100669A3 (en) 2001-12-28
CA2272548A1 (en) 1998-06-11
AU5589498A (en) 1998-06-29
WO1998024806A2 (en) 1998-06-11
HUP0100669A2 (hu) 2001-08-28
NO992734L (no) 1999-08-02

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