TR200002527T2 - Sistein aktivitesine bağımlı enzimlerin inhibitörleri olarak kullanılan tiyadiyazol bileşimleri. - Google Patents

Sistein aktivitesine bağımlı enzimlerin inhibitörleri olarak kullanılan tiyadiyazol bileşimleri.

Info

Publication number
TR200002527T2
TR200002527T2 TR2000/02527T TR200002527T TR200002527T2 TR 200002527 T2 TR200002527 T2 TR 200002527T2 TR 2000/02527 T TR2000/02527 T TR 2000/02527T TR 200002527 T TR200002527 T TR 200002527T TR 200002527 T2 TR200002527 T2 TR 200002527T2
Authority
TR
Turkey
Prior art keywords
thiadiazole
inhibitors
cysteine
activity
inhibition
Prior art date
Application number
TR2000/02527T
Other languages
English (en)
Inventor
Karimian Khashayar
F. Tam Tim
C.S.H. Leung-Toung Regis
Li Wanren
Original Assignee
Apotex 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 Apotex Inc. filed Critical Apotex Inc.
Publication of TR200002527T2 publication Critical patent/TR200002527T2/tr

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Sistein aktivitesine bagli enzimlerin, özellikle sistein proteazlarinin etki inhibitörleri olan yeni 1,2,4-thiadiazole bilesimleri saglanmistir. Bilesimler, transglutaminase inhibisyonuyla akne, insan nezle virüsü 3C proteazi inhibisyonuyla nezleyi, katepsinlerin inhibisyonuyla enflamatuar eklem hastaligini tedavide faydalidir. Bu bulus bilesimleri; Z' nin enzim için tanima sekansi olan bir nitrojen içerikli grup ve Y'nin inhibitör aktivitesini sistein aktivitesine bagli enzimin tiyol grubuna dogru ayarlayan bir ikame oldugu genel formül (I)'in 3,5-bi ikameli 1,2,4-thiadazole olur. Y grubu tanimada da kullanilabilir.
TR2000/02527T 1998-03-02 1999-02-23 Sistein aktivitesine bağımlı enzimlerin inhibitörleri olarak kullanılan tiyadiyazol bileşimleri. TR200002527T2 (tr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/033,937 US6162791A (en) 1998-03-02 1998-03-02 Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes

Publications (1)

Publication Number Publication Date
TR200002527T2 true TR200002527T2 (tr) 2001-01-22

Family

ID=21873323

Family Applications (1)

Application Number Title Priority Date Filing Date
TR2000/02527T TR200002527T2 (tr) 1998-03-02 1999-02-23 Sistein aktivitesine bağımlı enzimlerin inhibitörleri olarak kullanılan tiyadiyazol bileşimleri.

Country Status (14)

Country Link
US (1) US6162791A (tr)
EP (1) EP1058690A1 (tr)
JP (1) JP2002505339A (tr)
KR (1) KR20010041406A (tr)
CN (1) CN1291993A (tr)
AU (1) AU741295B2 (tr)
BR (1) BR9908441A (tr)
CA (1) CA2322838A1 (tr)
EA (1) EA200000892A1 (tr)
HU (1) HUP0101899A3 (tr)
IL (1) IL137929A0 (tr)
PL (1) PL342661A1 (tr)
TR (1) TR200002527T2 (tr)
WO (1) WO1999045027A1 (tr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6833369B2 (en) * 1997-06-24 2004-12-21 Janssen Pharmaceutica, Nv Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives
US6468977B1 (en) * 1998-03-02 2002-10-22 Apotex Inc. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes
US6258831B1 (en) 1999-03-31 2001-07-10 The Procter & Gamble Company Viral treatment
US6340696B1 (en) 1999-03-31 2002-01-22 The Procter & Gamble Company Viral treatment
US6245788B1 (en) 1999-03-31 2001-06-12 The Procter & Gamble Company Viral treatment
EP1201136A1 (en) 2000-10-31 2002-05-02 Nederlandse Organisatie voor toegepast-natuurwetenschappelijk Onderzoek TNO Food grade transglutaminase inhibitor and uses thereof
DE10054687A1 (de) * 2000-11-03 2002-05-16 N Zyme Biotec Gmbh Inhibitoren von Transglutaminasen
CA2379375A1 (en) * 2002-03-28 2003-09-28 Apotex Inc. Sulfonamide derivatives of 3-substituted imidazol[1,2-d]-1,2,4-thiadiazoles and 3-substituted-[1,2,4] thiadiazolo[4,5-a] benzimidazole as inhibitors of fibrin cross-linking and transglutaminases
KR101032834B1 (ko) * 2003-10-15 2011-05-06 스미또모 가가꾸 가부시키가이샤 1,2,4-티아디아졸 화합물 및 그를 함유하는 유해 생물 방제조성물
WO2007075297A2 (en) * 2005-12-27 2007-07-05 University Of Toledo Muscarinic agonists and methods of use thereof
US20110294835A1 (en) 2008-05-15 2011-12-01 The Board Of Trustees Of The University Of Illinois Muscarinic Agonists as Cognitive Enhancers
SG185414A1 (en) 2010-05-12 2012-12-28 Univ Vanderbilt Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2012149524A1 (en) 2011-04-29 2012-11-01 The University Of Toledo Muscarinic agonists as enhancers of working memory and cognitive flexibility
MX2022015207A (es) 2020-06-10 2023-02-13 Aligos Therapeutics Inc Compuestos antivirales para tratar infecciones por coronavirus, picornavirus, y norovirus.
EP4366831A1 (en) 2021-07-09 2024-05-15 Aligos Therapeutics, Inc. Anti-viral compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4874864A (en) * 1988-05-24 1989-10-17 Pfizer Inc. Benzamide protease inhibitors
DE3910358A1 (de) * 1989-03-31 1990-10-04 Bayer Ag Thiadiazol-substituierte acrylsaeureester und neue zwischenprodukte
DE4026904A1 (de) * 1990-08-25 1992-02-27 Bayer Ag Verfahren zur herstellung von 3-alkoxy-2-heteroazolyl-amino-acrylsaeureestern
JP2808877B2 (ja) * 1990-09-29 1998-10-08 大正製薬株式会社 エポキシスクシナム酸誘導体およびその中間体
DE4142191A1 (de) * 1991-12-20 1993-06-24 Bayer Ag Verfahren zur herstellung von 3-alkoxy-acrylestern
US5498616A (en) * 1994-11-04 1996-03-12 Cephalon, Inc. Cysteine protease and 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
US6004933A (en) * 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors

Also Published As

Publication number Publication date
EA200000892A1 (ru) 2001-02-26
KR20010041406A (ko) 2001-05-15
CN1291993A (zh) 2001-04-18
WO1999045027A1 (en) 1999-09-10
AU741295B2 (en) 2001-11-29
IL137929A0 (en) 2001-10-31
US6162791A (en) 2000-12-19
HUP0101899A3 (en) 2001-12-28
BR9908441A (pt) 2000-10-31
EP1058690A1 (en) 2000-12-13
PL342661A1 (en) 2001-07-02
HUP0101899A2 (hu) 2001-11-28
CA2322838A1 (en) 1999-09-10
JP2002505339A (ja) 2002-02-19
AU2606799A (en) 1999-09-20

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