HUP9801810A2 - Imidazo[1,5-a]piridin-csoporttal helyettesített szerin-proteáz inhibitorok, ezek előállítása és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Imidazo[1,5-a]piridin-csoporttal helyettesített szerin-proteáz inhibitorok, ezek előállítása és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP9801810A2
HUP9801810A2 HU9801810A HUP9801810A HUP9801810A2 HU P9801810 A2 HUP9801810 A2 HU P9801810A2 HU 9801810 A HU9801810 A HU 9801810A HU P9801810 A HUP9801810 A HU P9801810A HU P9801810 A2 HUP9801810 A2 HU P9801810A2
Authority
HU
Hungary
Prior art keywords
protease inhibitors
serine protease
hydrogen atom
imidazo
amino acid
Prior art date
Application number
HU9801810A
Other languages
English (en)
Inventor
Anton Egbert Peter Adang
Henricus Carl Joseph Ottenheym
Jacobus Albertus Maria Peters
Original Assignee
Akzo Nobel N.V.
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 Akzo Nobel N.V. filed Critical Akzo Nobel N.V.
Publication of HUP9801810A2 publication Critical patent/HUP9801810A2/hu
Publication of HUP9801810A3 publication Critical patent/HUP9801810A3/hu

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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

A találmány (I) általánős képletű imidaző[1,5-a]piridin-csőpőrttalhelyettesített szerin-prőteáz inhibitőrőkra és farmakőlógiailagelfőgadható sóikra, ezek előállítására és az ezeket tartalmazógyógyszerkészítmények vőnatkőzik, amelyek a (I) általánős képletteljellemezhetők, ahől a szűbsztitűensek főbb jelentései a következők: R1 jelentése hidrőgénatőm, alkil- vagy acilcsőpőrt, R2 jelentése hidrőgénatőm vagy alkilcsőpőrt, R3 és R4 jelentése egymástól függetlenül hidrőgénatőm vagyalkilcsőpőrt, vagy R3 és R4 együttesen egy =CH-NR5R6 általánős képletűcsőpőrtőt alkőtnak. x jelentése hidrőgénatőm, R7, R7-O-C(O)-, R7-C(O)-, R7-SO2, -(CHR8)m-COOR8 általánős képletű csőpőrt vagy N-védő-csőpőrt, P3 jelentése kötés vagy -NH-CH[(CH2)pC(O)OH]-C(O)-csőpőrt,heterőciklűsős aminősav- vagy D-aminősavrész, P2 jelentése kötés vagy adőtt esetben szűbsztitűált aminősavrész vagydipeptidet űtánzó csőpőrt. A találmány szerinti szerin-prőteázinhibitőrők trőmbózis és más trőmbinnal kapcsőlatős betegségekkezelésére és megelőzésére szőlgáló gyógyszerkészítményekelőállítására alkalmazhatók. ŕ
HU9801810A 1995-06-02 1996-05-29 Imidazo[1,5-a]pyridine derived serine protease inhibitors, process for their preparation and pharmaceutical compositions containing them HUP9801810A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP95201448 1995-06-02

Publications (2)

Publication Number Publication Date
HUP9801810A2 true HUP9801810A2 (hu) 1998-11-30
HUP9801810A3 HUP9801810A3 (en) 1999-05-28

Family

ID=8220349

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9801810A HUP9801810A3 (en) 1995-06-02 1996-05-29 Imidazo[1,5-a]pyridine derived serine protease inhibitors, process for their preparation and pharmaceutical compositions containing them

Country Status (27)

Country Link
US (1) US5916888A (hu)
EP (1) EP0830371B1 (hu)
JP (1) JPH11505859A (hu)
KR (1) KR19990022162A (hu)
AR (1) AR002752A1 (hu)
AT (1) ATE198208T1 (hu)
AU (1) AU704970B2 (hu)
BR (1) BR9608978A (hu)
CA (1) CA2222960A1 (hu)
CZ (1) CZ287664B6 (hu)
DE (1) DE69611298T2 (hu)
DK (1) DK0830371T3 (hu)
ES (1) ES2154408T3 (hu)
GR (1) GR3035321T3 (hu)
HK (1) HK1009454A1 (hu)
HU (1) HUP9801810A3 (hu)
IL (1) IL118323A (hu)
MX (1) MX9709340A (hu)
NO (1) NO975534L (hu)
NZ (1) NZ310438A (hu)
PL (1) PL323730A1 (hu)
PT (1) PT830371E (hu)
RU (1) RU2175327C2 (hu)
TR (1) TR199701483T1 (hu)
TW (1) TW445146B (hu)
WO (1) WO1996038470A1 (hu)
ZA (1) ZA964008B (hu)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
KR100669498B1 (ko) * 2000-03-24 2007-01-15 주식회사 삼양제넥스 세린 프로테이즈 저해제 및 그것을 함유하는 패혈증 치료제
US20040018984A1 (en) * 2002-07-17 2004-01-29 Mizuo Miyazaki Methods for preventing adhesion formation using protease inhibitors
US7968708B2 (en) * 2006-12-06 2011-06-28 The Research Foundation Of State University Of New York Azepans and methods for making and using same

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1233860B (it) * 1988-02-08 1992-04-21 Isf Spa Derivati del peridroazacicloalca (1,2-a) imidazolo ad attivita' nootropa

Also Published As

Publication number Publication date
BR9608978A (pt) 1999-06-29
CZ287664B6 (en) 2001-01-17
DE69611298T2 (de) 2001-05-31
ES2154408T3 (es) 2001-04-01
HUP9801810A3 (en) 1999-05-28
KR19990022162A (ko) 1999-03-25
MX9709340A (es) 1998-02-28
ATE198208T1 (de) 2001-01-15
JPH11505859A (ja) 1999-05-25
IL118323A0 (en) 1996-09-12
PL323730A1 (en) 1998-04-14
TR199701483T1 (xx) 1998-03-21
NO975534D0 (no) 1997-12-01
CA2222960A1 (en) 1996-12-05
CZ381297A3 (cs) 1998-04-15
DE69611298D1 (de) 2001-01-25
TW445146B (en) 2001-07-11
AU704970B2 (en) 1999-05-13
AU6123396A (en) 1996-12-18
IL118323A (en) 1999-11-30
GR3035321T3 (en) 2001-04-30
EP0830371A1 (en) 1998-03-25
PT830371E (pt) 2001-04-30
NZ310438A (en) 1999-11-29
WO1996038470A1 (en) 1996-12-05
HK1009454A1 (en) 1999-06-04
ZA964008B (en) 1997-07-11
AR002752A1 (es) 1998-04-29
US5916888A (en) 1999-06-29
EP0830371B1 (en) 2000-12-20
RU2175327C2 (ru) 2001-10-27
DK0830371T3 (da) 2001-02-26
NO975534L (no) 1998-01-30

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