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1. WO1996038470 - IMIDAZO[1,5a]PYRIDINE DERIVED SERINE PROTEASE INHIBITORS

Publication Number WO/1996/038470
Publication Date 05.12.1996
International Application No. PCT/EP1996/002298
International Filing Date 29.05.1996
Chapter 2 Demand Filed 07.11.1996
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07K 5/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
02containing at least one abnormal peptide link
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07K 5/0202
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
02containing at least one abnormal peptide link
0202containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of bulk chemicals
55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • AKZO NOBEL N.V. [NL]/[NL] (AllExceptUS)
  • OTTENHEYM, Henricus, Carl, Joseph [NL]/[NL] (UsOnly)
  • ADANG, Anton, Egbert, Peter [NL]/[NL] (UsOnly)
  • PETERS, Jacobus, Albertus, Maria [NL]/[NL] (UsOnly)
Inventors
  • OTTENHEYM, Henricus, Carl, Joseph
  • ADANG, Anton, Egbert, Peter
  • PETERS, Jacobus, Albertus, Maria
Agents
  • HERMANS, Franciscus, G., M.
Priority Data
95201448.402.06.1995EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) IMIDAZO[1,5a]PYRIDINE DERIVED SERINE PROTEASE INHIBITORS
(FR) INHIBITEURS DE SERINE PROTEASE DERIVES DE IMIDAZO[1,5A]PYRIDINE
Abstract
(EN)
The invention relates to an imidazo[1,5a]pyridine derived serine protease inhibitor comprising a unit having general formula (I) wherein R1 is hydrogen, lower alkyl or an acyl group; R2 is hydrogen or lower alkyl; R3 and R4 are independently hydrogen, lower alkyl or together form =CH-NR5R6, R5 and R6 being lower alkyl. The compounds are serine protease inhibitors and can be used for the treatment and prophylaxis of thrombosis and thrombin-associated diseases.
(FR)
Cette invention concerne un inhibiteur de sérine protéase dérivé de imidazo[1,5a]pyridine, lequel inhibiteur comprend une unité correspondant à la formule générale (I) où R1 représente hydrogène, alkyle inférieur ou un groupe acyle; R2 représente hydrogène ou alkyle inférieur; R3 et R4 représentent indépendamment hydrogène, alkyle inférieur ou forment ensemble =CH-NR5R6, R5 et R6 représentant un alkyle inférieur. Ces composés sont des inhibiteurs de sérine protéase et peuvent être utilisés dans le traitement et la prévention de thromboses et de maladies associées à la thrombine.
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