Patent · US Expired

1-amino-7-isoquinoline derivatives as serine protease inhibitors

US6262069A · kind A · utility

13Cited by
5References
28Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 25, 2000
Grant dateJul 17, 2001
Priority date
Expiry dateFeb 25, 2020

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K38/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

##STR1## The invention relates to serine protease inhibitor compounds of fornula (I) where R.sub.1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl amminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycabonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R.sub.2 is hydrogen, halo, methyl amino, hydroxy, or oxo; and R is X--X--Y(R.sub.7)--L--Lp(D)n; wheren each X independently is a C, N, O or S atom or a CO, CR.sub.1, C(R.sub.1).sub.2 or NR.sub.1 group, at least one X being C, CO, CR.sub.1 or a C(R.sub.1).sub.2 group; Y (the .alpha.-atom) is a nitrogen atom or a CR.sub.1 group or Y and L taken together form a cyclic group; R.sub.7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylakenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R.sub.1 ; L is an organic linker group containing 1 to 5 ba…

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.