Phenyl guanidinobenzoate derivatives which have protease inhibit

Details Phenyl guanidinobenzoate derivatives which have protease inhibit Phenyl guanidinobenzoate derivatives which have protease inhibit

1986-07-16

1988-05-24

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

540460, 544121, 544169, 544357, 544360, 544372, 544386, 544387, 544388, 548337, 548341, 564155, 564164, C07D24308, C07D26530

Patent

active

047467371

ABSTRACT:
Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.n --Y in which X represents a single bond, a linear or branched lower alkylene group or an alkenylene group, n is 0 or 1, Y represents a hydrogen atom, a cycloalkyl group, an aryl group, a hydroxyl group, a lower alkoxy group and the like are prepared by reacting para-nitrobenzoic acid or its derivative with a compound of the general formula (III) or its derivative ##STR2## to obtain a compound of the general formula (IV) ##STR3## followed by reducing the compound of the formula (IX) ##STR4## and subjecting the compound (IX) to guanidylation reaction, or by reaction para-guanidinobenzoic derivative with compound (III) or its derivative.
The benzoyl esters have strong anti-trypsin activity, anti-thrombin activity and anticoagulant activity with low toxicity and are useful as a medicine for treatment of pancreatitis and disseminated intravascular coagulation (DIC).

Affiliated with

Also associated with

Rating

Phenyl guanidinobenzoate derivatives which have protease inhibit does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Phenyl guanidinobenzoate derivatives which have protease inhibit, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phenyl guanidinobenzoate derivatives which have protease inhibit will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1059318