IP Library Granted Patent US 7,576,241
Granted Patent B2
US 7,576,241 · App. 11/250,783 · Granted Aug 18, 2009

Derivatives of amidines, their preparation, their use as medicaments and the pharmaceutical compositions containing them

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Quick Facts
Patent No.
US 7,576,241
App. No.
11/250,783
Granted
Aug 18, 2009
Kind
B2
Abstract

A compound of the formula wherein the substituents are defined as in the specification useful as intermediates.

Claims (26)

1. A compound of the formula

wherein

A is

in which R 18 , and R 19 and R 20 are, independently, selected from the group consisting of hydrogen, —OH or alkoxy of 1 to 6 carbon atoms;

R 21 and R 22 are, independently, alkyl of 1 to 6 carbon atoms;

X is —(CH 2 ) m —;

Y is a bond or —(CH 2 ) n —;

Φ is a bond or —(CH 2 ) p —NR 37 —(CH 2 ) q —;

Z is —NO 2 ;

R 39 is hydrogen;

R 37 is alkyl of 1 to 6 carbon atoms;

m and n are integers from 0 to 6, p is 1 and q is 2.

2. A compound of claim 1 wherein

R 18 , R 19 and R 20 are, independently, hydrogen, —OH group or methoxy;

R 21 and R 22 are methyl;

Φ is —(CH 2 ) p —NR 37 —(CH 2 ) q — with R 37 being methyl; and

m=0 and n=0.

3. A compound of claim 1 obtained by condensation of an aldehyde of formula

with an amine of the formula

in a reducing medium:

wherein A, R 39 , Y, m and Φ are as defined in claim 1 .

4. A compound of claim 3 wherein

R 18 is hydrogen, R 19 is hydroxyl, R 20 is methoxy;

R 36 is methyl; R 39 is hydrogen; Y is ethyl; m is O and Φ is a bond.

5. A compound of claim 3 wherein the reaction takes place in alcoholic solvent in the presence of a pulverulent 4 Å molecular sieve, activated beforehand, and of a reducing agent.

6. A compound of the formula

Assignments (2)
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY NAME PREVIOUSLY RECORDED AT REEL: 022466 FRAME: 0793. ASSIGNOR(S) HEREBY CONFIRMS THE CHANGE OF NAME. Recorded May 6, 2016
From: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
To: IPSEN PHARMA S.A.S.
Reel/Frame 038628/0931 →
CHANGE OF NAME Recorded Mar 30, 2009
From: SOCIETE DE CONSEILS DE RECHERCHES ET D`APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
To: IPSEN PHARMA S.A.S.
Reel/Frame 022466/0793 →