IP Library Granted Patent US 8,211,903
Granted Patent B2
US 8,211,903 · App. 12/968,950 · Granted Jul 3, 2012

Substituted pyrimido isoquinoline derivatives

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,211,903
App. No.
12/968,950
Granted
Jul 3, 2012
Kind
B2
Abstract

Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.

Claims (32)

1. A compound of formula (I):

wherein:

R1 represents a 4-pyridine ring or a 4-pyrimidine ring;

R2 represents a hydrogen atom;

R3 represents a hydrogen atom;

R4 represents a hydrogen atom or a halogen atom;

R7, R8, R9, R10 represent independently from each other a hydrogen atom, a halogen atom, a C 1-6 alkoxy group, a nitro, a hydroxyl or an amino; and

represents a single or a double bond, wherein when represents a single bond then there are hydrogen atoms attached to the carbon atoms adjacent to R3 and R4;

or an acid addition salt thereof.

2. The compound according to claim 1 of formula (I):

wherein:

R1 represents a 4-pyridine ring or a 4-pyrimidine ring;

R2 represents a hydrogen atom;

R3 represents a hydrogen atom;

R4 represents a hydrogen atom;

R7, R8, R9, R10 represent independently from each other a hydrogen atom, a halogen atom, a C 1-6 alkoxy group, a nitro, a hydroxyl or an amino; and

represents a single or a double bond, wherein when represents a single bond then there are hydrogen atoms attached to the carbon atoms adjacent to R3 and R4;

or an acid addition salt thereof.

3. The compound according to claim 1 selected from the group consisting of:

2-Pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

10-Bromo-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

10-Methoxy-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

8-Nitro-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

8-Amino-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

10-Hydroxy-2-pyridin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

10-Methoxy-2-pyrimidin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;

2-Pyridin-4-yl-6,7-dihydro-pyrimido[2,1-a]isoquinolin-4-one; and

9,10-Dimethoxy-2-pyridin-4-yl-6,7-dihydro-pyrimido[2,1-a]isoquinolin-4-one;

or an acid addition salt thereof.

4. A pharmaceutical composition comprising a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt thereof and one or more pharmaceutical additives.

5. A pharmaceutical composition comprising a compound of formula (I) according to claim 2 or a pharmaceutically acceptable salt thereof and one or more pharmaceutical additives.

6. A pharmaceutical composition comprising a compound according to claim 3 or a pharmaceutically acceptable salt thereof and one or more pharmaceutical additives.

Assignments (1)
CHANGE OF NAME Recorded Jun 20, 2012
From: SANOFI-AVENTIS
To: SANOFI
Reel/Frame 028413/0927 →