IP Library Granted Patent US 8,455,485
Granted Patent B2
US 8,455,485 · App. 13/120,436 · Granted Jun 4, 2013

Pyrazolo pyridine derivatives as NADPH oxidase inhibitors

Inventors: Patrick Page (Saint-Julien-en-Genevois, FR); Mike Orchard (Oxon, GB); Benoit Laleu (Collonges-Sous-Salève, FR); Francesca Gaggini (Geneva, CH)
Assignee: Genkyotex SA
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Quick Facts
Patent No.
US 8,455,485
App. No.
13/120,436
Granted
Jun 4, 2013
Kind
B2
Abstract

The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

Claims (201)

1. A pyrazolo pyridine compound of Formula (I):

wherein G 1 is selected from H; optionally substituted acyl; optionally substituted acyl C 1 -C 6 alkyl; optionally substituted alkyl; optionally substituted C 3 -C 8 -cycloalkyl alkyl; optionally substituted heterocycloalkyl alkyl; optionally substituted aryl alkyl; and optionally substituted heteroaryl alkyl; G 2 is selected from H; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl; G 3 is selected from —(CH 2 ) n —R 1 and —(CH 2 ) p —R 5 ; R l is selected from —NR 2 R 3 ; -OR 4 ; optionally substituted heterocycloalkyl; optionally substituted heteroaryl; -CHR 6 R 7 ; optionally substituted acyl and -C (O)NR 2 R 3 ; R 2 and R 3 are independently selected from H; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl or NR 2 R 3 form a ring selected from optionally substituted heteroaryl and optionally substituted heterocycloalkyl; R 4 is selected from H; optionally substituted alkoxy C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl; R 5 is selected from H; optionally substituted alkoxy; optionally substituted alkoxy C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl; R 6 and R 7 are independently selected from optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl or -CHR 6 R 7 forms an optionally substituted ring selected from optionally substituted heteroaryl, optionally substituted cycloalkyl and optionally substituted heterocycloalkyl; n is an integer selected from 0 to 5; p is an integer selected from 3 to 5; G 4 is selected from H; optionally substituted acyl; optionally substituted acyl amino; optionally substituted acyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted C 1 -C 6 alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C 1 -C 6 alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl; G 5 is selected from H; optionally substituted C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkynyl; optionally substituted aryl; optionally substituted C 1 -C 6 alkyl aryl; optionally substituted aryl C 1 -C 6 alkyl; optionally substituted heteroaryl; optionally substituted C 1 -C 6 alkyl heteroaryl; optionally substituted heteroaryl C 1 -C 6 alkyl; optionally substituted C 2 -C 6 alkenyl aryl; optionally substituted aryl C 2 -C 6 alkenyl; optionally substituted C 2 -C 6 alkenyl heteroaryl; optionally substituted heteroaryl C 2 -C 6 alkenyl; optionally substituted C 3 -C 8 -cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C 1 -C 6 alkyl C 3 -C 8 -cycloalkyl; optionally substituted C 3 -C 8 -cycloalkyl C 1 -C 6 alkyl; optionally substituted C 1 -C 6 alkyl heterocycloalkyl and optionally substituted heterocycloalkyl C 1 -C 6 alkyl; and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 wherein G 1 is H.

3. The compound of claim 1 wherein G 3 is —(CH 2 ) n —R 1 ; R 1 and n are as described in claim 1 .

4. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; R 1 is —NR 2 R 3 ; R 2 , R 3 and n are as described in claim 1 .

5. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; R 1 is —NR 2 R 3 ; R 3 is aryl C 1 -C 6 alkyl; R 2 and n are as described in claim 1 .

6. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; R 1 is heterocycloalkyl; n is as described in claim 1 .

7. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; R 1 is heteroaryl; n is as described in claim 1 .

8. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; R 1 is —NR 2 R 3 ; R 2 is C 1 -C 6 alkyl; R 3 and n are as described in claim 1 .

9. The compound of claim 1 , wherein G 3 is —(CH 2 ) n —R 1 ; n is 1; R 1 is as described in claim 1 .

10. The compound of claim 1 , wherein G 3 is —(CH 2 ) p —R 5 ; R 5 and p are as described in claim 1 .

11. The compound of claim 1 wherein G 5 is H.

12. The compound of claim 1 selected from the following compounds:

5-benzyl-2-(2-chlorophenyl)-4-(morpholin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-4-butyl-5-(4-chlorobenzyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-4-butyl-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-4-butyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-(furan-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-(3,5-dimethoxybenzyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[benzyl(methyl)amino]methyl}-2-(2-chloro-4-fluorophenyl)-5-(3-methoxy propyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-4-butyl-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-butyl-2-(2-chloro-4-fluorophenyl)-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-4-(methoxymethyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-4-(methoxymethyl)-5-[2-(morpholin-4-ylmethyl)benzyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-benzyl-5-(3-ethoxypropyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-5-methyl-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(4-chlorobenzyl)-2-(3-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-4-(methoxymethyl)-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(4-chlorobenzyl)-4-(methoxymethyl)-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-methyl-4-(3-phenoxypropyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-benzyl-5-(2-methoxyethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-benzyl-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(2-pyridin-2-yl ethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-5-(3,5-dimethoxybenzyl)-4-(methoxymethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-5-(2-pyridin-2-ylethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-5-(2-pyridin-2-ylethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-5-(furan-2-ylmethyl)-4-(methoxymethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-4-(methoxymethyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-benzyl-5-(3,5-dimethoxybenzyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(2-methoxy ethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-5-(pyridin-3-ylmethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-(methoxymethyl)-2-methyl-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-5-(2-methoxyethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-5-(2-methoxyethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chloro-4-fluorophenyl)-5-(3-ethoxypropyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(3-chlorophenyl)-5-(3-ethoxypropyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-benzyl-5-(3-ethoxypropyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-5-(4-chlorobenzyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-5-(4-chlorobenzyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-[4-(benzyloxy)phenyl]-5-methyl-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(4-chlorobenzyl)-2-methyl-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

N-[3-({2-[4-(benzyloxy)phenyl]-3,6-dioxo-4-(pyrrolidin-1-ylmethyl)-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl}methyl)phenyl]acetamide;

N-{3-[(2-[4-(benzyloxy)phenyl]-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)methyl]phenyl}acetamide;

2-(3-chlorophenyl)-5-(3-ethoxypropyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-methyl-4-(phenoxymethyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-fluorophenoxy)methyl]-2-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2,5-dichlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2,5-dichlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(4-chlorobenzyl)-4-[(4-fluorophenoxy)methyl]-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(2-methoxybenzyl)-2-methyl-4-(3-phenoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-fluorophenoxy)methyl]-2-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-fluorophenoxy)methyl]-2-methyl-5-[2-(tetrahydro-2H-pyran-2-yl)ethyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-fluorophenoxy)methyl]-2-methyl-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

5-(3-methoxybenzyl)-2-methyl-4-(3-phenoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-methyl-4-(3-phenoxypropyl)-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-5-(3-methoxybenzyl)-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-5-(3-ethoxypropyl)-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-5-(3-methoxybenzyl)-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-5-(3-ethoxypropyl)-2-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-2-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-methyl-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

N-[3-({4-[(benzyloxy)methyl]-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl}methyl)phenyl]acetamide;

N-[3-({4-[(4-chlorophenoxy)methyl]-2-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl}methyl)phenyl]acetamide;

4-[(4-fluorophenoxy)methyl]-2-methyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-methyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-(4-benzylmorpholin-2-yl)-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-(3-ethoxypropyl)-4-[(4-fluorophenoxy)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-[(2-methyl-1,3-thiazol-4-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-e]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(3-ethoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

N-[3-({2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-3,6-dioxo-1,2,3,6-tetra hydro-5H-pyrazolo[4,3-c]pyridin-5-yl}methyl)phenyl]acetamide;

4-[(4-chlorophenoxy)methyl]-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-e]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[methyl(phenyl)amino]methyl}-5-(2-pyridin-2-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-(3-ethoxypropyl)-4-{[methyl(phenyl)amino]methyl}-1H-pyrazolo[4,3-e]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[methyl(phenyl)amino]methyl}-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(3-ethyl-1,2,4-oxadiazol-5-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(1,3-thiazol-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

tert-butyl 4-({4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-3,6-dioxo-1,2,3,6-tetra hydro-5H-pyrazolo[4,3-c]pyridin-5-yl}methyl)piperidine-1-carboxylate;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(piperidin-4-ylmethyl)-1H-pyrazolo [4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[3-(diethylamino)propyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(4-chlorophenoxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(1-methylpiperidin-4-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(3-chlorophenoxy)methyl]-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-[(2,2,2-trifluoro-1-phenylethoxy)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-(3-phenoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(2-methyl-1,3-thiazol-4-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-[(4-phenylpiperidin-1-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-{4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl}-N,N-dimethylacetamide;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)oxy]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-{3-[methyl(phenyl)amino]propyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(4-methoxybenzyl)oxy]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[3-(2,3-dihydro-1H-indol-1-yl)propyl]-5-methyl-1H-pyrazolo[4,3-e]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-[(naphthalen-1-yloxy)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(4-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[2-(4-chlorophenyl)ethoxy]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[benzyl(methyl)amino]methyl}-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-[(4-methylmorpholin-2-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(piperidin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[3-(dimethylamino)phenoxy]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-{[methyl(pyridin-2-ylmethyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-(2-methoxyethyl)-4-[3-methoxyphenoxy)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(2-methoxy ethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(3-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-({[3-(dimethylamino)benzyl]oxy}methyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(diphenylmethoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)(methyl)amino]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)(methyl)amino]methyl}-2-(2-chlorophenyl)-5-(2-methoxy ethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-{[methyl(pyridin-3-ylmethyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)(methyl)amino]methyl}-2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)(methyl)amino]methyl}-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)oxy]methyl}-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-(2-methoxyethyl)-4-{[(3-methoxyphenyl)(methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxyphenyl)(methyl)amino]methyl}-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)(methyl)amino]methyl}-2-(2-chlorophenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)oxy]methyl}-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)oxy]methyl}-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)oxy]methyl}-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-fluorobenzyl)(methyl)amino]methyl}-5-(pyridin-3-yl methyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)(methyl)amino]methyl}-2-(2-chlorophenyl)-5-(pyrazin-2-yl methyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)(methyl)amino]methyl}-5-(pyridin-3-yl methyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-[(3-methoxyphenoxy)methyl]-5-[(4-methylmorpholin-2-yl) methyl]1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[4-(3-methoxyphenyl)piperazin-1-yl]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxyphenyl)(methyl)amino]methyl}-5-(pyridin-3-yl methyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[4-(2-chlorophenyl)piperazin-1-yl]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[4-(3-chlorophenyl)piperazin-1-yl]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-methoxyphenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-chlorophenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[methyl(pyridin-2-ylmethyl)amino]methyl}-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-4-{[methyl(pyridin-2-yl methyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(3-methoxybenzyl)oxy]methyl}-2-(2-methoxyphenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(3-methoxybenzyl)oxy]methyl}-2-(2-methoxyphenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[(3-methoxybenzyl)(methyl)amino]methyl}-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-methoxyphenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(3-methoxyphenoxy)methyl]-2-(2-methoxyphenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-4-{[methyl(pyridin-3-ylmethyl)amino]methyl}-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-4-{[methyl(pyridin-2-ylmethyl)amino]methyl}-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-methoxyphenyl)-4-{[4-(3-methoxyphenyl)piperazin-1-yl]methyl}-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-methoxyphenyl)-5-methyl-4-[(4-pyridin-2-ylpiperazin-1-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-methyl-4-[(4-pyridin-2-ylpiperazin-1-yl)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-{[(2-chlorobenzyl)oxy]methyl}-2-(2-methoxyphenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

4-[(benzyloxy)methyl]-2-(2-methoxyphenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione;

2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-4-[(pyridin-3-ylmethoxy) methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione; or

2-(2-chlorophenyl)-5-(pyrazin-2-ylmethyl)-4-[(pyridin-3-ylmethoxy)methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione.

13. A pharmaceutical composition containing at least one compound of claim 1 and a pharmaceutically acceptable carrier, diluent or excipient thereof.

14. A method for relieving symptoms of a disease or condition selected from pulmonary hypertension or chronic obstructive pulmonary disease (COPD) in a patient suffering from said disease or condition comprising administering a compound according to claim 1 to a patient having said disease or condition selected from pulmonary hypertension or chronic obstructive pulmonary disease (COPD).

15. A process for the preparation of a compound according to Formula (I), comprising the step of cyclizing a compound of Formula (VIII) in presence of a base:

wherein R 8 is a C 1 -C 6 alkyl; G 1 is H; G 2 , G 3 , G 4 and G 5 are as defined in claim 1 .

16. The method according to claim 14 , wherein said disease or condition is pulmonary hypertension.

17. The method according to claim 14 , wherein said disease or condition is chronic obstructive pulmonary disease (COPD).

18. The compound of claim 1 , wherein a substituent, when substituted, is substituted with from 1 to 5 substituent(s) selected from the group consisting of C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, C 1 -C 6 alkyl aryl, C 1 -C 6 alkyl heteroaryl, C 1 -C 6 alkyl cycloalkyl, C 1 -C 6 alkyl heterocycloalkyl, amino, aminosulfonyl, ammonium, acyl amino, amino carbonyl, aryl, heteroaryl, sulfonyl, sulfonyl, alkoxy, alkoxy carbonyl, carbamate, sulfanyl, halogen, trihalomethyl, cyano, hydroxy, mercapto and nitro.

19. A method for reducing or arresting growth of a cancer selected from acute myeloid leukemia, lung cancer, prostate cancer, lung carcinoma or prostatic carcinoma in a patient suffering from said cancer, comprising administering a compound according to claim 1 to a patient having said cancer selected from acute myeloid leukemia, lung cancer, prostate cancer, lung carcinoma or prostatic carcinoma.

20. The method according to claim 19 , wherein said cancer is acute myeloid leukemia.

21. The method according to claim 19 , wherein said cancer is lung cancer.

22. The method according to claim 19 , wherein said cancer is prostate cancer.

23. The method according to claim 19 , wherein said cancer is lung carcinoma.

24. The method according to claim 19 , wherein said cancer is prostatic carcinoma.

Assignments (3)
CHANGE OF NAME Recorded Aug 14, 2017
From: GENKYOTEX SA
To: GENKYOTEX SUISSE SA
Reel/Frame 043541/0392 →
CHANGE OF ADDRESS Recorded Aug 30, 2012
From: GENKYOTEX SA
To: GENKYOTEX SA
Reel/Frame 028885/0098 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 24, 2011
From: PAGE, PATRICK; ORCHARD, MIKE; LALEU, BENOIT; GAGGINI, FRANCESCA
To: GENKYOTEX SA
Reel/Frame 026140/0727 →
Priority Claims (1)
EP 08164853 · Sep 23, 2008 · regional
Continuity (1)
Related Publication 20110178081A1 · Jul 21, 2011