IP Library › Granted Patent US 12,565,497

Granted Patent B2

US 12,565,497 · App. 18/068,360 · Granted Mar 3, 2026

Sulfone derivatives

Inventors: Andrew Simon Bell (Dundee, GB); Jérémy Besnard (Dundee, GB); Anthony Richard Bradley (Dundee, GB); Luke Green (Basel, CH); Wolfgang Haap (Loerrach, DE); Buelent Kocer (Maulburg, DE); Andreas Kuglstatter (Loerrach, DE); Xavier Lucas (Basel, CH); Patrizio Mattei (Riehen, CH); Dmitry Mazunin (Grenzach-Wyhlen, DE); Claus Riemer (Freiburg, DE); Willem Paul Van Hoorn (Dundee, GB)

Assignee: Hoffmann-La Roche Inc.

C07D471/04 C07D209/08 C07D231/56

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Quick Facts

Patent No.: US 12,565,497
App. No.: 18/068,360
Granted: Mar 3, 2026
Kind: B2

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Abstract

The present invention provides compounds of formula I wherein X 1 , X 2 , X 3 , X 4 , R 1 , R 1a , R 1b , R 2′ , R 2 ″, R 3′ , R 3 ″, R 6 and R 7 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula I, pharmaceutical compositions comprising them and their use as medicaments.

Claims (269)

1 . A compound of formula 1:

wherein

X 1 is either N or C;

X 2 is either N or CR 4 ;

X 3 is either N or CR 5 ;

X 4 is either N or CH;

provided that no more than two of X 1 , X 2 and X 3 represent N;

the dotted lines represent a single or double bond, to enable the six membered rings to be aromatic with the proviso that when X 1 is N and X 2 is C═O then the bond between X 1 and X 2 , the bond between X 2 and X 3 , the bonds a and c are single bonds and the bond between X 3 and CR 7 and b are double bonds; and with the proviso that when X 1 is N and X 2 is not C═O then the bond between X 1 and X 2 , the bond between X 3 and CR 7 , the bonds b and c are single bonds and the bond between X 2 and X 3 and the bond a are double bonds;

R 1 is —SO 2 R 1a or —SOR 1b ;

R 1a and R 1b are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, NR 1′a R 1′b , oxetanyl, furanyl and pyranyl, wherein at least one of R 1′a and R 1′b is (C 1 -C 6 )alkyl and the other is H or (C 1 -C 6 )alkyl;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3″ hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 4 is hydrogen, cyano, oxo, hydroxy, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 3 -C 3 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4c , —SR 4f , —SO(NR 4h )R 4g or —SO 2 (NR 4i )R 4j ;

R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4d , R 4e and R 4f are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4h and R 4g are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 4 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4i and R 4j are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 5 is hydrogen, halogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyl, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 ) alkyl; and

R 7 is hydrogen, halogen, hydroxy, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo-(C 1 -C 6 )alkyl, halo-(C 1 -C 6 )alkoxy or NR 7′a R 7′b , wherein one of R 7′a and R 7′b is hydrogen and the other is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, —(C 1 -C 6 )alkyl-O—(C 1 -C 6 )alkyl-NHCO—(C 1 -C 6 )alkyl, —(C 1 -C 6 )alkyl-O—(C 1 -C 6 )alkyl-NH 2 , —(C 1 -C 6 )alkyl-NHCO—(C 1 -C 6 )alkyl or —(C 1 -C 6 )alkyl-NH 2 ;

or pharmaceutically acceptable salts thereof.

2 . A compound according to claim 1 , wherein the compound is of formula Ia;

wherein

X 1 is either N or C;

X 3 is either N or CR 5 ;

the dotted line represents a double bond to enable the six membered rings to be aromatic with the proviso that when X 1 is N and R 4 is oxo then the bond is a single bond;

R 1 is —SO 2 R 1a or —SOR 1b ;

R 1a and R 1b are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy(C 1 -C 6 )alkyl, NR 1′a R 1′b , oxetanyl, furanyl and pyranyl, wherein at least one of R 1′a and R 1′b is (C 1 -C 6 )alkyl and the other is H or (C 1 -C 6 )alkyl;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 4 is hydrogen, cyano, oxo, hydroxy, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4e , —SR 4f , —SO(NR 4h )R 4g or —SO 2 NR 4i )R 4j ;

R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 4 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4d , R 4e and R 4f rare independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4h and R 4g are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4i and R 4j are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyl, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 ) alkyl; and

or pharmaceutically acceptable salts thereof.

3 . The compound according to claim 1 , wherein the compound is of formula Ib:

wherein

X 3 is either N or CR

R 1 is —SO 2 R 1a or —SOR 1b ;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy,

R 4 is hydrogen, cyano, oxo, hydroxy, halogen, —NH 2 , (C 1 -C 4 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 6 alkoxy(C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4c , —SR 4f , —SO(NR 4h )R 4g or —SO 2 (NR 4i )R 4j ;

R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4d , R 4e and R 4f are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4h and R 4g are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4i and R 4j are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 5 is hydrogen, halogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyi, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 ) alkyl; and

or pharmaceutically acceptable salts thereof.

4 . The compound according to claim 1 , wherein the compound is of formula Ic:

wherein

R 1 is —SO 2 R 1a or —SOR 1b ;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 5 is hydrogen, halogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyl, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 ) alkyl; and

or pharmaceutically acceptable salts thereof.

5 . The compound according to claim 1 , wherein the compound is of formula Id;

wherein

R 1 is —SO 2 R 1a or —SOR 1b ;

R 1a and R 1b are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, -, NR 1′a R 1′b , oxetanyl, furanyl and pyranyl, wherein at least one of R 1′a and R 1′b is (C 1 -C 6 )alkyl and the other is H or (C 1 -C 6 )alkyl;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 4 is hydrogen, cyano, oxo, hydroxy, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4e , —SR 4f , —SO(NR 4h )R 4g or —SO 2 (NR 4i )R 4j ;

R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4d , R 4e and R 4f are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4h and R 4g are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4i and R 4j are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 5 is hydrogen, halogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyl, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 )alkyl; and

or pharmaceutically acceptable salts thereof.

6 . The compound according to claim 1 , wherein the compound is of formula Ie:

wherein

R 1 is —SO 2 R 1a or —SOR 1b ;

R 2′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3′ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 3″ is hydrogen, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkoxy;

R 4 is hydrogen, cyano, oxo, hydroxy, halogen, —NH 2 , (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl(C 1 -C 6 )alkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4e , —SO(NR 4h ) 4g or —SO 2 (NR 4i )R 4j ;

R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4d , R 4e and R 4f are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4h and R 4g are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 4i and R 4j are independently selected from hydrogen, (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl and oxetanyl;

R 6 is halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, cyano, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, (C 3 -C 6 )cycloalkyl, oxetanyl or thiophenyl or —SO 2 R 6a ;

R 6a is (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl or halo(C 1 -C 6 ) alkyl; and

or pharmaceutically acceptable salts thereof.

7 . The compound according to claim 1 , wherein X 4 is N.

8 . The compound according to claim 1 , wherein X 1 is N or C, X 2 is N or CR 4 and X 3 is N or CR 5 .

9 . The compound according to claim 1 , wherein R 1 is —SO 2 R 1a .

10 . The compound according to claim 1 , wherein R 4a and R 4b are independently selected from (C 1 -C 6 )alkyl, (C 3 -C 6 )cycloalkyl,(C 3 -C 6 )cycloalkyl-(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, NR 1′a R 1′b , oxetanyl, furanyl and pyranyl, wherein at least one of R 1′a and R 1′b is (C 1 -C 6 )alkyl and the other is H or (C 1 -C 6 )alkyl.

11 . The compound according to claim 1 , wherein R 1a is selected from methyl, ethyl, propyl, i-propyl, i-butyl, cyclopropyl,

fluoromethyl, difluoromethyl, fluoro-ethanyl, difluoro-ethanyl, 1,2 difluoroethanyl, 1,1,2-trifluoroethanyl, 1,2,2-trifluoroethanyl, Hydroxymethyl, hydroxyethyl, metoxymethyl, methylaminyl (—NHCH 3 ), dimethylaminyl (—N(CH 3 ) 2 ) and oxetanyl.

12 . The compound according to claim 1 , wherein R 1b is (C 1 -C 6 )alkyl.

13 . The compound according to claim 1 , wherein if R 2′ is other than hydrogen as defined according to claim 1 , then R 3′ is hydrogen, R 2″ is hydrogen and R 3″ is as defined according to claim 1 .

14 . The compound according to claim 1 , wherein one of R 2′ and R 2″ is hydrogen, halogen, —NH 2 , (C 1 -C 2 )alkyl, (C 1 -C 2 )alkoxy or halo(C 1 -C 2 )alkyl, while the other one is hydrogen.

15 . The compound according to claim 1 , wherein one of R 3′ and R 3″ is hydrogen, halogen, —NH 2 , (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy or halo(C 1 -C 3 )alkyl, while the other one is hydrogen.

16 . The compound according to claim 1 , wherein both R 3′ and R 3″ are hydrogen.

17 . The compound according to claim 1 , wherein R 4 is cyano, oxo, hydroxy, (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy, halo(C 1 -C 3 )alkyl, halo(C 1 -C 6 )alkoxy, (C 1 -C 3 )alkoxy-(C 1 -C 3 )alkyl, (C 3 -C 4 )cycloalkyl, —CO 2 R 4a , —CONR 4b R 4c , —SO 2 R 4d , —SOR 4e , —SR 4f or —SO(NR 4h )R 4g .

18 . The compound according to claim 1 , wherein R 4a , R 4b and R 4c are independently selected from hydrogen, (C 1 -C 3 )alkyl, (C 3 -C 4 )cycloalkyl, and oxetanyl.

19 . The compound according to claim 1 , wherein R 4a is hydrogen.

20 . The compound according to claim 1 , wherein R 4d , R 4c and R 4f are independently selected from (C 1 -C 3 )alkyl, (C 3 -C 4 )cycloalkyl, and oxetanyl.

21 . The compound according to claim 1 , wherein R 4d is methyl.

22 . The compound according to claim 1 , wherein R 4h and R 4g are independently selected from hydrogen and (C 1 -C 6 )alkyl.

23 . The compound according to claim 1 , wherein R 4i and R 4j are independently selected from hydrogen and (C1-C 6 )alkyl.

24 . The compound according to claim 1 , wherein R 5 is hydrogen, halogen, (C1-C 6 )alkyl, (C1-C 6 )alkoxy or (C3-C 6 )cycloalkyl.

25 . The compound according to claim 1 , wherein R 5 is hydrogen.

26 . The compound according to claim 1 , wherein R 6 is halogen, (C1-C 6 )alkyl, (C1-C 6 )alkoxy, cyano, halo(C1-C 6 )alkyl, halo(C1-C 6 )alkoxy, (C3-C 6 )cycloalkyl, thiophenyl, oxetanyl or —SO 2 R 6a .

27 . The compound according to claim 1 , wherein R 6a is (C1-C 6 )alkyl.

28 . The compound according to claim 1 , wherein R 7 is hydrogen, halogen, hydroxy or (C1-C 6 )alkyl.

29 . The compound according to claim 1 , wherein one of R 7′a and R 7′b is hydrogen and the other is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C6)alkoxy, -(C1-C 3 )alkyl-O—(C 1 -C 3 )alkyl-NHCO—(C 1 -C 3 )alkyl, —(C 1 -C 3 )alkyl-O—(C 1 -C 3 )alkyl-NH 2 , —(C 1 -C 3 )alkyl-NHCO—(C 1 -C 3 )alkyl or —(C 1 -C 3 )alkyl-NH 2 .

30 . The compound according to claim 1 , wherein R 1b is (C 1 -C 3 )alkyl.

31 . The compound according to claim 1 , wherein R 1b is methyl.

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

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(3-methoxy-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

4-(3-chloro-4-(methylsulfonyl)phenyl)-3-cyclopropyl-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(4-(methylsulfonyl)-3-(trifluoromethyl)phenyl)-1H-pyrazolo(4,3-c]pyridine;

4-(3-cyclopropyl-1 H-pyrazolo[4,3-c]pyridin-4-yl)-N,N,2-trimethylbenzenesulfonamide;

3-cyclopropyl-5-methoxy-4-(4-methylsulfonylphenyl)-1H-pyrazolo[3,4-c]pyridine;

3-cyclopropyl-4-(4-(cyclopropylsulfonyl)-3-methylphenyl)-1H-pyrazolo[4,3-c]pyridine;

4-(3-chloro-4-(cyclopropylsulfonyl)phenyl)-3-cyclopropyl-1H-pyrazolo[4,3-c]pyridine;

2-chloro-4-(3-cyclopropyl-1H-pyrazolo[4,3-c]pyridin-4-yl)-N,N-dimethylbenzenesulfonamide;

4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridine;

4-(4-(methylsulfonyl)phenyl)-3-(trifluoromethyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(3-(difluoromethyl)-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(3-(fluoromethyl)-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-bromo-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1 H-pyrrolo[3,2-c]pyridine;

3-cyclopropyl-4-(3-methyl-4-(oxetan-3-ylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-methoxy-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

5-(3-cyclopropyl-1H-pyrazolo[4,3-c]pyridin-4-yl)-2-(methylsulfonyl)aniline;

4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(methylsulfonyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

3-(1,1-difluoroethyl)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine-3-carbonitrile;

3-(difluoromethyl)-4-(3-methyl-4-methylsulfonylphenyl)-1H-pyrazolo[4,3-c]pyridine;

3-isopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(4-ethylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(2-fluoro-5-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-4-(2,5-dimethyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-c]pyridine hydrochloride;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxylic acid;

3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1H-indazole-5-carbonitrile;

3-cyclopropyl-4-(3-methyl-4-methylsulfinyl-phenyl)-1H-pyrazolo[4,3-c]pyridine hydrochloride;

3-cyclopropyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-c]pyridin-7-ol;

4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(thiophen-3-yl)-1H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-5-methoxy-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine;

3-ethoxy-4-(3-methyl-4-methylsulfonyl-phenyl)-1 H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-1H-pyrazolo[4,3-c]pyridine;

4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-3-(difluoromethoxy)-1 H-pyrazolo[4,3-c]pyridine;

3-cyclopropyl-7-fluoro-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-(4-ethylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

4-(3-methyl-4-methylsulfonyl-phenyl)-3-(oxetan-3-yl)-1H-pyrazolo[4,3-c]pyridine;

4-[4-(cyclopropylmethylsulfonyl)-3-methyl-phenyl]-3-(difluoromethoxy)-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-(3-methyl-4-propylsulfonyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-[3-(difluoromethyl)-4-methylsulfonyl-phenyl]-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-(4-isopropylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[4,3-c]pyridine;

4-[3-(difluoromethoxy)-1H-pyrazolo[4,3-c]pyridin-4-yl]-N,2-dimethyl-benzenesulfonamide;

3-methoxy-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carbonitrile;

3-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carbonitrile;

6-chloro-3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1H-pyrazolo[4,3-c]pyridine;

3-(difluoromethoxy)-4-[3-methyl-4-(oxetan-3-ylsulfonyl)phenyl]-1H-pyrazolo[4,3-c]pyridine;

2-[4-[3-(difluoromethoxy)-1H-pyrazolo[4,3-c]pyridin-4-yl]-2-methyl-phenyl]sulfanylethanol;

3-cyclopropyl-6-methoxy-4-(3-methyl-4-methylsulfonylphenyl)-1H-pyrazolo[4,3-c]pyridine 2,2,2-trifluoroacetic acid;

3-(difluoromethoxy)-4-[3-methyl-4-(1-methylcyclopropyl)sulfonyl-phenyl]-1H-pyrazolo[4,3-c]pyridine;

4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(trifluoromethoxy)-1 H-pyrazolo[4,3-c]pyridine,

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-N-methyl-4-(3-methyl-4-methylsulfonyl)phenyl)-1 H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyridazine;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylthio)-1H-indazole;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfinyl)-1H-indazole;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-1H-indazole;

3-(difluoromethoxy)-4-[4-(methoxymethylsulfonyl)-3-methyl-phenyl)-1 H-pyrazolo[4,3-c]pyridine formic acid;

5-methoxy-4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(trifluoromethyl)-1H-pyrazolo[3,4-c]pyridine;

4-(3-methyl-4-(methylsulfonyl)phenyl)-3-(trifluoromethyl)-1H-pyrrolo[3,2-c]pyridine,

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-b]pyridin-5-one;

3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-5-(trifluoromethyl)-1 H-pyrazolo(3,4-c]pyridine;

3-cyclopropyl-6-methyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-b]pyridin-5-one;

3,6-dicyclopropyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-b]pyridin-5-one;

3-cyclopropyl-5-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine;

3-cyclopropyl-N,N-dimethyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-5-(methoxymethyl)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine;

3-cyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-N-(oxetan-3-yl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3,5-dicyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1H-pyrazolo[3,4-c]pyridine;

N,3-dicyclopropyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-6-fluoro-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carbonitrile;

3-cyclopropyl-4-(4-ethylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

3-cyclopropyl-4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-3-(trifluoromethyl)-1H-indazole;

3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1H-indole-5-carbonitrile;

3-cyclopropyl-4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-6-fluoro-N-methyl-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carboxamide;

3-cyclopropyl-6-fluoro-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carboxamide;

6-chloro-3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1#H!-indazole-5-carbonitrile;

3-cyclopropyl-4-(2-fluoro-5-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-(3-methyl-4-methylsulfonyl-phenyl)-3-(trifluoromethoxy)-1H-pyrazolo[4,3-b]pyridin-5-one;

3-cyclopropyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrrolo(3,2-b]pyridin-5-one;

4-[3-(difluoromethoxy)-1H-pyrazolo[4,3-c]pyridin-4-yl]-2-(difluoromethyl)-N,N-dimethyl-benzenesulfonamide;

3-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-1H-indazole;

3-cyclopropyl-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-3-(trifluoromethoxy)-1H-indazole;

3-cyclopropyl-4-[3-(difluoromethyl)-4-methylsulfonyl-phenyl]-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

3-(difluoromethoxy)-4-[5-(difluoromethyl)-2-methyl-4-methylsulfinyl-phenyl]-1 H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-[3-(difluoromethyl)-4-methylsulfonyl-phenyl]-5-methoxy-3-(trifluoromethyl)-1H-pyrazolo[3,4-c]pyridine;

3-cyclopropyl-4-(3-(difluoromethyl)-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-1H-indazole;

3-(difluoromethoxy)-N-methyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-cyclopropyl-4-(4-cyclopropylsulfonyl-2-fluoro-5-methyl-phenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-3-(difluoromethoxy)-5-methylsulfonyl-1H-indazole;

3-cyclopropyl-4-(2-fluoro-5-methyl-4-methylsulfonyl-phenyl)-N-methyl-1H-pyrazolo(3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(4-((difluoromethyl)sulfonyl)-3-methylphenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-N-(oxetan-3-yl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-N-(2-methoxyethyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-N-methyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide,

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-5-(oxetan-3-ylsulfonyl)-1H-indazole;

[3-cyclopropyl-4-(3-methyl-4-methylsulfonylphenyl)-1H-indazol-5-yl]-imino-methyl-oxo-sulfane;

[3-cyclopropyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-indazol-5-yl]-methyl-methylimino-oxo-λ 6 -sulfane;

3-cyclopropyl-N,N-dimethyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-indazole-5-sulfonamide;

3-cyclopropyl-N-methyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-indazole-5-sulfonamide;

4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-3-(difluoromethoxy)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(4-((difluoromethyl)sulfonyl)-3-methylphenyl)-5-(methylsulfonyl)-1H-indazole;

5-cyclopropylsulfonyl-3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-indazole;

3-(difluoromethoxy)-4-(2-fluoro-5-methyl-4-methylsulfonyl-phenyl)-5-methylsulfonyl-1H-indazole; and

4-(4-cyclopropylsulfonyl-3-methyl-phenyl)-3-(difluoromethoxy)-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide or pharmaceutically acceptable salts thereof.

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

3-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-1H-indazole-5-carbonitrile;

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[4,3-b]pyridin-5-one;

3-cyclopropyl-4-(4-ethylsulfonyl-3-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-3-(trifluoromethyl)-1 H-indazole;

3-(difluoromethoxy)-4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-1H-indazole;

3-cyclopropyl-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

4-(3-methyl-4-(methylsulfonyl)phenyl)-5-(methylsulfonyl)-3-(trifluoromethoxy)-1H-indazole;

3-cyclopropyl-4-[3-(difluoromethyl)-4-methylsulfonyl-phenyl]-N-methyl-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carbonitrile;

3-(difluoromethoxy)-N-methyl-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide;

3-(difluoromethoxy)-4-(3-methyl-4-methylsulfonyl-phenyl)-1H-pyrazolo[3,4-c]pyridine-5-carboxamide; and

3-(difluoromethoxy)-4-[4-(difluoromethylsulfonyl)-3-methyl-phenyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide

or pharmaceutically acceptable salts thereof.

34 . A pharmaceutical composition comprising at least one compound of formula I according to claim 1 or its pharmaceutically acceptable salts and one or more pharmaceutically acceptable excipients.

35 . A method for the treatment of Lung Adenocarcinoma, Melanoma, Pancreatic Adenocarcinoma, Head and Neck Squamous Cell Carcinoma, Lung Squamous Cell Carcinoma, Esophageal Carcinoma, Glioblastmoa Multiforme, Mesothelioma, or a combination thereof, which method comprises administering at least one compound of formula 1 according to claim 1 or its pharmaceutically acceptable salts to a subject.

36 . A method for delaying the progression of Lung Adenocarcinoma, Melanoma, Pancreatic Adenocarcinoma, Head and Neck Squamous Cell Carcinoma, Lung Squamous Cell Carcinoma, Esophageal Carcinoma, Glioblastmoa Multiforme, Mesothelioma, or a combination thereof, which method comprises administering at least one compound of formula I according to claim 1 or its pharmaceutically acceptable salts to a subject.

Assignments (4)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2023

From: BELL, ANDREW SIMON; BESNARD, JÉRÉMY; BRADLEY, ANTHONY RICHARD; VAN HOORN, WILLEM PAUL

To: EXSCIENTIA LTD.

Reel/Frame 062746/0131 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2023

From: EXSCIENTIA LTD.

To: F. HOFFMANN-LA ROCHE AG

Reel/Frame 062746/0176 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2023

From: GREEN, LUKE; HAAP, WOLFGANG; KOCER, BUELENT; KUGLSTATTER, ANDREAS; LUCAS, XAVIER; MATTEI, PATRIZIO; MAZUNIN, DMITRY; RIEMER, CLAUS

To: F. HOFFMANN-LA ROCHE AG

Reel/Frame 062746/0183 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2023

From: F. HOFFMANN-LA ROCHE AG

To: HOFFMANN-LA ROCHE INC.

Reel/Frame 062746/0206 →

Priority Claims (1)

EP 20181363 · Jun 22, 2020 · regional

Continuity (2)

Continuation PCTEP2021066767 · Jun 21, 2021

Related Publication 20230219953A1 · Jul 13, 2023

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