IP Library Granted Patent US 10,501,479
Granted Patent B2
US 10,501,479 · App. 15/464,430 · Granted Dec 10, 2019

Benzenesulfonyl-asymmetric ureas and medical uses thereof

Inventors: Claudio Giuliano (Como, IT); Antoine Daina (Lausanne, CH); Claudio Pietra (Como, IT)
Assignee: Helsinn Healthcare SA
C07D513/04C07C311/47C07C317/14C07C317/26C07C317/42C07C317/44C07D209/04C07D209/08C07D209/44C07D213/34C07D213/76C07D215/06C07D215/08C07D215/10C07D215/58C07D217/04C07D217/10C07D223/16C07D231/56C07D233/64C07D235/14C07D237/20C07D239/26C07D239/48C07D241/04C07D241/12C07D295/088C07D307/87C07D311/76C07D317/34C07D401/12C07D403/12C07D405/04C07D405/06C07D405/12C07D409/12C07D413/12C07D417/10C07D417/12C07D471/04C07D471/08C07D487/04C07D495/04C07C2601/02
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Quick Facts
Patent No.
US 10,501,479
App. No.
15/464,430
Granted
Dec 10, 2019
Kind
B2
Abstract

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Claims (692)

1. A compound of Formula IV:

or a pharmaceutically acceptable salt thereof, wherein:

a dashed line indicates an optional bond;

X is a bond, CO, or CR 7 R 8 ;

k is 0-2;

R 1 and R 2 are each independently, H, C 1-3 alkyl, methoxy, halo or OH;

or R 1 and R 2 taken together with the atoms to which they are attached form a 5-6 membered ring;

or R 1 and X taken together with the atoms to which they are attached form a 5-6 membered ring;

R 3 is H, C 1-3 alkyl, methoxy, halo, OH, COOR 12 , CR 13 R 14 OH, COHNR 15 , cycloalkyl, or heteroaryl;

R 4 is a bond, NR 6 or CR 9 R 10 ;

or R 3 and R 4 taken together with the atoms to which they are attached form a 3-6-membered ring;

R 6 is a bond, H, or CH 3 ;

R 7 and R 8 are each, independently, H or C 1-3 alkyl, or CONH 2, wherein said C 1-3 alkyl is optionally substituted with halo;

R 9 and R l0 are each, independently, H or C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted with halo;

R 12 is H or C 1-3 alkyl;

R 13 and R 14 are each independently H or C 1-3 alkyl;

R 15 is H or C 1-3 alkyl;

U is C, N, S, or 0;

Z is halo or methoxy;

R′ is a halo, heteroaryl, C 1-6 alkoxy, C 1-6 alkyl, heterocycloalkyl, CN cycloalkyl, CO 2 (C 1-6 alkyl), or CO(C 1-6 alkyl);

or two R′ taken together with the atoms to which they are attached form a 5-6-membered ring;

R 16 is H or C 1-3 alkyl;

R 17 is H, halo, or C 1-3 alkyl;

1 is 0-3;

m is 0-3;

n is 0-3; and

p is 1-3.

2. The compound of claim 1 , wherein X is CO.

3. The compound of claim 1 , wherein X is a bond.

4. The compound of claim 1 , wherein said X is C 1-3 alkyl.

5. The compound of claim 1 , wherein X is CH(CH 3 ).

6. The compound of claim 1 , wherein X is C(CH 3 ) 2 .

7. The compound of claim 1 , wherein X is CHCF 3 .

8. The compound of claim 1 , wherein X is CH(CH 2 CH 3 ).

9. The compound of claim 1 , wherein X is C 1-3 alkyl substituted with halo.

10. The compound of claim 1 , wherein

is selected from the group consisting of

11. The compound of claim 1 , wherein

is phenyl.

12. The compound of claim 1 , wherein R 1 is OH.

13. The compound of claim 1 , wherein R 1 is CH 3 .

14. The compound of claim 1 , wherein R 2 is CH 3 .

15. The compound of claim 1 , wherein R 3 is F.

16. The compound of claim 1 , wherein R 3 is Cl.

17. The compound of claim 1 , wherein R 3 is methoxy.

18. The compound of claim 1 , wherein R 4 is CR 9 R 10 .

19. The compound of claim 1 , wherein R 4 is CH 2 .

20. The compound of claim 1 , wherein R 4 is CHCH 3 .

21. The compound of claim 1 , wherein R 4 is C(CH 3 ) 2 .

22. The compound of claim 1 , wherein R 4 is NCH 3.

23. The compound of claim 1 , wherein R 4 and R 3 come together to form a 5-membered heterocyclic ring.

24. The compound of claim 1 , wherein

is selected from the group consisting of

25. The compound of claim 1 , wherein

is

26. The compound of claim 1 , wherein

is

optionally substituted with 1-2 substituents from the group consisting of CH 3, CH 2 CH 3, and F.

27. The compound of claim 1 , wherein

is tetrahydroisoquinoline.

28. The compound of claim 1 , wherein

is tetrahydroisoquinoline substituted with 1-3 substituents from the group consisting of CH 3 , CH 2 CH 3 , F, and methoxy.

29. The compound of claim 1 , wherein

is selected from the group consisting of

30. The compound of claim 1 , wherein p is 1.

31. The compound of claim 1 , wherein p is 2.

32. The compound of claim 1 , wherein n is 0.

33. A compound or a pharmaceutically acceptable salt thereof selected from the group consisting of:

Compound

No.

Chemical Structure

Chemical Name

H0990

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N- (1H-indol-5-yl)benzenesulfonamide

H0991

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N-(1H- indol-5-yl)benzenesulfonamide

H0997

(S)-4-(3-(1-(2,3-dichloro-4-(pyrazin- 2-yl)phenyl)ethyl)ureido)-N-(1H- indol-5-yl)benzenesulfonamide

H1003

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroquinolin-6- yl)benzenesulfonamide

H1004

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1005

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1006

(S)-4-(3-(1-(2,3-dichloro-4-(pyrazin- 2-yl)phenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1008

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroquinolin-6- yl)benzenesulfonamide

H1017

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1018

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N-(2- ethyl-1,2,3,4-tetrahydroisoquinolin- 6-yl)benzenesulfonamide

H1024

(S)-1-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1025

(S)-1-(4-(((2-acetyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- (2,3-dichloro-4- methoxyphenyl)ethyl)urea

H1026

(S)-1-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-3-(4-(((2- (methylsulfonyl)-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1027

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1028

(S)-1-(1-phenylethyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1029

1-benzyl-3-(4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1033

(S)-4-(3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)ureido)-N-(2- (methylsulfonyl)-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1034

(S)-N-(2-acetyl-1,2,3,4- tetrahydroisoquinolin-6-yl)-4-(3-(1- (2,3-dichloro-4- methoxyphenyl)ethyl)ureido) benzenesulfonamide

H1038

l-(3-chlorobenzyl)-3-(4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1039

1-(2-chlorobenzyl)-3-(4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1040

1-(2,3-dichlorobenzyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1041

1-(1-(2-chlorophenyl)ethyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1042

1-(1-(3-chlorophenyl)ethyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1043

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((1,2,3,4- tetrahydroisoquinolin-7- yl)methyl)sulfonyl)phenyl)urea

H1044

1-(2,3-dichlorobenzyl)-3-(4- (((1,2,3,4-tetrahydroisoquinolin-7- yl)methyl)sulfonyl)phenyl)urea

H1045

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((indolin-6- ylmethyl)sulfonyl)phenyl)urea

H1046

1-(2,3-dichlorobenzyl)-3-(4- ((indolin-6- ylmethyl)sulfonyl)phenyl)urea

H1047

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((indolin-5- ylmethyl)sulfonyl)phenyl)urea

H1048

1-(2,3-dichlorobenzyl)-3-(4- ((indolin-5- ylmethyl)sulfonyl)phenyl)urea

H1049

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N- (1,2,3,4-tetrahydroisoquinolin-7- yl)benzenesulfonamide

H1054

ethyl (S)-6-((4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)phenyl) sulfonamido)-3,4- dihydroisoquinoline-2(1H)- carboxylate

H1055

ethyl (S)-6-(((4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)phenyl) sulfonyl)methyl)-3,4- dihydroisoquinoline-2(1H)- carboxylate

H1056

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1057

1-(2,3-dichlorobenzyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1067

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((2-((5-methyl-2-oxo-1,3- dioxol-4-yl)methyl)-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1068

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N-(2- ((5-methyl-2-oxo-1,3-dioxol-4- yl)methyl)-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1071

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1072

(S)-1-(4-(((2-benzyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- (2,3-dichlorophenyl)ethyl)urea

H1080

1-((S)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-((1-(1,2,3,4- tetrahydroisoquinolin-6- yl)ethyl)sulfonyl)phenyl)urea

H1081

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((2-(1,2,3,4- tetrahydroisoquinolin-6-yl)propan-2- yl)sulfonyl)phenyl)urea

H1092

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((isochroman-6- ylmethyl)sulfonyl)phenyl)urea

H1097

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-((isochroman-7- ylmethyl)sulfonyl)phenyl)urea

H1098

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((1,3-dihydroisobenzofuran-5- yl)methyl)sulfonyl)phenyl)urea

H1102

1-((S)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-((1-(1,2,3,4- tetrahydroisoquinolin-6- yl)ethyl)sulfonyl)phenyl)urea hydrochloride

H1103

1-((S)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-((1-(1,2,3,4- tetrahydroisoquinolin-6- yl)ethyl)sulfonyl)phenyl)urea hydrochloride

H1106

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N-(1H- indazol-5-yl)benzenesulfonamide

H1111

(S)-N-(1H-benzo[d]imidazol-5-yl)- 4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido) benzenesulfonamide

H1142

(S)-1-(4-(((1H-indol-5- yl)methyl)sulfonyl)phenyl)-3-(1- (2,3-dichlorophenyl)ethyl)urea

H1148

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1156

N-(isoindolin-5-yl)-4-(3-(1- phenylethyl)ureido) benzenesulfonamide

H1179

1-benzyl-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1188

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)-1- hydroxyureido)-N-(isoindolin-5- yl)benzenesulfonamide

H1190

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3- phenylurea

H1193

1-benzyl-3-(4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)urea

H1194

1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1199

4-(1-hydroxy-3-(1- phenylethyl)ureido)-N-(isoindolin-5- yl)benzenesulfonamide

H1203

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(4- methoxybenzyl)urea

H1204

1-benzyl-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1- methylurea

H1206

3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-methyl- 1-(1-phenylethyl)urea

H1212

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-((5- methoxypyridin-2-yl)methyl)urea

H1213

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-methyl- 3-(1-phenylethyl)urea

H1214

(R)-1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1215

(S)-1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1219

1-(4-(((2-benzylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1220

1-(4-(((2- (cyclopropylmethyl)isoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1221

1-(4-(((2-ethylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1227

1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(2,2,2- trifluoro-1-phenylethyl)urea

H1231

1-(4-((2-(2-benzylisoindolin-5- yl)propan-2-yl)sulfonyl)phenyl)-3- (1-phenylethyl)urea

H1232

1-(4-((2-(2-ethylisoindolin-5- yl)propan-2-yl)sulfonyl)phenyl)-3- (1-phenylethyl)urea

H1233

1-(4-((1-(2-benzylisoindolin-5- yl)ethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1234

1-(4-((1-(2-ethylisoindolin-5- yl)ethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1235

1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylpropyl)urea

H1248

2-chloro-5-ethyl-N-((4-((isoindolin- 5-ylmethyl)sulfonyl) phenyl)carbamoyl)benzamide

H1249

2-chloro-N-((4-((isoindolin-5- ylmethyl)sulfonyl)phenyl) carbamoyl)- 5-morpholinobenzamide

H1250

2-chloro-N-((4-(N-(isoindolin-5- yl)sulfamoyl)phenyl)carbamoyl)-5- morpholinobenzamide

H1251

2-chloro-5-ethoxy-N-((4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl) carbamoyl)benzamide

H1252

2-chloro-5-ethoxy-N-((4-(N- (isoindolin-5- yl)sulfamoyl)phenyl)carbamoyl) benzamide

H1256

(5-methyl-2-oxo-1,3-dioxol-4- yl)methyl 5-(((4-(3-(1- phenylethyl)ureido)phenyl)sulfonyl) methyl)isoindoline-2-carboxylate

H1259

2-chloro-5-ethyl-N-((4-(N- (isoindolin-5- yl)sulfamoyl)phenyl)carbamoyl) benzamide

H1260

1-(1-(3-chlorophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1261

1-(1-(2-chlorophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1262

1-(1-(4-fluorophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1263

2-chloro-5-ethyl-N-((4-(N-(1,2,3,4- tetrahydroisoquinolin-7- yl)sulfamoyl)phenyl)carbamoyl) benzamide

H1266

1-(1-(3-chlorophenyl)ethyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1267

1-(1-(2-chlorophenyl)ethyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1268

1-(1-(4-fluorophenyl)ethyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1269

1-(1-(3-fluorophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1272

1-(1-(2-fluorophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1281

1-(1-(2-chloro-5-ethylphenyl)ethyl)- 3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1283

1-(1-(2-chloro-5- morpholinophenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1284

1-(1-(2-chloro-5- morpholinophenyl)ethyl)-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1286

1-1-(2-chloro-5-ethylphenyl)ethyl)- 3-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1291

1-(4-(((3-oxoisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1292

1-(4-(((1-oxoisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1293

1-(4-(((3-hydroxy-2,3-dihydro-1H- inden-5-yl)methyl)sulfonyl)phenyl)- 3-(1-phenylethyl)urea

H1294

1-(1-phenylethyl)-3-(4-(((3- (pyrrolidin-1-yl)-2,3-dihydro-1H- inden-5- yl)methyl)sulfonyl)phenyl)urea

H1298

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1-(4- methoxyphenyl)ethyl)urea

H1299

(S)-1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1300

(R)-1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1306

(S)-1-(1-phenylethyl)-3-(4- (((2,3,4,5-tetrahydro-1H- benzo[d]azepin-7- yl)methyl)sulfonyl)phenyl)urea

H1308

N-(2-methylisoindolin-5-yl)-4-(3-(1- phenylethyl)ureido) benzenesulfonamide

H1310

4-(1-(3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)ureido) ethyl)phenyl acetate

H1311

(S)-1-(4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-7- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1315

(S)-N-(2-methyl-1,2,3,4- tetrahydroisoquinolin-6-yl)-4-(3-(1- phenylethyl)ureido) benzenesulfonamide

H1316

1-(2-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1317

1-(2-fluoro-4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1319

1-(4-(((2-(oxetan-3-yl)isoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1320

1-(4-(((5,6-dihydro-4H-thieno[2,3- c]pyrrol-2- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1321

1-(4-(((5-methyl-5,6-dihydro-4H- thieno[2,3-c]pyrrol-2- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1322

(S)-1-(4-(((3-methyl-2,3,4,5- tetrahydro-1H-benzo[d]azepin-7- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1323

1-(4-(((6-methyl-6,7-dihydro-5H- pyrrolo[3,4-b]pyridin-3- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1326

1-(1-(3-methoxyphenyl)ethyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1327

1-(1-(3-methoxyphenyl)ethyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1329

1-(4-(((2-methyl-2H-indazol-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1333

4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1334

4-(3-(1-(2- chlorophenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1337

(R)-N-(2-methylisoindolin-5-yl)-4- (3-(1-phenylethyl)ureido) benzenesulfonamide

H1338

1-(4-(((2-(2- methoxyethyl)isoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1339

1-(4-(((2-(cyanomethyl)isoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1340

1-(1-phenylethyl)-3-(4-(((2- (tetrahydrofuran-3-yl)isoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1341

1-(1-phenylethyl)-3-(4-(((2- ((tetrahydrofuran-2- yl)methyl)isoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1342

1-(1-(2-fluorophenyl)ethyl)-3-(4- (((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1343

(R)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1344

1-(1-(2-chlorophenyl)ethyl)-3-(4- (((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1345

1-(1-(2,3-difluorophenyl)ethyl)-3- (4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1346

4-(3-(1-(2,3- difluorophenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1347

4-(3-(1-(2- fluorophenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1348

(R)-1-(4-(((5-methyl-5,6-dihydro- 4H-thieno[2,3-c]pyrrol-2- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1349

1-(2,3-dichlorobenzyl)-3-(4-(((2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1350

2-methyl-5-(((4-(3-(1- phenylethyl)ureido)phenyl)sulfonyl) methyl)isoindoline 2-oxide

H1351

(R)-1-(4-(((5-methyl-5,6-dihydro- 4H-thieno[2,3-c]pyrrol-3- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1352

(S)-4-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-N-(2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)benzenesulfonamide

H1355

(R)-1-(4-(((7-fluoro-2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethy)urea

H1356

(R)-1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1357

(R)-1-(1-phenylethyl)-3-(4-(((1,1,2- trimethylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1363

(R)-1-(4-(((4-fluoro-2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1366

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((7-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1367

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((5-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1368

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((7-methoxy-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1369

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((5-methoxy-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1377

1-methyl-1-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1378

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((8-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1379

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((5-methyl-4,5,6,7- tetrahydrothiazolo[5,4-c]pyridin-2- yl)methyl)sulfonyl)phenyl)urea

H1380

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((2,3-dimethyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1381

1-methyl-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1382

1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1-(2- methoxyphenyl)ethyl)urea

H1383

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2- methoxyphenyl)-3-(1- phenylethyl)urea

H1384

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((6-methyl-4,5,6,7- tetrahydrothieno[2,3-c]pyridin-2- yl)methyl)sulfonyl)phenyl)urea

H1385

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((7-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1386

1-(2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1387

1-(2-methoxy-4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1388

1-(2-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1389

1-(2-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1-(2- fluorophenyl)ethyl)urea

H1390

1-(2-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1-(2- methoxyphenyl)ethyl)urea

H1391

1-(1-(2,6-difluorophenyl)ethyl)-3- (4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1392

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((7-methoxy-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfoyl)phenyl)urea

H1393

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2- methoxyphenyl)-3-(1-(2- methoxyphenyl)ethyl)urea

H1394

(R)-1-(4-(((7-fluoroisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1396

(R)-1-(4-(((4-fluoroisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1398

3-(4-((isoindolin-5- ylmethyl)sulfonyl)-2- methoxyphenyl)-1-methyl-1-(1- phenylethyl)urea

H1399

3-(2-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-methyl- 1-(1-phenylethyl)urea

H1400

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-fluoro-4-(((8-(trifluoromethyl)- 1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1401

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-fluoro-4-(((3-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1402

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-fluoro-4-(((3-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1- methylurea

H1403

1-((S)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((3-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1404

1-(2,6-difluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1405

1-(4-(((7-chloroisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1406

1-(4-(((3-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1407

1-(4-(((2,3-dimethyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1408

1-(5-((isoindolin-5- ylmethyl)sulfonyl)pyridin-2-yl)-3- (1-phenylethyl)urea

H1409

3-(4-(((4-fluoroisoindolin-5- yl)methyl)sulfonyl)phenyl)-1- methyl-1-(1-phenylethyl)urea

H1410

1-(1-(2,6-difluorophenyl)ethyl)-3- (4-(((4-fluoroisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1411

1-(1-(2,6-difluorophenyl)ethyl)-3- (2-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1412

1-(1-(2,6-difluorophenyl)ethyl)-3- (4-((isoindolin-5-ylmethyl)sulfonyl)- 2-methoxyphenyl)urea

H1413

3-(2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1- methyl-1-(1-phenylethyl)urea

H1414

3-(2-fluoro-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1- methyl-1-(1-phenylethyl)urea

H1415

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1416

1-benzyl-1-methyl-3-(4-(((3-methyl- 1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1417

(R)-1-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-3-(4-(((2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1420

1-(1-(2-fluorophenyl)ethyl)-3-(4- ((isoindolin-5-ylmethyl)sulfonyl)-2- methoxyphenyl)urea

H1421

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-((isoindolin-5-ylmethyl)sulfonyl)- 2-methoxyphenyl)urea

H1422

(R)-1-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-3-(2- methoxy-4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1423

(R)-1-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-3-(2-fluoro-4- (((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1424

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((8-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)urea

H1426

1-(1-(2-fluorophenyl)ethyl)-3-(2- methoxy-4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1427

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-methoxy-4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)urea

H1428

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-methoxy-4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1429

1-(1-(2,6-difluorophenyl)ethyl)-3- (4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1431

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((2,3-dimethyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)urea

H1436

1-(1-(2,6-difluorophenyl)ethyl)-3- (2-methoxy-4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1437

1-(1-(2,6-difluorophenyl)ethyl)-3- (2-methoxy-4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)urea

H1438

1-(2-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1-(2- methoxyphenyl)ethyl)urea

H1439

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((7-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)urea

H1440

1-(4-(((2,3-dimethyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)-3-(1- phenylethyl)urea

H1441

1-(2-methoxy-4-(((3-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1442

1-(2-methoxy-4-(((2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1-(4- methoxyphenyl)ethyl)urea

H1443

1-(1-(2,3-dichlorophenyl)ethyl)-3- (2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1- methylurea

H1444

1-(1-(3,4-dimethoxyphenyl)ethyl)-3- (4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1445

1-(1-(3,5-difluorophenyl)ethyl)-3- (4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1446

1-(1-(3,5-difluorophenyl)ethyl)-3- (4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1447

1-(2-methyl-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1448

1-(2-hydroxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1449

1-(1-(3,4-dimethoxyphenyl)ethyl)-3- (4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1450

1-(1-(2,6-dimethoxyphenyl)ethyl)-3- (4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1451

1-(1-(2,6-dimethoxyphenyl)ethyl)-3- (4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1454

1-(1-(2-fluoro-6- methoxyphenyl)ethyl)-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1455

1-(1-(2-fluoro-6- methoxyphenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1456

1-(2-chloro-4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1457

2-(3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)ureido-2- phenylacetamide

H1458

1-hydroxy-1-(4-(((2- methylisoindoIin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1459

methyl 5-((isoindolin-5- ylmethyl)sulfonyl)-2-(3-(1- phenylethyl)ureido)benzoate

H1460

3-(2-hydroxy-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-methyl- 1-(1-phenylethyl)urea

H1461

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-3- methoxyphenyl)-3-(1- phenylethyl)urea

H1462

1-(3-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1463

(S)-1-(4-(((5,6-dihydro-4H- pyrrolo[3,4-d]thiazol-2- yl)methyl)sulfonyl)-2- methoxyphenyl)-3-(1- phenylethyl)urea

H1464

(S)-1-(2-methoxy-4-(((5-methyl-5,6- dihydro-4H-pyrrolo[3,4-d]thiazol-2- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1465

(S)-1-(4-(((5,6-dihydro-4H- pyrrolo[3,4-d]thiazol-2- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1466

methyl 5-(((2-methylisoindolin-5- yl)methyl)sulfonyl)-2-(3-(1- phenylethyl)ureido)benzoate

H1467

1-(2-(hydroxymethyl)-4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1468

1-(2-(hydroxymethyl)-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1471

1-hydroxy-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1472

1-hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1473

1-hydroxy-1-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1474

3-(2-hydroxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1- methyl-1-(1-phenylethyl)urea

H1475

1-(1-(3-chloro-4- methoxyphenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1476

1-(1-(3-chloro-4- methoxyphenyl)ethyl)-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1477

1-(1-(3-chloro-4- methoxyphenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1478

1-(3-chloro-4-methoxybenzyl)-3-(4- (((2-methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1479

N-(isoindolin-5-yl)-4-(3-(1- phenylethyl)ureido)benzamide

H1480

N-(2-methylisoindolin-5-yl)-4-(3-(1- phenylethyl)ureido)benzamide

H1481

(R)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1482

(S)-1-(1-(2,3-dichlorophenyl)ethyl)- 3-(2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1484

1-(2-cyclopropyl-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1485

1-(2-bromo-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1486

5-((isoindolin-5-ylmethyl)sulfonyl)- 2-(3-(1-phenylethyl)ureido)benzoic acid

H1487

1-(3-hydroxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1490

1-(1-(2-fluorophenyl)ethyl)-1- hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1491

1-(1-(2-fluorophenyl)ethyl)-1- hydroxy-3-(4-(((2-methylisoindolin- 5-yl)methyl)sulfonyl)phenyl)urea

H1492

1-(3-fluoro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1493

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-3-methylphenyl)- 3-(1-phenylethyl)urea

H1494

1-(3-chloro-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1495

1-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)-2- methoxyphenyl)urea

H1496

1-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-3-(2-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1497

1-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-3-(2-methoxy-4-(((1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1498

1-hydroxy-3-(2-methoxy-4- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1499

5-((isoindolin-5-ylmethyl)sulfonyl)- N-methyl-2-(3-(1- phenylethyl)ureido)benzamide

H1500

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(oxazol-2- yl)phenyl)-3-(1-phenylethyl)urea

H1501

1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)-2-(oxazol-2- yl)phenyl)-3-(1-phenylethyl)urea

H1502

1-benzyl-1-hydroxy-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1503

1-benzyl-1-hydroxy-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1504

1-(3-bromo-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1505

methyl 2-((isoindolin-5- ylmethyl)sulfonyl)-5-(3-(1- phenylethyl)ureido)benzoate

H1506

1-(3-cyclopropyl-4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1507

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-3-(oxazol-2- yl)phenyl)-3-(1-phenylethyl)urea

H1508

1-(4-(((2-methylisoindolin-5- yl)methyl)sulfonyl)-3-(oxazol-2- yl)phenyl)-3-(1-phenylethyl)urea

H1509

1-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1510

1-(1-(2-fluorophenyl)ethyl)-1- hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)-3- methoxyphenyl)urea

H1511

1-(1-(2-fluorophenyl)ethyl)-1- hydroxy-3-(3-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)urea

H1512

1-(2-(2-hydroxypropan-2-yl)-4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1515

1-hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)-3- methoxyphenyl)-1-(1- phenylethyl)urea

H1516

1-hydroxy-3-(3-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1517

1-hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)-2- methoxyphenyl)-1-(1- phenylethyl)urea

H1518

1-hydroxy-3-(2-methoxy-4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1519

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(1H-pyrazol-3- yl)phenyl)-3-(1-phenylethyl)urea

H1520

1-(3-(hydroxymethyl)-4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1521

1-(1-(3-(difluoromethyl)-4- methylphenyl)ethyl)-3-(4- ((isoindolin-5- ylmethyl)sulfonyl)phenyl)urea

H1523

1-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-3-(2-methoxy-4-(((2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1524

1-hydroxy-3-(2-methoxy-4-(((3- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1525

1-hydroxy-3-(2-methoxy-4-(((2- methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1526

1-hydroxy-3-(4-((isoindolin-5- ylmethyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1527

1-hydroxy-3-(4-(((2- methylisoindolin-5- yl)methyl)sulfonyl)phenyl)-1-(1- phenylethyl)urea

H1528

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(1-methyl-1H- pyrazol-5-yl)phenyl)-3-(1- phenylethyl)urea

H1529

2-((isoindolin-5-ylmethyl)sulfonyl)- N-methyl-5-(3-1- phenylethyl)ureido)benzamide

H1530

2-((isoindolin-5-ylmethyl)sulfonyl)- 5-(3-(1-phenylethyl)ureido)benzoic acid

H1531

2-((isoindolin-5-ylmethyl)sulfonyl)- 5-(3-(1- phenylethyl)ureido)benzamide

H1532

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(1H-pyrazol-4- yl)phenyl)-3-(1-phenylethyl)urea

H1533

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(pyridin-3- yl)phenyl)-3-(1-phenylethyl)urea

H1534

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(pyridin-4- yl)phenyl)-3-(1-phenylethyl)urea

H1535

1-(4-((isoindolin-5- ylmethyl)sulfonyl)-2-(1-methyl-1H- pyrazol-4-yl)phenyl)-3-(1- phenylethyl)urea

H1537

1-((R)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((4-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1538

1-((R)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((4-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1539

1-(4-(((4-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-((R)- 1-phenylethyl)urea

H1540

1-(4-(((4-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-((R)- 1-phenylethyl)urea

H1541

2-(3-(1-phenylethyl)ureido)-5- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)benzoic acid

H1542

2-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-5- (((1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)benzoic acid

H1543

1-((R)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((4-fluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)urea

H1544

1-((R)-1-(2,3-dichlorophenyl)ethyl)- 3-(4-(((4-fluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)-2- methoxyphenyl)urea

H1545

1-(4-(((4,4-difluoro-1,2,3,4 tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1546

1-(4-(((4,4-difluoro-2-methyl- 1,2,3,4-tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)-3-(1- phenylethyl)urea

H1547

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((4,4-difluoro-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1548

1-(1-(2,3-dichlorophenyl)ethyl)-3- (4-(((4,4-difluoro-2-methyl-1,2,3,4- tetrahydroisoquinolin-6- yl)methyl)sulfonyl)phenyl)urea

H1549

2-(3-(1-(2,3- dichlorophenyl)ethyl)ureido)-5- ((isoindolin-5- ylmethyl)sulfonyl)benzoic acid.

34. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

35. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

36. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

37. The compound of claim 34 having the structure:

or a pharmaceutically acceptable thereof.

38. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

39. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

40. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

41. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

42. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

43. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

44. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

45. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

46. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

47. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

48. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

49. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

50. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

51. The compound of claim 34 having the structure:

or a pharmaceutically acceptable salt thereof.

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2023
From: HAMILTON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 064961/0567 →
SECURITY INTEREST Recorded Dec 30, 2022
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMILTON SA LLC
Reel/Frame 062254/0888 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 29, 2017
From: GIULIANO, CLAUDIO; DAINA, ANTOINE; PIETRA, CLAUDIO
To: HELSINN HEALTHCARE SA
Reel/Frame 041790/0608 →
Continuity (2)
Provisional Application 62311573 · Mar 22, 2016
Related Publication 20170275301A1 · Sep 28, 2017