IP Library Granted Patent US 8,470,860
Granted Patent B2
US 8,470,860 · App. 12/841,355 · Granted Jun 25, 2013

Phenyl-sulfamates as aromatase inhibitors

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,470,860
App. No.
12/841,355
Granted
Jun 25, 2013
Kind
B2
Abstract

There is provided a compound of Formula I wherein X, Y and Z are each independently of each other an optional linker group; R 1 is a ring system; R 2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO 2 ) and halogens; R 3 and R 4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.

Claims (39)

1. A compound of Formula I

wherein

X is a bond;

Y is (CH 2 ) m ,

wherein m is an integer from 1 to 6;

Z is a bond;

R 1 is selected from 4H-1,2,4-triazole 1H-1,2,4-triazole, and 1H-1,2,3-triazole;

R 2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO 2 ) and halogens;

R 3 and R 4 are independently selected from H and hydrocarbyl; and

ring A and B are independently optionally further substituted.

2. A compound according to claim 1 of Formula II

or of Formula III

or of Formula IV

or of Formula V

or of Formula VI

or of Formula VII

or of Formula VIII or Formula VIIIa

or of Formula VIII

3. A compound according to claim 1 wherein at least one of the optional linker groups is present.

4. A compound according to claim 1 wherein Y is —CH 2 —.

5. A compound according to claim 1 wherein R 1 is 1H-1,2,4-triazole.

6. A compound according to claim 1 wherein R 1 is

7. A compound according to claim 1 wherein R 2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO 2 ) and halogens, wherein the hydrocarbyl group is a straight of branched alkyl group.

8. A compound according to claim 7 wherein the hydrocarbyl group is a straight chain alkyl group.

9. A compound according to claim 7 wherein the hydrocarbyl group is (CH 2 )qCH 3 , wherein q is an integer from 0 to 6.

10. A compound according to claim 1 wherein R 2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO 2 ) and halogens, wherein the oxyhydrocarbyl group is —O-alkyl-, wherein alkyl is a straight or branched alkyl group.

11. A compound according to claim 10 wherein the oxyhydrocarbyl group is —O-alkyl-, wherein alkyl is a straight chain alkyl group.

12. A compound according to claim 11 wherein the oxyhydrocarbyl group is —O(CH) r CH 3 , wherein r is an integer from 0 to 6.

13. A compound according to claim 1 wherein R 2 is selected from —CH 3 , —OCH 3 , cyano (—CN), nitro (—NO 2 ) and halogens.

14. A compound according to claim 1 wherein R 3 and R 4 are independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl or optionally contain one or more hetero atoms or groups.

15. A compound according to claim 1 wherein at least one of R 3 and R 4 is H.

16. A compound according to claim 1 wherein R 3 is H and R 4 is H.

17. A compound according to claim 1 wherein rings A and B are independently not further substituted.

18. A compound according to claim 1 wherein neither ring A nor ring B is further substituted.

19. A compound according to claim 1 wherein rings A and B are independently further substituted by groups selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO 2 ) and halogens.

20. A compound according to claim 1 wherein rings A and B are independently further substituted by groups selected from C 1-6 alkyl groups, C 1-6 alkoxy groups, cyano (—CN), nitro (—NO 2 ) and halogens.

21. A compound according to claim 1 wherein rings A and B arc independently further substituted by groups selected from —CH 3 , —CH 2 CH 3 , —OCH 3 , cyano (—CN), nitro (—NO 2 ) and halogens.

22. A compound according to claim 1 with the following chemical structure:

23. A pharmaceutical composition comprising the compound according to claim 1 optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant.

Assignments (1)
CHANGE OF NAME Recorded Aug 2, 2016
From: ISIS INNOVATION LIMITED
To: OXFORD UNIVERSITY INNOVATION LIMITED
Reel/Frame 039550/0045 →