IP Library Granted Patent US 9,079,891
Granted Patent B2
US 9,079,891 · App. 13/219,393 · Granted Jul 14, 2015

Compounds that modulate intracellular calcium

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Quick Facts
Patent No.
US 9,079,891
App. No.
13/219,393
Granted
Jul 14, 2015
Kind
B2
Abstract

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Claims (24)

1. A compound having the structure of Formula (I):

wherein:

R 1 is

X is S, O, or NR 5 ;

Y is independently selected from CR 10 or N;

R 2 is aryl, heteroaryl, fused aryl or fused heteroaryl; wherein aryl, heteroaryl, fused aryl or fused heteroaryl is optionally substituted with at least one R 3 ;

R 3 is independently selected from H, F, D, Cl, Br, I, —CN, —NO 2 , —OH, —CF 3 , —OCF 3 , —OR 5 , optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted C 1 -C 6 heteroalkyl, C 1 -C 6 haloalkyl, optionally substituted C 2 -C 8 heterocycloalkyl, optionally substituted aryl, optionally substituted O-aryl, and optionally substituted heteroaryl;

R 5 is selected from H, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 8 cycloalkyl, phenyl, and benzyl;

R 9 and R 10 are each independently selected from H, D, optionally substituted C 1 -C 6 alkyl, halogen, C 1 -C 6 alkylcarbonyl, or CF 3 ;

R 12 is selected from CN, —OR 5 , optionally substituted C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, and optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl, optionally substituted O-aryl, and optionally substituted heteroaryl;

or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.

2. The compound of claim 1 wherein R 2 is phenyl.

3. The compound of claim 2 wherein phenyl is substituted with at least one R 3 independently selected from F, Cl, Br, and I.

4. The compound of claim 1 wherein R 2 is heteroaryl.

5. The compound of claim 4 wherein heteroaryl is pyridyl.

6. The compound of claim 5 wherein pyridyl is substituted with at least one R 3 independently selected from F and Cl.

7. The compound of claim 1 wherein R 1 is

8. The compound of claim 7 wherein R 5 is C 1 -C 6 alkyl; and R 12 is CF 3 .

9. A compound selected from:

or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.

10. A pharmaceutical composition comprising a pharmaceutically acceptable diluent, excipient or binder, and a compound of claim 1 or a pharmaceutically acceptable salt, pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate thereof.

11. The compound of claim 8 wherein R 2 is phenyl substituted with at least one R 3 independently selected from F, Cl, and Br.

12. The compound of claim 11 wherein R 2 is phenyl substituted with two R 3 and each R 3 is F.

13. The compound of claim 11 wherein R 2 is phenyl is substituted with three R 3 and each R 3 is F.

Assignments (2)
SECURITY INTEREST Recorded Mar 4, 2025
From: CALCIMEDICA, INC.
To: AVENUE CAPITAL MANAGEMENT II, L.P.
Reel/Frame 070394/0314 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 4, 2011
From: WHITTEN, JEFFREY P.; PEI, YAZHONG; CAO, JIANGUO; WANG, ZHIJUN; ROGERS, EVAN; DYCK, BRIAN; GREY, JONATHAN
To: CALCIMEDICA, INC.
Reel/Frame 027179/0586 →