IP Library Granted Patent US 10,703,722
Granted Patent B2
US 10,703,722 · App. 14/805,292 · Granted Jul 7, 2020

Compounds that modulate intracellular calcium

Inventors: Jeffrey P. Whitten (Santee, CA); Yazhong Pei (San Diego, CA); Jianguo Cao (San Diego, CA); Zhijun Wang (San Diego, CA); Evan Rogers (San Diego, CA); Brian Dyck (San Diego, CA); Jonathan Grey (San Diego, CA)
Assignee: CALCIMEDICA, INC.
C07D213/74C07D213/75C07D401/04C07D405/04C07D405/14C07D409/14C07D413/04C07D413/14C07D417/04C07D417/14C07D471/04
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Quick Facts
Patent No.
US 10,703,722
App. No.
14/805,292
Granted
Jul 7, 2020
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 (31)

1. A method of alleviating, abating, or ameliorating the symptoms of rheumatoid arthritis, asthma, psoriasis, arthritis, ulcerative colitis, rejection of skin transplant, or renal transplantation in a mammal comprising administering to the mammal a compound or pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof having the structure of Formula (VIA):

wherein:

R′ 1 is

L 2 is —NH—C(═O)—, or —C(═O)NH—;

X is CR 3 or N;

Y is independently selected from CR 9 or N;

R 2 is C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 8 heterocycloalkyl, C 1 -C 4 alkyleneC 2 -C 8 heterocycloalkyl, aryl, heteroaryl, fused aryl or fused heteroaryl; wherein C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 8 heterocycloalkyl, C 1 -C 4 alkyleneC 2 -C 8 heterocycloalkyl, 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 , C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 1 -C 6 heteroalkyl, C 1 -C 6 haloalkyl, C 2 -C 8 heterocycloalkyl, optionally substituted aryl, optionally substituted O-aryl, optionally substituted heteroaryl,

n is an integer selected from 0-2;

R 9 is independently selected from halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, —OR 5 , —OCF 3 , C 1 -C 6 carbonylalkyl, or —CF 3 ; or two R 9 attached to the same carbon atom form an oxetane ring;

R 10 is selected from halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, —OR 5 , —OCF 3 , C 1 -C 6 carbonylalkyl, or —CF 3 ; and

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

2. The method of claim 1 wherein R′ 1 is

L 2 is —NH—C(═O)—, or —C(═O)NH—;

X is CR 3 ;

Y is CR 9 ; and

R 2 is aryl optionally substituted with at least one R 3 .

3. The method of claim 2 wherein aryl is phenyl.

4. The method of claim 3 wherein phenyl is substituted with at least one R 3 selected from Cl, Br, F, I, CF 3 , C 1 -C 6 alkyl, or OC 1 -C 6 alkyl.

5. The method of claim 4 wherein C 1 -C 6 alkyl is methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, or tert-butyl.

6. The method of claim 4 wherein phenyl is substituted with at least one R 3 selected from Cl, Br, F, and I.

7. The method of claim 4 wherein phenyl is substituted with at least one F.

8. The method of claim 2 wherein R 10 is a halogen.

9. The method of claim 1 wherein R 2 is heteroaryl substituted with at least one R 3 .

10. The method of claim 9 wherein heteroaryl is selected from pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, thienyl, furyl, pyranyl, thiadiazolyl, pyrazolyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, indolyl, indazolyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, benzimidazolyl, quinolyl, pteridinyl, pyrazolopyridinyl, pyrazolopyrimidinyl, imidazolothiazolyl, quinoxazinyl, and indolizinyl.

11. The method of claim 10 wherein heteroaryl is pyridyl.

12. The method of claim 9 wherein heteroaryl is substituted with at least one R 3 selected from Cl, Br, F, I, CF 3 , C 1 -C 6 alkyl, or OC 1 -C 6 alkyl.

13. The method of claim 12 wherein heteroaryl is substituted with at least one R 3 selected from Cl, Br, F, and I.

14. The method of claim 13 wherein heteroaryl is substituted with at least one F.

15. The method of claim 1 wherein the compound is selected from

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

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 Aug 1, 2015
From: WHITTEN, JEFFREY P.; PEI, YAZHONG; CAO, JIANGUO; WANG, ZHIJUN; ROGERS, EVAN; DYCK, BRIAN; GREY, JONATHAN
To: CALCIMEDICA, INC.
Reel/Frame 036233/0727 →
Continuity (9)
Continuation 13969401 · Aug 16, 2013
Division 13085324 · Apr 12, 2011
Provisional Application 61439786 · Feb 4, 2011
Provisional Application 61430894 · Jan 7, 2011
Provisional Application 61422088 · Dec 10, 2010
Provisional Application 61407819 · Oct 28, 2010
Provisional Application 61377825 · Aug 27, 2010
Provisional Application 61328569 · Apr 27, 2010
Related Publication 20150322012A1 · Nov 12, 2015
Cited By (3)
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