IP Library Granted Patent US 11,905,248
Granted Patent B2
US 11,905,248 · App. 16/653,475 · Granted Feb 20, 2024

Compounds that modulate intracellular calcium

Inventors: Jeffrey P. Whitten (La Jolla, CA); Yazhong Pei (La Jolla, CA); Jianguo Cao (La Jolla, CA); Zhijun Wang (La Jolla, CA); Evan Rogers (La Jolla, CA); Brian Dyck (La Jolla, CA); Jonathan Grey (La Jolla, CA)
Assignee: CALCIMEDICA, INC.
C07D213/74A61K9/0014A61K9/0019A61K9/0031A61K9/0048A61K9/0056A61K9/0078A61K9/0095A61K9/02A61K9/06A61K9/2018A61K9/2054A61K9/2059A61K31/00A61K47/02A61K47/10A61K47/12A61K47/14A61K47/20A61K47/38C07D213/75C07D241/20C07D401/04C07D405/04C07D405/14C07D409/04C07D409/14C07D413/04C07D413/14C07D417/04C07D417/14C07D471/04C07D493/10C07D495/04
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Quick Facts
Patent No.
US 11,905,248
App. No.
16/653,475
Granted
Feb 20, 2024
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 (34)

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

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 heteroalkyl, 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 heteroalkyl, 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 H, D, 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 ;

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;

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

2. The compound 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 compound of claim 2 wherein aryl is phenyl.

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

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

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

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

10. The compound 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 compound of claim 10 wherein heteroaryl is pyridyl.

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

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

15. A compound selected from

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

16. The compound of claim 1 having the structure of Formula (VIA):

17. A pharmaceutical composition comprising a pharmaceutically acceptable diluent, excipient or binder, and a compound of claim 1 or pharmaceutically acceptable salt, pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate 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 Oct 16, 2019
From: WHITTEN, JEFFREY P.; PEI, YAZHONG; CAO, JIANGUO; WANG, ZHIJUN; ROGERS, EVAN; DYCK, BRIAN; GREY, JONATHAN
To: CALCIMEDICA, INC.
Reel/Frame 050733/0438 →