IP Library Granted Patent US 9,493,482
Granted Patent B2
US 9,493,482 · App. 15/017,472 · Granted Nov 15, 2016

Compounds and methods for preventing or treating sensory hair cell death

Inventors: Julian Simon (Seattle, WA); Graham Johnson (Sanbornton, NH); Edwin Rubel (Seattle, WA); David Raible (Seattle, WA); Mario D. Gonzalez (Winchester, MA); Peter C. Meltzer (Lexington, MA); Weishi Miao (Winchester, MA)
Assignees: University of Washington; Oricula Therapeutics LLC; Fred Hutchinson Cancer Research Center
C07D495/18A61K31/439A61K31/7036
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Quick Facts
Patent No.
US 9,493,482
App. No.
15/017,472
Granted
Nov 15, 2016
Kind
B2
Abstract

Disclosed herein are compounds, and pharmaceutical compositions that include such compounds, for preventing or treating hearing loss. The compounds and pharmaceutical compositions described herein prevent or treat hair cell death. In addition, the compounds and pharmaceutical compositions described herein protect against kidney damage in an individual receiving an aminoglycoside antibiotic. Methods of using the compounds, alone or in combination with other therapeutic agents, are also disclosed.

Claims (26)

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

Formula (I);

wherein:

R 1 is aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted with one or more R 4 ;

R 2 is H, C 1 -C 6 alkyl, C 1 -C 6 alkyl-OR 6 , C 1 -C 6 alkylC 3 -C 6 cycloalkyl, C 1 -C 6 alkylC 2 -C 7 heterocycloalkyl, C 1 -C 6 alkyl-CO 2 R 6 , optionally substituted C 1 -C 6 alkylaryl, or optionally substituted C 1 -C 6 alkylheteroaryl;

each R 4 is independently selected from F, Cl, Br, I, —CN, —NO 2 , —CF 3 , —OR 9 , —OCF 3 ,—NR 8 R 9 , —C(O)R 10 , —CO 2 R 9 , —C(O)NR 8 R 9 , —N(R 8 )C(O)R 10 , —N(R 8 )CO 2 R 10 , —NHS(O) 2 R 10 , —S(O) 2 NR 8 R 9 , C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 6 heteroalkyl, C 1 -C 6 haloalkyl, C 2 -C 7 heterocycloalkyl, aryl, and heteroaryl;

R 6 is H, or C 1 -C 6 alkyl;

R 8 is H, or C 1 -C 6 alkyl;

R 9 is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 2 -C 7 heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkylaryl, or C 1 -C 6 alkylheteroaryl;

R 10 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 2 -C 7 heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkylaryl, or C 1 -C 6 alkylheteroaryl;

R 11 is H, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 6 cycloalkyl, C 2 -C 7 heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkylC 3 -C 6 cycloalkyl, C 1 -C 6 alkylaryl, or C 1 -C 6 alkylheteroaryl; and

R 12 is H, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 6 cycloalkyl, C 2 -C 7 heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkylC 3 -C 6 cycloalkyl, C 1 -C 6 alkylaryl, or C 1 -C 6 alkylheteroaryl; or R 11 and R 12 together with the nitrogen to which they are attached form an optionally substituted C 2 -C 7 heterocycloalkyl ring;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein R 11 and R 12 are each H.

3. The compound of claim 2 wherein R 1 is aryl optionally substituted with one or more R 4 .

4. The compound of claim 3 wherein R 1 is phenyl optionally substituted with one or more R 4 .

5. The compound of claim 4 wherein R 1 is phenyl substituted with one or more R 4 , wherein each R 4 is independently selected from F, Cl, Br, I, —CN, —NO 2 , —CF 3 , —OR 9 , —OCF 3 , —NR 8 R 9 , —C(O)R 10 , —CO 2 R 9 , C 1 -C 6 alkyl, and C 1 -C 6 haloalkyl.

6. The compound of claim 5 wherein R 1 is phenyl substituted with one R 4 , wherein R 4 is selected from F, Cl, Br, I, —CN, —CF 3 , —OR 9 , —OCF 3 , —C(O)R 10 , —CO 2 R 9 , and C 1 -C 6 alkyl.

7. The compound of claim 6 wherein R 1 is 4-chlorophenyl.

8. The compound of claim 7 wherein R 2 is H.

9. The compound of claim 7 wherein R 2 is C 1 -C 6 alkyl.

10. The compound of claim 9 wherein R 2 is —CH 3 .

11. The compound of claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

13. The pharmaceutical composition of claim 12 further comprising an aminoglycoside antibiotic.

Assignments (5)
MERGER AND CHANGE OF NAME Recorded Jun 8, 2022
From: FRED HUTCHINSON CANCER RESEARCH CENTER; SEATTLE CANCER CARE ALLIANCE
To: FRED HUTCHINSON CANCER CENTER
Reel/Frame 060838/0852 →
CONFIRMATORY LICENSE Recorded Jan 23, 2017
From: UNIVERSITY OF WASHINGTON
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 041061/0181 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 17, 2016
From: SIMON, JULIAN
To: FRED HUTCHINSON CANCER RESEARCH CENTER
Reel/Frame 038944/0912 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 17, 2016
From: GONZALEZ, MARIO D.; MELTZER, PETER C.; MIAO, WEISHI; JOHNSON, GRAHAM
To: ORICULA THERAPEUTICS LLC
Reel/Frame 039072/0192 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 17, 2016
From: RUBEL, EDWIN W.; RAIBLE, DAVID W.
To: UNIVERSITY OF WASHINGTON
Reel/Frame 039072/0205 →
Continuity (2)
Provisional Application 62113245 · Feb 6, 2015
Related Publication 20160229869A1 · Aug 11, 2016