IP Library Granted Patent US 11,008,309
Granted Patent B2
US 11,008,309 · App. 16/507,927 · Granted May 18, 2021

Substituted benzofuranyl and benzoxazolyl compounds and uses thereof

Inventors: Erkan Baloglu (Stoneham, MA); Sharon Shacham (Newton, MA); William Senapedis (Millis, MA); Dilara McCauley (Arlington, MA); Yosef Landesman (Brookline, MA); Gali Golan (Mesilat Zion, IL); Ori Kalid (Pardes Hanna, IL); Sharon Shechter (Andover, MA)
Assignee: Karyopharm Therapeutics Inc.
C07D405/14C07D307/81C07D405/12C07D409/14C07D413/12C07D413/14C07D417/12C07D491/048C07D491/08
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Quick Facts
Patent No.
US 11,008,309
App. No.
16/507,927
Granted
May 18, 2021
Kind
B2
Abstract

The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula A: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula A, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

Claims (43)

1. A compound represented by Structural Formula IX:

or a pharmaceutically acceptable salt thereof, wherein:

m″ is 1 or 2;

R 1a is halogen, halo(C 1 -C 4 )alkyl, (C 1 -C 4 )alkyl, —O—(C 1 -C 4 )alkyl, —O-halo(C 1 -C 4 )alkyl, optionally substituted (C 5 -C 15 )aryl or optionally substituted (C 5 -C 15 )heteroaryl;

Z 5 is —N— or —C(H)—;

R 20 is (C 1 -C 4 )alkyl, (C 1 -C 4 )haloalkyl, —O—(C 0 -C 4 alkylene)carbocyclyl, —O—(C 0 -C 4 alkylene)heterocyclyl, —C(H)(OH)-carbocyclyl, —C(H)(OH)-heterocyclyl, —C(H)(CH 3 )-carbocyclyl, —C(H)(CH 3 )-heterocyclyl, —C(O)(C 1 -C 4 )alkyl, —C(S)(C 1 -C 4 )alkyl, —C(O)(C 0 -C 4 alkylene)NR 11 R 12 , —C(S)(C 0 -C 4 alkylene)NR 11 R 12 , —S(O) 2 (C 1 -C 4 )alkyl, —S(O) 2 NR 11 R 12 or —C(O)NR 13 NR 11 R 12 , wherein:

R 11 and R 12 are each independently hydrogen, optionally substituted C 1 -C 4 alkyl, optionally substituted carbocyclyl, or optionally substituted heterocyclyl; or

R 11 and R 12 are taken together with the nitrogen atom to which they are commonly attached to form an optionally substituted heterocyclyl; and

R 13 is hydrogen or optionally substituted (C 1 -C 4 )alkyl;

each R 21 , if present, is independently halo; and

q is 0, 1, 2, 3 or 4.

2. The compound of claim 1 , represented by Structural Formula XII:

or a pharmaceutically acceptable salt thereof, wherein:

each of Z 6 and Z 7 is independently —N— or —C(H)—, wherein no more than one of Z 6 and Z 7 is nitrogen;

each R 22 , if present, is independently halo, cyano, (C 1 -C 3 )alkyl, halo(C 1 -C 3 )alkyl, hydroxy, (C 1 -C 3 )alkoxy or halo(C 1 -C 3 )alkoxy; and

q′ is 0, 1, 2 or 3.

3. The compound of claim 1 , wherein q is 0, 1 or 2.

4. The compound of claim 1 , wherein R 21 , for each occurrence and if present, is fluoro.

5. The compound of claim 1 , wherein R 20 is —C(O)(C 0 -C 4 alkylene)NR 11 R 12 or —C(S)(C 0 -C 4 alkylene)NR 11 R 12 , wherein R 11 and R 12 are taken together with the nitrogen atom to which they are commonly attached to form an optionally substituted (C 3 -C 7 )heterocyclyl having 1 or 2 heteroatoms independently selected from nitrogen, oxygen and sulfur.

6. The compound of claim 1 , wherein the heterocyclyl formed by R 11 and R 12 taken together with the nitrogen atom to which they are commonly attached is optionally substituted with 1, 2, 3 or 4 substituents independently selected from halo, hydroxyl, halo(C 1 -C 3 )alkyl, (C 1 -C 3 )alkyl and (C 1 -C 3 )alkoxy.

7. The compound of claim 1 , wherein Z 5 is —C(H)—.

8. The compound of claim 1 , wherein Z 5 is —N—.

9. The compound of claim 1 , represented by Structural Formula X:

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , wherein the heterocyclyl formed by R 11 and R 12 taken together with the nitrogen atom to which they are commonly attached is optionally substituted with 1 or 2 substituents independently selected from halo, (C 1 -C 3 )alkyl, halo(C 1 -C 3 )alkyl, hydroxy, (C 1 -C 3 )alkoxy and halo(C 1 -C 3 )alkoxy.

11. The compound of claim 1 , wherein the carbocyclyl or heterocyclyl of R 1a is optionally substituted with 1, 2 or 3 substituents independently selected from halo, cyano, (C 1 -C 3 )alkyl, halo(C 1 -C 3 )alkyl, hydroxy, (C 1 -C 3 )alkoxy and halo(C 1 -C 3 )alkoxy.

12. The compound of claim 9 , represented by Structural Formula XI:

or a pharmaceutically acceptable salt thereof, wherein:

each of Z 6 and Z 7 is independently —N— or —C(H)—, wherein no more than one of Z 6 and Z 7 is nitrogen;

each R 22 , if present, is independently halo, cyano, (C 1 -C 3 )alkyl, halo(C 1 -C 3 )alkyl, hydroxy, (C 1 -C 3 )alkoxy or halo(C 1 -C 3 )alkoxy; and

q′ is 0, 1, 2 or 3.

13. A compound, represented by any one of the following structural formulas:

or a pharmaceutically acceptable salt thereof.

14. A pharmaceutical composition comprising:

(a) a compound of claim 1 , or a pharmaceutically acceptable salt thereof; and

(b) a pharmaceutically acceptable carrier.

15. A method of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of claim 14 .

16. The method of claim 15 , wherein the cancer is lymphoma.

17. The method of claim 15 , wherein the cancer is cervical cancer.

18. The method of claim 15 , wherein the cancer is mantle cell lymphoma.

19. A method of treating a PAK-mediated disorder in a subject in need thereof, comprising administering to the subject in need thereof a therapeutically effective amount of a compound of claim 1 , wherein the PAK-mediated disorder is cancer, a neurodegenerative disease or an immune system disease.

20. A compound represented by any one of the following structural formulas:

or a pharmaceutically acceptable salt thereof.

Assignments (6)
RELEASE OF SECURITY INTEREST IN PATENTS AT REEL/FRAME NO. 67396/0532 Recorded Oct 14, 2025
From: WILMINGTON SAVINGS FUND SOCIETY, FSB, AS AGENT
To: KARYOPHARM THERAPEUTICS INC.
Reel/Frame 073111/0142 →
PATENT SECURITY AGREEMENT Recorded Oct 10, 2025
From: KARYOPHARM THERAPEUTICS INC.
To: WILMINGTON SAVINGS FUND SOCIETY, FSB, AS COLLATERAL TRUSTEE
Reel/Frame 073058/0504 →
SECOND LIEN PATENT SECURITY AGREEMENT Recorded May 13, 2024
From: KARYOPHARM THERAPEUTICS INC.
To: WILMINGTON SAVINGS FUND SOCIETY, FSB
Reel/Frame 067396/0532 →
SECURITY INTEREST Recorded May 8, 2024
From: KARYOPHARM THERAPEUTICS INC.
To: WILMINGTON SAVINGS FUND SOCIETY, FSB
Reel/Frame 067345/0255 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2020
From: BALOGLU, ERKAN; SHACHAM, SHARON; SENAPEDIS, WILLIAM; MCCAULEY, DILARA; LANDESMAN, YOSEF; GOLAN, GALI; KALID, ORI; SHECHTER, SHARON
To: KARYOPHARM THERAPEUTICS INC.
Reel/Frame 053523/0811 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 24, 2019
From: BALOGLU, ERKAN; SHACHAM, SHARON; SENAPEDIS, WILLIAM; MCCAULEY, DILARA; LANDESMAN, YOSEF; GOLAN, GALI; KALID, ORI; SHECHTER, SHARON
To: KARYOPHARM THERAPEUTICS INC.
Reel/Frame 051416/0055 →