IP Library Patent Application 17747754
Patent Application
App. No. 17/747,754

THERAPEUTIC COMPOUNDS AND USES THEREOF

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Quick Facts
Patent No.
US None
App. No.
17/747,754
Abstract

Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.

Claims (73)

1 . A method of treating an ocular disease in an eye of a subject in need thereof, comprising injecting a compound to the eye, wherein the compound is:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is H or optionally substituted C 1-6 alkyl;

R 2 is optionally substituted bicyclic heterocyclyl having 1 or 2 heteroatoms;

X is a bond, —O—, or —C(═O)—;

Y is CH;

R 3 is optionally substituted heteroaryl; and

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

2 . The method of claim 1 , wherein the ocular disease is a growth factor-associated disorder.

3 . The method of claim 2 , wherein the growth factor is vascular endothelial growth factor.

4 . (canceled)

5 . (canceled)

6 . (canceled)

7 . The method of claim 1 , wherein R 1 is CH 3 .

8 . The method of claim 1 , wherein R 2 is

wherein p, q, s, and t are independently 0, 1, 2, 3, or 4.

9 . The method of claim 1 , wherein X is a bond or —C(═O)—.

10 . (canceled)

11 . The method of claim 1 , wherein n is 1 or 2

12 . (canceled)

13 . The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof,

wherein:

each instance of R 4 is independently H, optionally substituted C 1-6 alkyl, F, Cl, Br, I, CN, OH, or alkoxy;

R 5 is H or a nitrogen protecting group; and

m is 0, 1, 2, 3, 4, or 5.

14 . The method of claim 13 , wherein at least one instance of R 4 is CH 3 , F, or H.

15 . (canceled)

16 . (canceled)

17 . (canceled)

18 . The method of claim 1 , wherein R 2 is

19 . (canceled)

20 . (canceled)

21 . The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

22 . A method of inhibiting growth factor signaling in a cell, comprising contacting the cell with an effective amount of a compound, wherein the compound is:

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is H or optionally substituted C 1-6 alkyl;

R 2 is optionally substituted bicyclic heterocyclyl having 1 or 2 heteroatoms;

X is a bond, —O—, or —C(═O)—;

Y is CH;

R 3 is optionally substituted heteroaryl; and

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

23 . (canceled)

24 . (canceled)

25 . (canceled)

26 . The method of claim 22 , wherein R 1 is CH 3 .

27 . The method of claim 22 , wherein R 2 is

wherein p, q, s, and t are independently 0, 1, 2, 3, or 4.

28 . The method of claim 22 , wherein X is a bond or —C(═O)—.

29 . (canceled)

30 . The method of claim 22 , wherein n is 1 or 2.

31 . (canceled)

32 . The method of claim 22 , wherein the compound is:

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 is H or optionally substituted C 1-6 alkyl;

R 2 is optionally substituted bicyclic heterocyclyl having 1 or 2 heteroatoms;

X is a bond, —O—, or —C(═O)—;

each instance of R 4 is independently H, optionally substituted C 1-6 alkyl, F, Cl, Br, I, CN, OH, or alkoxy;

R 5 is H or a nitrogen protecting group;

m is 0, 1, 2, 3, 4, or 5; and

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

33 . The method of claim 32 , wherein at least one instance of R 4 is CH 3 , F, or H.

34 . (canceled)

35 . (canceled)

36 . (canceled)

37 . The method of claim 22 , wherein R 2 is

38 . (canceled)

39 . (canceled)

40 . The method of claim 22 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

41 .- 63 . (canceled)

Assignments (4)
FIRST AMENDMENT TO IP SECURITY AGREEMENT Recorded Dec 22, 2022
From: KALA PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC
Reel/Frame 062205/0883 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2022
From: ASKEW, BEN C.
To: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
Reel/Frame 059950/0997 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2022
From: BREAKTHROUGH CHEMISTRY ADVISORS, LLC
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 059951/0038 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2022
From: ONG, WINSTON ZAPANTA; NOWAK, PAWEL WOJCIECH; KIM, JINSOO
To: KALA PHARMACEUTICALS, INC.
Reel/Frame 059951/0073 →