IP Library › Granted Patent US 11,420,935
Granted Patent B2
US 11,420,935 · App. 16/849,728 · Granted Aug 23, 2022

Bicyclic compounds

Inventors: Andrei W. Konradi (Burlingame, CA); Tracy Tzu-Ling Tang Lin (Redwood City, CA)
Assignee: VIVACE THERAPEUTICS, INC.
C07C235/66C07C255/24C07C311/51C07D213/40C07D213/61C07D213/73C07D217/24C07D217/26C07D233/64C07D241/12C07D257/04C07D305/06C07D305/08C07D333/70C07D401/12C07C2601/02C07C2601/04
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Quick Facts
Patent No.
US 11,420,935
App. No.
16/849,728
Granted
Aug 23, 2022
Kind
B2
Abstract

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating deseases, such as cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Claims (26)

1. A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof:

wherein,

X 1 is CR X ; and each X 2 and X 3 is CR Y ;

each X 4 , X 5 , and X 6 , is independently N or CR X ;

each R X is independently hydrogen, halogen, nitro, —OR 3 , —SR 3 , —CN, —C(═O)R 3 , —C(═O)N(R 3 ) 2 , —C(═O)OR 3 , —S(═O)R 3 , —S(═O) 2 R 3 , —N(R 3 ) 2 , —NR 3 S(═O) 2 R 3 , —NR 3 C(═O)R 3 , —NR 3 C(═O)OR 3 , substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 2 -C 4 alkenyl, substituted or unsubstituted C 2 -C 4 alkynyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted C 3 -C 10 cycloalkyl, substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

each R Y is independently hydrogen, halogen, nitro, —CN, —C(═O)R 3 , —C(═O)N(R 3 ) 2 , —C(═O)OR 3 , —S(═O)R 3 , —S(═O) 2 R 3 , —N(R 3 ) 2 , —NR 3 S(═O) 2 R 3 , —NR 3 C(═O)R 3 , —NR 3 C(═O)OR 3 , substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 2 -C 4 alkenyl, substituted or unsubstituted C 2 -C 4 alkynyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted C 3 -C 10 cycloalkyl, substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R is halogen, nitro, —CN, —OR 3 , —SR 3 , —C(═O)R 3 , —C(═O)N(R 3 ) 2 , —C(═O)OR 3 , —S(═O)R 3 , —S(═O) 2 R 3 , —N(R 3 ) 2 , —NR 3 S(═O) 2 R 3 , —NR 3 C(═O)R 3 , —NR 3 C(═O)OR 3 , or substituted or unsubstituted C 1 -C 6 fluoroalkyl;

R 1 is C 1 -C 6 alkyl substituted with —OR 3 ; and R 3 is hydrogen, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, or substituted or unsubstituted C 3 -C 10 cycloalkyl;

each R 2 is independently halogen, nitro, —N 3 , —CN, —OR 3 , —SR 3 , —S(═O) 2 R 3 , —N(R 3 ) 2 , —C(═O)OR 3 , substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted C 3 -C 10 cycloalkyl, substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

each R 3 is independently hydrogen, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted C 1 -C 6 fluoroalkyl, substituted or unsubstituted C 1 -C 6 heteroalkyl, substituted or unsubstituted C 3 -C 10 cycloalkyl, substituted or unsubstituted C 2 -C 10 heterocycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; or if two R 3 are on the same nitrogen atom, then two R 3 are taken together with the nitrogen atom to which they are attached to form a substituted or unsubstituted C 3 -C 7 heterocycloalkyl; and

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

2. The compound or pharmaceutically acceptable salt or solvate thereof of claim 1 , wherein:

R is —CF 3 ; and

n is 0.

3. The compound or pharmaceutically acceptable salt or solvate thereof of claim 1 , wherein:

each X 4 , X 5 , and X 6 is CR X ;

or X 4 is N; and each X 5 and X 6 is CR X ;

or X 4 and X 5 is CR X ; and X 6 is N;

each R X is independently hydrogen, F, Cl, Br, —CH 3 , —OH, —OCH 3 , or —OCF 3 ; and

each R Y is hydrogen.

4. The compound or pharmaceutically acceptable salt or solvate thereof of claim 3 , wherein:

R 1 is C 1 -C 6 alkyl substituted with —OR 3 ; and R 3 is hydrogen or unsubstituted C 1 -C 6 alkyl;

R is —CF 3 ; and

n is 0.

5. The compound or pharmaceutically acceptable salt or solvate thereof of claim 1 , wherein the compound has one of the following structures:

pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 25, 2020
From: KONRADI, ANDREI W.; LIN, TRACY TZU-LING TANG
To: VIVACE THERAPEUTICS, INC.
Reel/Frame 053594/0797 →
Continuity (2)
Provisional Application 62834671 · Apr 16, 2019
Related Publication 20200347009A1 · Nov 5, 2020