IP Library Granted Patent US 10,618,912
Granted Patent B2
US 10,618,912 · App. 16/204,566 · Granted Apr 14, 2020

Diaryl macrocycles as modulators of protein kinases

Inventors: Jingrong Jean Cui (San Diego, CA); Yishan Li (San Diego, CA); Evan W. Rogers (San Diego, CA); Dayong Zhai (San Diego, CA)
Assignee: Turning Point Therapeutics, Inc.
C07D498/18C07B2200/13
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Quick Facts
Patent No.
US 10,618,912
App. No.
16/204,566
Granted
Apr 14, 2020
Kind
B2
Abstract

The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.

Claims (68)

1. A compound of the formula

wherein

Ring A′ is a monocyclic or bicyclic aryl or a heteroaryl; Ring B′ is of the formula

each L 1 and L 2 is independently —C(R 1′ )(R 2′ )—, —O—, —N(R k′ )—, —S—, —S(O)— or —S(O) 2 —;

each R 1′ and R 2′ is independently H, deuterium, halogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl, —OR a′ , —OC(O)R a′ , —OC(O)NR a′ R b′ , —OS(O)R a′ , —OS(O) 2 R a′ , —SR a′ , —S(O)R a′ , —S(O) 2 R a′ , —S(O)NR a′ R b′ , —S(O) 2 NR a′ R b′ , —OS(O)NR a′ R b′ , —OS(O) 2 NR a′ R b′ , —NR a′ R b′ , —NR a′ C(O)R b′ , —NR a′ C(O)OR b′ , —NR a′ C(O)NR a′ R b′ , —NR a′ S(O)R b′ , —NR a′ S(O) 2 R b′ , —NR a′ S(O)NR a′ R b′ , —NR a′ S(O) 2 NR a′ R b′ , —C(O)R a′ , —C(O)OR a′ , —C(O)NR a′ R b′ , —PR a′ R b′ , —P(O)R a′ R b′ , —P(O) 2 R a′ R b′ , —P(O)NR a′ R b′ , —P(O) 2 NR a′ R b′ , —P(O)OR a′ , —P(O) 2 OR a′ , —CN, or —NO 2 , or R 1′ and R 2′ taken together with the carbon or carbons to which they are attached form a C 3-6 cycloalkyl or a 4- to 6-membered heterocycloalkyl, wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, mono- or bicyclic heteroaryl, 4- to 6-membered heterocycloalkyl is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl, —OR e′ , —OC(O)R e′ , —OC(O)NR e′ R f′ , —OS(O)R e′ , —OS(O) 2 R e′ , —OS(O)NR e′ R f′ , —OS(O) 2 NR e′ R f′ , —SR e′ , —S(O)R e′ , —S(O) 2 R e′ , —S(O)NR e′ R f′ , —S(O) 2 NR e′ R f′ , —NR e′ R f′ , —NR e′ C(O)R f′ , —NR e′ C(O)OR f′ , —NR e′ C(O)NR e′ R f′ , —NR e′ S(O)R f′ , —NR e′ S(O) 2 R f′ , —NR e′ S(O)NR e′ R f′ , —NR e′ S(O) 2 NR e′ R f′ , —C(O)R e′ , —C(O)OR e′ , —C(O)NR e′ R f′ , —PR e′ R f′ , —P(O)R e′ R f′ , —P(O) 2 R e′ R f′ , —P(O)NR e′ R f′ , —P(O) 2 NR e′ R f′ , —P(O)OR e′ , —P(O) 2 OR e′ , —CN, or —NO 2 ;

each R k′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl, wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl, —OR e′ , —OC(O)R e′ , —OC(O)NR e′ R f′ , —OS(O)R e′ , —OS(O) 2 R e′ , —OS(O)NR e′ R f′ , —OS(O) 2 NR e′ R f′ , —SR e′ , —S(O)R e′ , —S(O) 2 R e′ , —S(O)NR e′ R f′ , —S(O) 2 NR e′ R f′ , —NR e′ R f′ , —NR e′ C(O)R f′ , —NR e′ C(O)OR f′ , —NR e′ C(O)NR e′ R f′ , —NR e′ S(O)R f′ , —NR e′ S(O) 2 R f′ , —NR e′ S(O)NR e′ R f′ , —NR e′ S(O) 2 NR e′ R f′ , —C(O)R e′ , —C(O)OR e′ , —C(O)NR e′ R f′ , —PR e′ R f′ , —P(O)R e′ R f′ , —P(O) 2 R e′ R f′ , —P(O)NR e′ R f′ , —P(O) 2 NR e′ R f′ , —P(O)OR e′ , —P(O) 2 OR e′ , —CN, or —NO 2 ;

each R 3′ and R 4′ is independently deuterium, halogen, —OR c′ , —OC(O)R c′ , —OC(O)NR c′ R d′ , —OC(═N)NR c′ R d′ , —OS(O)R c′ , —OS(O) 2 R c′ , —OS(O)NR c′ R d′ , —OS(O) 2 NR c′ R d′ , —SR c′ , —S(O)R c′ , —S(O) 2 R c′ , —S(O)NR c′ R d′ , —S(O) 2 NR c′ R d′ , —NR c′ R d′ , —NR c′ C(O)R d′ , —NR c′ C(O)OR d′ , —NR c′ C(O)NR c′ R d′ , —NR c′ C(═N)NR c′ R d′ , —NR c′ S(O)R d′ , —NR c′ S(O) 2 R d′ , —NR c′ S(O)NR c′ R d′ , —NR c′ S(O) 2 NR c′ R d′ , —C(O)R c′ , —C(O)OR c′ , —C(O)NR c′ R d′ , —C(═N)NR c′ R d′ , —PR c′ R d′ , —P(O)R c′ R d′ , —P(O) 2 R c′ R d′ , —P(O)NR c′ R d′ , —P(O) 2 NR c′ R d′ , —P(O)OR c′ , —P(O) 2 OR c′ , —CN, —NO 2 , C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl, or any two R 3′ groups or any two R 4′ groups taken together with the ring to which they are attached form a C 5-8 cycloalkyl or a 5- to 8-membered heterocycloalkyl, wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, mono- or bicyclic heteroaryl C 5-8 cycloalkyl or a 5- to 8-membered heterocycloalkyl is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl, —OR e′ , —OC(O)R e′ , —OC(O)NR e′ R f′ , —OS(O)R e′ , —OS(O) 2 R e′ , —OS(O)NR e′ R f′ , —OS(O) 2 NR e′ R f′ , —SR e′ , —S(O)R e′ , —S(O) 2 R e′ , —S(O)NR e′ R f′ , —S(O) 2 NR e′ R f′ , —NR e′ R f′ , —NR e′ C(O)R f′ , —NR e′ C(O)OR f′ , —NR e′ C(O)NR e′ R f′ , —NR e′ S(O)R f′ , —NR e′ S(O) 2 R f′ , —NR e′ S(O)NR e′ R f′ , —NR e′ S(O) 2 NR e′ R f′ , —C(O)R e′ , —C(O)OR e′ , —C(O)NR e′ R f′ , —PR e′ R f′ , —P(O)R e′ R f′ , —P(O) 2 R e′ R f′ , —P(O)NR e′ R f′ , —P(O) 2 NR e′ R f′ , —P(O)OR e′ , —P(O) 2 OR e′ , —CN, or —NO 2 ;

R 7′ is H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl, wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl is independently optionally substituted by deuterium, halogen, —OR i′ , —OC(O)R i′ , —OC(O)NR i′ R j′ , —OS(O)R i′ , —OS(O) 2 R i′ , —OS(O)NR i′ R j′ , —OS(O) 2 NR i′ R j′ , —SR i′ , —S(O)R i′ , —S(O) 2 R i′ , —S(O)NR i′ R j′ , —S(O) 2 NR i′ R j′ , —NR i′ R j′ , —NR i′ C(O)R j′ , —NR i′ C(O)OR j′ , —NR i′ C(O)NR i′ R j′ , —NR i′ S(O)R j′ , —NR i′ S(O) 2 R j′ , —NR i′ S(O)NR i′ R j′ , —NR i′ S(O) 2 NR i′ R j′ , —C(O)R i′ , —C(O)OR i′ , —C(O)NR i′ R j′ , —PR i′ R j′ , —P(O)R i′ R j′ , —P(O) 2 R i′ R j′ , —P(O)NR i′ R j′ , —P(O) 2 NR i′ R j′ , —P(O)OR i′ , —P(O) 2 OR i′ , —CN, or —NO 2 ;

each R a′ , R b′ , R c′ , R d′ , R e′ , R f′ , R i′ and R j′ is independently selected from the group consisting of H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, and heteroaryl;

m′ is 2, 3, 4, or 5;

n′ is 2, 3, or 4;

p′ is 0, 1, 2, 3, or 4; and

q′ is 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring A′ is monocyclic aryl or heteroaryl and Ring B′ is bicyclic heteroaryl.

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring A′ is phenyl or pyridyl.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring B′ is

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R 3′ is independently fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, —CN, or —CF 3 .

6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein each R 3′ is fluoro or chloro.

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 7′ is H or is methyl or ethyl, each unsubstituted or substituted with halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , cycloalkyl, or monocyclic heterocycloalkyl.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R k′ is independently H, methyl, ethyl, propyl, isopropyl, or cyclopropyl.

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein -(L 1 ) n′ — is —CH 2 CH 2 —, —CH 2 —S—, —CH 2 —SO 2 —, —SO 2 —N(C 1-4 alkyl)-, —SO 2 —NH—, —CH 2 —O—, —CH(C 1-4 alkyl)-O—, —CH(CH 2 F)—O—, —CH(C 3-6 cycloalkyl)-O—; —CH 2 NH—, —CH(C 1-4 alkyl)-NH—, —CH(C 1-4 alkylOH)-NH—, —CH(C 1-4 alkyl-C 3-6 cycloalkyl)-NH—, —CH 2 —N(C 1-4 alkyl)-, —CH 2 —N(C 3-6 cycloalkyl)-, —CH 2 —N(C 1-4 alkylOH)—, —CH(C 1-4 alkyl)-N(C 1-4 alkyl)-, —CH(CO 2 C 1-4 alkyl)-NH—, —CH(C(O)NH 2 )—NH—, —CH(CO 2 C 1-4 alkyl)-N(C 1-4 alkyl), —CH(C(O)NH 2 )—N(C 1-4 alkyl)-, —CH(C(O)NH(C 1-4 alkyl))-NH, —CH(C(O)NH(C 1-4 alkyl))-N(C 1-4 alkyl)-, —CH(C(O)N(C 1-4 alkyl) 2 )-NH—, or —CH(C(O)N(C 1-4 alkyl) 2 )-N(C 1-4 alkyl)-.

10. The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein -(L 2 ) m′ is —O—(C(R 1′ )(R 2′ )) 2 —, —O—(C(R 1′ )(R 2′ )) 3 —, —O—(CH 2 ) 2 —, —O—(CH 2 ) 3 —, —N(R k′ )—(C(R 1′ )(R 2′ )) 2 —, —N(R k′ )—(C(R 1′ )(R 2′ )) 3 —, —S—(C(R 1′ )(R 2′ )) 2 —, —S—(C(R 1′ )(R 2′ )) 3 —, —SO—(C(R 1′ )(R 2′ )) 2 —, —SO 2 —(C(R 1′ )(R 2′ )) 2 —, —SO 2 —(C(R 1′ )(R 2′ )) 3 —, —SO 2 —N(R k′ )—(C(R 1′ )(R 2′ )) 2 — or —(C(R 1′ )(R 2′ )) 3 —.

11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein m′ is 3, 4, or 5.

12. The compound of claim 11 , or a pharmaceutically acceptable salt thereof, wherein n′ is 2, 3 or 4.

13. The compound of claim 12 , or a pharmaceutically acceptable salt thereof, wherein p′ is 0, 1 or 2.

14. The compound of claim 13 , or a pharmaceutically acceptable salt thereof, wherein q′ is 0, 1 or 2.

15. A compound of the formula

wherein

M is CH or N;

X 1 and X 1′ are independently —C(R 1a )(R 2a )—, —S—, —S(O)—, —S(O) 2 —, —O— or —N(R k′ )—;

each R 1a and R 2a is independently H, deuterium, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, —C(O)OR a′ , —C(O)NR a′ R b′ , —NR a′ R b′ , —SR a′ , —S(O)R a′ , —S(O)NR a′ , —S(O) 2 R a′ , —S(O) 2 NR a′ or —OR a′ wherein each hydrogen atom in C 1-6 alkyl is independently optionally substituted by deuterium, halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , NHC(O)C 1-4 alkyl, —N(C 1-4 alkyl)C(O)C 1-4 alkyl, —NHC(O)NHC 1-4 alkyl, —N(C 1-4 alkyl)C(O)NHC 1-4 alkyl, —NHC(O)N(C 1-4 alkyl) 2 , —N(C 1-4 alkyl)C(O)N(C 1-4 alkyl) 2 , —NHC(O)OC 1-4 alkyl, —N(C 1-4 alkyl)C(O)OC 1-4 alkyl, —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —SC 1-4 alkyl, —S(O)C 1-4 alkyl, —S(O) 2 C 1-4 alkyl, —S(O)NH(C 1-4 alkyl), —S(O) 2 NH(C 1-4 alkyl), —S(O)N(C 1-4 alkyl) 2 , —S(O) 2 N(C 1-4 alkyl) 2 , C 3-6 cycloalkyl, or 3- to 7-membered heterocycloalkyl;

R 3a and R 3b are each independently H, deuterium, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, —CN, or —CF 3 ;

R 7a is H, C 1-6 alkyl or 3- to 7-membered heterocycloalkyl, wherein each hydrogen atom in C 1-6 alkyl or 3- to 7-membered heterocycloalkyl is independently optionally substituted by deuterium, halogen, —CN, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , cycloalkyl, or monocyclic heterocycloalkyl;

each R k′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl; wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl in R k′ is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl or —OR a′ ;

wherein each R a′ and R b′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or heteroaryl;

Z 3 is N, Z 7 is NH, and Z 1 , Z 2 , Z 4 , Z 5 , and Z 6 are each independently C(R x ), wherein each R x when present is independently H, deuterium, halogen, C 1-4 alkyl, —O—C 1-4 alkyl, —OH, —NH 2 , —NH(C 1-4 alkyl), —NH(phenyl), —NH(heteroaryl), CN, or —CF 3 ; and

m′ is 2 or 3;

or a pharmaceutically acceptable salt thereof.

16. A compound of the formula

wherein

M is CH or N;

X 1 and X 1′ are independently —C(R 1a )(R 2a )—, —S—, —S(O)—, —S(O) 2 —, —O— or —N(R k′ )—;

each R 1a and R 2a is independently H, deuterium, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, —C(O)OR a′ , —C(O)NR a′ R b′ , —NR a′ R b′ , —SR a′ , —S(O)R a′ , —S(O)NR a′ , —S(O) 2 R a′ , —S(O) 2 NR a′ or —OR a′ wherein each hydrogen atom in C 1-6 alkyl is independently optionally substituted by deuterium, halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , NHC(O)C 1-4 alkyl, —N(C 1-4 alkyl)C(O)C 1-4 alkyl, —NHC(O)NHC 1-4 alkyl, —N(C 1-4 alkyl)C(O)NHC 1-4 alkyl, —NHC(O)N(C 1-4 alkyl) 2 , —N(C 1-4 alkyl)C(O)N(C 1-4 alkyl) 2 , —NHC(O)OC 1-4 alkyl, —N(C 1-4 alkyl)C(O)OC 1-4 alkyl, —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —SC 1-4 alkyl, —S(O)C 1-4 alkyl, —S(O) 2 C 1-4 alkyl, —S(O)NH(C 1-4 alkyl), —S(O) 2 NH(C 1-4 alkyl), —S(O)N(C 1-4 alkyl) 2 , —S(O) 2 N(C 1-4 alkyl) 2 , C 3-6 cycloalkyl, or 3- to 7-membered heterocycloalkyl;

R 3a and R 3b are each independently H, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, —CN, or —CF 3 ;

R 7a is H, C 1-6 alkyl or 3- to 7-membered heterocycloalkyl, wherein each hydrogen atom in C 1-6 alkyl or 3- to 7-membered heterocycloalkyl is independently optionally substituted by halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , cycloalkyl, or monocyclic heterocycloalkyl;

each R k′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl; wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl in R k′ is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl or —OR a′ ;

wherein each R a′ and R b′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or heteroaryl;

Z 3 is N, Z 7 is NH, and Z 1 , Z 2 , Z 4 , Z 5 , and Z 6 are each independently C(R x ), wherein each R x when present is independently H, deuterium, halogen, C 1-4 alkyl, —O—C 1-4 alkyl, —OH, —NH 2 , —NH(C 1-4 alkyl), —NH(phenyl), —NH(heteroaryl), CN, or —CF 3 ; and

m′ is 2 or 3;

or a pharmaceutically acceptable salt thereof.

17. A compound selected from the group consisting of

wherein

M is CH or N;

X 1 and X 1′ are independently —C(R 1a )(R 2a )—, —S—, —S(O)—, —S(O) 2 —, —O— or —N(R k′ )—;

each R 1a and R 2a is independently H, deuterium, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, —C(O)OR a′ , —C(O)NR a′ R b′ , —NR a′ R b′ , —SR a′ , —S(O)R a′ , —S(O)NR a′ , —S(O) 2 R a′ , —S(O) 2 NR a′ or —OR a′ wherein each hydrogen atom in C 1-6 alkyl is independently optionally substituted by deuterium, halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , NHC(O)C 1-4 alkyl, —N(C 1-4 alkyl)C(O)C 1-4 alkyl, —NHC(O)NHC 1-4 alkyl, —N(C 1-4 alkyl)C(O)NHC 1-4 alkyl, —NHC(O)N(C 1-4 alkyl) 2 , —N(C 1-4 alkyl)C(O)N(C 1-4 alkyl) 2 , —NHC(O)OC 1-4 alkyl, —N(C 1-4 alkyl)C(O)OC 1-4 alkyl, —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , —SC 1-4 alkyl, —S(O)C 1-4 alkyl, —S(O) 2 C 1-4 alkyl, —S(O)NH(C 1-4 alkyl), —S(O) 2 NH(C 1-4 alkyl), —S(O)N(C 1-4 alkyl) 2 , —S(O) 2 N(C 1-4 alkyl) 2 , C 3-6 cycloalkyl, or 3- to 7-membered heterocycloalkyl;

R 3a and R 3b are each independently H, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, —CN, or —CF 3 ;

R 7a is H, C 1-6 alkyl or 3- to 7-membered heterocycloalkyl, wherein each hydrogen atom in C 1-6 alkyl or 3- to 7-membered heterocycloalkyl is independently optionally substituted by halogen, —OH, —OC 1-4 alkyl, —NH 2 , —NH(C 1-4 alkyl), —N(C 1-4 alkyl) 2 , —CO 2 H, —CO 2 C 1-4 alkyl, —CONH 2 , —CONH(C 1-4 alkyl), —CON(C 1-4 alkyl) 2 , cycloalkyl, or monocyclic heterocycloalkyl;

each R k′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl; wherein each hydrogen atom in C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or mono- or bicyclic heteroaryl in R k′ is independently optionally substituted by deuterium, halogen, C 1-6 alkyl, C 1-6 haloalkyl or —OR a′ ;

wherein each R a′ and R b′ is independently H, deuterium, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, 3- to 7-membered heterocycloalkyl, C 6-10 aryl, or heteroaryl;

Z 3 is N, Z 7 is NH, and Z 1 , Z 2 , Z 4 , Z 5 , and Z 6 are each independently C(R x ), wherein each R x when present is independently H, deuterium, halogen, C 1-4 alkyl, —O—C 1-4 alkyl, —OH, —NH 2 , —NH(C 1-4 alkyl), —NH(phenyl), —NH(heteroaryl), CN, or —CF 3 ; and

m′ is 2 or 3;

or a pharmaceutically acceptable salt thereof.

18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from the group consisting of

(13R)-12-chloro-11-fluoro-5,13-dimethyl-6,7-dihydro-2H,13H-1,15-(azenometheno)pyrrolo[3,4-f][1,10,4]benzodioxazacyclotridecin-4(5H)-one;

12-chloro-11-fluoro-5,13-dimethyl-6,7-dihydro-2H,13H-1,15-(azenometheno)pyrrolo[3,4-f][1,10,4]benzodioxazacyclotridecin-4(5H)-one; and

12-chloro-11-fluoro-5,14-dimethyl-6,7,13,14-tetrahydro-2H-1,15-(azenometheno)pyrrolo[3,4-f][1,4,10]benzoxadiazacyclotridecin-4(5H)-one.

19. A pharmaceutical composition comprising (a) at least one compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and (b) at least one pharmaceutically acceptable excipient.

Assignments (1)
CHANGE OF NAME Recorded Aug 19, 2019
From: TP THERAPEUTICS, INC.
To: TURNING POINT THERAPEUTICS, INC.
Reel/Frame 050084/0756 →
Continuity (6)
Continuation 15609962 · May 31, 2017
Continuation 15113583
Provisional Application 62106301 · Jan 22, 2015
Provisional Application 62049326 · Sep 11, 2014
Provisional Application 61931506 · Jan 24, 2014
Related Publication 20190169207A1 · Jun 6, 2019
Cited By (4)
US 50,634 US 12,351,572 US 12,404,281 US 12,679,850