US 11,078,207 B2 · Substituted pyrrolo[2,3-d]pyrimidines as HER2 inhibitors

Abstract

Provided are a novel pyrimidine compound that inhibits HER2 activity and exhibits brain penetration properties, or a salt thereof, and a pharmaceutical composition comprising the same. A compound represented by the following formula (I), or a salt thereof: wherein R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having 1 to 5 C1-C4 alkoxy groups or fluorine atoms each as a substituent(s), or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having 1 to 5 fluorine atoms as a substituent(s); R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having 1 to 3 substituents selected from fluorine atoms and chlorine atoms.

Claims19

Dependent claims

A compound represented by formula (I):

or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
wherein:
R1 represents C1-C4 alkyl or C3-C4 cycloalkyl, wherein the C1-C4 alkyl is optionally substituted with 1 OC1—C4 alkyl substituent;
R2 represents hydrogen, halogen, C1-C6 alkyl, or OC1—C6 alkyl, wherein the C1-C6 alkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of fluoro and OC1—C4 alkyl;
R3 represents hydrogen or C1-C4 alkyl, wherein the C1-C4 alkyl is optionally substituted with 1, 2, 3, 4, or 5 fluoro substituents;
R4 represents hydrogen or C1-C4 alkyl;
and
R5 represents phenyl, wherein the phenyl is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of fluoro and chloro.

5 more elements

Dependencies are inferred from the claim text.

Substituted pyrrolo[2,3-d]pyrimidines as HER2 inhibitors

Life of this patent

Substituted pyrrolo[2,3-d]pyrimidines as HER2 inhibitors

Life of this patent

Abstract

Claims19