Pyrazolo[3,4-d]pyrimidine compound or salt thereof
AssigneeTaiho Pharmaceutical Co., Ltd.
InventorsYuichi Kawai, Hiroki Irie, Takeshi Sagara, Kazutaka Miyadera
Life of this patent
Estimating the term…
Abstract
To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect. The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, Z3, Z4, W, n, R1, R2, and R3 have meanings as defined in the present specification, or a salt thereof.
Claims21
A method for inhibiting HER2, comprising administering an effective amount of a compound of formula (I) or a salt thereof to a subject in need thereof:
- wherein X represents an optionally substituted 4- to 10-membered nitrogen-containing saturated heterocyclic group;
- Y represents —C(R4)═C(R5)(R6);
- Z1, Z2, Z3, and Z4 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, an optionally substituted amino group, an optionally substituted C3-C7 cycloalkyl group, a C6-C14 aromatic hydrocarbon group, or a 4- to 14-membered unsaturated heterocyclic group, or Z1 and Z2, or Z3 and Z4 optionally form, together with the respective carbon atoms bonded thereto, a benzene ring or a 5- to 7-membered saturated or unsaturated heterocyclic ring;
- W represents —CH2—, an oxygen atom, or —NH—;
- n represents an integer of from 0 to 2;
- R1 represents an optionally substituted amino group;
- R2 and R3 are the same as or different from each other and each represent a hydrogen atom, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C6-C14 aromatic hydrocarbon group, or R2 and R3 optionally form, together with the nitrogen atom bonded thereto, an optionally substituted 4- to 8-membered nitrogen-containing saturated heterocyclic group;
- and
- R4, R5, and R6 are the same as or different from each other and each represent a hydrogen atom or an optionally substituted C1-C6 alkyl group.
A method for treating a tumor, comprising administering an effective amount of a compound of formula (I) or a salt thereof to a subject in need thereof:
- wherein X represents an optionally substituted 4- to 10-membered nitrogen-containing saturated heterocyclic group;
- Y represents —C(R4)═C(R5)(R6);
- Z1, Z2, Z3, and Z4 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, an optionally substituted amino group, an optionally substituted C3-C7 cycloalkyl group, a C6-C14 aromatic hydrocarbon group, or a 4- to 14-membered unsaturated heterocyclic group, or Z1 and Z2, or Z3 and Z4 optionally form, together with the respective carbon atoms bonded thereto, a benzene ring or a 5- to 7-membered saturated or unsaturated heterocyclic ring;
- W represents —CH2—, an oxygen atom, or —NH—;
- n represents an integer of from 0 to 2;
- R1 represents an optionally substituted amino group;
- R2 and R3 are the same as or different from each other and each represent a hydrogen atom, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C6-C14 aromatic hydrocarbon group, or R2 and R3 optionally form, together with the nitrogen atom bonded thereto, an optionally substituted 4- to 8-membered nitrogen-containing saturated heterocyclic group;
- and
- R4, R5, and R6 are the same as or different from each other and each represent a hydrogen atom or an optionally substituted C1-C6 alkyl group.
A method for treating a tumor having HER2 overexpression, HER2 gene amplification, or HER2 mutation, comprising administering an effective amount of a compound of formula (I) or a salt thereof to a subject in need thereof:
- wherein X represents an optionally substituted 4- to 10-membered nitrogen-containing saturated heterocyclic group;
- Y represents —C(R4)═C(R5)(R6);
- Z1, Z2, Z3, and Z4 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, an optionally substituted amino group, an optionally substituted C3-C7 cycloalkyl group, a C6-C14 aromatic hydrocarbon group, or a 4- to 14-membered unsaturated heterocyclic group, or Z1 and Z2, or Z3 and Z4 optionally form, together with the respective carbon atoms bonded thereto, a benzene ring or a 5- to 7-membered saturated or unsaturated heterocyclic ring;
- W represents —CH2—, an oxygen atom, or —NH—;
- n represents an integer of from 0 to 2;
- R1 represents an optionally substituted amino group;
- R2 and R3 are the same as or different from each other and each represent a hydrogen atom, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C6-C14 aromatic hydrocarbon group, or R2 and R3 optionally form, together with the nitrogen atom bonded thereto, an optionally substituted 4- to 8-membered nitrogen-containing saturated heterocyclic group;
- and
- R4, R5, and R6 are the same as or different from each other and each represent a hydrogen atom or an optionally substituted C1-C6 alkyl group.
Dependencies are inferred from the claim text.