Novel fused pyrimidine compound or salt thereof
AssigneeTaiho Pharmaceutical Co., Ltd.
InventorsIsao MIYAZAKI, Tadashi SHIMAMURA, Masanori KATO, Hidenori FUJITA, Satoru IGUCHI
Life of this patent
Estimating the term…
Abstract
The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.
Claims8
A method of inhibiting RET comprising administering a compound represented by Formula (I) below or a salt thereof to a mammal:
- wherein in Formula (I), A is
- wherein R1 is selected from the group consisting of
- halogen,
- cyano,
- nitro,
- substituted or unsubstituted C1-C6 alkyl,
- substituted or unsubstituted C1-C6 alkoxy,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C2-C6 alkynyl,
- substituted or unsubstituted amino, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur,
- Y is N or CH, and
- n is an integer of 0 to 2,
- wherein when n is 2, the two R1 may be identical or different from each other;
- in Formula A2, the group:
- forms, together with phenyl or pyridinyl to which this group is bonded, polycyclic C8-C14 aromatic hydrocarbon or an 8- to 14-membered polycyclic unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur;
- R2 is selected from the group consisting of
- substituted or unsubstituted C3-C10 alkyl,
- substituted or unsubstituted C3-C7 cycloalkyl,
- substituted or unsubstituted C4-C12 bridged cycloalkyl,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C3-C7 cycloalkenyl, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic saturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur,
- provided that when each group represented by R2 has a substituent, the substituent must not be a substituted or unsubstituted saturated heterocyclic group that may have at least one identical or different heteroatom selected from oxygen and sulfur, and has at least one nitrogen atom;
- and
- X is
- N or
- CR3, wherein R3 is selected from the group consisting of
- hydrogen,
- halogen,
- cyano,
- nitro,
- substituted or unsubstituted C1-C6 alkyl,
- substituted or unsubstituted C1-C6 alkoxy,
- substituted or unsubstituted C1-C6 alkylthio,
- substituted or unsubstituted C3-C7 cycloalkyl,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C2-C6 alkynyl,
- substituted or unsubstituted amino,
- substituted or unsubstituted carbamoyl,
- substituted or unsubstituted C6-C14 aromatic hydrocarbon, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic saturated or unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur.
A method for treating a malignant tumor comprising administering a compound represented by Formula (I) below or a salt thereof to a mammal:
- wherein in Formula (I), A is
- wherein R1 is selected from the group consisting of
- halogen,
- cyano,
- nitro,
- substituted or unsubstituted C1-C6 alkyl,
- substituted or unsubstituted C1-C6 alkoxy,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C2-C6 alkynyl,
- substituted or unsubstituted amino, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur,
- Y is N or CH, and
- n is an integer of 0 to 2,
- wherein when n is 2, the two R1 may be identical or different from each other;
- in Formula A2, the group:
- forms, together with phenyl or pyridinyl to which this group is bonded, polycyclic C8-C14 aromatic hydrocarbon or an 8- to 14-membered polycyclic unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur;
- R2 is selected from the group consisting of
- substituted or unsubstituted C3-C10 alkyl,
- substituted or unsubstituted C3-C7 cycloalkyl,
- substituted or unsubstituted C4-C12 bridged cycloalkyl,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C3-C7 cycloalkenyl, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic saturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur,
- provided that when each group represented by R2 has a substituent, the substituent must not be a substituted or unsubstituted saturated heterocyclic group that may have at least one identical or different heteroatom selected from oxygen and sulfur, and has
- at least one nitrogen atom;
- and
- X is
- N or
- CR3, wherein R3 is selected from the group consisting of
- hydrogen,
- halogen,
- cyano,
- nitro,
- substituted or unsubstituted C1-C6 alkyl,
- substituted or unsubstituted C1-C6 alkoxy,
- substituted or unsubstituted C1-C6 alkylthio,
- substituted or unsubstituted C3-C7 cycloalkyl,
- substituted or unsubstituted C2-C6 alkenyl,
- substituted or unsubstituted C2-C6 alkynyl,
- substituted or unsubstituted amino,
- substituted or unsubstituted carbamoyl,
- substituted or unsubstituted C6-C14 aromatic hydrocarbon, and
- a substituted or unsubstituted 4- to 10-membered monocyclic or polycyclic saturated or unsaturated heterocyclic group containing 1 to 3 identical or different heteroatoms selected from nitrogen, oxygen, and sulfur.
Dependencies are inferred from the claim text.