8-substituted isoquinoline derivative and the use thereof
AssigneeAsahi Kasei Pharma Corporation
InventorsShunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
Life of this patent
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Abstract
The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKKβ inhibiting activity and the like and is useful for the prevention and/or treatment of IKKβ-associated diseases or symptoms and the like.
Claims53
A compound represented by the following formula (1) or a salt thereof:
- wherein
- D1 represents a single bond, —N(R11)—, —O—, —S—, —S(O)—, or —S(O)2—, wherein R11 represents a hydrogen atom or an alkyl group that may be substituted;
- A1 represents a single bond, an alkylene that may be substituted, or any of divalent groups selected from the following formulas (1a-1) to (1a-6):
- wherein
- n1 is an integer of 0, 1, or 2;
- n2 is an integer of 2 or 3;
- n3 is an integer of 1 or 2;
- R12 and R13 may be identical to or different from each other and each independently represents a hydrogen atom, a hydroxyl group, or an alkyl group that may be substituted;
- X1 represents —N(R14)—, —O—, or —S—, wherein R14 represents a hydrogen atom or an alkyl group that may be substituted;
- v represents a bond with D1;
- and
- w represents a bond with D2
- D2 represents a single bond, an alkylene that may be substituted, —C(O)—, —C(S)—, —S(O)2, —C(O)—N(R15), —C(S)—N(R15)—, or -EC(O)—, wherein E represents an alkylene that may be substituted and R15 represents a hydrogen atom or an alkyl group;
- R1 represents a hydrogen atom, an alkyl group that may be substituted, an amino group that may be substituted, a saturated heterocyclic group that may be substituted, an aryl group that may be substituted, an aralkyl group that may be substituted, a carbamimidoyl group, or any of groups selected from the following formulas (1b-1) to (1b-4):
- wherein
- m1 is an integer of 0, 1, or 2;
- m2 is an integer of 1 or 2;
- m3 is an integer of 0, 1, or 2;
- X2 represents —N(R14)—, —O—, or —S—, wherein R14 represents a hydrogen atom or an alkyl group that may be substituted;
- D11 represents an alkylene that may be substituted;
- D12 represents a single bond, an alkylene that may be substituted, —C(O)—, —S(O)2—, or —C(O)—N(R15)—,wherein R15 represents a hydrogen atom or an alkyl group;
- R16, R18 and R19 may be identical to or different from one another and each independently represents a hydrogen atom or an alkyl group that may be substituted;
- R17 represents a hydrogen atom, an alkyl group that may be substituted, an aryl group that may be substituted, or an aralkyl group that may be substituted;
- and
- x represents a bond with D2;
- with the proviso that, when R17 represents a hydrogen atom, D12 represents a single bond;
- with the proviso that,
- when D1 represents a single bond, A1 represents a divalent group represented by the above -mentioned formula (1a-5) or (1a-6);
- when D1 represents —N(R11)—, —O—, —S—, —S(O)—, or —S(O)2, A1 represents a single bond, an alkylene that may be substituted, or any of divalent groups selected from the formulas (1a-1) to (1a-4), wherein, when A1 represents a single bond, D2 represents an alkylene that may be substituted or -E-C(O)—;
- when R1 represents an amino group that may be substituted, D2 represents an alkylene that may be substituted or -E-C(O)—;
- and
- D3 represents a single bond, —N(R21)—, —O—, —N(R21)—C(O)—, or —S—, wherein R21 represents a hydrogen atom or an alkyl group that may be substituted;
- and
- R2 represents an alkyl group that may be substituted or the following formula (2a-1):
- wherein
- Q represents an aryl group that may be substituted;
- and
- y represents a bond with D3;
- and
- R23, R24, and R25 may be identical to or different from one another and each independently represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group that may be substituted, an alkoxy group that may be substituted, an amino group that may be substituted, an aryl group that may be substituted, an aryloxy group that may be substituted, an aralkyl group that may be substituted, or the following formula (2b-I):
- wherein
- D21 represents a single bond or an alkylene that may be substituted;
- D22 represents a single bond, an alkylene that may be substituted, —C(O)—, —S(O)2—, or —C(O)—N(R28)—;
- R26, R27, and R28 may be identical to or different from one another and each independently represents a hydrogen atom or an alkyl group that may be substituted;
- and
- z represents a bond with Q;
- with the provisos that:
- when D22 represents a single bond, R27 represents a hydrogen atom;
- and
- when D3 is —O—, R2 is methyl, D1 is —O—, and A1 and D2 represent a single bond, R1 is not a methyl group.
A compound selected from the following groups or a salt thereof:
A compound selected from the following groups or a salt thereof:
Dependencies are inferred from the claim text.