发明名称 CYCLIC AMIDE DERIVATIVE
摘要 [Problem];To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like.;[Means of Solving the Problem];A compound of Formula (III):;(where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; his 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A′″ is a benzene ring, a pyridine ring; ring B′ is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups),a salt of the compound, or a solvate of the salt or the compound.
申请公布号 US2015266839(A1) 申请公布日期 2015.09.24
申请号 US201514729979 申请日期 2015.06.03
申请人 MOCHIDA PHARMACEUTICAL CO.., LTD. 发明人 OKANO Akihiro;OHKOUCHI Munetaka;MAKABE Muneyoshi
分类号 C07D275/03;C07D417/12;A61K31/4439;A61K45/06;A61K31/549;C07D279/02;A61K31/541;A61K31/4985;A61K31/425;C07D285/16 主分类号 C07D275/03
代理机构 代理人
主权项 1. A compound of Formula (III): (where n is an integer of 0 to 2; p is an integer of 0 to 4; h is an integer of 0 to 3; j is an integer of 0 to 3; k is an integer of 0 to 2; J1a is —CR11a- or a nitrogen atom; J2 is —CR12aR12b— or —NR12c— (with the proviso that when J1a is a nitrogen atom, h is 0); X is an oxygen atom, a sulfur atom, or —NR7—; a ring B′ is a benzene ring, a pyridine ring, or a pyrimidine ring; f is an integer of 0 to 2; g is an integer of 1 to 4; q1 is an integer of 0 to 3; q2 is 0 or 1; r1 is an integer of 0 to 2 (with the proviso that q1+q2+r1 is an integer of 0 to 5); a ring A′″ is a benzene ring or a pyridine ring; T is —CH2—, an oxygen atom, —S(O)i— (i is an integer of 0 to 2), or a group optionally selected from a —NR7— group; R1s are independently a group optionally selected from a halogen atom, a C1-6 alkyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-6 alkenyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-6 alkynyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C1-6 alkoxy group that is optionally substituted with 1 to 5 substituent(s) RI, and a cyano group; R2a and R2b are independently a group optionally selected from a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkoxy group, and a cyano group; R3, R4, R5, R6, and R7 are independently a group optionally selected from a hydrogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C2-6 alkenyl group, and a C2-6 alkynyl group; R11as are independently a group optionally selected from a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C2-7 alkanoyl group, and a carboxy group that is optionally protected; R12a and R12b are independently a group optionally selected from a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, and a cyano group; R12cs are independently a group optionally selected from a hydrogen atom, a C1-6 alkyl group, and a halogenated C1-6 alkyl group; R13s are independently a group optionally selected from a halogen atom, —OH, a cyano group, a C1-10 alkyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-10 alkenyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-10 alkynyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C1-10 alkoxy group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-10 alkenyloxy group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-10 alkynyloxy group that is optionally substituted with 1 to 5 substituent(s) RI, —SH, a —S(O)iRa (i is an integer of 0 to 2) group, and a —NRbRc group; R13a is a group optionally selected from an aryl group that is optionally substituted with 1 to 5 substituent(s) RII, a heterocyclic group that is optionally substituted with 1 to 5 substituent(s) RII, an aralkyl group that is optionally substituted with 1 to 5 substituent(s) RII, a heteroarylalkyl group that is optionally substituted with 1 to 5 substituent(s) RII, a non-aromatic heterocyclic alkyl group that is optionally substituted with 1 to 5 substituent(s) RII, an aryloxy group that is optionally substituted with 1 to 5 substituent(s) RII, a heteroaryloxy group that is optionally substituted with 1 to 5 substituent(s) RII, a non-aromatic heterocyclic oxy group that is optionally substituted with 1 to 5 substituent(s) RII, an aralkyloxy group that is optionally substituted with 1 to 5 substituent(s) RII, a heteroarylalkyloxy group that is optionally substituted with 1 to 5 substituent(s) RII, and a substituted spiropiperidinylmethyl group; R14s are independently a group optionally selected from a halogen atom, —OH, a cyano group, a C1-6 alkyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-6 alkenyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C2-6 alkynyl group that is optionally substituted with 1 to 5 substituent(s) RI, a C1-6 alkoxy group that is optionally substituted with 1 to 5 substituent(s) RI, —SH, a —S(O)iRa (i is an integer of 0 to 2) group, and a —NRbRc group; Ra is a C1-6 alkyl group or a halogenated C1-6 alkyl group; Rb and Rc are independently a group optionally selected from a hydrogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C2-7 alkanoyl group (the alkanoyl group is optionally substituted with —OH or a C1-6 alkoxy group), a C1-6 alkylsulfonyl group, an arylcarbonyl group, and a heterocyclic carbonyl group, where Rb and Rc optionally form together with a nitrogen atom to which Rb and Rc are bonded, a 3- to 8-membered cyclic group, where in the cyclic group, one or two carbon atom(s) is(are) optionally substituted with an atom optionally selected from an oxygen atom, a sulfur atom, and a nitrogen atom (the nitrogen atom is optionally substituted with a C1-6 alkyl group that is optionally substituted with 1 to 5 substituent(s) RI) or with a carbonyl group, and the cyclic group is further optionally substituted with 1 to 5 substituent(s) RII; the substituents RI are optionally the same as or different from each other and are each a group optionally selected from a halogen atom, —OH, a cyano group, a C1-6 alkoxy group (the C1-6 alkoxy group is optionally substituted with 1 to 5 halogen atom(s), 1 to 5 —OH, 1 to 5 C1-6 alkoxy group(s), 1 to 5 aryl group(s) (the aryl group is optionally substituted with 1 to 3 halogen atom(s)), 1 to 5 heterocyclic group(s) (the heterocyclic group is optionally substituted with 1 to 3 C1-6 alkyl group(s) or 1 to 3 oxo group(s)), 1 to 5 —S(O)iRa (i is an integer of 0 to 2) group(s), 1 to 5 —SO2NRdRe group(s), 1 to 5 —CONRdRe group(s), or 1 to 5 —NRb1Rc1 group(s)), a —NRb1Rc1 group, and a heterocyclic oxy group (the heterocyclic oxy group is optionally substituted with 1 to 3 C1-6 alkyl group(s) or 1 to 3 oxo group(s)); the substituents RII are optionally the same as or different from each other and are each a group optionally selected from the substituents RI, a C1-6 alkyl group (the C1-6 alkyl group is optionally substituted with 1 to 5 halogen atom(s), 1 to 5 —OH, 1 to 5 C1-6 alkoxy group(s), 1 to 5 —S(O)iRa (i is an integer of 0 to 2) group(s), 1 to 5 —NRb1Rc1 group(s), 1 to 5 —SO2NRdRe group(s), or 1 to 5 —CONRdRe group(s)), a C2-6 alkenyl group, a C2-7 alkanoyl group, an aralkyloxy group, a heterocyclic group (the heterocyclic group is optionally substituted with 1 to 3 C1-6 alkyl group(s) or 1 to 3 oxo group(s)), a heterocyclic carbonyl group (the heterocyclic carbonyl group is optionally substituted with 1 to 3 C1-6 alkyl group(s) or 1 to 3 oxo group(s)), a —S(O)iRa (i is an integer of 0 to 2) group, a —CONRdRe group, and a —CONRdRe1 group; Rd and Re are independently a hydrogen atom or a C1-6 alkyl group (the C1-6 alkyl group is optionally substituted with 1 to 5 halogen atom(s), 1 to 5 —OH, or 1 to 5 C1-6 alkoxy group(s)); Re1 is a C1-6 alkyl group (the C1-6 alkyl group is optionally substituted with 1 to 5 —OH, 1 to 5 C1-6 alkoxy group(s), 1 to 5 aryl group(s) (the aryl group is optionally substituted with 1 to 3 halogen atom(s)), 1 to 5 heterocyclic group(s) (the heterocyclic group is optionally substituted with 1 to 3 C1-6 alkyl group(s) or 1 to 3 oxo group(s)), 1 to 5 —S(O)iRa (i is an integer of 0 to 2) group(s), 1 to 5 —SO2NRdRe group(s), 1 to 5 —CONRdRe group(s), or 1 to 5 —NRb1Rc1 group(s)); and Rb1 and Rc1 are independently a group optionally selected from a hydrogen atom, a C1-6 alkyl group, a C2-7 alkanoyl group, and a C1-6 alkylsulfonyl group, where Rb1 and Rc1 optionally form together with a nitrogen atom to which Rb1 and Rc1 are bonded, a 3- to 8-membered cyclic group, where in the cyclic group, one or two carbon atom(s) is(are) optionally substituted with an atom optionally selected from an oxygen atom, a sulfur atom, and a nitrogen atom (the nitrogen atom is optionally substituted with a C1-6 alkyl group) or with a carbonyl group), or a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable solvate of the compound, or a pharmaceutically acceptable solvate of the salt.
地址 Tokyo JP