发明名称 AZAINDOLE DERIVATIVE
摘要 Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis.;An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same:;;where R1 to R4, m and n have the same meanings as those defined in the description.
申请公布号 US2016340353(A1) 申请公布日期 2016.11.24
申请号 US201515112070 申请日期 2015.02.04
申请人 TAIHO PHARMACEUTICAL CO., LTD. 发明人 NAKAMURA Masayuki;YAMANAKA Hiroyoshi;SHIBATA Kazuaki;MITSUYA Morihiro;HARADA Takafumi
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of the formula (I): wherein R1 represents an optionally substituted C4-C10 cycloalkyl group, an optionally substituted C4-C10 cycloalkenyl group, an optionally substituted C4-C10 cycloalkynyl group, an optionally substituted C6-C14 aromatic hydrocarbon group, or an optionally substituted 4- to 10-membered saturated or unsaturated heterocyclic group;R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a nitro group, —C(═O)Rx, —C(═O)ORx, —C(═O)N(Rx)(Ry), —N(Rx)(Ry), —NRxC(═O)Ry, —NRxS(═O)2Ry, —NRxC(═O)ORy, —NRxC(═O)N(Ry)(Rz), —NRxS(═O)2N(Ry)(Rz), —OC(═O)Rx, —OC(═O)ORx, —OC(═O)N(Rx)(Ry), —SRx, —S(═O)2Rx, —S(═O)2ORx, an optionally Rb-substituted C1-C6 alkyl group, an optionally Rb-substituted C2-C6 alkenyl group, an optionally Rb-substituted C2-C6 alkynyl group, an optionally Rb-substituted C1-C6 alkoxy group, an optionally Rc-substituted C3-C10 cycloalkyl group, an optionally Rc-substituted C6-C14 aromatic hydrocarbon group, or an optionally Rc-substituted 4- to 10-membered saturated or unsaturated heterocyclic group;R3 represents a halogen atom, an amino group, a hydroxy group, a cyano group, a nitro group, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C1-C6 alkoxy group;R4 represents an optionally Rb-substituted C2-C6 alkenyl group or an optionally Rb-substituted C2-C6 alkynyl group;Rb represents a halogen atom, an amino group, a hydroxy group, a cyano group, a nitro group, a C1-C6 alkoxy group, a di- or mono-(C1-C6 alkyl)amino group, or a 4- to 10-membered saturated or unsaturated heterocyclic group;Rc represents a halogen atom, an amino group, a hydroxy group, a cyano group, a nitro group, an oxo group, an imino group, an N-oxide group, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, or a di- or mono-(C1-C6 alkyl)amino group;Rx, Ry and Rz, which are the same or different, each represent a hydrogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C3-C10 cycloalkyl group, a C6-C14 aromatic hydrocarbon group, or a 4- to 10-membered saturated or unsaturated heterocyclic group;m represents an integer of 0 to 3; andn represents an integer of 0 toor a salt thereof.
地址 Tokyo JP