发明名称 TETRAHYDROBENZOTHIOPHENE COMPOUND
摘要 The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia.;A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia:;wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
申请公布号 US2014329802(A1) 申请公布日期 2014.11.06
申请号 US201414229146 申请日期 2014.03.28
申请人 Astellas Pharma Inc. 发明人 HACHIYA Shunichiro;Miura Masanori;Imamura Yoshimasa;Kaga Daisuke;Sato Ippei;Moritomo Hiroyuki;Kato Koji;Terai Kazuhiro;Terada Yoh
分类号 C07D333/66;C07D409/12 主分类号 C07D333/66
代理机构 代理人
主权项 1. A compound of the formula (I) or a salt thereof: wherein R1 represents —O-lower alkyl, -lower alkylene-phenyl, or -lower alkylene-pyridyl, in which phenyl or pyridyl may be substituted with carboxy or protected carboxy, R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl, nitrogen-containing saturated hetero ring, -lower alkylene-aryl, or -lower alkylene-heteroaryl, in which lower alkyl, cycloalkyl, aryl, heteroaryl, and nitrogen-containing saturated hetero ring may be substituted, or R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino, in which the 5- to 7-membered saturated cyclic amino may be substituted, R4's are the same as or different from each other and represent halogen, lower alkyl, —OH, —O-lower alkyl, —NO2, or a group represented by the formula (II): wherein R41 and R42 are the same as or different from each other and represent H or lower alkyl which may be substituted, or R41 and R42 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino, and n represents 0 to 2, provided that N-(4-methoxyphenyl)-2-({3-[(4-methylpiperazin-1-yl)sulfonyl]benzoyl}amino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide is excluded.
地址 Chuo-ku JP