发明名称 Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
摘要 A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.;
申请公布号 US8754100(B2) 申请公布日期 2014.06.17
申请号 US201013138504 申请日期 2010.02.24
申请人 EISAI R&D Management Co., Ltd. 发明人 Kitazawa Noritaka;Shinmyo Daisuke;Ito Koichi;Sato Nobuaki;Hasegawa Daiju;Uemura Toshiyuki;Watanabe Toru
分类号 A01N43/42;A61K31/44;A01N43/40;C07D471/02;C07D491/02;C07D498/02;C07D401/00 主分类号 A01N43/42
代理机构 Birch, Stewart, Kolasch & Birch, LLP 代理人 Birch, Stewart, Kolasch & Birch, LLP
主权项 1. A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein R1 and R2 are the same or different and each represent a substituent selected from the following Substituent Group a1; m represents an integer of 0 to 3; n represents an integer of 0 to 2; W represents a nitrogen atom; Ring A represents a five-membered aromatic heterocyclic group fused with a 5- to 14-membered non-aromatic ring group, which contains two or more nitrogen atoms and may have 1 to 3 substituents selected from the following Substituent Group b1 (wherein the 5- to 14-membered non-aromatic ring group may have a crosslinked structure); X1 represents i) a single bond, ii) a C1-6 alkylene group, iii) a vinylene group which may have 1 to 2 C1-6 alkyl groups or iv)-X2—(wherein X2 represents —NR3—, —NR3C(O)—, —C(O)NR3—, —O—, —S—, —S(O)— or —S(O)2— and R3 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C2-6 alkanoyl group or a C1-6 alkylsulfonyl group); and Ring B represents a monocyclic or fused cyclic aromatic ring group selected from the formulas [2] to [3]: each of which may have 1 to 3 substituents selected from the following Substituent Group c1 [Substituent Group a1: a C1-6 alkyl group, a C3-8 cycloalkyl group, a C2-6 alkenyl group, a C1-6 alkoxy group, a C2-6 alkenyloxy group, a C3-8 cycloalkyloxy group, an amino group (wherein the amino group may have one C2-6 alkanoyl group or C1-6 alkylsulfonyl group or 1 to 2 C1-6 alkyl groups or C3-8 cycloalkyl groups), a cyano group, a formyl group, a halogen atom, a hydroxyl group and a nitro group; Substituent Group b1: a C1-6 alkyl group (wherein the alkyl group may be substituted with 1 to 3 halogen atoms), a C2-6 alkenyl group, a C3-8 cycloalkyl group, a C6-14 aryl group, a C6-14 aryl-C1-6 alkyl group, a C1-6 alkoxy group, a C2-6 alkenyloxy group, a C3-8 cycloalkyloxy group, a C2-6 alkanoyl group, a C4-9 cycloalkylcarbonyl group, a C7-15 aroyl group, a C1-6 alkylsulfonyl group, a C2-6 alkenylsulfonyl group, a C3-8 cycloalkylsulfonyl group, a C6-14 arylsulfonyl group, a C1-6 alkylthio group, a C2-6 alkenylthio group, a C3-8 cycloalkylthio group, an aminosulfonyl group (wherein the aminosulfonyl group may have 1 to 2 C1-6 alkyl groups, C2-6 alkenyl groups or C3-8 cycloalkyl groups), an amino group (wherein the amino group may have one C2-6 alkanoyl group, C1-6 alkylsulfonyl group or C3-8 cycloalkylsulfonyl group or 1 to 2 C1-6 alkyl groups or C3-8 cycloalkyl groups), a cyano group, a formyl group, a halogen atom, a hydroxyl group, a nitro group, an oxo group, a 1-pyrrolidinyl group, a 1-piperidinyl group, a 1-homopiperidinyl group, an indolin-1-yl group, a 1,2,3,4-tetrahydroquinolin-1-yl group and a 4-morpholinyl group; Substituent Group c1: i) an amino group (wherein the amino group may have one C2-6 alkanoyl group, C1-6 alkylsulfonyl group or C3-8 cycloalkylsulfonyl group or 1 to 2 C1-6 alkyl groups or C3-8 cycloalkyl groups), ii) a cyano group, iii) a halogen atom, iv) a hydroxyl group and v) v-i) a C1-6 alkyl group, v-ii) a C2-6 alkenyl group, v-IIi) a C2-6 alkynyl group, v-iv) a C1-6 alkoxy group, v-v) a C1-6 alkylaminocarbonyl group, v-vi) a C1-6 alkylaminosulfonyl group, v-vii) a C1-6 alkylsulfonyl group, v-viii) a C1-6 alkylthio group, v-ix) a C2-6 alkanoyl group, v-x) a phenyl group, v-xi) a pyridyl group, v-xii) a pyridazinyl group, v-xiii) a pyrimidinyl group, v-xiv) a 1-pyrrolidinyl group, v-xv) a 1-piperidinyl group, v-xvi) a 1-homopiperidinyl group and v-xvii) a 4-morpholinyl group, each of which may have 1 to 3 substituents selected from the group consisting of a C1-6 alkyl group and a halogen atom].
地址 Tokyo JP