发明名称 PHENYL DERIVATIVE
摘要 The compound represented by the formula (I-1):;;wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
申请公布号 US2014235611(A1) 申请公布日期 2014.08.21
申请号 US201214347178 申请日期 2012.09.27
申请人 ONO PHARMACEUTICAL CO., LTD. 发明人 Naganawa Atsushi;Kusumi Kensuke;Otsuki Kazuhiro;Sekiguchi Tetsuya;Kakuuchi Akito;Shinozaki Koji;Yamamoto Hiroshi;Nonaka Shigeyuki
分类号 C07D211/48;C07D205/04;C07D207/12;C07D401/12 主分类号 C07D211/48
代理机构 代理人
主权项 1. A compound represented by the formula (I-1): wherein R1 represents (1) a C1-8 alkyl group which may be substituted with 1 to 5 R21 group(s), (2) a C2-8 alkenyl group which may be substituted with 1 to 5 R21 group(s), (3) a C2-8 alkynyl group which may be substituted with 1 to 5 R21 group(s), (4) a C3-7 carbocycle which may be substituted with 1 to 5 substituent(s) selected from the group consisting of a C1-4 alkyl group, a C1-4 haloalkyl group, a C1-4 alkoxy group and a halogen atom, or (5) —CONR31R32; R21 represents (1) a halogen atom, (2) —OR22 (in the group, R22 represents (1) a hydrogen atom, (2) a C1-4 alkyl group or (3) a C1-4 haloalkyl group), (3) —NR23R24 (in the group, R23 and R24 each independently represent (1) a hydrogen atom or (2) a C1-4 alkyl group) or (4) an oxo group; R31 and R32 each independently represent (1) a hydrogen atom or (2) a C1-4 alkyl group; R2 represents (1) a hydrogen atom, (2) a C1-4 alkyl group or (3) a C1-4 haloalkyl group; R3 and R4 each independently represent (1) a halogen atom, (2) a C1-4 alkyl group, (3) a C1-4 haloalkyl group, (4) a C1-4 alkoxy group, (5) a hydroxy group, (6) -L-CONR6R7, (7) -L-SO2R8 or (8) -L-COOR9; R5 represents (1) a halogen atom, (2) a C1-4 alkyl group or (3) a C1-4 haloalkyl group; L represents (1) a bond, (2) a group represented by the formula:wherein A represents (1) a bond or (2) an oxygen atom; R12 and R13 each independently represent (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) a hydroxy group or (4) NH2 or (5) R12 and R13 together with the carbon atom to which they are attached may form a C3-7 carbocycle; and the arrow on the right hand side binds to —CONR6R7, —SO2R8 or —COOR9, (3) a C2-4 alkenylene group, (4) a —O—C2-4 alkenylene group, (5) an oxygen atom or (6) a nitrogen atom which may be substituted with a C1-4 alkyl group; R6 and R7 each independently represent (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) a C1-4 haloalkyl group, (4) a hydroxy group, (5) —CONR15R16, (6) —SO2NR15R16, (7) —COR17 or (8) —SO2R17, or R6 and R7 together with the nitrogen atom to which they are attached may form a 4- to 7-membered nitrogen-containing saturated heterocycle that may be substituted with a hydroxy group; R8 represents (1) a C1-4 alkyl group, (2) a C1-4 haloalkyl group or (3) NR10R11; R9 represents (1) a hydrogen atom or (2) a C1-8 alkyl group; R10 and R11 each independently represent (1) a hydrogen atom, (2) a C1-4 alkyl group, (3) —CONR15R16, (4) —SO2NR15R16, COR17 or (6) —SO2R17; the ring 1 and the ring 2 each independently represent a 5- to 7-membered cyclic group; R14 represents (1) a hydrogen atom or (2) a hydroxy group; R15 and R16 each independently represent (1) a hydrogen atom, (2) a C1-4 alkyl group or (3) a 5- to 7-membered cyclic group; R17 represents (1) a C1-4 alkyl group or (2) a 5- to 7-membered cyclic group; M1 and M2 each independently represent (1) a bond, (2) —C(O)—, (3) —O—, (4) —S—, (5) —C(O)O—, (6) —CH2O— or (7) —C(O)NH—; n represents an integer of 1 to 2; m represents an integer of 1 to 2; p represents an integer of 0 to 5; q represents an integer of 0 to 5; r represents an integer of 0 to 4; t represents an integer of 1 to 4; when p is 2 or more, a plurality of R3 groups may be the same or different; when q is 2 or more, a plurality of R4 groups may be the same or different; when r is 2 or more, a plurality of R5 groups may be the same or different; and when t is 2 or more, a plurality of R12 and R13 groups may be respectively the same or different;a salt thereof, a solvate thereof, an N-oxide thereof or a prodrug thereof.
地址 Osaka JP