发明名称 HETEROCYCLIC DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY
摘要 The present invention is related to a compound represented by formula (I),;wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
申请公布号 US2014275074(A1) 申请公布日期 2014.09.18
申请号 US201214351234 申请日期 2012.10.24
申请人 Shionogi & Co., Ltd. 发明人 Hata Kayoko;Masuda Manami;Nakai Hiromi;Taniyama Daisuke;Tobinaga Hiroyuki;Hato Yoshio;Fujiu Motohiro
分类号 C07D413/14;C07D403/14;C07D401/14;C07D403/04 主分类号 C07D413/14
代理机构 代理人
主权项 1. A compound of general formula (I): wherein ring A is a nitrogen-containing non-aromatic heterocycle or a nitrogen-containing aromatic heterocycle; ring B is an aromatic carbocycle, a non-aromatic carbocycle, an aromatic heterocycle or a non-aromatic heterocycle; —X1═ is —N═ or —C(R1)═; —X2═ is —N═ or —C(R2)═; —X3═ is —N═ or —C(R3)═; —X4═ is —N═ or —C(R4)═; —X5═ is —N═ or —C(R12)═; wherein the number of “—N═” on the ring in —X1═, —X2═, —X3═ and —X4═ is 0, 1 or 2; R1, R2, R3 and R4 are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl; ortwo groups selected from R1, R2, R3 and R4 which are attached to neighboring ring constituent carbon atoms are taken together to form substituted or unsubstituted alkylene which may be intervened with one or two heteroatom(s); R12 is a hydrogen atom or substituted or unsubstituted alkyl; R5 is formula: -L-R9, wherein R9 is carboxy, alkyloxycarbonyl or a carboxy equivalent;-L- is substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, or substituted or unsubstituted alkynylene; R6 is each independently halogen, hydroxy, carboxy, formyl, formyloxy, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, cyano, nitro, nitroso, azido, amidino, guanidino, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl, substituted or unsubstituted alkynylcarbonyl, substituted or unsubstituted amino, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted alkenylsulfonyl, substituted or unsubstituted alkynylsulfonyl, substituted or unsubstituted imino, substituted or unsubstituted alkylcarbonyloxy, substituted or unsubstituted alkenylcarbonyloxy, substituted or unsubstituted alkynylcarbonyloxy, substituted or unsubstituted alkyloxycarbonyl, substituted or unsubstituted alkenyloxycarbonyl, substituted or unsubstituted alkynyloxycarbonyl, substituted or unsubstituted alkylsulfanyl, substituted or unsubstituted alkenylsulfanyl, substituted or unsubstituted alkynylsulfanyl, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkenylsulfinyl, substituted or unsubstituted alkynylsulfinyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted sulfamoyl, substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic heterocyclyl, substituted or unsubstituted aromatic carbocyclyl oxy, substituted or unsubstituted non-aromatic carbocyclyl oxy, substituted or unsubstituted aromatic heterocyclyl oxy, substituted or unsubstituted non-aromatic heterocyclyl oxy, substituted or unsubstituted aromatic carbocyclyl carbonyl, substituted or unsubstituted non-aromatic carbocyclyl carbonyl, substituted or unsubstituted aromatic heterocyclyl carbonyl, substituted or unsubstituted non-aromatic heterocyclyl carbonyl, substituted or unsubstituted aromatic carbocyclyl oxycarbonyl, substituted or unsubstituted non-aromatic carbocyclyl oxycarbonyl, substituted or unsubstituted aromatic heterocyclyl oxycarbonyl, substituted or unsubstituted non-aromatic heterocyclyl oxycarbonyl, substituted or unsubstituted aromatic carbocyclyl sulfanyl, substituted or unsubstituted non-aromatic carbocyclyl sulfanyl, substituted or unsubstituted aromatic heterocyclyl sulfanyl, substituted or unsubstituted non-aromatic heterocyclyl sulfanyl, substituted or unsubstituted aromatic carbocyclyl sulfonyl, substituted or unsubstituted non-aromatic carbocyclyl sulfonyl, substituted or unsubstituted aromatic heterocyclyl sulfonyl, or substituted or unsubstituted non-aromatic heterocyclyl sulfonyl; ortwo of R6 attached to the same ring constituent carbon atom are taken together to form a carbocycle containing the above ring constituent carbon atom, a heterocycle containing the above ring constituent carbon atom, oxo, or formula: ═CR6aR6b, wherein R6a and R6b are each independently a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; ortwo of R6 attached to the different ring constituent carbon atoms are taken together to form substituted or unsubstituted alkylene which may be intervened with one or two heteroatom(s); R7 is halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic carbocyclyl oxy or substituted or unsubstituted non-aromatic carbocyclyl oxy; R8 is each independently halogen, hydroxy, carboxy, formyl, formyloxy, sulfanyl, sulfino, sulfo, thioformyl, thiocarboxy, dithiocarboxy, cyano, nitro, nitroso, azido, amidino, guanidino, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl, substituted or unsubstituted alkynylcarbonyl, substituted or unsubstituted amino, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted alkenylsulfonyl, substituted or unsubstituted alkynylsulfonyl, substituted or unsubstituted imino, substituted or unsubstituted alkylcarbonyloxy, substituted or unsubstituted alkenylcarbonyloxy, substituted or unsubstituted alkynylcarbonyloxy, substituted or unsubstituted alkyloxycarbonyl, substituted or unsubstituted alkenyloxycarbonyl, substituted or unsubstituted alkynyloxycarbonyl, substituted or unsubstituted alkylsulfanyl, substituted or unsubstituted alkenylsulfanyl, substituted or unsubstituted alkynylsulfanyl, substituted or unsubstituted alkylsulfinyl, substituted or unsubstituted alkenylsulfinyl, substituted or unsubstituted alkynylsulfanyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted sulfamoyl, substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic heterocyclyl, substituted or unsubstituted aromatic carbocyclyl oxy, substituted or unsubstituted non-aromatic carbocyclyl oxy, substituted or unsubstituted aromatic heterocyclyl oxy, substituted or unsubstituted non-aromatic heterocyclyl oxy, substituted or unsubstituted aromatic carbocyclyl carbonyl, substituted or unsubstituted non-aromatic carbocyclyl carbonyl, substituted or unsubstituted aromatic heterocyclyl carbonyl, substituted or unsubstituted non-aromatic heterocyclyl carbonyl, substituted or unsubstituted aromatic carbocyclyl oxycarbonyl, substituted or unsubstituted non-aromatic carbocyclyl oxycarbonyl, substituted or unsubstituted aromatic heterocyclyl oxycarbonyl, substituted or unsubstituted non-aromatic heterocyclyl oxycarbonyl, substituted or unsubstituted aromatic carbocyclyl sulfanyl, substituted or unsubstituted non-aromatic carbocyclyl sulfanyl, substituted or unsubstituted aromatic heterocyclyl sulfanyl, substituted or unsubstituted non-aromatic heterocyclyl sulfanyl, substituted or unsubstituted aromatic carbocyclyl sulfonyl, substituted or unsubstituted non-aromatic carbocyclyl sulfonyl, substituted or unsubstituted aromatic heterocyclyl sulfonyl, or substituted or unsubstituted non-aromatic heterocyclyl sulfonyl; n is 0, 1, 2 or 3; q is 0, 1, 2 or 3; and p is 0 or 1, with the proviso that when the A ring is a ring represented by the formula: then n is 1, 2 or 3, or a pharmaceutically acceptable salt thereof.
地址 Osaka-shi, Osaka JP