发明名称 Ring-fused compound
摘要 The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.; [in the formula, R1 is -Q1-A1 and the like; is a double bond or a single bond; when is a double bond, W1 is a nitrogen atom or a group represented by the general formula: ═C(Ra)—, and W2 is a nitrogen atom or a group represented by the general formula: ═C(Rb)—; when is a single bond, W1 is a group represented by the general formula: —C(Raa)(Rab)— or a group represented by the general formula: —(C═O)—, and W2 is a group represented by the general formula: —C(Rba)(Rbb)—, a group represented by the general formula: —(C═O)— or a group represented by the general formula: —N(Rbc)—; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi′)n; and Z is a hydroxyl group or COOR2 and the like.
申请公布号 US9359350(B2) 申请公布日期 2016.06.07
申请号 US201514619980 申请日期 2015.02.11
申请人 SATO PHARMACEUTICAL CO., LTD. 发明人 Nagai Keita;Nagasawa Koh;Takahashi Hirobumi;Baba Motoaki;Fujioka Shinichi;Kondoh Eri;Tanaka Kenichi;Itoh Yoshiki
分类号 C07D401/14;A61K31/437;C07D471/04;C07D209/08;C07D209/30;C07D231/56;C07D235/08;C07D235/10;C07D401/06;C07D405/06;C07D235/06;C07D403/04;C07D409/06;C07D413/06;C07D209/12 主分类号 C07D401/14
代理机构 Sughrue Mion, PLLC 代理人 Sughrue Mion, PLLC
主权项 1. A compound represented by Formula (I): [in the formula, R1 represents a group represented by the general formula: -Q1-A1; Q1 represents a methylene group; A1 represents a phenyl group, which may be substituted with one to three substituents selected from the <Substituent group L> described later (herein any two substituents adjacent to each other on the phenyl group may join together to form a lower alkylenedioxy group); represents a double bond or a single bond; when is a double bond, W1 represents a nitrogen atom or a group represented by the general formula: ═C(Ra)—, and W2 represents a nitrogen atom or a group represented by the general formula: ═C(Rb)—; when is a single bond, W1 represents a group represented by the general formula: —C(Raa)(Rab)— or a group represented by the general formula: —(C═O)—, and W2 represents a group represented by the general formula: —C(Rba)(Rbb)—, a group represented by the general formula: —(C═O)— or a group represented by the general formula: —N(Rbc)—; Ra and Rb represent each independently a hydrogen atom, a substituent selected from the <Substituent group M> described later or a group represented by the general formula: -Q2-A2; Raa and Rab represent each independently a hydrogen atom, a substituent selected from the <Substituent group N> described later or a group represented by the general formula: -Q2-A2, or Raa and Rab may join together to form a lower alkylene group (herein 1 to 2 or more methylene groups constituting the lower alkylene group each independently may be substituted with an oxygen atom, a carbonyl group, a vinylene group or a group represented by the general formula: —N(Rc)— for the total methylene groups, and/or the hydrogen constituting the methylene group may be substituted with a hydroxyl group, a lower alkyl group or a halogen atom); Rba and Rbb represent each independently a hydrogen atom, a halogen atom, an amino group, a lower alkyl-amino group, a di-lower alkyl-amino group, a hydroxy-lower alkyl-amino group, a lower alkyl-sulfonylamino group, a lower alkoxy-carbonylamino group, a substituent selected from the <Substituent group N> or a group represented by the general formula: -Q2-A2, or Rba and Rbb may join together to form a lower alkylene group (herein 1 to 2 or more methylene groups constituting the lower alkylene group each independently may be substituted with an oxygen atom, a carbonyl group, a vinylene group or a group represented by the general formula: —N(Rc)— for the total methylene groups, and/or the hydrogen constituting the methylene group may be substituted with a hydroxyl group, a lower alkyl group or a halogen atom); Rbc represents a group selected from the group consisting of a hydrogen atom, a lower alkyl group, a cycloalkyl group, a halo-lower alkyl group, a lower alkoxy-carbonyl group, a carbamoyl group, a mono-lower alkyl-carbamoyl group, a di-lower alkyl-carbamoyl group and a lower alkanoyl group or a group represented by the general formula: -Q2-A2; Q2 represents a single bond, a lower alkylene group or a lower alkenylene group (herein 1 or 2, or more methylene groups constituting the lower alkylene group each independently may be substituted with an oxygen atom, a nitrogen atom or a carbonyl group for the total methylene groups, and/or the hydrogen constituting the methylene group may be substituted with a halogen atom, a cyano group, a hydroxyl group or a lower alkyl group); A2 represents a cycloalkyl group, an aliphatic heterocyclic group, an aryl group or a heteroaryl group, which may be substituted with one to three substituents selected from the <Substituent group L> (herein any two substituents adjacent to each other on the aryl group or the heteroaryl group may join together to form a lower alkylenedioxy group); W3 represents a nitrogen atom, and W4 and W5 represent each independently a methine group that may have a substituent selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a lower alkyl group, a cycloalkyl group, a halo-lower alkyl group, a lower alkoxy group and a halo lower alkoxy group; X represents a single bond; Y is a single bond; Z represents a 5-tetrazolyl group, a 5-oxo-1,2,4-oxadiazolyl group, a 2-oxo-1,3,4-oxadiazolyl group, a 5-imino-4,5-dihydro-1,3,4-oxadiazolyl group, a 2-thioxo-1,3,4-oxadiazolyl group or a 5-oxo-1,2,4-thiadiazolyl group; wherein, the <Substituent group L>, the <Substituent group M> and the <Substituent group N> are defined as described below: <Substituent group L>: a halogen atom, a hydroxyl group, a nitro group, a cyano group, a formyl group, an amino group, a carboxyl group, a lower alkyl group, a halo-lower alkyl group, a cycloalkyl group, a lower alkoxy group, a halo-lower alkoxy group, a hydroxy lower alkyl group, a lower alkoxy lower alkyl group, a lower alkoxycarbonyl group, a lower alkanoyl group, a lower alkylthio group, a lower alkylsulfonyl group, a lower alkylamino group, a di-lower alkylamino group, a carbamoyl group, a mono-lower alkyl carbamoyl group, a di-lower alkyl carbamoyl group, a lower alkanoylamino group, a lower alkylsulfonylamino group, a lower alkoxycarbonylamino group, an aralkyl group, an aryloxy group, a heteroaryloxy group, and a lower alkenyl group, <Substituent group M>: a halogen atom, a hydroxyl group, a nitro group, a cyano group, a formyl group, an amino group, a carboxyl group, a lower alkyl group, a halo-lower alkyl group, a cycloalkyl group, a lower alkoxy group, a halo-lower alkoxy group, a hydroxy lower alkyl group, a lower alkoxy lower alkyl group, a lower alkoxycarbonyl group, a lower alkanoyl group, a lower alkylthio group, a lower alkylsulfonyl group, a lower alkylamino group, a di-lower alkylamino group, a carbamoyl group, a mono-lower alkyl carbamoyl group, a di-lower alkyl carbamoyl group, a lower alkanoylamino group, a lower alkylsulfonylamino group, and a lower alkoxycarbonylamino group, <Substituent group N>: a hydroxyl group, a cyano group, a formyl group, a carboxyl group, a lower alkyl group, a halo-lower alkyl group, a cycloalkyl group, a lower alkoxy group, a halo-lower alkoxy group, a hydroxy lower alkyl group, a lower alkoxy lower alkyl group, lower alkoxycarbonyl group, a lower alkanoyl group, a carbamoyl group, a mono-lower alkyl carbamoyl group, and a di-lower alkyl carbamoyl group]; or a pharmaceutically acceptable salt or ester of the compound.
地址 Tokyo JP