发明名称 HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM
摘要 The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I);;in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
申请公布号 US2014187543(A1) 申请公布日期 2014.07.03
申请号 US201314037026 申请日期 2013.09.25
申请人 Abbott GmbH & Co. KG 发明人 Lubisch Wilfried;Hornberger Wilfried;Oost Thorsten K.;Sauer Daryl Richard;Unger Liliane;Wernet Wolfgang;Geneste Hervé
分类号 C07D403/14;C07D413/14;C07D405/14;C07D417/14;C07D401/14 主分类号 C07D403/14
代理机构 代理人
主权项 1. A compound of the formula (I) in which A is an aromatic heteromonocyclic, or an aromatic or partially aromatic heterobicyclic ring, where the heterocycles are 5- or 6-membered rings and comprise up to 4 heteroatoms selected from the group consisting of N, O and S, and up to 2 oxo groups, where not more than one of the heteroatoms is an oxygen atom,and A may be substituted by radicals R11, R12 and/or R13,whereR11, R12 and R13 at each occurrence are selected independently of one another from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, O-phenyl, O—C1-C4-alkylen-phenyl, phenyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2, R3 and R4 are selected independently of one another from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, O-phenyl, O—C1-C4-alkylen-phenyl, phenyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2, or R3 and R4 are connected to give —CH═CH—CH═CH—, —(CH2)4— or —(CH2)3—, R5 is a radical (W)—(X)—(Y)—Z, where W is selected from the group consisting of C1-C4-alkylen, C2-C4-alkenylen, C2-C4-alkynylen, O, O—(C1-C4-alkylen), S, S—(C1-C4-alkylen), NR54, NR54—(C1-C4-alkylen) and a bond,X is selected from the group consisting of CO, CO—O, SO2, NR54, NR54—CO, NR54—SO2, CO—NR58 and a bond,Y is C1-C6-alkylen, C2-C6-alkenylen, C2-C6-alkynylen, or a bond,Z is selected from the group consisting of hydrogen, E, O—R52, NR51R52, S—R52, whereE is an unsaturated, saturated or partially unsaturated mono-, bi- or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms and/or 0 to 2 sulfur atoms, said ring may comprise up to two oxo groups, and may be substituted by radicals R55, R56, R57, and/or up to three radicals R53,R51 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl and C1-C4-alkylen-phenyl, where the phenyl ring may be substituted by up to two radicals R53,R52 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, E and C1-C4-alkylen-E,R53 at each occurrence is independently selected from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2,R54 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl and C1-C4-alkylen-phenyl, where the phenyl ring may be substituted by up to two radicals R59,R55 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl, C1-C4-alkylen-phenyl, where the ring may be substituted by up to two radicals R60, and OH, O—C1-C4-alkyl, O-phenyl, O—C1-C4-alkylen-phenyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2,R56 is a group Q1-Q2-Q3, Q3, whereQ1 is selected from the group consisting of a bond, C1-C4-alkylen, C2-C4-alkenylen, C2-C4-alkynylen, C1-C4-alkylen-N(C1-C4-alkyl), N(C1-C4-alkyl), C1-C4-alkylen-NH, NH, N(C1-C4-alkyl)-C1-C4-alkylen, NH—C1-C4-alkylen, O, C1-C4-alkylen-O, O—C1-C4-alkylen, CO—NH, CO—N(C1-C4-alkyl), NH—CO, N(C1-C4-alkyl)-CO, CO, SO2, SO, S, O, SO2—NH, SO2—N(C1-C4-alkyl), NH—SO2, N(C1-C4-alkyl)-SO2, O—CO—NH, O—CO—N(C1-C4-alkyl), NH—CO—O, N(C1-C4-alkyl)-CO—O, N(C1-C4-alkyl)-CO—N(C1-C4-alkyl), NH—CO—N(C1-C4-alkyl), N(C1-C4-alkyl)-CO—NH, and NH—CO—NH,Q2 is selected from the group consisting of C1-C4-alkylen, C2-C4-alkenylen, C2-C4-alkynylen, and a bond,Q3 is a hydrogen or an unsaturated, saturated or partially unsaturated mono-, bi- or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms and/or 0 to 2 sulfur atoms, which may comprise up to two oxo groups and may be substituted by the radicals R63, R64 and/or R65,R57 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, phenyl, C1-C4-alkylen-phenyl, COOH, CO—O—C1-C4-alkyl, CONH2, CO—NH—C1-C4-alkyl, CO—N(C1-C4-alkyl)2, CO—C1-C4-alkyl, CH2—NH2, CH2—NH—C1-C4-alkyl and CH2—N(C1-C4-alkyl)2,R58 at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl and C1-C4-alkylen-phenyl, where the phenyl ring may be substituted by up to two radicals R62,R59, R69 and R62 at each occurrence are selected independently of one another from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2,R63, R64 and R65 at each occurrence are selected independently of one another from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, O-phenyl, O—C1-C4-alkylen-phenyl, phenyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2, R6 and R7 are selected independently of one another from the group consisting of hydrogen, chlorine, bromine, iodine, fluorine, CN, CF3, OCF3, NO2, OH, O—C1-C4-alkyl, O-phenyl, O—C1-C4-alkylen-phenyl, phenyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, NH2, NH(C1-C4-alkyl) and N(C1-C4-alkyl)2, and their tautomeric forms, enantiomeric and diastereomeric forms, and prodrugs thereof.
地址 Wiesbaden DE