发明名称 HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
摘要 The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
申请公布号 US2017121314(A1) 申请公布日期 2017.05.04
申请号 US201715404758 申请日期 2017.01.12
申请人 GRÜNENTHAL GMBH 发明人 SCHUNK STEFAN;Reich Melanie;Jakob Florian;Damann Nils;Haurand Michael;Kless Achim;Rogers Marc;Sutton Kathy
分类号 C07D405/04;C07D405/12;C07D413/04 主分类号 C07D405/04
代理机构 代理人
主权项 1. A compound of formula (I),  wherein m represents 0, 1 or 2; n denotes 0 or 1; Y is selected from the group consisting of bond and —C(R3)2—; wherein each R3 is independently selected from the group consisting of H and C1-6-alkyl, or two R3 form together with the C-atom connecting them a C3-10-cycloalkyl or a 3 to 7 membered heterocyclyl; L is —[C(R4)2]x—(X)y—[C(R4)2]z—, wherein x is 0, 1 or 2, y is 0 or 1 and z is 0 or 1, with the proviso that x≧y;each R4 is independently selected from the group consisting of H and C1-6-alkyl,or two R4 form together with the C-atom connecting them a C3-10-cycloalkyl or a 3 to 7 membered heterocyclyl or two R4 form together with two adjacent C-atoms connecting them a C3-10-cycloalkyl or a 3 to 7 membered heterocyclyl, X is selected from the group consisting of O, S, S(O)2, N(H) or N(C1-6-alkyl); R1 is selected from the group consisting of H; F; Cl; CN; C1-6-alkyl; C1-6-alkyl-O(R5) and C1-6-alkyl-N(R5)2; wherein each R5 is independently selected from H or C1-6-alkyl or two R5 form together with the N-atom connecting them a 3 to 7 membered heterocyclyl; R2 is selected from the group consisting of H; F; Cl; CN; C1-6-alkyl; C1-6-alkyl-O(R6) and C1-6-alkyl-N(R6)2; wherein each R6 is independently selected from H or C1-6-alkyl or two R6 form together with the N-atom connecting them a 3 to 7 membered heterocyclyl; Ar1 represents aryl or heteroaryl, wherein said aryl or said heteroaryl is substituted by zero or one or two or three substituents R7, Ar2 represents heteroaryl, substituted by zero or one or two or three substituents R8, wherein each R7 and each R8 is independently selected from the group consisting of F; Cl; Br; I; NO2; CN; C1-6-alkyl; CF3; CF2H; CFH2; CF2Cl; CFCl2; C(═O)—H; C(═O)—C1-6-alkyl; C(═O)—OH; C(═O)—O—C1-6-alkyl; C(═O)—N(H)(OH); C(═O)—NH2; C(═O)—N(H)(C1-6-alkyl); C(═O)—N(C1-6-alkyl)2; C(═N—OH)—H; C(═N—OH)—C1-6-alkyl; C(═N—O—C1-6-alkyl)-H; C(═N—O—C1-6-alkyl)-C1-6-alkyl; OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; O—C1-6-alkyl; O—C(═O)—C1-6-alkyl; O—C(═O)—O—C1-6-alkyl; O—(C═O)—N(H)(C1-6-alkyl); O—C(═O)—N(C1-6-alkyl)2; O—S(═O)2—C1-6-alkyl; O—S(═O)2—OH; O—S(═O)2—O—C1-6-alkyl; O—S(═O)2—NH2; O—S(═O)2—N(H)(C1-6-alkyl); O—S(═O)2—N(C1-6-alkyl)2; NH2; N(H)(C1-6-alkyl); N(C1-6-alkyl)2; N(H)—C(═O)—C1-6-alkyl; N(H)—C(═O)—O—C1-6-alkyl; N(H)—C(═O)—NH2; N(H)—C(═O)—N(H)(C1-6-alkyl); N(H)—C(═O)—N(C1-6-alkyl)2; N(C1-6-alkyl)-C(═O)—C1-6-alkyl; N(C1-6-alkyl)-C(═O)—O—C1-6-alkyl; N(C1-6-alkyl)-C(═O)—NH2; N(C1-6-alkyl)-C(═O)—N(H)(C1-6-alkyl); N(C1-6-alkyl)-C(═O)—N(C1-6-alkyl)2; N(H)—S(═O)2OH; N(H)—S(═O)2—C1-6-alkyl; N(H)—S(═O)2—O—C1-6-alkyl; N(H)—S(═O)2—NH2; N(H)—S(═O)2—N(H)(C1-6-alkyl); N(H)—S(═O)2N(C1-6-alkyl)2; N(C1-6-alkyl)-S(═O)2—OH; N(C1-6-alkyl)-S(═O)2—C1-6-alkyl; N(C1-6-alkyl)-S(═O)2—O—C1-6-alkyl; N(C1-6-alkyl)-S(═O)2—NH2; N(C1-6-alkyl)-S(═O)2—N(H)(C1-6-alkyl); N(C1-6-alkyl)-S(═O)2—N(C1-6-alkyl)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; S—C1-6-alkyl; S(═O)—C1-6-alkyl; S(═O)2—C1-6-alkyl; S(═O)2—OH; S(═O)2—O—C1-6-alkyl; S(═O)2—NH2; S(═O)2—N(H)(C1-6-alkyl); S(═O)2—N(C1-6-alkyl)2; C3-10-cycloalkyl; 3 to 7 membered heterocyclyl; aryl; heteroaryl; O—C3-10-cycloalkyl; O-(3 to 7 membered heterocyclyl); O-aryl; O-heteroaryl; N(H)—C3-10-cycloalkyl; N(H)-(3 to 7 membered heterocyclyl); N(H)-aryl; N(H)-heteroaryl; N(C1-6-alkyl)-C3-10-cycloalkyl; N(C1-6-alkyl)-(3 to 7 membered heterocyclyl); N(C1-6-alkyl)-aryl; N(C1-6-alkyl)-heteroaryl; C(═O)—C3-10-cycloalkyl; C(═O)-(3 to 7 membered heterocyclyl); C(═O)-aryl; C(═O)-heteroaryl; S(═O)2—C3-10-cycloalkyl; S(═O)2-(3 to 7 membered heterocyclyl); S(═O)2-aryl; S(═O)2-heteroaryl; S(═O)(═NR13)—C3-10-cycloalkyl; S(═O)(═NR13)-(3 to 7 membered heterocyclyl); S(═O)(═NR13)-aryl and S(═O)(═NR13)-heteroaryl, wherein R13 represents H or C1-6-alkyl; wherein in each case said C1-6-alkyl may be branched or unbranched; unsubstituted or mono- or polysubstituted; and wherein in each case said C3-10-cycloalkyl, 3 to 7 membered heterocyclyl aryl and heteroaryl may be unsubstituted or mono- or polysubstituted; optionally in the form of a single stereoisomer or a mixture of stereoisomers, in form of the free compound and/or a physiologically acceptable salt and/or a physiologically acceptable solvate thereof.
地址 Aachen DE