发明名称 Benzamides
摘要 Novel benzamide derivatives of formula (I); wherein W1, W2, R1 to R7, R6, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
申请公布号 US9498475(B2) 申请公布日期 2016.11.22
申请号 US201514863865 申请日期 2015.09.24
申请人 Merck Patent GmbH 发明人 Yu Henry;Goutopoulos Andreas;Richardson Thomas E.;Li Jiezhen;Heasley Brian H.;Bharathi Pandi
分类号 A61K31/496;C07D403/12;C07D401/14;C07D405/14;C07D413/14;C07D403/14;C07D405/12;C07D409/10;C07D409/12;C07D409/14;C07D417/14;A61K31/454;A61K31/498;A61K31/4985;A61K31/506;A61K31/5377;A61K31/541;A61K31/551;C07D413/12 主分类号 A61K31/496
代理机构 EMD Serono Research and Development Institute 代理人 Kim Dwight D.;EMD Serono Research and Development Institute
主权项 1. A method for treating fertility disorders, wherein at least one compound according to formula (I) is administered to a mammal in need of such treatment: wherein W1, W2 denote independently from one another N or CR8, with the proviso that at least one of W1 or W2 denotes N; R1 denotes —(CY2)n-E-(CY2)n-Het3, —(CY2)n-Cyc-Het3, —(CY2)n—NY-Het3, —(CY2)n—CONH-Het3, —(CY2)n—NHCO-Het3, —(CY2)n—C(Y)(OH)—(CY2)n-Het3, —(CY2)n-Het1, —(CY2)n—CONH-Het1, —(CY2)n—NHCO-Het1, —(CY2)n—Ar, -Cyc-Ar, —(CY2)n—NY—Ar, —(CY2)n—CONH—Ar, —(CY2)n—NHCO—Ar, —(CY2)n—C(Y)(OH)—(CY2)n—Ar, —(CY2)n-Cyc, —(CY2)n—NY-Cyc, —(CY2)n—CONH-Cyc, —(CY2)n—NHCO-Cyc, —(CY2)n—NHCO—NH-Cyc, Y, —(CYR8)n—OY, —(CY2)n—COOY, —(CY2)n—SO2Y, —(CYR8)n—CO—(CY2)n—N(R8)2, —(CY2)n—[C(Y)(OH)]m—(CYR8)n—NY2, [—(CY2)n—O]m—(CYR8)n—NYCOY, —(CY2)n—NYCOOY, —(CY2)n—NYSO2Y, —(CY2)n—NYCON(R8)2, —(CY2)n—NHCO—CH═CH2, —(CY2)n—NHCO—NH—(CY2)n═CH2 or —(CY2)n—CN; R2 denotes Y; R1, R2 together also denote —(CY2)p—NH—(CY2)p—, —(CY2)p—NHCO—(CY2)p—, —(CY2)p—CONH—(CY2)p—, —(CY2)p—N(COA)-(CY2)p—, —(CY2)p—N(COOA)-(CY2)p—, —(CY2)p—C(Y)(Het3)-(CY2)p—, R3 denotes —(CY2)n-Het1, —(CY2)n-Het3, —(CY2)n—Ar, —C(Y)(OY)—Ar, Y or —(CY2)n-Cyc; R4 denotes Y, COY or SO2Y; R5 denotes E-Ar, NY—Ar, Cyc, Y, OY, NYY, NYCOOY, NYCOY, COY, COOY, SO2Y, Het1 or Het3; R6, R7 denote independently from one another H; R6, R7 together also denote —(CY2)p—; R8 denotes Y or Ar; X, E denote independently from one another —(CY2)m—, O, CO, —COO— or SO2; Y denotes H or A; A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms can be replaced independently from one another by Hal, ═O and/or OH; Cyc denotes cycloalkyl having 3-7 C atoms, in which 1-4 H atoms can be replaced independently from one another by Hal and/or OH; Ar denotes an unsaturated or aromatic mono- or bicyclic carbocycle having 3-10 C atoms, which can be substituted by at least one substituent selected from the group of A, Hal, —(CY2)n—OY, COOY, CONH2, NHCOY, —(CY2)n—NYCOOY, —(CY2)n—NY2, NO2, SO2Y, SO2NY2, NYSO2Y, —(CY2)n—CN, —(CY2)n-Het2 and Cyc, or which can be fused to Cyc; Het1 denotes an unsaturated or aromatic mono- or bicyclic heterocycle having 1-10 C atoms and 1-4 N, O and/or S atoms, which can be substituted by at least one substituent selected from the group of Hal, A, Cyc, OY, ═O, COOY, CONH2, NHCOY, —(CY2)n—NY2, SO2Y, SO2NY2, NHSO2Y, CN, Ar and —(CY2)n-Het3; Het2 denotes a saturated or unsaturated monocyclic 5- or 6-membered heterocycle having 1-4 C atoms and 1-4 N, O and/or S atoms, which can be substituted by A and/or ═O; Het3 denotes a saturated mono- or bicyclic heterocycle having 3-7 C atoms and 1-4 N, O and/or S atoms, which can be substituted by at least one substituent selected from the group of ═O, A, Hal, —(CY2)n-Cyc, —(CY2)n—OY, COY, COOY, CONY2, NHCOY, —(CY2)n—NY2, CN, SO2Y and —(CY2)n—Ar; Hal denotes F, Cl, Br or I; m, n denote independently from one another 0, 1, 2, 3, 4, 5 or 6; and p denotes 1, 2 or 3;or a physiologically acceptable salt thereof.
地址 Darmstadt DE