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Benzamide derivatives as modulators of follicle stimulating hormone
专利权人:
Merck Patent GmbH
发明人:
YU, Henry,RICHARDSON, Thomas E.,BHARATHI, Pandi,HEASLEY, Brian H.,JENKS, Matthew G.,FOGLESONG, Robert J.
申请号:
ES13700819
公开号:
ES2663972T3
申请日:
2013.01.09
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compounds of formula (I) ** (See formula) ** where W1, W2 denotes N; R1 denotes - (CY2) nE-Het3, - (CY2) n-Cyc-Het3, - (CY2) n-Het1, - (CY2) n-CONH-Het1, - (CY2) n-NHCO-Het1, - ( CY2) n-Cyc, - (CY2) n-CONH-Cyc, - (CY2) n-NHCO-Cyc, A, - (CYR8) n-OY, - (CY2) n-COOY, - (CY2) n- SO2Y, - (CYR8) n-CONY2, - (CYR8) n-NY2, - (CYR8) n-NYCOY, - (CY2) n-NYCOOY, - (CY2) n-NYCONY2 or - (CY2) n-NHCO- CH>; = CH2; R2 denotes H; R1, R2 together also denote - (CY2) P-NH- (CY2) P-, - (CY2) p-NHCO- (CY2) p-, - (CY2) p-CONH- (CY2) p-, - ( CY2) pN (COA) - (CY2) p-, - (CY2) pN (COOA) - (CY2) p-, ** (See formula) ** R3 denotes furyl or oxazolyl, which may be monosubstituted with A or Cyc ; R4 denotes H; R5 denotes phenyl, which may be mono or disubstituted with A or Hal, or pyridyl, which may be monosubstituted with A or Hal; R6, R7 together denote - (CY2) 2-; R8 denotes Y or Ar; R9 denotes Y; R10 denotes Hal, Y, OY, -O (CY2) n-OY, NY2, Cyc, COOY, CONH2, NHCOY or CN; with the proviso that R 9 and R10 are not simultaneously H; R2, R10 together also denote - (CY2) P- or - (CY) 2-; X denotes CO; E denotes - (CY2) m-, O, CO, -COO- or SO2; And denotes H or A; A denotes unbranched or branched alkyl with 1-10 C atoms, where 1-7 H atoms can be independently replaced by Hal and / or>; = O; Cyc denotes cycloalkyl with 3-6 C atoms, where 1-3 H atoms can be replaced independently of each other by OH or COOH; Ar denotes an unsaturated or aromatic mono or bicyclic carbocycle with 3-10 C atoms, which may be substituted with at least one substituent selected from the group consisting of A, Hal, OY, COOY, CONH2, NHCOY, - (CY2) n -NY2, NO2, SO2Y, CN and Het2, or that can be merged into Cyc; Het1 denotes an unsaturated or aromatic mono or bicyclic heterocycle with 1-10 atoms of C and 1-4 atoms of N, O and / or S, which may be substituted with at least one substituent selected from the group consisting of Hal, A, Cyc, OY, COOY, CONH2, NHCOY, NY2, SO2Y, SO2NY2, NHSO2Y, CN and Ar; Het2 denotes a 5-membered u
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