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US 8,524,732 B2Granted
Substituted tetrahydroquinolines
AssigneeMerck Patent GmbH
InventorsKai Schiemann, Dirk Finsinger, Christiane Amendt, Frank Zenke
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I), in which R1, R2, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumors.
Claims16
Compounds of the formula I
- in which
- R1 denotes H, A, Hal, SA, (CH2)pCN, SCN, (CF2)pCF3, SF5, OA, O(CF2)pCF3, S(CF2)pCF3, NR2, NRCOR, NRSO2R, NR(CH2)pNR2, CONR(CH2)pNR2, SO2NR(CH2)pNR2, CONR2, SO2NR2, or COOR,
- R2 denotes H or Hal
- R3 denotes H or A
- A denotes linear or branched alkyl having 1 to 10 C atoms or cycloalkyl having 3 to 7 C atoms,
- R4 denotes aryl or heteroaryl, each of which is optionally substituted by Hal, NO2, CN, OR, A, —(CY2)n—OR, —OCOR, —(CY2)n—CO2R, —(CY2)n—CN or —(CY2)n—NR2, or
- R4 denotes aryl or heteroaryl each of which is unsubstituted or mono- or polysubstituted by aryl or heteroaryl, where each of the optional aryl or heteroaryl substituents are optionally substituted by Hal, NO2, CN, A, OR, OCOR, NR2, CF3, OCF3, OCH(CF3)2,
- X denotes O,
- Y denotes H, A, Hal or OR
- R denotes H, A, (CH2)pO(CH2)pR3 or (CH2)pNA(CH2)pR3,
- W denotes CH2, C═O or C═S,
- Q1 denotes NR, O or S,
- Z denotes —SO—,
- Q2 denotes NR, S, O or a single bond,
- R5 denotes H, (CY2)pNR2, (CY2)pOR, (CY2)pSR,
- (CY2)pQ1COQ1R or (CY2)pCOOR and, if Q2 denotes a single bond, also Hal,
- Hal denotes F, Br or Cl
- n denotes 1, 2, 3 or 4,
- m denotes 0, 1 or 2,
- p denotes 0, 1, 2, 3, 4, 5, 6, 7 or 8
- and
- s denotes 0, 1 or 2,
- and pharmaceutically usable tautomers, salts and stereoisomers thereof, including mixtures thereof in all ratios.
20 more elements
A compound selected from the following compounds:
- and pharmaceutically usable tautomers, salts and stereoisomers thereof, including mixtures thereof in all ratios.
Dependencies are inferred from the claim text.