N.v. Organon

Rudolf Gijsbertus Van Someren

Jurgen Schulz

Nicole Corine Renée Van Straten

The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein Ris formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; Rand Rare H or (1-4C)alkyl; Ris phenyl; Ris (1-4C)alkyl; Y&#x2014;X is (CO)&#x2014;O, (SO)&#x2014;O, NHC(O)&#x2014;O, NHC(S)&#x2014;O, OC(O)&#x2014;O, bond-O, C(O)&#x2014;NH, S(O)&#x2014;NH, NHC(O)&#x2014;NH, NHC(S)&#x2014;NH, OC(O)&#x2014;NH, bond-NH, NH&#x2014;C(O), O&#x2014;C(O), NH&#x2014;S(O), or O&#x2014;S(O)or Y&#x2014;X is a bond; Ris H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R,R-aminocarbonyl(1-4C)alkyl, R,R-amino(1-4C)alkyl, R-oxycarbonyl(1-4C)alkyl, R-oxy(1-4C)alkyl, R-carbonyl(1-4C)alkyl or (6-10C)aryl; Ris H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and Rand/or Ris H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)heterocycloylkyl, or Rand Rmay be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility. 

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N.V. Organon, Netherlands

Rudolf Gijsbertus Van Someren