C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/209, 260/237
C07D 471/16 (2006.01) A61K 31/44 (2006.01)
Patent
CA 2007815
DIR 0430 Abstract The invention relates to a new group of 8,9-annelated- 1,2,3,4-tetrahydro-.beta.-carbolines of the formula Image and the salts and prodrugs thereof. In this formula the symbols have the following meaning: R1 is straight or branched alkyl having 1-3 C-atoms, or is straight or branched alkoxy or alkylthio having 1-4 C-atoms , or R1 is a group R5R6N-CO- wherein R5 and R6 independently of each other are hydrogen, alkyl having 1-3 C-atoms, or together with the nitrogen atom constitute a heterocyclic 5- or 6-ring, or R1 is hydroxy, halogen, cyano, trifluoromethyl; n has the value 0 or l; Z , together with the two carbon atoms and the nitrogen atom, constitutes a heterocyclic group which consists of 9-12 ring atoms and which, in addition to the nitrogen atom already present, may comprise a sulpur atom as second hetero atom and which group may be substituted with 1-4 methyl groups or with a spiroal- kyl group; R2 is hydrogen, straight or branched alkyl having 1-8 C- atoms, alkenyl or alkynyl having 2-8 C-atoms, which groups may be substituted with one or more fluorine atoms, with a phenyl group which may be substituted with a halogen atom, an alkyl group having 1-3 C- DIR 0430 atoms, methoxy or trifluoromethyl, or with the cyclopropyl group or R2 is cycloalkyl having 3-8 C- atoms which may be substituted with one or more alkyl groups having 1-4 C-atoms, or R2 is cycloalkenyl having 5-7 C-atoms, or R2 is a phenyl group substitu- ted with 0-2 groups R7, wherein R7 is straight or branched alkyl having 1-4 C-atoms which may be substituted with one or more fluorine atoms, or two alkyl groups R7 bound to adjacent carbon atoms constitute a ring annelated to the phenyl group and consisting of 5-7 C-atoms, or R7 is cycloalkyl, cycloalkoxy or cycloalkylthio having 3-7 C-atoms, or R7 is straight or branched alkoxycarbonyl having 1-4 C-atoms in the alkoxy group, or R7 is halogen or hydroxy; R3 is hydrogen or straight or branched alkyl having 1-6 C-atoms; and R4 is hydrogen, straight or branched alkyl having 1-4 C- atoms. It has been found that the compounds have good fibrinolytic properties and can be used in particular as orally active fibrinolytics.
Hamminga Derk
Jansen Johannes W. C. M.
Wijngaarden Ineke V.
Duphar International Research B.v.
Fetherstonhaugh & Co.
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