C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 260/276
C07D 471/04 (2006.01) A61K 31/44 (2006.01) C07D 209/10 (2006.01) C07D 209/14 (2006.01) C07D 209/16 (2006.01) C07F 9/40 (2006.01) C07F 9/58 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 1260475
ABSTRACT OF THE DISCLOSURE A .beta.-carboline of the formula Image wherein R3 is halogen; ORI, wherein RI is H, C1-5 alkyl, C3-7- cycloalkyl, C7-10-aralkyl or C6-10-aryl; NRIIRIII, wherein RII is H, C1-5alkyl, C3-7-cycloalkyl. C7-10-aralkyl or C6-10 aryl and RIII is C1-5 alkyl. C1-3-alkanoyl, C1-6 alkoxycarbonyl, carbamoyl, or RII and RIII together with the connecting N-atom are pyrrolyl or piperidino; SOnRI, wherein n is 0, 1 or 2 and RI is as defined above; PO3RIVRV, wherein RIV each independently is H, C1-5-alkyl, C3-7-cycloalkyl, C7-10-aralkyl or C6-10 aryl; or C3-7-cycloalkyl, C8-12-aralkenyl, or C6-10-aryl, each of whose alkyl portion may be substituted by 1 to 3 of halogen, OR,INRIIRIII, SOnRI, COORI, CONRIIRIII, CSNRIIRIII, PO3RIVRV, CORI or CN, wherein RI, RII, RIII, RIV, RV and n are as defined above; R4 is H, C1-5 alkyl, C1-5 alkoxy-C1-5-alkyl, CORVI or CSRVII, wherein RVI is H, C1-5-alkyl, C3-7-cycloalkyl, C7-10- aralkyl, OH, O-C1-5-alkyl, O-C3-7-cycloalkyl, O-C7-10-aralkyl or NRIIRII, wherein RII is as defined above and the RII's can be the same or different or both RII's together with the N are pyrrolyl or piperidino and wherein RVII is H, C1-5 alkyl, C3-7-cycloalkyl or C7-10-aralkyl; R5-R8 each independently is H, halogen NO2, ORI, NRIIRIII, PO3RIVRV, SO2NRIRV, COORI, CONRIIRIII, CSNRIIRIII and CORI wherein RI-V are as defined above and at most two of R5- R8 can be non-H; and R9 is H, C1-5 alkyl, C1-3-alkanoyl, carbamoyl, C1-6-alkoxycarbonyl, or SO2RVIII wherein RVIII is methyl or p-tolyl are valuable pharmaceutical products with long lasting action on the central nervous system.
439951
Biere Helmut
Braestrup Claus T.
Huth Andreas
Rahtz Dieter
Schmiechen Ralph
Marks & Clerk
Schering Aktiengesellschaft
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