C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/225, 260/271
C07D 471/04 (2006.01) C07D 471/14 (2006.01) C07D 471/16 (2006.01) C07D 491/04 (2006.01) C07D 491/048 (2006.01) C07D 491/14 (2006.01) C07D 495/04 (2006.01) C07D 498/14 (2006.01) C07D 498/22 (2006.01) C07D 515/14 (2006.01) C07F 9/6584 (2006.01)
Patent
CA 1337200
The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogu- es, and to the preparation of these compounds. The new compounds can be represented by the formula Image (I) wherein - R, R1 and R2 are hydrogen, or R + R1 or R1 + R2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms; - R3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group; - R4 is a group of the formula -C(R11)2-X-R12, wherein the groups R11 are hydrogen, or both groups R11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR14, wherein R14 is hydrogen or alkyl having 1-4 Catoms, and R12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group; - R5 is hydrogen, alkanoyl or alkyl having 1-4 C-atoms, or R4 + R5 together form a group of the formula -C(R11)2-X-Z, wherein R11 and X have the above- mentioned meanings and Z is bound to the ring nitrogen atom and is a group Image , Image , Image or Image - R7 and R9 independently of each other are hydrogen or alkoxy having 1-4 C-atoms, trifluoromethyl or halogen; - R8 is hydrogen, alkoxy or alkanoyloxy having 1-4 C- atoms, hydroxy, halogen, benzyloxy, or R8 and R9 together constitute a dioxyalkylidene bridge; - A is oxygen, sulphur or a group Image , and - R6 and R13 independently of each other are hydrogen or methyl, or, when A is nitrogen, R6 and R13 together may form a ring having 5-7 C-atoms. The compounds have good cytostatic properies.
609208
Hulkenberg Antonius
Van Wijngaarden Ineke
Duphar International Reseatch B.v.
Fetherstonhaugh & Co.
Hulkenberg Antonius
Van Wijngaarden Ineke
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