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filingDate 1989-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1991-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0357122-A3
titleOfInvention Use of beta-carbolines, their bio-isosteric benzofuran and benzothiophene analogues for the manufacture of a medicament having cytostatic properties
abstract The invention relates to a group of new β-carbolines, ntheir bio-isosteric benzofuran and benzothiophene analogu­nes, and to the preparation of these compounds. n The new compounds can be represented by the formula n nwherein n- R, R₁ and R₂ are hydrogen, or R + R₁ or R₁ + R₂ form a nsaturated heterocyclic ring having 5 or 6 ring atoms, nwhich comprise 1 or 2 oxygen atoms; n-R₃ is hydrogen, or hydroxy optionally derivatised with a nsugar radical the 4,6-hydroxy groups of which are nacetalised with an -ylidene group; n-R₄ is a group of the formula -C(R₁₁)₂-X-R₁₂, wherein the ngroups R₁₁ are hydrogen, or both groups R₁₁ together nrepresent a double-bonded keto oxygen atom, X is noxygen or a group NR₁₄, wherein R₁₄ is hydrogen or nalkyl having 1-4 Catoms, and R₁₂ is hydrogen, alkyl nhaving 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the ncarbamoyl group or mono- or dialkylcarbamoyl group nhaving 1-4 C-atoms per alkyl group; n-R₅ is hydrogen, alkanoyl or alkyl having 1-4 C-atoms, or nR₄ + R₅ together form a group of the formula n-C(R₁₁)₂-X-Z, wherein R₁₁ and X have the above-­nmentioned meanings and Z is bound to the ring nnitrogen atom and is a group nC=O,C=S, S→O or n n n n- R₇ and R₉ independently of each other are hydrogen or nalkoxy having 1-4 C-atoms, trifluoromethyl or nhalogen; n- R₈ is hydrogen, alkoxy or alkanoyloxy having 1-4 C-­natoms, hydroxy, halogen, benzyloxy, or R₈ and R₉ ntogether constitute a dioxyalkylidene bridge; n- A is oxygen, sulphur or a group nNR₆, and n- R₆ and R₁₃ independently of each other are hydrogen or nmethyl, or, when A is nitrogen, R₆ and R₁₃ together nmay form a ring having 5-7 C-atoms. n The compounds have good cytostatic properies.
priorityDate 1988-08-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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