Dyarylacetylenes, their preparation and their use

C - Chemistry – Metallurgy – 07 – C

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C07C 65/19 (2006.01) C07C 33/38 (2006.01) C07C 43/168 (2006.01) C07C 43/215 (2006.01) C07C 45/44 (2006.01) C07C 45/68 (2006.01) C07C 47/548 (2006.01) C07C 47/57 (2006.01) C07C 47/575 (2006.01) C07C 49/683 (2006.01) C07C 49/747 (2006.01) C07C 49/757 (2006.01) C07C 49/798 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01) C07C 57/50 (2006.01) C07C 63/66 (2006.01) C07C 63/74 (2006.01) C07C 65/28 (2006.01) C07C 65/38 (2006.01) C07C 69/94 (2006.01) C07D 257/04 (2006.01)

Patent

CA 1266672

ABSTRACT OF THE DISCLOSURE: Disclosed are novel diarylacetylene of the formula I: Image I where R1 and R2 are each hydrogen or methyl, R3 is hydrogen, methyl, hydroxyl or C1-C6-alkoxy, R4 is hydrogen, methyl or methoxy, R5 is hydrogen, halogen, methoxy or C1-C4-alkyl, A is a methylene or ethylene radical which is unsubstituted or substituted by C1-C4-alkyl or is -CH=CH-, -CHOH-CH2- or -CO-CH2-, and R is hydrogen, methyl, nitrile, tetrazolyl, C2-C10-ketal or a radical -CHR7-OR8, -CHR7-NR9R10, -COR11, -CR12=CH-COOR13 or -CR12=CH-CO-NR14R15, where R7 is hydrogen or C1-C4-alkyl, R8 is hydrogen, C1-C4-alkyl, C1-C20- alkanoyl, unsubstituted or substituted benzoyl or a radical -P(0) (OR13)2 or -P(0) (NR14R15)2 (where R13 is hydrogen, unsubstituted or hydroxyl-substituted C1-C8-alkyl, unsubstituted or substituted aryl, or aralkyl which is unsubstituted or substituted in the aryl moiety, and R14 and R15 are each hydrogen, unsubstituted or hydroxyl-substituted C1-C6-alkyl, or an unsubstituted or substituted aralkyl or aryl group), R9 and R10 are each hydrogen, C1-C4-alkyl, C1- C6-unsubstituted or substituted benzoyl, R11 is hydrogen, halogen, C1-C4-alkyl or a radical NR14R15 or -OR13 (where R13, R14 and R15 have the above meanings) and R12 is hydrogen or methyl, and, where relevant, its physiologically tolerated salts. These derivatives are useful for the treatment of dermatological disorders and the prophylactic and therapeutic treatment of precanceroses and tumors.

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