Polycyclic compounds, their preparation and formulations...

C - Chemistry – Metallurgy – 07 – D

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167/207, 260/317

C07D 209/56 (2006.01) C07D 209/80 (2006.01) C07D 307/77 (2006.01) C07D 333/50 (2006.01)

Patent

CA 1256114

Abstract The present invention provides a compound of the formula (1): ArCH2NR1 (I) or a monomethyl or monoethyl ether thereof, the compound of formula (I) including the said ethers containing no more than 29 carbon atoms in total; an ester thereof; a salt thereof; wherein Ar is a 6,6,6,5 tetracyclic aromatic ring system having 15 to 17 ring atoms, the five membered ring containing one heteroatom, optionally substituted by one or two substituents, said substituents containing not more than four carbon atoms in total when taken together and being the same or different and are selected from halogen; cyano; C1-4 alkyl or C1-4 alkoxy, each optionally substituted by hydroxy or C1-2 alkoxy; halogen substituted C1-2 alkyl or C1-2 alkoxy; a group S(O)nR2 wherein n is an integer 0,1 or 2 and R is C1-2 alkyl optionally substituted by hydroxy or C1-2 alkoxy; or Ar is optionally substituted by a group NR3R4 containing not more than 5 carbon atoms wherein R3 and R4 are the same or different and each is a C1-3 alkyl group or NR3R4 forms a five- or six-membered heterocyclic ring optionally containing one or two additional heteroatoms; R1 contains not more than eight carbon atoms and is a group Image wherein m is 0 or 1; R5 and R6 are the same or different and each is hydrogen or C1-3 alkyl optionally substituted by hydroxy; R7 and R8 are the same or different and each is hydrogen or C1-3 alkyl; - Image is a five-or-six-membered saturated carbocyclic ring; R9 is hydrogen, methyl or hydroxymethyl; R10, R11 and R12 are the same or different and each is hydrogen or methyl; R13, is hydrogen, methyl, hydroxy, or hydroxymethyl. Also provided are methods for the preparation of the compounds of formula (I), intermediates in their preparations and pharmaceutical formulations containing them. The compounds of the Formula (I) are useful in the treatment of tumours.

495363

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