Tetrahydropyran derivatives
AssigneeSandoz Ltd.
InventorA. R. C. Murty Bulusu
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Abstract
The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances, in free form and, where such forms exist, in salt form. They can be prepared by various processes, e.g. by irradiation; oxidation; elimination; reduction; conversion by e.g. halogenation or acylation; deprotection of protected hydroxy groups; protection of free hydroxy groups; and separation of stereoisomeric mixtures into individual isomers. They are useful as pharmaceuticals, especially as antiinflammatory, and as antiproliferative and antiinflammatory agents.
Claims11
A compound of formula I ##STR24## wherein R.sub.1 represents a group of formula ##STR25## wherein either R.sub.7 represents optionally protected hydroxy, acyloxy, halogen,--OR.sub.10 wherein OR.sub.10 represents lower alkoxy, optionally protected --O(CH.sub.2).sub.m OH wherein m is a number from 2 to 4, or --OCONH.sub.2, and R.sub.7a represents hydrogen,
- or R.sub.7 and R.sub.7a together represent oxo,
- R.sub.8 represents hydroxy or methoxy, and
- R.sub.9 represents hydroxy or acyloxy;
- R.sub.2 represents hydrogen, acyloxy or optionally protected hydroxy and there is a single or a double bond between the two carbon atoms joined by a dotted line;
- R.sub.3 represents methyl, ethyl, n-propyl or allyl;
- either R.sub.4 represents hydrogen or hydroxy and R.sub.4a represents hydrogen,
- or R.sub.4 and R.sub.4a together represent oxo;
- either R.sub.5 represents hydroxy and R.sub.5a represents hydrogen,
- or R.sub.5 and R.sub.5a together represent oxo;
- and
- A represents a group of formula --CH(OR.sub.6)--CH.sub.2 --(CH.sub.2).sub.n -- or --CH.dbd.CH--(CH.sub.2).sub.n --, whereby the (CH.sub.2).sub.n -- part thereof is linked to the carbon atom,
- R.sub.6 represents lower alkyl and
- n represents the number 1 or 2;
- in free form or in pharmaceutically salt form.
The compound of formula I which is 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0..sup.4,9 ]-octacosa-5,18-diene-2,3,10,16-tetraone [1R,5Z,9S,12S-[1E(1R,3R,4R)], 13R,14S,17R,18E,21S,23S,24R,25S,27R].
Dependencies are inferred from the claim text.