Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsMasakuni Okuhara, Hirokazu Tanaka, Toshio Goto, Tohru Kino, Hiroshi Hatanaka
Life of this patent
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Abstract
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.
Claims12
A compound of the formula:
- ##STR10## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy and pharmaceutically acceptable organic sulfonic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond, provided that when R.sup.1 and R.sup.2 are each hydroxy, n is an integer of 2 and the symbol of a line and dotted line is a single bond, then R.sup.3 is methyl, propyl or allyl, and a pharmaceutically acceptable basic salt thereof.
A compound of the formula:
- ##STR11## wherein R.sup.1 is hydroxy;
- lower alkylthioalkoxy;
- tri(lower)alkylsilyloxy;
- lower alkyldiphenylsilyloxy;
- lower alkanoyloxy optionally substituted with carboxy;
- lower cycloalkoxy(lower)alkanoyloxy optionally substituted with two lower alkyl groups on the lower cycloalkyl moiety;
- camphorsulfonyloxy;
- aroyloxy optionally substituted with one or more nitro groups, in which the aroyl moiety is selected from the group consisting of benzoyl, toluoyl, xyloyl and naphthoyl;
- arenesulfonyloxy optionally substituted with halogen, in which the arene moiety is selected from the group consisting of benzene, toluene, xylene and naphthalene;
- or phenyl(lower)alkanoyloxy optionally substituted with lower alkoxy and trihalo(lower)alkyl;
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond, provided that when R.sup.1 and R.sup.2 are each hydroxy, n is an integer of 2 and the symbol of a line and dotted line is a single bond, then R.sup.3 is methyl, propyl or allyl, and a pharmaceutically acceptable basic salt thereof.
The compound 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-I-methylviny l]-23,25-dimethoxyI-3,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone.
The compound 12-[2-(4-acetoxy-3-methoxycyclohexyl)-1-methylvinyl]-17-allyl-1,14-dihydro xy-23,25-dimethoxy-13,191,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3. 1.0 4,9]-octacos-18-ene-2,3,10,16-tetraone.
The compound 14-acetoxy-12-[2-(4-acetoxy-3-methoxycyclohexyl)-1-methylvinyl]-17-allyl-1 -hydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[ 22.3.1.0 4,9]octacos-18-ene-2,3,10,16-tetraone.
The compound 1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25- dimethoxy-13,19,17,21,27-pentamethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9]-octacos-18-ene-2,3,10,16-tetraone.
The compound 16-allyl-1,13-dihydroxy-11-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-22,24-dimethoxy-12,18,20,26-tetramethyl-10,27-dioxa-4-azatricyclo[21.3.1 .0.sup.4,8 ]heptacos-17-ene-2,3,9,15-tetraone.
Dependencies are inferred from the claim text.