Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful

Details Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful

1992-03-05

1993-01-05

Bond, Robert T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

A61K 31395, C07D49106

Patent

active

051772035

ABSTRACT:
A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

REFERENCES:
patent: 3929992 (1975-12-01), Seghal et al.
patent: 5091389 (1992-02-01), Ondekye et al.
patent: 5100899 (1992-03-01), Calne
Can. J. Physiol. Pharmacol. 55, 48(1977).

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