# US 5,344,833 A · Oxepane isomers of rapamycin useful as immunosuppressive agents

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- Number: US 5,344,833 A
- Document ID: US5344833A
- Status: Granted
- Kind: A
- Application number: 08/032,910
- Filed: 1993-03-18
- Granted: 1994-09-06
- Earliest claimed: 1992-01-16
- Assignees: American Home Products Corporation
- Inventors: Philip F. Hughes
- Web page: https://patentgrep.com/patent/US5344833A

## CPC

- C07D 471/18: Bridged systems
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A derivative of rapamycin of general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen, acyl, sulfonyl or alkyl or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

## Claims

### Claim 1

A method of treating transplantation rejection, and host vs. graft disease, in a mammal by administering an effective amount of a compound of formula (I) ##STR5## wherein R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen, acyl, sulfonyl or alkyl or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof and a solid or liquid pharmaceutically acceptable carrier.