Rapamycin pyrazoles
US5164399A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 18, 1991 |
| Grant date | Nov 17, 1992 |
| Priority date | — |
| Expiry date | Nov 18, 2011 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D498/22
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A compound of the structure ##STR1## wherein Z is ##STR2## and R.sup.1 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.2 is present, R.sup.1 is absent; PA1 R.sup.2 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.1 is present, R.sup.2 is absent; PA1 the dotted lines in the pyrazole ring represent double bonds between the 31- and 32-positions and between the 33- and 53-positions when R.sup.1 is present and double bonds between the 31- and 52-positions and between the 32- and 33-positions when R.sup.2 is present; PA1 or a pharmaceutically acceptable salt thereof which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors. Intermediates possessing a 31,33-.beta.-dicarbonyl moiety that are useful for the same purposes are also described.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.