Prodrugs for the improved delivery of non-steroidal anti-inflammatory agents
US4206220A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Jul 13, 1978 |
| Grant date | Jun 3, 1980 |
| Priority date | — |
| Expiry date | Jul 13, 1998 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D209/28
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Novel prodrug forms of carboxylic acid, non-steroidal, anti-inflammatory agents are disclosed, having the structural formula ##STR1## wherein ##STR2## represents the acyloxy residue of any non-steroidal anti-inflammatory drug which contains a carboxylic acid function; R.sub.1 and R.sub.2, which can be the same or different, each represents a member selected from the group consisting of C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, aryl, aralkyl, C.sub.5 -C.sub.6 cycloalkyl and C.sub.5 -C.sub.6 cycloalkenyl; or R.sub.1 and R.sub.2 are combined so that --NR.sub.1 R.sub.2 together form a member selected from the group consisting of a cycloheteroalkyl radical such as morpholino, 1-pyrrolidinyl, 4-methyl-1-piperazinyl or piperidino and a heteroaryl radical, such as 1-imidazolyl or 1-pyrazolyl; and the nontoxic pharmaceutically acceptable acid addition salts thereof. These compounds exhibit oral and topical anti-inflammatory activity when administered to warmblooded animals and are characterized as being more readily bioavailable, less irritating to topical and gastric mucosal membranes and more permeable through topical membranes, e.g., ophthalmic membrane, skin, etc., than are the …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.