Benzylated PDE4 inhibitors
US6555572B2 · kind B2 · utility
25Cited by
18References
11Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Mar 16, 2001 |
| Grant date | Apr 29, 2003 |
| Priority date | — |
| Expiry date | Mar 16, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D473/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.