α-aminocyclolactam ligands for G-protein coupled receptors
US8008289B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 10, 2005 |
| Grant date | Aug 30, 2011 |
| Priority date | — |
| Expiry date | Jan 24, 2027 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/08
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein y is any integer from 1 to 8; z is one integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1; y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or y is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively R1 may be selected from a peptido radical, for example having from 1 to 4 pe…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.