| 摘要 |
<p>Preparation of cyclic urea compounds (I) from activated carbamic acid derivative(s) (II) is new. Preparation of cyclic urea compounds (I) from activated carbamic acid derivative(s) (II) containing a non-protected primary or secondary amine function involves selectively deprotecting a stable activated carbamic acid derivative (III) containing a protected primary or secondary amine function, by cleavage or conversion of the protecting group and cyclizing (II) by reaction between the amino and carbamic acid functions. Some compounds (I) are new. Independent claims are also included for the following: (1) new cyclic urea compounds (I'), having a ring of at least 7 (preferably 7-50, especially 7-20) members containing at least one amide function and at least one urea function, each of these functions being separated from the nearest adjacent amide or urea function by at least 1C (preferably 1-4C); and (2) new cyclic tri- and tetra-urea compounds of formula (I'') or (I'''). [Image] Q 1-Q 16H or the optionally protected side-chain of a natural or non-natural aminoacid; provided that the following compounds are excluded (with Q 1- Q 16being H unless specified otherwise): (I''; Q 3-Q 5, Q 7-Q 9, Q 11= Me), (I''; Q 3, Q 5, Q 7, Q 9, Q 11= Me), (I'''; Q 2, Q 6, Q 10, Q 14= Me) and (I'''; Q 2, Q 4, Q 6, Q 8, Q 10, Q 12, Q 14, Q 16= Me). ACTIVITY : Virucide; Anti-HIV. MECHANISM OF ACTION : HIV protease inhibitor; Factor Xa inhibitor.</p> |
