Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof
AssigneeTorrey Pines Institute for Molecular Studies
InventorsAdel Nefzi, John M. Ostresh, Richard A. Houghten
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Abstract
The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
Claims4
A compound having a structure corresponding to that shown in Formula III, below, or a pharmaceutically acceptable salt thereof:
- wherein:
- ═Z is ═O;
- Ra2 and Rb2 are absent;
- q is an integer that is one through seven;
- x and y are zero, and the sum of x+y is zero;
- the dotted line between the carbon atom of Ra1 and Ra2 and the carbon atom of Rb1 and Rb2 indicates the presence or absence of one additional bond between those depicted carbon atoms, so that when present, the additional bond is shown as a solid line, following usual conventions of organic chemistry, and Ra2 and Rb2 are absent;
- (a) Ra1, Ra2, Rb1 and Rb2 are independently selected from the group consisting of a hydrido, C1-C10 alkyl, C1-C10 substituted alkyl, C1-C10 phenylalkyl, C7-C16 substituted phenyalkyl, phenyl, substituted phenyl, C3-C7 cycloalkyl, and a C3-C7 substituted cycloalkyl group or (b) each of Ra1 and Rb1 is also bonded to the same saturated or unsaturated mono- or bicyclic ring that contains 5- to 8-members in each ring and zero to three heteroatoms in each ring that are independently oxygen, nitrogen or sulfur, or (c) one or both of Ra1 and Ra2 and Rb1 and Rb2 together are ═O, and wherein Ra2 and Rb2 are absent when a double bond is present between the depicted carbon atoms;
- R1 is selected from the group consisting of a hydrido, C1-C10 alkyl, C1-C10 substituted alkyl, C1-C10 phenylalkyl, C7-C16 substituted phenyalkyl, phenyl, substituted phenyl, C3-C7 cycloalkyl, and a C3-C7 substituted cycloalkyl group;
- R2 is a methyl, benzyl or naphthylmethyl group;
- R3 is selected from the group consisting of a hydrido, C1-C10 alkyl, C1-C10 substituted alkyl, C1-C16 phenylalkyl, C7-C16 substituted phenylalkyl, phenyl, substituted phenyl, C3-C7 cycloalkyl, and a C3-C7 substituted cycloalkyl group;
- R4 is selected from the group consisting of a hydrido, C1-C10 alkyl, C2-C10 alkenyl, C1-C10 substituted alkyl, C3-C7 substituted cycloalkyl, C7-C16 phenylalkyl, C7-C16 phenylalkenyl, and a C7-C16 substituted phenyl-alkenyl group;
- and
- R5 is selected from the group consisting of a hydrido, C1-C10 acyl, aroyl, C1-C10 alkylaminocarbonyl, C1-C10 alkylthiocarbonyl, arylaminocarbonyl, and an arylthiocarbonyl group.
Dependencies are inferred from the claim text.