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US 5,856,107 AGranted
Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein
AssigneeTrega Biosciences, Inc.
InventorsJohn M. Ostresh, Richard A. Houghten
Life of this patent
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Abstract
The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
Claims14
A library of two or more imidazole compounds comprising the structure:
- ##STR18## wherein R.sup.1 is selected from the group consisting of a hydrogen atom, halo, hydroxy, protected hydroxy, C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 substituted alkyl, amino, carboxy, and protected carboxy;
- R.sup.2 is selected from the group consisting of a hydrogen atom, C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 substituted alkyl, phenyl, substituted phenyl, C.sub.7 to C.sub.16 phenylalkyl, C.sub.7 to C.sub.16 substituted phenylalkyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.3 to C.sub.7 substituted cycloalkyl, benzyl, substituted benzyl, naphthyl, substituted naphthyl, and when taken in conjunction with C1 and N2 to form a piperidine or benzopiperidine;
- R.sup.3 is selected from the group consisting of C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 substituted alkyl, C.sub.2 to C.sub.10 alkenyl, C.sub.2 to C.sub.10 substituted alkenyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.3 to C.sub.7 substituted cycloalkyl, phenyl, substituted phenyl, C.sub.7 to C.sub.16 phenylalkyl, C.sub.7 to C.sub.16 substituted phenylalkyl, C.sub.7 to C.sub.16 phenylalkenyl, C.sub.7 to C.sub.16 substituted phenylalkenyl, benzyl, substituted benzyl, naphthyl, substituted naphthyl, heterocycle, and substituted heterocycle;
- X is selected from the group consisting of a nitrogen atom (N) and a sulfur atom (S);
- and
- Y is selected from the group consisting of a hydrogen atom and methyl.
3 more elements
A single imidazole compound comprising the structure:
- ##STR19## wherein:
- R.sup.1 is selected from the group consisting of a hydrogen atom, halo, hydroxy, protected hydroxy, C.sub.3 to C.sub.10 alkyl, C.sub.1 to C.sub.10 substituted alkyl, amino, carboxy, and protected carboxy;
- R.sup.2 is selected from the group consisting of a hydrogen atom, C.sub.1 to C.sub.10 alkyl, C.sub.3 to C.sub.10 substituted alkyl, phenyl, substituted phenyl, C.sub.7 to C.sub.16 phenylalkyl, C.sub.7 to C.sub.16 substituted phenylalkyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.3 to C.sub.7 substituted cycloalkyl, benzyl, substituted benzyl, naphthyl, substituted naphthyl, and when taken in conjunction with C1 and N2 to form a piperidine or benzopiperidine;
- R.sup.3 is selected from the group consisting of C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.10 substituted alkyl, C.sub.2 to C.sub.10 alkenyl, C.sub.2 to C.sub.10 substituted alkenyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.3 to C.sub.7 substituted cycloalkyl, phenyl, substituted phenyl, C.sub.7 to C.sub.16 phenylalkyl, C.sub.7 to C.sub.16 substituted phenylalkyl, C.sub.7 to C.sub.16 phenylalkenyl, C.sub.7 to C.sub.16 substituted phenylalkenyl, benzyl, substituted benzyl, naphthyl, substituted naphthyl, heterocycle, and substituted heterocycle;
- X is a nitrogen atom (N) or a sulfur atom (S);
- and
- Y is selected from the group consisting of a hydrogen atom and methyl.
4 more elements
Dependencies are inferred from the claim text.