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US 6,306,877 B1Granted
Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists
AssigneeThe Procter & Gamble Company
InventorsThomas Lee Cupps, Sophie Eva Bogdan, Raymond Todd Henry, Russell James Sheldon, William Lee Seibel, Jeffrey Joseph Ares
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Abstract
This invention involves compounds having the following structure as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.
Claims25
A compound of formula:
- wherein:
- a) R1 is selected from the group consisting of hydrogen, alkyl and nil;
- where R1 is nil, bond (a) is a double bond;
- b) D is CR2 where R2 is selected from the group consisting of hydrogen, unsubstituted C1-C3 alkanyl, amino, hydroxy, mercapto, C1-C3 alkylthio, C1-C3 alkoxy and C1-C3 alkylamino;
- c) B is CR3═CR8;
- wherein R3 and R8 are each independently selected from the group consisting of hydrogen, unsubstituted C1-C3 alkanyl, unsubstituted C1-C3 alkenyl, unsubstituted C1-C3 alkynyl, cycloalkanyl, cycloalkenyl, unsubstituted C1-C3 alkylthio, unsubstituted C1-C3 alkoxy, hydroxy, thio, nitro, cyano, amino, C1-C3 alkylamino, C1-C3 dialkylamino and halo;
- d) R4, R5 and R6 are each independently selected from the group consisting of hydrogen, unsubstituted C1-C3 alkanyl, unsubstituted C1-C3 alkenyl, unsubstituted C1-C3 alkynyl, cycloalkanyl, cycloalkenyl, unsubstituted C1-C3 alkylthio, unsubstituted C1-C3 alkoxy, hydroxy, thio, nitro, cyano, amino, C1-C3 alkylamino, C1-C3 dialkylamino, halo and NH—NH—C(═NR10)NHR11 (guanidinylamino);
- wherein R10 and R11 are independently selected from the group consisting of hydrogen, methyl and ethyl;
- wherein one and only one of R4, R5 and R6 is guanidinylamino;
- e) R7 is selected from the group consisting of hydrogen, unsubstituted C1-C3 alkanyl, unsubstituted C1-C3 alkenyl, unsubstituted C1-C3 alkynyl, cycloalkanyl, cycloalkenyl, unsubstituted C1-C3 alkylthio, unsubstituted C1-C3 alkoxy, hydroxy, thio, nitro, cyano, amino, C1-C3 alkylamino, C1-C3 dialkylamino and halo;
- or an enantiomer, optical isomer, stereoisomer, diastereomer, tautomer, addition salt, biohydrolyzable amide and ester thereof.
8 more elements
Dependencies are inferred from the claim text.