TH100511A - Morpholine derivatives - Google Patents

Abstract

DC60 (10/09/51) This invention provides morpholine derivatives according to the formula [I]; (chemical formula) where R1 is a substituted alkyl group, selectively substituted aryl group, selectively substituted heterocyclogroup, cycloalkyl group or alkyl group; R2 is a substituted alkyl group, selectively substituted aryl group, selectively substituted heterocyclogroup, selectively substituted alkylcarbonyl group, selectively substituted arylcarbonyl group, carbonyl group substituted by a selectively substituted heterocyclogroup or cycloalkylcarbonyl group; T is methylene group or carbonyl group; R3, R4, R5 and R6 are the same or different and are hydrogen atoms, selectively substituted carbamoyl group or selectively substituted alkyl group; These compounds would be useful as renin inhibitors. This invention provides morpholine derivatives according to the formula [I]; (chemical formula) where R1 is a substituted alkyl group, selectively substituted aryl group, selectively substituted heterocyclogroup, cycloalkyl group or alkyl group; R2 is a substituted alkyl group, selectively substituted aryl group, selectively substituted heterocyclogroup, selectively substituted alkylcarbonic group, selectively substituted arylcarbonic group, selectively substituted heterocyclogroup or cycloalkylcarbonyl group; T is methylene group or carbonyl group; R3, R4, R5 and R6 are identical or different and are hydrogen atoms, selectively substituted carbamoyl groups or selectively substituted alkyl groups; These compounds are useful as renin inhibitors.

Claims (2)

1. Morfoline derivative according to the general formula [I] (chemical formula) where R1 is A) alkyl group substituted by a selected group from 1) alkyl C substituted group. Selectively substituted groups are: 1) hydroxyl group, 2) halogen atom, 3) selectively substituted aryl group, 5) selectively substituted tetrahydronaphtyl group, 6) selectively substituted indolyl group, 7) selectively substituted basofuranyl group, 8) selectively substituted benzothiinyl group, 9) selectively substituted quinolyl group, 10) selectively substituted dihydrochrominyl group, 11) selectively substituted dihydrobonsofuranyl group, 12) selectively substituted indazolyl group, 13) selectively substituted pyrrolopyridinyl group, 14) selectively substituted benzoxazinyl group. Selectively replaced groups are: 15) selectively replaced xanthinyl groups, 16) selectively replaced indylyl groups, and 17) selectively replaced imidasopyridinyl groups; B) selectively replaced aryl groups; C) selectively replaced heterozocol groups; D) cycloalkyl groups; or E) alkyl groups; R2 is A) an alkyl group replaced by a group selected from 1) alkyl C groups. Selectively substituted groups are: 1) hydroxyl group, 2) halogen atom, 3) selectively substituted aryl group, 5) selectively substituted tetrahydronaphtyl group, 6) selectively substituted indolyl group, 7) selectively substituted basofuranyl group, 8) selectively substituted benzothiinyl group, 9) selectively substituted quinolyl group, 10) selectively substituted dihydrochrominyl group, 11) selectively substituted dihydrobonsofuranyl group, 12) selectively substituted indazolyl group, 13) selectively substituted pyrrolopyridinyl group, 14) selectively substituted benzoxazinyl group. The denominated groups are: 15) selectively denominated xanthinyl groups, 16) selectively denominated indylyl groups, and 17) selectively denominated imidazopyridinyl groups; B) selectively denominated aryl groups; C) selectively denominated heterocyclol groups; D) selectively denominated alkyl carbonyl groups; E) selectively denominated aryl carbonyl groups; F) carbonyl groups denominated by selectively denominated heterocyclol groups; or G) cycloalkyl carbonyl groups. T is either a methylene or carbonyl group; and R3, R4, R5, and R6 are the same or different. A is a hydrogen atom, a selectively denominated carbamoyl group, or a selectively denominated alkyl group; or their pharmaceutically acceptable salts. 2. Morpolyne derivatives according to the general formula [II], where R1 is A) the alkyl group substituted by the selected group from 1) the alkyl C group substituted. Selectively substituted groups are: 1) hydroxyl group, 2) halogen atom, 3) selectively substituted aryl group, 5) selectively substituted tetrahydronaphtyl group, 6) selectively substituted indolyl group, 7) selectively substituted basofuranyl group, 8) selectively substituted benzothiinyl group, 9) selectively substituted quinolyl group, 10) selectively substituted dihydrochrominyl group, 11) selectively substituted dihydrobonsofuranyl group, 12) selectively substituted indazolyl group, 13) selectively substituted pyrrolopyridinyl group, 14) selectively substituted benzoxazinyl group. Selectively replaced groups are: 15) selectively replaced xanthinyl groups, 16) selectively replaced indylyl groups, and 17) selectively replaced imidasopyridinyl groups; B) selectively replaced aryl groups; C) selectively replaced heterozocol groups; D) cycloalkyl groups; or E) alkyl groups; R2 is A) an alkyl group replaced by a group selected from 1) alkyl C groups. Selectively substituted groups are: 1) hydroxyl group, 2) halogen atom, 3) selectively substituted aryl group, 5) selectively substituted tetrahydronaphtyl group, 6) selectively substituted indolyl group, 7) selectively substituted basofuranyl group, 8) selectively substituted benzothiinyl group, 9) selectively substituted quinolyl group, 10) selectively substituted dihydrochrominyl group, 11) selectively substituted dihydrobonsofuranyl group, 12) selectively substituted indazolyl group, 13) selectively substituted pyrrolopyridinyl group, 14) selectively substituted benzoxazinyl group. The denominated groups are: B) selectively denominated xanthinyl groups, 16) selectively denominated indyl groups, and 17) selectively denominated imidazopyridinyl groups; C) selectively denominated heterocyclo groups; D) selectively denominated alkyl carbonyl groups; E) selectively denominated aryl carbonyl groups; F) carbonyl groups denominated by selectively denominated heterocyclo groups; or G) cycloalkyl carbonyl groups. T is either the methylene group or the carbonyl group; R3, R4, R5, and R6 are the same or different and represent the hydrogen atom, selectively denominated carbamoyl group, or selectively denominated alkyl group; and P1 is the protective group; or its pharmaceutically acceptable salts.