Amino alcohol derivatives
AssigneeSankyo Company, Limited
InventorsTakahide Nishi, Toshiyasu Takemoto, Takaichi Shimozato, Futoshi Nara
Life of this patent
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Abstract
Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 aklene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 akylene group.
Claims52
A compound of formula (I) or a pharmacologically acceptable salt, ester or other derivative thereof:
- wherein:
- R1 and R2 are the same or different and each represents a hydrogen atom or an amino protecting group;
- R3 represents a hydrogen atom or a hydroxy protecting group;
- R4 represents a lower alkyl group;
- n represents an integer from 1 to 6;
- X represents an ethylene group, a vinylene group, an ethynylene group, a group of formula —D—CH2— (wherein D represents a carbonyl group, a group of formula —CH(OH)—, an oxygen atom, a sulfur atom, or a nitrogen atom), an aryl group, or an aryl group substituted with 1 to 3 substituents selected from substituent group a;
- Y represent a single bond, a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent groups a and b, a C1-C10 alkylene group which has an oxygen atom or a sulfur atom in said carbon chain or at the end of said carbon chain, or a C1-C10 alkylene group which is substituted with 1 to 3 substituents selected from substituent groups a and b and has an oxygen atom or a sulfur atom in said carbon chain or at the end of said carbon chain;
- R5 represents a hydrogen atom, a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl group substituted with 1 to 3 substituents selected from substituent groups a and b, an aryl group substituted with 1 to 3 substituents selected from substituent groups a and b, or a heterocyclic group substituted with 1 to 3 substituents selected from substituent groups a and b;
- R6 and R7 are the same or different and each represent a hydrogen atom or a group selected from substituent group a;
- with the proviso that when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group;
- substituent group a consists of a halogen atom, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a lower alkylthio group, a carboxyl group, a lower alkoxycarbonyl group, a hydroxyl group, a lower aliphatic acyl group, an amino group, a mono lower alkylamino group, a di lower alkylamino group, a lower aliphatic acylamino group, a cyano group, and a nitro group;
- substituent group b consists of a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl group substituted with 1 to 3 substituents selected from substituent group a, an aryl group substituted with 1 to 3 substituents selected from substituent group a, and a heterocyclic group substituted with 1 to 3 substituents selected from substituent group a.
A compound according to claimed 3 wherein Y is a lower alkylene group or a lower alkylene group which has an oxygen atom in said carbon chain or at the end of said carbon chain, or a pharmacologically acceptable salt, ester or other derivative thereof.
Dependencies are inferred from the claim text.