首页> 外国专利> Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate receptor antagonist biological activity (S1P)

Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate receptor antagonist biological activity (S1P)

机译:带有芳基或杂芳基的吲哚-3-羧酸酰胺,酯,硫代酰胺和硫醇酸酯化合物具有鞘氨醇-1-磷酸受体拮抗剂的生物活性(S1P)

摘要

Compounds represented by having sphingosine-1-phosphate receptor agonist and / or antagonist biological activity represented by the general formula: ** Formula ** wherein: R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl having 1 to 12 carbons, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds, carbocyclic hydrocarbon groups having 3 to 20 carbon atoms, heterocyclic groups having up to 20 carbon atoms and at least one of oxygen, nitrogen and / or ring sulfur, halo, C1 to C12 haloalkyl, hydroxyl, C1 to C12 alkoxy, C3 to C20 arylalkyloxy, alkyl C1 to C12 carbonyl, formyl, oxycarbonyl, carboxy, C1 to C12 alkyl carboxylate, C1 to C12 alkyl amide, aminocarbonyl, amino, cyano, diazo, nitro, thio, sulfoxyl and sulfonyl groups; X is NH; X1 is selected from the group consisting of NR5, O, and S; R5 is hydrogen, an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons, phenyl or alkylphenyl where the alkyl group has 1-7 carbon atoms; Y is a phenyl group or a pyridyl group, each of which can be attached to A at any position; Z is O; n is 0 or an integer from 1 to 5; o is 0 or an integer from 1 to 3; p is 0 or an integer from 1 to 3; q is 1; r is 0 or 1; A is CH2; A1 and A2 are independently selected from the group consisting of (CH2) v where v is 0 or an integer from 1 to 12, branched chain alkyl having 3 to 12 carbons, cycloalkyl having 3 to 12 carbons, alkenyl which it has 2 to 10 carbons and 1-3 double bonds and alkynyl that has 2 to 10 carbons and 1 to 3 triple bonds; B is selected from the group consisting of hydrogen, OR6, COOR7, NR8R9, CONR8R9, COR10, CH = NOR11, CH = NNR12R13
机译:具有通式的代表的具有鞘氨醇-1-磷酸受体激动剂和/或拮抗剂生物活性的化合物代表:** **其中R1,R2,R3和R4独立地选自氢,直链或支链具有1至12个碳的链烷基,具有2至6个碳和1或2个双键的烯基,具有2至6个碳和1或2个三键的炔基,具有3至20个碳原子的碳环烃基,具有至多20个碳的杂环基碳原子和氧,氮和/或环硫,卤素,C1至C12卤代烷基,羟基,C1至C12烷氧基,C3至C20芳基烷氧基,烷基C1至C12羰基,甲酰基,氧羰基,羧基,C1至C12中的至少一个羧酸烷基酯,C1-C12烷基酰胺基,氨基羰基,氨基,氰基,重氮基,硝基,硫代,亚磺酰基和磺酰基。 X为NH; X1选自NR5,O和S; R5是氢,1至10个碳的烷基,5至10个碳的环烷基,苯基或烷基苯基,其中烷基具有1至7个碳原子; Y是苯基或吡啶基,它们各自可在任何位置连接于A; Z为O; n为0或1到5的整数; o是0或1到3的整数; p为0或1至3的整数; q是1; r为0或1; A是CH 2; A1和A2独立地选自(CH2)v,其中v为0或1至12的整数,具有3至12个碳的支链烷基,具有3至12个碳的环烷基,具有2至10的烯基碳和1-3个双键和具有2-10个碳和1-3个三键的炔基; B选自氢,OR6,COOR7,NR8R9,CONR8R9,COR10,CH> = NOR11,CH> = NNR12R13

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