Diphenyl-triazole derivatives and their use as anti-gestative, immuno-suppressant and anti-tumoral agents
AssigneeGeange Ltd.
InventorCarla Rossi
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I), wherein X and Y are independently carbon or nitrogen but not both simultaneously carbon, R1 is a group (II) and R2 is a group (III), R5 being a carbonate, carbamate or phosphate residue, are useful as anti-gestative, immuno-suppressant and anti-tumor agents
Claims22
A nitrogen heterocyclic aromatic derivative having the following general formula:
- where X and Y are selected from N, C and CH, provided they are different from each other, or X and Y are both nitrogen;
- R is hydrogen or —COR8 where R8 is a saturated or non-saturated C1-C10 alphatic hydrocarbon, R1 has the following general formula:
- where R3 is hydrogen, halogen, C1-C10 alkyl or C1-C10 alkoxyl, R4 is hydrogen, C1-C10 alkyl or C1-C10 alkoxyl, or R3 and R4 together form a methylendioxy group;
- R2 has the following general structure:
- and R5 is selected from:
- where Z=OR7 where R7 is a saturated or non-saturated, linear or branched C1-C10 aliphatic hydrocarbon, or R7 has the following formula:
- where R, R1, X and Y are defined as above and R6 is hydrogen, halogen, alkyl or alkoxyl C1-C10, or Z is NHR8 where R8 is a linear or branched C1-C20 alkyl chain,
- provided that when X=Y=N and R is H or —CONHCH2CH3, Z is not NHR8 where R8 is —CH2CH3, and provided that R1 and R2 are not located on two adjacent atoms of the heterocyclic aromatic ring, and further provided that when X=Y=N and R5 is —COZ where Z=OR7, R7 is a saturated or non-saturated linear or branched C5-C20 aliphatic hydrocarbon.
Nitrogen heterocyclic aromatic derivative having the following structure:
A method of reducing the humoral and cellular immunological response of a mammal comprising administering an effective amount of a nitrogen heterocyclic aromatic derivative having the following general formula:
- where X and Y are selected from N, C and CH, provided they are different from each other, or X and Y are both nitrogen;
- R is hydrogen or —COR8 where R8 is a saturated or non-saturated C1-C10 aliphatic hydrocarbon, R1 has the following general formula:
- where R3 is hydrogen, halogen,C1-C10 alkyl or C1-C10 alkoxyl, R4 is hydrogen, C1-C10 alkyl or C1-C10 alkoxyl, or R3 and R4 together form a methylendioxy group;
- R2 has the following general structure:
- and R5 is selected from:
- where Z=OR7 where R7 is a saturated or non-saturated, linear or branched C1-C10 aliphatic hydrocarbon, or R7 has the following formula:
- where R, R1, X and Y are defined as above and R6 is hydrogen, halogen, alkyl or alkoxyl C1-C10, or Z is NHR8 where R8 is a linear or branched C1-C20 alkyl chain,
- provided that when X=Y=N and R is H or —CONHCH2CH3, Z is not NHR8 where R8 is —CH2CH3, and provided that R1 and R2 are not located on two adjacent atoms of the heterocyclic aromatic ring, and further provided that when X=Y=N and R5 is —COZ where Z=OR7, R7 is a saturated or non-saturated linear or branched C5-C20 aliphatic hydrocarbon.
A method of treating a tumor susceptible to therapy comprising administering an effective amount of a nitrogen heterocyclic aromatic derivative having the following general formula:
- where X and Y are selected from N, C and CH, provided they are different from each other, or X and Y are both nitrogen;
- R is hydrogen or —COR8 where R8 is a saturated or non-saturated C1-C10 aliphatic hydrocarbon, R1 has the following general formula:
- where R3 is hydrogen, halogen, C1-C10 alkyl or C1-C10 alkoxyl, R4 is hydrogen, C1-C10 alkyl or C1-C10 alkoxyl, or R3 and R4 together form a methylendioxy group;
- R2 has the following general structure:
- and R5 is selected from:
- where Z=OR7 where R7 is a saturated or non-saturated, linear or branched C1-C10 aliphatic hydrocarbon, or R7 has the following formula:
- where R, R1, X and Y are defined as above and R6 is hydrogen, halogen, alkyl or alkoxyl C1-C10, or Z is NHR8 where R8 is a linear or branched C1-C20 alkyl chain,
- provided that when X=Y=N and R is H or —CONHCH2CH3, Z is not NHR8 where R8 is —CH2CH3, and provided that R1 and R2 are not located on two adjacent atoms of the heterocyclic aromatic ring, and further provided that when X=Y=N and R5 is —COZ where Z=OR7, R7 is a saturated or non-saturated linear or branched C5-C20 aliphatic hydrocarbon.
Dependencies are inferred from the claim text.