Stilbene derivatives

Claim 2

A stilbene compound represented by the formula (I): ##STR10## wherein R 1 and R 2 each independently represents hydrogen, lower alkyl, or cycloalkyl, with the proviso that both R 1 and R 2 cannot be hydrogen simultaneously, R 3 and R 4 independently represent hydrogen, methyl, or trifluoromethyl, and R 5 represents hydroxyl, lower alkoxyl, or lower alkylamino of the formula --NR 6 R 7 , wherein R 6 and R 7 each independently represents hydrogen or lower alkyl.

Claim 3

A compound according to claim 1, wherein R 1 represents isopropyl, cyclopropyl, or butyl.

Claim 4

A compound according to claim 1, wherein R 1 and R 2 each represents ethyl or isopropyl.

Claim 5

A compound according to claim 1, wherein R 3 and R 4 each represents hydrogen, methyl, or trifluoromethyl.

Claim 6

A compound of claim 1 which is [E-2-(3,4-di-isopropylphenyl)propenyl]benzoic acid.

Claim 7

A compound of claim 1 which is [E-2-(3-tert.-butylphenyl)ethenyl]benzoic acid.

Claim 8

Method for diagnosis to determine the type of leukemia which comprises the incubation of the blood of a patient with leukemia in vitro in the presence of a compound of claim 1, and the observation of morphological changes and/or of colony formation of the leukemia cell.

Claim 9

Use of one or more stilbene derivatives of claim 1 as medicaments for treatment of dermatological disorders of humans and animals.

Claim 10

A differentiation-inducing agent for neoplastic cells, especially leukemia cells, comprising as active ingredient one or more stilbene compounds of claim 1.

Claim 11

A compound of claim 1, which is [E-2-(4-tert.-butylphenyl)-3,3,3-trifluoropropenyl]-benzoic acid.

Claim 12

A compound of claim 1 which is [E-2-(3-cyclopropyl-phenyl)-ethenyl]benzoic acid.

Claim 13

A process for preparation of a stilbene represented by the formula (I): ##STR11## wherein R 1 and R 2 each independently represents hydrogen, lower alkyl or cycloalkyl, with the proviso that both R 1 and R 2 cannot be hydrogen simultaneously, R 3 and R 4 independently represent hydrogen, methyl, or trifluoromethyl, and R 5 represents hydroxyl, lower alkoxyl, or lower alkylamino of the formula --NR 6 R 7 , wherein R 6 and R 7 each independently represents hydrogen or lower alkyl, which comprises reacting a compound represented by the formula (II) ##STR12## wherein R 1 , R 2 and R 3 have the meanings previously assigned, with a compound represented by the formula (III) ##STR13## wherein R 5 has the meaning previously assigned and X represents a group represented by the formula: ##STR14## wherein R 4 has the meaning previously assigned and Y is an anion of an organic or inorganic acid or a dialkoxyphosphonylalkyl group represented by the formula: ##STR15## wherein R 4 has the value previously assigned and R represents a lower alkyl group and, if desired, converting the carboxylic acid ester group represented by the formula --COR 5 into the carboxylic acid group or a carbamide group.

Claim 14

A process for preparation of a stilbene represented by the formula (I): ##STR11## wherein R 1 and R 2 each independently represents hydrogen, lower alkyl or cycloalkyl, with the proviso that both R 1 and R 2 cannot be hydrogen simultaneously, R 3 and R 4 independently represent hydrogen, methyl, or trifluoromethyl, and R 5 represents hydroxyl, lower alkoxyl, or lower alkylamino of the formula --NR 6 R 7 , wherein R 6 and R 7 each independently represents hydrogen or lower alkyl, which comprises reacting a compound represented by the formula (II) ##STR12## wherein R 1 , R 2 and R 3 have the meanings previously assigned, with a compound represented by the formula (III) ##STR13## wherein R 5 has the meaning previously assigned and X represents a group represented by the formula: ##STR14## wherein R 4 has the meaning previously assigned and Y is an anion of an organic or inorganic acid or a dialkoxyphosphonylalkyl group represented by the formula: ##STR15## wherein R 4 has the value previously assigned and R represents a lower alkyl group and, if desired, converting the carboxylic acid ester group represented by the formula --COR 5 into the carboxylic acid group or a carbamide group.

Claim 15

Compound of claim 1 which is [E-2-(3,4-diethylphenyl)propenyl]benzoic acid.

Claim 16

Compound of claim 1 which is [E-2-(3,4-diethylphenyl)propenyl]benzoic acid methyl ester.