Patent EA-002123-B1 (EA)
Title: Compounds potentiating retinoids
Inventor: SHUDO KOICHI
IPC: A61K31/55
Filed: 1996-09-20
Abstract: 1. A compound represented by the following general formula (I):   or the following general formula (II) or salts thereof: wherein R<1> represents hydrogen atom or a C1-6 alkyl group; R<2> and R<3> independently represent hydrogen atom or a C1-6 alkyl group, or R<2> and R<3> may combine together with the carbon atoms of the phenyl ring to which R<2> and R<3> bind to represent a 5- or 6-membered cycloalkyl group which may optionally be substituted with one or more C1-4 alkyl groups; R<4> represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, hydroxyl group, nitro group, or a halogen atom; X represents -NR<7>-, -O-, -CHR<7>- or -S- in which R<7> represents hydrogen atom, a C1-6 alkyl group, or an aryl-substituted C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. 2. The compound according to claim 1 which is selected from the group consisting of the following compounds or a salt thereof: 4-[5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyldibenzo[b,e][1,4]diazepin-11-yl]benzoic acid (HX600); 4-[5H-2,3-diisopropyl-5-methyldibenzo[b,e][1,4]diazepin-11-yl]benzoic acid (HX610); 4-[5H-2-tert-butyl-5-methyldibenzo[b,e][1,4]diazepin-11-yl]benzoic acid (HX511); 4-[5H-3,4-(1,4-butano)-5-methyldibenzo[b,e][1,4]diazepin-11-yl]benzoic acid (HX545); 4-[5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyl-8-nitrodibenzo[b,e][1,4]-diazepin-11-yl]benzoic acid (HX531); 4-[2,3-(2,5-dimethyl-2,5-hexano)dibenzo[b,f][1,4]oxazepin-11-yl]benzoic acid (HX620); 4-[2,3-(2,5-dimethyl-2,5-hexano)dibenzo[b,f][1,4]thiazepin-11-yl]benzoic acid (HX630); 5-[5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyldibenzo[b,e][1,4]diazepin-11-yl]-2-pyridinecarboxylic acid; 6-[5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyldibenzo[b,e][1,4]diazepin-11-yl]-3-pyridinecarboxylic acid; and 4-[2,3-(2,5-dimethyl-2,5-hexano)dibenzo[b,e]azepin-11-yl]benzoic acid (HX640). 3. A medicament comprising a compound or a physiologically acceptable salt thereof according to claim 1. 4. The medicament according to claim 3, wherein said medicament is in the form of a pharmaceutical composition comprising a compound or a physiologically acceptable salt thereof according to claim 1 together with one or more pharmaceutical additives. 5. The medicament according to claim 3, wherein said medicament is used as an agent for enhancing the activity of a physiologically active substance which exerts the physiological activity by binding to an intranuclear receptor that belongs to the intranuclear receptor super family. 6. The medicament according to claim 5, wherein the physiologically active substance is a retinoid compound. 7. A pharmaceutical composition comprising a compound according to claim 1 or a physiologically acceptable salt thereof together with a retinoid compound. 8. A method for enhancing the activity of a physiologically active substance which exerts the physiological activity by binding to an intranuclear receptor that belongs to the intranuclear receptor super family, which comprises a step of administering a compound of claim 1 or a physiologically acceptable salt thereof to a mammal. 9. The method according to claim 8, wherein the physiologically active substance is a retinoid compound. 10. The method according to claim 8, wherein the physiologically active substance is retinoic acid which inherently exist in the living body of said mammal.