RU99101864A - NEW TIOPHENE DERIVATIVE AND CONTAINING HIS PHARMACEUTICAL COMPOSITION - Google Patents

Claims (11)

1. A thiophene derivative of the general formula I or a pharmaceutically acceptable salt thereof:

in which R ₁ represents the formula -A ₁ -X ₁ -R ₃ ,
R ₂ is a possible formula -A ₂ -X ₂ -R ₄ ,
ring B is 1) a 4-10-membered nitrogen-containing cycloalkyl ring, or 2) a 5- or 6-membered nitrogen-containing unsaturated heterocycle,
Ar ring is an aryl ring that can be substituted, or a 5- or 6-membered aromatic heterocycle, or an 8-10 membered aromatic bicyclic heterocycle that contains 1-4 one or more heteroatoms selected from the group consisting of nitrogen atom , the oxygen atom and the sulfur atom,
A ₁ , A ₂ and A _{3 are the} same or different from each other, and each represents a bond or a lower alkylene group,
X ₁ and X _{2 are the} same or different from each other, and each represents a bond or formula -O-, -S-, -NR ₅ -,

R ₅ , R ₆ , R ₇ , R ₈ , R ₉ , R ₁₀ , R ₁₁ , R ₁₂ and R _{13 are the} same or different from each other, and each represents a hydrogen atom or a lower alkyl group,
R ₃ and R _{4 are the} same or different from each other, and each represents a hydrogen atom, a cyclic imido group that can be substituted and can be condensed with a benzene ring, or a lower alkyl group, a cycloalkyl group, an aryl group or an aralkyl group, which can respectively be substituted, with the proviso that when Ar ring is thiazole ring, one of a ₁ and a ₂ represents a lower alkylene group when Ar ring is a thiophene ring, at least one of R ₃ and R ₄ represents a group Otley hydrochloric hydrogen atom; and if the Ar ring represents a benzene ring, the case when one of R ₁ and R ₂ represents a methyl group or a halogen atom, and the other represents a hydrogen atom, is excluded.  2. Derived thiophene or its pharmaceutically acceptable salt according to claim 1, where the ring is 4 - 10 membered nitrogen-containing cycloalkyl ring.  3. Derived thiophene or its pharmaceutically acceptable salt according to claim 1 or 2, where the ring is hexahydroazepine ring. 4. Derived thiophene or its pharmaceutically acceptable salt according to any one of paragraphs.1 to 3, where A ₃ represents a methylene group.  5. Derived thiophene or its pharmaceutically acceptable salt according to any one of paragraphs.1 to 4, where the ring Ar represents a 5-membered aromatic heterocycle, which contains 2 or 3 of one or more types of heteroatoms selected from the group consisting of a nitrogen atom, an atom oxygen and a sulfur atom, or a 9-membered aromatic heterocycle, which contains from 2 to 4 of one or more heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom.  6. Derived thiophene or its pharmaceutically acceptable salt according to any one of paragraphs. 1 to 5, where the ring Ar represents thiazole, oxadiazole, triazole, thiadiazole, imidazopyridine, imidazopyrimidine or triazolopyridazin.  7. The thiophene derivative according to claim 1, which is 5- [5 - [(Hexahydro-1H-azepin-1-yl) methyl] -2-thienyl] -3-phthalimidoyl-ethyl-1,2,4-oxadiazole , 5-amino-3- [5 - [(hexahydro-1H-azepin-1-yl) methyl] -2-thienyl] -1H-1,2,4-triazole or their pharmaceutically acceptable salts.  8. A pharmaceutical composition that contains a thiophene derivative or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 7 and a pharmaceutically acceptable carrier.  9. The pharmaceutical composition of claim 8, which is an anti-PCP agonist.  10. The pharmaceutical composition of claim 9, wherein the anti-PCP agonist is a psychotropic agent or an anti-schizophrenic agent.  11. The pharmaceutical composition according to claim 9, wherein the anti-PCP agonist is a medicine for preventing dementia, a medicine for improving problem behavior accompanied by dementia, a medicine for treating mental retardation in childhood and / or medicine for treating autism.