Diphenylalkylamine derivatives useful as opioid receptor agonists
First Claim
Patent Images
1. A compound represented by the following general formula (I) or a salt thereof:
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wherein, X represents the following group (II), (III), (IV), (V), or (VI),
n represents 1, 2 or 3, R1 and R2 each independently represent a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted, a lower alkenyl group which may be substituted, a lower alkoxy group which may be substituted or a hydroxy group, or R1 and R2 are combined to form the group —
O—
CH2—
O—
, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted, a lower alkenyl group which may be substituted, a lower alkoxy group which may be substituted, a hydroxy group, a cyano group, an amino group which may be substituted, a carbamoyl group which may be substituted, a carboxyl group, a (substituted or unsubstituted lower alkoxy)carbonyl group or a (substituted or unsubstituted lower alkyl)carbonyl group, R4 represents a saturated or unsaturated monocyclic or bicyclic carbocyclic group or a monocyclic or bicyclic heterocyclic group containing one or more hetero atoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom, R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom, a lower alkyl group which may be substituted, or a lower alkenyl group which may be substituted, and R3 and R4, R5 and R6, R7 and R8, or R9 and R10 may be linked to each other to form a cyclic structure.
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Abstract
A substance having affinity for an opioid δ receptor, which is represented by the following general formula (I):
wherein, X represents a group of the general formula: —CO—N(R5)(R6) (II) and the like, n represents 1 to 3, R1 and R2 represent a hydrogen atom, a halogen atom, a lower alkyl group and the like, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group and the like, R4 represents a saturated or unsaturated monocyclic or bicyclic carbocyclic group and the like, R5 to R12 represent a hydrogen atom, a lower alkyl group and the like, and R3 and R4, R5 and R6, R7 or R8 and R9 and R10 may bind to each other to form a cyclic structure, and a medicament useful for preventive and/or therapeutic treatment of central nervous system diseases and peripheral nervous system diseases comprising the substance as an active ingredient.
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Citations
20 Claims
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1. A compound represented by the following general formula (I) or a salt thereof:
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wherein, X represents the following group (II), (III), (IV), (V), or (VI), n represents 1, 2 or 3, R1 and R2 each independently represent a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted, a lower alkenyl group which may be substituted, a lower alkoxy group which may be substituted or a hydroxy group, or R1 and R2 are combined to form the group —
O—
CH2—
O—
,R3 represents a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted, a lower alkenyl group which may be substituted, a lower alkoxy group which may be substituted, a hydroxy group, a cyano group, an amino group which may be substituted, a carbamoyl group which may be substituted, a carboxyl group, a (substituted or unsubstituted lower alkoxy)carbonyl group or a (substituted or unsubstituted lower alkyl)carbonyl group, R4 represents a saturated or unsaturated monocyclic or bicyclic carbocyclic group or a monocyclic or bicyclic heterocyclic group containing one or more hetero atoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom, R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom, a lower alkyl group which may be substituted, or a lower alkenyl group which may be substituted, and R3 and R4, R5 and R6, R7 and R8, or R9 and R10 may be linked to each other to form a cyclic structure. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
wherein, R13 and R15 each independently represent a hydrogen atom, a lower alkyl group which may be substituted, or a lower alkenyl group which may be substituted, and R14 and R16 each independently represent a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted, a lower alkenyl group which may be substituted, a lower alkoxy group which may be substituted, a hydroxy group, a cyano group, an amino group which may be substituted, a nitro group, a carbamoyl group which may be substituted, a carboxyl group, a (substituted or unsubstituted lower alkoxy)carbonyl group or a (substituted or unsubstituted lower alkyl)carbonyl group.
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4. The compound or a salt thereof according to any one of claim 1, wherein X represents the group (II), (III), (V) or (VI),
n represents 2 or 3, R1 and R2 each independently represent a hydrogen atom, a halogen atom, a lower alkoxy group or a hydroxy group, or R1 and R2 represent — - O—
CH2—
O—R3 represents a hydrogen atom or a lower alkylcarbonyl group, R4 represents a residue of a benzene, indole and benzimidazole ring wherein a part of the unsaturated bonds of the ring may be hydrogenated to form a saturated bond(s), and a hydrogen atom on the ring may be substituted with an oxo group, a lower alkyl group, a hydroxymethyl group, or a benzyl group, or R3 and R4 are combined to form a cyclic structure selected from an imidazole, N-phenylimidazolidine, and an isoquinoline ring wherein the ring may be substituted with an oxo group or a lower alkyl group, and R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or a lower alkyl group, or R5 and R6 are combined to form a piperidine ring.
- O—
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5. The compound or a salt thereof according to any one of claim 1, wherein X represents the group (II).
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6. The compound or a salt thereof according to claim 2, wherein X represents the group (II).
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7. The compound or a salt thereof according to claim 3, wherein X represents the group (II).
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8. The compound or a salt thereof according to claim 4, wherein X represents the group (II).
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9. The compound or a salt thereof according to claim 1, wherein the compound or salt acts on an opioid δ
- receptor.
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10. A pharmaceutical composition, wherein the composition comprises at least one of a compound of general formula (I) according to claim 1 and a pharmacologically acceptable salt thereof as an active ingredient.
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11. The pharmaceutical composition according to claim 10, wherein the composition further comprises one or more pharmaceutical additives.
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12. The pharmaceutical composition according to claim 10, wherein the composition has an affinity for an opioid δ
- receptor.
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13. The pharmaceutical composition according to claim 10, wherein the composition is used for the treatment of at least one of depression, epilepsy and Parkinson'"'"'s disease.
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14. The pharmaceutical composition according to claim 10, wherein the composition is used for the treatment of pain.
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15. A method for the treatment of at least one of depression, epilepsy and Parkinson'"'"'s disease, wherein the method comprises the administration of a therapeutically effective amount of at least one of a compound according to claim 1 and a pharmacologically acceptable salt thereof to a mammal.
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16. The method according to claim 15, wherein the mammal is a human.
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17. A method for the treatment of pain, wherein the method comprises the administration of a therapeutically effective amount of at least one of a compound according to claim 1 and a pharmacologically acceptable salt thereof to a mammal.
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18. The method according to claim 17, wherein the mammal is a human.
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19. The compound or a salt thereof according to claim 1, wherein X represents the group (II), (III), (V) or (VI),
n represents 2 or 3, R1 and R2 each independently represent a hydrogen atom, a halogen atom, a lower alkoxy group or a hydroxy group, or R1 and R2 together represent — - O—
CH2—
O—
,R3 represents a hydrogen atom or a lower alkylcarbonyl group, R4 represents a residue of a benzene, an indole, or a benzimidazole ring, wherein a part of the unsaturated bonds of said ring may be hydrogenated to form one or more saturated bonds, and the ring may be substituted; and
R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or a lower alkyl group, or R5 and R6 are combined to form a piperidine ring.
- O—
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20. The compound or a salt thereof according to claim 1, wherein X represents the group (II), (III), (V) or (VI),
n represents 2 or 3, R1 and R2 each independently represent a hydrogen atom, a halogen atom, a lower alkoxy group or a hydroxy group, or R1 and R2 together represent — - O—
CH2—
O—
,R3 and R4 are combined to form a cyclic structure selected from an imidazole, an N-phenylimidazolidine, and an isoquinoline ring wherein the ring may be substituted with an oxo group or a lower alkyl group; and
R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or a lower alkyl group, or R5 and R6 are combined to form a piperidine ring.
- O—
Specification
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Current AssigneeMeiji Seika Kaisha Limited (Meiji Holdings Company Limited)
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Original AssigneeMeiji Seika Kaisha Limited (Meiji Holdings Company Limited)
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InventorsAsai, Kenji, Tsushima, Masaki, Kudo, Toshiaki, Miike, Naoko, Tadauchi, Kaori
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Primary Examiner(s)AULAKH, CHARANJIT
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Application NumberUS10/221,172Publication NumberTime in Patent Office551 DaysField of Search514/278, 514/322, 514/323, 514/331, 546/18, 546/20, 546/199, 546/201, 546/247US Class Current514/278CPC Class CodesA61P 25/00 Drugs for disorders of the ...A61P 25/04 Centrally acting analgesics...A61P 25/08 Antiepileptics; Anticonvuls...A61P 25/16 Anti-Parkinson drugsA61P 25/18 Antipsychotics, i.e. neurol...A61P 25/24 AntidepressantsA61P 25/28 for treating neurodegenerat...A61P 43/00 Drugs for specific purposes...C07D 211/32 by oxygen atoms
