Novel amide compounds
First Claim
1. A compound of the formula (I):
- R1-A-X-NHCO—
Y—
R2 wherein R1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents, R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents, A is a group of the formula;
—
(CH2)t—
(O)m—
or
in which R3 and R4 are each hydrogen or linked together to form imino, R5 is hydrogen or lower alkyl, t is 0, 1 or 2, p, m and n are each 0 or 1, X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents, Y is bond, lower alkylene, or lower alkenylene, and a salt thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
A compound of the formula (I):
R1-A-X-NHCO—Y—R2
wherein
R1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents,
R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents,
A is a group of the formula:
—(CH2)t—(O)m—
or
which R3 and R4 are each hydrogen or linked together to form imino,
R5 is hydrogen or lower alkyl,
t is 0, 1 or 2,
p, m and n are each 0 or 1,
X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents,
Y is bond, lower alkylene, or lower alkenylene,
and a salt thereof.
86 Citations
18 Claims
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1. A compound of the formula (I):
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R1-A-X-NHCO—
Y—
R2wherein R1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents, R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents, A is a group of the formula;
—
(CH2)t—
(O)m—
or
in which R3 and R4 are each hydrogen or linked together to form imino,R5 is hydrogen or lower alkyl, t is 0, 1 or 2, p, m and n are each 0 or 1, X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents, Y is bond, lower alkylene, or lower alkenylene, and a salt thereof. - View Dependent Claims (2, 12, 13, 14, 15, 16, 17, 18)
R2 is fluorenyl;
indolyl which have 1 to 3 lower alkyl;
phenyl;
phenyl which have 1 to 3 halogen;
phenyl which have 1 to 3 lower alkyl;
phenyl which have 1 to 3 lower alkoxy;
phenyl which have 1 to 3 trihalo(lower)alkyl;
phenyl which have 1 to 3 cyano;
phenyl which have halophenyl;
phenyl which have phenyl;
phenylsulfanyl;
phenyl which have lower alkylphenyl;
phenyl which have thienyl;
phenyl which have halothienyl;
pyridyl;
thienyl which have phenyl;
carbazolyl;
carbazolyl which have 1 to 3 halogen;
carbazolyl which have 1 to 3 trihalo(lower)alkyl and/or lower alkyl;
naphthyl;
2,3-dihydorobenzo[b]oxepinyl;
2,3-dihydorobenzo[b]oxepinyl which have 1 to 3 lower alkyl;
2,3-dihydorobenzo[b]oxepinyl which have 1 to 3 halogen;
2,3-dihydoro-benzo[b]oxepinyl which have 1 to 3 lower alkanesulfonyl;
2,3-dihydoro-benzo[b]oxepinyl which have 1 to 3 lower alkoxy;
2,3-dihydoro-benzo[b]thiepinyl which have dioxo;
8,9-dihydoro-benzocycloheptyl;
chromenyl which have 1 to 3 halogen;
indolyl;
indolyl which have 1 to 3 trihalo(lower)alkyl and/or lower alkyl, A is a group of the formula;
—
(CH2)t—
(O)m—
or
in which R3 and R4 are each hydrogen or linked together to form imino,R5 is hydrogen or lower alkyl, t is 0, 1 or 2, p, m and n are each 0 or 1, X is phenylene;
phenylene which have 1 to 3 halogen;
phenylene which have 1 to 3 cyano;
phenylene which have 1 to 3 lower alkyl;
phenylene which have 1 to 3 lower alkoxy;
phenylene which have 1 to 3 lower alkylsulfonylamino;
phenylene which have 1 to 3 halogen and/or lower alkoxy;
phenylene which have saturated heteromonocyclic group containing 1 or 2 oxygen atom(s) and 1 to 3 nitrogen atom(s);
pyridinylene;
pyridinylene which have 1 to 3 halogen;
pyridinylene which have 1 to 3 trihalo(lower)alkyl;
pyridinylene which have 1 to 3 lower alkyl;
pyridinylene which have saturated heteromonocyclic group containing 1 to 4 nitrogen atom(s);
piperadinylene which have unsaturated heteromonocyclic group containing 1 to 4 nitrogen atom(s);
pyrimidinylene;
isoindolinylene, Y is vinylene;
1-propenylene;
methylene;
ethylene.
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12. A pharmaceutical composition, which has a compound of claim 1 and a pharmaceutically acceptable carriers or excipients.
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13. A process for preparing a pharmaceutical composition, which comprises a compound of claim 1 in admixture with a pharmaceutically acceptable carriers or excipients.
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14. A use of a compound of claim 1 as a medicament.
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15. A use of a compound of claim 1 as a 5-HT antagonist.
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16. A use of a compound of claim 1 as a 5-HT2C antagonist.
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17. A use of a compound of claim 1 for preparing a medicament for treating 5-HT-mediated diseases.
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18. A method for treating 5-HT-mediated diseases which comprises administering a compound of claim 1 to human or animals.
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3. A compound of the formula (I):
R1-A-X-NHCO—
Y—
R2wherein R1 is phenyl, R2 is phenyl which have trihalo(lower)alkyl, A is a group of the formula;
in which R3 and R4 are linked together to form imino,R5 is hydrogen, p is 1, n is 0, X is phenylene which have halogen and lower alkoxy, Y is vinylene, and a salt thereof.
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4. A compound of the formula (I):
R1-A-X—
N HCO—
Y—
R2wherein R1 is unsaturated heteromonocyclic group containing 1 to 4 nitrogen atom(s) which have 1 to 3 lower alkyl, R2 is indolyl which have 1 to 3 lower alkyl, A is bond, X is phenylene which have 1 to 3 halogen, Y is bond, and a salt thereof. - View Dependent Claims (5)
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6. A compound of the formula (I):
R1-A-X-NHCO—
Y—
R2wherein R1 is unsaturated heteromonocyclic group containing 1 to 4 nitrogen atom(s) which have 1 to 3 lower alkyl, R2 is carbazolyl, A is bond, X is phenylene which have 1 to 3 lower alkoxy, Y is bond, and a salt thereof. - View Dependent Claims (7)
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8. A process for preparing a compound of the formula:
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R1-A-X-NHCO—
Y—
R2or a salt thereof, subjecting a compound of the formula;
R1-A-X—
NH2or a salt thereof, to amidation reaction with a compound of the formula;
HOOC—
Y—
R2or a salt thereof, wherein R1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents, R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents, A is a group of the formula;
—
(CH2)t—
(O)m—
orin which R3 and R4 are each hydrogen or linked together to form imino, R5 is hydrogen or lower alkyl, t is 0, 1 or 2, p, m and n are each 0 or 1, X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents, Y is bond, lower alkylene, or lower alkenylene.
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9. A process for preparing a compound of the formula:
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10. A process for preparing a compound of the formula:
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11. A process for preparing a compound of the formula:
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R1—
NH—
CH2—
X-NHCO—
Y—
R2or a salt thereof, subjecting a compound of the formula;
R1—
NH2or a salt thereof, to reaction with a compound of the formula;
or a salt thereof, wherein R1 is heterocyclic group which may have suitable substituents, or phenyl which may have suitable substituents, R2 is condensed phenyl which may have suitable substituents, phenyl which may have suitable substituents, or thienyl which may have suitable substituents, X is phenylene which may have suitable substituents, or bivalent heterocyclic group containing nitrogen which may have suitable substituents, Y is bond, lower alkylene, or lower alkenylene.
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Specification