Bagli Jehan F. (Kirkland CAX) Bgri Tibor (Montreal CAX) Voith Katherine (Dorval CAX)
출원인 / 주소
Ayerst, McKenna & Harrison Inc. (Montreal CAX 03)
인용정보
피인용 횟수 :
5인용 특허 :
0
초록▼
2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating
2-(1-Piperazinyl)-2,4,6-cycloheptatrien-1-one derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives are disclosed. The derivatives exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
대표청구항▼
A compound of the formula [Figure] in which R1 represents a substituent at positions 3, 4, 5, 6 or 7 of the 2,4,6-cycloheptatrien-1-one ring and is selected from hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, or 1-oxo(lower)alkylamino; R2 is hydrogen or lower alkyl having one to three c
A compound of the formula [Figure] in which R1 represents a substituent at positions 3, 4, 5, 6 or 7 of the 2,4,6-cycloheptatrien-1-one ring and is selected from hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, or 1-oxo(lower)alkylamino; R2 is hydrogen or lower alkyl having one to three carbon atoms; and R3 is hydrogen, phenyl, lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl, lower alkoxycarbonyl, 1-oxo(lower)alkyl, cyclo(lower)alkyl substituted with a lower alkyl; lower alkenyl substituted with phenyl; phenyl mono-, di or trisubstituted with lower alkyl, halo, lower alkoxy, hydroxy or trifluoromethyl; 2-(4,5-dihydro-2-oxazolyl)benzoyl, 2,3-dihydro-8-oxo-cyclohepta [b]furan-2-ylmethyl, 1-oxo-2,4,6-cycloheptatrien-2-yl, 2-(acetylamino)ethyl, 2,3-diacetyloxypropyl, 2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)ethyl or 5-methyl-2,4-imidazolidinedione-5-ylmethyl; or a therapeutically acceptable acid solution salt thereof. A pharmaceutical composition, for stimulating dopamine receptors in a mammal in need thereof, which comprises an effective dopamine receptor stimulating amount of a compound of the formula [Figure] in which R1 represents a substituent at positions 3, 4, 5, 6 or 7 of the 2,4,6-cycloheptatrien-1-one ring and is selected from hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, or 1-oxo(lower)alkylamino; R2 is hydrogen or lower alkyl having one to three carbon atoms; and R3 is hydrogen, phenyl, lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl, lower alkoxycarbonyl, 1-oxo(lower)-alkyl, cyclo(lower)alkyl substituted with a lower alkyl; lower alkenyl substituted with phenyl; phenyl mono-, di- or trisubstituted with lower alkyl, halo, lower alkoxy, hydroxy or trifluoromethyl; 2-(4,5-dihydro-2-oxazolyl)benzoyl, 2,3-dihydro-8-oxo-cyclohepta[b]furan-2-ylmethyl, oxo-2,4,6-cycloheptatrien-2-yl, 2-(acetylamino)ethyl, 2,3-diacetyloxypropyl, 2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)ethyl or 5-methyl-2,4-imidazolidinedione-5-ylmethyl; or a therapeutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier therefor.
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이 특허를 인용한 특허 (5)
Dempski Robert E. (Dresher PA) Scholtz Edward C. (King of Prussia PA) Nibbelink Donald W. (Lansdale PA) Reines Scott A. (New Hope PA), Controlled release combination of carbidopa/levodopa.
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Dempski Robert E. (Dresher PA) Scholtz Edward C. (King of Prussia PA) Nibbelink Donald W. (Lansdale PA) Reines Scott A. (New Hope PA), Controlled release combination of carbidopa/levodopa.
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