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-(4-Hydroxyalkyl-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-recep
2-(4-Hydroxyalkyl-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 Alk is a trivalent alkylene having one to six carbon atoms; R1 is hydrogen or lower alkyl having one to three carbon atoms; R2 and R3 each is hydrogen or lower alkyl having one to three carbon atoms; R4 is hydrogen, phenyl, hydroxy, phenoxy, phenyl mono-,
A compound of the formula [Figure] in which Alk is a trivalent alkylene having one to six carbon atoms; R1 is hydrogen or lower alkyl having one to three carbon atoms; R2 and R3 each is hydrogen or lower alkyl having one to three carbon atoms; R4 is hydrogen, phenyl, hydroxy, phenoxy, phenyl mono-, di- or trisubstituted with methylsulfonylamino, lower alkyl, halo, lower alkoxy, hydroxy or trifluoromethyl, or phenoxy mono-, di- or trisubstituted with lower alkyl, halo, lower alkoxy, hydroxy or trifluoromethyl; and R5 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; with the proviso that when R4 is hydroxy, the hydroxy groups are joined to different carbon atoms; or a therapeutically acceptable acid addition 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 Alk is a trivalent alkylene having one to three carbon atoms; R1 is hydrogen; R2 and R3 each is hydogen or lower alkyl having one to three carbon atoms; R4 is hydrogen, phenyl, hydroxy, phenoxy, phenyl mono-, di- or trisubstituted with lower alkoxy or hydroxy, or phenoxy monosubstituted with lower alkyl or halo; R5 represents a substituent at position 7 of the 2,4,6-cycloheptatrien-1-one ring and is selected from hydrogen or bromo; 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.
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.
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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