- SUBSTITUTED PIPERIDINE DERIVATIVES AS SOMATOSTATIN SST1 RECEPTOR ANTAGONISTS
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Compound of the formula (I) wherein R1, R2, n and m are as defined in the specification. The compounds of formula (I) are somatostatin sst1 receptor antagonists.
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Page/Page column 22
(2008/06/13)
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- Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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Page/Page column 29
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- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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- Synthesis of a spiro[cyclohex-1,1′-isobenzofuranyl] dopamine receptor antagonist
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Two syntheses of the novel CNS agent, 2-fluoro-4-(trans)-(4-(3'H-spiro[cyclohex-l,1'-isobenzofuran]-4-yl)-piperazin-1- yl)benzonitrile, 1, are presented. The first relied on a reductive alkylation with low regioselectivity (1:1) but was sufficient for the
- Urban, Frank J.,Anderson, Bruce G.,Stewart, Morgan A.,Young, Gregory R.
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p. 460 - 464
(2013/09/08)
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