- PROCESS FOR THE SYNTHESIS OF GEPIRONE
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Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.
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Page/Page column 15-16
(2020/07/31)
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- 3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors
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The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R1represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched1-C4alkyl group; a C1/
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- 3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands
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Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: Ar represents aryl or heteroaryl; R1 and R2 are the same or different and represent organic or inorganic substituents; R5 is hydrogen or C1-C6 alkyl; W represents CH or nitrogen; X is oxygen or sulfur; and A represents an alkylene group, which compounds bind selectively with high affinity to the dopamine D4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.
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- A new series of selective dopamine D4 ligands: 3-([4-arylpiperazin-1-yl]alkylamino)-2H-1,4-benzoxazines
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A series of 3-([4-arylpiperaz-1-yl)alkylamino]-2H-1,4-benzoxazines were prepared and their affinities for cloned human D2, D3, and D4 dopamine receptor subtypes were measured. This led to the identification of 1a, 1f, and 1g as high affinity selective antagonists at the D4 receptor.
- He, Xiao Shu,Woodruff, Kristine,Brodbeck, Robbin
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p. 2399 - 2402
(2007/10/03)
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- Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds
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A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.
- Ishizumi,Kojima,Antoku
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p. 2288 - 2300
(2007/10/02)
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- N-(substituted piperazinyl) alkylbicyclic succinimide derivatives
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A succinimide derivative of the formula: STR1 wherein A is straight or branched C2 -C6 alkylene or alkenylene, B is straight or branched C3 -C5 alkylene, D is straight or branched C2 -C3 alkylene, E is straight or branched C2 -C3 alkylene, R1 and R2 are each hydrogen or C1 -C4 alkyl, or they may form a single bond and R3 is a phenyl group optionally substituted with C1 -C4 alkyl, C1 -C4 alkoxy, halogen and/or trifluoromethyl, a 2-pyridyl group optionally substituted with halogen, a 2-pyrimidyl group optionally substituted with halogen, a group of the formula: STR2 (in which R4 is hydrogen or phenyl), a group of the formula: CO--R5 (in which R5 is adamantyl or furyl) or hydroxy (C2 -C4) alkyl, and an acid addition salt thereof, which are useful as anti-anxiety drugs and/or anti-allergic drugs.
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- 2-[4-[(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyrimidines
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1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-pyrimidyl substituents in the 4- position have been synthesized and demonstrate useful anxiolytic properties. The compound 4,4-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,6-piperidinedione, which has selective anxiolytic activity, constitutes the preferred embodiment of the invention.
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- Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones
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The present invention concerns the class of heterocyclic carbon compounds comprised of N-(heteroarcyclic)piperazinylalkyl derivatives of azaspiroalkanediones which have potent and specific tranquilizing action and anti-emetic properties. Typical embodiments of this invention are 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione and 8-[4-[4-(2-pyridyl)-1-piperazinyl]-butyl]-8-azaspiro[4.5]decane-7,9-dione.
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