5-fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985):: An orally active arginine vasopressin antagonist with selectivity for V2 receptors

被引：140

作者：

Albright, JD ^{[1
]}

Reich, MF

Delos Santos, EG

Dusza, JP

Sum, FW

Venkatesan, AM

Coupet, J

Chan, PS

Ru, X

Mazandarani, H

Bailey, T

机构：

[1] Wyeth Ayerst Res, Pearl River, NY 10965 USA

[2] Wyeth Ayerst Res, Princeton, NJ 08543 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 14期

关键词：

D O I：

10.1021/jm980179c

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

引用

页码：2442 / 2444

页数：3

共 49 条

[31] Theoretical studies, synthesis, and biological activity of 1-[(4-methylphenyl)sulfonyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-4-carbonitrile (C9) as a non-peptide antagonist of the arginine vasopressin V1a and V2 receptors
Citlalli Contreras-Romo, M.
Correa-Basurto, Jose
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Martinez-Archundia, Marlet
Martinez-Ramos, Federico
Slusarz, Magdalena J.
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MEDICINAL CHEMISTRY RESEARCH, 2014, 23 (03) : 1581 - 1590
[32] Theoretical studies, synthesis, and biological activity of 1-[(4-methylphenyl)sulfonyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-4-carbonitrile (C9) as a non-peptide antagonist of the arginine vasopressin V1a and V2 receptors
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[33] Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)
Suzuki, Gentaroh
Kimura, Toshifumi
Satow, Akio
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Hata, Mikiko
Azuma, Tomoko
Ito, Satoru
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JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2007, 321 (03): : 1144 - 1153
[34] Characterization of orally active nonpeptide vasopressin V2 receptor agonist.: Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-yl]-N-isopropylacetamide
Kondo, K
Kan, K
Tanada, Y
Bando, M
Shinohara, T
Kurimura, M
Ogawa, H
Nakamura, S
Hirano, T
Yamamura, Y
Kido, M
Mori, T
Tominaga, M
JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (17) : 3805 - 3808
[35] Ring - Ring interconversion: The rearrangement of 6-(4- Chlorophenyl)-3-methyl-5-nitrosoimidazo[2,1-b][1,3]thiazole into 8-(4-chlorophenyl)-8-hydroxy-5-methyl-8H-[1,4]thiazino[3,4-c][1,2,4]o xadiazol-3- one. Elucidation of the reaction product through spectroscopic and X-ray crystal structure analysis
J Chem Soc Perkin Trans 2, 11 (2407-2410):
[36] SYNTHESIS AND IN-VITRO CARDIOVASCULAR ACTIVITY OF 4-ARYL-2,3,3A,4-TETRAHYDRO-1H-PYRROLO[2,1-C][1,4]BENZOTHIAZIN-1-ONES AND 7-ACETOXY-6-PHENYL-7A,8,9,10-TETRAHYDROPYRROLO[2,1-D][1,5]BENZOTHIAZEPIN-10-ONE
CAMPIANI, G
GAROFALO, A
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BOTTA, M
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CHIARINI, A
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BRUNI, G
ROMEO, MR
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[37] Comparison of lorazepam [7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one] occupancy of rat brain γ-aminobutyric AcidA receptors measured using in vivo [3H] flumazenil (8-fluoro 5,6-dihydro-5 methyl-6-oxo-4-himidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester) binding and [11C] flumazenil micro-positron emission tomography
Atack, John R.
Scott-Stevens, Paul
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Fryer, Tim D.
Hughes, Jessica L.
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Baron, Jean-Claude
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Aigbirhio, Franklin I.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2007, 320 (03): : 1030 - 1037
[38] 4-氨基-5-氯-2-乙氧基-N-((3R,8aR)-六氢-1H-吡咯[2,1-c][1,4]噁嗪-3-基)甲基苯甲酰胺盐酸盐的合成
陈冉章
科技资讯, 2012, (05) : 79 - 79
[39] 5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide:: A [11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans
Rabiner, EA
Wilkins, MR
Turkheimer, F
Gunn, RN
De Haes, JU
De Vries, M
Grasby, PM
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2002, 301 (03): : 1144 - 1150
[40] Five-membered 2,3-dioxo heterocycles: LX. Reaction of 3-aroyl-1H-pyrrolo[2,1-c][1,4]benzoxazine-1,2,4-triones with cyclic enehydrazino ketones. Crystalline and molecular structure of N-[3′-benzoyl-4′-hydroxy-1′-(2-hydroxyphenyl)-6, 6-dimethyl-2,4,5′-trioxo-1′,4,5,5′,6,7-hexahydrospiro[indole-3,2′-pyrrol]-1(2H)-yl]-3-nitrobenzamide
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