- SUBSTITUTED SPIROHETEROCYCLES
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The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular
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Page/Page column 25; 26
(2008/06/13)
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- SPIROBENZOAZEPANES AS VASOPRESSIN ANTAGONISTS
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The present invention is directed to a compound of Formula (I) or a form thereof: wherein U, V, W and Ring A are as defined herein, useful as vasopressin receptor antagonists.
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Page/Page column 50
(2009/01/20)
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- Process for the preparation of nonpeptide substituted spirobenzoazepine derivatives
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Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.
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- Indoloazepines as vasopressin receptor antagonists
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The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions involving increased vascular resist
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Page column 14; 15
(2010/02/07)
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- Nonpeptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 2-phenyl-4'-(2,3,4,5- tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide derivatives
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A series of compounds structurally related to 2-phenyl-4'-(2,3,4,5- tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V(1A) and V2 receptors. The introduction of a hydrophilic substituent group into the 5-position of the benzodiazepine ring resulted in an increase in oral availability. Especially, the (3-pyridyl)methyl (31b), the 2-(4- methyl)-1,4-diazepan-1-yl)-2-oxoethyl (32i), and the 2-(4-methylpiperazin-1- yl)ethyl (33g) derivatives exhibited high antagonist activities and high oral availability. Details of the synthesis and pharmacological properties of this series are presented.
- Matsuhisa, Akira,Koshio, Hiroyuki,Sakamoto, Kenichiro,Taniguchi, Nobuaki,Yatsu, Takeyuki,Tanaka, Akihiro
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p. 1566 - 1579
(2007/10/03)
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