165309-36-4Relevant academic research and scientific papers
Benzoheterocyclic compounds and vasopressin antagonist and oxytocin antagonist compositions containing a benzoheterocyclic compound
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, (2008/06/13)
An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist. The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): STR1 (wherein R1, R2, R3, R4, R5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.
Orally active, nonpeptide vasopressin V2 receptor antagonists: A novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds
Ogawa, Hidenori,Yamashita, Hiroshi,Kondo, Kazumi,Yamamura, Yoshitaka,Miyamoto, Hisashi,Kan, Keizo,Kitano, Kazuyoshi,Tanaka, Michinori,Nakaya, Kenji,Nakamura, Shigeki,Mori, Toyoki,Tominaga, Michiaki,Yabuuchi, Youichi
, p. 3547 - 3555 (2007/10/03)
This paper describes a novel series of nonpeptide vasopressin V2 receptor antagonists. It has been demonstrated that the 1-[4- (benzoylamino)benzoyl]-2,3,4,5-1H-benzazepines and 1-[4- (benzoylamino)benzoyl]-2,3,4,5-1H-1,5-benzodiazepines show a high affinity for V2 (and V(1a)) receptors. Among the 1-[4-(benzoylamino)benzoyl]-2,3,4,5- 1H-benzazepine series, compounds with an alkylamino group on the benzazepine ring have been shown to have oral activity. A lipophilic group at the ortho position on the terminal benzoyl ring is important for both high V2 receptor affinity and oral activity. On the basis of these favorable properties, clinical testing of 31b has begun for use as an oral and iv aquaretic agent.
Benzoheterocyclic compounds
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, (2008/06/13)
Novel benzoheterocyclic compounds of the formula: STR1 wherein R1 is H, halogen, OH, etc,; R2 is H, alkyl, halogen or alkoxy; R3 is phenyl-alkanoylamino, or STR2 R4 is H, --NR6 R7, alkenylo
