182415-09-4Relevant articles and documents
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.
Kamei,Maeda,Ogino,Koyama,Nakajima,Tatsuoka,Ohno,Inoue
, p. 595 - 598 (2001)
A series of new 3-substituted-4-(4-aminobutyl)-1,4-benzoxazepin-5(4H)-one derivatives (1-5) which showed a very high affinity for 5-HT1A receptor with good selectivity over dopamine D2 receptor was synthesized. Among these compounds, 3-chloro-4-[4-[4-(2-p
Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan
Kamei, Katsuhide,Maeda, Noriko,Nomura, Kayoko,Shibata, Makoto,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Inoue, Teruyoshi,Ohno, Tomochika,Tatsuoka, Toshio
, p. 1978 - 1992 (2007/10/03)
A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D 2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]- 1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
Pyrimidine derivatives and their salts, useful for making benzoxazepine derivatives
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Example 86, (2010/11/29)
A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients: wherein, n is an integer of 2 to 5, R1indicates a hydrogen atom, halogen atom, C1to C4lo
Benzoxazepine derivatives and their salts and medicaments containing the same
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, (2008/06/13)
A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients: wherein, n is an integer of 2 to 5, R1indicates a hydrogen atom, halogen atom, C1to C4lower alkyl group, C1to C4lower alkoxyalkyl group, C1to C4halogenoalkyl group, cyano group, or ester group, R2indicates a hydrogen atom, halogen atom, C1to C4lower alkyl group, C1to C4lower alkoxy group, or hydroxy group, a dotted line indicates the presence or absence of a binding bond, W indicates C, CH, or CH2or a nitrogen atom, provided that, when W is a nitrogen atom, Z is bonded to W and the dotted line indicates the absence of a bond, and Z indicates an unsubstituted or substituted aromatic hydrocarbon ring group or an unsubstituted or substituted heterocyclic group). This benzoxazepine derivative and its salts are useful as medicaments for the treatment of anxiety neurosis, phobias, obsessive-compulsive disorders, schizophrenia, post-cardiac trauma stress, depression, psychosomatic and other psychoneurotic disorders, eating disorders, menopausal disorders, infantile autism and also emesis or disorders involving the cerebral circulatory system accompanying cerebral infarction and cerebral hemorrhage.
Process of production of 4-substituted-3-halogeno-1,4-benzoxazepine derivative and salts thereof
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, (2008/06/13)
A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): STR1 with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the formula (IV): STR2 and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) STR3 wherein X indicates a chlorine atom or a bromine atom, or its salt.
