- A new process for the preparation of 3-amino-9,13b-dihydro-1H-dibenz [c,f] imidazo[1,5-a]azepine bromic acid salt
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The present invention relates to a novel method for preparing an enhanced 3-amino-9, 13b-dihydro-1H-dibenz [c,f] imidazo [1,5-a] azepine bromic acid salt. The compound is used as an intermediate in manufacturing the epinastine hydrochloride. The compound is represented by the structural formula (I).COPYRIGHT KIPO 2015
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Paragraph 0017; 0060-0063
(2016/12/07)
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- NOVEL CRYSTAL MODIFICATION OF EPINASTINE OR SALTS THEREOF AND PROCESS FOR PREPARATION THEREOF
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The present invention provides novel crystalline forms of 3-amino-9,13b-dihydro-lH- dibenzo[c,f]imidazo[l55-a] azepine or salts thereof and process for preparation thereof.
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Page/Page column 25
(2009/06/27)
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- New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine
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A series of new tetracyclic guanides were synthesized by various methods. Specific binding of the described compounds to histamine-1 and histamine-2 receptors was determined. The compound 3-amino-9, 13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine (epinastine, WAL 801) combines high selectivity with high affinity for the H1 receptor and was selected from the compounds studied for further pharmacological and clinical investigations. Experimentally determined physicochemical parameters (pk(a)-value, partition coefficient) and the hydrogen-bonding ability of epinastine are indications that this compound will not easily cross the blood-brain barrier. This explains the absence of CNS side-effects of epinastine in pharmacological and clinical studies.
- Walther,Daniel,Bechtel,Brandt
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p. 440 - 446
(2007/10/02)
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- FUSED DIBENZO IMIDAZOLO COMPOUNDS, COMPOSITIONS AND USE
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This invention relates to a compound of the formula wherein R1, R2, R3, and R4, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl or alkoxy group of from 1 to 6 carbon atoms; R5 and R6, which may be the same or different, each represent a hydrogen atom, an alkyl group of from 1 to 6 carbon atoms, or an alkenyl group of from 3 to 6 carbon atoms, or R5 and R6 together with the nitrogen atom to which they are attached represent a pyrrolidino, piperidino, or morpholino group; and X represents oxygen, sulfur, or a methylene group, or a non-toxic, pharmacologically acceptable acid addition salt thereof, or a racemate, enantiomer, or mixture of enantiomers thereof. The compounds of Formula I are useful in pharmaceutical compositions for treating bronchial asthma and allergic bronchitis
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