- Processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole
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This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.
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Page/Page column 15-16
(2012/07/03)
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- PROCESS FOR THE PREPARATION OF (3ARS,12BRS)-5-CHLORO-2-METHYL-2,3,3A12B-TETRAHYDRO-1HDIBENZO[2,3:6,7] OXEPINO [4,5-C]PYRROLE MALEATE AND IT'S PHARMACEUTICAL COMPOSITION THEREOF
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The present invention relates to an improved process for the preparation (3aRS,12bRS)-5-Chloro-2-menthyl-2,3,3a,12b-tetrahydro-1Hdibenzo[2,3:6,7]oxepino [4,5-c]pyrrole maleate represented by the compound of formula-1a and its pharmaceutical composition.(F)
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Page/Page column 35
(2012/04/10)
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- ASENAPINE MALEATE
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Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof.
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Page/Page column 36
(2012/01/06)
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- PROCESS FOR PRODUCING TRANS-DIBENZOXENOPYRROLE COMPOUND AND INTERMEDIATE THEREFOR
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The invention provides a process for production of trans-dibenzoxenopyrrole compounds, in which reduction, leaving group conversion, hydrogenation and methylation are carried out in that order. The process of the invention allows trans-dibenzoxenopyrrole compounds to be produced by a simpler procedure than conventional processes. The invention further provides novel compounds obtained as intermediates in the process, and a process for their production.
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Page/Page column 13
(2010/04/24)
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- Design, synthesis and SAR of phenylamino-substituted 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones and 11H-dibenzo[b,f]oxepin-10-ones as p38 MAP kinase inhibitors
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The p38 MAP kinase is a key enzyme in inflammatory diseases as it is involved in the biosynthesis of proinflammatory cytokines such as TNF-α and IL-1β. Small molecule p38 inhibitors suppress the production of these cytokines and therefore p38 is a promisi
- Dorn, Angelika,Schattel, Verena,Laufer, Stefan
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scheme or table
p. 3074 - 3077
(2010/07/18)
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- Intermediate compounds for the prepation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1h-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
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Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.
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Page/Page column 10
(2008/06/13)
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- Intermediate compounds for the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
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Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.
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Page/Page column 7-8
(2010/11/24)
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- Substituted (2-Phenoxyphenyl)acetic Acids with Antiinflammatory Activity. 1
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The synthesis and antiinflammatory activity of a series of substituted (2-phenoxyphenyl)acetic acids are described.Initial screening in the adjuvant arthritis test showed that halogen substitution in the phenoxy ring enhanced activity considerably.Ulcerogenic potential, as measured by the minimum ulcerogenic dose (MUD), was low in almost all the acids tested. acetic acid possessed the most favorable combination of potency with low toxicity, including ulcerogenicity, and this compound is now in therapeutic use.
- Atkinson, David C.,Godfrey, Keith E.,Meek, Bernard,Saville, John F.,Stillings, Michael R.
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p. 1353 - 1360
(2007/10/02)
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- Affinity of 10-(4-Methylpiperazino)dibenzoxepins for Clozapine and Spiroperidol Binding Sites in Rat Brain
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10-(4-Methylpiperazino)dibenzoxepins were prepared and evaluated as potential antipsychotic agents using specific clozapine diazepine> binding sites in rat forebrain that are noncholinergic and nondopaminergic in nature and from which clozapine is displaced by known antipsychotic agents. Clozapine binding in the presence of atropine represents nonmuscarinic binding, while binding in the absence of atropine represents muscarinic (cholinergic) plus nonmuscarinic binding.The relative affinity for dopamine binding sites was determined by displacement of spiroperidol from binding sites in rat caudate nuclei.Thus, clozapine, its 2-chloro isomer, its dechloro analogue, and their 5H-dibenzocycloheptene and dibenzoxepin analogues have about the same relative affinity for the nonmuscarinic clozapine binding sites.At the spiroperidol (dopaminergic) sites, both the nature of the tricyclic system and the presence of chlorine atom on the tricyclic system have a substantial effect on the binding affinity.Within each series, shift of a chlorine atom from the position distal to the piperazino group to the proximal position increases the binding affinity by a factor of about nine, but removal of the chlorine atom substantially decreases the binding affinity.Nevertheless, 10-(4-methylpiperazino)dibenzoxepin has a threefold greater affinity for the dopaminergic binding sites than does clozapine itself.
- Harris, Terry W.,Smith, Howard E.,Mobley, Philip L.,Manier, D. Hal,Sulser, Fridolin
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p. 855 - 858
(2007/10/02)
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- Tricyclics with analgesic and antidepressant activity: I. [[(Alkylamino)ethyl]thio]dibenzo[b,f]oxepins and 10,11-dihydro derivatives
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A series of [[(alkylamino)ethyl]thio]dibenz[b,f]oxepins and their 10,11-dihydro derivatives was synthesized and subjected to broad analgesic/CNS screening. Several analogues of both types, carrying small N-substituents and frequently a nuclear fluorine fu
- Ong,Profitt,Anderson,Spaulding,Wilker,Geyer IIIrd,Kruse
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p. 494 - 501
(2007/10/02)
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