- CRYSTAL FORM OF ASENAPINE MALEATE
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The present invention relates to a form of Asenapine Maleate with XRPD peaks at about 5.5,12.5,19.0 and 25.3 and to methods for the preparation thereof. Furthermore the invention relates to a reproducible process for the preparation of pure monoclinic form of Asenapine Maleate in crystalline form and to pharmaceutical compositions comprising the pure monoclinic form of asenapine maleate.
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Page/Page column 17; 18
(2013/04/10)
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- A PROCESS FOR THE PREPARATION OF ASENAPINE AND NOVEL SALTS THEREOF
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A process for preparation of asenapine of formula (1) or its acid addition salts; The said process comprises preparation of trans racemate of asenapine by reacting trans- 1 1-chloro-2,3,3a, 12b-tetrahydro-2-methyl-lH-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-l-one with mixture of aluminium chloride and lithium aluminium hydride in solvent followed by converting it into acid addition salt of asenapine followed by hydrolyzing the acid addition salt into trans racemate asenapine base and converting the asenapine base into acid addition salt. Asenapine sulphate of formula (Via) and asenapine maleate of formula (IVb) are also disclosed. The co-precipitate of acid addition salt of asenapine with a pharmaceutically acceptable excipient of formula (V); is also disclosed.
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- COMPRESSED ORAL DOSAGE FORM FOR ASENAPINE MALEATE
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The present invention relates to a compressed pharmaceutical dosage form intended for sublingual or buccal administration and capable of being rapidly disintegrated, the compressed pharmaceutical dosage form containing asenapine maleate in a microcrystalline monoclinic form. It further relates to a method of preparing the same and to a container comprising the dosage form.
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Page/Page column 28
(2013/04/10)
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- PROCESS FOR THE PREPARATION OF TETRACYCLIC DERIVATIVES AND INTERMEDIATE PRODUCTS USED IN THE PROCESS
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A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.
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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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- CRYSTALLINE SALTS OF ASENAPINE
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Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.
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Page/Page column 14
(2012/11/14)
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- 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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- NOVEL PROCESS FOR THE PREPARATION OF ASENAPINE
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The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
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- NEW CRYSTAL FORMS OF THE SALT OF TRANS-5-CHLORO-2-METHYL-2,3,3A,12b-TETRAHYDRO-1H-DIBENZO[2,3:6,7]OXEPINO[4,5-c]PYRROLE WITH MALEIC ACID
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The present invention relates to two new crystal forms of the salt of trans-5-chloro-2- methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrolewith maleic acid, processes for preparing thereof and compositions comprising thereof. These new crystal forms of the salt of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenzo[2,3:6,7]oxepino[4,5-c]pyrrolewith maleic acid are stable under micronization and show an improved water solubility when compared to other asenapine maleate crystalline forms described in the prior art, such as the orthorhombic form (form L) and the monoclinic form (form H).
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Page/Page column 33-34
(2012/10/07)
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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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- 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 6
(2010/11/24)
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