- CRYSTALLINE FORMS OF NOVEL VARENICLINE SALTS, PREPARATION METHODS THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF
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The present invention refers to crystalline form of 7, 8, 9, 10 - tetrahydro - 6, 10 - methano - 6H - [3] [2, 3 a-h] pyrazole roh it cuts the person number pin new salt, and manufacturing method of including pharmaceutical compositions are disclosed. (by machine translation)
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Paragraph 0100-0101
(2018/03/23)
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- Process for Preparing Quinoxaline Derivatives
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The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof.
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Page/Page column 11
(2012/01/14)
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- HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY
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Provided herein is an impurity of varenicline, 6-methyl-5,8,14-triazatetracyclo[l 0.3.1.02'n,04'9]hexadeca-2(l l),3,5,7,9-pentaene (methylvarenicline) impurity, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity.
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- IMPROVED PROCESS FOR THE PREPARATION OF SUBSTITUTED QUINOXALINES
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The present invention is directed to an improved process for the preparation of substituted quinoxalines by cyclization of the corresponding dianiline in the presence of ion exchange resin.
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- PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien- 10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the pressence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2- trifluoro-ethanone.
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Page/Page column 19
(2010/04/06)
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- IMPROVED PROCESSES FOR THE SYNTHESIS OF VARENICLINE L-TARTRATE
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This invention provides a process of preparing varenicline L-tartrate salt. This invention also provides varenicline L-tartrate produced by the instant method, as well as a pharmaceutical composition comprising same.
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Page/Page column 12-13; 14-15; 18
(2009/06/27)
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- Preparations of new polymorphic forms of varenicline tartrate
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The present invention is directed to an amorphous form, three novel polymorph form of crystalline varenicline tartrate, namely Form D, Form E and Form F. The present invention also provides processes of their preparations and pharmaceutical composition comprising such material and their use in therapy. Form D is new anhydrous varenicline tartrate, and can be prepared from recrystallizing varenicline tartrate in a mixture of methanol and water or a mixture of N,N-dimethylformamide and water. Form E is a new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of isopropanol and water. Form F is another new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of acetone and water. The X-ray powder diffraction pattern (X-RPD), Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) techniques are used to characterize amorphous form and crystalline polymorphic forms.
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Page/Page column 15
(2009/09/07)
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- VARENICLINE STANDARDS AND IMPURITY CONTROLS
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The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamine mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than O ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.
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Page/Page column 10
(2008/06/13)
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- PREPARATION OF SUBSTITUTED QUINOXALINES FROM THE DIANLINE WITH 2,3-DIHYDROXY-1,4-DIOXANE
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The present invention relates to a new process for the preparation of substituted quinoxalines (I) by cyclization of the corresponding dianiline with 2,3 dihydroxy-1,4-dioxane. In a preferred embodiment, the invention provides a process for the preparation of compounds having the formula III wherein Q is a nitrogen protecting group. Compounds of formula III and their derivatives are precursors to certain aryl fused azapolycyclic compounds which exhibit activity as agents for the treatment of neurological and psychological disorders.
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