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公开(公告)号：EP1592401A2
公开(公告)日：2005-11-09
申请号：EP04703158.8
申请日：2004-01-19
申请人： Novartis AG , Novartis Pharma GmbH
发明人： PFEFFER, Sabine , WIECKHUSEN, Dierk
IPC分类号： A61K9/14
CPC分类号： C07D307/88 , A61K9/14 , A61K9/2866
摘要： A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.
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公开(公告)号：EP1592401B1
公开(公告)日：2012-02-22
申请号：EP04703158.8
申请日：2004-01-19
申请人： Novartis AG , Novartis Pharma GmbH
发明人： PFEFFER, Sabine , WIECKHUSEN, Dierk
IPC分类号： A61K9/14
CPC分类号： C07D307/88 , A61K9/14 , A61K9/2866
摘要： A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.
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4.发明授权
公开(公告)号：EP1523335B1
公开(公告)日：2006-12-20
申请号：EP03756455.6
申请日：2003-07-14
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： A61K47/38 , A61K47/10 , A61K47/26 , A61K31/454
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
摘要： An injectable depot formulation comprising crystals having Structure (I) wherein R is (FII) and the X5o value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolite have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
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5.发明公开
公开(公告)号：EP1523335A2
公开(公告)日：2005-04-20
申请号：EP03756455.6
申请日：2003-07-14
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： A61K47/38 , A61K47/10 , A61K47/26 , A61K31/454
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
摘要： An injectable depot formulation comprising crystals having Structure (I) wherein R is (FII) and the X5o value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolite have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
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公开(公告)号：EP0994880B1
公开(公告)日：2005-01-19
申请号：EP98936392.4
申请日：1998-06-26
申请人： Novartis AG , Novartis Pharma GmbH
发明人： DOSENBACH, Cornelia , GRASSBERGER, Maximilian , HARTMANN, Otto , HORVATH, Amarylla , MUTZ, Jean-Paul , PENN, Gerhard , PFEFFER, Sabine , WIECKHUSEN, Dierk
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , C30B7/00
摘要： 33-Epichloro-33-desoxyascomycin of formula (I) and various tautomeric or solvated forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula (I), or compound of formula (I) in other than Form A, or compound of formula (I) in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.
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公开(公告)号：EP0994880A1
公开(公告)日：2000-04-26
申请号：EP98936392.4
申请日：1998-06-26
发明人： DOSENBACH, Cornelia , GRASSBERGER, Maximilian , HARTMANN, Otto , HORVATH, Amarylla , MUTZ, Jean-Paul , PENN, Gerhard , PFEFFER, Sabine , WIECKHUSEN, Dierk
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , C30B7/00
摘要： 33-Epichloro-33-desoxyascomycin of formula (I) and various tautomeric or solvated forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula (I), or compound of formula (I) in other than Form A, or compound of formula (I) in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.
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