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公开(公告)号：US07671093B2
公开(公告)日：2010-03-02
申请号：US11139245
申请日：2005-05-27
IPC分类号： A61K31/165
CPC分类号： A61K31/165 , A61K9/145 , A61K31/191 , C07C55/10 , C07C57/15 , C07C317/44 , A61K2300/00
摘要： A mixed co-crystal comprising an API, a first co-crystal former, and a second co-crystal former which is isomorphically substitutable with said first co-crystal former is described. A pharmaceutical composition comprising a mixed co-crystal, methods of making mixed co-crystals, and methods of using mixed co-crystals are also described.
摘要翻译： 描述了包含API，第一共晶体形成器和与所述第一共晶体形成体同构取代的第二共晶体形成器的混合共晶体。 还描述了包含混合共晶的药物组合物，制备混合共晶体的方法和使用混合共晶体的方法。
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公开(公告)号：US20050267209A1
公开(公告)日：2005-12-01
申请号：US11139245
申请日：2005-05-27
IPC分类号： A01N37/18 , A61K9/00 , A61K9/20 , A61K9/26 , A61K31/165 , A61K31/191 , A61K31/205
CPC分类号： A61K31/165 , A61K9/145 , A61K31/191 , C07C55/10 , C07C57/15 , C07C317/44 , A61K2300/00
摘要： A mixed co-crystal comprising an API, a first co-crystal former, and a second co-crystal former which is isomorphically substitutable with said first co-crystal former is described. A pharmaceutical composition comprising a mixed co-crystal, methods of making mixed co-crystals, and methods of using mixed co-crystals are also described.
摘要翻译： 描述了包含API，第一共晶体形成器和与所述第一共晶体形成器同构取代的第二共晶体形成器的混合共晶体。 还描述了包含混合共晶的药物组合物，制备混合共晶体的方法和使用混合共晶体的方法。
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3.发明申请Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen 审中-公开卡马西平，塞来昔布，奥氮平，伊曲康唑，托吡酯，莫达非尼，5-氟尿嘧啶，氢氯噻嗪，对乙酰氨基酚，阿司匹林，氟比洛芬，苯妥英和布洛芬的药物共晶组合物公开(公告)号：US20070059356A1
公开(公告)日：2007-03-15
申请号：US10546963
申请日：2004-02-26
申请人： Örn Almarsson , Magali Bourghol Hickey , Matthew Peterson , Michael Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
发明人： Örn Almarsson , Magali Bourghol Hickey , Matthew Peterson , Michael Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
IPC分类号： A61K31/551 , A61K31/55 , A61K31/496 , A61K31/415 , A61K31/455
CPC分类号： A61K31/415 , A61K31/455 , A61K31/496 , A61K31/55 , A61K31/551
摘要： A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
摘要翻译： 一种药物组合物，其包含API和共晶体形成剂的共晶体; 其中API具有至少一个选自醚，硫醚，醇，硫醇，醛，酮，硫酮，硝酸酯，磷酸酯，硫代磷酸酯，酯，硫酯，硫酸酯，羧酸，次膦酸，膦酸， 磺酸，酰胺，伯胺，仲胺，氨，叔胺，亚胺，硫氰酸酯，氨腈，肟，腈重氮，有机卤化物，硝基，S-杂环，噻吩，N-杂环，吡咯， 呋喃，环氧化物，过氧化物，异羟肟酸，咪唑，吡啶和共结晶形成物具有至少一个选自胺，酰胺，吡啶，咪唑，吲哚，吡咯烷，羰基，羧基，羟基，苯酚，砜，磺酰基， 巯基和甲基硫基，使得API和共晶体形成剂能够在结晶条件下从溶液相共结晶。
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公开(公告)号：US20100210731A1
公开(公告)日：2010-08-19
申请号：US12708998
申请日：2010-02-19
IPC分类号： A61K31/165 , C07C233/11 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： C07C317/50 , A61K31/165 , C07C317/44
摘要： Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
摘要翻译： 形成和讨论了外消旋，对映异构体纯和对映体混合的莫达非尼的多晶型物和溶剂合物。 此外，所述形式被描述为可用于治疗许多病症，包括但不限于发作性睡病。
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公开(公告)号：US07566805B2
公开(公告)日：2009-07-28
申请号：US10570405
申请日：2004-09-04
IPC分类号： C07C323/22 , A61K31/165
CPC分类号： C07C317/38
摘要： Co-crystals and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and several important physical properties are modulated. The solubility, dissolution, bioavailability, dose response, and stability of modafinil can be modulated to improve efficacy in pharmaceutical compositions.
摘要翻译： 形成外消旋，对映异构体纯和对映异构体混合的莫达非尼的共晶体和溶剂合物，并调制几种重要的物理性质。 可以调节莫达非尼的溶解度，溶解度，生物利用度，剂量反应和稳定性，以提高药物组合物的功效。
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公开(公告)号：US08338646B2
公开(公告)日：2012-12-25
申请号：US12708998
申请日：2010-02-19
IPC分类号： C07C233/65
CPC分类号： C07C317/50 , A61K31/165 , C07C317/44
摘要： Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
摘要翻译： 形成和讨论了外消旋，对映异构体纯和对映体混合的莫达非尼的多晶型物和溶剂合物。 此外，所述形式被描述为可用于治疗许多病症，包括但不限于发作性睡病。
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公开(公告)号：US20090018202A1
公开(公告)日：2009-01-15
申请号：US10587086
申请日：2005-02-01
IPC分类号： A61K31/165 , C07C231/00 , A61P25/00
CPC分类号： C07C317/50 , A61K31/165 , C07C317/44
摘要： Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.
摘要翻译： 形成和讨论了外消旋，对映异构体纯和对映体混合的莫达非尼的多晶型物和溶剂合物。 此外，所述形式被描述为可用于治疗许多病症，包括但不限于发作性睡病。
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公开(公告)号：US20070026078A1
公开(公告)日：2007-02-01
申请号：US10660202
申请日：2003-09-11
申请人： Orn Almarsson , Magali Bourghol Hickey , Matthew Peterson , Michael Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
发明人： Orn Almarsson , Magali Bourghol Hickey , Matthew Peterson , Michael Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
IPC分类号： A61K9/14
CPC分类号： A61K9/145 , A61K9/0004 , A61K9/1617 , A61K9/1652 , A61K9/2077 , A61K9/209 , A61K31/167 , A61K31/192 , A61K31/4166 , A61K31/55 , A61K31/616 , A61K47/10 , A61K47/32 , C07C51/412 , C07C51/43 , C07C233/25 , C07D223/26 , C07D233/74 , C07D495/04 , C07C53/06 , C07C53/10 , C07C57/30 , C07C61/135
摘要： A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
摘要翻译： 一种药物组合物，其包含API和共晶体形成剂的共晶体; 其中API具有至少一个选自醚，硫醚，醇，硫醇，醛，酮，硫酮，硝酸酯，磷酸酯，硫代磷酸酯，酯，硫酯，硫酸酯，羧酸，膦酸，次膦酸， 磺酸，酰胺，伯胺，仲胺，氨，叔胺，sp2胺，硫氰酸酯，氨腈，肟，腈重氮，有机卤化物，硝基，S-杂环，噻吩，n-杂环，吡咯， ，呋喃，环氧化物，过氧化物，异羟肟酸，咪唑，吡啶和共结晶形成物具有至少一个选自胺，酰胺，吡啶，咪唑，吲哚，吡咯烷，羰基，羧基，羟基，苯酚，砜，磺酰基 ，巯基和甲基硫基，使得API和共结晶形成体能够在结晶条件下从溶液相共结晶。
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公开(公告)号：US20060134198A1
公开(公告)日：2006-06-22
申请号：US10541216
申请日：2003-12-24
申请人： Mark Tawa , Julius Remenar , Matthew Peterson , Orn Almarsson , Hector Guzman , Hongming Chen , Mark Oliveira
发明人： Mark Tawa , Julius Remenar , Matthew Peterson , Orn Almarsson , Hector Guzman , Hongming Chen , Mark Oliveira
IPC分类号： A61K9/20
CPC分类号： A61K9/1652 , A61K9/145 , A61K9/146 , A61K31/18 , A61K31/365 , A61K31/415 , A61K31/635 , A61K47/10 , A61K47/32 , C07D231/12
摘要： The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.
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公开(公告)号：US20060052432A1
公开(公告)日：2006-03-09
申请号：US10528244
申请日：2003-09-16
申请人： Julius Remenar , Matthew Peterson , Orn Almarsson , Hector Guzman , Hongming Chen , Mark Tawa , Mark Oliveira
发明人： Julius Remenar , Matthew Peterson , Orn Almarsson , Hector Guzman , Hongming Chen , Mark Tawa , Mark Oliveira
IPC分类号： A61K9/00 , A61K31/18 , A61K31/415 , A61K31/365
CPC分类号： A61K9/0019 , A61K9/145 , A61K9/146 , A61K31/18 , A61K31/365 , A61K31/415 , A61K31/635 , A61K47/10
摘要： The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.
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