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1. 发明申请

WO2004078161A1 PHARMACEUTICAL CO-CRYSTAL COMPOSITIONS OF DRUGS SUCH AS CARBAMAZEPTINE, CELECOXIB, OLANZAPINE, ITRACONAZOLE, TOPIRAMATE, MODAFINIL, 5-FLUOROURACIL, HYDROCHLOROTHIAZIDE, ACETAMINOPHEN, ASPIRIN, FLURBIPROFEN, PHENYTOIN AND IBUPROFEN 审中-公开
标题翻译：药物如卡巴西汀，CELECOXIB，OLANZAPINE，ITRACONAZOLE，TOPIRAMATE，MODAFINIL，5-氟尿嘧啶，氢氯噻嗪，乙酰胺苯丙氨酸，阿司匹林，氟苯比芬，苯丁酸和IBUPROFEN的药物组合物
公开(公告)号：WO2004078161A1
公开(公告)日：2004-09-16
申请号：PCT/US2003/027772
申请日：2003-09-04
申请人： TRANSFORM PHARMACEUTICALS, INC. , UNIVERSITY OF SOUTH FLORIDA , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , ALMARSSON, Örn , BOURGHOL HICKEY, Magali , PETERSON, Matthew , ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
发明人： ALMARSSON, Örn , BOURGHOL HICKEY, Magali , PETERSON, Matthew , ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
IPC分类号： A61K9/14
CPC分类号： A61K31/00
摘要： A pharmaceutical composition comprising a co-crystal of an API and a co-crystal forming compound; 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, oheterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal forming compound 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 forming compound 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和共晶形成化合物的共晶体; 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，sp 2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，杂环，呋喃环氧化物，过氧化物，异羟肟酸，咪唑，吡啶和共晶形成化合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和共晶形成化合物能够在结晶条件下从溶液相共结晶。

2. 发明申请

WO2003074474A2 MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT 审中-公开
标题翻译：含至少一种活性药物成分的多组分固体相
公开(公告)号：WO2003074474A2
公开(公告)日：2003-09-12
申请号：PCT/US2003/006662
申请日：2003-03-03
申请人： UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF MICHIGAN , ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
发明人： ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
IPC分类号： C07C233/25
CPC分类号： C07D223/26 , A61K9/1652 , A61K31/167 , A61K31/192 , A61K31/4166 , A61K31/55 , A61K31/616 , A61K47/10 , A61K47/32 , C07C47/544 , C07C51/412 , C07C51/43 , C07C53/02 , C07C53/08 , C07C53/124 , C07C57/30 , C07C57/58 , C07C61/135 , C07C63/307 , C07C69/157 , C07C205/57 , C07C233/03 , C07C233/25 , C07C233/75 , C07C317/04 , C07D213/06 , C07D213/22 , C07D213/69 , C07D213/79 , C07D213/82 , C07D233/74 , C07D275/06 , C07C53/06 , C07C53/10
摘要： The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
摘要翻译：本发明涉及一种鉴定互补化学官能团以形成所需超分子合成子的方法。本发明还涉及包含一种或多种药物实体的多组分相组合物以及生产这种组合物的方法。

3. 发明申请

WO2004078163A3 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
标题翻译：药物如碳水化合物，CELECOXIB，OLANZAPINE，ITRACONAZOLE，TOPIRAMATE，MODAFINIL，5-氟尿嘧啶，氢氯噻嗪，乙酰氨基丁酸，阿司匹林，氟苯尿酸，苯乙酸和IBUPROFEN的药物复方结晶组合物
公开(公告)号：WO2004078163A3
公开(公告)日：2005-01-20
申请号：PCT/US2004006288
申请日：2004-02-26
申请人： TRANSFORM PHARMACEUTICALS INC , UNIV SOUTH FLORIDA , UNIV MICHIGAN , ALMARSSON OERN , HICKEY MAGALI BOURGHOL , PETERSON MATTHEW , ZAWOROTKO MICHAEL J , MOULTON BRIAN , RODRIGUEZ-HORNEDO NAIR
发明人： ALMARSSON OERN , HICKEY MAGALI BOURGHOL , PETERSON MATTHEW , MOULTON BRIAN , RODRIGUEZ-HORNEDO NAIR
IPC分类号： A61K9/14 , A61K31/00 , C07C233/00 , C07D233/00
CPC分类号： A61K9/1623 , A61K9/145
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，吡啶和共结晶形成体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。

4. 发明申请

WO2004078163A2 PHARMACEUTICAL CO-CRYSTAL COMPOSITIONS 审中-公开
标题翻译：药用组合物
公开(公告)号：WO2004078163A2
公开(公告)日：2004-09-16
申请号：PCT/US2004/006288
申请日：2004-02-26
申请人： TRANSFORM PHARMACEUTICALS, INC. , UNIVERSITY OF SOUTH FLORIDA , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , ZAWOROTKO, Michael, J. , ALMARSSON, Örn , HICKEY, Magali, Bourghol , PETERSON, Matthew , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
发明人： ALMARSSON, Örn , HICKEY, Magali, Bourghol , PETERSON, Matthew , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
IPC分类号： A61K9/14
CPC分类号： A61K9/1623 , A61K9/145
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。

5. 发明申请

WO2007139731A1 NEUTRAL PHARMACEUTICALS 审中-公开
标题翻译：中性药物
公开(公告)号：WO2007139731A1
公开(公告)日：2007-12-06
申请号：PCT/US2007/011990
申请日：2007-05-21
申请人： BROWN UNIVERSITY , MOULTON, Brian, Douglas , MA, Zhenbo
发明人： MOULTON, Brian, Douglas , MA, Zhenbo
IPC分类号： A61K51/00 , A61K9/00
CPC分类号： A61K49/001
摘要： The invention comprises neutral multi-functionality assemblies of pharmaceuticals comprising an active medicinal functionality, a transition metal functionality, and an ancillary ligand functionality. An exemplary series of mixed-ligand coordination complexes comprised of copper(Il), a drug and an ancillary ligand were made and tested. It is demonstrated that the judicious choice of an ancillary ligand affords a large degree of control over die relative lipophilicity/hydrophiiicity of the complex in relation to the uncomplexed drug molecule. The important factors to be considered in the design of such complexes, such as the additive-constitutive nature of the partition coefficient of the ancillary ligand and the relative size of the two types of ligands are disclosed, and methods of designing neutral multi- functionality assemblies of pharmaceuticals are disclosed.
摘要翻译：本发明包括药物的中性多功能组件，其包含活性药用官能团，过渡金属官能团和辅助配体官能团。制备并测试了由铜（II），药物和辅助配体组成的示例性的一系列混合配体配位络合物。证明了辅助配体的明智选择可以大大控制复合物相对于未复合药物分子的相对亲油性/亲水性。公开了在这种配合物的设计中要考虑的重要因素，例如辅助配体的分配系数的添加组成性质和两种配体的相对大小，以及设计中性多功能组件的方法的药物被公开。

6. 发明申请

WO2003074474A3 MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT 审中-公开
公开(公告)号：WO2003074474A3
公开(公告)日：2003-09-12
申请号：PCT/US2003/006662
申请日：2003-03-03
申请人： UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF MICHIGAN , ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
发明人： ZAWOROTKO, Michael, J. , MOULTON, Brian , RODRIGUEZ-HORNEDO, Nair
IPC分类号： C07C233/25
摘要： The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

7. 发明申请

WO2002068430A1 POLYHEDRA 审中-公开
标题翻译：多面体
公开(公告)号：WO2002068430A1
公开(公告)日：2002-09-06
申请号：PCT/US2002/005743
申请日：2002-02-25
申请人： UNIVERSITY OF SOUTH FLORIDA , ZAWOROTKO, Michael, J. , MOULTON, Brian
发明人： ZAWOROTKO, Michael, J. , MOULTON, Brian
IPC分类号： C07F1/08
CPC分类号： C07F3/06 , C07F1/08 , C30B7/00 , C30B29/605
摘要： The subject invention pertains to nanoscale polyhedron-shaped molecules having molecular building blocks connected at their vertices. The subject invention also concerns methods of producing nanoscale polyhedrons utilizing a self-assembly reaction. The resultant molecules are faceted polyhedra that are porous, chemically robust, contain chemically accessible sites on their facets, and which are neutral and soluble in common laboratory solvents. The nanoscale polyhedrons can exhibit additional desirable physical properties, such as ferromagnetic properties.
摘要翻译：本发明涉及具有在其顶点连接的分子结构单元的纳米级多面体形分子。本发明还涉及利用自组装反应制备纳米级多面体的方法。所得分子是多面体，化学稳定的多面体，在其小面上含有化学可访问的位点，并且其在中性和可溶于常见的实验室溶剂中。纳米级多面体可以表现出额外的理想物理性质，例如铁磁性质。

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