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。

公开(公告)号：US20100311701A1

公开(公告)日：2010-12-09

申请号：US12792415

申请日：2010-06-02

申请人： Orn Almarsson ,  Magali Bourghol Hickey ,  Matthew Peterson ,  Michael J. Zaworotko ,  Brian Moulton ,  Nair Rodriguez-Hornedo

发明人： Orn Almarsson ,  Magali Bourghol Hickey ,  Matthew Peterson ,  Michael J. Zaworotko ,  Brian Moulton ,  Nair Rodriguez-Hornedo

IPC分类号： A61K31/616 ,  A61K31/415 ,  A61K31/455 ,  A61K31/335 ,  A61K31/357 ,  A61K31/5513 ,  A61K31/4196 ,  A61K31/194 ,  A61K31/165 ,  A61K31/191 ,  A61K31/513 ,  A61K31/17 ,  A61K31/549 ,  A61K31/167 ,  A61K31/444 ,  A61K31/4166 ,  A61K31/4412 ,  A61K31/192 ,  A61K31/55 ,  A61K31/12

CPC分类号： A61K31/12 ,  A61K31/165 ,  A61K31/167 ,  A61K31/17 ,  A61K31/191 ,  A61K31/192 ,  A61K31/194 ,  A61K31/335 ,  A61K31/357 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/455 ,  A61K31/513 ,  A61K31/549 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/616

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, imine, 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，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，O-杂环， 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。

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。

公开(公告)号：US07927613B2

公开(公告)日：2011-04-19

申请号：US10660202

申请日：2003-09-11

申请人： Örn Almarsson ,  Magali Bourghol Hickey ,  Matthew L. Peterson ,  Michael J. Zaworotko ,  Brian Moulton ,  Nair Rodriguez-Hornedo

发明人： Örn Almarsson ,  Magali Bourghol Hickey ,  Matthew L. Peterson ,  Michael J. Zaworotko ,  Brian Moulton ,  Nair Rodriguez-Hornedo

IPC分类号： A61K9/00 ,  A01N43/46 ,  A01N43/56

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。

公开(公告)号：US20080132419A1

公开(公告)日：2008-06-05

申请号：US11867432

申请日：2007-10-04

申请人： Nair Rodriguez-Hornedo

发明人： Nair Rodriguez-Hornedo

IPC分类号： C40B30/00 ,  C07D223/16

CPC分类号： C40B30/00 ,  C40B20/08 ,  C40B40/04

摘要： An approach to designing families of cocrystals with desired (tunable) pH dependent dissolution is developed. The solubility and dissolution rate of a family of cocrystals with the same API and a series of ligands that are weak acids or weak bases has been found to be determined and controlled by the acid or base dissociation constant of the ligand and the pH of the dissolution medium. In various aspects, pH dependent dissolution is imparted to a non-ionizable API or the dissolution of ionizable API's is modulated.

摘要翻译： 开发了设计具有期望（可调谐）pH依赖性溶解的共晶体家族的方法。 已经发现具有相同API的一系列共晶体和弱酸或弱碱的一系列配体的溶解度和溶解速率由配体的酸或碱解离常数和溶解的pH来确定和控制 中。 在各个方面，将pH依赖性溶解赋予不可离子化的API，或者调节可离子化的API的溶解。

公开(公告)号：US20070099237A1

公开(公告)日：2007-05-03

申请号：US11262995

申请日：2005-10-31

申请人： Nair Rodriguez-Hornedo

发明人： Nair Rodriguez-Hornedo

IPC分类号： C40B40/04 ,  A61K31/55 ,  A61K31/522 ,  A61K31/496 ,  A61K31/192 ,  A61K31/655

CPC分类号： A61K31/192 ,  A61K31/496 ,  A61K31/522 ,  A61K31/55 ,  A61K31/655

摘要： Multi-component crystals (co-crystals) are prepared by combining co-crystal components in non-stoichiometric concentrations in solution. The solubility of the molecular complex in the solvent is reduced, increasing the probability that the molecular complex is the least soluble form in the system, upon which it precipitates. A crystalline product is produced without the need for grinding, solvent evaporation, or temperature variation.

摘要翻译： 通过在溶液中组合非化学计量浓度的共晶组分来制备多组分晶体（共晶体）。 分子复合物在溶剂中的溶解度降低，增加了分子复合物在体系中最少溶解形式的可能性，在其上沉淀。 生产结晶产品而不需要研磨，溶剂蒸发或温度变化。