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11. 发明申请

US20120283181A1 CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME 审中-公开
标题翻译：萨克拉平的晶体形式及其制备方法
公开(公告)号：US20120283181A1
公开(公告)日：2012-11-08
申请号：US13546584
申请日：2012-07-11
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , A61K38/26 , A61K38/28 , A61K31/702 , A61K31/70 , A61P3/10 , A61P3/04 , A61P27/02 , A61P9/10 , A61P25/00 , A61P29/00 , A61P17/06 , A61P37/06 , A61P3/06 , A61P19/02 , A61P15/08 , C07D209/52
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。

12. 发明申请

US20110257085A1 Crystal Forms of Saxagliptin and Processes for Preparing Same 有权
标题翻译： Saxagliptin的晶体形式及其制备方法
公开(公告)号：US20110257085A1
公开(公告)日：2011-10-20
申请号：US13081341
申请日：2011-04-06
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , A61K31/702 , A61K31/445 , A61K31/4439 , A61K38/28 , A61K38/26 , A61K31/451 , A61K38/22 , A61K31/70 , A61K38/18 , A61K31/407 , A61K31/44 , A61K31/405 , A61K31/47 , A61P3/10 , A61P3/08 , A61P3/06 , A61P3/04 , A61P3/00 , A61P9/10 , A61P15/00 , A61P43/00 , A61P19/02 , A61P37/06 , A61P1/00 , A61P29/00 , A61P19/10 , A61K31/4965
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。

13. 发明授权

US07829720B2 Process for preparing atazanavir bisulfate and novel forms 有权
标题翻译：制备阿扎那韦硫酸氢盐和新型形式的方法
公开(公告)号：US07829720B2
公开(公告)日：2010-11-09
申请号：US11119558
申请日：2005-05-02
申请人： Soojin Kim , Bruce T. Lotz , Mary F. Malley , Jack Z. Gougoutas , Martha Davidovich , Sushil K. Srivastava
发明人： Soojin Kim , Bruce T. Lotz , Mary F. Malley , Jack Z. Gougoutas , Martha Davidovich , Sushil K. Srivastava
IPC分类号： C07D213/56
CPC分类号： C07D213/42
摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.
摘要翻译：提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法，其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量％的游离碱反应，阿扎那韦的A型晶体种子将硫酸氢盐加入到反应混合物中，并且以硫酸氢盐形式的结晶，按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸，以实现阿扎那韦硫酸氢盐的形式A晶体的形成。还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。还提供了一种新型形式的阿扎那韦硫酸氢盐，其为E3型，其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。

14. 发明申请

US20090312331A1 PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPYLPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN 审中-公开
标题翻译：制备4 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三氮杂- 碳酰胺和生产的新型稳定形式
公开(公告)号：US20090312331A1
公开(公告)日：2009-12-17
申请号：US12478210
申请日：2009-06-04
申请人： Soojin Kim , Mary F. Malley , Zhongping Shi
发明人： Soojin Kim , Mary F. Malley , Zhongping Shi
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well.Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.
摘要翻译：提供了选择性和一致地选择性制备新的稳定结晶盐形式的方法，即制备甲磺酸盐的N-1型，和p38激酶抑制剂4的盐酸盐的N-1和N-4型 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三嗪-6-甲酰胺。该方法优选使用包含甲酸/丙酮和甲酸/甲基乙基酮的溶剂体系，其产生具有合适流动性和所需粒径的晶体，并且也可以使用溶剂如N，N-二甲基甲酰胺和N，N-二甲基乙酰胺。上述游离碱的甲磺酸盐的盐酸盐形式的N-1型和N-4型结晶的新型N-1晶体和形式N-1晶体，含有这种新形式的药物组合物和治疗方法还提供p38激酶相关病症，包括类风湿性关节炎。

15. 发明申请

US20090054303A1 CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME 有权
标题翻译：萨克拉平的晶体形式及其制备方法
公开(公告)号：US20090054303A1
公开(公告)日：2009-02-26
申请号：US12105316
申请日：2008-04-18
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K38/28 , C07D209/52 , A61K31/403 , A61P3/04 , A61K38/17
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。

16. 发明申请

US20080269499A1 CRYSTALLINE FORMS AND PROCESS FOR PREPARING SPIRO-HYDANTOIN COMPOUNDS 审中-公开
标题翻译：晶体形式和制备SPIRO-HYDANTOIN化合物的方法
公开(公告)号：US20080269499A1
公开(公告)日：2008-10-30
申请号：US12130915
申请日：2008-05-30
申请人： Albert J. DelMonte , T.G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
发明人： Albert J. DelMonte , T.G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.
摘要翻译：提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及使用它。提供某些中间体的结晶形式。

17. 发明申请

US20080188517A1 CRYSTALLINE FORMS OF A FACTOR XA INHIBITOR 审中-公开
标题翻译：因子XA抑制剂的晶体形式
公开(公告)号：US20080188517A1
公开(公告)日：2008-08-07
申请号：US12099906
申请日：2008-04-09
申请人： Michael J. Orwat , Mary F. Malley , Roxana Schlam , Steven R. Fabian , Bing-Shiou Yang , Victor W. Rosso
发明人： Michael J. Orwat , Mary F. Malley , Roxana Schlam , Steven R. Fabian , Bing-Shiou Yang , Victor W. Rosso
IPC分类号： A61K31/437 , A61P9/00
CPC分类号： C07D471/04
摘要： The instant invention provides crystalline forms of 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one and its solvates thereof, processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.
摘要翻译：本发明提供3-（1-羟基-1-甲基 - 乙基）-1-（4-甲氧基 - 苯基）-6- [4-（2-氧代-2H-吡啶-1-基） - 苯基] -1,4,5,6-四氢 - 吡唑并[3,4-c]吡啶-7-酮及其溶剂合物，生产这种结晶形式的方法; 包含这种结晶形式的药物组合物; 以及用这种结晶形式或这种药物组合物治疗血栓栓塞障碍的方法。

18. 发明授权

US07381737B2 Crystalline forms and process for preparing spiro-hydantoin compounds 有权
标题翻译：结晶形式和制备螺 - 乙内酰脲化合物的方法
公开(公告)号：US07381737B2
公开(公告)日：2008-06-03
申请号：US11238427
申请日：2005-09-29
申请人： Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
发明人： Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
IPC分类号： A61K31/4188 , C07D235/00
CPC分类号： C07D487/10
摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.
摘要翻译：提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及使用它。提供某些中间体的结晶形式。

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