专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 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。

12. 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。

13. 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。

14. 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。

15. 发明授权

US07153879B2 Polymorphs of an epothilone analog 有权
公开(公告)号：US07153879B2
公开(公告)日：2006-12-26
申请号：US11271456
申请日：2005-11-10
申请人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
发明人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： C07D493/04 , A61K31/42 , A61P35/00
CPC分类号： C07D491/04 , C07D417/06
摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

16. 发明授权

US06982276B2 Polymorphs of an epothilone analog 有权
公开(公告)号：US06982276B2
公开(公告)日：2006-01-03
申请号：US10773819
申请日：2004-02-06
申请人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
发明人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： C07D493/04 , A61K31/42
CPC分类号： C07D491/04 , C07D417/06
摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

17. 发明申请

US20070238770A1 PROCESS FOR PREPARING NOVEL CRYSTALLINE FORMS OF PELIGLITAZAR, NOVEL STABLE FORMS PRODUCED THEREIN AND FORMULATIONS 审中-公开
标题翻译：制备新型结晶形式的方法，生产的新型稳定形式和配方
公开(公告)号：US20070238770A1
公开(公告)日：2007-10-11
申请号：US11695124
申请日：2007-04-02
申请人： Jack Z. Gougoutas , Yongmei Wu , Soojin Kim , Dejah T. Petsch
发明人： Jack Z. Gougoutas , Yongmei Wu , Soojin Kim , Dejah T. Petsch
IPC分类号： A61K31/421 , C07D263/34
CPC分类号： C07D263/32
摘要： A process is provided for selectively preparing novel stable crystalline forms, namely selectively and consistently preparing Form N-1 of the free acid peliglitazar, Form N-2 of the free acid peliglitazar and Form P-1 of the L-lysine salt of the free acid peliglitazar. The process preferably employs solvent systems which produce crystals having suitable flow properties and desired particle size.Novel Form N-1 crystals of the free acid, Form N-2 crystals of the free acid, Form P-1 crystals of the L-lysine salt of the free acid, pharmaceutical compositions containing such novel forms and a method of treating diabetes, dyslipidemia and atherosclerosis employing such novel forms are also provided.
摘要翻译：提供了一种选择性制备新的稳定结晶形式的方法，即选择性且一致地制备游离酸百日preparing唑形式的N-1，游离酸百日lit嗪的N-2型和游离酸性赖氨酸盐的L-赖氨酸盐形式P-1 酸苦瓜该方法优选使用产生具有合适流动性和所需粒度的晶体的溶剂体系。游离酸的新型N-1晶型，游离酸形式的N-2晶体，游离酸的L-赖氨酸盐的形式P-1晶体，含有这种新形式的药物组合物和治疗糖尿病的方法，还提供了使用这种新型形式的血脂异常和动脉粥样硬化。

18. 发明授权

US08501698B2 Crystal structures of SGLT2 inhibitors and processes for preparing same 有权
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US08501698B2
公开(公告)日：2013-08-06
申请号：US13049712
申请日：2011-03-16
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
IPC分类号： A61K31/351 , C07D309/10 , C07H7/04
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法，制备方法以及使用这种结构治疗糖尿病等疾病的方法。

19. 发明授权

US06858644B2 Paclitaxel solvates 失效
标题翻译：紫杉醇溶剂化物
公开(公告)号：US06858644B2
公开(公告)日：2005-02-22
申请号：US10304615
申请日：2002-11-26
申请人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
发明人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
IPC分类号： A61K31/337 , A61P35/00 , C07C233/03 , C07C233/05 , C07C255/03 , C07C317/04 , C07D305/14 , C07D409/12 , A61K31/335
CPC分类号： C07D409/12 , A61K31/337 , C07D305/14
摘要： Biologically active crystalline solvates of paclitaxel are precipitated using polar, aprotic, organic solvents. A pharmaceutical composition is also disclosed, as well as the preparation of the novel solvates and their uses as anti-tumor agents.
摘要翻译：使用极性，非质子，有机溶剂沉淀紫杉醇的生物活性结晶溶剂合物。还公开了药物组合物，以及新溶剂合物的制备及其作为抗肿瘤剂的用途。

20. 发明授权

US07919598B2 Crystal structures of SGLT2 inhibitors and processes for preparing same 有权
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US07919598B2
公开(公告)日：2011-04-05
申请号：US11765481
申请日：2007-06-20
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
IPC分类号： C07H7/04 , C07H1/00 , A61K31/70
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法，制备方法以及使用这种结构治疗糖尿病等疾病的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式