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1. 发明申请

WO2011133956A1 PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF 审中-公开
标题翻译：药物组合物及其药理学
公开(公告)号：WO2011133956A1
公开(公告)日：2011-10-27
申请号：PCT/US2011/033693
申请日：2011-04-22
申请人： VERTEX PHARMACEUTICALS INCORPORATED , VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , BINCH, Hayley, Marie , BOTFIELD, Martyn, Curtis , FANNING, Lev Tyler, Dewey , GROOTENHUIS, Peter Diederik, Jan , HURLEY, Dennis, James , KADIYALA, Irina, Nikolaevna , KAUSHIK, Ritu, Rohit , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , LUISI, Brian , MEDEK, Ales , NUMA, Mehdi , SHETH, Urvi, Jagdishbhai , SILINA, Alina , VERWIJS, Marinus, Jacobus , YANG, Xiaoqing , YOUNG, Christopher Ryan , ZAMAN, Noreen, Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
发明人： VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , BINCH, Hayley, Marie , BOTFIELD, Martyn, Curtis , FANNING, Lev Tyler, Dewey , GROOTENHUIS, Peter Diederik, Jan , HURLEY, Dennis, James , KADIYALA, Irina, Nikolaevna , KAUSHIK, Ritu, Rohit , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , LUISI, Brian , MEDEK, Ales , NUMA, Mehdi , SHETH, Urvi, Jagdishbhai , SILINA, Alina , VERWIJS, Marinus, Jacobus , YANG, Xiaoqing , YOUNG, Christopher Ryan , ZAMAN, Noreen, Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
CPC分类号： A61K31/4709 , A61K31/404 , A61K31/443 , A61K31/4704 , A61K45/06 , C07D405/12 , C12Q1/34 , G01N2500/04 , G01N2500/20 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.(Formula I), (Formula II), (Formula III).
摘要翻译：本发明涉及药物组合物，其包含与式II化合物和/或式III化合物中的一种或两种结合的式I化合物。本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法（式I），（式II），（式III）。

2. 发明申请

WO2013016492A1 THIOPHENE COMPOUNDS 审中-公开
标题翻译：噻吩化合物
公开(公告)号：WO2013016492A1
公开(公告)日：2013-01-31
申请号：PCT/US2012/048261
申请日：2012-07-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LUISI, Brian
发明人： LUISI, Brian
IPC分类号： C07D333/40 , A61K31/381 , A61P31/14
CPC分类号： C07D333/40 , A61K9/0019 , A61K9/1652 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866 , A61K31/381 , A61K47/40 , C07D333/38
摘要： A co-crystal of Compound (1) includes Compound (1) and a co-crystal former selected from the group consisting of urea, nicotinamide, and isonicotinamide, wherein Compound (1) is characterized by the following structural formula:(I) A pharmaceutical composition includes such a co-crystal of Compound (1) and at least one pharmaceutically acceptable carrier or excipient.
摘要翻译：化合物（1）的共晶包括化合物（1）和选自脲，烟酰胺和异烟酰胺的共结晶形成物，其中化合物（1）的特征在于以下结构式：（I）A 药物组合物包括化合物（1）和至少一种药学上可接受的载体或赋形剂的共晶体。

3. 发明申请

WO2013016490A1 THIOPHENE COMPOUNDS 审中-公开
标题翻译：噻吩化合物
公开(公告)号：WO2013016490A1
公开(公告)日：2013-01-31
申请号：PCT/US2012/048258
申请日：2012-07-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LUISI, Brian , WILLCOX, David , ROEPER, Stefanie , HU, Kan-Nian , LUONG, Hoa, Q.
发明人： LUISI, Brian , WILLCOX, David , ROEPER, Stefanie , HU, Kan-Nian , LUONG, Hoa, Q.
IPC分类号： C07D333/40 , A61K31/381 , A61P31/14
CPC分类号： C07D333/40 , A61K9/0019 , A61K9/1652 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866 , A61K31/381 , A61K47/40 , C07D333/38
摘要： Polymorph Forms M, H, P, X, and ZA of Compound (1) represented by the following structural formula: are described. A method of preparing polymorph Form M of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes isopropanol, ethyl acetate, n -butyl acetate, methyl acetate, acetone, 2-butanone (methylethylketone (MEK)), or heptane, or a combination thereof at a temperature in a range of 10 °C to 47 °C to form From M of Compound (1). A method of preparing polymorph Form H of Compound (1) includes stirring a solution of Compound (1) at a temperature in a range of 48 °C to 70 °C to form Form H of Compound (1). A method of preparing polymorph Form P of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes a solvent selected from the group consisting of dichloromethane and tetrahydrofuran (THF), and a mixture thereof at room temperature to form Form P of Compound (1). A method of preparing polymorph Form X of Compound (1) includes removing ethyl acetate from ethylacetate solvate G of Compound (1). A method of preparing polymorph Form ZA of Compound (1) includes removing n -butyl acetate from n-butyl acetate solvate A of Compound (1).
摘要翻译：描述了由以下结构式表示的化合物（1）的多晶型：M，H，P，X和ZA。制备化合物（1）的多晶型物M的方法包括搅拌化合物（1）和包括异丙醇，乙酸乙酯，乙酸正丁酯，乙酸甲酯，丙酮，2-丁酮（甲基乙基酮（MEK））的溶剂体系的混合物，）或庚烷或其组合，在10℃至47℃的温度范围内，以形成化合物（1）的M。制备化合物（1）的多晶型物H的方法包括在48℃至70℃的温度范围内搅拌化合物（1）的溶液以形成化合物（1）的H型。制备化合物（1）的多晶型P的方法包括：将化合物（1）和包含选自二氯甲烷和四氢呋喃（THF）的溶剂的溶剂体系的混合物及其混合物在室温下搅拌至形成化合物（1）的形式P. 制备化合物（1）的多晶型物X的方法包括从化合物（1）的乙酸乙酯溶剂化物G中除去乙酸乙酯。制备化合物（1）的多晶型ZA的方法包括从化合物（1）的乙酸正丁酯溶剂化物A中除去乙酸正丁酯。

4. 发明申请

WO2011133953A1 PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF 审中-公开
标题翻译：药物组合物及其药理学
公开(公告)号：WO2011133953A1
公开(公告)日：2011-10-27
申请号：PCT/US2011/033689
申请日：2011-04-22
申请人： VERTEX PHARMACEUTICALS INCORPORATED , VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , AREKAR, Sneha, G. , BINCH, Hayley, Marie , BOTFIELD, Martyn, Curtis , FANNING, Lev, Tyler Dewey , GROOTENHUIS, Peter, Diederik Jan , HURLEY, Dennis, James , JOHNSTON, Steven, C. , KADIYALA, Irina, Nikolaevna , KAUSHIK, Ritu, Rohit , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , LUISI, Brian , MEDEK, Ales , MUDUNURI, Praveen , NUMA, Mehdi , SHETH, Urvi Jagdishbhai , SILINA, Alina , SULLIVAN, Mark Jeffrey , VERWIJS, Marinus Jacobus , YANG, Xiaoqing , YOUNG, Christopher Ryan , ZAMAN, Noreen Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
发明人： VAN GOOR, Fredrick, F. , ALARGOVA, Rossitza, Gueorguieva , ALCACIO, Tim, Edward , AREKAR, Sneha, G. , BINCH, Hayley, Marie , BOTFIELD, Martyn, Curtis , FANNING, Lev, Tyler Dewey , GROOTENHUIS, Peter, Diederik Jan , HURLEY, Dennis, James , JOHNSTON, Steven, C. , KADIYALA, Irina, Nikolaevna , KAUSHIK, Ritu, Rohit , KESHAVARZ-SHOKRI, Ali , KRAWIEC, Mariusz , LEE, Elaine, Chungmin , LUISI, Brian , MEDEK, Ales , MUDUNURI, Praveen , NUMA, Mehdi , SHETH, Urvi Jagdishbhai , SILINA, Alina , SULLIVAN, Mark Jeffrey , VERWIJS, Marinus Jacobus , YANG, Xiaoqing , YOUNG, Christopher Ryan , ZAMAN, Noreen Tasneem , ZHANG, Beili , ZHANG, Yuegang , ZLOKARNIK, Gregor
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
CPC分类号： A61K31/4709 , A61K31/404 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/4704 , G01N33/6872 , G01N2333/4703 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.
摘要翻译：本发明涉及包含式I和II化合物，任选与式III化合物和/或式IV化合物组合的药物组合物。本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法。

5. 发明申请

WO2011050220A1 SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-TRIFLUOROMETHYL)PHENYL)-4-OXO-5-(TRIFLUOROMETHYL)-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE 审中-公开
标题翻译： N-（4-（7-亚氨基）[2.2.1]庚烷-7-YL）-2-三氟甲基）苯基）-4-氧代-5-（三氟甲基）-1,4-二氢喹啉-3-羧酰胺的固体形式
公开(公告)号：WO2011050220A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053633
申请日：2010-10-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ZHANG, Beili , KRAWIEC, Mariusz , LUISI, Brian , MEDEK, Ales
发明人： ZHANG, Beili , KRAWIEC, Mariusz , LUISI, Brian , MEDEK, Ales
IPC分类号： C07D487/08 , A61K31/407 , A61P11/00
CPC分类号： A61K31/4748 , A61K31/4709 , C07B2200/13 , C07D487/08
摘要： The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.
摘要翻译：本发明涉及N-（4-（7-氮杂双环[2.2.1]庚-7-基）-2-（三氟甲基）苯基）-4-氧代-5-（三氟甲基） -1,4-二氢喹啉-3-甲酰胺（A-HCl型，B型，B-HCl型，或这些形式的任何组合），其药物组合物及其处理方法。

6. 发明申请

WO2013158121A1 SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE 审中-公开
标题翻译： N- [2,4-BIS（1,1-二甲基乙基）-5-羟基苯基] -1,4-二氢-4-氧代喹啉-3-羧酰胺的固体形式
公开(公告)号：WO2013158121A1
公开(公告)日：2013-10-24
申请号：PCT/US2012/034578
申请日：2012-04-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LUISI, Brian , AREKAR, Sneha Ghanshyam , COSTACHE, Adriana , DINEHART, Kirk Raymond , JOHNSON, Steven, C. , NEUBERT-LANGILLE, Bobbianna, J.
发明人： LUISI, Brian , AREKAR, Sneha Ghanshyam , COSTACHE, Adriana , DINEHART, Kirk Raymond , JOHNSON, Steven, C. , NEUBERT-LANGILLE, Bobbianna, J.
IPC分类号： C07D215/56 , A61K31/47 , A61P25/00
CPC分类号： C07D215/56
摘要： The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1- dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.
摘要翻译：本发明涉及N- [2,4-双（1,1-二甲基乙基）-5-羟基苯基] -1,4-二氢-4-氧代喹啉-3-甲酰胺（化合物1）的结晶溶剂合物形式，他们的准备。本发明还涉及包含结晶溶剂化物形式的药物组合物，以及其处理方法。

7. 发明申请

WO2013016491A1 THIOPHENE COMPOUNDS 审中-公开
标题翻译：噻吩化合物
公开(公告)号：WO2013016491A1
公开(公告)日：2013-01-31
申请号：PCT/US2012/048260
申请日：2012-07-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LUISI, Brian , ROEPER, Stefanie , WILLCOX, David , WANG, Hongren , MUDUNURI, Praveen , LUONG, Hoa, Q.
发明人： LUISI, Brian , ROEPER, Stefanie , WILLCOX, David , WANG, Hongren , MUDUNURI, Praveen , LUONG, Hoa, Q.
IPC分类号： C07D333/40 , A61K31/381 , A61P31/14
CPC分类号： C07D333/40 , A61K9/0019 , A61K9/1652 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866 , A61K31/381 , A61K47/40 , C07D333/38
摘要： A solvate of Compound (1) is selected from the group consisting of: Compound 1⋅ H 2 0, Compound 1⋅ethanoHsopropanol, Compound 1⋅acetone, Compound 1⋅ethylacetate, Compound 1⋅isopropylacetate, Compound l⋅ethylacetate⋅2-methyl THF, Compound 1⋅ethanol, Compound 1⋅n-butylacetate; Compound 1 ⋅heptane; Compound 1⋅2-butanone; and Compound l»methylacetate, wherein Compound 1 is represented by the following structural formula (I): and wherein the Compound 1⋅H 2 0 are in a molar ratio of 1 : 0.5 to 1 :3 (Compound 1: H 2 0). A method of preparing such a solvate of Compound (1) includes stirring a mixture of Compound (1) and a solvent desired for the formation of the solvate of Compound (1).
摘要翻译：化合物（1）的溶剂合物选自：化合物1·H 2 O，化合物1·乙醇异丙醇，化合物1·丙酮，化合物1·乙酸乙酯，化合物1·乙酸异丙酯，化合物1·乙酸乙酯·2-甲基THF，化合物1·乙醇，化合物1·乙酸正丁酯; 化合物1·庚烷; 化合物1·2-丁酮; 和化合物I»乙酸甲酯，其中化合物1由以下结构式（I）表示：其中化合物1·H 2 O的摩尔比为1:0.5至1:3（化合物1：H 2 O）。制备化合物（1）的这种溶剂化物的方法包括搅拌化合物（1）和化合物（1）的溶剂合物形成所需溶剂的混合物。

8. 发明申请

WO2012097270A1 SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[5-[2-{1-HYDROXY-1-METHYL-ETHYL}PYRIMIDIN-5-YL]-7-(TETRAHYDROFURAN-2-YL}-1H-BENZIMIDAZOL-2-YL]UREA 审中-公开
标题翻译： γ-烯丙基-3- [5- [2- {1-羟基-1-甲基 - 乙基}嘧啶-5-基] -7-（四氢呋喃-2-基）-1H的固体形式苯并咪唑-2-基]脲
公开(公告)号：WO2012097270A1
公开(公告)日：2012-07-19
申请号：PCT/US2012/021275
申请日：2012-01-13
申请人： VERTEX PHARMACEUTICALS INCORPORATED , SHANNON, Dean , LUISI, Brian , LIAO, Yusheng , KRAWIEC, Mariusz
发明人： SHANNON, Dean , LUISI, Brian , LIAO, Yusheng , KRAWIEC, Mariusz
IPC分类号： C07D407/04 , A61K31/506
CPC分类号： C07D405/14 , C07D407/04
摘要： The present application is directed to solid forms of compounds of formula (I): and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infection.
摘要翻译：本申请涉及抑制细菌促旋酶和/或Topo IV的式（I）化合物及其药学上可接受的盐的固体形式，以及包含所述化合物和盐的药物组合物。这些化合物和盐可用于治疗细菌感染。

9. 发明申请

WO2012097273A1 SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL) PYRIMIDIN-5-YL]-7-(TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA 审中-公开
标题翻译： γ-烯丙基-3- [6-氟-5- [2-（1-羟基-1-甲基 - 乙基）嘧啶-5-基] -7-（四氢呋喃-2-基）基）-1H-苯并咪唑-2-基]脲
公开(公告)号：WO2012097273A1
公开(公告)日：2012-07-19
申请号：PCT/US2012/021280
申请日：2012-01-13
申请人： VERTEX PHARMACEUTICALS INCORPORATED , SHANNON, Dean , LUISI, Brian , KRAWIEC, Mariusz , KULDIPKUMAR, Anuj, K.
发明人： SHANNON, Dean , LUISI, Brian , KRAWIEC, Mariusz , KULDIPKUMAR, Anuj, K.
IPC分类号： C07D413/14 , A61K31/4184 , A61P31/00
CPC分类号： C07D405/14 , A61K31/4184 , A61K31/506
摘要： The present application is directed to solid forms of compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.
摘要翻译：本申请涉及抑制细菌促旋酶和/或Topo IV的式（I）化合物及其药学上可接受的盐的固体形式和包含所述化合物和盐的药物组合物。这些化合物和盐可用于治疗细菌感染。

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