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1. 发明申请

WO2013016499A1 METHODS FOR PREPARATION OF THIOPHENE COMPOUNDS 审中-公开
标题翻译：制备噻吩化合物的方法
公开(公告)号：WO2013016499A1
公开(公告)日：2013-01-31
申请号：PCT/US2012/048270
申请日：2012-07-26
申请人： VERTEX PHARMACEUTICALS INCORPORATED , JURKAUSKAS, Valdas , RUGGIERO, Piero, L. , ROEPER, Stefanie , WILLCOX, David , WALDO, Michael , GUERETTE, Dahrika, Milfred Yap , KLINE, Billie, J. , LUONG, Hoa, Q.
发明人： JURKAUSKAS, Valdas , RUGGIERO, Piero, L. , ROEPER, Stefanie , WILLCOX, David , WALDO, Michael , GUERETTE, Dahrika, Milfred Yap , KLINE, Billie, J. , LUONG, Hoa, Q.
IPC分类号： C07D333/40 , A61K31/381 , A61P31/14
CPC分类号： C07D333/40 , A61K9/1623 , A61K9/2018 , A61K9/2054 , A61K9/4858
摘要： A method of preparing Compound (1): or a pharmaceutically acceptable salt thereof includes: a) reacting Compound (A) with 3,3- dimetylbut-l-yne in the presence of one or more palladium catalysts selected from the group consisting of Pd(PPh3)4 and Pd(PPh3)2Cl2, and one or more copper catalysts selected from the group consisting of Cul, CuBr, and CuCl, to generate Compound (B); b) treating Compound (B) with an acid to generate Compound (C): c) reducing the cyclohexanone of Compound (C) to cyclohexanol to generate Compound (D); and d) reacting Compound (D) with a base to generate Compound (1), wherein Compounds (A), (B), (C), and (D) are each as depicted herein.
摘要翻译：制备化合物（1）的方法或其药学上可接受的盐包括：a）在一种或多种钯催化剂的存在下，使化合物（A）与3,3-二甲基丁-1-炔反应，所述钯催化剂选自Pd （PPh 3）4和Pd（PPh 3）2 Cl 2和一种或多种选自Cul，CuBr和CuCl的铜催化剂，以产生化合物（B）; b）用酸处理化合物（B）以产生化合物（C）：c）将化合物（C）的环己酮还原成环己醇以产生化合物（D）; 和d）使化合物（D）与碱反应以产生化合物（1），其中化合物（A），（B），（C）和（D）各自如本文所述。

2. 发明申请

WO2010093889A3 SOLID FORMS OF 2-(2, 4-DIFLUOROPHENYL)-6-(1-(2,6-DIFLUOROPHENYL)UREIDO)NICOTINAMIDE 审中-公开
标题翻译： 2-（2,4-二氟苯基）-6-（1-（2,6-二氟苯基）尿苷）的固体形式NICOTINAMIDE
公开(公告)号：WO2010093889A3
公开(公告)日：2010-10-28
申请号：PCT/US2010024053
申请日：2010-02-12
申请人： VERTEX PHARMA , HURREY MICHAEL , ALARGOV DIMITAR , JOHNSTON STEVEN C , ROEPER STEFANIE , SNOONIAN JOHN R , COWANS BRETT A , VLAHOVA PETINKA , EBERLIN ALEXANDER , EDDLESTON MARK , FRAMPTON CHRIS
发明人： HURREY MICHAEL , ALARGOV DIMITAR , JOHNSTON STEVEN C , ROEPER STEFANIE , SNOONIAN JOHN R , COWANS BRETT A , VLAHOVA PETINKA , EBERLIN ALEXANDER , EDDLESTON MARK , FRAMPTON CHRIS
IPC分类号： C07D213/82 , A61K31/4418
CPC分类号： C07D213/82
摘要： This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(l- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.
摘要翻译：本发明涉及2-（2,4-二氟苯基）-6-（1-（2,6-二氟苯基）脲基）烟酰胺及其药物组合物的固体形式及其方法和用途。

3. 发明申请

WO2009038683A2 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：WO2009038683A2
公开(公告)日：2009-03-26
申请号：PCT/US2008/010728
申请日：2008-09-15
申请人： VERTEX PHARMACEUTICALS INCORPORATED , DEMATTEI, John , FENG, Yushi , HARRISON, Cristian , LOOKER, Adam , MUDUNURI, Praveen , ROEPER, Stefanie , ZHANG, Yuegang
发明人： DEMATTEI, John , FENG, Yushi , HARRISON, Cristian , LOOKER, Adam , MUDUNURI, Praveen , ROEPER, Stefanie , ZHANG, Yuegang
IPC分类号： A61K31/47 , C07D215/233 , A61P3/00 , A61P35/00 , A61P25/28 , A61P27/02 , A61P3/10
CPC分类号： C07D215/56 , A61K31/47 , A61K45/06 , C07D215/233
摘要： Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.
摘要翻译：本文描述了固体形式的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，包括其结晶形式。

4. 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。

5. 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。

6. 发明申请

WO2010093890A2 PROCESSES FOR PRODUCING PHENYL-6-(1-(PHENYL)UREIDO)NICOTINAMIDES) 审中-公开
标题翻译：制备苯基-6-（1-（苯基）尿嘧啶）尼古丁的方法）
公开(公告)号：WO2010093890A2
公开(公告)日：2010-08-19
申请号：PCT/US2010/024054
申请日：2010-02-12
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ROEPER, Stefanie , LOOKER, Adam, R. , MARTINOT, Theodore, A. , NEUBERT-LANGILLE, Bobbianna , RYAN, Michael, P. , SNOONIAN, John, R.
发明人： ROEPER, Stefanie , LOOKER, Adam, R. , MARTINOT, Theodore, A. , NEUBERT-LANGILLE, Bobbianna , RYAN, Michael, P. , SNOONIAN, John, R.
IPC分类号： C07D213/80 , C07D213/803 , A61K31/4418 , A61P37/06 , A61P29/00
CPC分类号： C07D213/80 , C07D213/803
摘要： The present invention relates to processes for the preparation of compounds useful as inhibitors of p38 kinase. The processes of the present invention are amenable for large scale preparation and produce stable phenyl-6-(l-(phenyl)ureido)nicotinamides in high purity and yields.
摘要翻译：本发明涉及制备可用作p38激酶抑制剂的化合物的方法。本发明的方法适用于大规模制备，并以高纯度产生稳定的苯基-6-（1-（苯基）脲基）烟酰胺。

7. 发明申请

WO2010093889A2 SOLID FORMS OF 2-(2, 4-DIFLUOROPHENYL)-6-(1-(2,6-DIFLUOROPHENYL)UREIDO)NICOTINAMIDE 审中-公开
标题翻译： 2-（2,4-二氟苯基）-6-（1-（2,6-二氟苯基）脲基）烟酰胺的固体形式
公开(公告)号：WO2010093889A2
公开(公告)日：2010-08-19
申请号：PCT/US2010/024053
申请日：2010-02-12
申请人： VERTEX PHARMACEUTICALS INCORPORATED , HURREY, Michael , ALARGOV, Dimitar , JOHNSTON, Steven, C. , ROEPER, Stefanie , SNOONIAN, John, R. , COWANS, Brett, A. , VLAHOVA, Petinka , EBERLIN, Alexander , EDDLESTON, Mark , FRAMPTON, Chris
发明人： HURREY, Michael , ALARGOV, Dimitar , JOHNSTON, Steven, C. , ROEPER, Stefanie , SNOONIAN, John, R. , COWANS, Brett, A. , VLAHOVA, Petinka , EBERLIN, Alexander , EDDLESTON, Mark , FRAMPTON, Chris
IPC分类号： C07D213/82 , A61K31/4418
CPC分类号： C07D213/82
摘要： This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(l- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.
摘要翻译：本发明涉及2-（2,4-二氟苯基）-6-（1-（2,6-二氟苯基）脲基）烟酰胺的固体形式及其药物组合物，及其方法和用途

8. 发明申请

WO2011149878A1 AN AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE 审中-公开
标题翻译： C-MET蛋白激酶的氨基吡唑三唑并噻唑类抑制剂
公开(公告)号：WO2011149878A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/037659
申请日：2011-05-24
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LAUFFER, David, J. , LI, Pan , ROEPER, Stefanie , IBRAHIM, Shereen , KULDIPKUMAR, Anuj, K. , SHI, Yi , MILLER, David, B., Jr.
发明人： LAUFFER, David, J. , LI, Pan , ROEPER, Stefanie , IBRAHIM, Shereen , KULDIPKUMAR, Anuj, K. , SHI, Yi , MILLER, David, B., Jr.
IPC分类号： C07D513/04 , A61K31/4709 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention relates to anhydrous and hydrated forms of Compound 1, which are useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders.
摘要翻译：本发明涉及化合物1的无水和水合形式，其可用于抑制c-Met蛋白激酶。本发明还提供包含式I化合物的药学上可接受的组合物和使用该组合物治疗增殖性疾病的方法。

9. 发明申请

WO2011050215A1 PROCESS FOR PREPARING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
标题翻译： CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR制备调节剂的方法
公开(公告)号：WO2011050215A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053628
申请日：2010-10-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , AMBHAIKAR, Narendra, Bhalchandra , HUGHES, Robert , HURLEY, Dennis, James , LEE, Elaine, Chungmin , LITTLER, Benjamin , NUMA, Mehdi , ROEPER, Stefanie , SHETH, Urvi
发明人： AMBHAIKAR, Narendra, Bhalchandra , HUGHES, Robert , HURLEY, Dennis, James , LEE, Elaine, Chungmin , LITTLER, Benjamin , NUMA, Mehdi , ROEPER, Stefanie , SHETH, Urvi
IPC分类号： C07D215/56 , C07D487/08
CPC分类号： C07D487/08 , C07D215/56
摘要： The present invention relates to processes for preparing 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, including Compound 1 Form A, Compound 1 Form A- HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.
摘要翻译：本发明涉及制备固体形式的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，包括化合物1形式A，化合物1形式A- HCl，化合物1形式B和化合物1形式B-HCl，这些形式的任何组合，其药物组合物，以及治疗。

10. 发明申请

WO2010093890A3 PROCESSES FOR PRODUCING PHENYL-6-(1-(PHENYL)UREIDO)NICOTINAMIDES 审中-公开
标题翻译：生产苯基-6-（1-（苯基）尿嘧啶）的方法NICOTINAMIDES
公开(公告)号：WO2010093890A3
公开(公告)日：2010-12-16
申请号：PCT/US2010024054
申请日：2010-02-12
申请人： VERTEX PHARMA , ROEPER STEFANIE , LOOKER ADAM R , MARTINOT THEODORE A , NEUBERT-LANGILLE BOBBIANNA , RYAN MICHAEL P , SNOONIAN JOHN R
发明人： ROEPER STEFANIE , LOOKER ADAM R , MARTINOT THEODORE A , NEUBERT-LANGILLE BOBBIANNA , RYAN MICHAEL P , SNOONIAN JOHN R
IPC分类号： C07D213/80 , A61K31/4418 , A61P29/00 , A61P37/06 , C07D213/803
CPC分类号： C07D213/80 , C07D213/803
摘要： The present invention relates to processes for the preparation of compounds useful as inhibitors of p38 kinase. The processes of the present invention are amenable for large scale preparation and produce stable phenyl-6-(1-(phenyl)ureido)nicotinamides in high purity and yields.
摘要翻译：本发明涉及制备可用作p38激酶抑制剂的化合物的方法。本发明的方法适用于大规模制备，并以高纯度产生稳定的苯基-6-（1-（苯基）脲基）烟酰胺。

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