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1. 发明申请

WO2019084285A1 FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR 审中-公开
公开(公告)号：WO2019084285A1
公开(公告)日：2019-05-02
申请号：PCT/US2018/057542
申请日：2018-10-25
申请人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
发明人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
IPC分类号： A61K47/36 , A61K47/38 , A61K31/00 , C07D471/22
摘要： The present application in some embodiments provides a pharmaceutical composition comprising Compound (1), and a compounding agent. Further provided herein are methods of making and methods of using the pharmaceutical compositions, for example, in the treatment of cancer.

2. 发明申请

WO2019005796A1 PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF 审中-公开
公开(公告)号：WO2019005796A1
公开(公告)日：2019-01-03
申请号：PCT/US2018/039502
申请日：2018-06-26
申请人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
发明人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
IPC分类号： C07D471/22 , A61K31/519 , A61P35/00
摘要： In some embodiments, provided herein are processes for preparing a compound of Formula (C) or a salt thereof, as disclosed herein.

3. 发明申请

WO2018081417A2 PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF 审中-公开
标题翻译：制备吡唑并[1,5-a]嘧啶及其盐的方法
公开(公告)号：WO2018081417A2
公开(公告)日：2018-05-03
申请号：PCT/US2017/058518
申请日：2017-10-26
申请人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
发明人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
IPC分类号： A61K31/5025 , A61K31/519 , C12Q1/68 , A61P35/00 , G01N33/574
摘要： In some embodiments, provided herein are processes for preparing a compound of Formula C or a salt thereof, as disclosed herein. In some embodiments, provided herein is a compound of Formula I or a pharmaceutically acceptable salt, solvate or hydrate thereof. In some embodiments, provided herein is a solid form of the compound, such as a crystalline form of the compound crystalline Form I.
摘要翻译：在一些实施方案中，本文提供了制备如本文所公开的式C化合物或其盐的方法。在一些实施方案中，本文提供了式I的化合物或其药学上可接受的盐，溶剂合物或水合物。在一些实施方案中，本文提供化合物的固体形式，例如化合物晶型I的晶体形式。

4. 发明申请

WO2018081417A3 PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF 审中-公开
公开(公告)号：WO2018081417A3
公开(公告)日：2018-05-03
申请号：PCT/US2017/058518
申请日：2017-10-26
申请人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
发明人： ZHAO, Qian , SPENCER, Stacey , JIANG, Yutong , HAAS, Julia , EARY, Charles Todd
IPC分类号： C07D471/22 , A61K31/519 , A61P35/00
摘要： In some embodiments, provided herein are processes for preparing a compound of Formula C or a salt thereof, as disclosed herein. In some embodiments, provided herein is a compound of Formula I or a pharmaceutically acceptable salt, solvate or hydrate thereof. In some embodiments, provided herein is a solid form of the compound, such as a crystalline form of the compound crystalline Form I.

5. 发明申请

WO2017201241A1 PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDIN-3-Y L)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE 审中-公开
标题翻译：（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-3-基）-3-羟基吡咯烷 - -1-甲酰胺
公开(公告)号：WO2017201241A1
公开(公告)日：2017-11-23
申请号：PCT/US2017/033257
申请日：2017-05-18
申请人： REYNOLDS, Mark , EARY, Charles Todd , SPENCER, Stacey , JUENGST, Derrick , HACHE, Bruno , JIANG, Yutong , HAAS, Julia , ANDREWS, Steven W.
发明人： REYNOLDS, Mark , EARY, Charles Todd , SPENCER, Stacey , JUENGST, Derrick , HACHE, Bruno , JIANG, Yutong , HAAS, Julia , ANDREWS, Steven W.
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
摘要： Process for preparing (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)pyrazolo[l,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5- difluorophenyl)pyrrolidin-l-yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3- yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3- ol (formula 14). Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl) pyrrolidin-l-yl)-3-nitropyrazolo[l,5-a]pyrimidine (formula 11) to (R) -5-(2-(2,5-difluorophenyl)pyrrolidin-l-yl)pyrazolo[l,5-a]pyrimidin-3- amine (formula 12). Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R) -2-hydroxysuccinate (formula 10) by treating (R)-N-((R)-l-(2,5- difluorophenyl)-3-(l,3-dioxan-2-yl)propyl)-2-methylpropane-2- sulfinamide (formula 19) with an acid and a reducing agent. (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-l-yl)-pyrazolo[l,5- a]pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.
摘要翻译：制备（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-4 （5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）-3,3a（三唑-3-基）-3-羟基吡咯烷-1-甲酰胺（式I）或其盐 - 二氢吡唑并[1,5-a]嘧啶-3-基）氨基甲酸叔丁酯或类似衍生物（式13）与（S） - 吡咯烷-3-醇（式14）（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）-3,3a-二氢吡唑并[1,5-a]嘧啶-3-基）氨基甲酸酯（式13 ）或（R）-5-（2-（2,5-二氟苯基）吡咯烷-1-基）-3-硝基吡唑并[1,5-a]嘧啶（式11）还原成（R） -5-（2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-3-胺（式12）。通过处理（R）-N - （（R）-1-（2,5-二氟苯基）吡咯烷（R）-2-羟基琥珀酸盐（式10） -3-（1,3-二恶烷-2-基）丙基）-2-甲基丙烷-2-亚磺酰胺（式19）与酸和还原剂反应。（S）-N-（5 - （（R）-2-（2,5-二氟苯基） - 吡咯烷-1-基） - 吡唑并[1,5-a]嘧啶-3-基）-3-羟基吡咯烷-3-甲酸 1-甲酰胺是酪氨酸激酶（TRK）抑制剂，用于处理例如，癌症

6. 发明申请

WO2019075092A1 PROCESS FOR THE PREPARATION OF 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE 审中-公开
公开(公告)号：WO2019075092A1
公开(公告)日：2019-04-18
申请号：PCT/US2018/055255
申请日：2018-10-10
申请人： EARY, Charles Todd , SPENCER, Stacey , CRANE, Zack , CHANDO, Katelyn , ASSELIN, Sylvie , LIU, Weidong , WELCH, Mike , COOK, Adam , KOLAKOWSKI, Gabrielle R. , METCALF, Andrew T. , MORENO, David A. , TANG, Tony P.
发明人： EARY, Charles Todd , SPENCER, Stacey , CRANE, Zack , CHANDO, Katelyn , ASSELIN, Sylvie , LIU, Weidong , WELCH, Mike , COOK, Adam , KOLAKOWSKI, Gabrielle R. , METCALF, Andrew T. , MORENO, David A. , TANG, Tony P.
IPC分类号： C07D471/04 , C07D519/00
摘要： In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

7. 发明申请

WO2019075114A4 FORMULATIONS COMPRISING 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZAB ICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE 审中-公开
公开(公告)号：WO2019075114A4
公开(公告)日：2019-04-18
申请号：PCT/US2018/055285
申请日：2018-10-10
申请人： REYNOLDS, Mark , EARY, Charles Todd
发明人： REYNOLDS, Mark , EARY, Charles Todd
IPC分类号： A61K47/12 , A61K9/08 , A61K47/38 , A61K9/16 , A61K9/20 , A61K31/4985
摘要： 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.

8. 发明申请

WO2019075114A1 FORMULATIONS COMPRISING 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZAB ICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE 审中-公开
公开(公告)号：WO2019075114A1
公开(公告)日：2019-04-18
申请号：PCT/US2018/055285
申请日：2018-10-10
申请人： REYNOLDS, Mark , EARY, Charles Todd
发明人： REYNOLDS, Mark , EARY, Charles Todd
IPC分类号： A61K47/12 , A61K9/08 , A61K47/38 , A61K9/16 , A61K9/20 , A61K31/4985
摘要： 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.

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