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1. 发明专利

AR123427A1 PROCESOS E INTERMEDIOS PARA LA PREPARACIÓN DE (S)-5-AMINO-3-(4-((5-FLUORO-2-METOXIBENZAMIDO)METIL)FENIL)-1-(1,1,1-TRIFLUOROPROPAN-2-IL)-1H-PIRAZOL-4-CARBOXAMIDA 未知
公开(公告)号：AR123427A1
公开(公告)日：2022-11-30
申请号：ARP210102462
申请日：2021-09-02
申请人： LOXO ONCOLOGY INC
发明人： ARGUELLES DELGADO ALONSO JOSE , EARY CHARLES TODD , FENNELL JARED WADE , MAGNUS NICHOLAS ANDREW , ROTHHAAR ROGER RYAN , SPENCER STACEY RENEE , VAID RADHE KRISHAN , FRANK SCOTT ALAN , MFADDIN ELIZABETH ANN
IPC分类号： C07D231/38 , C07C235/60 , C07C255/44 , C07F5/02 , C07F5/04
摘要： La presente invención proporciona procesos e intermedios clave para la síntesis de (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida: de fórmula (I). Reivindicación 1: Un proceso para la preparación de (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) que comprende las etapas de: viii) acoplar el compuesto de fórmula (III), en donde PG¹ es -CH₃, -CH₂CH₃, -C(CH₃)₃, -CH₂CH=CH₂, metoximetilo, tetrahidropirano, bencilo, trimetilsililo, terc-butil dimetilsililo, di-terc-butilisobutilsililo, di-terc-butil[piren-1-ilmetoxi]sililo, terc-butil difenilsililo, acetilo o benzoilo; y [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina (8) o una sal de esta para dar N-[[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metiletil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida (10) o una sal de esta; ix) sintetizar (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) a partir de N-[[4-[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metil-etil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida (10) o una sal de esta; y x) opcionalmente, cristalizar (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) para proporcionar un (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) en forma cristalina. Reivindicación 9: Un proceso para la preparación de (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) que comprende las etapas de: i) convertir ácido 5-fluoro-2-metoxi-benzoico (1) o una sal de este en cloruro de 5-fluoro-2-metoxi-benzoilo (2); ii) acoplar cloruro de 5-fluoro-2-metoxi-benzoilo (2) con ácido 4-(aminometil)benzoico para dar ácido 4-[[(5-fluoro-2-metoxi-benzoil)amino]metil]benzoico (3) o una sal de este; iii) convertir ácido 4-[[(5-fluoro-2-metoxi-benzoil)amino]metil]benzoico (3) o una sal de este en cloruro de 4-[[(5-fluoro-2-metoxi-benzoil)amino]metil]benzoilo (4); iv) hacer reaccionar cloruro de 4-[[(5-fluoro-2-metoxi-benzoil)amino]metil]benzoilo (4) con malononitrilo para dar N-[[4-(2,2-diciano-1-hidroxi-vinil)fenil]metil]-5-fluoro-2-metoxi-benzamida (II); v) convertir N-[(1S)-2,2,2-trifluoro-1-metil-etil]benzohidrazida (6) o una sal de esta en clorhidrato de [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina (7); vi) convertir clorhidrato de [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina (7) en [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina (8); vii) convertir N-[[4-(2,2-diciano-1-hidroxi-vinil)fenil]metil]-5-fluoro-2-metoxibenzamida (II) en un compuesto de fórmula (III), en donde PG¹ es -CH₃, -CH₂CH₃, -C(CH₃)₃, -CH₂CH=CH₂, metoximetilo, tetrahidropirano, bencilo, trimetilsililo, terc-butil dimetilsililo, di-terc-butilisobutilsililo, di-terc-butil[piren-1-ilmetoxi]sililo, terc-butil difenilsililo, acetilo o benzoilo; viii) acoplar el compuesto de fórmula III, y [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina (8) o una sal de esta para dar N-[[4-[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metil-etil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida (10) o una sal de esta; ix) sintetizar (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) a partir de N-[[4-[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metil-etil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida (10) o una sal de esta; y x) opcionalmente, cristalizar (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) para proporcionar un (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamida (I) en forma cristalina.

2. 发明专利

CA3108065A1 SPRAY-DRIED DISPERSIONS AND FORMULATIONS OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)-1-(1,1,1-TRIFLUORO PROPAN-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE 未知
公开(公告)号：CA3108065A1
公开(公告)日：2020-02-06
申请号：CA3108065
申请日：2019-07-29
申请人： LOXO ONCOLOGY INC
发明人： BRANDHUBER BARBARA J , BRENT LAUREN T , EARY CHARLES TODD , KENNA ANDREW , KHAN FIRAS , RENSHAW VIVIAN F H , SPENCER STACEY RENEE
IPC分类号： A61K9/16 , A61K9/14 , A61K9/20 , A61K31/00 , A61P35/00
摘要： A spray-dried dispersions and pharmaceutical composition of (S)-5-amino-3-(4-((5-fluoro-2- methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4- carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use of the spray-dried dispersion and pharmaceutical composition in the treatment of cancer and autoimmune and inflammatory diseases are disclosed. Also provided are crystalline forms of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan- 2-yl)-1H-pyrazole-4-carboxamide also useful in the treatment of cancer and autoimmune and inflammatory diseases.

3. 发明专利

AU2019314302A1 Spray-dried dispersions and formulations of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1H-pyrazole-4-carboxamide 未知
公开(公告)号：AU2019314302A1
公开(公告)日：2021-01-28
申请号：AU2019314302
申请日：2019-07-29
申请人： LOXO ONCOLOGY INC
发明人： BRANDHUBER BARBARA J , BRENT LAUREN T , EARY CHARLES TODD , KENNA ANDREW , KHAN FIRAS , RENSHAW VIVIAN F H , SPENCER STACEY RENEE
IPC分类号： A61K9/16 , A61K9/14 , A61K9/20 , A61K31/00 , A61P35/00
摘要： A spray-dried dispersions and pharmaceutical composition of (

4. 发明专利

AU2022275440A1 Spray-dried dispersions, formulations, and polymorphs of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1- (1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide 未知
公开(公告)号：AU2022275440A1
公开(公告)日：2023-01-05
申请号：AU2022275440
申请日：2022-11-23
申请人： LOXO ONCOLOGY INC
发明人： BRANDHUBER BARBARA J , BRENT LAUREN T , EARY CHARLES TODD , KENNA ANDREW , KHAN FIRAS , RENSHAW VIVIAN F H , SPENCER STACEY RENEE
IPC分类号： A61K9/16 , A61K9/14 , A61K9/20 , A61K31/00 , A61P35/00
摘要： A spray-dried dispersions and pharmaceutical composition of (S)-5-amino-3-(4-((5-fluoro-2 methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4 carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use 5 of the spray-dried dispersion and pharmaceutical composition in the treatment of cancer and autoimmune and inflammatory diseases are disclosed. Also provided are crystalline forms of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan 2-yl)-1H-pyrazole-4-carboxamide also useful in the treatment of cancer and autoimmune and inflammatory diseases.

5. 发明专利

AU2022259781A1 Spray-dried dispersions and formulations of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1H-pyrazole-4-carboxamide 未知
公开(公告)号：AU2022259781A1
公开(公告)日：2022-12-01
申请号：AU2022259781
申请日：2022-10-26
申请人： LOXO ONCOLOGY INC
发明人： BRANDHUBER BARBARA J , BRENT LAUREN T , EARY CHARLES TODD , KENNA ANDREW , KAHN FIRAS , RENSHAW VIVIAN F H , SPENCER STACEY RENEE , GUISOT NICOLAS
IPC分类号： A61K9/16 , A61K9/14 , A61K9/20 , A61K31/00 , A61P35/00
摘要： A spray-dried dispersions and pharmaceutical composition of (S)-5-amino-3-(4-((5-fluoro-2 methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4 carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use 5 of the spray-dried dispersion and pharmaceutical composition in the treatment of cancer and autoimmune and inflammatory diseases are disclosed. Also provided are crystalline forms of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan 2-yl)-1H-pyrazole-4-carboxamide also useful in the treatment of cancer and autoimmune and inflammatory diseases.

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