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1. 发明申请

WO2011133751A3 PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS 审中-公开
标题翻译：生产环磷酰胺氧化物 - 吲哚化合物的方法
公开(公告)号：WO2011133751A3
公开(公告)日：2012-01-12
申请号：PCT/US2011033396
申请日：2011-04-21
申请人： VERTEX PHARMA , TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , LEE ELAINE CHUNGMIN , BELMONT DANIEL T
发明人： TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , LEE ELAINE CHUNGMIN , BELMONT DANIEL T
IPC分类号： C07D209/12 , C07D317/60 , C07D405/12
CPC分类号： C07D317/46 , C07C209/74 , C07C225/06 , C07D209/12 , C07D317/60 , C07D405/12
摘要： The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2- (1 -hydroxy-2-methylpropan-2-yl)- 1H-indol-5 -yl)cyclopropanecarboxamide (Compound 1 ), useful for treating CFTR mediated diseases such as cystic fibrosis.
摘要翻译：本发明的特征在于制备化合物如（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟基丙基） -6-氟-2-（1-羟基-2-甲基丙-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1），可用于治疗CFTR介导的疾病如囊性纤维化。

2. 发明申请

WO2011133751A9 PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS 审中-公开
标题翻译：生产环烷基甲酰胺基吲哚化合物的方法
公开(公告)号：WO2011133751A9
公开(公告)日：2012-02-16
申请号：PCT/US2011033396
申请日：2011-04-21
申请人： VERTEX PHARMA , TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , LEE ELAINE CHUNGMIN , BELMONT DANIEL T
发明人： TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , LEE ELAINE CHUNGMIN , BELMONT DANIEL T
IPC分类号： C07D209/12 , C07D317/60 , C07D405/12
CPC分类号： C07D317/46 , C07C209/74 , C07C225/06 , C07D209/12 , C07D317/60 , C07D405/12
摘要： The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2- (1 -hydroxy-2-methylpropan-2-yl)- 1H-indol-5 -yl)cyclopropanecarboxamide (Compound 1 ), useful for treating CFTR mediated diseases such as cystic fibrosis.
摘要翻译：（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟基丙基） -6-氟-2-（1-羟基-2-甲基丙烷-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1），用于治疗CFTR介导的疾病如囊性纤维化。

3. 发明专利

SG184987A1 PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS 未知
公开(公告)号：SG184987A1
公开(公告)日：2012-11-29
申请号：SG2012078374
申请日：2011-04-21
申请人： VERTEX PHARMA , LEE ELAINE CHUNGMIN
发明人： TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , LEE ELAINE CHUNGMIN , BELMONT DANIEL T
摘要： The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2- (1 -hydroxy-2-methylpropan-2-yl)- 1H-indol-5 -yl)cyclopropanecarboxamide (Compound 1 ), useful for treating CFTR mediated diseases such as cystic fibrosis.

4. 发明专利

ES2845449T3 Dispersión sólida de forma amorfa de (R)-1(2,2-difluorobenzo[d][1,3]dioxol-5-il)-N-(1-(2,3-dihidroxipropil)-6-fluoro-2(1-hidroxi-2-metilpropan-2-il)-1h-indol-5il)-ciclopropanocarboxamida 未知
公开(公告)号：ES2845449T3
公开(公告)日：2021-07-26
申请号：ES14172991
申请日：2011-03-25
申请人： VERTEX PHARMA
发明人： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC分类号： A61K9/10 , A61K31/404 , A61P11/00 , C07D405/12
摘要： Una dispersión sólida que comprende (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-N-(1-(2,3-dihidroxipropil)-6-fluoro- 2-(1-hidroxi-2-metilpropan-2-il)-1H-indol-5-il)ciclopropanocarboxamida amorfa sustancialmente sólida y un polímero, en donde la (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-N-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2- il)-1H-indol-5-il)ciclopropanocarboxamida amorfa sustancialmente sólida comprende menos de aproximadamente un 5% de (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-N-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)- 1H-indol-5-il)ciclopropanocarboxamida cristalina, en donde el polímero es hidroxipropilmetilcelulosa (HPMC) o acetato succinato de hidroxipropilmetilcelulosa (HPMCAS).

5. 发明专利

AR115261A2 UN MÉTODO PARA PREPARAR COMPUESTOS DE CICLOALQUILCARBOXAMIDOINDOL 未知
公开(公告)号：AR115261A2
公开(公告)日：2020-12-16
申请号：ARP190100511
申请日：2019-02-28
申请人： VERTEX PHARMA
发明人： BELMONT DANIEL T , LEE ELAINE CHUNGMIN , SIESEL DAVID A , JUNG YOUNG CHUN , HUGHES ROBERT M , ROSE PETER JAMISON , LITTLER BENJAMIN J , HARRISON CRISTIAN , TANOURY GERALD J
IPC分类号： C07D405/12 , C07D317/60
摘要： Reivindicación 1: Un método para preparar un compuesto de fórmula (1), en donde, independientemente, cada vez que aparecen: el anillo A es un anillo fusionado de cicloalquilo, heterocicloalquilo, arilo o heteroarilo; R¹ y R² se seleccionan independientemente entre -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; R³ es un alifático C₁₋₆ opcionalmente sustituido con OH, OP, -O-alifático C₁₋₆, arilo, heteroarilo, -O-arilo, u -O-heteroarilo; P es un grupo protector; m es un entero de 0 a 3 inclusive; n es un entero de 1 a 4 inclusive; y o es un entero de 1 a 3 inclusive; dicho método caracterizado porque comprende los pasos de: a) hacer reaccionar un compuesto de fórmula (2) en donde, independientemente, cada vez que aparecen: R² es -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; y o es un entero de 0 a 3; con un reactivo de halogenación en un primer solvente orgánico para formar un compuesto de fórmula (3) en donde, independientemente, cada vez que aparecen: R² es -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; o es un entero de 0 a 3; y Hal es un haluro; b) hacer reaccionar el compuesto de fórmula (3) en un segundo solvente orgánico con un compuesto de fórmula (4) en donde: P es un grupo protector; seguido de reducción y tratamiento con ácido para formar un compuesto de fórmula (5) en donde: R² es -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; o es un entero de 0 a 3; Hal es un haluro; P es un grupo protector; y A ²⁰; es un anión; c) neutralizar un compuesto de fórmula (5) en presencia de una base para formar un compuesto de fórmula (6) en donde: R² es -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; o es un entero de 0 a 3; Hal es un haluro; y P es un grupo protector; d) hacer reaccionar un compuesto de fórmula (6) en un tercer solvente orgánico con un compuesto de fórmula (7) en donde, independientemente, cada vez que aparecen: R³ es un alifático C₁₋₆ opcionalmente sustituido con OH, OP, -O-alifático C₁₋₆, arilo, heteroarilo, -O-arilo, u -O-heteroarilo; en presencia de un catalizador para formar un compuesto de fórmula (8) en donde, independientemente, cada vez que aparecen: R² es -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; R³ es alifático C₁₋₆ opcionalmente sustituido con OH, OP, -O-alifático C₁₋₆, arilo, heteroarilo, O-arilo, u -O-heteroarilo; P es un grupo protector; y o es un entero de 0 a 3; e) hacer reaccionar el compuesto de fórmula (8) en un cuarto solvente orgánico con un compuesto de fórmula (9) en donde, independientemente, cada vez que aparecen: el anillo A es un anillo fusionado de cicloalquilo, heterocicloalquilo, arilo o heteroarilo; Hal es un haluro; R¹ se selecciona independientemente entre -RJ, -ORJ, -N(RJ)₂, -NO₂, halógeno, -CN, -haloalquilo C₁₋₄, -haloalcoxi C₁₋₄, -C(O)N(RJ)₂, -NRJC(O)RJ, -SORJ, -SO₂RJ, -SO₂N(RJ)₂, -NRJSO₂RJ, -CORJ, -CO₂RJ, -NRJSO₂N(RJ)₂, -COCORJ; RJ es hidrógeno o alifático C₁₋₆; m es un entero de 0 a 3 inclusive; y n es un entero de 1 a 4 inclusive; para formar el compuesto de fórmula (1).

6. 发明专利

AU2018226453B2 Pharmaceutical Compositions and Administrations Thereof 未知
公开(公告)号：AU2018226453B2
公开(公告)日：2019-07-11
申请号：AU2018226453
申请日：2018-09-06
申请人： VERTEX PHARMA
发明人： ALARGOVA ROSSITZA GUEORGUIEVA , ALCACIO TIM EDWARD , JOHNSTON STEVEN C , VAN GOOR FREDRICK F , KESHAVARZ-SHOKRI ALI , LEE ELAINE CHUNGMIN , MEDEK ALES , SULLIVAN MARK JEFFREY , ZAMAN NOREEN TASNEEM , ZHANG BEILI , ZHANG YUEGANG , ZLOKARNIK GREGOR , AREKAR SNEHA G , KADIYALA IRINA NIKOLAEVNA , MUDUNURI PRAVEEN , KRAWIEC MARIUSZ
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
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. o o WR W4 N r O H WRw2 Formula I T \ N Formula II R 0 RN, R8 Ry Formula III

7. 发明专利

AU2018226453A1 Pharmaceutical Compositions and Administrations Thereof 未知
公开(公告)号：AU2018226453A1
公开(公告)日：2018-09-27
申请号：AU2018226453
申请日：2018-09-06
申请人： VERTEX PHARMA
发明人： ALARGOVA ROSSITZA GUEORGUIEVA , ALCACIO TIM EDWARD , JOHNSTON STEVEN C , VAN GOOR FREDRICK F , KESHAVARZ-SHOKRI ALI , LEE ELAINE CHUNGMIN , MEDEK ALES , SULLIVAN MARK JEFFREY , ZAMAN NOREEN TASNEEM , ZHANG BEILI , ZHANG YUEGANG , ZLOKARNIK GREGOR , AREKAR SNEHA G , KADIYALA IRINA NIKOLAEVNA , MUDUNURI PRAVEEN , KRAWIEC MARIUSZ
IPC分类号： A61K31/4704 , A61K31/404 , A61K31/443
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. o o WR W4 N r O H WRw2 Formula I T \ N Formula II R 0 RN, R8 Ry Formula III

8. 发明专利

AU2016202569A1 Process of producing cycloalkylcarboxamido-indole compounds 未知
公开(公告)号：AU2016202569A1
公开(公告)日：2016-05-19
申请号：AU2016202569
申请日：2016-04-22
申请人： VERTEX PHARMA
发明人： LEE ELAINE CHUNGMIN , TANOURY GERALD J , HARRISON CRISTIAN , LITTLER BENJAMIN JOSEPH , ROSE PETER JAMISON , HUGHES ROBERT MICHAEL , JUNG YOUNG CHUN , SIESEL DAVID ANDREW , BELMONT DANIEL T
IPC分类号： C07D209/12 , C07D317/60 , C07D405/12
摘要： PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE Abstract The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2 (1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound I), useful for treating CFTR mediated diseases such as cystic fibrosis.

9. 发明专利

AU2011242454A1 Pharmaceutical compositions and administrations thereof 未知
公开(公告)号：AU2011242454A1
公开(公告)日：2012-11-08
申请号：AU2011242454
申请日：2011-04-22
申请人： VERTEX PHARMA
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
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.

10. 发明专利

CA2796602A1 PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF 未知
公开(公告)号：CA2796602A1
公开(公告)日：2011-10-27
申请号：CA2796602
申请日：2011-04-22
申请人： VERTEX PHARMA
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
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.

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