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1.发明专利
公开(公告)号：JP2013253111A
公开(公告)日：2013-12-19
申请号：JP2013194966
申请日：2013-09-20
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , KRAWIEC MARIUSZ
IPC: C07D405/12 , A61K31/443 , A61K45/00 , A61P3/00 , C12Q1/02
Abstract: PROBLEM TO BE SOLVED: To provide a solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid.SOLUTION: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, pharmaceutical compositions thereof, and methods of treatment therewith.
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2.发明申请FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCKLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID 审中-公开3-（6-（1-（2,2-二氟苯并[D] [1,3]二氧戊环-5-基）环丙基碳酰氨基）-3-甲基吡啶-2-基）苯甲酸的制剂
公开(公告)号：WO2009076141A3
公开(公告)日：2009-11-12
申请号：PCT/US2008085457
申请日：2008-12-04
Applicant: VERTEX PHARMA , KESHAVARZ-SHOKRI ALI , YOUNG CHRISTOPHER
Inventor： KESHAVARZ-SHOKRI ALI , YOUNG CHRISTOPHER
CPC classification number: A61K9/10 , A61K9/0095 , A61K31/443
Abstract: The present invention relates to formulations of 3-(6-(l-(2,2- difluorobenzo[d] [ 1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, pharmaceutical packs or kits thereof, and methods of treatment therewith.
Abstract translation: 本发明涉及3-（6-（1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基）苯甲酸的制剂，药物 包装或药盒，以及用其治疗的方法。
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3.发明申请SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID 审中-公开3-（6-（1-（2,2-二氟苯并[D] [1,3]二氧杂环戊烯-5-YL）环丙烷氧羰基）-3-甲基吡啶-2-基）苯甲酸的固体形式
公开(公告)号：WO2011127290A2
公开(公告)日：2011-10-13
申请号：PCT/US2011031588
申请日：2011-04-07
Applicant: VERTEX PHARMA , KESHAVARZ-SHOKRI ALI , ZHANG BEILI , KRAWIEC MARIUSZ
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , KRAWIEC MARIUSZ
IPC: C07D405/12
CPC classification number: A61K31/443 , A61K31/47 , A61K45/06 , C07D213/75 , C07D405/12 , C07D405/14 , C07D407/12 , Y10T428/2982
Abstract: The present invention relates to a substantially a solid form of 3-(6-(l-(2,2- difluorobenzo[d][l,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.
Abstract translation: 本发明涉及基本上固体形式的3-（6-（1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基） 苯甲酸（化合物1，溶剂合物形式A和化合物1，HCl盐A型），制备这种形式的方法，其药物组合物及其处理方法。
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4.发明申请FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID 审中-公开3-（6-（1-（2,2-二氟苯并[D] [1,3]二氧杂环戊烯-5-基）环丙基）羰基氧基）-3-甲基吡啶-2-基）苯甲酸的制备
公开(公告)号：WO2009076141A8
公开(公告)日：2010-07-15
申请号：PCT/US2008085457
申请日：2008-12-04
Applicant: VERTEX PHARMA , KESHAVARZ-SHOKRI ALI , YOUNG CHRISTOPHER
Inventor： KESHAVARZ-SHOKRI ALI , YOUNG CHRISTOPHER
CPC classification number: A61K9/10 , A61K9/0095 , A61K31/443
Abstract: The present invention relates to formulations of 3-(6-(l-(2,2- difluorobenzo[d] [ 1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, pharmaceutical packs or kits thereof, and methods of treatment therewith.
Abstract translation: 本发明涉及3-（6-（1-（2,2-二氟苯并[d] [1,3]二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基）苯甲酸，药物 包装或试剂盒，以及其处理方法。
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公开(公告)号：EP3250562A4
公开(公告)日：2018-07-11
申请号：EP16744240
申请日：2016-01-29
Applicant: BIOMED VALLEY DISCOVERIES INC , VERTEX PHARMA
Inventor： DECRESCENZO GARY , WELSCH DEAN , VLAHOVA PETINKA I , BOERRIGTER STEPHAN X M , ARONOV ALEXANDER , KESHAVARZ-SHOKRI ALI , SCANGAS ALEXANDER N , STAVROPOULOS KATHY , LITTLER BENJAMIN , KADIYALA IRINA NIKOLAEVNA , ALARGOVA ROSSITZA GUEORGUIEVA
IPC: C07D401/04 , A61K31/4439 , A61K45/06 , A61P35/00
CPC classification number: C07D401/04 , A61K31/4439 , A61K45/06 , A61P35/00
Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
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Patent Agency Ranking
公开(公告)号：MX379264B
公开(公告)日：2025-03-11
申请号：MX2016007258
申请日：2016-06-03
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , LITTLER BENJAMIN JOSEPH , ANDERSON COREY , BELMONT DANIEL T , GOLEC JULIAN MARIAN CHARLES , HADIDA-RUAH SARA SABINA , ALCACIO TIM EDWARD
IPC: C07F9/576 , A61K31/675 , A61P19/02 , C07F9/58
Abstract: La invención se refiere a compuestos profármacos de la fórmula I: (ver Fórmula) en donde R2, R3, R5, R7 y X son como se definen en el presente documento. La invención también proporciona composiciones farmacéuticamente aceptables que comprenden los compuestos de la invención y métodos para usar las composiciones en el tratamiento de diversos trastornos, incluyendo dolor. Los compuestos de la fórmula I poseen solubilidad y propiedades fisicoquímicas adecuadas.
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公开(公告)号：ES2951520T3
公开(公告)日：2023-10-23
申请号：ES20206423
申请日：2011-03-25
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: C07D405/12
Abstract: La presente invención se refiere a la síntesis y a los intermedios para la preparación 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 (Compuesto 1). (Traducción automática con Google Translate, sin valor legal)
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公开(公告)号：PL3835297T3
公开(公告)日：2023-09-11
申请号：PL20206423
申请日：2011-03-25
Applicant: VERTEX PHARMA
Inventor： KESHAVARZ-SHOKRI ALI , ZHANG BEILI , ALCACIO TIM EDWARD , LEE ELAINE CHUNGMIN , ZHANG YUEGANG , KRAWIEC MARIUSZ
IPC: C07D405/12
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公开(公告)号：NZ772411A
公开(公告)日：2022-05-27
申请号：NZ77241116
申请日：2016-01-29
Applicant: VERTEX PHARMA , BIOMED VALLEY DISCOVERIES INC
Inventor： DECRESCENZO GARY , WELSCH DEAN , VLAHOVA PETINKA I , BOERRIGTER STEPHAN X M , ARONOV ALEXANDER , KESHAVARZ-SHOKRI ALI , SCANGAS ALEXANDER N , STAVROPOULOS KATHY , LITTLER BENJAMIN , KADIYALA IRINA NIKOLAEVNA , ALARGOVA ROSSITZA GUEORGUIEVA
IPC: C07D401/04
Abstract: The present invention provides crystalline forms of a compound of formula (I). Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
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公开(公告)号：ES2900263T3
公开(公告)日：2022-03-16
申请号：ES17792230
申请日：2017-09-29
Applicant: VERTEX PHARMA
Inventor： ALCACIO TIMOTHY , BAEK MINSON , GROOTENHUIS PETER , HADIDA RUAH SARA , HUGHES ROBERT , KESHAVARZ-SHOKRI ALI , MCAULEY-AOKI RACHEL , MCCARTNEY JASON , MILLER MARK , VAN GOOR FREDRICK , ZHANG BEILI , ANDERSON COREY , CLEVELAND THOMAS , FRIEMAN BRYAN , KHATUYA HARIPADA , JOSHI PRAMOD , KRENITSKY PAUL , MELILLO VITO , PIERRE FABRICE , TERMIN ANDREAS , UY JOHNNY , ZHOU JINGLAN , ABELA ALEXANDER , BUSCH BRETT , PARASELLI PRASUNA , SIESEL DAVID
IPC: C07D401/14 , A61K31/4439 , A61P11/12 , C07D471/14 , C07D498/14
Abstract: Un compuesto de Fórmula I: **(Ver fórmula)** una sal farmacéuticamente aceptable del mismo, o un derivado deuterado de cualquiera de los anteriores, en donde: - uno de Y1 e Y2 es N y el otro es CH; - X se elige entre los grupos O, NH y N(C1-C4 alquilo); - R1 se elige entre grupos -(CR2)k-O-(CR2)m(CR)n(Anillo A)n+1, en donde cada Anillo A se elige independientemente entre grupos C3-C10 cicloalquilo opcionalmente sustituidos con uno o más sustituyentes elegidos cada uno independientemente entre grupos C1-C2 alquilo, grupos C1-C2 alquilo halogenados y halógenos, y en los que cada R se elige independientemente entre H, OH y grupos C1-C2 alquilo opcionalmente sustituidos con uno o más halógenos; - cada R2 se elige independientemente entre grupos C1-C2 alquilo, OH, grupos C1-C2 alcoxi, halógenos y ciano; - cada R3 se elige independientemente entre grupos C1-C2 alquilo opcionalmente sustituidos con uno o más grupos OH; - cada R4 se elige independientemente entre halógenos; - k es 0 o 1; - r es 0 o 1; - m es 0, 1, 2 o 3; - n es 0 o 1; - p es 0, 1, 2, 3, 4 o 5; y - q es 0, 1, 2, 3, 4, 5, 6, 7 u 8.
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