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公开(公告)号:BR112014000115A2
公开(公告)日:2016-10-04
申请号:BR112014000115
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: LOOKER ADAM , OLMO BEATRIZ DOMINGUEZ , KLINE BILLIE J , MAGDZIAK DEREK , TANOURY GERALD J , JURCÍK VÁCLAV , JUNG YOUNG CHUN
IPC: C07D471/04
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公开(公告)号:NZ619699A
公开(公告)日:2016-03-31
申请号:NZ61969912
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , JURČÍK VÁCLAV , DOMINGUEZ OLMO BEATRIZ
IPC: C07D471/04 , A61K31/437 , C07D239/42 , C07F5/02 , C07F5/04
Abstract: Disclosed herein is a process for preparing an azaindole compound of Formula I, wherein the substituents are as defined in the specification. The process comprises reacting intermediates in water, organic solvents, a base, and a transition metal catalyst, wherein the organic solvents are selected from the group consisting of acetonitrile, toluene, N,N-dimethylformamide, N,N-dimethylacetamide, acetone, methyl tert-butyl ether, methanol, propanol, isopropanol, butanol, and tert-butanol. In a particular embodiment, the process produces compounds of Formula Ia [(R)-2-(2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-ylamino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide] and Ib [2-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)-2-methy-N-(2,2,2-trifluoroethy)propanamideand (Ib)]. The compounds of Formula I are useful as inhibitors of Janus kinases (JAK).
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公开(公告)号:AU2012279046A1
公开(公告)日:2014-01-23
申请号:AU2012279046
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , JURCIK VACLAV , DOMINGUEZ OLMO BEATRIZ
IPC: C07D471/04
Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).
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公开(公告)号:ES2804528T3
公开(公告)日:2021-02-08
申请号:ES16190960
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , DOMINGUEZ OLMO BEATRIZ , JURCÍK VÁCLAV
IPC: C07D471/04
Abstract: Un proceso para preparar un compuesto de Fórmula 1: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en donde R1 es -H, -Cl o -F; que comprende las etapas de: iva) hacer reaccionar un compuesto de Fórmula 5 con bromo en un disolvente orgánico para generar un compuesto de Fórmula 6: **(Ver fórmula)** va) hacer reaccionar el compuesto de Fórmula 6 con cloruro de p-toluenosulfonilo para generar un compuesto de Fórmula 7: **(Ver fórmula)** vi) hacer reaccionar el compuesto de Fórmula 7 con borato de triisopropilo, en presencia de un disolvente orgánico y una base de litio fuerte para generar un compuesto de Fórmula 8: **(Ver fórmula)** y vii) esterificar un compuesto de Fórmula 8 con alcohol pinacolítico en un disolvente orgánico para generar un compuesto de Fórmula 1.
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公开(公告)号:PL3141548T3
公开(公告)日:2020-09-07
申请号:PL16190960
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , DOMINGUEZ OLMO BEATRIZ , JURCÍK VÁCLAV
IPC: C07D471/04
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公开(公告)号:DK3141548T3
公开(公告)日:2020-07-06
申请号:DK16190960
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , DOMINGUEZ OLMO BEATRIZ , JURCÍK VÁCLAV
IPC: C07D471/04
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公开(公告)号:NZ714502A
公开(公告)日:2017-04-28
申请号:NZ71450212
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , LOOKER ADAM , KLINE BILLIE J , JURČÍK VÁCLAV , DOMINGUEZ OLMO BEATRIZ
IPC: C07D471/04 , A61K31/437 , C07D239/42 , C07F5/02 , C07F5/04
Abstract: Disclosed herein is a process for preparing an compound of Formula 1, wherein the substituents are as defined in the specification. The process comprises reacting intermediates with p-toluenesulfonyl chloride, triisopropyl borate and pinacolate alcohol in organic solvents in the presence of a lithium base. In a particular embodiment, the process produces the compound 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1-tosyl-1H-pyrrolo[2,3-b].
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公开(公告)号:MX2013015147A
公开(公告)日:2014-03-27
申请号:MX2013015147
申请日:2012-07-03
Applicant: VERTEX PHARMA
Inventor: LOOKER ADAM , TANOURY GERALD J , JUNG YOUNG CHUN , MAGDZIAK DEREK , KLINE BRILLIE J , JURCIK VÁCLAV , OLMO BEATRIZ DOMINGUEZ
IPC: C07D471/04
Abstract: La presente invención se refiere a procesos y productos intermediarios para la preparación de compuestos útiles como inhibidores de cinasas Janus (JAK).
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公开(公告)号:AU2008323994A1
公开(公告)日:2009-05-14
申请号:AU2008323994
申请日:2008-11-06
Applicant: VERTEX PHARMA
Inventor: FORSLUND RAYMOND , DONG YONG , MAGDZIAK DEREK , TANOURY GERALD
IPC: C07D401/14
Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of bacterial gyrase and Topoisomerase IV (Topo IV).
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