AR076897A1 - Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos - Google Patents

Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos

Info

Publication number
AR076897A1
AR076897A1 ARP100101869A AR076897A1 AR 076897 A1 AR076897 A1 AR 076897A1 AR P100101869 A ARP100101869 A AR P100101869A AR 076897 A1 AR076897 A1 AR 076897A1
Authority
AR
Argentina
Prior art keywords
compound
produce
order
organic solvent
produce compound
Prior art date
Application number
Other languages
English (en)
Inventor
David A Siesel
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR076897A1 publication Critical patent/AR076897A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Un proceso para la provision del acido 3-(6-(1-(2,2-difluorbenzo[d]1,3]dioxol-5-il) ciclopropanocarboxamido)-3-metilpiridin-2-il)benzoico en forma sustancialmente libre. Reivindicacion 1: Un proceso para la preparacion de Compuesto (1): que comprende las etapas de: i) la provision de 2-bromo-3-metilpiridina Compuesto (2) y ácido 3-(t-butoxicarbonil)fenilboronico Compuesto (3); ii) el acoplamiento cruzado de compuesto 2 y compuesto 3 en una mezcla bifásica que comprende agua, un primer solvente orgánico, una primera base y un catalizador de metal de transicion a fin de producir Compuesto (4); iii) la oxidacion de compuesto 4 para producir Compuesto (5); iv) el agregado de un grupo amina a la posicion 6 de la porcion piridilo a fin de producir Compuesto (6); v) la reaccion de compuesto 6 con compuesto (7); en un segundo solvente orgánico, en presencia de una segunda base, a fin de producir compuesto (8); vi) la desesterificacion de compuesto 8 en un mezcla bifásica que comprende agua, un tercer solvente orgánico y un primer ácido, a fin de producir compuesto (9); vii) la suspension o disolucion de compuesto 9 en un solvente apropiado durante una cantidad eficaz de tiempo para producir Compuesto 1. Reivindicacion 26: Un compuesto de la formula (10); donde: R es H, alifático C1-6, arilo, aralquilo, heteroarilo, cicloalquilo, o heterocicloalquilo; R1 y R2 se seleccionan de manera independiente de -RgJ, -ORJ, -N(RJ)2, -NO2, halogeno, -CN, -haloalquiloC1-4, -haloalcoxiC1-4, -C(O)N(RJ)2, -NRJC(O)RJ, -SORJ, -SO2RJ, -SO2N(RJ)2, -NRJSO2RJ, -CORJ, -CO2RJ, -NRJSO2N(RJ)2, -COCORJ; RJ es hidrogeno o alifático C1-6; o es un numero entero de 0 a 3 inclusive; y p es un numero entero de 0 a 5 inclusive.
ARP100101869 2009-05-29 2010-05-28 Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos AR076897A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12/474,590 US20100036130A1 (en) 2007-12-07 2009-05-29 Processes for producing cycloalkylcarboxamido-pyridine benzoic acids

Publications (1)

Publication Number Publication Date
AR076897A1 true AR076897A1 (es) 2011-07-13

Family

ID=43223322

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101869 AR076897A1 (es) 2009-05-29 2010-05-28 Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos

Country Status (4)

Country Link
US (4) US20100036130A1 (es)
AR (1) AR076897A1 (es)
TW (1) TWI589568B (es)
WO (1) WO2010138484A2 (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
WO2005026137A2 (en) 2003-09-06 2005-03-24 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
EP1682127B1 (en) * 2003-11-14 2009-07-29 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
DK1773816T3 (en) 2004-06-24 2015-01-26 Vertex Pharma Modulators of ATP-binding cassette transporters
WO2007021982A2 (en) * 2005-08-11 2007-02-22 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
KR101331768B1 (ko) 2005-11-08 2013-11-22 버텍스 파마슈티칼스 인코포레이티드 Ａｔｐ 결합 카세트 수송체의 헤테로사이클릭 조정제
JP5409010B2 (ja) 2005-12-28 2014-02-05 バーテックス ファーマシューティカルズ インコーポレイテッド Ｎ−［２，４−ビス（１，１−ジメチルエチル）−５−ヒドロキシフェニル］−１，４−ジヒドロ−４−オキソキノリン−３−カルボキサミドの固体形態
JP5165586B2 (ja) 2005-12-28 2013-03-21 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症の処置のためのＡＴＰ結合カセットトランスポーターのモジュレーターとしての、１−（ベンゾ［ｄ］［１，３］ジオキソール−５−イル）−Ｎ−（フェニル）シクロプロパン−カルボキサミド誘導体および関連化合物
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
PL3091011T3 (pl) * 2006-04-07 2018-06-29 Vertex Pharmaceuticals Incorporated Modulatory transporterów posiadających kasetę wiążącą ATP
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
WO2008141119A2 (en) 2007-05-09 2008-11-20 Vertex Pharmaceuticals Incorporated Modulators of cftr
WO2009038913A2 (en) 2007-08-24 2009-03-26 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
PL2217572T3 (pl) 2007-11-16 2014-04-30 Vertex Pharma Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP
KR20150066608A (ko) 2007-12-07 2015-06-16 버텍스 파마슈티칼스 인코포레이티드 사이클로알킬카복시아미도-피리딘 벤조산의 제조 방법
JP2011506331A (ja) * 2007-12-07 2011-03-03 バーテックス ファーマシューティカルズ インコーポレイテッド ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の処方物
SG186638A1 (en) 2007-12-07 2013-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
CA2716109C (en) 2008-02-28 2016-07-19 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
ES2442945T3 (es) 2008-03-31 2014-02-14 Vertex Pharmaceuticals Inc. Derivados de piridilo como moduladores del CFTR
AR073709A1 (es) 2008-09-29 2010-11-24 Vertex Pharma Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico
US8513282B2 (en) 2008-10-23 2013-08-20 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
NZ624460A (en) 2009-03-20 2015-12-24 Vertex Pharma Process for making modulators of cystic fibrosis transmembrane conductance regulator
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
TWI549950B (zh) 2010-04-07 2016-09-21 維泰克斯製藥公司 ３－（６－（１－（２，２－二氟苯并［ｄ］［１，３］二氧雜環戊烯－５－基）環丙烷甲醯胺基）－３－甲基吡啶－２－基）苯甲酸之固體形式
RU2592368C2 (ru) 2010-04-07 2016-07-20 Вертекс Фармасьютикалз Инкорпорейтед ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ 3-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНУЮ КИСЛОТУ, И ИХ ВВЕДЕНИЕ
EP3381899B1 (en) 2010-04-22 2021-01-06 Vertex Pharmaceuticals Incorporated Intermediate compound for process of producing cycloalkylcarboxamido-indole compounds
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (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
SI2776427T1 (sl) 2011-11-08 2017-05-31 Vertex Pharmaceuticals Incorporated Modulatorji prenašalcev ATP-vezavne kasete
CN104470518A (zh) 2012-02-27 2015-03-25 沃泰克斯药物股份有限公司 药物组合物及其施用
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
EP2872122A1 (en) 2012-07-16 2015-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (r)-1-(2,2-diflurorbenzo[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 and administration thereof
AU2014349010C1 (en) 2013-11-12 2020-08-06 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases
RS57476B9 (sr) 2014-04-15 2021-10-29 Vertex Pharma Farmaceutske kompozicije za lečenje bolesti posredovanih transmembranskim regulatorom provodljivosti cistične fibroze
GB201415381D0 (en) 2014-08-29 2014-10-15 Algipharma As Inhalable powder formulations of alginate oligomers
CA2963945C (en) 2014-10-07 2023-01-10 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
JP6494757B2 (ja) 2014-11-18 2019-04-03 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ハイスループット試験高速液体クロマトグラフィーを行うプロセス
GB201504878D0 (en) 2015-03-23 2015-05-06 Algipharma As Use of alginate oligomers and CFTR modulators in the treatment of conditions associated with CFTR dysfuntion
CN106432209A (zh) * 2015-08-11 2017-02-22 苏州晶云药物科技有限公司 Lumacaftor的新晶型及其制备方法
GB201517639D0 (en) 2015-10-06 2015-11-18 Algipharma As Use of alginate oligomers to treat or prevent microbial overgrowth in the intestinal tract
WO2017137900A1 (en) 2016-02-10 2017-08-17 Lupin Limited Amorphous lumacaftor and its solid dispersion

Family Cites Families (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US20050113423A1 (en) * 2003-03-12 2005-05-26 Vangoor Frederick F. Modulators of ATP-binding cassette transporters
EP1646615B1 (en) * 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
WO2005026137A2 (en) 2003-09-06 2005-03-24 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
CN1886393A (zh) 2003-10-08 2006-12-27 沃泰克斯药物股份有限公司 含有环烷基或吡喃基基团的atp－结合弹夹转运蛋白的调控剂
EP1682127B1 (en) * 2003-11-14 2009-07-29 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters
EP3219709B1 (en) * 2004-01-30 2020-03-18 Vertex Pharmaceuticals Incorporated Intermediate compound of modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
DK1773816T3 (en) 2004-06-24 2015-01-26 Vertex Pharma Modulators of ATP-binding cassette transporters
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
US7888374B2 (en) * 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
EP2363128B1 (en) 2005-03-11 2016-02-17 Vertex Pharmaceuticals Incorporated Indole modulators of ATP-binding cassette transporters
US8822451B2 (en) * 2005-05-24 2014-09-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2007021982A2 (en) * 2005-08-11 2007-02-22 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
JP2009511494A (ja) * 2005-10-06 2009-03-19 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｐ結合カセットトランスポーターのモジュレーター
KR101331768B1 (ko) * 2005-11-08 2013-11-22 버텍스 파마슈티칼스 인코포레이티드 Ａｔｐ 결합 카세트 수송체의 헤테로사이클릭 조정제
US20120232059A1 (en) 2005-11-08 2012-09-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette Transporters
US20090105272A1 (en) * 2005-12-24 2009-04-23 Grootenhuis Peter D J Prodrugs of modulators of ABC transporters
AU2006331565A1 (en) * 2005-12-27 2007-07-05 Vertex Pharmaceuticals Incorporated Compounds useful in CFTR assays and methods therewith
JP5409010B2 (ja) 2005-12-28 2014-02-05 バーテックス ファーマシューティカルズ インコーポレイテッド Ｎ−［２，４−ビス（１，１−ジメチルエチル）−５−ヒドロキシフェニル］−１，４−ジヒドロ−４−オキソキノリン−３−カルボキサミドの固体形態
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
JP5165586B2 (ja) 2005-12-28 2013-03-21 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症の処置のためのＡＴＰ結合カセットトランスポーターのモジュレーターとしての、１−（ベンゾ［ｄ］［１，３］ジオキソール−５−イル）−Ｎ−（フェニル）シクロプロパン−カルボキサミド誘導体および関連化合物
PL3091011T3 (pl) * 2006-04-07 2018-06-29 Vertex Pharmaceuticals Incorporated Modulatory transporterów posiadających kasetę wiążącą ATP
US7645789B2 (en) * 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
ES2377840T3 (es) * 2006-05-12 2012-04-02 Vertex Pharmaceuticals, Inc. Composiciones de N-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-dihidro-4-oxoquinolina-3-carboxamida
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US7754739B2 (en) * 2007-05-09 2010-07-13 Vertex Pharmaceuticals Incorporated Modulators of CFTR
CA2688004C (en) 2007-05-25 2016-07-05 Vertex Pharmaceuticals Incorporated Thienopyridone compounds for use as modulators of cystic fibrosis transmembrane conductance regulator
US20110177999A1 (en) * 2007-08-09 2011-07-21 Vertex Pharmaceuticals Incorporated Therapeutic Combinations Useful in Treating CFTR Related Diseases
WO2009038913A2 (en) * 2007-08-24 2009-03-26 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
WO2009038683A2 (en) 2007-09-14 2009-03-26 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
CN101821266B (zh) 2007-09-14 2014-03-12 沃泰克斯药物股份有限公司 囊性纤维化跨膜通道调节因子的调节剂
PL2217572T3 (pl) 2007-11-16 2014-04-30 Vertex Pharma Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP
KR20150066608A (ko) * 2007-12-07 2015-06-16 버텍스 파마슈티칼스 인코포레이티드 사이클로알킬카복시아미도-피리딘 벤조산의 제조 방법
JP2011506331A (ja) * 2007-12-07 2011-03-03 バーテックス ファーマシューティカルズ インコーポレイテッド ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の処方物
SG186638A1 (en) 2007-12-07 2013-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
WO2009076593A1 (en) * 2007-12-13 2009-06-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CA2716109C (en) * 2008-02-28 2016-07-19 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
ES2442945T3 (es) 2008-03-31 2014-02-14 Vertex Pharmaceuticals Inc. Derivados de piridilo como moduladores del CFTR
CN102231990B (zh) 2008-08-13 2013-09-25 沃泰克斯药物股份有限公司 N-[2，4-双(1，1-二甲基乙基)-5-羟基苯基]-1，4-二氢-4-氧代喹啉-3-甲酰胺的药物组合物和其给药
US20100256184A1 (en) 2008-08-13 2010-10-07 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
AR073709A1 (es) 2008-09-29 2010-11-24 Vertex Pharma Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico
US8513282B2 (en) 2008-10-23 2013-08-20 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20110257223A1 (en) 2008-10-23 2011-10-20 Vertex Pharmaceuticals Incorporated Modulators of Cystic Fibrosis Transmembrane Conductance Regulator
KR20110074916A (ko) 2008-10-23 2011-07-04 버텍스 파마슈티칼스 인코포레이티드 Ｎ-(4-(7-아자비시클로［2.2.1］헵탄-7-일)-2-(트리플루오로메틸)페닐)-4-옥소-5-(트리플루오로메틸)-1,4-디히드로퀴놀린-3-카르복스아미드의 고체 형태
AU2009308232B2 (en) * 2008-10-23 2016-02-04 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP2382197B1 (en) * 2008-12-30 2016-10-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
PT2408749T (pt) 2009-03-20 2018-10-08 Vertex Pharma Moduladores do regulador da condutância transmembranar da fibrose cística
NZ624460A (en) 2009-03-20 2015-12-24 Vertex Pharma Process for making modulators of cystic fibrosis transmembrane conductance regulator
JP5793496B2 (ja) * 2009-09-17 2015-10-14 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ アザ二環式化合物を調製するプロセス
WO2011050325A1 (en) 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
BR112012009583A2 (pt) 2009-10-23 2015-09-29 Vertex Pharma processo para preparação de moduladores de regulador de condutância de transmembrana de fibrose cística
CA2778493A1 (en) 2009-10-23 2011-04-28 Vertex Pharmaceuticals Incorporated Solid forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide
EP3037415A1 (en) 2010-03-19 2016-06-29 Vertex Pharmaceuticals Inc. Solid form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
ES2845449T3 (es) 2010-03-25 2021-07-26 Vertex Pharma 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
TWI549950B (zh) 2010-04-07 2016-09-21 維泰克斯製藥公司 ３－（６－（１－（２，２－二氟苯并［ｄ］［１，３］二氧雜環戊烯－５－基）環丙烷甲醯胺基）－３－甲基吡啶－２－基）苯甲酸之固體形式
RU2592368C2 (ru) 2010-04-07 2016-07-20 Вертекс Фармасьютикалз Инкорпорейтед ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ 3-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНУЮ КИСЛОТУ, И ИХ ВВЕДЕНИЕ
AU2011242454A1 (en) 2010-04-22 2012-11-08 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
NZ603044A (en) 2010-04-22 2015-08-28 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
EP3381899B1 (en) 2010-04-22 2021-01-06 Vertex Pharmaceuticals Incorporated Intermediate compound for process of producing cycloalkylcarboxamido-indole compounds
NZ603042A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
TW201202250A (en) 2010-05-20 2012-01-16 Vertex Pharma Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
AU2011255237A1 (en) 2010-05-20 2012-11-29 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (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
CA2808501A1 (en) 2010-08-23 2012-03-01 Vertex Pharmaceuticals Incorporated Pharmaceutical composition of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxy propyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration therof
CN103153286A (zh) 2010-08-27 2013-06-12 沃泰克斯药物股份有限公司 药物组合物及其施用
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
EP2773349A1 (en) 2011-11-02 2014-09-10 Vertex Pharmaceuticals Incorporated Use of (n- [2, 4 -bis (1, 1 -dimethylethyl) - 5 - hydroxyphenyl]- 1, 4 - dihydro - 4 - oxoquinoline - 3 - carboxamide) for treating cftr mediated diseases
SI2776427T1 (sl) 2011-11-08 2017-05-31 Vertex Pharmaceuticals Incorporated Modulatorji prenašalcev ATP-vezavne kasete
ES2742277T3 (es) 2012-01-25 2020-02-13 Vertex Pharma Composiciones farmacéuticas de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-ilo) ciclopropano carboxamido)-3metilpiridin-2-ilo)benzoico y su administración
CN104470518A (zh) 2012-02-27 2015-03-25 沃泰克斯药物股份有限公司 药物组合物及其施用
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
EP2872122A1 (en) 2012-07-16 2015-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (r)-1-(2,2-diflurorbenzo[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 and administration thereof
AU2013337730B2 (en) 2012-11-02 2018-06-14 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of CFTR mediated diseases
US20140221424A1 (en) 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis

Also Published As

Publication number Publication date
US20120203006A1 (en) 2012-08-09
WO2010138484A3 (en) 2011-01-20
TWI589568B (zh) 2017-07-01
US8816093B2 (en) 2014-08-26
US9012652B2 (en) 2015-04-21
US20100036130A1 (en) 2010-02-11
US8461342B2 (en) 2013-06-11
TW201512184A (zh) 2015-04-01
WO2010138484A2 (en) 2010-12-02
US20140330023A1 (en) 2014-11-06
US20130274477A1 (en) 2013-10-17

Similar Documents

Publication Publication Date Title
AR076897A1 (es) Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos
KR102371784B1 (ko) 활성화 혈액 응고 제 X 인자 (FXa) 의 저해약의 제조 방법
HRP20161543T1 (hr) Proces za proizvodnju cikloalkilkarboksiamido-piridin benzojevih kiselina
EA201201179A1 (ru) Способ получения изоксазолиновых производных
UA116876C2 (uk) Спосіб одержання хінолінових похідних
ECSP10010405A (es) Procesos e intermediarios para la preparacion de derivados de acido 5-bifenil-4-il-2-metilpentanoico
AR074845A1 (es) Procedimiento de sintesis de la ivabradina y de sus sales de adicion a un acido farmaceuticamente aceptable
CO6362007A2 (es) Derivados de azaspiranil-alquilcarbamatos de heterociclos de 5 eslabones, su preparación y su aplicación en terapeútica
AR077526A1 (es) Metodo para la sintesis de (1s,2r)- milnacipran
AR075227A1 (es) Procedimiento de sintesis de ivabradina y sus sales de adicion de acidos farmaceuticamente aceptables.
AR066709A1 (es) Proceso para la produccion de pirazoles
AR076969A1 (es) Un procedimiento para la preparacion de febuxostat
PE20090956A1 (es) PROCESO PARA LA OBTENCION DE DERIVADOS DE PIRIDO [2,1-a] - ISOQUINOLINA
CU20150051A7 (es) Derivados de n-(piridin-2-il)pirimidin-4-amina que contienen un grupo sulfoximina
AR088021A1 (es) Derivados de oxadiazoles y de piridazinas, su preparacion y su aplicacion en terapeutica
AR047686A1 (es) Un procedimiento de sintesis de compuestos de 1,3-dihidro-2h-3-benzazepin-2-ona, y su aplicacion a la sintesis de la ivabradina y sus sales de adicion con un acido farmaceuticamente aceptable
AR082370A1 (es) Proceso de preparacion de sales herbicidas
AR075977A1 (es) Procedimiento de sintesis de ivabradina y/o su derivado amino hidrogenado y de sus sales de adicion a un acido farmaceuticamente aceptable e intermediarios de sintesis.
AR075441A1 (es) Un proceso para la preparacion de etoricoxib
ATE532516T1 (de) Verfahren zur synthese von glyt-1-hemmern
AR080178A1 (es) Procedimiento de sintesis de la ivabradina y de sus sales de adicion a un acido farmaceuticamente aceptable
JP2016520090A5 (es)
CO5611115A2 (es) Proceso para la produccion de propionato de fluticasona, en particular de la forma polimorfica 1
AR075425A1 (es) Procedimiento de preparacion e intermediarios
DE602006008335D1 (de) Neuartiges verfahren zur herstellung von quaternärer säure und ammoniumsalzen

Legal Events

Date Code Title Description
FC Refusal