JP2009533351A5 - - Google Patents
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- JP2009533351A5 JP2009533351A5 JP2009504359A JP2009504359A JP2009533351A5 JP 2009533351 A5 JP2009533351 A5 JP 2009533351A5 JP 2009504359 A JP2009504359 A JP 2009504359A JP 2009504359 A JP2009504359 A JP 2009504359A JP 2009533351 A5 JP2009533351 A5 JP 2009533351A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- independently
- conr
- compound
- aliphatic
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 125000001931 aliphatic group Chemical group 0.000 claims description 29
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 19
- 239000001257 hydrogen Substances 0.000 claims description 18
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 11
- 125000004429 atom Chemical group 0.000 claims description 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 41
- -1 2- (tertbutyl) indol-5-yl Chemical group 0.000 claims 21
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- 108010006533 ATP-Binding Cassette Transporters Proteins 0.000 claims 12
- 102000005416 ATP-Binding Cassette Transporters Human genes 0.000 claims 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012472 biological sample Substances 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 239000012634 fragment Substances 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 4
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 235000019439 ethyl acetate Nutrition 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000012074 organic phase Substances 0.000 description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 2
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 238000004440 column chromatography Methods 0.000 description 1
- YMGUBTXCNDTFJI-UHFFFAOYSA-M cyclopropanecarboxylate Chemical compound [O-]C(=O)C1CC1 YMGUBTXCNDTFJI-UHFFFAOYSA-M 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- PSMIMDJBBPABLI-UHFFFAOYSA-N methyl 1-[4-hydroxy-3-(N-hydroxy-C-methylcarbonimidoyl)phenyl]cyclopropane-1-carboxylate Chemical compound C=1C=C(O)C(C(C)=NO)=CC=1C1(C(=O)OC)CC1 PSMIMDJBBPABLI-UHFFFAOYSA-N 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79045906P | 2006-04-07 | 2006-04-07 | |
| US60/790,459 | 2006-04-07 | ||
| PCT/US2007/008975 WO2007117715A2 (en) | 2006-04-07 | 2007-04-09 | Modulators of atp-binding cassette transporters |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013240205A Division JP5827297B2 (ja) | 2006-04-07 | 2013-11-20 | Atp結合カセット輸送体の調節剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009533351A JP2009533351A (ja) | 2009-09-17 |
| JP2009533351A5 true JP2009533351A5 (cg-RX-API-DMAC10.html) | 2010-06-03 |
| JP5420395B2 JP5420395B2 (ja) | 2014-02-19 |
Family
ID=38477342
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009504359A Active JP5420395B2 (ja) | 2006-04-07 | 2007-04-09 | Atp結合カセット輸送体の調節剤 |
| JP2013240205A Active JP5827297B2 (ja) | 2006-04-07 | 2013-11-20 | Atp結合カセット輸送体の調節剤 |
| JP2015073706A Pending JP2015120762A (ja) | 2006-04-07 | 2015-03-31 | Atp結合カセット輸送体の調節剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013240205A Active JP5827297B2 (ja) | 2006-04-07 | 2013-11-20 | Atp結合カセット輸送体の調節剤 |
| JP2015073706A Pending JP2015120762A (ja) | 2006-04-07 | 2015-03-31 | Atp結合カセット輸送体の調節剤 |
Country Status (22)
Families Citing this family (115)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2006111093A (ru) | 2003-09-06 | 2007-10-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Модуляторы атр-связывающих кассетных транспортеров |
| ZA200604578B (en) * | 2003-11-14 | 2008-05-28 | Vertex Pharma | Thiazoles and oxazoles.useful as modulators of ATP Binding cassette transporters |
| AU2005210474B2 (en) * | 2004-01-30 | 2011-07-07 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding cassette transporters |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| CN104788328B (zh) | 2004-06-24 | 2017-09-12 | 沃泰克斯药物股份有限公司 | Atp‑结合弹夹转运蛋白的调控剂 |
| JP5143738B2 (ja) | 2005-08-11 | 2013-02-13 | 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 | 嚢胞性線維症膜コンダクタンス制御因子の調節物質 |
| DK2774925T3 (en) * | 2005-11-08 | 2017-02-27 | Vertex Pharma | Heterocyclic modulators of ATP binding cassette transporters |
| US7671221B2 (en) * | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| ES2398319T3 (es) * | 2005-12-28 | 2013-03-15 | Vertex Pharmaceuticals Incorporated | Derivados de 1-(benzo[D][1,3]dioxol-5-il)-N-(fenil)ciclopropano-carboxamida y compuestos relacionados como moduladores de transportadores de casetes de unión a ATP para el tratamiento de la fibrosis quística |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US7645789B2 (en) * | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| EP2007756B1 (en) * | 2006-04-07 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US8563573B2 (en) * | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| CN101715450B (zh) | 2006-11-03 | 2013-03-13 | 沃泰克斯药物股份有限公司 | 作为cftr调控剂的氮杂吲哚衍生物 |
| US7754739B2 (en) * | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| BRPI0809498A2 (pt) * | 2007-04-02 | 2014-09-23 | Inst Oneworld Health | Compostos inibidores de cftr e seus usos |
| AU2008251504B2 (en) | 2007-05-09 | 2013-07-18 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| CA2687764A1 (en) * | 2007-05-25 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| AU2008302598B2 (en) | 2007-08-24 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis |
| DK2217572T3 (da) | 2007-11-16 | 2014-02-03 | Vertex Pharma | Isoquinoliner som modulatorer af ATP-bindingskassettetransportører |
| CN101998854A (zh) * | 2007-12-07 | 2011-03-30 | 沃泰克斯药物股份有限公司 | 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 |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| LT2225230T (lt) | 2007-12-07 | 2017-01-25 | Vertex Pharmaceuticals Incorporated | 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzoinės rūgšties kietos formos |
| EP2639222B1 (en) * | 2007-12-07 | 2016-08-31 | Vertex Pharmaceuticals Incorporated | Process for producing cycloalkylcarboxiamido-pyridine benzoic acids |
| EP2078711A1 (en) * | 2007-12-28 | 2009-07-15 | AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A. | (Aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor |
| CN102245573B (zh) * | 2008-02-28 | 2013-11-20 | 沃泰克斯药物股份有限公司 | 作为cftr调节剂的杂芳基衍生物 |
| JP5622285B2 (ja) * | 2008-03-31 | 2014-11-12 | 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 Pharmaceuticalsincorporated | Cftrモジュレーターとしてのピリジル誘導体 |
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| EP2278879B1 (en) * | 2008-04-21 | 2016-06-15 | PATH Drug Solutions | Compounds, compositions and methods comprising oxadiazole derivatives |
| AR072297A1 (es) | 2008-06-27 | 2010-08-18 | Novartis Ag | Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona. |
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| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| JP2012503005A (ja) * | 2008-09-19 | 2012-02-02 | インスティテュート フォア ワンワールド ヘルス | イミダゾール誘導体およびトリアゾール誘導体を含む、化合物、組成物ならびに方法。 |
| CN102164587A (zh) * | 2008-09-29 | 2011-08-24 | 沃泰克斯药物股份有限公司 | 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)苯甲酸的剂量单元 |
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| UA121188C2 (uk) * | 2008-11-06 | 2020-04-27 | Вертекс Фармасьютікалз Інкорпорейтед | Модулятори атф-зв'язувальних касетних транспортерів |
| SG10201504084QA (en) | 2009-03-20 | 2015-06-29 | Vertex Pharma | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
| US8511216B2 (en) * | 2009-03-30 | 2013-08-20 | Kanzaki Kokyukoki Mfg. Co., Ltd. | Hydraulic actuator unit |
| US8343976B2 (en) * | 2009-04-20 | 2013-01-01 | Institute For Oneworld Health | Compounds, compositions and methods comprising pyrazole derivatives |
| US8497271B2 (en) | 2009-10-07 | 2013-07-30 | Bristol-Myers Squibb Company | Modulators of G protein-coupled receptor 88 |
| US8304577B2 (en) | 2009-10-09 | 2012-11-06 | Bristol-Myers Squibb Company | Modulators of G protein-coupled receptor 88 |
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| MX2012004792A (es) | 2009-10-22 | 2013-02-01 | Vertex Pharma | Composiciones para el tratamiento de fibrosis quistica y otras enfermedades cronicas. |
| 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 |
| CN102892764B (zh) * | 2010-03-25 | 2016-07-06 | 弗特克斯药品有限公司 | (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)环丙烷甲酰胺的固体形式 |
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| LT3150198T (lt) | 2010-04-07 | 2021-12-10 | Vertex Pharmaceuticals Incorporated | 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il)benzoinės rūgšties farmacinė kompozicija ir jos įvedimas |
| WO2011133956A1 (en) * | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| EP3381899B1 (en) | 2010-04-22 | 2021-01-06 | Vertex Pharmaceuticals Incorporated | Intermediate compound for process of producing cycloalkylcarboxamido-indole compounds |
| CA2796642A1 (en) * | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| NZ603043A (en) | 2010-04-22 | 2015-02-27 | Vertex Pharma | Pharmaceutical compositions comprising cftr modulators and administrations thereof |
| AU2011255237A1 (en) | 2010-05-20 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
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| JP2013536231A (ja) * | 2010-08-23 | 2013-09-19 | 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 | (r)−1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)−n−(1−(2,3−ジヒドロキシプロピル)−6−フルオロ−2−(1−ヒドロキシ−2−メチルプロパン−2−イル)−1h−インドール−5−イル)シクロプロパンカルボキサミドを含む医薬組成物およびその投与 |
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| IN2014KN00885A (cg-RX-API-DMAC10.html) * | 2011-11-08 | 2015-10-02 | Vertex Pharma | |
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| CN107674071B (zh) * | 2012-05-11 | 2021-12-31 | 同步制药公司 | 作为隐花色素调节剂的含有咔唑的磺酰胺类 |
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| AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | 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 |
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| CN102816104B (zh) * | 2012-08-30 | 2014-05-21 | 浙江大学 | 一种3-氰基吲哚类化合物的合成方法 |
| ITMI20122065A1 (it) | 2012-12-03 | 2014-06-04 | Univ Padova | Uso dei correttori del cftr nel trattamento delle patologie del muscolo striato |
| EP2958924B1 (en) | 2013-02-22 | 2016-12-28 | Bristol-Myers Squibb Company | 5h-chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase 1 (aak1) |
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