CA2708146A1 - Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid - Google Patents
Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid Download PDFInfo
- Publication number
- CA2708146A1 CA2708146A1 CA2708146A CA2708146A CA2708146A1 CA 2708146 A1 CA2708146 A1 CA 2708146A1 CA 2708146 A CA2708146 A CA 2708146A CA 2708146 A CA2708146 A CA 2708146A CA 2708146 A1 CA2708146 A1 CA 2708146A1
- Authority
- CA
- Canada
- Prior art keywords
- formulation
- methylpyridin
- cyclopropanecarboxamido
- difluorobenzo
- dioxol
- 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.)
- Abandoned
Links
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- 238000009472 formulation Methods 0.000 title claims abstract description 121
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- 238000000034 method Methods 0.000 claims abstract description 31
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- 201000003883 Cystic fibrosis Diseases 0.000 claims description 17
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 16
- 239000003814 drug Substances 0.000 claims description 16
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- 239000011734 sodium Substances 0.000 claims description 10
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- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical group O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 claims description 8
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- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims description 6
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- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 6
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- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 6
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims description 6
- VKOBVWXKNCXXDE-UHFFFAOYSA-N icosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCC(O)=O VKOBVWXKNCXXDE-UHFFFAOYSA-N 0.000 claims description 6
- 239000002736 nonionic surfactant Substances 0.000 claims description 6
- SECPZKHBENQXJG-FPLPWBNLSA-N palmitoleic acid Chemical compound CCCCCC\C=C/CCCCCCCC(O)=O SECPZKHBENQXJG-FPLPWBNLSA-N 0.000 claims description 6
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- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims description 5
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- 229940082509 xanthan gum Drugs 0.000 claims description 5
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 4
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- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
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- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 claims description 3
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- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 3
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1216807P | 2007-12-07 | 2007-12-07 | |
| US61/012,168 | 2007-12-07 | ||
| PCT/US2008/085457 WO2009076141A2 (en) | 2007-12-07 | 2008-12-04 | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cycklopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
Publications (1)
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| CA2708146A1 true CA2708146A1 (en) | 2009-06-18 |
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| WO (1) | WO2009076141A2 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA201004124B (cg-RX-API-DMAC7.html) |
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| EP1664006A2 (en) | 2003-09-06 | 2006-06-07 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| RU2006120549A (ru) * | 2003-11-14 | 2007-12-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Тиазолы и оксазолы, применяемые в качестве модуляторов транспортеров арт-связывающей кассеты |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| BR122018075478B8 (pt) | 2004-06-24 | 2023-10-31 | Vertex Pharma | moduladores de transportadores de cassete de ligação de atp |
| EP1912983B1 (en) | 2005-08-11 | 2011-06-08 | Vertex Pharmaceuticals, Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
| ES2778846T3 (es) | 2005-11-08 | 2020-08-12 | Vertex Pharma | Moduladores heterocíclicos de transportadores de casete de unión a ATP |
| AU2006336504C9 (en) * | 2005-12-28 | 2015-05-14 | Vertex Pharmaceuticals Incorporated | 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis |
| US7671221B2 (en) * | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| HUE032813T2 (en) | 2005-12-28 | 2017-11-28 | Vertex Pharma | Solid forms of N- [2,4-bis (1,1-dimethyl ethyl) -5-hydroxyphenyl] -1,4-dihydro-4-oxoquinoline-3-carboxamide |
| ES2580803T3 (es) | 2006-04-07 | 2016-08-26 | Vertex Pharmaceuticals Incorporated | Moduladores de transportadores del casete de unión a ATP |
| 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 |
| 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 |
| CA2686838C (en) | 2007-05-09 | 2017-03-14 | Vertex Pharmaceuticals Incorporated | Modulators of cftr |
| CN101827593B (zh) | 2007-08-24 | 2013-07-24 | 沃泰克斯药物股份有限公司 | 用于治疗(特别是)囊性纤维化的异噻唑并吡啶酮 |
| SI2217572T1 (sl) | 2007-11-16 | 2014-05-30 | Vertex Pharmaceuticals Incorporated | Izokinolinski modulatorji prenaĺ alcev z atp-vezavno kaseto |
| MX364936B (es) | 2007-12-07 | 2019-05-15 | Vertex Pharma | Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos. |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| CN101910156B (zh) | 2007-12-07 | 2013-12-04 | 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)苯甲酸的固体形式 |
| NZ703814A (en) | 2008-02-28 | 2016-06-24 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| SI2615085T1 (sl) | 2008-03-31 | 2015-11-30 | Vertex Pharmaceuticals Incorporated | Piridilni derivati kot cftr-modulatorji |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| EP2349223A2 (en) | 2008-09-29 | 2011-08-03 | Vertex Pharmaceuticals Incorporated | Dosage units of 3-(6-(1-(2,2-difluorobenzo [d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| EA018891B1 (ru) * | 2008-10-23 | 2013-11-29 | Вертекс Фармасьютикалз, Инкорпорейтед | Модуляторы регулятора трансмембранной проводимости при муковисцидозе |
| HUE035160T2 (en) | 2009-03-20 | 2018-05-02 | Vertex Pharma | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
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| AR081760A1 (es) | 2010-04-07 | 2012-10-17 | Vertex Pharma | Una composicion farmaceutica para administracion oral que comprende acido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoico, un metodo para producir la misma, una tableta y una forma unitaria de dosificacion oral que la comprende y el uso de la misma para la fabricacion de un medicamento |
| RU2579370C2 (ru) * | 2010-04-07 | 2016-04-10 | Вертекс Фармасьютикалз Инкорпорейтед | Твердые формы 3-(2, 2-дифторбензо[d][1, 3] диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойной кислоты |
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| 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 |
| BR112015023328A2 (pt) | 2013-03-13 | 2017-07-18 | Flatley Discovery Lab | compostos de piridazinona e métodos para o tratamento de fibrose cística |
| RU2016122882A (ru) | 2013-11-12 | 2017-12-19 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний |
| MX387720B (es) | 2014-04-15 | 2025-03-12 | Vertex Pharma | Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de conductancia de transmembrana de fibrosis quística. |
| GB201415381D0 (en) | 2014-08-29 | 2014-10-15 | Algipharma As | Inhalable powder formulations of alginate oligomers |
| EP3204358B1 (en) | 2014-10-07 | 2018-09-19 | Vertex Pharmaceuticals Incorporated | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
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| 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 |
| GB201517639D0 (en) | 2015-10-06 | 2015-11-18 | Algipharma As | Use of alginate oligomers to treat or prevent microbial overgrowth in the intestinal tract |
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2008
- 2008-12-04 JP JP2010537038A patent/JP2011506331A/ja not_active Withdrawn
- 2008-12-04 WO PCT/US2008/085457 patent/WO2009076141A2/en not_active Ceased
- 2008-12-04 NZ NZ586272A patent/NZ586272A/en not_active IP Right Cessation
- 2008-12-04 CA CA2708146A patent/CA2708146A1/en not_active Abandoned
- 2008-12-04 BR BRPI0820681A patent/BRPI0820681A2/pt not_active IP Right Cessation
- 2008-12-04 AU AU2008335439A patent/AU2008335439A1/en not_active Abandoned
- 2008-12-04 EP EP08859627A patent/EP2237768A2/en not_active Withdrawn
- 2008-12-04 UA UAA201008466A patent/UA95199C2/ru unknown
- 2008-12-04 US US12/327,922 patent/US20090176839A1/en not_active Abandoned
- 2008-12-04 CN CN2008801251103A patent/CN101998854A/zh active Pending
- 2008-12-04 EA EA201070699A patent/EA201070699A1/ru unknown
- 2008-12-04 KR KR1020107014724A patent/KR20100098545A/ko not_active Withdrawn
- 2008-12-04 MX MX2010006238A patent/MX2010006238A/es not_active Application Discontinuation
-
2010
- 2010-06-06 IL IL206204A patent/IL206204A0/en unknown
- 2010-06-09 ZA ZA2010/04124A patent/ZA201004124B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20100098545A (ko) | 2010-09-07 |
| EA201070699A1 (ru) | 2011-02-28 |
| NZ586272A (en) | 2012-05-25 |
| ZA201004124B (en) | 2011-08-31 |
| BRPI0820681A2 (pt) | 2019-09-24 |
| JP2011506331A (ja) | 2011-03-03 |
| WO2009076141A8 (en) | 2010-07-15 |
| AU2008335439A1 (en) | 2009-06-18 |
| WO2009076141A2 (en) | 2009-06-18 |
| IL206204A0 (en) | 2010-12-30 |
| UA95199C2 (en) | 2011-07-11 |
| MX2010006238A (es) | 2010-08-11 |
| CN101998854A (zh) | 2011-03-30 |
| EP2237768A2 (en) | 2010-10-13 |
| US20090176839A1 (en) | 2009-07-09 |
| WO2009076141A3 (en) | 2009-11-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20131204 |