DK2709986T3 - Deutererede derivater af ivacaftor - Google Patents
Deutererede derivater af ivacaftor Download PDFInfo
- Publication number
- DK2709986T3 DK2709986T3 DK12725197.3T DK12725197T DK2709986T3 DK 2709986 T3 DK2709986 T3 DK 2709986T3 DK 12725197 T DK12725197 T DK 12725197T DK 2709986 T3 DK2709986 T3 DK 2709986T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- deuterium
- compounds
- acid
- pharmaceutically acceptable
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/12—Mucolytics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Claims (18)
1. Forbindelse med formel I:
formel I eller et farmaceutisk acceptabelt salt deraf, hvor hver af X1, X2, X3, X4, X5, X6, og X7 er uafhængigt hydrogen eller deuterium; Y1, Y2, og Y3 er CDs; hver af Y4, Y5, og Y6 er uafhængigt CH3 eller CD3; hvor den isotopiske berigelsesfaktor for hvert designeret deuteriumatom er mindst 3500; og hvor et hvilket som helst atom der ikke er designeret som deuterium er til stede ved dets naturlige isotopiske hyppighed, forudsat at forbindelsen med formel I ikke er forbindelse 100:
forbindelse 100
2. Forbindelsen ifølge krav 1, hvor X1, X2, X3, og X4 er den samme.
3. Forbindelsen ifølge krav 2, hvor Y4, Y5, og Y6 er den samme.
4. Forbindelsen ifølge krav 2 eller krav 3, hvor X6 og X7 er den samme.
5. Forbindelsen ifølge et hvilket som helst af de foregående krav, hvor X5 er deuterium.
6. Forbindelsen ifølge et hvilket som helst af de foregående krav hvor Y4, Y5, og Y6 er CD3.
7. Forbindelserne ifølge et hvilket som helst af kravene 1 til 4, hvor X5 er hydrogen.
8. Forbindelserne ifølge et hvilket som helst af kravene 1 til 4, hvor Y4, Y5, og Y6 er CHs.
9. Forbindelsen ifølge krav 1, hvor den isotopiske berigelsesfaktor for hvert designeret deuteriumatom er mindst 6000.
10. Forbindelsen ifølge krav 1, hvor den isotopiske berigelsesfaktor for hvert designeret deuteriumatom er mindst 6333.3.
11. Forbindelsen ifølge krav 1, hvor den isotopiske berigelsesfaktor for hvert designeret deuteriumatom er mindst 6466.7.
12. Forbindelsen ifølge krav 1 eller et hvilket som helst af kravene 9 til 11, hvor forbindelsen med formel I er en hvilken som helst af forbindelserne fra tabellen nedenfor,
eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelsen ifølge krav 1 eller et hvilket som helst af kravene 9 til 11, hvor forbindelsen med formel I er forbindelsen fra tabellen nedenfor,
eller et farmaceutisk acceptabelt salt deraf.
14. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af de foregående krav eller et farmaceutisk acceptabelt salt deraf; og en farmaceutisk acceptabel bærer.
15. Forbindelse ifølge et hvilket som helst af kravene 1-13 eller en sammensætning ifølge krav 14 til anvendelse i behandling af cystisk fibrose.
16. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-13, eller en sammensætning ifølge krav 14, i fremstillingen af et medikament til behandling af cystisk fibrose.
17. Forbindelse ifølge et hvilket som helst af kravene 1-13 eller en sammensætning ifølge krav 14 til anvendelse i behandling af kronisk obstruktiv pulmonær sygdom (COPD).
18. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-13, eller en sammensætning ifølge krav 14, i fremstillingen af et medikament til behandling af kronisk obstruktiv pulmonær sygdom (COPD).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161487497P | 2011-05-18 | 2011-05-18 | |
| PCT/US2012/038297 WO2012158885A1 (en) | 2011-05-18 | 2012-05-17 | Deuterated derivatives of ivacaftor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2709986T3 true DK2709986T3 (da) | 2017-05-08 |
Family
ID=46201810
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK17160386T DK3235812T3 (da) | 2011-05-18 | 2012-05-17 | Deutererede derivater af ivacaftor |
| DK12725197.3T DK2709986T3 (da) | 2011-05-18 | 2012-05-17 | Deutererede derivater af ivacaftor |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK17160386T DK3235812T3 (da) | 2011-05-18 | 2012-05-17 | Deutererede derivater af ivacaftor |
Country Status (20)
| Country | Link |
|---|---|
| EP (2) | EP2709986B1 (da) |
| JP (2) | JP6063455B2 (da) |
| AU (5) | AU2012255711B2 (da) |
| BR (1) | BR112013029240B1 (da) |
| CA (1) | CA2834574C (da) |
| CY (2) | CY1119090T1 (da) |
| DK (2) | DK3235812T3 (da) |
| EA (1) | EA028378B1 (da) |
| ES (2) | ES2758028T3 (da) |
| HK (1) | HK1244183A1 (da) |
| HR (2) | HRP20170754T1 (da) |
| HU (1) | HUE032771T2 (da) |
| LT (1) | LT2709986T (da) |
| ME (2) | ME02749B (da) |
| MX (1) | MX349159B (da) |
| PL (2) | PL3235812T3 (da) |
| PT (2) | PT3235812T (da) |
| RS (2) | RS56096B1 (da) |
| SI (2) | SI2709986T1 (da) |
| WO (1) | WO2012158885A1 (da) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT1993360T (lt) | 2005-12-28 | 2017-06-12 | Vertex Pharmaceuticals Incorporated | N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma |
| MX349159B (es) * | 2011-05-18 | 2017-07-14 | Concert Pharmaceuticals Inc | Derivados deuterados de ivacaftor. |
| HUE047354T2 (hu) | 2011-05-18 | 2020-04-28 | Vertex Pharmaceuticals Europe Ltd | Ivacaftor deuterizált származékai |
| CA2869257A1 (en) | 2012-04-06 | 2013-10-10 | The Uab Research Foundation | Methods for increasing cftr activity |
| JP6146990B2 (ja) * | 2012-11-16 | 2017-06-14 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化されたｃｆｔｒ増強物質 |
| MY183582A (en) * | 2012-11-19 | 2021-02-26 | Vertex Pharmaceuticals Europe Ltd | Deuterated cftr potentiators |
| CN112250627B (zh) | 2014-10-06 | 2024-02-02 | 弗特克斯药品有限公司 | 囊性纤维化跨膜转导调节因子调节剂 |
| AU2015330923B2 (en) | 2014-10-07 | 2020-03-12 | Vertex Pharmaceuticals Incorporated | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
| US10196384B2 (en) | 2015-03-31 | 2019-02-05 | Vertex Pharmaceuticals (Europe) Limited | Deuterated CFTR modulators |
| MA42488A (fr) | 2015-07-24 | 2018-05-30 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| CN108367002A (zh) * | 2015-09-21 | 2018-08-03 | 弗特克斯药品欧洲有限公司 | 氘化cftr增强剂的给予 |
| EP3352758A4 (en) * | 2015-09-25 | 2018-08-01 | Vertex Pharmaceuticals (Europe) Limited | Deuterated cftr potentiators |
| BR112018070747B1 (pt) * | 2016-04-07 | 2024-01-09 | Proteostasis Therapeutics, Inc | Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos |
| ES2954658T3 (es) | 2016-06-21 | 2023-11-23 | Proteostasis Therapeutics Inc | Compuestos, composiciones y procedimientos para aumentar la actividad de CFTR |
| JP2017105824A (ja) * | 2017-02-10 | 2017-06-15 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化されたｃｆｔｒ増強物質 |
| KR20200096560A (ko) * | 2017-12-01 | 2020-08-12 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막관통 조절 인자의 제조 방법 |
| JP6654223B2 (ja) * | 2018-08-13 | 2020-02-26 | バーテックス ファーマシューティカルズ （ヨーロッパ） リミテッド | 重水素化されたｃｆｔｒ増強物質 |
| WO2020214921A1 (en) | 2019-04-17 | 2020-10-22 | Vertex Pharmaceuticals Incorporated | Solid forms of modulators of cftr |
| AU2020328568A1 (en) | 2019-08-14 | 2022-03-03 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| TW202115092A (zh) | 2019-08-14 | 2021-04-16 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| BR112022002605A2 (pt) | 2019-08-14 | 2022-05-03 | Vertex Pharma | Formas cristalinas de moduladores de cftr |
| LV15575A (lv) | 2019-12-20 | 2021-06-20 | Latvijas Organiskās Sintēzes Institūts | Selenofēnhromēnu deiterēti analogi, to iegūšana un izmantošana |
| CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| US20230303589A1 (en) | 2020-08-13 | 2023-09-28 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| EP3970718A1 (en) | 2020-09-18 | 2022-03-23 | Charité - Universitätsmedizin Berlin | New medical use of cystic fibrosis transmembrane conductance regulator (cftr) modulators |
| AU2021358063A1 (en) | 2020-10-07 | 2023-05-18 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225737A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076618A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076629A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| PE20231108A1 (es) | 2020-10-07 | 2023-07-19 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica |
| WO2022076620A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2022076621A1 (en) | 2020-10-07 | 2022-04-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225763A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225748A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| BR112023006470A2 (pt) | 2020-10-07 | 2023-09-26 | Vertex Pharma | Moduladores de regulador de condutância transmembrana de fibrose cística |
| CA3204725A1 (en) | 2020-12-10 | 2022-06-16 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| WO2023150236A1 (en) | 2022-02-03 | 2023-08-10 | Vertex Pharmaceuticals Incorporated | Methods of preparing and crystalline forms of (6a,12a)-17-amino-12-methyl-6,15-bis(trifluoromethyl)-13,19-dioxa-3,4,18-triazatricyclo[ 12.3.1.12,5]nonadeca-1(18),2,4,14,16-pentaen-6-ol |
| WO2023150237A1 (en) | 2022-02-03 | 2023-08-10 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| WO2023154291A1 (en) | 2022-02-08 | 2023-08-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2023196429A1 (en) | 2022-04-06 | 2023-10-12 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| WO2023224931A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| WO2023224924A1 (en) | 2022-05-16 | 2023-11-23 | Vertex Pharmaceuticals Incorporated | Solid forms of a macrocyclic compounds as cftr modulators and their preparation |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69535592T2 (de) * | 1994-03-25 | 2008-06-12 | Isotechnika, Inc., Edmonton | Verbesserung der effektivität von arzneimitteln duren deuterierung |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| CZ20033211A3 (cs) | 2001-05-03 | 2004-09-15 | F. Hoffmann-La Roche Ag | Farmaceutická léková forma amorfního nelfinavir mesylátu |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| ME02970B (me) * | 2004-06-24 | 2018-07-20 | Vertex Pharma | Modulatori atp-vezujućih kasetnih transportera |
| AU2005292339A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| CA2635214A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
| LT1993360T (lt) | 2005-12-28 | 2017-06-12 | Vertex Pharmaceuticals Incorporated | N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma |
| WO2007134279A2 (en) | 2006-05-12 | 2007-11-22 | Vertex Pharmaceuticals Incorporated | Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| AU2008299921B2 (en) * | 2007-09-13 | 2012-03-01 | Concert Pharmaceuticals, Inc. | Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof |
| JP5575768B2 (ja) | 2008-08-13 | 2014-08-20 | 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 | 薬学的組成物およびその投与 |
| CN104311486A (zh) * | 2008-09-03 | 2015-01-28 | 泰华制药工业有限公司 | 2-羰基-1,2-二氢喹啉免疫功能调节剂 |
| MX349159B (es) * | 2011-05-18 | 2017-07-14 | Concert Pharmaceuticals Inc | Derivados deuterados de ivacaftor. |
-
2012
- 2012-05-17 MX MX2013013450A patent/MX349159B/es active IP Right Grant
- 2012-05-17 EP EP12725197.3A patent/EP2709986B1/en active Active
- 2012-05-17 DK DK17160386T patent/DK3235812T3/da active
- 2012-05-17 LT LTEP12725197.3T patent/LT2709986T/lt unknown
- 2012-05-17 PT PT171603863T patent/PT3235812T/pt unknown
- 2012-05-17 HU HUE12725197A patent/HUE032771T2/en unknown
- 2012-05-17 CA CA2834574A patent/CA2834574C/en active Active
- 2012-05-17 ES ES17160386T patent/ES2758028T3/es active Active
- 2012-05-17 ME MEP-2017-112A patent/ME02749B/me unknown
- 2012-05-17 PL PL17160386T patent/PL3235812T3/pl unknown
- 2012-05-17 EA EA201391615A patent/EA028378B1/ru unknown
- 2012-05-17 DK DK12725197.3T patent/DK2709986T3/da active
- 2012-05-17 PT PT127251973T patent/PT2709986T/pt unknown
- 2012-05-17 AU AU2012255711A patent/AU2012255711B2/en active Active
- 2012-05-17 ME MEP-2019-325A patent/ME03652B/me unknown
- 2012-05-17 WO PCT/US2012/038297 patent/WO2012158885A1/en active Application Filing
- 2012-05-17 RS RS20170601A patent/RS56096B1/sr unknown
- 2012-05-17 SI SI201230988A patent/SI2709986T1/sl unknown
- 2012-05-17 BR BR112013029240-7A patent/BR112013029240B1/pt active IP Right Grant
- 2012-05-17 EP EP17160386.3A patent/EP3235812B1/en active Active
- 2012-05-17 JP JP2014511524A patent/JP6063455B2/ja active Active
- 2012-05-17 PL PL12725197T patent/PL2709986T3/pl unknown
- 2012-05-17 RS RS20191494A patent/RS59744B1/sr unknown
- 2012-05-17 ES ES12725197.3T patent/ES2628465T3/es active Active
- 2012-05-17 SI SI201231694T patent/SI3235812T1/sl unknown
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2016
- 2016-12-16 JP JP2016243941A patent/JP2017078082A/ja active Pending
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2017
- 2017-05-19 HR HRP20170754TT patent/HRP20170754T1/hr unknown
- 2017-06-02 CY CY20171100584T patent/CY1119090T1/el unknown
- 2017-07-27 AU AU2017208313A patent/AU2017208313A1/en not_active Abandoned
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2018
- 2018-03-15 HK HK18103627.5A patent/HK1244183A1/zh unknown
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2019
- 2019-08-28 AU AU2019222862A patent/AU2019222862B2/en active Active
- 2019-11-25 HR HRP20192114TT patent/HRP20192114T1/hr unknown
- 2019-12-04 CY CY20191101275T patent/CY1122498T1/el unknown
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2021
- 2021-02-15 AU AU2021200970A patent/AU2021200970B2/en active Active
- 2021-06-08 AU AU2021203786A patent/AU2021203786B2/en active Active
Also Published As
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| AU2012255711A1 (en) | Deuterated derivatives of ivacaftor | |
| JP6146990B2 (ja) | 重水素化されたｃｆｔｒ増強物質 | |
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