AR108203A1 - Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística) - Google Patents
Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística)Info
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- AR108203A1 AR108203A1 ARP170100899A ARP170100899A AR108203A1 AR 108203 A1 AR108203 A1 AR 108203A1 AR P170100899 A ARP170100899 A AR P170100899A AR P170100899 A ARP170100899 A AR P170100899A AR 108203 A1 AR108203 A1 AR 108203A1
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- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/695—Silicon compounds
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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Abstract
Reivindicación 1: Un compuesto caracterizado porque se selecciona entre N-(2,4-di-tert-butil-5-hidroxifenil)-4-oxo-1,4-dihidroquinolin-3-carboxamida y una sal farmacéuticamente aceptable del mismo, donde al menos un átomo de carbono se reemplaza por silicio. Reivindicación 9: Un compuesto caracterizado porque se representa por medio de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde: X¹ se selecciona entre el grupo que consiste en -Si(R³)₃, -C(CY³)₃, hidrógeno, halógeno, C₁₋₃alquilo opcionalmente sustituido con uno o más halógenos, C₃₋₆cicloalquilo, y heterociclilo monocíclico saturado de 4 - 6 miembros; donde C₃₋₆cicloalquilo y heterociclilo monocíclico saturado de 4 - 6 miembros puede estar opcionalmente sustituido con uno, dos, tres o más sustituyentes seleccionados en forma independiente en cada caso entre R¹¹; X² se selecciona entre el grupo que consiste en -Si(R³)₃ y -C(CY³)₃; donde al menos uno de X¹ o X² es -Si(R³)₃; R³ se selecciona en forma independiente en cada caso entre el grupo que consiste en hidroxilo, C₁₋₄alquilo, C₁₋₄alcoxi, y fenilo, donde C₁₋₄alquilo, C₁₋₄alcoxi, y fenilo puede estar opcionalmente sustituido con uno, dos, tres o más átomos de deuterio; o dos grupos R³ junto con el silicio al cual están unidos forman un ciclosilano saturado de 4 - 6 miembros; Y se selecciona en forma independiente en cada caso entre el grupo que consiste en hidrógeno y deuterio; y R¹¹ se selecciona en forma independiente en cada caso entre el grupo que consiste en hidrógeno, halógeno, hidroxilo, ciano, y C₁₋₆alquilo; donde C₁₋₆alquilo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados en forma independiente en cada caso entre el grupo que consiste en halógeno, hidroxilo, y C₁₋₆alcoxi. Reivindicación 16: Una composición farmacéutica caracterizada porque comprende un compuesto de cualquiera de las reivindicaciones 1 a 15 y un excipiente farmacéuticamente aceptable. Reivindicación 21: El método de cualquiera de las reivindicaciones 18 - 20, caracterizado porque el sujeto sufre una enfermedad asociada con una actividad del CFTR disminuida. Reivindicación 27: Un método para tratar fibrosis quística en un paciente que lo necesite, caracterizado porque comprende administrar una cantidad eficaz de un compuesto de cualquiera de las reivindicaciones 1 - 15.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319439P | 2016-04-07 | 2016-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR108203A1 true AR108203A1 (es) | 2018-07-25 |
Family
ID=58549338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170100899A AR108203A1 (es) | 2016-04-07 | 2017-04-07 | Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística) |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US10662207B2 (es) |
| EP (1) | EP3440057B1 (es) |
| JP (1) | JP7061076B2 (es) |
| KR (1) | KR102448404B1 (es) |
| CN (1) | CN109563047A (es) |
| AR (1) | AR108203A1 (es) |
| AU (1) | AU2017248253B2 (es) |
| BR (1) | BR112018070747B1 (es) |
| CA (1) | CA3019663C (es) |
| IL (1) | IL262030B (es) |
| MA (1) | MA43775A (es) |
| MX (1) | MX386698B (es) |
| NZ (1) | NZ746793A (es) |
| SA (1) | SA518400164B1 (es) |
| SG (1) | SG11201808682XA (es) |
| WO (1) | WO2017177124A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT202000540T1 (it) | 2014-10-06 | 2020-11-10 | Vertex Pharma | Modulatori di regolatore di conduttanza transmembrana di fibrosi cistica |
| WO2017019589A1 (en) | 2015-07-24 | 2017-02-02 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| SG11201802798WA (en) | 2015-10-06 | 2018-05-30 | Proteostasis Therapeutics Inc | Compounds, compositions, and methods for modulating cftr |
| US10662207B2 (en) | 2016-04-07 | 2020-05-26 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating CFTR |
| ES2954658T3 (es) | 2016-06-21 | 2023-11-23 | Proteostasis Therapeutics Inc | Compuestos, composiciones y procedimientos para aumentar la actividad de CFTR |
| JOP20190042B1 (ar) | 2016-09-30 | 2021-08-17 | Vertex Pharma | مُعدِّل لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل |
| UY37513A (es) | 2016-12-09 | 2018-07-31 | Vertex Pharma | Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador |
| US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| US20200289482A1 (en) * | 2017-06-21 | 2020-09-17 | The Johns Hopkins University | Cystic fibrosis transmembrane conductance regulator modulators for treating autosomal dominant polycystic kidney disease |
| BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
| AU2018309043B2 (en) | 2017-08-02 | 2022-03-31 | Vertex Pharmaceuticals Incorporated | Processes for preparing pyrrolidine compounds |
| EP3691638B1 (en) * | 2017-10-06 | 2024-12-11 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing cftr activity |
| CA3078893A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | Crystalline forms and compositions of cftr modulators |
| US11465985B2 (en) | 2017-12-08 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| DK3752510T3 (da) | 2018-02-15 | 2023-01-16 | Vertex Pharma | Makrocyklusser som modulatorer af cystisk fibrose transmembrankonduktansregulator, farmaceutiske sammensætninger deraf, deres anvendelse i behandlingen af cystisk fibrose og fremgangsmåde til fremstilling deraf |
| WO2019195739A1 (en) | 2018-04-05 | 2019-10-10 | Alexander Russell Abela | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3774825A1 (en) | 2018-04-13 | 2021-02-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| JP7551087B2 (ja) | 2018-06-27 | 2024-09-17 | キネタ， インコーポレイテッド | プロテアソーム活性増強化合物 |
| CN109663129B (zh) * | 2019-02-27 | 2021-05-11 | 四川大学华西第二医院 | 扩张型心肌病治疗药物及其应用 |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| EP4013760A1 (en) | 2019-08-14 | 2022-06-22 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 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 |
| TWI899097B (zh) | 2019-08-14 | 2025-10-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| AU2021397294A1 (en) | 2020-12-10 | 2023-07-06 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| CN116425642B (zh) * | 2023-04-06 | 2025-06-10 | 浙江科聚生物医药有限公司 | 2-甲氧基-4-氟-5-胺基苯酚的制备方法 |
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| NZ746793A (en) | 2022-10-28 |
| JP2019513741A (ja) | 2019-05-30 |
| US20240368198A1 (en) | 2024-11-07 |
| JP7061076B2 (ja) | 2022-04-27 |
| CN109563047A (zh) | 2019-04-02 |
| US20210061823A1 (en) | 2021-03-04 |
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| BR112018070747A2 (pt) | 2019-06-18 |
| CA3019663A1 (en) | 2017-10-12 |
| EP3440057B1 (en) | 2021-09-22 |
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| US10662207B2 (en) | 2020-05-26 |
| AU2017248253B2 (en) | 2021-07-29 |
| MX2018012331A (es) | 2019-05-23 |
| US20240109922A1 (en) | 2024-04-04 |
| US11248010B2 (en) | 2022-02-15 |
| US20190153000A1 (en) | 2019-05-23 |
| KR102448404B1 (ko) | 2022-09-27 |
| MA43775A (fr) | 2021-05-05 |
| CA3019663C (en) | 2024-09-24 |
| RU2018137683A (ru) | 2020-05-12 |
| WO2017177124A1 (en) | 2017-10-12 |
| BR112018070747B1 (pt) | 2024-01-09 |
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| SA518400164B1 (ar) | 2022-05-08 |
| RU2018137683A3 (es) | 2020-05-18 |
| AU2017248253A1 (en) | 2018-10-18 |
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