ECSP19043120A - Pirrolopirimidinas como potenciadores de cftr - Google Patents
Pirrolopirimidinas como potenciadores de cftrInfo
- Publication number
- ECSP19043120A ECSP19043120A ECSENADI201943120A ECDI201943120A ECSP19043120A EC SP19043120 A ECSP19043120 A EC SP19043120A EC SENADI201943120 A ECSENADI201943120 A EC SENADI201943120A EC DI201943120 A ECDI201943120 A EC DI201943120A EC SP19043120 A ECSP19043120 A EC SP19043120A
- Authority
- EC
- Ecuador
- Prior art keywords
- cftr
- compounds
- cystic fibrosis
- pyrrolopyrimidines
- potentials
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- A61P1/10—Laxatives
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la Fórmula I, I en donde R1a, R1b, R2, R3, R4, W, Y y Z son como se describen en este documento, y a sales farmacéuticamente aceptable de los mismos. Los compuestos son potenciadores del regulador de conductancia transmembranal de la fibrosis quística (CFTR). La invención también da a conocer composiciones farmacéuticas que comprenden el compuesto opcionalmente en combinación con agentes terapéuticos adicionales, y métodos de potenciación, en mamíferos incluyendo humanos, de CFTR por la administración de los compuestos. Estos compuestos son útiles para el tratamiento de fibrosis quística (CF), asma, bronquiectasia, enfermedad pulmonar obstructiva crónica (COPD), constipación, diabetes mellitus, xeroftalmia, pancreatitis, rinosinusitis, síndrome de Sjögren y otros trastornos asociados con CFTR.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423919P | 2016-11-18 | 2016-11-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP19043120A true ECSP19043120A (es) | 2019-08-30 |
Family
ID=62144793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI201943120A ECSP19043120A (es) | 2016-11-18 | 2019-06-17 | Pirrolopirimidinas como potenciadores de cftr |
Country Status (21)
| Country | Link |
|---|---|
| US (5) | US10301315B2 (es) |
| EP (2) | EP4424311A3 (es) |
| JP (3) | JP6978507B2 (es) |
| KR (2) | KR102585398B1 (es) |
| CN (2) | CN110337294B (es) |
| AU (2) | AU2017362350B2 (es) |
| CL (1) | CL2019001334A1 (es) |
| CO (1) | CO2019005993A2 (es) |
| CR (1) | CR20190292A (es) |
| DO (1) | DOP2019000126A (es) |
| EC (1) | ECSP19043120A (es) |
| ES (1) | ES2983686T3 (es) |
| IL (3) | IL314404B2 (es) |
| MX (2) | MX387203B (es) |
| PE (1) | PE20200739A1 (es) |
| PH (1) | PH12019501098A1 (es) |
| PL (1) | PL3541390T3 (es) |
| RU (2) | RU2021129721A (es) |
| SG (1) | SG10202106949XA (es) |
| UA (1) | UA125400C2 (es) |
| WO (1) | WO2018094137A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2793148T3 (es) | 2012-01-06 | 2020-11-13 | Lundbeck La Jolla Research Center Inc | Compuestos de carbamato y métodos para fabricarlos y usarlos |
| EP3798214B1 (en) | 2014-10-06 | 2022-09-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3393465A1 (en) * | 2015-12-22 | 2018-10-31 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| SG10201913595YA (en) | 2016-09-30 | 2020-02-27 | Vertex Pharma | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| UA125400C2 (uk) * | 2016-11-18 | 2022-03-02 | Цистік Фіброзис Фаундейшн | Піролопіримідин як потенціатор трансмембранної провідності при муковісцидозі (cftr) |
| MA49235B1 (fr) | 2016-12-09 | 2021-02-26 | Vertex Pharma | Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur |
| AU2017378324B2 (en) * | 2016-12-16 | 2021-09-02 | Cystic Fibrosis Foundation | Bycyclic heteroaryl derivatives as CFTR potentiators |
| EP3634402B1 (en) | 2017-06-08 | 2026-01-21 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
| TWI799435B (zh) | 2017-08-02 | 2023-04-21 | 美商維泰克斯製藥公司 | 製備化合物之製程 |
| IL273831B2 (en) | 2017-10-19 | 2024-10-01 | Vertex Pharma | Crystalline forms and compositions of cftr modulators |
| CN111757874B (zh) | 2017-12-08 | 2024-03-08 | 弗特克斯药品有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| 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 |
| EP3752510B1 (en) | 2018-02-15 | 2022-12-07 | Vertex Pharmaceuticals Incorporated | Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them |
| US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| 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 |
| KR20220019015A (ko) * | 2019-06-10 | 2022-02-15 | 노파르티스 아게 | Cf, copd, 및 기관지확장증 치료를 위한 피리딘 및 피라진 유도체 |
| TW202116312A (zh) | 2019-07-15 | 2021-05-01 | 瑞士商諾華公司 | （ｓ）—３—胺基—６—甲氧基—ｎ—（３，３，３—三氟—２—羥基—２—甲基丙基）—５—（三氟甲基）吡啶甲醯胺配製物 |
| 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 |
| 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 |
| KR20220064366A (ko) | 2019-08-14 | 2022-05-18 | 버텍스 파마슈티칼스 인코포레이티드 | Cftr 조절제의 결정질 형태 |
| CN111138439B (zh) * | 2020-01-17 | 2021-06-25 | 厦门大学 | 氟代吡咯并嘧啶类化合物及其制备方法和应用 |
| US20230192700A1 (en) | 2020-03-06 | 2023-06-22 | Bayer Aktiengesellschaft | Pyrazolopyrazines acting on cancers via inhibition of cdk12 |
| CA3188787A1 (en) | 2020-08-13 | 2022-02-17 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| BR112023002651A2 (pt) | 2020-08-20 | 2023-04-04 | Univ Leland Stanford Junior | Métodos de tratamento de doenças respiratórias definidas por hipersecreção de muco |
| CA3204725A1 (en) | 2020-12-10 | 2022-06-16 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| TW202425990A (zh) * | 2022-11-02 | 2024-07-01 | 南韓商日東製藥股份有限公司 | 包含ｃｆｔｒ調節劑化合物之點眼用組成物 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6765008B1 (en) * | 1992-12-17 | 2004-07-20 | Pfizer Inc | Pyrrolopyrimidines as CRF antagonists |
| IL149462A0 (en) | 2001-05-09 | 2002-11-10 | Warner Lambert Co | Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor |
| WO2002096867A2 (en) | 2001-05-30 | 2002-12-05 | Lg Biomedical Institute | Inhibitors of protein kinase for the treatment of disease |
| US20050008640A1 (en) | 2003-04-23 | 2005-01-13 | Wendy Waegell | Method of treating transplant rejection |
| JP2007520559A (ja) * | 2004-02-03 | 2007-07-26 | アボット・ラボラトリーズ | 治療薬としてのアミノベンゾオキサゾール類 |
| WO2007079164A2 (en) * | 2005-12-29 | 2007-07-12 | Abbott Laboratories | Protein kinase inhibitors |
| BRPI0708779A2 (pt) * | 2006-03-11 | 2011-06-14 | Vernalis R & D | derivados de pirrolopirimidina utilizados como inibidores de hsp90 |
| KR101499783B1 (ko) * | 2006-04-04 | 2015-03-09 | 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 | 키나제 길항물질 |
| AU2008323694A1 (en) * | 2007-11-07 | 2009-05-14 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
| DK2385832T3 (en) | 2009-01-08 | 2015-09-21 | Curis Inc | Phosphoinositid-3-kinase-inhibitorer med en zink-bindingsdel |
| US20130123281A1 (en) | 2011-11-11 | 2013-05-16 | Beta Cat Pharmaceuticals, Llc | Compositions and Methods for Inhibition of TBL-1 Binding to Disease-Associated Molecules |
| US8828998B2 (en) * | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| WO2014060431A1 (en) * | 2012-10-16 | 2014-04-24 | Almirall, S.A. | Pyrrolotriazinone derivatives as pi3k inhibitors |
| WO2015091532A1 (en) * | 2013-12-19 | 2015-06-25 | Almirall, S.A. | Pyrrolopyrimidine derivatives as pi3k inhibitors |
| UA125400C2 (uk) | 2016-11-18 | 2022-03-02 | Цистік Фіброзис Фаундейшн | Піролопіримідин як потенціатор трансмембранної провідності при муковісцидозі (cftr) |
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2017
- 2017-11-17 UA UAA201906838A patent/UA125400C2/uk unknown
- 2017-11-17 US US15/815,809 patent/US10301315B2/en active Active
- 2017-11-17 CN CN201780083801.0A patent/CN110337294B/zh active Active
- 2017-11-17 KR KR1020197017510A patent/KR102585398B1/ko active Active
- 2017-11-17 EP EP24170395.8A patent/EP4424311A3/en active Pending
- 2017-11-17 AU AU2017362350A patent/AU2017362350B2/en active Active
- 2017-11-17 PL PL17872726.9T patent/PL3541390T3/pl unknown
- 2017-11-17 WO PCT/US2017/062148 patent/WO2018094137A1/en not_active Ceased
- 2017-11-17 JP JP2019547579A patent/JP6978507B2/ja active Active
- 2017-11-17 ES ES17872726T patent/ES2983686T3/es active Active
- 2017-11-17 MX MX2019005822A patent/MX387203B/es unknown
- 2017-11-17 CR CR20190292A patent/CR20190292A/es unknown
- 2017-11-17 IL IL314404A patent/IL314404B2/en unknown
- 2017-11-17 EP EP17872726.9A patent/EP3541390B1/en active Active
- 2017-11-17 IL IL296279A patent/IL296279A/en unknown
- 2017-11-17 RU RU2021129721A patent/RU2021129721A/ru unknown
- 2017-11-17 PE PE2019001045A patent/PE20200739A1/es unknown
- 2017-11-17 KR KR1020237033420A patent/KR102824092B1/ko active Active
- 2017-11-17 SG SG10202106949XA patent/SG10202106949XA/en unknown
- 2017-11-17 MX MX2021012639A patent/MX2021012639A/es unknown
- 2017-11-17 CN CN202211239693.0A patent/CN115850268B/zh active Active
- 2017-11-17 RU RU2019118623A patent/RU2757457C2/ru active
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2019
- 2019-04-05 US US16/377,005 patent/US10494374B2/en active Active
- 2019-05-15 IL IL266668A patent/IL266668B2/en unknown
- 2019-05-16 CL CL2019001334A patent/CL2019001334A1/es unknown
- 2019-05-16 PH PH12019501098A patent/PH12019501098A1/en unknown
- 2019-05-17 DO DO2019000126A patent/DOP2019000126A/es unknown
- 2019-06-07 CO CONC2019/0005993A patent/CO2019005993A2/es unknown
- 2019-06-17 EC ECSENADI201943120A patent/ECSP19043120A/es unknown
- 2019-09-20 US US16/578,277 patent/US20200017512A1/en not_active Abandoned
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2021
- 2021-02-18 US US17/179,062 patent/US20210171534A1/en not_active Abandoned
- 2021-11-10 JP JP2021183048A patent/JP7360434B2/ja active Active
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2022
- 2022-03-16 AU AU2022201816A patent/AU2022201816B2/en active Active
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2023
- 2023-04-13 US US18/134,455 patent/US20230250100A1/en active Pending
- 2023-09-29 JP JP2023169299A patent/JP7592814B2/ja active Active
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