CR20190292A - Pirrolopirimidinas como potenciadores de cftr - Google Patents
Pirrolopirimidinas como potenciadores de cftrInfo
- Publication number
- CR20190292A CR20190292A CR20190292A CR20190292A CR20190292A CR 20190292 A CR20190292 A CR 20190292A CR 20190292 A CR20190292 A CR 20190292A CR 20190292 A CR20190292 A CR 20190292A CR 20190292 A CR20190292 A CR 20190292A
- Authority
- CR
- Costa Rica
- Prior art keywords
- compounds
- cftr
- cystic fibrosis
- rhinosinusitis
- bronchiectasis
- Prior art date
Links
Classifications
-
- 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
-
- 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
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- 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)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Otolaryngology (AREA)
- Transplantation (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, 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.The present invention relates to compounds of Formula (I), wherein R1 a, R1 b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjogren's Syndrome, and other CFTR associated disorders.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423919P | 2016-11-18 | 2016-11-18 | |
| PCT/US2017/062148 WO2018094137A1 (en) | 2016-11-18 | 2017-11-17 | Pyrrolopyrimidines as cftr potentiators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20190292A true CR20190292A (es) | 2019-09-03 |
Family
ID=62144793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190292A CR20190292A (es) | 2016-11-18 | 2017-11-17 | Pirrolopirimidinas como potenciadores de cftr |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US10301315B2 (es) |
| EP (2) | EP4424311A3 (es) |
| JP (3) | JP6978507B2 (es) |
| KR (2) | KR102824092B1 (es) |
| CN (2) | CN115850268B (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 |
|---|---|---|---|---|
| PE20141702A1 (es) | 2012-01-06 | 2014-11-19 | Abide Therapeutics Inc | Compuestos de carbamato y preparacion y uso de los mismos |
| MA41051B1 (fr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose |
| US20180369209A1 (en) * | 2015-12-22 | 2018-12-27 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| CN109803962B (zh) | 2016-09-30 | 2022-04-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物 |
| MX387203B (es) * | 2016-11-18 | 2025-03-18 | Cystic Fibrosis Found | Pirrolopirimidinas como potenciadores de cftr. |
| MD3551622T2 (ro) | 2016-12-09 | 2021-03-31 | Vertex Pharma | Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului |
| SG10201911076QA (en) | 2016-12-16 | 2020-01-30 | Cystic Fibrosis Found | Bycyclic heteroaryl derivatives as cftr potentiators |
| US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| MA49631A (fr) | 2017-07-17 | 2020-05-27 | Vertex Pharma | Méthodes de traitement de la fibrose kystique |
| JP7121794B2 (ja) | 2017-08-02 | 2022-08-18 | 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 | ピロリジン化合物を調製するためのプロセス |
| WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
| EP3720849A2 (en) | 2017-12-08 | 2020-10-14 | 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 |
| JP7214743B2 (ja) | 2018-02-15 | 2023-01-30 | 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モジュレーターとしての大環状分子、それらの医薬組成物、嚢胞性線維症の治療におけるそれらの使用、及びそれらの製造方法 |
| 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 |
| UY38630A (es) | 2019-04-03 | 2020-10-30 | Vertex Pharma | Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| WO2020250116A1 (en) * | 2019-06-10 | 2020-12-17 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis |
| CN114007616A (zh) | 2019-07-15 | 2022-02-01 | 诺华股份有限公司 | (s)-3-氨基-6-甲氧基-n-(3，3，3-三氟-2-羟基-2-甲基丙基)-5-(三氟甲基)吡啶甲酰胺的配制品 |
| 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 |
| WO2021030552A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| 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 |
| WO2021176049A1 (en) | 2020-03-06 | 2021-09-10 | Bayer Aktiengesellschaft | Pyrazolopyrazines acting on cancers via inhibition of cdk12 |
| IL300413A (en) | 2020-08-13 | 2023-04-01 | Vertex Pharma | Crystal forms of CFTR modulators |
| WO2022040447A2 (en) | 2020-08-20 | 2022-02-24 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for treating respiratory diseases characterized by mucus hypersecretion |
| KR20230118123A (ko) | 2020-12-10 | 2023-08-10 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 치료 방법 |
| 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 |
|---|---|---|---|---|
| ATE177101T1 (de) * | 1992-12-17 | 1999-03-15 | Pfizer | Pyrrolopyrimidine als crf antagonisten |
| 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 |
| WO2004100868A2 (en) | 2003-04-23 | 2004-11-25 | Abbott Laboratories | 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 |
| TW200801008A (en) * | 2005-12-29 | 2008-01-01 | Abbott Lab | Protein kinase inhibitors |
| EA200801968A1 (ru) * | 2006-03-11 | 2009-02-27 | Вернэлис (Р&Д) Лтд. | Пирролопиримидиновые производные, используемые в качестве ингибиторов hsp90 |
| WO2007114926A2 (en) * | 2006-04-04 | 2007-10-11 | The Regents Of The University Of California | Kinase antagonists |
| US20100331297A1 (en) * | 2007-11-07 | 2010-12-30 | Foldrx Pharmaceuticals, Inc. | Modulation of protein trafficking |
| AU2010203512C1 (en) * | 2009-01-08 | 2013-10-17 | Curis, Inc. | Phosphoinositide 3-kinase inhibitors with a zinc binding moiety |
| 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 |
| MX387203B (es) * | 2016-11-18 | 2025-03-18 | Cystic Fibrosis Found | Pirrolopirimidinas como potenciadores de cftr. |
-
2017
- 2017-11-17 MX MX2019005822A patent/MX387203B/es unknown
- 2017-11-17 RU RU2021129721A patent/RU2021129721A/ru unknown
- 2017-11-17 MX MX2021012639A patent/MX2021012639A/es unknown
- 2017-11-17 RU RU2019118623A patent/RU2757457C2/ru active
- 2017-11-17 ES ES17872726T patent/ES2983686T3/es active Active
- 2017-11-17 CN CN202211239693.0A patent/CN115850268B/zh active Active
- 2017-11-17 WO PCT/US2017/062148 patent/WO2018094137A1/en not_active Ceased
- 2017-11-17 SG SG10202106949XA patent/SG10202106949XA/en unknown
- 2017-11-17 CN CN201780083801.0A patent/CN110337294B/zh active Active
- 2017-11-17 KR KR1020237033420A patent/KR102824092B1/ko active Active
- 2017-11-17 UA UAA201906838A patent/UA125400C2/uk unknown
- 2017-11-17 US US15/815,809 patent/US10301315B2/en active Active
- 2017-11-17 EP EP24170395.8A patent/EP4424311A3/en active Pending
- 2017-11-17 KR KR1020197017510A patent/KR102585398B1/ko active Active
- 2017-11-17 CR CR20190292A patent/CR20190292A/es unknown
- 2017-11-17 IL IL314404A patent/IL314404B2/en unknown
- 2017-11-17 PL PL17872726.9T patent/PL3541390T3/pl unknown
- 2017-11-17 AU AU2017362350A patent/AU2017362350B2/en active Active
- 2017-11-17 IL IL296279A patent/IL296279A/en unknown
- 2017-11-17 JP JP2019547579A patent/JP6978507B2/ja active Active
- 2017-11-17 EP EP17872726.9A patent/EP3541390B1/en active Active
- 2017-11-17 PE PE2019001045A patent/PE20200739A1/es unknown
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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 PH PH12019501098A patent/PH12019501098A1/en unknown
- 2019-05-16 CL CL2019001334A patent/CL2019001334A1/es 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
-
2023
- 2023-09-29 JP JP2023169299A patent/JP7592814B2/ja active Active
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