RU2753056C2 - Бициклические гетероарильные производные в качестве стимуляторов cftr - Google Patents

Бициклические гетероарильные производные в качестве стимуляторов cftr Download PDF

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Publication number
RU2753056C2
RU2753056C2 RU2019120990A RU2019120990A RU2753056C2 RU 2753056 C2 RU2753056 C2 RU 2753056C2 RU 2019120990 A RU2019120990 A RU 2019120990A RU 2019120990 A RU2019120990 A RU 2019120990A RU 2753056 C2 RU2753056 C2 RU 2753056C2
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RU
Russia
Prior art keywords
pyrimidin
pyrrolo
trifluoromethyl
triazine
amino
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RU2019120990A
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English (en)
Russian (ru)
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RU2019120990A (ru
RU2019120990A3 (enExample
Inventor
Джозеф Уолтер СТРОНБЕЧ
Дэвид Кристофер ЛИМБУРГ
Джон Пол МЭТИАС
Этли ТОРАРЕНСЕН
Джеймс Джон МУССО
Рейджиах Алдрин ДЕННИ
Кристоф Вольфганг ЦАПФ
Иван Викторович Ефремов
Original Assignee
Систик Файбросис Фаундейшн
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Publication of RU2019120990A3 publication Critical patent/RU2019120990A3/ru
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    • 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2019120990A 2016-12-16 2017-12-14 Бициклические гетероарильные производные в качестве стимуляторов cftr RU2753056C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662435253P 2016-12-16 2016-12-16
US62/435,253 2016-12-16
PCT/US2017/066317 WO2018112149A1 (en) 2016-12-16 2017-12-14 Bycyclic heteroaryl derivatives as cftr potentiators

Publications (3)

Publication Number Publication Date
RU2019120990A RU2019120990A (ru) 2021-01-18
RU2019120990A3 RU2019120990A3 (enExample) 2021-01-18
RU2753056C2 true RU2753056C2 (ru) 2021-08-11

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RU2019120990A RU2753056C2 (ru) 2016-12-16 2017-12-14 Бициклические гетероарильные производные в качестве стимуляторов cftr

Country Status (10)

Country Link
US (4) US10131670B2 (enExample)
EP (1) EP3554506B1 (enExample)
JP (1) JP7150721B2 (enExample)
CN (1) CN110300589B (enExample)
AU (2) AU2017378324B2 (enExample)
CA (1) CA3046968A1 (enExample)
MX (1) MX391651B (enExample)
RU (1) RU2753056C2 (enExample)
SG (2) SG10201911076QA (enExample)
WO (1) WO2018112149A1 (enExample)

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US20170166582A1 (en) 2015-11-25 2017-06-15 Gilead Apollo, Llc Pyrazole acc inhibitors and uses thereof
CN108347939B (zh) 2015-11-25 2021-09-28 吉利德阿波罗公司 含有2,4-二氧代-1,4-二氢噻吩并[2,3-d]嘧啶的衍生物的杀真菌组合物
EP3380478B1 (en) 2015-11-25 2020-12-23 Gilead Apollo, LLC Ester acc inhibitors and uses thereof
PL3380479T3 (pl) 2015-11-25 2023-05-08 Gilead Apollo, Llc Triazolowe inhibitory acc i ich zastosowania
GEP20217329B (en) 2016-09-30 2021-12-10 Vertex Pharma Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
SG10202106949XA (en) 2016-11-18 2021-07-29 Cystic Fibrosis Found Pyrrolopyrimidines as cftr potentiators
EA202192783A1 (ru) 2016-12-09 2022-02-24 Вертекс Фармасьютикалз Инкорпорейтед Модулятор регулятора трансмембранной проводимости при муковисцидозе, фармацевтические композиции, способы лечения и способ получения указанного модулятора
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
IL272032B2 (en) 2017-07-17 2026-04-01 Vertex Pharma Combination therapy for the treatment of cystic fibrosis including N-(1,3-DIMETHYLPYRAZOL-4-YL)SULFONYL-6-[3-(3,3,3-TRIFLUORO-2,2- DIMETHYL-PROPOXY)PYRAZOL-1-YL]-2-[(4S)-2,2,4- TRIMETHYLPYRROLIDIN-1-YL]PYRIDINE-3-CARBOXAMIDE and
MA49752A (fr) 2017-08-02 2021-04-21 Vertex Pharma Procédés de préparation de composés de pyrrolidine
CA3078893A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
KR102716244B1 (ko) 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
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
RS64018B1 (sr) 2018-02-15 2023-03-31 Vertex Pharma Makrocikli kao modulatori transmembranskog regulatora provodnosti cistične fibroze, njihove farmaceutske kompozicije, njihova upotreba u lečenju cistične fibroze i proces njihove izrade
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela 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
US20200383960A1 (en) * 2019-06-10 2020-12-10 Novartis Ag Pyridine and Pyrazine derivative for the Treatment of CF, COPD, and Bronchiectasis
WO2021009695A1 (en) 2019-07-15 2021-01-21 Novartis Ag Formulations of (s)-3-amino-6-methoxy-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide
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
US11873300B2 (en) 2019-08-14 2024-01-16 Vertex Pharmaceuticals Incorporated Crystalline forms of CFTR modulators
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
MX2022012558A (es) * 2020-04-07 2023-02-22 iTeos Belgium SA Derivados de diaminas macrocíclicas como inhibidores de ent para el tratamiento de cánceres y combinación de estos con antagonistas del receptor de adenosina.
WO2022036060A1 (en) 2020-08-13 2022-02-17 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
CN122537531A (zh) 2020-08-20 2026-08-11 小利兰·斯坦福大学托管委员会 用于治疗以黏液分泌过多为特征的呼吸系统疾病的方法
US12612416B2 (en) 2020-10-07 2026-04-28 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023006770A (es) 2020-12-10 2023-08-14 Vertex Pharma Metodos de tratamiento para fibrosis quistica.
CN112876524B (zh) * 2021-01-26 2022-10-28 上海法默生物科技有限公司 一种瑞德西韦中间体的制备方法

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WO2007079164A2 (en) * 2005-12-29 2007-07-12 Abbott Laboratories Protein kinase inhibitors
RU2331642C2 (ru) * 2002-07-19 2008-08-20 Бристол-Маерс Сквибб Компани Новые ингибиторы киназ
EA201070572A1 (ru) * 2007-11-07 2010-12-30 Фолдркс Фармасьютикалз, Инк. Модуляция транспорта белков
EA019961B1 (ru) * 2006-04-04 2014-07-30 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Антагонисты киназы
EA201400707A1 (ru) * 2011-12-15 2014-11-28 Байер Фарма Акциенгезельшафт Дизамещенные бензотиенил-пирролотриазины и их применение в качестве ингибиторов киназы рфрф
EA025177B1 (ru) * 2010-02-05 2016-11-30 Адверио Фарма Гмбх СТИМУЛЯТОР sGC ИЛИ АКТИВАТОР sGC, ПРИМЕНЯЕМЫЙ ДЛЯ ЛЕЧЕНИЯ КИСТОЗНОГО ФИБРОЗА ОТДЕЛЬНО ИЛИ В КОМБИНАЦИИ С ИНГИБИТОРОМ PDE5

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WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
BRPI0619146A2 (pt) * 2005-12-02 2011-09-13 Bayer Pharmaceuticals Corp derivados de 4-amino-pirroltriazina substituìda úteis no tratamento de disordens e doenças hiperproliferativas associadas com angiogênesis
ES2672018T3 (es) * 2013-07-02 2018-06-12 Rhizen Pharmaceuticals S.A. Inhibidores de proteína cinasa PI3K, particularmente inhibidores delta y/o gamma
SG10202106949XA (en) * 2016-11-18 2021-07-29 Cystic Fibrosis Found Pyrrolopyrimidines as cftr potentiators

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Publication number Priority date Publication date Assignee Title
RU2331642C2 (ru) * 2002-07-19 2008-08-20 Бристол-Маерс Сквибб Компани Новые ингибиторы киназ
WO2005007085A2 (en) * 2003-06-20 2005-01-27 The Regents Of The University Of California Pyrazolo pyrimidine derivatives and methods of use thereof
WO2007079164A2 (en) * 2005-12-29 2007-07-12 Abbott Laboratories Protein kinase inhibitors
EA019961B1 (ru) * 2006-04-04 2014-07-30 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Антагонисты киназы
EA201070572A1 (ru) * 2007-11-07 2010-12-30 Фолдркс Фармасьютикалз, Инк. Модуляция транспорта белков
EA025177B1 (ru) * 2010-02-05 2016-11-30 Адверио Фарма Гмбх СТИМУЛЯТОР sGC ИЛИ АКТИВАТОР sGC, ПРИМЕНЯЕМЫЙ ДЛЯ ЛЕЧЕНИЯ КИСТОЗНОГО ФИБРОЗА ОТДЕЛЬНО ИЛИ В КОМБИНАЦИИ С ИНГИБИТОРОМ PDE5
EA201400707A1 (ru) * 2011-12-15 2014-11-28 Байер Фарма Акциенгезельшафт Дизамещенные бензотиенил-пирролотриазины и их применение в качестве ингибиторов киназы рфрф

Also Published As

Publication number Publication date
SG10201911221RA (en) 2020-02-27
RU2019120990A (ru) 2021-01-18
AU2021277702B2 (en) 2023-11-30
EP3554506A1 (en) 2019-10-23
CA3046968A1 (en) 2018-06-21
AU2017378324A1 (en) 2019-06-27
AU2021277702A1 (en) 2021-12-23
SG10201911076QA (en) 2020-01-30
BR112019012335A2 (pt) 2020-03-03
US20180170938A1 (en) 2018-06-21
MX391651B (es) 2025-03-21
US10131670B2 (en) 2018-11-20
EP3554506A4 (en) 2020-06-10
US20190016727A1 (en) 2019-01-17
US20190330219A1 (en) 2019-10-31
US10766904B2 (en) 2020-09-08
US10208053B2 (en) 2019-02-19
AU2017378324B2 (en) 2021-09-02
CN110300589B (zh) 2023-03-10
MX2019007135A (es) 2019-11-18
US10377762B2 (en) 2019-08-13
JP2020502103A (ja) 2020-01-23
EP3554506B1 (en) 2021-04-28
RU2019120990A3 (enExample) 2021-01-18
CN110300589A (zh) 2019-10-01
US20190016728A1 (en) 2019-01-17
WO2018112149A1 (en) 2018-06-21
JP7150721B2 (ja) 2022-10-11

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