CN110300589B - 作为cftr增效剂的双环异杂芳基衍生物 - Google Patents

作为cftr增效剂的双环异杂芳基衍生物 Download PDF

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Publication number
CN110300589B
CN110300589B CN201780086700.9A CN201780086700A CN110300589B CN 110300589 B CN110300589 B CN 110300589B CN 201780086700 A CN201780086700 A CN 201780086700A CN 110300589 B CN110300589 B CN 110300589B
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China
Prior art keywords
pyrimidin
pyrrolo
trifluoromethyl
fluorophenyl
triazine
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CN201780086700.9A
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Chinese (zh)
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CN110300589A (zh
Inventor
约瑟夫·沃尔特·斯特罗巴赫
大卫·克里斯多夫·林伯格
约翰·保罗·马提亚斯
阿特利·托拉伦森
詹姆斯·约翰·穆苏
拉吉亚·阿尔德林·丹尼
克里斯托夫·沃尔夫冈·查普夫
伊凡·维克托罗维奇·叶夫列莫夫
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Cystic Fibrosis Foundation
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Cystic Fibrosis Foundation
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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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201780086700.9A 2016-12-16 2017-12-14 作为cftr增效剂的双环异杂芳基衍生物 Active CN110300589B (zh)

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 (2)

Publication Number Publication Date
CN110300589A CN110300589A (zh) 2019-10-01
CN110300589B true CN110300589B (zh) 2023-03-10

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CN201780086700.9A Active CN110300589B (zh) 2016-12-16 2017-12-14 作为cftr增效剂的双环异杂芳基衍生物

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) SG10201911221RA (enExample)
WO (1) WO2018112149A1 (enExample)

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IL313498A (en) 2014-10-06 2024-08-01 Vertex Pharma Modulators of the cystic fibrosis transmembrane conductance regulator
EA201890910A1 (ru) 2015-11-25 2018-11-30 Джилид Аполло, Ллс ФУНГИЦИДНЫЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ 2,4-ДИОКСО-1,4-ДИГИДРОТИЕНО[2,3-d]ПИРИМИДИНА
BR112018010453B1 (pt) 2015-11-25 2022-06-14 Gilead Apollo, Llc Compostos triazólicos inibindores de acetil coa carboxilase (acc)
JP2019502660A (ja) 2015-11-25 2019-01-31 ギリアド アポロ， エルエルシー ピラゾールａｃｃ阻害剤およびその使用
EA201890949A1 (ru) 2015-11-25 2018-12-28 Джилид Аполло, Ллс СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ
HRP20211683T1 (hr) 2016-09-30 2022-03-04 Vertex Pharmaceuticals Incorporated Modulator transmembranskog regulatora provodljivosti cistične fibroze, farmaceutski pripravci, postupci liječenja, i postupak za pripravu modulatora
MX2021013639A (es) 2016-12-09 2022-09-30 Vertex Pharma Forma cristalina del compuesto 1, un modulador del regulador de conductancia transmembrana de fibrosis quística, procesos para su preparación, composiciones farmacéuticas del compuesto 1, y su uso en el tratamiento de fibrosis quística.
AU2018279646B2 (en) 2017-06-08 2023-04-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
AU2018304168B2 (en) 2017-07-17 2023-05-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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
WO2019079760A1 (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
LT3752510T (lt) 2018-02-15 2023-04-11 Vertex Pharmaceuticals Incorporated Makrocikliniai junginiai kaip cistinės fibrozės transmembraninio laidumo reguliatoriaus moduliatoriai, jų farmacinės kompozicijos, jų panaudojimas cistinės fibrozės gydymui ir jų gamybos būdas
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
UY38630A (es) * 2019-04-03 2020-10-30 Vertex Pharma Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística
EP3980121A1 (en) * 2019-06-10 2022-04-13 Novartis AG Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis
MX2022000549A (es) 2019-07-15 2022-02-10 Novartis Ag Formulaciones de (s)-3-amino-6-metoxi-n-(3,3,3-trifluoro-2-hidroxi -2-metilpropil)-5-(trifluorometil)picolinamida.
EP4013760A1 (en) 2019-08-14 2022-06-22 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
US11584761B2 (en) 2019-08-14 2023-02-21 Vertex Pharmaceuticals Incorporated Process of making 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
KR20230052954A (ko) 2020-08-20 2023-04-20 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 쥬니어 유니버시티 점액 과다분비를 특징으로 하는 호흡기 질환의 치료 방법
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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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DE10135815A1 (de) 2001-07-23 2003-02-06 Bayer Ag Verwendung von 2-Alkoxyphenyl-substituierten Imidazotriazinonen
TWI329112B (en) * 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
EP1957485B1 (en) 2005-12-02 2013-02-13 Bayer HealthCare, LLC Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
TW201307354A (zh) 2005-12-29 2013-02-16 Abbott Lab 蛋白質激酶抑制劑
AU2007347115A1 (en) * 2006-04-04 2008-10-23 The Regents Of The University Of California PI3 kinase antagonists
CN101917999A (zh) * 2007-11-07 2010-12-15 弗尔德里克斯制药股份有限公司 蛋白质运输的调节
EP2531187B1 (en) * 2010-02-05 2015-08-12 Adverio Pharma GmbH sGC STIMULATORS OR sGC ACTIVATORS ALONE AND IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF CYSTIC FIBROSIS
UY34484A (es) 2011-12-15 2013-07-31 Bayer Ip Gmbh Benzotienilo-pirrolotriazinas disustituidas y sus usos
US11352359B2 (en) 2013-07-02 2022-06-07 Rhizen Pharmaceuticals Ag PI3K protein kinase inhibitors
AU2017362350B2 (en) 2016-11-18 2021-12-23 Cystic Fibrosis Foundation Pyrrolopyrimidines as CFTR potentiators

Also Published As

Publication number Publication date
US20190330219A1 (en) 2019-10-31
MX2019007135A (es) 2019-11-18
WO2018112149A1 (en) 2018-06-21
US20190016727A1 (en) 2019-01-17
BR112019012335A2 (pt) 2020-03-03
SG10201911076QA (en) 2020-01-30
CA3046968A1 (en) 2018-06-21
JP7150721B2 (ja) 2022-10-11
RU2019120990A3 (enExample) 2021-01-18
AU2017378324A1 (en) 2019-06-27
MX391651B (es) 2025-03-21
US10131670B2 (en) 2018-11-20
AU2021277702B2 (en) 2023-11-30
AU2021277702A1 (en) 2021-12-23
US20190016728A1 (en) 2019-01-17
US20180170938A1 (en) 2018-06-21
RU2019120990A (ru) 2021-01-18
SG10201911221RA (en) 2020-02-27
CN110300589A (zh) 2019-10-01
EP3554506A1 (en) 2019-10-23
AU2017378324B2 (en) 2021-09-02
US10208053B2 (en) 2019-02-19
US10377762B2 (en) 2019-08-13
EP3554506A4 (en) 2020-06-10
JP2020502103A (ja) 2020-01-23
US10766904B2 (en) 2020-09-08
EP3554506B1 (en) 2021-04-28
RU2753056C2 (ru) 2021-08-11

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