CN110337294B - 作为cftr增效剂的吡咯并嘧啶 - Google Patents

作为cftr增效剂的吡咯并嘧啶 Download PDF

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Publication number
CN110337294B
CN110337294B CN201780083801.0A CN201780083801A CN110337294B CN 110337294 B CN110337294 B CN 110337294B CN 201780083801 A CN201780083801 A CN 201780083801A CN 110337294 B CN110337294 B CN 110337294B
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pyrrolo
pyrimidin
preparation
stirred
fluorophenyl
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Chinese (zh)
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CN110337294A (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
拉吉亚·阿尔德林·丹尼
克里斯托夫·沃尔夫冈·查普夫
丹尼尔·埃尔鲍姆
洛里·克里姆·加夫林
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 Therapeutics Inc
Cystic Fibrosis Foundation
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Priority to CN202211239693.0A priority Critical patent/CN115850268B/zh
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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)
CN201780083801.0A 2016-11-18 2017-11-17 作为cftr增效剂的吡咯并嘧啶 Active CN110337294B (zh)

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US201662423919P 2016-11-18 2016-11-18
US62/423,919 2016-11-18
PCT/US2017/062148 WO2018094137A1 (en) 2016-11-18 2017-11-17 Pyrrolopyrimidines as cftr potentiators

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CN110337294B true CN110337294B (zh) 2022-11-01

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CN (2) CN110337294B (enExample)
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CL (1) CL2019001334A1 (enExample)
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HUE052205T2 (hu) 2016-12-09 2021-04-28 Vertex Pharma Cisztás fibrózis transzmembrán vezetõképesség szabályzó modulátora, gyógyszerészeti készítmények, kezelési eljárások és eljárás a modulátor elõállítására
SG10201911076QA (en) 2016-12-16 2020-01-30 Cystic Fibrosis Found Bycyclic heteroaryl derivatives as cftr potentiators
BR112019025801A2 (pt) 2017-06-08 2020-07-07 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
BR112020000941A2 (pt) 2017-07-17 2020-07-21 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
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CA3078893A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
CA3085006A1 (en) 2017-12-08 2019-06-13 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
HRP20230030T1 (hr) 2018-02-15 2023-03-03 Vertex Pharmaceuticals Incorporated Makrocikli kao modulatori regulatora provodljivosti transmembrane cistične fibroze, njihovi farmaceutski pripravci, njihova uporaba u liječenju cistične fibroze, i postupak za njihovu proizvodnju
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
AR118555A1 (es) 2019-04-03 2021-10-20 Vertex Pharma Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística
BR112021024668A2 (pt) * 2019-06-10 2022-05-31 Novartis Ag Derivado de piridina e pirazina para o tratamento de fc, dpoc e bronquiectasia
JP2022541178A (ja) 2019-07-15 2022-09-22 ノバルティス アーゲー （ｓ）－３－アミノ－６－メトキシ－ｎ－（３，３，３－トリフルオロ－２－ヒドロキシ－２－メチルプロピル）－５－（トリフルオロメチル）ピコリンアミド製剤
HUE066896T2 (hu) 2019-08-14 2024-09-28 Vertex Pharma Eljárás CFTR modulátorok elõállítására
CA3150162A1 (en) 2019-08-14 2021-02-18 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
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
CN116033895A (zh) 2020-08-20 2023-04-28 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
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JP7592814B2 (ja) 2024-12-02
WO2018094137A1 (en) 2018-05-24
AU2017362350B2 (en) 2021-12-23
EP3541390C0 (en) 2024-05-01
JP2023182694A (ja) 2023-12-26
CR20190292A (es) 2019-09-03
RU2757457C2 (ru) 2021-10-18
JP6978507B2 (ja) 2021-12-08
UA125400C2 (uk) 2022-03-02
PE20200739A1 (es) 2020-07-24
KR102824092B1 (ko) 2025-06-25
ES2983686T3 (es) 2024-10-24
MX2019005822A (es) 2019-09-09
RU2021129721A (ru) 2021-11-26
IL266668A (en) 2019-07-31
CN115850268A (zh) 2023-03-28
EP3541390B1 (en) 2024-05-01
BR112019010167A2 (pt) 2019-09-17
AU2022201816B2 (en) 2024-02-15
US10494374B2 (en) 2019-12-03
NZ754085A (en) 2025-05-02
MX387203B (es) 2025-03-18
IL266668B (en) 2022-10-01
PL3541390T3 (pl) 2024-09-09
AU2022201816A8 (en) 2022-04-21
CN115850268B (zh) 2025-06-27
AU2017362350A1 (en) 2019-06-20
IL314404B1 (en) 2025-09-01
US10301315B2 (en) 2019-05-28
IL266668B2 (en) 2023-02-01
EP3541390A1 (en) 2019-09-25
US20230250100A1 (en) 2023-08-10
RU2019118623A3 (enExample) 2021-03-18
ECSP19043120A (es) 2019-08-30
JP7360434B2 (ja) 2023-10-12
KR20190110088A (ko) 2019-09-27
KR102585398B1 (ko) 2023-10-10
CN110337294A (zh) 2019-10-15
EP3541390A4 (en) 2020-06-24
CA3044050A1 (en) 2018-05-24
PH12019501098A1 (en) 2019-09-09
US20190225621A1 (en) 2019-07-25
RU2019118623A (ru) 2020-12-21
IL296279A (en) 2022-11-01
DOP2019000126A (es) 2019-08-30
IL314404A (en) 2024-09-01
AU2022201816A1 (en) 2022-04-07
KR20230146104A (ko) 2023-10-18
JP2020510668A (ja) 2020-04-09
MX2021012639A (es) 2022-10-03
US20180141954A1 (en) 2018-05-24
US20200017512A1 (en) 2020-01-16
CO2019005993A2 (es) 2019-07-31
EP4424311A2 (en) 2024-09-04
SG10202106949XA (en) 2021-07-29
JP2022024023A (ja) 2022-02-08
US20210171534A1 (en) 2021-06-10
EP4424311A3 (en) 2024-12-18
CL2019001334A1 (es) 2019-11-15

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