KR102824092B1 - Cftr 강화제로서의 피롤로피리미딘 - Google Patents

Cftr 강화제로서의 피롤로피리미딘 Download PDF

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KR102824092B1
KR102824092B1 KR1020237033420A KR20237033420A KR102824092B1 KR 102824092 B1 KR102824092 B1 KR 102824092B1 KR 1020237033420 A KR1020237033420 A KR 1020237033420A KR 20237033420 A KR20237033420 A KR 20237033420A KR 102824092 B1 KR102824092 B1 KR 102824092B1
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pyrimidin
pyrrolo
fluorophenyl
amine
triazol
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KR20230146104A (ko
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조셉 월터 스트로바흐
데이비드 크리스토퍼 림버그
존 폴 마시아스
아틀리 소라렌센
라지아 알드린 데니
크리스토프 월프갱 자프
다니엘 엘바움
로리 크림 가브린
이반 빅토로비치 에프레모브
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시스틱 파이브로시스 파운데이션
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/12Mucolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (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)
KR1020237033420A 2016-11-18 2017-11-17 Cftr 강화제로서의 피롤로피리미딘 Active KR102824092B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662423919P 2016-11-18 2016-11-18
US62/423,919 2016-11-18
KR1020197017510A KR102585398B1 (ko) 2016-11-18 2017-11-17 Cftr 강화제로서의 피롤로피리미딘
PCT/US2017/062148 WO2018094137A1 (en) 2016-11-18 2017-11-17 Pyrrolopyrimidines as cftr potentiators

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KR20230146104A KR20230146104A (ko) 2023-10-18
KR102824092B1 true KR102824092B1 (ko) 2025-06-25

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US (5) US10301315B2 (enExample)
EP (2) EP4424311A3 (enExample)
JP (3) JP6978507B2 (enExample)
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CN (2) CN115850268B (enExample)
AU (2) AU2017362350B2 (enExample)
CA (1) CA3044050A1 (enExample)
CL (1) CL2019001334A1 (enExample)
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CR (1) CR20190292A (enExample)
DO (1) DOP2019000126A (enExample)
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WO2018094137A1 (en) * 2016-11-18 2018-05-24 Cystic Fibrosis Foundation Therapeutics Inc. Pyrrolopyrimidines as cftr potentiators
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RU2753056C2 (ru) 2016-12-16 2021-08-11 Систик Файбросис Фаундейшн Бициклические гетероарильные производные в качестве стимуляторов cftr
AU2018279646B2 (en) 2017-06-08 2023-04-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CA3069226A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
ES2912657T3 (es) 2017-08-02 2022-05-26 Vertex Pharma Procesos para preparar compuestos de pirrolidina
AU2018351533B2 (en) 2017-10-19 2023-02-02 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
JP7245834B2 (ja) 2017-12-08 2023-03-24 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を作成するためのプロセス
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
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
UY38630A (es) 2019-04-03 2020-10-30 Vertex Pharma Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística
KR20220019015A (ko) * 2019-06-10 2022-02-15 노파르티스 아게 Cf, copd, 및 기관지확장증 치료를 위한 피리딘 및 피라진 유도체
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
WO2021030552A1 (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
EP4013741B1 (en) 2019-08-14 2024-04-17 Vertex Pharmaceuticals Incorporated Process of making 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
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US20200017512A1 (en) 2020-01-16
CN110337294B (zh) 2022-11-01
MX2019005822A (es) 2019-09-09
CN110337294A (zh) 2019-10-15
EP4424311A2 (en) 2024-09-04
PL3541390T3 (pl) 2024-09-09
PE20200739A1 (es) 2020-07-24
WO2018094137A1 (en) 2018-05-24
IL266668A (en) 2019-07-31
KR20190110088A (ko) 2019-09-27
AU2022201816A1 (en) 2022-04-07
KR20230146104A (ko) 2023-10-18
EP3541390A1 (en) 2019-09-25
SG10202106949XA (en) 2021-07-29
EP3541390C0 (en) 2024-05-01
CN115850268A (zh) 2023-03-28
JP7360434B2 (ja) 2023-10-12
JP2022024023A (ja) 2022-02-08
US20180141954A1 (en) 2018-05-24
JP6978507B2 (ja) 2021-12-08
US20190225621A1 (en) 2019-07-25
UA125400C2 (uk) 2022-03-02
AU2022201816B2 (en) 2024-02-15
CA3044050A1 (en) 2018-05-24
CO2019005993A2 (es) 2019-07-31
US20210171534A1 (en) 2021-06-10
DOP2019000126A (es) 2019-08-30
IL314404B1 (en) 2025-09-01
US10301315B2 (en) 2019-05-28
CN115850268B (zh) 2025-06-27
BR112019010167A2 (pt) 2019-09-17
JP7592814B2 (ja) 2024-12-02
MX2021012639A (es) 2022-10-03
IL314404A (en) 2024-09-01
IL266668B (en) 2022-10-01
JP2020510668A (ja) 2020-04-09
KR102585398B1 (ko) 2023-10-10
MX387203B (es) 2025-03-18
US20230250100A1 (en) 2023-08-10
AU2022201816A8 (en) 2022-04-21
CL2019001334A1 (es) 2019-11-15
ECSP19043120A (es) 2019-08-30
PH12019501098A1 (en) 2019-09-09
RU2019118623A3 (enExample) 2021-03-18
RU2757457C2 (ru) 2021-10-18
IL266668B2 (en) 2023-02-01
EP3541390B1 (en) 2024-05-01
JP2023182694A (ja) 2023-12-26
US10494374B2 (en) 2019-12-03
EP3541390A4 (en) 2020-06-24
ES2983686T3 (es) 2024-10-24
RU2021129721A (ru) 2021-11-26
AU2017362350A1 (en) 2019-06-20
AU2017362350B2 (en) 2021-12-23
EP4424311A3 (en) 2024-12-18
CR20190292A (es) 2019-09-03
NZ754085A (en) 2025-05-02
IL296279A (en) 2022-11-01
RU2019118623A (ru) 2020-12-21

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