JP7150721B2 - Cftr増強物質としての二環式ヘテロアリール誘導体 - Google Patents

Cftr増強物質としての二環式ヘテロアリール誘導体 Download PDF

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JP7150721B2
JP7150721B2 JP2019531417A JP2019531417A JP7150721B2 JP 7150721 B2 JP7150721 B2 JP 7150721B2 JP 2019531417 A JP2019531417 A JP 2019531417A JP 2019531417 A JP2019531417 A JP 2019531417A JP 7150721 B2 JP7150721 B2 JP 7150721B2
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pyrrolo
trifluoromethyl
fluorophenyl
pyrimidin
triazine
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JP2020502103A5 (2
JP2020502103A (ja
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ジョセフ, ウォルター ストローバッハ,
デイビッド, クリストファー リンブルグ,
ジョン, ポール マティアス,
アトリ トーラレンセン,
ジェイムズ, ジョン ムーソー,
ラジア, アルドリン デニー,
クリストフ, ウルフギャング ツァップ,
イヴァン, ヴィクトロヴィッチ エフレモフ,
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システィック・ファイブロシス・ファンデーション
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    • 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
    • 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
    • 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
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs 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)
JP2019531417A 2016-12-16 2017-12-14 Cftr増強物質としての二環式ヘテロアリール誘導体 Active JP7150721B2 (ja)

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
JP2020502103A JP2020502103A (ja) 2020-01-23
JP2020502103A5 JP2020502103A5 (2) 2022-05-24
JP7150721B2 true JP7150721B2 (ja) 2022-10-11

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JP2019531417A Active JP7150721B2 (ja) 2016-12-16 2017-12-14 Cftr増強物質としての二環式ヘテロアリール誘導体

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

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BR112018009212B1 (pt) 2015-11-25 2022-06-14 Gilead Apollo, Llc Método para controlar patógenos fúngicos agrícolas
PL3380479T3 (pl) 2015-11-25 2023-05-08 Gilead Apollo, Llc Triazolowe inhibitory acc i ich zastosowania
AU2016361412A1 (en) 2015-11-25 2018-05-24 Gilead Apollo, Llc Pyrazole ACC inhibitors and uses thereof
EA201890949A1 (ru) 2015-11-25 2018-12-28 Джилид Аполло, Ллс СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ
SI3519401T1 (sl) 2016-09-30 2022-01-31 Vertex Pharmaceuticals Incorporated Modulator regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki, postopki zdravljenja in proces za izdelavo modulatorja
AU2017362350B2 (en) 2016-11-18 2021-12-23 Cystic Fibrosis Foundation Pyrrolopyrimidines as CFTR potentiators
CN110267948B (zh) 2016-12-09 2023-12-08 弗特克斯药品有限公司 囊性纤维化跨膜传导调控剂的调节剂、药物组合物、治疗方法和制备所述调节剂的方法
AU2018279646B2 (en) 2017-06-08 2023-04-06 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
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
US10654829B2 (en) 2017-10-19 2020-05-19 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
AU2019222758B2 (en) 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
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
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
AU2020290094B2 (en) * 2019-06-10 2024-01-18 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF, COPD, and bronchiectasis
BR112022000507A2 (pt) 2019-07-15 2022-05-10 Novartis Ag Formulações de (s)-3-amino-6-metóxi-n-(3,3,3-trifluoro-2-hidróxi-2-metilpropil)-5-(trifluorometil)picolinamida
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
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
CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
KR20230007369A (ko) * 2020-04-07 2023-01-12 아이테오스 벨지움 에스에이 암의 치료를 위한 ent 저해제로서의 거대환식 다이아민 유도체 및 이와 아데노신 수용체 길항제와의 조합물
IL300413A (en) 2020-08-13 2023-04-01 Vertex Pharma Crystal forms of CFTR modulators
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
EP4225762A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
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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JP2005504751A (ja) 2001-07-23 2005-02-17 バイエル・ヘルスケア・アクチェンゲゼルシャフト 2−アルコキシフェニル置換イミダゾトリアジノン類の使用
US20050085472A1 (en) 2003-06-20 2005-04-21 Masahiro Tanaka Pyrazolo pyrimidine derivatives and methods of use thereof
JP2005538989A (ja) 2002-07-19 2005-12-22 ブリストル−マイヤーズ スクイブ カンパニー キナーゼの新規インヒビター
JP2009518303A (ja) 2005-12-02 2009-05-07 バイエル・ヘルスケア・エルエルシー 過剰増殖性疾患および血管新生と関連する疾患を処置するために有用な置換された4−アミノ−ピロロトリアジン誘導体
JP2009522284A (ja) 2005-12-29 2009-06-11 アボット・ラボラトリーズ タンパク質キナーゼ阻害薬
JP2009532507A (ja) 2006-04-04 2009-09-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Pi3キナーゼアンタゴニスト
JP2015500307A (ja) 2011-12-15 2015-01-05 バイエル・ファルマ・アクチェンゲゼルシャフトBayer Pharma Aktiengesellschaft 二置換ベンゾチエニル−ピロロトリアジンおよびfgfr阻害剤としてのその使用
JP2016523892A (ja) 2013-07-02 2016-08-12 ライゼン・ファーマシューティカルズ・エスアー Pi3kタンパク質キナーゼ阻害剤、特に、デルタ及び/またはガンマ阻害剤

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JP2005504751A (ja) 2001-07-23 2005-02-17 バイエル・ヘルスケア・アクチェンゲゼルシャフト 2−アルコキシフェニル置換イミダゾトリアジノン類の使用
JP2005538989A (ja) 2002-07-19 2005-12-22 ブリストル−マイヤーズ スクイブ カンパニー キナーゼの新規インヒビター
US20050008640A1 (en) 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
US20050085472A1 (en) 2003-06-20 2005-04-21 Masahiro Tanaka Pyrazolo pyrimidine derivatives and methods of use thereof
JP2009518303A (ja) 2005-12-02 2009-05-07 バイエル・ヘルスケア・エルエルシー 過剰増殖性疾患および血管新生と関連する疾患を処置するために有用な置換された4−アミノ−ピロロトリアジン誘導体
JP2009522284A (ja) 2005-12-29 2009-06-11 アボット・ラボラトリーズ タンパク質キナーゼ阻害薬
JP2009532507A (ja) 2006-04-04 2009-09-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Pi3キナーゼアンタゴニスト
JP2009532476A (ja) 2006-04-04 2009-09-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア キナーゼ拮抗剤
JP2015500307A (ja) 2011-12-15 2015-01-05 バイエル・ファルマ・アクチェンゲゼルシャフトBayer Pharma Aktiengesellschaft 二置換ベンゾチエニル−ピロロトリアジンおよびfgfr阻害剤としてのその使用
JP2016523892A (ja) 2013-07-02 2016-08-12 ライゼン・ファーマシューティカルズ・エスアー Pi3kタンパク質キナーゼ阻害剤、特に、デルタ及び/またはガンマ阻害剤

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BR112019012335A2 (pt) 2020-03-03
RU2019120990A3 (2) 2021-01-18
CA3046968A1 (en) 2018-06-21
RU2019120990A (ru) 2021-01-18
US10766904B2 (en) 2020-09-08
SG10201911221RA (en) 2020-02-27
EP3554506A1 (en) 2019-10-23
AU2021277702A1 (en) 2021-12-23
US20190016728A1 (en) 2019-01-17
MX391651B (es) 2025-03-21
US10131670B2 (en) 2018-11-20
SG10201911076QA (en) 2020-01-30
RU2753056C2 (ru) 2021-08-11
US20180170938A1 (en) 2018-06-21
JP2020502103A (ja) 2020-01-23
AU2017378324B2 (en) 2021-09-02
AU2021277702B2 (en) 2023-11-30
AU2017378324A1 (en) 2019-06-27
EP3554506A4 (en) 2020-06-10
US10377762B2 (en) 2019-08-13
WO2018112149A1 (en) 2018-06-21
EP3554506B1 (en) 2021-04-28
US20190016727A1 (en) 2019-01-17
US10208053B2 (en) 2019-02-19
MX2019007135A (es) 2019-11-18
CN110300589B (zh) 2023-03-10
US20190330219A1 (en) 2019-10-31
CN110300589A (zh) 2019-10-01

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