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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Publication number
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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JP2020502103A (ja
JP2020502103A5 (enExample
JPWO2018112149A5 (enExample
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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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    • 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (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 (4)

Publication Number Publication Date
JP2020502103A JP2020502103A (ja) 2020-01-23
JP2020502103A5 JP2020502103A5 (enExample) 2021-01-28
JPWO2018112149A5 JPWO2018112149A5 (enExample) 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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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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SG10201913603QA (en) 2014-10-06 2020-02-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
EP3379933B1 (en) 2015-11-25 2023-02-15 Gilead Apollo, LLC Fungicidal compositions containing derivatives of 2,4-dioxo-1,4-dihydrothieno[2,3-d]pyrimidine
MX2018006286A (es) 2015-11-25 2018-09-07 Gilead Apollo Llc Inhibidores de acc pirazolicos y usos de los mismos.
JP2018536660A (ja) 2015-11-25 2018-12-13 ギリアド アポロ， エルエルシー エステルａｃｃ阻害剤およびその使用
AU2016361428A1 (en) 2015-11-25 2018-05-24 Gilead Apollo, Llc Triazole ACC inhibitors and uses thereof
US10570115B2 (en) 2016-09-30 2020-02-25 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
HRP20201946T1 (hr) 2016-12-09 2021-01-22 Vertex Pharmaceuticals Incorporated Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
US11517564B2 (en) 2017-07-17 2022-12-06 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
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
MA51039A (fr) 2017-12-08 2020-10-14 Vertex Pharma Procédés pour préparer des modulateurs du régulateur de la conductance transmembranaire de la mucoviscidose
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
MD3752510T2 (ro) 2018-02-15 2023-06-30 Vertex Pharma Macrociclii ca modulatori ai regulatorului conductanței transmembranare în fibroza chistică, compoziții farmaceutice ale acestora, utilizarea lor în tratamentul fibrozei chistice, și procedeu pentru fabricarea acestora
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
AU2020290094B2 (en) * 2019-06-10 2024-01-18 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF, COPD, and bronchiectasis
KR20220035421A (ko) 2019-07-15 2022-03-22 노파르티스 아게 (s)-3-아미노-6-메톡시-n-(3,3,3-트리플루오로-2-히드록시-2-메틸프로필)-5-(트리플루오로메틸)피콜린아미드의 제형
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
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
JP2023538125A (ja) 2020-08-20 2023-09-06 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー 粘液過剰分泌を特徴とする呼吸器疾患を処置するための方法
KR20230118123A (ko) 2020-12-10 2023-08-10 버텍스 파마슈티칼스 인코포레이티드 낭성 섬유증 치료 방법
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

Citations (9)

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US20050008640A1 (en) 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
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
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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WO2009062118A2 (en) * 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
DK2531187T3 (en) * 2010-02-05 2015-11-09 Adverio Pharma Gmbh sGC stimulators OR sGC activators alone and in combination with PDE5 inhibitors for the treatment of cystic fibrosis
AU2017362350B2 (en) * 2016-11-18 2021-12-23 Cystic Fibrosis Foundation Pyrrolopyrimidines as CFTR potentiators

Patent Citations (10)

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

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