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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    • 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)
  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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)

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

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TWI735416B (zh) 2014-10-06 2021-08-11 美商維泰克斯製藥公司 囊腫纖維化症跨膜傳導調節蛋白之調節劑
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
AU2016361414A1 (en) 2015-11-25 2018-05-24 Gilead Apollo, Llc Ester ACC inhibitors and uses thereof
PT3380479T (pt) 2015-11-25 2023-03-13 Gilead Apollo Llc Inhibidores de triazol acc e seus usos
JP2019503338A (ja) 2015-11-25 2019-02-07 ギリアド アポロ, エルエルシー 2,4−ジオキソ−1,4−ジヒドロチエノ[2,3−d]ピリミジンの誘導体を含む殺真菌組成物
EP3519401B1 (en) 2016-09-30 2021-09-29 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
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
CA3066084A1 (en) 2017-06-08 2018-12-13 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US11517564B2 (en) 2017-07-17 2022-12-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
KR102606188B1 (ko) 2017-08-02 2023-11-23 버텍스 파마슈티칼스 인코포레이티드 피롤리딘 화합물을 제조하기 위한 공정
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
JP7214743B2 (ja) 2018-02-15 2023-01-30 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としての大環状分子、それらの医薬組成物、嚢胞性線維症の治療におけるそれらの使用、及びそれらの製造方法
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
MX2021015133A (es) * 2019-06-10 2022-01-24 Novartis Ag Derivado de piridina y pirazina para el tratamiento de la fibrosis quistica, enfermedad pulmonar obstructiva cronica y 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
HRP20240606T1 (hr) 2019-08-14 2024-07-19 Vertex Pharmaceuticals Incorporated Postupak za proizvodnju modulatora za cftr
US11873300B2 (en) 2019-08-14 2024-01-16 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
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
IL303519A (en) 2020-12-10 2023-08-01 Vertex Pharma Cystic fibrosis treatment methods
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
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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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
SI2531187T1 (sl) * 2010-02-05 2016-01-29 Adverio Pharma Gmbh Stimulatorji sGC ali aktivatorji sGC sami in v kombinaciji z inhibitorji PDE5 za zdravljenje cistične fibroze
JP6978507B2 (ja) * 2016-11-18 2021-12-08 システィック・ファイブロシス・ファンデーション Cftr増強物質としてのピロロピリミジン

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

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