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

Info

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
Authority
JP
Japan
Prior art keywords
pyrrolo
trifluoromethyl
fluorophenyl
pyrimidin
triazine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2019531417A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020502103A5 (enExample
JP2020502103A (ja
Inventor
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，
Original Assignee
システィック・ファイブロシス・ファンデーション
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by システィック・ファイブロシス・ファンデーション filed Critical システィック・ファイブロシス・ファンデーション
Publication of JP2020502103A publication Critical patent/JP2020502103A/ja
Publication of JP2020502103A5 publication Critical patent/JP2020502103A5/ja
Application granted granted Critical
Publication of JP7150721B2 publication Critical patent/JP7150721B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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 (enExample) 2022-05-24
JP7150721B2 true JP7150721B2 (ja) 2022-10-11

Family

ID=62557188

Family Applications (1)

Application Number Title Priority Date Filing Date
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

Country Status (10)

Country Link
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)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS60906B1 (sr) 2014-10-06 2020-11-30 Vertex Pharma Modulatori regulatora transmembranske provodljivosti za cističnu fibrozu
EA201890913A1 (ru) 2015-11-25 2018-11-30 Джилид Аполло, Ллс Пиразоловые соединения в качестве ингибиторов акк и их применение
EA201890949A1 (ru) 2015-11-25 2018-12-28 Джилид Аполло, Ллс СЛОЖНОЭФИРНЫЕ ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ И ВАРИАНТЫ ИХ ПРИМЕНЕНИЯ
AU2016359626A1 (en) 2015-11-25 2018-05-17 Gilead Apollo, Llc Fungicidal compositions containing derivatives of 2,4-dioxo-1,4-dihydrothieno(2,3-d)pyrimidine
KR20180082557A (ko) 2015-11-25 2018-07-18 길리어드 아폴로, 엘엘씨 트리아졸 acc 억제제 및 그의 용도
LT3519401T (lt) 2016-09-30 2021-11-25 Vertex Pharmaceuticals Incorporated Cistinės fibrozės transmembraninio laidumo reguliavimo moduliatorius, farmacinės kompozicijos, gydymo būdai ir moduliatoriaus gamybos būdas
MX2021012639A (es) 2016-11-18 2022-10-03 Cystic Fibrosis Found Pirrolopirimidinas como potenciadores de cftr.
PT3551622T (pt) 2016-12-09 2020-11-12 Vertex Pharma Modulador do regulador da condutância transmembrana da fibrose quística, composições farmacêuticas, métodos de tratamento e processo de fabrico do modulador
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2019018395A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated METHODS OF TREATING CYSTIC FIBROSIS
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
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
CA3088577A1 (en) 2018-02-15 2019-08-22 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them
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
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
EP3980121A1 (en) * 2019-06-10 2022-04-13 Novartis AG Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis
CN114007616A (zh) 2019-07-15 2022-02-01 诺华股份有限公司 (s)-3-氨基-6-甲氧基-n-(3，3，3-三氟-2-羟基-2-甲基丙基)-5-(三氟甲基)吡啶甲酰胺的配制品
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
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
US11873300B2 (en) 2019-08-14 2024-01-16 Vertex Pharmaceuticals Incorporated Crystalline forms of CFTR modulators
JP7784041B2 (ja) * 2020-04-07 2025-12-11 アイテオ ベルギウム エスエー がんの治療のためのｅｎｔ阻害剤としての大環状ジアミン誘導体、及びそれとアデノシン受容体拮抗薬との組合せ
WO2022036060A1 (en) 2020-08-13 2022-02-17 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
IL300405A (en) 2020-08-20 2023-04-01 Univ Leland Stanford Junior Methods for treating respiratory diseases characterized by excessive secretion of mucus
US12612416B2 (en) 2020-10-07 2026-04-28 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR101793304B1 (ko) * 2010-02-05 2017-11-02 아드베리오 파마 게엠베하 낭성 섬유증의 치료를 위한, 단독으로의 및 ＰＤＥ5 억제제와 조합된 ｓＧＣ 자극제 또는 ｓＧＣ 활성화제
MX2021012639A (es) 2016-11-18 2022-10-03 Cystic Fibrosis Found Pirrolopirimidinas como potenciadores de cftr.

Patent Citations (10)

* Cited by examiner, † Cited by third party
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

Also Published As

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

Similar Documents

Publication Publication Date Title
AU2021277702B2 (en) Bicyclic heteroaryl derivatives as CFTR potentiators
US12612409B2 (en) Pyrrolopyrimidines as CFTR potentiators
CA2901047A1 (en) Octahydro-pyrrolo[3,4-c]-pyrrole derivatives and analogs thereof as autotaxin inhibitors
HK40015891A (en) Bycyclic heteroaryl derivatives as cftr potentiators
HK40015891B (en) Bycyclic heteroaryl derivatives as cftr potentiators
BR122024011694A2 (pt) Compostos derivados de heteroarila bicíclica como potenciadores de cftr, composição farmacêutica que compreende os mesmos e uso dos ditos compostos para tratar fibrose cística, asma, bronquiectasia, doença pulmonar obstrutiva crônica, constipação, diabetes mellitus, doença do olho seco, pancreatite, rinossinusite ou síndrome de sjogren
BR122024011694B1 (pt) Compostos derivados de heteroarila bicíclica como potenciadores de cftr, composição farmacêutica que compreende os mesmos e uso dos ditos compostos para tratar fibrose cística, asma, bronquiectasia, doença pulmonar obstrutiva crônica, constipação, diabetes mellitus, doença do olho seco, pancreatite, rinossinusite ou síndrome de sjogren
BR112019012335B1 (pt) Compostos derivados de heteroarila bicíclica como potenciadores de cftr, composição farmacêutica que compreende os mesmos e uso dos ditos compostos para tratar fibrose cística, asma, bronquiectasia, doença pulmonar obstrutiva crônica, constipação, diabetes mellitus, doença do olho seco, pancreatite, rinossinusite ou síndrome de sjogren
HK40014108A (en) Pyrrolopyrimidines as cftr potentiators
HK40014108B (en) Pyrrolopyrimidines as cftr potentiators
BR122022008825B1 (pt) Compostos pirrolopirimidinas potenciadores de cftr, composição farmacêutica que compreende os mesmos e usos terapêuticos dos ditos compostos e composição
BR112019010167B1 (pt) Compostos pirrolopirimidinas potenciadores de cftr

Legal Events

Date Code Title Description
RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20190912

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20200902

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20200902

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201211

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201211

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220111

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220405

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20220516

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20220830

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20220928

R150 Certificate of patent or registration of utility model

Ref document number: 7150721

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250