JP6845939B2 - イソキノリンおよびナフチドリン化合物 - Google Patents
イソキノリンおよびナフチドリン化合物 Download PDFInfo
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- JP6845939B2 JP6845939B2 JP2019542593A JP2019542593A JP6845939B2 JP 6845939 B2 JP6845939 B2 JP 6845939B2 JP 2019542593 A JP2019542593 A JP 2019542593A JP 2019542593 A JP2019542593 A JP 2019542593A JP 6845939 B2 JP6845939 B2 JP 6845939B2
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- mmol
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- refers
- compound
- ask1
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- JGZSLGXLSHEGFA-UHFFFAOYSA-N CC(C)[n]1c(-c2nc(Br)ccc2)nnc1 Chemical compound CC(C)[n]1c(-c2nc(Br)ccc2)nnc1 JGZSLGXLSHEGFA-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Description
XはCHおよびNからなる群から選択され、
QはCH3およびHからなる群から選択され、
Rは、
調製物1
6−アミノピリジン−2−カルボヒドラジド
N,6‐ビス[(E)−ジメチルアミノメチレンアミノ]ピリジン‐2‐カルボアミド
6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)ピリジン−2−アミン
2−クロロ−6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)ピリジン
2−ブロモ−6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)ピリジン
6−ブロモ−3,4−ジヒドロ−2H−イソキノリン−1−オン
6−メチル−3,4−ジヒドロ−2H−イソキノリン−1−オン
7−ヨード−6−メチル−3,4−ジヒドロ−2H−イソキノリン−1−オン
7−(1−イソプロピルピラゾール−4−イル)−6−メチル−3,4−ジヒドロ−2H−イソキノリン−1−オン
7−(4−シクロプロピルイミダゾール−1−イル)−6−メチル−3,4−ジヒドロ−2H−イソキノリン−1−オン
5−ブロモ−2−(ブロモメチル)ピリジン−3−カルボン酸エチル
5−ブロモ−2−(シアノメチル)ピリジン−3−カルボン酸エチル
3−ブロモ−7,8−ジヒドロ−6H−1,6−ナフチリジン−5−オン
3−(4−シクロプロピルイミダゾール−1−イル)−7,8−ジヒドロ−6H−1,6−ナフチリジン−5−オン
3−(1−イソプロピルピラゾール−4−イル)−7,8−ジヒドロ−6H−1,6−ナフチリジン−5−オン
7−(1−イソプロピルピラゾール−4−イル)−2−[6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)−2−ピリジル]−6−メチル−3,4−ジヒドロイソキノリン−1−オン
7−(4−シクロプロピルイミダゾール−1−イル)−2−[6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)−2−ピリジル]−6−メチル−3,4−ジヒドロイソキノリン−1−オン
3−(4−シクロプロピルイミダゾール−1−イル)−6−[6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)−2−ピリジル]−7,8−ジヒドロ−1,6−ナフチリジン−5−オン。塩酸塩
3−(1−イソプロピルピラゾール−4−イル)−6−[6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)−2−ピリジル]−7,8−ジヒドロ−1,6−ナフチリジン−5−オン
ASK1酵素アッセイにより測定されたASK1阻害剤の効果
このアッセイの目的は、ASK1によるADPの生成に対するASK1阻害剤の効果を決定することである。グルタチオンS−トランスフェラーゼでタグ付けされた組換えヒトASK1(hASK1)触媒ドメインが使用され、ヒスチジンタグ付き全長ヒトMAPキナーゼキナーゼ6(MKK6)およびATPは、それぞれ基質および補因子である。
このアッセイの目的は、ヒトASK1を過剰発現しているHEK293細胞におけるThr838でのH2O2刺激ASK1自己リン酸化に対するASK1阻害剤の効果を決定することである。
Claims (7)
- XがNである、請求項1に記載の化合物。
- QがHである、請求項1または2に記載の化合物。
- XがCHである、請求項1に記載の化合物。
- QがCH3である、請求項1または4に記載の化合物。
- 3−(4−シクロプロピルイミダゾール−1−イル)−6−[6−(4−イソプロピル−1,2,4−トリアゾール−3−イル)−2−ピリジル]−7,8−ジヒドロ−1,6−ナフチリジン−5−オンである化合物、またはその薬学的に許容される塩。
- 請求項1に記載の化合物、またはその薬学的に許容される塩と、薬学的に許容される担体、希釈剤、および賦形剤からなる群から選択される少なくとも1つとを含む、薬学的組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2017/075121 WO2018157277A1 (en) | 2017-02-28 | 2017-02-28 | Isoquinolin and naphthydrin compounds |
CNPCT/CN2017/075121 | 2017-02-28 | ||
PCT/US2018/018949 WO2018160406A1 (en) | 2017-02-28 | 2018-02-21 | Isoquinolin and naphthydrin compounds |
Publications (2)
Publication Number | Publication Date |
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JP2020507565A JP2020507565A (ja) | 2020-03-12 |
JP6845939B2 true JP6845939B2 (ja) | 2021-03-24 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2019542593A Active JP6845939B2 (ja) | 2017-02-28 | 2018-02-21 | イソキノリンおよびナフチドリン化合物 |
Country Status (7)
Country | Link |
---|---|
US (1) | US11117891B2 (ja) |
EP (1) | EP3589625B1 (ja) |
JP (1) | JP6845939B2 (ja) |
CN (1) | CN110325526B (ja) |
CA (1) | CA3050751C (ja) |
ES (1) | ES2875577T3 (ja) |
WO (2) | WO2018157277A1 (ja) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6754505B2 (ja) * | 2017-01-22 | 2020-09-09 | 福建広生堂薬業股▲ふん▼有限公司 | Ask1阻害剤、その調製方法および使用 |
JOP20190221A1 (ar) | 2017-04-05 | 2019-09-23 | Seal Rock Therapeutics Inc | مركبات مثبطات كيناز منظم لإشارات الاستماتة 1 (ask1) واستخداماتها |
IL270525B2 (en) | 2017-05-12 | 2024-06-01 | Enanta Pharm Inc | Apoptosis signal-regulated kinase 1 inhibitors and methods of using them |
WO2019015559A1 (zh) * | 2017-07-18 | 2019-01-24 | 南京圣和药业股份有限公司 | 作为ask抑制剂的杂环化合物及其应用 |
CN109456308B (zh) * | 2017-09-06 | 2022-11-29 | 南京圣和药业股份有限公司 | 作为ask抑制剂的杂环化合物及其应用 |
CN109956928B (zh) * | 2017-12-14 | 2021-07-09 | 四川科伦博泰生物医药股份有限公司 | 吡啶类化合物、其制备方法及用途 |
US11434249B1 (en) | 2018-01-02 | 2022-09-06 | Seal Rock Therapeutics, Inc. | ASK1 inhibitor compounds and uses thereof |
KR20210005195A (ko) | 2018-05-02 | 2021-01-13 | 이난타 파마슈티칼스, 인코포레이티드 | 아폽토시스 신호 조절 키나제 1 억제제를 포함하는 테트라졸 및 이의 사용 방법 |
US10968199B2 (en) | 2018-08-22 | 2021-04-06 | Enanta Pharmaceuticals, Inc. | Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
KR102288434B1 (ko) | 2018-10-18 | 2021-08-12 | 에이치케이이노엔 주식회사 | 신규한 (이소프로필-트리아졸릴)피리디닐 치환된 벤조옥사지논 또는 벤조티아지논 유도체 및 이의 용도 |
US11345699B2 (en) | 2018-11-19 | 2022-05-31 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
WO2020198214A1 (en) | 2019-03-25 | 2020-10-01 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
TWI779487B (zh) * | 2020-02-13 | 2022-10-01 | 大陸商勁方醫藥科技(上海)有限公司 | 二氫萘啶酮類化合物,其製法與醫藥上的用途 |
TWI824626B (zh) * | 2021-08-02 | 2023-12-01 | 大陸商勁方醫藥科技(上海)有限公司 | Ripk1抑制劑的晶型及其酸式鹽和其酸式鹽的晶型 |
Family Cites Families (5)
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TWI625121B (zh) * | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
UY34573A (es) * | 2012-01-27 | 2013-06-28 | Gilead Sciences Inc | Inhibidor de la quinasa que regula la señal de la apoptosis |
US20150342943A1 (en) * | 2014-06-03 | 2015-12-03 | Gilead Sciences, Inc. | Methods of treating liver disease |
JP6754505B2 (ja) * | 2017-01-22 | 2020-09-09 | 福建広生堂薬業股▲ふん▼有限公司 | Ask1阻害剤、その調製方法および使用 |
WO2018149284A1 (zh) * | 2017-02-16 | 2018-08-23 | 四川科伦博泰生物医药股份有限公司 | 激酶抑制剂及其制备方法和用途 |
-
2017
- 2017-02-28 WO PCT/CN2017/075121 patent/WO2018157277A1/en active Application Filing
-
2018
- 2018-02-21 US US16/489,101 patent/US11117891B2/en active Active
- 2018-02-21 JP JP2019542593A patent/JP6845939B2/ja active Active
- 2018-02-21 WO PCT/US2018/018949 patent/WO2018160406A1/en unknown
- 2018-02-21 ES ES18708558T patent/ES2875577T3/es active Active
- 2018-02-21 CN CN201880014028.7A patent/CN110325526B/zh active Active
- 2018-02-21 CA CA3050751A patent/CA3050751C/en active Active
- 2018-02-21 EP EP18708558.4A patent/EP3589625B1/en active Active
Also Published As
Publication number | Publication date |
---|---|
CA3050751A1 (en) | 2018-09-07 |
ES2875577T3 (es) | 2021-11-10 |
WO2018157277A1 (en) | 2018-09-07 |
CN110325526B (zh) | 2021-11-19 |
US11117891B2 (en) | 2021-09-14 |
EP3589625B1 (en) | 2021-04-14 |
JP2020507565A (ja) | 2020-03-12 |
CA3050751C (en) | 2021-03-16 |
EP3589625A1 (en) | 2020-01-08 |
CN110325526A (zh) | 2019-10-11 |
WO2018160406A1 (en) | 2018-09-07 |
US20200062751A1 (en) | 2020-02-27 |
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