WO2018001331A1 - 一种咪唑吡啶胺苯基衍生物及其用途 - Google Patents
一种咪唑吡啶胺苯基衍生物及其用途 Download PDFInfo
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- WO2018001331A1 WO2018001331A1 PCT/CN2017/090908 CN2017090908W WO2018001331A1 WO 2018001331 A1 WO2018001331 A1 WO 2018001331A1 CN 2017090908 W CN2017090908 W CN 2017090908W WO 2018001331 A1 WO2018001331 A1 WO 2018001331A1
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- WIPO (PCT)
- Prior art keywords
- imidazolidinium
- hydrate
- phenyl derivative
- metabolism
- pharmaceutically acceptable
- Prior art date
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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
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- A61P37/08—Antiallergic agents
Abstract
Description
化合物 | 激酶抑制活性(IC50,nM) |
式I a化合物 | 415 |
式I b化合物 | 50 |
式I c化合物 | 577 |
式I d化合物 | 4.8 |
Ibrutinib | 1.5 |
Acalabrutinib | 11 |
Claims (15)
- 根据权利要求1所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R1为苯环、含有1或2个氮的六元杂芳环,其任选地被0~2个C1-C4烷基取代。
- 根据权利要求1所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R2为H、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基。
- 根据权利要求1所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R5为H、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基。
- 根据权利要求7所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R1为苯环、含有1或2个氮的六元杂芳环,其任选地被0~2个C1-C4烷基取代。
- 根据权利要求7所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R2为H、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基。
- 根据权利要求7所述的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物,其特征在于:R5为H、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基。
- 如权利要求1至6中任一项权利要求所述的具有通式(I)的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物或如权利要求7至12中任一项权利要求所述的具有通式(II)的咪唑吡啶胺苯基衍生物,其可药用盐、水合物,或以任何形式代谢形成的代谢产物在制备预防和/或治疗与BTK功能有关的适应症的药物中的用途。
- 根据权利要求13所述的用途,其特征在于:所述与BTK功能相关的适应症包括类风湿性关节炎、B细胞淋巴瘤、白血病、多发性骨髓瘤、过敏、哮喘、多发性硬化、I型糖尿病和全身性红斑狼疮。
Priority Applications (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16/311,979 US10640512B2 (en) | 2016-06-30 | 2017-06-29 | Imidazopyrazinamine phenyl derivative and use thereof |
KR1020197002682A KR102215172B1 (ko) | 2016-06-30 | 2017-06-29 | 이미다조피라진아민 페닐 유도체 및 그의 용도 |
JP2018569169A JP6715357B2 (ja) | 2016-06-30 | 2017-06-29 | イミダゾピリジンアミンフェニル誘導体およびその使用 |
EP17819328.0A EP3480199B1 (en) | 2016-06-30 | 2017-06-29 | Imidazopyridinamine phenyl derivative and use thereof |
CA3032795A CA3032795C (en) | 2016-06-30 | 2017-06-29 | Imidazopyridinamine phenyl derivative and use thereof |
AU2017287553A AU2017287553B2 (en) | 2016-06-30 | 2017-06-29 | Imidazopyrazinamine phenyl derivative and use thereof |
ES17819328T ES2878973T3 (es) | 2016-06-30 | 2017-06-29 | Derivado de fenilo de imidazopiridinamina y uso del mismo |
Applications Claiming Priority (4)
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CN201610533291 | 2016-06-30 | ||
CN201610533291.X | 2016-06-30 | ||
CN201611062661 | 2016-11-25 | ||
CN201611062661.2 | 2016-11-25 |
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WO2018001331A1 true WO2018001331A1 (zh) | 2018-01-04 |
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PCT/CN2017/090908 WO2018001331A1 (zh) | 2016-06-30 | 2017-06-29 | 一种咪唑吡啶胺苯基衍生物及其用途 |
Country Status (9)
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US (1) | US10640512B2 (zh) |
EP (1) | EP3480199B1 (zh) |
JP (1) | JP6715357B2 (zh) |
KR (1) | KR102215172B1 (zh) |
CN (1) | CN107556317B (zh) |
AU (1) | AU2017287553B2 (zh) |
CA (1) | CA3032795C (zh) |
ES (1) | ES2878973T3 (zh) |
WO (1) | WO2018001331A1 (zh) |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108129483A (zh) * | 2018-01-26 | 2018-06-08 | 成都施贝康生物医药科技有限公司 | 一种btk抑制剂及其应用 |
US20190367524A1 (en) * | 2017-01-16 | 2019-12-05 | Dongguan Zhenxing-Beite Medicine Technology Co., Ltd. | Imidazopyrazine compounds, preparation methods and uses thereof |
WO2020188015A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
WO2021136219A1 (en) * | 2020-01-02 | 2021-07-08 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Btk inhibitors |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
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BR112019019588A2 (pt) | 2017-03-22 | 2020-04-22 | Suzhou Baijibugong Pharmaceutical Tech Co Ltd | composto, composição farmacêutica, método para tratar uma doença autoimune, composição farmacêutica para prevenir ou tratar cânceres, tumores, doenças inflamatórias, doenças autoimunes ou doença imunologicamente mediada, e método para tratar uma doença autoimune, cânceres, tumores, doenças inflamatórias ou doenças imunologicamente mediadas |
WO2020052628A1 (zh) * | 2018-09-14 | 2020-03-19 | 正大天晴药业集团股份有限公司 | 含有呋喃并[3,4-b]吡咯的BTK抑制剂 |
CN111471048B (zh) * | 2020-04-30 | 2021-06-15 | 成都海博为药业有限公司 | 一种具有含氮桥环、螺环或并环结构的化合物及其用途 |
CN115043841B (zh) * | 2021-03-09 | 2024-04-09 | 药雅科技(上海)有限公司 | 一种作为btk抑制剂杂环类化合物的制备及其应用 |
CN115073468B (zh) * | 2021-03-15 | 2023-12-22 | 药雅科技(上海)有限公司 | 咪唑并吡嗪类btk抑制剂的制备及用途 |
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- 2017-06-29 JP JP2018569169A patent/JP6715357B2/ja active Active
- 2017-06-29 KR KR1020197002682A patent/KR102215172B1/ko active IP Right Grant
- 2017-06-29 AU AU2017287553A patent/AU2017287553B2/en active Active
- 2017-06-29 ES ES17819328T patent/ES2878973T3/es active Active
- 2017-06-29 CA CA3032795A patent/CA3032795C/en active Active
- 2017-06-29 EP EP17819328.0A patent/EP3480199B1/en active Active
- 2017-06-29 WO PCT/CN2017/090908 patent/WO2018001331A1/zh unknown
- 2017-06-29 US US16/311,979 patent/US10640512B2/en active Active
- 2017-06-30 CN CN201710519104.7A patent/CN107556317B/zh active Active
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Cited By (11)
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US20190367524A1 (en) * | 2017-01-16 | 2019-12-05 | Dongguan Zhenxing-Beite Medicine Technology Co., Ltd. | Imidazopyrazine compounds, preparation methods and uses thereof |
US10919899B2 (en) * | 2017-01-16 | 2021-02-16 | Dongguan Zhenxing-Beite Medicine Technology Co., Ltd. | Imidazopyrazine compounds, preparation methods and uses thereof |
CN108129483A (zh) * | 2018-01-26 | 2018-06-08 | 成都施贝康生物医药科技有限公司 | 一种btk抑制剂及其应用 |
CN108129483B (zh) * | 2018-01-26 | 2019-06-04 | 成都施贝康生物医药科技有限公司 | 一种btk抑制剂及其应用 |
WO2020188015A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
WO2021136219A1 (en) * | 2020-01-02 | 2021-07-08 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Btk inhibitors |
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WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
Also Published As
Publication number | Publication date |
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JP2019524699A (ja) | 2019-09-05 |
KR20190033538A (ko) | 2019-03-29 |
CA3032795C (en) | 2021-06-22 |
AU2017287553B2 (en) | 2020-02-06 |
JP6715357B2 (ja) | 2020-07-01 |
CA3032795A1 (en) | 2018-01-04 |
CN107556317A (zh) | 2018-01-09 |
CN107556317B (zh) | 2020-06-09 |
EP3480199A1 (en) | 2019-05-08 |
AU2017287553A1 (en) | 2019-02-07 |
KR102215172B1 (ko) | 2021-02-16 |
EP3480199B1 (en) | 2021-03-17 |
US20190211023A1 (en) | 2019-07-11 |
US10640512B2 (en) | 2020-05-05 |
EP3480199A4 (en) | 2020-02-26 |
ES2878973T3 (es) | 2021-11-19 |
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