CN114761407A - 作为高选择性ros1抑制剂的化合物及其应用 - Google Patents
作为高选择性ros1抑制剂的化合物及其应用 Download PDFInfo
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- CN114761407A CN114761407A CN202080080094.1A CN202080080094A CN114761407A CN 114761407 A CN114761407 A CN 114761407A CN 202080080094 A CN202080080094 A CN 202080080094A CN 114761407 A CN114761407 A CN 114761407A
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- alkyl
- compound
- cycloalkyl
- pharmaceutically acceptable
- acceptable salt
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 163
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 title claims abstract description 23
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 title claims abstract description 23
- 239000003112 inhibitor Substances 0.000 title claims description 12
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 3
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- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 59
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 46
- 239000002904 solvent Substances 0.000 claims description 38
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 37
- 206010028980 Neoplasm Diseases 0.000 claims description 36
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- 125000000217 alkyl group Chemical group 0.000 claims description 27
- 229940079593 drug Drugs 0.000 claims description 26
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims description 24
- -1 tricresylphosphine Chemical compound 0.000 claims description 23
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 22
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Abstract
本发明公开了一类具有高选择性的ROS1抑制作用的化合物，及其在制备治疗与ROS1激酶异常表达的相关疾病的药物中的应用。具体公开了式(IV)所示化合物及其药学上可接受的盐。
Description
PCT国内申请，说明书已公开。
Claims (17)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019111283420 | 2019-11-18 | ||
| CN201911128342 | 2019-11-18 | ||
| CN202010388478 | 2020-05-09 | ||
| CN2020103884781 | 2020-05-09 | ||
| CN202010995918X | 2020-09-21 | ||
| CN202010995918 | 2020-09-21 | ||
| PCT/CN2020/129652 WO2021098703A1 (zh) | 2019-11-18 | 2020-11-18 | 作为高选择性ros1抑制剂的化合物及其应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN114761407A true CN114761407A (zh) | 2022-07-15 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080080094.1A Pending CN114761407A (zh) | 2019-11-18 | 2020-11-18 | 作为高选择性ros1抑制剂的化合物及其应用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230002410A1 (zh) |
| EP (1) | EP4063365A4 (zh) |
| JP (1) | JP7374532B2 (zh) |
| CN (1) | CN114761407A (zh) |
| WO (1) | WO2021098703A1 (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI807830B (zh) * | 2021-05-18 | 2023-07-01 | 大陸商廣州嘉越醫藥科技有限公司 | 一種含氰基取代的大環類化合物的晶型及其製備方法 |
| CN117427079A (zh) * | 2022-07-20 | 2024-01-23 | 广州嘉越医药科技有限公司 | 含氰基取代的大环类化合物的用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101679429A (zh) * | 2007-04-18 | 2010-03-24 | 阿斯利康(瑞典)有限公司 | 5-氨基吡唑-3-基-3h-咪唑并[4,5-b]吡啶衍生物及其治疗癌的用途 |
| CN102971322A (zh) * | 2010-05-20 | 2013-03-13 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| CN107735399A (zh) * | 2015-07-02 | 2018-02-23 | Tp生物医药公司 | 作为蛋白质激酶的调节剂的手性二芳基大环 |
| WO2018170381A1 (en) * | 2017-03-16 | 2018-09-20 | Andrews Steven W | Macrocyclic compounds as ros1 kinase inhibitors |
| WO2019165967A1 (zh) * | 2018-02-28 | 2019-09-06 | 南京明德新药研发有限公司 | 吡唑并嘧啶衍生物及其用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019094143A1 (en) | 2017-11-10 | 2019-05-16 | Angex Pharmaceutical, Inc. | Macrocyclic compounds as trk kinase inhibitors and uses thereof |
| WO2019206069A1 (zh) | 2018-04-25 | 2019-10-31 | 北京普祺医药科技有限公司 | 一种二芳基巨环化合物、药物组合物以及其用途 |
-
2020
- 2020-11-18 US US17/777,154 patent/US20230002410A1/en active Pending
- 2020-11-18 WO PCT/CN2020/129652 patent/WO2021098703A1/zh unknown
- 2020-11-18 JP JP2022529102A patent/JP7374532B2/ja active Active
- 2020-11-18 CN CN202080080094.1A patent/CN114761407A/zh active Pending
- 2020-11-18 EP EP20889015.2A patent/EP4063365A4/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101679429A (zh) * | 2007-04-18 | 2010-03-24 | 阿斯利康(瑞典)有限公司 | 5-氨基吡唑-3-基-3h-咪唑并[4,5-b]吡啶衍生物及其治疗癌的用途 |
| CN102971322A (zh) * | 2010-05-20 | 2013-03-13 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| CN107735399A (zh) * | 2015-07-02 | 2018-02-23 | Tp生物医药公司 | 作为蛋白质激酶的调节剂的手性二芳基大环 |
| WO2018170381A1 (en) * | 2017-03-16 | 2018-09-20 | Andrews Steven W | Macrocyclic compounds as ros1 kinase inhibitors |
| WO2019165967A1 (zh) * | 2018-02-28 | 2019-09-06 | 南京明德新药研发有限公司 | 吡唑并嘧啶衍生物及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021098703A1 (zh) | 2021-05-27 |
| EP4063365A1 (en) | 2022-09-28 |
| US20230002410A1 (en) | 2023-01-05 |
| EP4063365A4 (en) | 2023-01-11 |
| JP2023502407A (ja) | 2023-01-24 |
| JP7374532B2 (ja) | 2023-11-07 |
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