CN114728926A - 一种rock抑制剂及其制备方法和用途 - Google Patents

一种rock抑制剂及其制备方法和用途 Download PDF

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CN114728926A
CN114728926A CN202080078665.8A CN202080078665A CN114728926A CN 114728926 A CN114728926 A CN 114728926A CN 202080078665 A CN202080078665 A CN 202080078665A CN 114728926 A CN114728926 A CN 114728926A
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compound
group
aliphatic hydrocarbon
unsubstituted
fluoro
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李金平
娄军
郭晓丹
曾弦
陈永凯
张轶涵
彭微
王朝东
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Wuhan LL Science and Technology Development Co Ltd
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Wuhan LL Science and Technology Development Co Ltd
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • C07D513/04—Ortho-condensed systems

Abstract

下式(I)所示的化合物、其消旋体、立体异构体、互变异构体、同位素标记物、氮氧化物、溶剂化物、多晶型物、代谢产物、酯、药学上可接受的盐或前药。式(I)所示的化合物具有优异的ROCK抑制活性。此外，式(I)所示的化合物具有较好的安全性和代谢稳定性。进一步地，式(I)所示的化合物潜在肝毒性风险小。最后式(I)所示的化合物制备方法简单、易于提纯，因此具有良好的应用前景。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN202080078665.8A 2019-11-15 2020-11-12 一种rock抑制剂及其制备方法和用途 Pending CN114728926A (zh)

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CN201911121236X 2019-11-15
CN201911121236 2019-11-15
PCT/CN2020/128244 WO2021093795A1 (zh) 2019-11-15 2020-11-12 一种rock抑制剂及其制备方法和用途

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US (1) US20230050653A1 (zh)
EP (1) EP4059928A4 (zh)
JP (1) JP2023501799A (zh)
KR (1) KR20220102622A (zh)
CN (1) CN114728926A (zh)
AU (1) AU2020381792A1 (zh)
CA (1) CA3158241A1 (zh)
MX (1) MX2022005858A (zh)
WO (1) WO2021093795A1 (zh)

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WO2022212326A1 (en) 2021-03-29 2022-10-06 Halia Therapeutics, Inc. Nek7 inhibitors
CN117321047A (zh) * 2021-05-14 2023-12-29 武汉朗来科技发展有限公司 化合物的晶型、含晶型组合物及其制备方法和应用
AU2022271550A1 (en) * 2021-05-14 2023-11-30 Wuhan Ll Science And Technology Development Co., Ltd. Acid addition salt of rock inhibitor, and crystal form, composition and pharmaceutical use thereof
WO2023051753A1 (zh) * 2021-09-30 2023-04-06 武汉朗来科技发展有限公司 一种rock抑制剂的制备方法、其中间体及中间体的制备方法
WO2023134688A1 (zh) * 2022-01-13 2023-07-20 武汉朗来科技发展有限公司 一种rock抑制剂的盐及盐的晶型、组合物和药物用途
TW202402269A (zh) * 2022-05-26 2024-01-16 大陸商迪哲（江蘇）醫藥股份有限公司 ＲＯＣＫ（Ｒｈｏ相關激酶）抑制劑及其用途

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WO2021093795A1 (zh) 2021-05-20
CA3158241A1 (en) 2021-05-20
EP4059928A1 (en) 2022-09-21
EP4059928A4 (en) 2023-11-15
AU2020381792A1 (en) 2022-06-30
US20230050653A1 (en) 2023-02-16
JP2023501799A (ja) 2023-01-19
KR20220102622A (ko) 2022-07-20
MX2022005858A (es) 2022-06-14

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