JPWO2020177587A5 - - Google Patents
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- Publication number
- JPWO2020177587A5 JPWO2020177587A5 JP2021551785A JP2021551785A JPWO2020177587A5 JP WO2020177587 A5 JPWO2020177587 A5 JP WO2020177587A5 JP 2021551785 A JP2021551785 A JP 2021551785A JP 2021551785 A JP2021551785 A JP 2021551785A JP WO2020177587 A5 JPWO2020177587 A5 JP WO2020177587A5
- Authority
- JP
- Japan
- Prior art keywords
- body weight
- days
- ring
- membered
- alkylene
- 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.)
- Granted
Links
- 230000037396 body weight Effects 0.000 claims 69
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 15
- 229920006395 saturated elastomer Polymers 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 8
- 150000001204 N-oxides Chemical class 0.000 claims 8
- 150000002148 esters Chemical class 0.000 claims 8
- 239000002207 metabolite Substances 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 239000004215 Carbon black (E152) Substances 0.000 claims 4
- -1 N-methylpyrrolidinyl Chemical group 0.000 claims 4
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229930195733 hydrocarbon Natural products 0.000 claims 4
- 150000002430 hydrocarbons Chemical class 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 208000007082 Alcoholic Fatty Liver Diseases 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 239000002674 ointment Substances 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical group CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- 102000008186 Collagen Human genes 0.000 claims 1
- 108010035532 Collagen Proteins 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 239000007900 aqueous suspension Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229920001436 collagen Polymers 0.000 claims 1
- 235000009508 confectionery Nutrition 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000010255 intramuscular injection Methods 0.000 claims 1
- 239000007927 intramuscular injection Substances 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 230000002045 lasting effect Effects 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 239000007937 lozenge Substances 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000006072 paste Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019076688 | 2019-03-01 | ||
| CNPCT/CN2019/076688 | 2019-03-01 | ||
| PCT/CN2020/076723 WO2020177587A1 (zh) | 2019-03-01 | 2020-02-26 | 治疗脂肪性肝病和/或脂肪性肝炎的方法 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022522486A JP2022522486A (ja) | 2022-04-19 |
| JP2022522486A5 JP2022522486A5 (https=) | 2023-03-06 |
| JPWO2020177587A5 true JPWO2020177587A5 (https=) | 2023-03-06 |
| JP7565292B2 JP7565292B2 (ja) | 2024-10-10 |
Family
ID=72337009
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021551785A Active JP7565292B2 (ja) | 2019-03-01 | 2020-02-26 | 脂肪性肝疾患および/または脂肪性肝炎の処置方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US12485108B2 (https=) |
| EP (1) | EP3932404A4 (https=) |
| JP (1) | JP7565292B2 (https=) |
| KR (1) | KR102906316B1 (https=) |
| CN (1) | CN113490493B (https=) |
| AU (1) | AU2020230574B2 (https=) |
| BR (1) | BR112021017354A2 (https=) |
| CA (1) | CA3132228A1 (https=) |
| IL (1) | IL285989B2 (https=) |
| TW (1) | TWI852999B (https=) |
| WO (1) | WO2020177587A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023539276A (ja) * | 2020-08-31 | 2023-09-13 | ベイジン タイド ファーマシューティカル カンパニー リミテッド | Rho関連タンパク質キナーゼ阻害剤の塩、その固体形態、その調製方法およびその使用 |
| CN113135900B (zh) * | 2021-03-12 | 2022-05-24 | 中山大学 | 吲哚嘧啶类化合物及其合成方法和应用 |
| IL311447A (en) * | 2021-09-18 | 2024-05-01 | Beijing Tide Pharmaceutical Co Ltd | A solid form of a Rho-linked protein kinase inhibitor or a solvate thereof, a method of preparation and use thereof |
| KR20240095429A (ko) * | 2021-11-16 | 2024-06-25 | 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 | Rock2 억제제의 나노결정 제제 및 이의 제조방법 |
| CA3254208A1 (en) * | 2022-03-14 | 2023-09-21 | Purdue Research Foundation | SPLEEN TYROSINE KINASE INHIBITOR, COMPOSITION AND METHODS OF USE |
| CN117843618A (zh) * | 2022-08-29 | 2024-04-09 | 北京沐华生物科技有限责任公司 | 一种ep300/cbp调节剂及其制备方法和用途 |
| WO2025017499A1 (en) | 2023-07-17 | 2025-01-23 | Graviton Bioscience Bv | Formulations and uses of rock2 inhibitors for als |
| IL325831A (en) | 2023-07-17 | 2026-03-01 | Graviton Bioscience Bv | ROCK2 inhibitor formulations for central nervous system disorders |
| CN117122602B (zh) * | 2023-09-26 | 2026-03-20 | 赣南创新与转化医学研究院 | 化合物在制备治疗和/或预防脂肪肝病及相关疾病的药物中的用途 |
| WO2025069008A1 (en) | 2023-09-28 | 2025-04-03 | Graviton Bioscience Bv | Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors |
| WO2025069009A1 (en) | 2023-09-29 | 2025-04-03 | Graviton Bioscience Bv | Rock2 inhibitors in the treatment of obesity |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012040499A2 (en) * | 2010-09-22 | 2012-03-29 | Surface Logix, Inc. | Metabolic inhibitors |
| FR3017868A1 (fr) | 2014-02-21 | 2015-08-28 | Servier Lab | Derives d'isoquinoleine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2016004254A1 (en) | 2014-07-01 | 2016-01-07 | The Regents Of The University Of California | Combined modulation of ire1 |
| WO2018039539A1 (en) | 2016-08-26 | 2018-03-01 | Lycera Corporation | Indazolyl-l,2,4-thiadiazolamines and related compounds for inhibition of rho-associated protein kinase and the treatment of disease |
| CN110582489B (zh) | 2017-06-30 | 2023-10-27 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| WO2019000682A1 (zh) * | 2017-06-30 | 2019-01-03 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
| US10323023B2 (en) * | 2017-06-30 | 2019-06-18 | Beijing Tide Pharmaceutical Co., Ltd. | Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof |
| GB201801226D0 (en) | 2018-01-25 | 2018-03-14 | Redx Pharma Plc | Modulators of Rho-associated protein kinase |
-
2020
- 2020-02-26 BR BR112021017354A patent/BR112021017354A2/pt unknown
- 2020-02-26 AU AU2020230574A patent/AU2020230574B2/en active Active
- 2020-02-26 WO PCT/CN2020/076723 patent/WO2020177587A1/zh not_active Ceased
- 2020-02-26 US US17/435,061 patent/US12485108B2/en active Active
- 2020-02-26 EP EP20765982.2A patent/EP3932404A4/en active Pending
- 2020-02-26 CA CA3132228A patent/CA3132228A1/en active Pending
- 2020-02-26 CN CN202080017129.7A patent/CN113490493B/zh active Active
- 2020-02-26 IL IL285989A patent/IL285989B2/en unknown
- 2020-02-26 JP JP2021551785A patent/JP7565292B2/ja active Active
- 2020-02-26 KR KR1020217031621A patent/KR102906316B1/ko active Active
- 2020-02-27 TW TW109106569A patent/TWI852999B/zh active
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