TWI852999B - 治療脂肪性肝病及/或脂肪性肝炎的方法 - Google Patents

治療脂肪性肝病及/或脂肪性肝炎的方法 Download PDF

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TWI852999B
TWI852999B TW109106569A TW109106569A TWI852999B TW I852999 B TWI852999 B TW I852999B TW 109106569 A TW109106569 A TW 109106569A TW 109106569 A TW109106569 A TW 109106569A TW I852999 B TWI852999 B TW I852999B
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compound
pharmaceutically acceptable
fatty liver
polymorph
stereoisomer
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TW109106569A
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Chinese (zh)
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TW202045497A (zh
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姜媛媛
仲偉婷
趙焰平
王紅軍
趙靜
李晶
劉偉娜
周麗瑩
劉亞男
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大陸商北京泰德製藥股份有限公司
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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
    • A61K31/41—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
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—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
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
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    • A61K31/435—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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D495/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
TW109106569A 2019-03-01 2020-02-27 治療脂肪性肝病及/或脂肪性肝炎的方法 TWI852999B (zh)

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CN2019076688 2019-03-01
WOPCT/CN2019/076688 2019-03-01

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TW202045497A TW202045497A (zh) 2020-12-16
TWI852999B true TWI852999B (zh) 2024-08-21

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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=)

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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

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WO2019001572A1 (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
WO2019145729A1 (en) * 2018-01-25 2019-08-01 Redx Pharma Plc Heterocyclylamino-substituted triazoles as modulators of rho-associated protein kinase

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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
WO2019001572A1 (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
WO2019145729A1 (en) * 2018-01-25 2019-08-01 Redx Pharma Plc Heterocyclylamino-substituted triazoles as modulators of rho-associated protein kinase

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IL285989B2 (en) 2025-11-01
IL285989B1 (en) 2025-07-01
TW202045497A (zh) 2020-12-16
CN113490493B (zh) 2024-10-29
AU2020230574B2 (en) 2025-08-07
JP7565292B2 (ja) 2024-10-10
CN113490493A (zh) 2021-10-08
EP3932404A4 (en) 2022-11-30
BR112021017354A2 (pt) 2021-11-16
US12485108B2 (en) 2025-12-02
KR102906316B1 (ko) 2025-12-31
IL285989A (en) 2021-10-31
KR20210137086A (ko) 2021-11-17
EP3932404A1 (en) 2022-01-05
WO2020177587A1 (zh) 2020-09-10
AU2020230574A1 (en) 2021-10-28
US20220378743A1 (en) 2022-12-01
CA3132228A1 (en) 2020-09-10
JP2022522486A (ja) 2022-04-19

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