JP7518324B2 - Ｒｈｏ関連プロテインキナーゼのモジュレーター - Google Patents

Ｒｈｏ関連プロテインキナーゼのモジュレーター Download PDF

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Publication number
JP7518324B2
JP7518324B2 JP2020561950A JP2020561950A JP7518324B2 JP 7518324 B2 JP7518324 B2 JP 7518324B2 JP 2020561950 A JP2020561950 A JP 2020561950A JP 2020561950 A JP2020561950 A JP 2020561950A JP 7518324 B2 JP7518324 B2 JP 7518324B2
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disease
mmol
cancer
syndrome
alkyl
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JP2021512158A (ja
JPWO2019145729A5 (https=
JP2021512158A5 (https=
Inventor
クリフォード・ディ・ジョーンズ
ピーター・バンヤード
ゲイリー・ピット
リアム・バーン
トマ・ペノ
ニコラ・ウ・エス・ギゾー
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Redx Pharma Ltd
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Redx Pharma Ltd
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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
    • A61K31/535—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
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/535—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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2020561950A 2018-01-25 2019-01-25 Ｒｈｏ関連プロテインキナーゼのモジュレーター Active JP7518324B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023200631A JP2024026193A (ja) 2018-01-25 2023-11-28 Ｒｈｏ関連プロテインキナーゼのモジュレーター

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1801226.0 2018-01-25
GBGB1801226.0A GB201801226D0 (en) 2018-01-25 2018-01-25 Modulators of Rho-associated protein kinase
PCT/GB2019/050215 WO2019145729A1 (en) 2018-01-25 2019-01-25 Heterocyclylamino-substituted triazoles as modulators of rho-associated protein kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2023200631A Division JP2024026193A (ja) 2018-01-25 2023-11-28 Ｒｈｏ関連プロテインキナーゼのモジュレーター

Publications (4)

Publication Number Publication Date
JP2021512158A JP2021512158A (ja) 2021-05-13
JPWO2019145729A5 JPWO2019145729A5 (https=) 2022-01-31
JP2021512158A5 JP2021512158A5 (https=) 2022-01-31
JP7518324B2 true JP7518324B2 (ja) 2024-07-18

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ID=61558335

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JP2020561950A Active JP7518324B2 (ja) 2018-01-25 2019-01-25 Ｒｈｏ関連プロテインキナーゼのモジュレーター
JP2023200631A Pending JP2024026193A (ja) 2018-01-25 2023-11-28 Ｒｈｏ関連プロテインキナーゼのモジュレーター

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Country Status (25)

Country Link
US (4) US11497751B2 (https=)
EP (2) EP4026834A1 (https=)
JP (2) JP7518324B2 (https=)
KR (1) KR102737926B1 (https=)
CN (1) CN111655681B (https=)
AU (1) AU2019213214B2 (https=)
CA (1) CA3088330A1 (https=)
CY (1) CY1125017T1 (https=)
DK (1) DK3743420T3 (https=)
EA (1) EA202091711A1 (https=)
ES (1) ES2907833T3 (https=)
GB (1) GB201801226D0 (https=)
HR (1) HRP20220269T8 (https=)
HU (1) HUE058940T2 (https=)
IL (1) IL275988B2 (https=)
LT (1) LT3743420T (https=)
MX (1) MX2020007898A (https=)
PH (1) PH12020550986A1 (https=)
PL (1) PL3743420T3 (https=)
PT (1) PT3743420T (https=)
SG (1) SG11202006087UA (https=)
SI (1) SI3743420T1 (https=)
SM (1) SMT202200099T1 (https=)
WO (1) WO2019145729A1 (https=)
ZA (1) ZA202003983B (https=)

Cited By (1)

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JP2024026193A (ja) * 2018-01-25 2024-02-28 レデックス・ファーマ・パブリック・リミテッド・カンパニー Ｒｈｏ関連プロテインキナーゼのモジュレーター

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BR112021017354A2 (pt) 2019-03-01 2021-11-16 Beijing Tide Pharmaceutical Co Ltd Método para o tratamento de doença hepática adiposa e/ou esteatoepatite
CN111718310B (zh) * 2019-08-19 2021-06-11 中国药科大学 苯基取代的五元杂环类化合物及其制备方法、用途和药物组合物
CN110845410B (zh) * 2019-10-29 2021-02-26 暨明医药科技（苏州）有限公司 一种一锅法制备6,7-二甲氧基-3,4-二氢异喹啉盐酸盐的方法
US20240131029A1 (en) * 2021-02-04 2024-04-25 President And Fellows Of Harvard College Selective rock2 inhibition for treatment of edema and associated conditions
CA3226387A1 (en) * 2021-07-26 2023-02-02 Joel D. Moore Rock2 inhibitors and uses thereof
CN113999211B (zh) * 2021-11-23 2022-11-29 郑州大学 一类特异性抗前列腺癌活性的含1,2,3-三氮唑的吲唑骨架衍生物
GB202200735D0 (en) * 2022-01-20 2022-03-09 Redx Pharma Plc Compounds
WO2023182856A1 (ko) * 2022-03-24 2023-09-28 서울대학교산학협력단 로-키나제 억제제를 포함하는 켈로이드 등 피부 섬유화 질환의 예방 또는 치료용 약학적 조성물 및 그의 용도
DK4514782T3 (da) 2022-05-19 2025-12-15 Astrazeneca Ab Heteroaromatiske amidoforbindelser, der er nyttige ved behandling af leversygdomme
CN115124558B (zh) * 2022-07-08 2024-08-13 闽都创新实验室 一种芳基硼酸酯类化合物的制备方法及其应用
WO2024123129A1 (ko) * 2022-12-08 2024-06-13 한국과학기술원 파브리병의 예방 또는 치료용 조성물
CN116891460A (zh) * 2023-07-12 2023-10-17 浙江大学 一种吲唑类衍生物或其药用盐及应用
WO2025017499A1 (en) 2023-07-17 2025-01-23 Graviton Bioscience Bv Formulations and uses of rock2 inhibitors for als
GB202311061D0 (en) * 2023-07-19 2023-08-30 Redx Pharma Plc Modulators of rho-associated protein kinase
GB202311062D0 (en) * 2023-07-19 2023-08-30 Redx Pharma Plc Modulators of rho-associated protein kinase
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
TW202542129A (zh) * 2023-12-22 2025-11-01 美商美國禮來大藥廠 Rho相關蛋白激酶抑制劑
IT202400002560A1 (it) * 2024-02-07 2025-08-07 Univ Pisa Inibitori della proteina rock per uso nel trattamento della fibrosi polmonare
WO2025256614A1 (zh) * 2024-06-14 2025-12-18 北京普祺医药科技股份有限公司 一种促进胶原蛋白表达的抑制剂

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Cited By (1)

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Publication number Priority date Publication date Assignee Title
JP2024026193A (ja) * 2018-01-25 2024-02-28 レデックス・ファーマ・パブリック・リミテッド・カンパニー Ｒｈｏ関連プロテインキナーゼのモジュレーター

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EP3743420A1 (en) 2020-12-02
HUE058940T2 (hu) 2022-09-28
CY1125017T1 (el) 2023-03-24
US20210038606A1 (en) 2021-02-11
AU2019213214A1 (en) 2020-07-09
IL275988A (en) 2020-08-31
CN111655681A (zh) 2020-09-11
EP4026834A1 (en) 2022-07-13
CN111655681B (zh) 2024-01-05
KR102737926B1 (ko) 2024-12-04
IL275988B2 (en) 2023-07-01
SG11202006087UA (en) 2020-08-28
MX2020007898A (es) 2020-09-07
JP2021512158A (ja) 2021-05-13
WO2019145729A1 (en) 2019-08-01
KR20200113216A (ko) 2020-10-06
WO2019145729A9 (en) 2020-07-30
ZA202003983B (en) 2023-07-26
US11878020B2 (en) 2024-01-23
HRP20220269T1 (hr) 2022-05-13
US12453734B2 (en) 2025-10-28
EA202091711A1 (ru) 2020-10-20
US20260034140A1 (en) 2026-02-05
JP2024026193A (ja) 2024-02-28
SI3743420T1 (sl) 2022-06-30
SMT202200099T1 (it) 2022-03-21
GB201801226D0 (en) 2018-03-14
AU2019213214B2 (en) 2023-06-29
US20240216386A1 (en) 2024-07-04
PL3743420T3 (pl) 2022-03-21
PH12020550986A1 (en) 2021-03-22
EP3743420B1 (en) 2021-12-15
US11497751B2 (en) 2022-11-15
IL275988B1 (en) 2023-03-01
HRP20220269T8 (hr) 2022-12-09
PT3743420T (pt) 2022-02-04
BR112020013759A2 (pt) 2020-12-01
LT3743420T (lt) 2022-02-25
DK3743420T3 (da) 2022-03-07
US20230021916A1 (en) 2023-01-26
CA3088330A1 (en) 2019-08-01
ES2907833T3 (es) 2022-04-26

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