TW202334158A - 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途 - Google Patents

含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途 Download PDF

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TW202334158A
TW202334158A TW111141254A TW111141254A TW202334158A TW 202334158 A TW202334158 A TW 202334158A TW 111141254 A TW111141254 A TW 111141254A TW 111141254 A TW111141254 A TW 111141254A TW 202334158 A TW202334158 A TW 202334158A
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alkyl
pharmaceutically acceptable
compound
stereoisomer
acceptable salt
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TW111141254A
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丁曉
秦烈娜
任峰
徐劍宇
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香港商英矽智能科技知識產權有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW111141254A 2021-10-28 2022-10-28 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途 TW202334158A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2021127023 2021-10-28
WOPCT/CN2021/127023 2021-10-28
CN2022112270 2022-08-12
WOPCT/CN2022/112270 2022-08-12

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TW202334158A true TW202334158A (zh) 2023-09-01

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TW111141254A TW202334158A (zh) 2021-10-28 2022-10-28 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途
TW111141004A TW202334134A (zh) 2021-10-28 2022-10-28 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途
TW111141238A TW202332677A (zh) 2021-10-28 2022-10-28 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途

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TW111141238A TW202332677A (zh) 2021-10-28 2022-10-28 含脯胺醯羥化酶結構域之蛋白質(phd)抑制劑及其用途

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US (6) US20250034132A1 (https=)
EP (2) EP4422623A4 (https=)
JP (2) JP2024539946A (https=)
KR (2) KR20240095274A (https=)
CN (2) CN118488838A (https=)
AR (3) AR127501A1 (https=)
AU (1) AU2022378858A1 (https=)
CA (1) CA3235718A1 (https=)
IL (1) IL312220A (https=)
TW (3) TW202334158A (https=)
WO (3) WO2023072246A1 (https=)

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KR20240095274A (ko) 2021-10-28 2024-06-25 인실리코 메디신 아이피 리미티드 프롤릴 히드록실라제 도메인-함유 단백질 (phd) 억제제 및 그의 용도
GB202301059D0 (en) 2023-01-25 2023-03-08 Univ Oxford Innovation Ltd PHD inhibitors
EP4702023A1 (en) * 2023-04-28 2026-03-04 Insilico Medicine IP Limited Crystalline prolyl hydroxylase domain-containing protein (phd) inhibitor and uses thereof
AU2024261389A1 (en) * 2023-04-28 2025-10-30 Insilico Medicine Ip Limited Prolyl hydroxylase domain-containing protein (phd) inhibitors, combinations and uses thereof
CN121057737A (zh) * 2023-04-28 2025-12-02 英矽智能科技知识产权有限公司 含脯氨酰羟化酶结构域的蛋白质(phd)抑制剂结晶及其用途
CN117402178B (zh) * 2023-12-15 2024-03-08 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的嘧啶类化合物
CN117603230B (zh) * 2023-12-15 2025-03-21 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的三并环类化合物
CN117756822B (zh) * 2023-12-20 2025-04-18 英矽智能科技(上海)有限公司 作为jak抑制剂和phd抑制剂的嘧啶氨基类化合物
CN117736227B (zh) * 2023-12-20 2025-01-21 英矽智能科技(上海)有限公司 抑制jak和phd的一类化合物
CN117924326B (zh) * 2024-01-23 2025-01-21 英矽智能科技(上海)有限公司 一类抑制jak和phd的三并环类化合物

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US11780854B2 (en) 2023-10-10
JP2024539946A (ja) 2024-10-31
US20240002406A1 (en) 2024-01-04
EP4422623A4 (en) 2025-10-29
JP2024541910A (ja) 2024-11-13
AR127488A1 (es) 2024-01-31
AR127501A1 (es) 2024-01-31
AR127500A1 (es) 2024-01-31
TW202334134A (zh) 2023-09-01
US20250034132A1 (en) 2025-01-30
CN118488838A (zh) 2024-08-13
EP4422623A1 (en) 2024-09-04
US12209101B2 (en) 2025-01-28
KR20240095274A (ko) 2024-06-25
WO2023072257A1 (en) 2023-05-04
EP4423074A1 (en) 2024-09-04
CN118591533A (zh) 2024-09-03
US20230192688A1 (en) 2023-06-22
CA3235718A1 (en) 2023-05-04
US11731987B2 (en) 2023-08-22
WO2023072246A1 (en) 2023-05-04
US12071443B2 (en) 2024-08-27
TW202332677A (zh) 2023-08-16
US20240067661A1 (en) 2024-02-29
AU2022378858A1 (en) 2024-05-02
KR20240093899A (ko) 2024-06-24
US20230192723A1 (en) 2023-06-22
IL312220A (en) 2024-06-01
EP4423074A4 (en) 2025-09-03
WO2023072240A1 (en) 2023-05-04
US20260015349A1 (en) 2026-01-15

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