CN115776890A - 作为眼病治疗剂的trpv4抑制剂 - Google Patents

作为眼病治疗剂的trpv4抑制剂 Download PDF

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Publication number
CN115776890A
CN115776890A CN202180045312.2A CN202180045312A CN115776890A CN 115776890 A CN115776890 A CN 115776890A CN 202180045312 A CN202180045312 A CN 202180045312A CN 115776890 A CN115776890 A CN 115776890A
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China
Prior art keywords
cyclopropyl
hexahydro
pyrimido
phenyl
alkyl
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Pending
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CN202180045312.2A
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Chinese (zh)
Inventor
大原健太郎
渡边修造
原英彰
嶋泽雅光
须轻英仁
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Raqualia Pharma Inc
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Raqualia Pharma Inc
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Publication of CN115776890A publication Critical patent/CN115776890A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/535—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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
    • A01K2207/00—Modified animals
    • A01K2207/30—Animals modified by surgical methods
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
    • A01K2227/00—Animals characterised by species
    • A01K2227/10—Mammal
    • A01K2227/105—Murine
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
    • A01K2267/00—Animals characterised by purpose
    • A01K2267/03—Animal model, e.g. for test or diseases
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/158—Expression markers
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/16—Ophthalmology
    • G01N2800/164—Retinal disorders, e.g. retinopathy

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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Urology & Nephrology (AREA)
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  • Biotechnology (AREA)
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  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Ophthalmology & Optometry (AREA)
  • Wood Science & Technology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CN202180045312.2A 2020-07-16 2021-07-16 作为眼病治疗剂的trpv4抑制剂 Pending CN115776890A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063052572P 2020-07-16 2020-07-16
US63/052,572 2020-07-16
PCT/JP2021/026829 WO2022014707A1 (ja) 2020-07-16 2021-07-16 眼疾患の治療薬としてのｔｒｐｖ４阻害薬

Publications (1)

Publication Number Publication Date
CN115776890A true CN115776890A (zh) 2023-03-10

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CN202180045312.2A Pending CN115776890A (zh) 2020-07-16 2021-07-16 作为眼病治疗剂的trpv4抑制剂

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US (1) US20230255965A1 (https=)
EP (1) EP4183415A4 (https=)
JP (1) JPWO2022014707A1 (https=)
KR (1) KR20230041680A (https=)
CN (1) CN115776890A (https=)
BR (1) BR112022024553A2 (https=)
CA (1) CA3189206A1 (https=)
MX (1) MX2023000610A (https=)
TW (1) TW202216143A (https=)
WO (1) WO2022014707A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116726013A (zh) * 2023-04-25 2023-09-12 中国科学院大学深圳医院(光明) Gsk2193874在防治痛性糖尿病周围神经病变中的应用
WO2024217446A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217428A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217439A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用

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MX2017011166A (es) * 2017-08-31 2019-03-07 Univ Mexico Nac Autonoma Uso de los farmacos antagonistas del canal ionico transient receptor potential vaniloid 4 (trpv4) para el tratamiento del edema macular.
CN115427409A (zh) * 2020-04-30 2022-12-02 拉夸里亚创药株式会社 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物

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US20130303539A1 (en) * 2012-05-11 2013-11-14 David Krizaj Compounds with trpv4 activity, compositions and associated methods thereof
MX2017011166A (es) * 2017-08-31 2019-03-07 Univ Mexico Nac Autonoma Uso de los farmacos antagonistas del canal ionico transient receptor potential vaniloid 4 (trpv4) para el tratamiento del edema macular.
CN115427409A (zh) * 2020-04-30 2022-12-02 拉夸里亚创药株式会社 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024217446A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217428A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217439A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
CN116726013A (zh) * 2023-04-25 2023-09-12 中国科学院大学深圳医院(光明) Gsk2193874在防治痛性糖尿病周围神经病变中的应用

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BR112022024553A2 (pt) 2023-01-24
TW202216143A (zh) 2022-05-01
WO2022014707A1 (ja) 2022-01-20
US20230255965A1 (en) 2023-08-17
JPWO2022014707A1 (https=) 2022-01-20
EP4183415A4 (en) 2024-07-17
MX2023000610A (es) 2023-02-13
KR20230041680A (ko) 2023-03-24
EP4183415A1 (en) 2023-05-24
CA3189206A1 (en) 2022-01-20

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