JP7596257B2 - 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬 - Google Patents

一酸化窒素放出性ホスホジエステラーゼ５型阻害薬 Download PDF

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JP7596257B2
JP7596257B2 JP2021506326A JP2021506326A JP7596257B2 JP 7596257 B2 JP7596257 B2 JP 7596257B2 JP 2021506326 A JP2021506326 A JP 2021506326A JP 2021506326 A JP2021506326 A JP 2021506326A JP 7596257 B2 JP7596257 B2 JP 7596257B2
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compound
pyrimidin
nitrooxy
ethyl
methyl
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JP2021533152A5 (enExample
JP2021533152A (ja
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アルミランテ，ニコレッタ
ブランビッラ，ステファーニア
ストローニ，ラウラ
インパグナッティエッロ，フランチェスコ
バスティア，エレナ
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ニコックス エス．エー．
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021506326A 2018-08-06 2019-07-31 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬 Active JP7596257B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024125823A JP2024150732A (ja) 2018-08-06 2024-08-01 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP18187482.7 2018-08-06
EP18187482 2018-08-06
EP18210147 2018-12-04
EP18210147.7 2018-12-04
PCT/EP2019/070597 WO2020030489A1 (en) 2018-08-06 2019-07-31 Nitric oxide releasing phosphodiesterase type 5 inhibitor

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JP2024125823A Division JP2024150732A (ja) 2018-08-06 2024-08-01 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬

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JP2021533152A JP2021533152A (ja) 2021-12-02
JP2021533152A5 JP2021533152A5 (enExample) 2022-08-08
JP7596257B2 true JP7596257B2 (ja) 2024-12-09

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JP2024125823A Pending JP2024150732A (ja) 2018-08-06 2024-08-01 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬

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US (2) US11980618B2 (enExample)
EP (1) EP3833395A1 (enExample)
JP (2) JP7596257B2 (enExample)
KR (1) KR102836746B1 (enExample)
CN (2) CN112566670B (enExample)
AU (1) AU2019319004B2 (enExample)
BR (1) BR112021001950A2 (enExample)
CA (1) CA3108551A1 (enExample)
MX (2) MX2021001503A (enExample)
TW (1) TWI839375B (enExample)
WO (1) WO2020030489A1 (enExample)

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JP2023516891A (ja) * 2020-02-05 2023-04-21 ニコックス エス．エー． 緑内障及び高眼圧症の処置のための組成物

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CN111217834B (zh) * 2020-02-21 2021-10-26 维眸生物科技（上海）有限公司 Rock激酶抑制剂的硝基氧衍生物
WO2022022669A1 (en) * 2020-07-30 2022-02-03 Biofront Therapeutics (Beijing) Co., Ltd. Dual-functional compounds and methods of use
WO2022090379A1 (en) 2020-11-02 2022-05-05 Nicox S.A. No-pde5 inhibitor for use in treating dry age-related macular degeneration, geographic atrophy and glaucoma-associated neurodegeneration
UY39509A (es) * 2020-11-09 2022-01-31 Ildong Pharmaceutical Co Ltd Compuestos inhibidores de la pde-5 y/o la pde-6 donantes de óxido de nitrógeno, y usos de estos
WO2023005180A1 (en) * 2021-07-30 2023-02-02 Biofront Therapeutics (Beijing) Co., Ltd. Dual-functional compounds and methods of use
US20250017928A1 (en) 2021-12-02 2025-01-16 Nicox Sa Ophthalmic pharmaceutical compositions containing a nitric oxide-releasing phosphodiesterase 5 inhibitor and method for the preparation thereof
PL4233867T3 (pl) 2022-02-24 2026-02-09 Nicox Sa Inhibitor PDE5 do zastosowania w leczeniu przedniej niedokrwiennej neuropatii nerwu wzrokowego

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US20020168424A1 (en) 2002-07-31 2002-11-14 Dr. Mohsen Shahinpoor Nitric oxide (NO) donor+cGMP-PDE5 inhibitor as a topical drug for glaucoma
JP2011511022A (ja) 2008-02-07 2011-04-07 ニコックス エス エイ 一酸化窒素供与化合物
WO2016155906A1 (en) 2015-03-31 2016-10-06 Nicox S.A. Nitric oxide donating derivatives of fluprostenol
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WO2016156104A1 (en) 2015-03-31 2016-10-06 Nicox S.A. Nitric oxide donating derivatives of latanoprost free acid
WO2017085056A1 (en) 2015-11-16 2017-05-26 Topadur Pharma Ag 2-phenyl-3,4-dihydropyrrolo[2,1 -f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023516891A (ja) * 2020-02-05 2023-04-21 ニコックス エス．エー． 緑内障及び高眼圧症の処置のための組成物
JP7708771B2 (ja) 2020-02-05 2025-07-15 ニコックス エス．エー． 緑内障及び高眼圧症の処置のための組成物

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US12642800B2 (en) 2026-06-02
TWI839375B (zh) 2024-04-21
CN119350347A (zh) 2025-01-24
AU2019319004B2 (en) 2025-04-24
MX2021001503A (es) 2021-04-28
WO2020030489A1 (en) 2020-02-13
CA3108551A1 (en) 2020-02-13
US20210322413A1 (en) 2021-10-21
BR112021001950A2 (pt) 2021-04-27
KR20210041596A (ko) 2021-04-15
TW202019491A (zh) 2020-06-01
JP2021533152A (ja) 2021-12-02
US20240245684A1 (en) 2024-07-25
KR102836746B1 (ko) 2025-07-21
CN112566670B (zh) 2024-11-12
JP2024150732A (ja) 2024-10-23
MX2023012941A (es) 2023-11-13
CN112566670A (zh) 2021-03-26
US11980618B2 (en) 2024-05-14
AU2019319004A1 (en) 2021-03-25
EP3833395A1 (en) 2021-06-16

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