AU2019319004B2 - Nitric oxide releasing phosphodiesterase type 5 inhibitor - Google Patents

Nitric oxide releasing phosphodiesterase type 5 inhibitor Download PDF

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Publication number
AU2019319004B2
AU2019319004B2 AU2019319004A AU2019319004A AU2019319004B2 AU 2019319004 B2 AU2019319004 B2 AU 2019319004B2 AU 2019319004 A AU2019319004 A AU 2019319004A AU 2019319004 A AU2019319004 A AU 2019319004A AU 2019319004 B2 AU2019319004 B2 AU 2019319004B2
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Australia
Prior art keywords
compound
pyrimidin
nitrooxy
ethyl
methyl
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AU2019319004A
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AU2019319004A1 (en
Inventor
Nicoletta Almirante
Elena Bastia
Stefania Brambilla
Francesco Impagnatiello
Laura Storoni
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Nicox SA
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Nicox SA
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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
    • A61K31/185—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
    • 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
    • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2019319004A 2018-08-06 2019-07-31 Nitric oxide releasing phosphodiesterase type 5 inhibitor Active AU2019319004B2 (en)

Applications Claiming Priority (5)

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

Publications (2)

Publication Number Publication Date
AU2019319004A1 AU2019319004A1 (en) 2021-03-25
AU2019319004B2 true AU2019319004B2 (en) 2025-04-24

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AU2019319004A Active AU2019319004B2 (en) 2018-08-06 2019-07-31 Nitric oxide releasing phosphodiesterase type 5 inhibitor

Country Status (11)

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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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EP4100014B1 (en) * 2020-02-05 2024-01-03 Nicox S.A. Compositions for the treatment of glaucoma and ocular hypertension
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
CA3187693A1 (en) * 2020-07-30 2022-02-03 Zheng Huang Drug conjugates comprising apremilast, and a nitric oxide-releasing moiety and uses thereof
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
TW202233623A (zh) * 2020-11-09 2022-09-01 南韓商日東製藥股份有限公司 氮氧化物供與的pde-5及/或pde-6抑制劑化合物及其用途
WO2023005180A1 (en) * 2021-07-30 2023-02-02 Biofront Therapeutics (Beijing) Co., Ltd. Dual-functional compounds and methods of use
CA3239629A1 (en) 2021-12-02 2023-06-08 Nicoletta Almirante Ophthalmic pharmaceutical compositions containing a nitric oxide-releasing phosphodiesterase 5 inhibitor and method for the preparation thereof
EP4233867B1 (en) 2022-02-24 2025-09-03 Nicox SA Pde5 inhibitor for use in the treatment of anterior ischemic optic neuropathy

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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
WO2008075152A1 (en) * 2006-12-15 2008-06-26 Pfizer Products Inc. 1- [4- (sulfonyl) -phenyl] -5- (benzyl) -ih-i, 2, 4-triazol derivatives as inhibitors of carbonic anhydrase for treating glaucoma or ocular hypertension
CN102498088A (zh) * 2009-09-15 2012-06-13 帝斯曼知识产权资产管理有限公司 硝基氧基酯及其制备和用途
EP2826491A1 (en) * 2013-07-15 2015-01-21 Nicox Science Ireland Ophthalmic compositions containing a nitric oxide donor
WO2016156104A1 (en) * 2015-03-31 2016-10-06 Nicox S.A. Nitric oxide donating derivatives of latanoprost free acid
WO2016155906A1 (en) * 2015-03-31 2016-10-06 Nicox S.A. Nitric oxide donating derivatives of fluprostenol
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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JP2024150732A (ja) 2024-10-23
CA3108551A1 (en) 2020-02-13
AU2019319004A1 (en) 2021-03-25
BR112021001950A2 (pt) 2021-04-27
CN119350347A (zh) 2025-01-24
US20240245684A1 (en) 2024-07-25
KR102836746B1 (ko) 2025-07-21
MX2023012941A (es) 2023-11-13
TWI839375B (zh) 2024-04-21
WO2020030489A1 (en) 2020-02-13
MX2021001503A (es) 2021-04-28
CN112566670A (zh) 2021-03-26
US20210322413A1 (en) 2021-10-21
US11980618B2 (en) 2024-05-14
TW202019491A (zh) 2020-06-01
JP2021533152A (ja) 2021-12-02
CN112566670B (zh) 2024-11-12
EP3833395A1 (en) 2021-06-16
KR20210041596A (ko) 2021-04-15
JP7596257B2 (ja) 2024-12-09

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