CN119350347A - 一氧化氮释放第5型磷酸二酯酶抑制剂 - Google Patents

一氧化氮释放第5型磷酸二酯酶抑制剂 Download PDF

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Publication number
CN119350347A
CN119350347A CN202411482883.4A CN202411482883A CN119350347A CN 119350347 A CN119350347 A CN 119350347A CN 202411482883 A CN202411482883 A CN 202411482883A CN 119350347 A CN119350347 A CN 119350347A
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CN
China
Prior art keywords
compound
ethyl
pyrimidin
methyl
propyl
Prior art date
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Pending
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CN202411482883.4A
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English (en)
Chinese (zh)
Inventor
N·阿尔米兰特
S·布兰比拉
L·斯托洛尼
F·因派纳提洛
E·巴斯蒂亚
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Nicox SA
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Nicox SA
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Publication of CN119350347A publication Critical patent/CN119350347A/zh
Pending legal-status Critical Current

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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)
CN202411482883.4A 2018-08-06 2019-07-31 一氧化氮释放第5型磷酸二酯酶抑制剂 Pending CN119350347A (zh)

Applications Claiming Priority (6)

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
CN201980052271.2A CN112566670B (zh) 2018-08-06 2019-07-31 一氧化氮释放第5型磷酸二酯酶抑制剂

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201980052271.2A Division CN112566670B (zh) 2018-08-06 2019-07-31 一氧化氮释放第5型磷酸二酯酶抑制剂

Publications (1)

Publication Number Publication Date
CN119350347A true CN119350347A (zh) 2025-01-24

Family

ID=67539493

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202411482883.4A Pending CN119350347A (zh) 2018-08-06 2019-07-31 一氧化氮释放第5型磷酸二酯酶抑制剂
CN201980052271.2A Active CN112566670B (zh) 2018-08-06 2019-07-31 一氧化氮释放第5型磷酸二酯酶抑制剂

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Country Status (11)

Country Link
US (2) US11980618B2 (https=)
EP (1) EP3833395A1 (https=)
JP (2) JP7596257B2 (https=)
KR (1) KR102836746B1 (https=)
CN (2) CN119350347A (https=)
AU (1) AU2019319004B2 (https=)
BR (1) BR112021001950A2 (https=)
CA (1) CA3108551A1 (https=)
MX (2) MX2021001503A (https=)
TW (1) TWI839375B (https=)
WO (1) WO2020030489A1 (https=)

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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
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
KR102731727B1 (ko) * 2020-07-30 2024-11-20 바이오프런트 쎄라퓨틱스 (베이징) 컴퍼니 리미티드 이중-기능성 화합물 및 이의 사용 방법
CN116456963A (zh) * 2020-11-02 2023-07-18 尼科斯股份有限公司 用于治疗干性年龄相关性黄斑变性、地图状萎缩和青光眼相关性神经变性的no-pde5抑制剂
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
JP2024541626A (ja) 2021-12-02 2024-11-08 ニコックス エス．エー． 一酸化窒素放出ホスホジエステラーゼ５阻害剤を含有する眼科用医薬組成物及びその製造方法
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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JPS60149521A (ja) 1984-01-18 1985-08-07 Eisai Co Ltd 高眼圧・緑内障治療・予防用点眼剤
US4975428A (en) 1988-05-31 1990-12-04 Iolab Corporation Treatment of glaucoma using phosphodiesterase inhibitors
GB9013750D0 (en) 1990-06-20 1990-08-08 Pfizer Ltd Therapeutic agents
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KR100358083B1 (ko) * 2000-02-17 2002-10-25 에스케이케미칼주식회사 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도
US20020168424A1 (en) 2002-07-31 2002-11-14 Dr. Mohsen Shahinpoor Nitric oxide (NO) donor+cGMP-PDE5 inhibitor as a topical drug for glaucoma
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KR102670626B1 (ko) 2017-05-22 2024-05-29 토파두르 파마 아게 가용성 구아닐레이트 사이클라제 활성제 및 포스포디에스테라제 억제제의 신규한 이중 작용 방식 및 이의 용도

Also Published As

Publication number Publication date
JP2024150732A (ja) 2024-10-23
WO2020030489A1 (en) 2020-02-13
CN112566670B (zh) 2024-11-12
US20210322413A1 (en) 2021-10-21
JP7596257B2 (ja) 2024-12-09
EP3833395A1 (en) 2021-06-16
CA3108551A1 (en) 2020-02-13
US20240245684A1 (en) 2024-07-25
KR102836746B1 (ko) 2025-07-21
KR20210041596A (ko) 2021-04-15
US11980618B2 (en) 2024-05-14
MX2021001503A (es) 2021-04-28
BR112021001950A2 (pt) 2021-04-27
TW202019491A (zh) 2020-06-01
AU2019319004A1 (en) 2021-03-25
TWI839375B (zh) 2024-04-21
JP2021533152A (ja) 2021-12-02
MX2023012941A (es) 2023-11-13
AU2019319004B2 (en) 2025-04-24
CN112566670A (zh) 2021-03-26

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