CA3108551A1 - Nitric oxide releasing phosphodiesterase type 5 inhibitor - Google Patents

Nitric oxide releasing phosphodiesterase type 5 inhibitor Download PDF

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Publication number
CA3108551A1
CA3108551A1 CA3108551A CA3108551A CA3108551A1 CA 3108551 A1 CA3108551 A1 CA 3108551A1 CA 3108551 A CA3108551 A CA 3108551A CA 3108551 A CA3108551 A CA 3108551A CA 3108551 A1 CA3108551 A1 CA 3108551A1
Authority
CA
Canada
Prior art keywords
compound
pyrimidin
formula
nitrooxy
ethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3108551A
Other languages
English (en)
French (fr)
Inventor
Nicoletta Almirante
Stefania Brambilla
Laura Storoni
Francesco Impagnatiello
Elena Bastia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nicox SA
Original Assignee
Nicox SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Nicox SA filed Critical Nicox SA
Publication of CA3108551A1 publication Critical patent/CA3108551A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • 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
    • A61K31/505Pyrimidines; 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
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • 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)
CA3108551A 2018-08-06 2019-07-31 Nitric oxide releasing phosphodiesterase type 5 inhibitor Pending CA3108551A1 (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 (1)

Publication Number Publication Date
CA3108551A1 true CA3108551A1 (en) 2020-02-13

Family

ID=67539493

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3108551A Pending CA3108551A1 (en) 2018-08-06 2019-07-31 Nitric oxide releasing phosphodiesterase type 5 inhibitor

Country Status (11)

Country Link
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)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL137429A0 (en) 1999-07-28 2001-07-24 Pfizer Prod Inc Methods and compsitions for treating diseases and conditions of the eye
CN1374953A (zh) * 1999-09-16 2002-10-16 田边制药株式会社 含氮的6-员芳香环化合物
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
DE102005001989A1 (de) * 2005-01-15 2006-07-20 Bayer Healthcare Ag Intravenöse Formulierungen von PDE-Inhibitoren
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
US7993616B2 (en) 2007-09-19 2011-08-09 C-Quest Technologies LLC Methods and devices for reducing hazardous air pollutants
US8003811B2 (en) 2008-02-07 2011-08-23 Nicox S.A. Nitric oxide donor compounds
WO2010096320A2 (en) * 2009-02-18 2010-08-26 Bezwada Biomedical, Llc Controlled release of nitric oxide and drugs from functionalized macromers and oligomers
WO2011032936A1 (en) * 2009-09-15 2011-03-24 Dsm Ip Assets B.V. Nitrooxyesters, their preparation and use
CA2784788A1 (en) * 2009-12-18 2011-06-23 Exodos Life Sciences Limited Partnership Methods and compositions for treating peripheral vascular disease
EP2911656B1 (en) 2012-10-23 2020-12-02 Nicox SA Quinone based nitric oxide donating compounds for ophthalmic use
EP2826491A1 (en) * 2013-07-15 2015-01-21 Nicox Science Ireland Ophthalmic compositions containing a nitric oxide donor
TW201625584A (zh) 2014-07-02 2016-07-16 諾華公司 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途
ES2632808T3 (es) 2014-09-04 2017-09-15 Nicox Science Ireland Compuestos de carnosina donadores de óxido nítrico
JP6820847B2 (ja) 2014-11-19 2021-01-27 ニコックス エス.エー. プロスタグランジンと一酸化窒素供与体との組み合わせ
US10047047B2 (en) 2015-03-31 2018-08-14 Nicox S.A. Nitric oxide donating derivatives of latanoprost free acid
US10280138B2 (en) * 2015-03-31 2019-05-07 Nicox S.A. Nitric oxide donating derivatives of fluprostenol
EP3088388A1 (en) * 2015-04-30 2016-11-02 NicOx S.A. Nitric oxide donating derivatives of prostaglandins
SMT202200190T1 (it) 2015-11-16 2022-07-21 Topadur Pharma Ag Derivati del 2-fenil-3,4-diidropirrolo[2,1-f] [1,2,4]triazinone come inibitori della fosfodesterasi e loro usi
MX2019013626A (es) 2017-05-22 2020-01-13 Topadur Pharma Ag Modo de accion dual novedoso de activadores de guanilato ciclasa solubles e inhibidores de fosfodiesterasa y usos de los mismos.

Also Published As

Publication number Publication date
JP2024150732A (ja) 2024-10-23
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
AU2019319004B2 (en) 2025-04-24
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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