ES3018557T3 - Sal de un compuesto de pirimido[6,1-a]isoquinolin-4-ona - Google Patents

Sal de un compuesto de pirimido[6,1-a]isoquinolin-4-ona Download PDF

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Publication number
ES3018557T3
ES3018557T3 ES16704896T ES16704896T ES3018557T3 ES 3018557 T3 ES3018557 T3 ES 3018557T3 ES 16704896 T ES16704896 T ES 16704896T ES 16704896 T ES16704896 T ES 16704896T ES 3018557 T3 ES3018557 T3 ES 3018557T3
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ES
Spain
Prior art keywords
rpl554
salt
salts
acid
ethane
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Active
Application number
ES16704896T
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English (en)
Spanish (es)
Inventor
Peter Lionel Spargo
Edward James French
Julian Scott Northen
John Mykytiuk
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Verona Pharma Ltd
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Verona Pharma Ltd
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Application filed by Verona Pharma Ltd filed Critical Verona Pharma Ltd
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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
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
ES16704896T 2015-02-11 2016-02-10 Sal de un compuesto de pirimido[6,1-a]isoquinolin-4-ona Active ES3018557T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB201502260A GB201502260D0 (en) 2015-02-11 2015-02-11 Salt of Pyrimido[6,1-A]Isoquinolin-4-one compound
PCT/GB2016/050313 WO2016128742A1 (en) 2015-02-11 2016-02-10 Salt of a pyrimido[6,1-a]isoquinolin-4-one compound

Publications (1)

Publication Number Publication Date
ES3018557T3 true ES3018557T3 (es) 2025-05-16

Family

ID=52781414

Family Applications (1)

Application Number Title Priority Date Filing Date
ES16704896T Active ES3018557T3 (es) 2015-02-11 2016-02-10 Sal de un compuesto de pirimido[6,1-a]isoquinolin-4-ona

Country Status (13)

Country Link
US (2) US10463665B2 (enExample)
EP (2) EP3256472B1 (enExample)
JP (2) JP7089366B2 (enExample)
CN (2) CN113105453A (enExample)
AU (2) AU2016217674B2 (enExample)
CA (1) CA2974605C (enExample)
ES (1) ES3018557T3 (enExample)
GB (1) GB201502260D0 (enExample)
IL (1) IL253595B (enExample)
MX (1) MX382019B (enExample)
PT (1) PT3256472T (enExample)
WO (1) WO2016128742A1 (enExample)
ZA (1) ZA201705112B (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10864213B2 (en) 2014-05-12 2020-12-15 Verona Pharma Plc Treatment
MX2017003102A (es) 2014-09-15 2017-06-14 Verona Pharma Plc Formulacion para inhalacion liquida que comprende rpl554.
GB201502260D0 (en) 2015-02-11 2015-04-01 Verona Pharma Plc Salt of Pyrimido[6,1-A]Isoquinolin-4-one compound
GB201613054D0 (en) 2016-07-28 2016-09-14 Verona Pharma Plc New compound and process
GB2578093B (en) * 2018-10-09 2020-11-18 Verona Pharma Plc Liquid pharmaceutical composition comprising RPL554 and HFA-134A
GB201911517D0 (en) * 2019-08-12 2019-09-25 Verona Pharma Plc Pharmaceutical composition
JP7712276B2 (ja) * 2020-01-15 2025-07-23 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド 三環式pde3/pde4二重阻害剤化合物の医薬組成物
CA3176481A1 (en) * 2020-04-22 2021-10-28 Marjoh NAUTA Coronavirus vaccine
WO2023076205A1 (en) 2021-10-29 2023-05-04 Teva Pharmaceuticals International Gmbh Solid state forms of ensifentrine and process for preparation thereof
TW202325301A (zh) * 2021-12-14 2023-07-01 大陸商海思科醫藥集團股份有限公司 三環稠雜環類pde3/4雙重抑制及其用途
GB202202297D0 (en) 2022-02-21 2022-04-06 Verona Pharma Plc Formulation production process
JP2025527317A (ja) * 2022-08-08 2025-08-20 ヴェローナ ファーマ ピーエルシー 中等度の慢性閉塞性肺疾患(copd)の治療のためのエンシフェントリン(rpl-554)
EP4378942A1 (en) 2022-12-02 2024-06-05 Sandoz AG Crystal form of a pde3/4 inhibitor
US12194045B1 (en) 2023-06-26 2025-01-14 Verona Pharma Plc Particulate composition
WO2025176871A1 (en) 2024-02-23 2025-08-28 Inke, S.A. Process for preparing pyrimido[6,1-a]isoquinoline-4-ones
WO2026003867A1 (en) * 2024-06-24 2026-01-02 Neuland Laboratories Limited An improved process for the preparation of ensifentrine and its purification thereof

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZW6284A1 (en) 1983-05-05 1985-10-30 Hoffmann La Roche Novel pyrimidone derivatives
DE3816995A1 (de) 1988-05-19 1989-11-23 Hoechst Ag Verwendung von pyrimido-(6,1-a)-isochinolin-4-on-derivaten und medizinische zubereitungen auf basis dieser verbindungen
ES2208310T3 (es) 1999-03-31 2004-06-16 Vernalis Limited Derivados de pirimido(6,1-a) isoquinolin-4-ona.
US20030235631A1 (en) * 2002-06-17 2003-12-25 Pfizer Inc. Combination treatment for depression and anxiety
DE602005027866D1 (de) * 2004-09-08 2011-06-16 Nycomed Gmbh 3-oxa-10-aza-phenanthrene als pde4- oder pde3/4-inhibitoren
AU2008316284A1 (en) 2007-10-25 2009-04-30 Merck Frosst Canada Ltd. Novel crystalline salts of montelukast
EP2558101A4 (en) 2010-04-15 2013-09-18 Univ Mcgill TOPICAL TREATMENTS OF PAIN
CA2807082C (en) * 2010-08-09 2017-07-25 Verona Pharma Plc Crystalline form of pyrimido[6,1-a]isoquinolin-4-one compound
EP2647627A1 (en) * 2012-04-02 2013-10-09 Almirall, S.A. Salts of 5-[(1r)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl] ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1h)-one.
TWI643853B (zh) 2013-02-27 2018-12-11 阿爾米雷爾有限公司 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類
JP6560986B2 (ja) * 2013-03-15 2019-08-14 ヴェローナ ファーマ ピーエルシー 複合製剤
US10864213B2 (en) 2014-05-12 2020-12-15 Verona Pharma Plc Treatment
MX2017003102A (es) 2014-09-15 2017-06-14 Verona Pharma Plc Formulacion para inhalacion liquida que comprende rpl554.
GB201502260D0 (en) * 2015-02-11 2015-04-01 Verona Pharma Plc Salt of Pyrimido[6,1-A]Isoquinolin-4-one compound
GB201613054D0 (en) 2016-07-28 2016-09-14 Verona Pharma Plc New compound and process
GB2578093B (en) 2018-10-09 2020-11-18 Verona Pharma Plc Liquid pharmaceutical composition comprising RPL554 and HFA-134A
WO2023076205A1 (en) 2021-10-29 2023-05-04 Teva Pharmaceuticals International Gmbh Solid state forms of ensifentrine and process for preparation thereof

Also Published As

Publication number Publication date
CA2974605A1 (en) 2016-08-18
US10463665B2 (en) 2019-11-05
AU2016217674A1 (en) 2017-08-10
CN113105453A (zh) 2021-07-13
US20200016158A1 (en) 2020-01-16
MX2017010195A (es) 2017-11-17
EP4461358A3 (en) 2025-01-15
CN107406446B (zh) 2021-12-28
IL253595A0 (en) 2017-09-28
US11491155B2 (en) 2022-11-08
AU2016217674B2 (en) 2020-04-30
ZA201705112B (en) 2022-05-25
NZ733926A (en) 2023-10-27
JP7110303B2 (ja) 2022-08-01
MX382019B (es) 2025-03-13
EP3256472B1 (en) 2025-03-19
GB201502260D0 (en) 2015-04-01
JP7089366B2 (ja) 2022-06-22
PT3256472T (pt) 2025-04-11
IL253595B (en) 2021-04-29
EP4461358A2 (en) 2024-11-13
JP2018505192A (ja) 2018-02-22
US20180021337A1 (en) 2018-01-25
AU2020205281A1 (en) 2020-08-06
JP2021046405A (ja) 2021-03-25
AU2020205281B2 (en) 2021-07-15
EP3256472A1 (en) 2017-12-20
CA2974605C (en) 2024-02-13
WO2016128742A1 (en) 2016-08-18
CN107406446A (zh) 2017-11-28

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