PE20230466A1 - N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos - Google Patents

N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos

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Publication number
PE20230466A1
PE20230466A1 PE2022001688A PE2022001688A PE20230466A1 PE 20230466 A1 PE20230466 A1 PE 20230466A1 PE 2022001688 A PE2022001688 A PE 2022001688A PE 2022001688 A PE2022001688 A PE 2022001688A PE 20230466 A1 PE20230466 A1 PE 20230466A1
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PE
Peru
Prior art keywords
hydroxycytidine
derivatives
uses related
pharmaceutically acceptable
antiviral uses
Prior art date
Application number
PE2022001688A
Other languages
English (en)
Inventor
George R Painter
Gregory R Bluemling
Michael G Natchus
Shuli Mao
Jose Marengo
Michael W Hager
David Perryman
Original Assignee
Univ Emory
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 Univ Emory filed Critical Univ Emory
Publication of PE20230466A1 publication Critical patent/PE20230466A1/es

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    • AHUMAN NECESSITIES
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    • 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
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
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    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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
    • A61K31/4965Non-condensed pyrazines
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    • 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
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    • 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
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/665Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • AHUMAN NECESSITIES
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Abstract

Referida a una composicion farmaceutica que comprende un excipiente farmaceuticamente aceptable y un compuesto derivado de N4-hidroxicitidina representado por la Formula XXI o un tautomero del mismo, o una sal farmaceuticamente aceptable o fisiologicamente aceptable del mismo, en la que R1 es H, HO-P(O)(OH)-, HO-P(O)(OH)-O-P(O)(OH)-, HO-P(O)(OH)-O-P(O)(OH)-O-P(O)(OH) o R6-CO-, en donde R6 es alquilo o carbociclilo. Dichas composiciones estan relacionadas con el tratamiento o la profilaxis de infecciones virales, en particular, 2019-nCoV.
PE2022001688A 2020-02-07 2021-02-07 N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos PE20230466A1 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202062971559P 2020-02-07 2020-02-07
US202062988133P 2020-03-11 2020-03-11
US202062994604P 2020-03-25 2020-03-25
US202063006625P 2020-04-07 2020-04-07
PCT/US2021/016984 WO2021159044A1 (en) 2020-02-07 2021-02-07 N4-hydroxycytidine and derivatives and anti-viral uses related thereto

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PE20230466A1 true PE20230466A1 (es) 2023-03-14

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US (1) US20210252033A1 (es)
EP (1) EP4017501A4 (es)
JP (1) JP2023512666A (es)
KR (1) KR20220139914A (es)
CN (1) CN115666587A (es)
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AU (1) AU2021216049A1 (es)
BR (1) BR112022015479A2 (es)
CA (1) CA3167054A1 (es)
CL (1) CL2022000423A1 (es)
CO (1) CO2022008092A2 (es)
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KR20230130175A (ko) * 2014-12-26 2023-09-11 에모리 유니버시티 N4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도
AU2018378832B9 (en) 2017-12-07 2021-05-27 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
US20230270669A1 (en) * 2020-09-04 2023-08-31 Mexichem Fluor S.A. De C.V. Pharmaceutical composition
CN117642410A (zh) * 2021-06-18 2024-03-01 苏州春海生物医药有限公司 N4-羟基胞苷的酯衍生物及其用途
CN115960148B (zh) * 2021-08-27 2023-12-12 南京知和医药科技有限公司 一种新型的胞苷衍生物及其药物组合物和用途
CN115737665A (zh) * 2021-09-02 2023-03-07 广州谷森制药有限公司 胞苷衍生物和与其相关的抗病毒用途
WO2023070058A1 (en) * 2021-10-20 2023-04-27 Merck Sharp & Dohme Llc Treatment of viruses with antiviral nucleosides
WO2023067623A1 (en) * 2021-10-20 2023-04-27 Council Of Scientific And Industrial Research An Indian Registered Body Incorporated Under The Regn. Of Soc. Act (Act Xxi Of 1860) A short and cost effective synthetic route towards anti viral eidd-1931 and its hydrate polymorphs
CN114306254B (zh) * 2021-11-30 2023-11-03 南京正济医药研究有限公司 一种Molnupiravir口服固体制剂及其制备方法
US11541071B1 (en) 2021-12-16 2023-01-03 Ascletis BioScience Co., Ltd Nucleoside derivatives and methods of use thereof
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