CR20250310A - Profármacos de inhibidores de la transcriptasa inversa de nucleósidos sustituidos en 4' - Google Patents

Profármacos de inhibidores de la transcriptasa inversa de nucleósidos sustituidos en 4'

Info

Publication number
CR20250310A
CR20250310A CR20250310A CR20250310A CR20250310A CR 20250310 A CR20250310 A CR 20250310A CR 20250310 A CR20250310 A CR 20250310A CR 20250310 A CR20250310 A CR 20250310A CR 20250310 A CR20250310 A CR 20250310A
Authority
CR
Costa Rica
Prior art keywords
reverse transcriptase
prodrugs
nucleoside reverse
transcriptase inhibitors
substituted nucleoside
Prior art date
Application number
CR20250310A
Other languages
English (en)
Inventor
Izzat T Raheem
Mark E Layton
Jay A Grobler
Mark W Embrey
Original Assignee
Merck Sharp & Dohme Llc
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 Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme Llc
Publication of CR20250310A publication Critical patent/CR20250310A/es

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14—Pyrrolo-pyrimidine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • AIDS & HIV (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)

Abstract

La presente invención se refiere a profármacos del compuesto A: que son inhibidores nucleosídicos de la translocación de la transcriptasa inversa (NRTTI) y son útiles en la inhibición de la transcriptasa inversa del VIH. La presente invención también se refiere al uso de estos compuestos para la profilaxis de la infección por VIH, el tratamiento de la infección por VIH y la profilaxis, el tratamiento y el retraso del inicio o la progresión del SIDA y/o complejos relacionados con el SIDA.
CR20250310A 2023-01-30 2024-01-26 Profármacos de inhibidores de la transcriptasa inversa de nucleósidos sustituidos en 4' CR20250310A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202363482133P 2023-01-30 2023-01-30
US202363607595P 2023-12-08 2023-12-08
PCT/US2024/013021 WO2024163262A2 (en) 2023-01-30 2024-01-26 Prodrugs of 4'-substituted nucleoside reverse transcriptase inhibitors

Publications (1)

Publication Number Publication Date
CR20250310A true CR20250310A (es) 2025-08-25

Family

ID=90362074

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20250310A CR20250310A (es) 2023-01-30 2024-01-26 Profármacos de inhibidores de la transcriptasa inversa de nucleósidos sustituidos en 4'

Country Status (17)

Country Link
US (1) US20240287124A1 (es)
EP (1) EP4658663A2 (es)
JP (1) JP7888031B2 (es)
KR (1) KR20250140092A (es)
CN (1) CN120958007A (es)
AU (1) AU2024213822A1 (es)
CL (1) CL2025002243A1 (es)
CO (1) CO2025010224A2 (es)
CR (1) CR20250310A (es)
DO (1) DOP2025000179A (es)
GE (1) GEAP202516835A (es)
IL (1) IL322370A (es)
JO (1) JOP20250193A1 (es)
MX (1) MX2025008847A (es)
PE (1) PE20252245A1 (es)
TW (1) TW202434594A (es)
WO (1) WO2024163262A2 (es)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015143712A1 (en) * 2014-03-28 2015-10-01 Merck Sharp & Dohme Corp. 4'-substituted nucleoside reverse transcriptase inhibitors
LT3347352T (lt) 2016-08-19 2019-08-12 Gilead Sciences, Inc. Terapiniai junginiai, naudotini živ viruso infekcijos profilaktikai arba terapiniam gydymui
US20190185508A1 (en) * 2017-12-15 2019-06-20 Merck Sharp & Dohme Corp. Deuterated nucleoside reverse transcriptase inhibitors
US20210323993A1 (en) 2018-08-30 2021-10-21 Glaxosmithkline Intellectual Property (No. 2) Limited Compounds Useful in HIV Therapy
PH12021500034A1 (en) * 2019-03-06 2022-06-06 Glaxosmithkline Ip No 2 Ltd Compounds useful in hiv therapy
IL289925B2 (en) 2019-07-27 2026-03-01 Brii Biosciences Inc A derivative of adenosine and a pharmaceutical preparation containing it
KR102987126B1 (ko) * 2020-03-20 2026-07-07 길리애드 사이언시즈, 인코포레이티드 4'-c-치환된-2-할로-2'-데옥시아데노신 뉴클레오시드의 프로드러그 및 이의 제조 및 사용 방법
KR20230132476A (ko) * 2021-01-25 2023-09-15 브리 바이오사이언시스, 인크. 아데노신 유도체 및 이를 포함하는 약제학적 조성물

Also Published As

Publication number Publication date
EP4658663A2 (en) 2025-12-10
GEAP202516835A (en) 2025-11-25
DOP2025000179A (es) 2025-09-15
IL322370A (en) 2025-09-01
AU2024213822A1 (en) 2025-08-07
MX2025008847A (es) 2025-09-02
JP7888031B2 (ja) 2026-07-10
WO2024163262A2 (en) 2024-08-08
US20240287124A1 (en) 2024-08-29
KR20250140092A (ko) 2025-09-24
WO2024163262A3 (en) 2024-10-10
PE20252245A1 (es) 2025-09-15
CN120958007A (zh) 2025-11-14
CL2025002243A1 (es) 2025-11-03
JP2025541056A (ja) 2025-12-18
CO2025010224A2 (es) 2025-08-19
JOP20250193A1 (ar) 2025-07-29
TW202434594A (zh) 2024-09-01

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