AR113980A1 - Método para mejorar la biodisponibilidad oral de una droga - Google Patents

Método para mejorar la biodisponibilidad oral de una droga

Info

Publication number
AR113980A1
AR113980A1 ARP180103719A ARP180103719A AR113980A1 AR 113980 A1 AR113980 A1 AR 113980A1 AR P180103719 A ARP180103719 A AR P180103719A AR P180103719 A ARP180103719 A AR P180103719A AR 113980 A1 AR113980 A1 AR 113980A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
drug
aryl
cycloalkyl
Prior art date
Application number
ARP180103719A
Other languages
English (en)
Inventor
Gerrit Herman Veeneman
Cormick Somhairle Mac
Original Assignee
Pharmacytics Bv
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 Pharmacytics Bv filed Critical Pharmacytics Bv
Publication of AR113980A1 publication Critical patent/AR113980A1/es

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Classifications

    • 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
    • A61K47/549Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18Acyclic radicals, substituted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/067Pyrimidine radicals with ribosyl as the saccharide radical

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

La presente pertenece al campo de las ciencias médicas. Provee métodos y preparaciones farmacéuticas En particular, se refiere a un método para incrementar la biodisponibilidad oral de drogas. También provee composiciones que comprenden una droga covalentemente unida a un sacárido. Más en particular, se refiere a un método para incrementar la biodisponibilidad oral de una droga mediante unión covalente de un resto molecular carbamoilalquilideno N-sustituido o no sustituido unido a azúcar a un grupo hidroxilo o tiol de una droga. Reivindicación 1: Un compuesto de fórmula (1), en donde el Azúcar está seleccionado a partir del grupo que consiste en monosacáridos y disacáridos a- y b-enlazados, en donde opcionalmente, uno o más grupos OH están reemplazados por un grupo R⁴; en donde R⁴ está seleccionado a partir del grupo que consiste en C₁₋₆ alcoxilo, cloro, flúor, ciano, CF₃, NH₂, C₁₋₆ alquilo-NH, C₁₋₆ dialquilo-N, C₁₋₆ cicloalquilo-N, C₁₋₆ alquilo-C(O)NH, C₁₋₆ alquilo-C(O)(C₁₋₆ alquil)-N, HC(O)(C₁₋₆ alquil)-N, C₁₋₆ alquilo-O-C(O)NH, C₁₋₆ alquilo-O-C(O)(C₁₋₆ alquil)-N, y C₁₋₆ alquilo-O-C(O)-O; R¹ está seleccionado a partir del grupo que consiste en H, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -R⁵-O-R⁷, -R⁵-S-R⁷, -R⁶-C(O)-R⁷, -R⁶-C(O)-O-R⁷, -R⁵-SO₂-R⁷, -R⁵-SO₂-NR⁷R⁸, C₃₋₇ cicloalquilo, C₄₋₇ cicloalquenilo, un heterociclo de 4 a 7 miembros, arilo y (C₁₋₃ alquil)-arilo; en donde R⁵ es C₂ o C₃ alquilo, R⁶ es C₁₋₃ alquilo, R⁷ y R⁸ son independientemente hidrógeno o C₁₋₃-alquilo; y en donde los grupos C₃₋₇ cicloalquilo, C₄₋₇ cicloalquenilo, un heterociclo de 4 a 7 miembros, arilo y (C₁₋₃ alquil)-arilo pueden estar opcionalmente sustituidos con R⁹, en donde R⁹ está seleccionado a partir del grupo que consiste en C₁₋₄ alquilo, C₁₋₄ alcoxilo, cloro, flúor, ciano, CF₃, amina, amida, carbamato y -C(O)O-(C₁₋₄-alquilo); R² y R³ son ambos H, o uno de R² y R³ es H y el otro es C₁₋₆ alquilo; X-DM representa un resto molecular de droga en donde X es O ó S; o una sal farmacéuticamente aceptable del mismo.
ARP180103719A 2017-12-21 2018-12-19 Método para mejorar la biodisponibilidad oral de una droga AR113980A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17209734 2017-12-21

Publications (1)

Publication Number Publication Date
AR113980A1 true AR113980A1 (es) 2020-07-08

Family

ID=60813629

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180103719A AR113980A1 (es) 2017-12-21 2018-12-19 Método para mejorar la biodisponibilidad oral de una droga

Country Status (9)

Country Link
US (1) US11633484B2 (es)
EP (1) EP3728280B1 (es)
JP (1) JP7333335B2 (es)
KR (1) KR20200104352A (es)
CN (1) CN111712507B (es)
AR (1) AR113980A1 (es)
CA (1) CA3086233A1 (es)
TW (1) TWI820068B (es)
WO (1) WO2019121734A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110857285B (zh) * 2018-08-22 2022-12-20 江苏万高药业股份有限公司 取代吡唑类化合物、其制备方法、药物组合物及用途
NL2028506B1 (en) 2021-06-21 2022-12-29 Pharmacytics B V Prodrugs with 1-(disulfanyl)alkyloxy-carbonyl units

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4236237A1 (de) * 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
AU2001225363A1 (en) 2000-01-14 2001-07-24 Strakan Limited Glycosides and orthoester glycosides of glucocorticoids and uses thereof
EP1487460A2 (en) 2002-02-28 2004-12-22 A & D Bioscience, Inc. Glycuronamides, glycosides and orthoester glycosides of fluoxetine, analogs and uses thereof
EP2098533A1 (en) 2008-03-07 2009-09-09 Pharmachemie B.V. Esters of glucuronide prodrugs of anthracyclines and method of preparation and use in tumor-selective chemotherapy
US8722864B2 (en) 2010-07-22 2014-05-13 NuTek Pharma Ltd. Glycosylated acetaminophen pro-drug analogs
WO2012035346A1 (en) 2010-09-15 2012-03-22 Shire, Llc Prodrugs of guanfacine
US9023813B2 (en) 2011-04-13 2015-05-05 NuTek Pharma Ltd. Synthesis and use of glycoside derivatives of propofol
IL290330B2 (en) * 2013-12-19 2023-09-01 Seagen Inc Methylene carbamate binders for use with drug-targeting conjugates
CN108136208B (zh) * 2015-09-22 2022-07-15 统帅青凤蝶生物科学公司 大麻素糖苷前药以及合成方法

Also Published As

Publication number Publication date
JP7333335B2 (ja) 2023-08-24
EP3728280B1 (en) 2023-06-28
WO2019121734A1 (en) 2019-06-27
US11633484B2 (en) 2023-04-25
KR20200104352A (ko) 2020-09-03
JP2021508339A (ja) 2021-03-04
EP3728280A1 (en) 2020-10-28
TW202002986A (zh) 2020-01-16
CN111712507A (zh) 2020-09-25
CA3086233A1 (en) 2019-06-27
TWI820068B (zh) 2023-11-01
CN111712507B (zh) 2024-02-06
US20200330602A1 (en) 2020-10-22
EP3728280C0 (en) 2023-06-28

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