AR113980A1 - Método para mejorar la biodisponibilidad oral de una droga - Google Patents
Método para mejorar la biodisponibilidad oral de una drogaInfo
- 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
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/18—Acyclic radicals, substituted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
-
- 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
- C07H19/06—Pyrimidine radicals
-
- 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
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine 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.
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)
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)
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 |
-
2018
- 2018-12-18 CA CA3086233A patent/CA3086233A1/en active Pending
- 2018-12-18 WO PCT/EP2018/085567 patent/WO2019121734A1/en active Search and Examination
- 2018-12-18 JP JP2020554572A patent/JP7333335B2/ja active Active
- 2018-12-18 CN CN201880089355.9A patent/CN111712507B/zh active Active
- 2018-12-18 KR KR1020207021211A patent/KR20200104352A/ko not_active Application Discontinuation
- 2018-12-18 US US16/956,172 patent/US11633484B2/en active Active
- 2018-12-18 EP EP18816140.0A patent/EP3728280B1/en active Active
- 2018-12-19 AR ARP180103719A patent/AR113980A1/es unknown
- 2018-12-20 TW TW107146115A patent/TWI820068B/zh active
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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