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AR090044A1 - Agentes antivirales para la hepatitis b - Google Patents

Agentes antivirales para la hepatitis b

Info

Publication number
AR090044A1
AR090044A1 ARP120104951A ARP120104951A AR090044A1 AR 090044 A1 AR090044 A1 AR 090044A1 AR P120104951 A ARP120104951 A AR P120104951A AR P120104951 A ARP120104951 A AR P120104951A AR 090044 A1 AR090044 A1 AR 090044A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocycloalkyl
aryl
cycloalkyl
heteroaryl
Prior art date
Application number
ARP120104951A
Other languages
English (en)
Inventor
D Hartman George
A Flores Osvaldo
Original Assignee
Novira Therapeutics Inc
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 Novira Therapeutics Inc filed Critical Novira Therapeutics Inc
Publication of AR090044A1 publication Critical patent/AR090044A1/es

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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48Sulfur atoms
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/54Sulfur atoms
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    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/451Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o sales farmacéuticamente aceptables del mismo; donde R⁴ es H o alquilo C₁₋₆; donde cada R⁵ se selecciona en forma independiente en cada caso entre el grupo que consiste en CH₃, alcoxi C₁₋₆, halo, -CN, -NO₂, -(L)ₘ-SR⁹, -(L)ₘ-S(=O)R⁹, -(L)ₘ-S(=O)₂R⁹, -(L)ₘ-NHS(=O)₂R⁹, -(L)ₘ-C(=O)R⁹, -(L)ₘ-OC(=O)R⁹, -(L)ₘ-CO₂R⁸, -(L)ₘ-OCO₂R⁸, -(L)ₘ-N(R⁸)₂, -(L)ₘ-C(=O)N(R⁸)₂, -(L)ₘ-OC(=O)N(R⁸)₂, -(L)ₘ-NHC(=O)NH(R⁸), -(L)ₘ-NHC(=O)R⁹, -(L)ₘ-NHC(=O)OR⁹, -(L)ₘ-C(OH)(R⁸)₂, -(L)ₘ-C(NH₂)(R⁸)₂, -haloalquilo C₁₋₆, -dihaloalquilo C₁₋₆ y -trihaloalquilo C₁₋₆; L es en forma independiente, en cada caso, un radical bivalente seleccionado entre -(alquilen C₁₋₃)-, -(cicloalquilen C₃₋₇)-, -(alquilen C₁₋₃)ₘ-O-(alquilen C₁₋₃)ₘ-, o -(alquilen C₁₋₃)ₘ-NH-(alquilen C₁₋₃)ₘ-; cada R⁸ es en forma independiente, en cada caso, H, alquilo C₁₋₆, -haloalquilo C₁₋₆, -dihaloalquilo C₁₋₆, -trihaloalquilo C₁₋₆, heteroalquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo C₃₋₁₀, arilo, heteroarilo, -alquil C₁₋₄-(cicloalquilo C₃₋₁₀), -alquil C₁₋₄-(heterocicloalquilo C₃₋₁₀), -alquil C₁₋₄-(arilo), o -alquil C₁₋₄-(heteroarilo), y donde el alquilo, heteroalquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo está opcionalmente sustituido con 1 - 5 sustituyentes seleccionados entre R²; R⁹ es alquilo C₁₋₆, -haloalquilo C₁₋₆, -dihaloalquilo C₁₋₆, -trihaloalquilo C₁₋₆, heteroalquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo C₃₋₁₀, arilo, heteroarilo, -alquil C₁₋₄-(cicloalquilo C₃₋₁₀), -alquil C₁₋₄-(heterocicloalquilo C₃₋₁₀), -alquil C₁₋₄-(arilo), o -alquil C₁₋₄-(heteroarilo), y donde el anillo alquilo, heteroalquilo, cicloalquilo, heterocicloalquilo, arilo o heteroarilo está opcionalmente sustituido con 0 - 5 sustituyentes seleccionados entre R²; R¹⁰ es OH, alquilo C₁₋₆, alquil C₁₋₆-OH, -haloalquilo C₁₋₆, -dihaloalquilo C₁₋₆, -trihaloalquilo C₁₋₆, heteroalquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo C₃₋₁₀, arilo, heteroarilo, -alquil C₁₋₄-(cicloalquilo C₃₋₁₀), -alquil C₁₋₄-(heterocicloalquilo C₃₋₁₀), -alquil C₁₋₄-(arilo), o -alquil C₁₋₄-(heteroarilo), y donde el anillo alquilo, heteroalquilo, cicloalquilo, heterocicloalquilo, arilo o heteroarilo está opcionalmente sustituido con 1 - 5 sustituyentes seleccionados entre R²; R¹¹ es una unión o alquileno C₁₋₃, donde el alquileno C₁₋₃ está opcionalmente sustituido con 1 - 3 sustituyentes seleccionados entre R²; R² se selecciona en forma independiente en cada caso entre el grupo que consiste en halo, -CN, -NO₂, -alquilo C₁₋₆, -alcoxi C₁₋₆, -haloalquilo C₁₋₆, -dihaloalquilo C₁₋₆, -trihaloalquilo C₁₋₆, -heteroalquilo C₁₋₆, y C(O)-alquilo C₁₋₆; w es 0, 1 ó 2; cada instancia de x se selecciona en forma independiente entre el grupo que consiste en 0, 1, 2, 3 y 4; cada instancia de y se selecciona en forma independiente entre el grupo que consiste en 1, 2, y 3; cada instancia de z se selecciona en forma independiente entre el grupo que consiste en 0, 1, 2, y 3; cada instancia de m es en forma independiente 0, 1 ó 2.
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