AR087757A1 - Inhibidores selectivos y reversibles de la proteasa especifica de ubiquitina 7, sus composiciones farmaceuticas y sus aplicaciones terapeuticas - Google Patents

Inhibidores selectivos y reversibles de la proteasa especifica de ubiquitina 7, sus composiciones farmaceuticas y sus aplicaciones terapeuticas

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Publication number
AR087757A1
AR087757A1 ARP120103228A ARP120103228A AR087757A1 AR 087757 A1 AR087757 A1 AR 087757A1 AR P120103228 A ARP120103228 A AR P120103228A AR P120103228 A ARP120103228 A AR P120103228A AR 087757 A1 AR087757 A1 AR 087757A1
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nrr
alkylene
branched
linear
alkyl
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Collan Frederic
Gourdel Marie-Edith
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Hybrigenics Sa
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Application filed by Hybrigenics Sa filed Critical Hybrigenics Sa
Publication of AR087757A1 publication Critical patent/AR087757A1/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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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
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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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
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    • A61P31/20Antivirals for DNA viruses
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
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Abstract

Composición farmacéutica y proceso de preparación. Reivindicación 1: Compuesto de la fórmula (1), en el cual R¹, cada cual es idéntico o distinto, se escoge del grupo que consta de halógeno, R, OR, NRR, CN, CF₃, C(O)R, C(O)OR, C(O)NRR, NO₂, alquileno C₁₋₆-OR, alquileno C₁₋₆-NRR, alquileno C₁₋₆-CO₂R, alquileno C₁₋₆-C(O)NRR, -O-alquileno C₁₋₆-CO₂R, -O-alquileno C₁₋₆-C(O)NRR, CO₂-alquileno C₁₋₆-OR, CO₂-alquileno C₁₋₆-NRR, C(O)NH-alquileno C₁₋₆-OR, C(O)NH-alquileno C₁₋₆-NRR, OCF₃, SO₂R, SO₃H, SO₂NRR, NHSO₂R, R¹⁰CºCR¹¹, (R¹⁰)(R¹¹)C=C(R¹¹)₂, alquileno C₁₋₆-C(O)R, NHC(O)R, ó alquilo C₁₋₆, interrumpido por al menos un heteroátomo, escogido de preferencia de entre O, N o S, de preferencia O; L¹ es alquileno C₁₋₆ linear o ramificado sustituido optativamente por uno o más de =O, CN, C(O)R, C(O)OR o C(O)NRR, o bien CH₂-alquileno C₁₋₆ linear o ramificado, en el cual el alquileno C₁₋₆ posterior es sustituido optativamente por uno o más de halógeno, OR, NRR o CF₃; q es 0, 1, 2, 3 ó 4; X es CR⁷; R⁷ es OR, halógeno, alquilo C₁₋₆-OR linear o ramificado, C(O)OR, C(O)NRR, CN, OR⁹, NRR ó SR; n es 0, 1 ó 2; p es 1, 2 ó 3; R³, R⁴, R⁸ y R⁸, cada cual es idéntico o distinto, son escogidos del grupo que consta de H, alquilo C₁₋₆ linear o ramificado, halógeno, OH, -O-alquilo C₁₋₆, NRR, CN, CF₃, OR, C(O)R, C(O)OR o C(O)NRR; A es escogido del grupo que consta de: -C(O)-; -C(O)NH-; -SO₂-; o -SO₂N-; L² es alquileno C₁₋₆-O linear o ramificado o un alquileno C₁₋₆ linear o ramificado, interrumpido optativamente por al menos un heteroátomo escogido de entre O, NR o S y/o sustituido optativamente por: R, OR, NRR, alquilo C₁₋₆-OR alquilo C₁₋₆-NRR, OC(O)R, NHC(O)R, NHC(O)NRR, CN, C(=NH)NHOR; R⁶ es escogido del grupo que consta de arilo, heteroarilo, cicloalquilo, heterociclo, H, en el cual el arilo, heteroarilo, cicloalquilo o heterociclo es mono o policíclico y es sustituido optativamente por uno o más de alquilo C₁₋₆ linear o ramificado, halógeno, NRR, CN, CF₃, OR, =O, C(O)R, C(O)OR, NHC(O)R, OC(O)R, alquenileno C₂₋₆ linear o ramificado o CONRR; cada R y R, ya sea idéntico o distinto, es escogido de manera independiente, de entre H, alquilo C₁₋₆ linear o ramificado, cicloalquilo, arilo, heterociclo aromático o no aromático o -alquilo C₁₋₆-arilo linear o ramificado, o -alquilo C₁₋₆-heterociclo linear o ramificado, en el cual el heterociclo es aromático o no aromático; sustituido optativamente o no por OH, CO₂H, C(O)NH₂, NH₂; R⁹ es escogido del grupo que consta de -C(O)R, -C(O)NHR, -C(O)OR, -C(O)CH₂-NRR, -C(O)-CH₂-CH₂-CO₂R, -C(O)-CH₂-SO₃H, -C(O)-(C₅H₄N), -PO₃H₂, o su forma ionizada; R¹⁰ es escogido de manera independiente de entre un enlace, un alquilo C₁₋₆ linear o ramificado; R¹¹ es escogido de manera independiente de entre un átomo de hidrógeno, un alquilo C₁₋₆ linear o ramificado o un arilo, siendo el alquilo o arilo optativamente sustituido por OH, NH₂, C(O)OH o C(O)NH; o sus sales farmacéuticamente aceptables, o sus isómeros ópticos, racematos, diastereoisómeros, enantiómeros o tautómeros.
ARP120103228A 2011-09-02 2012-08-31 Inhibidores selectivos y reversibles de la proteasa especifica de ubiquitina 7, sus composiciones farmaceuticas y sus aplicaciones terapeuticas AR087757A1 (es)

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Application Number Priority Date Filing Date Title
EP11306096A EP2565186A1 (en) 2011-09-02 2011-09-02 Selective and reversible inhibitors of ubiquitin specific protease 7

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AR087757A1 true AR087757A1 (es) 2014-04-16

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US (1) US9546150B2 (es)
EP (2) EP2565186A1 (es)
JP (1) JP6059228B2 (es)
KR (1) KR20140085430A (es)
CN (1) CN103930415B (es)
AR (1) AR087757A1 (es)
AU (1) AU2012300944B2 (es)
BR (1) BR112014004649A2 (es)
CA (1) CA2847017A1 (es)
CL (1) CL2014000511A1 (es)
DK (1) DK2751092T3 (es)
ES (1) ES2594603T3 (es)
HU (1) HUE029418T2 (es)
IL (1) IL231203A (es)
LT (1) LT2751092T (es)
MA (1) MA35361B1 (es)
MX (1) MX340500B (es)
PL (1) PL2751092T3 (es)
PT (1) PT2751092T (es)
RU (1) RU2622640C2 (es)
SG (1) SG11201400205QA (es)
SI (1) SI2751092T1 (es)
TN (1) TN2014000079A1 (es)
WO (1) WO2013030218A1 (es)

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