AR084044A1 - Compuestos 2’-espiro-nucleosidos - Google Patents

Compuestos 2’-espiro-nucleosidos

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Publication number
AR084044A1
AR084044A1 ARP110104450A ARP110104450A AR084044A1 AR 084044 A1 AR084044 A1 AR 084044A1 AR P110104450 A ARP110104450 A AR P110104450A AR P110104450 A ARP110104450 A AR P110104450A AR 084044 A1 AR084044 A1 AR 084044A1
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Argentina
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alkyl
iii
hydrogen
acyl
formula
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ARP110104450A
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English (en)
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Jinfa Du
Michael Joseph Sofia
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Pharmasset Inc
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Publication of AR084044A1 publication Critical patent/AR084044A1/es

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    • 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
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C07H19/207—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine adenine dinucleotide or nicotinamide-adenine dinucleotide
    • 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
    • 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
    • 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
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—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 containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
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    • 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
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
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    • 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
    • C07H19/16—Purine radicals
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07H23/00—Compounds containing boron, silicon, or a metal, e.g. chelates, vitamin B12
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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Abstract

Se revelan en la presente 2’-espiro-nucleósidos y sus derivados de utilidad para tratar a un sujeto infectado por el virus de hepatitis C o el virus del dengue. Se revela también un procedimiento para preparar el compuesto.Reivindicación 1: Un compuesto o su estereoisómero o su sal o metabolito o su deuteruro representado por la fórmula (1), en donde: I) R1 está seleccionado de entre a) hidrógeno, b) -P(O)(OH)2, c) -P(O)(O(CH2)1-3OC(O)O(alquilo))2, d) -P(O)(O(CH2)1-3OC(O)(alquilo))2, e) -P(O)(O(CH2)1-3SC(O)(alquilo))2, f) -P(O)(O(CH2)1-3OCH2(arilo))2, g) -P(O)(O(CH2)1-3SCH2(arilo))2, h) -P*(O)(OR1a)(NHCHR1bC(O)OR1c), donde R1a es i) hidrógeno, ii) alquilo, iii) cicloalquilo o iv) arilo, R1b es i) hidrógeno, ii) alquilo C1-6, iii) cicloalquilo, iv) alcarilo o v) alk(heteroarilo) y R1c es i) hidrógeno, ii) alquilo, iii) cicloalquilo o iv) alcarilo, i) -P*(O)(NH(alcaril)(O(CH2)1-3SC(O)(alquilo)), j) un 1,3,2-dioxafosfinan-2-óxido, k) un 4H-benzo[d][1,3,2]dioxafosfinin-2-óxido, l) -P*(O)(OR1c) ~, cuando Y es -O~, donde R1c se define con anterioridad, m) -P(O)(OH)-O-P(O)(OH)2, n) -P(O)(OH)-O-P(O)(OH)-O-P(O)(OH)2, o) un acilo, p) un alquilen C1-6-oxi-acilo, y q) un -C(O)-O-alquilo; II) R2 está seleccionado de entre a) hidrógeno, b) fluoro, c) azido, d) ciano, e) un alquilo C1-6, f) un vinilo y g) un etinilo; III) R3 está seleccionado de entre a) hidrógeno, b) metilo, y c) ciano; IV) Y está seleccionado de entre a) hidrógeno, b) fluoro, c) -OH, d) -O~, cuando R1 es -P(O)(OR1c) ~, donde R1c se define con anterioridad, e) -O(acilo), f) -O(alquilen C1-6-oxi-acilo), g) -O-C(O)-O-alquilo, h) -NH2, i) -NH(acilo), j) -NH-C(O)-O-alquilo, y k) azido; V) X está seleccionado de entre a) -O-, b) -S-, c) -NH-, d) -CH2-, e) >C=CH2, y f) -NH-C(O)-O-alquilo; VI) el anillo Z es un anillo de cuatro o cinco miembros seleccionado de entre radicales representado por las estructuras de fórmulas (a) - (o), donde * representa el punto de unión con el carbono 2’ y donde a) A está seleccionado de entre i) -O-, ii) -S-, iii) -S(O)-, iv) -S(O)2-, y v) -NH-, b) D está seleccionado de entre i) -O-, ii) -S- excepto por los anillos de fórmula (i) y (j), iii) -S(O)- excepto por los anillos de fórmula (i) y (j), iv) -S(O)2- excepto por los anillos de fórmula (i) y (j), y v) -NH- excepto por los anillos de fórmula (i) y (j), vi) -N-, vii) un metileno excepto por los anillos de fórmula (i) y (j), viii) un metino, y ix) un vinilideno excepto por los anillos de fórmula (i) y (j), c) R4, R4’, R5, R5’, R6, R7, R8, R8’, R9 y R9’ están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) alquilo C1-6, iv) hidroxi, v) alcoxi, vi) cicloalcoxi, vii) -O(acilo), viii) -O(alquilen C1-6-oxiacilo), ix) -O-C(O)-O-alquilo, x) alquilen C1-6-oxi(alquilo), xi) alquenilo, xii) etinilo, xiii) -NH2, xiv) -NH(alquilo), xv) -NH(cicloalquilo), xvi) heterociclilo, xvii) arilo, y xviii) heteroarilo; y VII) B está seleccionado de entre las estructuras de fórmula (B1), (B2) y (B3), donde para la estructura de fórmula (B1), n es 0 ó 1, a) cuando n es 0, - - - - - es un enlace doble y R10 está seleccionado de entre i) -NH2, ii) -NH(alquilo), iii) -NH(acilo), iv) -NH-C(O)-O-alquilo, v) -cicloheteroalquilo, vi) -heteroarilo, vii) -O(alquilo), viii) -O(acilo), ix) -O(alquilen C1-6-oxiacilo) y x) -O-C(O)-O-alquilo, o b) cuando n es 1, - - - - - es un enlace simple y R10 está seleccionado de entre i) =O, ii) =NH, y iii) =N(alquilo), y c) independientemente del valor de n, R11 y R12 están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) ciano, iv) alquilo C1-6, v) alquenilo C2-5 y vi) alquinilo C2-5; donde para la estructura de fórmula (B2), a) R13 está seleccionado de entre i) hidrógeno, ii) halo, iii) ciano, iv) -C(O)NH2, v) alquilo C1-6, vi) vinilo, y vii) etinilo; donde para la estructura de fórmula (B3), m es 0 ó 1 y - - - - - es un enlace simple o doble a) cuando m es 0, - - - - - es un enlace doble y R16 y R17 están seleccionados, de modo independiente, de entre i) hidrógeno, ii) -NH2, iii) -NH(alquilo), iv) -NH(acilo), iv) -NH-C(O)-O-alquilo, v) -cicloheteroalquilo, vi) -O(alquilo), vii) -O(acilo), viii) -O(alquilen C1-6-oxiacilo), ix) -O-C(O)-O-alquilo, y x) -S(alquilo), o b) cuando m es 1, - - - - - es un enlace simple, b1) R16 está seleccionado de entre i) =O, ii) =NH y iii) =N(alquilo) y b2) R17 está seleccionado de entre i) -NH2, ii) -NH(alquilo), iii) -NH(acilo), iv) -NH-C(O)-O-alquilo, y v) -cicloheteroalquilo, c) independientemente del valor de m, cada par de enlace, W1- - - - -W2, W2- - - - -C, C- - - - -W4, W4- - - - -W3 y W3- - - - -W1, contenido en el anillo de cinco miembros comprende un enlace simple o doble y i) W1 es O, S, N o CR14, ii) W2 es N o CR15, iii) W3 es C o N, y iv) W4 es C o N y donde R14 y R15, de estar presentes, están seleccionados, de modo independiente, de entre i) hidrógeno, ii) halo, iii) ciano, iv) -C(O)NH2, iv) alquilo C1-6, vii) vinilo, y viii) etinilo.
ARP110104450A 2010-11-30 2011-11-30 Compuestos 2’-espiro-nucleosidos AR084044A1 (es)

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EP (2) EP2646453A1 (es)
JP (2) JP6069215B2 (es)
AR (1) AR084044A1 (es)
AU (1) AU2011336632B2 (es)
CA (1) CA2818853A1 (es)
ES (1) ES2716158T3 (es)
PT (1) PT3042910T (es)
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WO (1) WO2012075140A1 (es)

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