AR105122A1 - INHIBIDORES DE METALO-b-LACTAMASA - Google Patents

INHIBIDORES DE METALO-b-LACTAMASA

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Publication number
AR105122A1
AR105122A1 ARP160101905A ARP160101905A AR105122A1 AR 105122 A1 AR105122 A1 AR 105122A1 AR P160101905 A ARP160101905 A AR P160101905A AR P160101905 A ARP160101905 A AR P160101905A AR 105122 A1 AR105122 A1 AR 105122A1
Authority
AR
Argentina
Prior art keywords
ring
optionally substituted
alkyl
independently selected
ora
Prior art date
Application number
ARP160101905A
Other languages
English (en)
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of AR105122A1 publication Critical patent/AR105122A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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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    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

La presente se refiere a compuestos inhibidores de metalo-b-lactamasa. La presente también se refiere a composiciones que comprenden un compuesto inhibidor de metalo-b-lactamasa de la presente o una sal farmacéuticamente aceptable del mismo, y un vehículo farmacéuticamente aceptable, opcionalmente junto con un antibiótico betalactámico y/o un inhibidor de b-lactamasa. También se refiere a métodos para el tratamiento de una infección bacteriana que comprende administrar a un paciente una cantidad terapéuticamente eficaz de un compuesto de la presente, junto con una cantidad terapéuticamente eficaz de uno o más antibióticos betalactámicos y opcionalmente junto con uno o más compuestos inhibidores de b-lactamasa. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: X¹ es N o CH; X² es N o CH; Z es tetrazolilo, en la que Z está unido a través de un enlace carbono a carbono al anillo núcleo de seis miembros que tiene X¹ y X²; RA es -(CH₂)ₙ-AryA¹, -(CH₂)ₙ-HetA¹, -(CH₂)ₙ-cicloalquilo C₄₋₆ o (CH₂)ₙ-cicloalquenilo C₄₋₆, donde dicho -(CH₂)ₙ-cicloalquilo C₄₋₆ y -(CH₂)ₙ-cicloalquenilo C₄₋₆ están opcionalmente sustituidos con 1, 2 ó 3 sustituyentes seleccionados independientemente entre -NH₂, -OH, -F y -NRᵃC(O)alquilo C₁₋₆ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre -F, -CF₃, -NRᵃRᵇ y -ORᵃ; R¹ es 1) -NH₂; 2) -NRᵃ-alquilo C₁₋₆ opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes seleccionados independientemente entre: -F, -CF₃, alquilo C₁₋₆, -CH(NH₂)C(O)NH₂, -C(O)NRᵃRᵇ, -C(O)OH, -(CH₂)₁₋₂NH₂, -NRᵃ(CH₂)₂₋₃NH₂, -NRᵃRᵇ, -N⁺RᵃRᵇCH₃, -NHCH₂CH₂OCH₃, -ORᵃ y -O(CH₂)₂₋₃NH₂; 3) -NRᵃC(O)alquilo C₁₋₆ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre: -F, -CF₃, -C(O)NRᵃRᵇ, -C(O)OH, -NRᵃRᵇ, -N⁺RᵃRᵇCH₃, -NHCH₂CH₂OCH₃, -ORᵃ y -O(CH₂)₂₋₃NH₂; 4) -NRᵃ(CH₂)ₙ-cicloalquilo C₃₋₆, donde el cicloalquilo C₃₋₆ está opcionalmente sustituido con -CH₂OH o -NH₂; 5) un heterocicloalquilo monocíclico de 4 a 6 miembros unido a nitrógeno con 0, 1 ó 2 heteroátomos adicionales en el anillo seleccionados independientemente entre N, O y S, o un heterocicloalquilo bicíclico de 6 a 10 miembros unido a nitrógeno con 0, 1, 2 ó 3 heteroátomos adicionales en el anillo seleccionados entre N, O y S donde el anillo bicíclico puede estar puenteado, fusionado o ser espirocíclico, donde el heterocicloalquilo monocíclico de 4 a 6 miembros y el heterocicloalquilo bicíclico de 6 a 10 miembros están opcionalmente sustituidos con uno a tres sustituyentes, seleccionados independientemente entre: -F, -NRᵃRᵇ, oxo, -(CH₂)₁₋₂OH, -CH₂NH₂, -SO₂CH₃ y alquilo C₁₋₆ y donde un átomo de azufre del anillo está opcionalmente sustituido con uno o dos oxo; 6) -NRᵃ-(alquil C₁₋₃)ₙ-AryB¹, donde el alquilo C₁₋₃ está opcionalmente sustituido con -NH₂; y 7) -NRᵃ-(alquil C₁₋₃)ₙ-HetB¹; AryA¹ es un sistema de anillo aromático seleccionado entre: 3) un anillo monocíclico de 5 a 6 miembros con 0, 1, 2 ó 3 heteroátomos del anillo seleccionados independientemente entre N, O y S, opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados independientemente entre: a) halógeno, b) -alquilo C₁₋₆, c) -CN, d) -CH₂OH, e) -C(O)NRᵃRᵇ, f) -C(O)NH(CH₂)₂₋₄NH₂ opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre -NRᵃRᵇ y -(CH₂)ₙORᵃ, g) -C(O)ORᵃ, h) -(CH₂)ₚNHRᵃ opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre -NRᵃRᵇ o -ORᵃ, i) -(CH₂)ₚNRᵃC(=NH)NH₂, j) -NRᵃC(O)alquilo C₁₋₆ opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre -NRᵃRᵇ o -ORᵃ, k) -NRᵃSO₂-alquilo C₁₋₆, ₗ₎ ₋NRᵃSO₂-ciclopropilo, m) -ORᵃ, n) oxo, o) -S-alquilo C₁₋₆ opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre -NRᵃRᵇ o -ORᵃ; p) -SO₂Rᵃ, q) -SO₂NRᵃRᵇ, r) -SO₂NH-ciclopropilo, s) -AryA², t) -(CH₂)ₙNRᵃAryA², u) -C(O)NRᵃHetA² y v) -HetA², y 4) un anillo bicíclico de 8 a 10 miembros con 1, 2, 3 ó 4 heteroátomos del anillo seleccionados entre N, O y S, donde un átomo de S tiene opcionalmente uno o dos sustituyentes oxo y un átomo de N está opcionalmente en forma de un N-óxido, y donde el anillo está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre a) halógeno; b) alquilo C₁₋₆ opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre -NRᵃRᵇ, -F y -ORᵃ; c) -(CH₂)ₙCF₃; d) -C(=NH)NH₂; e) -CN; f) -C(O)CF₃; g) -C(O)NRᵃRᵇ; h) -C(O)NHCH₂C(O)ORᵃ; i) -C(O)NH-alquilo C₂₋₄-NH₂; j) -C(O)ORᵃ; k) -NRᵃRᵇ; l) -NHCH₂SO₃H; m) -(CH₂)ₙNHC(=NH)NH₂; n) -NHC(O)alquilo C₁₋₆; o) -NHC(O)NH₂; p) -NHC(O)ORᵃ; q) -NHSO₂CH₃; r) -ORᵃ; s) oxo; t) -SO₂Rᵃ, u) -CH₂-fenil-OCH₃; y v) -HetA²; HetA¹ es dihidrotiopiranilo o tetrahidropiranilo; AryA² es un anillo monocíclico, aromático, de 5 a 6 miembros, con 1, 2 ó 3 heteroátomos del anillo seleccionados independientemente entre N, N en forma de una sal cuaternaria, y S, o 4 átomos de N del anillo, opcionalmente sustituido con -CH₂OH, -COOH,-CONH₂, -C(O)O-alquilo C₁₋₆ y -(CH₂)ₚNHRᵃ opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre -NRᵃRᵇ y -ORᵃ; -HetA² es un anillo monocíclico, saturado, de 4 a 6 miembros, con 1 ó 2 heteroátomos del anillo seleccionados independientemente entre N, O y S, donde el S está opcionalmente sustituido con dos grupos oxo, y donde el anillo está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre alquilo C₁₋₆, -CN, -OH y oxo; AryB¹ es un anillo aromático seleccionado entre: 1) un anillo aromático, monocíclico, de 5 a 6 miembros, con 0, 1, 2 ó 3 átomos de N en el anillo, opcionalmente sustituido con 1 sustituyente seleccionado entre -CF₃, alquilo C₁₋₆, -(CH₂)ₙNH₂ y -OCH₃; o 2) un anillo bicíclico de 9 miembros con 2 átomos de N en el anillo; HetB¹ es un anillo saturado seleccionado entre: 1) un anillo monocíclico, saturado, de 4 a 6 miembros, con 1 ó 2 heteroátomos del anillo seleccionados independientemente entre N, O y S, donde un átomo de N en el anillo está opcionalmente en forma de una amina cuaternaria, donde el S está sustituido con dos grupos oxo, y donde el anillo está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados independientemente entre -F, alquilo C₁₋₆, hidroxialquilo C₁₋₆, -C(O)ORᵃ,-(CH₂)ₖNRᵃRᵇ, -ORᵃ y oxo, o 2) un anillo bicíclico, de 6 a 10 miembros, con 1 ó 2 heteroátomos del anillo seleccionados independientemente entre N y O, opcionalmente sustituido con -OH o -NH₂, donde el anillo bicíclico está enlazado o fusionado; Rᵃ y Rᵇ son independientemente H o alquilo C₁₋₆; k es 0, 1, 2, 3 ó 4; cada n es independientemente 0 ó 1; y cada p es independientemente 0, 1, 2 ó 3.
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