AR084857A1 - Derivados de azetidina utiles para el tratamiento de enfermedades metabolicas e inflamatorias - Google Patents

Derivados de azetidina utiles para el tratamiento de enfermedades metabolicas e inflamatorias

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Publication number
AR084857A1
AR084857A1 ARP120100129A ARP120100129A AR084857A1 AR 084857 A1 AR084857 A1 AR 084857A1 AR P120100129 A ARP120100129 A AR P120100129A AR P120100129 A ARP120100129 A AR P120100129A AR 084857 A1 AR084857 A1 AR 084857A1
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AR
Argentina
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optionally substituted
alkyl
halo
independently selected
alkoxy
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ARP120100129A
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Galapagos Nv
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Publication of AR084857A1 publication Critical patent/AR084857A1/es

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    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • 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
    • A61K31/403—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 carbocyclic rings, e.g. carbazole
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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
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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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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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
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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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
    • A61K31/4245—Oxadiazoles
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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
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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
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    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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    • 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
    • C07D403/06—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 only aliphatic carbon atoms
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    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
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    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos pueden ser preparados como una composición farmacéutica, y pueden ser empleados para la prevención y tratamiento de una variedad de afecciones en mamíferos incluyendo seres humanos, incluyendo a modo de ejemplo no limitativo afecciones inflamatorias, enfermedades infecciosas, enfermedades autoinmunes, enfermedades que involucran el deterioro de funciones de células inmunes, enfermedades cardiometabólicas, y/o enfermedades proliferativas.Reivindicación 1: Un compuesto de acuerdo con la fórmula (1) donde L1 es un enlace simple, o CRaRb; L2 es un enlace simple, O, NRe o CRcRd; cada uno de Ra, Rb, Rc, y Rd es independientemente seleccionado entre H, y alquilo C1-4; o Ra y Rb en conjunto con el carbono al cual están unidos pueden formar un cicloalquilo C3-7; o Rc y Rd en conjunto con el carbono al cual están unidos pueden formar un cicloalquilo C3-7; Re es alquilo C1-4; Y es alquilo C1-4 opcionalmente sustituido con uno o más grupos seleccionados independientemente entre flúor, OH, y fenilo (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre alquilo C1-4 (opcionalmente sustituido con uno o más halo), alcoxi C1-4, halo y ciano), o alquenilo C1-4 que comprende 1 doble enlace; cada uno de Cy1 y Cy2 es independientemente arilo C6-10, o heteroarilo de 5 - 10 miembros; cada R1 es independientemente seleccionado entre halo, alquilo C1-4 (opcionalmente sustituido con uno o más halo), y alcoxi C1-4 (opcionalmente sustituido con uno o más halo); R2 es: H; alquilo C1-4 opcionalmente sustituido con uno o más grupos R2a independientemente seleccionados; cicloalquilo C3-7 opcionalmente sustituido con uno o más grupos R2a independientemente seleccionados; R2a es halo, alcoxi C1-6, OH, C(=O)R4, S(O)2R4, CN, NHC(=O)R5, NHSO2R5, heterocicloalquilo de 5 - 7 miembros (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre alquilo C1-4, y oxo), o heteroarilo de 5 - 6 miembros (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre halo, OH, alcoxi C1-4 y alquilo C1-4); R3 se selecciona entre halo, alquilo C1-6 (opcionalmente sustituido con uno o más halo), alcoxi C1-6 (opcionalmente sustituido con uno o más halo, o fenilo), tioalcoxi C1-6, fenilo (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre halo, alquilo C1-4 (opcionalmente sustituido con uno o más halo), alcoxi C1-4, C(=O)-alcoxi C1-4 y CN); R4 es OH, alcoxi C1-6, heterocicloalquilo de 5 - 7 miembros N-ligado (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre alquilo C1-6, y oxo), NR4aR4b, o NHSO2R4c; cada uno de R4a y R4b es independientemente H, alquilo C1-4 (opcionalmente sustituido con fenilo (opcionalmente sustituido con uno o más grupos seleccionados independientemente entre halo, CN, alquilo C1-6, y alcoxi C1-6)), o cicloalquilo C3-7; R4c es fenilo, heteroarilo de 5 - 6 miembros, heterocicloalquilo de 5 - 6 miembros (opcionalmente sustituido con uno o más alquilo C1-4) o alquilo C1-4 (opcionalmente sustituido con uno o más halo); R5 es alquilo C1-4 (opcionalmente sustituido con uno o más halo) o fenilo; y los subíndices n y m se seleccionan independientemente entre 0, 1, y 2; o una sal farmacéuticamente aceptable, o un solvato, o un solvato de las sales farmacéuticamente aceptables.
ARP120100129A 2011-01-19 2012-01-13 Derivados de azetidina utiles para el tratamiento de enfermedades metabolicas e inflamatorias AR084857A1 (es)

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ZA201304822B (en) 2014-03-26
WO2012098033A1 (en) 2012-07-26
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CO6741223A2 (es) 2013-08-30
US20140371198A1 (en) 2014-12-18
EP2665704A1 (en) 2013-11-27
AU2012208693A1 (en) 2013-03-21
AU2012208693B2 (en) 2015-02-26
CN103328442A (zh) 2013-09-25
US8759334B2 (en) 2014-06-24
BR112013018286A2 (pt) 2016-11-16
KR20140040104A (ko) 2014-04-02
GB201213267D0 (en) 2012-09-05
CA2824460A1 (en) 2012-07-26
GB2489382A (en) 2012-09-26
MX2013008257A (es) 2013-08-12
RU2013138372A (ru) 2015-02-27
TW201245144A (en) 2012-11-16
SG191291A1 (en) 2013-07-31

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