AR075597A1 - Derivados de indol como antagonistas de receptores crth2, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del asma y otras enfermedades alergicas . - Google Patents

Derivados de indol como antagonistas de receptores crth2, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del asma y otras enfermedades alergicas .

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Publication number
AR075597A1
AR075597A1 ARP100100535A ARP100100535A AR075597A1 AR 075597 A1 AR075597 A1 AR 075597A1 AR P100100535 A ARP100100535 A AR P100100535A AR P100100535 A ARP100100535 A AR P100100535A AR 075597 A1 AR075597 A1 AR 075597A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
haloalkyl
substituted aryl
aryl
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ARP100100535A
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English (en)
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Merck Frosst Canada Ltd
Merck Sharp & Dohme
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Application filed by Merck Frosst Canada Ltd, Merck Sharp & Dohme filed Critical Merck Frosst Canada Ltd
Publication of AR075597A1 publication Critical patent/AR075597A1/es

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • 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
    • A61K31/435—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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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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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
    • C07D403/08—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 alicyclic rings

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Veterinary Medicine (AREA)
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  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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Abstract

Los compuestos de formula 1 son antagonistas del receptor PGD2, CRTH2, y de este modo son utiles en el tratamiento y/o prevencion de enfermedades mediadas por CRTH2 tales como asma. Reivindicacion 1: Un compuesto de la formula 1 y sales farmacéuticamente aceptables de los mismos, donde: -C---(>X1)(X2C=Ç-NN-Ç=C<; Y1 se selecciona entre arilo opcionalmente sustituido y -C(R2)(R3)(R4); Y2 se selecciona entre H y -alquilo C1-6; Z se selecciona entre H y -alquilo C1-6; R1a y R1b se seleccionan independientemente entre H, halogeno, -Oalquilo C1-6, -O-haloalquilo C1-6, alquilo C1-6, haloalquilo C1-6, arilo opcionalmente sustituido y - (alquileno C1-3)-arilo opcionalmente sustituido; R2 se selecciona entre H, -alquilo C1-6 opcionalmente sustituido por halogeno, -OH o -NHSO2CH3, -OH, Oalquilo C1-6, -S(O)n-alquilo C1-6, -CN, arilo opcionalmente sustituido, -O-arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido, donde n es 0, 1 o 2; R3 se selecciona entre H, -alquilo C1-6, haloalquilo C1-6, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; y R4 se selecciona entre H, -alquilo C1-6, haloalquilo C1-6, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; o R3, R4 y el átomo de carbono al que están unidos forman juntos -cicloalquilo C3-6, fluorenilo o heterociclilo C3-6 que tiene un heteroátomo en el anillo seleccionado entre -N(Ra), -O- y -S-; o R3, R4 juntos representan alquilideno C1-6; Ra es H, alquilo C1-6 o -C(O)-alquilo C1-6; y el sustituyente opcional para arilo y heteroarilo es de 1 a 4 grupos seleccionados independientemente entre halogeno, -alcoxi C1-3, -haloalquilo C1-3, hidroxi-alquilo C1-3, -S(O)n-alquilo C1-3, amino y mono- y di-(alquilo C1-3)amino.
ARP100100535A 2009-02-24 2010-02-24 Derivados de indol como antagonistas de receptores crth2, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del asma y otras enfermedades alergicas . AR075597A1 (es)

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US15496809P 2009-02-24 2009-02-24

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AR075597A1 true AR075597A1 (es) 2011-04-20

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US (2) US8394819B2 (es)
EP (2) EP2401269B1 (es)
JP (1) JP4989786B1 (es)
KR (2) KR101276530B1 (es)
CN (1) CN102333771B (es)
AR (1) AR075597A1 (es)
AU (1) AU2010218209B2 (es)
BR (1) BRPI1008906B1 (es)
CA (1) CA2752981C (es)
CL (1) CL2011002056A1 (es)
CO (1) CO6410295A2 (es)
CR (1) CR20110455A (es)
DK (1) DK2401269T3 (es)
DO (1) DOP2011000271A (es)
EA (1) EA021076B1 (es)
EC (1) ECSP11011288A (es)
ES (2) ES2450594T3 (es)
HK (1) HK1160465A1 (es)
HN (1) HN2011002272A (es)
HR (1) HRP20140384T1 (es)
IL (1) IL214342A0 (es)
MA (1) MA33134B1 (es)
MX (1) MX2011008869A (es)
MY (1) MY152062A (es)
NI (1) NI201100162A (es)
NZ (1) NZ594767A (es)
PE (1) PE20120056A1 (es)
PL (1) PL2401269T3 (es)
PT (1) PT2401269E (es)
RS (1) RS53268B (es)
SG (1) SG173775A1 (es)
SI (1) SI2401269T1 (es)
TN (1) TN2011000382A1 (es)
TW (2) TWI454474B (es)
UA (1) UA105039C2 (es)
WO (1) WO2010099039A1 (es)
ZA (1) ZA201105767B (es)

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