AR050557A1 - Compuestos heterociclicos sustituidos y sus usos - Google Patents

Compuestos heterociclicos sustituidos y sus usos

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Publication number
AR050557A1
AR050557A1 ARP050103694A ARP050103694A AR050557A1 AR 050557 A1 AR050557 A1 AR 050557A1 AR P050103694 A ARP050103694 A AR P050103694A AR P050103694 A ARP050103694 A AR P050103694A AR 050557 A1 AR050557 A1 AR 050557A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
nhc
alkyl
halogen
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ARP050103694A
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English (en)
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Celgene Corp
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Publication of AR050557A1 publication Critical patent/AR050557A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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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
    • A61K31/40—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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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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    • C07—ORGANIC CHEMISTRY
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    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
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    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring

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  • Life Sciences & Earth Sciences (AREA)
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Abstract

Métodos para prevenir o tratar cáncer o un trastorno inflamatorio al administrar a un sujeto que lo necesite uno o más compuestos heterocíclicos sustituidos. Reivindicacion 1: Un compuesto que tiene la formula (1) o una sal, solvato o hidrato farmacéuticamente aceptable del mismo, en donde: X es imidazol sustituido o insustituido, piridina sustituida o insustituida, pirrolidina sustituida o insustituida, tiofeno sustituido o insustituido, indol sustituido o insustituido, 2,3- dihidrobenzofurano sustituido o insustituido, 3,4-dihidro-2H-benzo(b)(1,4)oxazina sustituido o insustituido, 1H-benzo(d)(1,2,3)triazol sustituido o insustituido, quinolina sustituida o insustituida, benzofurano sustituido o insustituido, benzo(d)oxazol-2(3H)ona sustituida o insustituida, o pirimidina sustituida o insustituida; cada caso de R1 y R2 es independientemente -H, -CN, halogeno, alquilo inferior sustituido o insustituido, alquenilo sustituido o insustituido, alquinilo sustituido o insustituido, -NHC(O)R9, -NHC(O)OR9, COOH, -C(O)-alquilo inferior, -C(O)O-alquilo inferior, -C(O)N(R9)2, arilo sustituido o insustituido, heterociclo sustituido o insustituido; cada caso de Ra y Rb es independientemente -H, alquilo inferior sustituido o insustituido, arilo sustituido o insustituido, heterociclo sustituido o insustituido, cicloalquilo sustituido o insustituido, alcoxi sustituido o insustituido, halogeno, ciano, -NO2, -OH, OPO(OH)2, -N(R9)2, -OC(O)-R10, -OC(O)- R10-N(R10)2, -C(O)N(R10)2, -NHC(O)-R10, NHS(O)2-R10, -S(O)2-R10, -S(O)-NH2, -S(O)2-N(R10)2, -NHC(O)NH-R10, -NHC(O)N(R10)2, -NHC(O)NHSO2-R10, -NHC(O)-R10-N(R10)2, -NHC(O)CH(R10)(N(R9)2) o -NHC(O)-R10-NH2; R3 es -H, alquilo sustituido o insustituido, arilo sustituido o insustituido, heterociclo sustituido o insustituido, cicloalquilo sustituido o insustituido, alcoxi sustituido o insustituido, halogeno, ciano, -NO2, -OH, OPO(OH)2, -N(R9)2, -OC(O)-R10, -OC(O)-R10-N(R10)2, -OC(O)-R10-NH2, - C(O)N(R10)2, -NHC(O)-R10, NHS(O)2-R10, -S(O)2-R10, -S(O)-NH2, -S(O)2-N(R10)2, -S(O)2-NH2, -S(O)2-N(R10)2, -OS(O)2-NH2, -OS(O)2-N(R10)2, -NHC(O)O-R10, -NHC(O)NH-R10, -NHC(O)N(R10)2, -NHC(O)NHSO2-R10, -NHC(O)-R10-N(R10)2, -NHC(O)CH(R10)(N(R9)2) o - NHC(O)-R10-NH2, o R3 con ya sea Ra o con R4, juntos forman -O-(C(R16R17))-O-, -O-(C(R16R17))2-O-, o -O-(C(R16R17))3-O-; R4 es -H, alquilo sustituido o insustituido, arilo sustituido o insustituido, heterociclo sustituido o insustituido, cicloalquilo sustituido o insustituido, alcoxi sustituido o insustituido, halogeno, ciano, -NO2, -OH, OPO(OH)2, -N(R9)2, -OC(O)-R10, -OC(O)-R10-N(R10)2, -OC(O)-R10-NH2, -C(O)N(R10)2, -NHC(O)-R10, NHS(O)2-R10, -S(O)2-R10, -S(O)-NH2, -OS(O)2-R10, -S(O)2-NH2, - S(O)2-N(R10)2, -OS(O)2-NH2, -OS(O)2-N(R10)2, -NHC(O)O-R10, -NHC(O)NH-R10, -NHC(O)N(R10)2, -NHC(O)NHSO2-R10, -NHC(O)-R10-N(R10)2, -NHC(O)CH(R10)(N(R9)2) o -NHC(O)-R10-NH2; R5 es -H, alquilo sustituido o insustituido, arilo sustituido o insustituido, heterociclo sustituido o insustituido, cicloalquilo sustituido o insustituido, alcoxi sustituido o insustituido, halogeno, ciano, -NO2, -OH, OPO(OH)2, -N(R9)2, -OC(O)-R10, -OC(O)-R10-N(R10)2, -OC(O)-R10-NH2, -C(O)N(R10)2, -NHC(O)-R10, NHS(O)2-R10, - S(O)2-R10, -OS(O)2-R10, -S(O)-NH2, -S(O)2-N(R10)2, -OS(O)2-NH2, -OS(O)2-N(R10)2, NHC(O)O-R10, -NHC(O)NH-(R10), -NHC(O)N(R10)2, -NHC(O)NHSO2-R10, -NHC(O)-R10-N(R10)2, -NHC(O)CH(R10)(N(R9)2) o -NHC(O)-R10-NH2; cada caso de Rg es independientemente -H, alquilo inferior sustituido o insustituido, o cicloalquilo sustituido o insustituido; cada caso de R10 es independientemente alquilo inferior sustituido o insustituido, cicloalquilo sustituido o insustituido, arilo sustituido o insustituido, hidroxialquilo inferior sustituido o insustituido, o R10 y un N al cual está unido forman un heterociclo sustituido o insustituido, o R10 es -H donde correspondiere; cada caso de R16 y R17 es independientemente -H o halogeno; y en donde cuando: (1) X es piridina, piridina sustituida, pirrolidina, imidazol, naftaleno o tiofeno; (2) Ra y Rb son H; y (3) R4 es H, nitro, ciano, trifluorometilo, carboetoxi, carbometoxi, carbopropoxi, acetilo, carbamoílo, acetoxi, carboxi, hidroxi, amino, alquilo inferior, alquilidenmetilo inferior, alcoxi inferior o halo; si uno de R3 o R5 es H, entonces el otro no es -O-alquilo C1-10, -O-monocicloalquilo C1-10, -O-policicloalquilo C1-10, -O-benzocicloalquilo C1-10, -O-alquilo C0-3-C1-10, -O- monocicloalquilo C0-3-C1-10, -O-policicloalquilo C0-3-C1-10, -O-benzocicloalquilo C0-3-C1-10, -CH=alquilo C1-10, -CH=monocicloalquilo C1-10 o-CH=bicicloalquilo C1-10.
ARP050103694A 2004-09-03 2005-09-02 Compuestos heterociclicos sustituidos y sus usos AR050557A1 (es)

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US (2) US7468446B2 (es)
EP (1) EP1794139A2 (es)
JP (1) JP2008512378A (es)
KR (1) KR20070050987A (es)
CN (1) CN101052630A (es)
AR (1) AR050557A1 (es)
AU (1) AU2005282727A1 (es)
BR (1) BRPI0514857A (es)
CA (1) CA2578789A1 (es)
IL (1) IL181677A0 (es)
WO (1) WO2006028963A2 (es)
ZA (1) ZA200702380B (es)

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