AR076183A1 - Derivados heterociclicos inhibidores de dihidroorotato deshidrogenasa, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento del cancer y otros trastornos autoinmunes. - Google Patents

Derivados heterociclicos inhibidores de dihidroorotato deshidrogenasa, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento del cancer y otros trastornos autoinmunes.

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AR076183A1
AR076183A1 ARP100101112A ARP100101112A AR076183A1 AR 076183 A1 AR076183 A1 AR 076183A1 AR P100101112 A ARP100101112 A AR P100101112A AR P100101112 A ARP100101112 A AR P100101112A AR 076183 A1 AR076183 A1 AR 076183A1
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substituted
het
alkyl
atoms
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ARP100101112A
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Merck Serono Sa
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D403/04—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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    • C07D403/00—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
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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
    • C07D403/12—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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • 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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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos son utiles, por ejemplo, en el tratamiento de trastornos autoinmunes, como, por ejemplo, la esclerosis multiple y, también, en el tratamiento de trastornos de cáncer. Reivindicacion 1: Un compuesto de acuerdo con la formula 1 donde R1 denota COOH, COOA, COA, CF3, acilo, ciano, Het, tetrazoílo, sulfonilo, o si Q es -C=C- o hetarileno, o si Q es un arileno tetrasustituido, R1 también denota CON(R3)2 o CONHA; R2 denota H, Hal, A, O-A, Ar; Ra denota Ar, Het, O-Het, NH-Het, O-Ar, -O-(CH2)m-Het, -NH-(CH2)mHet, NH-Ar, S(O)2Ar, S(O)Ar, -S-Ar, OCF3, Y denota CRf o N, X1, X2 denotan cada uno de manera independiente uno del otro CRcRd, NRc, NRd, y cuando Y denota CRf, también O o S, con la condicion que uno de X1 y X2 sea CRcRd o NRc; Rb y Rc representan juntos un enlace químico; Rf y Re representan juntos un enlace químico, cuando Y es CRf; Re y Rc, en la definicion de X1, representan juntos un enlace químico cuando Y es N, y Rb y Rc, en la definicion de x2, representan juntos un enlace químico; Rd denota H, A, -(CH2)m-COOH; Q denota un grupo -C=C-, arileno, hetarileno, o el grupo de formula (2); Hal denota F, Cl, Br o I; A es un alquilo ramificado o lineal que posee 1 a 12 átomos de C, donde uno o más, con preferencia 1 a 7 átomos de H pueden estar reemplazados por Hal, OR3, CN o N(R3)2 y donde uno o más, con preferencia 1 a 7 grupos CH2 no adyacentes pueden estar reemplazados por O, o S y/o por grupos -CH=CH- o -C=O-, o denota cicloalquilo o cicloalquilalquileno que posee 3-7 átomos de C de anillo; Ar denota un anillo carbocíclico monocíclico o bicíclico, saturado, insaturado o aromático que posee 6 a 14 átomos de carbono que pueden no estar sustituidos o pueden estar sustituidos por un grupo seleccionado de (R4)n y/o (R5)n; Het denota un anillo heterocíclico monocíclico o bicíclico, saturado, insaturado o aromático que posee 1 a 4 átomos de N, O y/o S que pueden no estar sustituidos o estar sustituidos por un grupo seleccionado de (R4)n y/o (R5)n, arileno denota un anillo carbocíclico divalente, monocíclico o bicíclico, saturado, insaturado o aromático que posee 6 a 14 átomos de carbono que pueden no estar sustituidos o estar sustituidos por un grupo seleccionado de (R4)n y/o (R5)n; Hetarileno denota un anillo heterocíclico divalente, monocíclico o bicíclico, saturado, insaturado o aromático que posee 1 a 4 átomos de N, O y/o S que pueden no estar sustituidos o estar sustituidos por un grupo seleccionado de (R4)n y/o (R5)n; R3 es H o alquilo; R4 y R5 se seleccionan cada uno de manera independiente de Hal, hidroxi, alcoxi, carboxi, carboxi-alquilo, perfluor-alquilo, perfluor-alquiloxi, acilo, alquilsulfonilo, sulfonilo, ciano, nitro, amino, amido, alquilo opcionalmente sustituido por un carboxi, o Het-alquilo opcionalmente sustituido por un acilo, alquilsulfonilo, -O(CH2)nAr, -O(CH2)nHet, -(CH2)mHet, OA, -NHCO(CH2)mAr, NHCO(CH2)mHet , CONHA, o alquilo; n denota 0, 1, 2, 3, 4, 5; m denota 0, 1, 2, 3, 4, 5, 6; y sus derivados, solvatos, tautomeros, sales y estereoisomeros, con inclusion de sus mezclas en todas las relaciones.
ARP100101112A 2009-04-02 2010-03-31 Derivados heterociclicos inhibidores de dihidroorotato deshidrogenasa, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento del cancer y otros trastornos autoinmunes. AR076183A1 (es)

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IN696DE2009 2009-04-02
US17815609P 2009-05-14 2009-05-14
EP09160526 2009-05-18

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AR076183A1 true AR076183A1 (es) 2011-05-26

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US (1) US9006454B2 (es)
EP (1) EP2414328B1 (es)
JP (1) JP5680054B2 (es)
CN (2) CN104030987B (es)
AR (1) AR076183A1 (es)
AU (1) AU2010233917B2 (es)
ES (1) ES2882797T3 (es)
MY (1) MY159575A (es)
NZ (1) NZ595819A (es)
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