AR045896A1 - Bencimidazolcarboxamidas - Google Patents

Bencimidazolcarboxamidas

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Publication number
AR045896A1
AR045896A1 ARP040102410A ARP040102410A AR045896A1 AR 045896 A1 AR045896 A1 AR 045896A1 AR P040102410 A ARP040102410 A AR P040102410A AR P040102410 A ARP040102410 A AR P040102410A AR 045896 A1 AR045896 A1 AR 045896A1
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Argentina
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hal
group
independently selected
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conh2
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ARP040102410A
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English (en)
Inventor
Buchstaller Hans-Peter Dr
Wiesner Matthias Dr
Zenke Frank Dr
Amendt Christiane Dr
Grell Matthias Dr
Sirrenberg Christian Dr
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Merck Patent Gmbh
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Publication of AR045896A1 publication Critical patent/AR045896A1/es

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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
    • C07D401/12—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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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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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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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • C07D403/12—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Rheumatology (AREA)
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  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a bencimidazolcarboxamidas de la fórmula (1), en donde: R6, R7 son, de modo independiente entre sí, H, A o SO2A; A está seleccionado, de modo independiente, del grupo integrado por alquilo, alquenilo, cicloalquilo, alquilencicloalquilo, alcoxi y alcoxialquilo; Ar2 está seleccionado, de modo independiente, de hidrocarburos aromáticos C6-14 y residuos heterocíclicos insaturados o aromáticos etilénicos C3-10 y uno o dos heteroátomos, seleccionados de modo independiente de N, O y S; R8, R9 y R10 están seleccionados, de modo independiente, de un grupo integrado por H, A, cicloalquilo C3-7, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)nCN, (CH2)nNR11R12, (CH2)nOR11, (CH2)nO(CH2)kNR11R12, (CH2)nCOOR12, (CH2)nCONR11R12, (CH2)nNR11COR13, (CH2)nNR11CONR11R12, (CH2)nNR11SO2A, (CH2)nSO2NR11R12, (CH2)nS(O)uR13, (CH2)nOC(O)R13, (CH2)nCOR13, (CH2)nSR11, CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)nCH=N-R11, (CH2)nOC(O)NR11R12, (CH2)nNR11COOR12, (CH2)nN(R11)CH2CH2OR13, (CH2)nN(R11)CH2CH2OCF3, (CH2)nN(R11)C(R13)HCOOR12, C(R13)HCOR12, (CH2)nN(R11)CH2CH2N(R12)CH2COOR12, (CH2)nN(R11)CH2CH2NR11R12, CH=CHCOOR11, CH=CHCH2NR11R12, CH=CHCH2NR11R12, CH=CHCH2OR13, (CH2)nN(COOR11)COOR12, (CH2)nN(CONH2)COOR11, (CH2)nN(CONH2)CONH2, (CH2)nN(CH2COOR11)COOR12, (CH2)nN(CH2CONH2)COOR11, (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR13COR11, (CH2)nCHR13COOR11, (CH2)nCHR13CH2OR14, (CH2)nOCN y (CH2)nNCO, en donde R11, R12 están seleccionados, de modo independiente, de un grupo integrado por H, A, (CH2)mAr3 y (CH2)mHet, o en NR11R12; R11 y R12 forman, junto con el átomo de N al que están unidos, un heterociclo de 5, 6 ó 7 miembros que opcionalmente contiene 1 ó 2 heteroátomos adicionales seleccionado de N, O y S; R13, R14 están seleccionados, de modo independiente, de un grupo integrado por H, Hal, A, (CH2)mAr4 y (CH2)mHet; Ar3, Ar4 son, de modo independiente entre sí, residuos hidrocarbonados aromáticos que comprenden 5 a 12 y, con preferencia, C5-10 que están opcionalmente sustituidos con uno o varios sustituyentes, seleccionados de un grupo integrado por A, Hal, NO2, CN, OR15, NR15R16, COOR15, CONR15R16, NR15COR16, NR15CONR15R16, NR16SO2A, COR15, SO2R15R16, S(O)uA y OOCR15; Het es un residuo heterocíclico saturado, insaturado o aromático que está opcionalmente sustituido con uno o varios sustituyentes seleccionados de un grupo integrado por A, Hal, NO2, CN, OR15, NR15R16, COOR15, CONR15R16, NR15COR16, NR15CONR15R16, NR16SO2A, COR15, SO2R15R16, S(O)uA y OOCR15; R15, R16 están seleccionados, de modo independiente, de un grupo integrado por H, A y (CH2)mAr6, en donde: Ar6 es un hidrocarburo aromático de 5 ó 6 miembros que está opcionalmente sustituido con uno o varios sustituyentes seleccionados de un grupo integrado por metilo, etilo, propilo, 2-propilo, ter-butilo, Hal, CN, OH, NH2 y CF3; k, m y n son, de modo independiente entre sí, 0, 1, 2, 3, 4 ó 5; X representa un enlace o es (CR11R12)h o (CHR11)h-Q- (CHR12)i, en donde Q está seleccionado de un grupo integrado por O, S, N-R15, (CHal2)j, (O-CHR18)j, (CHR18-O)j, CR18=CR19, (O-CHR18CHR19)j, (CHR18CHR19-O)j, C=O, C=S, C=NR15, CH(OR15), C(OR15)(OR20), C(=O)O, OC(=O), OC(=O)O, C(=O)N(R15), N(R15)C(=O), OC(=O)N(R15), N(R15)C(=O)O, CH=N-O, CH=N-NR15, S=O, SO2, SO2NR15 y NR15SO2, en donde: R18, R19, R20 están seleccionado, de modo independiente, de los significados dados para R8, R9 y R10, con preferencia, seleccionados de modo independiente del grupo integrado por H, A, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)nCN, (CH2)nOR11, (CH2)nNR11R12, (CH2)nO(CH2)kNR11R12, (CH2)nCOOR13, (CH2)nCONR11R12, (CH2)nNR11COR13, (CH2)nNR11CONR11R12, (CH2)nNR11SO2A, (CH2)nSO2NR11R12, (CH2)nS(O)uR13, (CH2)nCOR13, (CH2)nSR11, (CH2)nNHOA y (CH2)nNR11COOR13; h, i son, de modo independiente entre sí, 0, 1, 2, 3, 4, 5 ó 6, y j es 1, 2, 3, 4, 5 ó 6; Y está seleccionado de O, S, NR21, C(R22)-NO2, C(R22)-CN y (CN2), en donde: R21 está seleccionado, de modo independiente, de los significados dados para R13, R14; y R22 está seleccionado, de modo independiente, de los significados dados para R11, R12; p, r son, de modo independiente entre sí, 0, 1, 2, 3, 4 ó 5; q es 0, 1, 2, 3 ó 4, con preferencia, 0, 1 ó 2; u es 0, 1, 2 ó 3, con preferencia, 0, 1 ó 2; y Hal está seleccionado, de modo independiente, de un grupo integrado por F, Cl, Br e I; sus formas tautoméricas; y sus derivados, solvatos, sales y estereoisómeros farmacéuticamente aceptables. Al uso de los compuestos de la fórmula (1) como inhibidores de una o varias quinasas, al uso de los compuestos de la fórmula (1) para preparar una composición farmacéutica y a un método de tratamiento que comprende la administración de dicha composición farmacéutica a un paciente.
ARP040102410A 2003-07-11 2004-07-08 Bencimidazolcarboxamidas AR045896A1 (es)

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US (1) US7691870B2 (es)
EP (1) EP1643991B1 (es)
JP (1) JP5001650B2 (es)
AR (1) AR045896A1 (es)
CA (1) CA2531856C (es)
ES (1) ES2465624T3 (es)
WO (1) WO2005004863A1 (es)

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US7691870B2 (en) 2010-04-06
US20070093532A1 (en) 2007-04-26
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CA2531856C (en) 2013-07-30
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