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AR058558A1 - Derivados de anilina sustituida utiles como antagonistas de la histamina h3 - Google Patents

Derivados de anilina sustituida utiles como antagonistas de la histamina h3

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Publication number
AR058558A1
AR058558A1 ARP060105614A ARP060105614A AR058558A1 AR 058558 A1 AR058558 A1 AR 058558A1 AR P060105614 A ARP060105614 A AR P060105614A AR P060105614 A ARP060105614 A AR P060105614A AR 058558 A1 AR058558 A1 AR 058558A1
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Argentina
Prior art keywords
alkyl
heteroaryl
haloalkyl
aryl
group
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ARP060105614A
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Schering Corp
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    • 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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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/20—Hypnotics; Sedatives
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    • A61P25/00—Drugs for disorders of the nervous system
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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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    • 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
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Pulmonology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
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  • Urology & Nephrology (AREA)
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  • Epidemiology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Reivindicacion 1: Un compuesto representado mediante la formula estructural (1) o su sal farmacéuticamente aceptable, donde: a es 0, 1 o 2; b es 0, 1, 2, 3 o 4; U y W son cada uno CH, o uno de U y W es CH y el otro es N; M1, M2, n, p, X e Y son segun lo definido en (a), (b) o (c): (a) M1 es un resto de formula (2); M2 es N; n es 1 o 2; p es 0, 1 o 2; X es un enlace, alquileno, alquenileno, -C(O)-, -C(R8)(R9)-, -C(=N-OR10)-, -C(=N-OR10)-CH(R11)-, -CH(R11)-C(N-OR10)-, -O-, -CH2N(R12)-, - N(R12)CH2-, -N(R12)-, -NHC(O)-, -OCH2-, -CH2O-, -CH(OH)-, -S-, -S(O)- o -S(O)2-; e Y es -CH2-, -(CH2)2-, -C(=O)-, -C(=NOR13)-, -S-, -S(O)- o -SO2-; (b) M1 es N; M2 es N; n es 2; p es 1 o 2; X es un enlace, alquileno, alquenileno, -C(O)-, -NHC(O)-; - OC(O)-, -S(O)- o -S(O)2-; e Y es -CH2-, -(CH2)2-, -C(=O)-, -S-, -S(O)- o -SO2-; (c) M1 es N; M2 es CH; n es 1 o 2; p es 0, 1 o 2; X es un enlace, alquileno, alquenileno, -C(O)-, -NHC(O)-, -OC(O)-, -S(O)- o -S(O)2-; y Y es -O-, -CH2-, -(CH2)2-, - C(=O)-, -C(=NOR13)-, -S-, -S(O)- o -SO2-; Z es un enlace, -CH(R14)-(R14a-alquileno(C1-4))- o -CH(R14)-CH(R14b)=CH(R14b)-(R14a-alquileno(C1-2))-; R1 es R15-alquilo, R15-cicloalquilo, R15-arilo, R15-arilalquilo, R15-(heteroarilo de 6 miembros), R15- (heteroarilo de 6 miembros)alquilo, R15-(heteroarilo de 5 miembros), R15-(heteroarilo de 5 miembros)alquilo, R15-heterocicloalquilo, difenilmetilo, o un resto seleccionado del grupo de formulas (3); siempre y cuando R1 esté unido a X por un átomo de nitrogeno y M1 sea un resto de formula (2), X es un enlace o alquileno; y siempre y cuando R1 esté unido a X por un átomo de nitrogeno y M1 sea N, X es -(CH2)2-6-; k es 0, 1, 2, 3 o 4; K1 es 0, 1, 2 o 3; K2 es 0, 1 o 2; Q es O u S; R2 es R18- alquilo, R18-alquenilo, R18-arilo, R18-arilalquilo, R18-heteroarilo, R18-heteroarilalquilo, R18-cicloalquilo o R18-heterocicloalquilo; cada R3 se selecciona independientemente del grupo formado por H, halo, alquilo, haloalquilo, -OH, alcoxi y -CN; cara R4 se selecciona independientemente del grupo formado por H, alquilo, -OH, alcoxi, halo, -CF3, -OCF3, -NO2, -CO2(R19)2, -NHC(O)R19, -SO2N(R19)2 y -CN; R5 es H, alquilo, haloalquilo, R21-cicloalquilo, R21-arilo, R21-heteroarilo o -C(O)R20; R6 es H o alquilo; y cuando R1 está unido a X mediante un átomo de carbono y X es un enlace o alquileno, R6 tambieén puede ser R21-cicloalquilo, R21-arilo, R21-heteroarilo, -NHC(O)R7, -CN, hidroxialquilo, alcoxialquilo, C(R7)=N(OR7), -C(O)R7 o -N(R7)2; R7 se selecciona independientemente del grupo formado por H y alquilo; R8 y R9, junto con el carbono al cual están unidos, forman un anillo carbocíclico de 3 a 7 miembros opcionalmente sustituido con 1 o 2 sustituyentes seleccionados independientemente del grupo formado por halo, alquilo y haloalquilo; o R8 y R9, junto con el carbono al cual están unidos, forman un anillo heterocíclico de 3 a 7 miembros que comprende 2 a 6 átomos de carbono y 1 o 2 heteroátomos seleccionados independientemente del grupo formado por O, S y N, siempre que no haya enlace -O-O-, -S-S- o -O-S- alguno, donde dicho anillo heterocíclico está opcionalmente sustituido con 1 o 2 sustituyentes seleccionados independientemente del grupo formado por halo, alquilo y haloalquilo; o R8 y R9 juntos son =CH2; R10 es H, alquilo, haloalquilo, R21-arilo, R21-heteroarilo, R21-cicloalquilo, R21-heterocicloalquilo o R21-arilalquilo; R11 es H o alquilo; R12 se selecciona independientemente del grupo formado por H, alquilo, -CH2CF2, R21-arilo y R21-heteroarilo; R13 es H, alquilo, haloalquilo, R21-arilo o R21-heteroarilo; R14 es H, alquilo o haloalquilo; R14a es 1 a 3 sustituyentes seleccionados independientemente del grupo formado por H, halo, -OH, alquilo, haloalquilo, R21-cicloalquilo, R21-heterocicloalquilo, R21-arilo, R21-heteroarilo, alcoxi, -OCF3, -OCHF2, -NO2, -CN y -N(R11)2; R14b es H, fluor, alquilo o haloalquilo; R15 es 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo formado por H, halo, alquilo, haloalquilo, -OH, alcoxi, alquiltio, R21-cicloalquilo, R21-heterocicloalquilo, R21-arilo, R21-arilalquilo, R21-heteroarilo, R21- heteroarilalquilo, ariloxo, -OCF3, -OCHF2, -SCF3, -NO2, -CO2R12, -C(O)R20, -N(R12)2, - CON(R12)2, -NHC(O)R12, _SO2N(R12)2 y -CN; o dos sustituyentes R15 en los átomos de carbono en el anillo adyacentes juntos son -O-CH2-O-; R15a es H, alquilo, haloalquilo, alcoxi, alquiltio, R21-cicloalquilo, R21-heterocicloalquilo, R21-arilo, R21- arilalquilo, R21-heteroarilo, R21-heteroarilalquilo, R21-ariloxo, -OCF3, -OCHF2, -N(R12)2 o -SCF2; R16 se selecciona independientemente del grupo formado por alquilo, halogeno, haloalquilo y alquenilo; R17 es H, alquilo, hidroxi(C2-6)alquil-, haloalquil-, haloalcoxialquil-, alcoxialquil-, R21-arilo, R21-arilalquil-, R21-heteroarilo, R21-heteroarilalquil-, R21-cicloalquilo o R21-cicloalquilalquilo, o R21-heterocicloalquilalquilo; R18 es 1, 2 o 3 sustituyentes seleccionados independientemente del grupo formado por H, halo, alquilo, haloalquilo, -OH, alcoxi, R21-arilo, R21-ariloxi, -OCF3, -OCHF2, -NO2, -CO2R19, -N(R19)2, -NHC(O)R19, -NHSO2R19, -SO2N(R19)2 y -CN; R19 se selecciona independientemente del grupo formado por H, alquilo, haloalquilo, R21-arilo, R21-heteroarilo, R21-cicloalquilo y R21-heterocicloalquilo; R20 es alquilo, R21-arilo o R21-heteroarilo; y R21 es 1, 2 o 3 sustituyentes seleccionados independientemente del grupo formado por H, alquilo, halo, alcoxi, -CF3, -N(R11)2 y alquileno-N(R11)2.
ARP060105614A 2005-12-21 2006-12-19 Derivados de anilina sustituida utiles como antagonistas de la histamina h3 AR058558A1 (es)

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EP (1) EP1966143A2 (es)
JP (1) JP2009521451A (es)
KR (1) KR20080080201A (es)
CN (1) CN101384553A (es)
AR (1) AR058558A1 (es)
AU (1) AU2006331850A1 (es)
CA (1) CA2634847A1 (es)
IL (1) IL192310A0 (es)
MX (1) MX2008008339A (es)
PE (1) PE20071136A1 (es)
TW (1) TW200734285A (es)
WO (1) WO2007075688A2 (es)

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