ES2634841T3 - Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina - Google Patents

Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina Download PDF

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ES2634841T3
ES2634841T3 ES04795270.0T ES04795270T ES2634841T3 ES 2634841 T3 ES2634841 T3 ES 2634841T3 ES 04795270 T ES04795270 T ES 04795270T ES 2634841 T3 ES2634841 T3 ES 2634841T3
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alkyl
membered
independently
heterocycloalkyl
ring
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Stan Mchardy
John A. Lowe
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Pfizer Products Inc
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de fórmula I:**Fórmula** en la que: Y es (R100)k-R1-(R6)m; k es 0 o 1; l >= 0, 1, 2 o 3; m >= 1, 2 o 3; n es 0, 1, 2, 3 o 4; o es 0 o 1; p es 0, 1, 2 o 3; q es 0, 1, 2, 3 o 4; r es 1 o 2; s es 0, 1, 2, 3 o 4; t es 0 o 1; u es 1, 2 o 3; v es 1, 2 o 3; R100 es -CH2-, -CHalquil (C1-C3)-, -C(>=O)- o -SO2-; R1 es -alquilo (C1-C6), -cicloalquilo (C3-C8), -heterocicloalquilo (de 4 a 7 miembros),-(CH2)|-(arilo C6-C10) o - heteroarilo (de 5 a 10 miembros), o -tetrahidro-heteroarilo (de 5 a 10 miembros); cada R6 puede ser igual o diferente y se selecciona independientemente de H, halo, -alquil (C1-C6)-B, alcoxi (C1- C7), alquenoxi (C2-C4), alquil (C1-C6)-OH, -OH, CN, -NO2, -CR7R8R9, -NR20R21, -NHCOalquil(C1-C3), NHSO2alquil(C1-C3), C(>=O)OR22, -R23-C(>=O)OR22, -C(>=O)NH2, fenil-E, fenoxi-F, morfolina, -NR20R21, arilo, heteroarilo, -S-R24, y -SO2-R25; cada uno de B y D es independientemente H, OH, fenilo, difenilo o triflúor; cada uno de E y F es independientemente H, alquilo, o halo; cada uno de R7, R8 y R9 es independientemente H, alquilo (C1-C4), -OH, -O-alquilo (C1-C4),-CN, -NR26R27 y -NHC(>=O)alquilo (C1-C3), en la que dichos grupos alquilo están opcionalmente sustituidos con OH, OCH3, NH2, NHC(>=O)alquilo (C1-C3), o R7 y R8 junto con el átomo de carbono, al que están unidos, forman opcionalmente un anillo de cicloalquilo (C3-C7), o un anillo de heterocicloalquilo (C4-C7) que contiene 1-3 heteroátomos seleccionados de N, O, S y opcionalmente contiene un grupo C>=O; cada uno de R20 y R21 es independientemente H o alquilo (C1-C6); o R20 y R21 pueden conectarse mediante 4 a 7 átomos de carbono en los que de uno a tres de dichos átomos de carbono pueden reemplazarse opcionalmente con O, N o S, para formar un anillo de heterocicloalquilo; o R20 y R21 pueden conectarse mediante 3 a 7 átomos seleccionados de C, N, O o S para formar un anillo de heteroarilo de 5 a 10 miembros; cada uno de R22, R23 y R24 es independientemente H, o alquilo (C1-C5); R25 es alquilo (C1-C5); cada uno de R26 y R27 es independientemente H o alquilo (C1-C3); o R26 y R27 pueden conectarse mediante 4 a 7 átomos de carbono para formar un anillo de heterocicloalquilo; cada uno de R2 y R3 es independientemente H o alquilo (C1-C3); cada uno de R4 y R5 es independientemente H o alquilo (C1-C3) ; A es H; cada uno de R12 y R13 es independientemente H o -alquilo (C1-C4); o R12 y R13 pueden conectarse mediante 4 a 7 átomos de carbono para formar un anillo heterocicloalquilo; X es un enlace, -CH2-(R29)p, -C(>=O) o -SO2; R29 es -alquilo (C1-C3); W es -cicloalquilo (C3-C6), -heterocicloalquilo (de 3 a 7 miembros), -heterocicloalquilo (de 3 a 7 miembros) con 1 o 2 grupos C>=O, fenilo, o -heteroarilo (de 5 a 7 miembros); R30 es -alquilo (C1-C4), -alcoxi (C1-C3), CN, -F, -Cl, -Br, -I, -NR18R19, -NHC(>=O)R18, -SCH3 o -C(>=O)CH3; cada uno de R18 y R19 es independientemente H o -alquilo (C1-C3); Q es un enlace, -CH-(R31)r, -C(>=O) o -SO2; R31 es independientemente H o -alquilo (C1-C3); Z es -cicloalquilo (C3-C8), -heterocicloalquilo (de 4 a 8 miembros), fenilo o -heteroarilo (de 5 a 7 miembros); R14 es F, Cl, Br, I, V, H, -NR16R17, -OR16, -C(>=O)NR16R17, -(SO2)NR16R17, o -NR32-C>=O-R33, R15 es -alquilo (C1-C3), -alcoxi (C1-C3), -F, -Br, -Cl, -I -OH o -CN; V es -cicloalquilo (C3-C8), -alquilo (C1-C5), heterocicloalquilo (de 5 a 7 miembros), heterocicloalquilo (de 5 a 7 miembros) sustituido con 1 o 2 grupos C>=O o 1, 2 o 3 grupos alquilo (C1-C5); cada uno de R16 y R17 es independientemente H, -alquil (C1-C6)-(R34)u, o cicloalquil (C3-C8)-(R35)v; o R16 y R17 junto con el átomo de nitrógeno al que están unidos forman un anillo de heterocicloalquilo de 4 a 7 miembros que contiene opcionalmente de 1 a 3 heteroátomos adicionales seleccionados independientemente de N, S y O, y contiene C>=O, en la que dicho anillo de heterocicloalquilo está opcionalmente e independientemente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre alquilo (C1-C4), OH, alcoxi (C1-C4), NH2, -NH(C>=O)alquilo, -Nalquil (C1-C3))2, -C(>=O)CH3, CONH2, CO2H, CH2OH, CH2Oalquil (C2-C4), y heterocicloalquilo (de 5 a 7 miembros); cada uno de R32 y R33 es independientemente H o alquilo (C1-C5); o R32 y R33 pueden tomarse juntos para formar un anillo de cicloalquilo de 3-7 miembros, un anillo de heterocicloalquilo de 3-7 miembros con 1 a 3 heteroátomos, o un anillo de heteroarilo de 5-7 miembros con 1 a 3 heteroátomos; cada uno de R34 y R35 es independientemente H, OH, alquilo (C1-C5), alcoxi (C2-C4), NH2, NH(C>=O)alquilo (C1- C3), o un heterocicloalquilo de 5 a 7 miembros; o R34 y R35 pueden tomarse juntos para formar un puente que contiene 1-2 átomos de carbono; o una sal farmacéuticamente aceptable del mismo.
ES04795270.0T 2003-10-14 2004-10-14 Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina Expired - Lifetime ES2634841T3 (es)

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US51084603P 2003-10-14 2003-10-14
US510846P 2003-10-14
PCT/US2004/034083 WO2005037216A2 (en) 2003-10-14 2004-10-14 Bicyclic [3.1.0] derivatives as glycine transporter inhibitors

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US (1) US7473787B2 (es)
EP (1) EP1680124B1 (es)
JP (2) JP4732354B2 (es)
KR (1) KR20060095865A (es)
CN (2) CN1867338A (es)
AP (1) AP2006003592A0 (es)
AU (1) AU2004281794B2 (es)
BR (1) BRPI0415356A (es)
CA (1) CA2542279C (es)
CR (2) CR8333A (es)
DK (1) DK1680124T3 (es)
EA (1) EA009903B1 (es)
EC (1) ECSP066504A (es)
ES (1) ES2634841T3 (es)
GE (1) GEP20104959B (es)
IL (1) IL174299A (es)
IS (1) IS8355A (es)
MA (1) MA28094A1 (es)
MX (1) MXPA06004279A (es)
NO (1) NO337361B1 (es)
NZ (1) NZ546012A (es)
RS (1) RS20060190A (es)
TN (1) TNSN06109A1 (es)
UA (1) UA86037C2 (es)
WO (1) WO2005037216A2 (es)
ZA (1) ZA200602174B (es)

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