发明名称 COMPUESTOS DERIVADOS 3,8-DIAZABICICLO[3.2.1]OCTANONAS, 8-AZABICICLO[3.2.1]OCTANO Y 2,5-DIAZABICICLO[2.2.2]OCTANO DE PIPERAZINA, SALES DE LOS MISMOS, COMPOSICION FARMACEUTICA Y USO DE LOS COMPUESTOS EN LA FABRICACION DE MEDICAMENTOS
摘要 Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de éste; en la que a es 1, 2, 3, 4 ó 5; c es 0 ó 1; d es 1, 2, 3, 4 ó 5; k es 0, 1, 2, 3 ó 4; l es 0, 1, 2, 3 ó 4; m es 0, 1, 2, 3 ó 4; k, l y m no pueden ser todos 0 y si m y/o k no son 0, entonces l debe ser 0; W es CH o N; X es C(O), C(S) o CH2; Y es CH2; Z es oxígeno, NR9 o CR11R12; cada R1 se selecciona independientemente de hidrógeno, hidroxi, hidroxisulfonilo, halo, alquilo C1-6, mercapto, mercaptoalquilo C1-6, alquil C1-6 tio, alquil C1-6 sulfinilo, alquil C1-6 sulfonilo, alquil C1-6 tioalquilo C1-6, alquil C1-6 sulfinilalquilo, alquil C1-6 sulfonilalquilo C1-6, alcoxi C1-6, aril C6-10 oxi, haloalquilo C1-6, trifluorometilo, formilo, formilalquilo C1-6, nitro, nitroso, ciano, aril C6-10 alcoxi C1-6, haloalcoxi C1-6, trifluorometoxi, cicloalquilo C3-7, cicloalquil C3-7, alquilo C1-6, hidroxicicloalquil C3-7 alquilo C1-6, cicloalquil C3-7 amino, cicloalquil C3-7 aminoalquilo C1-6, (cicloalquil C3-7) (alquil C1-6) amino (cicloalquil C3-7)(alquil C1-6) aminoalquilo C1-6, cianoalquilo C1-6, alquenilo C2-7, alquinilo C2-7, arilo C6-10, aril C6-10 alquilo C1-6, aril C6-10 alquenilo C2-6, hidroxialquilo C1-6, hidroxiaril C6-10 alquilo C1-6, hidroxialquil C1-6 tioalquilo C1-6, hidroxialquenilo C2-6, hidroxialquinilo C2-6, alcoxi C1-6 alquilo C1-6, alcoxi C1-6 aril C6-10 alquilo C1-6, ariloxi C6-10 alquilo C1-6, aril C6-10 alcoxi C1-6 alquilo C1-6, amino, alquil C1-6 amino, (alquil C1-6)2 amino, aril C6-10 amino, aril C6-10 alquil C1-6 amino, aminoalquilo C1-6, alquil C1-6 aminoalquilo C1-6, (alquil C1-6)2 aminoalquilo C1-6, hidroxialquil C1-6 aminoalquilo C1-6, aril C6-10 aminoalquilo C1-6, aril C6-10 alquil C1-6 aminoalquilo C1-6, alquil C1-6 carbonilamino, (alquil C1-6 carbonil)(alquil C1-6 amino), alquil C1-6 carbonilaminoalquilo C1-6, (alquil C1-6 carbonil)(alquil C1-6 aminoalquilo C1-6, alcoxi C1-6 carbonilamino, alcoxi C1-6 carbonilalquil C1-6 amino, alcoxi C1-6 carbonilaminoalquilo C1-6, alcoxi C1-6 carbonil (alquil C1-6) aminoalquilo C1-6, carboxi, alcoxi C1-6 carbonilo, aril C6-10 alcoxi C1-6 carbonilo, alquil C1-6 carbonilo, alquil C1-6 carbonilalquilo C1-6, aril C6-10 carbonilo, aril C6-10 carbonilalquilo C1-6, aril C6-10 alquil C1-6 carbonilo, aril C6-10 alquil C1-6 carbonilalquilo C1-6, carboxialquilo C1-6, alcoxi C1-6 carbonilalquilo C1-6, aril C6-10 alcoxi C1-6 carbonilalquilo C1-6, alcoxi C1-6 alquil C1-6 carboniloxialquilo C1-6, aminocarbonilo, alquil C1-6 aminocarbonilo, (alquil C1-6)2 aminocarbonilo, aril C6-10 aminocarbonilo, aril C6-10 alquil C1-6 aminocarbonilo, aminocarbonilalquilo C1-6, alquil C1-6 aminocarbonilalquilo C1-6, (alquil C1-6)2 aminocarbonilalquilo C1-6, aril C6-10 aminocarbonilalquilo C1-6, alquil C1-6 aminocarbonilalquilo C1-6, amidino, guanidino, ureido, (alquil C1-6)2 ureido, ureidoalquilo C1-6, alquil C1-6 ureidoalquilo C1-6, (alquil C1-6)2 ureidoalquilo C1-6, heterocicloalquilo C2-9, heteroarilo C2-9, heterocicloalquil C2-9 alquilo C1-6 y heteroaril C2-9 alquilo C1-6; R4 es (R5Qq)farilo C6-10, (R5Qq)fcicloalquilo C3-10, (R5Qq)fheteroarilo C2-9, (R5Qq)fheterocicloalquilo C2-9, siendo f = 0, 1, 2, 3, 4 ó 5; Q es alquilo C1-6; q es 0 ó 1; R5 se selecciona independientemente de heterocicloalquil C2-9 carbonilo, heteroaril C2-9 carbonilo, heteroaril C2-9 alquil C1-6 aminocarbonilo, heteroaril C2-9 aminocarbonilo, heterocicloalquil C2-9 alquil C1-6 aminocarbonilo, alquil C1-6 sulfonilaminocarbonilo, alquil C1-6 sulfonilaminoalquil C1-6 aminocarbonilo, ureidoalquil C1-6 aminocarbonilo, (alquil C1-6)2 ureidoalquil C1-6 aminocarbonilo, haloalquil C1-6 aminocarbonilo, alquil C1-6 carbonilaminoalquil C1-6 aminocarbonilo, hidroxialquil C1-6 aminocarbonilo, aminosulfonilalquil C1-6 aminocarbonilo, carboxialquil C1-6 aminocarbonilo, alquil C1-6 aminosulfonilalquil C1-6 aminocarbonilo, aminoalquil C1-6 carbonilamino, alquil C1-6 aminoalquil C1-6 carbonilamino, carboxialquil C1-6 carbonilamino, carboxialcoxi C1-6 carbonilamino, (alquil C1-6)2 aminoalquil C1-6 carbonilamino, acetilaminoalquil C1-6 carbonilamino, (acetil) (alquil C1-6) aminoalquil C1-6 carbonilamino, alquil C1-6 sulfonilaminoalquil C1-6 carbonilamino, cianoguanidino-alquil C1-6 carbonilamino, alquil C1-6 cianoguanidino-alquil C1-6 carbonilamino, (alquil C1-6)2 cianoguanidino-alquil C1-6 carbonilamino, aminocarbonilalquil C1-6 carbonilamino, aminocarbonilaminoalquil C1-6 carbonilamino, alquil C1-6 aminocarbonilaminoalquil C1-6 carbonilamino, (alquil C1-6)2 aminocarbonilaminoalquil C1-6 carbonilamino, heteroaril C2-9 alquil C1-6 carbonilamino, heterocicloalquil C2-9 alquil C1-6 carbonilamino, aminosulfonilalquil C1-6 carbonilamino, hidroxialquil C1-6 ureido, aminoalquil C1-6 ureido, alquil C1-6 aminoalquil C1-6 ureido, (alquil C1-6)2 aminoalquil C1-6 ureido, heterocicloalquil C2-9 alquil C1-6 ureido, heteroaril C2-9 ureido, heteroaril C2-9 alquil C1-6 ureido, alquil C1-6 sulfonilureido, aminosulfonilalquil C1-6 ureido, aminocarbonilalquil C1-6 ureido, alquil C1-6 aminocarbonilalquil C1-6 ureido, (alquil )2 aminocarbonilalquil C1-6 ureido, acetilaminoalquil C1-6 ureido, (acetil)(alquil C1-6) aminoalquil C1-6 ureido, carboxialquil C1-6 ureido, haloalquil C1-6 sulfonilamino, aminoalquil C1-6 sulfonilamino, alquil C1-6 aminoalquil C1-6 sulfonilamino, (alquil C1-6)2 aminoalquil C1-6 sulfonilamino, acetilaminoalquil C1-6 sulfonilamino, (acetil)(alquil C1-6) aminoalquil C1-6 sulfonilamino, ureidoalquil C1-6 sulfonilamino, alquil C1-6 ureidoalquil C1-6 sulfonilamino, (alquil C1-6)2 ureidoalquil C1-6 sulfonilamino, alquil C1-6 sulfonilaminoalquil C1-6 sulfonilamino, cianoguanidinoalquil C1-6 sulfonilamino, carboxialquil C1-6 sulfonilamino, alquil C1-6 cianoguanidinoalquil C1-6 sulfonilamino, (alquil C1-6)2 cianoguanidinoalquil C1-6 sulfonilamino, aminocarbonilalquil C1-6 sulfonilamino, alcoxi C1-6 carbonilaminoalquil C1-6 sulfonilamino, aminosulfonilaminocarbonilo, alquil C1-6 aminosulfonilaminocarbonilo, (alquil C1-6)2 aminosulfonilaminocarbonilo, aril C6-10 sulfonilo, alquil C1-6 aminosulfonilamino, (alquil C1-6)2 aminosulfonilamino, aminocarbonilalquil C1-6 aminoalquil C1-6 sulfonilamino, heterocicloalquil C2-9 oxicarbonilaminoalquil C1-6 sulfonilamino, heteroaril C2-9 oxicarbonilaminoalquil C1-6 sulfonilamino, cianoguanidino, alquil C1-6 cianoguanidino, (alquil C1-6)2 cianoguanidino, heterocicloalquil C2-9 cianoguanidino, heterocicloalquil C2-9 alquil C1-6 cianoguanidino, heteroaril C2-9 alquil C1-6 cianoguanidino, aminoalquil C1-6 cianoguanidino, alquil C1-6 aminoalquil C1-6 cianoguanidino, (alquil C1-6)2 aminoalquil C1-6 cianoguanidino, aminocarbonilalquil C1-6 cianoguanidino, carboxialquil C1-6 cianoguanidino, alquil C1-6 aminocarbonilalquil C1-6 cianoguanidino, (alquil C1-6)2 aminocarbonilalquil C1-6 cianoguanidino, hidroxialquil C1-6 amino, aminocarbonilalquil C1-6 amino, carboxialquil C1-6 amino, alquil C1-6 sulfonilaminoalquil C1-6 amino, alcoxi C1-6 carbonilaminoalquil C1-6 amino, aminosulfonilalquil C1-6 amino, heteroaril C2-9 alquil C1-6 amino, acetilaminoalquil C1-6 amino, (acetil)(alquil C1-6) aminoalquil C1-6 amino, heterocicloalquil C2-9 alquil C1-6 amino, (alquil C1-6)2 aminoalquil C1-6 amino, alquil C1-6 aminoalquil C1-6 amino, alcoxi C1-6 alquil C1-6 amino, alcoxi C1-6 carbonilalquilamino, cianoalquil C1-6 amino, heterocicloalquil C2-9 oxicarbonilaminoalquil C1-6 amino, heteroaril C2-9 oxicarbonilaminoalquil C1-6 amino, cianoguanidinoalquil C1-6 amino, alquil C1-6 cianoguanidinoalquil C1-6 amino, (alquil C1-6)2 cianoguanidinoalquil C1-6 amino, ureidoalquil C1-6 amino, alquil C1-6 ureidoalquil C1-6 amino, (alquil C1-6)2 ureidoalquil C1-6 amino, aminocarboniloxialquil C1-6 amino, hidroxialquil C1-6 carbonilamino, alquil C1-6 aminocarbonilalquil C1-6 carbonilamino, (alquil C1-6)2 aminocarbonilalquil C1-6 carbonilamino, alcoxi C1-6 carbonilaminoalquil C1-6 carbonilamino, aminosulfonilalquil C1-6 carbonilamino, hidroxialquil C1-6 aminoalquil C1-6 carbonilamino, (alquil C1-6)2 aminoalquil C1-6 aminoalquil C1-6 carbonilaminoalquil C1-6 aminoalquil C1-6 aminoalquil C1-6 carbonilamino, aminoalquil C1-6 aminoalquil C1-6 carbonilamino, alcoxi C1-6 alquil C1-6 aminoalquil C1-6 carbonilamino, heterocicloalquil C2-9 oxicarbonilamino, heteroaril C2-9 carbonilaminoalquil C1-6 carbonilamino, heteroaril C2-9 carbonilamino, heterocicloalquil C2-9 carbonilamino, heteroaril C2-9 alquil C1-6 carbonilamino, heterocicloalquil C2-9 alquil C1-6 carbonilamino, heterocicloalquil C2-9 carbonilaminoalquil C1-6 carbonilamino, cianoalquil C1-6 carbonilamino, alquil C1-6 sulfonilaminoalquil C1-6 aminocarbonilamino, alcoxi C1-6 carbonilaminoalquil C1-6 aminocarbonilamino, heterocicloalquil C2-9 oxicarbonilaminoalquil C1-6 aminocarbonilamino, heteroaril C2-9 oxicarbonilaminoalquil C1-6 aminocarbonilamino, ureidoalquil C1-6 ureido, alquil C1-6 ureidoalquil C1-6 ureido, (alquil C1-6)2 ureidoalquil C1-6 ureido, cianoguanidinoalquil C1-6 ureido, heteroaril C2-9 (cianoguanidino), aminosulfonilo, aminoalquil C1-6 sulfonilo, alquil C1-6 aminoalquil C1-6 sulfonilo, (alquil C1-6)2 aminoalquil C1-6 sulfonilo, alquil C1-6 aminosulfonilo, (alquil C1-6)2 aminosulfonilo, heterocicloalquil C2-9 sulfonilo, aminoalquil C1-6 aminosulfonilo, alquil C1-6 aminoalquil C1-6 aminosulfonilo, (alquil C1-6)2 aminoalquil C1-6 aminosulfonilo, heteroaril C2-9 aminosulfonilo, hidroxialquil C1-6 aminosulfonilo, alcoxi C1-6 alquil C1-6 aminosulfonilo, ureidoalquil C1-6 aminosulfonilo, alquil C1-6 ureidoalquil C1-6 aminosulfonilo, (alquil C1-6)2 ureidoalquil C1-6 aminosulfonilo, alquil C1-6 sulfonilaminoalquil C1-6 aminosulfonilo, alcoxi C1-6 carbonilaminoalquil C1-6 aminosulfonilo, heterocicloalquil C2-9 oxicarbonilaminoalquil C1-6 aminosulfonilo, heteroaril C2-9 oxicarbonilaminoalquil C1-6 aminosulfonilo, aminocarbonilalquil C1-6 aminosulfonilo, cianoguanidinoalquil C1-6 aminosulfonilo, heteroaril C2-9 aminosulfonilo, heteroaril C2-9 alquil C1-6 aminosulfonilo, heterocicloalquil C2-9 aminosulfonilo, alquil C1-6
申请公布号 AR035354(A1) 申请公布日期 2004.05.12
申请号 AR2001P104880 申请日期 2001.10.17
申请人 PFIZER PRODUCTS INC. 发明人
分类号 A61K;A61K31/46;A61K31/4995;A61P;A61P1/04;A61P1/16;A61P3/10;A61P9/04;A61P9/08;A61P9/10;A61P11/00;A61P11/04;A61P11/06;A61P11/16;A61P13/12;A61P17/00;A61P17/06;A61P19/02;A61P19/08;A61P21/00;A61P25/00;A61P27/02;A61P29/00;A61P31/04;A61P31/06;A61P31/08;A61P31/14;A61P31/16;A61P31/18;A61P31/20;A61P31/22;A61P33/06;A61P35/00;A61P37/00;A61P37/02;A61P37/06;A61P37/08;A61P43/00;C07D;C07D209/00;C07D221/00;C07D241/00;C07D451/02;C07D471/08;C07D487/08;(IPC1-7):C07D487/08;A61K31/499;A61K31/439 主分类号 A61K
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