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Heteroaryl-8-azabicyclo [3.2.1] octane compounds, as antagonists of the opioid receptor mu
专利权人:
THERAVANCE; INC.
发明人:
LONG, DANIEL D.,JIANG, LAN,SAITO, DAISUKE ROLAND,VAN DYKE, PRISCILLA
申请号:
ES08795593
公开号:
ES2465621T3
申请日:
2008.08.26
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of the formula (I): ** Formula ** (copy figure 1 - formula (I) - on page 2) where, A, is a five-membered heteroarylene ring, which contains one, two, three or four heteroatoms, selected from nitrogen, oxygen and sulfur, wherein, not more than one of the heteroatoms, is oxygen or sulfur; R1 is selected from -C (O) ORa, -C (O) NRbRc, C2-6 alkenyl, C1-6 alkyl, C3-12 cycloalkyl, and phenyl, wherein C1-6 alkyl is substituted, optionally, with one or two R3, C3-12 cycloalkyl, it is substituted, optionally, with or one or two halo, or with - ORa or NRbRc, and phenyl is substituted, in a way optionally, with one or two halo, or with - ORa, -NRbRc, or C1-4 alkyl, wherein, C1-4 alkyl, is optionally substituted, with - ORa; R2, is hydrogen or phenyl; R3, is selected from -C (O) ORa, -C (O) NRdRe, -ORf, -NRbRg, -CN, C3-6 cycloalkyl, phenyl, and naphthyl, where C3-6 cycloalkyl is substituted , optionally, with one or two halo, or with - ORa, and phenyl is optionally substituted, with one or two halo or with -CN; Ra, Rb, Rc, and Rd are, independently, hydrogen or C1-3 alkyl; Re, is hydrogen or C1-3 alkyl, optionally substituted with C3-6 cycloalkyl, -ORa, phenyl, pyridyl, or 4- phenylpiperazinyl; or Rd and Re, taken together with the nitrogen atom to which they are attached, form piperidinyl; Rf, is hydrogen, C1-3alkyl, or phenyl; Rg, is hydrogen or C1-3alkyl, optionally substituted with phenyl; and m, is 0, 1, or 2; with the proviso that, when m is 0, R2 is H; or a pharmaceutically acceptable salt thereof.Un compuesto de la fórmula (I):**Fórmula** (copiar figura 1 - fórmula (I) - de la página 2) en donde, A, es un anillo de heteroarileno de cinco miembros, el cual contiene un, dos, tres o cuatro heteroátomos, seleccionados de entre nitrógeno, oxígeno y azufre, en donde, no más de uno de los heteroátomos, es oxígeno o azufre; R1, se selecciona de entre -C(O)ORa, -C(O)NRbRc, alquenilo C2-6, alquilo C1-6, cicloalquilo C3-12, y fenilo, en donde el alquilo C1-6, se encuent
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