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Aminoester Alkaloid derivatives and medicinal composition thereof
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
AMARI GABRIELE,RICCABONI MAURO,CALIGIURI ANTONIO
申请号:
ARP110102147
公开号:
AR081965A1
申请日:
2011.06.21
申请国别(地区):
AR
年份:
2012
代理人:
摘要:
They act as muscarinic receptor antagonists, processes for the preparation thereof, compositions comprising them and the therapeutic use thereof. Claim 1: A compound characterized in that it is of general formula (1) where R1 is selected from the group consisting in aryl, heteroaryl, arylalkyl C 1-6 and heteroarylalkyl C 1-6, and is optionally substituted with one or more substituents selected from the group consisting of halogen atoms, OH, oxo, SH, NH2, NO2, CN, CON (R5 ) 2, NHCOR5, COR5, CO2R5, C1-6 alkylsulfanyl, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy and C1-6 haloalkoxy;R2 es H o se selecciona entre el grupo que consiste en alquilo C1-6 cicloalquilo C3-8 y arilalquilo C1-6 y est opcionalmente sustituido con uno oms sustituyentes seleccionados entre el grupo que consiste en tomos de hal geno OH oxo SH NH2 NO2 CN COR5, CO2R5, C1-6 alkylsulfanyl, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy and C1-6 haloalkoxy and C1-6 arylalkoxy; R5 is selected, independently in each case, from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, heteroaryl and aryl optionally substituted with one or more substituents selected from the group consisting of in halogen atoms, OH, oxo, SH, NH2, NO2, CN, CONH2, COOH, C1-6 alkoxycarbonyl, C1-6 alkylsulfanyl, C1-6 alkylsulfinyl, C1-6 alkyl, C1-6 haloalkyl , C1-6 alkoxy and halo C1-6 alkoxy; Q represents a group of formula (2) or (3),R4 is a set of formulas: - (CH2) P - (CH2) Q - (W, where p is an integer between 0 or 1 to 4; q is an integer between 0 or 1 to 4; P is not or from O, s, so, so, SO2, Co, nr5ch = Ch, n (R5) SO2, n (R5) coo, n (R5) C (o),SO2N (R5)CO (o) n (R5) and C (o) n (R5);W is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, aryl, and heteroaryl, and is optionally substituted with one or more substituents selected from the group consisting of halogen atoms, OH, oxo, SH, NH2, NO2, CN, CON (R5) 2,
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