发明名称 NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS
摘要 The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
申请公布号 US2014357617(A1) 申请公布日期 2014.12.04
申请号 US201414463994 申请日期 2014.08.20
申请人 FAB PHARMA S.A.S. 发明人 Gerusz Vincent;Escaich Sonia;Oxoby Mayalen;Denis Alexis
分类号 C07D471/20;C07D401/14;C07D471/04 主分类号 C07D471/20
代理机构 代理人
主权项 1. A compound of formula (I): wherein: W and X independently represent a bond or a —(CH2)1-4 group, such that W and X together contain 1-5 carbon atoms;R1 represents an H, F, CN, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, CO2Rd, CORd, CONRaRb, OCORd, ORd, NRaRb, ON═CRdRe, NRcCORd, NRcCOORd, OCONRaRb, NRcCONRaRb, NRcSO2Ra, S(O)nRa, SO2NRaRb, —C(Ra)═N—O—Rf, Y—Ar or a Z-Het group, wherein Ar represents phenyl or naphthyl, Het represents a 4-10 membered monocyclic or bicyclic saturated or unsaturated heterocycle containing 1-5 heteroatoms selected from N, O and S and Y and Z independently represent a bond or a linker selected from O, S, CO, (C1-C6) alkylene, —O—(C1-C6) alkylene, —CO—(C1-C6) alkylene or —ON═CRd—(C1-C6) alkylene, wherein said R1 group may be optionally substituted by one or more R4 groups;R2 represents an H, F, CN, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, CO2Rd, CORd, CONRaRb, OCORd, ORd, NRaRb, ON═CRdRe, NRcCORd, NRcCOORd, OCONRaRb, NRcCONRaRb, NRcSO2Ra, S(O)nRa or SO2NRaRb group;Ra, Rb and Rc independently represent H, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, or an NRaRb group may optionally form a 3- to 7-membered nitrogen containing saturated heterocycle optionally containing 1 to 3 additional heteroatoms selected from N, O or S wherein said heterocycle may be optionally substituted by one or more (C1-C6) alkyl groups;Rd and Re independently represent H, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, halo(C1-C6) alkyl, halo(C1-C6) alkyl-O—(C1-C6) alkyl- or (C1-C6) alkyl-O—(C1-C6) alkyl-;Rf represents (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, halo(C1-C6) alkyl or —(C1-C6) alkyl-Ar, wherein Ar represents phenyl or naphthyl;R4 represents halogen, CN, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, CO2Rd, CORd, CONRaRb, OCORd, ORd, NRaRb, ON═CRdRe, NRcCORd, NRcCOORd, OCONRaRb, NRcCONRaRb, NRcSO2Ra, S(O)nRa, or SO2NRaRb;n represents an integer selected from 0 to 2;R3 represents a heterocycle of formula (j) wherein said R3 group may be optionally substituted by one or more R5 groups; R5 is selected from the group consisting of F, CO2Rd, CORd, CONRaRb, ORd, =O, NRaRb, NRcCORd or (C1-C6) alkyl optionally substituted by F, CO2Rd, CONRaRb, ORd, NRaRb, NRaCORd or Het optionally substituted by one or more (C1-C6) alkyl groups, or two R5 groups together with the atom to which they are attached may together form a Het group optionally substituted by one or more (C1-C6) alkyl groups; or a pharmaceutically acceptable salt or solvate thereof.
地址 Paris FR