发明名称 ORALLY AVAILABLE COMPOUNDS, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS ANTI-ADHESIVE DRUGS FOR TREATING E. COLI INDUCED INFLAMMATORY BOWEL DISEASES SUCH AS CROHN'S DISEASE
摘要 Orally available compounds, a process for preparing the same and their uses as anti-adhesive drugs for treating E. coli induced inflammatory bowel diseases such as crohn's disease.
申请公布号 US2016340445(A1) 申请公布日期 2016.11.24
申请号 US201515113986 申请日期 2015.01.23
申请人 CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ;UNIVERSITE D'AUVERGNE ;UNIVERSITE DES SCIENCIES ET TECHNOLOGIES DE LILLE 1 ;UNIVERSITE DE NANTES ;INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE) 发明人 BOUCKAERT Julie;GOUIN Sebastien;SIVIGNON Adeline;DARFEUILLE-MICHAUD (Deceased) Arlette;BILYY Rostyslav;ALVAREZ-DORTA Dimitri;YAMAKAWA Nao;DUMYCH Tetiana
分类号 C08B37/16;A61K45/06;C07H7/02;A61K31/7056;C07H15/04;A61K31/7064;C07H15/14;A61K9/00;A61K31/724;A61K31/7028 主分类号 C08B37/16
代理机构 代理人
主权项 1. Compound of the following formula (I): wherein: X represents NH, O, S or CH2; n represents an integer comprised from 3 to 7, n being in particular equal to 5; Y represents a group selected from: Z representing O, S or NH; R representing: H,a linear or branched (C1-C7)-alkyl, in particular methyl, ethyl, isopropyl or isobutyl,a group of formula —(CH2)i—X′—(CH2)j—H, wherein X′ represents O, S or NH, i is an integer from 1 to 7, and j is an integer from 0 to 7, said group being in particular —CH2—O—CH3,a linear or branched (C2-C7)-alkenyl,a linear or branched (C2-C7)-alkynyl,a (C3-C7)-cycloalkyl,a (C5-C7)-cycloalkenyl,a (C3-C7)-heterocycloalkyl,a (C5-C7)-heterocycloalkenyl,an aryl, said aryl being an aromatic or heteroaromatic group,an alkyl aryl, wherein the aryl is an aromatic or heteroaromatic group,a CO—(C1-C7)-alkyl,a CO-aryl, wherein aryl is an aromatic or heteroaromatic group, a CO2H, a CO2—(C1-C7)-alkyl, a CONH—(C1-C7)-alkyl, CF3, adamantyl, CHRa—NH2, wherein Ra represents the side chain of a proteinogenic aminoacid, a cyclodextrin, said cyclodextrin being in particular chosen from α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD) and their derivatives, in particular alkylated α-cyclodextrins, alkylated β-cyclodextrins and alkylated γ-cyclodextrins, said cyclodextrin being more particularly a β-cyclodextrin, even more particularly a cyclodextrin of one of the following formulae: said (C1-C7)-alkyl, group of formula —(CH2)i—X′—(CH2)j—H, (C2-C7)-alkenyl, (C2-C7)-alkynyl, (C3-C7)-cycloalkyl, (C5-C7)-cycloalkenyl, (C3-C7)-heterocycloalkyl, (C5-C7)-heterocycloalkenyl, CO—(C1-C7)-alkyl, CO2—(C1-C7)-alkyl, CONH—(C1-C7)-alkyl, aryl, alkyl aryl, CO-aryl and cyclodextrin being substituted or not by one or more substituent(s), each independently selected from: a linear or branched (C1-C7)-alkyl,a linear or branched (C2-C7)-alkenyl,a linear or branched (C2-C7)-alkynyl,a (C3-C7)-cycloalkyl,a (C5-C7)-cycloalkenyl,a (C3-C7)-heterocycloalkyl,a (C5-C7)-heterocycloalkenyl,an aryl, wherein the aryl is an aromatic or heteroaromatic groupan alkyl aryl, wherein the aryl is an aromatic or heteroaromatic group,a CHO,a CO—(C1-C7)-alkyl,a CO-aryl, wherein aryl is an aromatic or heteroaromatic group,a CO2H,a CO2—(C1-C7)-alkyl,a CONH—(C1-C7)-alkyl,a halogen selected from the group comprising F, Cl, Br, and I,CF3,ORa, wherein Ra represents: H, a linear or branched (C1-C7)-alkyl, a (C3-C7)-cycloalkyl, CO—(C1-C7)-alkyl, or CO-aryl, wherein aryl is an aromatic or heteroaromatic group,NRbRc, wherein Rb and Rc represent independently from each other: H, a linear or branched (C1-C7)-alkyl, a (C3-C7)-cycloalkyl, CO—(C1-C7)-alkyl, or CO-aryl, wherein aryl is an aromatic or heteroaromatic group,NO2,CN,SO3H or one of its salts, in particular SO3Na; and its pharmaceutically acceptable salts, provided that when R represents CHRa—NH2, then Y can only represent the following group (a): for use in the treatment or the prevention of inflammatory bowel disease, in particular Crohn disease or ulcerative colitis.
地址 Paris Cedex 16 FR