发明名称 METHODS AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES
摘要 Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
申请公布号 US2014329746(A1) 申请公布日期 2014.11.06
申请号 US201414332675 申请日期 2014.07.16
申请人 Kong Xianqi;Wu Xinfu;Bouzide Abderrahim;Valade Isabelle;Migneault David;Gervais Francine;Delorme Daniel;Bachand Benoit;Atfani Mohamed;Levesque Sophie;Samim Bita 发明人 Kong Xianqi;Wu Xinfu;Bouzide Abderrahim;Valade Isabelle;Migneault David;Gervais Francine;Delorme Daniel;Bachand Benoit;Atfani Mohamed;Levesque Sophie;Samim Bita
分类号 C07C309/19;C07D211/64;C07D211/52;C07K5/06;C07D213/50;C07D295/088;C07D211/70;C07C309/24;C07D211/14;C07D213/04 主分类号 C07C309/19
代理机构 代理人
主权项 1. A compound of formula VIII, XII, XIV or XV:wherein: R1 is hydrogen, a substituted or unsubstituted cycloalkyl, heterocyclic, aryl, arylcycloalkyl, bicyclic or tricyclic ring, a bicyclic or tricyclic fused ring group, or a substituted or unsubstituted C2-C10 alkyl group; R2 is selected from a group consisting of hydrogen, alkyl, mercaptoalkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, thiazolyl, triazolyl, imidazolyl, benzothiazolyl, and benzoimidazolyl; Rh is hydrogen, benzyl, aryl-alkyl, aryl, or alkyl; Ri is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted benzyl, alkenyl, carbocyclic, heterocyclic, absent or together with Rk, Rk or Rm may be linked to form a ring structure; Rj, Rl, Rm, Rn, and Ro are each independently hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted benzyl, alkyl, alkenyl, carbocyclic, heterocyclic, absent or together may be linked to form a ring structure; Rs is hydrogen or when n2 is 3, Rs is (CH2)3—SO3−X+; Rq and Rr are each selected independently from hydrogen or alkyl, Rt is hydrogen, alkyl, or aryl; Ru and Rv are each independently for each occurrence selected from hydrogen, aryl, benzyl, alkyl, alkenyl, carbocyclic, heterocyclic, or two Ru or Rv groups on adjacent carbon atoms may form a double bound, or together with the carbon atoms they are attached to forming a carbocyclic or heterocyclic ring; Y is SO3−X+, OSO3−X+, or SSO3−X+; X+ is hydrogen, a cationic group, or an ester-forming group; L1 is a substituted or unsubstituted C1-C5 alkyl group or absent, B is C1-C5 alkyl, alkenyl, or alkynyl group, and optionally fused with W when M is absent; M is a covalent bond, amino, C1-C6 alkyl, alkenyl, alkynyl, carboxyl, oxy, amide, ester, thioether, thioester or absent; W is a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, bicyclic or tricyclic ring, a bicyclic or tricyclic fused ring group, heterocyclic, thiazolyl, triazolyl, imidazolyl, benzothiazolyl, or benzoimidazolyl; v is 1, 2, 3, 4, 5, or 6; n2 is 0, 1, 2, or 3, selected such that three carbons are between the SO3−X+ group and the nitrogen atom in the ring; n3 is 4, 5, 6, or 7; and t1 and t2 are each single or double bonds, provided that both t1 and t2 are not both double bonds: or a pharmaceutically acceptable salt, ester or prodrug thereof, provided that when Y is methyl, R1 and R2 are hydrogen, Y is SO3−X+, and M is a covalent bond, B is not CH2—CH(M-W)—CH2.
地址 Dollard-des-Ormeaux CA