Russell John TAIT,Andrew Craig DONOHUE,Asha Marina D'SOUZA,Adrian SULISTIO,Stephen Lonsdale BIRKETT,Alan NAYLOR,Carmen Vittoria SCULLINO,Sarah Man Yee NG,David VALADE,Jason WATLING
申请号：
MX2019010837
公开号：
MX2019010837A
申请日:
2018.03.14
申请国别(地区):
MX
年份:
2019
代理人:
摘要：
A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I): (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide； Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group； R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl； D is a releasable drug selected from prostaglandins, ß-blockers and mixtures thereof； L is a linker group group； and at least one co-monomer of Formula III III J represents a linking functional group, n is 2 to 8, preferably 3 to 8； Y comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched Ci to do alkylene, amino, ether, ester, amide, carbonate and carbamate； A may be the same or different at each occurrence and represents a group comprising a terminal functional group comprising an alkyne or an azide functionality, wherein said terminal functional group is complementary to the terminal functional group X of formula (I) providing triazole moieties from reaction of X and A.Un conjugado de fármaco-polímero, que es un copolímero de al menos un monómero de fórmula (I):(ver formula) en donde: X puede ser igual o diferente en cada instancia y representa un grupo funcional terminal que comprende una alquina o una azida； Q se selecciona independientemente en cada instancia y puede estar presente o ausente y, cuando está presente, representa un grupo de enlace； R se selecciona del grupo que consiste en hidrocarburo lineal o ramificado, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido； D es un fármaco liberable que se selecciona de prostagla
