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1. 发明公开

EP4321151A3 FIBERS COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 审中-实审转让
公开(公告)号：EP4321151A3
公开(公告)日：2024-05-22
申请号：EP23210470.3
申请日：2013-10-24
申请人： DSM IP Assets B.V.
发明人： GILLISEN-VAN DER VIGHT, Mirian Hendrika Jacoba , THIES, Jens Christoph , MIHOV, George
IPC分类号： C08G69/44 , C08L77/12 , A61K47/34 , D01F6/82
CPC分类号： A61K47/34 , C08G69/44 , C08L77/12 , A61K9/0048 , D01F6/82 , A61P27/02
摘要： The present invention relates to fibers comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV),

wherein
-m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9
-m+p+q=1 whereby m or p could be 0
-n is about 5 to about 300; (pref. 50-200)
-R1 is independently selected from the group consisting of (C2-C20) alkylene, (C2-C20) alkenylene, -(R9-CO-O-R10-O-CO-R9)-, -CHR11-O-CO-R12-COOCR11- and combinations thereof;
-R3 and R4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C10)aryl, (C1-C6)alkyl, -(CH2)SH, -(CH2)2S(CH 3), -CH2OH, -CH(OH)CH3, -(CH2)4NH3+, --(CH2)3NHC(=NH2+)NH2, -CH2COOH, -(CH2)COOH, -CH2-CO-NH2, -CH2CH2-CO-NH2, -- -CH2CH2COOH, CH3-CH2-CH(CH3)-, (CH3)2-CH-CH2-, H2N-(CH2)4-, Ph-CH2-, CH=C-CH2-, HO-p-Ph-CH2-, (CH3)2-CH-, Ph-NH-, NH-(CH2)3-C-, NH-CH=N-CH=C-CH2-.
-R5 is selected from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy or oligoethyleneglycol
-R6 is selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III);

- R7 is selected from the group consisting of (C6-C10)aryl (C1-C6)alkyl
- R8 is -(CH2)4-;
- R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene.
- R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

2. 发明公开

EP4321151A2 FIBERS COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 审中-实审转让
公开(公告)号：EP4321151A2
公开(公告)日：2024-02-14
申请号：EP23210470.3
申请日：2013-10-24
申请人： DSM IP Assets B.V.
发明人： GILLISEN-VAN DER VIGHT, Mirian Hendrika Jacoba , THIES, Jens Christoph , MIHOV, George
IPC分类号： A61K9/00
摘要： The present invention relates to fibers comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV),

wherein
-m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9
-m+p+q=1 whereby m or p could be 0
-n is about 5 to about 300; (pref. 50-200)
-R 1 is independently selected from the group consisting of (C 2 -C 20 ) alkylene, (C 2 -C 20 ) alkenylene, -(R 9 -CO-O-R 10 -O-CO-R 9 )-, -CHR 11 -O-CO-R 12 -COOCR 11 - and combinations thereof;
-R 3 and R 4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 6 -C 10 )aryl, (C 1 -C 6 )alkyl, -(CH 2 )SH, -(CH 2 ) 2 S(CH 3 ), -CH 2 OH, -CH(OH)CH 3 , -(CH 2 ) 4 NH 3 +, --(CH 2 ) 3 NHC(=NH 2 +)NH 2 , -CH 2 COOH, -(CH 2 )COOH, -CH 2 -CO-NH 2 , -CH 2 CH 2 -CO-NH 2 , -- -CH 2 CH 2 COOH, CH 3 -CH 2 -CH(CH 3 )-, (CH 3 ) 2 -CH-CH 2 -, H 2 N-(CH 2 ) 4 -, Ph-CH 2 -, CH=C-CH 2 -, HO-p-Ph-CH 2 -, (CH 3 ) 2 -CH-, Ph-NH-, NH-(CH 2 ) 3 -C-, NH-CH=N-CH=C-CH 2 -.
-R 5 is selected from the group consisting of (C 2 -C 20 )alkylene, (C 2 -C 20 )alkenylene, alkyloxy or oligoethyleneglycol
-R 6 is selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III);

- R 7 is selected from the group consisting of (C 6 -C 10 )aryl (C 1 -C 6 )alkyl
- R 8 is -(CH2)4-;
- R 9 or R 10 are independently selected from C 2 -C 12 alkylene or C 2 -C 12 alkenylene.
- R 11 or R 12 are independently selected from H, methyl, C 2 -C 12 alkylene or C 2 -C 12 alkenylene whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

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