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    Fibers comprising polyesteramide copolymers for drug delivery
    2.
    发明授权
    Fibers comprising polyesteramide copolymers for drug delivery 有权

    公开(公告)号：US10538864B2

    公开(公告)日：2020-01-21

    申请号：US14432349

    申请日：2013-10-24

    Applicant: DSM IP ASSETS B.V.

    Inventor： Mirian Hendrika Jacoba Gillissen-Van Der Vight ,  Jens Christoph Thies ,  George Mihov

    IPC: D01F6/82 ,  A61K47/34 ,  A61K9/00 ,  C08G69/44 ,  A61K9/70

    Abstract: 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 or (C2-C20) alkenylene 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, —(CH2)SH, —(CH2)2S(CH3), —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 (C1C6)alkyl, —R8 is —(CH2)4-; whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

    DRUG DELIVERY COMPOSITION COMPRISING PROTEINS AND BIODEGRADABLE POLYESTERAMIDES
    3.
    发明申请
    DRUG DELIVERY COMPOSITION COMPRISING PROTEINS AND BIODEGRADABLE POLYESTERAMIDES 有权
    包含蛋白质和生物可降解聚酯酶的药物递送组合物

    公开(公告)号：US20150216987A1

    公开(公告)日：2015-08-06

    申请号：US14425487

    申请日：2013-10-02

    Applicant: DSM IP ASSETS B.V.

    Inventor： Jens Christoph Thies ,  George Mihov ,  Guy Draaisma

    IPC: A61K47/34 ,  A61K38/44

    CPC classification number: A61K47/34 ,  A61K38/44 ,  C08G69/44 ,  C08L77/12 ,  C12Y111/01007 ,  C08L89/00

    Abstract: The present invention relates to a drug delivery composition comprising proteins and biodegradable polymers. The present invention further relates to a drug delivery system for controlled and long term release of proteins into a biological environment. The drug delivery composition comprises at least a protein and a biodegradable polymer possessing at least two different functional groups selected from the group of chosen among carboxyl-, ester-, amine-, amide-, thiol-, thioester- or hydroxyl groups pendant to the main polymer chain whereby the composition absorbs between 5-10% w/w water when exposed to physiological conditions for at least 20 days. The present invention further relates to a drug delivery system for controlled protein release comprising the composition. The drug delivery system may be chosen from microparticles, films, coatings, fibers, pellets, cylinders, discs, implants, microcapsules, microspheres, nanospheres, wafers, micelles, liposomes or woven or non-woven fabrics.

    Abstract translation: 本发明涉及包含蛋白质和生物可降解聚合物的药物递送组合物。 本发明还涉及用于将蛋白质控制和长期释放到生物环境中的药物递送系统。 药物递送组合物包含至少一种蛋白质和具有至少两种不同官能团的可生物降解的聚合物，其选自羧基，酯，胺，酰胺，硫醇，硫酯或羟基中的至少两个不同的官能团， 主要聚合物链，当组合物暴露于生理条件至少20天时，组合物吸收5-10％w / w的水。 本发明还涉及包含该组合物的用于受控蛋白质释放的药物递送系统。 药物递送系统可以选自微粒，膜，涂层，纤维，颗粒，圆柱体，盘，植入物，微胶囊，微球，纳米球，晶片，胶束，脂质体或织造或非织造织物。

    Biodegradable polyesteramide copolymers for drug delivery
    6.
    发明授权
    Biodegradable polyesteramide copolymers for drug delivery 有权

    公开(公告)号：US09896544B2

    公开(公告)日：2018-02-20

    申请号：US15252321

    申请日：2016-08-31

    Applicant: DSM IP ASSETS B.V.

    Inventor： Guy Draaisma ,  George Mihov

    IPC: A61K47/34 ,  A61K31/165 ,  C08G69/44 ,  A61K47/69 ,  C08L77/12 ,  C08J5/18

    CPC classification number: C08G69/44 ,  A61K31/165 ,  A61K47/34 ,  A61K47/6921 ,  C08J5/18 ,  C08J2377/12 ,  C08L77/12 ,  Y10T428/2982

    Abstract: The present invention relates to a poly (ester amide) (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)S(CH3), —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.

    Biodegradable polyesteramide copolymers for drug delivery
    7.
    发明授权
    Biodegradable polyesteramide copolymers for drug delivery 有权

    公开(公告)号：US09873765B2

    公开(公告)日：2018-01-23

    申请号：US15252350

    申请日：2016-08-31

    Applicant: DSM IP ASSETS B.V.

    Inventor： Guy Draaisma ,  George Mihov

    IPC: C08G69/44 ,  C08L77/12 ,  A61K31/165 ,  C09D177/12 ,  A61K47/34 ,  A61K9/70

    CPC classification number: C08G69/44 ,  A61K9/0048 ,  A61K9/7007 ,  A61K31/165 ,  A61K47/34 ,  C08L77/12 ,  C08L2203/16 ,  C09D177/12

    Abstract: The present invention relates to a poly (ester amide) (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(CH3), —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.

    FIBERS COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY
    8.
    发明申请
    FIBERS COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 审中-公开
    包含用于药物递送的聚酰胺酰胺共聚物的纤维

    公开(公告)号：US20150240387A1

    公开(公告)日：2015-08-27

    申请号：US14432349

    申请日：2012-10-24

    Applicant: DSM IP ASSETS B.V.

    Inventor： Mirian Hendrika Jacoba Gillissen-Van Der Vight ,  Jens Christoph Thies ,  George Mihov

    IPC: D01F6/82 ,  A61K9/70 ,  A61K9/00 ,  A61K47/34

    Abstract: 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 or (C2-C20) alkenylene 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, —(CH2)SH, —(CH2)2S(CH3), —CH2OH, —CH(OH)CH3, —(CH2)4NH3+, —(CH2)3NHC(═NH2+)NH2, —CH2COOH, —(CH2)COOH, —CH2—CO—NH2, —CH2CH2—CO—NH2, —NH—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 (C1C6)alkyl, —R8 is —(CH2)4-; whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

    Abstract translation: 本发明涉及包含具有结构式（Ⅳ）所述化学式的聚酯酰胺（PEA）的纤维，其中m + p为0.9-0.1，q为0.1-0.9，m + p + q = 1，由此m 或p可以为0，n为约5至约300; （优选50-200），-R 1独立地选自（C 2 -C 20）亚烷基或（C 2 -C 20）亚烯基及其组合; 分别独立地选自氢，（C1-C6）烷基，（C2-C6）烯基，（C2-C6）炔基，（C6-C10）烷基， ）芳基， - （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 -CH 2 - ，H 2 N - （CH 2）4 - （CH 2）2 CO-，CH 2 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选自（C 2 -C 20）亚烷基，（C 2 -C 20）亚烯基，烷氧基或低聚乙二醇，-R 6选自结构式为（III）的1,4：3,6-二脱氢己二醇的双环片段 ）; -R 7选自（C 6 -C 10）芳基（C 1 -C 6）烷基，-R 8是 - （CH 2）4 - ; 其中a为至少0.05，b为至少0.05，a + b = 1。

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