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    FIBER COMPRISING A BIODEGRADABLE POLYMER
    3.
    发明申请
    FIBER COMPRISING A BIODEGRADABLE POLYMER 审中-公开
    包含可生物降解聚合物的纤维

    公开(公告)号：US20160102176A1

    公开(公告)日：2016-04-14

    申请号：US14975156

    申请日：2015-12-18

    Applicant: DSM IP Assets B.V.

    Inventor： Astrid FRANKEN ,  George MIHOV ,  Jens Christoph THIES

    IPC: C08G69/44 ,  A61K47/34

    CPC classification number: A61K9/0051 ,  A61K9/0019 ,  A61K9/70 ,  A61K47/34 ,  C08G69/44 ,  D01F1/10 ,  D01F6/625 ,  D01F6/82 ,  D10B2331/02 ,  D10B2331/041 ,  D10B2401/12

    Abstract: The present invention relates to a fiber comprising a biodegradable polymer which undergoes dimensional change upon injection in the human or animal body wherein the dimensional change is a reduction of the surface area to volume ratio of a factor 2 to 10. The fiber is sized for injection via a pharmaceutical syringe needle having a bore of at least 25 Gauge. The biodegradable polymer is an amorphous biodegradable polymer selected from the group of poly-hex am ethylene carbonates or polyesteramides. The amorphous biodegradable polymer is a preferably a polyesteramide comprising alpha-amino acids, diols and dicarboxylic acids as building blocks. The invention further relates to the use of the fiber for the manufacturing of a medicament for the treatment of ophthalmic diseases. The invention also relates to a process for the manufacturing of the fiber comprising the following process steps; a. extruding a biodegradable polymer into a fiber fitting in a needle of at least 25 Gauge b. which while under tension is cooled below its glass transition temperature such that the resultant fiber is amorphous.

    Abstract translation: 本发明涉及一种包含生物可降解聚合物的纤维，其在人或动物体内注射时经历尺寸变化，其中尺寸变化是因子2至10的表面积与体积比的降低。纤维的尺寸用于注射 通过具有至少25度的孔的制药注射器针头。 可生物降解的聚合物是选自聚六亚甲基亚乙基碳酸酯或聚酯酰胺的无定形可生物降解的聚合物。 无定形生物可降解聚合物优选为包含α-氨基酸，二醇和二羧酸作为结构单元的聚酯酰胺。 本发明还涉及该纤维在制备用于治疗眼科疾病的药物中的用途。 本发明还涉及一种用于制造纤维的方法，包括以下工艺步骤; 一个。 将可生物降解的聚合物挤出到至少25巴的针中的纤维配合物中。 其在张力下被冷却到其玻璃化转变温度以下，使得所得纤维是无定形的。

    BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY
    5.
    发明申请
    BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 有权
    用于药物递送的生物可降解的聚酰胺酰胺共聚物

    公开(公告)号：US20170051110A1

    公开(公告)日：2017-02-23

    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.

    BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY
    10.
    发明申请
    BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 有权

    公开(公告)号：US20160367681A1

    公开(公告)日：2016-12-22

    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

    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(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.

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