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。

公开(公告)号：US20170216495A1

公开(公告)日：2017-08-03

申请号：US15493664

申请日：2017-04-21

Applicant: DSM IP Assets B.V.

Inventor： Soazig Claude Marie DELAMARRE ,  George MIHOV ,  Astrid FRANKEN ,  Kenneth MESSIER

IPC: A61L31/10 ,  A61F2/82 ,  A61L31/14 ,  C09D177/12 ,  A61L31/16 ,  A61L31/06

CPC classification number: A61L31/10 ,  A61F2/82 ,  A61F2210/0004 ,  A61F2240/001 ,  A61L27/34 ,  A61L29/085 ,  A61L31/06 ,  A61L31/08 ,  A61L31/148 ,  A61L31/16 ,  A61L2300/204 ,  A61L2300/252 ,  A61L2300/416 ,  A61L2300/602 ,  A61L2300/604 ,  A61L2300/606 ,  A61L2420/02 ,  A61L2420/06 ,  C09D177/12 ,  C08L77/12

Abstract: The present invention relates to a coating comprising at least one biodegradable polymer, wherein the polymer comprises at least one or a blend of a poly (ester amide) (PEA) having a chemical formula described by structural formula (II), wherein; R1 is independently selected from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, —(R9—CO—O—R10—O—CO—R9)—, CH R11—O—CO—R12—COOCR11— and combinations thereof; R3 and R4 in a single co-monomer 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, (C1C6)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)—, formula (a), HO-P-Ph-CH2—, (CH3)2—CH—, Ph- NH—, NH—(CH2)3—C—, NH—CH═N—CH═C—CH2—. R5 or R6 are independently selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols or from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy, oligoethyleneglycol with a Mw ranging from 44 Da up to 700 Da, —CH2—CH—(CH2OH)2, CH2CH(OH)CH2 whereby R5 and R6 are non identical. R7 is hydrogen, (C6-C10) aryl, (C1C6) alkyl or a protecting group such as benzyl- or a bioactive agent; R8 is independently (C1-C20) alkyl or (C2-C20)alkenyl; R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene and R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene.

公开(公告)号：US20160184490A1

公开(公告)日：2016-06-30

申请号：US14989273

申请日：2016-01-06

Applicant: DSM IP ASSETS B.V.

Inventor： Soazig Claude Marie DELAMARRE ,  George MIHOV ,  Astrid FRANKEN ,  Kenneth Alan MESSIER

IPC: A61L31/10 ,  A61L31/16 ,  A61L31/08

CPC classification number: A61L31/10 ,  A61F2/82 ,  A61F2210/0004 ,  A61F2240/001 ,  A61L27/34 ,  A61L29/085 ,  A61L31/06 ,  A61L31/08 ,  A61L31/148 ,  A61L31/16 ,  A61L2300/204 ,  A61L2300/252 ,  A61L2300/416 ,  A61L2300/602 ,  A61L2300/604 ,  A61L2300/606 ,  A61L2420/02 ,  A61L2420/06 ,  C09D177/12 ,  C08L77/12

Abstract: The present invention relates to a coating comprising at least one biodegradable polymer, wherein the polymer comprises at least one or a blend of a poly (ester amide) (PEA) having a chemical formula described by structural formula (II), wherein; 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 co-monomer 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, (C1C6)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)—, formula (a), HO—P-Ph-CH2—, (CH3)2—CH—, Ph-NH—, NH—(CH2)3—C—, NH—CH═N—CH═C—CH2—. R5 or R6 are independently selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols or from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy, oligoethyleneglycol with a Mw ranging from 44 Da up to 700 Da, —CH2—CH—(CH2OH)2, CH2CH(OH)CH2 whereby R5 and R6 are non identical. R7 is hydrogen, (C6-C10) aryl, (C1C6) alkyl or a protecting group such as benzyl- or a bioactive agent; R8 is independently (C1-C20) alkyl or (C2-C20)alkenyl; R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene and R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene.