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1. 发明申请

US20140120170A1 PARTICLES COMPRISING POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 有权
公开(公告)号：US20140120170A1
公开(公告)日：2014-05-01
申请号：US14128731
申请日：2012-06-25
申请人： George Mihov , John Andrew Zupancich
发明人： George Mihov , John Andrew Zupancich
IPC分类号： A61K47/34
CPC分类号： C08G69/44 , A61K31/165 , A61K47/34 , A61K47/6921 , C08J5/18 , C08J2377/12 , C08L77/12 , Y10T428/2982
摘要： The present invention relates to micro- or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), 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, (C1C6)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); 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. 发明授权

US09873764B2 Particles comprising polyesteramide copolymers for drug delivery 有权
公开(公告)号：US09873764B2
公开(公告)日：2018-01-23
申请号：US14128731
申请日：2012-06-25
申请人： George Mihov , John Andrew Zupancich
发明人： George Mihov , John Andrew Zupancich
IPC分类号： A61K47/34 , C08G69/44 , A61K47/69 , C08L77/12 , C08J5/18 , A61K31/165
CPC分类号： C08G69/44 , A61K31/165 , A61K47/34 , A61K47/6921 , C08J5/18 , C08J2377/12 , C08L77/12 , Y10T428/2982
摘要： The present disclosure relates to microparticles or nanoparticles 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(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 (C6-C10)aryl (C1-C6)alkyl; R8 is —(CH2)4—; 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; whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

3. 发明申请

US20140179802A1 FIBER COMPRISING A BIODEGRADABLE POLYMER 审中-公开
标题翻译：包含可生物降解聚合物的纤维
公开(公告)号：US20140179802A1
公开(公告)日：2014-06-26
申请号：US14115146
申请日：2012-05-02
申请人： Astrid Franken , George Mihov , Jens Christoph Thies
发明人： Astrid Franken , George Mihov , Jens Christoph Thies
IPC分类号： A61K9/00 , A61K47/34
CPC分类号： A61K9/0051 , A61K9/0019 , A61K9/70 , A61K47/34 , C08G69/44 , D01F1/10 , D01F6/625 , D01F6/82 , D10B2331/02 , D10B2331/041 , D10B2401/12
摘要： 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-hexamethylene 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.
摘要翻译：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碳酸酯或聚酯酰胺的无定形可生物降解的聚合物。无定形可生物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。

4. 发明申请

US20120177703A1 SOLID LINEAR OLIGO-OR POLY-E-CAPROLACTONE 审中-公开
标题翻译：固体线性寡糖或聚电子捕获剂
公开(公告)号：US20120177703A1
公开(公告)日：2012-07-12
申请号：US13382732
申请日：2010-07-09
申请人： George Mihov , Guy Draaisma
发明人： George Mihov , Guy Draaisma
IPC分类号： A61K47/34 , A61P27/02 , A61K9/14 , C08G63/66 , A61K9/00
CPC分类号： C08G63/664 , A61K9/0019 , A61K9/0024 , A61K9/0048 , A61K9/2031 , A61L27/18 , A61L27/34 , A61L31/06 , A61L31/10 , C08G63/78 , C08L71/12
摘要： The present invention relates to linear oligo- or poly-ε-caprolactones di-blockcopolymers, in solid form at room temperature, comprising monoalkyl oligoethyleneglycol residues. The present invention further relates to a drug delivery formulation comprising above materials and a process for the preparation of the drug delivery formulation. The oligoethyleneglycol residues are preferably selected from the group consisting of methyl diethylene glycol, methyl triethyleneglycol or methyl tetraethylene glycol. The oligo- or poly-ε-caprolactone derivatives are prepared via the reaction of mono-hydroxy-oligoethyleneglycol with ε-caprolactone, whereby the mono-hydroxy-oligoethyleneglycol acts as an initiator.
摘要翻译：本发明涉及在室温下为固体形式的线性低聚或多 - 己内酯二嵌段共聚物，其包含单烷基低聚乙二醇残基。本发明还涉及包含上述材料的药物递送制剂和用于制备药物递送制剂的方法。低聚乙二醇残基优选选自甲基二甘醇，甲基三乙二醇或甲基四甘醇。通过单羟基 - 低聚乙二醇与己内酯的反应制备低聚或多 - 己内酯衍生物，由此单羟基 - 低聚乙二醇用作引发剂。

5. 发明申请

US20140220099A1 BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY 有权
公开(公告)号：US20140220099A1
公开(公告)日：2014-08-07
申请号：US14128839
申请日：2012-06-25
申请人： Guy Draaisma , George Mihov
发明人： Guy Draaisma , George Mihov
IPC分类号： A61K47/34
CPC分类号： C08G69/44 , A61K31/165 , A61K47/34 , A61K47/6921 , C08J5/18 , C08J2377/12 , C08L77/12 , Y10T428/2982
摘要： 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.

6. 发明申请

US20120282299A1 COATINGS COMPRISING BIS-(ALPHA-AMINO-DIOL-DIESTER) CONTAINING POLYESTERAMIDE 审中-公开
公开(公告)号：US20120282299A1
公开(公告)日：2012-11-08
申请号：US13395527
申请日：2010-10-18
申请人： Soazig Claude Marie Delamarre , George Mihov , Astrid Franken , Kenneth Alan Messier
发明人： Soazig Claude Marie Delamarre , George Mihov , Astrid Franken , Kenneth Alan Messier
IPC分类号： A61K47/32 , A61K9/00 , A61P35/00 , A61K31/436
CPC分类号： 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
摘要： 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.

7. 发明授权

US09963549B2 Biodegradable polyesteramide copolymers for drug delivery 有权
公开(公告)号：US09963549B2
公开(公告)日：2018-05-08
申请号：US14128839
申请日：2012-06-25
申请人： Guy Draaisma , George Mihov
发明人： Guy Draaisma , George Mihov
IPC分类号： C08G69/44 , A61K47/69 , C08L77/12 , C08J5/18 , A61K47/34 , A61K31/165
CPC分类号： C08G69/44 , A61K31/165 , A61K47/34 , A61K47/6921 , C08J5/18 , C08J2377/12 , C08L77/12 , Y10T428/2982
摘要： 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.

8. 发明申请

US20140105957A1 BIS-(ALPHA-AMINO-DIOL-DIESTER) CONTAINING POLYESTERAMIDE FOR OPHTAMOLOGY 审中-公开
标题翻译：含有聚酰胺酰胺的BIS-（ALPHA-AMINO-DIOL-DIESTER）
公开(公告)号：US20140105957A1
公开(公告)日：2014-04-17
申请号：US14113521
申请日：2012-05-02
申请人： Astrid Franken , George Mihov , Jens Christoph Thies
发明人： Astrid Franken , George Mihov , Jens Christoph Thies
IPC分类号： A61K47/34 , A61K9/00
CPC分类号： A61K47/34 , A61K9/0048 , A61K9/0051 , A61K31/4535 , A61K31/5575
摘要： The present invention relates to an ocular polymer delivery composition comprising at least one ophthalmologic agent dispersed in at least one biodegradable polymer, wherein the polymer comprises at least one of a poly (ester amide) (PEA) having a chemical formula described by structural formula (I).
摘要翻译：本发明涉及一种眼部聚合物递送组合物，其包含分散在至少一种可生物降解的聚合物中的至少一种眼科剂，其中所述聚合物包含具有结构式（Q）所描述的化学式的聚（酯酰胺）（PEA）一世）。

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