公开(公告)号：US20190211206A1

公开(公告)日：2019-07-11

申请号：US15772992

申请日：2016-11-04

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： Ronald MEIJBOOM ,  Paul Marcel VAN MIDWOUD ,  Maarten VAN DIJK ,  Theodorus Adrianus Cornelius FLIPSEN ,  Esther DE BOEF

IPC分类号： C08L71/02 ,  C08G63/664 ,  A61L27/18 ,  A61L27/54 ,  A61K9/00 ,  A61K9/107 ,  A61K47/10 ,  A61K47/34 ,  A61L27/58

摘要： A composition including a) 55-98.9 wt % of at least one type of triblock copolymer (A) of formula (1) R—B-A-B—R   (1) b) 0.1-15 wt % of at least one surfactant (B) and c) 1-30 wt % of water, wherein A is a hydrophilic block having a number average molecular weight (Mn) of 100-1,000 Da, B is a hydrophobic block made from monomers having at least a monomer B1 and a monomer B2, wherein B1 and B2 have the largest weight contents in the hydrophobic block and B1 has a lower molecular weight than B2, wherein R is an end group which is H or a C1-C30 organic moiety, wherein the composition is fluid in a temperature range of 0° C. to 37° C., wherein the weight % are relative to the sum of a), b) and c), and wherein the sum of components a), b) and c) is at least 80 wt % of the entire composition, preferably at least 90 wt %; to the use of the composition and to pharmaceutical composiitons having said composition and an active pharmaceutical ingredient.

公开(公告)号：US09364544B2

公开(公告)日：2016-06-14

申请号：US14853181

申请日：2015-09-14

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： Sebastien Jerome Pierre ,  Mike De Leeuw

IPC分类号： A61K47/34 ,  A61K9/00 ,  A61K9/06 ,  A61L27/18 ,  A61L27/54 ,  A61L31/10 ,  A61L31/16 ,  C08G63/664

CPC分类号： A61K47/34 ,  A61K9/0024 ,  A61K9/06 ,  A61L27/18 ,  A61L27/54 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/414 ,  C08G63/664 ,  C08L67/04

摘要： Amphiphilic triblock copolymers B-A-B, wherein A is a linear poly(ethylene glycol) block, having a number average molecular weight (Mn) of between 900 and 3000 Daltons, determined with size exclusion chromatography; wherein B are hydrophobic blocks with at least two cyclic monomers selected from the group consisting of glycolide, lactide, 1,3-dioxan-2-one, 5,5-dimethyl-1,3-dioxan-2-one, 1,4-dioxan-2-one, 1,4-dioxepan-2-one, 1,5-dioxepan-2-one, each B-block having a number average molecular weight (Mn) of between 400 and 2000 Daltons, determined with size exclusion chromatography; and wherein 25% to 100% of the polymer hydroxyl end-groups are covalently modified with at least one derivative of a C2-C20 fatty acid. The invention also relates to compositions with such polymers and the use thereof.

摘要翻译： 两性三嵌段共聚物B-A-B，其中A是具有数均分子量（Mn）在900和3000道尔顿之间的直链聚（乙二醇）嵌段，其用尺寸排阻色谱法测定; 其中B是具有至少两种选自乙交酯，丙交酯，1,3-二恶烷-2-酮，5,5-二甲基-1,3-二恶烷-2-酮，1,4 - 二恶烷-2-酮，1,4-二氧杂环庚烷-2-酮，1,5-二氧杂环庚烷-2-酮，每个B嵌段的数均分子量（Mn）为400至2000道尔顿，用尺寸 排除色谱法; 并且其中25％至100％的聚合物羟基端基与C 2 -C 20脂肪酸的至少一种衍生物共价修饰。 本发明还涉及具有这种聚合物的组合物及其用途。

公开(公告)号：US10508200B2

公开(公告)日：2019-12-17

申请号：US15772992

申请日：2016-11-04

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： Ronald Meijboom ,  Paul Marcel Van Midwoud ,  Maarten Van Dijk ,  Theodorus Adrianus Cornelius Flipsen ,  Esther De Boef

IPC分类号： C08L71/02 ,  A61L27/18 ,  A61L27/54 ,  A61K9/00 ,  A61K47/10 ,  A61K47/34 ,  A61K9/107 ,  C08G63/664 ,  A61L27/58

摘要： A composition including a) 55-98.9 wt % of at least one type of triblock copolymer (A) of formula (1) R—B-A-B—R  (1) b) 0.1-15 wt % of at least one surfactant (B) and c) 1-30 wt % of water, wherein A is a hydrophilic block having a number average molecular weight (Mn) of 100-1,000 Da, B is a hydrophobic block made from monomers having at least a monomer B1 and a monomer B2, wherein B1 and B2 have the largest weight contents in the hydrophobic block and B1 has a lower molecular weight than B2, wherein R is an end group which is H or a C1-C30 organic moiety, wherein the composition is fluid in a temperature range of 0° C. to 37° C., wherein the weight % are relative to the sum of a), b) and c), and wherein the sum of components a), b) and c) is at least 80 wt % of the entire composition, preferably at least 90 wt %; to the use of the composition and to pharmaceutical compositions having said composition and an active pharmaceutical ingredient.

公开(公告)号：US10239991B2

公开(公告)日：2019-03-26

申请号：US15307862

申请日：2015-04-29

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： Ronald Meijboom ,  Theo Flipsen ,  Mike De Leeuw

IPC分类号： C08G63/664 ,  C08G64/18 ,  A61K9/00 ,  C12N9/00 ,  A61K31/167 ,  A61K31/635 ,  A61K38/47 ,  A61K47/34 ,  A61L27/18 ,  A61L27/54 ,  A61L27/58

摘要： A bioresorbable triblock copolymer according to Formula 1 R-B-A-B-R  (1) wherein A is a hydrophilic polymer, B a hydrophobic polymer and R are end-groups, wherein R is H or a C1-C30 organic moiety and wherein the copolymer is fluid in a temperature range of 0° C. to 37° C. A pharmaceutical composition including the triblock copolymer and at least one therapeutically active agent. The copolymer and pharmaceutical composition can be used for forming a depot in a human or animal body or as medical device.

公开(公告)号：US20170066874A1

公开(公告)日：2017-03-09

申请号：US15307862

申请日：2015-04-29

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： Ronald MEIJBOOM ,  Theo FLIPSEN ,  Mike DE LEEUW

IPC分类号： C08G63/664 ,  A61K31/167 ,  A61K31/635 ,  A61L27/58 ,  A61K9/00 ,  A61L27/18 ,  A61L27/54 ,  A61K38/47 ,  A61K47/34

CPC分类号： C08G63/664 ,  A61K9/0024 ,  A61K31/167 ,  A61K31/635 ,  A61K38/47 ,  A61K47/34 ,  A61L27/18 ,  A61L27/54 ,  A61L27/58 ,  A61L2400/06 ,  A61L2430/00 ,  C08G64/183 ,  C12N9/00 ,  C12Y302/01017

摘要： A bioresorbable triblock copolymer according to Formula 1 R-B-A-B-R  (1) wherein A is a hydrophilic polymer, B a hydrophobic polymer and R are end-groups, wherein R is H or a C1-C30 organic moiety and wherein the copolymer is fluid in a temperature range of 0° C. to 37° C. A pharmaceutical composition including the triblock copolymer and at least one therapeutically active agent. The copolymer and pharmaceutical composition can be used for forming a depot in a human or animal body or as medical device.

摘要翻译： 其中A是亲水性聚合物，B是疏水性聚合物，R是端基，其中R是H或C1-C30有机部分，并且其中共聚物是在0℃至37℃的温度范围内的流体。 药物组合物，包括三嵌段共聚物和至少一种治疗活性剂。 共聚物和药物组合物可以用于在人或动物体内形成贮库或用作医疗装置。

公开(公告)号：US20160000922A1

公开(公告)日：2016-01-07

申请号：US14853181

申请日：2015-09-14

申请人： INGELL TECHNOLOGIES HOLDING B.V.

发明人： SEBASTIEN JEROME PIERRE ,  MIKE DE LEEUW

IPC分类号： A61K47/34

CPC分类号： A61K47/34 ,  A61K9/0024 ,  A61K9/06 ,  A61L27/18 ,  A61L27/54 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/414 ,  C08G63/664 ,  C08L67/04

摘要： Amphiphilic triblock copolymers B-A-B, wherein A is a linear poly(ethylene glycol) block, having a number average molecular weight (Mn) of between 900 and 3000 Daltons, determined with size exclusion chromatography; wherein B are hydrophobic blocks with at least two cyclic monomers selected from the group consisting of glycolide, lactide, 1,3-dioxan-2-one, 5,5-dimethyl-1,3-dioxan-2-one, 1,4-dioxan-2-one, 1,4-dioxepan-2-one, 1,5-dioxepan-2-one, each B-block having a number average molecular weight (Mn) of between 400 and 2000 Daltons, determined with size exclusion chromatography; and wherein 25% to 100% of the polymer hydroxyl end-groups are covalently modified with at least one derivative of a C2-C20 fatty acid. The invention also relates to compositions with such polymers and the use thereof.

摘要翻译： 两性三嵌段共聚物B-A-B，其中A是具有数均分子量（Mn）在900和3000道尔顿之间的直链聚（乙二醇）嵌段，其用尺寸排阻色谱法测定; 其中B是具有至少两种选自乙交酯，丙交酯，1,3-二恶烷-2-酮，5,5-二甲基-1,3-二恶烷-2-酮，1,4 - 二恶烷-2-酮，1,4-二氧杂环庚烷-2-酮，1,5-二氧杂环庚烷-2-酮，每个B嵌段的数均分子量（Mn）为400至2000道尔顿，用尺寸 排除色谱法; 并且其中25％至100％的聚合物羟基端基与C 2 -C 20脂肪酸的至少一种衍生物共价修饰。 本发明还涉及具有这种聚合物的组合物及其用途。