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公开(公告)号:US08796207B2
公开(公告)日:2014-08-05
申请号:US13646605
申请日:2012-10-05
CPC分类号: A61K47/61 , A61K38/00 , A61K38/1816 , A61K38/193 , A61K38/465 , C07K14/505 , C07K14/52 , C07K14/535 , C07K14/575 , C12N9/22 , C12Y301/21001 , Y02A50/473
摘要: The present invention relates to a compound which is a polysaccharide derivative of EPO, or of an EPO like protein, wherein the polysaccharide is anionic and comprises between 2 and 200 saccharide units. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds.
摘要翻译: 本发明涉及作为EPO的多糖衍生物或EPO样蛋白质的化合物,其中所述多糖是阴离子型的,并且包含2至200个糖单元。 本发明还涉及包含新化合物的药物组合物和制备新化合物的方法。
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公开(公告)号:US20140127779A1
公开(公告)日:2014-05-08
申请号:US14155754
申请日:2014-01-15
发明人: Sanjay Jain , Ioannis Papaioannou , Peter Laing
IPC分类号: C07K14/61
CPC分类号: C08B37/0006 , A61K47/61 , B01D15/361 , B01D15/362 , B01D15/363 , B01D15/424 , B01D15/426 , C07K1/18 , C07K14/61 , C08B37/0003
摘要: Polydisperse and charged polysaccharides are fractionated into low polydispersity fractions (preferably having pd
摘要翻译: 多分散和带电多糖被分级成低分散度级分(优选具有pd <1.1),每个分子含有窄范围分子量范围内的物质。 将多分散多糖的水溶液与柱中的离子交换树脂接触,并通过水洗脱缓冲液对多糖进行选择性洗脱。 选择性洗脱由具有不同和恒定离子强度和/或pH值的至少3个顺序洗脱缓冲液组成,其中随后的缓冲液具有比前述步骤的离子强度和/或pH高的离子强度和/或pH。 新制剂特别适用于生产用于人和动物的PSA衍生化治疗剂。
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13.
公开(公告)号:US20220008544A1
公开(公告)日:2022-01-13
申请号:US17486833
申请日:2021-09-27
发明人: Dmitry Genkin
摘要: The present invention demonstrates that erythropoietin (EPO)-receptor (EPOR) is a malignant myeloma biomarker of sensitivity to EPO treatment and, itself a target for myeloma treatment. A low EPOR level in a myeloma cells of the subject indicates non-response to EPO treatment. Patients having high EPOR level in myeloma cells can be effectively treated with EPO, in particular an EPO derivatized with polysialic acid.
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公开(公告)号:US10406209B2
公开(公告)日:2019-09-10
申请号:US15276471
申请日:2016-09-26
发明人: Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
IPC分类号: C07H15/04 , A61K38/27 , C07K1/107 , C07H3/06 , C07K17/12 , C08B37/00 , A61K31/702 , A61K31/726 , C07H5/06 , A61K38/28 , A61K39/44 , A61K47/61 , A61K47/68
摘要: Derivatives are synthesized of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems.
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公开(公告)号:US20180289823A1
公开(公告)日:2018-10-11
申请号:US15811050
申请日:2017-11-13
发明人: Sanjay Jain , Rongsheng Zhang
IPC分类号: A61K47/61 , C12N9/22 , C07K14/575 , C07K14/535 , C07K14/52 , C07K14/505 , A61K38/18 , A61K38/46 , A61K38/19 , A61K38/00
摘要: The present invention relates to a composition comprising a population of polysaccharide derivatives of a protein, wherein the protein is insulin or an insulin-like protein and the polysaccharide is anionic and comprises between 2 and 125 saccharide units, and wherein the population consists of substantially only N-terminal derivatives of the protein. Typically, the polysaccharide is PSA. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds.
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公开(公告)号:US20170202827A1
公开(公告)日:2017-07-20
申请号:US15476617
申请日:2017-03-31
发明人: Dmitry Genkin , Kirill Surkov
IPC分类号: A61K31/473 , A61K31/138
CPC分类号: A61K31/473 , A61K31/135 , A61K31/138 , A61K31/40 , A61K31/565 , A61K31/57 , A61K31/58 , A61K2300/00
摘要: The invention provides a method for treatment of primary progesterone receptor-negative (PR−) endometrial cancer comprising administering (i) cridanimod or a salt or an ester thereof and (ii) a progesterone receptor (PR) agonist. The invention further provides a method for treatment of a primary estrogen receptor-negative (ER−) breast cancer, comprising administering (i) cridanimod or a salt or an ester thereof and (ii) a selective estrogen receptor modulator (SERM) or a selective estrogen receptor down-regulator (SERD). Also provided are compositions related to the above methods.
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17.
公开(公告)号:US20170007706A1
公开(公告)日:2017-01-12
申请号:US15276471
申请日:2016-09-26
发明人: Sanjay Jain , Peter Laing , Gregory Gregoriadis , Dale Howard Hreczuk-Hirst , Ioannis Papaioannou
CPC分类号: A61K38/27 , A61K31/702 , A61K31/726 , A61K38/28 , A61K39/44 , A61K47/61 , A61K47/6807 , C07H3/06 , C07H5/06 , C07H15/04 , C07K1/1077 , C07K17/12 , C08B37/00 , C08B37/0006 , C08B37/006 , C08B37/0063
摘要: Derivatives are synthesized of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems.
摘要翻译: 衍生物由还原性末端具有唾液酸的原料(通常为多糖)合成,其中还原末端单元转化为醛基。 当多糖在非还原末端具有唾液酸单元时,其可以被钝化,例如通过转化成羟基取代的部分。 衍生物可以与底物反应,例如含有胺或肼基团,以形成非交联的聚唾液酸化化合物。 底物可以例如是治疗上有用的药物肽或蛋白质或药物递送系统。
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公开(公告)号:US09492556B2
公开(公告)日:2016-11-15
申请号:US14614406
申请日:2015-02-04
发明人: Sanjay Jain , Peter Laing , Gregory Gregoriadis
IPC分类号: A61K38/00 , A61K47/48 , A61K38/18 , C07K14/535 , C07K14/52 , C07K14/505 , C07K14/575 , A61K38/46 , A61K38/19
CPC分类号: A61K47/61 , A61K38/00 , A61K38/1816 , A61K38/193 , A61K38/465 , C07K14/505 , C07K14/52 , C07K14/535 , C07K14/575 , C12N9/22 , C12Y301/21001 , Y02A50/473
摘要: The present invention relates to methods for producing N-terminal derivatives of proteins in which a polysaccharide, preferably having at least terminal sialic units, and preferably consisting essentially only of sialic acid units, is reacted at the N-terminus of a protein or peptide under controlled conditions to produce an N-terminal derivative. The controlled conditions include use of acidic pH for the derivatization step and a higher pH for purification. The derivatives are useful for improving pharmacokinetics and pharmacodynamics of proteins and peptides.
摘要翻译: 本发明涉及生产蛋白质N-末端衍生物的方法,其中优选具有至少末端唾液酸单元,优选仅由唾液酸单元组成的多糖,在蛋白质或肽下面的N末端进行反应 控制条件以产生N-末端衍生物。 受控条件包括使用酸性pH用于衍生化步骤和较高的pH用于纯化。 该衍生物可用于改善蛋白质和肽的药代动力学和药效学。
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公开(公告)号:US09266936B2
公开(公告)日:2016-02-23
申请号:US14313888
申请日:2014-06-24
IPC分类号: A61K38/00 , A61K38/18 , C07K14/535 , A61K47/48 , C07K14/52 , C07K14/505 , C07K14/575 , A61K38/46 , A61K38/19
CPC分类号: A61K47/61 , A61K38/00 , A61K38/1816 , A61K38/193 , A61K38/465 , C07K14/505 , C07K14/52 , C07K14/535 , C07K14/575 , C12N9/22 , C12Y301/21001 , Y02A50/473
摘要: The present invention relates to a compound which is a polysaccharide derivative of EPO, or of an EPO like protein, wherein the polysaccharide is anionic and comprises between 2 and 200 saccharide units. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds.
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公开(公告)号:US09102714B2
公开(公告)日:2015-08-11
申请号:US13650048
申请日:2012-10-11
发明人: Dale Howard Hreczuk-Hirst , Sanjay Jain , Peter Laing , Gregory Gregoriadis , Ioannis Papaioannou
CPC分类号: C08B37/0006 , A61K31/715 , A61K47/61 , A61K47/68 , C07K1/006 , C07K1/1077 , C07K1/13 , C07K14/001 , C07K17/10 , C08B37/00 , C12N9/96
摘要: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
摘要翻译: 将多唾液酸化合物与异双功能试剂反应以引入用于位点特异性缀合的侧链官能团,例如巯基,例如药物,药物递送系统,蛋白质或肽中半胱氨酸单元的侧链。 官能团是例如N-马来酰亚胺基团。
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