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公开(公告)号：EP1827501A2
公开(公告)日：2007-09-05
申请号：EP05855832.1
申请日：2005-12-21
发明人： MCMANUS, Samuel , KOZLOWSKI, Antoni
IPC分类号： A61K47/48 , C07C323/12 , C07D213/70
CPC分类号： A61K47/48215 , A61K31/415 , A61K47/60 , C07C323/12 , C07D213/70 , C07D213/71
摘要： Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y-S-W]x,, where POLY is a water soluble polymer; Y is a hydrocarbonbased spacer group, x is 1 to 25, and S-W is a thiol, protected thiol, or thiol-reactive derivative. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are conjugates of such polymeric reagents with pharmaceutically relevant molecules, and methods of their formation and use.
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公开(公告)号：EP1765411A2
公开(公告)日：2007-03-28
申请号：EP05767845.0
申请日：2005-06-30
CPC分类号： A61K47/48215 , A61K38/4846 , A61K47/60 , C12N9/644 , C12N9/96 , C12Y304/21022
摘要： Conjugates of a Factor IX moiety and one or more water-solute e polymers are provided. Typically, the water-soluble polymer is polyethylene glycol) or a derivative thereof. Also provided (among other things) are compositions comprising the conjugates, methods of making the conjugates, and methods of administering to a patient compositions comprising the conjugates.
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63.发明授权
公开(公告)号：EP1259262B1
公开(公告)日：2007-03-14
申请号：EP00984208.9
申请日：2000-12-08
IPC分类号： A61K47/48
CPC分类号： C08G65/33344 , A61K31/765 , A61K47/60 , C08G18/711 , C08G65/329 , C08G65/331 , C08G65/333 , C08G2210/00 , Y10S435/82
摘要： Poly(ethylene glycol) carbamate derivatives useful as water-soluble prodrugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be either trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the amine drug at a controllable rate as the gel degrades.
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公开(公告)号：EP1694363A2
公开(公告)日：2006-08-30
申请号：EP04814802.7
申请日：2004-12-16
CPC分类号： C08G65/337 , A61K47/60 , C08G65/332 , C08G65/33317 , C08G65/33396 , C08L2203/02
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
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公开(公告)号：EP1596887A2
公开(公告)日：2005-11-23
申请号：EP04715165.9
申请日：2004-02-26
IPC分类号： A61K47/48
摘要： Conjugates of a Factor VIII moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.
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66.发明公开MULTI-ARM POLYPEPTIDE-POLY(ETHYLENE GLYCOL) BLOCK COPOLYMERS AS DRUG DELIVERY VEHICLES 有权多臂多肽聚（乙二醇）嵌段共聚物AS药品供应车
公开(公告)号：EP1581583A1
公开(公告)日：2005-10-05
申请号：EP03814969.6
申请日：2003-12-24
发明人： ZHAO, Xuan, S. , REN, Zhongxu , EMOTO, Kazunori
CPC分类号： A61K9/5146 , A61K47/34 , A61K47/60 , A61K47/64 , C08G65/329 , C08L71/02 , C08L2203/02 , C08L2205/05 , C08L2666/26
摘要： The invention provides a mufti-arm block copolymer for use in delivering a variety of bioactive agents. The copolymer of the invention contains a central core from which extend multiple (3 or more) copolymer arms. Each copolymer arm possesses an inner polypeptide segment and an outer hydrophilic polymer segment. Thus, the overall structure of the copolymer comprises an inner core region that includes the central core and the inner polypeptide segment, while the outer core region is hydrophilic in nature. The mufti-arm copolymer of the invention is particularly useful for delivery of biologically active agents that can be entrapped within the inner core region.
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公开(公告)号：EP1581582A1
公开(公告)日：2005-10-05
申请号：EP04700409.8
申请日：2004-01-06
IPC分类号： C08G75/00
CPC分类号： A61K47/48215 , A61K47/60 , A61K47/62 , C07C319/06 , C07C323/41 , C08G65/00 , C08G65/2636 , C08G65/329 , C08G65/334 , C08L2203/02
摘要： The present invention provides water-soluble, polymer derivatives having a thiolselective terminus suitable for selective coupling to thiol groups, such as those contained in the cysteine residues of proteins.
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公开(公告)号：EP1578841A2
公开(公告)日：2005-09-28
申请号：EP03800397.6
申请日：2003-12-31
IPC分类号： C08G65/00
CPC分类号： C08G65/33337 , A61K47/60 , C08G65/329 , C08L2203/02
摘要： The present invention is directed to maleamic acid derivatives of water soluble polymers, to chemically stable water-soluble polymer succinamic acid -active agent conjugates, and to methods for reproducibly preparing, characterizing and using such polymer reagents and their conjugates.
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69.发明公开
公开(公告)号：EP1455839A1
公开(公告)日：2004-09-15
申请号：EP99951885.5
申请日：1999-10-08
IPC分类号： A61K47/48 , A61K47/34 , C08G65/329
CPC分类号： C08G65/329 , A61K47/60
摘要： This invention provides a method for preparing, in high purity and high yield, heterobifunctional derivatives of poly(ethylene glycol) or related polymers. A chromatographic purification step is not necessary in the method. In accordance with the method of the invention, an intermediate polymer having a formula of W-Poly-OH is provided bearing a removable group W at one terminus. The intermediate polymer W-Poly-OH is first altered by modifying the OH group to a first functional group X, followed by the removal of W to generate a second hydroxyl group. The latter hydroxyl group may then be further converted to a second functional group Y, thus providing the desired heterobifunctional derivative.
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公开(公告)号：EP1411075A3
公开(公告)日：2004-07-28
申请号：EP03028370.9
申请日：1999-03-11
IPC分类号： C08G65/333 , C08G65/329 , A61K47/48
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/329 , C08G65/33313 , C08G65/33337 , Y10S530/816
摘要： The invention relates to a method for preparing a polymer conjugate, in which a water-soluble polymer employed, the polymer having a linear or branched water-soluble polymer backbone and, at one end of the backbone, a branched moiety linked with two free reactive groups capable of covalent bonding to another molecule. Most specificly, it relates to an activated, substantially water soluble poly(ethylene glycol) having a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups is reacted with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated poly(ethylene glycol) and the biologically active agent.
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