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1. 发明申请

WO2006030217A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006030217A2
公开(公告)日：2006-03-23
申请号：PCT/GB2005/003559
申请日：2005-09-15
申请人： DRUG DISCOVERY LABORATORY AS , COCKBAIN, Julian , KLAVENESS, Jo , BRUDELI, Bjarne
发明人： KLAVENESS, Jo , BRUDELI, Bjarne
IPC分类号： A61K47/48
CPC分类号： A61K47/555 , A61K47/542
摘要： The invention provides a water-soluble prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a protein binding moiety, wherein said therapeutically effective moiety has an anticancer, antiinflammatory, antiinfective or antipain effect, said protein binding moiety binds non-covalently to blood proteins, and the protein binding of said compound is at least 100 % higher than that of the therapeutically effective moiety itself, with the exclusion of (i) the monoester of gemcitabine with azelaic acid, (ii) the monoester of dideoxycytidine with 1,12-dodecanedicarboxylic acid, (iii) 2-amino-l,9-dihydro-9(2'-(1-(10-acetyl-decanoyloxy)ethoxymethyl))-guanine, (iv) 5'-cytarabine monoester with 1,4-phenylene diacetic acid, (v) the monoester of metronidazole with 1,4-butanedicarboxylic acid, and (vi) the monoester of metronidazole with 1,6-phenylene diacetic acid; and pre-prodrugs metabolizable thereto.
摘要翻译：本发明提供了一种水溶性前药化合物，其包含通过可代谢切割键与蛋白质结合部分相连的治疗有效部分，其中所述治疗有效部分具有抗癌，抗炎，抗感染或抗胰蛋白酶作用，所述蛋白质结合部分非共价结合并且所述化合物的蛋白质结合比治疗有效部分本身的蛋白质结合至少高100％，排除（i）吉西他滨与壬二酸的单酯，（ii）双脱氧胞苷的单酯与1 ，12-十二烷二羧酸，（iii）2-氨基-1,9-二氢-9（2' - （1-（10-乙酰基 - 癸酰氧基）乙氧基甲基）） - 鸟嘌呤，（iv）5'-阿糖胞苷单酯与1 ，4-亚苯基二乙酸，（v）甲硝唑与1,4-丁烷二羧酸的单酯，和（vi）甲硝唑与1,6-亚苯基二乙酸的单酯; 和其可代谢的前药前药。

2. 发明申请

WO2016103034A1 PROTEIN COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：蛋白质组合物及其用途
公开(公告)号：WO2016103034A1
公开(公告)日：2016-06-30
申请号：PCT/IB2015/002540
申请日：2015-12-23
申请人： DRUG DISCOVERY LABORATORY AS
发明人： KLAVENESS, Aase, Jorun , KLAVENESS, Jo
IPC分类号： A61K9/00 , A61K38/17 , A61K39/395 , A61K47/12 , A61K9/19 , A61K47/26
CPC分类号： A61K9/19 , A61K9/0019 , A61K39/39591 , A61K47/12 , A61K47/26
摘要： The present invention relates to a method for stabilization of pharmaceutical formulation of proteins. In particular, the present invention relates to compositions and methods for stabilizing proteins via addition of methanesulphonic and/or meglumine and example, free from particles and/or microbubbles.
摘要翻译：本发明涉及稳定蛋白质药物制剂的方法。特别地，本发明涉及通过加入甲磺酸和/或葡甲胺来稳定蛋白质的组合物和方法，例如，没有颗粒和/或微泡。

3. 发明申请

WO2007063335A2 AMPHOTERICIN B SALT 审中-公开
标题翻译： AMPHOTERICIN B盐
公开(公告)号：WO2007063335A2
公开(公告)日：2007-06-07
申请号：PCT/GB2006/004514
申请日：2006-12-04
申请人： DRUG DISCOVERY LABORATORY AS , COCKBAIN, Julian , KLAVENESS, Jo
发明人： KLAVENESS, Jo
CPC分类号： A61K9/0019 , A61K31/13 , A61K31/133 , C07H17/08 , Y02A50/409
摘要： The invention provides a salt of amphotericin B and meglumine in which the molar ratio of amphotericin B to meglumine is about 1:1.
摘要翻译：本发明提供两性霉素B和葡甲胺的盐，其中两性霉素B与葡甲胺的摩尔比为约1:1。

4. 发明申请

WO2003082281A1 OBIDOXIME DIMESYLATE 审中-公开
公开(公告)号：WO2003082281A1
公开(公告)日：2003-10-09
申请号：PCT/GB2003/001329
申请日：2003-03-27
申请人： DRUG DISCOVERY LABORATORY AS , COCKBAIN, Julian , KLAVENESS, Jo
发明人： KLAVENESS, Jo
IPC分类号： A61K31/4425
CPC分类号： A61K31/55 , A61K31/4425 , A61K31/46 , A61K2300/00
摘要： The invention provides a pharmaceutical composition comprising a sterile aqueous solution of obidoxime dimesylate.
摘要翻译：本发明提供一种包含无水二肟酸二水溶液的药物组合物。

5. 发明申请

WO2016124966A1 INCLUSION COMPLEX BETWEEN CYCLODEXTRIN AND NON-IONIC SURFACTANTS 审中-公开
标题翻译：包含环糊精与非离子表面活性剂之间的复合物
公开(公告)号：WO2016124966A1
公开(公告)日：2016-08-11
申请号：PCT/IB2015/002553
申请日：2015-12-23
申请人： DRUG DISCOVERY LABORATORY AS
发明人： KLAVENESS, Aase, Jorun , KLAVENESS, Jo
IPC分类号： A61K9/00 , A61K47/34 , A61K47/40 , A61K47/48
CPC分类号： A61K9/0019 , A61K47/34 , A61K47/40 , A61K47/6951
摘要： The present invention relates to inclusion complexes between cyclodextrin and non-ionic surfactants, especially such inclusion complexes in the form of dry tabletable powder. Further, the present invention relates to use of such dry powder in oral dose units of drugs. The powders and tablets are new oral drug delivery systems, optionally solid self-emulsifying systems, with high stability and improved bioavailability compared to conventional tablets.
摘要翻译：本发明涉及环糊精与非离子表面活性剂之间的包合络合物，特别是可干燥可压片粉末形式的这种包合配合物。此外，本发明涉及这种干粉在口服药物单位中的用途。粉末和片剂是新的口服药物递送系统，任选的固体自乳化系统，与常规片剂相比具有高稳定性和改善的生物利用度。

6. 发明申请

US20180256717A1 PROTEIN COMPOSITIONS AND USE THEREOF 审中-公开
公开(公告)号：US20180256717A1
公开(公告)日：2018-09-13
申请号：US15538697
申请日：2015-12-23
申请人： Drug Discovery Laboratory AS
发明人： Jo KLAVENESS , Aase Jorun KLAVENESS
IPC分类号： A61K39/395 , A61K47/20 , A61K47/26 , A61K9/00 , A61K9/19
CPC分类号： A61K39/39591 , A61K9/0019 , A61K9/19 , A61K47/12 , A61K47/20 , A61K47/26
摘要： The present invention relates to a method for stabilization of pharmaceutical formulation of proteins. In particular, the present invention relates to compositions and methods for stabilizing proteins via addition of methanesulphonic and/or meglumine and example, free from particles and/or microbubbles.

7. 发明专利

AU2002343086C1 Double esters 未知
公开(公告)号：AU2002343086C1
公开(公告)日：2008-06-26
申请号：AU2002343086
申请日：2002-11-22
申请人： DRUG DISCOVERY LABORATORY AS
发明人： KLAVENESS JO
IPC分类号： A61P17/00 , A61K31/225 , A61K31/23 , A61K31/235 , A61K31/265 , A61P17/02 , A61P17/16 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , C07C67/10 , C07C69/34 , C07C69/44 , C07C69/46 , C07C69/48 , C07C69/50 , C07C69/52
摘要： The invention provides acyloxymethyl esters of C6-14 alkane-dicarboxylic acids, or physiologically tolerable salts or esters thereof, for use in medicine as therapeutic or prophylactic agents.

8. 发明公开

EP3236942A1 PROTEIN COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：蛋白质组合物及其用途
公开(公告)号：EP3236942A1
公开(公告)日：2017-11-01
申请号：EP15832693.4
申请日：2015-12-23
申请人： Drug Discovery Laboratory AS
发明人： KLAVENESS, Aase, Jorun , KLAVENESS, Jo
IPC分类号： A61K9/00 , A61K38/17 , A61K39/395 , A61K47/12 , A61K9/19 , A61K47/26
CPC分类号： A61K9/19 , A61K9/0019 , A61K39/39591 , A61K47/12 , A61K47/26
摘要： The present invention relates to a method for stabilization of pharmaceutical formulation of proteins. In particular, the present invention relates to compositions and methods for stabilizing proteins via addition of methanesulphonic and/or meglumine and example, free from particles and/or microbubbles.
摘要翻译：本发明涉及稳定蛋白质药物制剂的方法。具体而言，本发明涉及通过添加甲磺酸和/或葡甲胺和实例（不含颗粒和/或微泡）来稳定蛋白质的组合物和方法。

9. 发明授权

EP1448508B1 DOUBLE ESTERS 有权
标题翻译：双酯
公开(公告)号：EP1448508B1
公开(公告)日：2009-09-23
申请号：EP02779748.9
申请日：2002-11-22
申请人： Drug Discovery Laboratory AS
发明人： Klaveness, Jo, Drug Discovery Laboratory AS
IPC分类号： C07C69/50 , C07C69/48 , C07C69/46 , C07C69/44 , C07C69/34 , A61K31/225 , A61K31/23
CPC分类号： A61K31/225 , A61K31/23 , C07C69/34 , C07C69/48 , C07C69/96
摘要： The invention provides acyloxymethyl esters of C6-14 alkane-dicarboxylic acids, or physiologically tolerable salts or esters thereof, for use in medicine as therapeutic or prophylactic agents.

10. 发明公开

EP1960412A2 AMPHOTERICIN B SALT 审中-公开
标题翻译：两性霉素B SALT
公开(公告)号：EP1960412A2
公开(公告)日：2008-08-27
申请号：EP06820400.7
申请日：2006-12-04
申请人： Drug Discovery Laboratory AS , Cockbain, Julian
发明人： KLAVENESS, Jo
IPC分类号： C07H17/08 , A61K31/133 , A61K31/13 , A61K9/00
CPC分类号： A61K9/0019 , A61K31/13 , A61K31/133 , C07H17/08 , Y02A50/409
摘要： The invention provides a salt of amphotericin B and meglumine in which the molar ratio of amphotericin B to meglumine is about 1:1.

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