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11. 发明申请

WO2005025552A2 PROTEIN BINDING COMPOUNDS 审中-公开
标题翻译：蛋白结合化合物
公开(公告)号：WO2005025552A2
公开(公告)日：2005-03-24
申请号：PCT/GB2004/003939
申请日：2004-09-15
申请人： PHOTOCURE ASA , COCKBAIN, Julian , KLAVENESS, Jo , BRUDELI, Bjarne
发明人： KLAVENESS, Jo , BRUDELI, Bjarne
IPC分类号： A61K31/00
CPC分类号： A61K31/52 , A61K31/4164 , A61K31/513 , A61K31/7068 , A61K31/708 , A61K47/542 , A61K47/543
摘要： The present invention provides a prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a blood protein binding moiety.
摘要翻译：本发明提供了包含通过代谢可切割键与血液蛋白结合部分偶联的治疗有效部分的前药化合物。

12. 发明申请

WO2014020164A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2014020164A1
公开(公告)日：2014-02-06
申请号：PCT/EP2013/066317
申请日：2013-08-02
申请人： PHOTOCURE ASA
发明人： BRÆNDEN, Jon Erik , CHARNOCK, Colin Barry , GODAL, Aslak , KLAVENESS, Jo , NILSEN, Nils Olav
IPC分类号： C07C229/22
CPC分类号： C07C229/24 , A61K41/0061 , C07C229/22
摘要： The invention relates to new derivatives of 5-aminolevulinic acid (5-ALA) and their use as photosensitizing agents. In particular, it relates to compounds of general formula I and their pharmaceutically acceptable salts, to methods for preparing such compounds and their medical and cosmetic use, for example in methods of photodynamic therapy and diagnosis: wherein R 1 represents a hydrogen atom or an optionally substituted alkyl or cycloalkyl group; R 2 , each of which may be the same or different, represents a hydrogen atom or an optionally substituted alkyl group; and X is a linking group.
摘要翻译：本发明涉及5-氨基乙酰丙酸（5-ALA）的新衍生物及其作为光敏剂的用途。特别地，本发明涉及通式I化合物及其药学上可接受的盐，制备这些化合物的方法及其医疗和化妆品用途，例如光动力学治疗和诊断方法：其中R1代表氢原子或任选取代的烷基或环烷基; R2各自可以相同或不同，表示氢原子或任选取代的烷基; X是连接基团。

13. 发明申请

WO2011018635A2 PHOTOSENSITIZING COMPOSITIONS 审中-公开
标题翻译：光敏组合物
公开(公告)号：WO2011018635A2
公开(公告)日：2011-02-17
申请号：PCT/GB2010/001547
申请日：2010-08-16
申请人： PCI BIOTECH AS , KLAVENESS, Jo , HOGSET, Anders , GOLDING, Louise
发明人： KLAVENESS, Jo , HOGSET, Anders
IPC分类号： A61K41/00
CPC分类号： A61K41/0071
摘要： The invention relates to pharmaceutically acceptable salts of amphiphilic photosensitizing agents which have a water solubility of at least 0.5 mg/ml and to their use in methods of photochemical internalization. Such salts may be formed from a pharmaceutically acceptable base, for example an organic amine such as an amino alcohol, or from a pharmaceutically acceptable acid, for example a sulphonic acid or a sulphonic acid derivative. Due to their increased water solubility, such salts are particularly suitable for use in the preparation of parenteral pharmaceutical preparations, e.g. for use as solutions for injection or infusion.
摘要翻译：本发明涉及水溶性为至少0.5mg / ml的两亲性光敏剂的药学上可接受的盐及其在光化学内化方法中的用途。这样的盐可以由药学上可接受的碱形成，例如有机胺如氨基醇，或者来自药学上可接受的酸，例如磺酸或磺酸衍生物。由于它们水溶性增加，这些盐特别适用于制备胃肠外药物制剂，例如，用作注射或输液的溶液。

14. 发明申请

WO2010112865A1 5-HT RECEPTOR MODULATING COMPOUNDS 审中-公开
标题翻译： 5-HT受体调节化合物
公开(公告)号：WO2010112865A1
公开(公告)日：2010-10-07
申请号：PCT/GB2010/000656
申请日：2010-04-01
申请人： SERODUS AS , KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav , MOLTZAU, Lise Román , GULBRANDSEN, Trygve , GOLDING, Louise
发明人： KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav , MOLTZAU, Lise Román , GULBRANDSEN, Trygve
IPC分类号： C07D211/34 , C07D498/04 , A61K31/5365 , A61K31/445 , A61P1/00 , A61P9/00
CPC分类号： C07D498/04 , C07D211/34
摘要： The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT - L - A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety. Examples of particular preterred HT groups are: (a) (b). Examples of particular preferred L groups comprise formula ( Vl ) and (VII) moieties: Examples of acid moieties are: -C(O)OR I. -OP(O)(OR2)2, -P(O)(OR2)2, -SO2OR2, -S03H, -0S03H, -P(O)(OH )2.
摘要翻译：本发明涉及具有5-羟色胺受体调节活性的化合物，特别是具有通过刚性连接基保持远离5-HT药效团的酸性部分的化合物，含有这些化合物的组合物和使用它们的治疗方法。这样的化合物对5-HT受体的亲和力增加并且hERG效应降低。本发明的某些化合物还表现出血管紧张素II受体调节活性。要求的是式（I）的化合物：HT-L-A。HT是含有碱性氮原子的5-HT受体调节部分; A是酸性部分; L是连接体部分。特定的早产HT组的实例是：（a）（b）。特别优选的L基团的实例包括式（VI）和（VII）部分：酸部分的实例是：-C（O）OR I -OP（O）（OR 2）2，-P（O）（OR 2）2 ，-SO 2 OR 2，-SO 3 H，-OSO 3 H，-P（O）（OH）2。

15. 发明申请

WO2009136179A1 TOPICAL COMPOSITIONS 审中-公开
标题翻译：主题组成
公开(公告)号：WO2009136179A1
公开(公告)日：2009-11-12
申请号：PCT/GB2009/001187
申请日：2009-05-11
申请人： OMEGATRI AS , KLAVENESS, Jo , RONGVED, Pal , CAMPBELL, Neil
发明人： KLAVENESS, Jo , RONGVED, Pal
IPC分类号： A61K9/06 , A61K9/14 , A61P17/00
CPC分类号： A61K9/0014 , A61K8/0208 , A61K8/738 , A61K8/925 , A61K47/6951 , A61Q5/02 , A61Q11/00 , A61Q19/00 , A61Q19/10 , B82Y5/00
摘要： A topical composition e.g. pharmaceutical or cosmetic composition comprising at least one cyclodextrin complex of a marine unsaturated fatty acid or derivative thereof wherein the weight ratio of cyclodextrin to marine fatty acid or derivative thereof is between 1:10 10:1.
摘要翻译：局部组合物例如药物或化妆品组合物，其包含至少一种海洋不饱和脂肪酸或其衍生物的环糊精复合物，其中环糊精与海洋脂肪酸或其衍生物的重量比为1:10 10:1。

16. 发明申请

WO2008041003A2 TREATMENT OF INSULIN RESISTANCE AND DISORDERS ASSOCIATED THEREWITH 审中-公开
标题翻译：治疗与其相关的胰岛素抵抗和疾病
公开(公告)号：WO2008041003A2
公开(公告)日：2008-04-10
申请号：PCT/GB2007/003799
申请日：2007-10-08
申请人： UNIVERSITETET I OSLO , DZIEGLEWSKA, Hanna, Eva , KASE, Eili, Tranheim , RUSTAN, Arild, Chr. , THORESEN, Gunn, Hege , NEBB, Hilde, Irene , RONGVED, Pål , KLAVENESS, Jo , BRUDELI, Bjarne
发明人： KASE, Eili, Tranheim , RUSTAN, Arild, Chr. , THORESEN, Gunn, Hege , NEBB, Hilde, Irene , RONGVED, Pål , KLAVENESS, Jo , BRUDELI, Bjarne
IPC分类号： A61K31/575 , A61K45/06 , C07J9/00 , A61P3/10
CPC分类号： A61K31/575 , A61K45/06 , C07J9/00 , A61K2300/00
摘要： The present invention provides the use of an LXR antagonist, or a physiologically- acceptable pro-drug therefor, in the manufacture of a medicament for combating insulin resistance or a disorder associated therewith. Further provided is a compound being an ester or carbamate of a hydroxycholesterol, a pharmaceutical composition of such a compound or its use in therapy.
摘要翻译：本发明提供了LXR拮抗剂或其生理上可接受的前药用于制备用于对抗胰岛素抵抗或与其相关的病症的药物的用途。还提供了一种化合物，其是羟基胆固醇的酯或氨基甲酸酯，这种化合物的药物组合物或其在治疗中的用途。

17. 发明申请

WO2005061483A2 MODULATORS OF PERIPHERAL 5-HT RECEPTORS 审中-公开
标题翻译：外周5-HT受体的调节剂
公开(公告)号：WO2005061483A2
公开(公告)日：2005-07-07
申请号：PCT/NO2004/000399
申请日：2004-12-23
申请人： BIO-MEDISINSK INNOVASJON AS , KLAVENESS, Jo , LEVY, Finn, Olav , BRUDELI, Bjarne
发明人： KLAVENESS, Jo , LEVY, Finn, Olav , BRUDELI, Bjarne
IPC分类号： C07D401/00
CPC分类号： C07D401/12 , A61K31/343 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/428 , A61K31/445 , C07D209/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D405/12
摘要： Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.
摘要翻译：新型的5-HT 4受体调节剂已被开发出来，它们对外周受体而不是中枢神经系统的那些具有选择性。论文包括已知调制器的新颖衍生物以及完全新颖的实体。令人惊讶的是，尽管在任选链末端存在酸性部分，已知调节剂的衍生化合物仍维持对5-HT 4受体的高结合亲和力。全新的实体也表现出对5-HT 4受体的良好结合亲和力。本发明的所有化合物都具有包含碱性氮部分和酸性部分的共同基序。本发明化合物至少部分归因于它们在生理pH下的高电离电位，对于外周5HT4受体选择性优于CNS的独特性质，具有良好的结合亲和性，并且选择性地选择性拮抗其他血清素受体上的5HT4受体。

18. 发明申请

WO2005058371A1 OPTICAL IMAGING CONTRAST AGENTS 审中-公开
标题翻译：光学成像对比剂
公开(公告)号：WO2005058371A1
公开(公告)日：2005-06-30
申请号：PCT/NO2004/000393
申请日：2004-12-17
申请人： AMERSHAM HEALTH AS , KLAVENESS, Jo , JOHANNESEN, Edvin , TOLLESHAUG, Helge
发明人： KLAVENESS, Jo , JOHANNESEN, Edvin , TOLLESHAUG, Helge
IPC分类号： A61K49/00
CPC分类号： A61K49/0032 , A61K49/0043 , A61K49/0052 , A61K49/0056
摘要： The invention provides contrast agents for optical imaging of oesophageal cancer and Barrett's oesophagus in patients. The contrast agents may be used in diagnosis of oesophageal cancer and Barrett's oesophagus, for follow up of progress in disease development, for follow up of treatment of oesophageal cancer and Barrett's oesophagus and for surgical guidance. Further, the invention provides methods for optical imaging of oesophageal cancer and Barrett's oesophagus in patients.
摘要翻译：本发明提供了用于患者食管癌和Barrett食管的光学成像的造影剂。造影剂可用于食管癌和巴雷特食管的诊断，用于跟踪疾病发展进展，跟进食管癌和巴雷特食管的治疗以及手术指导。此外，本发明提供了食管癌和Barrett食管的光学成像方法。

19. 发明申请

WO2004073750A1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 审中-公开
标题翻译：改进或与对比剂相关
公开(公告)号：WO2004073750A1
公开(公告)日：2004-09-02
申请号：PCT/GB1996/001361
申请日：1996-06-07
申请人： DUGSTAD, Harald , KLAVENESS, Jo , RONGVED, Pal , SKURTVEIT, Roald , BRÆNDEN, Jorun
发明人： DUGSTAD, Harald , KLAVENESS, Jo , RONGVED, Pal , SKURTVEIT, Roald , BRÆNDEN, Jorun
IPC分类号： A61K49/00
CPC分类号： A61K49/223 , A61K49/227 , Y10T428/2982
摘要： Microbubble dispersions stabilised by phospholipids predominantly comprising molecules which individually have an overall net charge exhibit advantageous stability, rendering them useful both as efficacious contrast agent per se and as intermediates in the preparation of contrast agents wherein the phospholipids are cross-linked or polymerised. An improved process for preparing microbubble-containing contrast agents is also disclosed, this comprising lyophilising an aqueous dispersion of gas microbubbles stabilised by one or more membrane-forming lipids to yield a dried product which may be reconstituted in an injectable carrier liquid to generate a microbubble-containing contrast agent.
摘要翻译：由主要包含单独具有总净电荷的分子的磷脂稳定的微泡分散体显示出有利的稳定性，使得它们作为有效的造影剂本身以及作为制备其中磷脂交联或聚合的造影剂的中间体是有用的。还公开了一种用于制备含微泡的造影剂的改进方法，其包括将由一种或多种形成膜的脂质稳定的气体微泡的水性分散体冻干以产生可在可注射载体液体中重构以产生微泡的干燥产物含有造影剂。

20. 发明申请

WO2004069220A1 PEROXIDE COMPOSITIONS 审中-公开
标题翻译：过氧化物组合物
公开(公告)号：WO2004069220A1
公开(公告)日：2004-08-19
申请号：PCT/GB2004/000481
申请日：2004-02-06
申请人： DEHLI-CLEVE COLLECTION AS , COCKBAIN, Julian , KLAVENESS, Jo , CLEVE, Thomas , FINSTAD, Kenneth , BRUDELI, Bjame
发明人： KLAVENESS, Jo , CLEVE, Thomas , FINSTAD, Kenneth , BRUDELI, Bjame
IPC分类号： A61K7/48
CPC分类号： A61Q19/02 , A61K8/22
摘要： The invention provides a kit comprising: a sealed container containing a ready-to-use skin bleaching composition comprising an emulsion containing 2 to 6 % wt of a peroxide bleaching agent selected from the group consisting of hydrogen peroxide, organic peracids and salts thereof, hydrogen peroxide adducts, and metal peroxides, percarbonates and perborates; and instructions for the use of said composition to bleach chemically tanned skin.
摘要翻译：本发明提供了一种试剂盒，其包括：含有即用皮肤漂白组合物的密封容器，其包含含有2-6重量％的过氧化物漂白剂的乳液，所述过氧化物漂白剂选自过氧化氢，有机过酸及其盐，氢过氧化物加合物和金属过氧化物，过碳酸盐和过硼酸盐; 以及使用所述组合物漂白化学鞣制皮肤的说明书。

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