专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2006030217A3 DRUG CONJUGATES OF LONG CHAIN FATTY ACID OR ESTER MOIETIES AS PROTEIN BINDING PRODRUGS 审中-公开
标题翻译：长链脂肪酸或酯酶作为蛋白质结合原料的药物联合
公开(公告)号：WO2006030217A3
公开(公告)日：2007-03-22
申请号：PCT/GB2005003559
申请日：2005-09-15
申请人： DRUG DISCOVERY LAB AS , COCKBAIN JULIAN , KLAVENESS JO , BRUDELI BJARNE
发明人： KLAVENESS JO , BRUDELI BJARNE
IPC分类号： A61K47/48 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00
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

WO2005025552A3 PROTEIN BINDING COMPOUNDS 审中-公开
标题翻译：蛋白质结合化合物
公开(公告)号：WO2005025552A3
公开(公告)日：2005-10-13
申请号：PCT/GB2004003939
申请日：2004-09-15
申请人： DRUG DISCOVERY LAB AS , KLAVENESS JO , BRUDELI BJARNE , COCKBAIN JULIAN
发明人： KLAVENESS JO , BRUDELI BJARNE
IPC分类号： A61K31/00 , A61K31/4164 , A61K31/513 , A61K31/52 , A61K31/7068 , A61K31/708 , A61K38/38 , A61K47/48 , A61P29/00 , A61P31/00 , A61P35/00
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：本发明提供了一种前药化合物，其包含通过代谢可裂解键与血液蛋白质结合部分偶联的治疗有效部分。

3. 发明申请

WO2004087229A3 BONE CEMENT COMPOSITIONS 审中-公开
标题翻译：骨水泥组合物
公开(公告)号：WO2004087229A3
公开(公告)日：2005-02-17
申请号：PCT/GB2004001509
申请日：2004-04-05
申请人： TA CONTRAST AB , ALMEN TORSTEN , KLAVENESS JO , BRUDELI BJARNE , COCKBAIN JULIAN
发明人： ALMEN TORSTEN , KLAVENESS JO , BRUDELI BJARNE
IPC分类号： A61L24/00 , A61L24/06 , A61L27/50 , A61L24/04
CPC分类号： A61L27/50 , A61L24/001 , A61L24/06 , A61L2430/02
摘要： The present invention provides a bone cement comprising in admixture a monomer-containing liquid portion and a particulate polymer portion, characterized in that at least one of said portions comprises a dissolved nonpolymerizable organoiodine compound.
摘要翻译：本发明提供了一种含有含单体的液体部分和粒状聚合物部分的骨水泥，其特征在于，所述部分中的至少一个包含溶解的不可聚合的有机碘化合物。

4. 发明申请

WO2008146016A3 CYCLODEXTRINS FOR ADMINISTERING FATTY ACIDS IN TABLETS 审中-公开
标题翻译：用于在片剂中施用脂肪酸的环孢菌素
公开(公告)号：WO2008146016A3
公开(公告)日：2009-07-16
申请号：PCT/GB2008001861
申请日：2008-06-02
申请人： OMEGATRI AS , CAMPBELL NEIL , KLAVENESS JO , BRUDELI BJARNE , RONGVED PAL
发明人： KLAVENESS JO , BRUDELI BJARNE , RONGVED PAL
IPC分类号： A61K47/48 , A61K9/20
CPC分类号： C08L5/16 , A61K9/205 , A61K9/2054 , A61K31/232 , A61K31/351 , A61K31/40 , A61K31/519 , A61K31/7008 , A61K45/06 , A61K47/6951 , B82Y5/00 , C08B37/0015 , C08L1/02 , A61K2300/00 , C08L2666/26
摘要： A pharmaceutical or nutraceutical tablet for oral administration comprising at least two fatty acids or derivatives thereof and cyclodextrin. Surprisingly, we have now found that fatty acids or derivatives thereof, especially fatty acid esters, preferably in the form of complexes with cyclodextrins prepared as stable solid materials, can easily be transformed into tablets with very high concentration of the fatty acid compound. The present inventors have realised that ideal dosage forms for these compounds are tablets and these are readily swallowed and are cheap to manufacture. In particular, 4he inventors have found that tablets containing complexes of fatty acids or derivatives thereof with cycJodextrin can be prepared by direct compression and moreover they can be prepared having a very Mgh concentration of the desired active agent.
摘要翻译：一种用于口服给药的药物或营养片剂，其包含至少两种脂肪酸或其衍生物和环糊精。令人惊奇的是，现在我们已经发现脂肪酸或其衍生物，特别是脂肪酸酯，优选与作为稳定固体物质制备的环糊精的复合物形式，可以容易地转化成具有非常高浓度脂肪酸化合物的片剂。本发明人已经认识到，这些化合物的理想剂型为片剂，容易吞咽，制造便宜。特别地，本发明人已经发现，含有脂肪酸或其衍生物与环糊精的复合物的片剂可以通过直接压制制备，此外它们可以制备成具有非常高浓度的所需活性剂。

5. 发明申请

WO2009081169A3 BIODEGRADABLE CONTRAST AGENTS 审中-公开
标题翻译：生物可降解造影剂
公开(公告)号：WO2009081169A3
公开(公告)日：2009-12-10
申请号：PCT/GB2008004268
申请日：2008-12-22
申请人： IOPHARMA TECHNOLOGIES AB , ALMEN TORSTEN , BRUDELI BJARNE , KJELLSON FRED , KLAVENESS JO , WANG JIAN-SHENG , KIDD SARA
发明人： ALMEN TORSTEN , BRUDELI BJARNE , KJELLSON FRED , KLAVENESS JO , WANG JIAN-SHENG
IPC分类号： A61K49/04 , A61L31/18
CPC分类号： A61K49/0438 , A61K31/03 , A61K31/75 , A61K31/765 , A61K31/785 , A61K45/06 , A61K49/0461 , A61L29/18 , A61K2300/00
摘要： The present invention provides a radio-opaque composition comprising a cleavable, preferably enzymatically-cleavable, derivative of a physiologically tolerable organoiodine compound and a non-acrylic polymer wherein said derivative is incorporated in said non-acrylic polymer.
摘要翻译：本发明提供一种不透射线组合物，其包含可生理耐受的有机碘化合物的可裂解的，优选酶促裂解的衍生物和非丙烯酸类聚合物，其中所述衍生物掺入所述非丙烯酸类聚合物中。

6. 发明申请

WO2009081169A8 BIODEGRADABLE CONTRAST AGENTS 审中-公开
标题翻译：生物可比较对比剂
公开(公告)号：WO2009081169A8
公开(公告)日：2009-10-22
申请号：PCT/GB2008004268
申请日：2008-12-22
申请人： IOPHARMA TECHNOLOGIES AB , ALMEN TORSTEN , BRUDELI BJARNE , KJELLSON FRED , KLAVENESS JO , WANG JIAN-SHENG , KIDD SARA
发明人： ALMEN TORSTEN , BRUDELI BJARNE , KJELLSON FRED , KLAVENESS JO , WANG JIAN-SHENG
IPC分类号： A61K49/04
CPC分类号： A61K49/0438 , A61K31/03 , A61K31/75 , A61K31/765 , A61K31/785 , A61K45/06 , A61K49/0461 , A61L29/18 , A61K2300/00
摘要： The present invention provides a radio-opaque composition comprising a cleavable, preferably enzymatically-cleavable, derivative of a physiologically tolerable organoiodine compound and a non-acrylic polymer wherein said derivative is incorporated in said non-acrylic polymer.
摘要翻译：本发明提供一种不透射线组合物，其包含生理上可耐受的有机碘化合物和非丙烯酸类聚合物的可裂解，优选可酶切割的衍生物，其中所述衍生物掺入所述非丙烯酸类聚合物中。

7. 发明申请

WO2008041003A3 HYDROXYCHOLESTEROLS AND ITS PRODRUGS FOR THE TREATMENT OF INSULIN RESISTANCE AND DISORERS ASOCIATED THEREWITH 审中-公开
标题翻译：羟吗啉醇及其治疗胰岛素抵抗和分泌物的原则
公开(公告)号：WO2008041003A3
公开(公告)日：2008-05-29
申请号：PCT/GB2007003799
申请日：2007-10-08
申请人： UNI I OSLO , DZIEGLEWSKA HANNA EVA , KASE EILI TRANHEIM , RUSTAN ARILD CHR , THORESEN GUNN HEGE , NEBB HILDE IRENE , RONGVED PAAL , KLAVENESS JO , BRUDELI BJARNE
发明人： KASE EILI TRANHEIM , RUSTAN ARILD CHR , THORESEN GUNN HEGE , NEBB HILDE IRENE , RONGVED PAAL , KLAVENESS JO , BRUDELI BJARNE
IPC分类号： A61K31/575 , A61K45/06 , A61P3/10 , C07J9/00
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。

8. 发明申请

WO2005061483A3 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：WO2005061483A3
公开(公告)日：2005-10-27
申请号：PCT/NO2004000399
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： A61K31/343 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/428 , A61K31/445 , C07D209/14 , C07D211/00 , C07D211/22 , C07D211/26 , C07D211/58 , C07D401/00 , C07D401/12 , C07D405/12 , C07D498/04 , A61P1/00 , A61P9/00 , A61P13/00
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：已经开发了具有对外周受体而不是中枢神经系统的选择性的5-HT 4受体的新型调节剂。论文包括已知调制剂的新型衍生物以及完全新颖的实体。令人惊奇的是，尽管已知调节剂的衍生化合物在任选链的末端存在酸性部分，但仍保持与5-HT 4受体的高结合亲和力。完全新颖的实体也表现出对5-HT4受体的良好的结合亲和力。本发明的所有化合物都具有共同的基序，其包括碱性氮部分和酸性部分。本发明的化合物至少部分地由于其在生理pH下的高电离电位具有对于周围5HT4受体的选择性优于CNS的那些的独特性质，良好的结合亲和力以及5HT4受体的选择性超过其他5-羟色胺受体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式