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1. 发明申请

WO2007007072A1 5-HTX MODULATORS 审中-公开
标题翻译： 5-HTX调制器
公开(公告)号：WO2007007072A1
公开(公告)日：2007-01-18
申请号：PCT/GB2006/002542
申请日：2006-07-07
申请人： BIO-MEDISINSK INNOVASJON AS , COCKBAIN, Julian , KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav
发明人： KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav
IPC分类号： C07D401/06 , C07D401/04 , C07D401/12 , C07D211/58 , C07D211/22 , C07D498/04 , C07D405/12 , C07D405/14 , A61K31/517 , A61K31/4468 , A61K31/445 , A61K31/5365 , A61K31/501 , A61P25/00
CPC分类号： C07D211/62 , C07D207/14 , C07D209/42 , C07D209/80 , C07D211/22 , C07D211/26 , C07D211/58 , C07D211/70 , C07D295/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D471/04
摘要： This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT 2 or 5-HT 7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.
摘要翻译：本发明涉及在中枢神经系统内部或外部结合血清素受体的化合物，特别是结合5-HT 2或5-HT 7受体的化合物，其制备和使用，含有它们的组合物和使用它们的治疗方法。

2. 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。

3. 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。

4. 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。

5. 发明公开

EP1902044A1 5-HTX MODULATORS 审中-公开
标题翻译： 5- HTX调制器
公开(公告)号：EP1902044A1
公开(公告)日：2008-03-26
申请号：EP06755752.0
申请日：2006-07-07
申请人： Bio Medisinsk Innovasjon AS , Cockbain, Julian
发明人： KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn Olav
IPC分类号： C07D401/06 , C07D401/04 , C07D401/12 , C07D211/58 , C07D211/22 , C07D498/04 , C07D405/12 , C07D405/14 , A61K31/517 , A61K31/4468 , A61K31/445 , A61K31/5365 , A61K31/501 , A61P25/00
CPC分类号： C07D211/62 , C07D207/14 , C07D209/42 , C07D209/80 , C07D211/22 , C07D211/26 , C07D211/58 , C07D211/70 , C07D295/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D471/04
摘要： This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.

6. 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。

7. 发明申请

WO2003028742A1 STRONTIUM COMPOUND FOR TREATMENT OF SUB-DERMAL SOFT TISSUE PAIN 审中-公开
标题翻译：用于治疗次级软组织疼痛的锶化合物
公开(公告)号：WO2003028742A1
公开(公告)日：2003-04-10
申请号：PCT/GB2002/004418
申请日：2002-09-27
申请人： SANTOSOLVE AS , COCKBAIN, Julian , JELLUM, Egil , FAGERLUND, Bjørn, Jarl , KJØLBERG, Clas, Magne , KLAVENESS, Jo
发明人： JELLUM, Egil , FAGERLUND, Bjørn, Jarl , KJØLBERG, Clas, Magne , KLAVENESS, Jo
IPC分类号： A61K33/24
CPC分类号： A61K33/14 , A61K31/192 , A61K31/194 , A61K31/196 , A61K31/198 , A61K31/20 , A61K31/28 , A61K31/375 , A61K31/60 , A61K33/24 , Y10S514/936 , Y10S514/946 , Y10S514/947
摘要： The invention provides a method of treatment of a human or non-human subject to combat sub-dermal soft tissue pain therein, said method comprising administering to a said subject in need thereof an effective amount of a physiologically tolerable strontium compound.
摘要翻译：本发明提供一种治疗人或非人类受试者以防止其中的皮下软组织疼痛的方法，所述方法包括向有需要的所述受试者施用有效量的生理上可耐受的锶化合物。

8. 发明申请

WO2008035101A3 DISINFECTANT EMULSIONS CONTAINING AN ANTIMICROBIAL COMPOUND IN EACH PHASE 审中-公开
公开(公告)号：WO2008035101A3
公开(公告)日：2008-03-27
申请号：PCT/GB2007/003606
申请日：2007-09-21
申请人： MAINSANI AS , COCKBAIN, Julian , KILAAS, Lars , AASEN, Inga , DYRLI, Anne , JOHNSEN, Heidi , KLAVENESS, Jo , MEHREN, Petter
发明人： COCKBAIN, Julian , KILAAS, Lars , AASEN, Inga , DYRLI, Anne , JOHNSEN, Heidi , KLAVENESS, Jo , MEHREN, Petter
IPC分类号： A01N25/04 , A01N43/40 , A01N33/12 , A01N31/08 , A01N49/00 , A01N47/44 , A01N31/16 , A01N31/02 , A01N31/12 , A01P1/00
摘要： The invention provides a disinfectant emulsion composition having a continuous phase having dissolved therein a first antimicrobial agent and a discontinuous phase having dissolved therein a second antimicrobial agent.

9. 发明申请

WO2007104981A1 USE OF POLYAMINES IN THE TREATMENT OF PSORIASIS 审中-公开
标题翻译：聚氨酯在PSORIASIS治疗中的应用
公开(公告)号：WO2007104981A1
公开(公告)日：2007-09-20
申请号：PCT/GB2007/000894
申请日：2007-03-14
申请人： BIOFORSKNING PHARMA AS , COCKBAIN, Julian , KLAVENESS, Jo , KVALHEIM, Geir, Havard
发明人： KLAVENESS, Jo , KVALHEIM, Geir, Havard
IPC分类号： A61K31/132 , A61P17/06
CPC分类号： A61K31/132
摘要： The present invention provides unbranched aliphatic polyamines for use in therapy, particularly for use in the treatment of psoriasis and compositions containing polyamines.
摘要翻译：本发明提供了用于治疗的非支链脂族多胺，特别是用于治疗银屑病和含有多胺的组合物。

10. 发明申请

WO2005123755A2 PURINE NUCLEOTIDE DERIVATIVES 审中-公开
标题翻译：嘌呤核苷衍生物
公开(公告)号：WO2005123755A2
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002418
申请日：2005-06-20
申请人： LAURAS AS , COCKBAIN, Julian , UNDHEIM, Kjell , TASKÉN, Kjetil , KLAVENESS, Jo , LANGLI, Geir , BJØRNSTAD, Vidar
发明人： UNDHEIM, Kjell , TASKÉN, Kjetil , KLAVENESS, Jo , LANGLI, Geir , BJØRNSTAD, Vidar
IPC分类号： C07H
CPC分类号： C07H19/213 , Y10T436/143333
摘要： This invention provides novel 8-carbyl substituted cAMPS and a novel procedures for the preparation of 8-Br-cAMP, a key starting material.
摘要翻译：本发明提供新的8-羰基取代的cAMPS和用于制备8-Br-cAMP（一种关键起始物质）的新方法。

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