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31. 发明申请

US20120253264A1 PHOTOCHEMICAL INTERNALIZATION METHOD 审中-公开
标题翻译：光化学内在化方法
公开(公告)号：US20120253264A1
公开(公告)日：2012-10-04
申请号：US13390360
申请日：2010-08-16
申请人： Jo Klaveness , Anders Hogset
发明人： Jo Klaveness , Anders Hogset
IPC分类号： A61M37/00
CPC分类号： A61K9/0014 , A61K9/0019 , A61K9/0031 , A61K9/0034 , A61K9/006 , A61K9/107 , A61K9/2054 , A61K9/4858 , A61K41/0071
摘要： The invention relates to methods of introducing drugs into cells which are located in body cavities. In particular, it provides a photosensitizing agent for use in a method of introducing a drug molecule into the cytosol of a cell located within a body cavity, said method comprising the step of contacting said cell with said photosensitizing agent and said drug molecule, and irradiating the cell with light of a wavelength effective to activate the photosensitizing agent. Such methods are particularly suitable for use in the delivery of cytotoxic drugs in the treatment of cancer, especially bladder cancer, ovarian cancer, cervical cancer, lung cancer, brain cancer, colorectal cancer and cancers of the oral and nasal cavity.
摘要翻译：本发明涉及将药物引入位于体腔内的细胞中的方法。特别地，本发明提供一种用于将药物分子引入体腔内的细胞质的细胞溶质的方法中的光敏剂，所述方法包括使所述细胞与所述光敏剂和所述药物分子接触的步骤，以及照射具有有效激活光敏剂的波长的光的电池。这些方法特别适用于递送细胞毒性药物治疗癌症，特别是膀胱癌，卵巢癌，子宫颈癌，肺癌，脑癌，结肠直肠癌和口腔和鼻腔癌。

32. 发明申请

US20120245094A1 COMPOUNDS, COMPOSITIONS AND USE 有权
标题翻译：化合物，组合物和用途
公开(公告)号：US20120245094A1
公开(公告)日：2012-09-27
申请号：US13141465
申请日：2008-12-22
申请人： Oyvind Jacobsen , Jo Klaveness , Pal Rongved , Mahmood Amiry-Moghaddam , Ole Petter Ottersen
发明人： Oyvind Jacobsen , Jo Klaveness , Pal Rongved , Mahmood Amiry-Moghaddam , Ole Petter Ottersen
IPC分类号： C07K7/06 , A61P25/00 , A61K38/08
CPC分类号： A61K38/00 , A61K38/16 , C07K14/00 , C07K14/705
摘要： A peptide comprising a unit of formula (I) and having a molecular weight of less than 2000 wherein each X is independently an organic group, e.g. a C1-6 alkyl or C1-6 alkenyl group, preferably —CH2—CH═CH2, or the two X groups taken together can form a covalent or non-covalent link between the two O groups, preferably a C1-10 saturated or unsaturated carbon chain optionally interrupted by one or more heteroatoms selected from O, S, N, P, or Si, especially a C3-10 carbon chain or one X represents an azido group and the other an C2-6-alkynyl group; both Z's are the same and are O or S; each Y is independently C, CH, CH2, N or NH; R1 is H or C1-6 alkyl; R2 is H or C1-6 alkyl; R5 is a C1-6 alkyl group, preferably isopropyl; or a salt, ester or prodrug thereof.
摘要翻译：一种包含式（I）单元并且分子量小于2000的肽，其中每个X独立地是有机基团，例如， C 1-6烷基或C 1-6烯基，优选-CH 2 -CH 2 CH 2或两个X基团可以在两个O基之间形成共价或非共价键，优选为C1-10饱和或不饱和的碳链，任选地被一个或多个选自O，S，N，P或Si的杂原子中断，特别是C3-10碳链或一个X代表叠氮基，另一个是C 2-6炔基; 两个Z都是相同的，是O或S; 每个Y独立地为C，CH，CH 2，N或NH; R1是H或C1-6烷基; R2是H或C1-6烷基; R5是C1-6烷基，优选是异丙基; 或其盐，酯或前药。

33. 发明授权

US08153609B2 Purine nucleotide derivatives 有权
标题翻译：嘌呤核苷酸衍生物
公开(公告)号：US08153609B2
公开(公告)日：2012-04-10
申请号：US11629908
申请日：2005-06-20
申请人： Kjell Undheim , Kjetil Taskén , Jo Klaveness , Geir Langli , Vidar Bjørnstad
发明人： Kjell Undheim , Kjetil Taskén , Jo Klaveness , Geir Langli , Vidar Bjørnstad
IPC分类号： A01N43/04 , A61K31/70 , C07H19/20 , G01N33/00
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。

34. 发明申请

US20110125012A1 ACID ADDITION SALTS OF 5-AMINOLEVULINIC ACID OR ITS DERIVATIVES 有权
标题翻译： 5-氨基酸或其衍生物的酸添加量
公开(公告)号：US20110125012A1
公开(公告)日：2011-05-26
申请号：US12916326
申请日：2010-10-29
申请人： Jon Erik BRAENDEN , Aslak Godal , Nils Olav Nilsen , Jo Klaveness
发明人： Jon Erik BRAENDEN , Aslak Godal , Nils Olav Nilsen , Jo Klaveness
IPC分类号： A61B6/00 , C12Q1/02 , G01N21/64 , A61M37/00
CPC分类号： A61K41/0061 , C07C229/22
摘要： The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.
摘要翻译：本发明提供5-氨基乙酰丙酸（5-ALA）或5-ALA衍生物（例如5-ALA酯）与酸的加成盐，所述酸的pKa为约5或更小，优选约3或较少，条件是酸不是盐酸。特别优选的盐是衍生自选自磺酸及其衍生物，氢溴酸，硫酸，硝酸和磷酸的酸的酸。根据本发明的盐特别适用于诊断和光化学治疗身体的外表面或内表面的病症或异常的光敏剂。

35. 发明申请

US20110020441A1 USE OF 5-AMINOLEVULINIC ACID AND DERIVATIVES IN A SOLID FORM FOR PHOTODYNAMIC TREATMENT AND DIAGNOSIS 审中-公开
标题翻译：用于光化学治疗和诊断的固体形式中的5-氨基酸和衍生物的使用
公开(公告)号：US20110020441A1
公开(公告)日：2011-01-27
申请号：US12808177
申请日：2008-12-12
申请人： Jo Klaveness , Gry Stensrud , Aslak Godal , Jon Erik Braenden , Bjorn Klem
发明人： Jo Klaveness , Gry Stensrud , Aslak Godal , Jon Erik Braenden , Bjorn Klem
IPC分类号： A61K9/48 , A61K31/197 , A61K31/221 , A61K31/24 , A61K31/44 , A61P35/00
CPC分类号： A61K9/02 , A61K9/0031 , A61K9/0034 , A61K9/0075 , A61K9/14 , A61K9/1635 , A61K9/1652 , A61K9/20 , A61K9/2013 , A61K9/205 , A61K9/2054 , A61K9/2077 , A61K9/28 , A61K9/284 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/48 , A61K9/4858 , A61K9/4891 , A61K9/5042 , A61K9/5073 , A61K31/197 , A61K31/221 , A61K41/0057 , A61K41/0061 , A61K49/00 , A61K49/0021
摘要： The present invention relates to the use of a photosensitiser which is 5-ALA or a precursor or derivative thereof (e.g. an ALA ester), in the manufacture of a pharmaceutical product for use in the photodynamic treatment or diagnosis of cancer, an infection associated with cancer, or in the treatment or diagnosis of a non-cancerous condition, wherein said pharmaceutical product is in the form of a solid. The invention also relates to solid pharmaceutical products for use in such methods, e.g. suppositories, pessaries, tablets, pellets and capsules which comprise 5-ALA or a precursor or derivative thereof (e.g. an ALA ester) and at least one pharmaceutically acceptable carrier or excipient. Such products are particularly suitable for use in the photodynamic treatment or diagnosis of cancerous or non-cancerous conditions in the lower part of the gastrointestinal system or in the female reproductive system, e.g. in the treatment or diagnosis of colorectal cancer or cervical cancer.
摘要翻译：本发明涉及使用5-ALA或其前体或衍生物（例如ALA酯）的光敏剂在制造用于癌症的光动力学治疗或诊断的药物产品中，与癌症或治疗或诊断非癌症状况，其中所述药物产品为固体形式。本发明还涉及用于这些方法的固体药物产品，例如。栓剂，阴道栓剂，片剂，丸剂和胶囊，其包含5-ALA或其前体或衍生物（例如ALA酯）和至少一种药学上可接受的载体或赋形剂。这些产品特别适用于光动力学治疗或诊断胃肠系统下部或女性生殖系统中的癌性或非癌性病症。在结直肠癌或宫颈癌的治疗或诊断中。

36. 发明申请

US20100291206A1 ORAL DOSAGE FORM 审中-公开
标题翻译：口服剂型
公开(公告)号：US20100291206A1
公开(公告)日：2010-11-18
申请号：US12602317
申请日：2008-06-02
申请人： Jo Klaveness , Bjarne Brudeli , Pal Rongved
发明人： Jo Klaveness , Bjarne Brudeli , Pal Rongved
IPC分类号： A61K33/10 , A61K31/202 , A61K31/351 , A61K31/40 , A61K31/7008 , A61K31/519 , A61K9/20 , A61P9/00 , A61P19/00
CPC分类号： C08L5/16 , A61K9/205 , A61K9/2054 , A61K31/232 , A61K31/351 , A61K31/40 , A61K31/519 , A61K31/7008 , A61K45/06 , A61K47/6951 , A61P9/00 , A61P19/00 , 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, the inventors have found that tablets containing complexes of fatty acids or derivatives thereof with cyclodextrin can be prepared by direct compression and moreover they can be prepared having a very high 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片制备，而且它们可以制备成具有非常高浓度的所需活性剂。

37. 发明申请

US20100137439A1 USE OF AMINOLEVULINIC ACID AND DERIVATIVES THEREOF 有权
标题翻译：氨基酸及其衍生物的使用
公开(公告)号：US20100137439A1
公开(公告)日：2010-06-03
申请号：US12523048
申请日：2008-01-11
申请人： Hans Christian Wulf , Aslak Godal , Jo Klaveness
发明人： Hans Christian Wulf , Aslak Godal , Jo Klaveness
IPC分类号： A61K31/195 , A61P35/00
CPC分类号： A61K41/0061 , A61K31/221 , A61N5/062
摘要： The invention provides the use of a photosensitiser which is 5-aminolevulinic acid (5-ALA) or a derivative (e.g. an ester) of 5-ALA, or a pharmaceutically acceptable salt thereof, in the manufacture of a composition for use in methods of photodynamic therapy (PDT) on an animal, wherein said PDT comprises: (a) administering to said animal a composition comprising said photosensitiser; and (b) photoactivating said photosensitiser, and wherein side-effects (e.g. pain and/or erythema) of said PDT are prevented or reduced by use of one or more of (i)-(iv): (i) said composition comprises said photosensitiser in a concentration of less than 10% wt (e.g. 0.5 to 8% wt), (ii) said composition is administered for less than 2 hours (e.g. 30 minutes to 90 minutes) prior to said photoactivation, (iii) said photoactivation is carried out with a light source having a fluence rate of less than 50 mW/cm2 (e.g. 5 to 40 mW/cm2), (iv) said photoactivation is carried out with sunlight. Preferably, side-effects of PDT are prevented or reduced by using (iii) or (iv) in combination with (i) and/or (ii).
摘要翻译：本发明提供了5-氨基乙酰丙酸（5-ALA）或5-ALA衍生物（例如酯）或其药学上可接受的盐的光敏剂在制备用于光动力疗法（PDT），其中所述PDT包括：（a）向所述动物施用包含所述光敏剂的组合物; 和（b）光活化所述光敏剂，并且其中通过使用（i） - （iv）中的一种或多种来防止或减少所述PDT的副作用（例如疼痛和/或红斑）：（i）所述组合物包含浓度小于10％wt（例如0.5至8％wt）的光敏剂，（ii）所述组合物在所述光活化前施用少于2小时（例如30分钟至90分钟），（iii）所述光活化是用光通量小于50mW / cm2（例如5〜40mW / cm2）的光源进行，（iv）所述的光活化是在太阳光下进行的。优选地，通过使用（iii）或（iv）与（i）和/或（ii）组合来防止或减少PDT的副作用。

38. 发明申请

US20070259889A1 Protein Binding Compounds 审中-公开
标题翻译：蛋白结合化合物
公开(公告)号：US20070259889A1
公开(公告)日：2007-11-08
申请号：US10571890
申请日：2004-09-15
申请人： Jo Klaveness , Bjarne Brudeli
发明人： Jo Klaveness , Bjarne Brudeli
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。

39. 发明授权

US07241460B2 Strontium compound for treatment of sub-dermal soft tissue pain 有权
标题翻译：用于治疗皮肤软组织疼痛的锶化合物
公开(公告)号：US07241460B2
公开(公告)日：2007-07-10
申请号：US10488162
申请日：2002-09-27
申请人： Egil Jellum , Bjørn Jarl Fagerlund , Clas Magne Kjølberg , Jo Klaveness
发明人： Egil Jellum , Bjørn Jarl Fagerlund , Clas Magne Kjølberg , Jo Klaveness
IPC分类号： A61K33/00 , A61K33/14 , A61K33/42 , A61K31/185 , A61K31/19 , A61P21/00 , A61P25/02 , A61P29/00
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 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受试者的方法，以对抗其中的皮下软组织疼痛，所述方法包括向有需要的受试者施用有效量的生理上可耐受的锶化合物。

40. 发明申请

US20070116646A1 Optical imaging of endometriosis 审中-公开
标题翻译：子宫内膜异位症的光学成像
公开(公告)号：US20070116646A1
公开(公告)日：2007-05-24
申请号：US10573604
申请日：2004-09-28
申请人： Jo Klaveness , Edvin Johannesen , Helge Tolleshaug
发明人： Jo Klaveness , Edvin Johannesen , Helge Tolleshaug
IPC分类号： A61K49/00 , C07K16/46
CPC分类号： A61K49/0056 , A61K49/0032 , A61K49/0043 , A61K49/0052
摘要： The invention provides contrast agents for optical imaging of endometriosis in patients. The contrast agent may be used in diagnosis of endometriosis, for follow-up of progress in disease development, and for follow-up of treatment of endometriosis. Further, the invention provides methods for optical imaging of endometriosis. The contrast agent has affinity for an abnormally expressed target associated with endometriosis. By abnormally expressed, is meant that the target is either overexpressed or downregulated. Endometriotic tissue containing a downregulated target may be identified by a low amount of bound contrast agent compared to normal tissue. In this situation, the amount of contrast agent should be less than 50% of that in normal tissue, preferably less than 10%.
摘要翻译：本发明提供了用于患者子宫内膜异位症的光学成像的造影剂。造影剂可用于诊断子宫内膜异位症，用于随访疾病发展进展，以及随访子宫内膜异位症的治疗。此外，本发明提供了用于子宫内膜异位症的光学成像的方法。造影剂对与子宫内膜异位症相关的异常表达的靶标具有亲和力。通过异常表达意味着靶标过表达或下调。与正常组织相比，含有下调靶的子宫内膜异位组织可以通过少量结合的造影剂来鉴定。在这种情况下，造影剂的量应小于正常组织的50％，优选小于10％。

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