公开(公告)号：US08124806B2

公开(公告)日：2012-02-28

申请号：US12279100

申请日：2007-02-14

Applicant: Duncan Wynn ,  Robert James Domett Nairne ,  Oskar Axelsson ,  Mikkel Thaning ,  Nicolas Lasbistes

Inventor： Duncan Wynn ,  Robert James Domett Nairne ,  Oskar Axelsson ,  Mikkel Thaning ,  Nicolas Lasbistes

IPC: C07C233/65 ,  A61K49/00

CPC classification number: C07C237/46 ,  A61K49/0433 ,  A61K49/0438

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing amide functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract translation: 本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。 更具体地，含碘化合物是含有含有酰胺官能团的脂族中心部分的化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

公开(公告)号：US20100111859A1

公开(公告)日：2010-05-06

申请号：US12525389

申请日：2008-01-10

Applicant: Oskar Axelsson ,  Kajsa Uvdal

Inventor： Oskar Axelsson ,  Kajsa Uvdal

IPC: A61K51/00 ,  A61K49/06 ,  B05D3/00 ,  A61K49/04 ,  A61K49/00

CPC classification number: A61K49/1824 ,  A61K49/1848 ,  A61K49/186 ,  B82Y5/00

Abstract: A method for visualizing biological material, preferably by MRI, comprising the steps of: (i) bringing a population of coated nanoparticles into contact with said biological material, each of which nanoparticles comprises a) a metal oxide of a transition metal, said metal oxide preferably being paramagnetic and preferably comprising a lanthanide (+III) such as gadolinium (+III), and b) a coating covering the surface of the core particle, and (ii) recording the image; wherein the coating is hydrophilic and comprises a silane layer which is located next to the surface of the core particle and comprises one or more different silane groups which each comprises an organic group R and a silane-siloxane linkage where a) R comprises a hydrophilic organic group R′ and a hydrophobic spacer B, b) O is oxygen directly binding to a surface metal ion of the metal oxide, and c) C is carbon and is also part of B. A composition for visualization and methods for the manufacture of the nanoparticles and core particles are also disclosed. Visualization includes imaging by MR, CT, X-ray, near IR fluorescence, PET, microscopying etc with the largest advantages accomplished for in-vivo imaging.

Abstract translation: 一种用于使生物材料可视化的方法，优选通过MRI显示，其包括以下步骤：（i）使被覆纳米颗粒群与所述生物材料接触，其中每一种纳米颗粒包含a）过渡金属的金属氧化物，所述金属氧化物 优选是顺磁性的，优选包含镧系元素（+ III）如钆（+ III），和b）覆盖核心颗粒表面的涂层，和（ii）记录图像; 其中所述涂层是亲水性的并且包含位于所述核心颗粒表面旁边的硅烷层，并且包含一个或多个不同的硅烷基团，其各自包含有机基团R和硅烷 - 硅氧烷键，其中a）R包含亲水性有机物 基团R'和疏水性间隔物B，b）O是与金属氧化物的表面金属离子直接结合的氧，c）C是碳，也是B的一部分。用于可视化的组合物和用于制备 还公开了纳米颗粒和芯颗粒。 可视化包括MR，CT，X射线，近红外荧光，PET，显微镜等成像，具有体内成像最大的优点。

公开(公告)号：US20090053142A1

公开(公告)日：2009-02-26

申请号：US12279100

申请日：2007-02-14

Applicant: Duncan Wynn ,  Robert James Domett Nairne ,  Oskar Axelsson ,  Mikkel Thaning ,  Nicolas Lasbistes

Inventor： Duncan Wynn ,  Robert James Domett Nairne ,  Oskar Axelsson ,  Mikkel Thaning ,  Nicolas Lasbistes

IPC: A61K49/04 ,  C07C237/30

CPC classification number: C07C237/46 ,  A61K49/0433 ,  A61K49/0438

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing amide functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract translation: 本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。 更具体地，含碘化合物是含有含有酰胺官能团的脂族中心部分的化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

公开(公告)号：US07485753B2

公开(公告)日：2009-02-03

申请号：US11565673

申请日：2006-12-01

Applicant: Lars-Goran Wistrand ,  Mikkel Thaning ,  Oskar Axelsson ,  Sven Andersson

Inventor： Lars-Goran Wistrand ,  Mikkel Thaning ,  Oskar Axelsson ,  Sven Andersson

IPC: C07C233/58 ,  A61K49/04 ,  A61K31/16

CPC classification number: C07C237/46 ,  A61K49/0433 ,  C07C2601/02

Abstract: The present invention relates to iodine containing compounds containing a central cyclopropane scaffolding moiety allowing for the arrangement of three iodinated phenyl groups bound thereto.The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract translation: 本发明涉及含有中心环丙烷支架部分的含碘化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

公开(公告)号：US20080233052A1

公开(公告)日：2008-09-25

申请号：US11913079

申请日：2006-05-19

Applicant: Oskar Axelsson

Inventor： Oskar Axelsson

IPC: A61K49/18 ,  A61K49/04 ,  A61K49/00

CPC classification number: A61K49/0414 ,  A61K33/24 ,  A61K2300/00

Abstract: The present invention relates to particles comprising cores of tungsten or tungsten in mixture with other metallic elements wherein said cores are coated and have an average size of at least 20 nm. Further, the invention relates to pharmaceuticals containing such particles, and to the use of such pharmaceuticals specifically as contrast agents in diagnostic imaging, in particular in X-ray imaging of atherosclerotic plaque and liver tumours.

Abstract translation: 本发明涉及包含与其它金属元素混合的钨或钨的芯的颗粒，其中所述芯被涂覆并且具有至少20nm的平均尺寸。 此外，本发明涉及含有这种颗粒的药物，以及在诊断成像中特别是造影剂的这种药物的用途，特别是在动脉粥样硬化斑块和肝肿瘤的X射线成像中的用途。

公开(公告)号：US20080199402A1

公开(公告)日：2008-08-21

申请号：US11565673

申请日：2006-12-01

Applicant: Lars-Goran Wistrand ,  Mikkel Thaning ,  Oskar Axelsson ,  Sven Andersson

Inventor： Lars-Goran Wistrand ,  Mikkel Thaning ,  Oskar Axelsson ,  Sven Andersson

IPC: A61K49/04 ,  C07C237/00 ,  A61K49/00

CPC classification number: C07C237/46 ,  A61K49/0433 ,  C07C2601/02

Abstract: The present invention relates to iodine containing compounds containing a central cyclopropane scaffolding moiety allowing for the arrangement of three iodinated phenyl groups bound thereto.The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract translation: 本发明涉及含有中心环丙烷支架部分的含碘化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中的用途，特别是在X射线成像中以及含有这种化合物的造影剂的用途。

公开(公告)号：US20050152840A1

公开(公告)日：2005-07-14

申请号：US11002864

申请日：2004-12-02

Applicant: Oskar Axelsson ,  Charlotte Olofsson ,  Axel Morgenstjerne ,  Georg Hansson ,  Haukur Johannesson ,  Jan-Henrik Ardenkjaer-Larsen

Inventor： Oskar Axelsson ,  Charlotte Olofsson ,  Axel Morgenstjerne ,  Georg Hansson ,  Haukur Johannesson ,  Jan-Henrik Ardenkjaer-Larsen

IPC: A61K49/00 ,  A61K49/18 ,  C07C67/303 ,  C07C69/675 ,  G01R33/28 ,  G01R33/483

CPC classification number: A61K49/1815

Abstract: The present invention provides a process for the preparation of an MR contrast agent, said process comprising: i) obtaining a solution in a solvent of a hydrogenatable, unsaturated substrate compound and a catalyst for the hydrogenation of said substrate compound; ii) introducing said solution in droplet form into a chamber containing hydrogen gas (H2) enriched in para-hydrogen (p-1H2) and/or ortho-deuterium (o-2H2) whereby to hydrogenate said substrate to form a hydrogenated imaging agent; iii) optionally subjecting said hydrogenated imaging agent to a magnetic field having a field strength below earth's ambient field strength; iv) optionally dissolving said imaging agent in an aqueous medium; v) optionally separating said catalyst from the solution of said imaging agent in said aqueous medium; vi) optionally separating said solvent from the solution of said imaging agent in said aqueous medium; and vii) optionally freezing the solution of said imaging agent in said aqueous medium.

Abstract translation: 本发明提供了一种制备MR造影剂的方法，所述方法包括：i）获得在可氢化不饱和底物化合物的溶剂中的溶液和用于所述底物化合物氢化的催化剂; ii）将所述液滴形式的溶液引入含有富氢对二氢的氢气（H 2 S 2 H 2）的室中， ）和/或邻 - 氘（o-2 H 2 H 2），由此氢化所述底物以形成氢化显像剂; iii）任选地使所述氢化成像剂经受场强低于地球环境场强的磁场; iv）任选地将所述成像剂溶解在水性介质中; v）任选地将所述催化剂与所述显影剂的溶液在所述水性介质中分离; vi）任选地将所述溶剂与所述显影剂的溶液在所述水性介质中分离; 和vii）任选地将所述成像剂的溶液冷冻在所述水性介质中。

公开(公告)号：US06574496B1

公开(公告)日：2003-06-03

申请号：US09572949

申请日：2000-05-18

Applicant: Klaes Golman ,  Oskar Axelsson ,  Haukur Johannesson

Inventor： Klaes Golman ,  Oskar Axelsson ,  Haukur Johannesson

IPC: A61B505

CPC classification number: G01R33/5601 ,  G01R33/56308

Abstract: A method of magnetic resonance investigation of a sample by (i) reacting ortho-deuterium enriched hydrogen with a hydrogenatable MR imaging agent precursor to produce a hydrogenated (i.e. deuterated) MR imaging agent; (ii) optionally, subjecting the hydrogenated MR imaging agent to a low magnetic field;(iii) administering the hydrogenated MR imaging agent to the sample; (iv) exposing the sample to radiation of a frequency selected to excite nuclear spin transitions of selected non-zero nuclear spin nuclei in said hydrogenated MR imaging agent; (v) detecting magnetic resonance signals of the selected non-zero nuclear spin nuclei from the sample; and (vi) optionally, generating an image or biological functional data or dynamic flow data from the detected signals.

Abstract translation: 通过（i）使富氘氢与可氢化MR显像剂前体反应以产生氢化（即氘代）MR成像剂，对样品进行磁共振研究的方法; （ii）任选地，使氢化MR成像剂经受低磁场;（iii）向该样品施用氢化MR显像剂; （iv）将所述样品暴露于所选择的用于激发所述氢化MR成像剂中选定的非零核自旋核的核自旋跃迁的频率的辐射; （v）从所述样品检测所选择的非零核自旋核的磁共振信号; 和（vi）可选地，从检测到的信号生成图像或生物功能数据或动态流量数据。

公开(公告)号：US06180649B2

公开(公告)日：2001-01-30

申请号：US09171530

申请日：1998-11-19

Applicant: Peter Moldt ,  Bjarne Hugo Dahl ,  Jorgen Drejer ,  Oskar Axelsson

Inventor： Peter Moldt ,  Bjarne Hugo Dahl ,  Jorgen Drejer ,  Oskar Axelsson

IPC: A61K31445

CPC classification number: C07D401/04

Abstract: The present invention discloses compounds of the formula wherein the dotted bonds are optional extra bonds allowing any tautomeric isomers compatible with substituents X and R3; R3 is non-existing, hydrogen, or alkyl; X is O, S, imino, alkoxy, alkylthio, or amino; R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, acyl, acylalkyl, alkoxyalkyl, dialkoxyalkyl, or phenylalkyl which may be substituted with alkyl, halogen, amino, nitro or cyano; and R4, R5, R6 and R7 independently of each other are hydrogen; halogen; amino; nitro; CN; CF3; COOH; COO-alkyl; alkyl; acyl; alkoxy; —(CH2)n,—OH wherein n is 0, 1, 2, or 3; —(CH2)m—O-alkyl wherein m is 0, 1,2, or 3; —(CH2)p—O-acyl wherein p is 0, 1,2, or 3; or a pharmaceutically acceptable addition salt thereof. The compounds are useful as pharmaceuticals, for example, in the treatment of traumatic lesions of peripheral nerves, the medulla, and/or the spinal cord, cerebral ischaemic neuronal damage, neuropathy and especially peripheral neuropathy, dementia, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, or any other neurodegenerative disease.

Abstract translation: 本发明公开了以下结构的化合物：虚线键是任选的额外键，允许与取代基X和R 3相容的任何互变异构体; R3不存在，氢或烷基; X是O，S，亚氨基，烷氧基，烷硫基或 氨基; R 1是氢，烷基，烯基，炔基，环烷基，环烷基烷基，酰基，酰基烷基，烷氧基烷基，二烷氧基烷基或可被烷基，卤素，氨基，硝基或氰基取代的苯基烷基; 和R 4，R 5，R 6和R 7彼此独立地是氢; 卤素; 氨基; 硝基; CN; CF3; COOH; COO-烷基; 烷基; 酰基; 烷氧基 - （CH 2）n，-OH，其中n为0,1,2或3; - （CH 2）m -O-烷基，其中m为0,1,2或3; - （CH 2）p -O-酰基，其中p为0,1,2或3;或其药学上可接受的加成盐。 该化合物可用作药物，例如用于治疗周围神经，髓质和/或脊髓的创伤性损伤，脑缺血性神经元损伤，神经病变，特别是周围神经病变，痴呆，阿尔茨海默病，亨廷顿病，帕金森病 疾病，肌萎缩性侧索硬化或任何其他神经变性疾病。

公开(公告)号：US5210091A

公开(公告)日：1993-05-11

申请号：US888036

申请日：1992-05-22

Applicant: Oskar Axelsson ,  Mikkel Thaning ,  Peter Moldt

Inventor： Oskar Axelsson ,  Mikkel Thaning ,  Peter Moldt

IPC: C07D235/30

CPC classification number: C07D235/30

Abstract: The application discloses benzimidazole derivatives, pharmaceutical preparations comprised the compounds, their preparation and use in the treatment of disorders of the Central Nervous System such as ischemia, migraine, epilepsia, psychosis, Parkinsonism and depression.

Abstract translation: 该申请公开了苯并咪唑衍生物，药物制剂包括化合物，其制备和用于治疗中枢神经系统疾病如缺血，偏头痛，癫痫，精神病，帕金森综合征和抑郁症。