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1. 发明授权

US06320048B1 3-piperidinyl-1,2-benzisoxazoles 失效
标题翻译： 3-哌啶基-1,2-苯并异恶唑
公开(公告)号：US06320048B1
公开(公告)日：2001-11-20
申请号：US08100907
申请日：1993-08-03
申请人： Cornelus Gerardus Maria Janssen , Alfonsus Guilielmus Knaeps , Ludo Edmond Josephine Kennis , Jan Vandenberk
发明人： Cornelus Gerardus Maria Janssen , Alfonsus Guilielmus Knaeps , Ludo Edmond Josephine Kennis , Jan Vandenberk
IPC分类号： C07B5700
CPC分类号： C07D471/04
摘要： There is disclosed a process for preparing an enantiomeric form of the compound having the formula: or a pharmaceutically acceptable acid addition salt thereof, wherein said process comprises the steps of: (a) reacting a racemic mixture of said compound with a chiral acid or acid chloride selected from the group consisting of tartaric acid, malic acid, mandelic acid, camphor sulfonic acid, 4,5-dihydro-1H-2-benzopyran-2-carboxylic acid, and the acid chlorides thereof, to form a mixture of diastereomeric salts or esters; (b) physically separating said mixture of diastereomeric salts or esters by selective crystallization or chromatography; and (c) converting said separated diastereomeric salts or esters into the corresponding enantiomeric forms of said compound by hydrolysis in an acidic or basic aqueous medium.
摘要翻译：公开了具有下式的化合物或其药学上可接受的酸加成盐的对映体形式的方法，其中所述方法包括以下步骤：（a）使所述化合物的外消旋混合物与手性酸或酸反应选自酒石酸，苹果酸，扁桃酸，樟脑磺酸，4,5-二氢-1H-2-苯并吡喃-2-羧酸及其酰氯的氯化物，以形成非对映体盐的混合物或酯;（b）通过选择性结晶或色谱法物理分离所述非对映体盐或酯的混合物; 和（c）通过在酸性或碱性水性介质中水解将所述分离的非对映体盐或酯转化成所述化合物的相应对映体形式。

2. 发明授权

US07820453B2 Cardiovascular safety assay 有权
标题翻译：心血管安全性测定
公开(公告)号：US07820453B2
公开(公告)日：2010-10-26
申请号：US11593399
申请日：2006-11-06
申请人： Godelieve Irma Christine Maria Heylen , Cornelus Gerardus Maria Janssen , Mirek Jurzak , Henricus Petrus Martinus Maria Van Assouw
发明人： Godelieve Irma Christine Maria Heylen , Cornelus Gerardus Maria Janssen , Mirek Jurzak , Henricus Petrus Martinus Maria Van Assouw
IPC分类号： G01N33/567 , G01N33/53 , C12Q1/02 , G01N33/566
CPC分类号： G01N33/6893 , G01N33/5014 , G01N33/60 , G01N33/6887 , G01N2500/02 , G01N2800/32
摘要： The present invention provides assays and kits for the screening of test compounds for their capability to induce cardiotoxicity in a subject. Said assays and kits are based on the finding that the interaction of astemizole with the HERG potassium channel can be exploited to predict cardiotoxicity of compounds during the development of new therapeutics and other agents.
摘要翻译：本发明提供了用于筛选测试化合物在受试者中诱导心脏毒性的能力的测定和试剂盒。所述测定和试剂盒基于以下发现：可以利用阿司咪唑与HERG钾通道的相互作用来预测化合物在新治疗剂和其它药剂开发过程中的心脏毒性。

3. 发明授权

US07541476B2 Radiolabeled astemizole and method of making 有权
标题翻译：放射性标记的阿司咪唑及其制备方法
公开(公告)号：US07541476B2
公开(公告)日：2009-06-02
申请号：US11698383
申请日：2007-01-26
申请人： Godelieve Irma Christine Maria Heylen , Cornelus Gerardus Maria Janssen , Jurzak Mirek , Henricus Petrus Martinus Maria Van Assouw
发明人： Godelieve Irma Christine Maria Heylen , Cornelus Gerardus Maria Janssen , Jurzak Mirek , Henricus Petrus Martinus Maria Van Assouw
IPC分类号： C07D235/02 , C07D233/02 , A61K31/445 , A61K37/00
CPC分类号： G01N33/6872 , G01N33/5014
摘要： The present invention provides a radiolabeled astemizole of formula (III) and a process for preparing the radiolabeled astemizole of formula III.
摘要翻译：本发明提供式（III）的放射性标记的阿司咪唑和制备式III的放射性标记的阿司咪唑的方法。

4. 发明授权

US06451802B1 S-oxide lipid lowering compounds 失效
标题翻译： S-氧化物降脂化合物
公开(公告)号：US06451802B1
公开(公告)日：2002-09-17
申请号：US09857838
申请日：2001-06-08
申请人： Cornelus Gerardus Maria Janssen , Peter Walter Maria Roevens , Jozef Bertha August Thijssen
发明人： Cornelus Gerardus Maria Janssen , Peter Walter Maria Roevens , Jozef Bertha August Thijssen
IPC分类号： A61K31496
CPC分类号： C07D405/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I) the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts, wherein n is 1 or 2, R1 is hydrogen, C1-6alkyl or halo; R2 is hydrogen or halo; R3 is C1-8alkyl or C3-6cycloalkyl; Hetis an optionally substituted triazole, imidazole, or thiazole; and —A—B— is a bivalent radical of formula —CH═CH—, —N═CH—, —CH═N—, wherein optionally one of the hydrogen atoms is replaced by C1-4alkyl; having apolipoprotein B inhibiting activity and concomitant lipid lowering activity. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating disorders caused by an excess of very low density lipoproteins (VLDL) or low density lipoproteins (LDL), and especially disorders caused by the cholesterol associated with said VLDL and LDL, such as, for example, hyperlipidemia, obesitas or atherosclerosis.
摘要翻译：本发明涉及式（I）化合物的N-氧化物，其立体化学异构形式和药学上可接受的酸加成盐，其中n为1或2，R 1为氢，C 1-6烷基或卤素; R2是氢或卤素; R3是C1-8烷基或C3-6环烷基; Hetis是任选取代的三唑，咪唑或噻唑; 并且-A-B-是式-CH = CH-，-N = CH-，-CH = N-的二价基团，其中任选地一个氢原子被C 1-4烷基取代; 具有载脂蛋白B抑制活性和伴随的降脂活性。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗由过量非常低密度脂蛋白（VLDL）或低密度脂蛋白（LDL）引起的疾病，特别是由与所述VLDL和LDL相关的胆固醇，例如高脂血症，肥胖或动脉粥样硬化。

5. 发明授权

US07517517B2 Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands 有权
标题翻译：放射性标记喹啉和喹啉酮衍生物及其作为代谢型谷氨酸受体配体的用途
公开(公告)号：US07517517B2
公开(公告)日：2009-04-14
申请号：US10509069
申请日：2003-03-26
申请人： Anne Simone Josephine Lesage , François Paul Bischoff , Cornelus Gerardus Maria Janssen , Hilde Lavreysen
发明人： Anne Simone Josephine Lesage , François Paul Bischoff , Cornelus Gerardus Maria Janssen , Hilde Lavreysen
IPC分类号： A61K51/00 , A61M36/14 , G01N33/00
CPC分类号： A61K51/0459 , A61K51/0463
摘要： The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of of 3H, 11C and 18F. The invention also relates to their use in a diagnostic method, in particular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET.
摘要翻译：本发明涉及式（I-A）*或（I-B）*的放射性标记喹啉和喹啉酮衍生物，其表现出代谢型谷氨酸受体拮抗活性，特别是mGlu1受体活性及其制备; 它还涉及包含它们的组合物，以及它们用于标记和鉴定代谢型谷氨酸受体位点和成像器官的用途。在优选的实施方案中，X表示O; R1表示C1-6烷基; 环C 3-12烷基或（环C 3-12烷基）C 1-6烷基，其中C 1-6烷基部分或环C 3-12烷基部分中的一个或多个氢原子任选地可被C 1-6烷氧基，芳基，卤代或噻吩基取代; R2表示氢; 光环; C 1-6烷基或氨基; R3和R4各自独立地表示氢或C1-6烷基; 或者R 2和R 3可以一起形成-R 2 -R 3 - ，其表示式-Z 4 -CH 2 -CH 2 -CH 2 - 或-Z 4 -CH 2 - 的二价基团，其中Z 4为O或NR 11，其中R 11为C 1 -6-烷基; 并且其中每个二价基团任选被C 1-6烷基取代; 或者R 3和R 4可以一起形成式-CH 2 -CH 2 -CH 2 -CH 2 - 的二价基团; R5代表氢; Y表示O; 芳基表示任选被卤素取代的苯基。最优选的是放射性标记的化合物，其中放射性同位素选自3H，11C和18F。本发明还涉及其在诊断方法中的用途，特别是用于在生物材料中标记和鉴定mGluR1受体，以及其用于成像器官，特别是使用PET的用途。

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