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80 条记录 (耗时 0.037 秒)

    INDAZOLYL DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS
    72.
    发明申请
    INDAZOLYL DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS 有权
    有用的盐酸衍生物作为钾通道调节剂

    公开(公告)号：US20090325989A1

    公开(公告)日：2009-12-31

    申请号：US12444344

    申请日：2007-10-03

    申请人： Birgitte L. Eriksen ,  Ulrik Svane Sorensen ,  Charlotte Hougaard ,  Lene Teuber ,  Dan Peters ,  Palle Christophersen ,  Tina Holm Johansen

    发明人： Birgitte L. Eriksen ,  Ulrik Svane Sorensen ,  Charlotte Hougaard ,  Lene Teuber ,  Dan Peters ,  Palle Christophersen ,  Tina Holm Johansen

    IPC分类号： A61K31/506 ,  C07D401/04 ,  A61P9/10

    CPC分类号： C07D403/04 ,  C07D401/04

    摘要： This invention relates to novel indazolyl derivatives useful as potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular respiratory diseases, epilepsy, convulsions, seizures, absence seizures, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, erectile dysfunction, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, autism, ataxia, traumatic brain injury, Parkinson's disease, bipolar disorder, psychosis, schizophrenia, anxiety, depression, mania, mood disorders, dementia, memory and attention deficits, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, arrhythmia, hypertension, myotonic muscle dystrophia, spasticity, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, irritable bowel syndrome, immune suppression, migraine and pain.

    摘要翻译： 本发明涉及可用作钾通道调节剂的新的吲唑基衍生物及其在制备药物组合物中的用途。 此外，本发明涉及可用于治疗或减轻与钾通道活性相关的疾病或病症的药物组合物，特别是呼吸系统疾病，癫痫，抽搐，癫痫发作，不发作，痉挛，血管痉挛，冠状动脉痉挛，肾脏疾病， 多囊肾病，膀胱痉挛，尿失禁，膀胱流出阻塞，勃起功能障碍，胃肠功能障碍，分泌性腹泻，局部缺血，脑局部缺血，缺血性心脏病，心绞痛，冠心病，自闭症，共济失调，创伤性脑损伤，帕金森病， 双相障碍，精神病，精神分裂症，焦虑症，抑郁症，躁狂症，情绪障碍，痴呆，记忆和注意力缺陷，阿尔茨海默病，肌萎缩性侧索硬化（ALS），痛经，发作性睡眠，雷诺病，间歇性跛行，Sjorgren综合征，心律失常，高血压， 肌筋膜肌营养不良，痉挛，x 老年糖尿病，II型糖尿病，高胰岛素血症，早产，秃发，癌症，肠易激综合征，免疫抑制，偏头痛和疼痛。

    Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
    77.
    发明授权
    Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers 失效

    公开(公告)号：US06417393B1

    公开(公告)日：2002-07-09

    申请号：US09194083

    申请日：1999-01-22

    申请人： Palle Christophersen ,  Ove Pedersen

    发明人： Palle Christophersen ,  Ove Pedersen

    IPC分类号： C07C24100

    CPC分类号： C07C311/47 ,  A61K31/155 ,  A61K31/17 ,  C07C233/55 ,  C07C271/58 ,  C07C275/40 ,  C07C275/42 ,  C07C309/51 ,  C07C311/08 ,  C07C311/21 ,  C07C311/60 ,  C07C335/22

    摘要： The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl—CO—, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are as defined above; Y is —CO—, —CS—, —SO2—, or —C(═N—R8)—, wherein R8 is hydrogen, alkyl, or cyano; X is —NH—, —CH2—NH—, or —SO2—NH—; Z is NR6, O, —CH═CH—, —C═C—, —N═CH—, or —CH═N—; wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, —NHSO2—R7, —COOR7, —SO2N(R7)2, —SO2OR7 and —CO—R7, wherein R7 is hydrogen alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO—, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 and R13, R13 and R14 or R14 and R15 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R11, R12, R13, R14 and R15 are as defined above. The compounds are useful for the treatment of diseases and disorders responsive to the blockage of chloride channels.

    Patch clamp apparatus and technique having high throughput and low fluid volume requirements
    79.
    发明授权
    Patch clamp apparatus and technique having high throughput and low fluid volume requirements 失效
    具有高通量和低流体体积要求的贴片钳装置和技术

    公开(公告)号：US6063260A

    公开(公告)日：2000-05-16

    申请号：US836094

    申请日：1997-04-25

    申请人： S.o slashed.ren-Peter Olesen ,  Palle Christophersen

    发明人： S.o slashed.ren-Peter Olesen ,  Palle Christophersen

    IPC分类号： C12M1/34 ,  G01N1/00 ,  G01N1/10 ,  G01N33/15 ,  G01N33/487 ,  G01N27/33

    CPC分类号： G01N35/1097 ,  C12M29/10 ,  C12M33/04 ,  C12M41/48 ,  G01N33/48728

    摘要： Apparatus for carrying out patch clamp technique utilized in studying the effect of certain materials on ion transfer channels in biological tissue, and more particularly patch clamp apparatus utilizing an autosampler, such as those utilized with HPLC apparatus, to provide high throughput, is disclosed. The invention additionally includes novel microperfusion chamber assemblies capable of utilizing only small amounts of material to be tested and only small amounts of liquid carrier, thereby enabling many tests to be completed in a short period of time. The invention more broadly relates to a novel electrophysiology drug handling and application set up for screening of chemical substances while providing high throughput and requiring only low volume of solutions and samples to be tested. The invention also comprises several novel procedures for utilizing the apparatus of the invention.

    摘要翻译： PCT No.PCT / EP95 / 02204 Sec。 371日期1997年04月25日 102（e）日期1997年4月25日PCT提交1995年6月7日PCT公布。 第WO96 / 13721号公报 日期1996年5月9日用于研究某些材料对生物组织中的离子转移通道的影响的膜片钳技术的装置，更具体地，使用利用HPLC装置的自动进样器的膜片钳装置，以提供高通量， 被披露。 本发明另外包括能够仅使用少量待测试材料和仅少量液体载体的新型微灌注室组件，从而使得能够在短时间内完成许多试验。 本发明更广泛地涉及一种用于筛选化学物质的新型电生理学药物处理和应用，同时提供高通量并且仅需要低体积的溶液和样品进行测试。 本发明还包括利用本发明装置的若干新颖程序。