세로토닌 5-HT6 저해 활성을 갖는 5-설포닐아미노-5,6-다이하이드로-1H-피라졸로[3,4-c]피리딘-7(4H)-온 화합물
    2.
    发明公开
    세로토닌 5-HT6 저해 활성을 갖는 5-설포닐아미노-5,6-다이하이드로-1H-피라졸로[3,4-c]피리딘-7(4H)-온 화합물 有权
    新型5-磺酰氨基-5,6-二氢-1H-吡唑并[3,4-C]吡啶-7(4H) - 酮化合物,其具有丝氨酸5-HT6的抑制活性

    公开(公告)号:KR1020140118141A

    公开(公告)日:2014-10-08

    申请号:KR1020130033552

    申请日:2013-03-28

    Abstract: The present invention relates to a novel 5-sulfonylamino-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one compound having an inhibitory activity for 5-HT6, which is one of serotonin subtypes, and a pharmaceutical composition comprising the compound as an active ingredient. Since the novel compound of the present invention has 5-HT6 inhibitory activities, the compound can be used for diagnosing, preventing, and treating central nervous system (CNS) diseases such as Alzheimer′s disease (AD), attention deficit disorder (ADHD), epilepsy, depression, obesity, schizophrenia, sleep disorders, and pain disorders.

    Abstract translation: 本发明涉及对5-HT6具有抑制活性的新的5-磺酰基氨基-5,6-二氢-1H-吡唑并[3,4-c]吡啶-7(4H) - 酮化合物,其为5-羟色胺 亚型和包含该化合物作为活性成分的药物组合物。 由于本发明的新化合物具有5-HT 6抑制活性,所以该化合物可用于诊断,预防和治疗中枢神经系统(CNS)疾病如阿尔茨海默病(AD),注意缺陷障碍(ADHD) ,癫痫,抑郁症,肥胖,精神分裂症,睡眠障碍和疼痛障碍。

    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법
    6.
    发明公开
    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법 失效
    新型吡咯烷基胺化合物作为钙通道调节剂及其制备方法

    公开(公告)号:KR1020100042111A

    公开(公告)日:2010-04-23

    申请号:KR1020080101249

    申请日:2008-10-15

    Abstract: PURPOSE: A pyrazolylmethylamine-piperazine derivative which is effective as a calcium ion channel modulator is provided to ensure effective activation as an T-type calcium ion channel antagonist and to use as an agent for preventing and treating brain diseases, heart diseases and pain diseases. CONSTITUTION: A pyrazolylmethylamine-peperazine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases, heart diseases or pain diseases by T-type calcium ion channel antagonism contains the pyrazolylmethylamine-peperazine derivative of chemical formula 1 or its pharmaceutically acceptable salt an active ingredient. The brain disease is epilepsy, depression, Parkison's disease, dementia or somnipathy. The heart disease is hypertension, cardiac arrhythmia, myocardial infarction, or congestive failure. The pain disease is chronic pain, acute pain, or neurogenic pain. The pyrazolylmethylamine-peperazine derivative is prepared by binding pyrazolylmethylamine compound of chemical formula 3 with piperazine acetyl halide compound of chemical formula 2.

    Abstract translation: 目的:提供作为钙离子通道调节剂有效的吡唑基甲胺 - 哌嗪衍生物,以确保作为T型钙离子通道拮抗剂的有效活化,并用作预防和治疗脑疾病,心脏病和疼痛疾病的药剂。 构成:吡唑基甲胺 - 哌嗪衍生物由化学式1表示。用于通过T型钙离子通道拮抗作用预防和治疗脑疾病,心脏病或疼痛疾病的药物组合物含有化学式1的吡唑基甲基 - 哌嗪衍生物或其药学上可接受的盐 可接受的盐为活性成分。 脑疾病是癫痫,抑郁症,帕金森病,痴呆或嗜睡。 心脏病是高血压,心律失常,心肌梗死或充血性衰竭。 疼痛疾病是慢性疼痛,急性疼痛或神经源性疼痛。 通过将化学式3的吡唑基甲基胺化合物与化学式2的哌嗪乙酰卤化合物结合,制备吡唑基甲胺 - 哌嗪衍生物。

    5-HT7 수용체에 길항작용을 갖는 신규한 화합물
    8.
    发明公开
    5-HT7 수용체에 길항작용을 갖는 신규한 화합물 失效
    5-HT7受体拮抗剂的新化合物

    公开(公告)号:KR1020090011376A

    公开(公告)日:2009-02-02

    申请号:KR1020070074889

    申请日:2007-07-26

    Abstract: A novel compound having antagonism in 5-HT7 receptor is provided to be usefully used for relax and treatment of disease mediated in 5-HT7 or symptom and to have good pharmaceutical properties. A novel compound having antagonism in 5-HT7 receptor is represented by a chemical formula (I). In the chemical formula (I), R1 is substitution radical selected from a group consisting of alkyl of C1~C4 substituted for halogen or nitro and alkoxy of C1~C4 or phenyl or benzyl; R2 is anisole naphthalene or quinoline; R3 is H, C1~C4 alkyl, halogen or C1~C4 alkoxy; R4 is H or C1~C3 alkyl not substituted for cyclo C5~C7 alkyl or phenyl.

    Abstract translation: 提供了一种具有5-HT7受体拮抗作用的新化合物,可有效用于5-HT7或症状介导的疾病的放松和治疗,具有良好的药物性质。 在5-HT7受体中具有拮抗作用的新化合物由化学式(I)表示。 在化学式(I)中,R 1为选自被取代卤素或硝基的C 1 -C 4烷基和C 1 -C 4烷氧基或苯基或苄基的取代基; R2是苯甲醚萘或喹啉; R3是H,C1〜C4烷基,卤素或C1〜C4烷氧基; R4是H或C1-C3烷基,不代替环C5〜C7烷基或苯基。

    몰폴린-2-온 유도체를 포함하는 T-형 칼슘 채널 차단용조성물
    9.
    发明授权
    몰폴린-2-온 유도체를 포함하는 T-형 칼슘 채널 차단용조성물 失效
    用于阻断含有多环戊二烯-2-酮衍生物的T型钙通道的组合物

    公开(公告)号:KR100758317B1

    公开(公告)日:2007-09-13

    申请号:KR1020060039225

    申请日:2006-05-01

    CPC classification number: A61K31/5375

    Abstract: A composition for blocking T-type calcium channel comprising morpholin-2-one derivatives is provided to block the T-type calcium channel in the same level as the conventional T-type calcium channel blocker, mibefradil, without side effects. A composition for blocking T-type calcium channel comprises morpholin-2-one derivatives represented by the formula(1), or pharmaceutically acceptable salts thereof, wherein R^1 and R^2 are each independently hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy; and R^3 and R^4 are each independently hydrogen, C1-C6 alkyl, C1-C6 thioalkyl, amino or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy. The composition prevents or treats diseases caused by overexpression of T-type calcium channel including angina pectoris, hypertension, myocardiac infarction, pain and epilepsy.

    Abstract translation: 提供一种用于阻断包含吗啉-2-酮衍生物的T型钙通道的组合物,以阻断与常规T型钙通道阻滞剂米非司酮相同水平的T型钙通道,无副作用。 用于阻断T型钙通道的组合物包括由式(1)表示的吗啉-2-酮衍生物或其药学上可接受的盐,其中R 1和R 2各自独立地为氢,C 1 -C 6烷基, C 6环烷基或任选被卤素,硝基,羟基或C 1 -C 6烷氧基取代的苯基; R 3和R 4各自独立地为氢,C 1 -C 6烷基,C 1 -C 6硫代烷基,任选被卤素,硝基,羟基或C 1 -C 6烷氧基取代的氨基或苯基。 该组合物预防或治疗由过度表达T型钙通道引起的疾病,包括心绞痛,高血压,心肌梗塞,疼痛和癫痫。

    피페라지닐알킬피라졸계 T-타입 칼슘 채널 억제 화합물 및이의 제조방법
    10.
    发明授权
    피페라지닐알킬피라졸계 T-타입 칼슘 채널 억제 화합물 및이의 제조방법 失效
    피페라지닐알킬피라졸계T-타입칼슘억억제화합물및이의제조방피

    公开(公告)号:KR100654328B1

    公开(公告)日:2006-12-08

    申请号:KR1020050079095

    申请日:2005-08-26

    Abstract: A novel piperazinylalkylpyrazole derivative is provided to be able to selectively block T-type calcium ion channels, thereby showing better pain, hypertension, and epilepsy therapeutic effect compared to conventional medicines. The piperazinylalkylpyrazole derivative is represented by the formula(1), where R1 is phenyl, X1-substituted phenyl(where X1 is nitro, methyl, chloro, or methoxy, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), 1,1-diphenylmethyl or X2-substituted diphenylmethyl(where X2 is chloro or methyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), R2 is H, methyl or ethyl, R3 is methyl, propyl, isobutyl, phenyl, cyclohexyl, substituted phenyl(methyl, chloro, or methoxy as a substituent), naphthyl, piperidinyl, R4 is H, C1-6 alkyl, 2-furyl, phenyl or X3-substituted phenyl(where X3 is chloro, methyl, cyclohexyl or piperidinyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), and n is an integer from 0 to 3.

    Abstract translation: 提供了一种新的哌嗪基烷基吡唑衍生物,能够选择性阻断T型钙离子通道,因此与常规药物相比,表现出更好的疼痛,高血压和癫痫治疗效果。 哌嗪基烷基吡唑衍生物由式(1)表示,其中R 1为苯基,X 1取代的苯基(其中X 1为硝基,甲基,氯或甲氧基,取代位置为邻位,间位或对位, 三或四或全部能够被取代),1,1-二苯基甲基或X2-取代的二苯基甲基(其中X2是氯或甲基,取代位置是邻位,间位或对位,以及单,二,三,四或 全部能被取代),R2是H,甲基或乙基,R3是甲基,丙基,异丁基,苯基,环己基,取代的苯基(甲基,氯或甲氧基作为取代基),萘基,哌啶基,R4是H, C 1-6烷基,2-呋喃基,苯基或X 3 - 取代的苯基(其中X 3为氯,甲基,环己基或哌啶基,取代位置为邻位,间位或对位,并且单,二,三,四或全部 被取代),并且n是0至3的整数。

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