T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물
    11.
    发明公开
    T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물 有权
    5-(取代的烷基氨基甲酰基)异噻唑衍生物作为T型钙通道拮抗剂

    公开(公告)号:KR1020120096842A

    公开(公告)日:2012-08-31

    申请号:KR1020110016203

    申请日:2011-02-23

    CPC classification number: C07D413/12

    Abstract: PURPOSE: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is provided to have excellent activity as an antagonist of T- type calcium ion channel. CONSTITUTION: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is represented by chemical formula 1. The encephalopathy therapy and for prevention agent selected from epilepsy, depression, Parkinson's disease, dementia, sleep disorder, an agent for cancer treatment and prevention, an agent for heart disease treatment and prevention selected from hypertensive, cardiac arrhythmia, angina, myocardial infarction, congestive heart failure, pharmaceutical composition for alleviating pain selected from neuropathic pain and chronic and acute pain includes a compound represented by chemical formula 1.

    Abstract translation: 目的:提供作为T型钙通道阻滞剂的5-(取代的烷基氨基甲基)异恶唑基化合物作为T-型钙离子通道的拮抗剂具有优异的活性。 构成:以化学式1表示作为T型钙通道阻断剂的5-(取代烷基氨基甲基)异恶唑类化合物。脑病治疗和预防药物选自癫痫,抑郁症,帕金森病,痴呆,睡眠障碍, 癌症治疗和预防,选自高血压,心律失常,心绞痛,心肌梗塞,充血性心力衰竭,减轻选自神经性疼痛和慢性和急性疼痛的疼痛的药物组合物的心脏病治疗和预防剂,包括由化学式 1。

    세로토닌 5―HT₃A 길항적 효과를 갖는 퀴나졸린유도체 함유 약제 조성물
    13.
    发明授权
    세로토닌 5―HT₃A 길항적 효과를 갖는 퀴나졸린유도체 함유 약제 조성물 失效
    含有喹唑啉衍生物的药物组合物,用于治疗作为血清素受体拮抗剂

    公开(公告)号:KR100879636B1

    公开(公告)日:2009-01-21

    申请号:KR1020070084322

    申请日:2007-08-22

    CPC classification number: A61K31/517 A61K31/5377

    Abstract: A pharmaceutical composition for preventing and treating the disease related to the central nervous system, and a food composition are provided to obtain the effect on emesis, nausea, alcoholism, drugs abuse, depression, compulsion neurosis, anxiety, etc. A pharmaceutical composition for preventing and treating the disease related to the central nervous system comprises a quinoline derivative compound represented by the formula 1 or its pharmaceutically acceptable salt as an active ingredient, wherein R1 is H, a C1-C6 alkyl group, a phenyl group or a benzyl group; R2 is a heterocyclic group selected from morpholine, pyrrolidine and piperidine; the phenyl group or the benzyl group can be substituted with a substituent selected from a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group; and n is an integer of 1-6.

    Abstract translation: 提供了用于预防和治疗与中枢神经系统有关的疾病的药物组合物和食物组合物,以获得对呕吐,恶心,酒精中毒,药物滥用,抑郁,强迫性神经症,焦虑等的作用。 并且治疗与中枢神经系统相关的疾病包括由式1表示的喹啉衍生物化合物或其药学上可接受的盐作为活性成分,其中R1是H,C1-C6烷基,苯基或苄基; R2是选自吗啉,吡咯烷和哌啶的杂环基; 苯基或苄基可以被选自卤素原子,C1-C6烷基和C1-C6烷氧基的取代基取代; n为1-6的整数。

    신규한 D-에리트로-2-데옥시-2,2-디플루오로-1-옥소리보스화합물 및 그 제조방법
    14.
    发明公开
    신규한 D-에리트로-2-데옥시-2,2-디플루오로-1-옥소리보스화합물 및 그 제조방법 无效
    新型D-呋喃基-2-脱氧-2,2-二氟-1-氧化物及其制备方法

    公开(公告)号:KR1020070119422A

    公开(公告)日:2007-12-20

    申请号:KR1020060054040

    申请日:2006-06-15

    CPC classification number: C07H3/08 C07H1/00

    Abstract: A method for preparing a novel D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is provided to synthesize the compound with high purity and high yield selectively, which is able to be used as an intermediate for preparing beta-2,2-difluoro nucleoside. A D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is represented by the formula(1), wherein R1 is piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl; and R2 is benzoyl, biphenylcarbonyl, naphthoyl, benzyloxycarbonyl, para-methoxy benzyloxycarbonyl, or para-nitrobenzyloxycarbonyl substituted by a substituent selected from the group consisting of acetyl, monochloroacetyl, dichloroacetyl, pivaloyl, nitro, methyl, trifluoromethyl, chloro, fluoro, hydroxy and methoxy. A method for preparing the compound of the formula(1) comprises the steps of: reacting a compound represented by the formula(4) with piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl compound to prepare a compound represented by the formula(3); reacting the compound of the formula(3) with an acid to prepare a compound represented by the formula(2); and protecting 5-hydroxy of the compound of the formula(2). In the formulae(2) to (4), R is the same as defined above.

    Abstract translation: 提供了一种制备新型D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物的方法,可以选择性地合成具有高纯度和高产率的化合物,其能够用作制备β的中间体 -2,2-二氟核苷。 D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物由式(1)表示,其中R 1是哌嗪基,2,3-二甲氧基苯甲酰基或2,4-二甲氧基苯甲酰基; R2是由选自乙酰基,一氯乙酰基,二氯乙酰基,新戊酰基,硝基,甲基,三氟甲基,氯,氟,羟基的取代基取代的苯甲酰基,联苯基羰基,萘甲酰基,苄氧基羰基,对甲氧基苄氧基羰基或对硝基苄氧基羰基。 甲氧基。 制备式(1)化合物的方法包括以下步骤:使式(4)表示的化合物与哌嗪基,2,3-二甲氧基苯甲酰或2,4-二甲氧基苯甲酰化合物反应,制备式 (3); 使式(3)的化合物与酸反应以制备由式(2)表示的化合物; 并保护式(2)化合物的5-羟基。 式(2)〜(4)中,R与上述相同。

    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물
    15.
    发明授权
    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물 失效
    헬리코박터파이로리의성장억제효과를지닌신규마크로라이드화헬

    公开(公告)号:KR100428703B1

    公开(公告)日:2004-04-30

    申请号:KR1020000005140

    申请日:2000-02-02

    Abstract: PURPOSE: A novel macrolide compound having an inhibiting activity for the growth of Helicobacter pylori is provided, which is not easily decomposed by gastric acid. CONSTITUTION: The macrolide compound is represented by formula (1), in which R1 is hydrogen, 4-methoxy phenoxy methyl, 2-methoxy phenoxy methyl or methoxy ethoxy methyl; R2 is hydrogen, acyl or lower alkoxy; R3 is the same or different and hydrogen or acyl; and Q and W form oxo together or independently -OR4 and hydrogen, wherein R4 is hydrogen. It has an inhibiting activity for the growth of Helicobacter pylori which causes several stomach diseases.

    Abstract translation: 目的:提供一种对幽门螺杆菌生长具有抑制活性的新型大环内酯化合物,其不易被胃酸分解。 构成:大环内酯类化合物由式(1)表示,其中R1为氢,4-甲氧基苯氧基甲基,2-甲氧基苯氧基甲基或甲氧基乙氧基甲基; R2是氢,酰基或低级烷氧基; R3相同或不同,为氢或酰基; 并且Q和W一起或独立地形成氧代-OR 4和氢,其中R 4是氢。 它对幽门螺杆菌的生长具有抑制活性,引起多种胃病。

    신규한 피리도피리미딘 유도체, 그 제조방법 및 이를포함하는 약제학적 조성물
    16.
    发明授权
    신규한 피리도피리미딘 유도체, 그 제조방법 및 이를포함하는 약제학적 조성물 失效
    신규한피리도피리미딘유도체,그제조방법및이를포함하는약제학적조성물

    公开(公告)号:KR100377787B1

    公开(公告)日:2003-03-26

    申请号:KR1020000086254

    申请日:2000-12-29

    Abstract: PURPOSE: Provided are novel pyridopyrimidine derivatives which inhibit phosphodiesterase IV activity and TNF production. Also, provided are preparing process thereof and a pharmaceutical composition containing the same. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl amino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl; R is hydrogen, methyl, C3-7 lower alkyloxy, phenyl, benzyl, substituted phenyl(wherein a substituent group includes cyano, halogen, carboxylalkyl, nitro, methyl, trihalogenated ethyl or alkyloxy; and substitution site can be ortho-, meta-, or para- site), alkyloxy, C3-7 lower alkyloxy ethyl, benzyloxy, benzyloxyethyl, phenyloxyethyl, carboxyalkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

    Abstract translation: 目的:提供抑制磷酸二酯酶IV活性和TNF产生的新型吡啶并嘧啶衍生物。 另外,提供了其制备方法和含有其的药物组合物。 构成:新的吡啶并嘧啶衍生物由式(1)表示,其中R1为C1-3低级烷基,C3-7环烷基,环烷氧基,环烷基氨基,环烷基低级烷基,C1-3低级烷氧基,甲酰基,羟基低级烷基或 羧基; (其中取代基包括氰基,卤素,羧基烷基,硝基,甲基,三卤代乙基或烷氧基;取代位置可以是邻位,间位, 烷氧基,C 3-7低级烷氧基乙基,苄氧基,苄氧基乙基,苯氧基乙基,羧基烷基或氰基; 并且R4是氢或甲基,条件是R2和R3不相同。

    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물
    17.
    发明公开
    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물 失效
    具有抑制活性的新型马来酸化合物用于生长HELICOBACTER PYLORI

    公开(公告)号:KR1020010077376A

    公开(公告)日:2001-08-17

    申请号:KR1020000005140

    申请日:2000-02-02

    Abstract: PURPOSE: A novel macrolide compound having an inhibiting activity for the growth of Helicobacter pylori is provided, which is not easily decomposed by gastric acid. CONSTITUTION: The macrolide compound is represented by formula (1), in which R1 is hydrogen, 4-methoxy phenoxy methyl, 2-methoxy phenoxy methyl or methoxy ethoxy methyl; R2 is hydrogen, acyl or lower alkoxy; R3 is the same or different and hydrogen or acyl; and Q and W form oxo together or independently -OR4 and hydrogen, wherein R4 is hydrogen. It has an inhibiting activity for the growth of Helicobacter pylori which causes several stomach diseases.

    Abstract translation: 目的:提供一种具有幽门螺杆菌生长抑制活性的新型大环内酯类化合物,不易被胃酸分解。 构成:大环内酯类化合物由式(1)表示,其中R1是氢,4-甲氧基苯氧基甲基,2-甲氧基苯氧基甲基或甲氧基乙氧基甲基; R2是氢,酰基或低级烷氧基; R3相同或不同,为氢或酰基; 并且Q和W一起或独立地代表-OR4和氢,其中R4是氢。 它对幽门螺杆菌的生长具有抑制作用,导致多种胃部疾病。

    세로토닌 5-HT6 저해 활성을 갖는 5,6,7,8-테트라하이드로퀴나졸린-2-아민 화합물

    公开(公告)号:KR101730790B1

    公开(公告)日:2017-04-28

    申请号:KR1020150186413

    申请日:2015-12-24

    Abstract: 본발명은세로토닌서브타입중하나인 5-HT수용체에대하여저해활성을가지는신규 5,6,7,8-테트라하이드로퀴나졸린-2-아민화합물과상기화합물이포함된중추신경계 (CNC) 질환의예방또는치료용약제조성물또는중추신경계 (CNC) 질환의진단시약에관한것이다. 본발명의신규화합물은 5-HT수용체에대한결합력및 저해활성을가지므로알쯔하이머(AD), 주의력결핍증(ADHD), 간질, 우울증(depression), 비만, 정신분열증, 수면장애, 통증불안증과같은중추신경계(CNS, central nervous system) 질환의진단, 예방및 치료를목적으로유용하게사용될수 있다.

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