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    세로토닌 5-ＨＴ₃Ａ 길항적 효과를 갖는 피라졸 유도체함유 약제 조성물
    62.
    发明授权
    세로토닌 5-ＨＴ₃Ａ 길항적 효과를 갖는 피라졸 유도체함유 약제 조성물 失效
    含有用作5-羟色胺拮抗剂治疗的吡唑衍生物的药物组合物

    公开(公告)号：KR100882925B1

    公开(公告)日：2009-02-10

    申请号：KR1020070058542

    申请日：2007-06-14

    Applicant: 한국과학기술연구원

    Inventor： 남길수 ,  임혜원 ,  배애님 ,  최경일 ,  추현아 ,  나승렬

    IPC: A61K31/415 ,  A61K31/496 ,  A61P25/00

    CPC classification number: A61K31/496

    Abstract: 본 발명은 세로토닌 5-HT
    3 A에 대한 길항 활성 효과를 나타내어 구토증(emesis), 메스꺼움증(nausea), 알콜중독증, 약물남용증, 우울증, 강박노이로제, 불안증(anxiety), 발작, 알츠하이머형 치매, 파킨슨병, 헌팅턴 무도병(Huntington's chorea), 정신병(psychosis), 정신분열증, 자살성향(suicidal tendency), 수면장애(sleep disorders), 식욕장애(appetite disorders) 및 편두통 등의 중추신경계 질환의 예방 및 치료제로서 유용한 피라졸 유도체를 유효성분으로 함유하는 약제 조성물에 관한 것이다.
    세로토닌 5-ＨＴ₃Ａ 길항제, 피라졸 유도체, 구토, 알콜 중독, 약물 남용, 강박증, 우울증

    세로토닌 5-ＨＴ₃Ａ 길항적 효과를 갖는 피라졸 유도체함유 약제 조성물
    63.
    发明公开
    세로토닌 5-ＨＴ₃Ａ 길항적 효과를 갖는 피라졸 유도체함유 약제 조성물 失效
    含有吡唑衍生物的药物组合物用于治疗作为丝氨酸蛋白酶拮抗剂

    公开(公告)号：KR1020080110152A

    公开(公告)日：2008-12-18

    申请号：KR1020070058542

    申请日：2007-06-14

    Applicant: 한국과학기술연구원

    Inventor： 남길수 ,  임혜원 ,  배애님 ,  최경일 ,  추현아 ,  나승렬

    IPC: A61K31/415 ,  A61K31/496 ,  A61P25/00

    CPC classification number: A61K31/496

    Abstract: A pharmaceutical composition comprising pyrazole derivative having antagonistic effects against serotonin 5-HT3A(5-hydroxytryptamine(serotonin) receptor 3A) is provided to improve the inhibitory activity and bonding activity about 5-HT3A, thereby being applicable to the therapeutic agent of the central nervous system disease. The pharmaceutical composition for prevention and treatment of the central nervous system disease associated with serotonin 5-HT3A receptor comprises the pyrazole derivative compound and pharmaceutically acceptable salts, wherein the central nervous system disease is selected from emesis. nausea, alcoholism, drugs abuse, depression, compulsion neurosis, anxiety, seizure, Alzheimer type dementia, Parkinson's disease, Huntington`s chorea, psychosis, schizophrenia, suicidal tendency, somnopathy(sleep disorders), appetite disorder and migraine.

    Abstract translation: 提供了包含对5-羟色胺5-HT3A（5-羟色胺）受体3A具有拮抗作用的吡唑衍生物的药物组合物，以提高关于5-HT3A的抑制活性和结合活性，从而适用于中枢神经的治疗剂 系统疾病 用于预防和治疗与5-羟色胺5-HT 3 A受体相关的中枢神经系统疾病的药物组合物包括吡唑衍生物化合物和药学上可接受的盐，其中中枢神经系统疾病选自呕吐。 恶心，酒精中毒，药物滥用，抑郁症，强迫性神经症，焦虑症，癫痫发作，阿尔茨海默氏型痴呆，帕金森病，亨廷顿舞蹈病，精神病，精神分裂症，自杀倾向，睡眠障碍（睡眠障碍），食欲障碍和偏头痛。

    Ｔ-형 칼슘 채널 길항제로서의3-(4-클로로벤질)-4-옥소-2-티옥소-1,2,3,4-테트라히드로-퀴나졸린 유도체
    64.
    发明授权
    Ｔ-형 칼슘 채널 길항제로서의3-(4-클로로벤질)-4-옥소-2-티옥소-1,2,3,4-테트라히드로-퀴나졸린 유도체 失效
    3-（4-氯代）-4-氧代-2-噻唑-1,2,3,4-四氢喹啉酮衍生物作为T型钙通道拮抗剂

    公开(公告)号：KR100754325B1

    公开(公告)日：2007-09-05

    申请号：KR1020060052759

    申请日：2006-06-12

    Applicant: 한국과학기술연구원

    Inventor： 배애님 ,  조용서 ,  차주환 ,  추현아 ,  임혜원 ,  레디도다레디무니크말 ,  고훈영

    IPC: A61K31/517 ,  A61P25/04

    CPC classification number: A61K31/517

    Abstract: 3-(4-Chloro)-4-oxo-2-thioxo-1,2,3,4-tetrahydro-quinazoline derivatives as T-type calcium channel antagonists are provided to treat neurogenic pain, epilepsy, hypertension or angina pectoris by inhibiting the T-type calcium channel without side effects such as pharmacokinetic interactions. 3-(4-chloro)-4-oxo-2-thioxo-1,2,3,4-tetrahydro-quinazoline derivatives represented by the formula(I) is used as a pharmaceutical composition, wherein X is (3-piperidin-1-yl-propyl)-amide, [3-(2-ethyl-piperidin-1-yl)-propyl]-amide, [3-(4-methyl-piperidin-1-yl)-propyl]-amide, 2-(butyl-methyl-amino)-ethyl-amide, (3-pyrrolidin-1-yl-propyl)-amide, (3-azepan-1-yl-propyl)-amide, [3-(4-ethyl-piperazin-1-yl)-propyl]-amide, [3-(benzyl-methyl-amide)-propyl]-amide or (2-dimethylamino-ethyl)-amide, and the compound represented by the formula(I) includes 3-(4-chloro-benzyl)-7-(4-methyl-piperazine-1-carbonyl)-2-thioxo-2,3-dihydro-1H-quinazolin-4-one.

    Abstract translation: 提供3-（4-氯）-4-氧代-2-硫代-1,2,3,4-四氢 - 喹唑啉衍生物作为T型钙通道拮抗剂，用于通过抑制神经源性疼痛，癫痫，高血压或心绞痛来治疗 T型钙通道没有副作用，如药代动力学相互作用。 使用由式（I）表示的3-（4-氯）-4-氧代-2-硫代-1,2,3,4-四氢 - 喹唑啉衍生物作为药物组合物，其中X是（3-哌啶-4-基） 丙基） - 酰胺，[3-（2-乙基 - 哌啶-1-基） - 丙基] - 酰胺，[3-（4-甲基 - 哌啶-1-基） - 丙基] - 酰胺，2 - （丁基 - 甲基 - 氨基） - 乙基 - 酰胺，（3-吡咯烷-1-基 - 丙基） - 酰胺，（3-氮杂环庚烷-1-基 - 丙基） - 酰胺，[3-（4-乙基 - -1-基） - 丙基] - 酰胺，[3-（苄基 - 甲基 - 酰胺） - 丙基] - 酰胺或（2-二甲基氨基 - 乙基） - 酰胺，由式（I）表示的化合物包括3- （4-氯 - 苄基）-7-（4-甲基 - 哌嗪-1-羰基）-2-硫代-2,3-二氢-1H-喹唑啉-4-酮。

    Ｔ-형 칼슘 채널에 활성을 지닌 신규1,3-다이옥소아이소인돌 유도체
    65.
    发明授权
    Ｔ-형 칼슘 채널에 활성을 지닌 신규1,3-다이옥소아이소인돌 유도체 有权
    T-형칼슘채널에활을을규규규규1,3-이옥돌돌돌돌돌돌돌돌

    公开(公告)号：KR100743255B1

    公开(公告)日：2007-07-27

    申请号：KR1020060040614

    申请日：2006-05-04

    Applicant: 한국과학기술연구원

    Inventor： 조용서 ,  추현아 ,  배애님 ,  차주환 ,  고훈영 ,  김화실 ,  임혜원 ,  서선희

    IPC: C07D209/48

    Abstract: Novel 1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel are provided to treat brain diseases including epilepsy, hypertension and angina pectoris, heart disease and nerve system pain by inhibiting the T-type calcium channel as a representative low-voltage activated calcium channel. The 1,3-dioxoisoindole derivatives represented by the formula(1) or their pharmaceutically acceptable salts are provided, wherein R1 is phenyl group or benzyl group which is substituted or unsubstituted by halogen atom, C1-C6 alkoxy group, C1-C6 alkyl group, or cyano group; R2 is a hetero ring group selected from piperidinyl group, pyrolidinyl group, morpholinyl group and piperazinyl group which is substituted or unsubstituted by C1-C6 alkyl substituent; and n is 1 or 2, provided that a compound in which R2 is morpholinyl group when R1 is C1-C6 alkyl-substituted phenyl group is excluded.

    Abstract translation: 通过抑制T型钙通道作为代表性的低电压来提供具有T型钙通道选择性拮抗作用的新型1,3-二氧代异吲哚衍生物来治疗包括癫痫，高血压和心绞痛，心脏病和神经系统疼痛的脑疾病 激活钙通道。 由式（1）表示的1,3-二氧代异吲哚衍生物或它们的药学上可接受的盐，其中R1是被卤素原子，C1-C6烷氧基，C1-C6烷基取代或未被取代的苯基或苄基 或氰基; R2是选自哌啶基，吡咯烷基，吗啉基和由C1-C6烷基取代基取代或未取代的哌嗪基的杂环基; 并且n是1或2，条件是当R 1是C 1 -C 6烷基取代的苯基时，其中R 2是吗啉基的化合物被排除在外。

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