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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
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-
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
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。
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公开(公告)号：KR1020060035035A
公开(公告)日：2006-04-26
申请号：KR1020040084112
申请日：2004-10-20
Applicant: 한국과학기술연구원
IPC: C07D413/14
Abstract: 본 발명은 메티실린 저항성 스태필로코커스 아우레우스(MRSA) 및 벤코마이신 저항성 엔테로콕사이(VRE) 등의 내성균주를 포함한 그람 양성균주에 대하여 우수한 항균력을 가지는 신규 구조의 트리아졸릴메틸옥사졸리디논 유도체와 이 화합물의 제조방법, 그리고 이 화합물의 항생제로서의 의약적 용도에 관한 것이다.
트리아졸릴메틸옥사졸리디논, 항생제, 내성균주, 그람 양성균주-
44.发明公开신규 피리도[2,3-ｄ]피리미딘 카르보알데히드 옥심계ＰＤＥ Ⅳ 효소 저해 화합물 및 이의 제조방법 失效PYRIDO [2,3-D]吡啶二羰基氧化物衍生物作为PDE IV抑制剂及其制备方法有用
公开(公告)号：KR1020030076072A
公开(公告)日：2003-09-26
申请号：KR1020020015728
申请日：2002-03-22
IPC: C07D471/04
Abstract: PURPOSE: Pyrido£2,3-d|pyridine carboaldehyde oxime derivatives useful as PDE IV inhibitor and a preparation method thereof are provided, which compounds are useful for treatment of respiration diseases, and diseases associated with TNF(tumor necrosis factor) formation. CONSTITUTION: Pyrido£2,3-d|pyridine carboaldehyde oxime derivatives represented by formula (I) or pharmaceutically acceptable salts are provided, wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl, or X-substituted phenyl, in which X is methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, cyano, carboxylic acid, carboxymethyl ester, carboxyethyl ester, nitro, fluoro or trifluoromethyl; R2 is hydrogen or methyl; and R3 is hydrogen, methyl, C3-7 lower alkyloxy, allyl, phenyl, benzyl, X-substituted phenyl, methyloxyphenyl or methyloxy Y-substituted phenyl in which X is cyano, halogen, carboxyalkyl, nitro, methyl, trihalogenated methyl or alkyloxy, and Y is methoxy. A method for preparing pyrido£2,3-d|pyridine carboaldehyde oxime derivatives of formula (I) comprises preparing a compound of formula (III) from a compound of formula (II) in the presence of palladium catalyst and base; reacting the compound of formula (III) with hydroxylamine, alkyloxyamine or hydrochloric acid salts thereof.
Abstract translation: 目的：提供用作PDE IV抑制剂的吡啶2,3-d-吡啶甲醛肟衍生物及其制备方法，该化合物可用于治疗呼吸疾病和与TNF（肿瘤坏死因子）形成相关的疾病。 构成：提供由式（I）表示的吡啶2,3-d-吡啶甲醛肟衍生物或其药学上可接受的盐，其中R 1为C 1-3低级烷基，C 3-7环烷基，环烷氧基，环烷基氨基，环烷基低级烷基，C 1 -3低级烷氧基，甲酰基，羟基低级烷基或羧基烷基或X取代的苯基，其中X是甲基，乙基，丙基，异丙基，甲氧基，乙氧基，丙氧基，异丙氧基，氰基，羧酸，羧甲基酯，羧乙基酯， 硝基，氟或三氟甲基; R2是氢或甲基; R 3为氢，甲基，C 3-7低级烷氧基，烯丙基，苯基，苄基，X取代苯基，甲氧基苯基或甲氧基Y取代苯基，其中X为氰基，卤素，羧基烷基，硝基，甲基，三卤代甲基或烷氧基， Y为甲氧基。 制备式（I）的吡啶并[2,3-d]吡啶甲醛肟衍生物的方法包括在钯催化剂和碱的存在下由式（II）化合物制备式（III）化合物; 使式（III）的化合物与羟胺，烷氧基胺或其盐酸盐反应。
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公开(公告)号：KR100393523B1
公开(公告)日：2003-08-06
申请号：KR1020000002382
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: A pyrazolopyridine substituted cephalosporin compound is provided, which have the wide antimicrobial activity for gram positive and gram negative bacteria. And a producing method thereof is also provided. CONSTITUTION: The pyrazolopyridine substituted cephalosporin compound is represented by formula (1), in which R1 is hydrogen, C1 to C3 alkyl, C1 to C3 alkyl containing hydroxy, C1 to C3 alkyl containing amine; and R2 is hydrogen, amino, amino protected by amine protecting groups, carboxy or its inorganic salts, carbarmoyl, C1 to C3 alkyl substituted carbarmoyl, C1 to C3 alkyl containing hydroxy, and C1 to C3 alkyl esterified carboxy. The method for producing the pyrazolopyridine substituted cephalosporin compounds comprises the steps of: reacting the compounds of formula (2) and (3); and deprotecting R3 and R4, in which R3 is amine protecting groups, R4 is carboxylic acid protecting groups; and Y is halogen or acetoxy.
Abstract translation: 目的：提供吡唑并吡啶取代的头孢菌素化合物，其对革兰氏阳性和革兰氏阴性细菌具有广泛的抗微生物活性。 并且还提供了其制造方法。 组成：取代的头孢菌素化合物的吡唑并吡啶是由式（1）表示，其中R1是氢，C1-C3烷基，C1至C3烷基含羟基，C1至含胺C3烷基; 和R2是氢，氨基，被胺保护基团保护的氨基，羧基或其无机盐，氨基甲酰基，C1-C3烷基取代的氨基甲酰基，含有C1-C3烷基的羟基和C1-C3烷基酯化的羧基。 生产吡唑并吡啶取代的头孢菌素化合物的方法包括以下步骤：使式（2）和（3）的化合物反应; 并将R3和R4去保护，其中R3是胺保护基，R4是羧酸保护基; Y是卤素或乙酰氧基。
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Patent Agency Ranking
公开(公告)号：KR100393160B1
公开(公告)日：2003-07-31
申请号：KR1020010033382
申请日：2001-06-14
Applicant: 한국과학기술연구원
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: Novel pyrazolopyrimidinethione compounds of formula 1: wherein R1 and R2 are independently each hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, R3 is a C1-C6 alkyl group. C3-C6 cycloalkyl group or C3-C6 alkenyl group which is substituted or unsubstituted, X is O or NR4, and R4 is hydrogen atom, or a C1-C6 alkyl group, a C3-C6 cycloalkyl group or a C3-C6 alkenyl group which is unsubstituted or substituted with OH or an alkoxy group, pharmacologically acceptable salts or hydrates thereof, and preparation methods thereof are disclosed. Pharmaceutical compositions comprising the compounds are effectively used for the treatment of erectile dysfunction.
Abstract translation: 式1的新型吡唑并嘧啶硫酮化合物：其中R 1和R 2各自独立地为氢原子，C 1 -C 6烷基或C 3 -C 6环烷基，R 3为C 1 -C 6烷基。 C 3 -C 6环烷基或被取代或未被取代的C 3 -C 6烯基，X是O或NR 4，并且R 4是氢原子或C 1 -C 6烷基，C 3 -C 6环烷基或C 3 -C 6烯基 其未被取代或被OH或烷氧基取代，其药理学上可接受的盐或水合物及其制备方法。 包含这些化合物的药物组合物有效地用于治疗勃起功能障碍。
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公开(公告)号：KR100329808B1
公开(公告)日：2002-03-25
申请号：KR1020000001703
申请日：2000-01-14
Applicant: 한국과학기술연구원
IPC: C07D277/34
Abstract: 본 발명은 화학식 1을 갖는 2-펜아실리덴-3,5-알킬치환된-1,3-티아졸리딘-4-온을 효율적으로 제조하는 방법에 관한 것으로서, 그 반응은 반응식 1과 같다.
본 발명의 제조방법에 따르면, 상기 화학식 1의 화합물을 한 반응 용기 내에서, 그리고 보다 용이한 반응 조건 하에서 얻을 수 있다.-
公开(公告)号：KR1019950032220A
公开(公告)日：1995-12-20
申请号：KR1019950012400
申请日：1995-05-18
Applicant: 한국과학기술연구원
IPC: C07D501/46
Abstract: 본 발명은 그람 음성균 및 그람 양성균에 대해 폭넓은 항균력을 나타내며 여러 내성균에 대해서도 강한 항균력을 나타내는 일반식(I)로 표시되는 새로운 세팔로스포린 화합물, 이의 수화물, 이의 약리학적으로 허용가능한 염, 이의 제조방법 및 이의 제조에 사용되는 중간체 화합물에 관한것이다.
상기 일반식(I)에서 A, R
1 및 R
2 는 발명의 상세한 설명에서 정의한 바와 같다.-
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50.发明授权전압개폐 칼슘이온채널 억제 활성화능을 갖는 Ｎ-(피라졸릴메틸)아릴설폰아마이드 화합물 및 이를 포함하는 약학적 조성물 有权能够抑制电压门控钙离子通道的N-吡唑基甲基芳基磺酰胺化合物和包含其的药物组合物
公开(公告)号：KR101685993B1
公开(公告)日：2016-12-13
申请号：KR1020140058621
申请日：2014-05-15
Applicant: 한국과학기술연구원
IPC: C07D231/10 , C07D417/06 , A61K31/415
CPC classification number: C07D231/12 , C07D401/12 , C07D417/06 , C07D417/14
Abstract: 본발명은칼슘이온채널조절제로서유효한-(피라졸릴메틸)아릴설폰아마이드유도체및 이의약제학적으로허용가능한염, 그리고이 화합물이갖는칼슘이온채널억제효과에의한질환치료제로사용하는의약적용도에관한것이다.
Abstract translation: 本文公开了可用作钙离子通道阻断剂的N-（吡唑基甲基）芳基磺酰胺衍生物及其药学上可接受的盐，其药物用途为其钙离子通道阻断作用的治疗剂。
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