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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：KR100599882B1
公开(公告)日：2006-07-13
申请号：KR1020040041841
申请日：2004-06-08
Applicant: 한국과학기술연구원
CPC classification number: B01D53/8615
Abstract: 본 발명은 황화수소와 이산화황을 동시에 처리할 수 있는 고효율 탈황 방법에 관한 것으로, 본 발명의 탈황 방법은 반응가스 중에 함유된 이산화황을 1차적인 산화제로 이용하여 황화수소와 연속 반응시켜 이산화황과 대부분의 황화수소를 제거한 다음 나머지의 황화수소를 촉매 존재하에 산화제 가스에 의해 산화처리함으로써, 간단한 공정으로도, 특히 클라우스(Claus) 공정에서 배출된 3-5％의 황함유 테일(tail) 가스를 99％ 이상의 고효율로 처리할 수 있다.
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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-
35.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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Patent Agency Ranking
公开(公告)号：KR1020030065890A
公开(公告)日：2003-08-09
申请号：KR1020020005946
申请日：2002-02-01
Applicant: 한국과학기술연구원
IPC: C07D453/02
Abstract: PURPOSE: Provided are Quinuclidine compounds which are useful for treatment of brain-nervous diseases caused by cholinergic neurotransmission such as Alzheimer's disease and a preparation method thereof. CONSTITUTION: A quinuclidine compounds of the formula (I) and pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 1 to 5; R is a substituent on a benzene ring, hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-6 alkyl, 1,2 or 3 fluorine substituted C1-6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-6 alkenyl, 1,2 or 3 fluorine substituted C2-6 alkenyl, C2-6 alkynyl, 1,2 or 3 fluorine substituted C2-6 alkynyl, and C3-7 cycloalkyl. A method for preparing the quinuclidine compounds of the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III) or (IV), wherein R1 and R2 are independently C1-6 alkyl, aryl or arylalkyl.
Abstract translation: 目的：提供可用于治疗由胆碱能神经传递如阿尔茨海默病引起的脑神经疾病的奎宁环化合物及其制备方法。 构成：提供式（I）的奎宁环化合物及其药学上可接受的盐，其中n为1至5的整数; R是苯环上的取代基，氢，F，Cl，甲氧基，OH，NH2，NO2,3,4-二甲氧基，2,4-二甲氧基，氰基，C1-6烷基，1,2或3个氟取代的C1 -6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C2-6烯基，1,2或3个氟取代的C2-6烯基，C2-6炔基，1,2或3个氟取代的C2-6炔基，C3-7 环。 制备式（I）的奎宁环化合物的方法包括使式（II）的化合物与式（III）或（IV）的化合物反应，其中R 1和R 2独立地为C 1-6烷基，芳基或 芳。
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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：KR100373485B1
公开(公告)日：2003-02-25
申请号：KR1019990041612
申请日：1999-09-28
Applicant: 한국과학기술연구원
IPC: C07D295/22
Abstract: PURPOSE: Provided is a novel isooxazol piperazin derivative which is used as an antagonist against dopamine-1 receptor related to the central nerve system disorders. CONSTITUTION: A novel isooxazol piperazin derivative represented by the formula (1) is manufactured by reacting secondary amine of the formula (2) with aldehyde of the formula (3) in the presence of NaBh(OAc)3, NaBH3CN, or NaBH4 as a reductant and methylene chloride as a solvent at room temperature for 3-24 hours, preferably 12-14 hours. In the formula (1), n is an integer of between 1 and 4; R1 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen, trifluoromethyl, -NO2, alkyl group of C1-C3 , and alkoxy group of C1-C3, or an alkyl group of C1-C3, hydroxy group, 4-(2-keto-1-benzimidazolerynyl), 1-(2-(trifluoromethyl)benzene, 4-(4-chlorophenyl)-4-hydroxy, 1-(2-pyrimidyl), or 1-benzyl group; R2-R5 is hydrogen; R6 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen group, trifluoromethyl group , -CN, -NO2, an alkyl group of C1-C3, phenoxy group, and alkoxy group of C1-C3 and an unsaturated 5 or 6 hetero ring group having more than one atom from an alkyl group of C-C3, alkoxy group of C1-C3, thiophenyl group, (2-phenyl)vinyl group, pyridyl group, and from oxygen, sulfur, and nitrogen; and Q is isoxazol (A) or 4,5-dihydroisoxazole derivative (B).
Abstract translation: 用途：提供了一种新的异恶唑哌嗪衍生物，其用作针对与中枢神经系统疾病相关的多巴胺-1受体的拮抗剂。 结构式（1）表示的新型异恶唑哌嗪衍生物是通过使式（2）的仲胺与式（3）的醛在NaBh（OAc）3，NaBH3CN或NaBH4存在下反应制备的 还原剂和二氯甲烷作为溶剂在室温下反应3-24小时，优选12-14小时。 式（1）中，n为1〜4的整数， R 1是在卤素，三氟甲基，-NO 2，C 1 -C 3的烷基和C 1 -C 3的烷氧基中的多于一个基团取代的邻位，间位或对位的苯基，或者C1- C3-羟基，4-（2-酮-1-苯并咪唑基），1-（2-（三氟甲基）苯，4-（4-氯苯基）-4-羟基，1-（2-嘧啶基） 苄基; R 2 -R 5是氢; R 6是在卤素基团，三氟甲基，-CN，-NO 2，C 1 -C 3烷基，C 1 -C 3烷氧基， 苯氧基和C 1 -C 3的烷氧基以及具有超过一个来自C 1 -C 3的烷基，C 1 -C 3的烷氧基，噻吩基，（2-苯基）乙烯基的不饱和5或6个杂环基 ，吡啶基和氧，硫和氮;并且Q是异恶唑（A）或4,5-二氢异恶唑衍生物（B）。
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公开(公告)号：KR100362706B1
公开(公告)日：2002-12-11
申请号：KR1020000021258
申请日：2000-04-21
Applicant: 한국과학기술연구원
IPC: C07C209/32
Abstract: 본 발명은 인듐 금속을 이용하여 니트로기(-NO
2 )를 갖는 화합물을 아민(-NH
2 ) 화합물로 환원시키는 방법을 제공한다. 보다 구체적으로는 인듐 금속을 이용하여 화학식 1을 갖는 지방족 또는 방향족 화합물을 화학식 2의 화합물로 환원시키는 방법을 제공한다.
[화학식 1]
[화학식 2]
상기 화학식 1 및 2에서, R은 지방족 또는 방향족 화합물을 나타내며, n은 1-5의 정수, 바람직하게는 1-3의 정수, 가장 바람직하게는 1 또는 2이다.
인듐 금속을 이용한 본 발명의 환원 반응은 상온에서 짧은 시간 내에 진행될 뿐만 아니라 수개의 니트로기를 짧은 시간 내에 한번에 환원시킬 수 있다. 또한 분자내 다른 관능기에 영향을 미치지 아니하고 니트로기만 선택적으로 환원시킬 수 있으며, 수용액 상에서 반응이 쉽게 진행되므로 환경친화적 산업 공정이다는 장점을 가지고 있다. 따라서 화학 공업 분야에서 다양하게 응용될 수 있다.-
公开(公告)号：KR100309704B1
公开(公告)日：2001-09-29
申请号：KR1019990016355
申请日：1999-05-07
Applicant: 한국과학기술연구원
IPC: C07D499/00
CPC classification number: Y02P20/55
Abstract: 일반식(I')로표시되는 7-옥소세팔로스포린유도체를일반식(II)으로표시되는알릴할라이드또는일반식(III)으로표시되는아세틸렌할라이드와인듐또는아연금속존재하에용매와함께반응시켜신규한일반식(I)로표시되는세펨유도체및 이의제조방법에관한것으로, 이는베타-락타마제저해제및 항생제제조의중요한중간체로사용된다
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