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公开(公告)号：KR100355343B1
公开(公告)日：2002-10-12
申请号：KR1019990050823
申请日：1999-11-16
Applicant: 한국과학기술연구원
IPC: C07D261/14
Abstract: 본발명은신규삼차아미노에틸이소옥사졸유도체및 그제조방법에관한것으로서, 상기이소옥사졸유도체는여러가지중추신경계장애와관련이있는도파민-1 수용체의길항제로서작용하며, 그구조는화학식 1과같다. [화학식 1] 그제조방법은아래의화학식 2의아민과화학식 3의토실레이트의치환반응을이용한것으로서, 그반응은반응식 1과같다. [화학식 2] [화학식 3] [반응식 1] 상기화학식 1, 2, 3 및반응식 1에서, R는페닐, 할로겐원자에의해치환된페닐, 트리플루오로메틸에의해치환된페닐, 페닐기의 2, 3 또는 4 위치에트리플루오로메틸에의해치환된페닐메틸, 디페닐메틸, 페닐기의 2, 3 또는 4 위치에할로겐원자에의해치환된디페닐메틸, 벤질, 3-히드로벤즈이미다졸-2-온이며; R내지 R는모두수소이며; R는니트로기, 페녹시기, 메톡시기, 트리플루오로메틸기및 할로겐기로구성되는군에서선택되는하나이상에의해치환된페닐, 페닐기에의해치환된비닐또는 O, S 및 N으로구성되는군에서선택되는한가지원자에의해치환된 5환또는 6환의불포화또는포화헤테로고리화합물이며; X는질소또는 C-H이다.
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公开(公告)号：KR100343947B1
公开(公告)日：2002-07-22
申请号：KR1019990041613
申请日：1999-09-28
Applicant: 한국과학기술연구원
IPC: C07D413/06
Abstract: 본발명은화학식 1을갖는이소옥사졸피페라진계열의화합물또는그 염의제조방법및 상기방법에의해만들어진라이브러리에관한것으로, 상기방법은화학식 2의화합물과화학식 3의화합물을염기및 염소화제의존재하에 1,3-쌍극자고리화첨가반응시켜화학식 1 또는그 염의화합물을제조하는것으로구성된다. 그화학식 1, 2, 3과반응식 1은다음과같다. 상기화학식 1, 2, 3과반응식 1에서, R및 R는페닐, 벤질, 할로겐화페닐, C-C의알킬기로치환된페닐, C-C의알콕시기로치환된페닐, (트리플루오로)메틸페닐, 피리딜등의페닐유도체를말하며, R-R는수소이며, X는질소이며,는이중결합또는삼중결합을의미하며,는이중결합또는단일결합을의미한다.
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13.发明公开도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效在DOPAMINE D3和D4受体上具有选择性生物活性的新的4,5-二羟基甲基丙烯酰胺衍生物及其制备方法
公开(公告)号：KR1020020043413A
公开(公告)日：2002-06-10
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: PURPOSE: Provided are novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity to dopamine D3 and D4 receptors, and their preparation method by reductive amination in the presence of reductant. CONSTITUTION: 4,5-dihydroisoxazolylalkylpiperazine derivative is represented by the formula(1), wherein R1, R2, R3, R4 and R5 are identical or different from each other, and represents individually hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C2-C6 alkenyl group, hydroxy group , hydroxymethyl group, aryl group, heteroaryl group, amino group, C1-C6 alkyl amino group, carbonyl group, C3-C8 cycloalkyl group, or C3-C8 heterocyclic group; R6 represents hydrogen atom, halogen atom, alkyl group, C1-C6 alkoxy group, aryl group, pyridyl group, heterocyclic group or pyrimidyl group; X represents CH or nitrogen atom; and n is 3 or 4.
Abstract translation: 目的：提供对多巴胺D3和D4受体具有选择性生物活性的新型4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下还原胺化的制备方法。 构成：4,5-二氢异恶唑基烷基哌嗪衍生物由式（1）表示，其中R 1，R 2，R 3，R 4和R 5彼此相同或不同，并且表示单独的氢原子，卤素原子，C1-C6烷基， C1-C6烷氧基，C2-C6烯基，羟基，羟甲基，芳基，杂芳基，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6表示氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基或嘧啶基; X表示CH或氮原子; n为3或4。
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公开(公告)号：KR1020010046868A
公开(公告)日：2001-06-15
申请号：KR1019990050823
申请日：1999-11-16
Applicant: 한국과학기술연구원
IPC: C07D261/14
Abstract: PURPOSE: A novel tertiary aminoethyl isooxazol derivative is provided, which acts as an antagonist of dopamine-1 receptor relating to various central nervous system disorders. And a method for preparing the same is also provided. CONSTITUTION: The tertiary aminoethyl isooxazol derivative is represented by the formula (1) and is prepared by dissolving a compound represented by the formula (2) and a compound represented by the formula (3) in a solvent to react them with each other in the presence of base. In the formulae 1-3, R1 is phenyl, phenyl substituted by halogen atom, phenyl substituted by trifluoromethyl, phenyl methyl having a trifluoromethyl substituent in 2, 3 or 4 position of the phenyl group, diphenylmethyl having a halogen atom substituent in 2, 3 or 4 position of the phenyl group, benzyl or 3-hydrobenzimidazole-2-one, each R2-R5 is hydrogen, R6 is phenyl substituted by at least one selected from the group consisting of nitro group, phynoxy group, methoxy group, trifluoromethyl group and halogen group, vinyl substituted by phenyl group or C5 or C6 unsaturated or saturated hetero cyclic compound substituted by O, S or N, and X is nitrogen or carbon.
Abstract translation: 目的：提供一种新的叔氨基乙基异恶唑衍生物，其作为与各种中枢神经系统疾病有关的多巴胺-1受体的拮抗剂。 还提供了制备该方法。 构成：叔氨基乙基异恶唑衍生物由式（1）表示，通过将式（2）表示的化合物和式（3）表示的化合物溶解在溶剂中，使其在 存在基地 式1-3中，R 1为苯基，被卤素原子取代的苯基，被三氟甲基取代的苯基，苯基2,3或4位中具有三氟甲基取代基的苯基甲基，2,3或4位的卤素原子取代基的二苯基甲基 或4位，苯基或3-氢苯并咪唑-2-酮，每个R 2 -R 5是氢，R 6是被选自硝基，环氧基，甲氧基，三氟甲基中的至少一个取代的苯基 卤素基，被苯基取代的乙烯基或被O，S或N取代的C5或C6不饱和或饱和杂环化合物，X是氮或碳。
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公开(公告)号：KR100843351B1
公开(公告)日：2008-07-03
申请号：KR1020070009626
申请日：2007-01-30
Applicant: 한국과학기술연구원 , 주식회사 디비하이텍
CPC classification number: A61K31/18
Abstract: An N-benzyl-N-(2-dimethylamino-ethyl)benzenesulfonamide compound is provided to show selective antagonistic activity on serotonin 5-HT2a or 5-HT2c receptor and have selective serotonin reuptake inhibitor(SSRI) activity, thereby being used for a pharmaceutical composition for treating and preventing central nervous system diseases. A pharmaceutical composition for treating and preventing diseases such as anxiety, depression, stroke, obsessive neurosis, psychosis, schizophrenia, suicidal tendency, sleep disorders, appetite disorders, withdrawal symptoms caused by drug abuse, and migraine comprises an N-benzyl-N-(2-dimethylamino-ethyl)benzenesulfonamide compound represented by a formula(1) or a pharmaceutically acceptable salt thereof. In the formula(1), R is H, halogen, hydroxy, C1-10 alkyl, C1-10 alkoxy, C1-10 haloalkyl, C1-10 haloalkoxy, C1-10 acyl, phenyl or phenyloxy, provided that a benzen-ring of the phenyl or the phenyloxy may be substituted by H, halogen, cyano, C1-10 alkyl or C1-10 alkoxy.
Abstract translation: 提供N-苄基-N-（2-二甲基氨基 - 乙基）苯磺酰胺化合物以显示对5-羟色胺5-HT2a或5-HT2c受体的选择性拮抗活性，并且具有选择性5-羟色胺再摄取抑制剂（SSRI）活性，从而用于药物 用于治疗和预防中枢神经系统疾病的组合物。 用于治疗和预防诸如焦虑，抑郁，中风，强迫神经症，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍，药物滥用引起的戒断症状和偏头痛等疾病的药物组合物包含N-苄基-N-（ 2-二甲基氨基 - 乙基）苯磺酰胺化合物或其药学上可接受的盐。 在式（1）中，R为H，卤素，羟基，C 1-10烷基，C 1-10烷氧基，C 1-10卤代烷基，C 1-10卤代烷氧基，C 1-10酰基，苯基或苯氧基，条件是苯环 的苯基或苯氧基可以被H，卤素，氰基，C 1-10烷基或C 1-10烷氧基取代。
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Patent Agency Ranking
公开(公告)号：KR100448002B1
公开(公告)日：2004-09-13
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：提供用于治疗由胆碱能神经传递引起的脑神经疾病如阿尔茨海默氏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是1至5的整数; R为苯环上的取代基，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炔基和C3-7 环。 用于制备式（I）奎宁环化合物的方法包括使式（II）化合物与式（III）或（IV）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：KR100418915B1
公开(公告)日：2004-02-14
申请号：KR1020000071399
申请日：2000-11-28
Applicant: 한국과학기술연구원
IPC: C07D401/04
Abstract: PURPOSE: A 4-aminopiperidine analogue and a producing method thereof are provided, therefore the compound can be useful as a ligand of a muscarine receptor, and it is thus used in study on Alzheimer disease. CONSTITUTION: The 4-aminopiperidine analogue is represented by formula(I), wherein R1, R2, R3, R4, R5, R6 and R7 are hydrogen, cycloalkyl having carbon number of 1 to 6, alkoxy, halogen, hydroxy, hydroxymethyl, aryl, heteroaryl, amino, alkylamino, alkenyl, carbonyl or hetero ring having carbon number of 5 to 7 wherein aryl is a ring having 6 atoms, two rings having 10 atoms or a stable resonance form having double bond to adjacent carbon; heteroaryl is a single ring aromatic group having carbon number of 5 to 6 or a double ring aromatic group having carbon number of 10 in which the heteroaryl has at least one hetero atom of N, O or S; hetero ring consists of 5 to 7 atoms having 1 to 3 of N, O or S; X is carbon or sulfur; and n is an integer of 1 to 2 wherein n is 1 when X is carbon and is 2 when X is sulfur. The 4-aminopiperidine analogue is produced by reacting piperidine or amine(II) with piperazine with ketone(III) in the presence of 1 to 3 equivalent of acetic acid, 2 to 10 equivalent of reducing agent and solvent at room temperature for 3 to 24 hours to produce 4-aminopiperidine(I) and adding NaHCO3 solution and organic solvent to 4-aminopiperidine(I); and drying the extracted 4-aminopiperidine(I), dissolving it, adding 1 to 10 equivalent of hydrogen chloride to the solution, and separating, washing and drying the hydrochloride of 4-aminopiperidine.
Abstract translation: 目的：提供了4-氨基哌啶类似物及其生产方法，因此该化合物可用作毒蕈碱受体的配体，因此用于研究阿尔茨海默病。 构成：4-氨基哌啶类似物由式（I）表示，其中R1，R2，R3，R4，R5，R6和R7是氢，碳数为1-6的环烷基，烷氧基，卤素，羟基，羟甲基，芳基 杂芳基，氨基，烷基氨基，链烯基，羰基或杂环，其中芳基是具有6个原子的环，具有10个原子的两个环或具有与相邻碳双键的稳定的共振形式; 杂芳基为碳数为5至6的单环芳族基团或碳数为10的双环芳族基团，其中杂芳基具有至少一个N，O或S的杂原子; 杂环由5至7个具有1至3个N，O或S的原子组成; X是碳或硫; 并且n是1至2的整数，其中当X是碳时，n是1，当X是硫时，n是2。 4-氨基哌啶类似物是通过使哌啶或胺（II）与哌嗪与酮（III）在1至3当量乙酸，2至10当量还原剂和溶剂的存在下在室温下反应3至24 小时以产生4-氨基哌啶（I）并将NaHCO 3溶液和有机溶剂加入到4-氨基哌啶（I）中; 干燥提取的4-氨基哌啶（I），溶解，加入1至10当量的氯化氢至溶液中，分离，洗涤并干燥4-氨基哌啶的盐酸盐。
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18.发明授权도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效도파민D3및D4체택적택적택적규규,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5-규규규규규규규규규규규규규규규규규규규규
公开(公告)号：KR100394083B1
公开(公告)日：2003-08-06
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent,wherein R1, R2, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3和D4受体具有选择性生物活性的4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。
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公开(公告)号：KR1020030063853A
公开(公告)日：2003-07-31
申请号：KR1020020004199
申请日：2002-01-24
Applicant: 한국과학기술연구원
IPC: C07D453/02 , C07D471/08 , C07D261/06
Abstract: PURPOSE: An alkenyl azabicyclic compound and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders. CONSTITUTION: An alkenyl azabicyclic compound represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; and R is selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine substituted C2-C6 alkynyl and C3-C7 cyloalkyl. A method for preparing the alkenyl azabicyclic compound of the formula(I) comprises a compound of the formula(II) with a compound of the formula(III) or formula(IV), wherein R1, R2 and R3 are independently C1-C6 alkyl, aryl or arylalkyl.
Abstract translation: 目的：提供一种烯基氮杂双环化合物及其制备方法，其可用于治疗由胆碱神经传递障碍引起的脑神经疾病。 构成：提供由式（I）表示的烯基氮杂双环化合物及其药学上可接受的盐，其中n为1或2; 并且R选自氢，F，Cl，甲氧基，OH，NH 2，NO 2，3,4-二甲氧基，2,4-二甲氧基，氰基，C 1 -C 6烷基，1,2或3个氟取代的C 1 C 1-6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C 2 -C 6烯基，1,2或3个氟取代的C 2 -C 6炔基和C 3 -C 7环烷基。 制备式（I）的烯基氮杂双环化合物的方法包括式（II）化合物与式（III）或式（IV）化合物，其中R 1，R 2和R 3独立地为C 1 -C 6烷基 ，芳基或芳烷基。
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公开(公告)号：KR100394086B1
公开(公告)日：2003-08-06
申请号：KR1020000073121
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08 , C07D413/14
Abstract: The present invention relates to a novel isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, R3, R4, R5, R6, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3或D4受体具有选择性生物活性的新型异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2，R3， R4，R5，R6，X和n与说明书中的定义相同。
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