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公开(公告)号：KR100441404B1
公开(公告)日：2004-07-23
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紊乱引起的脑神经疾病。 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是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 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。 用于制备式（I）的烯基氮杂双环化合物的方法包括式（II）的化合物与式（III）或式（IV）的化合物，其中R 1，R 2和R 3独立地为C 1 -C 6烷基 ，芳基或芳基烷基。
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公开(公告)号：KR1020040037686A
公开(公告)日：2004-05-07
申请号：KR1020020066268
申请日：2002-10-29
Applicant: 한국과학기술연구원
IPC: C07D413/10
CPC classification number: C07D413/10 , C07D413/14 , C07D417/14
Abstract: PURPOSE: Methylidene piperidinyl oxazolidinone derivatives and a preparation method thereof are provided, which compounds have improved antimicrobial activity, so that they can be useful for treatment of infection of pathogenic bacteria having resistance to conventional antibiotics. CONSTITUTION: Methylidene piperidinyl oxazolidinone derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof are provided, wherein X is oxygen or sulfur atom; R1 and R2 are independently hydrogen, cyano, alkyl, halogen, acetoxy, ethoxycarbonyl, hydroxy, hydroxyamino, methoxyimino, aminoethyl, or one or more hetero atom selected from oxygen, nitrogen and sulfur; and n is 1 or 2. The method for preparing the methylidene piperidinyl oxazolidinone derivatives of the formula(1) comprises reacting a compound of the formula(2) with a compound of the formula(3) in the presence of catalyst with or without organic solvent.
Abstract translation: 目的：提供亚甲基哌啶基恶唑烷酮衍生物及其制备方法，该化合物具有改善的抗微生物活性，因此它们可用于治疗对常规抗生素具有抗性的病原菌的感染。 构成：提供由式（1）表示的亚甲基哌啶恶唑烷酮衍生物或其药学上可接受的盐，其中X是氧或硫原子; R 1和R 2独立地是氢，氰基，烷基，卤素，乙酰氧基，乙氧基羰基，羟基，羟基氨基，甲氧基亚氨基，氨基乙基或一个或多个选自氧，氮和硫的杂原子; 并且n为1或2.制备式（1）的亚甲基哌啶基恶唑烷酮衍生物的方法包括使式（2）化合物与式（3）化合物在催化剂存在或不与有机物 溶剂。
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公开(公告)号：KR1020030063854A
公开(公告)日：2003-07-31
申请号：KR1020020004200
申请日：2002-01-24
Applicant: 한국과학기술연구원
IPC: C07D453/02 , C07D471/08 , C07D261/06
Abstract: PURPOSE: Azabicyclic compounds having an oxime moiety and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders including Alzheimer's disease. CONSTITUTION: An azabicyclic compounds having an oxime moiety represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; m is 0 or 1; and R is at least one substituent 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 atom substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine atom substituted C2-C6 alkynyl, C3-C7 cycloalkyl and aromatic atom group, in which the aromatic atom group is selected from phenyl, 2- or 3-thienyl, 2- or 3-puridyl, 2- or 3-pyrrolyl; and the substituent of the aromatic atom group is selected from the group consisting of Cl, Br, F, trifluoromethyl, NH2, NO2 and C1-C4 straight or branched chain alkyl.
Abstract translation: 目的：提供具有肟部分的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（包括阿尔茨海默氏病）引起的脑神经疾病。 构成：提供具有由式（I）表示的肟部分及其药学上可接受的盐的氮杂双环化合物，其中n为1或2; m为0或1; R为至少一个选自氢，F，Cl，甲氧基，OH，NH2，NO2,3,4-二甲氧基，2,4-二甲氧基，氰基，C1-C6烷基，1,2或 3个氟原子取代的C1-C6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C2-C6烯基，1,2或3个氟原子取代的C2-C6炔基，C3-C7环烷基和芳族原子基团，其中芳族原子团 选自苯基，2-或3-噻吩基，2-或3-取代基，2-或3-吡咯基; 芳基原子的取代基选自Cl，Br，F，三氟甲基，NH 2，NO 2和C 1 -C 4直链或支链烷基。
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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：KR100343948B1
公开(公告)日：2002-07-24
申请号：KR1019990050824
申请日：1999-11-16
Applicant: 한국과학기술연구원
IPC: C07D403/02
Abstract: 본발명은화학식 1을갖는이소옥사졸피페라진계열의화합물또는그의허용되는염 및그 제조방법과관한것으로, 상기화합물은아래의화학식 1을갖고, 그제조방법은아래의화학식 2의화합물과화학식 3의화합물을 1,3-쌍극자고리화첨가반응시키는것으로구성된다. 본발명은또한상기제조방법을용액상조합합성에응용하여제조된라이브러리에관한것이다. [화학식 1] [화학식 2] [화학식 3] 상기화학식 1, 2 및 3에서 R은 C-C의방향족탄화수소, C-C의알킬기에의해치환된 C-C의방향족탄화수소, C-C의알콕시기에의해치환된 C-C의방향족탄화수소, 할로겐에의해치환된 C-C의방향족탄화수소또는 C-C의아릴알킬이며; R-R는서로독립적으로수소, 할로겐, 메틸또는에틸이며; R-R은서로독립적으로수소, 할로겐에의해치환된페녹시, -OC(O)R, -NRR,,또는이며, 상기식 중 Y는 O 또는 S이고, R은 C-C의알킬기이고, R및 R은서로독립적으로 C-C의알킬기이고, R은수소, C-C의알킬기또는페닐이고, R는서로독립적으로수소또는 C-C의알킬기이고, n는 1-2의정수이고, k는 n=1이면 5, n=2이면 6이고, m은 n=1이면 4, n=2이면 5이다.
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Patent Agency Ranking
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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107.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：KR100333493B1
公开(公告)日：2002-04-25
申请号：KR1019990019242
申请日：1999-05-27
Applicant: 한국과학기술연구원
IPC: C07D413/14
Abstract: 일반식(II)로표시되는옥사졸리디논유도체와일반식(III)으로표시되는카르복실산유도체를활성화제, 염기및 용매존재하에아실화반응시켜 MRSA 균주를포함한그람양성균에우수한신규의일반식 (I)로표시되는이소옥사졸릴카르보닐옥사졸리디논유도체및 이의제조방법에관한것이다. 상기식들중, R은수소, 알킬, 브롬또는염소의할로겐, 시아노, 알콕시, 히드록시, 카르복시, 카르바모일, N,N'-디메틸카르바모일, 카르바모일옥시, 산소, 황, 질소원자를적어도한 개이상포함하고있는티오펜, 티아졸, 티아디아졸, 아미노티아졸, 이소티아졸, 이소옥사졸, 옥사졸, 옥사디아졸, 테트라졸, 피리딘의불포화 5환또는 6환헤테로고리치환체, 알킬, 할로겐, 알콕시, 시아노또는페녹시가치환된벤젠고리치환체, 약제학적으로허용되는염의메탄설폰산염, 퓨마렌산염, 브롬산염, 시트릭산염, 말레인산염, 인산염, 황산염, 나트륨염, 염산염또는염이아닌아민을포함한다.
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公开(公告)号：KR100264156B1
公开(公告)日：2001-11-22
申请号：KR1019980002915
申请日：1998-02-03
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: PURPOSE: Provided is (E)-prophenyl quaternary ammonium cephem compound and a pharmaceutically acceptable salt and a method for preparation thereof. The prepared compound has excellent antibacterial activity against both gram positive and gram negative strains, and is thus used for Cephalosporin based medicines. CONSTITUTION: (E)-prophenyl quaternary ammonium cephem compound is represented by the formula(1), wherein R1 is hydrogen, formyl, t-buthoxycarbonyl, benzyloxycarbonyl, p-nitrobenzyloxycarbonyl or trithyl; R2 is hydrogen, methyl, 2-fluoroethyl, formyl, chloroacetyl, benzoyl, p-nitrobenzyl, 2,2,2-trichloroethoxycarbonly, tetrahydropyranyl or trithyl; R3 is hydrogen, group forming carboxylic salt, 2,2,2-trichloroethyl, p-methoxybenzyl, p-nitrobenzyl, benzhydryl or t-butyl; R4 is methoxy, carbamoyl having substituent, or C5 hetero ring substituent represented by oxydiazole or triazole; and n is an integer of 1 or 2.
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公开(公告)号：KR1020010097299A
公开(公告)日：2001-11-08
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.
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