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61. 发明授权

KR100432283B1 무스카린성 아세틸콜린 수용체에 작용하는테트라하이드로피리딘 유도체 失效
标题翻译： 무스카린성아세틸콜린수용체체에용하는테트라하이드로피리딘유도체
公开(公告)号：KR100432283B1
公开(公告)日：2004-05-22
申请号：KR1020010066568
申请日：2001-10-27
申请人： 한국과학기술연구원
发明人： 김유승 , 강순방 , 금교창 , 장민석 , 공재양 , 정대영
IPC分类号： C07D401/06 , A61K31/435 , A61K31/40
CPC分类号： C07D401/06
摘要： The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, wherein m is 0 or 1, n is 1 or 2, R1 is hydrogen, C1-4 alkyl, C2-4 alkynyl or aryl, R3 is C1-4 alkyl, which show high efficacy, low cholinergic adverse effects and high affinity for muscarinic acetylcholine receptor; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.
摘要翻译：本发明涉及具有适当取代的吡咯烷酮和肟的式1的四氢吡啶衍生物，其中m为0或1，n为1或2，R 1为氢，C 1-4烷基，C 2-4炔基或芳基，R 3为它表现出高效力，低胆碱能不良作用和对毒蕈碱乙酰胆碱受体的高亲和力; 和其药学上可接受的盐; 其制备方法; 和包含这些化合物或盐的药物组合物。

62. 发明公开

KR1020030063854A 신규한 옥심계 아자 두 고리 화합물 및 그 제조방법 失效
标题翻译：含氧化合物的亚甲基化合物及其制备方法
公开(公告)号：KR1020030063854A
公开(公告)日：2003-07-31
申请号：KR1020020004200
申请日：2002-01-24
申请人： 한국과학기술연구원
发明人： 고훈영 , 최경일 , 조용서 , 배애님 , 차주환 , 공재양 , 정대영
IPC分类号： C07D453/02 , C07D471/08 , C07D261/06
摘要： 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.
摘要翻译：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。

63. 发明授权

KR100355343B1 신규 삼차아미노에틸 이소옥사졸 유도체 및 그 제조 방법 失效
标题翻译：新型叔胺 - 氨基四唑衍生物及其制备方法
公开(公告)号：KR100355343B1
公开(公告)日：2002-10-12
申请号：KR1019990050823
申请日：1999-11-16
申请人： 한국과학기술연구원
发明人： 고훈영 , 조용서 , 최경일 , 배애님 , 강경호 , 이희윤 , 공재양 , 정대영
IPC分类号： C07D261/14
摘要： 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.

64. 发明授权

KR100343947B1 이소옥사졸 피페라진 계열의 화합물의 제조방법 및 그것에 의해 제조된 라이브러리 失效
标题翻译：用于制备具有异噻唑啉哌嗪类化合物及其文库的化合物的方法
公开(公告)号：KR100343947B1
公开(公告)日：2002-07-22
申请号：KR1019990041613
申请日：1999-09-28
申请人： 한국과학기술연구원
发明人： 고훈영 , 조용서 , 최경일 , 배애님 , 강경호 , 이지은 , 이희윤 , 공재양 , 정대영 , 정선호
IPC分类号： C07D413/06
摘要： 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.

65. 发明公开

KR1020010046868A 신규 삼차아미노에틸 이소옥사졸 유도체 및 그 제조 방법 失效
标题翻译：新型仲胺基异丙醇衍生物及其制备方法
公开(公告)号：KR1020010046868A
公开(公告)日：2001-06-15
申请号：KR1019990050823
申请日：1999-11-16
申请人： 한국과학기술연구원
发明人： 고훈영 , 조용서 , 최경일 , 배애님 , 강경호 , 이희윤 , 공재양 , 정대영
IPC分类号： C07D261/14
摘要： 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.
摘要翻译：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。

66. 发明公开

KR1020030034823A 아세틸콜린 수용체에 작용하는 이소옥사졸 또는이소옥사졸린 치환된 1,2,5,6-테트라하이드로피리딘 유도체 失效
标题翻译：取代异丙唑或异辛唑取代具有高亲和性的乙酰胆碱受体的1,2,5,6-四氢吡啶衍生物
公开(公告)号：KR1020030034823A
公开(公告)日：2003-05-09
申请号：KR1020010066579
申请日：2001-10-27
申请人： 한국과학기술연구원
发明人： 김유승 , 강순방 , 금교창 , 장민석 , 장택수 , 공재양 , 정대영
IPC分类号： C07D413/04
摘要： PURPOSE: Isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative having high affinity for an acetylcholine receiptor is provided, which compound is useful as a muscarine type acetylcholine receiptor agonist, a recognition improving agent and a treating agent of cerebral nervous disease such as Alzheimer's disease. CONSTITUTION: The isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula(1) and a pharmaceutically acceptable salt thereof are provided, wherein R2 is C1-4 alkyl; one of R3 and R4 is one functional group in claim 1 and another of them is H; R5 is hydrogen, hydroxy, hydroxy C1-6 alkyl, C1-6 alkoxymethyl, C1-6 alkoxy, acetoxy, C1-4 alkyl ester, nitrile, aryl, phenylthio, methylthiomethyl, phenylsulfoxide, dimethylthiomethyl, C1-4 alkylketo, C1-4 alkylketo oxime, C1-4 alkylketo C1-5 alkyl oxime, and N-pyrrolidine-2-on; R6 is hydrogen; and R5 and F6 form -CH2OCH2 together. The process for preparing the isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula comprises the steps of: reacting 3- or 4-pyridine aldehyde oxime compound of formula(2) with chlorox to prepare nitrile oxide of formula(4); and cycloadddition reaction of nitrile oxide of formula(4) with alkene or alkyne compound of formula(8) or formula(9) to prepare a compound of formula(5) or formula(6); reacting the compound of formula(5) or formula(6) with alkyl iodide to prepare alkyl pyridine salt of formula(7); and reducing the alkyl pyridine salt of formula(7).
摘要翻译：目的：提供对乙酰胆碱受体具有高亲和力的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物，该化合物可用作毒蕈碱型乙酰胆碱受体激动剂，识别改善剂和脑神经系统疾病的治疗剂如阿尔茨海默病。构成：提供由式（1）表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物及其药学上可接受的盐，其中R 2为C 1-4烷基; R3和R4之一是权利要求1中的一个官能团，另一个是H; R5是氢，羟基，羟基C1-6烷基，C1-6烷氧基甲基，C1-6烷氧基，乙酰氧基，C1-4烷基酯，腈，芳基，苯硫基，甲硫基甲基，苯基亚砜，二甲硫甲基，C1-4烷基酮，C1-4 烷基酮肟，C 1-4烷基酮C 1-5烷基肟和N-吡咯烷-2-酮; R6是氢; R5和F6一起形成-CH 2 OCH 2。制备由式表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物的方法包括以下步骤：使式（2）的3-或4-吡啶醛肟化合物与氯氧反应制备式（4）; 和式（4）的氧化腈与式（8）或式（9）的烯烃或炔化合物的环加成反应以制备式（5）或式（6）的化合物; 使式（5）或式（6）的化合物与烷基碘反应制备式（7）的烷基吡啶盐; 和还原式（7）的烷基吡啶盐。

67. 发明公开

KR1020030034822A 피롤리디논 유도체, 이의 제조 방법 및 이를 포함하는제약 조성물 失效
标题翻译：吡咯烷酮衍生物，其制备方法及其含有的药物组合物
公开(公告)号：KR1020030034822A
公开(公告)日：2003-05-09
申请号：KR1020010066578
申请日：2001-10-27
申请人： 한국과학기술연구원
发明人： 김유승 , 강순방 , 금교창 , 장민석 , 공재양 , 정대영
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： PURPOSE: Pyrrolidone derivative, a preparation process thereof and a pharmaceutical composition containing the same are provided, which pyrrolidone derivatives are useful as a muscarine type acetylcholine receiptor agonist, a recognition improving agent and a treating agent of cerebral nervous disease such as Alzheimer's disease. CONSTITUTION: The pyrrolidone derivative represented by formula(1) and a pharmaceutically acceptable salt thereof are provided, wherein n is 0 or 1; Aza is C1-4 alkyl substituted or unsubstituted heterocycle, or heterocycle substituted C1-4 alkyl; and heterocycle is hetero atom and saturated or unsaturated 5-membered ring or 5-membered ring containing nitrogen. The process for preparing the pyrrolidone derivative of formula(1) comprises the steps of: reacting azacyclo aldehyde oxime compound of formula(2) with chlorox to prepare nitrile oxide of formula(4); and cycloadddition reaction of nitrile oxide of formula(4) with pyrrolidone containing alkene or alkyne compound of formula(5).
摘要翻译：目的：提供吡咯烷酮衍生物及其制备方法和含有该吡咯烷酮衍生物的药物组合物，该吡咯烷酮衍生物可用作毒蕈碱型乙酰胆碱受体激动剂，识别改善剂和脑神经疾病如阿尔茨海默病的治疗剂。构成：提供由式（1）表示的吡咯烷酮衍生物及其药学上可接受的盐，其中n为0或1; 氮杂是C 1-4烷基取代或未取代的杂环，或杂环取代的C 1-4烷基; 杂环是杂原子和含氮的饱和或不饱和的5元环或5元环。制备式（1）的吡咯烷酮衍生物的方法包括以下步骤：使式（2）的唑烷酮肟化合物与氯氧化反应制备式（4）的氧化腈; 和式（4）的氧化腈与含有式（5）的烯烃或炔化合物的吡咯烷酮的环加成反应。

68. 发明公开

KR1020020041711A 4-아미노피페리딘 유도체 및 그의 제조방법 失效
标题翻译： 4-氨基哌啶类似物及其制备方法
公开(公告)号：KR1020020041711A
公开(公告)日：2002-06-03
申请号：KR1020000071399
申请日：2000-11-28
申请人： 한국과학기술연구원
发明人： 고훈영 , 조용서 , 최경일 , 배애님 , 강경호 , 이희윤 , 손정훈 , 공재양 , 정대영
IPC分类号： C07D401/04
摘要： 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.
摘要翻译：目的：提供4-氨基哌啶类似物及其制备方法，因此该化合物可用作毒蕈碱受体的配体，因此用于阿尔茨海默病的研究。构成：4-氨基哌啶类似物由式（I）表示，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7为氢，碳数为1至6的环烷基，烷氧基，卤素，羟基，羟甲基，芳基碳原子数为5〜7的杂芳基，氨基，烷基氨基，烯基，羰基或杂环，其中芳基为6原子的环，2个环为10个原子或具有与相邻碳原子双键的稳定共振形式; 杂芳基是碳数为5至6的单环芳基或碳数为10的双环芳基，其中杂芳基具有至少一个杂原子为N，O或S; 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; n为1〜2的整数，X为碳时n为1，X为硫时为2。 4-氨基哌啶类似物通过哌啶或胺（II）与哌嗪与酮（III）在1至3当量的乙酸，2至10当量的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; 并将提取的4-氨基哌啶（I）干燥，溶解，向溶液中加入1〜10当量的氯化氢，分离，洗涤和干燥4-氨基哌啶的盐酸盐。

69. 发明公开

KR1020010029025A 이소옥사졸 피페라진 계열의 화합물의 제조방법 및 그것에 의해 제조된 라이브러리 失效
标题翻译：制造ISO-OXAZOLE PIPERAZIN化合物的方法及其制造方法
公开(公告)号：KR1020010029025A
公开(公告)日：2001-04-06
申请号：KR1019990041613
申请日：1999-09-28
申请人： 한국과학기술연구원
发明人： 고훈영 , 조용서 , 최경일 , 배애님 , 강경호 , 이지은 , 이희윤 , 공재양 , 정대영 , 정선호
IPC分类号： C07D413/06
摘要： PURPOSE: Provided is a method for manufacturing an iso-oxazole piperazin compound and its salts which can end up developing a lead compound for new drugs. CONSTITUTION: An isooxazol compound is manufactured by the next step: reacting the compound of the formula (2) with the compound of the formula (3) at room temperature, at 0-7 deg.C, in the presence of organic solvent, 0.1-2 equivalent, preferably 1 equivalent of base, and chlorinating agent for 30 minutes-4 hours, preferably 2 hours. Wherein, organic solvent is selected from benzene, methylene chloride, and tetrahydrofuran; a base is selected from methyl amine, ethyl amine, diethyl amine, dimethyl amine, trimethyl amine, cyclohexylamine, diethylisopropylamine, pyridine, or preferably triethylamine; And chlorinating agent is one of chlorine, N-chlorosuccinimide, and sodium hypochlorite. In the formula (1), (2), and (3), R1 and R6 are a phenyl group, benzyl group, halide phenyl group, phenyl group having substituted C1-C6 alkyl group, phenyl group having substituted C1-C6 alkoxy group, methyl phenyl group, or pyridyl group. R2-R5 is hydrogen, and X is nitrogen.
摘要翻译：目的：提供一种制造异恶唑哌嗪化合物及其盐的方法，其可以最终形成用于新药的铅化合物。构成：通过下一步骤制备异恶唑化合物：在室温，0-7℃，有机溶剂存在下，将式（2）化合物与式（3）化合物反应，得到0.1 -2当量，优选1当量碱和氯化剂30分钟-4小时，优选2小时。其中有机溶剂选自苯，二氯甲烷和四氢呋喃; 碱选自甲胺，乙胺，二乙胺，二甲胺，三甲胺，环己胺，二乙基异丙胺，吡啶，或优选三乙胺; 而氯化剂是氯，N-氯代琥珀酰亚胺和次氯酸钠之一。在式（1），（2）和（3）中，R 1和R 6是苯基，苄基，卤化苯基，具有取代的C 1 -C 6烷基的苯基，具有取代的C 1 -C 6烷氧基的苯基，甲基苯基或吡啶基。 R2-R5是氢，X是氮。

70. 发明授权

KR100264158B1 [(아릴)이소옥소졸릴]메틸렌-아자비시클로 화합물 및 이의 제조방법 失效
标题翻译： [（ARYL）ISOXAZOLYL]甲基 - 亚甲基化合物及其制备方法
公开(公告)号：KR100264158B1
公开(公告)日：2000-08-16
申请号：KR1019980023118
申请日：1998-06-19
申请人： 한국과학기술연구원
发明人： 고훈영 , 장문호 , 김유승 , 최경일 , 조용서 , 배애님 , 차주환 , 공재양 , 천혜경 , 정대영
IPC分类号： C07D453/00 , C07D261/20
摘要： 일반식 (II)로 표시되는 카르보닐 화합물을 용매와 염기 존재하에 일반식 (III)으로 표시되는 포스포늄염 화합물이나 또는 일반식 (IV)로 표시되는 포스포네이트 화합물과 반응시켜 새로운 일반식 (I)로 표시되는 [(아릴)이소옥소졸릴]메틸렌-아자비시클로 화합물을 제조하는 것으로, 본 발명 화합물은 무스카린성 아세틸콜린 수용체에 높은 결합 친화도를 나타내므로 알쯔하이머씨 병 등의 뇌신경 질환 치료제로 유용하다.

상기 식들에서, R은 각각 수소, 할로, 알콕시, 시아노, 알킬, 알케닐, 알키닐, 히드록시, 아미노, 니트로, 4-메톡시벤질옥시, 3급-부톡시카르보닐아미노 또는 약제학적으로 가능한 염을, R
1 ,R
2 및R
R 는 각각 알킬, 아릴 또는 아랄킬을, X는 할로겐 원자를 각각 표시하며, n은 1 또는 2의 정수이다.

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