公开(公告)号：KR1020040008856A

公开(公告)日：2004-01-31

申请号：KR1020020042579

申请日：2002-07-19

Applicant: 한국화학연구원

Inventor： 박노상 ,  정영식 ,  성철민 ,  임희종 ,  윤중호 ,  공재양 ,  박우규

IPC: C07D409/12

Abstract: PURPOSE: Phenylamidine derivatives having anti-oxidant activity and a pharmaceutical composition containing the same are provided. The compounds have improved anti-oxidant activity and lower toxicity. CONSTITUTION: Phenylamidine derivatives are characterized by the formula 1, wherein X1 and X2 are independently hydrogen, or linear or branched chain alkyl having C1-C9 saturated or unsaturated carbon; Y is CH2 or CH=CH(C=O); and Ar is phenyl, thiopen or pyrrole. An anti-oxidant is characterized by containing the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof. The pharmaceutical composition for prevention of aging and treatment of cancer, diabetes, epilepsy, apoplexy, Parkinson's disease, Huntington's disease and dementia contains the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof.

Abstract translation: 目的：提供具有抗氧化活性的苯脒衍生物和含有它们的药物组合物。 该化合物具有改善的抗氧化活性和较低的毒性。 构成：苯基脒衍生物的特征在于式1，其中X 1和X 2独立地是氢，或具有C 1 -C 9饱和或不饱和碳的直链或支链烷基; Y是CH 2或CH = CH（C = O）; 和Ar是苯基，噻吩或吡咯。 抗氧化剂的特征在于含有式1的苯基脒衍生物及其药学上可接受的盐。 用于预防癌症，糖尿病，癫痫，中风，帕金森病，亨廷顿病和痴呆的衰老和治疗的药物组合物含有式1的苯基脒衍生物及其药学上可接受的盐。

公开(公告)号：KR1020030042586A

公开(公告)日：2003-06-02

申请号：KR1020010073301

申请日：2001-11-23

Applicant: 한국화학연구원

Inventor： 박노상 ,  정영식 ,  성철민 ,  임희종 ,  조향옥 ,  공재양 ,  박우규

IPC: C07C237/20

Abstract: PURPOSE: A 4-hydroxycinnamamide derivative, pharmaceutically acceptable salt thereof and preparation thereof are provided. A pharmaceutical composition containing them as an active ingredient for use in anti-aging, and treating cancers, diabetes, epilepsy and neurodegenerative diseases is also provided. CONSTITUTION: The 4-hydroxycinnamamide derivative has the formula 1, wherein each of X1 and X2 is independently hydrogen or a C1-C15 saturated or unsaturated, linear or branched alkyl group; each of Y1, Y2, Y3 and Y4 is independently hydrogen, halogen, hydroxy group, amino group, phenyl group, C1-C8 alkyl group or C1-C8 alkoxy group; and n is an integer between 0 and 9. The 4-hydroxycinnamamide derivative and pharmaceutically acceptable salt thereof have excellent anti-oxidant activity and low toxicity compared to other conventional anti-oxidants.

Abstract translation: 目的：提供4-羟基肉桂酰胺衍生物，其药学上可接受的盐及其制备方法。 还提供含有它们作为用于抗衰老的活性成分以及治疗癌症，糖尿病，癫痫和神经变性疾病的药物组合物。 构成：4-羟基肉桂酰胺衍生物具有式1，其中X1和X2各自独立地为氢或C1-C15饱和或不饱和的直链或支链烷基; Y1，Y2，Y3和Y4各自独立地为氢，卤素，羟基，氨基，苯基，C1-C8烷基或C1-C8烷氧基; n为0〜9的整数。与其它常规抗氧化剂相比，4-羟基肉桂酰胺衍生物及其药学上可接受的盐具有优异的抗氧化活性和低毒性。

公开(公告)号：KR1020020043413A

公开(公告)日：2002-06-10

申请号：KR1020000073122

申请日：2000-12-04

Applicant: 한국과학기술연구원 ,  한국과학기술원 ,  한국화학연구원 ,  학교법인 성신학원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  공재양 ,  정대영 ,  정선호 ,  정지영 ,  이희윤

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。

公开(公告)号：KR1020020040160A

公开(公告)日：2002-05-30

申请号：KR1020000070105

申请日：2000-11-23

Applicant: 한국화학연구원

Inventor： 박노상 ,  정영식 ,  성철민 ,  임희종 ,  조보영 ,  공재양

IPC: C07C50/26

Abstract: PURPOSE: Provided is a quinone compound having excellent antioxidant activity, which can be used for preventing aging and curing cancer, diabetes, epilepsy, imbecility, Parkinson's disease, and etc. CONSTITUTION: The quinone compound is represented by the formula 1 and produced from a compound represented by the formula 3, wherein R1 and R2 are independently methyl or methoxy or R1 and R2 are connectively -CH=CH-CH=CH-, R3 is -NH-(CH2)m-R5, -CO2R6, -OH, and etc., R5 is methyl, phenyl, benzyl, and etc., R6 is hydrogen atom or C1-C4 alkyl, X is CH2 or C=O, and n and m are each 0 or an integer of 1-10.

Abstract translation: 目的：提供具有优异抗氧化活性的醌化合物，其可用于预防老化和治愈癌症，糖尿病，癫痫，不育，帕金森病等。构成：醌化合物由式1表示并由 由式3表示的化合物，其中R 1和R 2独立地是甲基或甲氧基或R 1和R 2连接地是-CH = CH-CH = CH-，R 3是-NH-（CH 2）m -R 5，-CO 2 R 6，-OH， R 5是甲基，苯基，苄基等，R 6是氢原子或C 1 -C 4烷基，X是CH 2或C = O，n和m各自为0或1-10的整数。

公开(公告)号：KR1020020017137A

公开(公告)日：2002-03-07

申请号：KR1020000050262

申请日：2000-08-29

Applicant: 한국화학연구원

Inventor： 정명희 ,  이미정 ,  공재양

IPC: C07D417/14

Abstract: PURPOSE: Provided are 5-(4-Substituted-(1,2,5)thiadiazole-3-yl)-3-methyl-1,2,3,4-tetrahydropyrimidine derivatives which are a muscarinic receptor agonists and used as therapeutic agents in Alzheimer's disease. Also, provided are their pharmaceutically acceptable salt, their preparation process and their use. CONSTITUTION: 5-(4-Substituted-(1,2,5)thiadiazole-3-yl)-3-methyl-1,2,3,4-tetrahydropyrimidine derivatives are represented by the formula(1), wherein X represents dialkylamine group, piperidinyl group, morpholinyl group or N-methylpiperazinyl group. They are as follows: 3-dimethyl-(4-(3-methyl-1,2,3,4-tetrahydropyrimidine-5-yl)-(1,2,5)thiadiazole-3-yl)amine; 3-methyl-5-(4-pyrrolidine-1-yl-(1,2,5)thiadiazole-3-yl)-1,2,3,4-tetrahydropyrimidine; 3-methyl-5-(4-piperidine-1-yl-(1,2,5)thiazol-3-yl)-1,2,3,4-tetrahydropyrimidine; 4-(4-(3-methyl-1,2,3,4-tetrahydropyrimidine-5-yl)-(1,2,5)thiadiazole-3-yl)morpholine or 3-methyl-5-(4-(4-methylpiperazin-1-yl)-(1,2,5)thiadiazole-3-yl)-1,2,3,4-tetrahydropyrimidine. The therapeutic agent in Alzheimer's disease contains 5-(4-Substituted-(1,2,5)thiadiazole-3-yl)-3-methyl-1,2,3,4-tetrahydropyrimidine derivative or its pharmaceutically acceptable salt.

Abstract translation: 目的：提供作为毒蕈碱受体激动剂并用作治疗剂的5-（4-取代 - （1,2,5）噻二唑-3-基）-3-甲基-1,2,3,4-四氢嘧啶衍生物 在阿尔茨海默病。 此外，还提供其药学上可接受的盐，其制备方法及其用途。 构成：5-（4-取代的 - （1,2,5）噻二唑-3-基）-3-甲基-1,2,3,4-四氢嘧啶衍生物由式（1）表示，其中X表示二烷基胺 哌啶基，吗啉基或N-甲基哌嗪基。 它们如下：3-二甲基 - （4-（3-甲基-1,2,3,4-四氢嘧啶-5-基） - （1,2,5）噻二唑-3-基）胺; 3-甲基-5-（4-吡咯烷-1-基 - （1,2,5-）噻二唑-3-基）-1,2,3,4-四氢嘧啶; 3-甲基-5-（4-哌啶-1-基 - （1,2,5）噻唑-3-基）-1,2,3,4-四氢嘧啶; 4-（4-（3-甲基-1,2,3,4-四氢嘧啶-5-基） - （1,2,5）噻二唑-3-基）吗啉或3-甲基-5-（4-（ 4-甲基哌嗪-1-基） - （1,2,5-）噻二唑-3-基）-1,2,3,4-四氢嘧啶。 阿尔茨海默病中的治疗剂含有5-（4-取代 - （1,2,5）噻二唑-3-基）-3-甲基-1,2,3,4-四氢嘧啶衍生物或其药学上可接受的盐。

公开(公告)号：KR100274004B1

公开(公告)日：2000-12-15

申请号：KR1019980006274

申请日：1998-02-26

Applicant: 한국화학연구원

Inventor： 박노상 ,  성철민 ,  정영식 ,  이창우 ,  민충식 ,  이종철 ,  공재양 ,  박우규

IPC: C07D215/233

Abstract: PURPOSE: Provided are the novel NMDA receptor antagonist, 4-(3-substituted-propyloxy)-quinoline-2-carboxylic acid derivatives and the preparation method thereof. CONSTITUTION: The derivatives are represented as shown in the chemical formula 1, where A represents carbamate, amide, thiourea, sulfonylurea, acylthiourea, thiocarbamate, amidine, guanidine, imidate, thioimidate, phosphorylamide, sulfonamide, sulfonthiourea or amines and R represents alkyl (C1¯C20), aryl (C6¯C12), aralkyl, heterocycles, carbocycles (C3¯C14), fused bicyclic, hydrogen or cyano groups. The synthetic process comprises the steps of alkylating 5,7-dichlorokynurenic acid methylester with 1,3-dibromopropane; substitution of the bromine with NaN3 to make azidomine; reducing the resultant to amine compound with Pd-catalyst; converting to amide with the corresponding isocyanate, thioisocyanate or acid chloride and finally hydrolysing the ester group in the parent moiety to make the compound of formula 1. They are strong and unique antagonist acting on the coupling position of the strychnine non-susceptive glycine in the NMDA receptor complex and penetrate effectively into central nervous system. They are effective in the treatment of neurodegeneration, especially useful for the CNS damages effected by the diseases such as heart attack, low blood sugar, local anemia and heart beat halt arising from the low oxygen concentration caused by the external wounds or anemia.

Abstract translation: 目的：提供新型NMDA受体拮抗剂4-（3-取代 - 丙氧基） - 喹啉-2-羧酸衍生物及其制备方法。 构成：衍生物如化学式1所示，其中A表示氨基甲酸酯，酰胺，硫脲，磺酰脲，酰基硫脲，硫代氨基甲酸酯，脒，胍，亚氨酸酯，硫代亚氨酸酯，磷酰胺，磺酰胺，磺酰硫脲或胺，R代表烷基 C 20），芳基（C 6 -C 12），芳烷基，杂环，碳环（C 3 -C 14），稠合双环，氢或氰基。 该合成方法包括使5,7-二氯喹诺酮酸甲酯与1,3-二溴丙烷烷基化的步骤; 用NaN3取代溴以制备叠氮胺; 用Pd催化剂将产物还原成胺化合物; 用相应的异氰酸酯，硫代异氰酸酯或酰氯转化成酰胺，最后水解母体部分中的酯基以制备式1的化合物。它们是强力和独特的拮抗剂作用于士的宁非感受性甘氨酸的偶联位置 NMDA受体复合物并有效渗入中枢神经系统。 它们有效治疗神经变性，特别适用于由外部伤口或贫血引起的低氧浓度引起的心脏病，低血糖，局部贫血和心跳停止等疾病所致的CNS损伤。

公开(公告)号：KR100245980B1

公开(公告)日：2000-04-01

申请号：KR1019970031451

申请日：1997-07-08

Applicant: 한국화학연구원

Inventor： 박노상 ,  정영식 ,  성철민 ,  백기현 ,  조성주 ,  이광숙 ,  최진일 ,  공재양 ,  박우규 ,  김재홍

IPC: C07C233/04 ,  A61K31/16

Abstract: 본 발명은 진통작용이 우수한 하기 일반식(I)로 표시되는 N-아릴알킬호모바닐릭아미드 유도체에 관한 것이다:
(I)
상기식에서, X는 C
1-6 알킬, 또는 C
1-6 알킬로 치환되거나 치환되지 않은 아릴 또는 헤테로아릴이고; Y는 수소 또는 2-아미노에틸이며; Z는 서로 같거나 다를 수 있으며 수소, 할로겐, R
1 또는 OR
1 이고, 이때 R
1 은 C
1-5 알킬, 고리알킬, 페닐 또는 벤질이며; p는 0 내지 5의 정수이다.

公开(公告)号：KR100168494B1

公开(公告)日：1999-03-20

申请号：KR1019950048617

申请日：1995-12-12

Applicant: 한국화학연구원

Inventor： 박노상 ,  정영식 ,  성철민 ,  최승원 ,  최연주 ,  이종철 ,  최진일 ,  이광숙 ,  공재양 ,  이부연 ,  김재홍

IPC: C07C235/34 ,  A61K31/165 ,  C07C235/18 ,  C07C323/25

CPC classification number: C07C235/34 ,  C07C323/41

Abstract: 하기 일반식(I)의 N-아릴알킬호모바닐릭아미드 유도체 화합물은 보다 적은 용량에서 소염 및 진통효과를 나타내므로 진통 및 소염용 약학 조성물로서 유용하게 사용될 수 있다:

상기식에서, X, Y, Z, W, n, m 및 p는 명세서중에서 정의한 바와 같다.

公开(公告)号：KR1020120050841A

公开(公告)日：2012-05-21

申请号：KR1020100112296

申请日：2010-11-11

Applicant: 한국화학연구원

Inventor： 박우규 ,  공재양 ,  조희영 ,  정대영 ,  최길돈 ,  고훈영 ,  이희윤 ,  정선호 ,  이해황 ,  이정국 ,  서용완

IPC: C07D403/06 ,  A61K31/496 ,  A61P25/00

Abstract: PURPOSE: A pyrazole butyl compound and a pharmaceutical composition containing the same are provided to ensure dopamine D4 receptor affinity and to prevent and treat central nervous system diseases. CONSTITUTION: A pyrazole butyl compound and pharmaceutically acceptable salt thereof are denoted by chemical formula 1. The salt includes inorganic acid salt, organic acid salt, amino acid salt, alkali metal salt, or ammonium salt. A method for preparing the pyrazole butyl compounds comprises: a step of performing reductive amination of pyrazole aldehyde compound of chemical formula 2 with heterocycle compounds of chemical formula 3 under the presence of reducing agent and base. A pharmaceutical composition for treating central nervous system diseases contains 1-(4-chlorophenyl)-4-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)piperazine(compound No. 33) or 1-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)-4-(3-(trifluoromethyl)phenyl)piperazine(compound No. 36).

Abstract translation: 目的：提供吡唑丁基化合物和含有它们的药物组合物以确保多巴胺D4受体亲和力并预防和治疗中枢神经系统疾病。 构成：吡唑基丁基化合物及其药学上可接受的盐由化学式1表示。盐包括无机酸盐，有机酸盐，氨基酸盐，碱金属盐或铵盐。 制备吡唑丁基化合物的方法包括：在还原剂和碱的存在下，用化学式3的杂环化合物进行化学式2的吡唑醛化合物的还原胺化的步骤。 用于治疗中枢神经系统疾病的药物组合物含有1-（4-氯苯基）-4-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）哌嗪（化合物33）或 1-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）-4-（3-（三氟甲基）苯基）哌嗪（化合物36）。

公开(公告)号：KR1020110024940A

公开(公告)日：2011-03-09

申请号：KR1020090083133

申请日：2009-09-03

Applicant: 한국화학연구원 ,  인하대학교 산학협력단

Inventor： 고훈영 ,  김지희 ,  카말키숄포파트로랜지 ,  공재양 ,  박우규 ,  조희영 ,  정대영 ,  최길돈 ,  이희윤

IPC: C07D403/08 ,  C07D403/06 ,  A61K31/415 ,  A61P25/18

Abstract: PURPOSE: A pharmaceutical composition containing a novel 3-(methoxymethyl)pyrazole derivative is provided to ensure dopamine D3 and D4 receptor affinity and to suppress psychotic behavior(cage climbing) in a mouse. CONSTITUTION: A novel 3-(methoxymethyl)pyrazole derivative is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by reductive amination of pyrazole aldehyde derivative of chemical formula 2 with piperazine derivative of chemical formula 3 under the presence of reductant and base. A pharmaceutical composition for treating central nervous system diseases contains the compound of chemical formula 1.

Abstract translation: 目的：提供含有新的3-（甲氧基甲基）吡唑衍生物的药物组合物，以确保多巴胺D3和D4受体的亲和力，并抑制小鼠的精神病性行为（笼养）。 组成：化学式1表示新的3-（甲氧基甲基）吡唑衍生物。化学式1的化合物通过化学式2的吡唑醛衍生物与化学式3的哌嗪衍生物在还原剂的存在下还原胺化而制备， 基础。 用于治疗中枢神经系统疾病的药物组合物含有化学式1的化合物。