公开(公告)号：KR100654328B1

公开(公告)日：2006-12-08

申请号：KR1020050079095

申请日：2005-08-26

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  고훈영 ,  배애님 ,  임혜원 ,  최인성

IPC: C07D401/12

Abstract: A novel piperazinylalkylpyrazole derivative is provided to be able to selectively block T-type calcium ion channels, thereby showing better pain, hypertension, and epilepsy therapeutic effect compared to conventional medicines. The piperazinylalkylpyrazole derivative is represented by the formula(1), where R1 is phenyl, X1-substituted phenyl(where X1 is nitro, methyl, chloro, or methoxy, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), 1,1-diphenylmethyl or X2-substituted diphenylmethyl(where X2 is chloro or methyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), R2 is H, methyl or ethyl, R3 is methyl, propyl, isobutyl, phenyl, cyclohexyl, substituted phenyl(methyl, chloro, or methoxy as a substituent), naphthyl, piperidinyl, R4 is H, C1-6 alkyl, 2-furyl, phenyl or X3-substituted phenyl(where X3 is chloro, methyl, cyclohexyl or piperidinyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), and n is an integer from 0 to 3.

Abstract translation: 提供了一种新的哌嗪基烷基吡唑衍生物，能够选择性阻断T型钙离子通道，因此与常规药物相比，表现出更好的疼痛，高血压和癫痫治疗效果。 哌嗪基烷基吡唑衍生物由式（1）表示，其中R 1为苯基，X 1取代的苯基（其中X 1为硝基，甲基，氯或甲氧基，取代位置为邻位，间位或对位， 三或四或全部能够被取代），1,1-二苯基甲基或X2-取代的二苯基甲基（其中X2是氯或甲基，取代位置是邻位，间位或对位，以及单，二，三，四或 全部能被取代），R2是H，甲基或乙基，R3是甲基，丙基，异丁基，苯基，环己基，取代的苯基（甲基，氯或甲氧基作为取代基），萘基，哌啶基，R4是H， C 1-6烷基，2-呋喃基，苯基或X 3 - 取代的苯基（其中X 3为氯，甲基，环己基或哌啶基，取代位置为邻位，间位或对位，并且单，二，三，四或全部 被取代），并且n是0至3的整数。

公开(公告)号：KR100629327B1

公开(公告)日：2006-09-29

申请号：KR1020040084112

申请日：2004-10-20

Applicant: 한국과학기술연구원

Inventor： 최경일 ,  배애님 ,  남길수 ,  신효님 ,  강재훈 ,  김맹섭

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

公开(公告)号：KR1020030076073A

公开(公告)日：2003-09-26

申请号：KR1020020015729

申请日：2002-03-22

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김중협 ,  최경일 ,  남길수 ,  서재홍 ,  이재목 ,  송석범 ,  이건호 ,  전형옥

IPC: C07D471/04

Abstract: PURPOSE: Pyrido£2,3-d|pyridine-2,4-dione aminomethyl 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-2,4-dione aminomethyl derivatives represented by formula (I) or pharmaceutically acceptable salts are provided, wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl, phenyl 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 C1-3 lower alkyl, C3-7 cycloalkyl, hydroxy, C1-6 lower alkylhydroxy, benzyl, X-substituted phenyl, C1-3 lower alkylphenyl, C1-3 lower alkyl substituted pyridine, C1-3 lower alkyl imidazol, morpholine, C1-3 lower alkyl morpholine, C1-3 lower alkyl piperazine, 4-substituted C1-3 lower alkyl piperazine in which the substituent is hydroxyethyl or methyl, alkylpyrrol or N-substituted alkylpyrrol, in which X is cyano, halogen, carboxyalkyl, nitro, methyl, trihalogenated methyl or alkyloxy; and R3 is hydrogen or methyl, and R2 and R3 are the same or different together. A method for preparing pyrido£2,3-d|pyridine-2,4-dione aminomethyl derivatives of formula (I) comprises preparing a compound of formula (III) from a compound of formula (II), and reducing the compound of formula (III).

Abstract translation: 目的：提供用作PDE IV抑制剂的吡啶2,3-d-吡啶-2,4-二酮氨基甲基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相关的疾病（肿瘤坏死 因子）形成。 构成：提供由式（I）表示的吡啶并[2,3-d]吡啶-2,4-二酮氨基甲基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，苯基或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， ，羧乙基酯，硝基，氟或三氟甲基; R2是C1-3低级烷基，C3-7环烷基，羟基，C1-6低级烷基羟基，苄基，X取代的苯基，C1-3低级烷基苯基，C1-3低级烷基取代的吡啶，C1-3低级烷基咪唑，吗啉 ，C 1-3低级烷基吗啉，C 1-3低级烷基哌嗪，其中取代基为羟乙基或甲基的4-取代的C 1-3低级烷基哌嗪，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; 并且R 3是氢或甲基，并且R 2和R 3在一起是相同或不同的。 制备式（I）的吡啶并[2,3-d]吡啶-2,4-二酮氨基甲基衍生物的方法包括由式（II）化合物制备式（III）的化合物，还原式 （III）。

公开(公告)号：KR100380323B1

公开(公告)日：2003-04-16

申请号：KR1020000003695

申请日：2000-01-26

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김성훈 ,  남길수 ,  서재홍

IPC: C07D501/16

Abstract: PURPOSE: Provided is a novel cephalosporin which has an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at position number 3, and shows antibacterial activity against various gram positive bacteria and gram negative bacteria. CONSTITUTION: The cephalosporin is characterized by having an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at the position number 3 and represented by formula (1). In formula (1), R represents a saturated alkyl group of C1-3 and an unsaturated alkene group of C3-5; R1 is hydrogen, or a saturated alkyl group of C1-3; and R2 represents hydrogen, carboxyl group(or the inorganic cation thereof), carbamoyl group, carbamoyl group of which one or two hydrogen are substituted with an alkyl group of C1-3, or carboxyl group esterified with alkyl group of C1-3. Also, R1 and R2 represent a ring structure linked with 3 to 5 methylene groups.

Abstract translation: 用途：提供了一种新型头孢菌素，其在7号位具有氨基噻唑衍生物，在3号位具有N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，并且显示出抗菌 对各种革兰氏阳性菌和革兰氏阴性菌的活性。 构成：头孢菌素的特征在于在位置7具有氨基噻唑衍生物，在位置3具有N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，并由式 （1）。 在式（1）中，R表示C1-3的饱和烷基和C3-5的不饱和烯基; R1是氢或C1-3的饱和烷基; R2表示氢，羧基（或其无机阳离子），氨基甲酰基，其中一个或两个氢被C1-3的烷基取代的氨基甲酰基或被C1-3的烷基酯化的羧基。 此外，R1和R2表示与3至5个亚甲基连接的环结构。

公开(公告)号：KR1020020058217A

公开(公告)日：2002-07-12

申请号：KR1020000086254

申请日：2000-12-29

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김성훈 ,  남길수 ,  이정근 ,  이재목

IPC: C07D471/04

Abstract: PURPOSE: Provided are novel pyridopyrimidine derivatives which inhibit phosphodiesterase IV activity and TNF production. Also, provided are preparing process thereof and a pharmaceutical composition containing the same. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl amino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl; R is hydrogen, methyl, C3-7 lower alkyloxy, phenyl, benzyl, substituted phenyl(wherein a substituent group includes cyano, halogen, carboxylalkyl, nitro, methyl, trihalogenated ethyl or alkyloxy; and substitution site can be ortho-, meta-, or para- site), alkyloxy, C3-7 lower alkyloxy ethyl, benzyloxy, benzyloxyethyl, phenyloxyethyl, carboxyalkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生的新型吡啶并嘧啶衍生物。 此外，提供其制备方法和含有其的药物组合物。 构成：新颖的吡啶并嘧啶衍生物由式（1）表示，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; R为氢，甲基，C 3-7低级烷氧基，苯基，苄基，取代苯基（其中取代基包括氰基，卤素，羧基烷基，硝基，甲基，三卤代乙基或烷氧基;取代位点可以是邻位，间位， 或对位），烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R 4是氢或甲基，条件是R 2和R 3不相同。

公开(公告)号：KR1019980076908A

公开(公告)日：1998-11-16

申请号：KR1019970013814

申请日：1997-04-15

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김유승 ,  김성훈 ,  손현주 ,  남길수 ,  김하영 ,  장관영 ,  박태조

IPC: C07D501/57

Abstract: 본 발명은 일반식(Ⅱ)로 표시되는 카르복시 화합물 또는 그의 염을 일반식(Ⅲ)으로 표시되는 헤테로 화합물과 반응시켜 새로운 화합물인 일반식(Ⅰ)로 표시되는 세팔로스포린 화합물과 이의 약리학적으로 허용가능한 염 및 이의 제조방법에 관한 것이다.
일반식(Ⅰ)의 화합물은 그람 음성균 및 그람 양성균에 대해 폭넓은 항균력을 나타내며 여러 내성균에 대해서도 강한 항균력을 나타낸다.

일반식(Ⅰ)~(Ⅲ)에 있어서, A는 CH를, R1은 메틸기를, R2는 시아노기, t-1-1 기(X는 산소, 히드록실 아민을 표시하고, Y는 히드록시, 탄소수 1 ~ 5인 알킬옥시, 아미노기, 탄소수 1 ~ 5인 1급 히드록시알킬아미노, 포밀 히드라지노 또는 아실기로 보호된 히드라지노기를 표시한다)를 또는 하기 구조식의 헤테로환(R3는 수소 또는 메틸기를 의미하며, A2 및 A3는 각각 질소 또는 산소이고, A4는 질소를 표시한다)을 각각 표시하며, 그리고, Z는 요오드, 브롬 또는 아세톡시기이다.

公开(公告)号：KR100131993B1

公开(公告)日：1998-04-17

申请号：KR1019940016020

申请日：1994-07-05

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  지대윤 ,  김성훈 ,  남길수 ,  김하영 ,  손현주

IPC: C07D213/79

Abstract: Synthetic method of 4-ethoxycarbonyl-6,7-dihydro-5H-1-pyrindine repregented by formula(I) is provided in this invention. Sodium alkoxide prepared by dissolving sodium in alcohol is reacted with ethylcyanoacetate, then reacted with 2-halocyclopentanone to yield (+-)-2-(1-ethoxycarbonyl-1-cyanomethyl)cyclopentanone of formula(III). Compound of formula(III) is reacted with potassium t-butoxide in the presence of ether solvent, then reacted with allyl halogen to produce (+-)-2-cyano-2-(cyclopentanon-2-yl)pent-4-en-carboxylic acid ethyl ester of formula(IV). Compound of formula(IV) is reacted with ozone to yield (+-)-2-cyano-2-(cyclopentanon-2-yl)butan-4-oxo-carboxylic acid ethyl ester of formula(V), then lastly compound(V) is reacted successively with hydroxylamine and phosphorous trichloride to yield 4-ethoxycarbonyl-6,7-dihydro-5H-1-pyrindine.

Abstract translation: 在本发明中提供了由式（I）表示的4-乙氧基羰基-6,7-二氢-5H-1-氮茚的合成方法。 通过将钠溶解在醇中制备的醇钠与氰基乙酸乙酯反应，然后与2-卤代环戊酮反应，得到式（III）的（+）-2-（1-乙氧基羰基-1-氰基甲基）环戊酮。 式（III）化合物与叔丁醇钾在醚溶剂存在下反应，然后与烯丙基卤反应生成（±）-2-氰基-2-（环戊烷-2-基）戊-4-烯 （IV）的羧酸乙酯。 式（Ⅳ）化合物与臭氧反应，得到式（Ⅴ）的（±）-2-氰基-2-（环戊烷-2-基）丁-4-基 - 羧酸乙酯，最后为化合物 V）与羟胺和三氯化磷相继反应，得到4-乙氧基羰基-6,7-二氢-5H-1-氮茚。

公开(公告)号：KR1019960031472A

公开(公告)日：1996-09-17

申请号：KR1019950002382

申请日：1995-02-09

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  남길수 ,  김성훈 ,  김하영 ,  손현주

IPC: C07H15/236

Abstract: 본 발명은 양자성 용매하에 킬레이트화제를 사용하여 시소마이신을 킬레이트화하고, 킬레이트화된 시소마이신3,2',6' 위치의 아미노기를 아실화제로서 아실화 반응에 의해 보호하고, 암모니아수로 킬레이트화된 금속을 이탈시킨다음, 얻어진3,2',6'-트리치환 시소마이신을 비양자성 유기용매에서 에틸화제와 반응시켜 1위치의 아미노기만을 선택적으로 에틸화시키고, 이어서 탈보호하는 것으로 이루어진 다음 구조식(I)의 1-N-에틸시소마이신 및 그의 약리학적 허용염의 제조방법을 제시한다.:

상기 1-N-에틸시소마이신은 인체의 감염증을 치료하는데 사용되는 아미노글리코시드계의 항생제이며, 본 발명의 제조방법에 따라 고수율이 얻어진다.

公开(公告)号：KR1020170125255A

公开(公告)日：2017-11-14

申请号：KR1020160055552

申请日：2016-05-04

Applicant: 한국과학기술연구원 ,  주식회사 크린아이

Inventor： 정혜선 ,  장유라 ,  이정애 ,  남길수 ,  송영심

IPC: C09J11/08 ,  C09J11/06 ,  C09J133/00 ,  C08K5/00 ,  C08L5/08 ,  C08L5/04

CPC classification number: C09J11/08 ,  C08K5/00 ,  C08K2201/007 ,  C08L5/04 ,  C08L5/08 ,  C09J11/06 ,  C09J133/00

Abstract: 본발명은향오일점착제조성물및 그제조방법에관한것이다. 본발명의일 실시예에따른향오일점착제조성물제조방법은. (a) 키토산(Chitosan) 고분자를포함하는고분자수용액을제조하는단계(S10), (b) 고분자수용액에향오일(Fragrance Oil)을혼합하여향오일에멀젼을제조하는단계(S20), 및 (c) 상기향오일에멀젼을아크릴계점착제와혼합하는단계(S30)를포함한다.

Abstract translation: 香料油压敏粘合剂组合物及其制备方法本发明涉及香料油压敏粘合剂组合物及其制备方法。 根据本发明实施方案的生产香料油粘合剂组合物的方法包括： （A）脱乙酰壳多糖（壳聚糖）混合阶段（S10），（B）芳香油（芳香油）在聚合物水溶液，以制备包含聚合物来制备风味油乳液（S20）的聚合物溶液，和（c ）将香料油乳液与丙烯酸粘合剂混合（S30）。

公开(公告)号：KR101778938B1

公开(公告)日：2017-09-18

申请号：KR1020160075019

申请日：2016-06-16

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  강순방 ,  배애님 ,  남길수 ,  김은경 ,  서선희 ,  모하마드,아쉬라프카림 ,  이주현

IPC: C07D401/12 ,  C07D401/14 ,  C07D215/20 ,  A61K31/47 ,  A61K31/4725

CPC classification number: C07D401/12 ,  A61K31/47 ,  A61K31/4725 ,  C07D215/20 ,  C07D401/14

Abstract: 본발명은암세포에대한우수한항 증식효능을나타내는퀴놀린화합물, 이의약학적으로허용가능한염, 또는수화물과, 이의제조방법및 이를유효성분으로함유하는암 질환의예방또는치료용의약조성물에관한것으로서, 상기본 발명에따른화합물, 이의약학적으로허용가능한염, 또는수화물은우수한암세포억제활성과단백질키나아제및 돌연변이키나아제의억제활성을나타내고있으므로, 부작용이적은새로운항암제로유용하게사용될수 있다.

Abstract translation: 本发明涉及一种优良的抗 - 喹啉化合物为代表增殖作用，其药学上可接受的盐，或它们的水合物及它们的制备方法和预防或治疗的药物组合物含有与用于癌细胞的活性成分的癌症疾病， 因为这些化合物根据基本发明，其药学上可接受的盐，或水合物显示出优异的肿瘤抑制活性，并且所述蛋白激酶和所述突变体的激酶抑制活性，这种副作用可有利地具有小的新的抗癌药物使用。