公开(公告)号：KR100491100B1

公开(公告)日：2005-11-29

申请号：KR1019970036589

申请日：1997-07-31

Applicant: 동화약품주식회사

Inventor： 윤성준 ,  정용호 ,  이상욱 ,  심형수 ,  박용균 ,  김종우 ,  허용 ,  윤제인 ,  박상진

IPC: C07D401/04 ,  A61K31/395 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: 본 발명은 신규 테레프탈산아미드 유도체에 관한 것으로서, 더욱 상세하게는 HIV 및 HBV를 비롯한 각종 바이러스의 증식억제 효과가 우수하여 항바이러스제로서 유효한 다음 화학식 1로 표시되는 신규 테레프탈산아미드 유도체와 그의 약제학적으로 허용가능한 염, 그리고 그의 제조방법에 관한 것이다.
[화학식 1]

상기 화학식 1에서,
R
1 , R
2 및 R
3 은 발명의 상세한 설명에서 설명한 바와 같다.

公开(公告)号：KR100438482B1

公开(公告)日：2004-08-18

申请号：KR1019960051939

申请日：1996-11-05

Applicant: 동화약품주식회사 ,  정상헌

Inventor： 윤성준 ,  정용호 ,  이문선 ,  최동락 ,  이정아 ,  이덕근 ,  최청하 ,  이희순 ,  정상헌

IPC: C07D403/12 ,  A61K31/41

Abstract: PURPOSE: Diarylsulfonyl imidazolone derivative and a preparation method thereof are provided. The derivative has improved anticancer activity and do not form aniline derivative causing side-effects. CONSTITUTION: The 4-phenyl-1-(N-carbamoylindoline-5-sulfonyl)- 4,5-dihydro-2-imidazolone derivative is represented by the formula (I), wherein X is oxygen or sulfur; R is C1-C6 alkyl, chloroacetyl, benzyl, phenyl, methoxyphenyl, fluorophenyl, methylphenyl, aminophenyl or thiomethylphenyl; and R' is hydrogen or chlorine. An anticancer pharmaceutical composition comprises the diarylsulfonyl imidazolone derivative of the formula (I) and pharmaceutically acceptable salts thereof as effective components. The method for preparing the 4-phenyl-1-(N-carbamoylindoline-5-sulfonyl)- 4,5-dihydro-2-imidazolone derivative represented by the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III).

公开(公告)号：KR1020030081762A

公开(公告)日：2003-10-22

申请号：KR1020020020136

申请日：2002-04-12

Applicant: 동화약품주식회사

Inventor： 정용호 ,  최동락 ,  김익회 ,  신정한 ,  양진 ,  윤수혜

IPC: C07D401/04

CPC classification number: Y02P20/55

Abstract: PURPOSE: A quinoline carboxylic acid derivative with fluoropyrrolidine substituents and a preparation process thereof are provided. The compound has no toxicity and improved antimicrobial activity to both gram positive and negative bacteria. CONSTITUTION: A quinoline carboxylic acid derivative represented by the formula 1 in which 4-aminomethyl-4-fluoro-3-(Z)-alkoxyiminopyrrolidine is substituted at the 7-site of the quinolone scaffold, pharmaceutically acceptable acid adding salt and solvates thereof are provided. In the formula, Q is C-H, C-F, C-Cl, C-OCH3, C-OCHF2, C-CH3 or N; R is hydrogen, methyl or NH2; R1 is ethyl, cyclopropyl, t-butyl, or at least one fluoro substituted phenyl; R2 is hydrogen, C1-C5 alkyl, cyclopropyl, cyclopropyl methyl, C3-C6 alkenyl, C3-C6 alkynyl, phenyl or benzyl; and R3 or R4 is independently hydrogen, or C1-C3 alkyl, or R3 or R4 is hydrogen or C1-C3 alkyl bound nitrogen containing C3-C5 hetero ring compound. A process for preparing the quinoline carboxylic acid derivative represented by the formula 1 comprises the steps of: (1) reacting a quinolone scaffold compound of the formula 2 with a fluoro containing compound of the formula 3 in the presence of a solvent and a base to prepare a compound of the formula 4; and (2) deprotecting the compound of formula 4 with HX, wherein R3 or R4 is hydrogen; P is hydrogen or amine-protecting group; and X is F or Cl.

Abstract translation: 目的：提供具有氟吡咯烷取代基的喹啉羧酸衍生物及其制备方法。 该化合物对革兰氏阳性菌和阴性菌均无毒性和改善的抗微生物活性。 构成：在喹诺酮支架的7-位取代有4-氨基甲基-4-氟-3-（Z） - 烷氧基亚氨基吡咯烷的式1所示的喹啉羧酸衍生物，其药学上可接受的酸加成盐及其溶剂合物是 提供。 在该式中，Q为C-H，C-F，C-Cl，C-OCH 3，C-OCHF 2，C-CH 3或N; R是氢，甲基或NH 2; R 1是乙基，环丙基，叔丁基或至少一个氟取代的苯基; R 2是氢，C 1 -C 5烷基，环丙基，环丙基甲基，C 3 -C 6烯基，C 3 -C 6炔基，苯基或苄基; 并且R 3或R 4独立地是氢或C 1 -C 3烷基，或者R 3或R 4是氢或C 1 -C 3烷基键合的含有C 3 -C 5杂环化合物的氮。 制备由式1表示的喹啉羧酸衍生物的方法包括以下步骤：（1）在溶剂和碱的存在下使式2的喹诺酮支架化合物与式3的含氟化合物反应， 制备式4的化合物; 和（2）用HX使式4的化合物脱保护，其中R3或R4是氢; P是氢或胺保护基; X为F或Cl。

公开(公告)号：KR1020030075396A

公开(公告)日：2003-09-26

申请号：KR1020020014588

申请日：2002-03-18

Applicant: 동화약품주식회사 ,  이승택

Inventor： 이승택 ,  장진욱 ,  김주현 ,  장윤정 ,  정용호 ,  임문정 ,  성희진 ,  노양국 ,  신동혁 ,  장환봉

IPC: C07D311/40

Abstract: PURPOSE: A matrix metalloproteinase inhibitor and functional food containing flavonoid derivatives or extracts of Dalbergia odorifera containing the flavonoid derivatives are provided, thereby effectively treating diseases associated with matrix metalloproteinase. CONSTITUTION: Extracts of Dalbergia odorifera containing fisetin of formula 1 and 3'-hydroxydidzein of formula 2 are prepared by dissolving pulverized Dalbergia odorifera in a solvent selected from methanol, a mixed solvent of methanol and water and ethylacetate, filtering the solution, and concentrating the filtered solution under reduced pressure. A fraction of Dalbergia odorifera containing fisetin and 3'-hydroxydidzein is prepared by dissolving Dalbergia odorifera in methanol or a mixed solvent of water and methanol, filtering the solution, adding ethylacetate or butanol into the filtered solution, filtering the solution, and concentrating the filtered solution under reduced pressure.

Abstract translation: 目的：提供一种基质金属蛋白酶抑制剂和含有黄酮类衍生物的黄酮类衍生物或含有黄酮衍生物的提取物的功能性食品，从而有效治疗与基质金属蛋白酶相关的疾病。 构成：通过将粉碎的Dalbergia odorifera溶解在选自甲醇，甲醇和水与乙酸乙酯的混合溶剂的溶剂中，过滤该溶液并浓缩，得到含有式1的非瑟酮和式2的3'-氢氧根霉素的Dalbergia odorifera的提取物 在减压下过滤溶液。 通过将Dalbergia odorifera在甲醇或水和甲醇的混合溶剂中溶解，过滤该溶液，向过滤的溶液中加入乙酸乙酯或丁醇，过滤溶液，浓缩过滤的溶液，制备含有非丝氨酸和3'-羟基溶解素的Dalbergia odorifera的一小部分 溶液在减压下。

公开(公告)号：KR1020030050412A

公开(公告)日：2003-06-25

申请号：KR1020010080842

申请日：2001-12-18

Applicant: 동화약품주식회사

Inventor： 정용호 ,  오윤석 ,  임재경 ,  권오진 ,  강소연 ,  홍현수

IPC: C07D215/227

Abstract: PURPOSE: A process for preparing rebamipide is provided, thereby simplifying the preparing process of rebamipide and improving the preparation yield of rebamipide. CONSTITUTION: A process for preparing rebamipide of the formula(1) comprises the steps of: reacting 4-(bromomethyl)-1,2-dihydro-2-quinolinone of formula(2) with diethyl 2-£(4-chlorobenzoyl)amino|malonate of formula(3) to prepare a compound of formula(4); and reacting the compound of formula(4) under basic conditions, wherein R is alkyl having the carbon number of 1 to 6, wherein the diethyl 2-£(4-chlorobenzoyl)amino|malonate of formula(3) is prepared by reacting diethyl 2-aminomalonate hydrochloride with 4-chlorobenzoyl derivative of formula(6); and R is alkyl having the carbon number of 1 to 6 and X is OH or halogen atom.

Abstract translation: 目的：提供制备瑞巴派特的方法，从而简化了雷巴米特的制备过程，提高了瑞巴派特的制备成品率。 构成：制备式（1）的瑞巴派特的方法包括以下步骤：使式（2）的4-（溴甲基）-1,2-二氢-2-喹啉酮与2-（4-氯苯甲酰基）氨基 （3）的丙二酸酯以制备式（4）的化合物; 并在碱性条件下使式（4）的化合物反应，其中R是碳数为1至6的烷基，其中式（3）的2-（2-氯苯甲酰基）氨基丙二酸二乙酯是通过使二 2-氨基马来酸盐酸盐与式（6）的4-氯苯甲酰基衍生物反应; R为碳原子数1〜6的烷基，X为OH或卤素原子。

公开(公告)号：KR1020030008653A

公开(公告)日：2003-01-29

申请号：KR1020010043489

申请日：2001-07-19

Applicant: 동화약품주식회사 ,  서홍석

Inventor： 이진수 ,  김판수 ,  황연하 ,  유제만 ,  정용호 ,  서홍석 ,  김도희 ,  박용엽

IPC: A61K31/166

Abstract: PURPOSE: Provided is N,N-diisopropyl-4-(7-(4-aminophenoxy)heptoxy)-3-methoxybenzamide(DW1259) which has leukotriene-B4 receptor antagonistic action and has excellent effects on inhibition of bone absorption by effectively inhibiting the function of osteoclast cells. CONSTITUTION: The agent for prophylaxis and treatment of osteoporosis contains an effective amount of N,N-diisopropyl-4-(7-(4-aminophenoxy)heptoxy)-3-methoxybenzamide of formula(1). The compound has an excellent inhibition effect on a differentiation, formation, fusion process and bone absorption function of osteoclast cells, is excellent in an inhibition function of osteoclast cells as compared to any compound such as DW1231, DW1234, DW1166, DW1235 having structural similarity as well as HS-1141 and CGS-25019C and has increased efficacy in increasing the activity of osteoblast cells.

Abstract translation: 目的：提供具有白三烯-B4受体拮抗作用的N，N-二异丙基-4-（7-（4-氨基苯氧基）庚氧基）-3-甲氧基苯甲酰胺（DW1259），并且通过有效抑制 破骨细胞功能。 构成：用于预防和治疗骨质疏松症的药物含有有效量的式（1）的N，N-二异丙基-4-（7-（4-氨基苯氧基）乙氧基）-3-甲氧基苯甲酰胺。 该化合物对破骨细胞的分化，形成，融合过程和骨吸收功能具有优异的抑制作用，与​​具有结构相似性的任何化合物如DW1231，DW1234，DW1166，DW1235相比，破骨细胞的抑制功能优异 以及HS-1141和CGS-25019C，并且增加了成骨细胞活性的功效。

公开(公告)号：KR1020020076920A

公开(公告)日：2002-10-11

申请号：KR1020010017143

申请日：2001-03-31

Applicant: 동화약품주식회사

Inventor： 정용호 ,  이치우 ,  양왕용 ,  이학동 ,  박휘정 ,  장윤영 ,  이진수

IPC: C07D413/14

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14

Abstract: PURPOSE: Provided are a methoxy-1,3,5-triazine derivative which inhibit the growth of Hepatitis C virus(HCV) and a pharmaceutical composition containing the same, therefore it can be useful for the prevention and treatment of hepatitis type B and hepatitis type C. CONSTITUTION: The methoxy-1,3,5-triazine derivative is represented by formula(1) and its pharmaceutically acceptable salt are provided. In the formula(1), R1 is H or C1-C8 alkyl; R2 is H, hydroxy, C1-C4 linear or branched chain alkyl, C1-C3 linear or branched chain alkoxy, C1-C3 hydroxyalkyl, C2-C6 dialkylamino, C3-C6 cycloalkyl, lactam, saturated or unsaturated 5 or 6 atom hetero ring compound optionally substituted with C1-C3 linear or branched chain alkyl substituted or unsubstituted, and containing one or two hetero atom selected from N, O and S; or bicyclo compound containing one or two hetero atom selected from N, O and S; n is an integer of 0 to 4; and R3 is 5-indazolyl or 6-indazolyl. The method for producing the methoxy-1,3,5-triazine derivative comprises the steps of: reacting 2,4-dichloro-6-methoxy-1,3,5-triazine of formula(4) with 5-aminoindazole or 6-aminoindazole of formula(5) in the presence of base to prepare aminoindazole substituted 2-chloro-6-methoxy-1,3,5-triazine derivative of formula(6); and reacting the compound of formula(6) with amine compound of formula(7) in the presence of amine to prepare methoxy-1,3,5-triazine derivative of formula(1).

Abstract translation: 目的：提供抑制丙型肝炎病毒（HCV）生长的甲氧基-1,3,5-三嗪衍生物和含有该丙氨酸病毒（HCV）的药物组合物，因此可用于预防和治疗乙型肝炎和肝炎 C型。构成：提供甲氧基-1,3,5-三嗪衍生物由式（1）表示，并提供其药学上可接受的盐。 在式（1）中，R 1是H或C 1 -C 8烷基; R2是H，羟基，C1-C4直链或支链烷基，C1-C3直链或支链烷氧基，C1-C3羟基烷基，C2-C6二烷基氨基，C3-C6环烷基，内酰胺，饱和或不饱和的5或6原子杂环 任选被取代或未取代的C 1 -C 3直链或支链烷基取代的，含有一个或两个选自N，O和S的杂原子的化合物; 或含有一个或两个选自N，O和S的杂原子的双环化合物; n为0〜4的整数。 并且R 3是5-吲唑基或6-吲唑基。 制备甲氧基-1,3,5-三嗪衍生物的方法包括以下步骤：使式（4）的2,4-二氯-6-甲氧基-1,3,5-三嗪与5-氨基吲唑或6- 式（5）的氨基吲唑在碱的存在下反应，制备式（6）的氨基吲唑取代的2-氯-6-甲氧基-1,3,5-三嗪衍生物; 并在胺的存在下使式（6）的化合物与式（7）的胺化合物反应，制得式（1）的甲氧基-1,3,5-三嗪衍生物。

公开(公告)号：KR1020020002461A

公开(公告)日：2002-01-09

申请号：KR1020017014647

申请日：2000-05-18

Applicant: 동화약품주식회사

Inventor： 윤성준 ,  정용호 ,  이치우 ,  이진수 ,  김남두 ,  진윤호 ,  송완진 ,  김익회 ,  양왕용 ,  최동락 ,  신정한

IPC: C07D471/04

CPC classification number: C07D401/04 ,  C07D471/04 ,  C07D487/10

Abstract: PURPOSE: Provided are optically active quinoline carboxylic acid derivatives, pharmaceutically acceptable salts thereof, solvates thereof, and a process for preparation thereof, which are useful for an antibacterial agent. CONSTITUTION: The optically active quinoline carboxylic acid derivatives are represented by the following formula(1), and contains optical activity-causing 4-aminomethyl-4-methyl-3 (Z)-alkoxyiminopyrrolidine substituents at the 7-position of the quinolone nuclei, their pharmaceutically acceptable salts, and their solvates. In the formula(1), Q is C-H, C-F, C-Cl or N; Y is H or NH2; R is a straight or branched alkyl group of Cl-C, an allyl group or a benzyl group, and * represents optically pure chiral carbon atom. Their preparation process comprises the steps of: condensing the quinolone nuclei-containing compound of formula(3), with the ketal compound of formula(2a), in the presence of an acid acceptor to give the optically active quinoline carboxylic acid derivative of formula(4); deketalizing the optically active quinoline carboxylic acid derivative of formula(4) to give the pyrrolidinone compound of formula(5); and reacting the pyrrolidinone compound of formula(5) with an alkoxylamine in the presence of a base to obtain the desired compound of formula(1).

Abstract translation: 目的：提供可用于抗菌剂的光学活性喹啉羧酸衍生物，其药学上可接受的盐，溶剂合物及其制备方法。 构成：光学活性喹啉羧酸衍生物由下式（1）表示，并且在喹诺酮核的7-位含有光学活性的4-氨基甲基-4-甲基-3（Z） - 烷氧基亚氨基吡咯烷取代基， 其药学上可接受的盐及其溶剂合物。 在式（1）中，Q是C-H，C-F，C-Cl或N; Y为H或NH 2; R是Cl-C，烯丙基或苄基的直链或支链烷基，*表示光学上纯的手性碳原子。 它们的制备方法包括以下步骤：在酸受体存在下将式（3）的喹诺酮核含有化合物与式（2a）的缩酮化合物缩合，得到式（3）的光学活性喹啉羧酸衍生物 4）; 对式（4）的光学活性喹啉羧酸衍生物进行缩酮化，得到式（5）的吡咯烷酮化合物; 并在碱的存在下使式（5）的吡咯烷酮化合物与烷氧基胺反应，得到所需的式（1）化合物。

公开(公告)号：KR100231497B1

公开(公告)日：1999-11-15

申请号：KR1019970060990

申请日：1997-11-19

Applicant: 동화약품주식회사 ,  한국화학연구원

Inventor： 정용호 ,  이진수 ,  김재학 ,  김용주 ,  이홍우 ,  허재두 ,  이철해 ,  정희정

IPC: C07D471/04

Abstract: 본 발명은 그람 양성균은 물론 녹농균을 제외한 그람 음성균에 대하여 우수한 항균 작용을 나타내는, 하기 화학식 1a 또는 화학식 1b로 표시되는 카르바페넴 유도체 화합물, 구체적으로는 (1S, 5R, 6S)-2-치환된 히드록시메틸-6-[(1R)-1-히드록시에틸]-1-메틸-2-카르바페넴-3-카르복실산 유도체, 이의 제조 방법 및 이를 포함하는 약제학적 조성물을 제공한다.


식 중, R
1 은 수소 원자이거나, 또는 무기 또는 유기염으로부터 유도된 양이온이고, R
2 는 수소 원자이거나, 또는 C
1 -C
4 의 시클릭 또는 비시클릭 저급 알킬기 또는 할로 알킬기이며, n은 1 내지 3이다.

公开(公告)号：KR1019990076241A

公开(公告)日：1999-10-15

申请号：KR1019980011018

申请日：1998-03-30

Applicant: 한국화학연구원 ,  동화약품주식회사

Inventor： 이철해 ,  이주철 ,  김재학 ,  이진수 ,  정용호 ,  김용주 ,  이홍우 ,  허재두

IPC: C07D477/14 ,  C07D205/02 ,  C07D487/04

Abstract: 본 발명은 하기 구조식(I)의 1-베타메틸 카르바페넴 유도체 및 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 항균제 조성물에 관한 것이다.

상기 식에서,
R
1 은 수소, C
1-4 의 알킬, C
1-4 의 시클로알킬, 할로겐으로 치환된 C
1-4 의 알킬 또는 할로겐으로 치환된 C
1-4 의 시클로알킬이고,
n은 1 내지 3의 정수이다.