公开(公告)号：KR1020100067046A

公开(公告)日：2010-06-18

申请号：KR1020090119519

申请日：2009-12-04

Applicant: 동화약품주식회사

Inventor： 유제만 ,  이진수 ,  박휘정 ,  황연하 ,  김기윤

IPC: C07D213/16 ,  C07D213/53 ,  A61K31/44 ,  A61P19/10

CPC classification number: C07D213/74 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14

Abstract: PURPOSE: A 3-nitropyridine derivative compound which is substituted at 2,6-site is provided to suppress differentiation of osteoclast and to prevent and treat osteoporosis. CONSTITUTION: A 3-nitropyridine derivative compound which is substituted at 2,6-site is denoted by chemical formula 1. A method for preparing the 3-nitropyridine derivative compound comprises: a step of reacting aniline compound of chemical formula 3 with 2,6-dichloro-3-nitropyridine under the presence of base to obtain a 6-chloro-3-nitropyridine derivative compound of chemical formula 4; and a step of reacting amine compound of chemical formula 5 with a compound of chemical formula 4 to obtain the 3-nitropyridine derivative compound. A pharmaceutical composition for preventing or treating osteoporosis contains the 3-nitropyridine derivative or pharmaceutically acceptable salt as an active ingredient.

Abstract translation: 目的：提供在2,6位取代的3-硝基吡啶衍生物化合物，以抑制破骨细胞的分化和预防和治疗骨质疏松症。 构成：在2,6-位取代的3-硝基吡啶衍生物化合物由化学式1表示。制备3-硝基吡啶衍生物化合物的方法包括：使化学式3的苯胺化合物与2,6- - 二氯-3-硝基吡啶在碱存在下反应，得到化学式4的6-氯-3-硝基吡啶衍生物化合物; 和使化学式5的胺化合物与化学式4的化合物反应以获得3-硝基吡啶衍生物化合物的步骤。 用于预防或治疗骨质疏松症的药物组合物含有3-硝基吡啶衍生物或药学上可接受的盐作为活性成分。

公开(公告)号：KR1020100014173A

公开(公告)日：2010-02-10

申请号：KR1020090070534

申请日：2009-07-31

Applicant: 동화약품주식회사

Inventor： 이진수 ,  황연하 ,  유제만 ,  박재훈 ,  정덕균

IPC: A61K31/426 ,  A61P19/10 ,  A61K31/663

CPC classification number: A61K31/426 ,  A61K31/663 ,  A61K2300/00

Abstract: PURPOSE: A composition for preventing and treating osteoporosis is provided to suppress osteoclast and bone absorption by using two kinds of compounds. CONSTITUTION: A composition for preventing or treating osteoporosis contains N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thizole-4-yl)phenoxy]pentoxy}benzamidine of chemical formula 1, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazole-4-yl)phenoxy]pentoxy}benzamidine compound of chemical formula 2, alendronic acid of chemical formula 3 or its salt as an active ingredient.

Abstract translation: 目的：提供一种预防和治疗骨质疏松症的组合物，以通过使用两种化合物来抑制破骨细胞和骨吸收。 构成：用于预防或治疗骨质疏松症的组合物含有化学式1的N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基}苄脒 ，化学式2的4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基}苄脒化合物，其化学式3的阿仑膦酸或其盐作为 有效成分。

公开(公告)号：KR100789567B1

公开(公告)日：2007-12-28

申请号：KR1020010069013

申请日：2001-11-06

Applicant: 동화약품주식회사

Inventor： 이진수 ,  안석훈 ,  진영구 ,  진상미 ,  구세광 ,  유제만 ,  정용호 ,  김은주 ,  조순기

IPC: C07D261/20

CPC classification number: C07D261/20

Abstract: 본 발명은 하기 화학식 1로 표시되는 3-아미도-1,2-벤조이소옥사졸(3-amido-1,2-benzoisoxazole)유도체, 그의 염, 제조방법 및 용도에 관한 것으로 3-아미도-1,2-벤조이소옥사졸의 아민기에 아미노산 잔기를 도입하여 생체이용률을 개선하는 방법에 관한 것이다. 본 발명의 화합물은 류코트리엔-B-4 (Leukotriene-B-4)의 수용체 길항제, 골 흡수 억제 작용 및 골 형성 촉진 작용을 하는 골다공증의 억제 또는 치료에 유용하게 사용된다.

(상기 식에서, R
1 및 R
2 는 명세서 내에서 정의한 바와 같다.)
벤조이소옥사졸 유도체, 골다공증 치료제

公开(公告)号：KR100716389B1

公开(公告)日：2007-05-11

申请号：KR1020050111543

申请日：2005-11-22

Applicant: 동화약품주식회사

Inventor： 유제만 ,  이진수 ,  신동혁 ,  성승규 ,  조순기 ,  전찬석 ,  진영구 ,  이기영 ,  정세현 ,  조은희 ,  안석훈

IPC: C07D277/24 ,  C07D277/28 ,  A61P19/10

CPC classification number: C07D277/24 ,  A61K9/143 ,  A61K31/426

Abstract: 본 발명은 생체이용률이 우수한 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}벤즈아미딘 2 메탄술폰산염, 그의 제조방법 및 그를 포함하는 약제학적 조성물에 관한 것이다.
N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}벤즈아미딘 2 메탄술폰산염

公开(公告)号：KR100704992B1

公开(公告)日：2007-04-09

申请号：KR1020050060437

申请日：2005-07-05

Applicant: 동화약품주식회사

Inventor： 이진수 ,  안석훈 ,  진영구 ,  박재훈 ,  신동혁 ,  조은희 ,  장환봉 ,  정용호

IPC: C07D277/24

CPC classification number: C07D277/24

Abstract: 본 발명은 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}벤즈아미딘의 개선된 제조방법에 관한 것이다.
벤즈아미딘

公开(公告)号：KR100682199B1

公开(公告)日：2007-02-12

申请号：KR1020050060439

申请日：2005-07-05

Applicant: 동화약품주식회사

Inventor： 이진수 ,  구세광 ,  이상호 ,  유제만

IPC: A61K31/426 ,  A61K31/155

CPC classification number: A61K31/426

Abstract: 본 발명은 알러지성 염증 질환의 예방 및 치료용 조성물에 관한 것으로, 상세하게는 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘, 4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘 또는 이의 약제학적으로 허용 가능한 염을 포함하는 알러지성 염증 질환의 예방 및 치료용 조성물에 관한 것이다.
본 발명의 조성물은 천식시 유발되는 폐기관지세정액 내 산호성 백혈구의 증가, 혈중 총백혈구 수 및 산호성 백혈구의 증가, 기관지 상피의 점액생산세포 증가에 의한 비후 또는 증생, 폐포벽의 비후에 의한 폐포 면적의 감소 및 염증세포의 침윤과 같은 전형적인 만성염증을 감소시킴으로써, 알러지성 염증 질환의 예방 및 치료에 유용하게 사용할 수 있다.
알러지성 염증, 벤즈아미딘

公开(公告)号：KR100661081B1

公开(公告)日：2006-12-26

申请号：KR1020000031926

申请日：2000-06-10

Applicant: 동화약품주식회사

Inventor： 윤성준 ,  이상욱 ,  이진수 ,  김남두 ,  이근형 ,  이학동 ,  김종우 ,  박상진

IPC: C07D401/12

Abstract: 본 발명은 항바이러스제로 유용한 신규의 6-메틸니코틴아미드 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 6-메틸니코틴아미드 유도체는 HBV (Hepatitis B Virus) 및 HCV (Hepatitis C virus)의 증식 뿐만 아니라 HIV (Human Immunodeficiency Virus) 증식을 억제하는 효과도 나타내므로 B형 간염과 C형 간염 및 후천성 면역 결핍증의 치료제 및 예방제로 유용하게 사용될 수 있다.

상기 화학식 1에서, R 및 n은 명세서에 기재된 바와 같다.

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。