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公开(公告)号：KR1019970003501B1
公开(公告)日：1997-03-18
申请号：KR1019920006546
申请日：1992-04-18
Applicant: 동화약품주식회사
IPC: C07D401/14
Abstract: This invention provides quinolone derivatives represented by the structural formula (I) wherein X is N or C-H. The derivatives are produced by reacting a fluorine-substituted quinolinecarbonic acid, 1-cycloprophyl-6,7,8- trifluoro-1,4-dihydro-4-oxo-3-quinolinecarbonic acid, with one of substituted piperazines, 1-(2,6-diaminoprymidine-4-yl)-piperazine and 1-(4,6-diamino-1,3,5-triazine-2-yl)-piperazine, in a polar solvent. These quinolone derivatives have high antimicrobial activity especially against gram-positive bacteria.
Abstract translation: 本发明提供由结构式（I）表示的喹诺酮衍生物，其中X为N或C-H。 衍生物通过氟取代的喹啉碳酸1-环丙基-6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉碳酸与一个取代的哌嗪，1-（2 ，6-二氨基丙内酰胺-4-基） - 哌嗪和1-（4,6-二氨基-1,3,5-三嗪-2-基） - 哌嗪。 这些喹诺酮衍生物具有高抗微生物活性，特别是针对革兰氏阳性菌。
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公开(公告)号：KR1019960037643A
公开(公告)日：1996-11-19
申请号：KR1019950008856
申请日：1995-04-15
Applicant: 동화약품주식회사
IPC: C07C233/80
Abstract: 본 발명은 2-(4-시클로펜톡시벤조일아미노)벤즈아미드유도체에 관한 것으로 더욱 자세하게는 새로운 2-(4-시클로펜톡시벤조일아미노)벤즈 아미드 유도체 및 이들의 제조방법과 그것의 용도에 관한 것이다.
종래의 천연물성분인 멜란드린과 그의 에스테르유도체들은 진통작용이 다소약한 문제점이 있어 이러한 구조에 여러 작용기를 도입하여 진통 및 소염작용이 우수하고 독성과 위장장해등의 부작용이 거의 없는 약리학적 및 생리학적으로 탁월한 하기 구조식(Ⅰ)의 2-(4-시클로펜톡시벤조일아미노)벤즈아미드유도체 및 그 제조방법을 제공한다.
상기의 구조식(Ⅰ)의 화합물은 우수한 소염진통작용을 나타내는 화합물로 기존에 널리 쓰이고 있는 소염진통제들의 흔한 문제점인 위장장해등의 부작용과 독성이 거의 없는 안정성이 탁월한 화합물이다.-
公开(公告)号：KR1019960037642A
公开(公告)日：1996-11-19
申请号：KR1019950008823
申请日：1995-04-14
Applicant: 동화약품주식회사
IPC: C07C233/80
Abstract: 본 발명에 따르면, 하기 일반식(Ⅰ)로 표시되는 2-(4-알콕시벤조일아미노)벤즈아미드 유도체 및 그의 제조방법이 제공된다.
상기 식에서, R
1 은 수소, 탄소수 1-4의 히드록시 치환기를 가질 수 있는 저급 알킬기, 벤질기, 저급 아실기 또는 저급 알콕시카르보닐이고 ; R
2 , R
3 의 하나는 수소 원자, 다른 하나는 치환기를 가질 수도 있는 탄소수 1∼7의 직쇄 또는 분지쇄 알킬기 또는 고리형 알킬기, 또는 벤질기이거나 ; R
2 및 R
3 는 인접한 질소원자와 함께 헤테로고리를 형성할 수 있으며 ; R
4 는 탄소수 1∼4의 직쇄 또는 분지쇄 알킬기 또는 벤질기이다.
본 발명의 화합물은 소염 진통작용이 우수하고 독성과 위장장해 등의 부작용이 거의 없으므로 소염진통제로서 매우 유용하다.-
55.发明公开
公开(公告)号：KR1020100066868A
公开(公告)日：2010-06-18
申请号：KR1020080125361
申请日：2008-12-10
Applicant: 동화약품주식회사
IPC: C07D213/72 , C07D213/64 , C07D213/16
CPC classification number: C07D213/74
Abstract: PURPOSE: A 3-nitropyridine derivative compound in which 2,6-site is substituted is provided to suppress osteoclast formation and to prevent and treat osteoporosis. CONSTITUTION: A 3-nitropyridine derivative compound in which 2,6-site is substituted is denoted by chemical formula 1. A method for preparing the 3-nitropyridine derivative comprises: and a step of reacting 2,6dichloro-3-nitropyridine and 5-amino triazole under the presence of base to obtain 2-(1H-benzotriazole-5-yl)amino-6-chloro-3-nitropyridine with HNR_2(CH_2)nR1 amine compound to obtain 3-nitropyridine derivative in which 1,6 site of chemical formula 1. A pharmaceutical composition for preventing or treating osteoporosis contains 3-nitropyridine derivative compound or pharmaceutically acceptable salt as an active ingredient.
Abstract translation: 目的：提供2,6-取代的3-硝基吡啶衍生物，以抑制破骨细胞形成和预防和治疗骨质疏松症。 构成：其中2,6-位被取代的3-硝基吡啶衍生物化合物由化学式1表示。制备3-硝基吡啶衍生物的方法包括：使2,6-二氯-3-硝基吡啶与5- 氨基三唑在碱存在下反应，得到2-（1H-苯并三唑-5-基）氨基-6-氯-3-硝基吡啶与HNR 2（CH 2）n R 1胺化合物，得到3-硝基吡啶衍生物，其中， 化学式1.用于预防或治疗骨质疏松症的药物组合物含有3-硝基吡啶衍生物化合物或药学上可接受的盐作为活性成分。
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Patent Agency Ranking
公开(公告)号：KR100875596B1
公开(公告)日：2008-12-23
申请号：KR1020070009859
申请日：2007-01-31
Applicant: 동화약품주식회사
IPC: C07D277/22 , C07D413/04 , C07D401/04 , A61P19/10
CPC classification number: C07D417/04 , C07D277/28 , C07D417/12
Abstract: The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.
Abstract translation: 本发明涉及一种新的苯甲脒衍生物，其制备方法以及包含其的药物组合物。 本发明的苯甲脒衍生物以极低浓度有效地抑制破骨细胞分化，并且大大增加了骨小梁的体积，因此可有利地用于预防和治疗骨质疏松症。
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57.发明公开Ｎ-히드록시-4-｛5-〔4-（5-이소프로필-2-메틸-1,3-티아졸-4-일）페녹시〕펜톡시｝벤즈아미딘 2 에탄술폰산염, 이의제조방법 및 이를 포함하는 약학 조성물 失效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}苯甲胺二乙酸盐，其制备方法和包含药物组合物 一样
公开(公告)号：KR1020080094634A
公开(公告)日：2008-10-23
申请号：KR1020080036880
申请日：2008-04-21
Applicant: 동화약품주식회사
IPC: C07D277/24 , A61K31/426 , A61P19/10
CPC classification number: C07D277/24
Abstract: An N- hydroxy-4- benzamidine 2 ethansulfonic acid salt is provided to show excellent solubility, stability, and bioavailability, as well as a higher initial release rate than 2 methansulfonic acid salt thereof. An N-hydroxy-4-benzamidine 2 ethansulfonic acid salt is represented by a formula(1) and is prepared by reacting N- hydroxy-4-benzamidine and ethanesulfonic acid in an inert solvent. A pharmaceutical composition for preventing and treating osteoporosis, bone fractures, allergic or inflammatory diseases comprises the N- hydroxy-4-benzamidine 2 ethansulfonic acid salt and a pharmaceutically acceptable carrier. An oral formulation for preventing and treating osteoporosis, bone fractures, and allergic inflammatory diseases, comprises the N- hydroxy-4-benzamidine 2 ethansulfonic acid salt along with (a) at least one carbonate selected from the group consisting of alkali metal carbonate, alkali metal bicarbonate and alkaline earth metal carbonate; (b) at least one disintegrant selected from the group consisting of sodium carboxymethyl starch, sodium carmellose, calcium carmellose and sodium croscarmellose; or a combination of (a) and (b).
Abstract translation: 提供N-羟基-4-苄脒2乙磺酸盐以显示出优异的溶解性，稳定性和生物利用度，以及比其二甲基磺酸盐更高的初始释放速率。 N-羟基-4-苯甲脒2乙磺酸盐由式（1）表示，并通过N-羟基-4-苯甲脒和乙磺酸在惰性溶剂中反应制备。 用于预防和治疗骨质疏松症，骨折，过敏或炎性疾病的药物组合物包括N-羟基-4-苄脒2乙磺酸盐和药学上可接受的载体。 用于预防和治疗骨质疏松症，骨折和过敏性炎性疾病的口服制剂包括N-羟基-4-苯甲脒2乙磺酸盐以及（a）至少一种选自碱金属碳酸盐，碱金属的碳酸盐 金属碳酸氢盐和碱土金属碳酸盐; （b）至少一种选自羧甲基淀粉钠，羧甲纤维素钠，羧甲纤维素钙和交联羧甲纤维素钠的崩解剂; 或（a）和（b）的组合。
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公开(公告)号：KR1020070079043A
公开(公告)日：2007-08-03
申请号：KR1020070009859
申请日：2007-01-31
Applicant: 동화약품주식회사
IPC: C07D277/22 , C07D413/04 , C07D401/04 , A61P19/10
CPC classification number: C07D417/04 , C07D277/28 , C07D417/12
Abstract: A novel benzamidine derivative is provided to effectively inhibit osteoclast differentiation at an extremely low concentration, and significantly increase the trabecular bone volume, thereby being used for preventing and treating osteoporosis. The benzamidine derivative is represented by the formula(1), wherein R1 is C1-6 alkyl which is unsubstituted or substituted with one group selected from pyridine and a group represented by the structural formula(1-a), C3-6 cycloalkyl, phenyl, benzyl; pyridinyl which is unsubstituted or substituted with C1-6 alkyl, guanidino, NR6R7, a group represented by the structural formula(1-b); or a group represented by the structural formula(1-a) which is unsubstituted or substituted with C1-6 alkyl; R2 is a primary or secondary amine, which is NR8R9, a compound represented by the structural formula(1-c), pyrrolidine, piperidine or imidazole, each R3 and R4 is independently H, halogen, hydroxy, C1-6 alkyl which is unsubstituted or substituted with halogen, C3-6 cycloalkylamino, C1-6 alkoxy, C1-6 alkanoyloxy, C2-6 alkenyloxy, phenyl-C1-6 alkoxy, phenoxy, C2-6 alkenoyloxy or phenyl-C1-6 alkanoyloxy, or C3-6 cycloalkyloxy which is substituted with one group selected from carboxy, esterified carboxy and amidated carboxy or aminooxy; R5 is H or hydroxy group; each X1 and X3 is independently O, S, NH, or N-C1-6 alkyl, N-C3-6 cycloalkyl, N-benzyl or N-phenyl; X2 is C3-7 alkylene, C1-3 alkylene-C2-7 alkenylene-C1-3 alkylene, C1-3 alkylene-O-C1-3 alkylene, C1-3 alkylene-S-C1-3 alkylene, C1-3 alkylene-NH-C1-3 alkylene, C1-3 alkylene-phenylene-C1-3 alkylene, C1-3 alkylene-pyridylene-C1-3 alkylene or C1-3 alkylene-naphthylene-C1-3 alkylene, C3-7 alkylene which is substituted with C1-3 alkyl and hydroxyl, C3-7 alkylene carbonyl, or C3-7 alkylene which is interrupted by piperazine; Q is CH or carbonyl; and n is an integer of 0 to 6..
Abstract translation: 提供了一种新颖的苯甲脒衍生物，以极低浓度有效抑制破骨细胞分化，并显着增加小梁骨体积，从而用于预防和治疗骨质疏松症。 苯甲脒衍生物由式（1）表示，其中R 1是未被取代或被一个选自吡啶和由结构式（1-a）表示的基团，C 3-6环烷基，苯基 ，苄基; 吡啶基，其未被取代或被C 1-6烷基，胍基，NR 6 R 7，被结构式（1-b）表示的基团取代; 或由未被取代或被C 1-6烷基取代的结构式（1-a）表示的基团; R2是伯或仲胺，其为NR8R9，由结构式（1-c）表示的化合物，吡咯烷，哌啶或咪唑，每个R 3和R 4独立地为H，卤素，羟基，未被取代的C 1-6烷基 或被卤素取代，C 3-6环烷基氨基，C 1-6烷氧基，C 1-6烷酰氧基，C 2-6烯氧基，苯基-C 1-6烷氧基，苯氧基，C 2-6烯酰氧基或苯基-C 1-6烷酰氧基或C 3-6 被一个选自羧基，酯化的羧基和酰胺化的羧基或氨氧基的基团取代的环烷氧基; R5为H或羟基; 每个X 1和X 3独立地是O，S，NH或N-C 1-6烷基，N 3 -C 6环烷基，N-苄基或N-苯基; X2是C3-7亚烷基，C1-3亚烷基-C2-7亚烯基C1-3亚烷基，C1-3亚烷基-O-C1-3亚烷基，C1-3亚烷基-S-C1-3亚烷基，C1-3亚烷基 -NH-C 1-3亚烷基，C 1-3亚烷基 - 亚苯基-C 1-3亚烷基，C 1-3亚烷基 - 亚吡啶基-C 1-3亚烷基或C 1-3亚烷基 - 亚萘基-C 1-3亚烷基， 被C 1-3烷基和羟基取代，C 3-7亚烷基羰基或被哌嗪中断的C 3-7亚烷基; Q是CH或羰基; n为0〜6的整数。
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公开(公告)号：KR100609490B1
公开(公告)日：2006-08-09
申请号：KR1020000020137
申请日：2000-04-17
Applicant: 동화약품주식회사
IPC: C07D417/06
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 식에서, R
1 , R
2 및 n은 명세서에 기재된 바와 같다.Abstract translation: 本发明是在小说-6-甲基 - 烟酰胺衍生物的抗病毒剂是有用的，它涉及一种药物组合物，包括制造和他的方法，由通式-6-甲基 - 烟酰胺衍生物（1）具体地，核类化合物是HBV （乙肝病毒）和HCV增殖的（丙型肝炎病毒），以及HIV（人类免疫缺陷病毒），因此也表明抑制乙型肝炎和丙型肝炎的增殖的作用，并且可以是在爱滋病使用的有用的治疗和预防剂 有。
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60.发明公开Ｎ-히드록시－４－｛５－［４－（5－이소프로필－２－메틸－１,３－티아졸－4－일）페녹시］펜톡시｝벤즈아미딘 ２메탄술폰산염 有权N-羟基-4- ?? 5 ?? ?? 4？ δ5 ??异丙基?? 2 ??甲基?? 1,3 ??噻唑?? 4 ?? YL ??苯氧基??戊烷??苄嘧啶2甲磺酸盐
公开(公告)号：KR1020060057511A
公开(公告)日：2006-05-26
申请号：KR1020050111543
申请日：2005-11-22
Applicant: 동화약품주식회사
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
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