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公开(公告)号：KR1019960037644A
公开(公告)日：1996-11-19
申请号：KR1019950008857
申请日：1995-04-15
Applicant: 동화약품주식회사
IPC: C07C233/80
Abstract: 본 발명은 2-(4-아미노벤조일아미노)벤즈아미드유도체에 관한 것으로 더욱 자세하게는 새로운 2-(4-아미노벤조일아미노)벤즈아미드 유도체 및 이들의 제조방법과 그것의 용도에 관한 것이다.
종래의 천연물성분인 멜란드린과 그의 에스테르유도체들은 진통작용이 다소 약한 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-아미노벤조일아미노)벤즈아미드 유도체 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：KR101079916B1
公开(公告)日：2011-11-04
申请号：KR1020080123461
申请日：2008-12-05
Applicant: 동화약품주식회사
Abstract: 본발명에의한육두구추출물은고지방식이의섭취로인하여유발되는비만증상을개선및 예방할 수있어, 청소년, 성인및 노인층의광범위한계층까지비만증상의개선및 예방을위한기능성식품으로유용하게이용될수 있다.
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64.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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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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Patent Agency Ranking66.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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67.发明公开
公开(公告)号：KR1020070081294A
公开(公告)日：2007-08-16
申请号：KR1020060013167
申请日：2006-02-10
Applicant: 동화약품주식회사
IPC: A61K31/341 , A61K31/56 , A61K36/47 , A61P19/10
Abstract: A composition for preventing and treating osteoporosis comprising terpenoids isolated from Euphorbia kansui or the extracts thereof is provided to inhibit bone absorption of osteoclasts without side effects. The composition for preventing and treating osteoporosis comprises kansuinine A represented by the formula(1) and gamma-euphorbol represented by the formula(2) or the extracts thereof. The kansuinine A represented by the formula(1) and gamma-euphorbol represented by the formula(2) are isolated by extracting and concentrating Euphorbia kansui with methanol, suspending the concentrated extract of Euphorbia kansui in water, and adding nucleic acid into the suspension to separate a nucleic acid layer, adding methylene chloride into a water layer obtained by separating the nucleic acid layer to obtain a methylene chloride fraction, and subjecting the methylene chloride fraction to chromatography.
Abstract translation: 提供了用于预防和治疗包括从大戟属分离的萜类化合物或其提取物的骨质疏松症的组合物，以抑制破骨细胞的骨吸收而没有副作用。 用于预防和治疗骨质疏松症的组合物包括由式（1）表示的苦参碱A和由式（2）表示的γ-高效药或其提取物。 由式（1）表示的甘露宁A和由式（2）表示的γ-高效酚通过用甲醇萃取浓缩大戟甘油，将浓缩的大戟属浓缩提取物悬浮于水中，并将核酸加入到悬浮液中 分离核酸层，将二氯甲烷加入到通过分离核酸层获得的水层中，得到二氯甲烷部分，并将二氯甲烷部分进行色谱分离。
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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：KR1020070020977A
公开(公告)日：2007-02-22
申请号：KR1020050075414
申请日：2005-08-17
Applicant: 동화약품주식회사
IPC: A61K9/20 , A61K31/4439
CPC classification number: A61K9/2054 , A61K9/2886 , A61K31/4439 , Y10S514/97
Abstract: 본 발명은 판토프라졸 함유 약제의 경구 투여 형태에 관한 것이다.
특히, 본 발명은 코어, 중간물질 층 및 위액에 내성을 갖는 최외층으로 구성된 판토프라졸 경구 투여 형태에 있어서, 필수적으로 충전제로서 저치환도히드록시프로필셀룰로오스를 사용하므로서 저장 보관시 산 불안정성 약리활성물질인 판토프라졸의 안정성을 증진시킬 수 있다.
판토프라졸, 충전제, 저치환도히드록시프로필셀룰로오스-
公开(公告)号：KR1020060057514A
公开(公告)日：2006-05-26
申请号：KR1020050111779
申请日：2005-11-22
Applicant: 동화약품주식회사
IPC: A61K47/30 , A61K9/16 , A61K31/426
CPC classification number: C07D277/24 , A61K9/143 , A61K31/426
Abstract: 본 발명은 생체이용률이 향상된 N-히드록시-4-5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시-벤즈아미딘의 경구용 제제에 관한 것으로, 더욱 상세하게는 N-히드록시-4-5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시-벤즈아미딘 또는 이의 약학적으로 허용 가능한 염과 탄산 알칼리금속염, 탄산수소 알칼리 금속염 및 탄산 알칼리토금속염으로 이루어진 군으로부터 선택되는 1종 이상의 탄산염 및/또는 카르복시메틸스타치나트륨, 카르멜로오스칼슘 및 크로스카르멜로오스나트륨으로 이루어진 군에서 선택되는 1종 이상의 붕해제를 포함하는 경구용 제제에 관한 것이다. 본 발명에 따른 경구용 제제는 초기 용출단계에서 N-히드록시-4-5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시-벤즈아미딘 또는 이의 약학적으로 허용 가능한 염의 겔 형성을 억제하여 용출속도를 증가시키고 생체 이용률을 현저하게 상승시킬 수 있다.
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