公开(公告)号：KR1020080092893A

公开(公告)日：2008-10-16

申请号：KR1020080034411

申请日：2008-04-14

Applicant: 동화약품주식회사

Inventor： 유제만 ,  최동락 ,  양진 ,  윤수혜 ,  김승환 ,  구세광

IPC: C07D471/04 ,  A61K31/4375

CPC classification number: C07D519/00

Abstract: A 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt is provided to improve physicochemical properties including solubility and stability as compared to phosphate or hydrochloride thereof, and minimize toxicity, so that the compound is useful as antimicrobial agent in food and medicines. A 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt represented by the formula(1) is prepared by reacting 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid with aspartic acid in inert organic solvent selected from ethyl acetate, methanol, ethanol, isopropanol, acetone, acetonitrile, hexane, isopropyl ether and water. An antimicrobial pharmaceutical composition comprises 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt, and is formulated as injection. The aspartic acid salt is D-aspartic acid salt, L-aspartic acid salt or racemic mixture thereof.

Abstract translation: 1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8] 提供3-羧酸天冬氨酸盐以提高与其磷酸盐或盐酸盐相比的溶解度和稳定性的物理化学性质，并且使毒性最小化，使得该化合物可用作食品和药物中的抗微生物剂。 1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8] 由式（1）表示的3-羧酸天冬氨酸盐通过1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基） - 4-氧代-1,4-二氢 - [1,8]二氮杂萘-3-羧酸与天冬氨酸在惰性有机溶剂中的溶液，选自乙酸乙酯，甲醇，乙醇，异丙醇，丙酮，乙腈，己烷，异丙醚和水。 抗微生物药物组合物包含1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,3' 8]萘啶-3-羧酸天冬氨酸盐，并配制成注射剂。 天冬氨酸盐是D-天冬氨酸盐，L-天冬氨酸盐或其外消旋混合物。

公开(公告)号：KR1020080092515A

公开(公告)日：2008-10-16

申请号：KR1020070035881

申请日：2007-04-12

Applicant: 동화약품주식회사

Inventor： 오윤석 ,  임재경 ,  권오진 ,  최정욱 ,  신동혁 ,  정진용 ,  유제만

IPC: C07D211/22 ,  C07D295/02

CPC classification number: C07D211/32

Abstract: A process for preparing an intermediate of donepezil having dementia-treating effects is provided to improve preparation yield and convenience of mass production of the intermediate by replacing the base which is difficult to be used industrially. An intermediate of donepezil, 2-[(E)-1-(1-benzyl-4-piperidyl)methylidene]-5,6-dimethoxy-1-indanone represented by the formula(1) is prepared by reacting 1-indanone compound represented by the formula(2) with aldehyde compound represented by the formula(3) by using a base selected from sodium methoxide(MeONa), sodium ethoxide(EtONa), potassium t-butoxide, sodium hydride, sodium hydroxide, potassium hydroxide and sodium amide in a reaction solvent selected from methanol, ethanol, isopropanol, t-butanol, tetrahydrofuran, 1,4-dioxane, diisopropyl ether, dimethylform amide, dimethylsulfoxide and nitromethane.

Abstract translation: 提供一种制备具有痴呆症治疗效果的多奈哌齐中间体的方法，以通过更换难以在工业上使用的碱来改善中间体的制备产率和方便大量生产。 由式（1）表示的多奈哌齐2 - [（E）-1-（1-苄基-4-哌啶基）亚甲基] -5,6-二甲氧基-1-二氢茚酮的中间体是通过1- 由式（2）表示的醛与式（3）表示的醛化合物通过使用选自甲醇钠（MeONa），乙醇钠（EtONa），叔丁醇钾，氢化钠，氢氧化钠，氢氧化钾和钠 酰胺在选自甲醇，乙醇，异丙醇，叔丁醇，四氢呋喃，1,4-二恶烷，二异丙基醚，二甲基甲酰胺，二甲基亚砜和硝基甲烷的反应溶剂中。

公开(公告)号：KR100799821B1

公开(公告)日：2008-01-31

申请号：KR1020070011556

申请日：2007-02-05

Applicant: 동화약품주식회사

Inventor： 오윤석 ,  임재경 ,  신동혁 ,  성승규 ,  이상호 ,  이학수 ,  조은희 ,  유제만

IPC: C07D401/14

CPC classification number: C07D401/04

Abstract: An imatinib camsylate is provided to be more rapidly absorbed and show higher absorption concentration and excellent solubility in water than those of a commercially available imatinib mesylate in the pharmacokinetic aspect. An imatinib camsylate is represented by the formula(1), wherein HX is D-(+)-camphorsulfonic acid, L-(-)-camphorsulfonic acid or D,L-(±)-camphorsulfonic acid. A method for preparing the imatinib camsylate comprises the steps of: (a) dissolving an imatinib represented by the formula(2) in an organic solvent; (b) dissolving one acid represented by the formula(3) or (4), or an acid which is a mixture of the formula(3) and the formula(4) in a ratio of 1:1 in an organic solvent or adding the acid as it is to the reaction solution obtained from the step(a) to prepare a mixture; (c) filtering a solid extracted by agitating the mixture to form an acid addition salt; and (d) after dissolving the acid addition salt in an organic solvent and re-filtering it to extract crystal, purifying the crystal.

Abstract translation: 提供了一种伊马替尼樟脑磺酸盐以在药代动力学方面比在商业上可获得的甲磺酸伊马替尼的那些更快速地吸收并显示更高的吸收浓度和在水中的优异的溶解性。 伊马替尼樟脑磺酸盐由式（1）表示，其中HX是D - （+） - 樟脑磺酸，L - （ - ） - 樟脑磺酸或D，L-（±） - 樟脑磺酸。 制备伊马替尼樟脑磺酸盐的方法包括以下步骤：（a）将由式（2）表示的伊马替尼溶解在有机溶剂中; （b）在有机溶剂中溶解由式（3）或（4）表示的一种酸或以式（3）和式（4）的混合物形式的酸的比例为1:1，或者将 将酸从原来的步骤（a）获得的反应溶液制备成混合物; （c）过滤通过搅拌混合物提取的固体形成酸加成盐; 和（d）将酸加成盐溶解在有机溶剂中并对其进行再过滤以萃取晶体，纯化晶体。

公开(公告)号：KR100705875B1

公开(公告)日：2007-04-10

申请号：KR1020050071505

申请日：2005-08-04

Applicant: 동화약품주식회사

Inventor： 이진수 ,  안석훈 ,  진영구 ,  진상미 ,  박휘정 ,  구세광 ,  황연하 ,  김판수 ,  이순신 ,  유제만

IPC: C07D277/22 ,  C07D417/04 ,  A61P19/10 ,  A61P11/06

CPC classification number: C07D417/06 ,  C07D277/24 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D277/48 ,  C07D277/52 ,  C07D417/04 ,  C07D417/12

Abstract: 본 발명은 신규한 벤즈아미딘 유도체, 그의 제조방법 및 이를 포함하는 약학 조성물에 관한 것이다.
본 발명의 벤즈아미딘 유도체는 매우 낮은 농도에서 파골세포에 대한 분화를 효과적으로 억제하고 조골세포에 대한 활성이 우수하며 골다공증 동물 모델에서 골량 감소를 현저히 억제하여 골다공증의 예방 및 치료에 유용하게 사용될 수 있다. 또한, 본 발명의 벤즈아미딘 유도체는 골절시 형성된 가골의 소실 및 가골의 골화를 촉진시켜 골절 치료제로 유용하게 사용될 수 있으며, 알러지성 염증 질환의 예방 및 치료에도 유용하게 사용할 수 있다.
벤즈아미딘 유도체

公开(公告)号：KR1020060049858A

公开(公告)日：2006-05-19

申请号：KR1020050060425

申请日：2005-07-05

Applicant: 동화약품주식회사

Inventor： 이진수 ,  구세광 ,  이정우 ,  양희복 ,  유제만

IPC: A61K31/426 ,  A61K31/155

CPC classification number: A61K31/426

Abstract: 본 발명은 골절 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 골절 치료용 조성물에 관한 것이다.
본 발명의 조성물은 가골의 체적을 유의성 있게 감소시키고, 가골의 골밀도 및 골강도를 유의성 있게 증가시키며, 가골 조직내 결합조직 및 연골조직의 함량을 유의성 있게 감소시키고, 골조직 함량을 유의성 있게 증가시킴으로, 골절시 형성된 가골의 소실 및 가골의 골화를 촉진시킨다. 따라서, 본 발명의 조성물은 골절에 대한 치유 촉진제로 유용하게 사용할 수 있다.
골절, 벤즈아미딘

公开(公告)号：KR1020050025933A

公开(公告)日：2005-03-14

申请号：KR1020040071693

申请日：2004-09-08

Applicant: 한국원자력연구원 ,  동화약품주식회사

Inventor： 유제만 ,  신동혁 ,  성승규 ,  양희복 ,  배은정 ,  송영준 ,  박경배 ,  신병철

IPC: A61K51/00 ,  A61K31/722

CPC classification number: A61K51/06 ,  A61K51/1282

Abstract: A composition and kit for treatment of prostate cancer comprising the radioisotope-chitosan complex are provided, which radioisotope-chitosan complex is concentrated to a local region administered so as to prevent leakage of radiation, inhibits growth of prostate cancer cells, and minimizes side effects including urinary incontinence, stricture urethra and rectal hematochezia. The composition for treatment of prostate cancer comprises the radioisotope-chitosan complex, wherein the radioisotope emits high energy beta-ray and low energy gamma-ray simulteneously; the radioisotope is selected from 153Sm, 165Dy, 166Ho and 169 Er; and the molecular weight of chitosan is 100,000 to 1,500, 000 dalton. A kit for treatment of prostate cancer comprises a kit A containing 0.5 to 150 mCi of radioisotope and a kit B containing chitosan with molecular weight of 400,000 to 1,300,00 dalton, wherein the chitosan is weak acid chitosan solution; the chitosan solution comprises one or more selected from pH regulating agent, tonicity adjustment agent, preservative and stabilizing agent.

Abstract translation: 提供了一种用于治疗包括放射性同位素 - 壳聚糖复合物的前列腺癌的组合物和试剂盒，其将放射性同位素 - 壳聚糖复合物浓缩至施用的局部区域，以防止辐射泄漏，抑制前列腺癌细胞的生长，并且最小化副作用，包括 尿失禁，尿道狭窄和直肠血尿。 用于治疗前列腺癌的组合物包括放射性同位素 - 壳聚糖复合物，其中放射性同位素同时发射高能β射线和低能γ射线; 放射性同位素选自153Sm，165Dy，166Ho和169Er; 壳聚糖的分子量为100,000〜1,500,000道尔顿。 用于治疗前列腺癌的试剂盒包含含有0.5至150mCi的放射性同位素的试剂盒A和含有分子量为400,000至1,300,00道尔顿的壳聚糖的试剂盒B，其中壳聚糖是弱酸性壳聚糖溶液; 壳聚糖溶液包含选自pH调节剂，张力调节剂，防腐剂和稳定剂中的一种或多种。

公开(公告)号：KR101018577B1

公开(公告)日：2011-03-03

申请号：KR1020080121296

申请日：2008-12-02

Applicant: 동화약품주식회사

Inventor： 유제만 ,  이승률 ,  백남현 ,  임문정 ,  성승규 ,  이상호

IPC: A61K36/00 ,  A61P3/04

Abstract: 본 발명은 육두구 추출물을 유효성분으로 함유하는 비만 예방 및 치료용 약학 조성물에 관한 것이다.
본 발명은 육두구 추출물에 의해서 고지방 식이의 섭취로 인하여 유발되는 체중증가 억제, 난소주위 지방중량 증가억제 및 주로 지방 세포의 비대에 의해 초래되는 복부지방의 축적을 억제함으로써, 고지방 식이의 섭취에 의해 유발되는 비만 예방 및 치료용 약학조성물로 유용하게 이용될 수 있다.
육두구, 비만

公开(公告)号：KR101011333B1

公开(公告)日：2011-01-28

申请号：KR1020060009292

申请日：2006-01-31

Applicant: 동화약품주식회사

Inventor： 유제만 ,  임문정 ,  노양국 ,  장환봉 ,  오성준 ,  이현용 ,  구세광 ,  양희복 ,  이정우 ,  김윤중 ,  윤주병

IPC: A61K36/488 ,  A61K36/237 ,  A61K36/9068 ,  A61P13/12

CPC classification number: A61K36/25 ,  A61K36/488 ,  A61K36/60 ,  A61K2300/00

Abstract: 본 발명은 생약재 갈근(Puerariae Radix), 백강잠(Bombycis corpus) 또는 독활(Araliae Continentalis Radix)중에서 1 이상 선택되는 생약 추출물을 함유하는 의약 및 건강기능식품에 관한 것이다. 본 발명에 따른 생약재는 독립적으로 또는 혼합조성물로 하여 신장질환 예방 및 치료 또는 신장기능 개선을 위해 유용하게 이용될 수 있다.
갈근, 백강잠, 독활, 신장질환

公开(公告)号：KR1020100067047A

公开(公告)日：2010-06-18

申请号：KR1020090119520

申请日：2009-12-04

Applicant: 동화약품주식회사

Inventor： 유제만 ,  이진수 ,  박휘정 ,  황연하 ,  김기윤

IPC: C07D213/72 ,  C07D213/64 ,  A61K31/44 ,  A61P19/10

CPC classification number: C07D213/74 ,  A61K31/4439 ,  C07D401/14

Abstract: PURPOSE: A 2,6-site-substituted 3-nitropyridine derivative compound is provided to suppress formation of osteroclast and to use in preventing and treating osteroporosis. CONSTITUTION: A novel 2,6-substituted 3-nitro derivative compound is denoted by chemical formula 1. A method for manufacturing the 2,6-substituted 3-nitro derivative compound comprises: a step of reating 2,6-dichloro-3-nitropyridine and 5-aminoindazole under the presence of base to prepare 2(1H-indazole-5-yl)amino-6-chloro-3-nitropyridine; and a step of reacting an amine compound of 2-methyl-2-imidazoline, 2-methyl imidazole, 2-isopropylimidazol, or 5-methyl imidazole with 2(1H-indazole-5-yl)amion-6-chloro-3-nitropyridine. A composition for preventing or treating osteoporosis contains the 3-nitropyridine derivative compound or salt thereof.

Abstract translation: 目的：提供2,6-位取代的3-硝基吡啶衍生物化合物，以抑制成骨细胞的形成并用于预防和治疗卵巢疏松症。 构成：新的2,6-取代的3-硝基衍生物化合物由化学式1表示。制备2,6-取代的3-硝基衍生物化合物的方法包括：将2,6-二氯-3- 硝基吡啶和5-氨基吲唑在碱存在下反应制备2（1H-吲唑-5-基）氨基-6-氯-3-硝基吡啶; 和2-甲基-2-咪唑啉，2-甲基咪唑，2-异丙基咪唑或5-甲基咪唑的胺化合物与2（1H-吲唑-5-基）氨基-6-氯-3- 硝基吡啶。 用于预防或治疗骨质疏松症的组合物含有3-硝基吡啶衍生物化合物或其盐。

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。