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1. 发明公开

KR1020030008653A 엔,엔-디이소프로필-4-[7-(4-아미노페녹시)헵톡시]-3-메톡시벤즈아미드의 골다공증 예방 및 치료제로서의 용도 失效
标题翻译：使用N，N-二异丙基-4-（7-（4-氨基苯氧基）羟基）-3-甲氧基苯甲酰胺作为预防和/或治疗剂用于卵泡发育
公开(公告)号：KR1020030008653A
公开(公告)日：2003-01-29
申请号：KR1020010043489
申请日：2001-07-19
申请人： 동화약품주식회사 , 서홍석
发明人： 이진수 , 김판수 , 황연하 , 유제만 , 정용호 , 서홍석 , 김도희 , 박용엽
IPC分类号： A61K31/166
摘要： 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.
摘要翻译：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。

2. 发明授权

KR100705173B1 엔,엔-디이소프로필-4-[7-(4-아미노페녹시)헵톡시]-3-메톡시벤즈아미드의 골다공증 예방 및 치료제로서의 용도 失效
标题翻译：使用N，N-二异丙基-4- [7-4-氨基苯氧基丁氧基] -3-甲氧基苯甲酰胺治疗骨质疏松症
公开(公告)号：KR100705173B1
公开(公告)日：2007-04-06
申请号：KR1020010043489
申请日：2001-07-19
申请人： 동화약품주식회사 , 서홍석
发明人： 이진수 , 김판수 , 황연하 , 유제만 , 정용호 , 서홍석 , 김도희 , 박용엽
IPC分类号： A61K31/166
摘要： 본 발명은 류코트리엔-B
4 (Leukotriene-B
4 ; 이하 "LTB-4"로 약칭한다)의 수용체 길항작용을 갖는 것으로 알려진 하기 화학식 1로 표시되는 N,N-디이소프로필-4-[7-(4-아미노페녹시)헵톡시]-3-메톡시벤즈아미드의 골다공증의 예방 및 치료제로서의 용도에 관한 것이다.
[화학식 1]

골다공증, 골 흡수, 류코트리엔-B4, 파골세포

3. 发明授权

KR100454767B1 4-[(4-티아졸릴)페녹시]알콕시-벤즈아미딘 유도체의골다공증 예방 및 치료제로서의 용도 有权
标题翻译： 4 - [（4-티아졸릴）페녹시]알콕시 - 벤즈아미딘유도체의골다공증치치제제로서의용도
公开(公告)号：KR100454767B1
公开(公告)日：2004-11-03
申请号：KR1020010043490
申请日：2001-07-19
申请人： 동화약품주식회사 , 서홍석
发明人： 이진수 , 김판수 , 황연하 , 유제만 , 정용호 , 서홍석 , 김은주 , 김도희 , 박용엽
IPC分类号： A61K31/426
CPC分类号： A61K31/426 , Y10S514/878
摘要： 본 발명은 류코트리엔-B
4 (Leukotriene-B
4 ; 이하 "LTB-4"로 약칭한다)의 수용체 길항작용을 갖는 것으로 알려진 하기 화학식 1로 표시되는 4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘 또는 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘의 골다공증의 예방 및 치료제로서의 용도에 관한 것이다.
[화학식 1]

상기 식에서 R은 H 또는 OH이다.
摘要翻译：本发明涉及含有下式1表示的4 - [（4-噻唑基）苯氧基]烷氧基 - 苄脒衍生物用于预防和治疗骨质疏松症的药物组合物，更具体地涉及4- {5- [4 - （5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒或N-羟基-4- {5- [4-（5-异丙基-2-甲基 - 噻唑-4-基）苯氧基]戊氧基} - 苄脒作为用于预防和治疗骨质疏松症的药物组合物，其已知为白三烯-B4受体的拮抗剂。 [通式1]其中，R是氢原子或羟基。

4. 发明公开

KR1020030008654A 4-[(4-티아졸릴)페녹시]알콕시-벤즈아미딘 유도체의골다공증 예방 및 치료제로서의 용도 有权
标题翻译：使用4 - （（4-三唑基）苯氧基）烷基苯甲胺衍生物作为预防和/或治疗药物用于卵泡发育
公开(公告)号：KR1020030008654A
公开(公告)日：2003-01-29
申请号：KR1020010043490
申请日：2001-07-19
申请人： 동화약품주식회사 , 서홍석
发明人： 이진수 , 김판수 , 황연하 , 유제만 , 정용호 , 서홍석 , 김은주 , 김도희 , 박용엽
IPC分类号： A61K31/426
CPC分类号： A61K31/426 , Y10S514/878
摘要： PURPOSE: Provided are 4-((4-thiazolyl)phenoxy)alkoxy-benzamidine derivatives(DW1350 and DW1352) acting as leukotriene-B4 receptor antagonistic action. The compounds exhibit an excellent inhibition effect on a differentiation, formation, fusion process and bone absorption function of osteoclast cells, therefore they can be effectively used as an prophylaxis and treatment of osteoporosis. CONSTITUTION: The agent for prophylaxis and treatment of osteoporosis contains an effective amount of 4-((4-thiazolyl)phenoxy)alkoxy-benzamidine derivative of formula(1) or a salt thereof. In formula, R is H or OH. The agent is excellent in an inhibition of osteoclast cells as compared to any compound such as DW1349 and DW1351 having structural similarity as well as HS-1141 and CGS-25019C and has increased efficacy in increasing the activity of osteoblast cells.
摘要翻译：目的：提供作为白三烯-B4受体拮抗作用的4 - （（4-噻唑基）苯氧基）烷氧基 - 苄脒衍生物（DW1350和DW1352）。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，因此可有效用于预防和治疗骨质疏松症。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4 - （（4-噻唑基）苯氧基）烷氧基 - 苄脒衍生物或其盐。在式中，R是H或OH。与具有结构相似性的DW1349和DW1351以及HS-1141和CGS-25019C的化合物相比，该试剂在破骨细胞抑制方面优异，并且在增加成骨细胞活性方面具有增加的功效。

5. 发明授权

KR101047614B1 신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물 失效
公开(公告)号：KR101047614B1
公开(公告)日：2011-07-07
申请号：KR1020080073710
申请日：2008-07-28
申请人： 동화약품주식회사
发明人： 유제만 , 이진수 , 진영구 , 박재훈 , 김보경 , 원대연 , 황연하 , 김기윤 , 구세광
IPC分类号： C07D417/06 , C07D417/04 , C07D277/42
CPC分类号： C07D277/22 , C07D277/28 , C07D277/40 , C07D417/06
摘要： 본 발명은 신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를 포함하는 골다공증의 예방 또는 치료용 약학 조성물에 관한 것이다. 본 발명의 벤즈아미딘 유도체는 매우 낮은 농도에서 파골세포에 대한 분화를 효과적으로 억제하여 골다공증의 예방 또는 치료에 유용하게 사용될 수 있다.

6. 发明公开

KR1020110054670A 2-시아노-3-히드록시-엔-[(4-트리플루오로메틸)페닐]부트-2-엔아미드의 제조방법 无效
标题翻译：制备2-氰基-3-羟基-N - [（4-三氟甲基）苯基] -2-ENAMIDE的方法
公开(公告)号：KR1020110054670A
公开(公告)日：2011-05-25
申请号：KR1020090111413
申请日：2009-11-18
申请人： 동화약품주식회사
发明人： 오윤석 , 임재경 , 최정욱 , 권오진 , 이준상 , 유제만
IPC分类号： C07C253/00 , C07C255/40 , A61K31/277
摘要： PURPOSE: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide is provided to easily remove by-products generated during the manufacturing process of final products. CONSTITUTION: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide of chemical formula 1 from a compound of chemical formula 5 comprises the steps of: activating a compound of chemical formula 2 to an esterified compound using a carbodiimide compound; and reacting the resultant with a compound of chemical formula 4 to prepare a compound of chemical formula 5. The carbodiimide compound is selected from 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride, 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide, 1,3-diisopropylcarbodiimide or 1,3-dicyclohexylcarbodiimide.
摘要翻译：目的：提供2-氰基-3-羟基-N - [（4-三氟甲基）苯基]丁-2-烯酰胺的制备方法，以便容易地除去最终产品的制造过程中产生的副产物。构成：由化学式5的化合物制备化学式1的2-氰基-3-羟基-N - [（4-三氟甲基）苯基]丁-2-烯酰胺的方法包括以下步骤：活化化学式式2与使用碳二亚胺化合物的酯化化合物反应; 将所得物与化学式4的化合物反应，制备化学式5的化合物。碳二亚胺化合物选自1- [3-（二甲基氨基）丙基] -3-乙基碳二亚胺盐酸盐，1- [3-（二甲基氨基）丙基] -3-乙基碳二亚胺，1,3-二异丙基碳二亚胺或1,3-二环己基碳二亚胺。

7. 发明公开

KR1020100014174A 벤즈아미딘 유도체 또는 이의 염, 및 비스포스포네이트를 포함하는 골다공증의 예방 또는 치료용 약학 조성물 无效
标题翻译：一种用于预防或治疗包含苯甲胺衍生物或其盐的骨质疏松症的药物组合物和双膦酸盐
公开(公告)号：KR1020100014174A
公开(公告)日：2010-02-10
申请号：KR1020090070538
申请日：2009-07-31
申请人： 동화약품주식회사
发明人： 이진수 , 황연하 , 유제만 , 진영구 , 김기윤
IPC分类号： A61K31/426 , A61P19/10 , A61K31/663
CPC分类号： A61K31/426 , A61K31/663 , A61K2300/00
摘要： PURPOSE: A pharmaceutical composition for preventing or treating osteoporosis, which contains benzamidine derivative and bisphosphonate is provided to effectively suppress differentiation of osteoclast and prevent and treat lesion relating to bone absorption. CONSTITUTION: A pharmaceutical composition for preventing or treating contains a novel benzamidine derivative of chemical formula 1 or its salt and bisphosphonate of chemical formula 2 as active ingredient. The compounds of chemical formula 1 and 2 are used simuntaneously, separately or successively. The bisphosphonate of chemical formula 2 is etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, ibandronic acid, zoledronic acid or Allen drone acid. The pharmaceutical composition is formulated with compounds of chemical formulas 1 and 2 integrally or separately.
摘要翻译：目的：提供含有苯甲脒衍生物和二膦酸盐的预防或治疗骨质疏松症的药物组合物，以有效抑制破骨细胞分化，预防和治疗与骨吸收有关的病变。构成：用于预防或治疗的药物组合物含有化学式1的新型苄脒衍生物或其化学式2的盐和二膦酸盐作为活性成分。化学式1和化合物2分别或相继使用。化学式2的二膦酸盐是依替膦酸，氯膦酸，帕米膦酸，替鲁膦酸，利塞膦酸，伊班膦酸，唑来膦酸或艾伦无机碱。药物组合物与化学式1和化合物2一体或分开配制。

8. 发明公开

KR1020100014090A 벤즈아미딘 유도체 또는 이의 염, 및 비스포스포네이트를 포함하는 골다공증의 예방 또는 치료용 약학 조성물 无效
标题翻译：一种用于预防或治疗包含苯甲胺衍生物或其盐的骨质疏松症的药物组合物和双膦酸盐
公开(公告)号：KR1020100014090A
公开(公告)日：2010-02-10
申请号：KR1020090007774
申请日：2009-01-31
申请人： 동화약품주식회사
发明人： 이진수 , 황연하 , 유제만 , 진영구 , 김기윤
IPC分类号： A61K31/426 , A61P19/10 , A61K31/662
CPC分类号： A61K31/426 , A61K31/663 , A61K2300/00
摘要： PURPOSE: A pharmaceutical composition containing benzamidine derivative and bisphosphonate is provided to suppress osteoclasts and prevent or treat osteoporosis. CONSTITUTION: A pharmaceutical composition for preventing or treating osteoporosis contains a novel benzamidine derivative of chemical formula 1 or its salt, and bisphosphonate of chemical formula 2. The benzamidine derivative and bisphosphonate are used simultaneously, separately, or in order. The bisphosphonate is etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, ibandronic acid, or zoledronic acid.
摘要翻译：目的：提供含有苯甲脒衍生物和双膦酸盐的药物组合物，以抑制破骨细胞，预防或治疗骨质疏松症。构成：用于预防或治疗骨质疏松症的药物组合物含有化学式1的新的苯甲脒衍生物或其盐，以及化学式2的双膦酸盐。苄脒衍生物和双膦酸盐同时，分别或按顺序使用。二膦酸盐是依替膦酸，氯膦酸，帕米膦酸，替鲁膦酸，利塞膦酸，伊班膦酸或唑来膦酸。

9. 发明公开

KR1020090012190A 신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물 失效
标题翻译：新型苯甲酸衍生物，其制备方法和用于预防或治疗包含其的药物组合物的药物组合物
公开(公告)号：KR1020090012190A
公开(公告)日：2009-02-02
申请号：KR1020080073710
申请日：2008-07-28
申请人： 동화약품주식회사
发明人： 유제만 , 이진수 , 진영구 , 박재훈 , 김보경 , 원대연 , 황연하 , 김기윤 , 구세광
IPC分类号： C07D417/06 , C07D417/04 , C07D277/42
CPC分类号： C07D277/22 , C07D277/28 , C07D277/40 , C07D417/06
摘要： A benzamidine derivative is provided to be used for a pharmaceutical composition for preventing and treating osteoporosis and to suppress effectively differentiation of osteoclast at very low concentration. A benzamidine derivative is indicated as a chemical formula 1. In the chemical formula 1: R1 is methyl, ethyl, isopropyl, phenyl, pyridinyl, cyclohexyl, morpholinyl, group substituted or not substituted into C1~C6 alkyl, NR6R7 or CH2NR6R7; R2 is NR8R9, piperidine, pyrrolidine, imidazole or triazole; R3 and R4 are hydrogen, methyl, ethyl, halogen, hydroxy or methoxy group; R5 is hydroxy group; and R6 and R7 are hydrogen, methyl, ethyl, profile, hydroxyethyl, methoxyethyl, 2-morpholinoethyl, benzyl, pyridine-3-1-methyl, pyridine-4-1-methyl, 3-pyridinyl carbonyl or ethanesulfonyl.
摘要翻译：提供了一种苄脒衍生物，用于预防和治疗骨质疏松症的药物组合物，并以非常低的浓度有效地抑制破骨细胞的分化。化学式1中，R1为甲基，乙基，异丙基，苯基，吡啶基，环己基，吗啉基，取代或未被C1〜C6烷基，NR6R7或CH2NR6R7取代的基团。 R2是NR8R9，哌啶，吡咯烷，咪唑或三唑; R3和R4是氢，甲基，乙基，卤素，羟基或甲氧基; R5是羟基; R 6和R 7是氢，甲基，乙基，异构体，羟乙基，甲氧基乙基，2-吗啉代乙基，苄基，吡啶-3-甲基，吡啶-4-甲基，3-吡啶基羰基或乙磺酰基。

10. 发明公开

KR1020080092893A 1-시클로프로필-6-플루오로-7-(8-메톡시이미노-2,6-디아자-스피로[3.4]옥트-6-일)-4-옥소-1,4-디히드로-[1,8]나프티리딘-3-카르복실산 아스파르트산 염, 이의 제조방법 및 이를포함하는 항균용 약학 조성물 有权
标题翻译： 1-环丙基-6-氟-7-（8-甲氧基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8]萘啶-3- - 羧酸类阿糖酸盐，其制备方法和包含其抗药性的药物组合物
公开(公告)号：KR1020080092893A
公开(公告)日：2008-10-16
申请号：KR1020080034411
申请日：2008-04-14
申请人： 동화약품주식회사
发明人： 유제만 , 최동락 , 양진 , 윤수혜 , 김승환 , 구세광
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D519/00
摘要： 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.
摘要翻译： 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。

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