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1.发明申请
公开(公告)号：WO2010067987A2
公开(公告)日：2010-06-17
申请号：PCT/KR2009/007216
申请日：2009-12-04
IPC: C07D213/16 , C07D213/53
CPC classification number: C07D213/74 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
Abstract: 본 발명은 신규한 2, 6-위치에 치환된 3-니트로피리딘 유도체 화합물, 그의 제조방법 및 이를 포함하는 골다공증 예방 또는 치료용 약학 조성물에 관한 것이 다. 본 발명의 2, 6-위치에 치환된 3-니트로피리딘 유도체 화합물은 조골세포의 활 성을 증가시킬 뿐 아니라 동시에 파골세포의 분화를 효과적으로 억제함으로, 골다 공증의 예방 및 치료에 유용하게 사용될 수 있다.
Abstract translation: 本发明涉及一种新的2,6-取代-3-硝基吡啶衍生物化合物及其制备方法，以及包含其的用于预防和治疗骨质疏松症的药物组合物。 本发明的2,6-取代-3-硝基吡啶衍生物化合物增加成骨细胞活性，有效抑制破骨细胞的分化，因此可有效地用于预防和治疗骨质疏松症。
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公开(公告)号：WO2010067989A3
公开(公告)日：2010-06-17
申请号：PCT/KR2009/007218
申请日：2009-12-04
IPC: C07D213/72 , C07D213/64 , C07D213/16
Abstract: 본 발명은 신규한 2, 6-위치가 치환된 3-니트로피리딘 유도체 화합물, 그의 제조방법, 이를 포함하는 골다공증 예방 또는 치료용 약제학적 조성물, 골다공증 예방 또는 치료 약제를 제조하기 위한 이의 용도, 이를 이용한 골다공증 예방 및 치료방법에 관한 것이다. 본 발명의 2, 6-위치가 치환된 3-니트로피리딘 유도체 화합물은 조골세포의 활성을 증가시킬 뿐 아니라 동시에 파골세포의 형성을 효과적 으로 억제함으로, 골다공증의 예방 및 치료에 유용하게 사용될 수 있다.
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3.发明公开
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
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。
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Patent Agency Ranking4.发明公开
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
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。
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公开(公告)号：KR101047614B1
公开(公告)日：2011-07-07
申请号：KR1020080073710
申请日：2008-07-28
Applicant: 동화약품주식회사
IPC: C07D417/06 , C07D417/04 , C07D277/42
CPC classification number: C07D277/22 , C07D277/28 , C07D277/40 , C07D417/06
Abstract: 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.
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6.发明公开
公开(公告)号：KR1020100014174A
公开(公告)日：2010-02-10
申请号：KR1020090070538
申请日：2009-07-31
Applicant: 동화약품주식회사
IPC: A61K31/426 , A61P19/10 , A61K31/663
CPC classification number: A61K31/426 , A61K31/663 , A61K2300/00
Abstract: 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.
Abstract translation: 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。
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7.发明公开
公开(公告)号：KR1020100014090A
公开(公告)日：2010-02-10
申请号：KR1020090007774
申请日：2009-01-31
Applicant: 동화약품주식회사
IPC: A61K31/426 , A61P19/10 , A61K31/662
CPC classification number: A61K31/426 , A61K31/663 , A61K2300/00
Abstract: 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.
Abstract translation: 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。
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8.发明公开
公开(公告)号：KR1020090012190A
公开(公告)日：2009-02-02
申请号：KR1020080073710
申请日：2008-07-28
Applicant: 동화약품주식회사
IPC: C07D417/06 , C07D417/04 , C07D277/42
CPC classification number: C07D277/22 , C07D277/28 , C07D277/40 , C07D417/06
Abstract: 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.
Abstract translation: 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。
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