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1. 发明公开

KR1020100053458A 멜라노코틴 수용체의 항진제 有权
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020100053458A
公开(公告)日：2010-05-20
申请号：KR1020090108283
申请日：2009-11-10
申请人： 주식회사 엘지생명과학
发明人： 이구 , 이상대 , 문상필 , 안인애 , 최성필 , 이현호 , 심동섭 , 정수용 , 이현민
IPC分类号： C07D403/14 , C07D401/14 , A61K31/4025 , A61P3/10
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/496 , C07D207/16 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14
摘要： PURPOSE: A compound having excellent activity to melanocortin is provided to apply to functional agonist of the melanocortin receptor and to prevent and treat obesity, electrile dysfunction, diabetes, or inflammation. CONSTITUTION: A composition having excellent activity to melanocortin receptor is denoted by chemical formula 1. The compound of chemical formula 1 is obtained by amide-coupling a compound of chemical formula 2 with a compound of chemical formula 3. A method for preparing the compound of chemical formula 1 comprises: a step of deprotecting a compound of chemical formula 1' or 2'; a step of performing reductive amine reaction of oxo substituent with C1-C2 alkyl, C3-C7 cycloalkyl, or heterocycle; or a step of performing coupling reaction with arylhalide or hetero arylhalide. The composition contains pharmaceutically acceptable carrier, and the compound of chemical formula 1, pharmaceutically acceptable salt, or isomer. The composition is used for treating obesity, electrile dysfunction, diabetes, or inflammation.
摘要翻译：目的：提供对黑皮质素具有优异活性的化合物以适用于黑皮质素受体的功能性激动剂并预防和治疗肥胖症，电功能障碍，糖尿病或炎症。构成：化学式1表示对黑皮质素受体具有优异活性的组合物。化学式1的化合物通过化学式2的化合物与化学式3的化合物酰胺偶联而获得。一种制备化合物化学式1包括：使化学式1'或2'的化合物脱保护的步骤; 氧代取代基与C 1 -C 2烷基，C 3 -C 7环烷基或杂环进行还原胺反应的步骤; 或与芳基卤或异芳基卤化物进行偶联反应的步骤。组合物含有药学上可接受的载体，化学式1的化合物，药学上可接受的盐或异构体。该组合物用于治疗肥胖症，电疗功能障碍，糖尿病或炎症。

2. 发明公开

KR1020080062981A ＰＰＡＲγ의 활성을 항진시키는 신규 화합물, 그의제조방법, 및 이를 함유하는 약제학적 조성물 无效
标题翻译：作为PPARGAMMA的激素的化合物，其制备方法和包含其的药物组合物
公开(公告)号：KR1020080062981A
公开(公告)日：2008-07-03
申请号：KR1020060139217
申请日：2006-12-30
申请人： 주식회사 엘지생명과학
发明人： 김근태 , 한희운 , 주현우 , 송정욱 , 문상필 , 김승해 , 박옥구 , 전상권 , 구선영 , 임현주 , 허광청 , 김경희 , 이승주 , 이주연
IPC分类号： C07D207/34 , C07D401/12
摘要： A novel compound is provided to show excellent agonistic effect on peroxisome proliferator-activated receptor gamma(PPARgamma), thereby being used as a medicine for treating and preventing human PPARgamma related diseases such as diabetes, diabetic complications and inflammation. A compound as an agonist for PPARgamma is represented by a formula(1) and is prepared by reacting a compound represented by a formula(2) with a compound represented by a formula(3). In the formulae, A is oxazole or iso-oxazole which may be substituted or unsubstituted by a substituent selected from the group consisting of halogen, C1-4 alkyl, halogen substituted C1-4 alkyl and phenyl, or phenyl which may be substituted by 1-3 substituent(s) selected from the group consisting of hydroxy, halogen, C1-4 alkyl, halogen substituted C1-4 alkyl, C1-4 alkoxy, halogen substituted C1-4 alkoxy, phenyl, phenoxy, pyridinyl and pyridinyloxy; E is C(=)NG1G2 or CO2G3(wherein each G1, G2 and G3 is independently H, C1-8 alkyl, halogen substituted C1-8 alkyl, C1-8 alkoxy or halogen substituted C1-8 alkoxy); W is C6-10 aryl or heteroaryl which may be substituted or unsubstituted by one or 2 substituent(s) selected from the group consisting of halogen, C1-4 alkyl, halogen substituted C1-4 alkyl, C1-4 alkoxy and halogen substituted C1-4 alkoxy; X is halogen substituted or unsubstituted C1-8 alkyl; and L is Cl, Br, I or methane sulfonyl. A pharmaceutical composition for preventing or treating PPARgamma related diseases comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
摘要翻译：提供了一种新型化合物以显示对过氧化物酶体增殖物激活受体γ（PPARγ）的极好的激动作用，从而被用作治疗和预防人类PPARγ相关疾病如糖尿病，糖尿病并发症和炎症的药物。作为PPARγ的激动剂的化合物由式（1）表示，通过使由式（2）表示的化合物与式（3）表示的化合物反应来制备。在该式中，A是恶唑或异恶唑，其可以被选自卤素，C 1-4烷基，卤素取代的C 1-4烷基和苯基的取代基取代或未取代，或可被1个 3个取代基，选自羟基，卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基，卤素取代的C 1-4烷氧基，苯基，苯氧基，吡啶基和吡啶氧基; E为C（=）NG1G2或CO2G3（其中每个G1，G2和G3独立地为H，C1-8烷基，卤素取代的C1-8烷基，C1-8烷氧基或卤素取代的C1-8烷氧基）; W是可以被选自卤素，C 1-4烷基，卤素取代的C 1-4烷基，C 1-4烷氧基和卤素取代的C 1的一个或两个取代基取代或未取代的C 6-10芳基或杂芳基 -4-烷氧基 X为卤素取代或未取代的C 1-8烷基; L是Cl，Br，I或甲磺酰。用于预防或治疗PPARγ相关疾病的药物组合物包括式（1）化合物或其药学上可接受的盐和药学上可接受的载体。

3. 发明公开

KR1020080061610A ＰＰＡＲγ의 활성을 항진시키는 화합물, 그의 제조방법,및 이를 함유한 약제학적 조성물 无效
标题翻译：作为PPARGAMMA的激素的化合物，其制备方法和包含其的药物组合物
公开(公告)号：KR1020080061610A
公开(公告)日：2008-07-03
申请号：KR1020060136533
申请日：2006-12-28
申请人： 주식회사 엘지생명과학
发明人： 김근태 , 한희운 , 주현우 , 송정욱 , 문상필 , 김승해 , 박옥구 , 전상권 , 구선영 , 임현주 , 허광청 , 김경희 , 이승주 , 이주연
IPC分类号： C07D209/18 , C07D413/04
摘要： Compounds as agonist for PPARgamma(peroxisome proliferator-activated receptor gamma) are provided to activate human PPARgamma, reduce the amounts of glucose and insulin, and minimize side effects such as body weight increase, so that the compounds are useful for prevention and treatment of diabetes and hyperlipidemia as complication of diabetes. The compounds represented by the formula(1), its pharmaceutically acceptable salts or isomers activate PPARgamma, wherein A is a radical selected from a linear, branched or cyclic C1-C6 alkyl optionally substituted by halogen, structural formulae (1), (2), (3) and (4) in which R1 is hydrogen, halogen, linear or branched C1-C4 alkyl optionally substituted by halogen, or linear or branched C1-C4 alkoxy optionally substituted by halogen; R2 is linear or branched C1-C4 alkyl optionally substituted by halogen; and n is 0 or 1; X is linear or branched C1-C5 alkyl optionally substituted by halogen; Y is linear or branched C1-C5 alkoxy optionally substituted by halogen; Q is hydrogen, halogen, or linear or branched C1-C4 alkyl optionally substituted by halogen; D is selected from structural formulae (5) and (6) in which n is 0 or 1; E is hydrogen, halogen, linear or branched C1-C6 alkyl optionally substituted by halogen, or linear or branched C1-C6 alkoxy optionally substituted by halogen; and G is hydrogen. The compounds represented by the formula(1) are prepared by reacting compounds represented by the formula(2) with compounds represented by the formula(3) of H-D in the presence of base, wherein L is a leaving group.
摘要翻译：提供作为PPARγ（过氧化物酶体增殖物激活受体γ）的激动剂的化合物以激活人类PPARγ，减少葡萄糖和胰岛素的量，并尽量减少诸如体重增加的副作用，使得该化合物可用于预防和治疗糖尿病和高脂血症作为糖尿病并发症。由式（1）表示的化合物及其药学上可接受的盐或异构体活化PPARγ，其中A是选自被卤素任意取代的直链，支链或环状C 1 -C 6烷基的基团，结构式（1），（2），（3）和（4）其中R1是氢，卤素，任选被卤素取代的直链或支链C 1 -C 4烷基，或被卤素任选取代的直链或支链C 1 -C 4烷氧基; R2是任选被卤素取代的直链或支链C 1 -C 4烷基; 并且n为0或1; X是任选被卤素取代的直链或支链C 1 -C 5烷基; Y是任选被卤素取代的直链或支链C 1 -C 5烷氧基; Q是氢，卤素或任选被卤素取代的直链或支链C 1 -C 4烷基; D选自结构式（5）和（6），其中n为0或1; E是氢，卤素，任选被卤素取代的直链或支链C 1 -C 6烷基，或被卤素任选取代的直链或支链C 1 -C 6烷氧基; G为氢。由式（1）表示的化合物通过在碱存在下使由式（2）表示的化合物与H-D式（3）表示的化合物反应而制备，其中L为离去基团。

4. 发明授权

KR101141976B1 멜라노코틴 수용체의 항진제 有权
标题翻译：黑皮质素受体激动剂
公开(公告)号：KR101141976B1
公开(公告)日：2012-05-07
申请号：KR1020090108283
申请日：2009-11-10
申请人： 주식회사 엘지생명과학
发明人： 이구 , 이상대 , 문상필 , 안인애 , 최성필 , 이현호 , 심동섭 , 정수용 , 이현민
IPC分类号： C07D403/14 , C07D401/14 , A61K31/4025 , A61P3/10
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/496 , C07D207/16 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14
摘要： 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염 또는 이성체, 및 이를 유효성분으로 함유하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다:

상기 식에서 R
1 , R
2 , R
3 , R
4 및 R
5 는 명세서에 정의한 바와 같다.

5. 发明公开

KR1020080061599A ＰＰＡＲγ의 활성을 항진시키는 화합물, 그의 제조방법,및 이를 함유한 약제학적 조성물 无效
标题翻译：作为PPARGAMMA的激素的化合物，其制备方法和包含其的药物组合物
公开(公告)号：KR1020080061599A
公开(公告)日：2008-07-03
申请号：KR1020060136517
申请日：2006-12-28
申请人： 주식회사 엘지생명과학
发明人： 김근태 , 한희운 , 주현우 , 송정욱 , 문상필 , 김승해 , 박옥구 , 전상권 , 구선영 , 임현주 , 허광청 , 김경희 , 이승주 , 이주연
IPC分类号： C07D257/04 , C07D413/12
摘要： Compounds as agonist for PPARgamma(peroxisome proliferator-activated receptor gamma) are provided to increase insulin sensitivity and reduce the amounts of glucose and insulin by activating human PPARgamma, so that the compounds are useful for prevention and treatment of diabetes, complications related to diabetes, inflammation and osteoporosis. The compounds represented by the formula(1) function as agonist for PPARgamma, wherein A is selected from structural formulae(1) to (3); R1 is hydrogen, halogen, linear or branched C1-C4 alkyl optionally substituted by halogen, or linear or branched C1-C4 alkoxy optionally substituted by halogen; R2 is linear or branched C1-C5 alkyl optionally substituted by halogen; X is linear or branched C1-C5 alkyl optionally substituted by halogen; and D is hydrogen or a structural formula(4) in which R3 is hydrogen or linear, branched or cyclic C1-C6 alkyl optionally substituted by halogen. A method for preparing the compounds represented by the formula(1) comprises the steps of: reacting compounds represented by the formula(2) with compounds represented by the formula(3) in the presence of base to prepare compounds represented by the formula(4); and reacting the compounds represented by the formula(4) with trimethyltin azide, wherein L is a leaving group.
摘要翻译：提供作为PPARγ（过氧化物酶体增殖物激活受体γ）的激动剂的化合物以增加胰岛素敏感性并通过激活人PPARγ来减少葡萄糖和胰岛素的量，使得该化合物可用于预防和治疗糖尿病，与糖尿病有关的并发症，炎症和骨质疏松症。由式（1）表示的化合物用作PPARγ的激动剂，其中A选自结构式（1）至（3）; R1是氢，卤素，任选被卤素取代的直链或支链C 1 -C 4烷基，或被卤素任选取代的直链或支链C 1 -C 4烷氧基; R2是任选被卤素取代的直链或支链C 1 -C 5烷基; X是任选被卤素取代的直链或支链C 1 -C 5烷基; 和D是氢或结构式（4），其中R 3是氢或任选被卤素取代的直链，支链或环状的C 1 -C 6烷基。制备由式（1）表示的化合物的方法包括以下步骤：使由式（2）表示的化合物与由式（3）表示的化合物在碱的存在下反应，以制备由式（4）表示的化合物）; 并使由式（4）表示的化合物与叠氮化三甲基铵反应，其中L是离去基团。

6. 发明公开

KR1020070053622A ＰＰＡＲγ와 ＰＰＡＲα의 활성을 항진시키는 신규화합물, 그것의 제조방법및 그것을 함유한 약제 조성물 无效
标题翻译：新型化合物作为PPARgamma的助剂; 和PPARALPHA，其制备方法和含有其的药物组合物
公开(公告)号：KR1020070053622A
公开(公告)日：2007-05-25
申请号：KR1020060114304
申请日：2006-11-20
申请人： 주식회사 엘지생명과학
发明人： 김근태 , 한희운 , 고종성 , 김승해 , 김경희 , 정희경 , 박옥구 , 전상권 , 우성호 , 임현주 , 허광청 , 홍성운 , 구기동 , 이창석 , 장민선 , 구선영 , 주현우 , 송정욱 , 문상필 , 송미아
IPC分类号： C07D261/08 , C07D271/10 , C07D413/06
CPC分类号： A61K31/192 , C07C251/48 , C07C309/65 , C07C2601/08 , C07D209/22 , C07D209/42 , C07D213/643 , C07D239/34 , C07D261/08 , C07D263/20 , C07D265/36 , C07D271/10 , C07D277/28 , C07D401/12 , C07D413/06 , C07D413/12
摘要： 본 발명은 Peroxisome proliferator-activated receptor gamma (PPARγ)와 alpha (PPARα)의 활성을 항진시키는 신규 화합물, 그것의 제조방법 및 그것을 약리학적 유효량으로 함유하는 약제 조성물에 관한 것이다.

상기 식에서, A, D 및 X는 명세서에서 정의되어 있는 바와 같다.

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