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1. 发明授权

KR100854584B1 피리다지논, 피리미돈 또는 피리돈 구조를 포함하는선택적인 트롬빈 억제제 失效
标题翻译：基于哒嗪酮，嘧啶酮或吡啶酮支架的选择性凝血酶抑制剂
公开(公告)号：KR100854584B1
公开(公告)日：2008-08-27
申请号：KR1020070027069
申请日：2007-03-20
申请人： 주식회사 엘지생명과학
发明人： 박태교 , 이현호 , 박종우 , 송호영 , 최증순 , 박희동 , 김태훈 , 김경희 , 이태수 , 장민선 , 이재익 , 권태식 , 하용화 , 서동욱 , 최윤희 , 이정애 , 오영수 , 백승엽 , 김형진 , 박미정 , 윤하식 , 정수용
IPC分类号： C07D237/14 , C07D237/22 , C07D401/10
摘要： 본 발명은 트롬빈에 대한 억제 활성과 선택성이 높은 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 수화물, 용매화물, 이성체, 대사산물, 또는 전구약물에 관한 것이다. 본 발명은 또한 화학식 1의 화합물을 제조하는 방법, 및 화학식 1의 화합물을 유효 성분으로 함유함을 특징으로 하여 트롬빈에 의해 매개되는 질병 치료에 탁월한 효과를 나타내는 약제학적 조성물에 관한 것이다.

상기 식에서 A, B, R
3 , R
4 , R
5 , P
1 , L, Q, m, n 및 k는 명세서에 정의한 바와 같다.
피리다지논, 피리미돈, 피리돈, 선택적 트롬빈 억제, 혈전증

2. 发明公开

KR1020080007051A 멜라노코틴 수용체의 항진제 无效
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020080007051A
公开(公告)日：2008-01-17
申请号：KR1020060066610
申请日：2006-07-14
申请人： 주식회사 엘지생명과학
发明人： 최성필 , 안인애 , 이상협 , 이상대 , 신미숙 , 이구 , 최덕영 , 심동섭 , 임현주 , 윤민경 , 정수용 , 이정애 , 하용화 , 김영관
IPC分类号： C07D403/06 , C07D405/14 , C07D417/14 , C07D403/14
摘要： A novel compound is provided to be effective as melanocortin receptor agonists and particularly effective as selective agonists of melanocortin-4 receptor(MC-4R), thereby being useful for preventing and treating obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and inflammation. A compound as a melanocortin receptor agonist is represented by the formula(1), wherein R^1 is H, amidino, C1-4 alkylamidino, C1-4 alkanoylamidino, C1-10 alkyl, C3-7 cycloalkyl, C6-10 aryl, heterocycle, heteroaryl, C1-6 alkylcarbonyl, C3-7 cycloalkylcarbonyl, C1-4 alkoxycarbonyl, (C6-10)-aryl-(C1-4)alkoxycarbonyl, SO2-(C1-4)alkyl, C(O)N(R^5)(R^6) or C(S)N(R^5)(R^6)(each R^5 and R^6 is independently H, C1-6 alkyl or C3-7 cycloalkyl); R^2 is C6-10 aryl which may be mono- or di-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-4 alkyl and C1-4 alkoxy; R^3 is C3-8 cycloalkyl, heterocycle, C6-10 aryl or heteroaryl; and R^4 is H, C1-6 alkyl, C(O)R^7, (CH2)p-(C6-10)aryl, (CH2)p-heterparyl or (CH2)p-(C3-8)cycloalkyl(where p is 1 or 2, and R^7 is C1-10 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, amino, C1-4 alkylamino, (C1-4)alkyl(C1-4 alkyl)amino, SO2-(C1-7)alkyl, C6-10 aryl, heteroaryl or heterocycle). A method for preparing the compound of the formula(1) comprises a step of amide-coupling a compound represented by the formula(2) with a compound represented by the formula(3). A functional agonist composition of melanocortin receptor comprises a pharmaceutically acceptable carrier and the compound of the formula(1), a pharmaceutically acceptable salt thereof or an isomer thereof.
摘要翻译：提供新的化合物作为黑皮质素受体激动剂是有效的，并且特别有效作为黑皮质素-4受体（MC-4R）的选择性激动剂，因此可用于预防和治疗肥胖症，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍，和炎症。作为黑皮质素受体激动剂的化合物由式（1）表示，其中R 1是H，脒基，C 1-4烷基脒基，C 1-4烷酰基脒基，C 1-10烷基，C 3-7环烷基，C 6-10芳基，杂环，杂芳基，C 1-6烷基羰基，C 3-7环烷基羰基，C 1-4烷氧基羰基，（C 6-10） - 芳基 - （C 1-4）烷氧基羰基，SO 2 - （C 1-4）烷基，C（O）（R ^ 6）或C（S）N（R 5）（R 6）（每个R 5和R 6独立地是H，C 1-6烷基或C 3-7环烷基）; R 2是可以被选自卤素，羟基，C 1-4烷基和C 1-4烷氧基的取代基单取代或二取代的C 6-10芳基; R 3是C 3-8环烷基，杂环，C 6-10芳基或杂芳基; 且R 4为H，C 1-6烷基，C（O）R 9，（CH 2）p - （C 6-10）芳基，（CH 2）p - 杂芳基或（CH 2）（其中p为1或2，R 7为C 1-10烷基，C 2-6烯基，C 3-8环烷基，C 3-8环烯基，氨基，C 1-4烷基氨基，（C 1-4）烷基（C 1-4）烷基）氨基，SO 2 - （C 1-7）烷基，C 6-10芳基，杂芳基或杂环）。制备式（1）化合物的方法包括将由式（2）表示的化合物与式（3）表示的化合物酰胺偶联的步骤。黑皮质素受体的功能性激动剂组合物包含药学上可接受的载体和式（1）的化合物，其药学上可接受的盐或其异构体。

3. 发明公开

KR1020070095236A 피리다지논, 피리미돈 또는 피리돈 구조를 포함하는선택적인 트롬빈 억제제 失效
标题翻译：基于吡咯烷酮，吡咯烷酮或吡咯烷酮的选择性硫蛋白抑制剂
公开(公告)号：KR1020070095236A
公开(公告)日：2007-09-28
申请号：KR1020070027069
申请日：2007-03-20
申请人： 주식회사 엘지생명과학
发明人： 박태교 , 이현호 , 박종우 , 송호영 , 최증순 , 박희동 , 김태훈 , 김경희 , 이태수 , 장민선 , 이재익 , 권태식 , 하용화 , 서동욱 , 최윤희 , 이정애 , 오영수 , 백승엽 , 김형진 , 박미정 , 윤하식 , 정수용
IPC分类号： C07D237/14 , C07D237/22 , C07D401/10
摘要： A novel compound is provided to secure excellent thrombin inhibitory activity and excellent selectivity on the thrombin and is able to be orally absorbed. And a method for preparing the same and a pharmaceutical composition comprising the same are provided. A compound is represented by the formula(1), wherein A is N or CR^1, B is N or CR^2, each R^3 and R^4 is H, OH, halogen, CN, CF3, or C1-8 alkyl, or R^3 and R^4 together with a carbon atom attached thereto forms C=O, 3 to 8 membered cycloalkyl, or 3 to 8 membered heterocycle having at least one atom selected from the group consisting of N, O and S, R^5 is (a) H, (b) halogen, (c) CN or CH2CN, (d) CF3, OR^6, S(O)0-2R^6, C(=O)R^6, S(O)2NHR^6, and NR^6R^6a, (e) halogen, CN, CF3, OH, and phenyl substituted or unsubstituted by C1-4 alkoxy, (f) halogen, OH, CN, C1-8 alkoxy, COOH, COO-C1-8 alkyl and C1-8 alkyl mono-substituted or poly-substituted by COO-C1-8 alkyl, (g) halogen, OH, CN, C1-8 alkoxy, COOH, COO-C1-8 alkyl and 3 to 8 membered cycloalkyl mono-substituted or poly-substituted by COO-C1-8 alkyl, or (h) 3 to 8 membered heterocycle or 5 to 8 membered heteroaryl including at least one hetero atom selected from the group consisting of N, O and S, m is an integer from 0 to 3, n is an integer from 1 to 6, k is an integer from 0 to 3, and P1 is C1-8 alkyl substituted or unsubstituted by one or two radicals selected from R^7 and R^7, C2-8 alkenyl, 3 to 8 membered cycloalkyl, 4 to 8 membered cycloalkenyl, phenyl, 3 to 8 membered heterocycle including 1-5 heteroatoms selected from the group consisting of N, O and S, or 5 to 8 membered heteroaryl including 1-5 heteroatoms selected from the group consisting of N, O and S.
摘要翻译：提供了一种新颖的化合物以确保优良的凝血酶抑制活性和对凝血酶的优异选择性，并且能够被口服吸收。并提供其制备方法和包含其的药物组合物。化合物由式（1）表示，其中A是N或CR 1，B是N或CR 2，每个R 3和R 4是H，OH，卤素，CN，CF 3或C1- 8烷基或R 3和R 4与连接的碳原子一起形成C = O 3至8元环烷基或具有至少一个选自N，O的原子的3至8元杂环，以及 S，R 5是（a）H，（b）卤素，（c）CN或CH 2 CN，（d）CF 3，OR 6，S（O）0-2R 6，C（= O），（C）卤素，CN，CF 3，OH和被C 1-4烷氧基取代或未取代的苯基，（f）卤素，OH，CN，C 1-8 烷氧基，COOH，COO-C 1-8烷基和被COO-C 1-8烷基单取代或多取代的C 1-8烷基，（g）卤素，OH，CN，C 1-8烷氧基，COOH，COO- 8烷基和3至8元环烷基，其被COO-C 1-8烷基单取代或多取代，或（h）3至8元杂环或5至8元杂芳基，包括至少一个选自以下的杂原子： N，O和S，m为0〜3的整数，n为整数 r为1至6，k为0至3的整数，P1为被一个或两个选自R 7和R 7的基团取代或未取代的C 1-8烷基，C 2-8链烯基，3至8元环烷基，4至8元环烯基，苯基，3至8元杂环，包括1-5个选自N，O和S的杂原子，或5至8元杂芳基，包括1-5个选自N， O和S.

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