公开(公告)号：KR1020090084149A

公开(公告)日：2009-08-05

申请号：KR1020080010155

申请日：2008-01-31

Applicant: 한국과학기술연구원

Inventor： 이창준 ,  노은주 ,  최진규 ,  한경석 ,  박정은 ,  강상수

IPC: A61K31/522 ,  A61K31/52 ,  A61P35/00

CPC classification number: A61K31/522

Abstract: A composition which contains caffeine, its analog, or its pharmaceutically allowable salt is provided to suppress infiltration, metastasis, and proliferation and prevent and/or treat brain cancer. A composition for preventing and treating brain cancer comprises caffeine, caffeine anaolog, or its pharmaceutically allowable salt as an active ingredient. The caffeine, caffeine analog or its pharmaceutically allowable salt has the content of 0.3-30 mM. The daily dose of the composition is 1-5 mg/kg and the composition is administered at one time or several times. The brain cancer is glioma, exothelioma, pituitary adenoma, schwannoma, craniopharyngioma or the congenital brain tumor. The composition selectively block the subtype 3 of activation of inositol-1,4,5-triphosphate receptoer(IP3R).

Abstract translation: 提供含有咖啡因，其类似物或其药学上可允许的盐的组合物以抑制浸润，转移和增殖，并预防和/或治疗脑癌。 用于预防和治疗脑癌的组合物包括咖啡因，咖啡因厌氧菌或其药学上可允许的盐作为活性成分。 咖啡因，咖啡因类似物或其药学上允许的盐的含量为0.3-30mM。 组合物的日剂量为1-5mg / kg，组合物一次或多次施用。 脑癌是神经胶质瘤，外皮瘤，垂体腺瘤，神经鞘瘤，颅咽管瘤或先天性脑瘤。 组合物选择性阻断肌醇-1,4,5-三磷酸盐受体（IP3R）的活化亚型3。

公开(公告)号：KR100848601B1

公开(公告)日：2008-07-28

申请号：KR1020070022119

申请日：2007-03-06

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  박정환 ,  최진규 ,  이은정

IPC: C07D295/104 ,  C07D401/06

Abstract: Alkanoyl piperazine derivatives are provided to block the T-type calcium channel in nerve cells and inhibit side effects, so that the compounds are useful for prevention and treatment of neuropathic pain, hypertension, angina pectoris, heart failure or arrhythmia. The alkanoyl piperazine derivatives represented by the formula(1) are prepared by reacting compounds represented by the formula(2) with carbonyl compound of which ends are substituted by halogen to prepare compounds represented by the formula(3), and reacting the compounds represented by the formula(3) with piperazine compound having a substituent at N-1 site to induce C-N coupling, wherein R is C1-C4 linear or branched alkyl, benzyl optionally substituted by 1 or more than 2 halogen or C1-C4 alkoxy, phenyl optionally substituted by 1 or more than 2 halogen or C1-C4 alkoxy, or C5-C10 monocyclo or C5-C10 bicycloaryl having at least one hetero atom selected from N, O or S; X is halogen, C1-C4 linear or branched alkyl optionally substituted by halogen, C1-C4 alkoxy optionally substituted by halogen or cyano group; and n is an integer from 1 to 10 and m is an integer from 0 to 5.

Abstract translation: 提供烷酰基哌嗪衍生物以阻断神经细胞中的T型钙通道并抑制副作用，使得该化合物可用于预防和治疗神经性疼痛，高血压，心绞痛，心力衰竭或心律失常。 式（1）表示的烷酰基哌嗪衍生物通过使式（2）表示的化合物与其末端被卤素取代的羰基化合物反应，制备由式（3）表示的化合物，并使由 式（3）与在N-1位具有取代基的哌嗪化合物诱导CN偶联，其中R是C1-C4直链或支链烷基，任选被1或多于2个卤素或C 1 -C 4烷氧基取代的苄基，任选的苯基 或具有至少一个选自N，O或S的杂原子的C 5 -C 10单环或C 5 -C 10二环芳基取代的卤素或C 1 -C 4烷氧基; X是卤素，任选被卤素取代的C 1 -C 4直链或支链烷基，任选被卤素或氰基取代的C 1 -C 4烷氧基; n为1〜10的整数，m为0〜5的整数。