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公开(公告)号：KR1020100005476A
公开(公告)日：2010-01-15
申请号：KR1020080065522
申请日：2008-07-07
Applicant: 한국과학기술연구원
IPC: C07D403/12
CPC classification number: C07D401/12 , A61K31/454
Abstract: PURPOSE: An isoindolinone derivative having pharmaceutical activation to T-type calcium channel is provided to have antagonistic activity to T-type calcium channel and use as a therapeutic agent for hypertension, cancer, and neurogenic pain. CONSTITUTION: An isoindolinone derivative is denoted by chemical formula 1. In chemical formula 1, R1 is hydrogen atom, halogen atom, alkoxy group of C1-C6, haloalkyl group of C1-C6, nitro group, cyano group, or hydroxyl group. R2 is hydrogen atom, alkyl group of C1-C6, or aryl group. The isoindolinone derivative is obtained by reacting piperidinyl propylamine derivative of chemical formula 9 with isoindolinone carboxylic acid derivative of chemical formula 8 through amide reaction. A pharmaceutical composition for treating hypertension, cancer, epilepsy, and neurogenic pain contains the isoindolinone derivative and its pharmaceutically acceptable salt.
Abstract translation: 目的：提供具有T型钙通道药学活性的异吲哚啉酮衍生物，对T型钙通道具有拮抗作用，用作高血压，癌症和神经源性疼痛的治疗剂。 构成：异吲哚啉酮衍生物由化学式1表示。在化学式1中，R 1为氢原子，卤素原子，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，硝基，氰基或羟基。 R2是氢原子，C1-C6烷基或芳基。 异吲哚啉酮衍生物通过化学式9的哌啶基丙胺衍生物与化学式8的异吲哚酮羧酸衍生物反应而得到。 用于治疗高血压，癌症，癫痫和神经原性疼痛的药物组合物含有异吲哚啉酮衍生物及其药学上可接受的盐。
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公开(公告)号：KR100892591B1
公开(公告)日：2009-04-08
申请号：KR1020070117886
申请日：2007-11-19
Applicant: 한국과학기술연구원
IPC: C07C229/58 , C07C229/52
CPC classification number: C07C229/58
Abstract: A chloride channel blocking agent containing anthranilic acid derivative is provided to show excellent validity and selectivity which result from excellent blocking activities of the anthranilic acid derivative. An anthranilic acid derivative is a compound having a structure represented by the formula I. In the formula I, R1 and R2 are independently selected from the group consisting of pentyl group, hexyl group, heptyl group, octyl group, decyl group, dodecyl group, tetradecyl group, hexadecyl group, cyclohexyl group, phenyl group, benzyl group, racemic-alphamethyl-benzyl group, chiral-alpha methyl-benzyl group, trifluoromethyl group, ethoxy group, butyloxy group, pentyloxy group, hexyloxy group, trifluoromethyloxy group and nitro group or two identical or different halogen atoms.
Abstract translation: 提供含有邻氨基苯甲酸衍生物的氯化物通道阻断剂，以显示由于邻氨基苯甲酸衍生物的优异的阻断活性而产生的优异的有效性和选择性。 邻氨基苯甲酸衍生物是具有由式I表示的结构的化合物。在式I中，R 1和R 2独立地选自戊基，己基，庚基，辛基，癸基，十二烷基， 十四烷基，十六烷基，环己基，苯基，苄基，外消旋 - 甲基 - 苄基，手性-α甲基 - 苄基，三氟甲基，乙氧基，丁氧基，戊氧基，己氧基，三氟甲氧基和硝基 或两个相同或不同的卤素原子。
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公开(公告)号：KR1020010060120A
公开(公告)日：2001-07-06
申请号：KR1019990068242
申请日：1999-12-31
Applicant: 한국과학기술연구원 , 한화화인케미칼 주식회사
IPC: C07C51/00
Abstract: PURPOSE: A method for preparing ethyl (R)-2-bromo-4-phenylbutyrate and intermediates for preparing the compound are provided, which compound is useful as the intermediate for the preparation of antihypertensive. CONSTITUTION: The intermediates for preparing ethyl (R)-2-bromo-4-phenylbutyrate represented by the formula 1 is the oxazolidinone derivatives of 4-phenylbutyric acid represented by the formula 2, and the oxazolidinone derivatives of (2R)-2-bromo-4-phenylbutyric acid represented by the formula 3. The method comprises the steps of reacting 4-phenylburyric acid and the oxazolidinone of the formula 5 to obtain the compound of the formula 2; reacting the compound of the formula 2 and a bromization agent to obtain the compound of the formula 3; and reacting the compound of the formula 3 and a nucleophilic ethoxide to obtain the compound of the formula 1. Preferably the bromization agent is N-bromosuccinimide or bromine; and the ethoxide is lithium ethoxide, sodium ethoxide, magnesium ethoxide or titanium ethoxide. In the formulas 1, 2, 3 and 5, R1 is a methyl group and R2 is a phenyl group, or R1 is a phenyl group and R2 is H.
Abstract translation: 目的：提供（R）-2-溴-4-苯基丁酸乙酯的制备方法和制备该化合物的中间体，该化合物可用作制备抗高血压药物的中间体。 构成：由式1表示的（R）-2-溴-4-苯基丁酸乙酯的中间体是由式2表示的4-苯基丁酸的恶唑烷酮衍生物，（2R）-2-溴的恶唑烷酮衍生物 -4-苯基丁酸。该方法包括使4-苯基丙酸与式5的恶唑烷酮反应得到式2化合物的步骤; 使式2的化合物与溴化剂反应得到式3的化合物; 并使式3化合物与亲核乙醇盐反应，得到式1的化合物。优选溴化剂为N-溴代琥珀酰亚胺或溴; 乙醇钠是乙醇锂，乙醇钠，乙醇镁或乙醇钛。 在式1，2，3和5中，R 1是甲基，R 2是苯基，或者R 1是苯基，R 2是H.
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