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公开(公告)号：KR101664969B1
公开(公告)日：2016-10-12
申请号：KR1020150025825
申请日：2015-02-24
Applicant: 한국과학기술연구원
IPC: C07D403/04 , C07D249/04 , A61K31/4192
Abstract: 본발명은미토콘드리아의기능을조절하여신경보호제로서의약효활성을보이면서동시에사이토크롬 P450 이소자임의활성이저하되어독성을유발하는약물과병용투여시에약물의독성을감소시키는 4-(2-벤질옥시페닐)-1-(피롤리딘-3-일)-1,2,3-트리아졸화합물과, 상기화합물의제조방법, 그리고상기화합물을포함하는약제조성물에관한것이다.
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公开(公告)号：KR101435496B1
公开(公告)日：2014-08-28
申请号：KR1020120117057
申请日：2012-10-22
Applicant: 한국과학기술연구원
IPC: C07D235/08 , C07D235/14 , A61K31/4184 , A61P25/00
CPC classification number: C07D413/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/28 , C07D401/06 , C07D403/06 , C07D403/12
Abstract: 본 발명은 미토콘드리아의 기능을 조절하여 신경보호제로서의 약학적 활성을 보이는 벤즈이미다졸 유도체, 및 이 화합물이 유효성분으로 함유된 약제조성물에 관한 것이다.
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公开(公告)号：KR1020130088492A
公开(公告)日：2013-08-08
申请号：KR1020120009756
申请日：2012-01-31
Applicant: 한국과학기술연구원
IPC: C07D471/04 , C07D217/04 , A61K31/4375 , A61P25/00
CPC classification number: C07D455/06 , C07F7/0812
Abstract: PURPOSE: A method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) is provided to simplify a process and to produce a large amount of TBZ or DTBZ. CONSTITUTION: A method for preparing TBZ comprises the steps of: performing alkylation of a compound of chemical formula 3 and a compound of chemical formula 4 to prepare a compound of chemical formula 5; performing aza-prins cyclization of the compound of chemical formula 5 under the presence of an oxidant to prepare a cyclic compound of chemical formula 6; and oxidizing the cyclic compound to convert a methylene group into a keto group and preparing TBZ of chemical formula 1.
Abstract translation: 目的：提供一种制备丁苯那嗪（TBZ）和二氢丁苯那嗪（DTBZ）的方法，以简化工艺并产生大量的TBZ或DTBZ。 构成：制备TBZ的方法包括以下步骤：进行化学式3的化合物和化学式4的化合物的烷基化以制备化学式5的化合物; 在氧化剂存在下进行化学式5的化合物的氮杂稠合环化，制备化学式6的环状化合物; 氧化环状化合物，将亚甲基转化为酮基，制备化学式1的TBZ。
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公开(公告)号：KR1020120096842A
公开(公告)日：2012-08-31
申请号：KR1020110016203
申请日：2011-02-23
Applicant: 한국과학기술연구원
Inventor： 추현아 , 배애님 , 조용서 , 이효선 , 이지은 , 조경희 , 임혜원 , 서선희 , 송치만 , 정혜진 , 남길수 , 금교창 , 김동진 , 최경일 , 최기현 , 이재균 , 강용구 , 박웅서 , 이주현 , 신선미 , 아미드,압둘와히드 , 김영수 , 민선준
IPC: C07D413/12 , A61K31/496 , A61P25/00 , A61P9/00
CPC classification number: C07D413/12
Abstract: PURPOSE: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is provided to have excellent activity as an antagonist of T- type calcium ion channel. CONSTITUTION: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is represented by chemical formula 1. The encephalopathy therapy and for prevention agent selected from epilepsy, depression, Parkinson's disease, dementia, sleep disorder, an agent for cancer treatment and prevention, an agent for heart disease treatment and prevention selected from hypertensive, cardiac arrhythmia, angina, myocardial infarction, congestive heart failure, pharmaceutical composition for alleviating pain selected from neuropathic pain and chronic and acute pain includes a compound represented by chemical formula 1.
Abstract translation: 目的：提供作为T型钙通道阻滞剂的5-（取代的烷基氨基甲基）异恶唑基化合物作为T-型钙离子通道的拮抗剂具有优异的活性。 构成：以化学式1表示作为T型钙通道阻断剂的5-（取代烷基氨基甲基）异恶唑类化合物。脑病治疗和预防药物选自癫痫，抑郁症，帕金森病，痴呆，睡眠障碍， 癌症治疗和预防，选自高血压，心律失常，心绞痛，心肌梗塞，充血性心力衰竭，减轻选自神经性疼痛和慢性和急性疼痛的疼痛的药物组合物的心脏病治疗和预防剂，包括由化学式 1。
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公开(公告)号：KR1020120088398A
公开(公告)日：2012-08-08
申请号：KR1020110009730
申请日：2011-01-31
Applicant: 한국과학기술연구원
IPC: C07D413/06 , C07D413/12 , A61K31/496 , A61P9/00
Abstract: PURPOSE: A pharmaceutical composition containing pentagonal heteroaromatic compound, a pharmaceutically acceptable salt thereof having a pharmaceutical activity to T-type calcium channel is provided to treat heart disease, brain diseases, stroma, chronic pain, neuropathic pain, and cancer. CONSTITUTION: A pentagonal heteroaromtaic compound with T-type calcium channel is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating stroma, hypertension, angina, chronic pain, neuropathic pain, and cancer contains the compound as an active ingredient. A method for preparing the compound comprises a step of binding carbochloride compound of chemical formula 3a and heterocyclic amine compounds of chemical formula 2a under the presence of an alkyl amine base.
Abstract translation: 目的：提供含有对T型钙通道具有药学活性的五价杂芳族化合物及其药学上可接受的盐的药物组合物，用于治疗心脏病，脑疾病，基质，慢性疼痛，神经性疼痛和癌症。 构成：用化学式1表示具有T型钙通道的五价杂合化合物。用于预防和治疗基质，高血压，心绞痛，慢性疼痛，神经性疼痛和癌症的药物组合物含有该化合物作为活性成分。 制备该化合物的方法包括在烷基胺基的存在下结合化学式3a的氯化碳化合物和化学式2a的杂环胺化合物的步骤。
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Patent Agency Ranking76.发明公开
公开(公告)号：KR1020110115374A
公开(公告)日：2011-10-21
申请号：KR1020100034846
申请日：2010-04-15
Applicant: 한국과학기술연구원
IPC: C07D243/08 , C07D243/06 , A61P9/12
Abstract: 본 발명은 T-형 칼슘 채널에 대한 활성을 갖는 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물, 상기 화합물의 제조방법, 그리고 상기 화합물을 유효성분으로 포함하는 약학조성물에 관한 것이다. 본 발명의 신규 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물 또는 약학적으로 허용 가능한 이의 염은 T-형 칼슘 채널에 대한 길항작용을 가지므로 간질, 고혈압 등의 뇌질환 치료제, 협심증 등의 심장질환 치료제, 만성 통증, 신경성 통증 등의 통증질환 치료제, 또는 항암제로 유용하다.
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公开(公告)号：KR101064258B1
公开(公告)日：2011-09-14
申请号：KR1020080135519
申请日：2008-12-29
Applicant: 한국과학기술연구원
Inventor： 한호규 , 남기달 , 신동윤 , 박찬호 , 조성우 , 김은아 , 남길수 , 최경일 , 서선희 , 신희섭 , 김동진 , 배애님 , 정혜진 , 추현아 , 임혜원 , 조용서 , 노은주 , 금교창 , 최기현 , 신계정 , 정찬성 , 이재균 , 강용구 , 김영수 , 박웅서 , 김기선 , 정혜선 , 송치만 , 민선준 , 김은경 , 이철주 , 강순방
IPC: C07D277/82 , C07D263/58 , C07D235/30 , A61P25/28
CPC classification number: C07D277/82 , C07D235/22 , C07D263/58 , C07D327/04 , C07D333/06
Abstract: 본 발명은 신규한 벤조아릴우레이도 화합물, 및 이의 퇴행성 뇌질환 예방 또는 치료에 있어서의 용도에 관한 것으로, 보다 상세하게는, 화학식 1의 구조를 갖는 벤조아릴우레이도 화합물, 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 예방 또는 치료용 조성물에 관한 것이다. 상기 퇴행성 뇌질환은 알츠하이머, 치매, 파킨슨병, 뇌졸중, 아밀로이드증, 픽 질환 (Pick's disease), 루게릭병, 헌팅턴병, 크로이츠펠트-야콥(Creutzfeld-Jakob)병 등일 수 있다.
[화학식 1]-
公开(公告)号：KR1020110020023A
公开(公告)日：2011-03-02
申请号：KR1020090077687
申请日：2009-08-21
Applicant: 한국과학기술연구원
IPC: C07D413/12 , C07D413/10
Abstract: PURPOSE: An oxazole-piperazine compound having a pharmaceutical activity with respect to T-type calcium channel is provided to ensure excellent activity as an antagonist of the channel and to prevent and treat cancer, epilepsy, heart diseases, and pain. CONSTITUTION: An oxazole-piperazine compounds is denoted by chemical formula 1. A pharmaceutical composition for treating epilepsy, cancer, hypertension, myocardial infarction, neuropathic pain, and acute and chronic pain contains the oxazole-piperazine compound of chemical formula 1. The compound of chemical formula 1 is prepared by reacting piperazine-amine compound of chemical formula 2 and oxazole aldehyde compound of chemical formula 3 by reductive amination. The reductive amination is performed under the presence of molecules of 4-8 meshes and NaBH(OAc)_3, NaBH_3CN, or NaBH_4.
Abstract translation: 目的：提供相对于T型钙通道具有药学活性的恶唑 - 哌嗪化合物，以确保作为通道拮抗剂的优异活性，并预防和治疗癌症，癫痫，心脏病和疼痛。 构成：化学式1表示恶唑 - 哌嗪化合物。用于治疗癫痫，癌症，高血压，心肌梗死，神经性疼痛和急性和慢性疼痛的药物组合物含有化学式1的恶唑 - 哌嗪化合物。 化学式1通过化学式2的哌嗪 - 胺化合物和化学式3的恶唑醛化合物通过还原胺化反应来制备。 还原胺化在4-8目和NaBH（OAc）3，NaBH 3 CN或NaBH 4的分子存在下进行。
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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：KR100645371B1
公开(公告)日：2006-11-14
申请号：KR1020050061697
申请日：2005-07-08
Applicant: 한국과학기술연구원
IPC: C07D493/04
Abstract: Novel bicyclic tetrahydrofuran derivatives, and a process for preparing the same compounds are provided to improve efficiency of preparation, so that they are useful as intermediates for synthesis of natural products. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are provided, wherein n is 1 or 2; R is phenyl group or substituted phenyl group by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is C1-C6 alkyl group. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenol derivatives in the presence of alcohol compounds, transition metal catalyst and carbon monoxide(CO), wherein the transition metal catalyst is palladium chloride or copper chloride; and the reaction temperature is 0 to 25 deg.C.
Abstract translation: 新型双环四氢呋喃衍生物及其制备方法可提高制备效率，因此它们可用作合成天然产物的中间体。 提供由式（1）表示的双环四氢呋喃衍生物，其中n是1或2; R 1为C 1 -C 6烷基，C 1 -C 6烷氧基，羟基或C 1 -C 6羟烷基的苯基或取代的苯基; 并且R 1是C 1 -C 6烷基。 由式（1）表示的双环四氢呋喃衍生物是在醇化合物，过渡金属催化剂和一氧化碳（CO）存在下通过分子内环化四氢呋喃 - 烯醇衍生物制备的，其中过渡金属催化剂为氯化钯或氯化铜; 反应温度为0〜25℃。
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