公开(公告)号：KR1020140118141A

公开(公告)日：2014-10-08

申请号：KR1020130033552

申请日：2013-03-28

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  추현아 ,  임혜원 ,  금교창 ,  와니

IPC: C07D471/04 ,  A61K31/437 ,  A61P25/00

Abstract: The present invention relates to a novel 5-sulfonylamino-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one compound having an inhibitory activity for 5-HT6, which is one of serotonin subtypes, and a pharmaceutical composition comprising the compound as an active ingredient. Since the novel compound of the present invention has 5-HT6 inhibitory activities, the compound can be used for diagnosing, preventing, and treating central nervous system (CNS) diseases such as Alzheimer′s disease (AD), attention deficit disorder (ADHD), epilepsy, depression, obesity, schizophrenia, sleep disorders, and pain disorders.

Abstract translation: 本发明涉及对5-HT6具有抑制活性的新的5-磺酰基氨基-5,6-二氢-1H-吡唑并[3,4-c]吡啶-7（4H） - 酮化合物，其为5-羟色胺 亚型和包含该化合物作为活性成分的药物组合物。 由于本发明的新化合物具有5-HT 6抑制活性，所以该化合物可用于诊断，预防和治疗中枢神经系统（CNS）疾病如阿尔茨海默病（AD），注意缺陷障碍（ADHD） ，癫痫，抑郁症，肥胖，精神分裂症，睡眠障碍和疼痛障碍。

公开(公告)号：KR101389374B1

公开(公告)日：2014-06-05

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: 본 발명은 T-형 칼슘 채널에 대하여 약학적 활성을 보이는 5-(치환된알킬아미노메틸)아이속사졸계 화합물 및 약제학적으로 허용 가능한 이의 염, 이들 화합물의 제조방법, 그리고 이들 화합물이 유효성분으로 함유된 약제조성물에 관한 것이다.

公开(公告)号：KR101284174B1

公开(公告)日：2013-07-09

申请号：KR1020110000897

申请日：2011-01-05

Applicant: 한국과학기술연구원

Inventor： 배애님 ,  김은경 ,  금교창 ,  서선희 ,  홍승곤 ,  무하마드무다사

IPC: A61K31/435 ,  A61K31/4418 ,  A61P31/04 ,  A61P31/00

Abstract: 박테리아의 지방산 생합성을 억제하고, 마이코박테리아에 대한 항균제 및 감염 치료제로 유용한 신규 디페닐 유도체 또는 이의 약학적으로 허용되는 염, 및 이를 유효성분으로 함유하는 항균 조성물이 제공된다.

公开(公告)号：KR1020120066699A

公开(公告)日：2012-06-25

申请号：KR1020100093304

申请日：2010-09-27

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  박정은 ,  지완근 ,  신계정 ,  배애님 ,  최경일 ,  김동진 ,  금교창

IPC: C07D295/033 ,  A61K31/495 ,  A61P25/08 ,  A61P9/12

Abstract: PURPOSE: A pharmaceutical composition containing a novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propane-2-ol derivative is provided to effectively suppress T type calcium channel activation and to prevent or treat hypertension, cancer, epilepsy, and neurogenic pain. CONSTITUTION: A novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propan-2-ol derivative is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 comprises: a step of reacting a compound of chemical formula 2 with chiral epichlorohydrin under the presence of a base and solvent to prepare an epoxy compound of chemical formula 3; and a step of reacting the epoxy compound of chemical formula 3 with piperazine derivative of chemical formula 4. The base is potassium carbonate, sodium carbonate or pyridine. A pharmaceutical composition for preventing or treating diseases caused by overactivation of T type calcium channel contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract translation: 目的：提供含有新型1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物的药物组合物，以有效抑制T型钙通道激活和预防 或治疗高血压，癌症，癫痫和神经源性疼痛。 构成：化学式1表示新的1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物。一种制备化学式1化合物的方法 包括：在碱和溶剂的存在下使化学式2的化合物与手性表氯醇反应以制备化学式3的环氧化合物的步骤; 和使化学式3的环氧化合物与化学式4的哌嗪衍生物反应的步骤。碱是碳酸钾，碳酸钠或吡啶。 用于预防或治疗由T型钙通道过度活化引起的疾病的药物组合物含有其衍生物或药学上可接受的盐作为活性成分。

公开(公告)号：KR101124628B1

公开(公告)日：2012-06-12

申请号：KR1020090115388

申请日：2009-11-26

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  김은경 ,  배애님 ,  서선희 ,  홍승곤 ,  바타라이디팍 ,  슬린코인나 ,  조상래

IPC: C07C235/32 ,  A61K31/165 ,  A01N37/18 ,  C07C231/02

CPC classification number: Y02A50/473 ,  Y02A50/481

Abstract: PURPOSE: A triclosan derivative is provided to inhibit the activity of a FabI strain and to enable use as an antimicrobial agent for tuberculous bacillus including introspection strains and various strains. CONSTITUTION: A triclosan derivative is represented by chemical formula 1. In chemical formula 1, n is an integer of 1-6; X is primary or secondary amine, C1-C4 alkylamine, C1-C6 alkylamine including at least one hetero atom selected from oxygen and nitrogen, C5-C10 heterocyclic amine including at least one hetero atom selected from oxygen and nitrogen, phenylamine including at least one hydroxy group, phenylamine in which C1-C4 alkyl ester group or carboxylic acid is substituted, and 6-membered heteroarylamine including at least nitrogen.

公开(公告)号：KR101052065B1

公开(公告)日：2011-07-27

申请号：KR1020080101249

申请日：2008-10-15

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  김혜란 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  추현아 ,  임혜원 ,  조용서 ,  노은주 ,  금교창 ,  최기현 ,  신계정 ,  한호규 ,  정찬성 ,  이재균 ,  남기달 ,  강용구 ,  김영수 ,  박웅서 ,  김은경 ,  김기선 ,  정혜선 ,  신동윤 ,  송치만

IPC: C07D403/12 ,  C07D403/10

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12

Abstract: 본 발명은 칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체 및 이의 약제학적으로 허용 가능한 염, 이들 화합물의 제조방법, 그리고 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴메틸아민-피페라진 유도체, 칼슘이온 채널 조절제, 뉴런, 탈분극화, 급성통증, 만성통증, 신경병증성 통증, 고혈압치료제

Abstract translation: 本发明是有效的吡唑基甲胺作为钙离子通道调节剂 - 哌嗪衍生物和化学，以允许它的药学上可接受的盐，在疾病治疗由钙用于生产这些化合物和药物用于化合物工艺通道具有抑制作用 等等。

公开(公告)号：KR1020110058557A

公开(公告)日：2011-06-01

申请号：KR1020090115388

申请日：2009-11-26

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  김은경 ,  배애님 ,  서선희 ,  홍승곤 ,  바타라이디팍 ,  슬린코인나 ,  조상래

IPC: C07C235/32 ,  A61K31/165 ,  A01N37/18 ,  C07C231/02

CPC classification number: Y02A50/473 ,  Y02A50/481

Abstract: PURPOSE: A triclosan derivative is provided to inhibit the activity of a FabI strain and to enable use as an antimicrobial agent for tuberculous bacillus including introspection strains and various strains. CONSTITUTION: A triclosan derivative is represented by chemical formula 1. In chemical formula 1, n is an integer of 1-6; X is primary or secondary amine, C1-C4 alkylamine, C1-C6 alkylamine including at least one hetero atom selected from oxygen and nitrogen, C5-C10 heterocyclic amine including at least one hetero atom selected from oxygen and nitrogen, phenylamine including at least one hydroxy group, phenylamine in which C1-C4 alkyl ester group or carboxylic acid is substituted, and 6-membered heteroarylamine including at least nitrogen.

Abstract translation: 目的：提供三氯生衍生物以抑制FabI菌株的活性，并且可用作结核菌杆菌的抗微生物剂，包括内省菌株和各种菌株。 构成：三氯生衍生物由化学式1表示。在化学式1中，n为1-6的整数; X是伯或仲胺，C 1 -C 4烷基胺，包括至少一个选自氧和氮的杂原子的C 1 -C 6烷基胺，包括至少一个选自氧和氮的杂原子的C 5 -C 10杂环胺，包括至少一个 羟基，其中C 1 -C 4烷基酯基或羧酸被取代的苯胺和至少包含氮的6元杂芳基胺。

公开(公告)号：KR1020100042111A

公开(公告)日：2010-04-23

申请号：KR1020080101249

申请日：2008-10-15

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  김혜란 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  추현아 ,  임혜원 ,  조용서 ,  노은주 ,  금교창 ,  최기현 ,  신계정 ,  한호규 ,  정찬성 ,  이재균 ,  남기달 ,  강용구 ,  김영수 ,  박웅서 ,  김은경 ,  김기선 ,  정혜선 ,  신동윤 ,  송치만

IPC: C07D403/12 ,  C07D403/10

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12

Abstract: PURPOSE: A pyrazolylmethylamine-piperazine derivative which is effective as a calcium ion channel modulator is provided to ensure effective activation as an T-type calcium ion channel antagonist and to use as an agent for preventing and treating brain diseases, heart diseases and pain diseases. CONSTITUTION: A pyrazolylmethylamine-peperazine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases, heart diseases or pain diseases by T-type calcium ion channel antagonism contains the pyrazolylmethylamine-peperazine derivative of chemical formula 1 or its pharmaceutically acceptable salt an active ingredient. The brain disease is epilepsy, depression, Parkison's disease, dementia or somnipathy. The heart disease is hypertension, cardiac arrhythmia, myocardial infarction, or congestive failure. The pain disease is chronic pain, acute pain, or neurogenic pain. The pyrazolylmethylamine-peperazine derivative is prepared by binding pyrazolylmethylamine compound of chemical formula 3 with piperazine acetyl halide compound of chemical formula 2.

Abstract translation: 目的：提供作为钙离子通道调节剂有效的吡唑基甲胺 - 哌嗪衍生物，以确保作为T型钙离子通道拮抗剂的有效活化，并用作预防和治疗脑疾病，心脏病和疼痛疾病的药剂。 构成：吡唑基甲胺 - 哌嗪衍生物由化学式1表示。用于通过T型钙离子通道拮抗作用预防和治疗脑疾病，心脏病或疼痛疾病的药物组合物含有化学式1的吡唑基甲基 - 哌嗪衍生物或其药学上可接受的盐 可接受的盐为活性成分。 脑疾病是癫痫，抑郁症，帕金森病，痴呆或嗜睡。 心脏病是高血压，心律失常，心肌梗死或充血性衰竭。 疼痛疾病是慢性疼痛，急性疼痛或神经源性疼痛。 通过将化学式3的吡唑基甲基胺化合物与化学式2的哌嗪乙酰卤化合物结合，制备吡唑基甲胺 - 哌嗪衍生物。

公开(公告)号：KR100758317B1

公开(公告)日：2007-09-13

申请号：KR1020060039225

申请日：2006-05-01

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  김유승 ,  강순방 ,  임혜원 ,  장민석 ,  구일회

IPC: A61K31/5375 ,  A61P9/04

CPC classification number: A61K31/5375

Abstract: A composition for blocking T-type calcium channel comprising morpholin-2-one derivatives is provided to block the T-type calcium channel in the same level as the conventional T-type calcium channel blocker, mibefradil, without side effects. A composition for blocking T-type calcium channel comprises morpholin-2-one derivatives represented by the formula(1), or pharmaceutically acceptable salts thereof, wherein R^1 and R^2 are each independently hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy; and R^3 and R^4 are each independently hydrogen, C1-C6 alkyl, C1-C6 thioalkyl, amino or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy. The composition prevents or treats diseases caused by overexpression of T-type calcium channel including angina pectoris, hypertension, myocardiac infarction, pain and epilepsy.

Abstract translation: 提供一种用于阻断包含吗啉-2-酮衍生物的T型钙通道的组合物，以阻断与常规T型钙通道阻滞剂米非司酮相同水平的T型钙通道，无副作用。 用于阻断T型钙通道的组合物包括由式（1）表示的吗啉-2-酮衍生物或其药学上可接受的盐，其中R 1和R 2各自独立地为氢，C 1 -C 6烷基， C 6环烷基或任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的苯基; R 3和R 4各自独立地为氢，C 1 -C 6烷基，C 1 -C 6硫代烷基，任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的氨基或苯基。 该组合物预防或治疗由过度表达T型钙通道引起的疾病，包括心绞痛，高血压，心肌梗塞，疼痛和癫痫。

公开(公告)号：KR1020030034823A

公开(公告)日：2003-05-09

申请号：KR1020010066579

申请日：2001-10-27

Applicant: 한국과학기술연구원

Inventor： 김유승 ,  강순방 ,  금교창 ,  장민석 ,  장택수 ,  공재양 ,  정대영

IPC: C07D413/04

Abstract: PURPOSE: Isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative having high affinity for an acetylcholine receiptor is provided, which compound is useful as a muscarine type acetylcholine receiptor agonist, a recognition improving agent and a treating agent of cerebral nervous disease such as Alzheimer's disease. CONSTITUTION: The isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula(1) and a pharmaceutically acceptable salt thereof are provided, wherein R2 is C1-4 alkyl; one of R3 and R4 is one functional group in claim 1 and another of them is H; R5 is hydrogen, hydroxy, hydroxy C1-6 alkyl, C1-6 alkoxymethyl, C1-6 alkoxy, acetoxy, C1-4 alkyl ester, nitrile, aryl, phenylthio, methylthiomethyl, phenylsulfoxide, dimethylthiomethyl, C1-4 alkylketo, C1-4 alkylketo oxime, C1-4 alkylketo C1-5 alkyl oxime, and N-pyrrolidine-2-on; R6 is hydrogen; and R5 and F6 form -CH2OCH2 together. The process for preparing the isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula comprises the steps of: reacting 3- or 4-pyridine aldehyde oxime compound of formula(2) with chlorox to prepare nitrile oxide of formula(4); and cycloadddition reaction of nitrile oxide of formula(4) with alkene or alkyne compound of formula(8) or formula(9) to prepare a compound of formula(5) or formula(6); reacting the compound of formula(5) or formula(6) with alkyl iodide to prepare alkyl pyridine salt of formula(7); and reducing the alkyl pyridine salt of formula(7).

Abstract translation: 目的：提供对乙酰胆碱受体具有高亲和力的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物，该化合物可用作毒蕈碱型乙酰胆碱受体激动剂，识别改善剂和脑神经系统疾病的治疗剂 如阿尔茨海默病。 构成：提供由式（1）表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物及其药学上可接受的盐，其中R 2为C 1-4烷基; R3和R4之一是权利要求1中的一个官能团，另一个是H; R5是氢，羟基，羟基C1-6烷基，C1-6烷氧基甲基，C1-6烷氧基，乙酰氧基，C1-4烷基酯，腈，芳基，苯硫基，甲硫基甲基，苯基亚砜，二甲硫甲基，C1-4烷基酮，C1-4 烷基酮肟，C 1-4烷基酮C 1-5烷基肟和N-吡咯烷-2-酮; R6是氢; R5和F6一起形成-CH 2 OCH 2。 制备由式表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物的方法包括以下步骤：使式（2）的3-或4-吡啶醛肟化合物与氯氧反应制备式 （4）; 和式（4）的氧化腈与式（8）或式（9）的烯烃或炔化合物的环加成反应以制备式（5）或式（6）的化合物; 使式（5）或式（6）的化合物与烷基碘反应制备式（7）的烷基吡啶盐; 和还原式（7）的烷基吡啶盐。