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：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：KR101043815B1

公开(公告)日：2011-06-27

申请号：KR1020090068834

申请日：2009-07-28

Applicant: 한국과학기술연구원 ,  서울대학교산학협력단

Inventor： 신계정 ,  노은주 ,  정민경 ,  차현주 ,  서선희

IPC: C07D309/34 ,  C07D213/06 ,  A61K31/351 ,  A61P31/00

CPC classification number: C07D213/06 ,  A61K31/351 ,  C07D309/34

Abstract: 본 발명은 하기 화학식 1로 표시되는 신규 3-페녹시-4-파이론, 3-페녹시-4-피리돈 또는 4-피리돈 유도체, 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 항균 조성물에 관한 것으로, 본 발명에 따른 신규 3-페녹시-4-파이론, 3-페녹시-4-피리돈 또는 4-피리돈 유도체를 함유하는 조성물은 박테리아 지방산 생합성 효소인 에노일-ACP 환원효소(FabI)를 효과적으로 억제하므로 항균제로서 유용하게 사용될 수 있다.
[화학식 1]
.
(상기 화학식 1에서, 상기 X, Y, R
1 및 R
2 는 본 명세서에서 정의된 바와 같다.)
박테리아 지방산 생합성, 3-페녹시-4-파이론, 3-페녹시-4-피리돈 또는 4-피리돈, 항균, 에노일-ACP 환원효소, FabI

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：KR1020090044924A

公开(公告)日：2009-05-07

申请号：KR1020070111220

申请日：2007-11-01

Applicant: 한국과학기술연구원

Inventor： 최경일 ,  남길수 ,  황현숙 ,  임혜원 ,  서선희 ,  신희섭 ,  김동진 ,  한호규 ,  조용서 ,  배애님 ,  신계정 ,  강순방 ,  신동윤 ,  추현아 ,  노은주

IPC: C07D401/12 ,  C07D401/14

Abstract: 본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제

Abstract translation: 本发明涉及一种药用根据新颖吡唑基 - 甲酰氨基烷基哌嗪衍生物及其制备方法和用这种化合物钙离子通道抑制作用在治疗疾病，其使用。

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。

公开(公告)号：KR1020040004862A

公开(公告)日：2004-01-16

申请号：KR1020020038929

申请日：2002-07-05

Applicant: 한국과학기술연구원

Inventor： 송충의 ,  노은주 ,  양정운

IPC: B01J20/02

CPC classification number: B01J31/06 ,  B01J35/023 ,  B01J35/1004 ,  B01J35/1052 ,  B01J37/0009 ,  C07C29/00

Abstract: PURPOSE: Provided are osmium tetroxide fixed onto porous adsorbent of nonionic polymer wherein the osmium tetroxide has low toxicity, and high activity and selectivity, the osmium tetroxide being capable of being recovered by a normal filtration and being reused, and further being capable of producing diols with high purity with high efficiency by being used as catalyst in a dihydroxylation process, a method for preparing the same and its use. CONSTITUTION: The osmium tetroxide-adsorbent complex comprises osmium tetroxide fixed onto porous nonionic polymer adsorbent which is a copolymer containing styrene, divinylbenzene, acrylate, or methacrylate monomer, has a pore with 50 to 1000Å and is 20 to 200 μm, wherein the surface area of the polymer is 200 to 1500 m¬2/g. The method comprises the steps of (a) dispersing porous nonionic polymer adsorbent into solvent, and (b) adding osmium tetroxide into the solution obtained at the step (a) so as to cause reaction between the adsorbent and osmium tetroxide, wherein the solvent is water, C1-C4 alcohol or its mixture solution and the reaction of the step (b) is performed at 0 to 60°C for 2 to 6 hrs. The osmium tetroxide is used as a catalyst in asymmetric dihydroxylation, thereby producing diols.

Abstract translation: 目的：提供四氧化锇固定在非离子聚合物的多孔吸附剂上，其中四氧化锇具有低毒性，高活性和选择性，四氧化锇能够通过正常过滤回收并再次使用，并且还能够生产二醇 通过在二羟基化方法中用作催化剂，其高纯度，高效率，其制备方法及其用途。 构成：四氧化锇 - 吸附剂络合物包括固定在多孔非离子聚合物吸附剂上的四氧化锇，其是含有苯乙烯，二乙烯基苯，丙烯酸酯或甲基丙烯酸酯单体的共聚物，具有50至1000埃的孔，为20至200微米，其中表面积 的聚合物为200〜1500m2 / g。 该方法包括以下步骤：（a）将多孔非离子聚合物吸附剂分散在溶剂中，（b）在步骤（a）中得到的溶液中加入四氧化锇，以使吸附剂与四氧化锇之间发生反应，其中溶剂为 水，C1-C4醇或其混合溶液，并且步骤（b）的反应在0至60℃下进行2至6小时。 四氧化锇用作不对称二羟基化反应中的催化剂，从而产生二醇。

公开(公告)号：KR100404587B1

公开(公告)日：2003-11-05

申请号：KR1020010011600

申请日：2001-03-07

Applicant: 한국과학기술연구원

Inventor： 송충의 ,  노은주

IPC: C07D301/03

Abstract: 본 발명은 키랄 에폭사이드를 제조하는 방법에 관한 것으로서, 구체적으로 이온성 액체 용매에서 키랄 살렌금속촉매 존재하에 올레핀과 산화제를 반응시켜 비대칭 에폭시화 반응에 의해 키랄 에폭사이드를 제조하는 방법에 관한 것으로, 본 발명의 제조방법에 의하면 반응 후 고가의 키랄 살렌금속촉매의 회수를 용이하게 하여 반복적으로 사용할 수 있으므로 경제적으로 키랄 에폭사이드를 제조할 수 있다.

公开(公告)号：KR100392710B1

公开(公告)日：2003-07-28

申请号：KR1020010015739

申请日：2001-03-26

Applicant: 한국과학기술연구원

Inventor： 송충의 ,  노은주 ,  오천림

IPC: C07C247/04 ,  C07D211/00 ,  C07D231/00

Abstract: PURPOSE: Provided is a process for producing a chiral compound by using an enantioselective ring-opening reaction of epoxides in the presence of a chiral salen metal catalyst, which can recover or reuse the chiral salen metal catalyst. CONSTITUTION: The chiral compound is produced by using the enantioselective ring-opening reaction of epoxides in the presence of a salt represented by the formula 1 and the chiral salen metal catalyst represented by the formula 3. In the formula 1, when X is nitrogen, Z is -C(R5)-, R1 and R2 are each C1-C18 alkyl, R3-R5 are each hydrogen or C1-C18 alkyl and when X is carbon, Z is -C(R5)-C(R6)-, R1 is C1-C18 alkyl, R2-R6 are each hydrogen or C1-C18 alkyl, n is an integer of 1-3, and Y- is an anion capable of forming a salt. In the formula 3, R1-R4 are independently hydrogen, alkyl, carboxyl, aryl, and substituted aryl, X1-X8 are independently hydrogen, halogen, alkyl, silyl, silyloxy, alkenyl, and etc., Y1 and Y2 are each hydrogen and alkyl, M is a metal, and A is an anion.

Abstract translation: 目的：提供一种在手性salen金属催化剂存在下使用环氧化物的对映选择性开环反应生产手性化合物的方法，该催化剂可以回收或再利用手性salen金属催化剂。 构成：手性化合物是通过在式1所示的盐和式3所示的手性salen金属催化剂存在下使用环氧化物的对映选择性开环反应而制备的。在式1中，当X是氮时， Z为-C（R 5） - ，R 1和R 2各自为C 1 -C 18烷基，R 3 -R 5各自为氢或C 1 -C 18烷基，并且当X为碳时，Z为-C（R 5）-C（R 6） - ， R1是C1-C18烷基，R2-R6各自是氢或C1-C18烷基，n是1-3的整数，Y-是能形成盐的阴离子。 在式3中，R 1 -R 4独立地为氢，烷基，羧基，芳基和取代的芳基，X 1 -X 8独立地为氢，卤素，烷基，甲硅烷基，甲硅烷氧基和链烯基等，Y 1和Y 2各自为氢， 烷基，M是金属，A是阴离子。

公开(公告)号：KR100386552B1

公开(公告)日：2003-06-02

申请号：KR1020000045098

申请日：2000-08-03

Applicant: 한국과학기술연구원 ,  한화화인케미칼 주식회사

Inventor： 송충의 ,  노은주 ,  김수창 ,  채기병 ,  김근식

IPC: C07C251/24

Abstract: PURPOSE: Provided are a chiral salen derivative bonded to a polymer and a chiral salen-metal complex produced from the chiral salen derivative polymer, wherein the chiral salen-metal complex is used as a chiral catalyst in an asymmetric epoxidation of olefin. CONSTITUTION: The chiral salen derivative is represented by the formula 1 and the chiral salen-metal complex is represented by the formula 5, wherein m is 0 or 1, n is an integer of 0-24, Y is O, NH, or C(O)NH, p is a polymer insoluble in water and organic solvents, H(1) and H(2) are trans each other, M is a transition metal ion selected from the group consisting of Cr, Mn, V, Fe, Mo, W, Ru, Co, Ti, and Os, and A is an anion selected from the group consisting of Cl-, CH3COO-, PF6-, and SbF6-.

Abstract translation: 目的：提供键合到聚合物上的手性salen衍生物和由手性salen衍生物聚合物产生的手性salen-金属配合物，其中手性salen-金属配合物用作烯烃的不对称环氧化中的手性催化剂。 构成：手性salen衍生物由式1表示，手性salen-金属配合物由式5表示，其中m为0或1，n为0-24的整数，Y为O，NH或C （O）NH，p是不溶于水和有机溶剂的聚合物，H（1）和H（2）彼此反式，M是选自Cr，Mn，V，Fe， Mo，W，Ru，Co，Ti和Os，并且A是选自Cl-，CH 3 COO-，PF 6 - 和SbF 6 - 的阴离子。