公开(公告)号：KR1020110118441A

公开(公告)日：2011-10-31

申请号：KR1020100038033

申请日：2010-04-23

Applicant: 한국과학기술연구원 ,  주식회사 녹십자

Inventor： 배애님 ,  추현아 ,  조용서 ,  이지은 ,  박혜실 ,  박우규 ,  김정민 ,  이진화

IPC: C07D403/12 ,  C07D237/32 ,  C07D407/12 ,  A61P25/28

Abstract: 하기 화학식 1의 프탈라지논 유도체 또는 이의 약학적으로 허용 가능한 염은, 세로토닌 수용체 길항 작용과 세로토닌 재흡수 억제 작용을 동시에 지니고 있으므로, 이를 함유하는 약학적 조성물은, 우울증, 정신분열증, 불안증, 강박노이로제, 편두통, 식욕부진, 수면장애, 알츠하이머 병, 발작, 약물남용 등의 중추신경계에 관련된 질환 등의 치료제로서 유용하게 사용될 수 있다.
[화학식 1]

상기 식에서, R
1 내지 R
4 , n, p 및 q은 명세서에서 정의한 바와 같다.

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：KR1020100090979A

公开(公告)日：2010-08-18

申请号：KR1020090010234

申请日：2009-02-09

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  이재균 ,  민선준 ,  배애님 ,  추현아 ,  사티쉬샤브로

IPC: C07D307/90 ,  C07D307/93

Abstract: PURPOSE: An oxaspiro compound and a method for preparing the same are provided to be used as an intermediate in a natural product or novel drug synthesis. CONSTITUTION: An oxaspiro compound is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are hydrogen, alkyl group of C1-C6, halogen, nitro, alkyl of C1-C6, or substituted or non-substituted phenyl group as a substituent of C1-C6 alkoxy. The oxaspiro compound of chemical formula 1 is prepared by reacting a carbo compound of chemical formula 3 with methylene cycloalkandiol of chemical formula 2 under the presence of lewis acid. The reaction solvent is dichloro methane. Trimethylsilyl trifluoromethansulfonate(TMSOTf) is used as the lewis acid.

Abstract translation: 目的：提供氧杂螺环化合物及其制备方法，用作天然产物或新药合成中的中间体。 化学式1中，R1和R2为氢，C1-C6烷基，卤素，硝基，C1-C6烷基或取代或未取代的苯基，为 C1-C6烷氧基的取代基。 化学式1的氧杂螺环化合物通过在路易斯酸存在下使化学式3的碳化合物与化学式2的亚甲基环二醇反应来制备。 反应溶剂是二氯甲烷。 三氯甲磺酸三甲基甲硅烷基酯（TMSOTf）用作路易斯酸。

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：KR1020090090224A

公开(公告)日：2009-08-25

申请号：KR1020080015550

申请日：2008-02-20

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  이재균 ,  추현아 ,  배애님 ,  사티쉬샤브로

IPC: C07D309/04

CPC classification number: C07D309/06

Abstract: A method for manufacturing a tetrahydropyran derivative is provided to produce an intermediate for synthesizing functional natural material using a homopropagylic alcohol derivative and aldehyde compound. A tetrahydropyran derivative having cis-substituent on C2 and C6 is denoted by the chemical formula 1. In the chemical formula 1, R1 and R2 are separately C1-C6 alkyl group, C6-C15 aryl C1-C6 alkyl group, or C6-C15 aryl group. A method for manufacturing the tetrahydropyran derivative comprises a step of performing prince reaction of aldehyde compound of the chemical formula 3 with homopropagylic alcohol derivative of the chemical formula 2 to produce dihydropyran-3-ilyden triplate compound of the chemical formula 1a.

Abstract translation: 提供四氢吡喃衍生物的制造方法，以制备使用高分子量醇衍生物和醛化合物合成官能天然材料的中间体。 化学式1表示在C2和C6上具有顺式取代基的四氢​​吡喃衍生物。在化学式1中，R 1和R 2分别是C 1 -C 6烷基，C 6 -C 15芳基C 1 -C 6烷基或C 6 -C 15 芳基。 四氢吡喃衍生物的制造方法包括使化学式3的醛化合物与化学式2的异丙醇衍生物进行王子反应的步骤，得到化学式1a的二氢吡喃-3-基锂化合物。

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：KR1020090011376A

公开(公告)日：2009-02-02

申请号：KR1020070074889

申请日：2007-07-26

Applicant: 한국과학기술연구원

Inventor： 박혜영 ,  배애님 ,  임혜원 ,  윤주희

IPC: C07D295/145 ,  C07D241/04 ,  A61K31/4965

Abstract: A novel compound having antagonism in 5-HT7 receptor is provided to be usefully used for relax and treatment of disease mediated in 5-HT7 or symptom and to have good pharmaceutical properties. A novel compound having antagonism in 5-HT7 receptor is represented by a chemical formula (I). In the chemical formula (I), R1 is substitution radical selected from a group consisting of alkyl of C1~C4 substituted for halogen or nitro and alkoxy of C1~C4 or phenyl or benzyl; R2 is anisole naphthalene or quinoline; R3 is H, C1~C4 alkyl, halogen or C1~C4 alkoxy; R4 is H or C1~C3 alkyl not substituted for cyclo C5~C7 alkyl or phenyl.

Abstract translation: 提供了一种具有5-HT7受体拮抗作用的新化合物，可有效用于5-HT7或症状介导的疾病的放松和治疗，具有良好的药物性质。 在5-HT7受体中具有拮抗作用的新化合物由化学式（I）表示。 在化学式（I）中，R 1为选自被取代卤素或硝基的C 1 -C 4烷基和C 1 -C 4烷氧基或苯基或苄基的取代基; R2是苯甲醚萘或喹啉; R3是H，C1〜C4烷基，卤素或C1〜C4烷氧基; R4是H或C1-C3烷基，不代替环C5〜C7烷基或苯基。

公开(公告)号：KR100654328B1

公开(公告)日：2006-12-08

申请号：KR1020050079095

申请日：2005-08-26

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  고훈영 ,  배애님 ,  임혜원 ,  최인성

IPC: C07D401/12

Abstract: A novel piperazinylalkylpyrazole derivative is provided to be able to selectively block T-type calcium ion channels, thereby showing better pain, hypertension, and epilepsy therapeutic effect compared to conventional medicines. The piperazinylalkylpyrazole derivative is represented by the formula(1), where R1 is phenyl, X1-substituted phenyl(where X1 is nitro, methyl, chloro, or methoxy, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), 1,1-diphenylmethyl or X2-substituted diphenylmethyl(where X2 is chloro or methyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), R2 is H, methyl or ethyl, R3 is methyl, propyl, isobutyl, phenyl, cyclohexyl, substituted phenyl(methyl, chloro, or methoxy as a substituent), naphthyl, piperidinyl, R4 is H, C1-6 alkyl, 2-furyl, phenyl or X3-substituted phenyl(where X3 is chloro, methyl, cyclohexyl or piperidinyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), and n is an integer from 0 to 3.

Abstract translation: 提供了一种新的哌嗪基烷基吡唑衍生物，能够选择性阻断T型钙离子通道，因此与常规药物相比，表现出更好的疼痛，高血压和癫痫治疗效果。 哌嗪基烷基吡唑衍生物由式（1）表示，其中R 1为苯基，X 1取代的苯基（其中X 1为硝基，甲基，氯或甲氧基，取代位置为邻位，间位或对位， 三或四或全部能够被取代），1,1-二苯基甲基或X2-取代的二苯基甲基（其中X2是氯或甲基，取代位置是邻位，间位或对位，以及单，二，三，四或 全部能被取代），R2是H，甲基或乙基，R3是甲基，丙基，异丁基，苯基，环己基，取代的苯基（甲基，氯或甲氧基作为取代基），萘基，哌啶基，R4是H， C 1-6烷基，2-呋喃基，苯基或X 3 - 取代的苯基（其中X 3为氯，甲基，环己基或哌啶基，取代位置为邻位，间位或对位，并且单，二，三，四或全部 被取代），并且n是0至3的整数。

公开(公告)号：KR100645373B1

公开(公告)日：2006-11-14

申请号：KR1020050061721

申请日：2005-07-08

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  차주환 ,  배애님 ,  고훈영 ,  신철

IPC: C07D493/04

Abstract: Novel tricyclic tetrahydrofuran lactone derivatives, and a preparation process thereof are provided to reduce the preparation procedures of tricyclic tetrahydrofuran lactone derivatives into one step, so that preparation costs are reduced. The tricyclic tetrahydrofuran lactone derivatives represented by the formula(1) are provided in which R is phenyl group optionally substituted by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is hydrogen, C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group. The tricyclic tetrahydrofuran lactone derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenic acid derivatives represented by the formula(2) in the presence of phenyl halide, palladium catalyst and base; the reaction solvent is diethylether, tetrahydrofuran, dichloromethane, dimethylformamide, ethylacetate or chloroform; the palladium catalyst is tetrakis(triphenylphosphin) palladium; the base is carbonate, hydrogen carbonate or sulfate of alkali metals or alkali earth metals; and the reaction temperature is 0 to 90 deg.C.

Abstract translation: 提供新型三环四氢呋喃内酯衍生物及其制备方法，以将三环四氢呋喃内酯衍生物的制备过程减少为一步，从而降低制备成本。 提供了式（1）所示的三环四氢呋喃内酯衍生物，其中R为任选被C1-C6烷基，C1-C6烷氧基，羟基或C1-C6羟烷基取代的苯基; 和R1是氢，C1-C6烷基，C1-C6烷氧基，羟基或C1-C6羟烷基。 由式（1）表示的三环四氢呋喃内酯衍生物是在苯基卤化物，钯催化剂和碱的存在下，通过分子内环化式（2）表示的四氢呋喃 - 反应溶剂是乙醚，四氢呋喃，二氯甲烷，二甲基甲酰胺，乙酸乙酯或氯仿; 钯催化剂是四（三苯基膦）钯; 碱是碱金属或碱土金属的碳酸盐，碳酸氢盐或硫酸盐; 反应温度为0〜90℃。