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    사이클로펜타[ｄ][1,2]-옥사진 유도체
    31.
    发明公开
    사이클로펜타[ｄ][1,2]-옥사진 유도체 失效
    具有改善蛋白质磷酸酶（PPASE）抑制活性的环丙基（D）（1,2） - 恶唑衍生物

    公开(公告)号：KR1020040090614A

    公开(公告)日：2004-10-26

    申请号：KR1020030024557

    申请日：2003-04-18

    Applicant: 한국화학연구원

    Inventor： 최중권 ,  조성윤 ,  천혜경 ,  양승돈 ,  하재두 ,  안진희 ,  강승규 ,  김광록 ,  이상달 ,  정원훈

    IPC: C07D265/02

    Abstract: PURPOSE: Cyclopenta(d)(1,2)-oxazine derivatives are provided. The compounds have improved inhibiting activity on protein phosphatase(PPase) such as PTP-1B(protein tyrosine phosphatase 1B), CD45, LAR(leukocyte antigen-related), Cdc25B, VHR(vaccina human-related), Cdc25A, Cdc25C, Yop and PP1, so that they are useful for prevention and treatment of autoimmune disease, acute and chronic inflammation, diabetes, damaged glucose resistance, obesity, cancer, malignant disease, etc. CONSTITUTION: The cyclopenta(d)(1,2)-oxazine derivatives represented by formula (1), or pharmaceutically acceptable salts or optical isomers thereof are provided, wherein A is hydrogen, hydroxy, C1-C15 alkoxy, acetoxy, alkylcarbomethoxy, hydroxyacetamide or 3-oxydihydro-furan-2-one; B is hydrogen, chlorine or bromine containing halogen, hydroxy, carboxy or C1-C5 alkoxycarbonyl; D is hydrogen, or R1-(CO); E is optionally substituted aryl, optionally substituted C1-C15 alkyl, or optionally substituted C1-C15 alkyl or optionally substituted C7 to C20 arylalkyl; R2 is hydrogen, benzyl, hydroxyethyl, or CO2R3; R3 is hydrogen or C1-C5 alkyl; and R4 and R5 are independently hydrogen, optionally substituted C1-C15 alkyl, optionally substituted C7-C20 arylalkyl or nitrogen or oxygen containing ring-linked heteroalkyl.

    Abstract translation: 目的：提供环戊二烯（d）（1,2） - 恶嗪衍生物。 该化合物对蛋白磷酸酶（PPase）如PTP-1B（蛋白酪氨酸磷酸酶1B），CD45，LAR（白细胞抗原相关），Cdc25B，VHR（人类相关抗原），Cdc25A，Cdc25C，Yop和 PP1，因此它们可用于预防和治疗自身免疫性疾病，急性和慢性炎症，糖尿病，葡萄糖耐量降低，肥胖，癌症，恶性疾病等。构成：环戊二烯（d）（1,2） - 恶嗪衍生物 其中A为氢，羟基，C 1 -C 15烷氧基，乙酰氧基，烷基甲氧基，羟基乙酰胺或3-氧代二氢 - 呋喃-2-酮;或其药学上可接受的盐或旋光异构体。 B是氢，含氯或溴的卤素，羟基，羧基或C 1 -C 5烷氧基羰基; D是氢或R1-（CO）; E是任选取代的芳基，任选取代的C 1 -C 15烷基或任选取代的C 1 -C 15烷基或任选取代的C 7至C 20芳烷基; R2是氢，苄基，羟乙基或CO 2 R 3; R3是氢或C1-C5烷基; 并且R 4和R 5独立地为氢，任选取代的C 1 -C 15烷基，任选取代的C 7 -C 20芳烷基或含氮或含氧环的杂烷基。

    아다만틸기를 갖는 설파마이드 유도체를 유효성분으로 포함하는 뇌질환 또는 허혈성 심장질환의 예방 또는 치료용 조성물
    32.
    发明公开
    아다만틸기를 갖는 설파마이드 유도체를 유효성분으로 포함하는 뇌질환 또는 허혈성 심장질환의 예방 또는 치료용 조성물 有权
    用于预防或治疗具有作为活性成分的ADAMANTYL组的磺酰胺衍生物的脑疾病或异常心脏疾病的组合物

    公开(公告)号：KR1020140042991A

    公开(公告)日：2014-04-08

    申请号：KR1020120109316

    申请日：2012-09-28

    Applicant: 한국화학연구원

    Inventor： 김기영 ,  곽현정 ,  강승규 ,  이상달 ,  김희연 ,  정원훈 ,  안성훈 ,  이병호 ,  이정현 ,  서호원 ,  오광석

    IPC: A61K31/549 ,  A61P25/00 ,  A61P9/10

    CPC classification number: A61K31/549

    Abstract: The present invention relates to a pharmaceutical composition comprising a sulfamide derivative having an adamantyl group as an active ingredient for preventing or treating brain diseases or ischemic heart diseases. The sulfamide derivative compound having an adamantyl group according to the present invention can efficiently inhibit the activity of 11beta-HSD1, thereby being effectively used in preventing or treating not only ischemic heart diseases but also various 11beta-HSD1-mediated brain diseases such as neurodegenerative diseases, cerebrovascular diseases caused by ischemia or reperfusion, and mental diseases. [Reference numerals] (AA) Compounds of chemical formula 6(mg/kg)

    Abstract translation: 本发明涉及包含具有金刚烷基作为预防或治疗脑部疾病或缺血性心脏病的活性成分的磺酰胺衍生物的药物组合物。 具有根据本发明的金刚烷基的磺酰胺衍生物化合物可以有效地抑制11beta-HSD1的活性，从而有效地用于预防或治疗不仅缺血性心脏病，而且可用于各种11beta-HSD1介导的脑疾病如神经变性疾病 ，由缺血或再灌注引起的脑血管疾病和精神疾病。 （AA）化学式6化合物（mg / kg）

    아다만틸기를 갖는 설파마이드 유도체 및 이의 약제학적으로 허용 가능한 염
    34.
    发明公开
    아다만틸기를 갖는 설파마이드 유도체 및 이의 약제학적으로 허용 가능한 염 有权
    具有ADAMANTYL GROUP的药物及其药物可接受的盐

    公开(公告)号：KR1020120111965A

    公开(公告)日：2012-10-11

    申请号：KR1020120004235

    申请日：2012-01-13

    Applicant: 한국화학연구원

    Inventor： 김기영 ,  안진희 ,  강승규 ,  이상달 ,  배명애 ,  안성훈 ,  김희연 ,  정원훈 ,  강남숙

    IPC: C07C311/59 ,  A61K31/13 ,  A61K31/18 ,  A61P3/10

    CPC classification number: C07D417/04 ,  A61K31/18 ,  C07C307/10 ,  C07C2603/74 ,  C07D285/10 ,  C07D285/14 ,  C07D285/15 ,  C07D285/16 ,  C07D285/36 ,  C07D417/10 ,  C07D417/12

    Abstract: PURPOSE: A sulfamie derivative is provided to have excellent restraining activity to 11B-hydroxysteroid dehydrogenase type 1 and to be useful for preventing and treating various diseases mediated by 11B-HSD1. CONSTITUTION: A sulfamie derivative and pharmaceutically acceptable salts thereof are represented by chemical formula 1. In chemical formula 1, R^1 is H, C1-6 alkyl, cyano C1-6 alkyl, C3-8 cycloalkyl, substituted or unsubstituted benzyl, phenylethyl, C1-6 alkoxycarbonyl, phenylacetyl, naphthyl, or aryl of substituted 5-10 membered ring, R^2 and R^3 is respectively C1-6 alkyl or C2-6 alkenyl or R^2 and R^3 forms a ring, R^4 and R^5 is respectively H or C1-C^ alkyl, R^6 is H, OH, COOR^7 or CONR^7R^7, R^7 is H or C1-6 alkyl, and n is an integer from 1-3.

    Abstract translation: 目的：提供一种磺胺衍生物，对1型11B-羟类固醇脱氢酶具有优异的抑制活性，可用于预防和治疗11B-HSD1介导的各种疾病。 组成：氨基磺酸衍生物及其药学上可接受的盐由化学式1表示。在化学式1中，R 1是H，C 1-6烷基，氰基C 1-6烷基，C 3-8环烷基，取代或未取代的苄基，苯乙基 C 1-6烷氧基羰基，苯乙酰基，萘基或被取代的5-10元环的芳基，R 2和R 3分别是C 1-6烷基或C 2-6烯基，或者R 2和R 3形成环， R 4和R 5分别是H或C 1 -C 12烷基，R 6是H，OH，COOR 7或CONR 7 R 17，R 7是H或C 1-6烷基，n是 1-3的整数。

    Ｎ1-(펜에틸)-Ｎ2-치환된 바이구아나이드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물
    35.
    发明公开
    Ｎ1-(펜에틸)-Ｎ2-치환된 바이구아나이드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물 失效
    N1-（苯乙烯）-N取代的双胍衍生物，其制备方法和包含该化合物的药物组合物

    公开(公告)号：KR1020110053837A

    公开(公告)日：2011-05-24

    申请号：KR1020090110521

    申请日：2009-11-16

    Applicant: 한올바이오파마주식회사 ,  한국화학연구원

    Inventor： 김성욱 ,  전성수 ,  오병규 ,  강민석 ,  천혜경 ,  김광록 ,  이상달 ,  정원훈 ,  이종철

    IPC: C07C279/26 ,  C07C277/04 ,  A61K31/155 ,  A61P3/10

    Abstract: PURPOSE: An N1-(phenethyl)-N2-substituted biguanide derivative is provided to ensure excellent blood glucose drop action and lipid lowering action even with a little dosage compared existing drug and to enable use for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, steatosis, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer etc. CONSTITUTION: A compound or pharmaceutically acceptable salts are represented by chemical formula 1. In chemical formula 1, R is C1-12 alkyl, C1-12 alkenyl or C1-12 alkynyl substituted or unsubstituted with one or more substituents selected from C3-8 cycloalkyl and C5-12 aryl; C3-8 cycloalkyl substituted or unsubstituted with one or more substituents selected from halogen, hydroxyl, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 alkoxy and C5-12 aryl; and C5-12 aryl substituted or unsubstituted with one or more substituents selected from halogen, hydroxyl, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 alkoxy and C3-8 cycloalkyl.

    Abstract translation: 目的：提供N1-（苯乙基）-N2-取代双胍衍生物，以确保优异的血糖降低作用和降脂作用，即使与现有药物相比，用量少，可用于治疗糖尿病，肥胖，高脂血症，高胆固醇血症 ，脂肪变性，冠状动脉疾病，骨质疏松症，多囊卵巢综合征，代谢综合征，癌症等。构成：化学式1表示化合物或其药学上可接受的盐。在化学式1中，R是C 1-12烷基，C 1-12链烯基 或被一个或多个选自C 3-8环烷基和C 5--12芳基的取代基取代或未取代的C1-12炔基; 羟基，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6烷氧基和C 5-12芳基的取代或未取代的C 3-8环烷基; 和被选自卤素，羟基，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6烷氧基和C 3-8环烷基的一个或多个取代基取代或未取代的C 5-12芳基。

    싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물
    36.
    发明公开
    싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물 失效
    噻唑衍生物，其制备方法及包括其的药物组合物

    公开(公告)号：KR1020080016249A

    公开(公告)日：2008-02-21

    申请号：KR1020060078095

    申请日：2006-08-18

    Applicant: 한국화학연구원

    Inventor： 천혜경 ,  유성은 ,  조영식 ,  송진숙 ,  김희연 ,  정원훈 ,  배명애 ,  서지희 ,  이규양 ,  김낙정 ,  황순희 ,  송종환

    IPC: C07D277/42 ,  C07D277/36 ,  C07D277/34 ,  A61P29/00

    Abstract: A novel thiazole derivative is provided to inhibit effectively the enzymatic activity of 5-lipoxygenase(5-LO) acting when an arachidonic acid is converted into a leukotriene metabolite, thereby being used as a prophylactic and therapeutic agent of various inflammatory diseases and cancers. A thiazole derivative is represented by the formula(1), wherein each R1 and R2 is independently H, OR7, NO2, halogen or C1-4 linear, branched, or cyclic alkyl; each R3, R4, R5 and R6 is independently H, CF3, OR7, CO2R7, NR7R8, NO2, NHCOR7, C(=O)R7, SR7, halogen, C1-4 linear, branched or cyclic alkyl(in which each R7 and R8 is independently H, unsubstituted or F-substituted C1-6 linear, branched, or cyclic alkyl, or aryl); X is NH, O, S or SO2; Y is C or N. A method for preparing a thiazole derivative represented by the formula(1a) comprises a step of reacting an acetophenone derivative represented by the formula(2) with an aniline derivative represented by the formula(2) and a thiocyanate salt, wherein the R1 to R6, and Y are same as defined above. A pharmaceutical composition for preventing or treating asthma, chronic obstructive lung disease, arthritis, psoriasis, atopic dermatitis, allergy, enteritis, and cancer comprises the thiazole derivative, or a pharmaceutically acceptable salt thereof, a hydrate, solvate or isomer thereof as an effective ingredient.

    Abstract translation: 提供了一种新的噻唑衍生物，用于有效地抑制花生四烯酸转化为白三烯代谢物时作用的5-脂氧合酶（5-LO）的酶活性，从而用作各种炎性疾病和癌症的预防和治疗剂。 噻唑衍生物由式（1）表示，其中每个R 1和R 2独立地为H，OR 7，NO 2，卤素或C 1-4直链，支链或环状烷基; 每个R 3，R 4，R 5和R 6独立地是H，CF 3，OR 7，CO 2 R 7，NR 7 R 8，NO 2，NHCOR 7，C（= O）R 7，SR 7，卤素，C 1-4直链，支链或环状烷基（其中每个R 7和 R8独立地是H，未取代的或F-取代的C 1-6直链，支链或环状烷基或芳基）; X是NH，O，S或SO 2; Y为C或N.由式（1a）表示的噻唑衍生物的制备方法包括使式（2）表示的苯乙酮衍生物与式（2）表示的苯胺衍生物和硫氰酸盐 ，其中R1至R6和Y与上述定义相同。 用于预防或治疗哮喘，慢性阻塞性肺病，关节炎，牛皮癣，特应性皮炎，过敏，肠炎和癌症的药物组合物包含噻唑衍生物或其药学上可接受的盐，其水合物，溶剂化物或异构体作为有效成分 。

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