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    싸이아졸리딘 유도체 및 이의 제조 방법
    14.
    发明公开
    싸이아졸리딘 유도체 및 이의 제조 방법 无效
    噻唑烷衍生物及其制备方法

    公开(公告)号：KR1020100094337A

    公开(公告)日：2010-08-26

    申请号：KR1020097017134

    申请日：2008-01-16

    Applicant: (주) 카이노스메드 ,  한국화학연구원 ,  영진약품 주식회사

    Inventor： 김성수 ,  안진희 ,  천혜경 ,  이상달 ,  강남숙 ,  김기영 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기 ,  하니나

    IPC: C07D277/22 ,  C07D417/12 ,  A61K31/427 ,  A61P19/10

    CPC classification number: C07D277/06 ,  C07D417/12 ,  Y02P20/55

    Abstract: PURPOSE: A dipeptidyl peptidase(DPP-IV) inhibitor is provided to use in treating DPP-IV-mediated disease. CONSTITUTION: A 2-carbonyl-3-acyl-1,3-thiazolidine of salt or prodrug form has a beta-amino group on acyl chain. A method for preparing the 2-carbonyl-3-acyl-1,3-thiazolidine derivative comprises: a step of condensing an amino acid of chemical formula Q-2 with a 2-cabonyl-1,3-thiazolidine compounds of chemical formula Q-3 to form a compound of chemical formula Q-4; and a step of deprotecting the compound of chemical formula Q-4 to obtain 2-carbonyl-3-acyl-1,3-thiazolidine derivative of chemical formula Q-1a. A pharmaceutical composition contains the 2-carbonyl-3-acyl-1,3-thiazolidine, pharmaceutically acceptable diluents, or carrier. The pharmaceutical composition is used for preventing or treating dipeptidyl peptidase IV(DPP-IV)-mediated disease.

    Abstract translation: 目的：提供二肽基肽酶（DPP-IV）抑制剂用于治疗DPP-IV介导的疾病。 构成：盐或前药形式的2-羰基-3-酰基-1,3-噻唑烷在酰基链上具有β-氨基。 制备2-羰基-3-酰基-1,3-噻唑烷衍生物的方法包括：将化学式Q-2的氨基酸与化学式Q的2-缩水甘油基-1,3-噻唑烷化合物缩合的步骤 -3以形成化学式Q-4的化合物; 以及使化学式Q-4的化合物脱保护，得到化学式Q-1a的2-羰基-3-酰基-1,3-噻唑烷衍生物的工序。 药物组合物含有2-羰基-3-酰基-1,3-噻唑烷，药学上可接受的稀释剂或载体。 该药物组合物用于预防或治疗二肽基肽酶IV（DPP-IV）介导的疾病。

    베타아미노기를 갖는 2-싸이아졸리딘 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
    15.
    发明授权
    베타아미노기를 갖는 2-싸이아졸리딘 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有βA的2-噻唑烷衍生物; - 氨基，药物可接受的盐及其制备方法

    公开(公告)号：KR100848491B1

    公开(公告)日：2008-07-28

    申请号：KR1020070004577

    申请日：2007-01-16

    Applicant: 영진약품 주식회사 ,  한국화학연구원

    Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  김기영 ,  강남숙 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기 ,  하니나

    IPC: C07D277/06 ,  C07D417/06 ,  A61P3/08 ,  A61P3/04

    CPC classification number: C07D277/06 ,  C07D417/12 ,  Y02P20/55

    Abstract: 2-Thiazolidine derivatives having beta-amino group are provided to inhibit activity of DPP-IV(dipeptidyl peptidase-IV) associated with activity regulation of various hormones, so that the compounds are useful for treating diseases mediated by DPP-IV including type 2 diabetes mellitus. The 2-thiazolidine derivatives having beta-amino group represented by the formula(1) are prepared by reacting an amino acid represented by the formula(2) with 2-thiazolidine compounds represented by the formula(3) to prepare compounds represented by the formula(4), and deprotecting the compounds represented by the formula(4), wherein BOC is a protecting group; A is -NR^e(CH2)nR2 or -OR^b; R^a is hydrogen, C1-6 alkyl, C1-6 alkoxy, -OCF3, halogen, -CN or -CF3; R^b is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, isopropyl, t-butyl, -CH2CH2OH, -CH2CH2NH2, -CH2CH2N(CH2CH2)2O, -CH2CH2N(CH2CH3)2 or -CH2CH2NHCOCH3; R^c is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, benzyl, isopropyl or t-butyl; R^d and R^e are each independently hydrogen, C1-6 alkyl or C3-6 cycloalkyl; Y is carbon, oxygen, sulfur or nitrogen; Z is hydrogen, C1-6 alkyl, C3-6 cycloalkyl or -CO2R^b; and n is an integer of 0, 1 or 2.

    Abstract translation: 提供具有β-氨基的2-噻唑烷衍生物以抑制与各种激素的活性调节相关的DPP-IV（二肽基肽酶-IV）的活性，使得该化合物可用于治疗包括2型糖尿病的DPP-IV介导的疾病 糖尿病。 由式（1）表示的具有β-氨基的2-噻唑烷衍生物通过使由式（2）表示的氨基酸与由式（3）表示的2-噻唑烷化合物反应来制备由式 （4）表示的化合物，并使由式（4）表示的化合物脱保护，其中BOC为保护基; A是-NR e（CH 2）n R 2或-OR b; R a a是氢，C 1-6烷基，C 1-6烷氧基，-OCF 3，卤素，-CN或-CF 3; 异丙基，叔丁基，-CH 2 CH 2 OH，-CH 2 CH 2 NH 2，-CH 2 CH 2 N（CH 2 CH 2）2 O，-CH 2 CH 2 N（CH 2 CH 3）2或-CH 2 CH 2 NHCOCH 3; R c是氢，C 1-6烷基，C 3-6环烷基，苄基，异丙基或叔丁基; R d和R e e各自独立地为氢，C 1-6烷基或C 3-6环烷基; Y是碳，氧，硫或氮; Z是氢，C 1-6烷基，C 3-6环烷基或-CO 2 R b; 且n为0,1或2的整数。

    베타아미노기를 갖는 1,2,5-트리아제판 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
    17.
    发明公开
    베타아미노기를 갖는 1,2,5-트리아제판 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有β型-AMINO ACYL组的1,2,5-三唑衍生物及其药物可接受的盐及其制备方法

    公开(公告)号：KR1020080007764A

    公开(公告)日：2008-01-23

    申请号：KR1020060066812

    申请日：2006-07-18

    Applicant: 한국화학연구원 ,  영진약품 주식회사

    Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  김기영 ,  강남숙 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기

    IPC: C07D255/02 ,  A61P3/00

    Abstract: A 1,2,5-triazepane derivative showing excellent DPP-IV inhibitory activity is provided to be effectively used for preventing or treating diseases mediated by DPP-IV such as insulin-dependent, insulin non-dependent diabetes, arthritis, obesity, osteoporosis, and damaged glucose resistance. A 1,2,5-triazepane derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(1-1) or (1-2); R2 is H, C1-6 alkyl, or a group represented by the structural formula(1-3); R3 is H, C1-6 alkyl, C3-6 cycloalkyl, CH2CO2R^b, COCO2R^b, pyrazine, and a group represented by the structural formula(1-4), (1-5) or (1-6); R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCF3, halogen, CN, CF3, COOR^b or NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl; R^d is C1-6 alkyl, trifluoromethyl, and a group represented by the structural formula(1-1), (1-7), (1-8), or (1-9); R^e is C1-6 alkyl, C3-6 cycloalkyl, and a group represented by the structural formula(1) or (2); R^f is H, halogen, NR^bR^c, tetrazole, proline, and a group represented by the structural formula(1-10), (1-11), (1-12), or (1-13); A is CH, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl or CO2R^d; X is O or S; and n is 0 or 1. A method for preparing the 1,2,5-triazepane derivative comprises the steps of: (a) subjecting an amino acid represented by the formula(2) and 1,2,5-triazepane to a condensation reaction to prepare a compound represented by the formula(4); (b) reacting the compound of the formula(4) with an electrophilic compound substituted with R2 to prepare a compound represented by the formula(5); and (c) deprotecting the compound of the formula(5). A pharmaceutical composition for preventing or treating diseases mediated by DPP-IV comprises an effective amount of the 1,2,5-triazepane derivative or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

    Abstract translation: 提供了显示优异的DPP-IV抑制活性的1,2,5-三氮丙平衍生物，其有效用于预防或治疗由DPP-IV介导的疾病，例如胰岛素依赖性，胰岛素非依赖型糖尿病，关节炎，肥胖症，骨质疏松症， 并损害葡萄糖耐量。 具有β-氨基的1,2,5-三氮杂环庚烷衍生物由式（1）表示，其中R1是由结构式（1-1）或（1-2）表示的基团。 R2是H，C1-6烷基或由结构式（1-3）表示的基团; R 3是H，C 1-6烷基，C 3-6环烷基，CH 2 CO 2 R b，COCO 2 R b，吡嗪和由结构式（1-4），（1-5）或（1-6）表示的基团。 R a a独立地为H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCF 3，卤素，CN，CF 3，COOR b或NR b R c; 每个R b和R c独立地是H，C 1-6烷基或C 3-6环烷基; R 1-6是C1-6烷基，三氟甲基和由结构式（1-1），（1-7），（1-8）或（1-9）表示的基团。 R 1-6是C 1-6烷基，C 3-6环烷基和由结构式（1）或（2）表示的基团。 （1-10），（1-11），（1-12）或（1-13）表示的基团，其中R为氢，卤素，NR 4 b R c，四唑，脯氨酸和由结构式 ; A是CH，N，O或S; B是H，C 1-6烷基，C 3-6环烷基，苄基或CO 2 R d; X是O或S; 并且n为0或1.制备1,2,5-三氮杂环庚烷衍生物的方法包括以下步骤：（a）使由式（2）表示的氨基酸和1,2,5-三氮杂环庚烷进行缩合 反应制备式（4）表示的化合物; （b）使式（4）的化合物与被R 2取代的亲电子化合物反应，制备由式（5）表示的化合物。 和（c）使式（5）的化合物脱保护。 用于预防或治疗由DPP-IV介导的疾病的药物组合物包含有效量的1,2,5-三氮丙烯衍生物或其药学上可接受的盐和药学上可接受的载体。

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