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    베타아미노기를 갖는 고리화된 히드라자이드 유도체, 이의 약학적으로 허용 가능한 염 및 이의 제조 방법
    31.
    发明公开
    베타아미노기를 갖는 고리화된 히드라자이드 유도체, 이의 약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有β型-AMINO组的环状氢化衍生物及其药物可接受的盐及其制备方法

    公开(公告)号：KR1020070087953A

    公开(公告)日：2007-08-29

    申请号：KR1020060017372

    申请日：2006-02-22

    Applicant: 영진약품 주식회사 ,  한국화학연구원

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

    IPC: C07D231/04 ,  C07D237/04

    CPC classification number: Y02P20/55 ,  C07D231/04 ,  C07D237/04 ,  C07D243/02 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D417/12

    Abstract: A cyclic hydrazide derivative having a beta-amino group is provided to inhibit the activity of DPP-IV, thereby being useful for treating various diseases mediated by the DPP-IV. The cyclic hydrazide derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(a) or (b), R2 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, or a group represented by the structural formula(a), (b), (c), (d), (e), (f), (g), or (h)[wherein R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCH2O, OCF3, phenoxy, halogen, CN, NO2, CF3, COOR^b or NR^bR^c(wherein each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl), R^d is a group represented by the structural formula(a), (b), (i), (j), (k), (l), or (m), R^e is C1-6 alkyl, C3-6 cycloalkyl, or a group represented by the structural formula(a) or (b), R^f is halogen, NR^b, R^c, a group represented by the structural formula(n) or (o), -S-heteroayl, tetrahydroisoquinoline, thiazolidine, proline, piperidine-4-carboxylic acid or tetrahydropyrimidine(where X is O or S)], and n is an integer from 1 to 3. The method comprises the steps of: (a) performing a condensation reaction of an amino acid represented by the formula(2) and a cyclic hydrazine represented by the formula(3) to obtain a compound represented by the formula(4); (b) reacting the compound of the formula(4) with chloroacetyl chloride to obtain a compound represented by the formula(6); (c) reacting the compound of the formula(6) with an R2 substituted nucleophilic compound to obtain a compound represented by the formula(5); and (d) deprotecting the compound of the formula(5). In the reaction formula(2), BOC is a protecting group, and each R1, R2, and n is the same as defined above.

    Abstract translation: 提供具有β-氨基的环状酰肼衍生物以抑制DPP-IV的活性，从而可用于治疗由DPP-IV介导的各种疾病。 具有β-氨基的环状酰肼衍生物由式（1）表示，其中R 1是由结构式（a）或（b）表示的基团，R 2是H，C 1-6烷基，C 3-6环烷基 或者由结构式（a），（b），（c），（d），（e），（f），（g）或（h） a独立地是H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCH 2 O，OCF 3，苯氧基，卤素，CN，NO 2，CF 3，COOR b或NR b R c c（其中每个R b和 （a），（b），（i），（j），（k），（j），（k） 1）或（m）R e是C 1-6烷基，C 3-6环烷基或由结构式（a）或（b）表示的基团，R f是卤素，NR b， c，由结构式（n）或（o）表示的基团，-S-杂芳基，四氢异喹啉，噻唑烷，脯氨酸，哌啶-4-甲酸或四氢嘧啶（其中X为O或S）]，n为 从1到3的整数。该方法包括以下步骤：（a）pe （2）表示的氨基酸与式（3）表示的环状肼的缩合反应，得到式（4）表示的化合物。 （b）使式（4）的化合物与氯乙酰氯反应，得到式（6）表示的化合物; （c）使式（6）化合物与R2取代的亲核化合物反应得到式（5）表示的化合物; 和（d）使式（5）的化合物脱保护。 在反应式（2）中，BOC为保护基，R1，R2和n各自与上述相同。

    아세트아마이드기를 갖는 사이클릭설폰아미드 유도체, 이의 제조방법 및 이를 함유하는 약학 조성물
    35.
    发明公开
    아세트아마이드기를 갖는 사이클릭설폰아미드 유도체, 이의 제조방법 및 이를 함유하는 약학 조성물 失效
    具有乙酰胺基团的环己基酰胺衍生物及其制备方法及含有其的药物组合物

    公开(公告)号：KR1020110060653A

    公开(公告)日：2011-06-08

    申请号：KR1020090117302

    申请日：2009-11-30

    Applicant: 한국화학연구원 ,  에스케이 주식회사

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

    IPC: C07D279/14 ,  C07D279/16 ,  A61K31/5415 ,  A61P3/10

    Abstract: PURPOSE: A cyclic sulfonamide derivative with an acetamide group is provided to suppress activation of 11beta-hydroxysteroid dehydrogenase type1(11beta-HSD1) and to treat various diseases. CONSTITUTION: A cyclic sulfonamide derivative with an acetamide group is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating 11beta-HSD1-mediated diseases contains cyclic sulfonamide derivative of chemical formula 1 or pharmaceutically acceptable salt as an active ingredient and pharmaceutically acceptable carrier. The 11beta-HSD2-mediated diseases are insulin-dependent diabetes, insulin non-dependent diabetes, arthritis, obesity, hypertension, hyperlipidemia, or depression.

    Abstract translation: 目的：提供具有乙酰胺基团的环状磺酰胺衍生物，以抑制11β-羟类固醇脱氢酶1型（11beta-HSD1）的活化并治疗各种疾病。 构成：具有乙酰胺基团的环状磺酰胺衍生物由化学式1表示。用于预防或治疗11β-HSD1介导的疾病的药物组合物含有化学式1的环状磺酰胺衍生物或其药学上可接受的盐作为活性成分和药学上可接受的载体 。 11beta-HSD2介导的疾病是胰岛素依赖性糖尿病，胰岛素非依赖性糖尿病，关节炎，肥胖症，高血压，高脂血症或抑郁症。

    페닐테트라졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증 또는 비만의 예방 또는 치료용 약학적 조성물
    37.
    发明公开
    페닐테트라졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증 또는 비만의 예방 또는 치료용 약학적 조성물 失效
    用于预防或治疗包含苯并噻唑衍生物的药物或药物的药物组合物或其作为活性成分的药物可接受的盐

    公开(公告)号：KR1020100130139A

    公开(公告)日：2010-12-10

    申请号：KR1020090121291

    申请日：2009-12-08

    Applicant: 한국화학연구원

    Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  장성연 ,  황은숙 ,  홍정호

    IPC: C07D487/04 ,  A61K31/437 ,  A61P19/08 ,  A61P3/04

    Abstract: PURPOSE: A pharmaceutical composition containing phenyltetrazole derivatives for preventing or treating osteoporosis, obesity, diabetes or hyperlipidemia is provided to control TAZ(transcriptional coactivator with PDZbinding motif) protein. CONSTITUTION: A pharmaceutical composition for preventing or treating osteoporosis contains a compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing or treating obesity, diabetes or hyperlipidemia contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. The compound is phenyltetrazole derivatives.

    Abstract translation: 目的：提供含有苯基四唑衍生物用于预防或治疗骨质疏松症，肥胖症，糖尿病或高脂血症的药物组合物以控制TAZ（具有PDZ结合基序的转录共激活物）蛋白质。 构成：用于预防或治疗骨质疏松症的药物组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。 用于预防或治疗肥胖症，糖尿病或高脂血症的药物组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。 该化合物是苯基四唑衍生物。

    신규한 카보니트릴 화합물, 이의 제조방법 및 이를포함하는 류마티스성 관절염, 골관절염, 파제트병,악성고칼슘혈증, 대사성골질환 및 각종 암의 치료 및예방을 위한 약제학적 조성물
    39.
    发明公开
    신규한 카보니트릴 화합물, 이의 제조방법 및 이를포함하는 류마티스성 관절염, 골관절염, 파제트병,악성고칼슘혈증, 대사성골질환 및 각종 암의 치료 및예방을 위한 약제학적 조성물 失效
    新型碳青霉烯类化合物，其制备方法以及用于治疗或预防特发性恶病质，糖皮质激素，帕格病，恶性高血压，代谢性骨髓疾病和包含其中的癌症的药物组合物

    公开(公告)号：KR1020090005842A

    公开(公告)日：2009-01-14

    申请号：KR1020070069210

    申请日：2007-07-10

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  김순기 ,  강남숙 ,  천혜경 ,  조영식 ,  송진숙 ,  민용기 ,  김성환

    IPC: C07D231/04 ,  A61K31/415 ,  A61P19/04

    Abstract: A novel carbonitrile compound or its pharmaceutically acceptable salt, a method for preparing the compound, and a pharmaceutical composition containing compound are provided to prevent and treat osteoarthritis and various cancer without side effect. A carbonitrile compound is represented by the formula 1, wherein n is 1 or 2; R1 is H, halogen-substituted or unsubstituted linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C1-C10 alkoxy, C1-C10 alkylthio, hydroxy-C1-C10 alkyl, C1-C10 alkylcarbonyl, C1-C10 alkylthio-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C1-C10 alkoxy-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, or ar-C1-C10 alkoxy group; and R2 linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, C1-C10 alkoxycarbonyl, or ar-C1-C10 alkoxycarbonyl group.

    Abstract translation: 提供新的腈化合物或其药学上可接受的盐，制备该化合物的方法和含有药物组合物的化合物以预防和治疗骨关节炎和各种癌症而没有副作用。 腈化合物由式1表示，其中n为1或2; R1是H，卤素取代或未取代的直链或支链饱和或不饱和C 1 -C 10烷基，C 3 -C 7环烷基，C 1 -C 10烷氧基，C 1 -C 10烷硫基，羟基-C 1 -C 10烷基，C 1 -C 10烷基羰基，C 1 -C 10 烷硫基-C 1 -C 10烷基，C 3 -C 7环烷基-C 1 -C 10烷基，C 3 -C 7环烷基-C 1 -C 10烷基，C 1 -C 10烷氧基-C 1 -C 10烷基，苯基，芳基-C 1 -C 10烷基或芳烷基 -C 10烷氧基 和R 2直链或支链饱和或不饱和的C 1 -C 10烷基，C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 10烷基，苯基，芳基-C 1 -C 10烷基，C 1 -C 10烷氧基羰基或芳基-C 1 -C 10烷氧基羰基 。

    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1Ｈ-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물
    40.
    发明授权
    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1Ｈ-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-（3,4-二甲氧基乙基） - 吡咯烷基] -1H-吡唑化合物，其制备方法和包含该化合物的药物组合物

    公开(公告)号：KR100833799B1

    公开(公告)日：2008-05-30

    申请号：KR1020070002725

    申请日：2007-01-10

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  박창민 ,  소원영 ,  이지선 ,  김은주 ,  강남숙 ,  천혜경 ,  조영식 ,  송진숙 ,  배명애 ,  김지현 ,  조중명 ,  노성구 ,  현영란 ,  이철순 ,  이재일 ,  유성은

    IPC: C07D401/06 ,  C07D413/14

    Abstract: 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds are provided to inhibit activity of PDE-4(phosphodiesterase-4) with high activity and selectivity without side effects, so that the compounds are useful for treating inflammation diseases, neurodegenerative disease and cancers. 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds represented by the formula(1) are provided, wherein A is N or CH; R1 is linear or branched, saturated or unsaturated (C1-C7)alkyl or halogen-substituted linear or branched, saturated or unsaturated (C1-C7)alkyl; R2 is hydrogen atom, (C3-C7)cycloalkyl or (C3-C8)cycloalkylmethyl; R3, R4 and R5 are each independently hydrogen atom, phenyl, pyridinyl, N-oxypyridinyl, linear or branched, saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C3-C10)cycloalkyl(C1-C7)alkyl, halogen atom, cyano, nitro, amino, mono- or di(C1-C7)alkylamino, mono- or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamino, 3- to 7-membered saturated or unsaturated hetero ring containing oxygen, nitrogen or sulfur in hetero ring, guanidinyl, ureido, benzyl, benzyloxy, formyl, (C1-C7)alkanoyl, (C1-C7)alkoxy, (C1-C7)alkoxy(C1-C7)alkyl, hydroxy(C1-C7)alkyl, carboxyl or (C1-C7)alkoxycarbonyl; and R6 is pyridinyl or N-oxypyridinyl group.

    Abstract translation: 提供1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物以抑制具有高活性和选择性的PDE-4（磷酸二酯酶-4）的活性而没有副作用，使得该化合物可用于 治疗炎症疾病，神经退行性疾病和癌症。 提供由式（1）表示的1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物，其中A是N或CH; R1是直链或支链饱和或不饱和（C1-C7）烷基或卤素取代的直链或支链饱和或不饱和（C1-C7）烷基; R2是氢原子，（C3-C7）环烷基或（C3-C8）环烷基甲基; R 3，R 4和R 5各自独立地为氢原子，苯基，吡啶基，N-氧代吡啶基，直链或支链，饱和或不饱和的（C1-C7）烷基，（C3-C7）环烷基，（C3-C10）环烷基 ）（C 1 -C 7）烷基氨基羰基，（C 3 -C 7）环烷基氨基，3至7元饱和或不饱和的（C 1 -C 7）烷基氨基， 杂环中含氧，氮或硫的杂环，胍基，脲基，苄基，苄氧基，甲酰基，（C1-C7）烷酰基，（C1-C7）烷氧基，（C1-C7）烷氧基（C1-C7） （C 1 -C 7）烷基，羧基或（C 1 -C 7）烷氧基羰基; R6是吡啶基或N-氧代吡啶基。

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