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    베타아미노기를 갖는 1,4-디아제펜 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
    5.
    发明公开
    베타아미노기를 갖는 1,4-디아제펜 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有β; -AMINO组的1,4-DIAZEPANE衍生物，药物可接受的盐及其制备方法

    公开(公告)号：KR1020080067391A

    公开(公告)日：2008-07-21

    申请号：KR1020070004576

    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: C07D243/14 ,  C07D417/12 ,  C07D403/12

    CPC classification number: Y02P20/55

    Abstract: A 1,4-diazepane derivative is provided to inhibit the activity of DPP-IV excellently, thereby being effectively used to treat or prevent diseases such as insuline-dependent and insuline-independent diabetes, arthritis, obesity, osteoporosis and injured glucose resistance. A 1,4-diazepane derivative having a beta-amino group is represented by a formula(1), wherein R1 is a group(1) or a group(2); R2 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, heteroaryl, a group(1), a group(2), a group(3), a group(4), a group(5), a group(6), a group(7), a group(8), or a group(9); R2 is H, C1-6 alkyl, C3-6 cycloalkyl, heteroaryl, C1-6 alkoxy, -OCH2O, -SO2NH3, -OCF3, phenoxy, halogen, -CN, -NO2, -CF3, -CONH2, -COOR^b, -CH2COOR^b, -OCHR^bCOOR^b or -NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl, aryl, alkylaryl, arylsulfonyl, arylcarbonyl, amino acid derivative or -CH2OCOC(CH3)3; R^d is C1-6 alkyl, trifluoromethyl, a group(1), a group(2), a group(10), a group(11), a group(12), a group(13), pyrazinyl, pyrimidinyl or pyrrolyl; R^e is C1-6 alkyl, C3-6 cycloalkyl, a group(1) or a group(2); R^f is, halogen, NR^bR^c, a group(14), a group(15), a group(16), a group(17), a group(10), heteroaryl, -S-heteroaryl, tetrahydroisoquinoline, thiazolidine, piperidin-4-carboxylic acid or tetrahydropyrimidine; A is CH2, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl, CO2R^d, 2-pyridyl or aryl; X is O or S; and n is an integer from 1 to 3. A method for preparing the 1,4-diazepane derivative comprises the steps of: (a) subjecting an amino acid represented by a formula(2) and a diazepane compound represented by a formula(3) to condensation to obtain a compound represented by a formula(4); and (b) deprotecting the compound of the formula(4), wherein BOC is a protecting group, and other substitutents are same as defined above. A pharmaceutical composition comprises an effective amount of the 1,4-diazepane derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

    Abstract translation: 提供1,4-二氮杂环庚烷衍生物，以有效地抑制DPP-IV的活性，从而有效地用于治疗或预防诸如胰岛素依赖性和胰岛素依赖性糖尿病，关节炎，肥胖症，骨质疏松症和受损葡萄糖耐药性的疾病。 具有β-氨基的1,4-二氮杂环庚烷衍生物由式（1）表示，其中R1是基团（1）或基团（2）。 R2是H，C1-6烷基，C3-6环烷基，C1-6卤代烷基，杂芳基，基团（1），基团（2），基团（3），基团（4），基团（5） ，组（6），组（7），组（8）或组（9）; R2是H，C1-6烷基，C3-6环烷基，杂芳基，C1-6烷氧基，-OCH2O，-SO2NH3，-OCF3，苯氧基，卤素，-CN，-NO2，-CF3，-CONH2，-COOR2b ，-CH 2 COOR b，-OCHR 2 bCOOR 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，芳基，烷基芳基，芳基磺酰基，芳基羰基，氨基酸衍生物或-CH 2 OCOC（CH 3）3; R 1是C 1-6烷基，三氟甲基，基团（1），基团（2），基团（10），基团（11），基团（12），基团（13），吡嗪基， 或吡咯基; R 6是C 1-6烷基，C 3-6环烷基，基团（1）或基团（2）; （14），基团（15），基团（16），基团（17），基团（10），杂芳基，-S-杂芳基， 四氢异喹啉，噻唑烷，哌啶-4-羧酸或四氢嘧啶; A是CH 2，N，O或S; B是H，C 1-6烷基，C 3-6环烷基，苄基，CO 2 R 12，2-吡啶基或芳基; X是O或S; n为1〜3的整数。一种1,4-二氮杂环庚烷衍生物的制备方法，其特征在于：（a）使式（2）表示的氨基酸和式（3）表示的二氮杂环丁烷化合物 ）缩合得到由式（4）表示的化合物; 和（b）使式（4）的化合物脱保护，其中BOC是保护基，其它取代基与上述定义相同。 药物组合物包含有效量的1,4-二氮杂环庚烷衍生物或其药学上可接受的盐和药学上可接受的载体。

    1-(3,4-디알콕시벤질)-1Ｈ-피라졸 화합물, 이의 제조방법및 이를 포함하는 천식 및 만성폐쇄성 폐질환을 포함한염증관련 질환, 관절염, 아토피 피부염, 암 및 뇌질환의치료 및 예방을 위한 약제학적 조성물
    6.
    发明授权
    1-(3,4-디알콕시벤질)-1Ｈ-피라졸 화합물, 이의 제조방법및 이를 포함하는 천식 및 만성폐쇄성 폐질환을 포함한염증관련 질환, 관절염, 아토피 피부염, 암 및 뇌질환의치료 및 예방을 위한 약제학적 조성물 失效
    1-（3,4-二甲氧基苄基）-1H-吡唑化合物，其制备方法和用于治疗或预防哮喘，慢性阻塞性肺动脉疾病，ARTHRITIS，原发性恶性肿瘤，包括其中的肿瘤和变应性脑病的药物组合物

    公开(公告)号：KR100820246B1

    公开(公告)日：2008-04-07

    申请号：KR1020060098670

    申请日：2006-10-10

    Applicant: 한국화학연구원

    Inventor： 노재성 ,  전동주 ,  송종환 ,  정준원 ,  박창민 ,  소원영 ,  강남숙 ,  서지희 ,  김낙정 ,  박순찬 ,  천혜경 ,  조영식 ,  배명애 ,  김기영 ,  송진숙 ,  현영란 ,  김용은 ,  노성구 ,  이태규 ,  조중명 ,  유성은

    IPC: C07D231/12 ,  C07D401/04

    Abstract: A novel pyrazole compound is provided to show excellent inhibitory activity on PDE-4 enzyme, thereby being used in order to prevent and treat asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases. A 1-(3,4-dialkoxybenzyl)-1H-pyrazole compound is represented by the formula(1), wherein each R1 and R2 is independently H, linear or branched C1-7 alkyl, linear or branched C1-7 C1-7 alkyl including halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, phenyl, benzyl or allyl, or R1 and R2 may be linked to each other with C1-3 alkylene or C1-3 alkylene including halogen; R3 is H, formyl, halogen, linear or branched C1-10 alkyl, C1-10 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, (C1-10)alkylcarboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl; (C3-7)cycloalkylamino, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide, cyano, nitro, carboxylic acid guanidine, urea, phenoxy, benzyloxy, or an Aryl represented by the group(I); each R4 and R5 is independently H, halogen, formyl, linear or branched C1-10 alkyl, C1-10 alkoxy, (C1-10)alkoxy(C1-10)alkyl, C1-7 alkylketone, hydroxy(C1-10)alkyl, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, carboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, phenyl, phenoxy, benzyl, benzyloxy, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkoxy including O, N or S in a hetero-cycle, cyano, nitro, (C3-7)cycloalkylamino, guanidine, or urea. A method for preparing the compound of the formula(1) comprises a step of reacting a halobenzyl compound represented by the formula(3) with a pyrazole compound represented by the formula(4), each R1, R2, R3, R4, and R5 are same as defined above, and X is halogen. A pharmaceutical composition for preventing and treating inflammation related diseases such as asthma and chronic obstructive pulmonary diseases comprises the compound of the formula(1) as an effective ingredient.

    Abstract translation: 提供了一种新的吡唑化合物，以显示对PDE-4酶的优异抑制活性，从而用于预防和治疗哮喘，慢性阻塞性肺病，关节炎，特应性皮炎，肿瘤和退行性脑疾病。 1-（3,4-二烷氧基苄基）-1H-吡唑化合物由式（1）表示，其中每个R 1和R 2独立地为H，直链或支链C 1-7烷基，直链或支链C 1-7 C1-7 烷基，包括卤素，C 3-7环烷基，（C 3-7）环烷基（C 1-7）烷基，在杂环中包括O，N或S的3-至7-元杂环烷基，3-至7-元杂环烷基 -7）烷基，包括异环周期中的O，N或S，苯基，苄基或烯丙基，或者R 1和R 2可以与C 1-3亚烷基或包括卤素的C 1-3亚烷基彼此连接; R 3为H，甲酰基，卤素，直链或支链C 1-10烷基，C 1-10烷氧基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，C 1-7烷基酮，（C 3-7） 环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，（C1-10）烷基羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺，氨基，单或二 （C 1-7）烷基氨基，单或二（C 1-7）烷基氨基羰基; （C3-7）环烷基氨基，吗啉，吗啉氧化物，哌啶，哌嗪，哌嗪氧化物，氰基，硝基，羧酸胍，脲，苯氧基，苄氧基或由基团（I）表示的芳基。 每个R 4和R 5独立地为H，卤素，甲酰基，直链或支链C 1-10烷基，C 1-10烷氧基，（C 1-10）烷氧基（C 1-10）烷基，C 1-7烷基酮，羟基（C 1-10）烷基 ，C3-7环烷基，（C3-7）环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺 ，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，苯基，苯氧基，苄基，苄氧基，包含异质周期中的O，N或S的3-至7-元杂环烷基， 包含杂环中的O，N或S的3-至7-元杂环烷基（C 1-7）烷基，异异环中包括O，N或S的3-至7-元杂环烷基（C 1-7）烷氧基， 氰基，硝基，（C 3-7）环烷基氨基，胍或脲。 制备式（1）化合物的方法包括使由式（3）表示的卤苄基化合物与式（4）表示的吡唑化合物反应，每个R 1，R 2，R 3，R 4和R 5 与上述相同，X为卤素。 用于预防和治疗炎症相关疾病如哮喘和慢性阻塞性肺疾病的药物组合物包含式（1）化合物作为有效成分。

    아다만틸기를 갖는 설파마이드 유도체 및 이의 약제학적으로 허용 가능한 염
    9.
    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。

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