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    7-(3′,4′-디알콕시페닐)-[1,2,4]트리아졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는 천식 및만성폐쇄성 폐질환을 포함한 염증관련 질환, 관절염,아토피 피부염, 암 및 뇌질환의 치료 및 예방을 위한약제학적 조성물
    31.
    发明授权
    7-(3′,4′-디알콕시페닐)-[1,2,4]트리아졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는 천식 및만성폐쇄성 폐질환을 포함한 염증관련 질환, 관절염,아토피 피부염, 암 및 뇌질환의 치료 및 예방을 위한약제학적 조성물 失效
    7-（3'，4'-二烷氧基苯基） - [1,2,4] - 三唑并[1,5-A]吡啶化合物，其制备方法和药物组合物，用于治疗或预防哮喘，慢性阻塞性肺动脉疾病， ARTHRITIS，ATOPIC DERMATITIS，TUMOR AND DEGENERATIVE BRAIN DISEASES COMPATH THE SAME

    公开(公告)号：KR100844125B1

    公开(公告)日：2008-07-04

    申请号：KR1020070028620

    申请日：2007-03-23

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  박창민 ,  천혜경 ,  조영식 ,  송진숙 ,  배명애 ,  유성은

    IPC: C07D487/04 ,  A61K31/519

    CPC classification number: C07D487/04

    Abstract: A 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes and improve vomiting related side effects, which is one most serious problem of the PDE-4 inhibitors, thereby being used as a therapeutic agent of asthma and chronic obstructive pulmonary diseases, arthritis, atopic dermatitis, leukemia, cancer and brain diseases. A 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound is represented by a formula(1) and is prepared by reacting 3-amino-triazole compound represented by a formula(4) with 3-(dimethylamino)-1-(3,4-dialkoxyphenyl)prophenone compound represented by a formula(5) or 3-(3,4-dialkoxyphenyl)3-oxopropionealdehyde compound represented by a formula(6) in the presence of acetic acid. In the formulae, each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl, linear or branched saturated or unsaturated C1-7 alkyl including O, N or S, C3-7 cycloalkyl, C3-7 cycloalkyl including O, N or S, (C3-7)cycloalkyl(C1-7)alkyl, 3 to 7-membered saturated or unsaturated heterocycloalkyl including O, N, or S in a heterocycle, phenyl or benzyl, or R1 and R2 may be linked to each other by C1-3 alkylene or C1-3 alkylene including halogen; R3 is aryl selected from groups(1) to (4). A pharmaceutical composition for treating or preventing diseases related to bronchial inflammation such as asthma and chronic obstructive pulmonary disease, arthritis, atopic dermatitis, leukemia, cancer and brain diseases such as Alzheimer's disease, depression and memory decrease comprises the 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound or a pharmaceutically acceptable carrier as an effective ingredient.

    Abstract translation: 提供7-（3'，4'-二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物以显示对PDE-4酶的优异活性和对其它PDE酶的高选择性， 改善呕吐相关的副作用，这是PDE-4抑制剂的一个最严重的问题，从而被用作哮喘和慢性阻塞性肺疾病，关节炎，特应性皮炎，白血病，癌症和脑疾病的治疗剂。 7-（3'，4'-二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物由式（1）表示，并通过3-氨基 - 三唑化合物 由式（4）与由式（5）表示的3-（二甲基氨基）-1-（3,4-二烷氧基苯基）丙烯酮化合物或由式（5）表示的3-（3,4-二烷氧基苯基）3-氧代丙醛化合物 （6）在乙酸存在下。 在该式中，每个R 1和R 2独立地为H，直链或支链饱和或不饱和的C 1-7烷基，包括O，N或S，C 3-7环烷基，C 3-7环烷基的直链或支链饱和或不饱和C 1-7烷基，包括 O，N或S，（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元饱和或不饱和杂环烷基，苯基或苄基，或R 1和R 2可以相连 通过C1-3亚烷基或包括卤素的C1-3亚烷基; R3是选自（1）〜（4）的芳基。 用于治疗或预防与哮喘和慢性阻塞性肺病，关节炎，特应性皮炎，白血病，癌症和脑疾病如阿尔茨海默病，抑郁和记忆减退等支气管炎有关的疾病的药物组合物包括7-（3'，4 '二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物或药学上可接受的载体作为有效成分。

    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
    32.
    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。

    아세트아마이드기를 갖는 사이클릭설폰아미드 유도체, 이의 제조방법 및 이를 함유하는 약학 조성물
    38.
    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
    40.
    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。

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