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    신규한 헤테로사이클릭다이온 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 뇌신경세포 보호용 약학적 조성물
    4.
    发明公开
    신규한 헤테로사이클릭다이온 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 뇌신경세포 보호용 약학적 조성물 有权
    新型杂环衍生物或药物可接受的盐，其制备方法和药物组合物，用于保护含有其作为活性成分的脑神经细胞

    公开(公告)号：KR1020140139669A

    公开(公告)日：2014-12-08

    申请号：KR1020130059719

    申请日：2013-05-27

    Applicant: 한국화학연구원

    Inventor： 정영식 ,  한수봉 ,  박우규 ,  이정현 ,  이병호 ,  송진숙

    IPC: C07D471/04 ,  C07D215/22 ,  A61K31/4375 ,  A61P25/00

    Abstract: 본 발명은 신규한 헤테로사이클릭다이온 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 뇌신경세포 보호용 약학적 조성물에 관한 것이다. 본 발명에 따른 화학식 1로 표시되는 헤테로사이클릭다이온 유도체는 항경련 효과가 뛰어날 뿐만 아니라, 허혈이 발생할 경우 허혈에 의한 세포 손상을 지연시키고 재관류 이후에 일어나는 손상을 최소화하여 뇌세포를 보호하는 효과가 우수하므로 이를 유효성분으로 함유하는 약학적 조성물은 뇌신경세포 보호용 약학적 조성물로 유용하게 사용될 수 있다.

    Abstract translation: 本发明涉及一种新型杂环二酮衍生物或其药学上可接受的盐，其制备方法和用于保护含有该活性成分的脑细胞的药物组合物。 由本发明的化学式1表示的杂环二酮衍生物具有优异的抗惊厥作用，延缓缺血发生时由局部缺血引起的细胞损伤，并且使再灌注后发生的损伤最小化，从而具有优异的保护细胞的效果。 因此，包含杂环二酮作为活性成分的药物组合物可用作保护脑细胞的药物组合物。

    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
    6.
    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
    7.
    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。

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