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    히스톤 디아세틸라제 저해활성을 갖는 알킬아미노나프탈렌일옥시 메틸옥트 Ｎ-하이드록시엔아마이드 유도체,이의 제조방법 및 이를 유효성분으로 하는 항암제용 약학조성물
    12.
    发明授权
    히스톤 디아세틸라제 저해활성을 갖는 알킬아미노나프탈렌일옥시 메틸옥트 Ｎ-하이드록시엔아마이드 유도체,이의 제조방법 및 이를 유효성분으로 하는 항암제용 약학조성물 失效
    含有甲基脱乙酰壳多糖的抑制活性的亚氨基亚甲氧基甲基甲氧基羰基衍生物，其制备方法和包含其的抗原组合物

    公开(公告)号：KR100814098B1

    公开(公告)日：2008-03-14

    申请号：KR1020060108228

    申请日：2006-11-03

    Applicant: 한국화학연구원 ,  크리스탈지노믹스(주)

    Inventor： 이철해 ,  정희정 ,  김재학 ,  정원장 ,  조중명 ,  노성구 ,  현영란 ,  이철순

    IPC: C07C237/16 ,  C07C237/14 ,  C07C233/19

    Abstract: An alkylcarbamoyl naphthalenyloxy methyloct N-hydroxyenamide derivative, its pharmaceutically acceptable salt, a method for preparing the derivative, and an anticancer pharmaceutical composition containing the derivative are provided to inhibit the enzymatic activity of histone deacetylase effectively and the proliferation of tumor cells. An alkylcarbamoyl naphthalenyloxy methyloct N-hydroxyenamide derivative is represented by the formula 1, wherein R1 is a C1-C3 alkyl group substituted or unsubstituted with at least one substituent selected from the group consisting of a C1-C3 alkyl group, a C1-C3 alkoxy group, a hydroxy C1-C3 alkyl group, a halophenyl group, a piperidinyl group, a morpholinyl group, a cyanomethyl group, a piperazinyl group, a di-C1-C3 alkylamino group, a di-C1-C3 alkylamino C1-C3 alkyl group, a piperidinyl C1-C3 alkyl group, a C1-C3 alkoxy C1-C3 alkyl group, a morpholino C1-C3 alkyl group, a piperazino C1-C3 alkyl group, a pyrrolidinyl group, an oxopyrrolidinyl group, a C1-C3 alkylpyrrolidinyl group, an imidazole group, an imidazolyl C1-C3 alkyl group and a thiophenyl group.

    Abstract translation: 提供烷基氨基甲酰基萘氧基甲基N-羟基酰胺衍生物，其药学上可接受的盐，制备该衍生物的方法和含有该衍生物的抗癌药物组合物，以有效抑制组蛋白脱乙酰酶的酶活性和肿瘤细胞的增殖。 烷基氨基甲酰基萘氧基甲基N-羟基酰胺衍生物由式1表示，其中R 1是被至少一个选自C 1 -C 3烷基，C 1 -C 3烷氧基的取代基取代或未取代的C 1 -C 3烷基 基团，羟基C 1 -C 3烷基，卤代苯基，哌啶基，吗啉基，氰基甲基，哌嗪基，二-C 1 -C 3烷基氨基，二-C 1 -C 3烷基氨基C 1 -C 3烷基 基团，哌啶基C1-C3烷基，C1-C3烷氧基C1-C3烷基，吗啉代C1-C3烷基，哌嗪基C1-C3烷基，吡咯烷基，氧代吡咯烷基，C1-C3烷基吡咯烷基 基团，咪唑基，咪唑基C1-C3烷基和噻吩基。

    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
    15.
    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。

    히스톤 디아세틸라제 저해활성을 갖는 알킬아미노나프탈렌일옥시메틸 프로페닐 하이드록시벤즈아마이드유도체, 이의 제조방법 및 이를 유효성분으로 하는항암제용 약학 조성물
    16.
    发明授权
    히스톤 디아세틸라제 저해활성을 갖는 알킬아미노나프탈렌일옥시메틸 프로페닐 하이드록시벤즈아마이드유도체, 이의 제조방법 및 이를 유효성분으로 하는항암제용 약학 조성물 失效
    具有抗组氨酸脱乙酰酶的抑制活性的烷基亚胺基甲基丙烯酰羟基苯甲酸衍生物，其制备方法和包含其的抗体组合物

    公开(公告)号：KR100820039B1

    公开(公告)日：2008-04-07

    申请号：KR1020060109436

    申请日：2006-11-07

    Applicant: 한국화학연구원 ,  크리스탈지노믹스(주)

    Inventor： 이철해 ,  정희정 ,  김재학 ,  정원장 ,  조중명 ,  노성구 ,  현영란 ,  이철순

    IPC: C07C233/22 ,  C07C233/21 ,  C07C217/16

    Abstract: An alkylamino naphthalenyloxymethyl propenyl hydroxybenzamide derivative is provided to obtain a pharmaceutical composition having an anti-cancer effect by inhibiting activity of histone deacetylase, inducing differentiation of tumor cells and inhibiting growth of tumor cells. An alkylamino naphthalenyloxymethyl propenyl hydroxybenzamide derivative is represented by the following formula 1. In formula 1, R1 is H or a C1-C3 alkyl; R2 is a C1-C6 alkyl non-substituted or substituted with a substituent selected from the group consisting of di-C1-C3 alkylamino, C1-C4 alkylpyrrolidinyl, morpholinyl, imidazolyl, methoxy and thiophenyl, a C1-C6 alkyl substituted with hydroxyphenyl, di-C1-C3 alkylaminophenyl, methoxyphenyl or trifluoromethoxyphenyl, pyrrolidine non-substituted or substituted with C1-C3 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl C1-C3 alkyl, benzyl or C3-C8 cycloalkylcarbonyl, piperidine substituted with a C3-C8 cycloalkyl or C1-C6 alkyl, or a C3-C8 cycloalkyl, with the proviso that when R1 is H or CH3, R2 is not non-substituted C1-C2 alkyl and morpholinyl-substituted C1-C2 alkyl.

    Abstract translation: 提供烷基氨基萘氧基甲基丙烯基羟基苯甲酰胺衍生物，通过抑制组蛋白脱乙酰酶的活性，诱导肿瘤细胞的分化和抑制肿瘤细胞的生长来获得具有抗癌作用的药物组合物。 烷基氨基萘氧基甲基丙烯基羟基苯甲酰胺衍生物由下式1表示。在式1中，R 1为H或C 1 -C 3烷基; R2是未取代或被选自二C1-C3烷基氨基，C1-C4烷基吡咯烷基，吗啉基，咪唑基，甲氧基和噻吩基的取代基取代的C1-C6烷基，被羟基苯基取代的C1-C6烷基， 二-C 1 -C 3烷基氨基苯基，甲氧基苯基或三氟甲氧基苯基，未被取代或被C 1 -C 3烷基，C 3 -C 8环烷基，C 3 -C 8环烷基C 1 -C 3烷基，苄基或C 3 -C 8环烷基羰基取代的吡咯烷， C8环烷基或C1-C6烷基，或C3-C8环烷基，条件是当R 1为H或CH 3时，R 2不是未取代的C 1 -C 2烷基和吗啉基取代的C 1 -C 2烷基。

    히스톤 디아세틸라제 저해활성을 갖는 알킬카바모일나프탈렌일옥시 옥테노일 하이드록시아마이드 유도체, 이의제조방법 및 이를 유효성분으로 하는 항암제용 약학조성물
    17.
    发明授权
    히스톤 디아세틸라제 저해활성을 갖는 알킬카바모일나프탈렌일옥시 옥테노일 하이드록시아마이드 유도체, 이의제조방법 및 이를 유효성분으로 하는 항암제용 약학조성물 有权
    具有抗组氨酸脱乙酰酶的抑制活性的亚苄基氨基亚磺酰基羟基酰胺衍生物，其制备方法和包含其的抗体组合物

    公开(公告)号：KR100814092B1

    公开(公告)日：2008-03-14

    申请号：KR1020060108230

    申请日：2006-11-03

    Applicant: 한국화학연구원 ,  크리스탈지노믹스(주)

    Inventor： 이철해 ,  정희정 ,  김재학 ,  정원장 ,  조중명 ,  노성구 ,  현영란 ,  이철순

    IPC: C07C235/18 ,  C07C235/10 ,  C07C233/05

    Abstract: An alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide derivative, its pharmaceutically acceptable salt, a method for preparing the derivative, and an anticancer pharmaceutical composition containing the derivative or the salt are provided to inhibit the enzymatic activity of histone deacetylase effectively and to suppress the proliferation of tumor cells. An alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide derivative is represented by the formula 1, wherein R1 is a C1-C3 alkyl group substituted or unsubstituted with at least one substituent selected from the group consisting of a halophenyl group, a C1-C3 alkoxy C1-C3 alkyl group, a cyclohexanyl group, a furanyl group, a thiophenyl group, an imidazole group, an imidazolidyl C1-C3 alkyl group, a C1-C3 alkylamino group, a di-C1-C3 alkylamino group, a hydroxyphenyl group, a tetrahydrofuranyl group, a cyclohexyl group, a cyclohexenyl group, an oxopyrrolidinyl group, an alkoxyphenyl group, a di-C1-C3 alkylaminophenyl group, a C1-C3 alkylpyrrolidinyl group and a trifluoromethoxyphenyl group; a pyrrolidine group substituted or unsubstituted with at least one substituent selected from the group consisting of a C3-C8 cycloalkyl group, a C3-C8 cycloalkyl C1-C3 alkyl group, a benzyl group, a C1-C3 alkyl group or a C3-C8 cycloalkylcarbonyl group; a piperidine group substituted with a C1-C3 alkyl group or a C3-C8 cycloalkyl group; a furan group; or a C3-C8 cycloalkyl group.

    Abstract translation: 提供烷基氨基甲酰基萘氧基辛烯酰羟基酰胺衍生物，其药学上可接受的盐，制备该衍生物的方法和含有该衍生物或其盐的抗癌药物组合物，以有效抑制组蛋白脱乙酰酶的酶活性并抑制肿瘤细胞的增殖。 烷基氨基甲酰基萘氧基辛烯酰羟基酰胺衍生物由式1表示，其中R1是被至少一个选自卤代苯基，C1-C3烷氧基C1-C3烷基的取代基取代或未取代的C1-C3烷基 环己烷基，呋喃基，噻吩基，咪唑基，咪唑烷基C1-C3烷基，C1-C3烷基氨基，二C1-C3烷基氨基，羟基苯基，四氢呋喃基， 环己基，环己烯基，氧代吡咯烷基，烷氧基苯基，二-C1-C3烷基氨基苯基，C1-C3烷基吡咯烷基和三氟甲氧基苯基; 用至少一个选自C 3 -C 8环烷基，C 3 -C 8环烷基C 1 -C 3烷基，苄基，C 1 -C 3烷基或C 3 -C 8的取代基取代或未取代的吡咯烷基 环烷基羰基; 被C1-C3烷基或C3-C8环烷基取代的哌啶基; 一个呋喃组; 或C 3 -C 8环烷基。

    히스톤 디아세틸라제 저해활성을 갖는 퀴녹살린 유도체 및그의 제조방법
    20.
    发明授权
    히스톤 디아세틸라제 저해활성을 갖는 퀴녹살린 유도체 및그의 제조방법 失效
    具有抗组氨酸脱乙酰酶的抑制活性的喹啉衍生物及其制备方法

    公开(公告)号：KR100555021B1

    公开(公告)日：2006-03-03

    申请号：KR1020030060178

    申请日：2003-08-29

    Applicant: 한국화학연구원 ,  크리스탈지노믹스(주)

    Inventor： 이철해 ,  김봉진 ,  정희정 ,  김재학 ,  전미애 ,  성태현 ,  조중명 ,  노성구 ,  이태규 ,  현영란 ,  김진환

    IPC: C07D241/44

    Abstract: 발명은 하기 화학식 1의 퀴녹살린 유도체, 이의 제조방법 및 이를 함유하는 항암 조성물에 관한 것으로, 본 발명의 퀴녹살린 유도체는 히스톤 디아세틸라제의 효소활성을 효과적으로 억제하여 종양세포의 증식을 억제할 수 있다.

    상기 식에서,
    R
    1 은 히드록시, 할로겐, 알킬옥시, 알킬, 아미노, 알킬아미노, 카르복실, 니트로, 아미드 및 술폰으로 이루어진 군으로부터 선택된 하나 이상의 치환체로 치환되거나 치환되지 않은, 아릴, 헤테로아릴 또는 C
    3-8 사이클로알킬이고, 이때 상기 헤테로아릴은 고리 중에 질소, 황 또는 산소를 하나 이상 포함하며;
    R
    2 는 수소 또는 아릴알킬이고;
    A는 O, S, CH
    2 , 술폰(SO
    2 ), 술폭사이드(SO), CONH, NHCO, NX 또는 NXSO
    2 (이때, X는 수소, C
    1-5 알킬, 또는 독립적으로 상기 R
    1 과 동일하게 정의된다)이고;
    n은 0, 1, 2 또는 3이다.

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