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    황반변성 예방 또는 치료용 약학 조성물
    2.
    发明公开
    황반변성 예방 또는 치료용 약학 조성물 审中-实审
    用于预防或治疗谷物变性的药物组合物

    公开(公告)号：KR1020120112162A

    公开(公告)日：2012-10-11

    申请号：KR1020120032161

    申请日：2012-03-29

    Applicant: 한국화학연구원 ,  가톨릭대학교 산학협력단

    Inventor： 이규양 ,  유성은 ,  김낙정 ,  서지희 ,  주천기 ,  최준섭 ,  양재식 ,  이근혁 ,  조윤석 ,  박진하 ,  이혜성

    IPC: A61K31/4164 ,  A61K31/35 ,  A61P27/02

    CPC classification number: A61K9/0048 ,  A61K31/4178

    Abstract: PURPOSE: A pharmaceutical composition containing secondary amine-substituted benzopyrane derivative is provided to prevent or treat macular degeneration. CONSTITUTION: A pharmaceutical composition for preventing or treating macular degeneration contains a compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. The composition is used in the form of eye drops and the active ingredients are delivery to retina. Eye drops for preventing or treating macular degeneration contain the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing or treating macular degeneration contains (2R,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(1H-imidazole-2-ylmethyl)amino]-3-hydroxy-2-methyl-2-dimethoxymethyl-3,4-dihydro-2H-1-benzopyrane or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的：提供含有仲胺取代苯并吡喃衍生物的药物组合物，用于预防或治疗黄斑变性。 构成：用于预防或治疗黄斑变性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。 组合物以眼药水的形式使用，活性成分被输送到视网膜。 用于预防或治疗黄斑变性的眼药水含有化学式1的化合物或其药学上可接受的盐作为活性成分。 用于预防或治疗黄斑变性的药物组合物含有（2R，3R，4S）-6-氨基-4- [N-（4-氯苯基）-N-（1H-咪唑-2-基甲基）氨基] -3-羟基 -2-甲基-2-二甲氧基甲基-3,4-二氢-2H-1-苯并吡喃或其药学上可接受的盐作为活性成分。

    1-(6,7-다이플루오르-3-메톡시퀴녹살린-2-일)-3-［1-(헤테로아릴메틸)피페리딘-4-일］ 우레아 유도체, 그 제조방법 및 그의 용도
    4.
    发明公开
    1-(6,7-다이플루오르-3-메톡시퀴녹살린-2-일)-3-［1-(헤테로아릴메틸)피페리딘-4-일］ 우레아 유도체, 그 제조방법 및 그의 용도 有权
    1-（6,7-二氟-3-甲氧基喹啉-2-基）-3- [1-（异丁基甲基）哌啶-4-基]脲衍生物及其药学上可接受的盐，其制备和使用方法

    公开(公告)号：KR1020110094566A

    公开(公告)日：2011-08-24

    申请号：KR1020100014043

    申请日：2010-02-17

    Applicant: 한국화학연구원

    Inventor： 전문국 ,  이태호 ,  황순희 ,  이지민 ,  유성은 ,  이병호 ,  오광석 ,  공영대 ,  이승호

    IPC: C07D403/12 ,  C07D413/14 ,  A61P3/04

    Abstract: PURPOSE: A 1-(6,7-difluoro-3-methoxyquinoxaline-2-yl)-3-[1-(heteroarylmethyl)piperidine-4-yl]urea derivatives is provided to suppress MCH1R and to prevent and treat obesity without side effects. CONSTITUTION: A 1-(6,7-difluoro-3-methoxyquinoxaline-2-yl)-3-[1-(heteroarylmethyl)piperidine-4-yl]urea derivative is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by reduction alkylation of a compound of chemical formula 5 with heteraryl aldehyde compound of chemical formula 6. A MCH1R inhibitor composition contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing and treating obesity contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的：提供1-（6,7-二氟-3-甲氧基喹喔啉-2-基）-3- [1-（杂芳基甲基）哌啶-4-基]脲衍生物以抑制MCH1R并预防和治疗无侧面肥胖 效果。 构成：化学式1表示1-（6,7-二氟-3-甲氧基喹喔啉-2-基）-3- [1-（杂芳基甲基）哌啶-4-基]脲衍生物。化学式1的化合物 通过用化学式6的杂芳基醛化合物将化学式5的化合物还原烷基化制备.MCH1R抑制剂组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。 用于预防和治疗肥胖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。

    아릴 피페리딘기-함유 이미다졸 유도체, 이의 제조방법 및이를 유효성분으로 포함하는 약학적 조성물
    7.
    发明公开
    아릴 피페리딘기-함유 이미다졸 유도체, 이의 제조방법 및이를 유효성분으로 포함하는 약학적 조성물 失效
    具有芳基哌啶取代基的咪唑衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：KR1020080100024A

    公开(公告)日：2008-11-14

    申请号：KR1020070046073

    申请日：2007-05-11

    Applicant: 한국화학연구원

    Inventor： 김낙정 ,  유성은 ,  이규양 ,  서지희 ,  이병호

    IPC: C07D471/04 ,  C07D401/06 ,  A61K31/4439

    Abstract: An imidazol derivative having an aryl piperidine substituent is provided to prevent and cure diseases relating to MCH by acting on an antagonist to a melanin-concentrating hormone receptor. An imidazole derivative or a salt pharmaceutically allowable is indicated as a chemical formula 1. In the chemical formula 1: R1 is C1~C4 of straight-chain or side chain alkyl; R2 is H, halogen, C1~C3 of straight-chain or side chain alkyl, phenyl, OR4, NO2, CN, pyridyl, CHO or -CONR5R6; X is H, halogen, OR4 or NO2, C1~C3 of straight-chain or side chain alkyl; R4, R5 and R6 are independently H, C1~C3 of straight-chain or side chain alkyl or phenyl; ; R3 is C1~C3 of straight-chain or side chain alkyl and phenyl substituted into halogen or methyl; A is CH or N; and n is an integer of 2 - 5.

    Abstract translation: 提供具有芳基哌啶取代基的咪唑衍生物，以通过作用于黑色素浓缩激素受体的拮抗剂来预防和治愈与MCH相关的疾病。 化学式1表示咪唑衍生物或其药学上可接受的盐。在化学式1中：R1是直链或侧链烷基的C1〜C4; R2是H，卤素，C1-C3直链或侧链烷基，苯基，OR4，NO2，CN，吡啶基，CHO或-CONR5R6; X为H，卤素，OR4或NO2，C1〜C3为直链或侧链烷基; R4，R5和R6独立地为H，直链或侧链烷基或苯基的C1〜C3; ; R3是直链或侧链烷基的C1〜C3，被卤素或甲基取代的苯基; A是CH或N; n为2〜5的整数。

    신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1Ｈ-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물
    8.
    发明公开
    신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1Ｈ-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-（3,4-二甲氧基苯基） - 乙基] -1H-吡唑化合物，其制备方法和包含其的药物组合物

    公开(公告)号：KR1020080065722A

    公开(公告)日：2008-07-15

    申请号：KR1020070002715

    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: C07D231/12 ,  C07D401/04 ,  C07D403/10 ,  C07D413/04

    Abstract: A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.

    Abstract translation: 提供了一种新型化合物，以显示对PDE-4酶的优异活性和对其他PDE酶的高选择性，从而被用作炎症相关疾病，关节炎，特应性皮炎，白血病，各种癌症和退行性脑病的治疗剂 效果。 1-（1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑化合物由式（1）表示，通过式（2）表示的卤代苄基化合物与吡唑化合物 由公式（3）表示。 在式（1）中，每个R 1和R 2独立地为H，可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基，C 3-7环烷基，（C 3-7）环烷基（C 1-7） 烷基，芳基或杂芳基，芳（C 1-5）烷基或芳（C 1-5）烷氧基，或者R 1和R 2可以被C 1-3亚烷基相互连接; 每个R 3，R 4和R 5独立地为H，苯基，吡啶基，N-氧代吡啶基，直链或支链饱和和不饱和C 1-7烷基，C 3-7环烷基，（C 3-10）环烷基（C 1-7）烷基，卤素，氰基 ，硝基，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，C3-7环烷基氨基，3至7元饱和或不饱和杂环，包括O，N或S，胍基 （C 1-7）烷基，羟基（C 1-7）烷基，羧基或（C 1-7）烷氧基羰基;（C 1-7）烷氧基， R6是直链或支链饱和和不饱和的C1-7烷基，C3-7环烷基，（C3-10）环烷基（C1-7）烷基，苯基，苯氧基，苄基，苄氧基，C1-7烷氧基或（C1-7） 烷氧基（C 1-7）烷基。 用于治疗或预防与气道炎症，关节炎，特应性皮炎，白血病，癌症或退行性脑疾病相关的疾病的药物组合物包括1- [1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑衍生物作为有效的 成分。

    7-(3,4-디알콕시페닐)-피라졸로[1,5-ａ]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물
    9.
    发明授权
    7-(3,4-디알콕시페닐)-피라졸로[1,5-ａ]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물 失效
    7-（3,4-디알콕시페닐） - 피라졸로[1,5-α]피리미딘화합물을포함하는관절염，아토피피부염，백혈병을포함한암및알쯔하이머，우울증또는기억력감소등의뇌질환의치료및 예방을위약제제학적조성

    公开(公告)号：KR100753017B1

    公开(公告)日：2007-08-30

    申请号：KR1020060046860

    申请日：2006-05-25

    Applicant: 한국화학연구원

    Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  박창민 ,  소원영 ,  강남숙 ,  홍석주 ,  천혜경 ,  조영식 ,  김기영 ,  배명애 ,  송진숙 ,  노성구 ,  현영란 ,  이운영 ,  김용은 ,  강봉균 ,  이혜련 ,  유성은

    IPC: A61K31/437 ,  A61P35/00

    Abstract: A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.

    Abstract translation: 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病，其包括7-（3,4-二烷氧基） - 吡唑并提供[1,5-a]嘧啶化合物抑制PDE-4的活性（phosphodiesterase-的药物组合物 4）并通过减少HARBS（高亲和力咯利普兰结合位点）亲和力来减少副作用，例如呕吐。 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病的药物组合物包含7-（3,4-二烷氧基） - 吡唑并[1,5-a]嘧啶化合物由式（1）表示，其中R1和R2 （C 1 -C 7）烷基，含有卤素原子的直链或支链饱和或不饱和（C 1 -C 7）烷基，（C 3 -C 7）环烷基，含有3至7元杂环烷基的3元至7元杂环烷基 （C4-C10）环烷基（C1-C7）烷基，在杂环中含有氧，氮或硫的3元至7元杂环烷基（C1-C7）烷基，苯基 ，苄基或烯丙基; （C 1 -C 7）烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，（C 1 -C 7）烷氧基， （C 1 -C 7）烷基，羧酸，羧基（C 1 -C 7）烷基酯，羧基（C 1 -C 7）烷基酰胺，氨基或单或二（C 1 -C 7）烷基氨基羰基; （C 1 -C 7）烷基，（C 3 -C 7）环烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，羟基（C 1 -C 7）烷基， C1-C7）烷基酮，（C1-C10）烷基羧酸，羧基（C1-C10）烷基酯，羧基（C1-C10）烷基酰胺，氨基，单或二（C1-C7）烷基氨基，单或二（C1-C7 ）烷基氨基羰基，（C3-C7）环烷基胺，吗啉，氧化吗啉，哌啶，哌嗪，哌嗪氧化物或芳基。

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