公开(公告)号：KR1020100130027A

公开(公告)日：2010-12-10

申请号：KR1020090048675

申请日：2009-06-02

Applicant: 한국화학연구원

Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  임채조 ,  황은숙 ,  홍정호

IPC: C07D257/04 ,  C07D403/08 ,  A61P19/10

Abstract: PURPOSE: A pharmaceutical composition containing imidazo phenyltetrazole derivative for preventing and treating osteoporosis, obesity, diabetes or hyperlipidemia is provided. CONSTITUTION: A pharmaceutical composition for preventing or treating osteroporosis contaisn imidazo phenyltetrazole derivative 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.

Abstract translation: 目的：提供含有咪唑并噻唑衍生物的预防和治疗骨质疏松症，肥胖症，糖尿病或高脂血症的药物组合物。 构成：用于预防或治疗化学式1的咪唑并苯并噻唑衍生物或其药学上可接受的盐作为有效成分的药物组合物。 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。

公开(公告)号：KR1020090032809A

公开(公告)日：2009-04-01

申请号：KR1020070098323

申请日：2007-09-28

Applicant: 한국화학연구원

Inventor： 배명애 ,  안도연 ,  이정은 ,  허자명 ,  김희연 ,  이상달 ,  정원훈 ,  천혜경

IPC: C12N15/12

CPC classification number: A01K67/027 ,  A01K2227/105 ,  A01K2267/03

Abstract: A method for screening medicine for treatment and prevention of osteoporosis and metabolic bone disease using TALLYHO/JngJ mouse is provided to facilitate an examination process. A method for screening medicine for treatment and prevention of osteoporosis and metabolic bone disease comprises the following steps of: injecting medicine candidates for treating osteoporosis and metabolic bone disease to a TALLYHO/JngJ male mouse; measuring an index value correlated to osteoporosis and metabolic bone disease from the medicine candidate-injected mouse; and selecting medicine candidates which change the index values of the medicine candidate-injected mouse by comparing to a control group to which the medicine candidate is not injected.

Abstract translation: 提供了使用TALLYHO / JngJ小鼠筛选药物治疗和预防骨质疏松症和代谢性骨病的方法，以便于检查过程。 一种用于治疗和预防骨质疏松症和代谢性骨病的药物的方法，包括以下步骤：向TALLYHO / JngJ雄性小鼠注射用于治疗骨质疏松症和代谢性骨病的候选药物; 从候选药物注射的小鼠中测量与骨质疏松症和代谢性骨病相关的指标值; 并且通过与不注射药物候选者的对照组进行比较来选择改变注射了候选药物的小鼠的指标值的候选药物。

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。

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。