会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明公开
    • 베타아미노기를 갖는 1,4-디아제펜 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
    • 具有β; -AMINO组的1,4-DIAZEPANE衍生物,药物可接受的盐及其制备方法
    • KR1020080067391A
    • 2008-07-21
    • KR1020070004576
    • 2007-01-16
    • 영진약품 주식회사한국화학연구원
    • 김성수천혜경이상달안진희김기영강남숙강승규정원훈김성규김선영권재홍손상권신민기하니나
    • C07D243/14C07D417/12C07D403/12
    • Y02P20/55
    • A 1,4-diazepane derivative is provided to inhibit the activity of DPP-IV excellently, thereby being effectively used to treat or prevent diseases such as insuline-dependent and insuline-independent diabetes, arthritis, obesity, osteoporosis and injured glucose resistance. A 1,4-diazepane derivative having a beta-amino group is represented by a formula(1), wherein R1 is a group(1) or a group(2); R2 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, heteroaryl, a group(1), a group(2), a group(3), a group(4), a group(5), a group(6), a group(7), a group(8), or a group(9); R2 is H, C1-6 alkyl, C3-6 cycloalkyl, heteroaryl, C1-6 alkoxy, -OCH2O, -SO2NH3, -OCF3, phenoxy, halogen, -CN, -NO2, -CF3, -CONH2, -COOR^b, -CH2COOR^b, -OCHR^bCOOR^b or -NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl, aryl, alkylaryl, arylsulfonyl, arylcarbonyl, amino acid derivative or -CH2OCOC(CH3)3; R^d is C1-6 alkyl, trifluoromethyl, a group(1), a group(2), a group(10), a group(11), a group(12), a group(13), pyrazinyl, pyrimidinyl or pyrrolyl; R^e is C1-6 alkyl, C3-6 cycloalkyl, a group(1) or a group(2); R^f is, halogen, NR^bR^c, a group(14), a group(15), a group(16), a group(17), a group(10), heteroaryl, -S-heteroaryl, tetrahydroisoquinoline, thiazolidine, piperidin-4-carboxylic acid or tetrahydropyrimidine; A is CH2, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl, CO2R^d, 2-pyridyl or aryl; X is O or S; and n is an integer from 1 to 3. A method for preparing the 1,4-diazepane derivative comprises the steps of: (a) subjecting an amino acid represented by a formula(2) and a diazepane compound represented by a formula(3) to condensation to obtain a compound represented by a formula(4); and (b) deprotecting the compound of the formula(4), wherein BOC is a protecting group, and other substitutents are same as defined above. A pharmaceutical composition comprises an effective amount of the 1,4-diazepane derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
    • 提供1,4-二氮杂环庚烷衍生物,以有效地抑制DPP-IV的活性,从而有效地用于治疗或预防诸如胰岛素依赖性和胰岛素依赖性糖尿病,关节炎,肥胖症,骨质疏松症和受损葡萄糖耐药性的疾病。 具有β-氨基的1,4-二氮杂环庚烷衍生物由式(1)表示,其中R1是基团(1)或基团(2)。 R2是H,C1-6烷基,C3-6环烷基,C1-6卤代烷基,杂芳基,基团(1),基团(2),基团(3),基团(4),基团(5) ,组(6),组(7),组(8)或组(9); R2是H,C1-6烷基,C3-6环烷基,杂芳基,C1-6烷氧基,-OCH2O,-SO2NH3,-OCF3,苯氧基,卤素,-CN,-NO2,-CF3,-CONH2,-COOR2b ,-CH 2 COOR b,-OCHR 2 bCOOR b或-NR b R c; 每个R b和R c独立地是H,C 1-6烷基或C 3-6环烷基,芳基,烷基芳基,芳基磺酰基,芳基羰基,氨基酸衍生物或-CH 2 OCOC(CH 3)3; R 1是C 1-6烷基,三氟甲基,基团(1),基团(2),基团(10),基团(11),基团(12),基团(13),吡嗪基, 或吡咯基; R 6是C 1-6烷基,C 3-6环烷基,基团(1)或基团(2); (14),基团(15),基团(16),基团(17),基团(10),杂芳基,-S-杂芳基, 四氢异喹啉,噻唑烷,哌啶-4-羧酸或四氢嘧啶; A是CH 2,N,O或S; B是H,C 1-6烷基,C 3-6环烷基,苄基,CO 2 R 12,2-吡啶基或芳基; X是O或S; n为1〜3的整数。一种1,4-二氮杂环庚烷衍生物的制备方法,其特征在于:(a)使式(2)表示的氨基酸和式(3)表示的二氮杂环丁烷化合物 )缩合得到由式(4)表示的化合物; 和(b)使式(4)的化合物脱保护,其中BOC是保护基,其它取代基与上述定义相同。 药物组合物包含有效量的1,4-二氮杂环庚烷衍生物或其药学上可接受的盐和药学上可接受的载体。
    • 6. 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
    • 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
    • KR100820246B1
    • 2008-04-07
    • KR1020060098670
    • 2006-10-10
    • 한국화학연구원
    • 노재성전동주송종환정준원박창민소원영강남숙서지희김낙정박순찬천혜경조영식배명애김기영송진숙현영란김용은노성구이태규조중명유성은
    • C07D231/12C07D401/04
    • 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.
    • 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。