Abstract:
본 발명은 신규한 티에노피리미딘 유도체 및 이를 유효성분으로 포함하는 당뇨병 및 다양한 당뇨 관련 질환의 예방 또는 치료용 약제학적 조성물에 관한 것이다. 본 발명의 티에노피리미딘 유도체는 당-의존적 인슐린 분비를 증가시키고 섭식과 체중 증가의 억제효과가 있는 GPR119(G protein-coupled receptor 119)의 활성을 효율적으로 항진시킴으로써 당 및 지질 대사를 개선시켜, 당뇨 뿐 아니라, 비만, 고지혈증, 당뇨병성 혈관질환 등 다양한 당뇨병성 합병증에 대한 효율적인 예방 및 치료용 조성물로 유용하게 이용될 수 있다.
Abstract:
본 발명은 하기 화학식 1 표시되는, 아다만틸기를 갖는 설파마이드 유도체 또는 이의 약제학적으로 허용 가능한 염이 제공된다. 상기 설파마이드 유도체는 11베타 하이드록시스테로이드 디하이드로게나아제 유형1(11 β -hydroxysteroid dehydrogenase type1, 11 β -HSD1)의 활성을 억제하여, 11 β -HSD1에 의해 매개되는 각종 질환을 치료하는데 유용하다.
Abstract:
PURPOSE: A novel quinoxaline derivative is provided to differentiate neural progenitor cells or stem cells into nerve cells, and the differentiated neural progenitor cells into specific cells or oligodendrocytes with high efficiency, and to apply the differentiation-induced neural progenitor cells for treating intractable nervous system diseases. CONSTITUTION: A quinoxaline derivative or a salt thereof is denoted by chemical formula 1. A composition for inducing the differentiation of neural progenitor cells or stem cells into nerve cells contains the quinoxaline derivative or the salt thereof as an active ingredient. The stem cells include embryonic stem cells, embryonic germ cells, adult stem cells, and induced pluripotent stem cells. A method for differentiating the neural progenitor cells or the stem cells comprises the step of culturing the neural progenitor cells or the stem cells with the composition.
Abstract:
PURPOSE: A composition containing a novel 3-indolinone derivative is provided to selectively stain fluorescence to fat and to be used as a diagnosis reagent. CONSTITUTION: A 3-indolinone derivative is denoted by chemical formula 1 or 2. A composition for fluorescence dyeing contains the derivative or salt thereof as an active ingredient. The concentration of the derivative or salt thereof is 1-100 uM. The composition is used for straining fluorescent to fat and diagnosing organism. A kit for detecting lipid contains the derivative or salt thereof as an active ingredient. A kit for diagnosing metabolic diseases contains the derivatives or salt thereof as an active ingredient.
Abstract:
PURPOSE: A composition for inducing differentiation of neural precursor cells or stem cells to neural cells is provided to usefully treat nerve injury diseases. CONSTITUTION: A composition for inducing differentiation of neural precursor cells or stem cells to neural cells contains 10-20 Um of hydroxylamide derivative of chemical formula 1 or salt thereof as an active ingredient. The hydroxyamide derivative is denoted by chemical formula 1a or 1b. The stem cells are embryonic stem cells, adult stem cells, germiparity stem cells, or embryonic tumor stem cell. The neural precursor cells or stem cells are differentiated to neural cells by culturing with the composition.
Abstract:
하기 화학식 1로 표시되는, 베타아미노기를 갖는 1,2,5-트리아제판 유도체 또는 이의 약학적으로 허용 가능한 염이 제공된다. 이 1,2,5-트리아제판 유도체는 DPP-IV의 활성을 억제하여, DPP-IV에 의해 매개되는 각종 질환을 치료하는데 유용하다. [화학식 1]
상기 식에서, R 1 , R 2 및 R 3 은 명세서에 정의되는 바와 같다. 1,2,5-트리아제판 유도체, DPP-IV, 제조 방법, 약학 조성물
Abstract:
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.
Abstract translation: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。