티오우레아 유도체를 포함하는 자가면역질환 예방 또는 치료용 약학적 조성물
    1.
    发明授权
    티오우레아 유도체를 포함하는 자가면역질환 예방 또는 치료용 약학적 조성물 有权
    用于预防或治疗自身免疫性疾病的药物组合物,其包含硫脲衍生物

    公开(公告)号:KR101834005B1

    公开(公告)日:2018-03-05

    申请号:KR1020160102224

    申请日:2016-08-11

    CPC classification number: A61K31/17 A61P1/00 A61P3/10 A61P17/06 A61P19/02

    Abstract: 본발명은티오우레아유도체의신규한용도에관한것으로서, 보다구체적으로는티오우레아유도체를유효성분으로포함하는자가면역질환예방또는치료용약학적조성물에관한것이다. 본발명에따른티오우레아유도체는 TNF-α, IL-1β, NOS2, IL-6 등의염증유전자의전사를억제할뿐만아니라, Th17의활성또는생성을억제하고, 조절 T 세포(Regulatory T cell: Treg)의활성또는생성을증가시킬수 있기때문에, 류마티스관절염을비롯한다양한자가면역질환의예방, 개선또는치료를위한약학적조성물, 건강식품조성물등에유용하게사용할수 있을것으로기대된다.

    Abstract translation: 本发明涉及硫脲衍生物的新用途,更具体地涉及用于预防或治疗包含硫脲衍生物作为活性成分的自身免疫性疾病的药物组合物。 硫基根据本发明的尿素衍生物是TNF-α,IL-1β,NOS2,IL-6等,以及抑制炎性基因的转录,抑制Th17细胞和调节性T细胞(调节性T细胞的活性或产生的: Treg),预计其可用于预防,改善或治疗包括类风湿性关节炎的各种自身免疫疾病的药物组合物和保健食品组合物。

    RORα의 활성자로서의 신규한 thiourea 유도체 및 이를 함유하는 약학적 조성물
    4.
    发明公开
    RORα의 활성자로서의 신규한 thiourea 유도체 및 이를 함유하는 약학적 조성물 有权
    新的硫脲衍生物作为ROR活化剂,以及含有它们的药物组合物

    公开(公告)号:KR1020120130733A

    公开(公告)日:2012-12-03

    申请号:KR1020120054540

    申请日:2012-05-23

    CPC classification number: C07C335/12

    Abstract: PURPOSE: A compound is provided to treat and prevent metabolic diseases and inflammatory diseases through various biofunctions of RORα, being especially useful for preventing and treating liver aliments by controlling cholesterol homeostasis and suppression of lipids. CONSTITUTION: A compound is represented by chemical formula 1. In chemical formula 1, R is hydrogen or a C1-3 alkyl group, R2 is hydrogen, a halogen, a C1-3 alkyl, a C1-3 alkoxy, a nitro group, a hydroxyl group, or a phenoxy group, R3 is hydrogen, a halogen, a C1-3 alkyl group, a C1-3 alkoxy group, a nitro group, a hydroxy group, or a phenoxy group, R4 is hydrogen, a halogen, a C1-3 alkyl group, a C1-3 alkoxy group, a nitro group, a hydroxy group, a cyano group, a dimethylamino group, a methylsulfonylamide group, a trifluoromethyl group, a binylbenzene group, a phenoxy group, a benzoxy group, a aryl group, or a phenylamine group, R5 is hydrogen, a halogen, a C1-3 alkyl group, a C1-3 alkoxy group, a nitro group, a hydroxy group, or aphenoxy group.

    Abstract translation: 目的:提供一种化合物,通过RORα的各种生物功能治疗和预防代谢疾病和炎症疾病,特别适用于通过控制胆固醇体内平衡和抑制脂质来预防和治疗肝脏营养。 化学式为化学式1中,R为氢或C 1-3烷基,R 2为氢,卤素,C 1-3烷基,C 1-3烷氧基,硝基, 羟基或苯氧基,R3是氢,卤素,C1-3烷基,C1-3烷氧基,硝基,羟基或苯氧基,R4是氢,卤素, C 1-3烷基,C 1-3烷氧基,硝基,羟基,氰基,二甲基氨基,甲基磺酰胺基,三氟甲基,乙烯基苯基,苯氧基,苯氧基, 芳基或苯胺基,R 5为氢,卤素,C 1-3烷基,C 1-3烷氧基,硝基,羟基或苯氧基。

    알파-알킬-알파-카르보닐-락탐 유도체 및 이의 입체이성질체 및 이를 함유하는 조성물
    5.
    发明授权
    알파-알킬-알파-카르보닐-락탐 유도체 및 이의 입체이성질체 및 이를 함유하는 조성물 有权
    α-ALKYL-α-CARBONYL LACTAM衍生物及其立体异构体及含有其的药物组合物

    公开(公告)号:KR101497962B1

    公开(公告)日:2015-03-03

    申请号:KR1020130104922

    申请日:2013-09-02

    Abstract: 본원은 신규한 항암활성을 갖는 알파-알킬-알파-카르보닐-락탐 유도체와 그 입체 이성질체 및 이를 함유하는 약학적 조성물을 개시하며, 본원에 따른 화합물을 포함하는 조성물은 암의 예방 및 치료에 유용하다.

    Abstract translation: 公开了具有新抗癌活性的α-烷基-α-羰基内酰胺衍生物,其立体异构体和含有它们的药物组合物。 包含本发明化合物的组合物可有效预防和治疗癌症。 根据本发明,通过抑制癌细胞生长的功能,α-烷基-α-羰基内酰胺衍生物具有预防和治疗癌症的作用,特别是在不存在p53蛋白质的情况下,对p53蛋白质灭活的癌细胞中具有效果 MDM2抑制剂,从而用于抗癌治疗。

    비대칭 상이동 촉매반응을 이용한 알파,알파-디알킬말로네이트의 합성방법
    7.
    发明公开
    비대칭 상이동 촉매반응을 이용한 알파,알파-디알킬말로네이트의 합성방법 无效
    α,α-二甲基马来酸酐的新型选择性相转移催化合成方法

    公开(公告)号:KR1020120065115A

    公开(公告)日:2012-06-20

    申请号:KR1020100126456

    申请日:2010-12-10

    CPC classification number: C07C67/343 B01J31/02 C07C69/38

    Abstract: PURPOSE: A manufacturing method of optically pure alpha-dialkyl malonate is provided to manufacture asymmetric malonate having desired substituent through successive dialkylation. CONSTITUTION: A manufacturing method of optically pure alpha-dialkyl malonate which is represented by chemical formula 2 comprises the following steps: mixing a compound which is represented by chemical formula 1 and solvent with alkyl halide R-X under existence of (S,S)-NAS which is represented by chemical formula 4; and cooling the mixture down to -100-10 deg/ Celsius; and adding base to the frozen mixture. In the chemical formula 1 and 2, A and A' can be identical different, and are selected from phenyl radical, cyclohexyl group, and cyclopentyl group. The phenyl radical, cyclohexyl group, and cyclopentyl group can be substituted with a substituent which is selected from alkyl group having 1-10 carbons, phenyl radical, benzyl radical, allyl group, alkoxy radical, halogen, alkylester having 1-10 carbons, phenylester, and benzylester group. B is selected from hydrogen, alkyl group having 1-10 carbons, phenyl radical, allyl group, benzyl radical, and halogen. R is selected from alkyl group having 1-10 carbons, phenyl radical, allyl group, and benzyl radical.

    Abstract translation: 目的:提供光学纯的丙二酸二烷基酯的制备方法,以通过连续二烷基化制备具有所需取代基的不对称丙二酸酯。 构成:由化学式2表示的光学纯的α-二烷基丙二酸酯的制造方法包括以下步骤:将由(S,S)-NAS存在的化学式1表示的化合物与溶剂与烷基卤RX混合 其由化学式4表示; 并将混合物冷却至-100-10℃/摄氏度; 并向冷冻混合物中加入碱。 在化学式1和化学式2中,A和A'可以相同,选自苯基,环己基和环戊基。 苯基,环己基和环戊基可以被选自具有1-10个碳的烷基,苯基,苄基,烯丙基,烷氧基,卤素,具有1-10个碳的烷基酯,苯基酯 ,和苄基酯基。 B选自氢,具有1-10个碳的烷基,苯基,烯丙基,苄基和卤素。 R选自具有1-10个碳的烷基,苯基,烯丙基和苄基。

    RORα의 활성자로서의 신규한 thiourea 유도체 및 이를 함유하는 약학적 조성물
    10.
    发明公开
    RORα의 활성자로서의 신규한 thiourea 유도체 및 이를 함유하는 약학적 조성물 无效
    新的硫脲衍生物作为ROR活化剂,以及含有它们的药物组合物

    公开(公告)号:KR1020120130678A

    公开(公告)日:2012-12-03

    申请号:KR1020110128903

    申请日:2011-12-05

    Abstract: PURPOSE: A compound is provided to prevent and treat inflammatory diseases and metabolic disease through various biofunctions, being especially useful for preventing and treating liver ailments by controlling cholesterol homeostasis and suppressing the synthesis of lipids. CONSTITUTION: A compound is indicated in chemical formula 1. In chemical formula 1, R1 is hydrogen or a C1-3 alkyl, each of R2 and R3 is hydrogen, or a C1-3 alkyl, alkoxy, hydroxy, nitro, hydroxy or phenoxy group. R4 is hydrogen, a halogen, or a C1-3 alkyl, alkoxy, nitro, hydroxy, cyano, dimethylamino, methylsulfonylamide, trifluoromethyl, vinyl benzene, phenoxy, benzoxy, aryl or phnylamine group, R5 is hydrogen, halogen, or a C1-3 alkyl, alkoxy, nitro, hydroxy or phenoxy group.

    Abstract translation: 目的:提供一种化合物,通过各种生物功能预防和治疗炎症性疾病和代谢疾病,特别适用于通过控制胆固醇体内平衡和抑制脂质合成来预防和治疗肝脏疾病。 化学式为化学式1中,R1为氢或C1-3烷基,R2和R3分别为氢或C1-3烷基,烷氧基,羟基,硝基,羟基或苯氧基 组。 R4是氢,卤素或C1-3烷基,烷氧基,硝基,羟基,氰基,二甲基氨基,甲基磺酰胺,三氟甲基,乙烯基苯,苯氧基,苯氧基,芳基或芳基,R5是氢,卤素或C1- 3烷基,烷氧基,硝基,羟基或苯氧基。

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