中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

121 records (took 0.04 seconds)

    퀴나졸린 유도체
    11.
    发明授权
    퀴나졸린 유도체 失效
    喹唑啉衍生物

    公开(公告)号：KR100584157B1

    公开(公告)日：2006-05-26

    申请号：KR1020040035452

    申请日：2004-05-19

    Applicant: 한국화학연구원

    Inventor： 하재두 ,  김군도 ,  공재양 ,  최중권

    IPC: C07D491/056

    Abstract: 본 발명은 티로신 키나제에 대한 억제활성이 우수하여 비정상적인 키나제의 활성으로 야기되는 질환 예를 들면 암, 건선, 류마티스 관절염, 당뇨병성 망막증 등의 치료에 유용한 신규 화합물로서 퀴나졸린의 C-6과 C-7번 위치가 1,4-디옥산기에 의해 연결된 3환 구조의 퀴나졸린 유도체와 이의 제조방법 그리고 이의 의약적 용도에 관한 것이다.
    티로신 키나제, 퀴나졸린 유도체, 1,4-디옥산

    베타-메틸카바페넴 유도체 및 그의 제조방법
    13.
    发明授权
    베타-메틸카바페넴 유도체 및 그의 제조방법 失效
    β-甲基胆碱衍生物及其制备方法

    公开(公告)号：KR100574352B1

    公开(公告)日：2006-04-27

    申请号：KR1020040033474

    申请日：2004-05-12

    Applicant: 한국화학연구원

    Inventor： 김봉진 ,  김재학 ,  김광호 ,  정희정 ,  전미애 ,  공재양 ,  조희영

    IPC: C07D477/20

    CPC classification number: Y02P20/55

    Abstract: 본 발명은 그람양성균 및 그람음성균에 대해 광범위하게 항균효과를 나타내며, 메티실린 내성 스타필로코쿠스 아우레우스(methicillin resistant staphylococcus aureus, MRSA)를 비롯한 내성균에도 우수한 항균효과를 갖는 하기 화학식 1의 카바페넴 유도체, 이의 제조 방법 및 이를 함유하는 항생제 조성물에 관한 것이다.

    상기 식에서, R
    1 , R
    2 및 R
    3 는 각각 독립적으로, 수소, 탄소수 1-3개의 알킬기를 의미하며, M은 수소 또는 약리학적으로 허용가능한 금속염을 형성하는 금속이온을 나타낸다.

    카스파제-3 저해제로서의 퀴놀린 유도체, 이의 제조방법및 이를 포함하는 약제학적 조성물
    17.
    发明公开
    카스파제-3 저해제로서의 퀴놀린 유도체, 이의 제조방법및 이를 포함하는 약제학적 조성물 失效
    喹啉衍生物作为CASPASE-3抑制剂，其制备方法和含有它的药物组合物

    公开(公告)号：KR1020030086417A

    公开(公告)日：2003-11-10

    申请号：KR1020030027872

    申请日：2003-04-30

    Applicant: 영진약품 주식회사 ,  한국화학연구원

    Inventor： 김성규 ,  정윤성 ,  공재양 ,  박우규

    IPC: C07D215/44

    CPC classification number: C07D409/12 ,  C07D215/42 ,  C07D215/44 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

    Abstract: PURPOSE: Quinoline derivatives as a caspase-3 inhibitor, a preparation process thereof and a pharmaceutical composition containing the same are provided. The compounds are useful for prevention and treatment of diseases associated with caspase-3. CONSTITUTION: Quinoline derivatives of the formula 1 or pharmaceutically acceptable salts thereof are provided, wherein R2 is H, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxyalkyl or C3-6 cycloalkyl; R1 is COYA, -CN or NHOSOn(H2C)R3; Y is O, N or S; A is H, C1-3 alkyl optionally substituted C3-6 alkenyl, C3-6 cycloalkyl, halogen, C1-6 alkyl or C1-6 alkoxy optionally substituted C6-14 aryl, C1-6 alkoxyalkyl, or C6-14 aryl or 5 to 15 membered ring heteroaryl optionally substituted C1-6 alkyl; R3 is H, halogen, optionally substituted amino, C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxyalkyl, or C3-6 cycloalkyl; n is 0, 1, 2 or 3; R is H, halogen, C1-6 alkyl, C1-6 alkoxy or amino optionally substituted C6-14 aryl, halogen, C1-6 alkyl, C1-6 alkoxy or amino optionally substituted 5 to 15 membered ring heterocyclic, or -(CH2)n-CHR4R5; R4 is H, C1-6 alkyl, C1-6 alkoxy, halogen, C1-6 alkyl, C1-6 halogenoalkyl, C1-6 alkoxy or amino optionally substituted C6-14 aryl, 5 to 15 membered ring heteroaryl, C3-6 cycloalkyl, C1-6 alkyl optionally substituted 5 to 15 membered ring heterocyclic, or 5 to 15 membered ring heterocyclic fused C6-14 aryl; and R5 is H, C1-6 alkyl, C1-6 alkoxy or C1-6 alkoxyalkyl.

    Abstract translation: 目的：提供作为半胱天冬酶-3抑制剂的喹啉衍生物及其制备方法和含有它们的药物组合物。 该化合物可用于预防和治疗与半胱天冬酶-3相关的疾病。 提供：式1的喹啉衍生物或其药学上可接受的盐，其中R 2是H，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基烷基或C 3-6环烷基; R1是COYA，-CN或NHOSOn（H2C）R3; Y为O，N或S; A是H，C 1-3烷基任选取代的C 3-6烯基，C 3-6环烷基，卤素，C 1-6烷基或C 1-6烷氧基任选取代的C 6-14芳基，C 1-6烷氧基烷基或C 6-14芳基或5 至15元环杂芳基任选取代的C 1-6烷基; R3是H，卤素，任选取代的氨基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基烷基或C 3-6环烷基; n为0,1,2或3; 或者 - （CH 2）2，其中R 1是H，卤素，C 1-6烷基，C 1-6烷氧基或氨基任意取代的C 6-14芳基，卤素，C 1-6烷基，C 1-6烷氧基或氨基任选取代的5至15元环杂环，或 - ）正CHR4R5; R 4是H，C 1-6烷基，C 1-6烷氧基，卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或氨基任选取代的C 6-14芳基，5至15元环杂芳基，C 3-6环烷基 任选取代的5至15元环杂环的C 1-6烷基或5至15元环杂环稠合的C 6-14芳基; R5是H，C1-6烷基，C1-6烷氧基或C1-6烷氧基烷基。

    NMDA수용체길항제로작용하는4-(말단치환-알콕시)-퀴놀린-2-카복실산유도체
    18.
    发明授权
    NMDA수용체길항제로작용하는4-(말단치환-알콕시)-퀴놀린-2-카복실산유도체 失效
    作为NMDA受体拮抗剂的4-（末端烷基） - 喹啉-2-羧酸衍生物

    公开(公告)号：KR100274171B1

    公开(公告)日：2000-12-15

    申请号：KR1019970078811

    申请日：1997-12-30

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정영식 ,  이종철 ,  최진일 ,  이광숙 ,  공재양

    IPC: C07D215/20

    Abstract: PURPOSE: Provided are the novel NMDA receptor antagonists, 4-(end-substituted-alkoxy)-quinoline-2-carboxylic acid derivatives and the preparation method thereof. CONSTITUTION: The novel derivatives are represented as shown in the chemical formula 1, where n is 0¯3, Nu are appropriately substituted arylthio, heterocyclicthio, alkylphoshponate, arylsulfonyl, phthalimide, alkylthio, aralkylthio, carbocyclic thio, non-aromatic thio, arylphosphonate, C3¯C7 heterocyclo alkyl, C3¯C7 heterocyclo alkyl(C1¯C6)alkyl, hetero aryl, hetero aryl(C1¯C6)alkyl heterocycle, C1¯C20 alkyl, C6¯ C12 aryl, cyano, hydroxyl, halogen or alkylsufonyl groups. The synthetic process comprises the steps of: alkylating 5,7-dichlorokynurenic acid methylester with α,ω -dibromoalkane; substituting the bromine with nucleophilic groups and hydrolysing with bases to make the compound of formula 1. When Nu is sulfonyl group, preparation method consists of two more steps of oxidizing the sulfide group of Nu in the chemical formula 1 with m-CPBA and hydrolysing the resultant with aqueous sodium hydroxide. They are strong and unique antagonists acting on the coupling position of the strychnine non-susceptive glycine in the NMDA receptor complex and penetrate effectively into central nervous system. Their tautomer, isomer and pharmaceutically acceptable salts are effective treatment and/or preventive drugs for the neurodegeneration and are specially useful for the CNS damage effected by the diseases such as heart attack, low blood sugar, local anemia and heart beat halt, arising from the low oxygen concentration caused by the external wounds or anemia. For the treatment of neurodegeneration, 0.05¯5.0mg/kg dosages are injected intravenously.

    Abstract translation: 目的：提供新型NMDA受体拮抗剂4-（末端取代 - 烷氧基） - 喹啉-2-羧酸衍生物及其制备方法。 构成：新型衍生物如化学式1所示，其中n为0〜3，Nu为适当取代的芳硫基，杂环硫基，烷基磷酸酯，芳基磺酰基，邻苯二甲酰亚胺，烷硫基，芳烷硫基，碳环硫基，非芳族硫基，芳基膦酸酯， C 3 -C 7杂环烷基，C 3 -C 7杂环烷基（C 1 -C 6）烷基，杂芳基，杂芳基（C 1 -C 6）烷基杂环，C 1 -C 20烷基，C 6 -C 12芳基，氰基，羟基，卤素或烷基磺酰基。 合成方法包括以下步骤：用α，ω-二溴烷烃将5,7-二氯喹诺酮酸甲酯烷基化; 用亲核基团取代溴并用碱水解制备式1的化合物。当Nu为磺酰基时，制备方法由化学式1中的Nu的硫化物基团与m-CPBA氧化两个步骤，并水解 与氢氧化钠水溶液混合。 它们是强力和独特的拮抗剂，作用于NMDA受体复合物中士的宁非感受性甘氨酸的偶联位置，并有效渗入中枢神经系统。 它们的互变异构体，异构体和药学上可接受的盐是用于神经变性的有效治疗和/或预防药物，并且特别适用于由诸如心脏病发作，低血糖，局部贫血和心跳停止等疾病影响的CNS损伤 由外部伤口或贫血造成的低氧浓度。 为了治疗神经变性，静脉注射0.05〜5.0mg / kg剂量。

    히스타민 Ｈ3 수용체에 대한 길항 작용을 갖는 화합물 및이를 함유하는 중추 신경계 질환의 예방 및 치료용 약학적조성물
    20.
    发明公开
    히스타민 Ｈ3 수용체에 대한 길항 작용을 갖는 화합물 및이를 함유하는 중추 신경계 질환의 예방 및 치료용 약학적조성물 有权
    在组胺H3受体上具有拮抗活性的化合物和用于预防和治疗含有其的中枢神经系统疾病的药物组合物

    公开(公告)号：KR1020090128768A

    公开(公告)日：2009-12-16

    申请号：KR1020080054697

    申请日：2008-06-11

    Applicant: 한국화학연구원

    Inventor： 박우규 ,  공재양 ,  조희영 ,  정대영 ,  최길돈 ,  채종학

    IPC: A61K31/167 ,  A61K31/17 ,  A61K31/496 ,  A61K31/551

    Abstract: PURPOSE: A pharmaceutical composition for preventing and treating narcolepsy, congnitive disorder, ADHD(attention-deficit hyperactivity disorder), obesity, epilepsy, schizophrenia, depression, and pain. CONSTITUTION: A pharmaceutical composition for preventing and treating central nervous system disease contains a compound having histamine H3 receptor antagonism. The compound is 4-[3-methyl-3-(1-methyl-pyperidine-4-yl)-ureido]-benzoic acid ethyl ester of chemical formula 1, 1-benzyloxy-3-(4-pyridine-2-yl-piperazine-1-yl)-propan-2-ol of chemical formula 2, N-{4-[4-(2-bromo-4-fluoro-phenyutiocarbamoyl)-[1,4]diazepan-1-yl-methyl]-phenyl}-aceteamide of chemical formula 3, 2-[4-(5-bromo-2H-1λ4-thiophene-2-carbonyl)-[1,4]diazepan-1-yl]-N-phenethyl-aceteamide of chemical formula 4. 1-[benzyl-(2,2-diethoxy-ethyl)-amino]-3-(4-chloro-phenoxy)-propan-2-ol of chemical formula 5, and 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid-[2-(1-benzyl-piperidine-4-yl) ethyl]-amide of chemical formula 6.

    Abstract translation: 目的：预防和治疗发作性睡病，认知障碍，ADHD（注意力缺陷多动障碍），肥胖，癫痫，精神分裂症，抑郁症和疼痛的药物组合物。 构成：用于预防和治疗中枢神经系统疾病的药物组合物含有具有组胺H3受体拮抗作用的化合物。 化合物是化学式1的4- [3-甲基-3-（1-甲基 - 哌啶-4-基） - 脲基] - 苯甲酸乙酯，1-苄氧基-3-（4-吡啶-2-基 - 哌嗪-1-基） - 丙-2-醇，N- {4- [4-（2-溴-4-氟 - 苯基氨基甲酰基） - [1,4]二氮杂环庚烷-1-基 - 甲基 ] - 苯基} - 乙酰胺，2- [4-（5-溴-2H-1λ4-噻吩-2-羰基） - [1,4]二氮杂环庚烷-1-基] -N-苯乙基 - 乙酰胺 化学式4.化学式5的1- [苄基 - （2,2-二乙氧基 - 乙基） - 氨基] -3-（4-氯 - 苯氧基） - 丙-2-醇和5-氯-1,3- - 二甲基-1H-吡唑-4-磺酸 - [2-（1-苄基 - 哌啶-4-基）乙基] - 酰胺。

Patent Agency Ranking