中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

130 records (took 0.034 seconds)

    신규한 세팔로스포린계 화합물 및 약제학적으로 허용되는염과 그의 제조 방법
    12.
    发明公开
    신규한 세팔로스포린계 화합물 및 약제학적으로 허용되는염과 그의 제조 방법 失效
    具有改善抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株及其药学上可接受的盐及其制备方法的CEPHOROSPORIN衍生物

    公开(公告)号：KR1020050001245A

    公开(公告)日：2005-01-06

    申请号：KR1020030042826

    申请日：2003-06-27

    Applicant: 영진약품 주식회사 ,  한국과학기술연구원

    Inventor： 김성규 ,  이정민 ,  전종옥 ,  손상권 ,  최경일 ,  김중협 ,  남길수

    IPC: C07D501/24

    CPC classification number: C07D501/00 ,  Y02P20/55

    Abstract: PURPOSE: Cephalosporin derivatives, its pharmaceutically acceptable salts and a manufacturing process thereof are provided, which cephalosporin derivatives have improved anti-microbial activity, particularly, for methicillin-resistant Staphylococcus aureus(MRSA) strain, so that they can be useful for antibiotics. CONSTITUTION: The cephalosporin derivatives represented by formula (I), or pharmaceutically acceptable salts thereof are provided, wherein X, Y and Z are the same or different, and independently hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 halogenoalkyl, C1-6 alkoxy alkyl or C3-6 cycloalkyl; R1 is an isoxazol compound in which the 3-site is substituted with a compound of formula (A), wherein Q is a substituent useful for cephalosporin-based compound, and is selected from hydrogen, halogen, hydroxyl, mercapto, cyano, carboxy, carboxylic acid, ester, carbamoyloxy, carbamoyl, N,N-dimethylcarbamoyl, C1-4 alkyl, C1-4 alkyloxy, halogen substituted alkyl, aryl or hetero ring substituent; and R2 is hydrogen, an ester-forming group as an ester of carboxy group, salt-forming atom or carboxy-protecting group. The process for preparing the cephalosporin derivatives represented by formula (I), or pharmaceutically acceptable salts thereof comprises reacting an ilide compound of formula (VI) with an aldehyde compound of formula (VII) in the presence of base and organic solvent at -40 to 25 deg. C.

    Abstract translation: 目的：提供头孢菌素衍生物及其药学上可接受的盐及其制备方法，其头孢菌素衍生物具有改善的抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株，因此它们可用于抗生素。 构成：提供由式（I）表示的头孢菌素衍生物或其药学上可接受的盐，其中X，Y和Z相同或不同，独立地是氢，卤素，C 1-6烷基，C 1-6烷氧基， 6卤代烷基，C 1-6烷氧基烷基或C 3-6环烷基; R1是其中3-位被式（A）化合物取代的异恶唑化合物，其中Q是可用于头孢菌素类化合物的取代基，并且选自氢，卤素，羟基，巯基，氰基，羧基， 羧酸，酯，氨基甲酰氧基，氨基甲酰基，N，N-二甲基氨基甲酰基，C 1-4烷基，C 1-4烷氧基，卤素取代的烷基，芳基或杂环取代基; 并且R 2是氢，作为羧基的酯形成基团，成盐原子或羧基保护基。 制备由式（I）表示的头孢菌素衍生物或其药学上可接受的盐的方法包括：在碱和有机溶剂的存在下，使式（VI）的铱化合物与式（Ⅶ）的醛化合物在-40至 25度 C。

    신규한 퀴누클리딘 화합물 및 그 제조방법
    14.
    发明授权
    신규한 퀴누클리딘 화합물 및 그 제조방법 失效
    신규한퀴누클리딘화합물및그제조방법

    公开(公告)号：KR100448002B1

    公开(公告)日：2004-09-13

    申请号：KR1020020005946

    申请日：2002-02-01

    Applicant: 한국과학기술연구원

    Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  석미영 ,  공재양 ,  정대영

    IPC: C07D453/02

    Abstract: PURPOSE: Provided are Quinuclidine compounds which are useful for treatment of brain-nervous diseases caused by cholinergic neurotransmission such as Alzheimer's disease and a preparation method thereof. CONSTITUTION: A quinuclidine compounds of the formula (I) and pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 1 to 5; R is a substituent on a benzene ring, hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-6 alkyl, 1,2 or 3 fluorine substituted C1-6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-6 alkenyl, 1,2 or 3 fluorine substituted C2-6 alkenyl, C2-6 alkynyl, 1,2 or 3 fluorine substituted C2-6 alkynyl, and C3-7 cycloalkyl. A method for preparing the quinuclidine compounds of the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III) or (IV), wherein R1 and R2 are independently C1-6 alkyl, aryl or arylalkyl.

    Abstract translation: 目的：提供用于治疗由胆碱能神经传递引起的脑神经疾病如阿尔茨海默氏病的奎宁环化合物及其制备方法。 构成：提供式（I）的奎宁环化合物及其药学上可接受的盐，其中n是1至5的整数; R为苯环上的取代基，氢，F，Cl，甲氧基，OH，NH2，NO2,3,4-二甲氧基，2,4-二甲氧基，氰基，C1-6烷基，1,2或3个氟取代的C1 -6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C2-6烯基，1,2或3个氟取代的C2-6烯基，C2-6炔基，1,2或3个氟取代的C2-6炔基和C3-7 环。 用于制备式（I）奎宁环化合物的方法包括使式（II）化合物与式（III）或（IV）化合物反应，其中R 1和R 2独立地为C 1-6烷基，芳基或 芳。

    4-아미노피페리딘 유도체 및 그의 제조방법
    15.
    发明授权
    4-아미노피페리딘 유도체 및 그의 제조방법 失效
    4-아미노피페리딘유도체및그의제조방법

    公开(公告)号：KR100418915B1

    公开(公告)日：2004-02-14

    申请号：KR1020000071399

    申请日：2000-11-28

    Applicant: 한국과학기술연구원

    Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이희윤 ,  손정훈 ,  공재양 ,  정대영

    IPC: C07D401/04

    Abstract: PURPOSE: A 4-aminopiperidine analogue and a producing method thereof are provided, therefore the compound can be useful as a ligand of a muscarine receptor, and it is thus used in study on Alzheimer disease. CONSTITUTION: The 4-aminopiperidine analogue is represented by formula(I), wherein R1, R2, R3, R4, R5, R6 and R7 are hydrogen, cycloalkyl having carbon number of 1 to 6, alkoxy, halogen, hydroxy, hydroxymethyl, aryl, heteroaryl, amino, alkylamino, alkenyl, carbonyl or hetero ring having carbon number of 5 to 7 wherein aryl is a ring having 6 atoms, two rings having 10 atoms or a stable resonance form having double bond to adjacent carbon; heteroaryl is a single ring aromatic group having carbon number of 5 to 6 or a double ring aromatic group having carbon number of 10 in which the heteroaryl has at least one hetero atom of N, O or S; hetero ring consists of 5 to 7 atoms having 1 to 3 of N, O or S; X is carbon or sulfur; and n is an integer of 1 to 2 wherein n is 1 when X is carbon and is 2 when X is sulfur. The 4-aminopiperidine analogue is produced by reacting piperidine or amine(II) with piperazine with ketone(III) in the presence of 1 to 3 equivalent of acetic acid, 2 to 10 equivalent of reducing agent and solvent at room temperature for 3 to 24 hours to produce 4-aminopiperidine(I) and adding NaHCO3 solution and organic solvent to 4-aminopiperidine(I); and drying the extracted 4-aminopiperidine(I), dissolving it, adding 1 to 10 equivalent of hydrogen chloride to the solution, and separating, washing and drying the hydrochloride of 4-aminopiperidine.

    Abstract translation: 目的：提供了4-氨基哌啶类似物及其生产方法，因此该化合物可用作毒蕈碱受体的配体，因此用于研究阿尔茨海默病。 构成：4-氨基哌啶类似物由式（I）表示，其中R1，R2，R3，R4，R5，R6和R7是氢，碳数为1-6的环烷基，烷氧基，卤素，羟基，羟甲基，芳基 杂芳基，氨基，烷基氨基，链烯基，羰基或杂环，其中芳基是具有6个原子的环，具有10个原子的两个环或具有与相邻碳双键的稳定的共振形式; 杂芳基为碳数为5至6的单环芳族基团或碳数为10的双环芳族基团，其中杂芳基具有至少一个N，O或S的杂原子; 杂环由5至7个具有1至3个N，O或S的原子组成; X是碳或硫; 并且n是1至2的整数，其中当X是碳时，n是1，当X是硫时，n是2。 4-氨基哌啶类似物是通过使哌啶或胺（II）与哌嗪与酮（III）在1至3当量乙酸，2至10当量还原剂和溶剂的存在下在室温下反应3至24 小时以产生4-氨基哌啶（I）并将NaHCO 3溶液和有机溶剂加入到4-氨基哌啶（I）中; 干燥提取的4-氨基哌啶（I），溶解，加入1至10当量的氯化氢至溶液中，分离，洗涤并干燥4-氨基哌啶的盐酸盐。

    신규한 알케닐 아자 두 고리 화합물 및 그 제조방법
    17.
    发明公开
    신규한 알케닐 아자 두 고리 화합물 및 그 제조방법 失效
    亚苄基偶氮化合物及其制备方法

    公开(公告)号：KR1020030063853A

    公开(公告)日：2003-07-31

    申请号：KR1020020004199

    申请日：2002-01-24

    Applicant: 한국과학기술연구원

    Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  공재양 ,  정대영

    IPC: C07D453/02 ,  C07D471/08 ,  C07D261/06

    Abstract: PURPOSE: An alkenyl azabicyclic compound and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders. CONSTITUTION: An alkenyl azabicyclic compound represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; and R is selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine substituted C2-C6 alkynyl and C3-C7 cyloalkyl. A method for preparing the alkenyl azabicyclic compound of the formula(I) comprises a compound of the formula(II) with a compound of the formula(III) or formula(IV), wherein R1, R2 and R3 are independently C1-C6 alkyl, aryl or arylalkyl.

    Abstract translation: 目的：提供一种烯基氮杂双环化合物及其制备方法，其可用于治疗由胆碱神经传递障碍引起的脑神经疾病。 构成：提供由式（I）表示的烯基氮杂双环化合物及其药学上可接受的盐，其中n为1或2; 并且R选自氢，F，Cl，甲氧基，OH，NH 2，NO 2，3,4-二甲氧基，2,4-二甲氧基，氰基，C 1 -C 6烷基，1,2或3个氟取代的C 1 C 1-6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C 2 -C 6烯基，1,2或3个氟取代的C 2 -C 6炔基和C 3 -C 7环烷基。 制备式（I）的烯基氮杂双环化合物的方法包括式（II）化合物与式（III）或式（IV）化合物，其中R 1，R 2和R 3独立地为C 1 -C 6烷基 ，芳基或芳烷基。

    이소옥사졸릴 메틸렌 옥사졸리디논 유도체 및 이의 제조방법
    18.
    发明公开
    이소옥사졸릴 메틸렌 옥사졸리디논 유도체 및 이의 제조방법 失效
    ISOOXAZOLYL甲基氧杂环丁酮衍生物

    公开(公告)号：KR1020000074954A

    公开(公告)日：2000-12-15

    申请号：KR1019990019241

    申请日：1999-05-27

    Applicant: 한국과학기술연구원

    Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

    IPC: C07D413/14

    Abstract: PURPOSE: Provided is an isooxazolyl methylene oxazolidinone derivative represented by the formula (I) which is superior in antibacterial activity. Also, a method for preparing the compound is provided. CONSTITUTION: An isooxazoly methylene oxazolidinone derivative is represented by the formula (I): wherein, R is hydrogen, alkyl, halogen such as bromine or chlorine, cyano, alkoxy, hydroxy, carboxy, carbamoyl, N,N'-dimethylcarbamoyl, carbamoyloxy, oxygen, sulfur, thiopene having more than one nitrogen atom, thiazole, aminothiazole, isothiazole, isooxazole, oxazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogenalkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, phosphate, sulfate or amine not being salt. The isooxazoly methylene oxazolidinone derivative is prepared by reacting oxazolidine derivative represented by the formula (II) and isooxazole derivative represented by the formula (III) a using a reductant in the presence of a solvent.

    Abstract translation: 目的：提供抗菌活性优异的由式（I）表示的异恶唑基亚甲基恶唑烷酮衍生物。 此外，提供了制备该化合物的方法。 构型：异恶唑基亚甲基恶唑烷酮衍生物由式（I）表示：其中R是氢，烷基，卤素如溴或氯，氰基，烷氧基，羟基，羧基，氨基甲酰基，N，N'-二甲基氨基甲酰基，氨基甲酰氧基， 氧，硫，具有多于一个氮原子的噻吩，噻唑，氨基噻唑，异噻唑，异恶唑，恶唑，四唑，吡啶，烷基，卤代烷氧基，被氰基或苯氧基取代的苯环的5或6元不饱和杂环取代基， 甲磺酸盐，富马酸盐，溴酸盐，柠檬酸盐，磷酸盐，硫酸盐或胺不是盐。 异恶唑亚甲基恶唑烷酮衍生物通过使用还原剂在溶剂存在下使式（II）表示的恶唑烷衍生物和由式（III）a表示的异恶唑衍生物反应来制备。

    인듐과 아연 금속을 이용한 신규 페남 유도체 및 이의 제조 방법
    19.
    发明公开
    인듐과 아연 금속을 이용한 신규 페남 유도체 및 이의 제조 방법 失效
    使用印度和锌的新PENAM衍生物及其制备方法

    公开(公告)号：KR1020000073204A

    公开(公告)日：2000-12-05

    申请号：KR1019990016354

    申请日：1999-05-07

    Applicant: 한국과학기술연구원

    Inventor： 조용서 ,  최경일 ,  배애님 ,  고훈영 ,  장문호 ,  김유승 ,  이지은

    IPC: C07D499/00

    CPC classification number: Y02P20/55

    Abstract: PURPOSE: A new penam derivative using indium and zinc and a preparation method thereof are provided CONSTITUTION: A novel penam derivative represented by formula(I) is prepared by reacting 6-oxopenam of the formula(I') with ally halide of the formula (II) or acetylene halide of the formula (III) in the presence of indium or zinc. In the formula(I): R1 is allyl derivative and acetylene derivative; R2 is hydrogen, carboxylic acid salt(sodium salt and potassium salt as inorganic salt, alkyl amine salt, aromatic amine salt as organic salt) or carboxy protecting group(4-methoxy benzyl, diphenylmethyl, 4-nitrobenzyl, useful thing as protecting group of molecule in penicillin or cephalosporin compound field); R3 is hydrogen, halogen, hydroxy, acetoxy group.

    Abstract translation: 目的：提供使用铟和锌的新的penam衍生物及其制备方法构成：式（I）表示的新型penam衍生物通过式（I'）的6-氧代青霉素与式（I'）的式 II）或式（III）的炔酰卤在铟或锌的存在下进行。 在式（I）中：R 1是烯丙基衍生物和乙炔衍生物; R2为氢，羧酸盐（钠盐和钾盐为无机盐，烷基胺盐，芳族胺盐为有机盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基，有用物质为保护基 分子在青霉素或头孢菌素化合物领域）; R3是氢，卤素，羟基，乙酰氧基。

Patent Agency Ranking