-
公开(公告)号：KR1020000007667A
公开(公告)日：2000-02-07
申请号：KR1019980027115
申请日：1998-07-06
Applicant: 한국과학기술연구원
IPC: C07D501/24 , C07D501/20
Abstract: PURPOSE: A cephem compound for an oral administration having a broad spectrum antibacterial activity is prepared by esterifying cephalosporin compound in the presence of solvent. CONSTITUTION: The compound(I) is manufactured by reacting cephalosporin compound(Korea patent application No.1997-36921) and halide compound in the presence of solvent such as acetone, acetonitrile, dioxane, N,N-dimethylformamide, dimethylsulfoxide at -10 to 25°C for 10 min-12hr(preferably at 0 to 5°C for 10 min-1 hr). In formula(I), R1 = H or trityl, R2 = H, trityl, methyl or cyclopentyl; R3 = H, chloro, bromo or methoxy; R4 = acethoxyethyl, pyvaloyloxymethyl or isopropoxycarbonyloxymethyl. It shows a broad spectrum antibacterial activity about a staphylococcus aureus containing gram-positive bacterium and a gram-positive bacterium, especially methicillin-resistant staphylococcus aureus.
Abstract translation: 目的：通过在溶剂存在下酯化头孢菌素化合物来制备具有广谱抗菌活性的口服给药的头孢烯化合物。 构成：化合物（I）通过在-10℃下在溶剂如丙酮，乙腈，二恶烷，N，N-二甲基甲酰胺，二甲亚砜等溶剂存在下使头孢菌素化合物（韩国专利申请No.1997-36921）与卤化物反应制造而成 25℃10分钟-12小时（优选0-5℃10分钟-1小时）。 在式（I）中，R 1 = H或三苯甲基，R 2 = H，三苯甲基，甲基或环戊基; R3 = H，氯，溴或甲氧基; R4 =乙氧基乙基，吡喃酰氧基甲基或异丙氧羰基氧基甲基。 它显示了对含有革兰氏阳性菌和革兰氏阳性菌，特别是耐甲氧西林金黄色葡萄球菌的金黄色葡萄球菌的广谱抗菌活性。
-
-
公开(公告)号：KR1019940002255A
公开(公告)日：1994-02-17
申请号：KR1019920012642
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
Abstract: 본 발명은 일반구조식(I)의 광범위한 항균력을 지난 세라포스포린 화합물 및 그의 약제학적으로 허용되는 염 및 그 제조방법에 관한 것이다.
본 발명에서 합성된 화합물들은 그람양성균이나, 그람음성균에서 뛰어난 항균력을 나타내므로 세파로스포린 화합물 계열 의약품에 유용하게 사용할 수 있다.-
公开(公告)号：KR1019930007815B1
公开(公告)日：1993-08-20
申请号：KR1019910019260
申请日：1991-10-31
Applicant: 한국과학기술연구원
IPC: C07D501/34
Abstract: Cephalosporin esters of formula (I) and their pharmaceutical salts are prepd. by esterification of cephalosporin cpds. of formula (II) with a halide cpds. of formula (III) in the inert solvent at -10 deg.C to 25 deg.C. (III) are described in KR 89-14873 and us 5051530. In (I), R1=H or a protecting gp. as in cephalosporin and penicillin cpds.; R2, R3= alkyl, C3-7 cycloalkyl or aryl such as phenyl, halophenyl, nitrophenyl or alkoxyphenyl.
Abstract translation: 式（I）的头孢菌素酯及其药用盐是制备的。 通过酯化头孢菌素cpds。 的式（II）与卤素cpds反应。 的式（III）的化合物在惰性溶剂中在-10℃至25℃下反应。 （III）描述于KR 89-14873和US 5051530中。在（I）中，R1 = H或保护性gp。 如头孢菌素和青霉素cpds。 R2，R3 =烷基，C3-7环烷基或芳基如苯基，卤代苯基，硝基苯基或烷氧基苯基。
-
-
Patent Agency Ranking
公开(公告)号：KR1019950008319B1
公开(公告)日：1995-07-27
申请号：KR1019920012642
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
Abstract: This is new cephalosphorin compd. and its parmaceutically acceptable salt of formula(I). In formula, R1 is H, or trityl, tert-butoxycarbonyl, or formyl; R2 H, p-methoxybenzyl, diphenylmethyl or salting compd. such as Na or K; R3 and R4 are same or different, and H, acetyl, or p-methoxybenzyl; X,Y are H, F, Cl, Br, or I; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, pyridiniummethyl, N- ethyl pyridiniumyl thiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, carbamoyloxymethyl, and N-methyl-tetrazolyl thiomethyl gp. This compd. is prepared by acylation of the aminothiazol compd of (II) with cephalosphorin of (III). This cephem compd. has good antibacterial activity.
Abstract translation: 这是新头孢菌素 和其药学上可接受的式（I）盐。 在式中，R 1是H或三苯甲基，叔丁氧基羰基或甲酰基; R2H，对甲氧基苄基，二苯甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，乙酰基或对甲氧基苄基; X，Y是H，F，Cl，Br或I; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，吡啶鎓甲基，N-乙基吡啶鎓硫代甲基，N-羧甲基吡啶鎓硫代甲基，氨基甲酰氧基甲基和N-甲基 - 四唑基硫代甲基gp。 这个compd 通过（II）的氨基噻唑化合物与（III）的头孢菌素的酰化制备。 这个cephem compd 具有良好的抗菌活性。
-
公开(公告)号：KR1019950008318B1
公开(公告)日：1995-07-27
申请号：KR1019920012641
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
CPC classification number: Y02A50/473 , Y02A50/481
Abstract: This is new cephalosphorin compd. and its parmaceutically acceptable salt of formula(I). In formula, R1 is H, or trityl, tert-butoxycarbonyl, or formyl; R2 hydrogen, p-methoxybenzyl, diphenylmethyl, or salting compd. such as Na or K; R3 and R4 are same or different, and H, p-methoxybenzyl or diphenylmethyl; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, N- ethylpyridiniumylthiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, and N- methyl- tetrazolyl thiomethyl gp. This cephem compd. manufacturing method comprises A) condensing the amine compd. of (VIII) with ketone of (VII) and producing the compd of (II); and B) acylating the aminothiazol compd of (II) with cephalosphorin of (III). This cephem compd. has good antibacterial activity.
Abstract translation: 这是新头孢菌素 和其药学上可接受的式（I）盐。 在式中，R 1是H或三苯甲基，叔丁氧基羰基或甲酰基; R2氢，对甲氧基苄基，二苯基甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，对甲氧基苄基或二苯基甲基; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，N-乙基吡啶鎓硫基甲基，N-羧甲基吡啶鎓硫代甲基和N-甲基 - 四唑基硫代甲基gp。 这个cephem compd 制造方法包括：A）冷凝胺化合物。 （VIII）与（Ⅶ）的酮反应并制备（Ⅱ）化合物; 和B）用（III）的头孢菌素酰化（II）的氨基噻唑化合物。 这个cephem compd 具有良好的抗菌活性。
-
-
-
公开(公告)号：KR100267260B1
公开(公告)日：2000-11-01
申请号：KR1019980027115
申请日：1998-07-06
Applicant: 한국과학기술연구원
IPC: C07D501/24 , C07D501/20
Abstract: 본 발명은 경구 투여가 가능한 새로운 세펨 에스테르 화합물 및 이의 제조방법에 관한 것으로, 그램 양성균과 그램 음성균에 대해 광범위의 항균력을 나타내며, 특히 MRSA를 포함한 여러 내성균에 강한 항균력을 나타내는 약제학적으로 유용한 화합물이다.
(I)
일반식 (I)에 있어서, R
1 은 수소 또는 트리틸기를 표시하며, R
2 는 수소, 트리틸기, 메틸기 또는 시클로펜틸기를 표시하며, R
3 는 수소, 클로로, 브로모 또는 메톡시기를 표시하며, R
4 는 아세톡시에틸, 피발로일옥시메틸 또는 이소프로폭시카르보닐옥시에틸기를 표시한다.
-
-
-
-
-
-
-
-
-
Search Results
14
records
(took 0.02 seconds)
