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1. 发明公开

KR1020030080509A 우레아, 티오우레아 및 설파마이드 유도체를 함유하는항균제 조성물 无效
标题翻译：含有尿素，硫脲和磺酰胺衍生物的抗菌剂组合物
公开(公告)号：KR1020030080509A
公开(公告)日：2003-10-17
申请号：KR1020020019177
申请日：2002-04-09
申请人： 주식회사 엘지생명과학
发明人： 윤주용 , 김원섭 , 이현호 , 임재홍 , 이석원 , 윤승현 , 송정욱 , 김종엽 , 최성필 , 윤하식 , 조양래
IPC分类号： A61K31/18
摘要： PURPOSE: An antibacterial agent composition containing urea, thiourea and sulfamide derivatives as an effective ingredient is provided. Therefore, it shows antimicrobial activity and an antibacterial spectrum against wide pathogens containing various Gram positive bacteria and thus is expected to be useful in the prevention and treatment of animal disease caused by bacterial infection. CONSTITUTION: The antibacterial agent composition contains urea, thiourea, sulfamide derivatives and a pharmaceutically acceptable salt, hydrate and solvate thereof represented by the formula I. In formula, each of X and Y is hydrogen, chlorine or trifluoromethyl, Z is -CO-, -CS- or -SO2-. Therefore, it exhibits excellent antibacterial activity against methicillin-resistant Staphylococcus aureus. It can be administered in the form of injectable formulations or oral formulations.
摘要翻译：目的：提供含有脲，硫脲和磺酰胺衍生物作为有效成分的抗菌剂组合物。因此，它表现出抗菌活性和对含有各种革兰氏阳性菌的广病原体的抗菌谱，因此预期可用于预防和治疗由细菌感染引起的动物疾病。构成：抗菌剂组合物含有式I所示的尿素，硫脲，磺酰胺衍生物及其药学上可接受的盐，水合物和溶剂合物。在式中，X和Y各自为氢，氯或三氟甲基，Z为-CO-， -CS-或-SO 2 - 。因此，对耐甲氧西林金黄色葡萄球菌具有优异的抗菌活性。其可以以可注射制剂或口服制剂的形式施用。

2. 发明公开

KR1020030076759A 신규 세팔로스포린 화합물 및 그의 제조 방법 无效
标题翻译： CEPHOROSPORIN化合物及其制备方法
公开(公告)号：KR1020030076759A
公开(公告)日：2003-09-29
申请号：KR1020020015248
申请日：2002-03-21
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 김근태 , 장용진 , 구기동 , 조양래 , 주형렬
IPC分类号： C07D501/56 , A61P31/04
CPC分类号： Y02P20/55
摘要： PURPOSE: Cephalosporin compounds and a preparation method thereof are provided, which compound has antimicrobial activity to the wide range of gram positive bacteria. CONSTITUTION: Cephalosporin compounds represented by formula (1), pharmaceutically acceptable nontoxic salts thereof, physiologically hydrolyzable esters, hydrides, solvates and isomers thereof are provided, wherein A is hydrogen or amino protecting group; R1 is hydrogen, C1-6 alkoxy, cyano, halogen, C3-6 cycloalkyl or C1-6 alkyl substituted by one to three of one or two nitrogen or oxygen containing C5-6 heteroaryl, C3-4 alkenyl, amino substituted or unsubstituted C3-4 alkynyl, or C3-6 cycloalkyl; R2 is hydrogen or carboxyl protecting group; V is N or C; W is C, N or N+-U, in which W is C when V is N, and W is N or N+-U when V is C; U is C1-5 alkyl; Y is hydrogen, hydroxyl, C1-6 alkyl, C1-6 alkyl substituted or unsubstituted amino, C1-6 hydroxyalkyl or C1-6 alkylthio; Z is a compound of I and J; I is S, SO or SO2; n is 1,2,3 or 4; J is C1-6 alkyl substituted or unsubstituted amino, hydroxy or substituted C1-6 alkoxy; Q is CH, CX' or N; and X' is halogen.
摘要翻译：目的：提供头孢菌素化合物及其制备方法，该化合物对革兰氏阳性细菌的广泛范围具有抗菌活性。构成：提供由式（1）表示的头孢菌素化合物，其药学上可接受的无毒盐，生理上可水解的酯，氢化物，溶剂化物和异构体，其中A是氢或氨基保护基; R 1是氢，C 1-6烷氧基，氰基，卤素，C 3-6环烷基或被1至3个一个或两个含氮或含氧的C 3-6杂芳基取代的C 1-6烷基，C 3-4链烯基，氨基取代或未取代的C 3 -4-炔基或C 3-6环烷基; R2是氢或羧基保护基; V是N或C; W为C，N或N + -U，当V为N时W为C，当V为C时，W为N或N + -U; U是C 1-5烷基; Y是氢，羟基，C 1-6烷基，C 1-6烷基取代或未取代的氨基，C 1-6羟烷基或C 1-6烷硫基; Z是I和J的化合物; 我是S，SO或SO2; n为1,2,3或4; J为C 1-6烷基取代或未取代的氨基，羟基或取代的C 1-6烷氧基; Q是CH，CX'或N; X'为卤素。

3. 发明公开

KR1020030064970A 신규 살리실아닐라이드 유도체 및 그를 함유하는 항균제조성물 无效
标题翻译：新型磺胺衍生物和抗生素组合物
公开(公告)号：KR1020030064970A
公开(公告)日：2003-08-06
申请号：KR1020020005069
申请日：2002-01-29
申请人： 주식회사 엘지생명과학
发明人： 윤승현 , 김원섭 , 이현호 , 임재홍 , 윤주용 , 김종엽 , 송정욱 , 이석원 , 최성필 , 바실리아티모프 , 윤하식 , 조양래
IPC分类号： C07D213/75
摘要： PURPOSE: Provided are novel salicylanilide derivatives represented by formula 1 which are useful as antibiotic against methicillin resistant Staphylococcus aureus(MRSA), their pharmaceutically acceptable non toxic salts, their biologically hydrolyzable ester, hydrate, solution product and their isomers. CONSTITUTION: The novel salicylanilide derivatives are represented by formula 1, wherein R is hydrogen, C1-6 alkyl, C1-3 alkoxy, acetyl or benzyl; X and Y are independently hydrogen, halogen, amino or nitro; Z is nitrogen, oxygen, sulfur, -O-(CH2)m-, -(CH2)m-O-, sulfone or sulfonamino where m is an integer of 1 to 3; A is I, V, W substituted hetero aryl containing Q2, V, W substituted bicyclic hetero aryl containing Q2 and Q3 and I, W substituted indane containing Q2, Q3, Q4 where Q1, Q2, Q3 and Q4 are each independently, one selected from N, C and S; G, J, I, V, W are each independently hydrogen, C1-6 alkyl substituted or non-substituted by halogen, C3-6 cyclo alkyl, C1-6 alkoxy, hydroxy, halogen, cyano, nitro, sulfone sulfonamide, hydroxy carbonyl, C1-6alkoxy carbonyl, C6-8 aryl, C5-8 hetero aryl substituted or non-substituted by halogen, which contains one or two atom selected from N, O and S, or C2-9 hetero aryl oxy substituted or non-substituted by halogen, which contains one or two atom selected from N, O and S. The compounds of formula 1 is synthesized by reacting compounds of formula 2 with compounds of formula 3 in a solvent in presence of base and catalyst. In the formula 2 and 3, R, X, Y, Z, A, Q1, G and J are the same as above.
摘要翻译：目的：提供由式1表示的新型水杨酰苯胺衍生物，其可用作耐甲氧西林金黄色葡萄球菌（MRSA），其药学上可接受的无毒盐，其生物可水解酯，水合物，溶液产物及其异构体的抗生素。构成：新型水杨酰苯胺衍生物由式1表示，其中R是氢，C 1-6烷基，C 1-3烷氧基，乙酰基或苄基; X和Y独立地是氢，卤素，氨基或硝基; Z是氮，氧，硫，-O-（CH 2）m - ， - （CH 2）m -O-，砜或磺氨基，其中m是1至3的整数; A是I，V，W取代的含有Q2的杂芳基，V，含有Q2和Q3的W取代的双环杂芳基和I，含有Q 2，Q 3，Q 4的W取代的二氢化茚，其中Q1，Q2，Q3和Q4各自独立地选自来自N，C和S; G，J，I，V，W各自独立地为氢，被卤素取代或不被取代的C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，羟基，卤素，氰基，硝基，砜磺酰胺，羟基羰基取代或未被卤素取代的C 1-6烷氧基羰基，C 6-8芳基，C 5-8杂芳基，其含有一个或两个选自N，O和S的原子，或C 2-9杂芳氧基取代或未取代的通过卤素，其含有一个或两个选自N，O和S的原子。式1的化合物通过在碱和催化剂存在下在溶剂中使式2化合物与式3化合物反应来合成。在式2和3中，R，X，Y，Z，A，Q 1，G和J与上述相同。

4. 发明公开

KR1020020085180A 신규 세팔로스포린계 항생제 및 이의 제조 방법 无效
标题翻译：新CEPHALOSPORIN抗生素及其制备方法
公开(公告)号：KR1020020085180A
公开(公告)日：2002-11-16
申请号：KR1020010024547
申请日：2001-05-07
申请人： 주식회사 엘지생명과학
发明人： 김근태 , 이창석 , 유은정 , 장용진 , 황상열 , 조양래
IPC分类号： C07D501/44
摘要： PURPOSE: Provided is a novel cephalosporin compound which is represented by the formula(1) and has strong antibiotic effect on MRSA. Also, provided are its preparation process and a composition of antibiotics containing the compound of the formula(1). CONSTITUTION: The cephalosporin compound of the formula(1), wherein the formula is as described in the description, its pharmaceutically acceptable nontoxic salts, its physiologically hydrolyzable ester, hydrate, solvate and its isomer display antibiotic effect on gram positive bacteria and have broad antibiotic spectrum. Thus, they are very useful for the prevention and treatment of diseases associated with infection of bacteria in a human and an animal.
摘要翻译：目的：提供由式（1）表示的新型头孢菌素化合物，对MRSA具有很强的抗生素作用。还提供其制备方法和含有式（1）化合物的抗生素的组合物。构型：式（1）的头孢菌素化合物，其中式如描述中所述，其药学上可接受的无毒盐，其生理上可水解的酯，水合物，溶剂合物及其异构体对革兰氏阳性细菌显示出抗生素效应并具有广泛的抗生素光谱。因此，它们对于预防和治疗与人和动物中的细菌感染相关的疾病非常有用。

5. 发明授权

KR100453713B1 신규 세팔로스포린 화합물 및 그의 제조 방법 失效
标题翻译： 신규세팔로스포린화합물및그의제조방법
公开(公告)号：KR100453713B1
公开(公告)日：2004-10-20
申请号：KR1020020010786
申请日：2002-02-28
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 김근태 , 장용진 , 유은정 , 조양래 , 주형렬 , 신정은 , 이선화 , 구기동
IPC分类号： C07D501/56
CPC分类号： Y02P20/55
摘要： PURPOSE: Cephalosporin compounds and a preparation process thereof are provided, which compounds have strong antimicrobial activity, especially to methicillin resistant Staphylococcus aureus(MRSA). CONSTITUTION: Cephalosporin compounds represented by the formula (1) are provided, wherein A is hydrogen or amino protecting group; R1 is hydrogen, or C1-6 alkyl, C3-4 alkynyl, C3-6 cycloalkyl or C3-6 cycloalkyl-methyl containing 1 to 3 oxygen or halogen; R2 is hydrogen or carboxyl protecting group; Ar is one compound selected from one compound containing Y, W, R3, R4, R5 and R6 or one compound containing W, Y, z, R7, R8 and R9; R3, R4 and R7 are independently hydrogen, hydroxyl, C1-6 alkyl, C1-6 substituted or unsubstituted amino, C1-6 hydroxyalkyl or C1-6 alkylthio; R6 is hydrogen, hydroxyl, C1-6 alkyl substituted or unsubstituted amino, C1-6 alkyl or a compound containing I and J; I is S, NH, CH2 or O; n is 0, 1, 2, 3 or 4; J is C1-6 alkyl substituted or unsubstituted amino, hydroxy or C1-6 alkoxy; R8 and R9 are hydrogen, C1-6 alkyl, C1-6 alkylamino, hydroxy or C1-6 alkoxy; W and Y are independently N or C, provided that R3, R5 and R8 are not present when W or Y is N; Z is CH or N; Q is CH, C-G or N; G is halogen; and ethenyl positioned at the C-3 site where heteroarylthio is substituted may be present in the form of cis or trans.
摘要翻译：目的：提供了头孢菌素化合物及其制备方法，该化合物具有很强的抗菌活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）。构成：提供由式（1）表示的头孢菌素化合物，其中A是氢或氨基保护基; R1为氢或含有1至3个氧或卤素的C1-6烷基，C3-4炔基，C3-6环烷基或C3-6环烷基 - 甲基; R2是氢或羧基保护基; Ar是选自含有Y，W，R3，R4，R5和R6的一种化合物或含有W，Y，z，R7，R8和R9的一种化合物的一种化合物; R3，R4和R7独立地为氢，羟基，C1-6烷基，C1-6取代或未取代的氨基，C1-6羟烷基或C1-6烷硫基; R6是氢，羟基，C1-6烷基取代或未取代的氨基，C1-6烷基或含有I和J的化合物; I是S，NH，CH2或O; n是0,1,2,3或4; J为C 1-6烷基取代或未取代的氨基，羟基或C 1-6烷氧基; R8和R9是氢，C1-6烷基，C1-6烷基氨基，羟基或C1-6烷氧基; W和Y独立地为N或C，条件是当W或Y是N时，R3，R5和R8不存在; Z是CH或N; Q是CH，C-G或N; G是卤素; 位于杂芳硫基被取代的C-3位的乙烯基可以以顺式或反式的形式存在。

6. 发明公开

KR1020020001542A 신규 세팔로스포린 화합물 및 그의 제조방법 失效
标题翻译：新型CEPHOROSPORIN化合物及其制备方法
公开(公告)号：KR1020020001542A
公开(公告)日：2002-01-09
申请号：KR1020010034340
申请日：2001-06-18
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 오성호 , 류은정 , 백경숙 , 윤하식 , 장용진 , 김근태 , 조양래
IPC分类号： C07D501/24
CPC分类号： C07D501/00
摘要： PURPOSE: Provided are a novel cephalosporin compound of the formula(1), its pharmaceutically acceptable nontoxic salt, physiologically hydrolyzable ester, hydrate and solvate and their enantiomer. And a pharmaceutical composition containing them and their manufacturing method are also provided. CONSTITUTION: The novel cephalosporin compound is represented by the formula(1), wherein R1 and R2 individually represent C5-6 heteroaryl including 1-2 heteroatom selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkylthio, aryl, arylthio or nitrogen atom and oxygen atom; R3 is hydrogen or carboxyl protection group; Q is sulfur, oxygen, CH2, NH or NR (wherein, R is hydrogen, C1-6 alkyl or benzyl); Z is CH or N; n is an integer of 1 or 2; Ar is heteroaryl represented by the structural formulae (wherein, X, Y, W, A, B, D, E, G and I are individually represent N or C(or CH)); R4 hydrogen or C1-C4-alkyl, or substituted or unsubstituted amino group by a substituent selected from C1-C6-alkyl and C1-C6-hydroxyalkyl; R5 an R6 are individually hydrogen, hydroxy or C1-C4-alkyl, or substituted or unsubstituted C1-C6-alkylthio or amino by a substituent selected from the group consisting of C1-C6-alkyl, C1-C6-hydroxyalkyl and C1-C6-aminoalkyl; and R7, R8, R9, R10 and R11 are individually hydrogen or C1-C6-alkyl, or substituted or unsubstituted amino by a substituent selected from the group consisting of C1-C6-alkyl, C1-C6-hydroxyalkyl and C1-C6-aminoalkyl.
摘要翻译：目的：提供式（1）的新型头孢菌素化合物，其药学上可接受的无毒盐，生理上可水解的酯，水合物和溶剂合物及其对映异构体。还提供含有它们的药物组合物及其制造方法。构成：新型头孢菌素化合物由式（1）表示，其中R 1和R 2各自表示包括选自氢，卤素，C 1-6烷基，C 1-6烷硫基，C 1-6烷基，芳基，芳硫基或氮原子和氧原子; R3是氢或羧基保护基; Q是硫，氧，CH 2，NH或NR（其中，R是氢，C 1-6烷基或苄基）; Z是CH或N; n为1或2的整数; Ar是由结构式表示的杂芳基（其中X，Y，W，A，B，D，E，G和I各自表示N或C（或CH））; R 4为氢或C 1 -C 4烷基，或被选自C 1 -C 6烷基和C 1 -C 6羟基烷基的取代基取代或未取代的氨基; R5和R6分别独立地为氢，羟基或C1-C4-烷基，或者取代或未取代的C1-C6-烷硫基或氨基，所述取代基选自C1-C6-烷基，C1-C6-羟基烷基和C1-C6 氨基烷基; 并且R 7，R 8，R 9，R 10和R 11各自独立地为氢或C 1 -C 6烷基，或者被选自C 1 -C 6烷基，C 1 -C 6羟基烷基和C 1 -C 6 - 羟基烷基的取代基取代或未取代的氨基，氨基。

7. 发明公开

KR1020030071200A 신규 세팔로스포린 화합물 및 그의 제조 방법 失效
标题翻译： CEPHOROSPORIN化合物及其制备方法
公开(公告)号：KR1020030071200A
公开(公告)日：2003-09-03
申请号：KR1020020010786
申请日：2002-02-28
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 김근태 , 장용진 , 유은정 , 조양래 , 주형렬 , 신정은 , 이선화 , 구기동
IPC分类号： C07D501/56
CPC分类号： Y02P20/55
摘要： PURPOSE: Cephalosporin compounds and a preparation process thereof are provided, which compounds have strong antimicrobial activity, especially to methicillin resistant Staphylococcus aureus(MRSA). CONSTITUTION: Cephalosporin compounds represented by the formula (1) are provided, wherein A is hydrogen or amino protecting group; R1 is hydrogen, or C1-6 alkyl, C3-4 alkynyl, C3-6 cycloalkyl or C3-6 cycloalkyl-methyl containing 1 to 3 oxygen or halogen; R2 is hydrogen or carboxyl protecting group; Ar is one compound selected from one compound containing Y, W, R3, R4, R5 and R6 or one compound containing W, Y, z, R7, R8 and R9; R3, R4 and R7 are independently hydrogen, hydroxyl, C1-6 alkyl, C1-6 substituted or unsubstituted amino, C1-6 hydroxyalkyl or C1-6 alkylthio; R6 is hydrogen, hydroxyl, C1-6 alkyl substituted or unsubstituted amino, C1-6 alkyl or a compound containing I and J; I is S, NH, CH2 or O; n is 0, 1, 2, 3 or 4; J is C1-6 alkyl substituted or unsubstituted amino, hydroxy or C1-6 alkoxy; R8 and R9 are hydrogen, C1-6 alkyl, C1-6 alkylamino, hydroxy or C1-6 alkoxy; W and Y are independently N or C, provided that R3, R5 and R8 are not present when W or Y is N; Z is CH or N; Q is CH, C-G or N; G is halogen; and ethenyl positioned at the C-3 site where heteroarylthio is substituted may be present in the form of cis or trans.
摘要翻译：目的：提供头孢菌素化合物及其制备方法，该化合物具有很强的抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）。构成：提供由式（1）表示的头孢菌素化合物，其中A为氢或氨基保护基; R1是氢或C1-6烷基，C3-4炔基，C3-6环烷基或含1-3个氧或卤素的C3-6环烷基 - 甲基; R2是氢或羧基保护基; Ar是选自含有Y，W，R3，R4，R5和R6的一种化合物或含有W，Y，z，R7，R8和R9的一种化合物的一种化合物; R3，R4和R7独立地是氢，羟基，C1-6烷基，C1-6取代或未取代的氨基，C1-6羟烷基或C1-6烷硫基; R6是氢，羟基，C1-6烷基取代或未取代的氨基，C1-6烷基或含I和J的化合物; I是S，NH，CH 2或O; n为0,1,2,3或4; J为C 1-6烷基取代或未取代的氨基，羟基或C 1-6烷氧基; R8和R9是氢，C1-6烷基，C1-6烷基氨基，羟基或C1-6烷氧基; W和Y独立地为N或C，条件是当W或Y为N时不存在R3，R5和R8; Z是CH或N; Q是CH，C-G或N; G是卤素; 位于杂芳硫基被取代的C-3位点的乙烯基可以以顺式或反式的形式存在。

8. 发明授权

KR100437277B1 신규 세팔로스포린 화합물 및 그의 제조방법 失效
标题翻译： 신규세팔로스포린화합물및그의제조방법
公开(公告)号：KR100437277B1
公开(公告)日：2004-06-23
申请号：KR1020010034340
申请日：2001-06-18
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 오성호 , 류은정 , 백경숙 , 윤하식 , 장용진 , 김근태 , 조양래
IPC分类号： C07D501/24
CPC分类号： C07D501/00
摘要： The present invention relates to a novel cephalosporin compound in which thiomethylthio chain is introduced into C-3 position of cephem ring and pharmaceutically acceptable non-toxic salt, physiologically hydrolysable ester, hydrate, solvate or isomer thereof. The present invention also relates to a pharmaceutical composition containing the compound and to a process for preparing the compound.
摘要翻译：本发明涉及一种新的头孢菌素化合物，其中硫代甲硫基链被引入到头孢烯环的C-3位上，以及药学上可接受的无毒盐，生理上可水解的酯，水合物，溶剂化物或异构体。本发明还涉及含有该化合物的药物组合物以及制备该化合物的方法。

9. 发明公开

KR1020030076760A 신규 세팔로스포린 화합물 및 그의 제조 방법 无效
标题翻译： CEPHOROSPORIN化合物及其制备方法
公开(公告)号：KR1020030076760A
公开(公告)日：2003-09-29
申请号：KR1020020015249
申请日：2002-03-21
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 김근태 , 장용진 , 구기동 , 조양래 , 주형렬
IPC分类号： C07D501/56
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided are cephalosporin compounds and a preparation method thereof, which compounds have antimicrobial activity to the wide range of gram positive bacteria. CONSTITUTION: Cephalosporin compounds represented by formula (1), pharmaceutically acceptable nontoxic salts thereof, physiologically hydrolyzable esters, hydrides, solvates and isomers thereof are provided, wherein A is hydrogen or amino protecting group; R1 is hydrogen, one to three oxygen or halogen C1-6 alkyl, C3-4 alkenyl, one nitrogen containing C3-4 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkyl-methyl or one to two nitrogen or oxygen containing C5-6 heteroarylmethyl; R2 is hydrogen or carboxyl protecting group; V is N or C; W is C, N or N+-U, in which W is C when V is N, and W is N or N+-U when V is C; U is C1-5 alkyl or amino; Y is hydrogen, hydroxyl, C1-6 alkyl, C1-6 alkyl substituted or unsubstituted amino, C1-6 hydroxyalkyl or C1-6 alkylthio; Z is a compound of I and J; I is S, SO or SO2; n is 1, 2, 3 or 4; J is C1-6 alkyl substituted or unsubstituted amino, hydroxy or substituted C1-6 alkoxy; Q is CH, CX' or N; and X' is halogen.
摘要翻译：目的：提供头孢菌素化合物及其制备方法，该化合物对革兰氏阳性细菌的广泛范围具有抗微生物活性。构成：提供由式（1）表示的头孢菌素化合物，其药学上可接受的无毒盐，生理上可水解的酯，氢化物，溶剂化物和异构体，其中A是氢或氨基保护基; R1是氢，一至三个氧或卤素C1-6烷基，C3-4烯基，一个含氮的C3-4炔基，C3-6环烷基，C3-6环烷基 - 甲基或一至二个含有或含有C 5-6的氮或氧杂芳; R2是氢或羧基保护基; V是N或C; W为C，N或N + -U，当V为N时W为C，当V为C时，W为N或N + -U; U是C 1-5烷基或氨基; Y是氢，羟基，C 1-6烷基，C 1-6烷基取代或未取代的氨基，C 1-6羟烷基或C 1-6烷硫基; Z是I和J的化合物; 我是S，SO或SO2; n为1,2,3或4; J为C 1-6烷基取代或未取代的氨基，羟基或取代的C 1-6烷氧基; Q是CH，CX'或N; X'为卤素。

10. 发明公开

KR1020030071311A 신규 세팔로스포린 화합물 및 그의 제조방법 无效
标题翻译： CEPHOROSPORIN化合物及其制备方法
公开(公告)号：KR1020030071311A
公开(公告)日：2003-09-03
申请号：KR1020020010960
申请日：2002-02-28
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 김근태 , 장용진 , 유은정 , 조양래 , 주형렬
IPC分类号： C07D501/36
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided are cephalosporin compounds and a preparation process thereof, which compounds have strong antimicrobial activity, especially to methicillin resistant Staphylococcus aureus(MRSA). CONSTITUTION: Cephalosporin compounds represented by the formula (1) are provided, wherein R1 and R2 are independently hydrogen, halogen, C1-6 alkyl, C1-6 alkylthio, aryl, arylthio or C5-6 heteroaryl containing 1 to 2 hetero atoms selected from nitrogen and oxygen; R3 is hydrogen or carboxy protecting group; R4, R5 and R6 are independently hydrogen, hydroxy, C1-6 alkyl, C1-6 alkyloxy or C1-6 alkylamino; R7 is hydrogen, hydroxy, amino, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylamino, or amino or hydroxy substituted or unsubstituted C1-6 alkylthio; Q is sulfur, oxygen or carbon; W and Y are independently C or N, provided that R4 and R6 are not present when W or Y is N; and olefin positioned at the C-3 site where heteroarylthio is substituted comprises cis or trans forms. A process for preparing the cephalosporin compounds of the formula (1) comprises the steps of: activating a compound of the formula (6) or salts thereof with an acylating agent; reacting the activated compound of the formula (6) with a compound of formula (5) to prepare a compound of the formula (11); and reducing the compound of the formula (11) from S to oxide, wherein p is 0 or 1; and a double bond positioned at the C-3 site comprises trans and cis forms.
摘要翻译：目的：提供头孢菌素化合物及其制备方法，该化合物具有很强的抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）。构成：提供由式（1）表示的头孢菌素化合物，其中R 1和R 2独立地为氢，卤素，C 1-6烷基，C 1-6烷硫基，芳基，芳硫基或C 1-6杂芳基，其含有1至2个选自氮和氧; R3是氢或羧基保护基; R4，R5和R6独立地是氢，羟基，C1-6烷基，C1-6烷氧基或C1-6烷基氨基; R7是氢，羟基，氨基，C1-6烷基，C1-6烷氧基，C1-6烷基氨基或氨基或羟基取代或未取代的C1-6烷硫基; Q是硫，氧或碳; W和Y独立地为C或N，条件是当W或Y为N时不存在R4和R6; 并且位于被取代杂芳硫基的C-3位置的烯烃包括顺式或反式。制备式（1）的头孢菌素化合物的方法包括以下步骤：用酰化剂活化式（6）化合物或其盐; 使式（6）的活化化合物与式（5）化合物反应以制备式（11）化合物; 并将式（11）的化合物从S还原成氧化物，其中p为0或1; 并且位于C-3位点的双键包含反式和顺式形式。

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