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公开(公告)号：KR1019910009334B1
公开(公告)日：1991-11-11
申请号：KR1019890016019
申请日：1989-11-06
Applicant: 한국화학연구원
IPC: C07D498/06
Abstract: Benzoxazine carboxylic acid derivs. of formula (I) are new. In (I), R1-R5 each = H or lower alkyl; R6 and R7 each = H or C1-3 linear or cyclic lower alkyl, or substd. lower alkyl; the methyl gp. in the 3-position may be (S)-form or racemic form. Also claimed is the prepn. of (I) which comprises condensing a corresp. benzoxazine carboxylic acid deriv. of formula (II) with a 2,5- dihydropyrrole deriv. of formula (III) in the presence or absence of a solvent. Cpds. (I) have a good antibacterial activity and broad spectrum antibacterial action against Gram positive and Gram negative bacteria.
Abstract translation: 苯并恶嗪羧酸衍生物。 式（I）的化合物是新的。 在（I）中，R 1 -R 5各自为H或低级烷基; R6和R7各自为H或C1-3直链或环状低级烷基，或被取代。 低级烷基 甲基gp。 在3位可以是（S）形式或外消旋形式。 还声称是prepn。 （I），其包括冷凝对应物。 苯并恶嗪羧酸衍生物。 式（II）与2,5-二氢吡咯衍生物反应。 在式（III）的存在或不存在下进行。 CPDS。 （I）对革兰氏阳性和革兰氏阴性菌具有良好的抗菌活性和广谱抗菌作用。
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公开(公告)号：KR1019910009333B1
公开(公告)日：1991-11-11
申请号：KR1019890015203
申请日：1989-10-23
Applicant: 한국화학연구원
IPC: C07D498/04 , C07D498/06
CPC classification number: C07D519/00
Abstract: Quinolone derivs. of formula (I) and, when R1 is H, their acid addn. salts and hydrates are new. Z = halo or NH2; R1 = H or a cation. R2 = H, lower alkyl or formyl; m = 1-3; n = 1 or 2. Also claimed is the prepn. of (I) which comprises e.g. condensing corresp. quinolone deriv. with a leaving gp. in the 10-position with a diazabicycloamine. (I) may be orally or parenterally administered at a dose of 0.1-1.5 (0.2-0.8) g/kay to a 60 kg adult. Cpds. (I) are used for the treatment of bacterial infections. (I) have a better and wider range of activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) also have a good antibacterial activity against methicillin resistant bacteria.
Abstract translation: 喹诺酮衍生物。 的式（I）化合物，当R 1为H时，其酸加成。 盐和水合物是新的。 Z =卤素或NH 2; R1 = H或阳离子。 R2 = H，低级烷基或甲酰基; m = 1-3; n = 1或2.还要求是prepn。 的（I），其包含例如 冷凝对应 喹诺酮衍生物 离开gp。 在10位与二氮杂双环胺。 （I）可以以0.1-1.5（0.2-0.8）g / kay的剂量口服或非肠道给药至60kg成人。 CPDS。 （I）用于治疗细菌感染。 （I）比现有的喹诺酮抗菌剂具有更好和更广泛的抗革兰氏阳性和革兰氏阴性菌的活性，特别是。 诺氟沙星，环丙沙星和氧氟沙星。 （I）对耐甲氧西林细菌也具有良好的抗菌活性。
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公开(公告)号：KR100044555B1
公开(公告)日：1991-09-25
申请号：KR1019890003658
申请日：1989-03-23
Applicant: 한국화학연구원
IPC: C07D207/22 , C07D207/20
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公开(公告)号：KR1019900005955B1
公开(公告)日：1990-08-18
申请号：KR1019880007217
申请日：1988-06-16
Applicant: 한국화학연구원
IPC: C07D417/04
Abstract: Benzothiazine derivs. of formula (I) are prepd. by (a) reacting a cpd. of formula (II) with mCPBA to obtain sulfoxide cpds. of formula (III); (b) hydrolyzing (III) to obtain carboxylic acid cpds. of formula (IV); and (c) forming amine cpds. of pyrrolidine or piperazine of formula (I) by the neucleophyllic substitution reaction. In the formulas, R= piperazinyl opt. substd. by C1-6 alkyl; R'= C1-3 alkyl (I) have antibacterial activity.
Abstract translation: 苯并噻嗪衍生物 式（I）的化合物是制备的。 通过（a）反应cpd。 的式（II）与mCPBA反应，得到亚砜cpds。 的式（III）; （b）水解（III）以获得羧酸cpds。 的式（IV）化合物; 和（c）形成胺cpds。 的式（I）的吡咯烷或哌嗪通过核碱基取代反应。 在式中，R =哌嗪基。 substd。 通过C 1-6烷基; R'= C 1-3烷基（I）具有抗菌活性。
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Patent Agency Ranking
公开(公告)号：KR1020130054211A
公开(公告)日：2013-05-24
申请号：KR1020120129805
申请日：2012-11-15
Applicant: 한국화학연구원
IPC: C07D471/04 , A61K31/437 , A61P31/12
CPC classification number: C07D471/04
Abstract: PURPOSE: A compound, or a pharmaceutically acceptable salt, a hydrate, a solvate, or an isomer thereof is provided to ensure high selectivity and physiological activity to HIV-1 and low toxicity, and to treat HIV infection. CONSTITUTION: An antiviral composition contains a compound of chemical formula I, or a racemic body, a stereomer, or a pharmaceutically acceptable salt thereof. A method for preparing the compound of chemical formula I comprises: a step of reacting a compound of chemical formula II with a compound of chemical formula III and preparing a compound of chemical formula IV; and a step of hydrolyzing the compound of chemical formula IV.
Abstract translation: 目的：提供化合物或其药学上可接受的盐，水合物，溶剂化物或其异构体，以确保对HIV-1的高选择性和生理活性，低毒性，以及治疗HIV感染。 构成：抗病毒组合物含有化学式I的化合物或外消旋体，立体异构体或其药学上可接受的盐。 制备化学式I化合物的方法包括：使化学式II化合物与化学式III化合物反应并制备化学式IV化合物的步骤; 以及水解化学式IV化合物的步骤。
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公开(公告)号：KR1020030023968A
公开(公告)日：2003-03-26
申请号：KR1020010056740
申请日：2001-09-14
Applicant: 한국화학연구원
IPC: C07D477/14
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided are carbapenem derivatives represented by formula(1) and a preparation method thereof. The carbapenem derivatives have antibacterial activity against the resistant strains such as methicillin resistant Staphylococcus aureus(MRSA) and resistant strain against Ofloxacin. CONSTITUTION: The method of preparation comprises: reacting a compound of formula(2) with a compound of formula(3) to make an ester derivatives of carbapenem represented by formula(4); and de-protecting carboxy group and hydroxy group. In formula(1), X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group, or C1-2 alkoxy group; M is hydrogen atom or a pair ion forming a pharmaceutically allowable salt. In formula(2,3 and 4), R1 is hydrogen atom or hydroxy protecting group; R2 is carboxy protecting group; X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group.
Abstract translation: 目的：提供式（1）表示的碳青霉烯衍生物及其制备方法。 碳青霉烯衍生物对抗性菌株如耐甲氧西林金黄色葡萄球菌（MRSA）和耐氧沙星的抗性菌株具有抗菌活性。 构成：制备方法包括：使式（2）化合物与式（3）化合物反应，制得由式（4）表示的碳青霉烯的酯衍生物; 并脱保护羧基和羟基。 在式（1）中，X是S或O原子; Y是苯基或C1-2烷氧基中某一位置上的氢或卤素原子; M是氢原子或形成药学上允许的盐的成对离子。 在式（2,3和4）中，R 1是氢原子或羟基保护基; R2是羧基保护基; X是S或O原子; Y是苯基中某一位置的氢或卤素原子。
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公开(公告)号：KR1020020006889A
公开(公告)日：2002-01-26
申请号：KR1020000040396
申请日：2000-07-14
Applicant: 한국화학연구원
IPC: C07D205/08
Abstract: PURPOSE: Provided are 2-arylethenyl carbapenem derivative of the formula(1) and its pharmaceutically acceptable salt which have therapeutic effect in methicillin resistant staphylococcus aureus(MRSA) infection. And its manufacturing method and an antibacterial composition containing it as an active ingredient are also provided. CONSTITUTION: 2-arylethenyl carbapenem derivative is represented by the formula(1), wherein R is halogen, nitro, hydroxy or cyano substituted phenyl or fused aryl group; or halogen or C1-3 alkyl group substituted monocyclic, bicyclic or tricyclic 5 or 6 membered hetero aryl group containing at least one of O, S or N atom; and M is hydrogen or zwitterion forming pharmaceutically acceptable salts.
Abstract translation: 目的：提供式（1）的2-亚乙烯基碳青霉烯衍生物及其药用盐，其在耐甲氧西林金黄色葡萄球菌（MRSA）感染中具有治疗作用。 还提供其制造方法和含有它作为活性成分的抗菌组合物。 构成：2-亚乙烯基碳代青霉烯衍生物由式（1）表示，其中R是卤素，硝基，羟基或氰基取代的苯基或稠合芳基; 或含有O，S或N原子中的至少一个的卤素或C 1-3烷基取代的单环，双环或三环5或6元杂芳基; M是氢或两性离子形成药学上可接受的盐。
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公开(公告)号：KR100231498B1
公开(公告)日：1999-11-15
申请号：KR1019970060989
申请日：1997-11-19
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: 본 발명은 그람 양성균은 물론 녹농균을 제외한 그람 음성균에 대하여 우수한 항균 작용을 나타내는, 하기 화학식 1a 또는 화학식 1b로 표시되는 카르바페넴 유도체 화합물, 이의 제조 방법 및 이를 포함하는 약제학적 조성물을 제공한다.
식 중, R은 수소, 카르복실 음이온, 카르복실 보호기, 또는 제약학상 허용가능한 무기 또는 유기염이고, R
1 은 수소 또는 히드록시 보호기이며, R
2 는 C
1 내지 C
5 의 시클릭 또는 비시클릭 저급 알킬기 또는 방향족 알킬기이거나, 또는 질소, 황 및 산소로 이루어지는 군으로부터 선택된 1개 이상의 헤테로 원자를 함유하는 모노 또는 비시클릭, 포화 또는 불포화 고리인, 임의 치환된 헤테로시클릭 라디칼이고, R
3 은 수소, C
1 내지 C
5 의 시클릭 또는 비시클릭 저급 알킬기, 카르바모일기 또는 아세틸기이다.-
公开(公告)号：KR100229817B1
公开(公告)日：1999-11-15
申请号：KR1019970025647
申请日：1997-06-19
Applicant: 한국화학연구원
IPC: C07D499/87
Abstract: 본 발명은 하기 일반식(I)의 페넴 유도체 및 그의 약제학적으로 허용되는 염, 제조방법 및 이를 활성 성분으로 함유하는 항생제 조성물에 관한 것으로, 일반식(I)의 화합물은 경구흡수도가 높고, 항균력이 우수하여 항생제로 유용하다:
(I)
상기식에서,
R
1 은 수소, 카르복실기, 알릴, 카르복실 보호기 또는 약제학적으로 허용가능한 무기 또는 유기염이고;
R
2 는 C
1- C
6 의 알킬기, C
3 -C
6 사이클릭 알킬기, C
3- C
10 의 방향족 알킬기 또는 C
2 -C
6 의 알케닐기이고;
R
3 는 C
1- C
6 의 알킬기, C
3 -C
6 사이클릭 알킬기, 카바모일기 또는 아세틸기이다.
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