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公开(公告)号：KR100629327B1
公开(公告)日：2006-09-29
申请号：KR1020040084112
申请日：2004-10-20
Applicant: 한국과학기술연구원
IPC: C07D413/14
Abstract: 본 발명은 메티실린 저항성 스태필로코커스 아우레우스(MRSA) 및 벤코마이신 저항성 엔테로콕사이(VRE) 등의 내성균주를 포함한 그람 양성균주에 대하여 우수한 항균력을 가지는 신규 구조의 트리아졸릴메틸옥사졸리디논 유도체와 이 화합물의 제조방법, 그리고 이 화합물의 항생제로서의 의약적 용도에 관한 것이다.
트리아졸릴메틸옥사졸리디논, 항생제, 내성균주, 그람 양성균주-
公开(公告)号：KR100545785B1
公开(公告)日：2006-01-24
申请号：KR1020030055099
申请日：2003-08-08
Applicant: 한국과학기술연구원
IPC: C07D401/06
Abstract: 본 발명은 피페라지닐알킬 트리아졸 화합물에 관한 것으로서, 도파민 수용체에 대한 선택적 길항작용을 가지고 있어 정신병 치료제로 유효한 다음 화학식 1로 표시되는 피페라지닐알킬 트리아졸 화합물과 이 화합물을 용액상 조합 합성법을 이용하여 제조하는 방법, 그리고 이 화합물을 유효성분으로 함유하는 약제조성물에 관한 것이다.
상기 화학식 1에서, n, R
1 , R
2 및 R
3 은 각각 발명의 상세한 설명에서 정의한 바와 같다.
피페라지닐알킬 트리아졸, 도파민 수용체, 정신병 치료제Abstract translation: 本发明的血液约烷基三唑类化合物，哌嗪烷基三唑化合物和由下式表示的化合物的哌嗪基（1）有效地作为抗精神病药物得到了多巴胺受体具有选择性拮抗溶液相组合的合成 以及含有该化合物作为有效成分的药物组合物。
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公开(公告)号：KR100490643B1
公开(公告)日：2005-05-19
申请号：KR1020020066268
申请日：2002-10-29
Applicant: 한국과학기술연구원
IPC: C07D413/10
CPC classification number: C07D413/10 , C07D413/14 , C07D417/14
Abstract: 본 발명은 아래의 화학식 1로 표시되는 메틸리덴 피페리딘일 옥사졸리딘온 유도체 화합물, 그 염 및 이들의 제조방법에 관한 것이다. 본 발명의 화합물은 메티실린 저항성 스타필로코코스 아우레우스 및 반코마이신 저항성 엔테로코코스 등과 같은 내성 균주를 포함하는 그람 양성균에 대하여 우수한 항균 활성을 나타낸다.
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公开(公告)号：KR1020050017158A
公开(公告)日：2005-02-22
申请号：KR1020030055099
申请日：2003-08-08
Applicant: 한국과학기술연구원
IPC: C07D401/06
Abstract: PURPOSE: Piperazinyl alkyl triazole compounds having selectively inhibiting activity at dopamine receptors are provided, which compounds are dopamine antagonists, so that they can be useful for treatment of psychomancy disease. CONSTITUTION: The piperazinyl alkyl triazole compounds represented by formula (1) or pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 3 or 4; R1 is optionally substituted phenyl or optionally substituted benzhydryl, in which the substituent is C1-C6 alkyl, C1-C6 alkoxy, hydroxy, C1-C6 hydroxyalkyl, aryl, heteroaryl, amino, C1-C6 alkylamino, C2-C6 alkenyl, carbonyl, C3-C9 cycloalkyl and C3-C9 hetero ring; and R2 and R3 are independently hydrogen, C1-C6 alkyl or C1-C6 alkylester. A method for preparing the piperazinyl alkyl triazole compounds of formula (1) comprises reacting azide compound of formula (2) with alkylester compound of formula (3) in solution through combinatorial synthesis, wherein the solvent is dimethylformamide or acetonitrile.
Abstract translation: 目的：提供在多巴胺受体上具有选择性抑制活性的哌嗪基烷基三唑化合物，这些化合物是多巴胺拮抗剂，因此它们可用于治疗心理病。 构成：提供由式（1）表示的哌嗪基烷基三唑化合物或其药学上可接受的盐，其中n为3或4的整数; R1是任选取代的苯基或任选取代的二苯甲基，其中取代基是C1-C6烷基，C1-C6烷氧基，羟基，C1-C6羟基烷基，芳基，杂芳基，氨基，C1-C6烷基氨基，C2-C6烯基，羰基， C3-C9环烷基和C3-C9杂环; 且R 2和R 3独立地是氢，C 1 -C 6烷基或C 1 -C 6烷基酯。 制备式（1）的哌嗪基烷基三唑化合物的方法包括通过组合合成使式（2）的叠氮化合物与式（3）的烷基酯化合物在溶液中反应，其中溶剂是二甲基甲酰胺或乙腈。
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公开(公告)号：KR100445437B1
公开(公告)日：2004-08-21
申请号：KR1020020007495
申请日：2002-02-08
Applicant: 한국과학기술연구원
IPC: C07H15/22
CPC classification number: C07H15/232
Abstract: The present invention relates to novel oxazolidinone derivatives represented as following compound I and a process for the preparation thereof. The compounds of the present invention have wide antibacterial spectrums superior antibacterial activity and low toxicity. Therefore, it can be expected to use as novel antibacterial agent. wherein, R 1 is alkylcarboxyl group or -CH 2 R 2 (wherein, R 2 is OH, argido group, -OR 3 (wherein, R 3 is C 1-4 alkyl, methansulfonyl, p-toluensulfonyl, carboxyl, C 1-4 alkylcarboxyl, C 1-4 alkylcarbonyl, benzyloxycarbonyl, or imidazolylcarbonyl), or -NHR 4 ).
Abstract translation: 本发明涉及下述化合物I所代表的新型恶唑烷酮衍生物及其制备方法。 本发明的化合物具有优异的抗菌活性和低毒性的广谱抗菌谱。 因此，可以期待用作新型抗菌剂。 其中R SUB 1 1是烷基羧基或-CH 2 SUB 2 R SUB 2 SUB（其中，R SUB 2 2 SUB是 OH，Argido基团，-OR SUB 3（其中，R SUB 3是SUB 1-4烷基，甲磺酰基，对甲苯磺酰基， 羧基，C 1-4亚烷基羧基，C 1-4亚烷基羰基，苄氧基羰基或咪唑基羰基）或-NHR SUB 4 / SUB）。
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Patent Agency Ranking
公开(公告)号：KR1020030067355A
公开(公告)日：2003-08-14
申请号：KR1020020007495
申请日：2002-02-08
Applicant: 한국과학기술연구원
IPC: C07H15/22
CPC classification number: C07H15/232
Abstract: PURPOSE: Provided is a heterodimeric conjugate of neomycin-oxazolidinone which is useful as an antiviral agent and an antibacterial agent. Also, provided are the preparation method and use thereof. CONSTITUTION: A heterodimeric conjugate of neomycin-oxazolidinone is represented by the formula(1), wherein n is an integer of 2-10 and Ac represents an acetyl group. It is characterized by specifically bonding to 16S rRNA, RRE, RNA or 23S rRNA.
Abstract translation: 目的：提供新霉素 - 恶唑烷酮的异二聚体缀合物，其可用作抗病毒剂和抗菌剂。 此外，提供其制备方法和用途。 构成：新霉素 - 恶唑烷酮的异二聚体缀合物由式（1）表示，其中n为2-10的整数，Ac为乙酰基。 其特征是特异性结合16S rRNA，RRE，RNA或23S rRNA。
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公开(公告)号：KR100394086B1
公开(公告)日：2003-08-06
申请号：KR1020000073121
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08 , C07D413/14
Abstract: The present invention relates to a novel isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, R3, R4, R5, R6, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3或D4受体具有选择性生物活性的新型异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2，R3， R4，R5，R6，X和n与说明书中的定义相同。
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公开(公告)号：KR1020030058740A
公开(公告)日：2003-07-07
申请号：KR1020010089274
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07D215/56
Abstract: PURPOSE: Quinolone derivatives and a preparation process thereof are provided, thereby cheaply preparing quinolone derivatives under mild conditions. CONSTITUTION: Quinolone derivatives are represented by the formula 6, wherein R is H, or halogen selected from Cl, F, Br and I; R1 and R2 are independently H, alkyl or OH; and Y is -Ts(tosyl), -Ms(mesyl) or -Ac(acetyl). A process for preparing the quinolone derivatives of the formula 6 comprises the steps of: reacting a compound of the formula 1 with a compound of the formula 2 in the presence of indium metal and acid to simultaneously perform allylation of aldehyde and reduction of nitro group, thereby preparing a compound of the formula 3; protecting amine group of the compound of the formula 3 to prepare a compound of the formula 4; oxidizing secondary alcohol of the compound of the formula 4 to prepare a compound of the formula 5; and cyclization of the compound of the formula 5 in the presence of organic base, wherein the oxidation of secondary alcohol uses pyridinium chlorochromate(PCC) or pyridinium dichromate(PDC) or Swern's oxidation or Dess-Martin periodinane oxidation; and the organic base is diisopropylethylamine, DBU (1,8-diazabicyclo£5.4.0|undec-7-ene), DBN (1,5-diazabicyclo£4.3.0|non-5-ene), triethylamine or pyridine.
Abstract translation: 目的：提供喹诺酮衍生物及其制备方法，从而在温和条件下廉价制备喹诺酮衍生物。 组成：喹诺酮衍生物由式6表示，其中R是H，或选自Cl，F，Br和I的卤素; R1和R2独立地为H，烷基或OH; 和Y是-T（甲苯磺酰基），-Ms（甲磺酰）或-Ac（乙酰基）。 制备式6的喹诺酮衍生物的方法包括以下步骤：在铟金属和酸存在下使式1的化合物与式2的化合物反应，以同时进行醛的还原和烯丙基的还原， 从而制备式3的化合物; 保护式3化合物的胺基以制备式4的化合物; 氧化式4化合物的仲醇制备式5的化合物; 在有机碱的存在下环化式5的化合物，其中仲醇的氧化使用氯铬酸吡啶鎓（PCC）或重铬酸吡啶鎓（PDC）或Swern的氧化或Dess-Martin氧化氧化; 有机碱是二异丙基乙胺，DBU（1,8-二氮杂双环{5.4.0 |十一-7-烯），DBN（1,5-二氮杂双环{4.3.0 |非-5-烯），三乙胺或吡啶。
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公开(公告)号：KR100387581B1
公开(公告)日：2003-06-18
申请号：KR1019990016354
申请日：1999-05-07
Applicant: 한국과학기술연구원
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：提供一种新的使用铟和锌的青蒿衍生物及其制备方法。结构式（I）代表的新型青蒿衍生物通过使式（I'）的6-氧代戊酸与式 II）或式（III）的乙炔卤化物在铟或锌存在下反应。 在式（I）中：R1是烯丙基衍生物和乙炔衍生物; R 2为氢，羧酸盐（作为无机盐的钠盐和钾盐，烷基胺盐，芳香胺盐作为有机盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基，作为 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。
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公开(公告)号：KR100380324B1
公开(公告)日：2003-04-16
申请号：KR1020000009065
申请日：2000-02-24
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided is a cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compounds represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compounds; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).
Abstract translation: 目的：提供具有广泛抗微生物活性的头孢烯衍生物。 并提供其制作方法。 构成：生产式（1）代表的头孢菌素化合物及其药学上可接受的盐。 在该式中，R1是氢或通常用于头孢菌素化合物中的胺保护基; R2是氢或肟保护基; R3是氢或氯基; R5是氢或产酯基团，产盐原子或羧基保护基团; 其中Q为氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基，C1-C4烷基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。
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