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公开(公告)号：KR100329808B1
公开(公告)日：2002-03-25
申请号：KR1020000001703
申请日：2000-01-14
Applicant: 한국과학기술연구원
IPC: C07D277/34
Abstract: 본 발명은 화학식 1을 갖는 2-펜아실리덴-3,5-알킬치환된-1,3-티아졸리딘-4-온을 효율적으로 제조하는 방법에 관한 것으로서, 그 반응은 반응식 1과 같다.
본 발명의 제조방법에 따르면, 상기 화학식 1의 화합물을 한 반응 용기 내에서, 그리고 보다 용이한 반응 조건 하에서 얻을 수 있다.-
公开(公告)号：KR1019990068967A
公开(公告)日：1999-09-06
申请号：KR1019980002915
申请日：1998-02-03
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: 본 발명은 신규한 일반식(I)로 표시되는 (E)-프로페닐 4급 암모늄 세펨 화합물과 그의 약제학적으로 허용되는 염 및 이의 제조 방법에 관한 것이다. 본 발명에서 제조된 화합물들은 그람 양성균이나 그람 음성균에 대해 우수한 항균력을 나타내므로 세팔로스포린 계열 의약품에 유용하게 사용될 수 있다.
일반식(I)에 있어서, R
1 은 수소 또는 아민보호기를 표시하며, R
2 는 수소, 메틸, 2-플루오르에틸 또는 옥심보호기를 표시하며, R
3 는 수소, 카르복실산염 형성기 또는 카르복실 보호기를 표시하며, R
4 는 메톡시, 치환체를 가진 카바모일, 옥사디아졸 또는 트리아졸로 표시되는 5환 헤테로고리 치환체를 표시하며, n은 1 또는 2를 표시한다.-
公开(公告)号：KR1019950032220A
公开(公告)日：1995-12-20
申请号：KR1019950012400
申请日：1995-05-18
Applicant: 한국과학기술연구원
IPC: C07D501/46
Abstract: 본 발명은 그람 음성균 및 그람 양성균에 대해 폭넓은 항균력을 나타내며 여러 내성균에 대해서도 강한 항균력을 나타내는 일반식(I)로 표시되는 새로운 세팔로스포린 화합물, 이의 수화물, 이의 약리학적으로 허용가능한 염, 이의 제조방법 및 이의 제조에 사용되는 중간체 화합물에 관한것이다.
상기 일반식(I)에서 A, R
1 및 R
2 는 발명의 상세한 설명에서 정의한 바와 같다.-
公开(公告)号：KR1019880002313B1
公开(公告)日：1988-10-22
申请号：KR1019860002080
申请日：1986-03-20
Applicant: 한국과학기술연구원 , 대한민국(농촌진흥청장)
IPC: C12N1/00
Abstract: Root-nodle bacteria inocula for leguminous plants were prepd. Thus, Rhizobium japonicum KLTL 8182p was cultured on the medium contg. 10 mannitol. 1.0 yeast extract, 0.2 MgSO4, 0.2 NaCl, and 0.2g K2HPO4 per liter of water for 3 days at 28↿C. 100 peat, or 100 lignite, or 100 zelite, or 100 g leaf mold was pulverized to > 100 mesh particles, autoclaved for 3 hr at 121↿C,and mixed with the above cultures (40ml), 0.5 g Me, and 5 g B. The mixt. was packed into a polyethylenevinyl bag, sealed, and incubated for 2 weeks at room temp. to provide inocula availible for 1000m2 soils.
Abstract translation: 豆科植物根瘤细菌接种物 因此，日本根瘤菌KLTL 8182p在培养基上培养。 10甘露醇。 1.0酵母提取物，0.2 MgSO 4，0.2 NaCl和0.2g K 2 HPO 4 /升水，在28℃下3天。 将100个泥炭或100个褐煤或100个zelite或100g叶霉粉碎至> 100目的颗粒，在121℃下高压灭菌3小时，并与上述培养物（40ml），0.5g Me和5g 混合 装入聚乙烯乙烯基袋中，密封，并在室温下孵育2周。 提供可用于1000m2土壤的接种物。
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公开(公告)号：KR102168095B1
公开(公告)日：2020-10-20
申请号：KR1020190067418
申请日：2019-06-07
Applicant: 한국과학기술연구원 , 가천대학교 산학협력단
IPC: A61K36/282 , A61K8/9789 , A23L33/105 , A61P17/00 , A61Q19/00 , A61K31/365 , A61K31/198 , A61K31/201
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Patent Agency Ranking
公开(公告)号：KR1020100087496A
公开(公告)日：2010-08-05
申请号：KR1020090006515
申请日：2009-01-28
Applicant: 한국과학기술연구원
Abstract: PURPOSE: A marine bacteria strain KME-002 isolated from sea squirt is provided to produce 7-ketodexoycholic acid and 3-oxodeoxycholic acid. CONSTITUTION: A novel bacteria strain KME-002 is deposited as a number of KFCC11437P. The strain has 16S rDNA nucleotide sequence. The strain produces 7-ketodexoycholic acid of chemical formula 1 and 3-oxodeoxycholic acid of chemical formula 2. A method for preparing 7-ketodexoycholic acid and 3-oxodeoxycholic acid comprises: a step of inoculating bacteria strain KME-002 to liquid medium and culturing; a step of adding adsorption resin and organic solvent to culture medium or directly adding organic solvent to culture medium; a step of decompression-drying the extract and performing column chromatography to obtain a fraction; and a step of performing additional column chromatography from the fraction to isolate or purify 7-ketodexoycholic acid and 3-oxodeoxycholic acid.
Abstract translation: 目的：提供从海上喷雾分离的海洋细菌菌株KME-002，以产生7-酮异精氨酸和3-氧代脱氧胆酸。 构成：一种新型细菌菌株KME-002作为一批KFCC11437P保藏。 该菌株具有16S rDNA核苷酸序列。 该菌株产生化学式1的3-酮基脱氧胆酸和化学式2的3-氧代脱氧胆酸。一种制备7-酮异精氨酸和3-氧代脱氧胆酸的方法，包括：将细菌菌株KME-002接种于液体培养基中培养 ; 向培养基中加入吸附树脂和有机溶剂或直接向培养基中加入有机溶剂的步骤; 减压干燥提取物并进行柱色谱以获得级分的步骤; 以及从级分进行附加的柱色谱以分离或纯化7-酮基脱氧胆酸和3-氧代脱氧胆酸的步骤。
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公开(公告)号：KR100377788B1
公开(公告)日：2003-03-26
申请号：KR1020000086255
申请日：2000-12-29
IPC: C07D471/04
Abstract: PURPOSE: Provided is a novel pyridopyrimidine derivative inhibiting phosphodiesterase IV activity, and TNF generation and its side effects. Also, provided are its manufacturing method and a pharmaceutical composition containing it. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is aryl, substituted aryl(wherein, a substitution group can be C1-3 lower alkyl group, C1-3 lower alkoxy group, halogen, aryl, or substituted aryl), aryl oxy, aryl amino, aryl substituted lower alkyl, pyridine, alkyl substituted pyridine, halogen substituted pyridine, C1-3 lower alkyl ester, substituted hetero cycle, hetero cycle oxy, hetero cycle, or amino hetero cycle lower alkyl; R2 hydrogen, C3-7 lower alkyl oxy, phenyl, benzyl, or substituted phenyl(wherein, a substitution group can be cyano, halogen, carboxy alkyl, methyl, trihalogenated methyl, or alkyl oxy, and substitution site can be ortho-, para-, or meta- site), alkyl oxy, C3-7 lower alkyl oxy ethyl, benzyl oxy, benzyl oxy ethyl, phenyl oxy ethyl, carboxy alkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.
Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生及其副作用的新型吡啶并嘧啶衍生物。 另外，提供了其制造方法和含有它的药物组合物。 构成：新的吡啶并嘧啶衍生物由式（1）表示，其中R1为芳基，取代的芳基（其中，取代基可以为C1-3低级烷基，C1-3低级烷氧基，卤素，芳基或取代的 芳基氧基，芳基氨基，芳基取代的低级烷基，吡啶，烷基取代的吡啶，卤素取代的吡啶，C 1-3低级烷基酯，取代的杂环，杂环氧基，杂环或氨基杂环低级烷基; 苯基，苄基或取代的苯基（其中，取代基可以是氰基，卤素，羧基烷基，甲基，三卤代甲基或烷基氧基，取代位置可以是邻位，对位 - 或间位），烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R4是氢或甲基，条件是R2和R3不相同。
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公开(公告)号：KR1020020058218A
公开(公告)日：2002-07-12
申请号：KR1020000086255
申请日：2000-12-29
IPC: C07D471/04
Abstract: PURPOSE: Provided is a novel pyridopyrimidine derivative inhibiting phosphodiesterase IV activity, and TNF generation and its side effects. Also, provided are its manufacturing method and a pharmaceutical composition containing it. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is aryl, substituted aryl(wherein, a substitution group can be C1-3 lower alkyl group, C1-3 lower alkoxy group, halogen, aryl, or substituted aryl), aryl oxy, aryl amino, aryl substituted lower alkyl, pyridine, alkyl substituted pyridine, halogen substituted pyridine, C1-3 lower alkyl ester, substituted hetero cycle, hetero cycle oxy, hetero cycle, or amino hetero cycle lower alkyl; R2 hydrogen, C3-7 lower alkyl oxy, phenyl, benzyl, or substituted phenyl(wherein, a substitution group can be cyano, halogen, carboxy alkyl, methyl, trihalogenated methyl, or alkyl oxy, and substitution site can be ortho-, para-, or meta- site), alkyl oxy, C3-7 lower alkyl oxy ethyl, benzyl oxy, benzyl oxy ethyl, phenyl oxy ethyl, carboxy alkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.
Abstract translation: 目的：提供抑制磷酸二酯酶IV活性的新型吡啶并嘧啶衍生物，以及TNF的产生及其副作用。 此外，其制造方法和含有它的药物组合物。 构成：新颖的吡啶并嘧啶衍生物由式（1）表示，其中R1为芳基，取代芳基（其中取代基可为C1-3低级烷基，C1-3低级烷氧基，卤素，芳基或取代基 芳基氧基，芳基氨基，芳基取代的低级烷基，吡啶，烷基取代的吡啶，卤素取代的吡啶，C1-3低级烷基酯，取代的杂环，杂环氧，杂环或氨基杂环低级烷基; R 2氢，C 3-7低级烷基氧基，苯基，苄基或取代的苯基（其中，取代基可以是氰基，卤素，羧基烷基，甲基，三卤代甲基或烷氧基，取代位点可以是邻位，对位 - 或间位），烷基氧基，C 3-7低级烷基氧基乙基，苄基氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R 4是氢或甲基，条件是R 2和R 3不相同。
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公开(公告)号：KR1020010075920A
公开(公告)日：2001-08-11
申请号：KR1020000002868
申请日：2000-01-21
Applicant: 한국과학기술연구원
IPC: C07D413/08
Abstract: PURPOSE: Provided is a novel oxazolidinone derivative which includes a thiophene ring and has antibacterial effects on gram positive bacterial. Also, its pharmaceutically acceptable salt and hydrate are provided. CONSTITUTION: A novel oxazolidinone derivative or its pharmaceutically acceptable salt and hydrates includes a thiophene ring and is represented by the formula (1). in the formula, R1 is a phenyl group or halogen, a phenyl group of which an alkoxy group is substituted; R2 is a saturated alkyl group of C1-4 or an alkyl group of C1-3 of which one hydrogen is substituted with a phenyl group, a cycloalkyl group of C3-8, a benzyl group of which an aryl group is substituted with an alkyl group of C1-3; and R3 is hydrogen or fluorine. The compound of the formula (1) is prepared by reacting a compound of the formula (2) with a compound of formula (3).
Abstract translation: 目的：提供一种新颖的恶唑烷酮衍生物，其包含噻吩环，对革兰氏阳性细菌具有抗菌作用。 此外，提供其药学上可接受的盐和水合物。 构成：一种新的恶唑烷酮衍生物或其药学上可接受的盐和水合物包括噻吩环并由式（1）表示。 在该式中，R 1是苯基或卤素，其中烷氧基被取代的苯基; R2是C1-4的饱和烷基或其一个氢被苯基取代的C1-3烷基，C3-8的环烷基，其中一个芳基被烷基取代的苄基 C1-3组; R3是氢或氟。 式（1）的化合物通过使式（2）的化合物与式（3）的化合物反应来制备。
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公开(公告)号：KR1020010073620A
公开(公告)日：2001-08-01
申请号：KR1020000002382
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: A pyrazolopyridine substituted cephalosporin compound is provided, which have the wide antimicrobial activity for gram positive and gram negative bacteria. And a producing method thereof is also provided. CONSTITUTION: The pyrazolopyridine substituted cephalosporin compound is represented by formula (1), in which R1 is hydrogen, C1 to C3 alkyl, C1 to C3 alkyl containing hydroxy, C1 to C3 alkyl containing amine; and R2 is hydrogen, amino, amino protected by amine protecting groups, carboxy or its inorganic salts, carbarmoyl, C1 to C3 alkyl substituted carbarmoyl, C1 to C3 alkyl containing hydroxy, and C1 to C3 alkyl esterified carboxy. The method for producing the pyrazolopyridine substituted cephalosporin compounds comprises the steps of: reacting the compounds of formula (2) and (3); and deprotecting R3 and R4, in which R3 is amine protecting groups, R4 is carboxylic acid protecting groups; and Y is halogen or acetoxy.
Abstract translation: 目的：提供吡唑并吡啶取代的头孢菌素化合物，对革兰氏阳性菌和革兰氏阴性菌具有广泛的抗菌活性。 并提供其制造方法。 构成：吡唑并吡啶取代的头孢菌素化合物由式（1）表示，其中R1为氢，C1至C3烷基，含羟基的C1至C3烷基，含C1至C3烷基的胺; 羧基或其无机盐，氨甲酰基，C 1至C 3烷基取代的氨甲酰基，含C 1至C 3烷基的羟基和C 1至C 3烷基酯化羧基保护的氨基。 制备吡唑并吡啶取代的头孢菌素化合物的方法包括以下步骤：使式（2）和（3）的化合物反应; 并使R3和R4脱保护，其中R3是胺保护基，R4是羧酸保护基; Y为卤素或乙酰氧基。
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