公开(公告)号：KR100458866B1

公开(公告)日：2004-12-03

申请号：KR1019990018380

申请日：1999-05-21

Applicant: 한국화학연구원

Inventor： 박창식 ,  김영섭 ,  김우정

IPC: C07D249/08

Abstract: PURPOSE: Provided is 1,3-dioxolane-2-ilidene derivative represented by the formula (1) which is superior in antifungal activity. Also, a preparation method thereof is provided. CONSTITUTION: 1,3-dioxolane-2-ilidene derivatives is represented by the formula (1), wherein R1 is hydrogen, C1-C6 alkyl, cyclohexyl, thioalkyl, thiophenyl, phenylsulfonyl, trifluoromethyl or pentafluoroethyl; R2 is C1-C6 alkyl, phenyl, naphthyl, thiopene, phenyl substituted with 1-3 halogen, alkyl, alkoxy or trifluoromethyl; and X and Y are hydrogen, alkyl, alkoxy, trifluoromethyl or halogen. A method for preparing 1,3-dioxolane-2-ilidene derivative of the formula (1) comprises a condensation reaction of compounds of the formula (2) and (3) in the presence of a base.

Abstract translation: 目的：提供一种抗真菌活性优异的由式（1）表示的1,3-二氧戊环-2-亚基衍生物。 而且，提供了其制备方法。 结构式：其中R1为氢，C1-C6烷基，环己基，硫代烷基，噻吩基，苯基磺酰基，三氟甲基或五氟乙基的1,3-二氧戊环-2-亚基衍生物由式（1） R2是C1-C6烷基，苯基，萘基，噻吩基，被1-3个卤素，烷基，烷氧基或三氟甲基取代的苯基; X和Y是氢，烷基，烷氧基，三氟甲基或卤素。 用于制备式（1）的1,3-二氧戊环-2-基亚甲基衍生物的方法包括式（2）和（3）的化合物在碱存在下的缩合反应。

公开(公告)号：KR100572996B1

公开(公告)日：2006-04-25

申请号：KR1020030055590

申请日：2003-08-12

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균 ,  김우정

IPC: C07D403/06

CPC classification number: C07D403/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: 본 발명은 항진균제의 용도를 갖는 신규 화합물에 대한 관한 것으로서, 본 발명에 따른 하기 화학식 1의, 불소화비닐에테르 치환기를 가진 아졸계 화합물은 시험관내 및 생체내
항진균활성이 기존의 항진균제에 비하여 우수하며 특히 기존 항진균제의 내성 진균류에 대한 활성이 탁월하고 특히 최근 문제시되고 있는 칸디다 및 아스퍼길러스 등의 진균에 대한 항진균 효과가 우수한 광범위 활성을 나타내고 있는 장점이 있을 뿐 아니라 항진균제의 가장 큰 문제점으로 지적되고 있는 인간의 CytP450의 3A4 효소에 대한 안전성이 매우 크다는 장점을 가지고 있어 장기 복용에 따른 간독성을 최소화할 수 있는 특징을 가지고 있으며 경구 독성에 있어서도 매우 안전하다.


상기 식에서, A는 산소(-O-), 또는 4-(1,2,4-트리아졸-3-일)페닐에테르, 4-(1,2,4-트리아졸-5-온-4-일)페닐에테르, 4-(이미다졸-2-온-3일)페닐에테르, 또는 4-(이미다졸리딘-2-온-3일)페닐에테르를 나타내며, R은 수소 또는 트리플루오르메틸(CF
3 )를 나타내고, R'는 수소 또는 C
1-4 알킬를 나타내며, X는 수소, 할로겐, C
1-4 알킬기, 할로알킬, 알콕시, 3,4 디옥시메틸렌고리 등을 나타낸다.

公开(公告)号：KR1020050017962A

公开(公告)日：2005-02-23

申请号：KR1020030055590

申请日：2003-08-12

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균 ,  김우정

IPC: C07D403/06

CPC classification number: C07D403/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: PURPOSE: Antifungal azole compounds having fluorovinyl ether group as a side chain and an antifungal composition comprising the same compounds are provided, which compounds have improved antifungal activity, especially against antifungal agent resistant fungi, and improved stability in relation to human CytP450 3A4 enzyme, so that they can minimize liver toxicity due to the long time dosage, and also be stable in relation to the oral dosage toxicity. CONSTITUTION: The antifungal azole compounds having fluorovinyl ether group represented by formula (I) or pharmaceutically acceptable salts, isomers or ester compounds thereof are provided, wherein A is oxygen(-O-) or 4-(1,2,4-triazol-3-yl) phenylether, 4-(1,2,4-triazol-5-one-4-yl) phenylether, 4-(imidazol-2-one-3-yl) phenylether, or 4-(imidazolidine-2-one-3-yl) phenylether; R is hydrogen or trifluoromethy; R' is hydrogen or C1-4 alkyl; and X is hydrogen, halogen, C1-4 alkyl, haloalkyl, alkoxy or 3,4-dioxyalkylene ring. The antifungal composition comprises the antifungal azole compounds having fluorovinyl ether group represented by formula (I) and pharmaceutically acceptable carriers.

Abstract translation: 目的：提供具有氟乙烯基醚基作为侧链的抗真菌唑类化合物和包含相同化合物的抗真菌组合物，这些化合物具有改善的抗真菌活性，特别是抗真菌药物抗真菌，并且改善了与人类CytP450 3A4酶相关的稳定性。 它们可以由于长时间剂量而使肝毒性最小化，并且与口服剂量毒性相关也是稳定的。 构成：提供具有式（I）表示的氟乙烯基醚基的抗真菌唑化合物或其药学上可接受的盐，异构体或酯化合物，其中A是氧（-O-）或4-（1,2,4-三唑 - 苯基醚，4-（1,2,4-三唑-5-酮-4-基）苯基醚，4-（咪唑-2-酮-3-基）苯基醚或4-（咪唑烷-2-基） 苯基醚; R是氢或三氟甲基; R'是氢或C 1-4烷基; X为氢，卤素，C 1-4烷基，卤代烷基，烷氧基或3,4-二氧亚烷基环。 抗真菌组合物包含具有由式（I）表示的氟乙烯基醚基团和药学上可接受的载体的抗真菌唑类化合物。

公开(公告)号：KR100342383B1

公开(公告)日：2002-12-06

申请号：KR1019990022778

申请日：1999-06-17

Applicant: 한국화학연구원

Inventor： 박창식 ,  김영섭 ,  김범태 ,  박노균 ,  김우정 ,  김흥태

IPC: C07D413/06

Abstract: 본발명은이소옥사졸리딘유도체에관한것으로서, 이이소옥사졸리딘유도체는하기화학식 1을갖는다. 이화합물은흰가루병에대한살균효과가매우우수하다. [화학식 1] (상기식에서, R은수소원자, C알킬, 시클로헥실, 티오알킬, 티오페닐, 페닐술폰닐, 트리플루오로메틸또는펜타플루오로에틸기이며, R는 C알킬, 페닐, 치환된페닐, 나프틸또는티오펜기이며, 여기서치환된페닐은할로겐원자, 알킬, 알콕시또는트리플루오로메틸기가 1 내지 3개가치환된페닐기를나타내며, X, Y는수소원자, 할로겐원자, C알킬기, 알콕시기이고, Z는질소원자또는메틸렌기이다.)

公开(公告)号：KR1020010002796A

公开(公告)日：2001-01-15

申请号：KR1019990022778

申请日：1999-06-17

Applicant: 한국화학연구원

Inventor： 박창식 ,  김영섭 ,  김범태 ,  박노균 ,  김우정 ,  김흥태

IPC: C07D413/06

Abstract: PURPOSE: The isooxazolidine derivatives, their preparation process, and a bactericidal composition containing the same are provided. The composition has a strong bactericidal activity and is useful in the treatment of the powdery mildew in plants. CONSTITUTION: The isooxazolidine derivatives useful in the treatment of the powdery mildew are represented by formula (1), in which R1 is hydrogen, C1-C6 alkyl, cyclohexyl, thioalkyl, phenylsulfonyl, trifluoromethyl or pentafluoroethyl; R2 is C1-C6 alkyl, phenyl, substituted phenyl, naphthyl, or thiophen, in which substituted phenyl is phenyl substituted with 1 to 3 groups selected from halogen, alkyl, alkoxy, or trifluoromethyl; X, Y are hydrogen, halogen, C1-C4 alkyl, and alkoxy; and Z is nitrogen or methylene. The isooxazolidine derivatives of formula (1) are prepared by condensation of a compound of formula (2) and a compound of formula (3) in the presence of base.

Abstract translation: 目的：提供异恶唑烷衍生物及其制备方法和含有它们的杀菌组合物。 该组合物具有很强的杀菌活性，可用于处理植物中的白粉病。 构成：用于治疗白粉病的异恶唑烷衍生物由式（1）表示，其中R 1是氢，C 1 -C 6烷基，环己基，硫代烷基，苯基磺酰基，三氟甲基或五氟乙基; R2是C1-C6烷基，苯基，取代的苯基，萘基或噻吩，其中取代的苯基是被1至3个选自卤素，烷基，烷氧基或三氟甲基的基团取代的苯基; X，Y是氢，卤素，C 1 -C 4烷基和烷氧基; Z是氮或亚甲基。 式（1）的异恶唑烷衍生物通过式（2）化合物与式（3）化合物在碱存在下缩合制备。

公开(公告)号：KR1020000074444A

公开(公告)日：2000-12-15

申请号：KR1019990018380

申请日：1999-05-21

Applicant: 한국화학연구원

Inventor： 박창식 ,  김영섭 ,  김우정

IPC: C07D249/08

Abstract: PURPOSE: Provided is 1,3-dioxolane-2-ilidene derivative represented by the formula (1) which is superior in antifungal activity. Also, a preparation method thereof is provided. CONSTITUTION: 1,3-dioxolane-2-ilidene derivatives is represented by the formula (1), wherein R1 is hydrogen, C1-C6 alkyl, cyclohexyl, thioalkyl, thiophenyl, phenylsulfonyl, trifluoromethyl or pentafluoroethyl; R2 is C1-C6 alkyl, phenyl, naphthyl, thiopene, phenyl substituted with 1-3 halogen, alkyl, alkoxy or trifluoromethyl; and X and Y are hydrogen, alkyl, alkoxy, trifluoromethyl or halogen. A method for preparing 1,3-dioxolane-2-ilidene derivative of the formula (1) comprises a condensation reaction of compounds of the formula (2) and (3) in the presence of a base.

Abstract translation: 目的：提供抗真菌活性优异的式（1）表示的1,3-二氧戊环-2-亚异
丁基衍生物。 另外，提供了其制备方法。 构成：1,3-二氧杂环戊烯-2-亚炔基衍生物由式（1）表示，其中R 1是氢，C 1 -C 6烷基，环己基，硫代烷基，噻吩基，苯基磺酰基，三氟甲基或五氟乙基; R2是C1-C6烷基，苯基，萘基，噻吩，被1-3个卤素，烷基，烷氧基或三氟甲基取代的苯基; 并且X和Y是氢，烷基，烷氧基，三氟甲基或卤素。 制备式（1）的1,3-二氧戊环-2-亚联衍生物的方法包括式（2）和（3）化合物在碱的存在下的缩合反应。