公开(公告)号：KR101512845B1

公开(公告)日：2015-04-17

申请号：KR1020080020935

申请日：2008-03-06

Applicant: 성균관대학교산학협력단

Inventor： 류도현 ,  황금숙 ,  김건홍 ,  박진현 ,  김화진

IPC: C07C69/52

Abstract: 본 발명은 하기 화학식 1로 표시되는 베타 치환된 모리타-베일리스-힐만 유도체, 그의 약제학적 허용가능한 염, 수화물, 용매화물 및 입체이성질체에 관한 것으로, 상기 유도체는 루이스산의 존재하에 다양한 알데히드나 케톤 등의 카르보닐 화합물, 또는 다양한 이민을 사용하여 베타-아이오도-모리타-베일리스-힐만 에스테르를 제조하고, 이를 기본 골격으로 하고 비닐 위치에 있는 아이오다이드를 다양한 치환기로 치환하여 제조할 수 있다. 또한, 본 발명에 따른 베타 치환된 모리타-베일리스-힐만 유도체들은 항암효과 등 뛰어난 약리효과를 가진다.
[화학식 1]

모리타-베일리스-힐만 부가물 유도체, 프로피올레이트, 알돌, 받게, 아이오다이드, 세코코토몰라이드 A

公开(公告)号：KR1020090095791A

公开(公告)日：2009-09-10

申请号：KR1020080020935

申请日：2008-03-06

Applicant: 성균관대학교산학협력단

Inventor： 류도현 ,  황금숙 ,  김건홍 ,  박진현 ,  김화진

IPC: C07C69/52

CPC classification number: C07C67/31 ,  C07B2200/09 ,  C07C67/343 ,  C07C69/73 ,  C07C69/732 ,  C07C69/738 ,  C07C255/57 ,  C07C311/19 ,  C07F7/1852

Abstract: A beta-substituted Morita-Baylis-Hillman derivative, its preparation method, and its stereoisomer are provided to obtain a compound useful as an anticancer drug or an antiviral agent and useful for the treatment of the infectious disease caused by the bacteria which are parasitic within cells such as tuberculosis and leprosy. A beta-substituted Morita-Baylis-Hillman derivative is represented by the formula 1, wherein R_1a and R_1b are independently hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl group; X_1 is OR_4, or NR_(5a)R_(5b); X_2 is oxygen, sulfur or NR_6; R_2 is hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl; R_3a and R_3b are independently hydrogen, halo, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy or aryl; and methyl-2-(1-hydroxy-2-oxopropyl)hexadeca-2-noate is excluded in the compound of the formula 1.

Abstract translation: 提供β-取代的Morita-Baylis-Hillman衍生物及其制备方法及其立体异构体以获得可用作抗癌药物或抗病毒剂的化合物，并且可用于治疗由寄生在其中的细菌引起的感染性疾病 细胞如结核病和麻风病。 β-取代的Morita-Baylis-Hillman衍生物由式1表示，其中R_1a和R_1b独立地为氢，卤素，羟基，烷基，环烷基，烯基，炔基，烷氧基或芳基; X_1为OR_4，或NR_（5a）R_（5b）; X_2是氧，硫或NR_6; R 2是氢，卤素，羟基，烷基，环烷基，烯基，炔基，烷氧基或芳基; R_3a和R_3b独立地是氢，卤素，羟基，烷基，环烷基，烯基，炔基，烷氧基或芳基; 并且在式1的化合物中不包括甲基-2-（1-羟基-2-氧代丙基）十六烷-2-基。

公开(公告)号：KR1020080100886A

公开(公告)日：2008-11-21

申请号：KR1020070046877

申请日：2007-05-15

Applicant: 주식회사 푸드사이언스 ,  성균관대학교산학협력단 ,  연세대학교 산학협력단 ,  한국기초과학지원연구원

Inventor： 류도현 ,  황금숙 ,  김건홍 ,  김화진 ,  박진현 ,  김경화 ,  심재의 ,  이미영

IPC: C07D471/04 ,  A61P31/12 ,  A61P35/00

Abstract: An octahydro indeno derivative is provided to have a high biological activity, to have a high cytotoxin to cancer cells with a minimum amount and to be used as an anti-cancer drug or an antibiotic. A composition of treating and preventing cancers includes a compound indicated by a chemical formula 1 and a pharmaceutically allowed carrier. In the chemical formula 1: X is oxygen, sulfur or NH; R1 is hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl or alkoxy; R2 and R3 are independently hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl or heteroaryl; R4a and R4b are hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl or alkoxy; R5a and R5b are hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; R6a and R6b are hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl, alkoxy or the carbonyl radical; R7a and R7b are the hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; R8 is hydrogen, hollow, hydroxy, alkyl, alkenyl, alkynyl or alkoxy; and R9a and R9b are hydrogen, hollow, hydroxy, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl or heteroaryl.

Abstract translation: 提供八氢茚并衍生物以具有高生物活性，以最小量对癌细胞具有高细胞毒素，并用作抗癌药物或抗生素。 治疗和预防癌症的组合物包括由化学式1表示的化合物和药学上允许的载体。 在化学式1中：X是氧，硫或NH; R1是氢，中空，羟基，烷基，环烷基，烯基，炔基或烷氧基; R2和R3独立地是氢，中空，羟基，烷基，环烷基，烯基，炔基，烷氧基，芳基或杂芳基; R4a和R4b是氢，中空，羟基，烷基，环烷基，烯基，炔基或烷氧基; R5a和R5b是氢，中空，羟基，烷基，烯基，炔基或烷氧基; R6a和R6b是氢，中空，羟基，烷基，烯基，炔基，烷氧基或羰基; R7a和R7b是氢，中空，羟基，烷基，烯基，炔基或烷氧基; R8是氢，中空，羟基，烷基，烯基，炔基或烷氧基; R9a和R9b是氢，中空，羟基，烷基，环烷基，烯基，炔基，烷氧基，芳基或杂芳基。