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1. 发明公开

KR1020040101992A 간 질환에서의 유전자 발현 프로파일 无效
标题翻译：肝病中的基因表达谱
公开(公告)号：KR1020040101992A
公开(公告)日：2004-12-03
申请号：KR1020047009882
申请日：2002-12-20
申请人： 주식회사 엘지생명과학
发明人： 고상석 , 리우킹 , 정현호 , 젱웬 , 이복만 , 웨라밀리수브라매니암 , 송시용
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/136 , C12Q2600/158 , Y02A90/26 , G01N33/57438 , G01N2033/57461
摘要： 본 발명은 암화 간 조직과 병에 걸렸지만 암화되지 않은 조직에서 다르게 발현되는 유전자들을 확인하기 위하여 간 종양으로부터의 조직을 검사함으로써 얻어진다. 본 발명은, 차등 발현된 유전자들에 상보적이거나 또는 그것에 혼성화되는 올리고뉴클레오티드 어레이를 포함하는 것으로 구성된 고체 지지체뿐만 아니라, 상기 유전자들을 이용하여 진단하는 방법, 약제 설계를 모니터링하는 방법 및 치료방법들 포함하고 있다.

2. 发明授权

KR100388794B1 피페리딘구조를갖는파네실전이효소억제제및그의제조방법 失效
公开(公告)号：KR100388794B1
公开(公告)日：2003-10-10
申请号：KR1019980032150
申请日：1998-08-07
申请人： 주식회사 엘지생명과학
发明人： 이현일 , 고종성 , 신유승 , 김종현 , 정원희 , 이진호 , 정현호 , 박기원 , 김귀화 , 최태생 , 오영훈 , 김청미 , 노성구 , 이선화 , 김현성
IPC分类号： C07D401/14
摘要： PURPOSE: The compounds are prepared which has an anticancer effect. CONSTITUTION: Title compounds(formula 1; A is hydrogen or -B-D; B is CH2, C=O, or SO2; E is phenyl or naphthyl) having piperidine structure, which can inhibit the farnesyl transferase are prepared. For example, 612 mg of N-methylpiperazyl-4-(1-naphthyl)- -1H-pyrrol-3-carboxamide is dissolved in 10ml of dimethyl formamide, followed by addition of 264mg of 60% sodium hydride at 0 degree C for 5 minutes. Obtained reactant and 765mg of 4-(5-chloromethyl-imidazol-1ylmethyl)-piperidine-1-carboxylic acid benzyl ester are reacted at room temperature for 5 hours, and extracted by ethyl acetate to give 930 mg of 4-methylpiperazino-1-{£1-(1-benzyloxycarbonylpiperidin- -4-ylmethyl)-1H-imidazol-5-yl|methyl}-4-(1-naphthyl)-1H-pyrrol-3-carboxamide.
摘要翻译：目的：制备具有抗癌作用的化合物。构成：制备具有哌啶结构的标题化合物（式1; A是氢或-B-D; B是CH2，C = O或SO2; E是苯基或萘基），其可以抑制法尼基转移酶。例如，将612mg N-甲基哌嗪基-4-（1-萘基）-1H-吡咯-3-甲酰胺溶于10ml二甲基甲酰胺中，然后在0℃下加入264mg 60％氢化钠，5 分钟。得到的反应物和765mg 4-（5-氯甲基 - 咪唑-1-基甲基） - 哌啶-1-羧酸苄酯在室温下反应5小时，用乙酸乙酯萃取，得到930mg 4-甲基哌嗪-1-基 - {1-（1-苄氧基羰基哌啶-4-基甲基）-1H-咪唑-5-基}甲基} -4-（1-萘基）-1H-吡咯-3-甲酰胺。

3. 发明授权

KR100388790B1 파네실전이효소저해제로서유용한피리딘-2-온유도체 失效
公开(公告)号：KR100388790B1
公开(公告)日：2003-10-04
申请号：KR1019980007573
申请日：1998-03-06
申请人： 주식회사 엘지생명과학
发明人： 김종현 , 이진호 , 고종성 , 이현일 , 신유승 , 정원희 , 정현호 , 박기원 , 문경덕 , 김귀화 , 곽태환 , 노성구 , 백선관 , 안인애
IPC分类号： C07D401/10
摘要： PURPOSE: Provided is a pyridin-2-one derivative of the formula(1) which is useful as a farnesyl transferase inhibitor. Also, provided are its pharmaceutically acceptable salt, solvate and manufacturing method. CONSTITUTION: A pyridin-2-one derivative is represented by the formula(1), wherein R1 is C1-4 linear or branched alkyl, halogen or C1-4 linear or branched alkyl substituted or unsubstituted aryl, or mono or bicyclic aromatic radical containing one or two hetero atom selected from nitrogen or sulfur atom; R2 is hydrogen or C1-4 linear or branched alkyl; R3 and R4 are hydrogen; and n is an integer of 1-3.

4. 发明授权

KR100388789B1 피롤구조를갖는파네실전이효소억제제및그의제조방법 失效
公开(公告)号：KR100388789B1
公开(公告)日：2003-10-04
申请号：KR1019980002777
申请日：1998-02-02
申请人： 주식회사 엘지생명과학
发明人： 정원희 , 이현일 , 고종성 , 이진호 , 신유승 , 김종현 , 정현호 , 박기원 , 문경덕 , 김귀화 , 곽태환 , 노성구 , 백선관
IPC分类号： C07D403/06
摘要： PURPOSE: Provided are a farnesyl transferase inhibitor of the formula(1) having pyrrole structure and its pharmaceutically acceptable salt. Also provided is a method for manufacturing the same having excellent anticancer activity. CONSTITUTION: A farnesyl transferase inhibitor is characteristically represented by the formula(1), as defined in the specification. A farnesyl transferase is manufactured by (a) reacting a compound of the formula(2) with a compound of the formula(3), or (b) coupling a compound of the formula(1a) with a compound of the formula(4):R2-X to give a compound of the formula(1b).

5. 发明授权

KR100388792B1 피페리딘구조를갖는파네실전이효소억제제및그의제조방법 失效
标题翻译：具有PEPERIDINE结构的PANE酶酶抑制剂及其生产方法
公开(公告)号：KR100388792B1
公开(公告)日：2003-09-22
申请号：KR1019980028340
申请日：1998-07-14
申请人： 주식회사 엘지생명과학
发明人： 신유승 , 고종성 , 이현일 , 이진호 , 정원희 , 김종현 , 정현호 , 박기원 , 문경덕 , 김귀화 , 곽태환 , 노성구 , 안인애
IPC分类号： C07D401/14
摘要： PURPOSE: Provided are a farnesyl transferase inhibitor of the formula(1) having piperidine structure, its pharmaceutically acceptable salt and a method for manufacturing the same, as well as a useful intermediate used in manufacturing the same. CONSTITUTION: A farnesyl transferase inhibitor represented by the formula(1), wherein A, E and G are as defined in the specification, is characterized by having piperidine structure and showing excellent anticancer activity.

6. 发明授权

KR100381216B1 피롤구조를갖는파네실전이효소억제제및그의제조방법 失效
公开(公告)号：KR100381216B1
公开(公告)日：2003-08-30
申请号：KR1019980035652
申请日：1998-08-31
申请人： 주식회사 엘지생명과학
发明人： 이현일 , 고종성 , 정원희 , 이진호 , 김종현 , 신유승 , 노성구 , 안인애 , 박기원 , 문경덕 , 곽태환 , 정현호 , 최태생
IPC分类号： C07D403/06
摘要： PURPOSE: Provided are a farnesyl transferase inhibitor of the formula(1) having pyrrole structure, its pharmaceutically acceptable salt or isomer and a method for manufacturing the same. Also provided is an anticancer composition containing the farnesyl transferase inhibitor as an active ingredient. CONSTITUTION: A farnesyl transferase inhibitor is characteristically represented by the formula(1), wherein n1 is an integer of 1-4; x is O or S; A is hydrogen, C3-7 cycloalkyl or lower alkoxy substituted or unsubstituted linear or branched C1-10 alkyl, or halogen, cyano, nitro, hydroxycarbonyl, aminocarbonyl, aminothiocarbonyl, lower alkoxy, phenoxy, or lower alkyl substituted or unsubstituted benzyl; B is hydrogen, or hydroxy, mercapto, lower alkoxy, lower alkylthio or aryl substituted or unsubstituted lower alkyl; C is aryl substituted or unsubstituted lower alkyl; and D is amino acid residue or its lower alkylester.

7. 发明授权

KR100385095B1 파네실전이효소저해효능을갖는2환또는3환방향족화합물 失效
公开(公告)号：KR100385095B1
公开(公告)日：2003-08-19
申请号：KR1019970032805
申请日：1997-07-15
申请人： 주식회사 엘지생명과학
发明人： 정원희 , 이현일 , 고종성 , 이진호 , 유정권 , 노성구 , 백선관 , 정현호 , 곽태환 , 문경덕 , 박기원
IPC分类号： C07D233/66 , C07D403/12 , C07D407/12
摘要： PURPOSE: Provided are a 2- or 3-membered ring aromatic compound having farnesyl transferase inhibiting activity, its isomer, pharmaceutically acceptable salt, hydrate or solvate, and its manufacturing method as well as a pharmaceutical composition of an anticancer agent containing the same. CONSTITUTION: A 2- or 3-membered ring aromatic compound having farnesyl transferase inhibiting activity is represented by the formula(1), wherein A is hydrogen; methyl, ethyl, isopropyl, isobutyl, t-butyl containing C1-4 linear or branched alkyl, or represented by the formula(2); B is one of oxygen (-O-) and sulfur (-S-) or represented by the formula(3); R is 3-membered ring aromatic derivative or selected from substituents represented by the formulae(4 and 5); and n is 0-2.

8. 发明授权

KR100375421B1 항암효과를갖는파네실전이효소저해제 失效
标题翻译：抗肿瘤酶抑制剂，
公开(公告)号：KR100375421B1
公开(公告)日：2003-05-12
申请号：KR1019970032870
申请日：1997-07-15
申请人： 주식회사 엘지생명과학
发明人： 이현일 , 정원희 , 이진호 , 고종성 , 정현호 , 문경덕 , 박기원 , 곽태환 , 유정권 , 노성구 , 백선관 , 안인애
IPC分类号： C07D403/06 , A61K31/395 , C07D403/14 , C07D405/14 , C07D409/14
摘要： PURPOSE: A farnesyl transferase inhibitor having anti-tumor properties is provided, which is useful for treatment of cancers caused by farnesyl transferase. CONSTITUTION: The farnesyl transferase inhibitor represented by formula 1, and pharmaceutically acceptable salts, hydrides or solvates thereof are provided, wherein (1) W is selected from -CH2, -CH2CH2, -CH2CH2CH2, -CH2CH2CH2CH2, -CH=CHCH2, -CH2CH=CH, -CH2CH=CHCH2, -CH=CHCH2CH2 or -CH2CH2CH=CH; (2) X is selected from hydrogen and C1-C4 alkyl or selected from benzyl derivatives of formula 2, wherein R1 is selected from halogen, cyano, carboxy, amide, phenoxy, phenyl and C1-C4 alkyl; (3) Y is 5-membered heterocyclic aromatic compound of formula 3, wherein R2 is selected from hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkyl substituted phenoxy, or selected from derivatives of formula 4, wherein R3 is hydroxy, C1-C4 alkyl and C1-C4 alkoxy; and (4) Z is selected from C1-C4 alkyl, phenyl derivatives and bicyclic aromatic compound.

9. 发明公开

KR1020010103618A 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸 失效
标题翻译：具有作为细胞生长抑制剂的1,1-二氧硫杂环己烷的吲哚
公开(公告)号：KR1020010103618A
公开(公告)日：2001-11-23
申请号：KR1020010022268
申请日：2001-04-25
申请人： 주식회사 엘지생명과학
发明人： 이진호 , 홍창용 , 박태식 , 김종현 , 최세현 , 윤숙경 , 정현호 , 정신우 , 황광연 , 신동규
IPC分类号： C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： 본 발명은 사이클린 의존 키나아제(CDK)의 저해제로 유용한 1,1-디옥소이소티아졸리딘 그룹을 가진 하기 화학식 1의 인다졸 유도체, 그의 약제학적으로 허용되는 염, 용매화물 및 이성체에 관한 것이다. 본 발명은 또한 화학식 1의 화합물을 제조하는 방법 및 약제학적으로 허용되는 담체와 함께 화학식 1의 화합물을 활성성분으로 함유함을 특징으로 하는 암, 염증, 혈관 협착증 및 혈관생성 등 세포 증식에 관련된 질병의 억제제 및 치료제에 관한 것이다.
[화학식 1]

상기식에서 R
1 , R
2 , R
3 , R
4 , X 및 n은 명세서에서 정의된 바와 같다.

10. 发明公开

KR1020010017458A 피롤구조를 갖는 파네실 전이효소 억제제 및 그의 제조방법 失效
标题翻译：具有微晶结构的农业转基因抑制剂及其生产方法
公开(公告)号：KR1020010017458A
公开(公告)日：2001-03-05
申请号：KR1019990032972
申请日：1999-08-11
申请人： 주식회사 엘지생명과학
发明人： 신유승 , 고종성 , 이현일 , 김학중 , 정양식 , 정현호 , 정신우 , 김귀화 , 최태생 , 김청미 , 이선화 , 이상균
IPC分类号： A01N43/36
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14
摘要： PURPOSE: An inhibitor of farnesyl transferase having a pyrrole structure and a producing method are provided for inhibiting the activation of K-Ras which induces several cancers in human body. CONSTITUTION: The inhibitor of farnesyl transferase is represented by formula (1), in which A is hydrogen, lower alkyl, or a compound selected from the following four formulas represented in the description, in which m and n are individually integers of 0 to 4; R1 and R5 are individually hydrogen, lower alkyl, lower alkoxy or halogen; R2 and R4 are individually hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, second amine substituted by lower alkyl, C3-C6 cycloalkyl, lower alkyl substituted by C3-C6 cycloalkyl, halogen, phenyl or phenoxy; R6 is hydrogen or lower alkyl, and R7 is lower alkyl, aromatics or aromatics substituted by halogen; B is hydrogen, thio substituted by lower alkyl or NH2; D is hydrogen, lower alkyl, halogen, thio substituted by lower alkyl, NO2 or NH2; E is naphtyl or phenyl; F is a compound selected from the following two formulas represented in the description, in which R8 is lower alkyl or lower alkoxy; R9 is lower alkyl; and R10 is hydrogen or lower alkyl; and G is hydrogen, lower alkyl, thio substituted by lower alkyl or phenyl. The farnesyl transferase inhibitor is prepared by reacting compounds of formula (2) with compounds of formula (3) in a solvent in the presence of base to produce compounds of formula (1a) or (1b) or reacting compounds of formula (1a) in the presence of base to produce compounds of formula (1b).
摘要翻译：目的：提供具有吡咯结构的法呢基转移酶抑制剂和制备方法，用于抑制在人体中诱导数种癌症的K-Ras的活化。构成：法呢基转移酶的抑制剂由式（1）表示，其中A是氢，低级烷基或选自以下描述的四个式中的化合物，其中m和n各自为0-4的整数 ; R1和R5分别是氢，低级烷基，低级烷氧基或卤素; R2和R4分别是氢，低级烷基，低级烷氧基，卤素或羟基; R3是氢，低级烷基，低级烷氧基，羟基，被低级烷基取代的第二胺，C3-C6环烷基，被C3-C6环烷基取代的低级烷基，卤素，苯基或苯氧基; R6为氢或低级烷基，R7为卤素取代的低级烷基，芳烃或芳烃; B是氢，被低级烷基或NH 2取代的硫; D是氢，低级烷基，卤素，被低级烷基，NO 2或NH 2取代的硫基; E是萘基或苯基; F是选自以下描述中所示的两个式的化合物，其中R8是低级烷基或低级烷氧基; R9是低级烷基; 和R 10是氢或低级烷基; 和G是氢，低级烷基，被低级烷基或苯基取代的硫代。法尼基转移酶抑制剂通过使式（2）化合物与式（3）化合物在溶剂中在碱存在下反应制备，以制备式（1a）或（1b）化合物或使式（1a）化合物在碱的存在以产生式（1b）化合物。

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