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1. 发明授权

KR100388791B1 티아졸또는옥사졸구조를갖는파네실전이효소억제제및그의제조방법 失效
公开(公告)号：KR100388791B1
公开(公告)日：2003-10-10
申请号：KR1019980023697
申请日：1998-06-23
申请人： 주식회사 엘지생명과학
发明人： 정원희 , 이현일 , 고종성 , 신유승 , 이진호 , 김종현 , 박기원 , 최태생 , 정현호 , 김귀화 , 문경덕 , 노성구 , 김현성
IPC分类号： C07D413/06 , C07D417/06
摘要： PURPOSE: A novel compound having a superior anticancer effect is prepared. CONSTITUTION: The compounds of the formula (I) are manufactured and estimated for inhibiting activity of enzyme activity in K-Ras substrate. In the formula (I): X is O or S; A is H, lower alkyl, or one of formula (II) wherein, R1 is H, halogen, cyano, nitro and formula (III) wherein, R2 is H, lower alkyl, formyl, lower alkylcarbonyl, or aryl-substituted(unsubstituted) lower alkoxycarbonyl; B is one of formula (IV) and (V) wherein R3 and R4 are H, lower alkyl, lower alkoxy, halogen, cyano, hydroxy, phenyl or phenoxy, respectively; C is lower alkoxy or one of formula (VI) wherein, R5 and R6 are H, lower alkyl, aryl and the formula (VII) wherein, R7 is O or S.
摘要翻译：目的：制备具有优异抗癌效果的新型化合物。构成：制备和估计式（I）化合物用于抑制K-Ras底物中酶活性的活性。在式（I）中：X是O或S; A是H，低级烷基或式（II）中的一个，其中R1是H，卤素，氰基，硝基和式（III），其中R2是H，低级烷基，甲酰基，低级烷基羰基或芳基取代的）低级烷氧基羰基; B是式（IV）和（V）之一，其中R3和R4分别为H，低级烷基，低级烷氧基，卤素，氰基，羟基，苯基或苯氧基; C是低级烷氧基或式（VI）中的一个，其中R5和R6是H，低级烷基，芳基和式（VII），其中R7是O或S.

2. 发明公开

KR1020000055994A 피페리딘 작용기를 갖는 선택적 트롬빈 억제제 失效
标题翻译：具有哌啶功能组的血栓抑制剂
公开(公告)号：KR1020000055994A
公开(公告)日：2000-09-15
申请号：KR1019990004971
申请日：1999-02-12
申请人： 주식회사 엘지생명과학
发明人： 박태교 , 이태희 , 장혜경 , 권오환 , 박희동 , 김현성 , 유영준 , 윤미경
IPC分类号： A61K31/40
摘要： PURPOSE: A novel thrombin inhibitor and a manufacturing method thereof are provided. The pharmaceutical preparation includes the thrombin inhibitor as an effective component and is administrated orally to prevent blood coagulation and treat thrombosis. CONSTITUTION: A novel thrombin inhibitor is represented by the following formula (1): wherein R1 is a hydrogen, R2NCOCO-, RCO-, RSO2-, ROCO-, R2NHSO2 or ROSO2-; R2 is a hydrogen, C1-C8 low alkyl, C6-C10 aryl, C5-C12 arylalkyl, C4-C10 heteroaryl, C5-C11 heteroarylalkyl or C3-C8 cycloalkyl; R2 is a hydrogen, fluoride, chloride bromide, iodine, hydroxy or methoxy; X and X' are independently hydrogen, fluoride chloride bromide, iodine, formyl, cyano, hydroxy or methoxy; n is an integer of 0, 1 or 2; m is an integer of 1 or 2.
摘要翻译：目的：提供一种新型凝血酶抑制剂及其制备方法。药物制剂包括凝血酶抑制剂作为有效成分并口服给药以防止凝血和治疗血栓形成。构成：新型凝血酶抑制剂由下式（1）表示：其中R1是氢，R2NCOCO-，RCO-，RSO2-，ROCO-，R2NHSO2或ROSO2-; R2是氢，C1-C8低级烷基，C6-C10芳基，C5-C12芳基烷基，C4-C10杂芳基，C5-C11杂芳基烷基或C3-C8环烷基; R2是氢，氟化物，氯化溴，碘，羟基或甲氧基; X和X'独立地是氢，氟化氯化物溴，碘，甲酰基，氰基，羟基或甲氧基; n是0,1或2的整数; m为1或2的整数。

3. 发明公开

KR1020000015758A 피롤 구조를 갖는 파네실 전이효소 억제제 및 그의 제조방법 无效
标题翻译：含有微生物转运蛋白结构的抑制剂及其制备方法
公开(公告)号：KR1020000015758A
公开(公告)日：2000-03-15
申请号：KR1019980046457
申请日：1998-10-30
申请人： 주식회사 엘지생명과학
发明人： 정원희 , 고종성 , 이현일 , 신유승 , 이진호 , 김종현 , 정현호 , 박기원 , 최태생 , 김귀화 , 정신우 , 유정권 , 노성구 , 이선화 , 김현성
IPC分类号： C07D403/06 , A61K31/40
摘要： PURPOSE: Compounds containing pyrrole ring; pharmaceutically acceptable salts, optical isomers and esters thereof; and preparation method thereof are provided, which compounds inhibit farnesyl transferase and are used as an anticancer agent. CONSTITUTION: The compounds is represented by the formula 1, and inhibits the farnesylation of H-Ras and N-Ras substrates as well as the farnesylation of K-Ras substrate. The compounds of the formula 1 are prepared by reacting the compounds of the formula 2 with the compounds of the formula 3 in the presence of a base such as sodium hydride, potassium t-butoxide, sodium bis(trimethylsilyl)amide, sodium amide and potassium bis(trimethylsilyl)amide in solvent such as dimethylformamide, dichloromethane, tetrahydrofuran, chloroform and dimethylacetamide.
摘要翻译：目的：含吡咯环的化合物其药学上可接受的盐，旋光异构体和酯; 并提供其制备方法，该化合物抑制法呢基转移酶并用作抗癌剂。构成：化合物由式1表示，并且抑制H-Ras和N-Ras底物的法呢基反应以及K-Ras底物的法呢基化。式1的化合物通过在碱如氢化钠，叔丁醇钾，双（三甲基甲硅烷基）氨基钠，氨基钠和钾的钠存在下使式2的化合物与式3的化合物反应来制备。二（三甲基甲硅烷基）酰胺在溶剂如二甲基甲酰胺，二氯甲烷，四氢呋喃，氯仿和二甲基乙酰胺中。

4. 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。

5. 发明公开

KR1020000002787A 티아졸또는옥사졸구조를갖는파네실전이효소억제제및그의제조방법 失效
标题翻译：具有噻唑或奥沙唑结构的PANESYL转移抑制剂及其制造方法
公开(公告)号：KR1020000002787A
公开(公告)日：2000-01-15
申请号：KR1019980023697
申请日：1998-06-23
申请人： 주식회사 엘지생명과학
发明人： 정원희 , 이현일 , 고종성 , 신유승 , 이진호 , 김종현 , 박기원 , 최태생 , 정현호 , 김귀화 , 문경덕 , 노성구 , 김현성
IPC分类号： C07D413/06 , C07D417/06
摘要： PURPOSE: A novel compound having a superior anticancer effect is prepared. CONSTITUTION: The compounds of the formula (I) are manufactured and estimated for inhibiting activity of enzyme activity in K-Ras substrate. In the formula (I): X is O or S; A is H, lower alkyl, or one of formula (II) wherein, R1 is H, halogen, cyano, nitro and formula (III) wherein, R2 is H, lower alkyl, formyl, lower alkylcarbonyl, or aryl-substituted(unsubstituted) lower alkoxycarbonyl; B is one of formula (IV) and (V) wherein R3 and R4 are H, lower alkyl, lower alkoxy, halogen, cyano, hydroxy, phenyl or phenoxy, respectively; C is lower alkoxy or one of formula (VI) wherein, R5 and R6 are H, lower alkyl, aryl and the formula (VII) wherein, R7 is O or S.
摘要翻译：目的：制备具有优异抗癌作用的新型化合物。构成：制备和估计式（I）化合物以抑制K-Ras底物中酶活性的活性。在式（I）中：X是O或S; A是H，低级烷基或式（II）中的一种，其中R 1是H，卤素，氰基，硝基和式（III）其中R 2是H，低级烷基，甲酰基，低级烷基羰基或芳基取代的）低级烷氧基羰基; B是式（Ⅳ）和（Ⅴ）中的一种，其中R 3和R 4分别是H，低级烷基，低级烷氧基，卤素，氰基，羟基，苯基或苯氧基; C是低级烷氧基或式（VI）之一，其中R 5和R 6是H，低级烷基，芳基和式（Ⅶ），其中R 7是O或S.

6. 发明公开

KR1020000013335A 피페리딘구조를갖는파네실전이효소억제제및그의제조방법 失效
标题翻译：具有管状结构和制备他们的粉末转移抑制剂
公开(公告)号：KR1020000013335A
公开(公告)日：2000-03-06
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为氢或-B-D; B为CH 2，C = O或SO 2; E为苯基或萘基），其可抑制法呢基转移酶。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-甲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。

7. 发明公开

KR1019980075900A 선택적트롬빈억제제 失效
公开(公告)号：KR1019980075900A
公开(公告)日：1998-11-16
申请号：KR1019970012287
申请日：1997-04-03
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 오성호 , 류은정 , 이구 , 황상열 , 홍성원 , 이영진 , 유영준 , 김현성 , 김희진
IPC分类号： C07C237/04 , C07C251/46 , C07C311/16
摘要： 본 발명은 트롬빈 억제제로 유용한 신규 화합물에 관한 것이다. 더욱 구체적으로, 본 발명은 트로빈을 선택적으로 억제하여 강력한 혈전생성 억제효과를 나타내는 하기 화학식 1 의 신규한 술포닐 유도체, 그의 제조방법 및 이 화합물을 유효성분으로 함유하는 혈액응고 예방 또는 각종 혈전증 치료를 위한 의약조성물에 관한 것이다:
[화학식 1]

상기식에서,
R
1 은 하이드록실, 알킬옥시, 아미노 또는 알킬아미노를 나타내며,
R
2 및 R
3
는 각각 독립적으로 저급알킬 또는 사이클로알킬을 나타내고,
R
4 는 수소, 저급알킬 또는 아미노를 나타내며,
n 은 1 내지 5 의 정수이다.

8. 发明授权

KR100377558B1 피페리딘 작용기를 갖는 선택적 트롬빈 억제제 失效
标题翻译： 피페리딘작용기를갖는선택적트롬빈억제제
公开(公告)号：KR100377558B1
公开(公告)日：2003-03-26
申请号：KR1019990004971
申请日：1999-02-12
申请人： 주식회사 엘지생명과학
发明人： 박태교 , 이태희 , 장혜경 , 권오환 , 박희동 , 김현성 , 유영준 , 윤미경
IPC分类号： A61K31/40
摘要： PURPOSE: A novel thrombin inhibitor and a manufacturing method thereof are provided. The pharmaceutical preparation includes the thrombin inhibitor as an effective component and is administrated orally to prevent blood coagulation and treat thrombosis. CONSTITUTION: A novel thrombin inhibitor is represented by the following formula (1): wherein R1 is a hydrogen, R2NCOCO-, RCO-, RSO2-, ROCO-, R2NHSO2 or ROSO2-; R2 is a hydrogen, C1-C8 low alkyl, C6-C10 aryl, C5-C12 arylalkyl, C4-C10 heteroaryl, C5-C11 heteroarylalkyl or C3-C8 cycloalkyl; R2 is a hydrogen, fluoride, chloride bromide, iodine, hydroxy or methoxy; X and X' are independently hydrogen, fluoride chloride bromide, iodine, formyl, cyano, hydroxy or methoxy; n is an integer of 0, 1 or 2; m is an integer of 1 or 2.
摘要翻译：目的：提供一种新型凝血酶抑制剂及其制造方法。该药物制剂包括凝血酶抑制剂作为有效成分，并且口服给药以防止血液凝固并治疗血栓形成。构成：新的凝血酶抑制剂由下式（1）表示：其中R1是氢，R2NCOCO-，RCO-，RSO2-，ROCO-，R2NHSO2或ROSO2-; R2是氢，C1-C8低级烷基，C6-C10芳基，C5-C12芳基烷基，C4-C10杂芳基，C5-C11杂芳基烷基或C3-C8环烷基; R2是氢，氟，溴化物，碘，羟基或甲氧基; X和X'独立地为氢，氟化氯化物，碘，甲酰基，氰基，羟基或甲氧基; n是0,1或2的整数; m是1或2的整数。

9. 发明授权

KR100441635B1 경구투여가가능한선택적트롬빈억제제 失效
标题翻译：可以口服给药的选择性凝血酶抑制剂
公开(公告)号：KR100441635B1
公开(公告)日：2006-01-12
申请号：KR1019970012289
申请日：1997-04-03
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 류은정 , 오성호 , 임종찬 , 신유승 , 윤경희 , 유영준 , 김현성
IPC分类号： C07D317/62 , A61K31/34 , A61K31/425 , C07D277/70
摘要： 본 발명은 트롬빈 억제제로 유용한 신규 화합물에 관한 것이다. 더욱 구체적으로, 본 발명은 트롬빈을 선택적으로 억제하여 강력한 혈전생성 억제효과를 나타내며, 경구투여에 의해서도 유효한 하기 화학식 1 의 신규한 술포닐 유도체, 그의 제조방법 및 이 화합물을 유효성분으로 함유하는 혈액응고 예방 또는 각종 혈전증 치료를 위한 의약조성물에 관한 것이다:
[화학식 1]

상기식에서,
X, Y 및 Z 는 각각 독립적으로 CH
2 , CH, NH, N, O 또는 S 를 나타내거나,
X 가 카르보닐을 나타내고 Y 및 Z 에는 치환된 페닐이 융합된 형태로 결합될 수 있으며,
R
1 및 R
2 는 각각 독립적으로 저급알킬 또는 사이클로알킬을 나타내며,
R
3 는 수소, 저급알킬 또는 아미노를 나타낸다.

10. 发明授权

KR100373373B1 선택적트롬빈억제제 失效
标题翻译：选择性凝血酶抑制剂
公开(公告)号：KR100373373B1
公开(公告)日：2003-05-16
申请号：KR1019970012287
申请日：1997-04-03
申请人： 주식회사 엘지생명과학
发明人： 이창석 , 오성호 , 류은정 , 이구 , 황상열 , 홍성원 , 이영진 , 유영준 , 김현성 , 김희진
IPC分类号： C07C237/04 , C07C251/46 , C07C311/16
摘要： PURPOSE: A novel compound as a selective thrombin inhibitor having improved selectivity to thrombin versus trypsin is provided to prevent blood coagulation and treat thrombosis by thrombus formation inhibiting activity. CONSTITUTION: The selective thrombin inhibitor is provided by the novel sulfonyl derivatives having the formula 1: wherein R1 is hydroxyl, an alkyloxy, amino or an alkylamino; each of R2 and R3 is independently a lower alkyl or a cycloalkyl; R4 is hydrogen, a lower alkyl or amino; and n is an integer of 1 to 5. The pharmaceutical composition for preventing blood coagulation and treating thrombosis comprises the sulfonyl derivatives of the formula 1 as an active ingredient with pharmaceutically acceptable carriers.

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