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1. 发明公开

KR1020020078025A 5-아미노메틸-2-티오펜카보니트릴 염산염의 제조방법 失效
标题翻译：制备5-氨基-2-巯基苯并噻唑的方法
公开(公告)号：KR1020020078025A
公开(公告)日：2002-10-18
申请号：KR1020010017841
申请日：2001-04-04
申请人： 주식회사 엘지생명과학
发明人： 이구 , 정원혁 , 박철원 , 윤석균 , 김봉찬 , 이재철
IPC分类号： C07D333/36
摘要： PURPOSE: Provided is a process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl which is a useful intermediate of oral thrombin inhibitor. CONSTITUTION: The process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl of the formula(6) comprises the steps of: brominating a compound of the formula(3) to obtain a compound of the formula(4); azidating the compound of the formula(4) to manufacture a compound of the formula(5); and performing Staudinger reaction of iminophosphorane then hydrolysis.
摘要翻译：目的：提供一种有效制备作为口服凝血酶抑制剂有用中间体的5-氨基甲基-2-噻吩甲腈HCl的方法。构成：有效制备式（6）的5-氨基甲基-2-噻吩甲腈HCl的方法包括以下步骤：将式（3）的化合物溴化得到式（4）的化合物; 叠加式（4）的化合物以制备式（5）的化合物; 并进行亚氨基磷烷的Staudinger反应，然后进行水解。

2. 发明公开

KR1020000052621A 경구흡수가 뛰어난 펩티드성 트롬빈 억제제 失效
标题翻译： PEPTIDIC THROMBIN INHIBITOR SHOWING DISTINGUISHED OAL-ABSORPTION
公开(公告)号：KR1020000052621A
公开(公告)日：2000-08-25
申请号：KR1019990064851
申请日：1999-12-29
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박철원 , 정원혁 , 이승학 , 이상구
IPC分类号： C07D401/12
摘要： PURPOSE: A peptidic thrombin inhibitor composition showing distinguished oral-absorption is provided, which shows excellent thrombus production inhibiting effect, so which can be used for preventing blood coagulation and treating various thrombosis. CONSTITUTION: A process for the preparation of (2S)-N-{4-£amino(imino)methyl|benzyl}-1-{(2R)-2-£(aminosulfonyl)amino|-3,3-diphenylpropanoyl}-2-pyr olidinecarboxyamide trifluoroacetate(TFA)(a kind of peptidic thrombin inhibitor composition) comprises of: a)preparing NH2SH2-D-diphenylalanine(Dpa)-proline(Pro)-OMe by adding sulfamoyl chloride and trimethylamine to D-Dpa-Pro-OMe.HCl dichloromethane solution; b)making NH2SO2-D-Dpa-Pro-OH by suspending the a) compound to water and methanol, adding LiOH solution, shaking, and filtering; c)manufacturing NH2SO2-D-Dpa-Pro-(4-CN)-benzylamide(bnamd) by dissolving the b) compound in dimethylformamide, cooling, adding 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide.HCl and 1-hydroxybenzotriazole hydrate, adding 4-cyanobenzylamine.HCl and N-methylmorpholine; d) dissolving the c) compound in pyridine, adding trimethylamine, saturating with H2S gas, eliminating volatile material, drying, adding acetone, iodine methane, eliminating volatile material, drying, dissolving the residue with acetonitrile, adding ammonium acetate, concentrating, and refining to get the objective material.
摘要翻译：目的：提供显示出优异的口服吸收的肽凝血酶抑制剂组合物，其显示出优异的血栓生成抑制作用，因此可用于预防凝血和治疗各种血栓形成。构成：制备（2S）-N- {4- {氨基（亚氨基）甲基|苄基} -1 - {（2R）-2-（氨基磺酰基）氨基| -3,3-二苯基丙酰基} - 2-吡咯烷羧酰胺三氟乙酸盐（TFA）（一种肽凝血酶抑制剂组合物）包括：a）通过向D-Dpa-Pro中加入氨磺酰氯和三甲胺来制备NH2SH2-D-二苯丙氨酸（Dpa） - 脯氨酸（Pro） -OMe.HCl二氯甲烷溶液; b）通过将a）化合物悬浮于水和甲醇中，加入LiOH溶液，摇动和过滤，制备NH2SO2-D-Dpa-Pro-OH; c）通过将b）化合物溶解在二甲基甲酰胺中，冷却，加入1-（3-二甲基氨基丙基）-3-乙基碳二亚胺·HCl和1-羟基苯并三唑制备NH 2 SO 2 -D-Dpa-Pro-（4-CN） - 苄基酰胺（bnamd）水合，加入4-氰基苄胺.HCl和N-甲基吗啉; d）将c）化合物溶解在吡啶中，加入三甲胺，用H 2 S气体饱和，除去挥发物，干燥，加入丙酮，碘甲烷，除去挥发物，干燥，残留物用乙腈溶解，加入乙酸铵，浓缩，精制得到客观资料。

3. 发明公开

KR1020030063046A 엘비84068을 함유하는 염증으로 인한 질환의 예방 및치료용 조성물 및 이를 포함하는 제제 无效
标题翻译：含有LB84068的组合物，用于预防和治疗炎症疾病和包含其的配方
公开(公告)号：KR1020030063046A
公开(公告)日：2003-07-28
申请号：KR1020020003600
申请日：2002-01-22
申请人： 주식회사 엘지생명과학
发明人： 박미정 , 박정규 , 김성섭 , 김민정 , 박철원 , 성정희 , 박태교 , 장혜경
IPC分类号： A61K31/42
摘要： PURPOSE: A composition containing LB84068 as caspase inhibitors as an effective ingredient is provided. The LB84068 is excellent in anti-inflammatory effect and can be effectively used as prophylactic and therapeutic agents for various diseases caused by inflammation, namely glomerulonephritis, rheumatoid arthritis, chronic colitis(IBD) and systemic inflammatory response syndrome. CONSTITUTION: A composition for the prevention and treatment of inflammatory disease comprises LB84068 of the formula(1), a pharmaceutically acceptable salt, a pharmacologically active material selected from the group consisting of a hydrate, a solvate or an isomer, or two or more mixtures thereof and a pharmaceutically acceptable carrier. The LB84068 has a daily dosage between about 0.3 and 100 mg/day/kg body weight. A formulation containing the composition is selected from the group consisting of tablets, soft or hard gelatin capsules, liquids, suspensions, injectable formulations, ointments, creams, gelling agents or lotions.
摘要翻译：目的：提供含有作为半胱天冬酶抑制剂的LB84068作为有效成分的组合物。 LB84068具有优异的抗炎作用，可有效用作炎症引起的各种疾病，即肾小球肾炎，类风湿关节炎，慢性结肠炎（IBD）和全身炎症反应综合征的预防和治疗药物。构成：用于预防和治疗炎性疾病的组合物包括式（1）的LB84068，药学上可接受的盐，选自水合物，溶剂合物或异构体或两种或更多种混合物的药理学活性物质和药学上可接受的载体。 LB84068的日剂量为约0.3至100mg /天/ kg体重。含有该组合物的制剂选自片剂，软或硬明胶胶囊，液体，悬浮液，可注射制剂，软膏剂，霜剂，胶凝剂或洗剂。

4. 发明授权

KR100403950B1 5-아미노메틸-2-티오펜카보니트릴 염산염의 제조방법 失效
标题翻译： 5-아미노메틸-2-티오펜카보니트릴염산염의제조방5-
公开(公告)号：KR100403950B1
公开(公告)日：2003-10-30
申请号：KR1020010017841
申请日：2001-04-04
申请人： 주식회사 엘지생명과학
发明人： 이구 , 정원혁 , 박철원 , 윤석균 , 김봉찬 , 이재철
IPC分类号： C07D333/36
摘要： PURPOSE: Provided is a process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl which is a useful intermediate of oral thrombin inhibitor. CONSTITUTION: The process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl of the formula(6) comprises the steps of: brominating a compound of the formula(3) to obtain a compound of the formula(4); azidating the compound of the formula(4) to manufacture a compound of the formula(5); and performing Staudinger reaction of iminophosphorane then hydrolysis.
摘要翻译：目的：提供一种有效制备作为口服凝血酶抑制剂有用中间体的5-氨基甲基-2-噻吩腈HCl的方法。构成：有效制备式（6）的5-氨基甲基-2-噻吩腈HCl的方法包括以下步骤：溴化式（3）化合物，得到式（4）化合物; 叠氮化式（4）的化合物以制备式（5）的化合物; 并进行亚氨基正膦的Staudinger反应，然后进行水解。

5. 发明授权

KR100594544B1 이소옥사졸린 구조를 갖는 캐스파제 저해제 有权
标题翻译：含有异恶唑啉环的胱天蛋白酶抑制剂
公开(公告)号：KR100594544B1
公开(公告)日：2006-06-30
申请号：KR1020040066726
申请日：2004-08-24
申请人： 주식회사 엘지생명과학
发明人： 장혜경 , 오영수 , 박철원 , 장용진 , 박태교 , 김성섭 , 김민정 , 박미정 , 박정규 , 박희동 , 민경식 , 이태수 , 이상균 , 김수헌 , 정희경 , 이선화 , 김화동 , 김애리 , 박기숙 , 신현익 , 최형욱 , 이규웅 , 이재훈 , 허태호 , 김호준 , 권태식
IPC分类号： C07D261/04 , C07D413/12
CPC分类号： C07D261/04 , C07D413/04 , C07D413/12 , C07D413/14
摘要： 본 발명은 캐스파제(Caspase) 저해제로서 사용되는 하기 화학식 1의 이소옥사졸린 유도체, 그의 제조방법, 및 이를 함유하는 소염 또는 세포고사 방지용 약제학적 조성물에 관한 것이다.

상기 식에서
A, B, R, R
1 , R
2 및 X는 명세서에 정의한 바와 같다.

6. 发明公开

KR1020050022364A 이소옥사졸린 구조를 갖는 캐스파제 저해제 有权
标题翻译： CASPASE抑制剂含有具有由CASPAS引起的治疗或缓解症状的改善活性的异丙嗪环，包括炎症或病毒性
公开(公告)号：KR1020050022364A
公开(公告)日：2005-03-07
申请号：KR1020040066726
申请日：2004-08-24
申请人： 주식회사 엘지생명과학
发明人： 장혜경 , 오영수 , 박철원 , 장용진 , 박태교 , 김성섭 , 김민정 , 박미정 , 박정규 , 박희동 , 민경식 , 이태수 , 이상균 , 김수헌 , 정희경 , 이선화 , 김화동 , 김애리 , 박기숙 , 신현익 , 최형욱 , 이규웅 , 이재훈 , 허태호 , 김호준 , 권태식
IPC分类号： C07D261/04 , C07D413/12
CPC分类号： C07D261/04 , C07D413/04 , C07D413/12 , C07D413/14
摘要： PURPOSE: Caspase inhibitors containing an isoxazoline ring are provided, which caspase inhibitors have improved activity of treating or alleviating sympthoms caused by the caspase including inflammation or apoptosis. CONSTITUTION: The caspase inhibitors containing an isoxazoline ring, represented by formula (1), salts thereof or stereochemical isomers thereof are provided, wherein R is H, simple alkyl chain(-SAC), simple cycloalkyl chain(-SCAC), aryl(-Ar) or aryl substituted simple alkyl chain(-SAC-Ar); R1 is -CH2COOH, -CH2COOR3(R3 = SAC) or -CH2CONHSO2R4(R4 = SAC); R2 is H, -SAC, -Ar or -(CH2)nOR7(R7 = -SAC, -SCAC, -Ar or -SAC-Ar, and n = 1 or 2); A is -(CH2)n- (n = 0-4), -O-(CH2)n- (n = 0-4) or -NR 9-(CH2)n-(n = 0-4, and R9 is -SAC, -SCAC, -Ar or -SAC-Ar); B is H, -SAC, -SCAC, -Ar or -SAC-Ar; -R-R1 is -(CH2)n-, -(CH2)n-O-(CH 2)m- or -(CH2)n-NR10-(CH2)m-(n+m
摘要翻译：目的：提供含有异恶唑啉环的胱天蛋白酶抑制剂，其中胱天蛋白酶抑制剂具有改善的治疗或减轻由胱天蛋白酶引起的症状（包括炎症或细胞凋亡）的活性。提供含有式（1）表示的异恶唑啉环的胱天蛋白酶抑制剂，其盐或其立体化学异构体，其中R为H，简单烷基链（-SAC），简单环烷基链（-SCAC），芳基（ - Ar）或芳基取代的简单烷基链（-SAC-Ar）; R1是-CH2COOH，-CH2COOR3（R3 = SAC）或-CH2CONHSO2R4（R4 = SAC）; R2是H，-SAC，-Ar或 - （CH2）nOR7（R7 = -SAC，-SCAC，-Ar或-SAC-Ar，n = 1或2）。 A是 - （CH 2）n - （n = 0-4），-O-（CH 2）n - （n = 0-4）或-NR 9 - （CH 2）n - （n = 0-4，是-SAC，-SCAC，-Ar或-SAC-Ar）; B是H，-SAC，-SCAC，-Ar或-SAC-Ar; -R-R 1是 - （CH 2）n - ， - （CH 2）n O-（CH 2）m-或 - （CH 2）n -NR 10 - （CH 2）m - （n + m <9，R 10 = -SAC ，-SCAC，-Ar，-SAC-Ar，-C（= O）-SAC，-C（= O）-SSCAC，-C（= O）-Ar或-C（= O）-SAC-Ar） ; X是-C（= O）CH 2 O 2，-C（= O）CH 2 OC（= O）Ar或-COCH 2 -W（W是-N 2，-F，-Cl，-Br，-I，-NR 15 R 16（R 15和 R 16是独立的-SAC，-SCAC，-Ar或-SAC-Ar）或形成3至6元环饱和或不饱和的环状基团或-SR 17（R 17 = -SAC，-SCAC，-Ar或-SAC- Ar）; Y是H，-OH，-OR 18（R 18 = -SAC，-SCAC），-C（= O）R 19（R 19 = -H，-SAC，-SCAC），-F，-Cl，-Br ，-I，-CN，-NC，-N3，-CO2H，CF3，-CO2R20（R20 = -SAC，-SCAC），-C（= O）NHR21（R21 = -SAC，-SCAC）或-C = O）NR22R23（R22和R23独立为-SAC，-SCAC，-Ar或-SAC-Ar））; 和R 24是H，-SAC，-SAC-Ar或-Ar。

7. 发明公开

KR1020030076446A (2Ｓ)-Ｎ-[5-[아미노(이미노)메틸]-2-티에닐]메틸-1-[(2Ｒ)-2-[(카복시메틸)아미노]-3,3-디페닐프로파노일]-2-피롤리딘카르복사미드 말레산 염 및 그의 제조방법 无效
标题翻译：（2S）-N- [5- [氨基（亚氨基）甲基] -2-苯基]甲基-1 - [（2R）-2 - [（羧甲基）氨基] -3,3-二苯基丙酰基] -2-吡咯烷酮甲酰胺酸盐和制剂
公开(公告)号：KR1020030076446A
公开(公告)日：2003-09-26
申请号：KR1020030017853
申请日：2003-03-21
申请人： 주식회사 엘지생명과학
发明人： 김애리 , 박재현 , 윤석균 , 박철원 , 조관형
IPC分类号： C07D409/12
CPC分类号： C07K5/06078 , C07K2299/00
摘要： PURPOSE: (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts and a preparation method thereof are provided, which compounds has improved properties such as improved stability and undeliquescence at 93% of relative humidity, so that it can be useful as a thrombin inhibitor. CONSTITUTION: (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts represented by formula 1 are provided. A method for preparing (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts of formula 1 comprises reacting a free compound of formula 1 with maleic acid in the presence of alcohol solvent, wherein alcohol solvent is selected from methanol, ethanol, propanol, butanol, isopropanol and octanol. Crystalline forms of (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts of formula 1 is prepared by recrystallizing the amorphous compound of formula 1.
摘要翻译：目的：（2S） - N - 5 - £氨基（亚氨基）甲基 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基 -2-吡咯烷甲酰胺马来酸盐及其制备方法，该化合物具有改善的性能，例如93％相对湿度下的稳定性和未起泡性改善，因此可用作凝血酶抑制剂。构成：（2S） - N - 5 - £氨基（亚氨基）甲基 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基 -2-吡啶烷甲酰胺马来酸盐由式1表示。制备（2S）-N - 5-£氨基（亚氨基）甲基的方法 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基式2的吡咯烷甲酰胺马来酸盐包括在醇溶剂存在下使游离的式1化合物与马来酸反应，其中醇溶剂选自甲醇，乙醇，丙醇，丁醇，异丙醇和辛醇。（2S）-N - 5-£氨基（亚氨基）甲基的结晶形式 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基式2的吡咯烷甲酰胺马来酸盐通过将式1的无定形化合物重结晶来制备。

8. 发明公开

KR1020020077806A 5-(아미노메틸)-2-티오펜카보니트릴 염산염의 연속반응에의한 새로운 제조방법 失效
标题翻译：通过一次反应制备5-氨基-2-羟基乙酸烯丙酯的新方法
公开(公告)号：KR1020020077806A
公开(公告)日：2002-10-14
申请号：KR1020020013770
申请日：2002-03-14
申请人： 주식회사 엘지생명과학
发明人： 윤석균 , 김봉찬 , 정원혁 , 이재철 , 이구 , 박철원
IPC分类号： C07D333/36
CPC分类号： C07D333/38
摘要： PURPOSE: Provided is a novel process for preparing 5-aminomethyl-2-thiophenecarbonitrile HCl which is a useful intermediate of oral thrombin inhibitor by one-pot reaction. CONSTITUTION: The novel process for preparing 5-aminomethyl-2-thiophenecarbonitrile HCl of the formula(7) comprises the steps of: reacting a compound of the formula(1) with hydroxylamine to obtain a compound of the formula(2); O-acetylating the compound of the formula(2) to manufacture a compound of the formula(3); removing an acetyl group from the compound of the formula(3) and introducing a cyano group thereto to manufacture a compound of the formula(4); brominating the methyl group of the compound of the formula(4) to obtain a compound of the formula(5); azidating the compound of the formula(5) to obtain a compound of the formula(6); and producing iminophosphorane with the compound of the formula(6) then hydrolyzing it.
摘要翻译：目的：提供一种通过一锅反应制备口服凝血酶抑制剂的有用中间体的5-氨基甲基-2-噻吩甲腈HCl的新方法。组成：式（7）的5-氨基甲基-2-噻吩甲腈HCl的新方法包括以下步骤：使式（1）的化合物与羟胺反应得到式（2）的化合物; O-乙酰化式（2）化合物以制备式（3）化合物; 从式（3）的化合物中除去乙酰基，并向其中引入氰基以制备式（4）的化合物; 溴化式（4）化合物的甲基，得到式（5）化合物; 将式（5）的化合物叠氮，得到式（6）的化合物; 并用式（6）的化合物生产亚氨基磷烷，然后水解。

9. 发明公开

KR1020010086468A 트롬빈 억제제 失效
标题翻译：冷冻抑制剂
公开(公告)号：KR1020010086468A
公开(公告)日：2001-09-12
申请号：KR1020017008401
申请日：1999-12-29
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박철원 , 정원혁 , 이상구 , 이선화 , 박희동
IPC分类号： C07D409/12
CPC分类号： C07K5/0222 , A61K38/00 , C07K5/06078
摘要： PURPOSE: Provided are thrombin inhibitors that are useful as anticoagulants. In particular, peptide derivatives having high antithrombotic activity and high oral bioavailability are provided. CONSTITUTION: A compound is represented by the formula (l) wherein, n is 1,2 or 3; A is hydrogen, cycloalkyl, aryl, -SO2R1, -SO3R1, -COR1, -CO2R2, -PO(OR1)2, -C3-7-(CH2)mSO3R1, (CH2)mCO2R1,-(CH2)mSO2R1, or -(CH2)mPO(OR1)2, wherein P1 is hydrogen, C1-6 alkyl, C3-7cycloalkyl, aryl, -(CH2)maryl, alkyl, or-NR3R4; R2 is C1-6 alkyl, C3-7 cycloalkyl, aryl, -(CH2)maryl or alkenyl, and m is 1,2, or 3, wherein aryl is unsubsituted or substituted phenyl or 5-6 membered aromatic heterocyclic ring, and R3 and R4 are independently hydrogen, Cl-, alkyl, or C3 7 cycloalkyl; B is hydrogen or C1-6 alkyl; C and D are independently hydrogen, phenyl unsubsituted or substituted with one or two substituents selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, CF3, methylenedioxy, halogen, hydroxy and-NR3R4; C37 cycloalkyl; or a 5-6 membered heterocyclic ring system which may be saturated or unsaturated, and which consists of carbon atoms and 1-3 heteroatoms selected from the group consisting of N, O, and S; E is wherein X is S, O or NR5, and Y and Z are independently N or CR6, wherein Rs is hydrogen or C, 4 alkyl, and R6 is hydrogen, halogen, CF3 or C14 alkyl ; and F is-C (NH) N (R') 2,-C (NH2) NN (R') 2,-C (NH2) NOH or-CH2NH (R') 2 wherein R7 is the same or different and is hydrogen, C14 perfluoroalkyl or C14 alkyl.
摘要翻译：目的：提供可用作抗凝血剂的凝血酶抑制剂。特别地，提供了具有高抗血栓活性和高口服生物利用度的肽衍生物。构成：化合物由式（1）表示，其中n为1,2或3; A是氢，环烷基，芳基，-SO 2 R 1，-SO 3 R 1，-COR 1，-CO 2 R 2，-PO（OR 1）2，-C 3 -7 - （CH 2）m SO 3 R 1，（CH 2）m CO 2 R 1， - （CH 2）m SO 2 R 1，（CH2）mPO（OR1）2，其中P1是氢，C1-6烷基，C3-7环烷基，芳基， - （CH2）马来酰基，烷基或-NR3R4; R2是C1-6烷基，C3-7环烷基，芳基， - （CH2）马来酰基或烯基，m是1,2或3，其中芳基是未取代的或取代的苯基或5-6元芳族杂环，R3 和R 4独立地是氢，C 1 - ，烷基或C 3-7环烷基; B是氢或C 1-6烷基; C和D独立地是氢，未取代或被一个或两个选自C 1-4烷基，C 1-4烷氧基，CF 3，亚甲二氧基，卤素，羟基和-NR 3 R 4的取代基取代的苯基; C37环烷基; 或可以是饱和或不饱和的5-6元杂环系，其由碳原子和1-3个选自N，O和S的杂原子组成; E是其中X是S，O或NR 5，Y和Z独立地是N或CR 6，其中R 5是氢或C 1-4烷基，R 6是氢，卤素，CF 3或C 14烷基; 并且F是-C（NH）N（R'）2，-C（NH 2）NN（R'）2，-C（NH 2）NOH或-CH 2 NH（R'）2，其中R 7相同或不同，氢，C14全氟烷基或C14烷基。

10. 发明公开

KR1020050034922A 2-알킬-4-옥소부타노일 그룹을 함유하는 케스페이즈저해제 및 그의 약제학적 조성물 无效
标题翻译：包含2-烷基-4-氧代丁酰基的CASPASE抑制剂及其药物组合物
公开(公告)号：KR1020050034922A
公开(公告)日：2005-04-15
申请号：KR1020030070696
申请日：2003-10-10
申请人： 주식회사 엘지생명과학
发明人： 장혜경 , 오영수 , 박철원 , 박태교 , 김성섭 , 박미정 , 박희동 , 이선화 , 맹한주 , 박수경 , 박기숙 , 장용진 , 김민정 , 박정규 , 김애리
IPC分类号： C07D209/12
CPC分类号： C07C235/74 , C07D209/12 , C07D217/16
摘要： 본 발명은 케스페이즈(Caspase)의 활동을 방해하는 저해제인 하기 화학식 1의 신규한 화합물, 그의 약제학적으로 허용되는 염, 생리학적으로 가수분해가능한 에스테르, 수화물, 용매화물 또는 이들의 입체이성체, 및 약제학적으로 허용되는 담체와 함께 이를 함유하는 약제학적 조성물에 관한 것이다. 하기 화학식 1의 화합물은 지금까지 알려지지 않은 새로운 골격, 즉 2-알킬-4-옥소부타노일 그룹을 함유하고 있다. 본 발명은 또한 명세서에서 화학식 1의 화합물을 합성하는 방법과 바인딩을 측정하는 방법을 예시하였다. 본 방법으로부터 얻어진 화학식 1의 저해제는 케스페이즈의 작용으로 인하여 생겨나는 여러 형태의 질병을 완화하거나, 치료하는데 효과적으로 사용될 수 있다.

상기 식에서, R, R
1 , R
2 , R
3 , X 및 Ar 은 명세서에서 정의한 바와 같다.

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