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1. 发明授权

KR101046846B1 고체상 합성법을 이용한 펩타이드의 제조방법 有权
标题翻译：用固相合成法生产肽的方法
公开(公告)号：KR101046846B1
公开(公告)日：2011-07-06
申请号：KR1020070102700
申请日：2007-10-11
申请人： 동국제약 주식회사
发明人： 차경회 , 임대성 , 이한원 , 김경민 , 유선종
IPC分类号： C07K7/06 , C07K7/00 , C07K1/06
CPC分类号： Y02P20/55
摘要： 본 발명은 약리활성을 갖는 펩타이드인 고세렐린(goserelin), 부세렐린(buserelin) 및 루프롤라이드(leuprolide)의 제조방법에 관한 것으로, 본 발명의 제조방법은 고분자 지지체 상에서 아미노산을 순차적으로 결합시킨 후 최종적으로 고분자 지지체에서 유리시켜 고순도로 펩타이드를 제조할 수 있는 새로운 펩타이드 제조방법에 관한 것이다.
펩타이드, 고세렐린, 부세렐린, 루프롤라이드
摘要翻译：本发明涉及一种具有药理活性的戈舍瑞林，布舍瑞林和亮丙瑞林的制备方法，其特征在于氨基酸依次结合在聚合物支架并且最后涉及一种制备可以从聚合物支架中释放以产生高纯度肽的新型肽的方法。

2. 发明公开

KR1020030032185A Ｎ,Ｎ'-비스[2,3-디히드록시프로필]-2,4,6-트리요오드-5-아세틸아미도 이소 프탈아미드의 결정화방법 无效
标题翻译： N，N'-二（2,3-二羟基丙基）-2,4,6-三异丙基-5-乙酰氨基乙酰胺的结晶
公开(公告)号：KR1020030032185A
公开(公告)日：2003-04-26
申请号：KR1020010063774
申请日：2001-10-16
申请人： 동국제약 주식회사
发明人： 최경석 , 홍순명 , 이승화 , 신순철 , 송경상 , 박진규 , 차경회 , 임대성 , 이인규 , 백동렬
IPC分类号： C07F13/00
CPC分类号： C07C231/22 , C07C231/14 , C07C235/48
摘要： PURPOSE: Provided is a crystallization method of crude N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-acetylamidoisophthalamide in a mixed solvent of water and acetone or methanol and ethanol to obtain N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-acetylamidoisophthalamide having high purity of 99.4% in a high yield of 99.9%. CONSTITUTION: The N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-acetylamidoisophthalamide is represented by formula(1) and is an intermediate of iohexol which is used as a contrast medium in X-ray picture. Its crystallization method comprises the steps of: preparing a crude solution of N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-acetylamidoisophthalamide by using, as starting material, 5-acetamido-2,4,6-triiodoisophthaloyl chloride and 3-amino 1,2-propanediol; concentrating the solvent, dimethylacetamide in the crude solution; adding to the concentrate a mixed solvent consisting of 30-60%(v/v) of water and 40-70%(v/v) of acetone or mixture of 40-60%(v/v) of methanol and 40-60% of ethanol with refluxing to obtain crystals; and cooling the obtained crystals at room temperature then purifying them.
摘要翻译：目的：提供粗N，N'-双（2,3-二羟基丙基）-2,4,6-三碘-5-乙酰氨基间苯二甲酰胺在水和丙酮或甲醇和乙醇的混合溶剂中的结晶方法，得到N，（2,3-二羟基丙基）-2,4,6-三碘-5-乙酰氨基间苯二甲酰胺，高纯度为99.4％，99.9％的高收率。构成：N，N'-双（2,3-二羟基丙基）-2,4,6-三碘-5-乙酰氨基间苯二甲酰胺由式（1）表示，是在X中用作造影剂的碘海醇中间体 -ray图片。其结晶方法包括以下步骤：以N，N'-双（2,3-二羟基丙基）-2,4,6-三碘-5-乙酰氨基间苯二甲酰胺为原料，使用5-乙酰氨基-2 ，4,6-三碘间苯二酰氯和3-氨基1,2-丙二醇; 浓缩溶剂，二甲基乙酰胺在粗溶液中; 向浓缩物中加入由30-60％（v / v）水和40-70％（v / v）丙酮或40-60％（v / v）甲醇和40-60％（v / v）甲醇的混合物组成的混合溶剂％的乙醇回流以获得晶体; 并在室温下冷却所得晶体，然后进行纯化。

3. 发明授权

KR100991096B1 고체상 합성법을 이용한 옥트레오타이드의 제조방법 有权
标题翻译：用固相合成法制备奥曲肽的方法
公开(公告)号：KR100991096B1
公开(公告)日：2010-11-01
申请号：KR1020100002115
申请日：2010-01-11
申请人： 동국제약 주식회사
发明人： 차경회 , 임대성 , 이한원
IPC分类号： C07K1/04 , C07K7/04 , C07K7/06 , C07K14/655
CPC分类号： Y02P20/55
摘要： 본 발명은 약리활성을 갖는 펩타이드인 옥트레오타이드(octreotide)의 제조방법에 관한 것으로, 본 발명의 제조방법은 고분자 지지체 상에서 아미노산을 순차적으로 결합시킨 후 최종적으로 고분자 지지체에서 유리시켜 고순도로 펩타이드를 제조할 수 있는 새로운 펩타이드 제조방법에 관한 것이다.
摘要翻译：本发明是在辛酸的苏式潮汐（奥曲肽）的肽由涉及的制造方法，本发明的玻璃终于在聚合物支架被连接到所述氨基酸序列上的聚合物支架肽以高纯度与药理学活性的制造方法生产新型肽的方法。

4. 发明公开

KR1020030033386A 이오헥솔의 제조방법 无效
标题翻译：制备IOHEXOL的方法
公开(公告)号：KR1020030033386A
公开(公告)日：2003-05-01
申请号：KR1020010065135
申请日：2001-10-22
申请人： 동국제약 주식회사
发明人： 최경석 , 홍순명 , 이승화 , 신순철 , 송경상 , 박진규 , 차경회 , 임대성 , 이인규 , 백동렬
IPC分类号： C07F13/00
CPC分类号： C07C231/22 , C07C231/12 , C07C235/48
摘要： PURPOSE: Provided is a process for preparing iohexol by using ethanol or dimethylacetamide as a reaction solvent, thereby rapidly and simply preparing the iohexol in higher yield. CONSTITUTION: A process for preparing iohexol of the formula(1) comprises the steps of: dissolving N,N' - bis £2,3 - dihydroxypropyl| - 2,4,6 - triiodine - 5 - acetylamido isophthalamide and lithium hydroxide monohydrate in ethanol or dimethylacetamide; cooling the solution at 0 to 4 deg. C; and adding 3-chloro-1,2-propanediol into the solution and reacting them to crystalize iohexol, wherein lithium hydroxide monohydrate is added in an amount of 0.5 to 2.5 moles per 1 mole of N,N' - bis £2,3 - dihydroxypropyl| - 2,4,6 - triiodine - 5 - acetylamido isophthalamide; the volume of ethanol or dimethylacetamide used is 1.2 to 1.4 times of 1 mole of N,N' - bis £2,3 - dihydroxypropyl| - 2,4,6 - triiodine - 5 - acetylamido isophthalamide; 3-chloro-1,2-propanediol is added in an amount of 0.5 to 2.5 moles per 1 mole of N,N' - bis £2,3 - dihydroxypropyl| - 2,4,6 - triiodine - 5 - acetylamido isophthalamide; and the reaction is carried out at 0 to 60 deg. C for 25 to 37 hours.
摘要翻译：目的：提供通过使用乙醇或二甲基乙酰胺作为反应溶剂制备碘海醇的方法，从而快速且简单地以高产率制备碘海醇。构成：式（1）的碘海醇的制备方法包括以下步骤：将N，N'-二2,3-二羟丙基| -2,4,6-三碘乙酰乙酰氨基间苯二甲酰胺和氢氧化锂一水合物在乙醇或二甲基乙酰胺中; 在0至4度冷却溶液。 C; 并向溶液中加入3-氯-1,2-丙二醇，并使它们与碘海醇结晶反应，其中每1摩尔N，N'-双2,3,3-三氟乙醇加入0.5至2.5摩尔的氢氧化锂一水合物，二羟基| -2,6,6-三碘代-5-乙酰氨基间苯二胺; 使用的乙醇或二甲基乙酰胺的体积为1摩尔N，N'-二2,3-二羟丙基| -2,6,6-三碘代-5-乙酰氨基间苯二胺; 加入3-氯-1,2-丙二醇的量为0.5至2.5摩尔/ 1摩尔N，N'-二2,3-二羟丙基| -2,6,6-三碘代-5-乙酰氨基间苯二胺; 反应在0〜60℃进行。 C为25至37小时。

5. 发明公开

KR1020000075115A 불순물 Ｃ가 제거된 이오파미돌의 신규 제조방법 无效
标题翻译：通过去除污染物制备IOPAMIDOL的新方法C
公开(公告)号：KR1020000075115A
公开(公告)日：2000-12-15
申请号：KR1019990019517
申请日：1999-05-28
申请人： 동국제약 주식회사
发明人： 허정호 , 박진규 , 최경석 , 임대성
IPC分类号： C07C233/02
摘要： PURPOSE: A novel method for preparing iopamidol useful as an X-ray contrast medium by controlling a precursor of an impurity C in a synthetic process is provided which produces the iopamidol in a simple manner and in high yields. CONSTITUTION: In the process for manufacturing iopamidol by synthesizing 5-amino-2,4,6-triiodoisophthalic acid dichloride and L-2-acetoxypropionyl chloride, it comprises the steps of adding L-2-acetoxypropionyl chloride to a basic solvent such as N,N-dimethylacetamide dichloride or N,N-dimethylformamide and agitating at ordinary temperatures; and adding 5-amino-2,4,6-triiodoisophthalic acid dichloride thereto.
摘要翻译：目的：提供通过在合成方法中控制杂质C的前体而用作X射线造影剂的碘帕醇的新方法，其以简单的方式和高产率产生碘帕醇。构成：在通过合成5-氨基-2,4,6-三碘代邻苯二甲酸二氯化物和L-2-乙酰氧基丙酰氯制备碘帕醇的方法中，包括将L-2-乙酰氧基丙酰氯加入到碱性溶剂如N ，N-二甲基乙酰胺二氯化物或N，N-二甲基甲酰胺，并在常温下搅拌; 并向其中加入5-氨基-2,4,6-三碘代邻苯二甲酸二氯化物。

6. 发明公开

KR1020090074316A 고체상 합성법을 이용한 소마토스타틴 유사체 펩타이드의제조방법 无效
标题翻译：通过固相合成制备SOMATOSTATIN类似物的方法
公开(公告)号：KR1020090074316A
公开(公告)日：2009-07-07
申请号：KR1020080000060
申请日：2008-01-02
申请人： 동국제약 주식회사
发明人： 차경회 , 임대성 , 이한원
IPC分类号： C07K7/04 , C07K7/06
摘要： A method for producing a somatostatin analogues using solid phase synthesis method is provided to manufacture a peptide of high purity and yield by fixing a side chain of cystein on the solid phase support. A method for producing somastatin of the structure formula (a) or octreotide of the structure formula (b) comprises: a step of binding a sided chain of cystein or C-terminal on solid support resin; a step of synthesizing the peptide by binding amino acid derivative in the resin; and a step of performing peptide separation and cyclization through disulfide chain. The amino acid derivatives is protected by the protection group of Boc(tert-butoxycarbonyl), Fmoc(9-fluorenylmethoxycarbonyl), Cbz(benzyl-oxycarbonyl), tBu(tert-butyl), StBu(tert-butylthio), Trt(triphenyl-methyltrityl), Acm(acetamidomethyl) Tacm(trimethylacetamidomethyl) or Tmob(2,4,6-trimethoxybenzyl). The cyclization through disulfide chain is the TFA(trifluoroacetic acid).
摘要翻译：提供使用固相合成法生产生长抑素类似物的方法，通过将半胱氨酸的侧链固定在固相载体上来制备高纯度的肽和产率。制备结构式（a）的莫斯他汀或结构式（b）的奥曲肽的方法包括：将半胱氨酸或C末端的双链结合在固体支持树脂上的步骤; 通过结合树脂中的氨基酸衍生物合成肽的步骤; 以及通过二硫键进行肽分离和环化的步骤。氨基酸衍生物由Boc（叔丁氧羰基），Fmoc（9-芴基甲氧基羰基），Cbz（苄氧基羰基），tBu（叔丁基），StBu（叔丁硫基），Trt（三苯基 - 甲基三苯甲基），Acm（乙酰氨基甲基）Tacm（三甲基乙酰胺基甲基）或Tmob（2,4,6-三甲氧基苄基）。通过二硫键环化是TFA（三氟乙酸）。

7. 发明授权

KR100474653B1 타이코플라닌의 고순도 생산방법 有权
标题翻译： Tykoplanin的高纯度生产方法
公开(公告)号：KR100474653B1
公开(公告)日：2005-03-14
申请号：KR1020040026354
申请日：2004-04-16
申请人： 동국제약 주식회사
发明人： 윤덕중 , 류호명 , 이강희 , 임대성 , 이인규 , 김성우 , 팽현기 , 차경회
IPC分类号： C12P21/00
摘要： PURPOSE: A preparation method of Teicoplanin with high productivity and purity is provided, which method is performed under neutral pH condition to improve stability, and effectively removes impurities including staining components to improve purity. CONSTITUTION: The preparation method of Teicoplanin with high productivity and purity comprises the steps of: (a) eluting the cultured medium of Actinoplanes teichomyceticus DKB 53 with porous adsorption resin by using eluting solvent to obtain crude purified solution containing Teicoplanin; and (b) treating the crude purified solution of step (a) with active carbon, and subjecting the solution treated by the active carbon to ultrafiltration, wherein the eluting solvent has pH 6.0 to 8.0 and comprises 40 to 90%(v/v) C1-C4 water miscible alcohol or C3-C6 water miscible ketone; and the porous adsorption resin is selected from DOWEX OPTIPORE L493, DOWEX OPTIPORE L323, DOWEX OPTIPORE SD-2, DIAION HP20, DIAION HP2MG, DIAION HP20SS, SEPABEADS SP825, SEPABEADS SP850, SEPABEADS SP700, SEPABEADS SP207, SEPABEADS SP20SS, AMBERLITE XAD4, AMBERLITE XAD7, AMBERLITE XAD16 and AMBERLITE XAD1600T which have porous diameter of 20 to 300 angstrom.

8. 发明公开

KR1020030032184A 이오헥솔의 결정화방법 无效
标题翻译： IOHEXOL的结晶方法
公开(公告)号：KR1020030032184A
公开(公告)日：2003-04-26
申请号：KR1020010063773
申请日：2001-10-16
申请人： 동국제약 주식회사
发明人： 최경석 , 홍순명 , 이승화 , 신순철 , 송경상 , 박진규 , 차경회 , 임대성 , 이인규 , 백동렬
IPC分类号： C07C231/24
摘要： PURPOSE: A crystallization method of iohexol is provided to obtain the iohexol of high purity in a high production yield from the unpurified iohexol by using a mixture solvent of methanol and ethanol without using a crystal seed. CONSTITUTION: The crystallization method comprises the steps of adding methanol to the unpurified iohexol to dissolve iohexol into methanol, and decolorizing the solution and removing the impurities from the solution by using an adsorbent; and concentrating the methanol solution, adding ethanol to the solution and refluxing the obtained solvent mixture. Preferably, the absorbent is active carbon; and the solvent mixture comprises 1-20 vol% of methanol and 80-99 vol% of ethanol.
摘要翻译：目的：提供碘海醇的结晶方法，通过使用不使用晶种的甲醇和乙醇的混合溶剂，从未纯化的碘海醇中获得高产率的高纯度碘海醇。结论：结晶方法包括将甲醇加入到未纯化的碘海醇中以将碘海醇溶解在甲醇中，并使用吸附剂将溶液脱色并从溶液中除去杂质的步骤; 并浓缩甲醇溶液，向溶液中加入乙醇并回流得到的溶剂混合物。优选地，吸收剂是活性炭; 溶剂混合物含有1-20体积％的甲醇和80-99体积％的乙醇。

9. 发明公开

KR1020100021501A 고체상 합성법을 이용한 옥트레오타이드의 제조방법 有权
标题翻译：一种通过固相合成制备异戊烯酸酯的方法
公开(公告)号：KR1020100021501A
公开(公告)日：2010-02-24
申请号：KR1020100002115
申请日：2010-01-11
申请人： 동국제약 주식회사
发明人： 차경회 , 임대성 , 이한원
IPC分类号： C07K1/04 , C07K7/04 , C07K7/06 , C07K14/655
CPC分类号： Y02P20/55 , C07K7/64 , C07K1/04 , C07K1/061
摘要： PURPOSE: A method for preparing octreotide having pharmacological activity is provided to release peptide on solid phase support and massively produce a target material with high yield and low cost. CONSTITUTION: A method for preparing octreotide comprises: a first step of reacting 3-methyl-3-butene-1-ol in bromo resin and reacting protected cystein with Fmoc group; a second step of reacting threoninol acetal in the resin to obtain amino acid-bound resin; a third step of synthesizing peptide to obtain peptide-resin connector of straight chain; a fourth step of adding DMF/anisole solution, Tl(tfa)3[thalium trifluoroacetate] mixsture liquid, iodine, Hg(mercury) bivalent ion or Ag(silver) monovalent ion sulfide grouop forming reagent to the connector; and a step of adding TFA[trifluoroacetic acid]: TIS[triisopropylsilane] mixture solution or DCM[dichloromethane] weak acid cleavage solution to the connector to remove side chain protection group.
摘要翻译：目的：提供一种制备具有药理活性的奥曲肽的方法，在固相支持下释放肽，并以高产率和低成本大量生产靶材。构成：制备奥曲肽的方法包括：使3-甲基-3-丁烯-1-醇与溴树脂反应并使受保护的半胱氨酸与Fmoc基团反应的第一步; 在树脂中使苏糖醇缩醛反应得到氨基酸结合树脂的第二步骤; 合成肽以获得直链的肽 - 树脂连接体的第三步; 向连接器中加入DMF /苯甲醚溶液，Tl（tfa）3 [三氟乙酸三钠]混合液，碘，Hg（汞）二价离子或Ag（银）一价离子硫化物组合试剂的第四步骤; 以及将TFA [三氟乙酸]：TIS [三异丙基硅烷]混合物溶液或DCM [二氯甲烷]弱酸裂解溶液加入连接器以除去侧链保护基团的步骤。

10. 发明公开

KR1020080033120A 고체상 합성법을 이용한 펩타이드의 제조방법 有权
标题翻译：一种通过固相合成制备肽的方法
公开(公告)号：KR1020080033120A
公开(公告)日：2008-04-16
申请号：KR1020070102700
申请日：2007-10-11
申请人： 동국제약 주식회사
发明人： 차경회 , 임대성 , 이한원 , 김경민 , 유선종
IPC分类号： C07K7/06 , C07K7/00 , C07K1/06
CPC分类号： Y02P20/55 , C07K7/06 , C07K1/04 , C07K1/061
摘要： A method for preparing peptides having medicinal activity is provided to improve the purity and yield of preparation through the solid phase synthesis by sequentially binding amino acid derivatives with protected side chains to the polymer support. A method for preparing peptides including goserelin, buserelin and leuprolide comprises the steps of: sequentially binding amino acid derivatives with protected N-terminal and side chains to a polymer support resin containing a link amide linker and a resin containing trityl group by using a reaction solvent; and separating peptides from the resins and selectively removing side chain protecting groups, wherein the goserelin has the amino acid sequence of Pyr-His-Trp-Ser-Tyr_D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH2 (acetate salt), the buserelin has the amino acid sequence of Pyr-His-Trp-Ser-Tyr_D-Ser(tBu)-Leu-Arg-Pro-NH-CH2CH2 (acetate salt), and the leuprolide has the amino acid sequence of Pyr-His-Trp-Ser-Tyr_D-Leu-Leu-Arg-Pro-NH-CH2CH2 (acetate salt); the polymer resin is selected from polystyrene, polyamide, glass and silica; the N-terminal and side chains of the amino acid derivatives are protected by Boc(tert-butoxycarbonyl), Fmoc(9-fluorenylmethoxycarbonyl) or Cbz(benzyloxycarbonyl); and the reaction solvent is dichloromethane, chloroform, dichloroethane, dimethylformamide, dimethylacetamide, N-methylpyrrolidinone, tetrahydrofuran, trifluoroacetic acid, dioxane or a mixed solvent thereof. Further, the reaction temperature is 0 to 70 °C.
摘要翻译：提供一种制备具有药用活性的肽的方法，通过将具有受保护侧链的氨基酸衍生物与聚合物载体相连接来提高通过固相合成制备的纯度和产率。制备包括戈舍瑞林，布舍瑞林和亮丙瑞林的肽的方法包括以下步骤：通过使用反应溶剂将氨基酸衍生物与保护的N-末端和侧链依次结合到含有连接酰胺接头的聚合物载体树脂和含有三苯甲基的树脂 ; 并从树脂中分离肽并选择性地除去侧链保护基团，其中戈舍瑞林具有Pyr-His-Trp-Ser-Tyr_D-Ser（tBu）-Leu-Arg-Pro-Azagly-NH2（乙酸盐）的氨基酸序列），布舍瑞林具有Pyr-His-Trp-Ser-Tyr_D-Ser（tBu）-Leu-Arg-Pro-NH-CH 2 CH 2（乙酸盐）的氨基酸序列，亮丙瑞林具有Pyr- His-Trp-Ser-Tyr_D-Leu-Leu-Arg-Pro-NH-CH 2 CH 2（乙酸盐）; 聚合物树脂选自聚苯乙烯，聚酰胺，玻璃和二氧化硅; 氨基酸衍生物的N-末端和侧链由Boc（叔丁氧基羰基），Fmoc（9-芴基甲氧羰基）或Cbz（苄氧基羰基）保护; 反应溶剂为二氯甲烷，氯仿，二氯乙烷，二甲基甲酰胺，二甲基乙酰胺，N-甲基吡咯烷酮，四氢呋喃，三氟乙酸，二恶烷或其混合溶剂。此外，反应温度为0〜70℃。

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