Abstract:
The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Abstract:
The present invention relates to a method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof, which comprises reacting a clopidogrel-acid addition salt with disodium 1,5-naphthalenedisulfonate or its hydrate in water, or a mixture of water and an organic solvent. High quality clopidogrel 1,5-naphthalenedisulfonate can be prepared by the inventive method by way of using non-corrosive disodium 1,5-naphthalenedisulfonate.
Abstract:
The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.
Abstract:
A modified human granulocyte-colony stimulating factor (hG-CSF) is produced by culturing a microorganism transformed with an expression vector comprising a gene encoding a modified hG-CSF to produce and secrete the modified hG-CSF to periplasm, said modified hG-CSF being obtained by replacing at least one of the 1st, 2nd, 3rd and 17th amino acids of wild-type hG-CSF (SEQ ID NO: 2) with other amino acid
Abstract translation:通过培养用包含编码修饰的hG-CSF的基因的表达载体转化的微生物来产生修饰的人粒细胞集落刺激因子(hG-CSF),以产生和分泌经修饰的hG-CSF至周质,所述修饰的hG-CSF 通过将野生型hG-CSF(SEQ ID NO:2)的第1,第2,第3和第17氨基酸中的至少一个替换为其他氨基酸而获得
Abstract:
3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.
Abstract:
High purity cefdinir is prepared in a high yield by a process comprising the steps of: treating a crystalline salt of a cefdinir intermediate with a formic acid-sulfuric acid mixture or a formic acid-methanesulfonic acid mixture to obtain a crystalline salt of cefdinir and reacting the crystalline salt with a base in a solvent.
Abstract:
7-amino-3-methoxymethyl-3-cephem-4-carboxylic acid of formula (I) can be easily prepared by reacting 7-aminocephalosporanic acid of formula (II) with an azeotropic mixture of trimethyl borate and methanol in the presence of methanesulfonic acid:
Abstract:
A heterologous protein is produced by: (i) culturing a microorganism transformed with an expression vector comprising a gene encoding a modified E. coli enterotoxin II signal peptide fused with the heterologous protein to produce and secrete the heterologous protein to periplasm, the modified E. coli enterotoxin II signal peptide being obtained by replacing at least one of the 2nd, 4th, 5th, 12th, 20th, and 22nd amino acids of E. coli enterotoxin II signal peptide of the following amino acid sequence (SEQ ID NO: 1) with another amino acid, with the proviso that at least one of the 2nd and 4th amino acid of the modified peptide is lysine; and (ii) recovering the heterologous protein from the periplasm.
Abstract translation:通过以下方式产生异源蛋白质:(i)培养用包含编码与异源蛋白质融合的修饰的大肠杆菌肠毒素II信号肽的基因的表达载体转化的微生物,以产生和分泌异源蛋白质至周质,修饰的E. 通过将下述氨基酸序列(SEQ ID NO:1)的大肠杆菌肠毒素II信号肽的第2,第4,第5,第12,第20和第22氨基酸中的至少一个替换为大肠杆菌肠毒素II信号肽, 另一氨基酸,条件是修饰肽的第二和第四氨基酸中的至少一个是赖氨酸; 和(ii)从周质中回收异源蛋白质。
Abstract:
Disclosed is a protein complex, comprising a physiologically active polypeptide, a dimeric protein and a non-peptidyl polymer having three functional ends (3-arm), with the linkage of both the physiologically active polypeptide and the dimeric protein to the 3-arm non-peptidyl polymer via respective covalent bonds. The protein complex guarantees the long acting activity and biostability of a physiologically active polypeptide. Having the ability to maintain the bioactivity of physiologically active polypeptides or peptides highly and to significantly improve the serum half life of the polypeptides or peptides, the protein complex can be applied to the development of sustained release formulations of various physiologically active polypeptide drugs. Also, it utilizes raw materials including the physiologically active polypeptides without significant loss, thereby increasing the production yield. Further, it can be easily purified.
Abstract:
The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.