Abstract:
A method for preparing anhydrous hydrochloride salt of 1,4-dihydropyridine derivative is provided to obtain the desired product with high purity and high yield under mild and safe conditions using an activated intermediate. The method comprises the steps of: (a) reacting a compound of the formula(III) with a compound of the formula(IV) to prepare a compound of the formula(V); (b) reacting the compound of the formula(V) with a compound of the formula(II) to prepare an activated intermediate of a compound of the formula(VII) and/or the formula(VI); (c) reacting the intermediate with a compound of the formula(VIII) to prepare a compound of the formula(I); and (d) treating the compound with hydrochloric acid and then crystallizing it.
Abstract:
A pharmaceutical composition comprising ramipril is provided to show excellent stability against mechanical stress by granulation with mannitol solution. And a method for preparing a pharmaceutical formulation comprising stabilized ramipril is provided to simplify the preparation process, thereby obtaining the ramipril containing formulation within short period of time and maintaining the stability of the formulation for a long time. The pharmaceutical composition is characterized in that ramipril as an active ingredient is granulated with mannitol solution. In the composition, the weight ratio of the ramipril to mannitol is 1:0.25-1. The pharmaceutical oral formulation comprises the pharmaceutical composition and a pharmaceutically acceptable excipient.
Abstract:
PURPOSE: Provided is (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid which is prepared through simplified processing steps at high yield and high purity. CONSTITUTION: 4-halomethyl-2(1H)-quinolinone(formula III) reacts with dialkyl 4-chlorobenzoylamino malonate(formula IV) in the presence of an inorganic base in an alcoholic solvent to prepare alkyl 2-(4-chlorobenzoylamino)-2-(alkoxycarbonyl)-3-(2(1H)-quinolinone-4-mono)propionate(formula II) as an intermediate. It selectively suffers decarboxylation and hydrolysis using an acids mixture wherein acetic acid is mixed with other acids in a volume ratio of 1:0.3-10.2, thereby preparing the (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid(formula I). In the formulas, R is C1-6 alkyl group, and X1 is halogen.
Abstract:
PURPOSE: A recombinant vector for animal cells and a method for producing erythropoietin using the same vector are provided, thereby the erythropoietin can be mass-produced and the erythropoietin produced has the same physiological activity as natural erythropoietin. CONSTITUTION: The recombinant vector for animal cells comprises a promoter of cytomegalovirus containing a binding sequence of a mutated methylated DNA binding protein wherein a low affinity binding portion is substituted by a high affinity binding portion, dhfr operably linked to the cytomegalovirus promoter and replication origin. The expression vector for animal cell to mass-produce erythropoietin comprises a promoter of cytomegalovirus containing a binding sequence of modified methylated DNA binding protein wherein a low affinity binding portion is substituted by a high affinity binding portion, dhfr operably linked to the cytomegalovirus promoter, replication origin, a gene encoding erythropoietin, and a promoter operably linked to the erythropoietin gene which is operated in eukaryotic cells.
Abstract:
본 발명은 해열제, 골관절염 및 류마티스관절염 등의 관절질환과 각종 통증에 우수한 치료 효과를 나타내는 소염진통제로 널리 알려져 있는 화학식 1의 화합물[관용명:아세클로페낙(Aceclofenac)]의 신규 제조방법 및 그 제조 과정에서 중간체로 사용되는 화학식 2의 화합물 및 그의 제조방법에 관한 것이다:
상기식에서, R 1 은 C 1-4 알킬렌이고 R 2 는 C 1-4 알킬이다. 본 발명은 매우 저렴하고 사용이 편리한 산(acid)을 사용하여 선택적으로 가수분해시킴으로써 고수율 및 고순도의 화학식 1의 아세클로페낙을 간편하게 제조할 수 있다.
Abstract:
본 발명은 구인(Lumbricus rubellus)으로부터 추출되는 단백질분해 효소인 롬브로키나제를 함유하는 혈관근이완제 조성물에 관한 것이다. 더욱 구체적으로, 본 발명은 구인으로부터 일련의 과정을 거쳐 분리되는 롬브로키나제 활성분획을 활성성분으로 함유하는 이완제 조성물에 관한 것이다.
Abstract:
PURPOSE: An immune enhancer is provided to be used as an antibiotic and an anti-cancer medicine separately or mixed with another ingredient. CONSTITUTION: An immune enhancer containing a lombricine as an effective ingredient activates an immuno-cell of an organism for having an effect of enhancing an immune of the organism. The immune enhancer may be used as an antibiotic and an anti-cancer medicine separately or by mixed with other antibiotic or anti-cancer medicine for minimizing a virulence and maximizing an effect.
Abstract:
The present invention provides 1-beta-D-arobino furanocyl cytocin-5'-stearylphosphate mono sodium salt, which is used as cytocine arabinocide derivatives having great usefulness as anticancer drugs. 1-beta-D-arabinofuranocyl cytocin-5'-stearylphosphate or its amonium salt dissolved in halogenated hydrogen chlorides such as chloroform, dichloromethane or alcohol is passed through cationic ion exchange resin to produce 1-beta-D-arabinofuranocyl cytocin-5'-stearyl phosphate mono ammonium salt.
Abstract:
본 발명은 경구용 백혈병 치료제로서 유용한 시티라빈 옥포스페이트를 함유하는 경질컵셀제에 관한 것이다. 더욱 구체적으로 본 발명은(1) 시타라빈 옥포스페이트, (2) 나트륨라우릴설페이트 및 나트륨도큐세이트 중에서 선택된 계면활성제, (3) 붕해제인 콜로이드성 이산화규소, (4) 알칼리화제인 나트륨시트레이트를 함유함을 특징으로 하는 경질캅셀제에 관한 것이다. 본 발명의 경질 캅셀제는 상기한 바와 같은 특정의 성분들의 조합으로 이루어져 있기 때문에 산성용액중에서도 탁월한 용출성, 붕해성 및 안정성을 제공한다.