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公开(公告)号：WO2017116150A1
公开(公告)日：2017-07-06
申请号：PCT/KR2016/015439
申请日：2016-12-28
Applicant: 신풍제약주식회사
Abstract: 본 발명은 활성성분으로서 칸데사르탄 또는 칸데사르탄 실렉세틸 및 암로디핀 또는 이의 약학적으로 허용가능한 염을 함유하는 정제에 있어서, 상기 활성성분의 안정성 및 용출성을 유의적으로 향상시키기 위하여 특정 가용화제를 사용한 정제에 관한 것이다. 또한, 본 발명은 상기 정제를 제조하는 방법에 관한 것이다.
Abstract translation:
本发明涉及含有坎地沙坦或坎地沙坦酯和氨氯地平或作为活性成分的药学上可接受的盐的片剂，注意活性成分的稳定性和溶出特性 本发明涉及使用某些增溶剂以改善它们的片剂。 本发明还涉及制备所述片剂的方法。
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公开(公告)号：KR100811497B1
公开(公告)日：2008-03-07
申请号：KR1020050098640
申请日：2005-10-19
Applicant: 신풍제약주식회사
IPC: C07D211/90
Abstract: 본 발명은 하기 화학식 I의 화합물인 메틸 1,1,N-트리메틸-N-(3,3-디페닐프로필)-2-아미노에틸 1,4-디하이드로-2,6-디메틸-4-(3-니트로페닐)피리딘-3,5-디카르복실레이트(이하, “1,4-디하이드로피리딘 유도체”)를 무수 염산염 형태로 제조하는 방법에 관한 것이다. 구체적으로는 혼합산 무수물 및/또는 활성화된 에스테르 중간체를 형성시키는 것을 특징으로 하는 화학식 I의 무수 염산염을 제조하는 방법에 관한 것이다.
[화학식 I]
레르카리디핀, 무수 염산염, 페닐디클로로 포스페이트-
公开(公告)号：KR1020070087753A
公开(公告)日：2007-08-29
申请号：KR1020050098640
申请日：2005-10-19
Applicant: 신풍제약주식회사
IPC: C07D211/90
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 translation: 提供了制备1,4-二氢吡啶衍生物的无水盐酸盐的方法，使用活化的中间体在温和和安全条件下获得高纯度和高产率的所需产物。 该方法包括以下步骤：（a）使式（III）的化合物与式（Ⅳ）的化合物反应制备式（Ⅴ）化合物; （b）使式（V）的化合物与式（II）的化合物反应以制备式（VII）和/或式（VI）的化合物的活化中间体; （c）使中间体与式（Ⅷ）化合物反应制备式（Ⅰ）化合物; 和（d）用盐酸处理化合物，然后使其结晶。
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公开(公告)号：KR100679166B1
公开(公告)日：2007-02-06
申请号：KR1020050093008
申请日：2005-10-04
Applicant: 신풍제약주식회사
IPC: A61K9/16 , A61K31/403
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 translation: 提供包含雷米普利的药物组合物，以通过用甘露糖醇溶液造粒显示优异的抗机械应激稳定性。 并且提供了一种用于制备包含稳定的雷米普利的药物制剂的方法，以简化制备过程，从而在短时间内获得含有雷米普利的制剂并长时间保持制剂的稳定性。 该药物组合物的特征在于作为活性成分的雷米普利与甘露醇溶液一起造粒。 在该组合物中，雷米普利与甘露糖醇的重量比为1:0.25-1。 药物口服制剂包含药物组合物和药学上可接受的赋形剂。
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5.发明公开
公开(公告)号：KR1020030059961A
公开(公告)日：2003-07-12
申请号：KR1020020000516
申请日：2002-01-04
Applicant: 신풍제약주식회사
IPC: C07D215/14
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 translation: 目的：提供（±）-2-（4-氯苯甲酰氨基）-3-（2（1H） - 喹啉酮-4-单）丙酸，其通过简单的加工步骤以高产率和高纯度制备。 构成：4-卤代甲基-2（1H） - 喹啉酮（式III）在无水碱存在下在醇溶剂中与4-氯苯甲酰基氨基丙二酸二烷基酯（式Ⅳ）反应制备2-（4-氯苯甲酰氨基）-2 - （烷氧基羰基）-3-（2（1H） - 喹啉酮-4-单）丙酸酯（式II）作为中间体。 它选择性地使用酸混合物进行脱羧和水解，其中乙酸与体积比为1:0.3-10.2的其它酸混合，从而制备（±）-2-（4-氯苯甲酰氨基）-3-（2（1H， ） - 喹啉酮-4-单）丙酸（式I）。 式中，R为C1-6烷基，X1为卤素。
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Patent Agency Ranking
公开(公告)号：KR100354271B1
公开(公告)日：2002-09-28
申请号：KR1020000005071
申请日：2000-02-02
Applicant: 신풍제약주식회사
IPC: C07C229/00
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.-
公开(公告)号：KR102209441B1
公开(公告)日：2021-01-29
申请号：KR1020160113284
申请日：2016-09-02
Applicant: 신풍제약주식회사
IPC: C07D495/04 , C07D261/20 , C07D413/04 , A61K31/4365 , A61K31/423 , A61K31/5375
Abstract: 본발명은혈소판응집저해효과를갖는신규한화합물및 그염류에관한것으로서, 더욱상세하게는전단응력에의한혈소판응집(shear stress-induced platelet aggregation)을선택적으로저해하는새로운혈소판응집저해제및 이를유효성분으로하는약학적조성물및 그제조방법에관한것이다.
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8.发明授权(±)-2-(4-클로로벤조일아미노)-3-[2(1Ｈ)-퀴놀리논-4-일]프로피오닉산의 제조 방법 失效（±）-2-（4-클로로벤조일아미노）-3- [2（1H） - 퀴놀리논-4-일]프로피오닉산의제조방（
公开(公告)号：KR100439733B1
公开(公告)日：2004-07-12
申请号：KR1020020000516
申请日：2002-01-04
Applicant: 신풍제약주식회사
IPC: C07D215/14
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 translation: 目的：提供通过简单的加工步骤以高收率和高纯度制备的（（±）） - 2-（4-氯苯甲酰氨基）-3-（2（1H） - 喹啉酮-4-单）丙酸。 结构式：4-卤代甲基-2（1H） - 喹啉酮（式III）与无水碱存在下在醇溶剂中与4-氯苯甲酰氨基丙二酸二烷基酯（式IV）反应，制得2-（4-氯苯甲酰氨基）-2 - （烷氧基羰基）-3-（2（1H） - 喹啉酮-4-酮）丙酸酯（式II）。 由此制备（±）-2-（4-氯苯甲酰基氨基）-3-（ 2（1H） - 喹啉酮-4-单）丙酸（式I）。 在通式中，R是C 1-6烷基，并且X 1是卤素。
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公开(公告)号：KR1020000037954A
公开(公告)日：2000-07-05
申请号：KR1019980052783
申请日：1998-12-03
Applicant: 신풍제약주식회사
IPC: C07C229/40
Abstract: PURPOSE: Provided is a process for producing a £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (aceclofenac) being used for an antipyretic, an analgesic in a high purity and yield, which is an economical and safe process. CONSTITUTION: A aceclofenac (formula 1) is produced by hydrolyzing an ester of a 2,2,2-trihaloethyl ester £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (formula 2) having two esters with Zn or Zn-Cu catalyst in a formic acid, an acetic acid or a trifluoro acetate at 30-60°C for 3-8 hrs. The compound (formula 2) is produced by reacting a sodium or potassium £2-(2,6-dichloroanilino)phenyl| acetate (diclofenac) and a trihaloethyl halo acetate in an equivalent ratio of 1:1.1-1.5 in a dimethyl formamide or a dimethyl sulfoxide at 30-50°C. In the formula, X is a halogen.
Abstract translation: 目的：提供一种用于解热的2-（2,6-二氯苯胺基）苯基|乙酰氧基乙酸酯（醋氯芬酸），高纯度和高产率的止痛剂的方法，这是一种经济且安全的方法。 组成：通过水解具有两个酯的2,2,2-三卤代乙基酯（2-（2,6-二氯苯胺基）苯基|乙酰氧基乙酸酯（式2））的酯来制备醋氯芬酸（式1），其具有Zn或Zn- Cu催化剂在甲酸，乙酸或三氟乙酸酯中在30-60℃下反应3-8小时。 化合物（式2）通过使2-或2,6-二（2,6-二氯苯胺基）苯基钠钠或钾反应来制备 乙酸酯（双氯芬酸）和三卤代乙酸卤乙酸酯，其当量比为1:1.1-1.5，在二甲基甲酰胺或二甲基亚砜中，在30-50℃。 在该式中，X是卤素。
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公开(公告)号：KR100399195B1
公开(公告)日：2003-09-26
申请号：KR1020010013859
申请日：2001-03-17
Applicant: 신풍제약주식회사
IPC: C07D501/12
Abstract: PURPOSE: Provided is a process for preparing amorphous form of cefuroxime axetil, thereby producing amorphous form of cefuroxime axetil, which is excellent in elution in a living body and has stability, in high yield and purity. CONSTITUTION: The amorphous cefuroxime axetil represented by the formula(1) is manufactured by the steps of: dissolving cefuroxime axetil in a polar organic solvent; passing CO2 gas therethrough; and adding a water soluble solution containing inorganic salts to precipitate amorphous cefuroxime axetil.
Abstract translation: 用途：提供一种制备无定形头孢呋辛酯的方法，由此制得无定形形式的头孢呋辛酯，其在生物体中洗脱性能优异，并且具有稳定性，高产率和纯度。 构成：由式（1）表示的无定形头孢呋辛酯通过以下步骤制备：将头孢呋辛酯溶解在极性有机溶剂中; 通过二氧化碳气体; 并加入含有无机盐的水溶性溶液以沉淀无定形头孢呋辛酯。
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