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1. 发明申请

WO2007073095A1 PROCESS FOR THE PREPARATION OF (S)-(+)-CLOPIDOGREL ON A SOLID-PHASE 审中-公开
标题翻译：在固体相上制备（S） - （+） - 螯合物的方法
公开(公告)号：WO2007073095A1
公开(公告)日：2007-06-28
申请号：PCT/KR2006/005602
申请日：2006-12-20
申请人： SK CHEMICALS CO., LTD. , LEE, Jin Young , KIM, Nam Ho , KIM, Jae-Sun , LEE, Nam Kyu
发明人： LEE, Jin Young , KIM, Nam Ho , KIM, Jae-Sun , LEE, Nam Kyu
IPC分类号： C07D495/04 , C07D513/08 , C07D498/02 , A61P7/02 , A61P9/10
CPC分类号： C07D495/04
摘要： The present invention relates to a process for preparing S-(+)-clopidogrel using a solid-phase reaction, and more particularly, to a process for preparing S-(+)- clopidogrel represented by the following formula 1 with high optical and chemical purity by carrying out a series of reactions and purifications more simply by a solid- phase synthetic approach using a polymer support.
摘要翻译：本发明涉及一种使用固相反应制备S - （+） - 氯吡格雷的方法，更具体地说，涉及一种用高光学和化学药物制备由下式1表示的S - （+） - 氯吡格雷的方法通过使用聚合物载体的固相合成方法更简单地进行一系列反应和纯化，从而获得纯度。

2. 发明申请

WO2005077942A1 PROCESS FOR PREPARING SUBSTITUTED BENZOPYRAN COMPOUNDS 审中-公开
标题翻译：制备取代苯并噻吩化合物的方法
公开(公告)号：WO2005077942A1
公开(公告)日：2005-08-25
申请号：PCT/KR2005/000365
申请日：2005-02-07
申请人： SK CHEMICALS, CO., LTD. , LEE, Nam Kyu , LEE, Ju Young , KIM, Jae-Sun , JUNG, Jae Yoon , UM, Key An , OH, Yong Ho , SHIN, Ho Chul , JANG, Woo Jae , IM, Guang-Jin , KIM, Tae Kon
发明人： LEE, Nam Kyu , LEE, Ju Young , KIM, Jae-Sun , JUNG, Jae Yoon , UM, Key An , OH, Yong Ho , SHIN, Ho Chul , JANG, Woo Jae , IM, Guang-Jin , KIM, Tae Kon
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： The present invention relates to a novel method of synthesizing substituted benzopyran compounds, their novel intermediates and a method of their preparation thereof.
摘要翻译：本发明涉及一种合成取代苯并吡喃化合物的新方法及其新型中间体及其制备方法。

3. 发明申请

WO2008072939A1 INCLUSION COMPLEX CONTAINING CLOPIDOGREL WITH IMPROVED STORAGE STABILITY 审中-公开
标题翻译：包含CLOPIDOGREL的复合物具有改进的储存稳定性
公开(公告)号：WO2008072939A1
公开(公告)日：2008-06-19
申请号：PCT/KR2007/006599
申请日：2007-12-17
申请人： SK CHEMICALS CO., LTD. , KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , OH, Joon Gyo , SHIN, Ji Young , KIM, Tae-Kon , YOON, Mi-Sun , SUNG, Jin-Heung , LEE, Yoon-Jung , PARK, Yeo-Jin , UM, Key An
发明人： KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , OH, Joon Gyo , SHIN, Ji Young , KIM, Tae-Kon , YOON, Mi-Sun , SUNG, Jin-Heung , LEE, Yoon-Jung , PARK, Yeo-Jin , UM, Key An
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to an inclusion complex containing clopidogrel with superior storage stability, more particularly to a pharmaceutically stable and suitable inclusion complex obtained by reacting S-(+)-clopidogrel [methyl (+)-(S)-α- (o-chlorophenyl)-6/7-dihydrothieno[3,2-c]pyridin-5(4H)-acetate] represented by the formula (1) below with β-cyclodextrin at a specific equivalence ratio, and an antiplatelet agent composition comprising the same as an active ingredient:
摘要翻译：本发明涉及具有优异储存稳定性的含有氯吡格雷的包合络合物，更具体地涉及通过使S-（+） - 氯吡格雷[甲基（+） - （S）-α-（o- 氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸酯]和具有特定当量比的β-环糊精的抗血小板药剂组合物作为有效成分：

4. 发明申请

WO2008018779A1 PROCESS FOR HIGH YIELD PRODUCTION OF CLOPIDOGREL BY RACEMIZATION OF RESIDUAL LIQUID 审中-公开
标题翻译：通过残留液体重组制备高效液相色谱法的方法
公开(公告)号：WO2008018779A1
公开(公告)日：2008-02-14
申请号：PCT/KR2007/003868
申请日：2007-08-13
申请人： SK CHEMICALS CO., LTD. , KIM, Nam Ho , LEE, Jin Young , KIM, Jae-Sun , LEE, Nam Kyu
发明人： KIM, Nam Ho , LEE, Jin Young , KIM, Jae-Sun , LEE, Nam Kyu
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , Y02P20/582
摘要： The present invention relates to a process for preparing S-(+)-clopidogrel in high yield by means of racemization of filtrate, and particularly to a process comprising (a) conducting an optical resolution by converting racemic carboxylic acid of clopidogrel to diastereomer salt using (+)-cinchonine, (b) preparing carboxylic acid of S-(+)-clopidogrel by extraction using an appropriate solvent under an acidic condition, (c) preparing optically pure S-(+)-clopidogrel by reacting the carboxylic acid of S-(+)-clopidogrel with methanol, wherein a filtrate, which remains after collecting the diastereomer salt as solid precipitates, is recycled after being converted to a racemic carboxylic acid of clopidogrel via racemization under a basic condition, thereby maximizing the yield of S-(+)-clopidogrel.
摘要翻译：本发明涉及通过滤液的外消旋化制备S - （+） - 氯吡格雷的方法，特别涉及一种方法，其包括（a）通过将氯吡格雷的外消旋羧酸转化为非对映体盐进行光学拆分，该方法使用（+） - 辛可宁，（b）通过在酸性条件下使用适当的溶剂进行萃取来制备S - （+） - 氯吡格雷的羧酸，（c）通过使光学纯的S - （+） - 氯吡格雷 S - （+） - 氯吡格雷与甲醇，其中在收集非对映异构体盐作为固体沉淀物后保留的滤液在通过基本条件下通过外消旋化转化为氯吡格雷的外消旋羧酸后被再循环，从而最大化S - （+） - 氯吡格雷。

5. 发明申请

WO2008004796A1 SALTS OF PYRROLOPYRIMIDINONE DERIVATIVES AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：吡咯烷酮衍生物的制备方法及其制备方法
公开(公告)号：WO2008004796A1
公开(公告)日：2008-01-10
申请号：PCT/KR2007/003213
申请日：2007-07-03
申请人： SK CHEMICALS CO., LTD. , KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , LEE, Yoon-Jung , JANG, Woo Jae , YOUN, Won-No , OH, Joon Gyo , SUNG, Jin-Heung , UM, Key An
发明人： KIM, Jae-Sun , KIM, Nam Ho , LEE, Jin Young , LEE, Nam Kyu , LEE, Yoon-Jung , JANG, Woo Jae , YOUN, Won-No , OH, Joon Gyo , SUNG, Jin-Heung , UM, Key An
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to salts of a pyrrolopyrimidinone derivative having superior PDE-5 inhibition activity and a process for preparing the same. More particularly, the present invention relates to a crystalline acid addition salt prepared by reacting a pyrrolopyrimidinone derivative with an acid selected from gentisic acid, maleic acid, citric acid, fumaric acid and tartaric acid. With no hygroscopic property and superior long-term storage stability, photostability and thermal stability, the salts of the pyrrolopyrimidinone derivative are appropriate to be prepared into medications and, with superior PDE-5 inhibition activity, are useful for the treatment and prevention of erectile dysfunction, pulmonary arterial hypertension, chronic obstructive pulmonary disease, benign prostatic hypertrophy and lower urinary tract diseases.
摘要翻译：本发明涉及具有优异的PDE-5抑制活性的吡咯并嘧啶酮衍生物的盐及其制备方法。更具体地，本发明涉及通过使吡咯并嘧啶酮衍生物与选自龙胆酸，马来酸，柠檬酸，富马酸和酒石酸的酸反应制备的结晶酸加成盐。无吸湿性和优异的长期保存稳定性，光稳定性和热稳定性，吡咯并嘧啶酮衍生物的盐适于制备成药物，并且具有优异的PDE-5抑制活性，可用于治疗和预防勃起功能障碍肺动脉高压，慢性阻塞性肺疾病，良性前列腺肥大和下尿路疾病。

6. 发明申请

WO2012036529A3 (S)-N,N-DIMETHYL-3-(NAPHTHALEN-1-YLOXY)-1-PHENYLPROPAN-1-AMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE DERIVATIVES AND MANUFACTURING METHODS THEREOF 审中-公开
公开(公告)号：WO2012036529A3
公开(公告)日：2012-03-22
申请号：PCT/KR2011/006892
申请日：2011-09-16
申请人： SK CHEMICALS CO., LTD. , OH, Jung-Hoon , RYU, Keun-Ho , KIM, Jae-Sun , KIM, Tae Kon , LEE, Soo-Min , LEE, Bong-yong , PARK, Minseok , HONG, Seok Hyun , LEE, Jung A , KIM, Hyuk Min
发明人： OH, Jung-Hoon , RYU, Keun-Ho , KIM, Jae-Sun , KIM, Tae Kon , LEE, Soo-Min , LEE, Bong-yong , PARK, Minseok , HONG, Seok Hyun , LEE, Jung A , KIM, Hyuk Min
IPC分类号： C07F9/10 , A61K31/661 , A61P15/00
摘要： Disclosed are novel dapoxetine derivatives and pharmaceutically acceptable salts thereof. The compounds are soluble in water, stable, and easy to process into preparations. In addition, the compounds exhibit improved dissolution rate and taste. Furthermore, the compounds exhibit a small difference in dissolution rate depending on pH. Further disclosed are pharmaceutical compositions including the compounds. The pharmaceutical compositions are useful for the treatment, management or prevention of premature ejaculation. Methods for preparing the dapoxetine derivatives are also disclosed.

7. 发明申请

WO2009145368A1 IMPROVED PREPARING METHOD OF (S)-OMEPRAZOLE FROM OMEPRAZOLE RACEMATE USING OPTICAL RESOLUTION AGENT 审中-公开
标题翻译：使用光学分解剂改进从奥美拉唑的（S） - 甲基吡咯的制备方法
公开(公告)号：WO2009145368A1
公开(公告)日：2009-12-03
申请号：PCT/KR2008/002961
申请日：2008-05-27
申请人： SK CHEMICALS CO., LTD. , KIM, Jae-Sun , LEE, Jin Young , KIM, Sun Ho , KIM, Nam ho , LEE, Nam Kyu , PARK, Eun Ju , KUM, Do Seung
发明人： KIM, Jae-Sun , LEE, Jin Young , KIM, Sun Ho , KIM, Nam ho , LEE, Nam Kyu , PARK, Eun Ju , KUM, Do Seung
IPC分类号： C07D401/12 , C07D277/30 , A61K31/415 , A61K31/44
CPC分类号： C07D401/12
摘要： The present invention relates to an improved preparing method of ( S )-omeprazole from omeprazole racemate. In an exemplary embodiment, the preparing method according to the present invention comprises the steps of: a) reacting omeprazole racemate with optically active diethyl-D-tartrate and a titanium compound in an alcohol solvent to prepare an omeprazole racemic complex; b) reacting the omeprazole racemic complex with 1.5-3.0 molar equivalents of ( S )-(+)-mandelic acid as optical resolution agent to prepare an optically active ( S )-omeprazole complex; and c) dissociating the optically active ( S) -omeprazole complex with a basic solution to prepare an ( S )-omeprazole free base or reacting the ( S )- omeprazole free base with a metal salt to transfer to a metal salt or a metal salt hydrate of ( S )- omeprazole. With optical purity of 99.0 %ee or better, the ( S )-omeprazole, the metal salt thereof or the hydrate thereof prepared in accordance with the present invention is useful as a medicinal material.
摘要翻译：本发明涉及一种改善奥美拉唑外消旋物（S） - 奥美拉唑的制备方法。在一个示例性实施方案中，根据本发明的制备方法包括以下步骤：a）使奥美拉唑外消旋物与光学活性的D-酒石酸二乙酯和钛化合物在醇溶剂中反应以制备奥美拉唑外消旋体; b）将奥美拉唑外消旋配合物与1.5-3.0摩尔当量的（S） - （+） - 扁桃酸作为光学拆分剂反应，制备光学活性（S） - 奥美拉唑复合物; 和c）用碱性溶液解离光学活性（S） - 奥美拉唑复合物以制备（S） - 奥美拉唑游离碱或使（S） - 奥美拉唑游离碱与金属盐反应转移至金属盐或金属（S） - 奥美拉唑盐水合物。光学纯度为99.0％ee或更好，根据本发明制备的（S） - 奥美拉唑，其金属盐或其水合物可用作药用材料。

8. 发明申请

WO2007074996A1 STABLE PHARMACEUTICAL COMPOSITION CONTAINING S-OMEPRAZOLE AND A METHOD OF MANUFACTURING THE SAME 审中-公开
标题翻译：包含S-奥美拉唑的稳定的药物组合物及其制备方法
公开(公告)号：WO2007074996A1
公开(公告)日：2007-07-05
申请号：PCT/KR2006/005601
申请日：2006-12-20
申请人： SK CHEMICALS CO., LTD. , KIM, Nam Ho , LEE, Jin Young , KIM, Jae-Sun , LEE, Nam Kyu , HWANG, Yong Youn , SHIN, Ho Chul , UM, Key An
发明人： KIM, Nam Ho , LEE, Jin Young , KIM, Jae-Sun , LEE, Nam Kyu , HWANG, Yong Youn , SHIN, Ho Chul , UM, Key An
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K9/2054 , A61K9/4866 , A61K47/6951
摘要： The present invention relates to a stable inclusion complex of S-omeprazole with great storage stabilities and a method for preparing the same. More particularly, it relates to a stable inclusion complex containing S-omeprazole with greater storage stabilities than other conventional pharmaceutical compositions, which is prepared by mixing and stabilizing acid labile S-omeprazole with cyclodextrin and a water-soluble polymer in an aqueous alkaline solution, and a method of its preparation.
摘要翻译：本发明涉及具有良好储存稳定性的S-奥美拉唑稳定的包合物及其制备方法。更具体地说，本发明涉及含有S-奥美拉唑的稳定包合配合物，其比通过将酸不稳定性S-奥美拉唑与环糊精和水溶性聚合物在碱性水溶液中混合稳定而制备的其它常规药物组合物具有更大的储存稳定性，及其制备方法。

9. 发明申请

WO2005058825A1 AMLODIPINE GENTISATE AND A METHOD OF ITS PREPARATION 审中-公开
标题翻译： AMLODIPINE GENTISATE及其制备方法
公开(公告)号：WO2005058825A1
公开(公告)日：2005-06-30
申请号：PCT/KR2004/003309
申请日：2004-12-15
申请人： SK CHEMICALS, CO., LTD. , KIM, Jae-Sun , CHOI, Jin, Young , RYU, Je, Ho , LEE, Nam, Kyu , JANG, jeong-soo , JANG, Woo, Jae , UM, Key, An , KUM, Do, Seung
发明人： KIM, Jae-Sun , CHOI, Jin, Young , RYU, Je, Ho , LEE, Nam, Kyu , JANG, jeong-soo , JANG, Woo, Jae , UM, Key, An , KUM, Do, Seung
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The present invention relates to an acid salt of amlodipine gentisate and a method of its preparation. More particularly, the present invention relates to a crystalline acid salt of amlodipine gentisate of the following formula 1 prepared by reacting amlodipine and gentisic acid, which is useful for the treatment of cardiovascular diseases and has the advantages of low toxicity, excellent stability, improved pharmaceutical efficacies and long-lasting concentration in blood.
摘要翻译：本发明涉及一种氨氯地平龙胆酸的酸性盐及其制备方法。更具体地说，本发明涉及通过使氨氯地平和龙胆酸反应制备的下式1的氨氯地平结晶酸盐，其可用于治疗心血管疾病，并且具有毒性低，稳定性优异的药物血液中的功效和持久的浓度。

10. 发明申请

WO2013129879A1 GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译： GONADOTROPIN释放激素受体拮抗剂，其制备方法和包含其的药物组合物
公开(公告)号：WO2013129879A1
公开(公告)日：2013-09-06
申请号：PCT/KR2013/001660
申请日：2013-02-28
申请人： SK CHEMICALS CO., LTD.
发明人： KIM, Seon-Mi , KIM, Jae-Sun , LEE, Minhee , LEE, So-Young , LEE, Bong-Yong , SHIN, Young Ah , PARK, Euisun , LEE, Jung A , HAN, Min-Young , AHN, Jaeseung , YOO, Taekyung , KIM, Hun-Taek
IPC分类号： C07D491/02 , C07D491/107 , A61K31/527 , A61P35/00
CPC分类号： C07D491/20 , C07D471/10 , C07D491/10
摘要： The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
摘要翻译：本发明提供促性腺激素释放激素受体拮抗剂及其组合物，其可用于预防或治疗性激素相关疾病如子宫内膜异位症，闭经，月经不调，子宫肌瘤，子宫肌瘤，多囊性卵巢疾病，红斑狼疮，肥大症，性早熟，身材矮小，痤疮，脱发，性腺类固醇依赖性肿瘤，促性腺激素产生垂体腺瘤，睡眠呼吸暂停，肠易激综合征，经前期综合征，良性前列腺增生，避孕和不育症，以及阿尔茨海默病疾病。

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