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1. 发明申请

WO2011052940A3 PROCESS FOR PREPARING CLOPIDOGREL HYDROGENSULFATE FORM I 审中-公开
标题翻译：制备氯吡格雷氢过硫酸盐的方法
公开(公告)号：WO2011052940A3
公开(公告)日：2011-10-20
申请号：PCT/KR2010007321
申请日：2010-10-25
申请人： DONG A PHARM CO LTD , KIM MOON-SUNG , YOO MOO-HI , KIM YONG-JIK , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON , SON BYOUNG-HWA , RYU KI-MOON
发明人： KIM MOON-SUNG , YOO MOO-HI , KIM YONG-JIK , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON , SON BYOUNG-HWA , RYU KI-MOON
IPC分类号： C07D495/04 , A61K31/519 , A61P9/10 , C07D495/02
CPC分类号： C07D495/04
摘要： The present invention relates to a process for preparing clopidogrel hydrogensulfate Form I having a large particle size and containing 0.1% or less impurities, and clopidogrel hydrogensulfate Form I produced thereby. The process of the present invention allows a clopidogrel hydrogensulfate Form I to have a pharmaceutically useful particle size and an even spherical form, and to contain 0.1% or less of impurities.
摘要翻译：制备氯吡格雷硫酸氢盐晶型I的方法本发明涉及一种制备氯吡格雷硫酸氢盐晶型I的方法，该方法具有较大的颗粒尺寸并且含有0.1％或更少的杂质，以及由此生产的氯吡格雷硫酸氢盐晶型I。本发明的方法允许硫酸氢氯吡格雷晶型I具有药学上有用的粒径和均匀的球形，并且含有0.1％或更少的杂质。

2. 发明申请

WO2010035985A2 METHOD FOR PRODUCING TAXANE DERIVATIVES 审中-公开
标题翻译：生产紫杉烷衍生物的方法
公开(公告)号：WO2010035985A2
公开(公告)日：2010-04-01
申请号：PCT/KR2009005279
申请日：2009-09-17
申请人： DONG A PHARM CO LTD , KIM MOON-SUNG , YOO MOO-HI , RHEE JAE-KEOL , KIM YONG-JIK , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON , SON BYOUNG-HWA , RYU KI-MOON
发明人： KIM MOON-SUNG , YOO MOO-HI , RHEE JAE-KEOL , KIM YONG-JIK , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON , SON BYOUNG-HWA , RYU KI-MOON
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The present invention relates to a method for producing taxane derivatives with anticancer activity. The method of the present invention produces taxane derivatives in a short time under mild conditions by employing phenyl oxazinan dione compounds which are novel compounds, as a reactant, such that the phenyl oxazinan dione compounds react to baccatin III derivatives.
摘要翻译：本发明涉及生产具有抗癌活性的紫杉烷衍生物的方法。本发明的方法通过使用作为新化合物的苯基恶嗪烷二酮化合物作为反应物，在温和条件下在短时间内产生紫杉烷衍生物，使得苯基恶嗪烷二酮化合物与浆果赤霉素III衍生物反应。

3. 发明申请

WO2009084827A3 SYNTHETIC INTERMEDIATES, PROCESS FOR PREPARING PYRROLYLHEPTANOIC ACID DERIVATIVES THEREFROM 审中-公开
标题翻译：合成中间体，制备吡咯烷酮酸衍生物的方法
公开(公告)号：WO2009084827A3
公开(公告)日：2009-08-27
申请号：PCT/KR2008007350
申请日：2008-12-12
申请人： DONG A PHARM CO LTD , KIM MOON-SUNG , YOO MOO-HI , RHEE JAE-KEOL , KIM YONG-JIK , PARK SEONG-JIN , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON
发明人： KIM MOON-SUNG , YOO MOO-HI , RHEE JAE-KEOL , KIM YONG-JIK , PARK SEONG-JIN , CHOI JUN-HO , SUNG SI-YOUNG , LIM HONG-GYU , CHA DAE-WON
IPC分类号： C07D207/34 , A61P3/06
CPC分类号： C07D207/416
摘要： There are provided intermediates used to prepare a derivative, (3R,5R)-7-[2-(4-fluorphenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-di hydroxyheptanoic acid, which has an effect to suppress cholesterol in blood, and a process for preparing pyrrolylheptanoic acid derivatives therefrom. In accordance with the present invention, the 5-(4-fluorphenyl)-2-isopropyl-4-phenyl-lH-pyrrole-3-carbonyl derivative is provided as one of the novel synthetic intermediates that are used to prepare pyrrolylheptanoic acid derivatives including a derivative, (3R,5R)-7-[2-(4-fluorphenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-di hydroxyheptanoic acid. Therefore, the (3R,5R)-7-[2-(4-fluorphenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-di hydroxyheptanoic acid derivative may be prepared from the carbonyl derivative in a high yield for a short time period under a moderate condition.
摘要翻译：提供用于制备衍生物的中间体（3R，5R）-7- [2-（4-氟苯基）-5-异丙基-3-苯基-4-（苯基氨基甲酰基）-1H-吡咯-1-基] - 具有抑制血液中胆固醇的作用的3,5-二羟基庚酸及其制备吡咯并庚酸衍生物的方法。根据本发明，提供5-（4-氟苯基）-2-异丙基-4-苯基-1H-吡咯-3-羰基衍生物作为用于制备吡咯基庚酸衍生物的新型合成中间体之一，包括衍生物（3R，5R）-7- [2-（4-氟苯基）-5-异丙基-3-苯基-4-（苯基氨基甲酰基）-1H-吡咯-1-基] -3,5-二羟基庚酸。因此，（3R，5R）-7- [2-（4-氟苯基）-5-异丙基-3-苯基-4-（苯基氨基甲酰基）-1H-吡咯-1-基] -3,5-二羟基庚酸衍生物可以在中等条件下以高产率从羰基衍生物制备短时间段。

4. 发明申请

WO2010071320A3 CONTROLLED-RELEASE COMPOSITION FOR PRODUCING SUSTAINED-RELEASE PREPARATION CONTAINING UDENAFIL 审中-公开
标题翻译：用于生产含有UDENAFIL的持续释放制剂的控制释放组合物
公开(公告)号：WO2010071320A3
公开(公告)日：2010-09-30
申请号：PCT/KR2009007382
申请日：2009-12-10
申请人： DONG A PHARM CO LTD , YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , HAN SANG-DUG
发明人： YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , HAN SANG-DUG
IPC分类号： A61K47/48 , A61K9/22 , A61K31/519
CPC分类号： A61K31/519 , A61K9/2031 , A61K9/2054
摘要： The present invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil. More particularly, the present invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil, said composition comprising (A) udenafil and a pharmaceutically acceptable salt, (B) a solubility modulator, (C) an adsorbent, and (D) a hydrophilic polymer. The controlled-release composition for producing a sustained-release preparation containing udenafil according to the present invention releases drugs constantly regardless of the pH level in the gastrointestinal tract, and thus freely controls the drug release time within the range of 3 to 24 hours, and reduces the variability in the effect of drugs among individuals. In addition, the composition of the present invention can be produced into a sustained-release preparation which has an optimum condition for expressing the effect of drugs in the treatment of diseases such as pulmonary arterial hypertension, hepatic portal vein hypertension, benign prostatic hyperplasia, and the like, which can be treated by udenafil and which requires the administration of drugs over a long period of time. Further, the composition of the present invention can control the release of drugs in accordance with the time taken for the absorption thereof when said drugs are applied to a living body, and thus can be valuably used in preventing and treating erectile dysfunction.
摘要翻译：本发明涉及一种用于制备含有乌来萘非缓释制剂的控释组合物。更具体地说，本发明涉及一种用于制备含有乌来啡非的缓释制剂的控释组合物，所述组合物包含（A）胭脂红和药学上可接受的盐，（B）溶解性调节剂，（C）吸附剂，和（D）亲水性聚合物。本发明的含有乌来那非的缓释制剂的控释组合物不管胃肠道的pH值如何，均不断释放药物，因此可以将药物释放时间自由控制在3〜24小时的范围内，降低药物在个体间的作用的变异性。此外，本发明的组合物可以制成缓释制剂，其具有表达药物治疗肺动脉高压，肝门静脉高压，良性前列腺增生等疾病的效果的最佳条件，类似物，可以被乌多那非治疗，需要长时间的药物治疗。此外，本发明的组合物可以在将药物施用于生物体时根据吸收时间来控制药物的释放，因此可以有效地用于预防和治疗勃起功能障碍。

5. 发明申请

WO2010008224A3 FAST-DISSOLVING AMLODIPINE TABLETS OF IMPROVED STABILITY AND A METHOD OF MANUFACTURE THEREOF 审中-公开
标题翻译：改善稳定性的快速溶解的AMLODIPINE片剂及其制造方法
公开(公告)号：WO2010008224A3
公开(公告)日：2010-04-22
申请号：PCT/KR2009003931
申请日：2009-07-16
申请人： DONG A PHARM CO LTD , YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , PARK CHAN-WOONG
发明人： YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , PARK CHAN-WOONG
IPC分类号： A61K9/22 , A61K9/20 , A61K9/28 , A61K31/215 , A61K31/44
CPC分类号： A61K9/0056
摘要： The present invention relates to a method for manufacturing fast-dissolving amlodipine tablets having improved storage stability as a result of containing amlodipine or a pharmaceutically acceptable salt and having physicochemical stability. Fast-dissolving amlodipine tablets manufactured according to the present invention exhibit excellent results when evaluated in terms of appearance, content and impurities, and therefore have sufficient storage stability up to their expiration date, despite amlodipine's characteristic physicochemical instability in the presence of moisture. Said amlodipine tablets dissolve quickly in the mouth with no discomfort.
摘要翻译：本发明涉及由于含有氨氯地平或其药学上可接受的盐并具有物理化学稳定性而具有改善的储存稳定性的快速溶解氨氯地平片剂的方法。尽管在水分存在下氨氯地平特有的物理化学不稳定性，但根据本发明制造的快速溶解氨氯地平片剂在外观，含量和杂质方面评估时表现出优异的结果，并因此具有足够的储存稳定性直至其有效期。所述氨氯地平片在口中迅速溶解而没有不适。

6. 发明申请

WO2010095849A2 ACID ADDITION SALT OF UDENAFIL, PREPARATION METHOD THEREOF AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：醋酸的添加盐，其制备方法和包含其的药物组合物
公开(公告)号：WO2010095849A2
公开(公告)日：2010-08-26
申请号：PCT/KR2010000976
申请日：2010-02-17
申请人： DONG A PHARM CO LTD , LEE CHAN-HO , SHIN CHANG-YONG , CHOI SEUL-MIN , KANG KYUNG-KOO , KIM DONG-SEONG , AHN BYOUNG-OK , YOO MOO-HI
发明人： LEE CHAN-HO , SHIN CHANG-YONG , CHOI SEUL-MIN , KANG KYUNG-KOO , KIM DONG-SEONG , AHN BYOUNG-OK , YOO MOO-HI
IPC分类号： C07D487/04 , C07D487/02
CPC分类号： C07D487/04
摘要： The present invention provides an acid addition salt of Udenafil, a preparation method thereof and a pharmaceutical composition comprising the same. The acid addition salt of Udenafil in which Udenafil is bonded to an organic acid selected from the group consisting of oxalic acid, benzenesulfonic acid, camphorsulfonic acid, cinnamic acid, adipic acid and cyclamic acid, has excellent solubility in an aqueous medium, water stability and crystallinity, thereby being suitably applied for a pharmaceutical composition.
摘要翻译：本发明提供了Udenafil的酸加成盐，其制备方法和包含其的药物组合物。乌代那芬的酸加成盐，其中，阿登奈芬与选自草酸，苯磺酸，樟脑磺酸，肉桂酸，己二酸和环己烷氨基酸的有机酸结合，在水性介质中具有优异的溶解性，水稳定性和结晶度，从而适合用于药物组合物。

7. 发明申请

WO2009107983A3 STABILIZED SINGLE-LIQUID PHARMACEUTICAL COMPOSITION CONTAINING DOCETAXEL 审中-公开
标题翻译：含有多西他赛的稳定的单一液体药物组合物
公开(公告)号：WO2009107983A3
公开(公告)日：2009-12-03
申请号：PCT/KR2009000911
申请日：2009-02-26
申请人： DONG A PHARM CO LTD , YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , WON DONG-HAN
发明人： YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , WON DONG-HAN
IPC分类号： A61K9/08 , A61K31/337 , A61K47/08 , A61P35/00
CPC分类号： A61K9/0019 , A61K47/26
摘要： The present invention relates to a liquid pharmaceutical composition for injection containing docetaxel. The composition of the present invention contains (A) docetaxel and a pharmaceutically acceptable salt, (B) a surface active agent selected from polysorbate, polyoxyethylene glycol ester and polyoxyethylene castor oil derivatives, (C) a solvent containing anhydrous ethanol in the range of concentration of 100 to 800mg/ml in an injection solution, and (D) a pH adjuster of the amount suitable for adjusting pH of the liquid composition to 5 or lower. The composition of the present invention can be directly diluted in a perfusion liquid even without using an intermediary dilute solution in cases where the composition of the present invention is used as injectable preparations as the composition is formed into a single liquid phase. Further, the composition of the present invention is suitable for effective injection of docetaxel as the pharmaceutical stability of the composition is significantly improved.
摘要翻译：本发明涉及含有多西他赛的注射用液体药物组合物。本发明的组合物含有（A）多西紫杉醇及其药学上可接受的盐，（B）选自聚山梨酸酯，聚氧乙烯乙二醇酯和聚氧乙烯蓖麻油衍生物的表面活性剂，（C）含有浓度范围的无水乙醇的溶剂（D）适于将液体组合物的pH调节至5或更低的量的pH调节剂。在本发明的组合物用作可注射制剂的情况下，即使不使用中间稀释溶液，本发明的组合物也可以在灌注液中直接稀释，因为组合物形成单一液相。此外，由于组合物的药物稳定性显着改善，本发明的组合物适合有效注射多西紫杉醇。

8. 发明申请

WO2011059198A3 PHARMACEUTICAL COMPOSITION CONTAINING A BISPHOSPHONATE 审中-公开
标题翻译：含有二磷酸的药物组合物
公开(公告)号：WO2011059198A3
公开(公告)日：2011-10-20
申请号：PCT/KR2010007643
申请日：2010-11-02
申请人： DONG A PHARM CO LTD , YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , LEE JUNG-WOO , RYU DONG-SUNG
发明人： YOO MOO-HI , CHA BONG-JIN , KIM JEONG-HOON , JANG SUN-WOO , LEE JUNG-WOO , RYU DONG-SUNG
IPC分类号： A61K31/663 , A61K9/46 , A61K33/00 , A61K47/36
CPC分类号： A61K31/485 , A61K31/663 , A61K31/7084 , A61K31/734 , A61K45/06 , A61K2300/00
摘要： Provided is a pharmaceutical composition comprising a bisphosphonate having an osteoporosis treating effect, a pH-sensitive macromolecular substance, a foaming agent and a buffering agent. The composition of the present invention imposes no obligatory requirement to take a large amount of water when it is taken, and also has a buffering ability sufficient to keep the pH in the stomach at or above 3.5 after taking, and thus it prevents oesophageal irritation due to gastric reflux and so entails no need to maintain a particular standing posture. Also, even if the pH inside the stomach falls below 3.5 in that portion of patients whose stomach acidity is excessively low, oesophageal irritation due to gastric reflux can be prevented by forming a floating and swelling type of RAFT, and there is a dramatic improvement in convenience of drug taking for patients who take bisphosphonate drugs over the longer term, and there is a foaming effect which extends across two stages.
摘要翻译：本发明提供包含具有骨质疏松症治疗效果的双膦酸盐，pH敏感性高分子物质，发泡剂和缓冲剂的药物组合物。本发明的组合物在使用时不强制需要大量的水，并且具有足以使胃中的pH保持在3.5以上或3.5以上的缓冲能力，因此防止食管刺激胃反流，因此不需要保持特定的站立姿势。此外，即使在胃酸过少的患者中胃内pH值低于3.5，也可以通过形成漂浮型和RAFT型来防止胃反流引起的食管刺激，并且有显着的改善长时间服用双膦酸药物的患者服用方便，并且有两个阶段延伸的起泡作用。

9. 发明申请

WO2009057974A3 NOVEL 1,3-DIHYDRO-5-ISOBENZOFURANCARBONITRILE DERIVATIVES AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF PREMATURE EJACULATION 审中-公开
标题翻译：新型1,3-二氢-5-ISOBENZFURBANITRILE衍生物及其药物组合物，用于治疗预防性呕吐
公开(公告)号：WO2009057974A3
公开(公告)日：2009-07-16
申请号：PCT/KR2008006445
申请日：2008-10-31
申请人： DONG A PHARM CO LTD , LEE YEONG GEON , CHOI SOO-JUNG , KANG TAE-KYUNG , SEO MI-JEONG , SHIN CHANG-YONG , LEE KYUNG-SEOK , AHN GOOK-JUN , CHOI SEUL-MIN , KIM YONG-DUCK , KIM DONG-HWAN , KANG KYUNG-KOO , SHIM HYUN-JOO , KIM DONG-SUNG , AHN BYOUNG-OK , YOO MOO-HI
发明人： LEE YEONG GEON , CHOI SOO-JUNG , KANG TAE-KYUNG , SEO MI-JEONG , SHIN CHANG-YONG , LEE KYUNG-SEOK , AHN GOOK-JUN , CHOI SEUL-MIN , KIM YONG-DUCK , KIM DONG-HWAN , KANG KYUNG-KOO , SHIM HYUN-JOO , KIM DONG-SUNG , AHN BYOUNG-OK , YOO MOO-HI
IPC分类号： C07D307/87
CPC分类号： C07D307/87 , C07D405/06 , C07D409/04 , C07D409/06
摘要： Disclosed herein are novel l,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The l,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half- life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
摘要翻译：本文公开了由式1表示的新的1,3-二氢-5-异苯并呋喃腈衍生物或其药学上可接受的盐。还公开了用于治疗或预防早泄的药物组合物，包括该化合物。 1,3-二氢-5-异苯并呋喃腈衍生物具有短的半衰期，并通过选择性地通过存在于突触前神经元中的5-羟色胺再摄取转运蛋白选择性抑制5-羟色胺再摄取来抑制射精过程。因此，这些化合物可用于治疗和预防早泄。

10. 发明申请

WO2009045019A2 COMPOSITION AND METHOD FOR TREATMENT OR PREVENTION OF BENIGN PROSTATIC HYPERPLASIA AND LOWER URINARY TRACT SYMPTOMS 审中-公开
标题翻译：治疗或预防复发性高血压和下尿路症状的组合物和方法
公开(公告)号：WO2009045019A2
公开(公告)日：2009-04-09
申请号：PCT/KR2008005669
申请日：2008-09-24
申请人： DONG A PHARM CO LTD , CHOI SEUL-MIN , KIM JU-MI , KANG KYUNG-KOO , AHN BYOUNG-OK , YOO MOO-HI
发明人： CHOI SEUL-MIN , KIM JU-MI , KANG KYUNG-KOO , AHN BYOUNG-OK , YOO MOO-HI
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , A61K31/18 , A61K31/405 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a composition and a method for treating or preventing benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) without showing the side effect, by dramatically relaxing the smooth muscle in prostate and bladder.
摘要翻译：本发明涉及通过显着放松前列腺和膀胱平滑肌，治疗或预防良性前列腺增生（BPH）和下尿路症状（LUTS）而不显示副作用的组合物和方法。

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