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1. 发明申请

WO2022155037A1 HETEROCYCLIC P2Y 14 RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2022155037A1
公开(公告)日：2022-07-21
申请号：PCT/US2022/011226
申请日：2022-01-05
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , JUNG, Young-Hwan , WEN, Zhiwei
发明人： JACOBSON, Kenneth A. , JUNG, Young-Hwan , WEN, Zhiwei
IPC分类号： C07D211/18 , C07D249/06 , C07D205/04 , C07D209/02 , C07D211/34 , C07D211/70 , C07D223/04 , C07D255/02 , C07D261/08 , C07D403/10 , A61P29/00 , A61P25/00 , A61P3/10 , A61K31/4192 , A61K31/44
摘要： Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R1‑R8, X, Y, Z, X', Y', Z', and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

2. 发明申请

WO2005102284A1 PROTEIN-CONTAINING LIPID IMPLANT FOR SUSTAINED DELIVERY AND ITS PREPARATION METHOD 审中-公开
标题翻译：含蛋白质的脂肪植入物及其制备方法
公开(公告)号：WO2005102284A1
公开(公告)日：2005-11-03
申请号：PCT/KR2005/001111
申请日：2005-04-19
申请人： PEPTRON CO., LTD , LEE, Hee Yong , KIM, Sung Kyu , KIM, Jung Soo , JUNG, Young Hwan , KIM, Jung In , SEO, Yun Mi , LEE, Ji Suk , SEOL, Eun Young , CHANG, Seung Gu , CHOI, Ho Il
发明人： LEE, Hee Yong , KIM, Sung Kyu , KIM, Jung Soo , JUNG, Young Hwan , KIM, Jung In , SEO, Yun Mi , LEE, Ji Suk , SEOL, Eun Young , CHANG, Seung Gu , CHOI, Ho Il
IPC分类号： A61K9/16
CPC分类号： A61K9/0024 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2013 , A61K9/2077
摘要： Disclosed are a protein-containing lipid implant for sustained delivery, which comprises a compressed mixture of a protein drug coated with a hydrophilic polymer and a lipid, and a method of preparing the lipid implant. The protein-containing lipid implant for sustained delivery sustains the in vivo release of a protein drug in an active state for a long period of time because the protein drug is evenly distributed in a lipid matrix in a stable state, and thus maintains constant serum levels of the protein drug. Thus, the lipid implant is capable of effectively treating diseases and reducing injection frequency.
摘要翻译：公开了一种用于持续递送的含蛋白质的脂质植入物，其包含涂覆有亲水性聚合物和脂质的蛋白质药物的压缩混合物，以及制备脂质植入物的方法。用于持续释放的含蛋白质的脂质植入物长时间维持活性状态的蛋白质药物的体内释放，因为蛋白质药物在稳定状态下均匀分布在脂质基质中，因此保持恒定的血清水平的蛋白质药物。因此，脂质植入物能够有效治疗疾病并降低注射频率。

3. 发明申请

WO2003087047A1 METAL CHELATE COMPOSITION, MACROMOLECULE COMPLEX THEREOF, PREPARING METHOD THEREOF AND USE 审中-公开
标题翻译：金属螯合物组合物，其分子复合物，其制备方法和用途
公开(公告)号：WO2003087047A1
公开(公告)日：2003-10-23
申请号：PCT/KR2002/000948
申请日：2002-05-20
申请人： PEPTRON CO., LTD. , KIM, Seong-Kyu , CHOI, Ho-Il , JUNG, Young-Hwan , LIM, Chae-Jin
发明人： KIM, Seong-Kyu , CHOI, Ho-Il , JUNG, Young-Hwan , LIM, Chae-Jin
IPC分类号： C07C323/23
CPC分类号： C07C323/58 , B01J45/00
摘要： The present invention provides a novel metal chelate composition and its macromolecule complex. The invention also provides a preparation method of the metal chelate composition and method of using the metal chelate composition in purifying substance like peptide. The metal chelate composition of the present invention is expressed by the formula HS-R.sub.1 -CH(COOH)-N-(CH.sub.2 COOH).sub.2 (wherein R.sub.1 represents alkyl group linker having 1∼5 carbon atoms), and exhibits sufficient affinity and stability on the substance to be purified by simple process.
摘要翻译：本发明提供了一种新型金属螯合物组合物及其大分子复合物。本发明还提供了金属螯合物组合物的制备方法以及使用金属螯合物组合物来纯化物质如肽的方法。本发明的金属螯合物组合物由式HS-R表示-CH（COOH）-N-（CH 2 COOH）2（其中R 1表示烷基具有1〜5个碳原子的连接体），并且通过简单的方法对待纯化的物质表现出足够的亲和力和稳定性。

4. 发明申请

WO2019157417A1 HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2019157417A1
公开(公告)日：2019-08-15
申请号：PCT/US2019/017422
申请日：2019-02-11
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , JACOBSON, Kenneth A. , YU, Jinha , CIANCETTA, Antonella , WEN, Zhiwei , JUNG, Young-Hwan
发明人： JACOBSON, Kenneth A. , YU, Jinha , CIANCETTA, Antonella , WEN, Zhiwei , JUNG, Young-Hwan
IPC分类号： C07D235/18 , A61K31/439 , A61K31/44 , C07D403/04 , C07D409/10 , C07D249/06 , C07D471/08 , C07D209/10 , C07D211/18 , C07D211/70 , A61P29/00 , A61P13/12 , A61P11/06
摘要： Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y 14 R receptor agonist in a mammal in need thereof, wherein R 1 -R 8 , X, Y, Z, X', Y', Z', and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

5. 发明申请

WO2003094887A1 SUSTAINED RELEASE FORMULATION OF PROTEIN AND PREPARATION METHOD THEREOF 审中-公开
标题翻译：持续释放蛋白质的配制及其制备方法
公开(公告)号：WO2003094887A1
公开(公告)日：2003-11-20
申请号：PCT/KR2003/000921
申请日：2003-05-09
申请人： PEPTRON CO., LTD , LEE, Hee-Yong , KIM, Jung-Soo , LEE, Ji-Suk , KIM, Jung-In , SEO, Yun-Mi , LIM, Chae-Jin , KIM, Sung-Kyu , JUNG, Young-Hwan , CHANG, Seung-Gu , CHOI, Ho-Il
发明人： LEE, Hee-Yong , KIM, Jung-Soo , LEE, Ji-Suk , KIM, Jung-In , SEO, Yun-Mi , LIM, Chae-Jin , KIM, Sung-Kyu , JUNG, Young-Hwan , CHANG, Seung-Gu , CHOI, Ho-Il
IPC分类号： A61K9/00
CPC分类号： A61K9/1617 , A61K9/1652
摘要： The present invention relates to a sustained release formulation comprising protein as an active ingredient, and a preparation method thereof. According to the present invention, the sustained release formulation contains protein drugs that are encapsulated in biodegradable hydrophobic matrices as pharmaceutically active forms by forming complexes with sulfated polysaccharides. The sustained release formulation prepared by the present invention can be used to effectively treat a disease without frequent injections by keeping the protein concentration at a sufficiently high level for a long period when injected in vivo once.
摘要翻译：本发明涉及包含蛋白质作为活性成分的缓释制剂及其制备方法。根据本发明，持续释放制剂含有通过与硫酸化多糖形成复合物而包封在可生物降解的疏水基质中作为药物活性形式的蛋白质药物。通过本发明制备的持续释放制剂可以用于通过在体内注射一次时将蛋白质浓度保持在足够高的水平长时间来有效地治疗疾病而不经常注射。

6. 发明申请

WO2009064082A1 COMPOSITION COMPRISING GALLA RHOIS EXTRACT FOR PREVENTION AND TREATMENT OF OBESITY BY MEANS OF AUTOPHAGIC MECHANISM 审中-公开
标题翻译：包含GALLA RHOIS提取物的组合物，用于通过自动机械手段预防和治疗肥胖
公开(公告)号：WO2009064082A1
公开(公告)日：2009-05-22
申请号：PCT/KR2008/006294
申请日：2008-10-24
申请人： IGSBIO , KANG, Se Chan , CHOI, Han , CHEONG, Young Jun , JUNG, Young Hwan , KIM, Hee Jeong , SON, Eun Hwa
发明人： KANG, Se Chan , CHOI, Han , CHEONG, Young Jun , JUNG, Young Hwan , KIM, Hee Jeong , SON, Eun Hwa
IPC分类号： A61K36/22 , A61K31/351 , A61P3/00 , A61K31/70
CPC分类号： A61K36/22 , A61K31/351 , A61K31/70
摘要： The present invention relates to a composition comprising a Galla Rhois extract for the prevention and treatment of obesity based on the mechanism of autophagocytosis. In particular, the present invention has found that the Galla Rhois extract or fraction thereof exhibits inhibitory effects on the proliferation of adipocytes by inducing autophagocytosis thereof, and therefore, provides a method of isolating active ingredients capable of being used as a composition for the prevention and treatment of obesity from Galla Rhois, and a composition for the prevention and treatment of obesity which comprises a Galla Rhois extract or a fraction thereof. That is, the Galla Rhois extract according to the present invention exerts beneficial activities of inducing autophagocytosis of adipocytes in vitro, inhibiting body weight gain in an obesity-induced animal model, reducing the body weight of a body weight gain-induced animal model, and lowering the levels of triglycerides and low density lipoproteins in the blood. Therefore, the Galla Rhois extract according to the present invention can be effectively used as a pharmaceutical composition and health foods for the prevention of obesity and complications thereof and treating the same.
摘要翻译：本发明涉及一种包含根据自噬作用机理预防和治疗肥胖症的加洛氏提取物的组合物。特别地，本发明已经发现，加洛氏提取物或其部分通过诱导其自身吞噬作用而对脂肪细胞的增殖表现出抑制作用，因此，提供了分离能够用作预防和/或免疫的组合物的活性成分的方法治疗来自Galla Rhois的肥胖症，以及用于预防和治疗肥胖症的组合物，其包含加利罗非鱼提取物或其一部分。也就是说，根据本发明的加拉罗氏菌提取物在体外发挥诱导脂肪细胞的自噬作用的有益活性，抑制肥胖诱导的动物模型中的体重增加，减轻体重增加诱导的动物模型的体重，以及降低血液中甘油三酸酯和低密度脂蛋白的含量。因此，根据本发明的加拉罗氏菌提取物可以有效地用作药物组合物和用于预防肥胖及其并发症并进行治疗的保健食品。

7. 发明申请

WO2005023224A1 PREPARATION METHOD FOR SUSTAINED RELEASE MICROSPHERES USING A DUAL-FEED NOZZLE 审中-公开
标题翻译：使用双向喷嘴的持续释放微球的制备方法
公开(公告)号：WO2005023224A1
公开(公告)日：2005-03-17
申请号：PCT/KR2004/002241
申请日：2004-09-03
申请人： PEPTRON CO., LTD , LEE, Hee Yong , JUNG, Young Hwan , KIM, Jung In , KIM, Sung Kyu , KIM, Jung Soo , CHANG, Seung Gu , PARK, Kee Don , CHOI, Ho Il
发明人： LEE, Hee Yong , JUNG, Young Hwan , KIM, Jung In , KIM, Sung Kyu , KIM, Jung Soo , CHANG, Seung Gu , PARK, Kee Don , CHOI, Ho Il
IPC分类号： A61K9/16
CPC分类号： A61K9/1647 , A61K9/1682 , A61K9/1694 , A61K38/09
摘要： Disclosed is a method of preparing sustained release microspheres by spray-drying liquids with different compositions for preparation the sustained release microspheres through an ultrasonic dual-feed nozzle. Unlike conventional methods of preparing sustained release microspheres by spray-drying a single liquid containing a biodegradable polymer, a drug, an additive and a solvent through a single-feed nozzle, the present method is characterized by simultaneously spray-drying two liquids with different compositions for preparation of the sustained release microspheres respectively through internal and external channels of an ultrasonic dual-feed nozzle to coat sprayed droplets through the internal channel with other sprayed droplets through the external channel. The present method is effective in achieving a low initial release and a desired continuous release.
摘要翻译：公开了一种通过喷雾干燥具有不同组成的液体制备缓释微球的方法，用于通过超声波双重给料喷嘴制备缓释微球。与通过单一进料喷嘴喷雾干燥含有可生物降解的聚合物，药物，添加剂和溶剂的单一液体制备缓释微球体的常规方法不同，本方法的特征在于同时喷雾干燥具有不同组成的两种液体分别通过超声双馈喷嘴的内部和外部通道制备缓释微球，通过内部通道将喷雾的液滴通过外部通道与其他喷雾液滴一起涂覆。本发明的方法在实现低的初始释放和期望的连续释放方面是有效的。

8. 发明申请

WO2004112752A1 METHOD OF PREPARING MIXED FORMULATION OF SUSTAINED RELEASE MICROSPHERES BY CONTINUOUS ONE-STEP PROCESS 审中-公开
标题翻译：通过连续一步法制备可持续释放微生物的混合配方的方法
公开(公告)号：WO2004112752A1
公开(公告)日：2004-12-29
申请号：PCT/KR2004/001558
申请日：2004-06-25
申请人： PEPTRON CO., LTD , LEE, Hee Yong , KIM, Sung Kyu , KIM, Jung Soo , LEE, Ji Suk , JUNG, Young Hwan , KIM, Jung In , SEO, Yun Mi , CHANG, Seung Gu , PARK, Kee Don , CHOI, Ho Il
发明人： LEE, Hee Yong , KIM, Sung Kyu , KIM, Jung Soo , LEE, Ji Suk , JUNG, Young Hwan , KIM, Jung In , SEO, Yun Mi , CHANG, Seung Gu , PARK, Kee Don , CHOI, Ho Il
IPC分类号： A61K9/16
CPC分类号： A61K9/1694 , A61K9/1647 , A61K9/5084 , A61K38/24
摘要： Disclosed is a method for preparing a mixed formulation of sustained release microspheres with various compositions by a continuous one-step process. The present method is characterized by preparing the mixed formulation of sustained release microspheres with different compositions by a continuous one-step process by continuously introducing the mixed fluids into a dryer from the two or more different fluids for preparation of sustained release microspheres containing a biodegradable polymer, a drug, an additive and a solvent with different types of contents or both of the components, by controlling the mixing ratios of the fluids according to the time, unlike a conventional method including spray-drying a mixture of microspheres containing a biodegradable polymer, a drug, an additive and a solvent with a single composition. The present method can achieve a desired drug release, which is difficult to be obtained by conventional microspheres with a single composition, by preparing microspheres by a continuous one-step process, and can simplify the conventional complex process of separately preparing several microsphere formulations and then mixing the formulations at a proper ratio to achieve a desired drug release.
摘要翻译：公开了通过连续一步法制备具有各种组成的缓释微球混合制剂的方法。本发明的方法的特征在于通过连续一步法制备具有不同组成的缓释微球的混合制剂，通过从两种或更多种不同的流体连续引入混合流体到干燥器中，用于制备含有可生物降解聚合物的缓释微球，药物，添加剂和具有不同类型含量的溶剂或两种组分的溶剂通过控制流体的混合比而不同于常规方法，包括喷雾干燥含有可生物降解的聚合物的微球体的混合物，药物，添加剂和具有单一组成的溶剂。本发明方法可以通过连续一步法制备微球，实现通过具有单一组成的常规微球难以获得的所需药物释放，并且可以简化分别制备几种微球制剂的常规复合方法，然后以适当的比例混合制剂以实现期望的药物释放。

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