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1. 发明授权

US08088753B2 Heparin conjugates and methods 失效
标题翻译：肝素共轭物和方法
公开(公告)号：US08088753B2
公开(公告)日：2012-01-03
申请号：US12188138
申请日：2008-08-07
申请人： Youngro Byun , E Sak Lee , Ok-cheol Jeon , Sang Yoon Kim , Rang-Woon Park
发明人： Youngro Byun , E Sak Lee , Ok-cheol Jeon , Sang Yoon Kim , Rang-Woon Park
IPC分类号： A61K31/727 , A61K31/575 , A61K31/50
CPC分类号： A61K31/727 , C08B37/0075 , C08L5/10
摘要： Heparin conjugates and methods of making and use thereof are disclosed. An illustrative heparin conjugate includes a composition wherein a bile acid is bonded to heparin through the 3-carbon of the bile acid. A spacer may be interposed between the bile acid and the heparin. Another embodiment includes a targeting moiety bonded to the heparin-bile acid conjugate through a spacer. Another illustrative heparin conjugate includes heparin covalently bonded to a sulfonated moiety, such as a naphthalene trisulfonate residue. A method of treating cancer includes administering a heparin conjugate to an individual in need thereof.
摘要翻译：公开了肝素缀合物及其制备和使用方法。示例性肝素缀合物包括其中胆汁酸通过胆汁酸的3-碳键合到肝素的组合物。可以在胆汁酸和肝素之间插入间隔物。另一个实施方案包括通过间隔基键合到肝素 - 胆汁酸缀合物的靶向部分。另一个说明性的肝素缀合物包括与磺化部分共价结合的肝素，例如萘三磺酸盐残基。治疗癌症的方法包括向有需要的个体施用肝素缀合物。

2. 发明申请

US20090149424A1 HEPARIN CONJUGATES AND METHODS 失效
标题翻译： HEPARIN结合和方法
公开(公告)号：US20090149424A1
公开(公告)日：2009-06-11
申请号：US12188138
申请日：2008-08-07
申请人： Youngro Byun , E. Sak Lee , Ok-cheol Jeon , Sang Yoon Kim , Rang-Woon Park
发明人： Youngro Byun , E. Sak Lee , Ok-cheol Jeon , Sang Yoon Kim , Rang-Woon Park
IPC分类号： A61K31/727 , C08B37/10 , A61P35/00
CPC分类号： A61K31/727 , C08B37/0075 , C08L5/10
摘要： Heparin conjugates and methods of making and use thereof are disclosed. An illustrative heparin conjugate includes a composition wherein a bile acid is bonded to heparin through the 3-carbon of the bile acid. A spacer may be interposed between the bile acid and the heparin. Another embodiment includes a targeting moiety bonded to the heparin-bile acid conjugate through a spacer. Another illustrative heparin conjugate includes heparin covalently bonded to a sulfonated moiety, such as a naphthalene trisulfonate residue. A method of treating cancer includes administering a heparin conjugate to an individual in need thereof.
摘要翻译：公开了肝素缀合物及其制备和使用方法。示例性肝素缀合物包括其中胆汁酸通过胆汁酸的3-碳键合到肝素的组合物。可以在胆汁酸和肝素之间插入间隔物。另一个实施方案包括通过间隔基键合到肝素 - 胆汁酸缀合物的靶向部分。另一个说明性的肝素缀合物包括与磺化部分共价结合的肝素，例如萘三磺酸盐残基。治疗癌症的方法包括向有需要的个体施用肝素缀合物。

3. 发明申请

US20100021538A1 PHARMACEUTICAL COMPOSITIONS CONTAINING HEPARIN DERIVATIVES 审中-公开
标题翻译：含有HEPARIN衍生物的药物组合物
公开(公告)号：US20100021538A1
公开(公告)日：2010-01-28
申请号：US12414549
申请日：2009-03-30
申请人： Youngro Byun , Jinwoo Park , Ok-Cheol Jeon , Hyun Tae Moon
发明人： Youngro Byun , Jinwoo Park , Ok-Cheol Jeon , Hyun Tae Moon
IPC分类号： A61K9/48 , A61K31/727 , A61K9/00 , A61K9/16 , A61K9/28 , A61P7/04
CPC分类号： A61K9/2054 , A61K9/1641 , A61K9/2018 , A61K9/2846 , A61K9/2866 , A61K31/727 , A61K47/554
摘要： An oral pharmaceutical composition for anticoagulation of blood includes a conjugate of an anticoagulation polysaccharide, such as heparin, covalently bonded to a hydrophobic agent wherein the conjugate is mixed with a solubilizer for inhibiting self-aggregation of the conjugate into nanoparticles. The composition can be coated, formed into tablets, or placed in capsules. Methods of making these oral formulations are also described.
摘要翻译：用于血液抗凝的口服药物组合物包括共价键合到疏水剂的抗凝多糖如肝素的缀合物，其中缀合物与增溶剂混合以抑制缀合物自身聚集成纳米颗粒。组合物可以被包衣，形成片剂，或放在胶囊中。还描述了制备这些口服制剂的方法。

4. 发明申请

US20160144050A1 PRODRUGS ACTIVATED BY CASPASE 有权
标题翻译：由CASPASE启动的PRODRUGS
公开(公告)号：US20160144050A1
公开(公告)日：2016-05-26
申请号：US14796219
申请日：2015-07-10
申请人： Sang-Yoon Kim , Youngro Byun , Seung Woo Chung
发明人： Sang-Yoon Kim , Youngro Byun , Seung Woo Chung
IPC分类号： A61K47/48 , A61B18/02 , A61K38/05 , A61K45/06 , A61K31/65 , A61K31/337
CPC分类号： A61K47/551 , A61B18/02 , A61K31/337 , A61K31/65 , A61K38/14 , A61K45/06 , A61K47/542 , A61K47/545 , A61K47/60 , A61K47/61 , A61K47/643 , A61K47/65 , A61N1/403 , A61N5/062 , A61N7/02 , A61N2005/067 , A61N2007/0004
摘要： Described are prodrug conjugates that release a chemotherapeutic agent upon activation by caspase, and methods using such prodrug conjugates to induce apoptosis, amplify apoptosis, and treat cancer.
摘要翻译：描述了在通过胱天蛋白酶激活时释放化学治疗剂的前药缀合物，以及使用这种前药缀合物诱导凋亡，扩增凋亡和治疗癌症的方法。

5. 发明授权

US07906137B2 Delivery agents for enhancing mucosal absorption of therapeutic agents 有权
标题翻译：用于增强治疗剂的粘膜吸收的递送剂
公开(公告)号：US07906137B2
公开(公告)日：2011-03-15
申请号：US10851477
申请日：2004-05-21
申请人： Youngro Byun , Seulki Lee , Hyuntae Moon
发明人： Youngro Byun , Seulki Lee , Hyuntae Moon
IPC分类号： A61F13/00 , A61K31/21 , A61K9/20 , A01N37/00 , C07J9/00
CPC分类号： A61K9/0095 , A61K9/0053 , A61K38/28 , A61K47/28
摘要： A delivery agent for delivering a biologically active agent to a warm-blooded animal includes a hydrophobic moiety covalently bonded to a hydrophilic moiety. The hydrophobic moiety can include bile acids, sterols, or hydrophobic small molecules. The hydrophilic moiety can include α-amino acids, dipeptides or tripeptides, or hydrophilic small molecules. An illustrative delivery agent is Nα-deoxycholyl-L-lysine-methylester. The delivery agent and the biologically active agent are mixed together to form a complex, which is then administered to the animal. These complexes are particularly useful for oral administration of biologically active agents, but other routes of administration may be used.
摘要翻译：用于将生物活性剂递送至温血动物的递送剂包括与亲水部分共价结合的疏水部分。疏水部分可以包括胆汁酸，甾醇或疏水小分子。亲水部分可包括α-氨基酸，二肽或三肽或亲水性小分子。说明性递送剂是Nα-脱氧胆
基-L-赖氨酸 - 甲酯。将递送剂和生物活性剂混合在一起形成复合物，然后将其施用于动物。这些配合物特别可用于口服给药生物活性剂，但可以使用其它给药途径。

6. 发明授权

US06624141B1 Protamine fragment compositions and methods of use 失效
标题翻译：鱼精蛋白片段组合物和使用方法
公开(公告)号：US06624141B1
公开(公告)日：2003-09-23
申请号：US09700967
申请日：2000-11-16
申请人： Victor C. Yang , Youngro Byun
发明人： Victor C. Yang , Youngro Byun
IPC分类号： A01N3718
CPC分类号： C07K14/46 , A61K38/00 , A61K39/00
摘要： Provided are bioactive, low-toxicity protamine fragments, compositions, combinations, kits and methods of using these components in a variety of embodiments, including neutralizing heparin and reducing post-operative bleeding. Improved protamine fragment-insulin solutions and methods for treating diabetes are also provided.
摘要翻译：提供了在各种实施方案中使用这些组分的生物活性，低毒鱼精蛋白片段，组合物，组合，试剂盒和方法，包括中和肝素和减少术后出血。还提供了改进的鱼精蛋白片段 - 胰岛素溶液和治疗糖尿病的方法。

7. 发明申请

US20050260237A1 Delivery Agents for enhancing mucosal absorption of therapeutic agents 有权
标题翻译：用于增强治疗剂粘膜吸收的递送剂
公开(公告)号：US20050260237A1
公开(公告)日：2005-11-24
申请号：US10851477
申请日：2004-05-21
申请人： Youngro Byun , Seulki Lee
发明人： Youngro Byun , Seulki Lee
IPC分类号： A61K47/22 , A61K9/00 , A61K38/17 , A61K38/22 , A61K38/28 , A61K47/14 , A61K47/28 , A61K47/30 , A61K47/42
CPC分类号： A61K9/0095 , A61K9/0053 , A61K38/28 , A61K47/28
摘要： A delivery agent for delivering a biologically active agent to a warm-blooded animal includes a hydrophobic moiety covalently bonded to a hydrophilic moiety. The hydrophobic moiety can include bile acids, sterols, or hydrophobic small molecules. The hydrophilic moiety can include α-amino acids, dipeptides or tripeptides, or hydrophilic small molecules. An illustrative delivery agent is Nα-deoxycholyl-L-lysine-methylester. The delivery agent and the biologically active agent are mixed together to form a complex, which is then administered to the animal. These complexes are particularly useful for oral administration of biologically active agents, but other routes of administration may be used.
摘要翻译：用于将生物活性剂递送至温血动物的递送剂包括与亲水部分共价结合的疏水部分。疏水部分可以包括胆汁酸，甾醇或疏水小分子。亲水部分可包括α-氨基酸，二肽或三肽或亲水性小分子。说明性递送剂是N，N'-二脱氧胆
基-L-赖氨酸 - 甲酯。将递送剂和生物活性剂混合在一起形成复合物，然后将其施用于动物。这些配合物特别可用于口服给药生物活性剂，但可以使用其它给药途径。

8. 发明授权

US06702850B1 Multi-coated drug-eluting stent for antithrombosis and antirestenosis 失效
标题翻译：用于抗血栓形成和抗再狭窄的多层药物洗脱支架
公开(公告)号：US06702850B1
公开(公告)日：2004-03-09
申请号：US10262432
申请日：2002-09-30
申请人： Youngro Byun , Jung Han Yoon
发明人： Youngro Byun , Jung Han Yoon
IPC分类号： A61F206
CPC分类号： A61L31/10 , A61L31/16 , A61L33/0029 , A61L2300/41 , A61L2300/416 , A61L2300/42 , A61L2420/08
摘要： A stent having a multi-layered coating adhered to its surface which can prevent restenosis and thrombosis at the implant site. The stent coating is comprised of two layers. The first layer is a polymeric coating with one or more biologically active agent(s) dispersed therein. The second layer is comprised of a hydrophobic heparinized polymer that inhibits blood coagulation and provides a hydrophilic surface for reducing the friction between stent and lesion site. In preferred embodiments of the invention, the multi-layered stent is effective in deterring restenosis and thrombosis at the implant site. In these same preferred embodiments, the multi-layered stent is capable of reducing the burst release of the biologically active agents from the first layer and sustaining a release of an effective amount of these agents for a relatively extended period of time. Methods of applying the multi-layered coating to the stent surface are also part of this invention.
摘要翻译：具有粘附到其表面上的多层涂层的支架，其能够防止植入部位的再狭窄和血栓形成。支架涂层由两层组成。第一层是其中分散有一种或多种生物活性剂的聚合物涂层。第二层由抑制血液凝固的疏水性肝素化聚合物组成，并提供亲水性表面以减少支架和病变部位之间的摩擦。在本发明的优选实施方案中，多层支架有效地阻止了植入部位的再狭窄和血栓形成。在这些相同的优选实施方案中，多层支架能够减少生物活性剂从第一层的爆发释放并且在相对延长的时间段内维持有效量的这些试剂的释放。将多层涂层施加到支架表面的方法也是本发明的一部分。

9. 发明申请

US20110237504A1 DELIVERY AGENTS FOR ENHANCING MUCOSAL ABSORPTION OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于增强治疗药物的粘膜吸收的递送剂
公开(公告)号：US20110237504A1
公开(公告)日：2011-09-29
申请号：US13048739
申请日：2011-03-15
申请人： Youngro Byun , Seulki Lee , Hyuntae Moon
发明人： Youngro Byun , Seulki Lee , Hyuntae Moon
IPC分类号： A61K38/28 , C07J41/00 , A61P5/48 , A61K31/727
CPC分类号： A61K9/0095 , A61K9/0053 , A61K38/28 , A61K47/28
摘要： A delivery agent for delivering a biologically active agent to a warm-blooded animal includes a hydrophobic moiety covalently bonded to a hydrophilic moiety. The hydrophobic moiety can include bile acids, sterols, or hydrophobic small molecules. The hydrophilic moiety can include α-amino acids, dipeptides or tripeptides, or hydrophilic small molecules. An illustrative delivery agent is Nα-deoxycholyl-L-lysine-methylester. The delivery agent and the biologically active agent are mixed together to form a complex, which is then administered to the animal. These complexes are particularly useful for oral administration of biologically active agents, but other routes of administration may be used.
摘要翻译：用于将生物活性剂递送至温血动物的递送剂包括与亲水部分共价结合的疏水部分。疏水部分可以包括胆汁酸，甾醇或疏水小分子。亲水部分可包括α-氨基酸，二肽或三肽或亲水性小分子。说明性递送剂是Nα-脱氧胆
基-L-赖氨酸 - 甲酯。将递送剂和生物活性剂混合在一起形成复合物，然后将其施用于动物。这些配合物特别可用于口服给药生物活性剂，但可以使用其它给药途径。

10. 发明授权

US06656922B2 Oral delivery of macromolecules 失效
公开(公告)号：US06656922B2
公开(公告)日：2003-12-02
申请号：US09845827
申请日：2001-04-30
申请人： Youngro Byun , Yong-Kyu Lee
发明人： Youngro Byun , Yong-Kyu Lee
IPC分类号： A61K31727
CPC分类号： C08B37/00 , A61K31/727 , A61K47/542 , A61K47/554 , A61K47/61 , C08B37/0075
摘要： Polysaccharides, which are widely used as an anticoagulation drugs, especially heparin, are clinically administered only by intravenous or subcutaneous injection because of their strong hydrophilicity and high negative charge. Amphiphilic heparin derivatives were synthesized by conjugation to bile acids, sterols, and alkanoic acids, respectively. These heparin derivatives were slightly hydrophobic, exhibited good solubility in water, and have high anticoagulation activity. These slightly hydrophobic heparin derivatives are efficiently absorbed in the gastrointestinal tract and can be used in oral dosage forms. Methods of using these amphiphilic heparin derivatives and similarly modified macromolecules for oral administration are also disclosed.

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