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1. 发明授权

US06602861B1 Acylated phospholipid drugs 失效
标题翻译：酰化磷脂药物
公开(公告)号：US06602861B1
公开(公告)日：2003-08-05
申请号：US07869697
申请日：1992-04-16
申请人： Charles Pidgeon , Robert J. Markovich
发明人： Charles Pidgeon , Robert J. Markovich
IPC分类号： A61K31685
CPC分类号： C07F9/10 , C07F9/117
摘要： This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: or pharmaceutically acceptable salts thereof wherein one of R1 and R2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources; R3 is hydrogen or lower alkyl and R4 is hydrogen, hydrocarbyl containing from 1-18 carbon atoms in a principal chain and up to a total of 23 carbon atoms, said principal chain may contain 1-5 double bonds or 1-2 triple bonds; phenyl which may be unsubstituted or substituted with lower alkyl; naphthyl which may be unsubstituted or substituted with lower alkoxy; or R5ZR6; Z is O or S; R5 and R6 are independently a hydrocarbyl chain containing from 1-18 carbon atoms in the principal chain and up to a total of 23 carbon atoms, said chain may be completely saturated or may contain 1-5 double bonds or 1-2 triple bonds; and the sum of the carbon atoms in R3 and R4 does not exceed 23. This invention also relates to the compounds prepared therefrom as well as the use of the compounds to treat diseases in animals.
摘要翻译：本发明涉及一种提高含有游离羧基的药物效率的方法，其改进包括将所述羧基酯化为具有下式的甘油磷脂酯的甘油部分的羟基：或其药学上可接受的盐，其中， R1和R2是氢，另一个是氢，具有4-26个碳原子的烃基脂肪酸酰基或具有3-25个碳原子的烃基杂原子脂肪酸酰基，或者R是甘油磷脂特征的天然存在的极性头基从内源中分离; R 3是氢或低级烷基，R 4是氢，在主链中含有1-18个碳原子和至多总共23个碳原子的烃基，所述主链可以含有1-5个双键或1- 2个三键; 苯基，其可以是未取代的或被低级烷基取代; 萘基，其可以是未取代的或被低级烷氧基取代; 或R5ZR6; Z为O或S; R5和R6独立地是在主链中含有1-18个碳原子和至多总共23个碳原子的烃基链，所述链可以是完全饱和的或可以含有1-5个双键或1-2个三键; 并且R3和R4中的碳原子的总和不超过23.本发明还涉及由其制备的化合物以及该化合物用于治疗动物疾病的用途。

2. 发明授权

US06576625B2 Targeted vesicular constructs for cytoprotection and treatment of H. pylori infections 失效
公开(公告)号：US06576625B2
公开(公告)日：2003-06-10
申请号：US09809516
申请日：2001-03-16
申请人： Amarjit Singh , Rajesh Jain
发明人： Amarjit Singh , Rajesh Jain
IPC分类号： A61K31685
CPC分类号： A61K9/1271
摘要： A composition for targeted vesicular for treatment of H-Pylori infections and for protection of the cell. The composition contains lectins, phospholipids, sterols, and one or more drugs. The composition is useful for treating H-Pylori infections and other diseases associated therewith and also helps in protecting cell walls.

3. 发明授权

US06306838B1 Targeted vesicular constructs for cyto protection and treatment of h. pylori 失效
标题翻译：用于细胞保护和h处理的靶向囊泡构建体。幽门螺杆菌
公开(公告)号：US06306838B1
公开(公告)日：2001-10-23
申请号：US09490127
申请日：2000-01-24
申请人： Amarjit Singh , Rajesh Jain
发明人： Amarjit Singh , Rajesh Jain
IPC分类号： A61K31685
CPC分类号： A61K9/1271
摘要： A Novel Composition for targeted vesicular for treatment of H-Pylori infections and for protection of the cell is disclosed. The Composition Comprises Lectins, Phospholipids sterols an one or more drugs. The Composition is useful since not only it treats H-Pylori infections and other diseases associated therewith but also helps in protection of the cell walls.
摘要翻译：公开了用于治疗幽门螺杆菌感染和保护细胞的靶向囊泡的新型组合物。组合物包含凝胶素，磷脂甾醇一种或多种药物。该组合物是有用的，因为它不仅治疗H-Pylori感染和与其相关的其它疾病，而且还有助于保护细胞壁。

4. 发明授权

US06191121B1 Treatment of skin damage using polyenylphosphatidylcholine 有权
标题翻译：使用聚烯基磷脂酰胆碱治疗皮肤损伤
公开(公告)号：US06191121B1
公开(公告)日：2001-02-20
申请号：US09543947
申请日：2000-04-06
申请人： Nicholas V. Perricone
发明人： Nicholas V. Perricone
IPC分类号： A61K31685
CPC分类号： A61Q19/007 , A61K8/553 , A61K31/685 , A61Q19/00 , A61Q19/08
摘要： Polyenylphosphatidylcholine is topically applied to treat skin damage, such as contact dermatitis (particularly diaper area dermatitis), atopic dermatitis, xerosis, eczema (including severe hand and foot eczema), rosacea, seborrhea, psoriasis, thermal and radiation burns, other types of skin inflammation, and aging. Typical compositions contain from about 0.25% to about 10% of a polyenylphosphatidylcholine preparation obtained from natural sources such as soybean oil which contains at least about 25% by weight, preferably about 40% or more, dilinoeoylphosphatidylcholine.
摘要翻译：多烯基磷脂酰胆碱局部应用于治疗皮肤损伤，如接触性皮炎（特别是尿布区皮炎），特应性皮炎，干燥症，湿疹（包括严重的手脚湿疹），酒渣鼻，皮脂溢，银屑病，热和放射性灼伤，其他类型的皮肤炎症和衰老。典型的组合物含有约0.25％至约10％的天然来源的多烯基磷脂酰胆碱制剂，例如含有至少约25重量％，优选约40重量％或更多的二磷酸基磷脂酰胆碱的大豆油。

5. 发明授权

US06500810B2 Method of regulating expression of adhesion molecules on circulating leukocytes 失效
标题翻译：调节循环白细胞粘附分子表达的方法
公开(公告)号：US06500810B2
公开(公告)日：2002-12-31
申请号：US09738411
申请日：2000-12-14
申请人： Allan M. Lefer , J. Graham Goddard
发明人： Allan M. Lefer , J. Graham Goddard
IPC分类号： A61K31685
CPC分类号： A61K31/661 , A61K31/00 , A61K31/66 , A61K31/683 , A61K31/685 , A61K45/06 , A61K2300/00
摘要： A method to inhibit inflammation in a mammal is disclosed. The method includes administering to the mammal a composition comprising a phospholipid, which can be lysophosphatidic acid. The administration of a phospholipid is believed to down regulate expression of adhesion molecules on the surface of vascular endothelial cells and circulating leukocytes of the mammal.
摘要翻译：公开了抑制哺乳动物炎症的方法。该方法包括向哺乳动物施用包含磷脂的组合物，其可以是溶血磷脂酸。据信磷脂的施用可以下调哺乳动物血管内皮细胞和循环白细胞表面的粘附分子的表达。

6. 发明授权

US06329352B1 Method and composition for treating sleep apnea 失效
标题翻译：治疗睡眠呼吸暂停的方法和组成
公开(公告)号：US06329352B1
公开(公告)日：2001-12-11
申请号：US09313110
申请日：1999-05-17
申请人： Keith C. Meyer , M. Safwan Badr
发明人： Keith C. Meyer , M. Safwan Badr
IPC分类号： A61K31685
CPC分类号： A61K31/685 , A61K9/006 , A61K38/1709
摘要： Application of synthetic or naturally occurring lung surfactant to the posterior pharyngeal region prior to a period of sleep significantly reduces episodes of sleep disturbance resulting in apnea or hypopnea. The present invention provides lung surfactant in a convenient applicator container for easy use and storage. Incidents of oxygen desaturation are reduced, thereby lowering the risks of apnea-associated pathologies.
摘要翻译：合成或天然存在的肺表面活性剂在睡眠期之前对后咽部区域的应用显着减少了导致呼吸暂停或呼吸不足的睡眠障碍。本发明在方便的施用容器中提供肺表面活性剂，便于使用和储存。氧饱和度降低的事件减少，从而降低呼吸暂停相关病变的风险。

7. 发明授权

US06316428B1 Topical moisturizing composition and method 失效
标题翻译：局部保湿成分及方法
公开(公告)号：US06316428B1
公开(公告)日：2001-11-13
申请号：US09383779
申请日：1999-08-26
申请人： Wilson Trafton Crandall
发明人： Wilson Trafton Crandall
IPC分类号： A61K31685
CPC分类号： A61K8/671 , A61K8/0291 , A61K8/365 , A61K8/37 , A61K8/46 , A61K8/4913 , A61K8/553 , A61K8/60 , A61K8/63 , A61K8/676 , A61K8/678 , A61K8/90 , A61Q3/00 , A61Q5/00 , A61Q19/00 , A61Q19/005 , A61Q19/08 , Y10S514/847 , Y10S514/861 , Y10S514/936 , Y10S514/937 , Y10S514/944
摘要： The present invention comprises methods and compositions for topically treating and moisturizing keratinous structures of humans and animals including skin, hair, fingernails, toenails, hooves, and horns.
摘要翻译：本发明包括用于局部治疗和保湿包括皮肤，毛发，指甲，脚趾甲，蹄和角在内的人和动物的角蛋白结构的方法和组合物。

8. 发明授权

US06248728B1 Phosphatidylcholine compositions and methods for lowering intestinal absorption and plasma levels of cholesterol 失效
标题翻译：磷脂酰胆碱组合物和降低胆汁吸收和血浆胆固醇水平的方法
公开(公告)号：US06248728B1
公开(公告)日：2001-06-19
申请号：US09523042
申请日：2000-03-10
申请人： Sung I. Koo
发明人： Sung I. Koo
IPC分类号： A61K31685
CPC分类号： A61K31/685
摘要： A method and composition for reducing the intestinal absorption of cholesterol in humans or animals are provided. Broadly, the methods comprise ingesting a composition (or a food product including the composition) comprising a substituted phosphatidylcholine compound, or comprising sufficient quantities of a phosphatidylcholine compound to provide from about 20-70% by weight of C18 or higher alkyl groups. Preferred substituted phosphatidylcholine compounds include monoether phosphatidylcholines, diether phosphatidylcholines (wherein the alkyl group bonded to the second carbon atom of the glycerol moiety is a C17 or higher alkyl group), or ester or diester phosphatidylcholines. Preferred C18 or higher alkyl groups include C18-C22 alkyl groups, preferably bonded to the second carbon atom of the glycerol moiety of the phosphatidylcholine compound.
摘要翻译：提供了减少人或动物胆固醇肠吸收的方法和组合物。广泛地，该方法包括摄取包含取代的磷脂酰胆碱化合物的组合物（或包含组合物的食品），或包含足够量的磷脂酰胆碱化合物，以提供约20-70重量％的C 18或更高级烷基。优选的取代的磷脂酰胆碱化合物包括单醚磷脂酰胆碱，二醚磷脂酰胆碱（其中与甘油部分的第二个碳原子键合的烷基是C17或更高级的烷基）或酯或二酯磷脂酰胆碱。优选的C18或更高级烷基包括优选与磷脂酰胆碱化合物的甘油部分的第二个碳原子键合的C18-C22烷基。

9. 发明授权

US06576624B1 Use of dopamine receptor antagonists in palliative tumor therapy 失效
公开(公告)号：US06576624B1
公开(公告)日：2003-06-10
申请号：US09599561
申请日：2000-06-23
申请人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jürgen Engel
发明人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jürgen Engel
IPC分类号： A61K31685
CPC分类号： A61K31/685 , A61K31/454 , A61K2300/00
摘要： The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

10. 发明授权

US06525034B2 Clear personal care formulations containing quaternary ammonium compounds and other nitrogen-containing compounds 有权
标题翻译：含有季铵化合物和其他含氮化合物的清洁个人护理制剂
公开(公告)号：US06525034B2
公开(公告)日：2003-02-25
申请号：US10001123
申请日：2001-10-19
申请人： Damon M. Dalrymple , Mona Manning , Frank Merz
发明人： Damon M. Dalrymple , Mona Manning , Frank Merz
IPC分类号： A61K31685
CPC分类号： A61K8/42 , A61K8/442 , A61K8/463 , A61K8/466 , A61K2800/596 , A61Q5/02 , A61Q5/12
摘要： A composition formulated from a primary anionic surfactant; optionally a secondary surfactant and/or a resin; and a nitrogen-containing compound of the structural formula: wherein R is a saturated, linear, branched or cyclic alkyl or aryl group containing 12 to 22 carbon atoms, with the proviso that R contains at least 80% of a single chain length and R is not lanolin, wheat germ or other natural broad-based chain distribution oil, R1 is a saturated or unsaturated, linear, branched or cyclic alkyl or aryl group containing 1 to 6 carbon atoms and may contain one or more hydroxyl groups, R2 is selected from the group consisting of hydrogen, methyl, ethyl and benzyl; and A− is a monovalent anion.
摘要翻译：由初级阴离子表面活性剂配制的组合物; 任选的第二表面活性剂和/或树脂; 和具有以下结构式的含氮化合物：其中R是含有12-22个碳原子的饱和，直链，支链或环状烷基或芳基，条件是R含有至少80％的单链长度，R 不是羊毛脂，小麦胚芽或其他天然宽链型分配油，R1是含有1至6个碳原子的饱和或不饱和的直链，支链或环状的烷基或芳基，并且可以含有一个或多个羟基，选择R 2 由氢，甲基，乙基和苄基组成的组; 而A-是一价阴离子。

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