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1. 发明授权

US5565439A Methods of using lysophosphatidic acid for treating hyperproliferative conditions 失效
标题翻译：使用溶血磷脂酸治疗过度增殖症状的方法
公开(公告)号：US5565439A
公开(公告)日：1996-10-15
申请号：US334888
申请日：1994-11-04
申请人： Gary A. Piazza , Adam W. Mazur
发明人： Gary A. Piazza , Adam W. Mazur
IPC分类号： A61K31/665 , A61K31/66
CPC分类号： A61K31/661 , A61K31/662 , A61K31/665 , Y10S514/859 , Y10S514/88
摘要： The subject invention involves a method for treating hyperproliferative conditions in mammalian epithelial cells comprising administering to the mammal a composition containing a safe and effective amount of a lysophosphatidic acid compound or derivative having the structure ##STR1## or a cyclic derivative thereof having the structure ##STR2## or a pharmaceutically acceptable salt thereof, wherein: a) --Y-- is --0-- or --CH.sub.2 --;b) --Z is --XH, --H or halo;c) each --X-- is independently --0-- or --S--; andd) --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 11 to about 23 carbon atoms.
摘要翻译：本发明涉及一种用于治疗哺乳动物上皮细胞中过度增殖病症的方法，其包括向哺乳动物施用含有安全有效量的具有结构为“IMAGE”的结构为“IMAGE”或其环状衍生物的抗凝血磷酸化合物或其衍生物的组合物或其药学上可接受的盐，其中：a）-Y-是-O-或-CH 2 - ; b）-Z是-XH，-H或卤素; c）每个-X-独立地为-O-或-S-; 和d）-R是未取代或取代的饱和或不饱和的具有11至约23个碳原子的直链或支链烷基。

2. 发明授权

US5238965A Methods of using lysophosphatidic acids for regulating skin wrinkles 失效
标题翻译：使用水溶性脂肪酸调节皮肤皱纹的方法
公开(公告)号：US5238965A
公开(公告)日：1993-08-24
申请号：US708270
申请日：1991-05-31
申请人： Gary A. Piazza , Adam W. Mazur
发明人： Gary A. Piazza , Adam W. Mazur
IPC分类号： A61K8/55 , A61K31/66 , A61K31/665 , A61Q17/04 , A61Q19/00 , A61Q19/08
CPC分类号： A61Q19/08 , A61K31/66 , A61K31/665 , A61K8/553 , A61Q17/04 , Y10S424/05 , Y10S514/836 , Y10S514/844 , Y10S514/846 , Y10S514/847 , Y10S514/873 , Y10S514/886 , Y10S514/887 , Y10S514/937 , Y10S514/938 , Y10S514/944 , Y10S514/946 , Y10S514/947 , Y10S514/96 , Y10S514/969
摘要： The subject invention relates to methods for regulating wrinkles in mammalian skin comprising topical application of a lysophosphatidic acid compound having the structure: ##STR1## or a cyclic derivative thereof having the structure: ##STR2## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 12 to about 23 carbon atoms; each --X-- is independently --O-- or --S--; and --Y-- is --O-- or --CH.sub.2 --.
摘要翻译：本发明涉及用于调节哺乳动物皮肤中的皱纹的方法，其包括局部施用具有以下结构的溶血磷脂酸化合物：其具有下列结构的化合物或其药学上可接受的盐：其中-R为未取代或取代的饱和或不饱和的具有12至约23个碳原子的直链或支链烷基; 每个-X-独立地是-O-或-S-; 和-Y-是-O-或-CH2-。

3. 发明授权

US5521223A Methods of using lysophosphatidic acids for regulating skin wrinkles 失效
标题翻译：使用溶血磷脂酸调节皮肤皱纹的方法
公开(公告)号：US5521223A
公开(公告)日：1996-05-28
申请号：US61660
申请日：1993-05-13
申请人： Gary A. Piazza , Adam W. Mazur
发明人： Gary A. Piazza , Adam W. Mazur
IPC分类号： A61K8/55 , A61K31/66 , A61K31/665 , A61Q17/04 , A61Q19/00 , A61Q19/08 , A61K7/42 , A61K7/48 , A61K9/10 , C11D3/48
CPC分类号： A61Q19/08 , A61K31/66 , A61K31/665 , A61K8/553 , A61Q17/04 , Y10S424/05 , Y10S514/836 , Y10S514/844 , Y10S514/846 , Y10S514/847 , Y10S514/873 , Y10S514/886 , Y10S514/887 , Y10S514/937 , Y10S514/938 , Y10S514/944 , Y10S514/946 , Y10S514/947 , Y10S514/96 , Y10S514/969
摘要： The subject invention relates to methods for regulating wrinkles in mammalian skin comprising topical application of a lysophosphatidic acid compound having the structure: ##STR1## or a cyclic derivative thereof having the structure: ##STR2## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 12 to about 23 carbon atoms; each --X-- is independently --O-- or --S--; and --Y-- is --O-- or --CH.sub.2 --.
摘要翻译：本发明涉及用于调节哺乳动物皮肤中的皱纹的方法，其包括局部施用具有以下结构的溶血磷脂酸化合物：其具有下列结构的化合物或其药学上可接受的盐：其中-R为未取代或取代的饱和或不饱和的具有12至约23个碳原子的直链或支链烷基; 每个-X-独立地是-O-或-S-; 和-Y-是-O-或-CH2-。

4. 发明授权

US5340568A Topical composition and method containing deoxy and halo derivatives of lysophosphatidic acids for regulating skin wrinkles 失效
标题翻译：含有用于调节皮肤皱纹的溶血磷脂酸的脱氧和卤代衍生物的局部组合物和方法
公开(公告)号：US5340568A
公开(公告)日：1994-08-23
申请号：US907265
申请日：1992-07-01
申请人： Gary A. Piazza , Adam W. Mazur , Gerald B. Kasting
发明人： Gary A. Piazza , Adam W. Mazur , Gerald B. Kasting
IPC分类号： A61K8/37 , A61K8/49 , A61K8/55 , A61K8/81 , A61Q17/04 , A61Q19/00 , A61Q19/08 , A61K7/42 , A61K7/44 , A61K9/10 , A61K9/12
CPC分类号： A61Q19/08 , A61K8/37 , A61K8/4973 , A61K8/553 , A61K8/8152 , A61Q17/04 , Y10S424/05 , Y10S514/847 , Y10S514/873 , Y10S514/938 , Y10S514/944 , Y10S514/946 , Y10S514/969
摘要： The subject invention relates to compositions and methods for regulating wrinkles in mammalian skin by topical application of a 2-deoxy- or 2-deoxy-2-halo-lysophosphatidic acid compound having the structure: ##STR1## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 11 to about 23 carbon atoms; each --X-- is independently --0-- or --S--; --Y-- is --0-- or --CH.sub.2 --; and Z is --H or halo.
摘要翻译：本发明涉及通过局部施用具有以下结构的2-脱氧-2-脱氧-2-卤代 - 溶血磷脂酸化合物或其药学上可接受的盐来调节哺乳动物皮肤中的皱纹的组合物和方法，其中 -R为未取代或取代的饱和或不饱和的具有11至约23个碳原子的直链或支链烷基; 每个-X-独立地为-O-或-S-; -Y-是-O-或-CH2-; Z为-H或卤素。

5. 发明授权

US5116745A Process for preparing 2-acylglycerides or 1,2-diacyl diglycerides or 2,3-diacyl diglycerides 失效
标题翻译：制备2-乙酰胆碱酯或1,2-二柠檬酸二钠或2,3-二氨基吡啶的方法
公开(公告)号：US5116745A
公开(公告)日：1992-05-26
申请号：US511115
申请日：1990-04-19
申请人： Adam W. Mazur , George D. Hiler, II , Magda El-Nokaly
发明人： Adam W. Mazur , George D. Hiler, II , Magda El-Nokaly
IPC分类号： C07C69/003 , C11C3/08 , C12P7/64
CPC分类号： C12P7/6418 , C07C69/003 , C11C3/08 , C12P7/6445 , C12P7/6454
摘要： A process for the selective hydrolysis of triglyderides to 2-acyl glycerides is disclosed. This process uses a primary lower alkyl alcohol selected from the group consisting of methanol, the primary butanols and the primary pentanols and 2-butanol, an aqueous buffer system and a 1,3-lipase. The 2-acylmonglycerides can be used to make stereospecific 1,2-diacyl glycerides or 2,3-diacyl glycerides through esterification with acid anhydrides and 1,3-lipase catalysis. Stereospecific 1,2,3-triglycerides can be made from these materials by standard esterification reactions under conditions which control rearrangement.
摘要翻译：公开了将甘油三酯选择性水解成2-酰基甘油酯的方法。该方法使用选自甲醇，主要丁醇和伯戊醇和2-丁醇的初级低级烷基醇，水性缓冲体系和1,3-脂肪酶。 2-酰基甘油酸甘油酯可用于通过用酸酐和1,3-脂肪酶催化进行酯化来制备立体特异性1,2-二酰基甘油酯或2,3-二酰基甘油酯。在控制重排的条件下，通过标准酯化反应可以从这些物质制备立体特异性的1,2,3-甘油三酸酯。

6. 发明授权

US5591836A Cholesterol lowering compounds 失效
标题翻译：胆固醇降低化合物
公开(公告)号：US5591836A
公开(公告)日：1997-01-07
申请号：US133822
申请日：1993-10-07
申请人： Adam W. Mazur , Stanislaw Pikul , Bruce P. Daggy
发明人： Adam W. Mazur , Stanislaw Pikul , Bruce P. Daggy
IPC分类号： C07H13/04 , C07J17/00 , C07J71/00 , A61K31/705 , C07H15/24
CPC分类号： C07H13/04 , C07J17/005 , C07J71/0005
摘要： Disclosed are novel saponins containing 5-C-hydroxymethylhexose and a sterol or triterpene. These materials, when consumed by humans and animals, lower the cholesterol level in the blood. These compounds can be administered as pharmaceutical preparation to the diet, or incorporated into food compositions.
摘要翻译：公开了含有5-C-羟甲基己糖和甾醇或三萜烯的新型皂苷。这些材料在人类和动物食用时会降低血液中的胆固醇水平。这些化合物可作为药物制剂施用于饮食，或并入食物组合物中。

7. 发明授权

US5104797A Process for preparing 5-C-hydroxymethyl aldohexose-based compounds 失效
标题翻译：制备5-C-羟基甲基铝酸盐的化合物的方法
公开(公告)号：US5104797A
公开(公告)日：1992-04-14
申请号：US337725
申请日：1989-04-17
申请人： Adam W. Mazur , George D. Hiler, II , Gordon K. Stipp , Bernard W. Kluesener
发明人： Adam W. Mazur , George D. Hiler, II , Gordon K. Stipp , Bernard W. Kluesener
IPC分类号： C12P19/04 , C07H1/00 , C07H15/04 , C07H19/01 , C12P19/02 , C12P19/44
CPC分类号： C07H15/04 , C07H19/01 , C12P19/02 , C12P19/44
摘要： Processes of the present invention provide economical methods for preparing derivatives 5-C-hydroxymethyl-D-aldohexose and their bicyclic anhydro tautomeric forms. The 5-C-hydroxymethylation process comprises an enzymic oxidation reaction followed by a condenation reaction with formaldehyde.

8. 发明授权

US5041541A Functional sugar substituted with reduced calories 失效
标题翻译：功能性糖代替热量减少
公开(公告)号：US5041541A
公开(公告)日：1991-08-20
申请号：US339531
申请日：1989-04-20
申请人： Adam W. Mazur
发明人： Adam W. Mazur
IPC分类号： A23L1/29 , A23G3/34 , A23L1/09 , A23L1/236 , C07H3/02 , C07H3/04 , C07H3/06 , C07H7/02 , C08B37/00 , C13B50/00
CPC分类号： C13B50/002 , A23G3/346 , A23L27/32 , C07H7/02 , A23G2200/06
摘要： Disclosed are novel 5-C-hydroxymethylhexose compounds and their derivatives which exhibit sugar-like functionality when used in food compositions. The derivatives include stereoisomers, di-, tri-, and polysaccharides, alkyl glycosides, polyol, and alditol derivatives. Also disclosed are sugar substitute compositions and food compositions containing these compounds and their derivatives.

9. 发明授权

US5149642A Process for preparing 2-acylglycerides or 1,2 or 2,3-diacylglycerides 失效
标题翻译：制备2-乙酰胆碱酯酶或1,2或2,3-二乙酰胆碱酯酶的方法
公开(公告)号：US5149642A
公开(公告)日：1992-09-22
申请号：US511674
申请日：1990-04-20
申请人： Adam W. Mazur , George D. Hiler, II , Magda El-Nokaly
发明人： Adam W. Mazur , George D. Hiler, II , Magda El-Nokaly
IPC分类号： C07C69/003 , C11C3/08 , C12P7/64
CPC分类号： C12P7/6418 , C07C69/003 , C11C3/08 , C12P7/6445 , C12P7/6454
摘要： A process for the selective hydrolysis of triglycerides to mixtures of 1,3 or 2,3-diacyl glycerides and 2-acyl glycerides is disclosed. This process uses an alkyl alcohol selected from the group consisting of 2-methyl-2-propanol, 2-butanol and the primary, secondary or tertiary branched or straight chain alkyl alcohols having from 5 to 8 carbon atoms, and mixtures thereof, an aqueous buffer system and a 1,3-lipase. The 2-acyl glycerides in the mixture are esterified to make stereospecific 1,2-diacyl glycerides or 2,3-diacyl glycerides with acid anhydrides and a lipase catalyst. Under the reaction conditions, there is little rearrangement of the diacyl glycerides in the mixture and less than 20% triglyceride is formed. Stereospecific 1,2,4-triglycerides can be made from these materials by standard esterification reactions under conditions which control rearrangement.
摘要翻译：公开了将甘油三酯选择性水解成1,3或2,3-二酰基甘油酯和2-酰基甘油酯的混合物的方法。该方法使用选自2-甲基-2-丙醇，2-丁醇和具有5至8个碳原子的伯，仲或叔支链或直链烷基醇的烷基醇及其混合物，水溶液缓冲系统和1,3-脂肪酶。将混合物中的2-酰基甘油酯酯化以制备具有酸酐和脂肪酶催化剂的立体特异性1,2-二酰基甘油酯或2,3-二酰基甘油酯。在反应条件下，混合物中二酰基甘油酯的重排很少，形成少于20％的甘油三酯。在控制重排的条件下，可通过标准酯化反应从这些物质制备立体特异性的1,2,4-甘油三酸酯。

10. 发明授权

US5106967A Functional sugar substitutes with reduced calories 失效
标题翻译：功能性糖替代品具有降低的热量
公开(公告)号：US5106967A
公开(公告)日：1992-04-21
申请号：US706445
申请日：1991-05-28
申请人： Adam W. Mazur
发明人： Adam W. Mazur
IPC分类号： A23G3/34 , A23L27/30 , C07H7/02 , C13B50/00
CPC分类号： C13B50/002 , A23G3/346 , A23L27/32 , C07H7/02 , A23G2200/06
摘要： Disclosed are novel 5-C-hydroxymethylhexose compounds and their derivatives which exhibit sugar-like functionality when used in food compositions. The derivatives include stereoisomers, di-, tri-, and polysaccharides, alkyl glycosides, polyol, and alditol derivatives. Also disclosed are sugar substitute compositions and food compositions containing these compounds and their derivatives.
摘要翻译：公开了当用于食品组合物时显示糖状官能团的新的5-C-羟甲基己糖化合物及其衍生物。衍生物包括立体异构体，二，三和多糖，烷基糖苷，多元醇和糖醇衍生物。还公开了含有这些化合物及其衍生物的糖替代组合物和食品组合物。

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