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1. 发明授权

US6111105A Processes and intermediates for preparing 3-(1-piperazinyl)-1,2-benzisothiazole 失效
标题翻译：制备3-（1-哌嗪基）-1,2-苯并异噻唑的方法和中间体
公开(公告)号：US6111105A
公开(公告)日：2000-08-29
申请号：US68285
申请日：1998-10-15
申请人： Darrell E. Fox , John F. Lambert , Terry G. Sinay , Stanley W. Walinsky
发明人： Darrell E. Fox , John F. Lambert , Terry G. Sinay , Stanley W. Walinsky
IPC分类号： C07D295/22 , C07C313/16 , C07D275/04 , C07D295/26 , C07D417/04
CPC分类号： C07D275/04 , C07D295/26
摘要： The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzoisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process.
摘要翻译： PCT No.PCT / IB96 / 01079 Sec。 371日期：1998年10月15日 102（e）1998年10月15日日期PCT 1996年10月11日PCT PCT。公开号WO97 / 17336 日期1997年5月15日本发明涉及制备3-（1-哌嗪基）-1,2-苯并异噻唑或其药学上可接受的盐的方法和本方法中使用的新型中间体。

2. 发明授权

US5530107A Method for making steroidal peracyl glycosides 失效
标题翻译：制备甾体过酰基甙的方法
公开(公告)号：US5530107A
公开(公告)日：1996-06-25
申请号：US244403
申请日：1994-05-23
申请人： Douglas J. M. Allan , Frank R. Busch , John F. Lambert , Russell J. Shine , Stanley W. Walinsky
发明人： Douglas J. M. Allan , Frank R. Busch , John F. Lambert , Russell J. Shine , Stanley W. Walinsky
IPC分类号： C07J71/00 , C07J53/00 , C07H1/00
CPC分类号： C07J71/0005
摘要： Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypocholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate, 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.
摘要翻译： PCT No.PCT / US92 / 08638 Sec。 371日期1994年5月23日 102（e）日期1994年5月23日PCT提交1992年10月15日PCT公布。公开号WO93 / 11150 PCT 日期：1994年6月10日。用于合成已知低血胆固醇代谢细胞因子β-纤维二糖苷的中间体的十位素β-O-纤维二糖苷七链烷酸酯的合成过程。该方法包括在能够形成所述tigogenylβ-O-二十七烷基硫酸酯的条件的条件下，在氟化锌或氰化锌存在下，使α-烯烃二溴七烷酸酯和β-同位素配合物反应。还公开了类胡萝卜素β-O-纤维二糖苷七链烷酸酯，11-酮替培霉素β-O-纤维二糖七庚酸酯和薯di皂苷β-O-纤维二糖七庚酸酯的类似制剂。该方法提供高β-丁二醇选择性和高产率。

3. 发明授权

US5563259A Process for making .beta.-O-cellobiosyl steroid derivatives and trimethyl silyl steroid intermediates used therein 失效
标题翻译：制备β-O-纤维二糖类固醇衍生物及其中使用的三甲基甲硅烷基类固醇中间体的方法
公开(公告)号：US5563259A
公开(公告)日：1996-10-08
申请号：US351471
申请日：1994-12-20
申请人： Kathleen D. Goggin , John F. Lambert , Stanley W. Walinsky
发明人： Kathleen D. Goggin , John F. Lambert , Stanley W. Walinsky
IPC分类号： C07J71/00 , C07J75/00 , C07G17/00
CPC分类号： C07J71/0005
摘要： A process for the synthesis of peracyl-1-O-steroidal-.beta.-cellobiosides that provides excellent .beta.-anomeric selectivity without the use of a metal salt promoter. The process comprises reacting heptaacyl-.beta.-D-cellobiosyl-1-fluoride and a trisubstituted silyl-3-O-steroid, wherein the steroid is tigogenin, hecogenin, 11-ketotigogenin or diosgenin in the absence of a metal salt under suitable conditions.
摘要翻译： PCT No.PCT / US93 / 01709 Sec。 371日期1994年12月20日第 102（e）日期1994年12月20日PCT 1993年3月2日PCT公布。公开号WO94 / 00478 日期1994年1月6日一种合成过酰基-1-O-甾体-β-胆碱酯酶的方法，其在不使用金属盐促进剂的情况下提供优异的β-异戊醇选择性。该方法包括使七酰基-β-D-纤维二糖基-1-氟化物和三取代的甲硅烷基-3-O-类固醇反应，其中在合适的条件下，在不存在金属盐的条件下，类固醇是替宁戈宁，hecogenin，11-酮替曲连根素或薯di皂苷元。

4. 发明授权

US4602067A High temperature drilling fluids 失效
公开(公告)号：US4602067A
公开(公告)日：1986-07-22
申请号：US716908
申请日：1985-03-28
申请人： Randel E. Stong , Stanley W. Walinsky
发明人： Randel E. Stong , Stanley W. Walinsky
IPC分类号： C09K8/24 , C08F8/32
CPC分类号： C09K8/24
摘要： An aqueous drilling fluid suitable for high-temperature use comprising a water base, clay suspended in said base and from about 0.01-25 pounds per barrel total composition of a hydrolyzed terpolymer of maleic anhydride, styrene and a third monomer selected from acrylamide, methacrylamide, acrylic acid or methacrylic acid, the molar ratio of maleic anhydride to styrene to said third monomer being from about 30:10:60 to 50:40:10, and the alkali metal, ammonium and lower aliphatic amine salts thereof, the weight-average molecular weight of said hydrolyzed terpolymer being from about 500-10,000. An improved drilling process wherein such fluids remain flowable at elevated temperatures is also disclosed.

5. 发明授权

US5935960A Pro-drugs of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihy dro-2H-indol-2-one 失效
标题翻译： 5-（2-（4-（1,2-苯并异噻唑-3-基）-1-哌嗪基）乙基）-6-氯-1,3-二氢-2H-吲哚-2-酮的前药
公开(公告)号：US5935960A
公开(公告)日：1999-08-10
申请号：US798395
申请日：1997-02-07
申请人： Stanley W. Walinsky , John F. Lambert
发明人： Stanley W. Walinsky , John F. Lambert
IPC分类号： C07D417/12 , A61K31/495 , A61P25/18 , A61P25/20 , A61P43/00 , C07D209/34 , C07D403/06
CPC分类号： C07D209/34
摘要： The present invention relates to a pro-drug of ziprasidone or pharmaceutically acceptable salts thereof, processes for its preparation, and pharmaceutical compositions and methods of treatment comprising said pro-drug.
摘要翻译：本发明涉及齐拉西酮的前药或其药学上可接受的盐，其制备方法以及包含所述前药的药物组合物和治疗方法。

6. 发明授权

US4710537A Substantially homogeneous copolymers of acrylic or methacrylic acid and maleic acid 失效
公开(公告)号：US4710537A
公开(公告)日：1987-12-01
申请号：US786422
申请日：1985-10-11
申请人： Stanley W. Walinsky
发明人： Stanley W. Walinsky
IPC分类号： C02F5/10 , C08F220/04 , C08F220/06 , C08F222/04 , C08F222/06 , C08F8/12 , C08F122/02
CPC分类号： C08F220/06 , C02F5/10 , C08F220/04 , C08F222/04 , C08F222/06
摘要： Substantially homogeneous acrylate/maleate copolymers of number average molecular weight of 500 to 5000 are prepared by copolymerizing 35 to 65 mole percent acrylic or methacrylic acid with 65 to 35 mole percent maleic anhydride at 80.degree. to 150.degree. C. in the presence of a polymerization initiator and a chain-transfer solvent such that both the monomers and the formed polymer remain in solution and the mole ratio of the acrylic or methacrylic acid monomer to the maleic anhydride monomer in the solvent is maintained below about 0.2 throughout the polymerization. The copolymers in hydrolyzed form are employed at a level of from about 0.1 to 100 ppm for prevention of alkaline calcium and magnesium scale formation, such as during seawater evaporative desalination.

7. 发明授权

US4566978A High temperature drilling fluids 失效
标题翻译：高温钻井液
公开(公告)号：US4566978A
公开(公告)日：1986-01-28
申请号：US612280
申请日：1984-05-21
申请人： Randel E. Stong , Stanley W. Walinsky
发明人： Randel E. Stong , Stanley W. Walinsky
IPC分类号： C09K8/02 , C08F8/00 , C08F8/12 , C08F8/32 , C08F8/44 , C08L33/00 , C08L33/02 , C08L33/24 , C08L35/06 , C09K8/24 , C09K7/02
CPC分类号： C09K8/24
摘要： An aqueous drilling fluid suitable for high-temperature use comprising a water base, clay suspended in said base and from about 0.01-25 pounds per barrel total composition of a hydrolyzed terpolymer of maleic anhydride, styrene and a third monomer selected from acrylamide, methacrylamide, acrylic acid or methacrylic acid, the molar ratio of maleic anhydride to styrene to said third monomer being from about 30:10:60 to 50:40:10, and the alkali metal, ammonium and lower aliphatic amine salts thereof, the weight-average molecular weight of said hydrolyzed terpolymer being from about 500-10,000. An improved drilling process wherein such fluids remain flowable at elevated temperatures is also disclosed.
摘要翻译：适用于高温用途的含水钻井液包括水基，悬浮在所述底部的粘土和约0.01-25磅/桶的总组合物，马来酸酐，苯乙烯和第三单体的水解三元共聚物，选自丙烯酰胺，甲基丙烯酰胺，丙烯酸或甲基丙烯酸，马来酸酐与苯乙烯与所述第三单体的摩尔比为约30:10:60至50:40:10，其碱金属，铵和低级脂族胺盐的重均分子量所述水解三元共聚物的分子量为约500-10,000。还公开了一种改进的钻井工艺，其中这种流体在升高的温度下保持流动。

8. 发明授权

US4486581A Use of fumaric acid polymers as antiscalants 失效
标题翻译：使用富马酸聚合物作为防垢剂
公开(公告)号：US4486581A
公开(公告)日：1984-12-04
申请号：US441189
申请日：1982-11-12
申请人： Stanley W. Walinsky
发明人： Stanley W. Walinsky
IPC分类号： C02F5/10 , C08F222/02
CPC分类号： C02F5/10
摘要： Pumaric acid polymers may be used to control or inhibit scaling in boilers, desalination plants, steam generators, cooling equipment and the like. A novel process for their synthesis employs a mono or dialkyl ester of fumaric acid as a starting material.
摘要翻译：可以使用富马酸聚合物来控制或抑制锅炉，海水淡化厂，蒸汽发生器，冷却设备等中的结垢。其合成的新方法使用富马酸的单或二烷基酯作为起始原料。

9. 发明授权

US4390670A Acrylate/maleate copolymers, their preparation and use as antiscalants 失效
公开(公告)号：US4390670A
公开(公告)日：1983-06-28
申请号：US232475
申请日：1981-02-09
申请人： Stanley W. Walinsky
发明人： Stanley W. Walinsky
IPC分类号： C08F220/00 , C02F5/00 , C02F5/08 , C02F5/10 , C08F2/06 , C08F20/02 , C08F220/04 , C08F220/06 , C08F222/04 , C08F222/06
CPC分类号： C02F5/10 , C08F220/04 , C08F220/06 , C08F222/04 , C08F222/06
摘要： Substantially homogeneous acrylate/maleate copolymers of number average molecular weight of 500 to 5000 are prepared by copolymerizing 35 to 65 mole percent acrylic or methacrylic acid with 65 to 35 mole percent maleic anhydride at 80.degree. to 150.degree. C. in the presence of a polymerization initiator and a chain-transfer solvent such that both the monomers and the formed polymer remain in solution and the mole ratio of the acrylic or methacrylic acid monomer to the maleic anhydride monomer in the solvent is maintained below about 0.2 throughout the polymerization. The copolymers in hydrolyzed form are employed at a level of from about 0.1 to 100 ppm for prevention of alkaline calcium and magnesium scale formation, such as during seawater evaporative desalination.

10. 发明授权

US4547559A Acrylate/maleate copolymers, their preparation and use as antiscalants 失效
标题翻译：丙烯酸酯/马来酸酯共聚物，其制备和用作防垢剂
公开(公告)号：US4547559A
公开(公告)日：1985-10-15
申请号：US476668
申请日：1983-03-18
申请人： Stanley W. Walinsky
发明人： Stanley W. Walinsky
IPC分类号： C02F5/10 , C08F220/04 , C08F220/06 , C08F222/04 , C08F222/06 , C08F120/08
CPC分类号： C02F5/10 , C08F220/04 , C08F220/06 , C08F222/04 , C08F222/06
摘要： Substantially homogeneous acrylate/maleate copolymers of number average molecular weight of 500 to 5000 are prepared by copolymerizing 35 to 65 mole percent acrylic or methacrylic acid with 65 to 35 mole percent maleic anhydride at 80.degree. to 150.degree. C. in the presence of a polymerization initiator and a chain-transfer solvent such that both the monomers and the formed polymer remain in solution and the mole ratio of the acrylic or methacrylic acid monomer to the maleic anhydride monomer in the solvent is maintained below about 0.2 throughout the polymerization. The copolymers in hydrolyzed form are employed at a level of from about 0.1 to 100 ppm for prevention of alkaline calcium and magnesium scale formation, such as during seawater evaporative desalination.
摘要翻译：数均分子量为500至5000的丙烯酸酯/马来酸共聚物的基本上均匀的共聚物是通过在80-150℃下在聚合反应的存在下将35-65摩尔％的丙烯酸或甲基丙烯酸与65-35摩尔％马来酸酐共聚而制备的引发剂和链转移溶剂，使得单体和形成的聚合物都保留在溶液中，并且丙烯酸或甲基丙烯酸单体与溶剂中马来酸酐单体的摩尔比在整个聚合过程中保持低于约0.2。水解形式的共聚物以约0.1至100ppm的水平使用，以防止碱性钙和镁结垢形成，例如在海水蒸发脱盐期间。

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