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1. 发明授权

US07358374B2 Purified racemic lasofoxifene and purified lasofoxifene D-tartrate and a method for effective purification of racemic lasofoxifene 有权
标题翻译：纯化的外消旋拉唑昔芬和精制的德福沙芬D-酒石酸盐和有效纯化外消旋拉唑昔芬的方法
公开(公告)号：US07358374B2
公开(公告)日：2008-04-15
申请号：US11092240
申请日：2005-03-28
申请人： Robert W. McLaughlin , Harry A. Watson, Jr. , Constantine Sklavounos
发明人： Robert W. McLaughlin , Harry A. Watson, Jr. , Constantine Sklavounos
IPC分类号： C07D207/04
CPC分类号： C07D295/088 , C07D207/08
摘要： A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.
摘要翻译：从外消旋顺式-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇和纯化的顺-6-苯基中除去杂质的方法 -5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇可用作雌激素激动剂/拮抗剂。

2. 发明申请

US20050171189A1 Purified racemic lasofoxifene and purified lasofoxifene D-tartrate and a mehtod for effective purification of racemic lasofoxifene 有权
标题翻译：纯化的外消旋拉唑昔芬和精制的德伐他他芬D-酒石酸盐和有效纯化外消旋拉唑昔芬的方法
公开(公告)号：US20050171189A1
公开(公告)日：2005-08-04
申请号：US11092240
申请日：2005-03-28
申请人： Robert McLaughlin , Harry Watson , Constantine Sklavounos
发明人： Robert McLaughlin , Harry Watson , Constantine Sklavounos
IPC分类号： C07D295/08 , A61K31/40 , A61K31/4015 , C07D207/04 , C07D207/08 , C07D207/12 , C07D295/092
CPC分类号： C07D295/088 , C07D207/08
摘要： A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.
摘要翻译：从外消旋顺式-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇和纯化的顺-6-苯基中除去杂质的方法 -5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇可用作雌激素激动剂/拮抗剂。

3. 发明授权

US4782165A Process for biotin intermediates 失效
标题翻译：生物素中间体的方法
公开(公告)号：US4782165A
公开(公告)日：1988-11-01
申请号：US90300
申请日：1987-10-01
申请人： Constantine Sklavounos
发明人： Constantine Sklavounos
IPC分类号： C07D233/70 , C07D513/04 , C07D473/00
CPC分类号： C07D513/04 , C07D233/70
摘要： In the synthesis of biotin and decarboxybiotin, a more direct method for the conversion of 1,3-diacyl-4-(bromomethyl)-5-[(5-alkoxycarbonylpentanoyl) or hexanoyl]-4-imidazolin-2-ones to 1,3-diacyl-4-[(4-alkoxybutanoyl) or pentanoyl]-1H,3H-thieno (3,4-b)imidazol-2-one via the Bunte salt of the formula ##STR1## wherein R is (C.sub.1 -C.sub.5)alkanoyl or (C.sub.2 -C.sub.5) alkoxycarbonyl, X is methyl or (C.sub.2 -C.sub.5)alkoxycarbonyl an Y is an alkali metal.
摘要翻译：在生物素和脱羧基生物素的合成中，将1,3-二酰基-4-（溴甲基）-5 - [（5-烷氧羰基戊酰基）或己酰基] -4-咪唑啉-2-酮转化为1， 3-二酰基-4 - [（4-烷氧基丁酰基）或戊酰基] -1H，3H-噻吩并（3,4-b）咪唑-2-酮，其通式为其中R为（C 1 -C 5））烷酰基或（C 2 -C 5）烷氧基羰基，X为甲基或（C 2 -C 5）烷氧基羰基，Y为碱金属。

4. 发明授权

US5665708A Process and antiparasitic intermediates for doramectin 失效
标题翻译：多拉菌素的过程和抗寄生虫中间体
公开(公告)号：US5665708A
公开(公告)日：1997-09-09
申请号：US617740
申请日：1996-03-08
申请人： Constantine Sklavounos , Thomas Charles Crawford , Neil Demers , Stephen Paul Gibson , Charles William Murtiashaw, deceased
发明人： Constantine Sklavounos , Thomas Charles Crawford , Neil Demers , Stephen Paul Gibson , Charles William Murtiashaw, deceased
IPC分类号： A01N43/90 , A01N47/06 , A01P3/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , C07H17/08 , C07H19/01
CPC分类号： C07H17/08 , A01N43/90 , A01N47/06 , C07H19/01
摘要： Intermediates and a process for preparing doramectin, the compound of formula (I), semisynthetically from by-product in the fermentation procedure which also yields the compound of formula (I). The intermediates prepared by the process of this invention also have utility as antiparasitic agents. The process of this invention utilizes continuous reaction inert gas sparging during the pyrolysis step, resulting in a significant improvement in the overall yield of this conversion. ##STR1##
摘要翻译： PCT No.PCT / IB94 / 00283 Sec。 371日期：1996年3月8日 102（e）1996年3月8日PCT PCT 1994年9月19日PCT公布。公开号WO95 / 09863 日期1995年04月13日中间体和制备多拉菌素的方法，式（I）化合物在发酵过程中半合成来自副产物，其也产生式（I）化合物。通过本发明方法制备的中间体也可用作抗寄生虫剂。本发明的方法在热解步骤期间利用连续反应惰性气体喷射，导致该转化率的总收率显着提高。（一）

5. 发明授权

US4375430A Processes for preparation, isolation and purification of dipeptide sweeteners 失效
标题翻译：二肽甜味剂的制备，分离和纯化方法
公开(公告)号：US4375430A
公开(公告)日：1983-03-01
申请号：US300366
申请日：1981-09-08
申请人： Constantine Sklavounos
发明人： Constantine Sklavounos
IPC分类号： A23L27/30 , C07K1/02 , C07K1/06 , C07K5/072 , C07K5/075 , C07C103/52
CPC分类号： C07K5/06113 , Y10S530/801
摘要： Aromatic sulfonic acid salts of certain dipeptide sweeteners which are L-aspartyl-D-alaninamides or L-aspartyl-D-serinamides, each substituted on amide nitrogen with an organic radical having a highly branched carbon skeleton; the process for preparing said salts by crystallization; and utilization of this crystallization process in processes for the preparation, isolation and purification of said amides.
摘要翻译：某些二肽甜味剂的芳香磺酸盐是L-天冬氨酰-D-丙氨酰胺或L-天冬氨酰-D-丝氨酰胺，其各自在酰胺氮上被具有高支链碳骨架的有机基团取代; 通过结晶制备所述盐的方法; 以及在制备，分离和纯化所述酰胺的方法中利用该结晶过程。

6. 发明授权

US6153746A Process for making a cyclodextrin 失效
标题翻译：制备环糊精的方法
公开(公告)号：US6153746A
公开(公告)日：2000-11-28
申请号：US106983
申请日：1998-06-29
申请人： Bharat K. Shah , Constantine Sklavounos
发明人： Bharat K. Shah , Constantine Sklavounos
IPC分类号： C08B37/16 , C07H1/00
CPC分类号： C08B37/0012
摘要： Sulfoalkyl ether cyclodextrins are produced by a process of treating an unsubstituted cyclodextrin starting material with an alkyl sultone in the presence of a base. The base is added in a stepwise, pH controlled manner so that substantially the entire initial charge of cyclodextrin starting material is at least partially reacted. Additional base is then added to complete the reaction, and residual alkyl suftone is destroyed. The product advantageously contains low levels of both residual cyclodextrin and residual alkyl sultone.
摘要翻译：磺基烷基醚环糊精通过在碱存在下用烷基磺内酯处理未取代的环糊精起始原料的方法制备。以逐步，pH控制的方式加入碱，使得基本上环糊精起始原料的全部初始电荷至少部分地反应。然后加入另外的碱以完成反应，并且残留的烷基磺酸酯被破坏。产物有利地含有低水平的残留环糊精和残留的烷基磺内酯。

7. 发明授权

US5942611A Process for natamycin recovery 失效
标题翻译：游霉素回收方法
公开(公告)号：US5942611A
公开(公告)日：1999-08-24
申请号：US696841
申请日：1996-08-28
申请人： George Wayne Borden , John Michael Maher , Constantine Sklavounos
发明人： George Wayne Borden , John Michael Maher , Constantine Sklavounos
IPC分类号： C07H1/08 , C07H17/08 , C07H1/00
CPC分类号： C07H17/08 , C07H1/08
摘要： A new process for recovering high purity natamycin from fermentation broth containing natamycin comprises the steps of adjusting the pH of the broth to above about 10 and adding an amount of a water-miscible solvent, such as isopropanol, sufficient to dissolve the natamycin in the broth, followed by removing insoluble solids from the pH-adjusted broth, followed by lowering the pH of the broth to a level sufficient to precipitate the natamycin, and removing the natamycin from the broth.
摘要翻译： PCT No.PCT / IB95 / 00040 Sec。 371日期：1996年8月28日 102（e）日期1996年8月28日PCT提交1995年1月19日PCT公布。公开号WO95 / 27073 日期1995年10月12日从含有游霉素的发酵液中回收高纯度纳他霉素的新方法包括以下步骤：将培养液的pH调节至约10以上，并加入足量溶解的量的水混溶性溶剂如异丙醇培养基中的那他霉素，然后从pH调节的肉汤中除去不溶性固体，然后将肉汤的pH降低到足以沉淀那他霉素的水平，并从肉汤中除去那他霉素。

8. 发明授权

US06906202B2 Purified racemic lasofoxifene and purified lasofoxifene D-tartrate and a method for effective purification of racemic lasofoxifene 有权
标题翻译：纯化的外消旋拉唑昔芬和精制的德福沙芬D-酒石酸盐和有效纯化外消旋拉唑昔芬的方法
公开(公告)号：US06906202B2
公开(公告)日：2005-06-14
申请号：US10397654
申请日：2003-03-26
申请人： Robert W. McLaughlin , Harry A. Watson, Jr. , Constantine Sklavounos
发明人： Robert W. McLaughlin , Harry A. Watson, Jr. , Constantine Sklavounos
IPC分类号： C07D295/08 , A61K31/40 , A61K31/4015 , C07D207/04 , C07D207/08 , C07D207/12 , C07D295/092
CPC分类号： C07D295/088 , C07D207/08
摘要： A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.
摘要翻译：从外消旋顺式-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇和纯化的顺-6-苯基中除去杂质的方法 -5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇可用作雌激素激动剂/拮抗剂。

9. 发明授权

US06825327B2 Process for preparing 4″-substituted-9-deoxo-9a-aza-9a-homoerythromycin a derivatives 有权
标题翻译：制备4“ - 取代-9-脱氧-9a-氮杂-9a-高红霉素衍生物的方法
公开(公告)号：US06825327B2
公开(公告)日：2004-11-30
申请号：US10133472
申请日：2002-04-25
申请人： Constantine Sklavounos , John L. Tucker , Lulin Wei , Kerry P. Mahon , Philip Hammen , Joanna T. Negri , Richard S. Lehner
发明人： Constantine Sklavounos , John L. Tucker , Lulin Wei , Kerry P. Mahon , Philip Hammen , Joanna T. Negri , Richard S. Lehner
IPC分类号： C07H100
CPC分类号： C07H17/08 , C07H1/00 , Y02P20/55
摘要： The invention relates to processes for preparing compounds of formula 1 wherein R3 is as defined herein, and to pharmaceutically acceptable salts thereof, as well as intermediates useful in such processes. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing compounds prepared by the processes of the invention and to methods of treating bacterial protozoa infections by administering such compounds.
摘要翻译：本发明涉及制备式I化合物的方法，其中R 3如本文所定义，及其药学上可接受的盐，以及可用于此类方法的中间体。式1的化合物是可用于治疗各种细菌和原生动物感染的抗菌剂。本发明还涉及含有通过本发明的方法制备的化合物的药物组合物和通过施用这些化合物治疗细菌原生动物感染的方法。

10. 发明授权

US5601863A Reduced polydextrose 失效
标题翻译：减少的聚葡萄糖
公开(公告)号：US5601863A
公开(公告)日：1997-02-11
申请号：US313940
申请日：1994-09-28
申请人： G. Wayne Borden , Raymond C. Glowaky , Russell J. Hausman , Constantine Sklavounos , Harry O. Tobiassen
发明人： G. Wayne Borden , Raymond C. Glowaky , Russell J. Hausman , Constantine Sklavounos , Harry O. Tobiassen
IPC分类号： C08B37/00 , A23L1/236 , A23L1/29 , A23L1/308 , B01J31/04 , C07B61/00 , C08L20060101 , A23L1/00 , C07H1/00
CPC分类号： C08B37/0009 , A23L27/32 , A23L33/26
摘要： A polydextrose having improved color, flavor and decreased reactivity toward food ingredients having amine functionality. The polydextrose comprises a water-soluble highly branched polydextrose having been prepared by a process which comprises melting dextrose in the presence of a food-acceptable acid catalyst. The improved polydextrose of this invention has substantially no reducing glucose groups. Another aspect of this invention is directed to a method of making the above-described improved polydextrose which comprises exposing unimproved polydextrose to an environment capable of chemically transforming the reducing glucose groups contained in the unimproved polydextrose, thereby substantially eliminating their reducing properties. An improved polymaltose prepared by heating maltose in the presence of a food-acceptable acid catalyst and chemically transforming the reducing glucose groups contained in the polymaltose, thereby eliminating their reducing properties, is also described.
摘要翻译：具有改善的颜色，风味和对具有胺官能团的食品成分的反应性降低的聚葡萄糖。聚右旋糖包含通过包括在食品可接受的酸催化剂存在下熔融葡萄糖的方法制备的水溶性高度支化的聚右旋糖。本发明的改进的聚右旋糖基本上没有还原葡萄糖基团。本发明的另一方面涉及制备上述改进的聚右旋糖的方法，其包括将未改良的聚右旋糖暴露于能够化学转化未改良的聚右旋糖中所含的还原葡萄糖基团的环境，从而基本上消除其还原性能。还描述了通过在食物可接受的酸催化剂的存在下加热麦芽糖并化学转化聚麦芽糖中包含的还原葡萄糖基，从而消除它们的还原性质而制备的改进的聚麦芽糖。

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