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1. 发明授权

US4707554A Method of obtaining derivatives of 4.beta.-/1'-alken-1'-yl/-2.xi.,5.alpha.-d.alpha..beta.-4,5,6,6.alpha..beta . 失效
标题翻译：获得4β-/ 1'-链烯-1'-基/ -2xi，5α-二羟基-3,3αβ-4,4,5,6,6α-六氢-2H-环戊二烯（ b）呋喃
公开(公告)号：US4707554A
公开(公告)日：1987-11-17
申请号：US802702
申请日：1985-11-27
申请人： Barbara Achmatowicz , Andrzej R. Daniewski , Stanislaw Marczak , Jacek Pankowski , Jerzy Wicha
发明人： Barbara Achmatowicz , Andrzej R. Daniewski , Stanislaw Marczak , Jacek Pankowski , Jerzy Wicha
IPC分类号： C07D307/935
CPC分类号： C07D307/935 , Y02P20/55
摘要： A new method has been disclosed for obtaining derivatives of 4.beta.-/1'-alken-1'-yl/-2.xi.,5.dbd.-dihydroxy-3,3a.beta.,4,5,6,6a.beta.-hexahydro-2H-cyclopenta [b] furane useful in the synthesis of prostaglandins or their analogs, and a method for obtaining new sulphonyl initial compounds of the general formula 4, in which Z denotes a hydrogen atom or a protective group, Y denotes a group of the formula .dbd.CHOZ.sup.1, in which Z.sup.1 has the meaning stated for Z, whereby protective groups Z and Z.sup.1 may be the same or different, and Ar denotes optionally a substituted aryl group.In the method according to the invention the new sulphonyl derivative of the general formula 4 is alkylated with an electrophilic agent comprising: carbonyl derivatives, oxiranes and halohydrins or their derivatives; the alkylation product is transformed into derivatives of 4.beta.-/1'-alken-1'-yl/-2.xi.,5.alpha.-dihydroxy-3,3a.beta.,4,5,6,6a.beta.-hexahydro-2H-cyclopenta[b] furane in reactions which ensure obtaining a double bond C.sub.13 -C.sub.14.New sulphonyl initial compounds of the general formula 4 are obtained from lactone of the general formula 11, in which Z has the above stated meaning and L.degree. denotes a leaving group, which is transformed into a sulphide; the obtained lactone-sulphide is reduced to lactol, and thereafter lactol-sulphide is oxidized to the sulphonyl derivative.
摘要翻译：已经公开了一种新的方法来获得4β-/ 1'-链烯-1'-基/ 2i，5 =二羟基-3,3aβ，4,5,6,6aβ-六氢-2H- 可用于合成前列腺素或其类似物的环戊二烯并[b]呋喃，以及获得通式4的新的磺酰基初始化合物的方法，其中Z表示氢原子或保护基，Y表示式 = CHOZ1，其中Z1具有对Z所定义的含义，由此保护基Z和Z1可以相同或不同，Ar表示任选取代的芳基。在根据本发明的方法中，通式4的新磺酰基衍生物用亲电子试剂烷基化，包括：羰基衍生物，环氧乙烷和卤代醇或其衍生物; 将烷基化产物转化成4β-/ 1'-链烯-1'-基/ -2xi，5α-二羟基-3,3aβ，4,5,6,6a-六氢-2H-环戊二烯的衍生物 [b]呋喃在确保获得双键C13-C14的反应中。通式4的新型磺酰基初始化合物由通式11的内酯得到，其中Z具有上述含义，L DEG表示转化成硫化物的离去基团; 将所得内酯硫化物还原成乳糖，然后硫化内脂被氧化成磺酰基衍生物。

2. 发明授权

US6030520A Nitrate reduction 失效
标题翻译：硝酸盐还原
公开(公告)号：US6030520A
公开(公告)日：2000-02-29
申请号：US857232
申请日：1997-05-16
申请人： Jacek J. Dziewinski , Stanislaw Marczak
发明人： Jacek J. Dziewinski , Stanislaw Marczak
IPC分类号： B01D53/54 , B01D53/86 , C02F1/467 , C02F1/52 , C02F1/54 , C02F1/70 , C02F1/461
CPC分类号： C02F1/70 , B01D53/54 , B01D53/8621 , C02F1/705 , C02F1/4678 , C02F1/5236 , C02F1/54 , C02F2101/163
摘要： Nitrates are reduced to nitrogen gas by contacting the nitrates with a metal to reduce the nitrates to nitrites which are then contacted with an amide to produce nitrogen and carbon dioxide or acid anions which can be released to the atmosphere. Minor amounts of metal catalysts can be useful in the reduction of the nitrates to nitrites. Metal salts which are formed can be treated electrochemically to recover the metals.
摘要翻译：通过使硝酸盐与金属接触来将硝酸盐还原成氮气，以将硝酸盐还原成亚硝酸盐，然后将其与酰胺接触以产生可释放到大气中的氮气和二氧化碳或酸性阴离子。少量的金属催化剂可用于将硝酸盐还原成亚硝酸盐。可以电化学处理形成的金属盐以回收金属。

3. 发明申请

US20090298800A1 1,25-DIHYDROXY, 20-CYCLOPROPYL,26-27-DEUTEROALKYL VITAMIN D3 COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译： 1,25-二羟基，20-环丙基，26-27-去甲基维生素D 3化合物及其使用方法
公开(公告)号：US20090298800A1
公开(公告)日：2009-12-03
申请号：US12067873
申请日：2006-09-21
申请人： Milan R. Uskokovic , Stanislaw Marczak , Pawel Jankowski , Luciano Adorini
发明人： Milan R. Uskokovic , Stanislaw Marczak , Pawel Jankowski , Luciano Adorini
IPC分类号： A61K31/59 , C07C401/00 , A61P37/00 , A61P35/00
CPC分类号： C07C401/00 , C07C2601/02
摘要： The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbons-26 and 27 with deuterated alkyl groups, e.g., trideuteromethyl, wherein carbon-16 is a single or double bond, and carbon-23 is a single, double, or triple bond. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
摘要翻译：本发明提供了在碳-26和27与氘化烷基取代的维生素D 3类似物，例如三氘代甲基，其中碳-16是单键或双键，碳-23是单键，双键或三键。本发明提供其药学上可接受的酯，盐和前药。还公开了使用该化合物治疗维生素D3相关状态的方法和含有该化合物的药物组合物。

4. 发明申请

US20090137828A1 Synthesis of 1A-Fluoro-25-Hydroxy-16-23E-Diene-26,27-Bishomo-20-Epi-Cholecalciferol 审中-公开
标题翻译： 1A-Fluoro-25-羟基-16-23E-二烯-26,27-双 - 20-Epi-胆钙化甾醇的合成
公开(公告)号：US20090137828A1
公开(公告)日：2009-05-28
申请号：US12063955
申请日：2006-08-18
申请人： Milan R. Uskokovic , Stanislaw Marczak , Ralf Loo , Marcel Van Der Sluis , Pawel Jankowski , Hubert Maehr
发明人： Milan R. Uskokovic , Stanislaw Marczak , Ralf Loo , Marcel Van Der Sluis , Pawel Jankowski , Hubert Maehr
IPC分类号： C07C401/00
CPC分类号： C07C29/48 , C07B2200/07 , C07C29/147 , C07C35/17 , C07C35/23 , C07C45/292 , C07C45/30 , C07C67/08 , C07C67/29 , C07C67/293 , C07C67/297 , C07C67/343 , C07C69/013 , C07C69/73 , C07C401/00 , C07C2601/16 , C07C2602/24 , C07C49/743 , C07C47/192 , C07C69/14 , C07C69/16 , C07C69/145 , C07C35/32 , C07C35/48
摘要： The invention provides a method of producing 20-methyl vitamin D3 compounds of formula (I). The method includes allylic and olefin oxidation, de-carbonylation, carbonyl reduction, fluoride substitution, epoxide deoxygenation, and Wittig-type couplings.
摘要翻译：本发明提供一种生产式（I）的20-甲基维生素D3化合物的方法。该方法包括烯丙基和烯烃氧化，脱羰基，羰基还原，氟化物取代，环氧化物脱氧和Wittig型偶联。

5. 发明申请

US20080318911A1 20-Cyclopropyl, 26,27-Alkyl/Haloalkyl Vitamin D3 Compounds and Methods of Use Thereof 审中-公开
标题翻译： 20-环丙基，26,27-烷基/卤代烷基维生素D3化合物及其使用方法
公开(公告)号：US20080318911A1
公开(公告)日：2008-12-25
申请号：US11663704
申请日：2005-09-23
申请人： Milan R. Uskokovic , Luciano Adorini , Guiseppe Penna , Enrico Colli , Stanislaw Marczak
发明人： Milan R. Uskokovic , Luciano Adorini , Guiseppe Penna , Enrico Colli , Stanislaw Marczak
IPC分类号： C07C401/00 , A61K31/593 , A61P37/00 , A61P25/00 , A61P13/10
CPC分类号： C07C401/00
摘要： The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbon 20 with cycloalkyl, e.g., cyclopropyl, wherein carbon-16 is a double bond, and carbon-23 is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated as carbon-25. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
摘要翻译：本发明提供了在碳20与环烷基例如环丙基取代的胆钙化甾醇的维生素D3类似物，其中碳-16是双键，碳-23是单键，双键或三键。各种烷基或卤代烷基取代作为碳-25引入。本发明提供其药学上可接受的酯，盐和前药。还公开了使用该化合物治疗维生素D3相关状态的方法和含有该化合物的药物组合物。

6. 发明授权

US06436275B1 Electrochemical reduction of nitrate in the presence of an amide 失效
标题翻译：在酰胺存在下电化学还原硝酸盐
公开(公告)号：US06436275B1
公开(公告)日：2002-08-20
申请号：US09584627
申请日：2000-05-31
申请人： Jacek J. Dziewinski , Stanislaw Marczak
发明人： Jacek J. Dziewinski , Stanislaw Marczak
IPC分类号： C25C100
CPC分类号： C02F1/4676 , C02F2101/16 , C02F2101/163
摘要： The electrochemical reduction of nitrates in aqueous solutions thereof in the presence of amides to gaseous nitrogen (N2) is described. Generally, electrochemical reduction of NO3 proceeds stepwise, from NO3 to N2, and subsequently in several consecutive steps to ammonia (NH3) as a final product. Addition of at least one amide to the solution being electrolyzed suppresses ammonia generation, since suitable amides react with NO2 to generate N2. This permits nitrate reduction to gaseous nitrogen to proceed by electrolysis. Suitable amides include urea, sulfamic acid, formamide, and acetamide.
摘要翻译：描述了在酰胺存在下将其在其水溶液中的硝酸盐在气态氮（N 2）下的电化学还原。通常，NO 3的电化学还原逐步进行，从NO 3到N 2，随后在几个连续步骤中作为最终产物进行氨（NH 3）。在正在电解的溶液中加入至少一种酰胺抑制氨的产生，因为合适的酰胺与NO2反应生成N 2。这允许硝酸盐还原成气态氮以通过电解进行。合适的酰胺包括尿素，氨基磺酸，甲酰胺和乙酰胺。

7. 发明专利

AU6951998A Nitrate reduction 未知
公开(公告)号：AU6951998A
公开(公告)日：1998-11-13
申请号：AU6951998
申请日：1998-04-03
申请人： UNIV CALIFORNIA , JACEK J DZIEWINSKI , STANISLAW MARCZAK
发明人： DZIEWINSKI JACEK J , MARCZAK STANISLAW
IPC分类号： B01D53/54 , B01D53/86 , C02F1/467 , C02F1/52 , C02F1/54 , C02F1/70 , C02F1/46 , C02F1/461 , B01D53/34
摘要： Nitrates are reduced to nitrogen gas by contacting the nitrates with a metal to reduce the nitrates to nitrites which are then contacted with an amide to produce nitrogen and carbon dioxide or acid anions which can be released to the atmosphere. Minor amounts of metal catalysts can be useful in the reduction of the nitrates to nitrites. Metal salts which are formed can be treated electrochemically to recover the metals.

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