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1. 发明授权

US4870199A Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 失效
标题翻译：合成二保护R [R *，S *] - 3,5-二羟基-6-氧代己酸酯的方法
公开(公告)号：US4870199A
公开(公告)日：1989-09-26
申请号：US166594
申请日：1988-03-10
申请人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
发明人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
IPC分类号： C07D209/18 , C07D233/54 , C07F7/18
CPC分类号： C07D233/64 , C07D209/18 , C07F7/1852 , Y02P20/55
摘要： Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.3 ' is methyl or ethyl,processes for the synthesis of compounds of the formula ##STR6## comprising reacting a compound of the formula ##STR7## with the reaction product of a strong base and a compound of the formula ##STR8## optionally followed by, when R.sub.2z is allyl, cleavage of the allyl and P.sub.1 groups to obtain the corresponding compound of the formula ##STR9## wherein each R.sub.7 is methyl or ethyl,R is as defined in the specification, and eachP.sub.1 independently and R.sub.2z are as defined above, andthe compounds of the formula ##STR10## wherein R and each R.sub.7 are as defined above.
摘要翻译：用于合成R [R *，S *]对映体形式的式“IMAGE”的化合物的方法，其中每个P1独立地是羟基保护基，R2z是C1-4烷基，苄基或烯丙基，包括作为 R2z为R2x时的关键步骤，式（S）对映异构形式的式（IMA）化合物与式Mg＆cir＆+2（（ - ）OOC-CH2-COOR2x）2的化合物的反应，得到化合物式（S）对映体形式的式（IMAGE）式中，作为R2z为R2y的关键步骤，式（S）对映异构体形式的式“IMAGE”的化合物与式Li ）（ - ）CH2-COOR2y，得到（S）对映异构体形式的下式的化合物，其中R2x是伯或仲C 1-4烷基，苄基或烯丙基，R2y是不含不对称碳原子的C 1-4烷基，并且R 3'是甲基或乙基，用于合成式IMA化合物的方法包括使式IMA的化合物与强碱的反应产物 da化合物，其中当R 2z是烯丙基时，烯丙基和P1基团裂解，得到相应的式“IMAGE”化合物，其中每个R 7是甲基或乙基，R如说明书中所定义，每个P1独立地和R2z如上所定义，并且式“IMAGE”的化合物其中R和每个R 7如上所定义。

2. 发明授权

US5189164A Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof 失效
标题翻译：合成顺式（E）-3,5-二羟基-7-取代的庚-6-烯酸和庚酸及其衍生物及其中间体的方法
公开(公告)号：US5189164A
公开(公告)日：1993-02-23
申请号：US482433
申请日：1990-02-20
申请人： Prasad K. Kapa , Kau-Ming Chen
发明人： Prasad K. Kapa , Kau-Ming Chen
IPC分类号： C07C51/367 , C07D209/12 , C07D209/24 , C07D233/54
CPC分类号： C07D233/64 , C07C51/367 , C07D209/12 , C07D209/24
摘要： A process for synthesizing syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof from the corresponding keto-hydroxy compounds, which process comprises: providing a reaction medium comprising sodium borohydride and an alkoxydialkylborane compound; treating the keto-hydroxy compound with said reaction medium under conditions wherein a cyclic boronate ester is formed; and cleaving the cyclic boronate ester to obtain the dihydroxy product.The product compounds, or derivatives thereof, are useful as anti-atherosclerotic agents.
摘要翻译：从相应的酮 - 羟基化合物合成顺式 - （E）-3,5-二羟基-7-取代的庚-6-烯酸和庚酸及其衍生物及其中间体的方法，该方法包括：提供包含钠硼氢化物和烷氧基二烷基硼烷化合物; 在形成环状硼酸酯的条件下用所述反应介质处理酮 - 羟基化合物; 并切割环状硼酸酯以获得二羟基产物。产物化合物或其衍生物可用作抗动脉粥样硬化剂。

3. 发明授权

US4847384A Process for the preparation of certain nitrogen-containing mono- and bicyclic ace inhibitors, and novel intermediates useful therefor 失效
标题翻译：用于制备某些含氮单环和双环ace抑制剂的方法，以及可用于其的新型中间体
公开(公告)号：US4847384A
公开(公告)日：1989-07-11
申请号：US24959
申请日：1987-03-12
申请人： Prasad K. Kapa , Kau-Ming Chen
发明人： Prasad K. Kapa , Kau-Ming Chen
IPC分类号： C07K5/02
CPC分类号： C07K5/0222
摘要： An improved process for preparing certain nitrogen-containing mono- and bicyclic ACE inhibitors comprising reacting an .alpha.-alkyl amino acid with a disulfide compound to form a thioester intermediate, which intermediate is then amidated with a mono- or bicyclic amino acid. The invention also relates to the novel thioester intermediates prepared by the first step of the process.
摘要翻译：一种用于制备某些含氮单环和双环ACE抑制剂的改进方法，包括使α-烷基氨基酸与二硫化物化合物反应形成硫酯中间体，然后将该中间体与单环或双环氨基酸酰胺化。本发明还涉及通过该方法的第一步制备的新的硫酯中间体。

4. 发明授权

US5319123A Process for preparing substituted N-oxy-imidic acid derivatives 失效
标题翻译：制备取代的N-氧代亚氨基酸衍生物的方法
公开(公告)号：US5319123A
公开(公告)日：1994-06-07
申请号：US701933
申请日：1991-05-17
申请人： George T. Lee , Ustun B. Sunay , Prasad K. Kapa
发明人： George T. Lee , Ustun B. Sunay , Prasad K. Kapa
IPC分类号： C07C259/06 , C07C259/10 , C07C249/00
CPC分类号： C07C259/06 , C07C259/10 , Y02P20/55
摘要： N-oxy substituted imidic acid derivative of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are alkyl and aryl substituents, which are useful as antidiabetic and hypolipidemic agents are prepared by the following procedure: ##STR2## where X is chlorine, bromine, or iodine, and R.sub.1 ' is the same as R.sub.1 but with any hydroxy or carboxy groups present protected by a hydroxy or carboxy protecting group and, when R.sub.1 ' is a protected hydroxy or carboxy substituent, deprotecting the substituent.
摘要翻译：其中R 1，R 2和R 3是烷基和芳基取代基的N-氧取代的亚氨基酸衍生物，其用作抗糖尿病和降血脂剂是通过以下方法制备的：其中X是氯，溴，或碘，并且R 1'与R 1相同，但具有由羟基或羧基保护基团保护的任何羟基或羧基，并且当R 1'为被保护的羟基或羧基取代基时，使取代基脱保护。

5. 发明授权

US5290946A Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes 失效
标题翻译：用于合成3-（取代的吲哚基-2-基）丙醛的方法
公开(公告)号：US5290946A
公开(公告)日：1994-03-01
申请号：US980055
申请日：1992-11-23
申请人： George T. Lee , Prasad K. Kapa , Oljan Repic
发明人： George T. Lee , Prasad K. Kapa , Oljan Repic
IPC分类号： C07C51/367 , C07C59/48 , C07C223/02 , C07D209/12 , C07D209/24 , C07D233/54
CPC分类号： C07D233/64 , C07C223/02 , C07C51/367 , C07C59/48 , C07D209/12 , C07D209/24
摘要： A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R.sub.1 R.sub.2 N--CHO and CH.sub.2 .dbd.CH--O--R.sub.10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R.sub.1 is phenyl or substituted phenyl or intermediates in the synthesis of the compounds of formula I which intermediates have the formula ##STR3## wherein R.sub.1 is C.sub.1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),R.sub.2 is C.sub.1-3 alkyl,R.sub.10 is C.sub.1-6 alkyl,X.sup..crclbar. is chloride or bromide, andR.sub.3 -R.sub.6 are as defined in the specification.The compounds of Formula II are intermediates in the synthesis of known HMB-CoA reductase inhibitors which inhibit the biosynthesis of cholesterol and are useful as antihyperchloesterolemic agents.
摘要翻译：合成式（I）化合物的方法利用草酰氯或溴化物作为中间体，式R1R2N-CHO和CH2 = CH-O-R10的化合物是合成下式化合物的方法：（II）使用式I化合物，其中R 1是苯基或取代的苯基或中间体在合成式I化合物中的中间体具有下式其中R 1是C 1-3烷基，苯基或苯基取代 1至3个取代基，各自独立地为C 1-3烷基，C 1-3烷氧基，氟，氯，溴或硝基（最多为两个硝基），R 2为C 1-3烷基，R 10为C 1-6烷基，X（ - ）为氯化物或溴化物，和R3-R6如说明书中所定义。式II化合物是合成已知的抑制胆固醇生物合成的HMB-CoA还原酶抑制剂的中间体，可用作抗高胆固醇酯剂。

6. 发明授权

US5412137A Process for preparing phosphinyloxy propanaminium inner salt derivatives 失效
标题翻译：制备膦酰氧基丙胺内盐衍生物的方法
公开(公告)号：US5412137A
公开(公告)日：1995-05-02
申请号：US197050
申请日：1994-02-16
申请人： Mahavir Prashad , Prasad K. Kapa
发明人： Mahavir Prashad , Prasad K. Kapa
IPC分类号： C07F9/09 , C07F9/113 , C07F9/165 , C07F9/173
CPC分类号： C07F9/173 , C07F9/091 , C07F9/113 , C07F9/1651
摘要： A process for preparing compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined herein,R.sub.2, R.sub.3, and R.sub.4 are each independently straight or branched chain (C.sub.1-4)alkyl,and pharmaceutically acceptable salts, physiological hydrolyzable esters, and pro-drug forms thereof, which are useful as hypoglycemic agents.
摘要翻译：制备式（I）的化合物的方法，其中X 1和X 2独立地为O或S，R 1如本文所定义，R 2，R 3和R 4各自独立地为直链或支链（C 1-4）烷基，以及其可用作降血糖剂的药学上可接受的盐，生理可水解的酯和其前药形式。

7. 发明授权

US4571428A 6-Substituted-4-hydroxy-tetrahydropyran-2-ones 失效
标题翻译： 6-取代的-4-羟基 - 四氢吡喃-2-酮
公开(公告)号：US4571428A
公开(公告)日：1986-02-18
申请号：US512163
申请日：1983-07-08
申请人： Prasad K. Kapa
发明人： Prasad K. Kapa
IPC分类号： C07D209/24 , C07D309/20 , C07D405/06 , C07F7/18 , C07F7/08 , C07F7/10 , C07C69/76
CPC分类号： C07D405/06 , C07D209/24 , C07D309/20 , C07F7/1856
摘要： 6-Substituted-4-hydroxy-tetrahydropyran-2-ones, useful as anti-atherosclerotic agents, are obtainable by the process of the invention. The 6-substituents have a phenyl, naphthyl, tetrahydronaphthyl or indolyl nucleus bound through an ethenyl unit. The invention includes novel intermediates.
摘要翻译：可用作抗动脉粥样硬化剂的6-取代的4-羟基 - 四氢吡喃-2-酮可通过本发明的方法获得。 6-取代基具有通过乙烯单元结合的苯基，萘基，四氢萘基或吲哚基核。本发明包括新型中间体。

8. 发明申请

US20120245182A1 CRYSTALLINE FORMS OF 3-(2,6-DICHLORO-3,5-DIMETHOXY-PHENYL)-1--1-METHYL-UREA AND SALTS THEREOF 有权
标题翻译： 3-（2,6-二氯-3,5-二甲氧基苯基）-1- -1-甲基尿素及其盐的结晶形式
公开(公告)号：US20120245182A1
公开(公告)日：2012-09-27
申请号：US13514308
申请日：2010-12-06
申请人： Joerg Berghausen , Prasad K. Kapa , Joseph McKenna , Joel Slade , Raeann Wu , Zhengming Du , Frank Stowasswer
发明人： Joerg Berghausen , Prasad K. Kapa , Joseph McKenna , Joel Slade , Raeann Wu , Zhengming Du , Frank Stowasswer
IPC分类号： A61K31/506 , A61P35/00 , A61P35/02 , C07D403/12
CPC分类号： C07D239/48
摘要： The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.
摘要翻译：本技术提供3-（2,6-二氯-3,5-二甲氧基 - 苯基）-1- {6- [4-（4-乙基 - 哌嗪-1-基） - 苯基氨基）的新的无水和水合结晶形式 ] - 嘧啶-4-基} -1-甲基 - 脲，其单磷酸盐的无定形和无水结晶多晶型物，以及其盐酸盐，包括其二水合物。本技术还提供了制备各种形式的方法，含有它们的组合物和使用它们的治疗方法。

9. 发明授权

US5596094A Process for preparing 2' -0- alkyl adenosine derivatives 失效
标题翻译： 2'-烷基腺苷衍生物的制备方法
公开(公告)号：US5596094A
公开(公告)日：1997-01-21
申请号：US485595
申请日：1995-06-07
申请人： Mahavir Prashad , Prasad K. Kapa
发明人： Mahavir Prashad , Prasad K. Kapa
IPC分类号： C07H19/16 , C07H1/00 , C07H19/167
CPC分类号： C07H19/16
摘要： A process for alkylating the 2'-OH of N.sup.6 -modified adenosine comprising the reacting of an unprotected N.sup.6 -alkyl adenosine with dimethyl sulfate and tetrabutylammonium hydrogen sulfate in a non-polar solvent, preferably dichloromethane, and 5% sodium hydroxide. The products of the reaction are useful as anti-diabetic, hypolipidemic, and analgesic agents.
摘要翻译：使N6-修饰的腺苷的2'-OH烷基化的方法包括在非极性溶剂，优选二氯甲烷和5％氢氧化钠中使未受保护的N6 - 烷基腺苷与硫酸二甲酯和硫酸氢四丁基铵的反应。该反应的产物可用作抗糖尿病，降血脂和止痛剂。

10. 发明授权

US5338730A Use of the (R) isomer of 2-[(2-octa-decyloxymethyl-tetrahydro-2-furanylmethoxy)-hydroxyphosphinyl oxy]-N,N,N-trimethylethanaminium hydroxide inner salt-4-oxide in treating multiple sclerosis 失效
标题翻译： 2 - [（2-八氢 - 癸氧基甲基 - 四氢-2-呋喃基甲氧基） - 羟基氧膦基氧基] -N，N，N-三甲基乙基氢氧化铵内盐-4-氧化物的（R）异构体在治疗多发性硬化
公开(公告)号：US5338730A
公开(公告)日：1994-08-16
申请号：US073215
申请日：1993-06-04
申请人： Heinrich Estermann , Prasad K. Kapa , Russell L. Underwood , William J. Houlihan
发明人： Heinrich Estermann , Prasad K. Kapa , Russell L. Underwood , William J. Houlihan
IPC分类号： C07D307/12 , C07F9/655 , C07F9/6574 , A61K31/665 , C07F9/141
CPC分类号： C07D307/12 , C07F9/65515 , C07F9/65742 , Y10S514/903
摘要： A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
摘要翻译：制备2,2-双（羟基甲基） - 四氢呋喃单丁酸酯的（R）立体异构体的方法，包括使2,2-双（羟甲基） - 四氢呋喃的二酯进行酶水解。本发明还涉及通过本方法制备的新型（R）立体异构体及其更稳定的形式。此外，本发明涉及（R）立体异构体在制备药理活性化合物和由此制备的某些特定立体异构体的立体异构体中的用途。

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