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21. 发明授权

US5916891A Pyrimidinyl imidazoles 失效
标题翻译：嘧啶基咪唑
公开(公告)号：US5916891A
公开(公告)日：1999-06-29
申请号：US481671
申请日：1995-06-07
申请人： Jerry Leroy Adams , Timothy Francis Gallagher , John C. Lee , John Richard White
发明人： Jerry Leroy Adams , Timothy Francis Gallagher , John C. Lee , John Richard White
IPC分类号： C07D401/04 , C07D403/04 , C07D409/14 , C07D413/14 , C07D495/04 , C07F9/6506 , C07F9/6558 , A61K31/505
CPC分类号： C07D401/04 , C07D403/04 , C07D409/14 , C07D413/14 , C07D495/04 , C07F9/65062 , C07F9/65583
摘要： Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.
摘要翻译：新型2,4,5-三芳基咪唑化合物和用于治疗的组合物。

22. 发明授权

US5538957A Phosphonosuccinic acid derivatives, processes for their preparation and medicaments containing these compounds 失效
标题翻译：膦酸琥珀酸衍生物，其制备方法和含有这些化合物的药物
公开(公告)号：US5538957A
公开(公告)日：1996-07-23
申请号：US244245
申请日：1994-06-03
申请人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
发明人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
IPC分类号： A61K31/66 , A61K31/662 , A61K31/675 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/58 , C07F9/6506 , C07F9/6509 , C07C229/24
CPC分类号： C07F9/65062 , C07F9/3808 , C07F9/4006 , C07F9/5532 , C07F9/5721 , C07F9/5722 , C07F9/582 , C07F9/65061
摘要： Compounds of the formula (I) in which: R is a possibly substituted amino group of the general form --NR.sub.1 R.sub.2, in which R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, lower alkenyl or lower alkinyl, or R is a saturated, unsaturated or aromatic heterocyclic ring which may be mono or bi-substituted by lower alkyl or halogen; alk is a valency bond, a methylene, a saturated or unsaturated, straight or branched-chain alkylene chain with 2-6 carbon atoms; and R.sup.3, R.sup.4, R.sup.5 are independently hydrogen, lower alkyl or benzyl; and their pharmacologically acceptable salts and enantiomers where, if R.sup.3 .dbd.R.sup.4 .dbd.R.sup.5 .dbd.CH.sub.3 and alk is a valency bond, R may not be the dimethyl amino group. Process for their production and medicaments containing these compounds, for the treatment of calcium metabolic complaints.
摘要翻译： PCT No.PCT / EP92 / 02890 Sec。 371日期：1994年6月3日 102（e）日期1994年6月3日PCT提交1992年12月14日PCT公布。出版物WO93 / 12122 （I）式（I）的化合物，其中：R为通式-NR1R2的可能取代的氨基，其中R1和R2独立地为氢，低级烷基，低级烯基或低级炔基，或R是可以被低级烷基或卤素单取代或二取代的饱和，不饱和或芳族杂环; alk是具有2-6个碳原子的价键，亚甲基，饱和或不饱和的直链或支链亚烷基链; 且R 3，R 4，R 5独立地是氢，低级烷基或苄基; 和其药理学上可接受的盐和对映异构体，其中如果R3 = R4 = R5 = CH3且alk为价键，R可能不是二甲基氨基。其生产工艺及含有这些化合物的药物，用于治疗钙代谢性疾病。

23. 发明授权

US5489717A Glutamate (NMDA) receptor antagonists 失效
标题翻译：谷氨酸（NMDA）受体拮抗剂
公开(公告)号：US5489717A
公开(公告)日：1996-02-06
申请号：US271961
申请日：1994-07-08
申请人： Christopher F. Bigge , James J. Li
发明人： Christopher F. Bigge , James J. Li
IPC分类号： C07C17/14 , C07C22/04 , C07F9/38 , C07F9/40 , C07F9/6506
CPC分类号： C07F9/65062 , C07C17/14 , C07C22/04 , C07F9/3882 , C07F9/4056
摘要： Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.
摘要翻译：描述了新的萘基取代的α-氨基酸衍生物，含有它们的药物组合物及其使用方法，用于封闭天冬氨酸和谷氨酸受体。公开了萘基取代的α-氨基酸衍生物的新型中间体。

24. 发明授权

US5276021A Phosphorus-containing HMG-COA reductase inhibitors, new intermediates and method 失效
标题翻译：含磷的HMG-COA还原酶抑制剂，新的中间体和方法
公开(公告)号：US5276021A
公开(公告)日：1994-01-04
申请号：US810099
申请日：1991-12-19
申请人： Donald S. Karanewsky , Michael C. Badia , Scott A. Biller , Eric M. Gordon , Michael J. Sofia
发明人： Donald S. Karanewsky , Michael C. Badia , Scott A. Biller , Eric M. Gordon , Michael J. Sofia
IPC分类号： C07F9/30 , C07F9/32 , C07F9/40 , C07F9/572 , C07F9/6503 , C07F9/6506 , C07F9/02 , C07C69/73 , A61K31/66
CPC分类号： C07F9/65062 , C07F9/301 , C07F9/302 , C07F9/303 , C07F9/306 , C07F9/3211 , C07F9/3217 , C07F9/3241 , C07F9/4006 , C07F9/5721 , C07F9/5722 , C07F9/5728 , C07F9/65033
摘要： Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## wherein R is OH, or salts thereof or lower alkoxy;R.sup.x is H or alkyl;X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 CH.sub.2 CH.sub.2 -- or --CH.sub.2 O-- (where O is linked to Z);Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds.
摘要翻译：提供可用作胆固醇生物合成抑制剂，因此作为低胆固醇血症药物的化合物，其具有其中R为OH的结构（*化学结构*），或其盐或低级烷氧基; Rx是H或烷基; X是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - ， - C（三键）C - ， - CH 2 CH 2 CH 2 - 或-CH 2 O-（其中O与Z连接）; （*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）（*化学结构*）其中虚线表示任选的双键。

25. 发明授权

US5116934A Polyimidazoles via aromatic nucleophilic displacement 失效
标题翻译：聚咪唑通过芳族亲核取代
公开(公告)号：US5116934A
公开(公告)日：1992-05-26
申请号：US732884
申请日：1991-07-19
申请人： John W. Connell , Paul M. Hergenrother
发明人： John W. Connell , Paul M. Hergenrother
IPC分类号： C07D233/54 , C07F9/6506 , C08G65/40 , C08G73/06 , C08G73/18
CPC分类号： C07D233/64 , C07F9/65062 , C08G65/4037 , C08G73/0616 , C08G73/18
摘要： Polyimidazoles (Pl) are prepared by the aromatic nucleophilic displacement reaction of di(hydroxyphenyl)imidazole monomers with activated aromatic dihalides or activated aromatic dinitro compounds. The reactions are carried out in polar aprotic solvents such as N,N-dimethylacetamide, sulfolane, N-methylpyrrolidinone, dimethylsulfoxide, or diphenylsulfone using alkali metal bases such as potassium carbonate at elevated temperatures under nitrogen. The di(hydroxyphenyl)imidazole monomers are prepared by reacting an aromatic aldehyde with a dimethoxybenzil or by reacting an aromatic dialdehyde with a methoxybenzil in the presence of ammonium acetate. The di(methoxyphenyl)imidazole is subsequently treated with aqueous hydrobromic acid to give the di(hydroxyphenyl)imidazole monomer. This synthetic route has provided high molecular weight Pl of new chemical structure, is economically and sythetically more favorable than other routes, and allows for facile chemical structure variation due to the availability of a large variety of activated aromatic dihalides and dinitro compounds.
摘要翻译：通过二（羟基苯基）咪唑单体与活性芳族二卤化物或活性芳族二硝基化合物的芳族亲核取代反应制备聚咪唑（P1）。反应在极性非质子溶剂如N，N-二甲基乙酰胺，环丁砜，N-甲基吡咯烷酮，二甲基亚砜或二苯基砜中，使用碱金属碱如碳酸钾，在氮气下在升高的温度下进行。二（羟基苯基）咪唑单体是通过使芳族醛与二甲氧基苯甲醚反应或在乙酸铵存在下使芳族二醛与甲氧基苯甲醚反应来制备的。随后用氢溴酸水溶液处理二（甲氧基苯基）咪唑，得到二（羟基苯基）咪唑单体。这种合成路线提供了新的化学结构的高分子量P1，在经济上和应用上比其他途径更有利，并且由于大量活性芳族二卤化物和二硝基化合物的可用性而允许容易的化学结构变化。

26. 发明授权

US5066811A Polyimidazoles via aromatic nucleophilic displacement 失效
标题翻译：聚咪唑通过芳族亲核取代
公开(公告)号：US5066811A
公开(公告)日：1991-11-19
申请号：US508316
申请日：1990-04-12
申请人： John W. Connell , Paul M. Hergenrother
发明人： John W. Connell , Paul M. Hergenrother
IPC分类号： C07D233/54 , C07F9/6506 , C08G65/40 , C08G73/06 , C08G73/18
CPC分类号： C07D233/64 , C07F9/65062 , C08G65/4037 , C08G73/0616 , C08G73/18
摘要： Polyimidazoles (Pl) are prepared by the aromatic nucleophilic displacement reaction of di(hydroxyphenyl)imidazole monomers with activated aromatic dihalides or activated aromatic dinitro compounds. The reactions are carried out in polar aprotic solvents such as N,N-dimethylacetamide, sulfolane, N-methylpyrroldinone, dimethylsulfoxide, or diphenylsulfone using alkali metal bases such as potassium carbonate at elevated temperature under nitrogen. The di(hydroxyphenyl)imidazole monomers are prepared by reacting an aromatic aldehyde with a dimethoxybenzil or by reacting an aromatic dialdehyde with a methoxybenzil in the presence of ammonium acetate. The di(methoxyphenyl)imidazole is subsequently treated with aqueous hydrobromic acid to give the di(hydroxyphenyl)imidazole monomer. This synthetic route has provided high molecular weight Pl of new chemical structure, is economically and synthetically more favorable than other routes, and allows for facile chemical structure variation due to the availability of a large variety of activated aromatic dihalides and dinitro compounds.
摘要翻译：通过二（羟基苯基）咪唑单体与活性芳族二卤化物或活性芳族二硝基化合物的芳族亲核取代反应制备聚咪唑（P1）。反应在极性非质子溶剂如N，N-二甲基乙酰胺，环丁砜，N-甲基吡咯烷酮，二甲基亚砜或二苯基砜中，使用碱金属碱如碳酸钾，在升高的温度下在氮气下进行。二（羟基苯基）咪唑单体是通过使芳族醛与二甲氧基苯甲醚反应或在乙酸铵存在下使芳族二醛与甲氧基苯甲醚反应来制备的。随后用氢溴酸水溶液处理二（甲氧基苯基）咪唑，得到二（羟基苯基）咪唑单体。这种合成路线提供了新的化学结构的高分子量Pl，在经济上和综合性上比其他途径更有利，并且由于大量活性芳族二卤化物和二硝基化合物的可用性而允许容易的化学结构变化。

27. 发明授权

US4894463A Process for preparing thiophene derivatives 失效
标题翻译：制备噻吩衍生物的方法
公开(公告)号：US4894463A
公开(公告)日：1990-01-16
申请号：US232678
申请日：1988-08-16
申请人： Holger Blum
发明人： Holger Blum
IPC分类号： C07D495/04 , C07F9/6506
CPC分类号： C07D495/04 , C07F9/65062
摘要： Thiophene derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, each are hydrogen or lower acyl and R.sub.6 is hydrogen or lower alkyl, are prepared by the reaction of a compound of the general formula ##STR2## wherein R.sub.3 is lower alkyl, R.sub.4 and R.sub.5 are lower acyl and X is chlorine, bromine or iodine, with a strong basic quaternary ammonium anion exchange resin in the monothiophosphate form to form a polymer intermediate product of the formula ##STR3## wherein R.sub.3, R.sub.4, and R.sub.5 have the significances given above, and (P).sup.+++ represents a polymer cation, which after purification in an acidic medium is reacted to the thiophene derivative of formula (I).The invention further relates to the novel polymer compound of formula (III) obtained in this process as an intermediate product.
摘要翻译：通式为其中R 1和R 2可以相同或不同，各自为氢或低级酰基，R6为氢或低级烷基的噻吩衍生物通过通式图像（II）其中R3是低级烷基，R4和R5是低级酰基，X是氯，溴或碘，具有一种硫代磷酸盐形式的强碱性季铵阴离子交换树脂，以形成下式的聚合物中间产物：（III）其中R3，R4和R5具有上述含义，（P）+++表示在酸性介质中纯化后与式（I）的噻吩衍生物反应的聚合物阳离子。本发明还涉及在该方法中获得的作为中间产物的新型式（III）的聚合物化合物。

28. 发明授权

US4755606A Imidazolyl-3,5-di-(diphenyl-butylsilyloxy) carboxylic acid ester intermediates 失效
标题翻译：咪唑基-3,5-二 - （二苯基 - 丁基甲硅烷氧基）羧酸酯中间体
公开(公告)号：US4755606A
公开(公告)日：1988-07-05
申请号：US79194
申请日：1987-07-29
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D233/54 , C07D233/64 , C07F7/18 , C07F9/6506 , C07D7/18
CPC分类号： C07D233/64 , C07F7/1852 , C07F7/1856 , C07F9/65062
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined herein below,the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
摘要翻译：式IMA的化合物及其药学上可接受的酸加成盐，其中各种取代基如下文所定义，其用于抑制胆固醇生物合成和降低血液胆固醇水平，因此用于治疗高脂蛋白血症和动脉粥样硬化，包含这些化合物的药物组合物和合成这些化合物的方法和中间体。

29. 发明授权

US4687767A Certain 1-hydroxyethane, 1,1-di-phosphonic acid derivatives useful in treating calcium metabolism disturbances 失效
标题翻译：某些用于治疗钙代谢紊乱的1-羟基乙烷，1,1-二膦酸衍生物
公开(公告)号：US4687767A
公开(公告)日：1987-08-18
申请号：US759608
申请日：1985-07-26
申请人： Elmar Bosies , Rudi Gall
发明人： Elmar Bosies , Rudi Gall
IPC分类号： A61K31/675 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/553 , C07F9/58 , C07F9/6506 , C07F9/6515 , C07F9/6518 , C07F9/653 , C07F9/65 , A61K31/44 , A61K31/415
CPC分类号： C07F9/3839 , C07F9/582 , C07F9/65062 , C07F9/65182 , C07F9/653
摘要： The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.
摘要翻译：本发明提供了以下通式的二膦酸盐：其中Het是咪唑，恶唑，异恶唑，噻唑，吡啶，1,2,3-三唑，1,2,4-三唑或苯并咪唑基，其中烷氧基，卤素，羟基，羧基，任选被烷基或烷酰基取代的氨基或任选被烷基，硝基，氨基或氨基烷基取代的苄基，A是直链或支链，饱和或含有2至8个碳原子的不饱和烃链，X是任选被烷酰基取代的氢原子或任选被烷基或烷酰基取代的氨基，R是氢原子或烷基; 及其药理学上可接受的盐。本发明还提供了制备这些二膦酸盐和含有它们的药物组合物的方法。

30. 发明授权

US3883546A S-heterocyclic derivatives of phosphine or phosphite gold mercaptides 失效
标题翻译：膦或亚磷酸盐金硫醇的S-杂环衍生物
公开(公告)号：US3883546A
公开(公告)日：1975-05-13
申请号：US38466673
申请日：1973-08-01
申请人： SMITHKLINE CORP
发明人： SUTTON BLAINE M , WEINSTOCK JOSEPH
IPC分类号： C07D235/24 , A61K31/66 , A61P29/00 , C07F9/02 , C07F9/143 , C07F9/145 , C07F9/50 , C07F9/62 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/6541 , C07D91/32 , C07D49/36 , C07D85/44
CPC分类号： C07F9/6541 , C07F9/65062 , C07F9/65068 , C07F9/6539 , Y10S514/825
摘要： S-Heterocyclic derivatives of phosphine or phosphite gold mercaptides are prepared by reaction of an heterocyclic mercaptan compound with an appropriate phosphine or phosphite gold halide in the presence of alkali.
摘要翻译：膦或亚磷酸盐金硫醇的S-杂环衍生物通过在碱存在下使杂环硫醇化合物与适当的膦或亚磷酸盐卤化金卤反应来制备。

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