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51. 发明授权

US6077805A Hexacoordinated ruthenium or osmium carbene catalysts 失效
标题翻译：六配位的钌或镉卡因催化剂
公开(公告)号：US6077805A
公开(公告)日：2000-06-20
申请号：US33265
申请日：1998-03-02
申请人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Muhlebach
发明人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Muhlebach
IPC分类号： B01J31/22 , B01J31/24 , C07F15/00 , C08G61/02 , C08G61/08 , B01J31/00 , C07D231/00 , C07D233/00 , C07F17/02
CPC分类号： B01J31/1815 , B01J31/181 , B01J31/183 , B01J31/2265 , B01J31/24 , B01J31/2404 , C07F15/002 , C07F15/0046 , C08G61/02 , B01J2231/14 , B01J2231/543 , B01J2531/821 , B01J2531/825
摘要： Hexacoordinated ruthenium and osmium catalysts of the formulae ##STR1## in which M and M' independently of one another are ruthenium or osmium;X, X', Y and Y' independently of one another are anionic ligands, or X and Y and X' and Y' in each case together are bis-anionic ligandsL.sup.1 and L.sup.1' independently of one another are tertiary phosphine;L.sup.2 and L.sup.3 independently of one another are a monodentate ligand, or L.sup.2 and L.sup.3 together are bidentate, neutral electron donor ligands;L.sup.4 is tetradentate, neutral electron donor ligand;L.sup.5 is a bidentate, neutral electron donor ligand; andT and T' indepedently of one another are H or organic substituents, are useful for the synthesis of custom-tailored polymers and for the ring-closing metathesis of olefins.
摘要翻译：其中M和M'彼此独立的下式的六配位钌和锇催化剂是钌或锇; X，X'，Y和Y'彼此独立的是阴离子配体，或者X和Y以及X'和Y'各自在一起是双阴离子配体，L1和L1'彼此独立地是叔膦; L2和L3彼此独立是单齿配体，或L2和L3一起是双齿中性电子给体配体; L4是四齿中性电子给体配体; L5是二齿中性电子给体配体; 且T和T'彼此独立地是H或有机取代基，可用于合成定制聚合物和烯烃的闭环复分解。

52. 发明授权

US5560862A Multiple-substituted bleach activators 失效
公开(公告)号：US5560862A
公开(公告)日：1996-10-01
申请号：US486905
申请日：1995-06-07
申请人： Eugene P. Gosselink , Gregory S. Miracle , Alan D. Willey , Michael E. Burns , Kevin L. Kott , Mark R. Sivik , Lucille F. Taylor
发明人： Eugene P. Gosselink , Gregory S. Miracle , Alan D. Willey , Michael E. Burns , Kevin L. Kott , Mark R. Sivik , Lucille F. Taylor
IPC分类号： B01J31/16 , C11D3/39 , C11D3/395 , C11D7/54 , C11D7/38 , C07D233/00
CPC分类号： C11D3/3927
摘要： Bleaching compositions, laundry and automatic dishwashing detergent compositions comprising multiple-substituted bleach activators which have at least one quaternary nitrogen atom, are provided. More specifically, the invention relates to compositions which provide enhanced cleaning/bleaching benefits though the selection of multiple-substituted quaternary bleach activators having specific leaving groups with a conjugate acid aqueous pK.sub.a above 13 and with advantageous ratios of rate of perhydrolysis to rate of hydrolysis and of rate of perhydrolysis to rate of diacylperoxide production. Included are preferred activator compounds and methods for washing fabrics, hard surfaces, and tableware using the activators.

53. 发明授权

US5358946A Heterocycle-substituted amides, carbamates and ureas as agents for the treatment of atherosclerosis 失效
标题翻译：杂环取代的酰胺，氨基甲酸酯和脲作为治疗动脉粥样硬化的药物
公开(公告)号：US5358946A
公开(公告)日：1994-10-25
申请号：US889896
申请日：1992-05-29
申请人： Richard G. Wilde
发明人： Richard G. Wilde
IPC分类号： C07D233/54 , C07D233/66 , C07D233/84 , C07D233/88 , C07D405/14 , A61K31/535 , A61K31/415 , C07D233/00 , C07D265/28 , C07D413/02
CPC分类号： C07D233/64 , C07D233/84 , C07D233/88 , C07D405/14
摘要： This invention relates to imidazoles, namely, heterocycle-substituted amides, carbamates and ureas as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), pharmaceutical compositions containing them, and their use as antihypercholesterolemic and/or antiatherosclerotic agents for the treatment of atherosclerosis.
摘要翻译：本发明涉及咪唑，即杂环取代的酰胺，氨基甲酸酯和尿素作为酰基-CoA：胆固醇酰基转移酶（ACAT）的抑制剂，含有它们的药物组合物，以及它们作为抗高胆固醇血症和/或抗动脉粥样硬化治疗动脉粥样硬化的用途。

54. 发明授权

US5294722A Process for the preparation of imidazoles useful in angiotensin II antagonism 失效
标题翻译：用于制备用于血管紧张素II拮抗作用的咪唑的方法
公开(公告)号：US5294722A
公开(公告)日：1994-03-15
申请号：US869971
申请日：1992-04-16
申请人： Kyoung S. Kim
发明人： Kyoung S. Kim
IPC分类号： C07D233/54 , C07D233/90 , C07D403/06 , C07D403/14 , C07D235/30 , C07D233/00 , C07D235/04
CPC分类号： C07D233/54 , C07D233/90 , C07D403/06 , C07D403/14
摘要： Imidazoles of the formula ##STR1## are prepared by treating a ketone ##STR2## with a nitrogenic acid, nitrite or nitrate in the presence of an acid to form a hydroxynitrile ##STR3## which is treated with R.sup.2 --CHO and an ammonium to form an N-hydroxyimidazole ##STR4## which is reduced in the presence of a buffer. In these compounds, R.sup.1 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, or --(CH.sub.2).sub.m Z(CH.sub.2).sub.n R.sup.3, each of which is optionally substituted with F or --CO.sub.2 R.sup.1 ; or aryl or aralkyl, each of which is optionally substituted with 1 or 2 groups selected from halogen, lower alkoxy, lower alkyl, or nitro;R.sup.3 is hydrogen, alkyl, cycloalkyl, lower alkenyl, or lower alkynyl;and the remaining symbols are as defined in the specification.
摘要翻译：通过在酸存在下用氮酸，亚硝酸盐或硝酸盐处理酮，制备式“IMAGE”的咪唑，以形成羟基腈，其用R2-CHO和铵处理形成在缓冲液存在下还原的N-羟基咪唑。在这些化合物中，R 1是氢，烷基，卤代烷基，环烷基，环烷基烷基，芳基或芳烷基; R2是烷基，烯基，炔基，环烷基，环烷基烷基，环烷基烯基，环烷基炔基或 - （CH2）mZ（CH2）nR3，其各自任选被F或-CO 2 R 1取代; 或芳基或芳烷基，其各自任选被1或2个选自卤素，低级烷氧基，低级烷基或硝基的基团取代; R3是氢，烷基，环烷基，低级烯基或低级炔基; 其余符号如说明书中所定义。

55. 发明授权

US4711855A Derivatives of 3,5,3-triiodothyronine 失效
标题翻译： 3,5,3-三碘甲状腺原氨酸衍生物
公开(公告)号：US4711855A
公开(公告)日：1987-12-08
申请号：US698108
申请日：1985-02-05
申请人： Richard R. Feinberg
发明人： Richard R. Feinberg
IPC分类号： C07D233/54 , G01N33/78 , G01N33/534 , C07D233/00 , C07D239/00 , G01N33/543
CPC分类号： C07D233/64 , G01N33/78 , Y10S436/804
摘要： A derivative of 3,5,3'-triiodothyronine having the following general formula: ##STR1## in which m is an integer from 2 to 4, n is an integer from 1 to 4, and R is a monovalent, unsubstituted, fully unsaturated five- or six-membered monocyclic heterocyclic group containing either one or two nitrogen atoms as the only hetero atoms.
摘要翻译：具有以下通式的3,5,3'-三碘甲腺原氨酸的衍生物：其中m为2至4的整数，n为1至4的整数，R为单价含有一个或两个氮原子作为唯一的杂原子的未取代的，完全不饱和的五元或六元单环杂环基。

56. 发明授权

US4690704A Derivatives of tetrahydrobenzothiazole and herbicidal compositions containing the same as an active ingredient 失效
标题翻译：四氢苯并噻唑的衍生物和含有其作为活性成分的除草组合物
公开(公告)号：US4690704A
公开(公告)日：1987-09-01
申请号：US820278
申请日：1986-01-17
申请人： Katsumichi Aoki , Takafumi Shida , Hideo Arabori , Satoru Kumazawa , Susumu Shimizue , Takeo Watanave , Yohichi Kanda , Keigo Satake , Shiro Yamazaki , Hiroyasu Shinkawa , Tsuneaki Chida
发明人： Katsumichi Aoki , Takafumi Shida , Hideo Arabori , Satoru Kumazawa , Susumu Shimizue , Takeo Watanave , Yohichi Kanda , Keigo Satake , Shiro Yamazaki , Hiroyasu Shinkawa , Tsuneaki Chida
IPC分类号： A01N43/78 , A01N43/82 , C07D233/00 , C07D271/00 , C07D277/00 , C07D417/04 , A01N47/38
CPC分类号： C07D417/04 , A01N43/78 , A01N43/82
摘要： Disclosed herein are a derivative of tetrahydrobenzothiazole represented by the formula (I): ##STR1## wherein R represents a methyl group or ethyl group; R.sup.1 represents a hydrogen atom, a hydroxyl group, methoxy group or O.dbd.=together with R.sup.2 ; R.sup.2 represents a hydrogen atom or O.dbd.=together with R.sup.1 ; and X represents a methylene group, hydroxymethylene group, carbonyl group or --O-- with the proviso that R is not a methyl group when (1) R.sup.1 represents a hydroxyl group or methoxy group and X represents a methylene group or hydroxymethylene group or (2) R.sup.2 represents .dbd.O together with R.sup.1 and X represents a carbonyl group, and a herbicidal composition containing the same as an active ingredient.

57. 发明授权

US4636505A Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US4636505A
公开(公告)日：1987-01-13
申请号：US514332
申请日：1983-07-15
申请人： Howard Tucker
发明人： Howard Tucker
IPC分类号： A61K31/165 , A61K8/00 , A61K8/11 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/505 , A61P5/00 , A61P15/00 , A61P17/00 , A61P43/00 , A61Q5/00 , C07C59/68 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/08 , C07C233/02 , C07C235/16 , C07C235/24 , C07C237/00 , C07C237/04 , C07C237/30 , C07C253/00 , C07C255/60 , C07C313/00 , C07C315/02 , C07C317/00 , C07C317/18 , C07C317/28 , C07C317/32 , C07C317/40 , C07C317/46 , C07C317/48 , C07C317/50 , C07C319/20 , C07C323/25 , C07C323/26 , C07C323/31 , C07C323/32 , C07C323/41 , C07C323/60 , C07C323/63 , C07C323/65 , C07D213/32 , C07D213/70 , C07D213/71 , C07D233/00 , C07D233/84 , C07D239/10 , C07D239/38 , C07D277/20 , C07D277/36 , C07D277/70 , C07D277/74 , C07D285/12 , C07D285/125 , C07D303/48 , C07D333/34 , C07D333/62 , A61K31/16
CPC分类号： C07D285/125 , C07C255/00 , C07C321/00 , C07C323/00 , C07C59/68 , C07D213/70 , C07D233/84 , C07D239/38 , C07D277/36 , C07D303/48 , C07D333/62
摘要： Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.9 ; processes for their manufacture and pharmaceutical compositions containing them. The acylanilides possess antiandrogenic activity.
摘要翻译：其中R 1和R 2相同或不同，各自为氰基，氨基甲酰基，硝基，卤代，全氟烷基或其它限定的取代基的酰基酰亚胺; R3是氢或卤素; R4是氢或烷基，或与R5连接; R5是氢，羟基，烷氧基或酰氧基或与R4连接; R6是烷基或卤代烷基，或具有式-A3-R8或-A4-X2-A5-R9; A1和A4相同或不同，各自为亚烷基; A2，A3和A5相同或不同，各自是直链或亚烷基; X1和X2相同或不同，分别为氧，硫，亚磺酰基，磺酰基，亚氨基或烷基亚氨基; R 7和R 9相同或不同，各自为烷基，烯基，羟基烷基，环烷基，任选取代的苯基，任选取代的萘基或杂环; 并且R 8是如上定义的对于R 7或R 9的苯基，萘基或杂环; 其制造方法和含有它们的药物组合物。酰苯胺具有抗雄激素活性。

58. 发明授权

US4631282A Antihypertensive chromans and chromenes 失效
标题翻译：抗高血压染色剂和色烯
公开(公告)号：US4631282A
公开(公告)日：1986-12-23
申请号：US746968
申请日：1985-06-20
申请人： Frederick Cassidy
发明人： Frederick Cassidy
IPC分类号： C07D311/68 , A61K20060101 , A61K31/35 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/50 , A61P9/12 , C07D20060101 , C07D207/00 , C07D233/00 , C07D241/00 , C07D311/00 , C07D311/70 , C07D405/04 , C07D405/12
CPC分类号： C07D405/04 , C07D311/70
摘要： Antihypertensive compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow.
摘要翻译：式（I）的抗高血压化合物：其中各种取代基如下文所定义。

59. 发明授权

US4619931A [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-diox olan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles 失效
标题翻译： [[4- [4-（4-苯基-1-哌嗪基）苯氧基甲基] -1,3-二氧戊环-2-基]甲基] -1H-咪唑和1H-1,2,4-三唑
公开(公告)号：US4619931A
公开(公告)日：1986-10-28
申请号：US569122
申请日：1984-01-09
申请人： Jan Heeres , Raymond A. Stokbroekx , Leo J. J. Backx
发明人： Jan Heeres , Raymond A. Stokbroekx , Leo J. J. Backx
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/42 , A61K31/425 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/54 , A61P31/04 , C07C233/43 , C07D233/00 , C07D233/32 , C07D233/36 , C07D233/38 , C07D233/40 , C07D233/42 , C07D233/44 , C07D233/50 , C07D233/72 , C07D233/74 , C07D233/78 , C07D233/96 , C07D239/00 , C07D239/10 , C07D241/00 , C07D249/00 , C07D249/08 , C07D249/12 , C07D263/28 , C07D263/44 , C07D265/08 , C07D277/18 , C07D277/42 , C07D279/06 , C07D285/08 , C07D295/096 , C07D295/135 , C07D403/04 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D521/00 , C07D403/14
CPC分类号： C07D295/096 , C07D231/12 , C07D233/32 , C07D233/36 , C07D233/56 , C07D233/72 , C07D249/08 , C07D277/42 , C07D279/06 , C07D295/135 , C07D487/04
摘要： Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.
摘要翻译：取代的[[4- [4-（4-苯基-1-哌嗪基）苯氧基甲基] -1,3-二氧戊环-2-基]甲基] -1H-咪唑和具有抗微生物性质的1 H-1,2,4-三唑特别适用于治疗阴道念珠菌病。

60. 发明授权

US4496542A N-substituted-amido-amino acids 失效
标题翻译： N-取代的酰氨基 - 氨基酸
公开(公告)号：US4496542A
公开(公告)日：1985-01-29
申请号：US484729
申请日：1983-04-13
申请人： Jerry W. Skiles , Raymond D. Youssefyeh , John T. Suh , Howard Jones
发明人： Jerry W. Skiles , Raymond D. Youssefyeh , John T. Suh , Howard Jones
IPC分类号： A61K38/00 , C07D233/56 , C07D233/88 , C07K5/02 , A61K37/00 , A61K31/40 , A61K31/425 , C07C103/52 , C07D211/30 , C07D211/56 , C07D211/72 , C07D215/00 , C07D221/02 , C07D233/00 , C07D233/28 , C07D233/66 , C07D235/04 , C07D265/30 , C07D279/10 , C07D403/00 , C07D405/00 , C07D413/00 , C07D415/00
CPC分类号： C07K5/0222 , A61K38/00
摘要： Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclic and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.
摘要翻译：其中R和R9独立地是羟基和低级烷氧基，R1和R2独立地是氢，具有7-12个碳原子的低级烷基，芳基 - 低级烷基或具有6-12个碳原子的杂环 - 低级烷基碳原子，R3，R4，R5，R7和R8是氢或低级烷基，R6是杂环及其药学上可接受的无毒酸加成盐，其中R或R9或两者均为羟基，其药学上可接受的无毒碱性盐具有抗高血压活动。

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