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1. 发明授权

US5612002A Apparatus and method for multiple simultaneous synthesis 失效
标题翻译：多种同步合成的装置和方法
公开(公告)号：US5612002A
公开(公告)日：1997-03-18
申请号：US430696
申请日：1995-04-28
申请人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
发明人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： A method for the multiple, simultaneous synthesis of compounds comprising the steps of: 1) providing an apparatus comprising a plurality of reaction tubes having filter members on their lower ends, a reservoir member for receiving the filter member, a holder member having a plurality of apertures for supporting the reaction tubes, and a manifold member adjacent to the holder member and enclosing the upper ends of the reaction tubes; 2) charging the apparatus with reactants required for synthesis; 3) synthesizing the compounds in solution; or optionally 4) cleaving the compounds from a solid support within the apparatus.
摘要翻译：一种用于多次同时合成化合物的方法，包括以下步骤：1）提供一种装置，包括在其下端具有多个具有过滤器构件的反应管，用于容纳过滤构件的储存器构件，具有多个用于支撑反应管的孔，以及与保持器构件相邻并包围反应管的上端的歧管构件; 2）用合成所需的反应物对设备进行充电; 3）在溶液中合成化合物; 或任选地4）在装置内从固体支持物上切割化合物。

2. 发明授权

US5489611A Method for lowering plasma levels of lipoprotein (a) 失效
标题翻译：降低脂蛋白血浆水平的方法（a）
公开(公告)号：US5489611A
公开(公告)日：1996-02-06
申请号：US388043
申请日：1995-02-10
申请人： Helen T. Lee , Joseph A. Picard , Randy R. Ramharack , Bruce D. Roth , Drago R. Sliskovic
发明人： Helen T. Lee , Joseph A. Picard , Randy R. Ramharack , Bruce D. Roth , Drago R. Sliskovic
IPC分类号： A61K31/07 , A61K31/11 , A61K31/203 , A61K31/215 , A61K31/23 , A61P7/00 , A61K31/19
CPC分类号： A61K31/11 , A61K31/07 , A61K31/203 , A61K31/215 , Y10S514/824
摘要： Retinoids are effective to lower plasma levels of Lp (a) in mammals.
摘要翻译：类维生素A有助于降低哺乳动物中的Lp（a）的血浆水平。

3. 发明授权

US5324483A Apparatus for multiple simultaneous synthesis 失效
标题翻译：多次同时合成的装置
公开(公告)号：US5324483A
公开(公告)日：1994-06-28
申请号：US12557
申请日：1993-02-02
申请人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
发明人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , C08F283/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
摘要翻译：提供合适的位置用于多次同时合成化合物的装置和方法。该装置包括：具有多个井的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 以及可以具有允许引入/维护受控环境的端口的歧管。歧管顶壁具有孔和具有相同孔的可拆卸板。该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。垫片放在组件之间。提供杆或夹具用于将部件固定在一起。设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。该装置提供超过1mg每种产品的结构知识和对每种化合物的控制。使用该装置，一系列构建块共价连接到固体支持物上。然后通过共价添加其他不同的构建块或化学修饰一些现有功能来修改这些构建块，直到实现倒数第二个结构。然后通过另一种化学反应将固体支持物从该固体支持物中裂解成孔内的溶液，得到新合成的单独化合物的阵列，其在反应后修饰（如果需要）适于测试活性。

4. 发明授权

US5245047A Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis 失效
标题翻译：反式-6- [2-（取代 - 吡咯-1-基）烷基]吡喃-2-酮胆固醇合成抑制剂的方法
公开(公告)号：US5245047A
公开(公告)日：1993-09-14
申请号：US18481
申请日：1993-02-16
申请人： Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
发明人： Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
IPC分类号： C07C235/80 , C07D207/34 , C07D319/06 , C07D319/08 , C07D405/06
CPC分类号： C07D319/08 , C07C235/80 , C07D207/34 , C07D319/06 , C07D405/06
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl) ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2 H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl) dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.
摘要翻译：描述了通过新的合成制备反式-6- [2-（取代的 - 吡咯-1-基）烷基]吡喃-2-酮的改进方法，其中将1,6-庚二烯-4-醇转化为8 （2R-反式）和反 - （+/-） - 5-（4-氟苯基）-2-（1-甲基乙基）-N，4- 二苯基-1- [2-（叔 - 羟基-6-氧代-2H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺，通过新的合成法，其中4-甲基-3-氧代 - N-苯基戊酰胺在八个操作中转化成所需产物，或者4-氟-α-[2-甲基-1-氧代丙基]-γ-氧代-N，β-二苯基苯丁酰胺在一个步骤中转化为所需产物，和另外，制备（2R-反式）-5-（4-氟苯基）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢-4-羟基-6-氧代 -2H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺，由（R）-4-氰基-3 - [[（1,1-二甲基乙基）二甲基甲硅烷基]氧基]丁酸，以及其他有价值的中间体使用 d在进程中。

5. 发明授权

US5102893A Trans-6-(2-(n-heteroaryl-3,5-disubstituted)pyrazol-4-yl)-ethyl- or ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis 失效
标题翻译：反式-6-（2-（正 - 杂芳基-3,5-二取代）吡唑-4-基） - 乙基或乙烯基）四氢-4-羟基吡喃-2-酮胆固醇生物合成抑制剂
公开(公告)号：US5102893A
公开(公告)日：1992-04-07
申请号：US540047
申请日：1990-06-19
申请人： Joseph A. Picard , Bruce D. Roth , Drago R. Sliskovic
发明人： Joseph A. Picard , Bruce D. Roth , Drago R. Sliskovic
IPC分类号： C07D405/14 , C07D409/14 , C07D417/14
CPC分类号： C07D405/14 , C07D409/14 , C07D417/14
摘要： Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted) pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids, esters and N-oxides derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hydrolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
摘要翻译：某些反式-6- [2-（N-杂芳基-3,5-二取代）吡唑-4-基）乙基] - 或乙烯基]四氢-4-羟基-2H-吡喃-2-酮和相应的开环酸，酯和N-氧化物，其是3-羟基-3-甲基戊二酰辅酶A还原酶（HMG CoA还原酶）的有效抑制剂，因此是有用的水溶性血液或低胆固醇血症药。还公开了含有这些化合物的药物组合物和使用这种药物组合物抑制胆固醇生物合成的方法。

6. 发明授权

US5003080A Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis 失效
标题翻译：用于反式-6-（2-（取代 - 吡咯-1-基）烷基）戊二烯-2-酮胆固醇合成抑制剂的方法
公开(公告)号：US5003080A
公开(公告)日：1991-03-26
申请号：US303733
申请日：1989-02-01
申请人： Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
发明人： Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
IPC分类号： A61K31/40 , A61K31/4025 , A61P3/06 , C07C235/80 , C07D207/34 , C07D319/06 , C07D319/08 , C07D405/06 , C07D405/14
CPC分类号： C07D319/08 , C07C235/80 , C07D207/34 , C07D319/06 , C07D405/06
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-4-diphenyl-1-[2-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

7. 发明授权

US4681893A Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis 失效
标题翻译：胆固醇合成的反式-6- [2-（3-或4-甲酰氨基取代的吡咯-1-基）烷基] -4-羟基吡喃-2-酮抑制剂
公开(公告)号：US4681893A
公开(公告)日：1987-07-21
申请号：US868867
申请日：1986-05-30
申请人： Bruce D. Roth
发明人： Bruce D. Roth
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/44 , A61P3/06 , C07D207/325 , C07D207/33 , C07D401/14 , C07D405/06 , A61K31/35 , C07D207/327
CPC分类号： C07D405/06
摘要： Certain trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.

8. 发明授权

US5593967A Cholecystokinin antagonists, their preparation and therapeutic use 失效
标题翻译：缩胆囊素拮抗剂，其制备和治疗用途
公开(公告)号：US5593967A
公开(公告)日：1997-01-14
申请号：US41647
申请日：1993-04-01
申请人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
发明人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
IPC分类号： A61K38/00 , C07D209/14 , C07D209/20 , C07K5/02 , C07K5/065 , C07K5/078 , C07K14/595 , C07D209/18 , C07D217/00
CPC分类号： C07K14/595 , C07D209/14 , C07D209/20 , C07K5/0202 , C07K5/06078 , C07K5/06156 , A61K38/00
摘要： Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with use of nicotine, diazepam, alcohol, cocaine, coffee, or opioids. The compounds of the invention are also useful in treating and/or preventing panic. Also disclosed are pharmaceutical compositions and methods of treatment using the antagonists as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.
摘要翻译：新颖的缩胆囊素拮抗剂可用作治疗肥胖的药物，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药。此外，化合物是抗焦虑剂和抗溃疡剂。它们是用于防止使用尼古丁，地西泮，酒精，可卡因，咖啡或阿片样物质从慢性治疗中撤回的反应的药剂。本发明的化合物也可用于治疗和/或预防恐慌。还公开了使用拮抗剂的药物组合物和治疗方法以及制备它们的方法和可用于其制备的新型中间体。本发明的另一个特征是本发明化合物在诊断组合物中的用途。

9. 发明授权

US5441975A Pyrazolo-substituted alkyl amide acat inhibitors 失效
标题翻译：吡唑并 - 取代的烷基酰胺亚胺抑制剂
公开(公告)号：US5441975A
公开(公告)日：1995-08-15
申请号：US274088
申请日：1994-07-12
申请人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
发明人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
IPC分类号： A61K31/41 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/337 , C07D215/38 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D249/04 , C07D249/06 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/22 , C07D277/30 , C07D285/12 , C07D307/54 , C07D333/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04
摘要： Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
摘要翻译：对于除了四唑之外的X，n = 2，然后R2 = R3 = H，具有式IMAImage的ACAT抑制活性的药学上有用的化合物，其中n为0,1或2。 R 1是苯基，取代的苯基，萘基，取代的萘基，杂芳基或具有1至18个碳原子的烃基; R2和R3是氢，卤素，羟基，烷基，烯基，环烷基，苯基，取代的苯基，杂芳基或形成螺烷基; X是含有一至四个杂原子的杂单环五元环，所述杂原子是氮，氧或硫，以及它们的组合; 并且描述了R4是具有1至20个碳原子的烃基以及它们的制备方法。

10. 发明授权

US5385929A [(Hydroxyphenylamino) carbonyl] pyrroles 失效
标题翻译： [（羟基苯基氨基）羰基]吡咯
公开(公告)号：US5385929A
公开(公告)日：1995-01-31
申请号：US238120
申请日：1994-05-04
申请人： Susan M. Bjorge , Ann E. Black , Bruce D. Roth , Thomas Woolf
发明人： Susan M. Bjorge , Ann E. Black , Bruce D. Roth , Thomas Woolf
IPC分类号： A61K31/40 , A61K31/4025 , A61P3/06 , C07D207/34 , C07D405/06 , C07D207/327
CPC分类号： C07D405/06 , C07D207/34
摘要： 2-(4-Fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, and their lactone forms, and salts and solyates thereof, inhibit cholesterol biosynthesis, and thus are useful in treating hypercholesterolemia.
摘要翻译： 2-（4-氟苯基）-β，δ-二羟基-5-（1-甲基乙基）-3-苯基-4 - [（羟基苯基氨基）羰基] -1H-吡咯-1-庚酸及其内酯形式，和其盐和盐酸盐抑制胆固醇生物合成，因此可用于治疗高胆固醇血症。

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