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21. 发明授权

US4735958A Trans-6-[2-[2-(substituted-phenyl)-3- (or 4-) heteroaryl-5-substituted-1H-pyrrol-1-yl]-ethyl]tetrahydro-4-hydroxy-2H-p yran-2-one inhibitors of cholesterol biosynthesis 失效
标题翻译：反式-6- [2- [2-（取代的苯基）-3-（或4-）杂芳基-5-取代-1H-吡咯-1-基] - 乙基]四氢-4-羟基-2H-吡喃-2-酮 2-one胆固醇生物合成抑制剂
公开(公告)号：US4735958A
公开(公告)日：1988-04-05
申请号：US944318
申请日：1986-12-22
申请人： Bruce D. Roth , Drago R. Sliskovic
发明人： Bruce D. Roth , Drago R. Sliskovic
IPC分类号： C07D405/14 , A61K31/395 , A61K31/44
CPC分类号： C07D405/14
摘要： Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding lactone-ring-opened acids 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.
摘要翻译：某些反式-6- [2- [2-（取代的 - 苯基）-3-（或4-）杂芳基-5-取代的-1H-吡咯-1-基]乙基]四氢-4-羟基-2H- 2-酮和相应的内酯开环酸是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，因此可用于降血脂或降胆固醇。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。

22. 发明授权

US4716175A Saturated fatty acid amides as inhibitors of acyl-CoA:cholesterol acyltransferase 失效
标题翻译：饱和脂肪酸酰胺作为酰基辅酶A的抑制剂：胆固醇酰基转移酶
公开(公告)号：US4716175A
公开(公告)日：1987-12-29
申请号：US17960
申请日：1987-02-24
申请人： Milton L. Hoefle , Ann Holmes , Bruce D. Roth
发明人： Milton L. Hoefle , Ann Holmes , Bruce D. Roth
IPC分类号： C12N9/99 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P3/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/04 , C07C233/05 , C07C233/07 , C07C233/09 , C07C233/12 , C07C233/13 , C07C233/15 , C07C233/16 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/25 , C07C233/27 , C07C233/29 , C07D213/40 , C07D213/75 , C07D239/42 , C07D239/52 , A61K31/16 , A61K31/165 , C07C103/19 , C07D213/36
CPC分类号： C07D213/40 , C07C233/07 , C07C233/09 , C07D239/52
摘要： Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.

23. 发明授权

US06951848B2 Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor 有权
标题翻译：功能化杂环作为趋化因子受体功能的调节剂及其使用方法
公开(公告)号：US06951848B2
公开(公告)日：2005-10-04
申请号：US10096361
申请日：2002-03-12
申请人： Geraldine C. B. Harriman , Kenneth G. Carson , Daniel L. Flynn , Michael E. Solomon , Yuntao Song , Bharat K. Trivedi , Bruce D. Roth , Christine N. Kolz , Ly Pham , Kuai-lin Sun
发明人： Geraldine C. B. Harriman , Kenneth G. Carson , Daniel L. Flynn , Michael E. Solomon , Yuntao Song , Bharat K. Trivedi , Bruce D. Roth , Christine N. Kolz , Ly Pham , Kuai-lin Sun
IPC分类号： A61P31/18 , C07D209/42 , C07D235/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D487/04 , C07D491/04 , C07D491/08 , A61K31/33 , A61K31/40 , A61K31/405 , C07D209/04
CPC分类号： C07D401/04 , C07D209/42 , C07D235/26 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D487/04 , C07D491/04 , C07D491/08
摘要： Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.
摘要翻译：公开了具有下式的新化合物或其生理上可接受的盐，酰胺，酯或前药。该化合物可用于调节（拮抗，激动）趋化因子受体功能。还公开了一种治疗患有炎性疾病和/或病毒感染的患者的方法，其包括施用有效量的式I化合物。在具体实施方案中，本发明是用于治疗感染HIV的患者的方法。

24. 发明授权

US5366987A Isoxazolyl-substituted alkyl amide ACAT inhibitors 失效
标题翻译：异唑基取代的烷基酰胺ACAT抑制剂
公开(公告)号：US5366987A
公开(公告)日：1994-11-22
申请号：US19411
申请日：1993-02-18
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。

25. 发明授权

US5280126A 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：US5280126A
公开(公告)日：1994-01-18
申请号：US58349
申请日：1993-05-06
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]-Y-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.
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）和反式 - （+/-） - 5-（4-氟苯基）-2-（1-甲基乙基）-N，4- 二苯基-1- [2-（二氢 - 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为所需产物，或者4-氟-α-[2-甲基-1-氧代丙基] -Y-氧代-N，β-二苯基苯丁酰胺在一个步骤中转化成所需产物，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]丁酸以及其它有价值的中间体的过程。

26. 发明授权

US5273995A [R-(R*R*)]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-( 1-methylethyl-3-phenyl-4-[(phenylamino) carbonyl]- 1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof 失效
标题翻译： [R-（R * R *）] -2-（4-氟苯基）-β，二羟基-5-（1-甲基乙基-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1 - 庚酸，其内酯形式及其盐
公开(公告)号：US5273995A
公开(公告)日：1993-12-28
申请号：US660976
申请日：1991-02-26
申请人： Bruce D. Roth
发明人： Bruce D. Roth
IPC分类号： C07D207/416 , A61K31/40 , A61P3/06 , A61P43/00 , C07D207/34 , C07D405/06
CPC分类号： C07D405/06 , C07D207/34
摘要： [R-(R*,R*)]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-((1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl]-1H-pyrrole-1-heptanoic acid or (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; and pharmaceutically acceptable salts thereof.
摘要翻译： [R-（R *，R *）] -2-（4-氟苯基）-β，二羟基-5 - （（1-甲基乙基）-3-苯基-4 - [（苯基氨基） - 羰基] -p-吡咯-1-庚酸或（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-甲酰胺及其药学上可接受的盐。

27. 发明授权

US5254589A Sulfonyl urea and carbamate ACAT inhibitors 失效
标题翻译：磺酰脲和氨基甲酸酯ACAT抑制剂
公开(公告)号：US5254589A
公开(公告)日：1993-10-19
申请号：US776112
申请日：1991-10-15
申请人： Joseph A. Picard , William H. Roark , Bruce D. Roth
发明人： Joseph A. Picard , William H. Roark , Bruce D. Roth
IPC分类号： C07C311/53 , C07C311/55 , A61K31/175
CPC分类号： C07C311/53 , C07C311/55
摘要： A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.
摘要翻译：降低具有式“IMAGE”的血液胆固醇水平的药学上有用的化合物，其中X是氧或-NH-; Ar是苯基，取代的苯基，萘基或取代的萘基; R1是氢，低级烷基或苄基; 并且R 2是具有5至17个碳原子的直链或支链烷基，其可以在1-碳位上被甲基，乙基，苯基或取代的苯基或具有3至8个碳原子的环烷基取代。

28. 发明授权

US5124482A 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：US5124482A
公开(公告)日：1992-06-23
申请号：US792311
申请日：1991-11-14
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-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.
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）和反式（+/-） - 5-（4-氟苯基）-2-（1-甲基乙基）-N，4-二苯基的改进方法 -1- [2-（四氢-4-羟基-6-氧代-2H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺的新型合成法，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成所需产物，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 - （R）-4-氰基-3 - [[（1,1-二甲基乙基）二甲基甲硅烷基]氧基]丁酸，以及其它有价值的（R）-4-氰基-3 - [（1H-吡喃-2-基）乙基] -1H-吡咯-3-甲酰胺中间体的过程。

29. 发明授权

US5097045A 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：US5097045A
公开(公告)日：1992-03-17
申请号：US595461
申请日：1990-10-09
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-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.
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-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成所需产物，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 - （R）-4-氰基-3 - [[（1,1-二甲基乙基）二甲基甲硅烷基]氧基]丁酸，以及其它有价值的（R）-4-氰基-3 - [（1H-吡喃-2-基）乙基] 中间体使用 d在进程中。

30. 发明授权

US4957940A Bicyclo heptane and bicyclo octane substituted inhibitors of cholesterol synthesis 失效
标题翻译：双环庚烷和双环辛烷基取代的胆固醇合成抑制剂
公开(公告)号：US4957940A
公开(公告)日：1990-09-18
申请号：US439719
申请日：1989-11-21
申请人： Bruce D. Roth
发明人： Bruce D. Roth
IPC分类号： C07D309/30 , A61K31/23 , A61K31/20 , C07C61/12 , C07C69/753
CPC分类号： C07D309/30 , Y10S514/824
摘要： Certain bicyclo [2.2.1] heptane and bicyclo [2.2.2] octane substituted tetrahydro-2H-pyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
摘要翻译：某些双环[2.2.1]庚烷和双环[2.2.2]辛烷取代的四氢-2H-吡喃-2-酮及其衍生的相应的开环酸是3-羟基-3-甲基戊二酰辅酶3的有效抑制剂还原酶（HMG-CoA还原酶），可用作低胆固醇血症和降血脂药。

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