公开(公告)号：US07112669B2

公开(公告)日：2006-09-26

申请号：US11052549

申请日：2005-02-07

申请人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph J. Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

发明人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph J. Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

IPC分类号： C07J21/00 ,  C07J71/00

CPC分类号： C07J71/00 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0015 ,  C07J75/00 ,  C12P33/005 ,  C12P33/10

摘要： Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.

摘要翻译： 公开了制备9,11-环氧类固醇的中间体。 特别公开的是11,12-环氧类固醇，4,5-9,11-二环氧类固醇和12-酮类固醇中间体。

公开(公告)号：US06887991B1

公开(公告)日：2005-05-03

申请号：US10647866

申请日：2003-08-25

申请人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

发明人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

IPC分类号： A61K31/58 ,  C07D301/12 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J53/00 ,  C07J71/00 ,  C12P33/00 ,  C12P33/10

CPC分类号： C07J71/00 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0015 ,  C07J75/00 ,  C12P33/005 ,  C12P33/10

摘要： Processes for the preparation of 4,5-dihydro-5,7-lactone steroid compounds are provided.

摘要翻译： 提供了制备4,5-二氢-5,7-内酯类固醇化合物的方法。

公开(公告)号：US06610844B2

公开(公告)日：2003-08-26

申请号：US10112355

申请日：2002-03-29

申请人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

发明人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas R. Kowar ,  Julio A. Baez ,  Bernhard Erb

IPC分类号： C07J2100

CPC分类号： C12P33/10 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0015 ,  C12P33/005

摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein —A—A— represents the group —CHR4—CHR5— or —CR4═CR5—; R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano and aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; —B—B— represents the group —CHR6—CHR7— or an alpha- or beta-oriented group: where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

摘要翻译： 提供了多种新的反应方案，新工艺步骤和新的中间体，用于合成环氧麦芽糖酮和式I的其它化合物，其中AA-代表基团-CHR4-CHR5-或-CR4 = CR5-; R3，R4和R5独立地选自 卤代，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基和芳氧基; R1代表α-取代的低级烷氧基羰基或羟基烷基; -BB-代表基团-CHR6-CHR7- 或α-取代或β-取代基团：其中R 6和R 7独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基。 R 8和R 9独立地选自氢，羟基，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基烷基，烷氧基羰基烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基，或R8和R9一起包含碳环或杂环结构 ，或R 8或R 9与R 6一起或包含与五环D环稠合的碳环或杂环结构。

公开(公告)号：US5432284A

公开(公告)日：1995-07-11

申请号：US118073

申请日：1993-09-08

申请人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

发明人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

IPC分类号： C07D295/145 ,  C07D207/09 ,  C07D211/32 ,  C07D211/60

CPC分类号： C07D295/145

摘要： The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.3 represents acetyl, benzoyl, phenacetyl or trifluoroacetyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; which comprises alkylating an aminoalkanol using a benzaldehyde/aminoalkanol/ketone mixture in the presence of a platinum catalyst to give an alkyl substituted phenylmethylaminoalkanol; halogenating the alkanol using a halogenating agent to give a haloalkyl alkylbenzenemethanamine salt; treating the salt with substituted phenyl piperidinealkanenitrile or substituted phenyl pyrrolidinealkanenitrile in the presence of base and dimethyl sulfoxide to give a substituted phenyl substituted aminoalkyl piperidinealkanenitrile or substituted aminoalkyl pyrrolidinealkanenitrile; hydration of the nitrile to give the corresponding amide; and N-debenzylation of the amide followed by acetylation to give the compounds of formula I wherein Y is --CONH.sub.2.

摘要翻译： 本发明涉及制备具有下式的杂环烷基酰胺衍生物的新方法：其中X表示卤素，具有1至6个碳原子的烷基，羟基，三氟甲基（I）及其药学上可接受的酸加成盐 ，苯基或具有1至6个碳原子的低级烷氧基; Y代表基团-CN或-CONH 2; R 2表示具有1至6个碳原子的烷基; R3表示乙酰基，苯甲酰基，苯乙酰基或三氟乙酰基; m为1或2的整数，n为1〜3的整数， 其包括在铂催化剂存在下使用苯甲醛/氨基烷醇/酮混合物烷基化氨基烷醇，得到烷基取代的苯基甲基氨基烷基醇; 使用卤化剂卤化烷醇得到卤代烷基烷基苯甲胺盐; 在碱和二甲基亚砜的存在下用取代的苯基哌啶烷腈或取代的苯基吡咯烷烷腈处理盐，得到取代的苯基取代的氨基烷基哌啶烷腈或取代的氨基烷基吡咯烷烷腈; 腈水合得到相应的酰胺; 和酰胺的N-去苄基化，然后进行乙酰化，得到其中Y为-CONH 2的式I化合物。