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1. 发明申请

US20090306428A1 Process for the Synthesis of C-2, C-3 Substituted N-Alkylated Indoles Useful as cPLA2 Inhibitors 失效
标题翻译：用作CPLA2抑制剂的C-2，C-3取代的N-烷基化吲哚的合成方法
公开(公告)号：US20090306428A1
公开(公告)日：2009-12-10
申请号：US12542914
申请日：2009-08-18
申请人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
发明人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
IPC分类号： C07C311/13
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.
摘要翻译：本发明提供了制备式1化合物的方法：包括使式2和3化合物反应的步骤：制备式4化合物：其中R 1，R 2，R 3，R 4和R 5如本文所述定义。然后将式4的化合物转化为式1的化合物。本发明还包括式3和4的化合物以及制备式3和4的化合物的方法。

2. 发明授权

US07582772B2 Process for the synthesis C-2, C-3 substituted N-alkylated indoles useful as CPLA2 inhibitors 失效
标题翻译：合成用作CPLA2抑制剂的C-2，C-3取代的N-烷基化吲哚的方法
公开(公告)号：US07582772B2
公开(公告)日：2009-09-01
申请号：US11207072
申请日：2005-08-18
申请人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
发明人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
IPC分类号： C07D209/04 , C07C255/58
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.
摘要翻译：本发明提供了制备式1化合物的方法：包括使式2和3化合物反应的步骤：制备式4化合物：其中R 1，R 2，R 3，R 4和R 5如本文所述定义。然后将式4的化合物转化为式1的化合物。本发明还包括式3和4的化合物以及制备式3和4的化合物的方法。

3. 发明申请

US20050187408A1 Processes for the preparation of aryl-and heteroaryl-alkylsulfonyl halides 失效
标题翻译：制备芳基和杂芳基 - 烷基磺酰卤的方法
公开(公告)号：US20050187408A1
公开(公告)日：2005-08-25
申请号：US11064241
申请日：2005-02-23
申请人： Ronald Michalak , Mousumi Ghosh , Mahmut Levent
发明人： Ronald Michalak , Mousumi Ghosh , Mahmut Levent
IPC分类号： C07C303/20 , C07C303/22 , C07C303/32 , C07C309/24 , C07C309/81 , C07C309/83 , C07C39/86
CPC分类号： C07C303/32 , C07C303/22 , C07C309/24 , C07C309/81 , C07C309/82
摘要： The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula I: Ar—R—SO2—X, that are useful as intermediates in the preparation of pharmaceuticals.
摘要翻译：本发明提供了制备式I的芳基烷基磺酰卤和杂芳基烷基磺酰卤的方法：Ar-R-SO 2 -X，其可用作制备药物的中间体。

4. 发明申请

US20050054870A1 Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile 失效
标题翻译：合成3-（3-氟-4-羟基苯基）-7-羟基萘腈的方法
公开(公告)号：US20050054870A1
公开(公告)日：2005-03-10
申请号：US10933184
申请日：2004-09-01
申请人： Yanzhong Wu , Jianxin Ren , Mousumi Ghosh , Mahmut Levent , Karen Sutherland , Panolil Raveendranath
发明人： Yanzhong Wu , Jianxin Ren , Mousumi Ghosh , Mahmut Levent , Karen Sutherland , Panolil Raveendranath
IPC分类号： C07C37/055 , C07C41/24 , C07C41/30 , C07C253/30 , C07C255/53 , C07C255/54 , C07C39/12
CPC分类号： C07C255/54 , C07C37/055 , C07C253/30 , C07C255/53 , C07C39/38
摘要： A process for making a compound of formula I and intermediate compounds thereof, wherein R1 is CN, F or Cl; R2 is H or Br; and R3 and R4 are each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
摘要翻译：制备式I化合物及其中间体化合物的方法，其中R 1为CN，F或Cl; R2是H或Br; 并且R 3和R 4各自独立地为H或F.式I化合物可用于治疗慢性炎性疾病，例如类风湿性关节炎。

5. 发明申请

US20110178311A1 Purification of Progesterone Receptor Modulators 审中-公开
标题翻译：孕酮受体调节剂的纯化
公开(公告)号：US20110178311A1
公开(公告)日：2011-07-21
申请号：US13078273
申请日：2011-04-01
申请人： Mahmut Levent , Panolil Raveendranath , Bogdan Wilk , Donald Carl Boop , Marinus Cornelis Hofman
发明人： Mahmut Levent , Panolil Raveendranath , Bogdan Wilk , Donald Carl Boop , Marinus Cornelis Hofman
IPC分类号： C07D403/10
CPC分类号： C07D403/04
摘要： Processes are provided for purifying a compound of the structure (I): wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.
摘要翻译：提供用于纯化结构（I）的化合物的方法：其中A，B，T，Q和R 1在本文中定义，并且其中所述方法包括将式I化合物溶解在含有丙酮，水和碱的溶液在约30℃。在约30℃下过滤含有式I化合物的溶液; 并通过将过滤的溶液调节至酸性pH而沉淀出纯化的式I化合物。理想地，式I化合物是5-（2-噻吩并[环己烷-1,3- [3 H]吲哚] -5-基）-1-甲基吡咯-2-腈或十八碳炔。

6. 发明申请

US20110054189A1 Process For The Synthesis C-2, C-3 Substituted N-Alkylated Indoles Useful As CPLA2 Inhibitors 有权
标题翻译：用作CPLA2抑制剂的合成C-2，C-3取代的N-烷基化吲哚的方法
公开(公告)号：US20110054189A1
公开(公告)日：2011-03-03
申请号：US12943958
申请日：2010-11-11
申请人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
发明人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
IPC分类号： C07D209/20
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H, R3 is H, and R4 is H.
摘要翻译：本发明提供式1化合物：其中R1为CF3，R2为H，R3为H，R4为H。

7. 发明授权

US5166355A Process for preparing substituted 2,2'-methylene-bis-[6-(2H-benzotriazol-2-yl)-4-hydrocarbyl-phenols] 失效
标题翻译：取代的2,2'-亚甲基 - 双 - [6-（2H-苯并三唑-2-基）-4-烃基 - 酚]的制备方法]
公开(公告)号：US5166355A
公开(公告)日：1992-11-24
申请号：US649972
申请日：1991-02-04
申请人： William E. Leistner , Semyon Moshchitsky , Mahmut Levent
发明人： William E. Leistner , Semyon Moshchitsky , Mahmut Levent
IPC分类号： C07C45/72 , C07C49/84 , C07D249/20
CPC分类号： C07D249/20 , C07C45/72 , C07C49/84
摘要： A method is described for preparing compounds of Formula I and Formula II: ##STR1## R.sub.1 is an alkyl group of one to twelve carbon atoms or a cycloalkyl group of five to eight carbons, X is chloro or hydrogen, and R.sub.2 is an alkoxy group having one to twelve carbons. In accordance with the method:(a) a bis(dialkylamino)methane is formed, preferably by reacting a dialkylamine of the formula HNR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are independently alkyl groups having three or more carbons) and a solid formaldehyde material to produce the corresponding bis(dialkylamino)methane,(b) a monomer of Formula III or IV ##STR2## in which R.sub.1 is an alkyl group of one to twelve carbons or a cycloalkyl group of five to eight carbons, X is chloro or hydrogen and R.sub.2 is an alkoxy group having one to twelve carbon atoms, is mixed with an alkaline catalyst with heating at a temperature high enough to drive off the liquid formed in the reaction,(c) the product of steps (a) and (b) are combined and stirred at a temperature sufficient to drive the reaction for six to fourteen hours, and(d) thereafter the resulting compound of Formula I is collected.
摘要翻译：描述了制备式I和式II化合物的方法：R 1是1至12个碳原子的烷基或5至8个碳的环烷基，X是氯或氢，以及 R2是具有1〜12个碳原子的烷氧基。根据以下方法：（a）形成双（二烷基氨基）甲烷，优选通过使式HNR 3 R 4的二烷基胺（其中R 3和R 4独立地为具有三个或更多个碳的烷基）和固体甲醛材料反应，生成对应的双（二烷基氨基）甲烷，（b）式III或IV的单体IV，其中R 1是1至12个碳的烷基或5至8个碳的环烷基，X是氯或氢，R2为具有1〜12个碳原子的烷氧基，与碱催化剂在足够高的温度下加热以除去反应中形成的液体，（c）步骤（a）和（ b）在足以驱动反应6至14小时的温度下混合并搅拌，然后收集所得到的式I化合物。

8. 发明授权

US08034960B2 Process for the synthesis C-2, C-3 substituted N-alkylated indoles useful as cPLA2 inhibitors 有权
标题翻译：用于合成C-2，C-3取代的N-烷基化吲哚的方法，其用作cPLA2抑制剂
公开(公告)号：US08034960B2
公开(公告)日：2011-10-11
申请号：US12943958
申请日：2010-11-11
申请人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
发明人： Ronald S. Michalak , Mahmut Levent , Frederick J. Vyverberg , Ara R. Boyajian , Panolil Raveendranath , Michel Cantin , Alan Stockton , Michael W. Winkley , Mousumi Ghosh , Christoph Dehnhardt , Charles Guinosso
IPC分类号： C07D209/20
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H′ R3 is H.
摘要翻译：本发明提供式1化合物：其中R1是CF3，R2是H'R3是H.

9. 发明授权

US07557237B2 Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile 失效
标题翻译：合成3-（3-氟-4-羟基苯基）-7-羟基萘腈的方法
公开(公告)号：US07557237B2
公开(公告)日：2009-07-07
申请号：US10933184
申请日：2004-09-01
申请人： Yanzhong Wu , Jianxin Ren , Mousumi Ghosh , Mahmut Levent , Karen W. Sutherland , Panolil Raveendranath
发明人： Yanzhong Wu , Jianxin Ren , Mousumi Ghosh , Mahmut Levent , Karen W. Sutherland , Panolil Raveendranath
IPC分类号： C07C255/03
CPC分类号： C07C255/54 , C07C37/055 , C07C253/30 , C07C255/53 , C07C39/38
摘要： A process for making a compound of formula I and intermediate compounds thereof, wherein R1 is CN, F or Cl; R2 is H or Br; and R3 and R4 are each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
摘要翻译：制备式I化合物及其中间体化合物的方法，其中R 1为CN，F或Cl; R2是H或Br; 并且R 3和R 4各自独立地为H或F.式I化合物可用于治疗慢性炎性疾病，例如类风湿性关节炎。

10. 发明授权

US5237071A Process for preparing 2,2'-methylene-bis(6-(2H-benzotriazol-2-yl)-4-hydrocarbyl phenols) 失效
标题翻译：制备2,2'-亚甲基 - 双（6-（2H-苯并三唑-2-基）-4-烃基酚的方法）
公开(公告)号：US5237071A
公开(公告)日：1993-08-17
申请号：US644299
申请日：1991-01-22
申请人： William E. Leistner , Semyon Moshchitsky , Mahmut Levent
发明人： William E. Leistner , Semyon Moshchitsky , Mahmut Levent
IPC分类号： C07D249/20
CPC分类号： C07D249/20
摘要： A method for preparing 2,2'-methylene-bis-[6-(2H)-benzotriazol-2-yl)-4-hydrocarbyl phenols] is disclosed. According to the process(i) formaldehyde, a dialkylamine and a 4-hydrocarbyl-6-benzotriazolyl phenol as monomer are mixed;(ii) the mixture is heated to a temperature high enough to remove the water produced by the reaction of the mixture;(iii) thereafter an alkaline catalyst is added with heating for several hours;(iv) the phenol compound precipitates when the reaction mixture is neutralized and solvent for the salt product of the neutralization reaction is added in an amount sufficient to permit stirring.The solid product produced is 2,2'-methylene-bis-[6-(2H-benzotriazol-2-yl)-4-hydrocarbyl phenol] having the formula I: ##STR1## in which each R group is an alkyl group of one to twelve carbons or a cycloalkyl group of five to eight carbons and X is chloro or hydrogen.
摘要翻译：公开了一种制备2,2'-亚甲基 - 双 - [6-（2H） - 苯并三唑-2-基）-4-烃基酚的方法]。根据方法（i）甲醛，将二烷基胺和作为单体的4-烃基-6-苯并三唑基苯酚混合; （ii）将混合物加热到足够高的温度以除去由混合物反应产生的水; （iii）然后加热碱性催化剂数小时; （iv）当反应混合物中和时，酚化合物沉淀，并且以足以允许搅拌的量加入中和反应的盐产物的溶剂。产生的固体产物是具有式I的2,2'-亚甲基 - 双[6-（2H-苯并三唑-2-基）-4-烃基苯酚]，其中每个R基团是一至十二个碳或五至八个碳的环烷基，X是氯或氢。

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