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1. 发明申请

US20080188545A1 Synthesis of pyrrolidine compounds 审中-公开
标题翻译：吡咯烷化合物的合成
公开(公告)号：US20080188545A1
公开(公告)日：2008-08-07
申请号：US12005118
申请日：2007-12-20
申请人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveeendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh
发明人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveeendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh
IPC分类号： A61K31/40 , C07D207/08 , A61P9/06 , A61P9/10
CPC分类号： C07D207/16
摘要： Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
摘要翻译：提供制备某些取代的吡咯烷化合物的方法，（2S，4R）-1-（2-氨基乙酰基）-4-苯甲酰基吡咯烷-2-甲酸盐酸盐的形式，以及制备和使用这些形式的方法。

2. 发明申请

US20100249207A1 SYNTHESIS OF PYRROLIDINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物的合成
公开(公告)号：US20100249207A1
公开(公告)日：2010-09-30
申请号：US12690043
申请日：2010-01-19
申请人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath
发明人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath
IPC分类号： A61K31/40 , C07D207/14 , A61P9/10 , A61P3/10 , A61P25/00 , A61P35/00 , A61P39/00 , A61P39/06 , A61P3/14 , A61P9/00
CPC分类号： C07D207/16
摘要： Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
摘要翻译：提供制备某些取代的吡咯烷化合物的方法，（2S，4R）-1-（2-氨基乙酰基）-4-苯甲酰基吡咯烷-2-甲酸盐酸盐的形式，以及制备和使用这些形式的方法。

3. 发明授权

US08927590B2 Synthesis of pyrrolidine compounds 有权
标题翻译：吡咯烷化合物的合成
公开(公告)号：US08927590B2
公开(公告)日：2015-01-06
申请号：US13593110
申请日：2012-08-23
申请人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath
发明人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Panolil Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh
IPC分类号： A61K31/40 , C07D207/02 , C07D207/16
CPC分类号： C07D207/16
摘要： Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
摘要翻译：提供制备某些取代的吡咯烷化合物的方法，（2S，4R）-1-（2-氨基乙酰基）-4-苯甲酰基吡咯烷-2-甲酸盐酸盐的形式，以及制备和使用这些形式的方法。

4. 发明申请

US20130053344A1 SYNTHESIS OF PYRROLIDINE COMPOUNDS 有权
公开(公告)号：US20130053344A1
公开(公告)日：2013-02-28
申请号：US13593110
申请日：2012-08-23
申请人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh
发明人： Asaf R. Alimardanov , Lalitha Krishnan , Maotang Zhou , Ting-Zhong Wang , Jianxin Ren , John Leo Considine , Charles C. Wu , Jason Brazzillo , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath , Karen Sutherland , Mahmoud Mirmehrabi , Subodh S. Deshmukh
IPC分类号： C07D207/08 , A61K31/4985 , A61K31/66 , A61K31/4192 , A61P9/00 , A61P19/10 , A61P29/00 , A61P13/10 , A61P27/16 , A61P3/10 , A61P27/02 , A61P9/10 , A61P25/00 , A61P25/08 , A61P13/12 , A61P17/02 , A61P19/08 , A61P15/10 , A61P35/00 , A61P39/06 , A61P15/00 , A61P15/08 , A61K31/40
CPC分类号： C07D207/16
摘要： Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.

5. 发明申请

US20080146645A1 Process for Preparing Indolinone Phenylaminopropanol Derivatives 审中-公开
标题翻译：制备吲哚啉酮苯基氨基丙醇衍生物的方法
公开(公告)号：US20080146645A1
公开(公告)日：2008-06-19
申请号：US11843364
申请日：2007-08-22
申请人： Anita Wai-Yin Chan , Zhixian Ding , Mousumi Ghosh , Mahmut Levent , Panolil Raveendranath , Jianxin Ren , Maotang Zhou , Asaf Alimardanov , Alexander V. Gontcharov , Antonia A. Nikitenko , John R. Potoski , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath
发明人： Anita Wai-Yin Chan , Zhixian Ding , Mousumi Ghosh , Mahmut Levent , Panolil Raveendranath , Jianxin Ren , Maotang Zhou , Asaf Alimardanov , Alexander V. Gontcharov , Antonia A. Nikitenko , John R. Potoski , Girija Raveendranath , Vijay Raveendranath , Sanjay Raveendranath
IPC分类号： C07D209/34 , A61K31/4015
CPC分类号： C07D209/34
摘要： Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.
摘要翻译：公开了制备吲哚啉酮苯基氨基丙醇衍生物的方法，特别是具有以下通式的手性吲哚啉酮苯基氨基丙醇衍生物：所公开的方法可用于特别地制备7-氟-1 - [（1S，2R）-1-（3- 氟甲基）-2-羟基-3-（甲基氨基）丙基] -3,3-二甲基-1,3-二氢-2H-吲哚-2-酮和7-氟-1 - [（1S，2R）-1 - （3,5-二氟苯基）-2-羟基-3-（甲基氨基）丙基] -3,3-二甲基-1,3-二氢-2H-吲哚-2-酮。还公开了该方法的中间体。

6. 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。

7. 发明授权

US07582771B2 Process for the synthesis of cPLA2 inhibitors 失效
标题翻译：合成cPLA2抑制剂的方法
公开(公告)号：US07582771B2
公开(公告)日：2009-09-01
申请号：US10930534
申请日：2004-08-31
申请人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath , Jianxin Ren , Charles C. Wu , Yangzhong Wu
发明人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath , Jianxin Ren , Charles C. Wu , Yangzhong Wu
IPC分类号： C07D209/10 , C07D209/14
CPC分类号： C07D209/14
摘要： A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3, OH, C1-C6alkyl, C1-C6alkoxy, C1-C6thioalkyl, NH2, N(C1-C6alkyl)2, NH(C1-C6alkyl), NC(O)—(C1C6alkyl), and NO2. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
摘要翻译：制备式（I）的化合物的方法，其中Ac表示乙酸酯; X表示O或CH2; Y表示C1-C6烷基; 和Z选自H，卤素，CN，CHO，CF 3，OCF 3，OH，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，NH 2，N（C 1 -C 6烷基）2，NH（C 1 -C 6烷基），NC（O） - （C 1 -C 6烷基）和NO 2。在其工艺中，将式（II）化合物与肼反应以形成伯烷基胺，然后将伯烷基胺与乙酸酐反应，生成式（I）化合物。

8. 发明授权

US07687666B2 Methods for preparing sulfonamide substituted alcohols and intermediates thereof 失效
标题翻译：制备磺酰胺取代醇的方法及其中间体
公开(公告)号：US07687666B2
公开(公告)日：2010-03-30
申请号：US11706636
申请日：2007-02-15
申请人： Anita Wai-Yin Chan , Jianxin Ren , Mousumi Ghosh , Arkadiy Rubezhov , Panolil Raveendranath , Joseph Zeldis
发明人： Anita Wai-Yin Chan , Jianxin Ren , Mousumi Ghosh , Arkadiy Rubezhov , Panolil Raveendranath , Joseph Zeldis
IPC分类号： C07C209/78 , C07C303/12 , C07C29/147
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/34 , C07C215/08
摘要： Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
摘要翻译：提供了制备氨基醇或其盐和磺酰胺取代的醇化合物的方法。理想地，磺酰胺取代的醇化合物是杂环磺酰胺三氟烷基取代的醇化合物或苯基磺酰胺三氟烷基取代的醇化合物。

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

US06268504B1 Aryloxy-alkyl-dialkylamines 失效
标题翻译：芳氧基 - 烷基 - 二烷基胺
公开(公告)号：US06268504B1
公开(公告)日：2001-07-31
申请号：US09458317
申请日：1999-12-10
申请人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
发明人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
IPC分类号： C07D27704
CPC分类号： C07D295/088 , C07C217/48
摘要： The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要翻译：本发明提供了可用于合成生物活性化合物的化合物及其制备方法，具有下式的化合物：其中：R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A是O或S; m为1〜3的整数，优选为2; R 3，R 4，R 5和R 6独立地选自H，卤素，-NO 2，烷基，烷氧基，C 1 -C 6全氟烷基，OH或其C 1 -C 4酯或其烷基醚，-CN，-O-R 1， O-Ar，-S-R 1，-S-Ar，-SO-R 1，-SO-Ar，-SO 2 -R 1，-SO 2 -Ar，-CO-R 1，-CO-Ar，-CO 2 -R -CO 2 -Ar; 并且Y选自a）部分：其中R 7和R 8独立地选自H，C 1 -C 6烷基或苯基; 或b）任选取代的五元，六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环，其含有至多两个选自-O - ， - NH - ， - N（C 1 -C 4烷基） - ， - N =和-S（O）n - 。

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