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1. 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。

2. 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.

3. 发明授权

US07842837B2 Process for the synthesis of 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：US07842837B2
公开(公告)日：2010-11-30
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。

4. 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。

5. 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。

6. 发明授权

US06693207B2 B-ring estratriene diols 有权
标题翻译： B环雌二醇
公开(公告)号：US06693207B2
公开(公告)日：2004-02-17
申请号：US10164149
申请日：2002-06-05
申请人： Michael Z. Kagan , Panolil Raveendranath , Syed M. Shah , Michael W. Winkley
发明人： Michael Z. Kagan , Panolil Raveendranath , Syed M. Shah , Michael W. Winkley
IPC分类号： C07J100
CPC分类号： A61K31/56 , C07J1/00
摘要： This invention provides estrogenic agents having the formula wherein A and B are each, independently, R is SO3−X+; X+ is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium containing 1-6 carbon atoms in each alkyl group, or trialkylammonium containing 1-6 carbon atoms in each alkyl group; with the proviso that at least one of A or B is
摘要翻译：本发明提供具有马来酰亚胺A的雌激素剂，B各自独立地是R 3是SO 3 - ，X +; X +是含有1-6个碳原子的碱金属，碱土金属，铵，烷基铵或二烷基铵每个烷基中含有1-6个碳原子，或每个烷基含有1-6个碳原子的三烷基铵;条件是A或B中的至少一个为

7. 发明授权

US4935515A 2,3,4,5-tetrahyd ro-1H-[1,2,5]triazocino(1,2-a)[1,2,4]benzotriazin-7(8H)-ones, thiones and derivatives 失效
公开(公告)号：US4935515A
公开(公告)日：1990-06-19
申请号：US432245
申请日：1989-11-06
申请人： Michael W. Winkley , James L. Diebold
发明人： Michael W. Winkley , James L. Diebold
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed herein are novel 1,2,3,4,5,6-hexahydro[1,3,6]triazocino[1,2-a]benzimidazole of Formulas I and II: ##STR1## wherein R.sup.1 may be phenyl, m- or p-nitrophenyl, m- or p-methylsulfonylaminophenyl, napthtyl, naphthyl mono-substituted by nitro or methylsulfonylamino, benzofurazanyl, 2-pyrimidinyl, 2- or 4-pyridinyl, 2- or 4-naphthyridinyl, pyrazinyl, isoquinolinyl, or quinolinyl;R.sup.2 may be hydrogen; C.sub.1 -C.sub.8 alkyl; phenyl(C.sub.1 -C.sub.4)alkyl or substituted-phenyl(C.sub.1 -C.sub.4)alkyl, in which phenyl may have one to three substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluorine, chlorine or bromine; phenyl or substituted-phenyl in which the phenyl substituents are the same as for substituted-phenyl (C.sub.1 -C.sub.4)alkyl; 2- or 4-pyrimidinyl; pyrazinyl; imidazolyl; C.sub.1 -C.sub.4 alkanoyl; halo or dihalo-(C.sub.1 -C.sub.4)alkanoyl, in which halo is fluoro or chloro; benzoyl or benzoyl substituted on the phenyl ring by one or two C.sub.1 -C.sub.4 alkyl groups; C.sub.1 -C.sub.4 alkanoyloxy; C.sub.1 -C.sub.4 alkylamino(C.sub.1 -C.sub.4 alkanoyl; C.sub.1 -C.sub.4 alkyloxycarbonyl; C.sub.1 -C.sub.4 alkylaminocarbonyl; phenylaminocarbonyl in which phenyl may have one to three C.sub.1 -C.sub.4 alkyl groups; phenyloxy or naphthyloxy-(C.sub.1 -C.sub.4)alkyl in which the phenyl or naphthyl ring may be substituted by one to three C.sub.1 -C.sub.4 alkyl groups; C.sub.1 -C.sub.4 alkylsulfonyl; (C.sub.1 -C.sub.4)alkyl- or N-di-(C.sub.1 -C.sub.4 alkyl)carboxamido(C.sub.1 -C.sub.4)alkyl; N-phenyl or substituted phenyl-carboxamido-(C.sub.1 -C.sub.4)alkyl in which phenyl may be substituted as above for C.sub.1 -C.sub.4 alkyl-substituted phenyl; cyano; amidino in which each N atom is substituted by a C.sub.1 -C.sub.4 alkyl group; and C.sub.1 -C.sub.4 alkylguanidino; andR.sup.3 and R.sup.4 are, independently, selected from hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluorine and chlorine, or acid addition salts thereof. Compounds of formulas I and II having certain values of R.sup.2 are antiarrhythmic or antiischaemic agents. The remaining values of R.sup.2 provide intermediate compounds of formulas I and II.Also disclosed herein a novel tetrahydro-3-substituted-7-substituted-1H[1,2,5]triazepino[1,2-a][1,2,4]benzotriazines, wherein the 7 substituent may be --SMe, --Cl or Br and the 3 substituent is the same as R.sup.2 in formulas I and II above. These compounds also serve as intermediates for the production of the antiarrhythmic agents for formula II above.

8. 发明授权

US4801706A N-substituted-hexahydro-1,2,5-triazepines 失效
标题翻译： N-取代 - 六氢-1,2,5-三氮杂
公开(公告)号：US4801706A
公开(公告)日：1989-01-31
申请号：US187187
申请日：1988-04-28
申请人： Michael W. Winkley , James L. Diebold
发明人： Michael W. Winkley , James L. Diebold
IPC分类号： C07D255/02 , A61K31/55
CPC分类号： C07D255/02 , Y02P20/55
摘要： Disclosed herein are N-substituted-hexahydro-1,2,5-triazepines of formula I, which is ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.1 is (R.sup.6).sub.2 --CH--(CH.sub.2).sub.n -- in which n is 0, 1, 2 or 3 and R.sup.6 is p-fluoro, chloro or methoxyphenyl; andR.sup.3 is hydrogen and R.sup.2 is benzoyl, 2,6-dimethyl or diethylbenzoyl, 2,6-dichlorobenzoyl, N-methyl, ethyl or propylcarboxamido, N-phenylcarboxamido, N-2,6-dimethyl or diethylphenylcarboxamido, N-2,6-dichlorophenylcarboxamido, N-methyl, ethyl or propylacetamido, N-phenylacetamido, N-2,6-dimethyl or diethylphenylacetamido, or N-2,6-dichlorophenylacetamido orR.sup.2 and R.sup.3 are the same and are N-methyl, ethyl or propylcarboxamido, benzoyl, 2,6-dimethyl or diethlbenzoyl, 2,6-dichlorobenzoyl, benzyl, 2,6-dimethyl or diethlbenzoyl, 2,6-dichlorobenzoyl, or a removable amino protective group. Also disclosed are N-substituted-hexahydro-1,2,5-triazepines of formula II in which R.sup.1 of formula I is replaced by R.sup.7 which is C.sub.1 -C.sub.4 alkyl, and R.sup.2 and R.sup.3 of formula I are replaced by R.sup.8 and R.sup.9 which are, respectively, N-2,6-dimethyl, diethyl or dichlorophenylcarboxamido or N-2,6-dimethyl, diethyl or dichlorophenylacetamido and hydrogen. The compounds of the invention have antiarrhythmic properties or are intermediates for the preparation thereof.
摘要翻译：本文公开了式I的N-取代 - 六氢-1,2,5-三氮杂，其为I或其药学上可接受的酸加成盐，其中R 4和R 5独立地为氢或C 1 -C 4烷基; R1是（R6）2-CH-（CH2）n-，其中n是0,1,2或3，R6是对氟，氯或甲氧基苯基; 并且R 3是氢，R 2是苯甲酰基，2,6-二甲基或二乙基苯甲酰基，2,6-二氯苯甲酰基，N-甲基，乙基或丙基甲酰胺基，N-苯基甲酰胺基，N-2,6-二甲基或二乙基苯基甲酰胺基，N-2,6 乙基或丙基乙酰氨基，N-苯基乙酰胺基，N-2,6-二甲基或二乙基苯基乙酰胺基，或N-2,6-二氯苯乙酰氨基或R2和R3相同，为N-甲基，乙基或丙基甲酰胺基，苯甲酰基，2,6-二甲基或二乙基苯甲酰基，2,6-二氯苯甲酰基，苄基，2,6-二甲基或二乙基苯甲酰基，2,6-二氯苯甲酰或可除去的氨基保护基。还公开了式II的N-取代 - 六氢-1,2,5-三氮杂，其中式I的R 1被作为C 1 -C 4烷基的R 7代替，式I的R 2和R 3被R 8和R 9取代，分别为N-2,6-二甲基，二乙基或二氯苯基甲酰胺基或N-2,6-二甲基，二乙基或二氯苯乙酰氨基和氢。本发明的化合物具有抗心律失常性质或者是其制备的中间体。

9. 发明授权

US4001214A Aminoalkyl ethers of 2,2'- and 3,3'-dihydroxybenzil 失效
标题翻译： 2,2'-和3,3'-二羟基苯胺的氨基烷基醚
公开(公告)号：US4001214A
公开(公告)日：1977-01-04
申请号：US627486
申请日：1975-10-30
申请人： Gerhard R. Wendt , Michael W. Winkley
发明人： Gerhard R. Wendt , Michael W. Winkley
IPC分类号： C07D295/092 , C07D295/08
CPC分类号： C07D295/088 , Y10S514/821
摘要： Octamethyleneiminoalkyl and heptamethyleneiminoalkyl ethers of 2,2'- and 3,3'-dihydroxybenzil are prepared by reacting the dithallium salt of 2,2'- or 3,3'-dihydroxybenzil with an N-chloroalkyl octamethyleneimine or heptamethyleneimine. The products have antiarrhythmic activity.

10. 发明申请

US20090018208A1 Novel Succinate Salt of O-Desmethyl-Venlafaxine 审中-公开
标题翻译： O-去甲基 - 文拉法辛的新型琥珀酸盐
公开(公告)号：US20090018208A1
公开(公告)日：2009-01-15
申请号：US11841638
申请日：2007-08-20
申请人： Anthony F. Hadfield , Syed M. Shah , Michael W. Winkley , Karen W. Sutherland , Jmaes A. Provost , Aeri Park , Rex A. Shipplett , Brenton W. Russell , Beat T. Weber
发明人： Anthony F. Hadfield , Syed M. Shah , Michael W. Winkley , Karen W. Sutherland , Jmaes A. Provost , Aeri Park , Rex A. Shipplett , Brenton W. Russell , Beat T. Weber
IPC分类号： A61K31/135 , A61P25/24
CPC分类号： C07C55/10 , A61K9/2013 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K31/137 , C07B2200/13 , C07C215/64 , C07C2601/14
摘要： A novel salt of O-desmethyl venlafaxine is provided, O-desmethylvenlafaxine succinate. Pharmaceutical compositions, dosage forms and methods of use are also provided.
摘要翻译：提供O-去甲基文拉法辛的新型盐，O-去甲基文拉法辛琥珀酸酯。还提供了药物组合物，剂型和使用方法。

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