公开(公告)号：US20110117057A1

公开(公告)日：2011-05-19

申请号：US12973020

申请日：2010-12-20

申请人： Anil K. Saksena ,  Viyyoor Moopil Girijavallabhan ,  Raymond G. Lovey ,  Edwin Jao ,  Frank Bennett ,  Jinping L. McCormick ,  Haiyan Wang ,  Russell E. Pike ,  Stephane L. Bogen ,  Tin-Yau Chan ,  Yi-Tsung Liu ,  Zhaoning Zhu ,  F. George Njoroge ,  Ashok Arasappan ,  Tejal Parekh ,  Ashit K. Ganguly ,  Kevin X. Chen ,  Srikanth Venkatraman ,  Henry A. Vaccaro ,  Patrick A. Pinto ,  Bama Santhanam ,  Scott Jeffrey Kemp ,  Odile Esther Levy ,  Marguerita Lim-Wilby ,  Susan Y. Tamura ,  Wanli Wu ,  Siska Hendrata ,  Yuhua Huang

发明人： Anil K. Saksena ,  Viyyoor Moopil Girijavallabhan ,  Raymond G. Lovey ,  Edwin Jao ,  Frank Bennett ,  Jinping L. McCormick ,  Haiyan Wang ,  Russell E. Pike ,  Stephane L. Bogen ,  Tin-Yau Chan ,  Yi-Tsung Liu ,  Zhaoning Zhu ,  F. George Njoroge ,  Ashok Arasappan ,  Tejal Parekh ,  Ashit K. Ganguly ,  Kevin X. Chen ,  Srikanth Venkatraman ,  Henry A. Vaccaro ,  Patrick A. Pinto ,  Bama Santhanam ,  Scott Jeffrey Kemp ,  Odile Esther Levy ,  Marguerita Lim-Wilby ,  Susan Y. Tamura ,  Wanli Wu ,  Siska Hendrata ,  Yuhua Huang

IPC分类号： A61K38/06 ,  C07D207/16 ,  C07D403/10 ,  C07K5/083 ,  C07D209/42 ,  C07K5/107 ,  C07D215/48 ,  A61K38/05 ,  A61K38/07 ,  A61K38/21 ,  A61P31/14

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827 ,  C07K7/02

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。

公开(公告)号：US5750532A

公开(公告)日：1998-05-12

申请号：US453723

申请日：1995-05-30

申请人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

发明人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

IPC分类号： C07D213/30 ,  C07D213/70 ,  C07D233/54 ,  C07D233/60 ,  C07D233/90 ,  C07D233/94 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D239/54 ,  C07D257/04 ,  C07D257/06 ,  C07D277/36 ,  C07D295/092 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D521/00 ,  A61K31/505 ,  A61K31/52

CPC分类号： C07D213/30 ,  C07D213/70 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/90 ,  C07D233/94 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D239/54 ,  C07D249/08 ,  C07D257/04 ,  C07D257/06 ,  C07D277/36 ,  C07D295/088 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

摘要： The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen, X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, loweralkanediyl-dihydrofurandiyl-loweralkanediyl, tetrahydrofurandiyl, tetrahydropyrandiyl, loweralkanediyl-tetrahydropyrandiyl-loweralkanediyl or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and with the further proviso that when Z is 2-chloro-4-methoxyphenyl, X is --O--, Q is C.sub.5 -C.sub.7 alkanediyl and Y is a bond, W is not imidazolyl substituted at positions 2, 4 and 5 with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyloweralkyl, nitro, loweralkoxycarbonyl, lower alkyl and amino methylene; W' is divale W. The compound is have antiviral activity, antiinflammatory activity and are PAF inhibitors.

公开(公告)号：US5559133A

公开(公告)日：1996-09-24

申请号：US167812

申请日：1993-12-16

申请人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Richard W. Versace ,  Anil K. Saksena ,  Patrick A. Pinto

发明人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Richard W. Versace ,  Anil K. Saksena ,  Patrick A. Pinto

IPC分类号： A61K31/085 ,  A61K31/09 ,  A61K31/185 ,  A61K31/235 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/421 ,  A61P31/00 ,  C07C43/205 ,  C07C43/225 ,  C07C43/23 ,  C07C69/92 ,  C07C205/38 ,  C07C233/25 ,  C07C255/54 ,  C07C317/22 ,  C07C323/19 ,  C07D213/30 ,  C07D213/65 ,  C07D263/12 ,  C07D263/14 ,  C07D307/12 ,  C07D307/28 ,  C07D307/42 ,  C07D333/16 ,  A61K31/44 ,  C07D213/63

CPC分类号： C07D213/30 ,  C07C43/225 ,  C07C43/23 ,  C07C69/92 ,  C07D263/14 ,  C07D307/12 ,  C07D307/28 ,  C07D307/42 ,  C07D333/16

摘要： A compound represented by formula I, Ar.sub.1 --O--M--O--Ar.sub.2, wherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10) alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## O is oxygen; R' is (C.sub.1 -C.sub.3 alkyl or H; A is oxygen or sulfur; Q is selected from hydrogen, halogen, nitro, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 C.sub.6) perhaloalkyl, (C.sub.1 -C.sub.6) alkylthio (C.sub.1 -C.sub.6) or alkyl sulfonyl; the dotted lines in M-3 and M-4 between carbons, 2 and 3 and 3 and 4, and 4 and 5 mean that the bonds between carbons 2 and 3, and 3 and 4, and 5 and 6, may each be a single or double bond; n=1 or 2; m=1 or 2; p=0 or 1; or pharmaceutically acceptable salts thereof as well as pharmaceutical compositions containing such compounds and methods of treating or preventing viral infections, especially picornaviral infections using the compounds of formula I, are disclosed.

摘要翻译： PCT No.PCT / US92 / 04961 Sec。 371日期：1993年12月16日 102（e）日期1993年12月16日PCT提交1992年6月17日PCT公布。 出版物WO92 / 22520 日期1992年12月23日由式I表示的化合物Ar1-OMO-Ar2，其中Ar1和Ar2独立地为取代的苯基或取代的吡啶基，所述苯基或吡啶基上的取代基独立地选自（C1- （C 1 -C 10）烷氧基，羟基或（C 1 -C 10）烷基，（C 1 -C 10）烷基，（C 1 -C 10）烷氧基，卤素，氨基甲酰基，（C 1 -C 10）烷氧基羰基，恶唑基， 烷氧基羰基 M是图像M-1图像M-2图像M-3图像M-3 O是氧气; R 1是（C 1 -C 6烷基或H; A是氧或硫; Q选自氢，卤素，硝基，（C 1 -C 6）烷基，（C 1 -C 6）全卤烷基，（C 1 -C 6）烷硫基 或烷基磺酰基;碳原子数2和3，3和4以及4和5之间的M-3和M-4中的虚线意味着碳2和3之间，3和4和5和6之间的键， 可以是单键或双键; n = 1或2; m = 1或2; p = 0或1;或其药学上可接受的盐以及含有这些化合物的药物组合物和治疗或预防病毒感染的方法，特别是 公开了使用式I化合物的小RNA病毒感染。

公开(公告)号：US4584133A

公开(公告)日：1986-04-22

申请号：US549535

申请日：1983-11-07

申请人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

发明人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

IPC分类号： C07D499/897 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  C07D205/09 ,  C07D499/00 ,  C07D499/06 ,  C07D499/88 ,  C07D499/893 ,  C07F7/08 ,  C07F7/18 ,  C07D205/08 ,  C07D487/04

CPC分类号： C07D205/09 ,  C07D499/88 ,  C07F7/0818 ,  C07F7/186 ,  Y02P20/55

摘要： Improved processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates which eliminate the step of using a silver reagent are disclosed.

摘要翻译： 公开了用于生产6-羟乙基-2-取代的硫代青霉烯-3-羧酸盐的改进方法，其消除了使用银试剂的步骤。

公开(公告)号：US20110189127A1

公开(公告)日：2011-08-04

申请号：US12997654

申请日：2009-06-10

申请人： Srikanth Venkatraman ,  Anilkumar Gopinadhan Nair ,  Kevin X. Chen ,  Francisco Valazquez ,  Qingbei Zeng ,  Duan Liu ,  Yueheng Jiang ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Stuart B. Rosenblum ,  Stephen J. Gavalas ,  Patrick A. Pinto ,  Oleg B. Selyutin ,  Bancha Vibulbhan

发明人： Srikanth Venkatraman ,  Anilkumar Gopinadhan Nair ,  Kevin X. Chen ,  Francisco Valazquez ,  Qingbei Zeng ,  Duan Liu ,  Yueheng Jiang ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Stuart B. Rosenblum ,  Stephen J. Gavalas ,  Patrick A. Pinto ,  Oleg B. Selyutin ,  Bancha Vibulbhan

IPC分类号： A61K31/4439 ,  C07D401/14 ,  C07D491/22 ,  A61K31/437 ,  A61K31/517 ,  A61K31/47 ,  A61K38/21 ,  A61K31/7052 ,  A61K39/00 ,  A61K39/395 ,  A61K31/7056 ,  A61P31/12

CPC分类号： C07D491/048 ,  C07D491/04 ,  C07D519/00

摘要： The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

摘要翻译： 本发明涉及三环吲哚衍生物，包含至少一种三环吲哚衍生物的组合物，以及使用三环吲哚衍生物治疗或预防患者病毒感染或病毒相关病症的方法。

公开(公告)号：US20110033417A1

公开(公告)日：2011-02-10

申请号：US12675897

申请日：2008-08-27

申请人： Gopinadhan N. Anilkumar ,  Frank Bennett ,  Tin-Yau Chan ,  Kevin X. Chen ,  Mousumi Sannigrahi ,  Francisco Velazquez ,  Srikanth Venkatraman ,  Qingbei Zeng ,  Jose S. Duca ,  Charles A. Lesburg ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Stuart B. Rosenblum ,  Neng-Yang Shih ,  Stephen J. Gavalas ,  Yueheng Jiang ,  Patrick A. Pinto ,  Haiyan Pu ,  Oleg B. Selyutin ,  Bancha Vibulbhan ,  Li Wang ,  Wanli Wu ,  Weiying Yang ,  Yuhua Huang ,  Hsueh-Cheng Huang ,  Robert Palermo ,  Boris Feld

发明人： Gopinadhan N. Anilkumar ,  Frank Bennett ,  Tin-Yau Chan ,  Kevin X. Chen ,  Mousumi Sannigrahi ,  Francisco Velazquez ,  Srikanth Venkatraman ,  Qingbei Zeng ,  Jose S. Duca ,  Charles A. Lesburg ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Stuart B. Rosenblum ,  Neng-Yang Shih ,  Stephen J. Gavalas ,  Yueheng Jiang ,  Patrick A. Pinto ,  Haiyan Pu ,  Oleg B. Selyutin ,  Bancha Vibulbhan ,  Li Wang ,  Wanli Wu ,  Weiying Yang ,  Yuhua Huang ,  Hsueh-Cheng Huang ,  Robert Palermo ,  Boris Feld

IPC分类号： A61K38/21 ,  C07D401/04 ,  C07D413/14 ,  C07D209/42 ,  C07D401/14 ,  C07D417/14 ,  C07D407/14 ,  C07D409/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/404 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/4436 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/7088 ,  A61K31/7052 ,  A61K39/12 ,  A61K39/42 ,  A61P31/12 ,  A61P31/14

CPC分类号： C07D417/14 ,  C07D209/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

摘要翻译： 本发明涉及2,3-取代的吲哚衍生物，包含至少一种2,3-取代的吲哚衍生物的组合物和使用2,3-取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关的方法 病人无序。

公开(公告)号：US07012066B2

公开(公告)日：2006-03-14

申请号：US09908955

申请日：2001-07-19

申请人： Anil K. Saksena ,  Viyyoor Moopil Girijavallabhan ,  Raymond G. Lovey ,  Edwin Jao ,  Frank Bennett ,  Jinping L. Mc Cormick ,  Haiyan Wang ,  Russell E. Pike ,  Stephane L. Bogen ,  Tin-Yau Chan ,  Yi-Tsung Liu ,  Zhaoning Zhu ,  F. George Njoroge ,  Ashok Arasappan ,  Tejal Parekh ,  Ashit K. Ganguly ,  Kevin X. Chen ,  Srikanth Venkatraman ,  Henry A. Vaccaro ,  Patrick A. Pinto ,  Bama Santhanam ,  Scott Jeffrey Kemp ,  Odile Esther Levy ,  Marguerita Lim-Wilby ,  Susan Y. Tamura ,  Wanli Wu ,  Siska Hendrata ,  Yuhua Huang

发明人： Anil K. Saksena ,  Viyyoor Moopil Girijavallabhan ,  Raymond G. Lovey ,  Edwin Jao ,  Frank Bennett ,  Jinping L. Mc Cormick ,  Haiyan Wang ,  Russell E. Pike ,  Stephane L. Bogen ,  Tin-Yau Chan ,  Yi-Tsung Liu ,  Zhaoning Zhu ,  F. George Njoroge ,  Ashok Arasappan ,  Tejal Parekh ,  Ashit K. Ganguly ,  Kevin X. Chen ,  Srikanth Venkatraman ,  Henry A. Vaccaro ,  Patrick A. Pinto ,  Bama Santhanam ,  Scott Jeffrey Kemp ,  Odile Esther Levy ,  Marguerita Lim-Wilby ,  Susan Y. Tamura ,  Wanli Wu ,  Siska Hendrata ,  Yuhua Huang

IPC分类号： A61K38/07 ,  A61K38/06 ,  C07K5/08 ,  C07K5/10

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827 ,  C07K7/02

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

公开(公告)号：US5852034A

公开(公告)日：1998-12-22

申请号：US877399

申请日：1997-06-17

申请人： F. George Njoroge ,  Bancha Vibulbhan ,  Patrick A. Pinto ,  Viyyoor M. Girijavallabhan

发明人： F. George Njoroge ,  Bancha Vibulbhan ,  Patrick A. Pinto ,  Viyyoor M. Girijavallabhan

IPC分类号： A61K31/4545 ,  A61K31/506 ,  A61K31/513 ,  A61P35/00 ,  A61P43/00 ,  C07D401/14 ,  A61K31/44 ,  A61K31/445 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D401/14

摘要： Compounds of the following formula useful for inhibiting Ras function and therefore inhibiting or treating the abnormal growth of cells are disclosed: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R and R.sup.2 are halo; R.sup.1 and R.sup.3 are H and halo, provided that at least one is H; W is N, CH or C when the double bond is present at the C-11 position; R.sup.4 is --(CH.sub.2).sub.n --R.sup.5 or ##STR2## R.sup.5 is ##STR3## R.sup.6 is R.sup.5 or ##STR4## Z.sup.1 and Z.sup.2 are independently selected from the group consisting of .dbd.O and .dbd.S; n is 1-6; and n.sub.1 is 0 or 1.

摘要翻译： 公开了可用于抑制Ras功能并因此抑制或治疗细胞异常生长的下式的化合物：或其溶剂合物，其中：R和R 2为卤素; R1和R3是H和卤素，条件是至少一个是H; 当双键存在于C-11位置时，W是N，CH或C; R 4是 - （CH 2）n -R 5或者R 5是R 6是R 5或Z 1，Z 2独立地选自= O和= S; n为1-6; n1为0或1。

公开(公告)号：US4814442A

公开(公告)日：1989-03-21

申请号：US757047

申请日：1985-07-19

申请人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

发明人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

IPC分类号： C07D499/897 ,  A61K31/43 ,  A61P31/04 ,  C07D205/09 ,  C07D499/86 ,  C07D499/87 ,  C07D499/88 ,  C07F7/18 ,  C07D499/00 ,  A61K31/425

CPC分类号： C07F7/186 ,  C07D205/09 ,  C07D499/88

摘要： Processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates are disclosed as well as novel penems.

公开(公告)号：US4443373A

公开(公告)日：1984-04-17

申请号：US363710

申请日：1982-03-30

申请人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

发明人： Viyyoor M. Girijavallabhan ,  Ashit K. Ganguly ,  Patrick A. Pinto ,  Richard W. Versace

IPC分类号： C07D499/06 ,  C07D499/88 ,  C07F7/08 ,  C07D499/04 ,  C07D499/00

CPC分类号： C07D499/88 ,  C07F7/0812 ,  Y02P20/55

摘要： There is disclosed a process for preparing 6-hydroxyethyl-2-alkylthio penem-3-carboxylates by a multi-step process comprising reacting an azetidinone having a protected hydroxy group at the 5 position with a diester of ketomalonic acid, chlorinating the resulting N-substituted azetidinone, removing the chlorine and OH protecting group, reacting the resulting compound with a silver salt to form a silver thio substituted at the 4 position of the azetidinone, cyclizing with a thiocarbonyl compound, then reacting the resulting penam with a fluoride to form a penam-penem tautomer, reacting the tautomer with a halide or ethylenically unsaturated compound followed by deprotecting the carboxyl at the 3 position to form the final penem product in high yield.

摘要翻译： 公开了通过多步法制备6-羟乙基-2-烷硫基半胱胺-3-羧酸盐的方法，包括使5位具有被保护的羟基的氮杂环丁酮与酮缩醇酸的二酯反应，氯化得到的N- 取代的氮杂环丁酮，除去氯和OH保护基团，使所得化合物与银盐反应，形成在氮杂环丁酮的4位被取代的硫代硫酸酯，用硫代羰基化合物环化，然后使所得的penam与氟化物反应形成 双氯吡啶互变异构体，使互变异构体与卤化物或烯属不饱和化合物反应，然后在3位上脱羧保护羧基，以高产率形成最终的penem产物。