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1. 发明专利

CA1340543C PHARMACEUTICALLY ACTIVE COMPOUNDS 未知
公开(公告)号：CA1340543C
公开(公告)日：1999-05-18
申请号：CA553925
申请日：1987-12-09
申请人： PINTO PATRICK ANTHONY , GANGULY ASHIT KUMAR , VERSACE RICHARD WILLIAM , GIRIJAVALLABHAN VIYYOOR MOOPIL
发明人： PINTO PATRICK ANTHONY , GANGULY ASHIT KUMAR , VERSACE RICHARD WILLIAM , GIRIJAVALLABHAN VIYYOOR MOOPIL
IPC分类号： C07D249/08 , A61K31/075 , A61K31/095 , A61K31/12 , A61K31/15 , A61K31/165 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/443 , A61K31/496 , A61K31/505 , A61K31/52 , A61P7/02 , A61P29/00 , A61P31/12 , C07C45/00 , C07C49/00 , C07C67/00 , C07C313/00 , C07C317/24 , C07C317/26 , C07C317/44 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/36 , C07C323/41 , C07C323/47 , C07C323/65 , C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/84 , C07D233/90 , C07D233/91 , C07D233/94 , C07D235/06 , C07D235/12 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D263/32 , C07D277/24 , C07D277/36 , C07D295/08 , C07D295/092 , C07D307/20 , C07D405/04 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00 , C07D235/04
摘要： The disclosed invention is compounds represented by the formula Z-X-Q-Y-W , Z-X-Q-Y-W'-Y-Q-X-Z I II and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates 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; 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining members of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl; X and Y are each independently a bond, -O-, -S-, -SO2-, (see fig.I), (see fig.II), (see fig.III), (see fig.IV), or (see fig.V), 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, tetrahydrofurandiyl, tetrahydropyrandiyl, or, loweralkanediyltetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, epoxy, fluorine, chlorine, azide, or amino; 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, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.

2. 发明申请

WO1992022520A1 ORALLY ACTIVE ANTIVIRAL COMPOUNDS 审中-公开
标题翻译： ORALLY活性抗病毒化合物
公开(公告)号：WO1992022520A1
公开(公告)日：1992-12-23
申请号：PCT/US1992004961
申请日：1992-06-17
申请人： SCHERING CORPORATION , GIRIJAVALLABHAN, Viyyoor, M. , GANGULY, Ashit, K. , VERSACE, Richard, W. , SAKSENA, Anil, K. , PINTO, Patrick, A.
发明人： SCHERING CORPORATION
IPC分类号： C07C43/225
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) Ar1-O-M-O-Ar2 wherein Ar1 and Ar2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C1-C10)alkyl, (C1-C10)alkoxy, halogen, carbamyl, dialkylcarbamyl, (C1-C10)-alkoxycarbonyl, oxazoyl, and (C1-C10)alkyl substituted by halogen, (C1-C10)alkoxy, hydroxy, or (C1-C10)alkoxycarbonyl; M is M-1, M-2, M-3 or M-4 (C4-C8)alkylene, (C4-C8) alkenylene or (C4-C8)-alkynylene; O is oxygen; R' is (C1-C3)alkyl or H; A is oxygen or sulfur; Q is selected from hydrogen, halogen, nitro, (C1-C6) alkyl, (C1-C6) perhaloalkyl, (C1-C6) alkylthio (C1-C6) alkyl sulfonyl; the dotted lines in M-3 and M-4 between carbons 2 and 3, 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 the compounds and the use of the compounds of formula (I) for preparation of a medicament for methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
摘要翻译：由式I Ar1-OMO-Ar2I表示的化合物，其中Ar1和Ar2独立地是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-C10）烷基，（C1-C10）烷基中的一个，两个或三个（C1-C10）烷氧基羰基，恶唑基和被卤素取代的（C1-C10）烷基，（C1-C10）烷氧基，羟基或（C1-C10）烷氧羰基;（C1-C10）烷氧基，（C 4 -C 8）亚烷基，（C 4 -C 8）亚烯基或（C 4 -C 8） - 亚炔基; O是氧; R min为（C 1 -C 3）烷基或H; A是氧或硫; Q选自氢，卤素，硝基，（C1-C6）烷基，（C1-C6）全卤烷基，（C1-C6）烷硫基（C1-C6）烷基磺酰基; 碳素2,3和4以及5和6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之间的键可以是单或双键; n = 1或2m = 1或2p = 0或1及其药学上可接受的盐。以及含有该化合物的药物组合物和式I化合物用于制备治疗或预防病毒感染，特别是小RNA病毒感染的方法的药物的用途。

3. 发明申请

WO2009152200A1 TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：三环吲哚衍生物及其使用方法
公开(公告)号：WO2009152200A1
公开(公告)日：2009-12-17
申请号：PCT/US2009/046822
申请日：2009-06-10
申请人： SCHERING CORPORATION , VENKATRAMAN, Srikanth , ANILKUMAR, Gopinadhan, N. , CHEN, Kevin, X. , VELAZQUEZ, Francisco , ZENG, Qingbei , LIU, Duan , JIANG, Yueheng , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , GAVALAS, Stephen, J. , PINTO, Patrick, A. , SELYUTIN, Oleg, B. , VIBULBHAN, Bancha
发明人： VENKATRAMAN, Srikanth , ANILKUMAR, Gopinadhan, N. , CHEN, Kevin, X. , VELAZQUEZ, Francisco , ZENG, Qingbei , LIU, Duan , JIANG, Yueheng , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , GAVALAS, Stephen, J. , PINTO, Patrick, A. , SELYUTIN, Oleg, B. , VIBULBHAN, Bancha
IPC分类号： C07D491/048 , C07D519/00 , A61P31/14 , A61K31/4439 , A61K31/444
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

4. 发明申请

WO2009058856A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE 审中-公开
标题翻译：丙型肝炎病毒NS3丝氨酸蛋白酶的大分子抑制剂
公开(公告)号：WO2009058856A1
公开(公告)日：2009-05-07
申请号：PCT/US2008/081575
申请日：2008-10-29
申请人： SCHERING CORPORATION , VENKATRAMAN, Srikanth , NJOROGE, F., George , WU, Wanli , GIRIJAVALLABHAN, Viyyoor , MCKITTRICK, Brian , SU, Jing , VELAZQUEZ, Francisco , PINTO, Patrick, A.
发明人： VENKATRAMAN, Srikanth , NJOROGE, F., George , WU, Wanli , GIRIJAVALLABHAN, Viyyoor , MCKITTRICK, Brian , SU, Jing , VELAZQUEZ, Francisco , PINTO, Patrick, A.
IPC分类号： C07K5/06 , A61P31/22
CPC分类号： A61K31/541 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/55 , A61K38/21 , A61K45/06 , C07K5/06026 , C07K5/0606 , C07K5/06069 , A61K2300/00
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。

5. 发明申请

WO1991000858A1 PHARMACEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：药物活性化合物
公开(公告)号：WO1991000858A1
公开(公告)日：1991-01-24
申请号：PCT/US1990003694
申请日：1990-07-06
申请人： SCHERING CORPORATION , GIRIJAVALLABHAN, Viyyoor, M. , GANGULY, Ashit, K. , PINTO, Patrick, A. , VERSACE, Richard, W.
发明人： SCHERING CORPORATION
IPC分类号： C07D233/60
CPC分类号： C07D213/30 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04
摘要： The disclosed invention relates to compounds represented by the formula (I): Z-X-Q-Y-W, (II): Z-X-Q-Y-W'-Y-Q-X-Z and pharmaceutically acceptable salts thereof, wherein each Z is independently tertiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, 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, -O-, -S-, -SO2-, (a), (b), (c), (d), (e), (f), (g), (h) or -CH2-O-; 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, wherein the substituents are one or more of hydroxy, ketalized adjacent hydroxys, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring, 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 C5-C7 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 divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.

6. 发明申请

WO2014025736A1 HCV NS3 PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：WO2014025736A1
公开(公告)日：2014-02-13
申请号：PCT/US2013/053725
申请日：2013-08-06
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , BARA, Thomas , BHAT, Sathesh , BISWAS, Dipshika , BROCKUNIER, Linda , BURNETTE, Duane , CHACKALAMANNIL, Samuel , CHELIAH, Mariappan, V. , CHEN, Austin , CLASBY, Martin , COLANDREA, Vince, J. , GUO, Zhuyan , HAN, Yongxin , JAYNE, Charles , JOSIEN, Hubert , MARCANTONIO, Karen , MIAO, Shouwu , NEELAMKAVIL, Santhosh , PINTO, Patrick , RAJAGOPALAN, Murali , SHAH, Unmesh , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , XIA, Yan
发明人： BARA, Thomas , BHAT, Sathesh , BISWAS, Dipshika , BROCKUNIER, Linda , BURNETTE, Duane , CHACKALAMANNIL, Samuel , CHELIAH, Mariappan, V. , CHEN, Austin , CLASBY, Martin , COLANDREA, Vince, J. , GUO, Zhuyan , HAN, Yongxin , JAYNE, Charles , JOSIEN, Hubert , MARCANTONIO, Karen , MIAO, Shouwu , NEELAMKAVIL, Santhosh , PINTO, Patrick , RAJAGOPALAN, Murali , SHAH, Unmesh , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , XIA, Yan
IPC分类号： C07D491/107 , A61K31/343 , A61K31/407 , A61P1/16 , A61P31/14
CPC分类号： C07K5/08 , A61K38/06 , A61K45/06 , C07D419/00 , C07D491/22
摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
摘要翻译：本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

7. 发明申请

WO2009032116A1 2, 3-SUBSTITUTED INDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS 审中-公开
标题翻译： 2，3替代的用于治疗病毒感染的吲哚酚衍生物
公开(公告)号：WO2009032116A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/010130
申请日：2008-08-27
申请人： SCHERING CORPORATION , ANILKUMAR, Gopinadhan, N. , BENNETT, Frank , CHAN, Tin-Yau , CHEN, Kevin, X. , SANNIGRAHI, Mousumi , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , ZENG, Qingbei , DUCA, Jose, S. , LESBURG, Charles, A. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , GAVALAS, Stephen, J. , JIANG, Yueheng , PINTO, Patrick, A. , PU, Haiyan , SELYUTIN, Oleg, B. , VIBULBHAN, Bancha , WANG, Li , WU, Wanli , YANG, Weiying , HUANG, Yuhua , HUANG, Hsueh-Cheng , PALERMO, Robert , FELD, Boris
发明人： ANILKUMAR, Gopinadhan, N. , BENNETT, Frank , CHAN, Tin-Yau , CHEN, Kevin, X. , SANNIGRAHI, Mousumi , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , ZENG, Qingbei , DUCA, Jose, S. , LESBURG, Charles, A. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , GAVALAS, Stephen, J. , JIANG, Yueheng , PINTO, Patrick, A. , PU, Haiyan , SELYUTIN, Oleg, B. , VIBULBHAN, Bancha , WANG, Li , WU, Wanli , YANG, Weiying , HUANG, Yuhua , HUANG, Hsueh-Cheng , PALERMO, Robert , FELD, Boris
IPC分类号： C07D209/42 , C07D401/04 , C07D401/14 , A61K31/404 , A61P31/12
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。

8. 发明申请

WO2005030796A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE 审中-公开
标题翻译：丙型肝炎病毒NS3丝氨酸蛋白酶的大分子抑制剂
公开(公告)号：WO2005030796A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/031136
申请日：2004-09-23
申请人： SCHERING CORPORATION , VENKATRAMAN, Srikanth , NJOROGE, F., George , WU, Wanli , GIRIJAVALLABHAN, Viyyoor, M. , MCKITTRICK, Brian , SU, Jing , VELASQUEZ, Francisco , PINTO, Patrick, A.
发明人： VENKATRAMAN, Srikanth , NJOROGE, F., George , WU, Wanli , GIRIJAVALLABHAN, Viyyoor, M. , MCKITTRICK, Brian , SU, Jing , VELASQUEZ, Francisco , PINTO, Patrick, A.
IPC分类号： C07K5/12
CPC分类号： C07D245/04 , A61K31/33 , A61K38/12 , A61K38/21 , A61K38/212 , C04B35/632 , C07D401/12 , C07D403/12 , C07D409/12 , C07D487/04 , C07D513/04 , C07K5/0217 , C07K5/0802 , A61K2300/00
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula (1): wherein Z', L', M', R 1 , X and D are defined herein.
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以及包含这些化合物的药物组合物及其用于治疗与HCV蛋白酶相关的病症的方法。新化合物通常包括15-20个成员大环，并具有结构式（1）的通式结构：其中Z'，L'，M'，R 1，X和D在本文中定义。

9. 发明申请

WO1991003451A1 ASYMMETRIC CHEMICAL SYNTHESIS AND INTERMEDIATES FOR MAKING ANTIFUNGAL COMPOUNDS 审中-公开
标题翻译：不对称化学合成和制备抗真菌化合物的中间体
公开(公告)号：WO1991003451A1
公开(公告)日：1991-03-21
申请号：PCT/US1990004843
申请日：1990-08-30
申请人： SCHERING CORPORATION , GIRIJAVALLABHAN, Viyyoor, M. , GANGULY, Ashit, K. , PINTO, Patrick , SARRE, Olga, Z.
发明人： SCHERING CORPORATION
IPC分类号： C07C49/80
CPC分类号： C07D231/12 , C07C33/46 , C07C49/80 , C07D233/56 , C07D249/08 , C07D303/08 , C07D309/12 , C07D407/12 , Y02P20/55
摘要： Intermediates of structural formula (II), (III), (IV), (VIII), (XI), or (XII), wherein said compound has an asymmetric center(s) as indicated by the single asterisk (*) and the double asterisk (**) and wherein the compound is substantially free from compound (s) having the same chemical structure but having other absolute stereochemical configurations at the asterisked carbon centers, or a pharmaceutically acceptable salt thereof, wherein Ar represents phenyl, substituted phenyl, 3-thienyl, substituted 3-thienyl, 3-furanyl or substituted 3-furanyl; R represents alkyl or cycloalkyl; R1 represents H or alkyl; X represents chloro, bromo or iodo; X1 represents OH, chloro, bromo, iodo or P1 where P1 represents alkoxy-substituted phenyloxy, benzyloxy, substituted benzyloxy, acyloxy, phenylthio, substituted phenylthio or -NHP2 where P2 is an amino protecting group; and P represents H or a hydroxy protecting group and processes for making chemically pure, enantiomeric antifungal compounds.

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