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111. 发明授权

US07704992B2 Hepatitis C virus inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US07704992B2
公开(公告)日：2010-04-27
申请号：US12358308
申请日：2009-01-23
申请人： Carol Bachand , Makonen Belema , Daniel H. Deon , Andrew C. Good , Jason Goodrich , Clint A. James , Rico Lavoie , Omar D. Lopez , Alain Martel , Nicholas A. Meanwell , Van N. Nguyen , Jeffrey Lee Romine , Edward H. Ruediger , Lawrence B. Snyder , Denis R. St. Laurent , Fukang Yang , David R. Langley , Gan Wang , Lawrence G. Hamann
发明人： Carol Bachand , Makonen Belema , Daniel H. Deon , Andrew C. Good , Jason Goodrich , Clint A. James , Rico Lavoie , Omar D. Lopez , Alain Martel , Nicholas A. Meanwell , Van N. Nguyen , Jeffrey Lee Romine , Edward H. Ruediger , Lawrence B. Snyder , Denis R. St. Laurent , Fukang Yang , David R. Langley , Gan Wang , Lawrence G. Hamann
IPC分类号： A61K31/55 , A61K31/4155 , C07D223/18 , C07D233/54
CPC分类号： C07D403/14 , C07D405/14
摘要： The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
摘要翻译：本公开涉及用于治疗丙型肝炎病毒（HCV）感染的化合物，组合物和方法。还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

112. 发明申请

US20090253741A1 ALKENE PIPERIDINE DERIVATIVES AS ANTIVIRAL AGENTS 有权
标题翻译： ALKENE PIPERIDINE DERIVATIVES作为抗病毒剂
公开(公告)号：US20090253741A1
公开(公告)日：2009-10-08
申请号：US12484407
申请日：2009-06-15
申请人： Tao Wang , Ying Han , John F. Kadow , Zhongxing Zhang , Nicholas A. Meanwell
发明人： Tao Wang , Ying Han , John F. Kadow , Zhongxing Zhang , Nicholas A. Meanwell
IPC分类号： A61K31/4709 , C07D401/12 , A61P31/18
CPC分类号： A61K31/445 , A61K31/4545 , A61K45/06 , C07D211/70 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.
摘要翻译：本公开提供具有药物和生物影响性质的化合物，其药物组合物和使用方法。特别地，本公开涉及具有独特抗病毒活性的烯烃哌啶衍生物。更具体地，本公开涉及可用于治疗HIV和AIDS的化合物。

113. 发明授权

US07485633B2 Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors 有权
标题翻译：环丙基稠合吲哚并苯并氮平HCV NS5B抑制剂
公开(公告)号：US07485633B2
公开(公告)日：2009-02-03
申请号：US11684710
申请日：2007-03-12
申请人： Nicholas A. Meanwell , Robert G. Gentles , Min Ding , John A. Bender , John F. Kadow , Piyasena Hewawasam , Thomas W. Hudyma , Xiaofan Zheng
发明人： Nicholas A. Meanwell , Robert G. Gentles , Min Ding , John A. Bender , John F. Kadow , Piyasena Hewawasam , Thomas W. Hudyma , Xiaofan Zheng
IPC分类号： A61K31/55 , A61P31/00 , C07D223/14
CPC分类号： C07D487/04
摘要： The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
摘要翻译：本发明包括式I的化合物，其药学上可接受的盐，组合物和使用该化合物的方法。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

114. 发明申请

US20080145334A1 HEPATITIS C VIRUS INHIBITORS 有权
标题翻译： HEPATITIS C病毒抑制剂
公开(公告)号：US20080145334A1
公开(公告)日：2008-06-19
申请号：US11939768
申请日：2007-11-14
申请人： Alan Xiangdong Wang , Barbara Zhizhen Zheng , Stanley D'Andrea , Nicholas A. Meanwell , Paul Michael Scola
发明人： Alan Xiangdong Wang , Barbara Zhizhen Zheng , Stanley D'Andrea , Nicholas A. Meanwell , Paul Michael Scola
IPC分类号： A61K31/407 , A61K38/20 , A61K38/48 , A61K38/21 , A61K31/7056 , A61P31/12 , A61K31/437 , A61K38/45 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D498/04 , C07K5/0812
摘要： Macrocyclic peptides having the general formula: are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
摘要翻译：公开了具有以下通式的大环肽。还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

115. 发明申请

US20080132516A1 INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC N-SUBSTITUTED PIPERAZINE DERIVATIVES 有权
标题翻译：吲哚，氮杂和相关杂环N-取代的哌嗪衍生物
公开(公告)号：US20080132516A1
公开(公告)日：2008-06-05
申请号：US12028189
申请日：2008-02-08
申请人： Kap-Sun Yeung , Michelle E. Farkas , John F. Kadow , Nicholas A. Meanwell , Malcolm Taylor , David Johnston , Thomas Stephen Coulter , J.J Kim Wright
发明人： Kap-Sun Yeung , Michelle E. Farkas , John F. Kadow , Nicholas A. Meanwell , Malcolm Taylor , David Johnston , Thomas Stephen Coulter , J.J Kim Wright
IPC分类号： A61K31/496 , C07D401/14 , A61P31/18
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D491/04
摘要： This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is
摘要翻译：本发明提供具有药物和生物影响性质的式I化合物，包括其药学上可接受的盐，其药物组合物和使用方法。这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。式I的化合物具有下式：其中：Z为Q选自m为2; A选自噌啉基，萘啶基，喹喔啉基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹唑啉基，氮杂苯并呋喃基和酞嗪基，其各自可以任选被一个或两个独立地选自甲基，甲氧基，羟基，氨基和卤素; 和-W-是

116. 发明授权

US07323447B2 Hepatitis C virus inhibitors 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：US07323447B2
公开(公告)日：2008-01-29
申请号：US11348721
申请日：2006-02-06
申请人： Ny Sin , Andrew Charles Good , Brian Lee Venables , Paul Michael Scola , Nicholas A. Meanwell
发明人： Ny Sin , Andrew Charles Good , Brian Lee Venables , Paul Michael Scola , Nicholas A. Meanwell
IPC分类号： A61K38/00 , C07D215/00 , C07D207/00
CPC分类号： C07D401/12 , A61K38/2013 , A61K38/204 , A61K38/208 , A61K38/212 , C07D401/14 , C07D403/12 , C07K5/06139 , A61K2300/00
摘要： The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which inhibit the function of the NS3 protease (also referred to herein as “serine protease”) encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS3 protease.
摘要翻译：本公开一般涉及抗病毒化合物，更具体地涉及抑制由丙型肝炎病毒（HCV）编码的NS3蛋白酶（本文中也称为“丝氨酸蛋白酶”）的功能的化合物，包含这些化合物的组合物，和抑制NS3蛋白酶功能的方法。

117. 发明授权

US06908936B2 Substituted benzimidazole antiviral agents 失效
公开(公告)号：US06908936B2
公开(公告)日：2005-06-21
申请号：US10289829
申请日：2002-11-07
申请人： Kuo-Long Yu , Rita Lee Civiello , Mark R. Krystal , Kathleen F. Kadow , Nicholas A. Meanwell
发明人： Kuo-Long Yu , Rita Lee Civiello , Mark R. Krystal , Kathleen F. Kadow , Nicholas A. Meanwell
IPC分类号： A61K31/4192 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P31/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D455/02 , C07D249/18
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
摘要： The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazole derivatives for the treatment of respiratory syncytial virus infection.

118. 发明授权

US5348960A Imidazo[4,5-b]quinolinyl oxy alkyl tetrazolyl piperidine derivatives 失效
标题翻译：咪唑并[4,5-b]喹啉基氧基烷基四唑基哌啶衍生物
公开(公告)号：US5348960A
公开(公告)日：1994-09-20
申请号：US114262
申请日：1993-08-30
申请人： Piyasena Hewawasam , Nicholas A. Meanwell
发明人： Piyasena Hewawasam , Nicholas A. Meanwell
IPC分类号： C07D471/04 , A61K31/445
CPC分类号： C07D471/04
摘要： A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or (CH.sub.2).sub.m R.sup.3 ;R.sup.3 is tetrahydro-2H-pyranyl, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy, or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
摘要翻译：具有增强的水溶性生物利用度和代谢稳定性的一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的图像中，其中R1是H或C1-C4 低级烷基 R2是H或（CH2）mR3; R3是四氢-2H-吡喃基，C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

119. 发明授权

US5208237A 7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones 失效
标题翻译： 7-氧代丙基磺酰氨基 - 咪唑并[4,5-b]喹啉-2-酮
公开(公告)号：US5208237A
公开(公告)日：1993-05-04
申请号：US862879
申请日：1992-04-03
申请人： Piyasena Hewawasam , Nicholas A. Meanwell
发明人： Piyasena Hewawasam , Nicholas A. Meanwell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ; benzoxazol-2yl, or benzothiazol2-yl;R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
摘要翻译：具有增强的水溶性生物利用度和代谢稳定性的新一系列1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮公开在式I的化合物中，其中R 1是H或C1- C4低级烷基; R2是H，（CH2）mR3; 苯并恶唑-2-基或苯并噻唑-2-基; R3是C1-C8烷基，C4-C8环烷基或取代或未取代的苯基，其中取代基是卤素，烷氧基或三氟甲基; m为1-3的整数; n为1-5的整数; 或其药学上可接受的盐。该化合物可用作富含人血小板的血浆中ADP诱导的血小板聚集的抑制剂。

120. 发明授权

US5071866A Arylpyrazole derivatives as anti-platelet agents 失效
标题翻译：芳吡唑衍生物作为抗血小板剂
公开(公告)号：US5071866A
公开(公告)日：1991-12-10
申请号：US624822
申请日：1990-12-10
申请人： Nicholas A. Meanwell
发明人： Nicholas A. Meanwell
IPC分类号： C07D231/12 , C07D403/06 , C07D403/12
CPC分类号： C07D231/12 , C07D403/06 , C07D403/12
摘要： Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or phenyl, provided that R.sup.1 and R.sup.2 may not both be hydrogen;m is an integer from 3 to 9;n is an integer from 0 to 3 and the sum ofm+n is an integer from 5 to 12;Z is O, S, SO, SO.sub.2, --CH.dbd.CH-- or a direct bond;A is ##STR2## R.sup.3 is hydrogen or C.sub.1-6 alkyl; and R.sup.4 is hydrogen, C.sub.1-4 alkyl or methylsulfonyl;and pharmaceutically acceptable salts or hydrates thereof are novel inhibitors of adenosine diphosphate and collagen-induced aggregation of human platelet-rich plasma and are particularly useful as inhibitors of mammalian blood platelet aggregation.
摘要翻译：其中R 1和R 2各自独立地为氢或苯基，其中R 1和R 2不能均为氢; m为3〜9的整数; n为0〜3的整数，m + n的和为5〜12的整数。 Z是O，S，SO，SO 2，-CH = CH-或直接键; A是R 3是氢或C 1-6烷基; 且R 4为氢，C 1-4烷基或甲基磺酰基; 和其药学上可接受的盐或水合物是二磷酸腺苷和人血小板富集的胶原诱导的聚集的新型抑制剂，并且特别可用作哺乳动物血小板聚集的抑制剂。

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