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公开(公告)号：US08785478B2
公开(公告)日：2014-07-22
申请号：US13861325
申请日：2013-04-11
IPC分类号： A61K31/4427 , A61K31/427 , A61K31/416 , C07D401/02 , C07D417/02 , C07D231/56 , C07D417/04 , C07D403/12 , C07D401/14 , C07D401/04 , A61K38/08 , C07D405/14 , C07D405/12 , A61K31/706 , A61K31/4439 , A61K38/05 , A61K45/06
CPC分类号： C07D405/12 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/706 , A61K38/05 , A61K38/06 , A61K38/08 , A61K45/06 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/14 , C07D417/04 , A61K2300/00
摘要： The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
摘要翻译： 本发明涉及式（I）的病毒聚合酶抑制剂或其盐，N-氧化物，溶剂合物，水合物，外消旋物，对映体或异构体，其制备方法及其用于治疗黄病毒病毒感染如丙型肝炎病毒 （HCV）感染。
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![Substituted imidazo[1,2-α]pyrrolo[1,2-d]pyrazines for treating respiratory syncytial virus (RSV) infections](/abs-image/US/2013/12/10/US08604034B2/abs.jpg.150x150.jpg)
32.发明授权Substituted imidazo[1,2-α]pyrrolo[1,2-d]pyrazines for treating respiratory syncytial virus (RSV) infections 有权用于治疗呼吸道合胞病毒（RSV）感染的取代的咪唑并[1,2-α]吡咯并[1,2-d]吡嗪公开(公告)号：US08604034B2
公开(公告)日：2013-12-10
申请号：US13023473
申请日：2011-02-08
申请人： Jeffrey Peter Mitchell , Gary Pitt , Alistair George Draffan , Penelope Anne Mayes , Laura Andrau , Kelly Anderson
发明人： Jeffrey Peter Mitchell , Gary Pitt , Alistair George Draffan , Penelope Anne Mayes , Laura Andrau , Kelly Anderson
IPC分类号： A61K31/495
CPC分类号： C07D487/14 , A61K31/407 , A61K31/4162 , A61K31/4188 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D207/333 , C07D207/34 , C07D213/79 , C07D405/12
摘要： The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
摘要翻译： 本发明涉及其用于治疗病毒感染，特别是呼吸道合胞病毒（RSV）感染的其盐，异构体或前药的式（I）化合物。 本发明还涉及制备用于其制备的化合物和中间体的方法。
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公开(公告)号：US08546389B2
公开(公告)日：2013-10-01
申请号：US13278021
申请日：2011-10-20
申请人： Rosliana Halim , Michael Harding , Richard Hufton , Craig James Morton , Saba Jahangiri , Brett Raymond Pool , Tyrone Pieter Jeynes , Alistair George Draffan , Barbara Frey , Michael John Lilly
发明人： Rosliana Halim , Michael Harding , Richard Hufton , Craig James Morton , Saba Jahangiri , Brett Raymond Pool , Tyrone Pieter Jeynes , Alistair George Draffan , Barbara Frey , Michael John Lilly
IPC分类号： A61K31/5377 , A61K31/416 , A61K31/41 , A61K31/4178 , A61K31/4523 , A61K31/4427 , A61K31/497 , A61K31/427 , A61K31/422 , A61K31/501 , A61K31/4245 , C07D413/04 , C07D231/56 , C07D257/04 , C07D233/54 , C07D211/00 , C07D401/02 , C07D417/02 , C07D261/06 , C07D403/02 , C07D413/02 , C07D271/08
CPC分类号： C07D231/56 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04
摘要： The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:
摘要翻译： 本发明涉及式（I）的病毒聚合酶抑制剂，其盐，N-氧化物，溶剂合物，水合物，外消旋物，对映体或异构体，其制备方法及其在治疗黄病毒病毒感染如丙型肝炎病毒 （HCV）感染：
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公开(公告)号：US20130072520A2
公开(公告)日：2013-03-21
申请号：US13304748
申请日：2011-11-28
申请人： David BROWN , Ian COLLINS , Lloyd CZAPLEWSKI , David HAYDON
发明人： David BROWN , Ian COLLINS , Lloyd CZAPLEWSKI , David HAYDON
IPC分类号： A61K31/437 , A61K31/166 , C07D215/14 , A61K31/47 , C07C235/84 , A61K31/216 , C07D333/24 , A61K31/381 , C07D307/54 , A61K31/341 , C07C309/73 , A61K31/255 , C07C255/44 , A61K31/277 , C07D213/81 , A61K31/44 , C07D319/20 , A61K31/357 , C07D513/04 , A61P31/04 , C07D277/64 , C07D277/30 , A61K31/428 , A61K31/426 , A01P1/00 , A01N43/78 , A01N43/90 , A01N43/32 , A01N43/40 , A01N37/34 , A01N41/04 , A01N43/08 , A01N43/10 , A01N37/44 , A01N43/42 , A01N37/18 , C07C235/46
CPC分类号： C07C235/46 , A01N37/40 , A01N41/04 , A01N43/08 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/76 , A01N43/78 , A01N43/82 , A01N43/90 , A61K31/166 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4422 , A61K31/4523 , A61K31/4709 , C07C255/16 , C07C309/73 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/81 , C07D215/12 , C07D215/14 , C07D231/12 , C07D233/64 , C07D249/04 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/24 , C07D277/32 , C07D277/64 , C07D307/42 , C07D307/56 , C07D319/20 , C07D333/06 , C07D333/12 , C07D333/16 , C07D333/56 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ═C(R1)— or ═N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(═O)—, —O—(C═O)—, —C(═O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.
摘要翻译： 式（I）化合物具有抗菌活性：其中R表示氢或1,2或3个任选的取代基; W是≡C（R1） - 或=N-; R1是氢或任选的取代基，R 2是氢，甲基或氟; 或R 1和R 2一起为-CH 2 - ， - CH 2 CH 2 - ， - O-，或者在任一取向为-O-CH 2 - 或-OCH 2 CH 2 - ; R3是式 - （Alk1）m-（Z）p-（Alk2）nQ的基团，其中m，p和n独立地为0或1，条件是m，p和n中的至少一个为1，Z为 - （O） - ， - S（O 2） - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - （C = O） - ， - C（= O）-O-，或具有3至6个环原子的任选取代的二价单环碳环或杂环基; 或具有5至10个环原子的任选取代的二价双环杂环基; Alk1和Alk2是任选取代的C 1 -C 6亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基，其可以任选地被-O - ， - S - ， - S（O） - ， - S（ O，-N（CH 3） - 或-N（CH 2 CH 3） - ; 和Q是氢，卤素，腈或羟基或任选取代的具有3-6个环原子的单环碳环或杂环基; 或具有5〜10个环原子的任意取代的双环杂环基。
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公开(公告)号：US20120135998A1
公开(公告)日：2012-05-31
申请号：US13302975
申请日：2011-11-22
申请人： Penelope Anne Mayes , Jeffrey Peter Mitchell , Alistair George Draffan , Gary Robert William Pitt , Kelly Helen Anderson , Chin Yu Lim
发明人： Penelope Anne Mayes , Jeffrey Peter Mitchell , Alistair George Draffan , Gary Robert William Pitt , Kelly Helen Anderson , Chin Yu Lim
IPC分类号： A61K31/4985 , A61P11/00 , A61P31/14 , C07D471/14 , A61K31/4375
CPC分类号： C07D471/14
摘要： The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.
摘要翻译： 本发明涉及用于治疗病毒感染，特别是呼吸道合胞病毒（RSV）感染的式（I）化合物，外消旋物，异构体和/或盐。 本发明还涉及制备该化合物的方法。
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公开(公告)号：US20110212966A1
公开(公告)日：2011-09-01
申请号：US13100931
申请日：2011-05-04
IPC分类号： A61K31/53 , C07D413/14 , A61K31/501 , A61P31/16 , A61K31/454
CPC分类号： C07D417/14 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , Y02A50/463
摘要： This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
摘要翻译： 本发明涉及式I化合物及其药学上可接受的衍生物，包含这些化合物的药物组合物及其在哺乳动物中治疗微小RNA病毒感染的用途，以及可用于制备式I化合物的新型中间体。
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公开(公告)号：US07951955B2
公开(公告)日：2011-05-31
申请号：US12113718
申请日：2008-05-01
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/16
CPC分类号： C07D417/14 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , Y02A50/463
摘要： This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
摘要翻译： 本发明涉及式I化合物及其药学上可接受的衍生物，包含这些化合物的药物组合物及其在哺乳动物中治疗微小RNA病毒感染的用途，以及可用于制备式I化合物的新型中间体。
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公开(公告)号：US07829705B2
公开(公告)日：2010-11-09
申请号：US11559253
申请日：2006-11-13
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/4523 , A61K31/496 , A61K31/501 , A61P31/12
CPC分类号： C07D417/14 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , Y02A50/463
摘要： This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
摘要翻译： 本发明涉及式I化合物及其药学上可接受的衍生物，包含这些化合物的药物组合物及其在哺乳动物中治疗微小RNA病毒感染的用途，以及可用于制备式I化合物的新型中间体。
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公开(公告)号：US07598230B2
公开(公告)日：2009-10-06
申请号：US11818990
申请日：2007-06-14
申请人： Phillip D. Cook , Guangyi Wang , Thomas W. Bruice , Nicholas A. Boyle , Janet M. Leeds , Jennifer L. Brooks , Marija Prhavc , Maria Eugenia Ariza , Patrick C. Fagan , Yi Jin , Vivek K. Rajwanshi , Kathleen D. Tucker
发明人： Phillip D. Cook , Guangyi Wang , Thomas W. Bruice , Nicholas A. Boyle , Janet M. Leeds , Jennifer L. Brooks , Marija Prhavc , Maria Eugenia Ariza , Patrick C. Fagan , Yi Jin , Vivek K. Rajwanshi , Kathleen D. Tucker
IPC分类号： C07H19/10
摘要： The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.
摘要翻译： 本发明涉及核苷二磷酸模拟物和核苷三磷酸模拟物，其含有二磷酸酯或三磷酸酯部分模拟物和任选的糖修饰和/或碱基修饰。 本发明的核苷酸模拟物以药学上可接受的盐，药学上可接受的前药或药物制剂的形式可用作抗病毒，抗微生物剂和抗癌剂。 本发明提供了治疗病毒感染，微生物感染和增殖性疾病的方法。 本发明还涉及包含任选与其它药物活性剂组合的本发明化合物的药物组合物。
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公开(公告)号：US20070225358A1
公开(公告)日：2007-09-27
申请号：US11734394
申请日：2007-04-12
申请人： Betty JIN , Simon MacDonald , Darryl McConnell , Van Nguyen , Stephen Shanahan , Wen-Yang Wu
发明人： Betty JIN , Simon MacDonald , Darryl McConnell , Van Nguyen , Stephen Shanahan , Wen-Yang Wu
IPC分类号： A61K31/35
CPC分类号： A61K31/351 , A61K31/13 , A61K31/7056 , A61K38/00 , A61K45/06 , A61K47/54 , A61K47/55 , C07D309/28 , C07K5/06104 , A61K2300/00
摘要： The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2-C9 alkyl C3-8 cycloalkyl, C1-C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.
摘要翻译： 本发明涉及通式（I）的化合物; 其中R是氨基或胍基; R 2是乙酰基或三氟乙酰基; X是CONH，NHCO或O; n为2-6的整数; 且Y为C 2 -C 9烷基C 3-8环烷基，C 1 -C 3烷基， 4烷氧基烷基，氨基酸或二肽或其药学上可接受的衍生物，其制备方法，含有它们的药物制剂或其在预防或治疗病毒感染中的用途。
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