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41. 发明公开

EP1778702A2 ANTIVIRAL COMPOUNDS 有权
标题翻译：抗病毒化合物
公开(公告)号：EP1778702A2
公开(公告)日：2007-05-02
申请号：EP05791144.8
申请日：2005-07-18
申请人： GILEAD SCIENCES, INC.
发明人： CHAUDHARY, Kleem , FLEURY, Melissa , KIM, Choung, U. , MCMURTRIE, Darren, J. , SHENG, Xiaoning C.
IPC分类号： C07F9/141 , C07D207/08 , A61K31/662 , A61P31/12
CPC分类号： C07K5/0827 , A61K38/00 , C07F9/5727 , C07F9/65583 , C07K5/06191 , C07K5/0808
摘要： The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及磷取代的抗病毒抑制化合物，含有这些化合物的组合物，以及包括给予这些化合物的治疗方法，以及可用于制备这些化合物的方法和中间体。

42. 发明公开

EP1509537A2 CELLULAR ACCUMULATION OF PHOSPHONATE ANALOGS OF HIV PROTEASE INHIBITOR COMPOUNDS AND THE COMPOUNDS AS SUCH 有权转让
标题翻译：富集在单元格中膦酸酯类似物的HIV蛋白酶抑制剂化合物和接线SELF
公开(公告)号：EP1509537A2
公开(公告)日：2005-03-02
申请号：EP03747326.1
申请日：2003-04-25
申请人： GILEAD SCIENCES, INC.
发明人： ARIMILLI, Murty, N. , BECKER, Mark, M. , BRYANT, Clifford , CHEN, James, M. , CHEN, Xiaowu , DASTGAH, Azar , FARDIS, Maria , HE, Gong-Xin , JIN, Haolun , KIM, Choung, U. , LEE, William, A. , LEE, Christopher, P. , LIN, Kuei-Ying , LIU, Hongtao , MACKMAN, Richard, L. , MITCHELL, Michael, L. , NELSON, Peter, H. , PYUN, Hyung-Jung , ROWE, Tanisha, D. , SWAMINATHAN, Sundaramoorthi , TARIO, James, D. , ZHANG, Lijun , SPARACINO, Mark , WANG, Jianying , WILLIAMS, Matthew, A , XU, Lianhong , YANG, Zheng-Yu , YU, Richard, H. , ZHANG, Jiancun
IPC分类号： C07F9/40 , C07F9/02 , C07F9/38
CPC分类号： A61K31/66 , A61K31/675 , C07D213/75 , C07D213/85 , C07D231/12 , C07D231/20 , C07D233/42 , C07D239/49 , C07D239/80 , C07D243/04 , C07D265/18 , C07D307/68 , C07D401/06 , C07D403/06 , C07D471/14 , C07D491/04 , C07F9/4006 , C07F9/582 , C07F9/588 , C07F9/645 , C07F9/65061 , C07F9/65062 , C07F9/65067 , C07F9/650911 , C07F9/650917 , C07F9/650947 , C07F9/65121 , C07F9/65122 , C07F9/65127 , C07F9/65128 , C07F9/65335 , C07F9/65515 , C07F9/65583 , C07F9/6561 , C12N9/16 , C12Q1/18 , C12Q1/37 , C12Q1/44 , C40B40/04 , G01N33/5038 , G01N2333/16 , G01N2500/04
摘要： Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.

43. 发明授权

EP0920410B1 PREPARATION OF CYCLOHEXENE CARBOXYLATE DERIVATIVES 失效
标题翻译：用于生产环己烯羧酸酯衍生物
公开(公告)号：EP0920410B1
公开(公告)日：2002-03-27
申请号：EP97939508.4
申请日：1997-08-22
申请人： GILEAD SCIENCES, INC.
发明人： KENT, Kenneth, M. , KIM, Choung, U. , MCGEE, Lawrence, R. , MUNGER, John, D. , PRISBE, Ernest, J. , POSTICH, Michael, J. , ROHLOFF, John, C. , KELLY, Daphne, E. , WILLIAMS, Matthew, A. , ZHANG, Lijun
IPC分类号： C07C227/08 , C07C247/14 , C07D317/46 , C07D203/26 , C07D303/40 , C07F7/18 , C07C227/16
CPC分类号： C07D203/26 , C07C227/08 , C07C2601/16 , C07D303/40 , C07D317/46 , Y02P20/55
摘要： The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.

44. 发明公开

EP0915894A1 NUCLEOTIDE ANALOGS 有权
标题翻译： NUKLEOTID，类比
公开(公告)号：EP0915894A1
公开(公告)日：1999-05-19
申请号：EP97936257.0
申请日：1997-07-25
申请人： GILEAD SCIENCES, INC.
发明人： ARIMILLI, Murty, N. , CUNDY, Kenneth, C. , DOUGHERTY, Joseph, P. , KIM, Choung, U. , OLIYAI, Reza , STELLA, Valentino, J.
IPC分类号： A61K31 , A61P31 , C07F9
CPC分类号： C07F9/65121 , C07F9/65616
摘要： Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R2)2OC(O)X(R)a, wherein R2 independently is H, C¿1?-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR?3¿ in which R3 is C1-C12 alkyl; X is N or O; R is independently H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, -O-, -N=, -NR?4-, -N(R4)¿2- or OR3, R4 independently is -H or C¿1?-C8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR?3¿. The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis. Embodiments are particularly useful when administered orally.
摘要翻译：本发明涉及下式（1a）中的化合物或药学上可接受的盐，互变异构体或溶剂化物，其中每个取代基的定义如权利要求所示，本发明还涉及其制备方法，以及该化合物在制备药物中的用途用于治愈病毒感染。

45. 发明公开

EP0789695A2 THIEPANE COMPOUNDS INHIBITING AND DETECTING HIV PROTEASE 失效
标题翻译： THIEPANE于抑制和HIV蛋白酶的检测
公开(公告)号：EP0789695A2
公开(公告)日：1997-08-20
申请号：EP95940672.0
申请日：1995-11-03
申请人： GILEAD SCIENCES, INC.
发明人： BISCHOFBERGER, Norbert, W. , KIM, Choung, U. , KRAWCZYK, Steven, H. , MCGEE, Lawrence, R. , POSTICH, Michael J., Apartment 109 , YANG, Wenjin
IPC分类号： A61K31 , A61P31 , A61P43 , C07D337 , C07D409 , C07D417 , C07D495
CPC分类号： C07D495/04 , C07D337/04
摘要： Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositons are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.

46. 发明授权

EP2268642B1 1' -SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT 有权
标题翻译： 1“取代的碳代核苷类似物FOR抗病毒治疗
公开(公告)号：EP2268642B1
公开(公告)日：2015-02-25
申请号：EP09734175.4
申请日：2009-04-22
申请人： Gilead Sciences, Inc.
发明人： BUTLER, Thomas , CHO, Aesop , KIM, Choung, U. , SAUNDERS, Oliver, L. , ZHANG, Lijun , PARRISH, Jay
IPC分类号： C07D487/04 , A61K31/395 , A61K31/41 , A61K31/4188 , C07H19/23 , A61K31/7052 , A61P31/12
CPC分类号： C07H19/23 , C07D487/04

47. 发明授权

EP2396340B1 CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT 有权
标题翻译：卡巴 - 核苷类似物用于抗病毒治疗
公开(公告)号：EP2396340B1
公开(公告)日：2013-12-18
申请号：EP10704068.5
申请日：2010-02-09
申请人： Gilead Sciences, Inc.
发明人： BUTLER, Thomas , CHO, Aesop , KIM, Choung, U. , XU, Jie
IPC分类号： C07H19/24 , A61K31/7064 , A61P31/14
CPC分类号： C07D495/04
摘要： Provided are thieno[3,4-d]pyrimidin-7-yl and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.
摘要翻译：提供了噻吩并[3,4-d]嘧啶-7-基和呋喃并[3,4-d]嘧啶-7-基核糖苷，核苷磷酸酯及其前药，以及中间体和制备方法。所提供的化合物，组合物和方法可用于治疗黄病毒科病毒感染。

48. 发明授权

EP2480559B1 PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 1'-CYANO-CARBANUCLEOSIDE ANALOGS 有权
标题翻译：过程和中间产物1'-取代的碳代核苷类似物的制造
公开(公告)号：EP2480559B1
公开(公告)日：2013-07-03
申请号：EP10757699.3
申请日：2010-09-20
申请人： Gilead Sciences, Inc.
发明人： BUTLER, Thomas , CHO, Aesop , GRAETZ, Benjamin, R. , KIM, Choung, U. , METOBO, Samuel, E. , SAUNDERS, Oliver, L. , WALTMAN, Andrew, W. , XU, Jie , ZHANG, Lijun
IPC分类号： C07H1/00 , C07H19/23
CPC分类号： C07H1/00 , A61K31/7052 , A61K31/7056 , A61K31/706 , C07H19/23
摘要： Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,24][1,2,4]triazinyl heterocycles of Formula I.

49. 发明公开

EP2480552A1 2' -FLUORO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT 有权
标题翻译： FOR抗病毒治疗2“-FLUORSUBSTITUIERTE碳代核苷类似物
公开(公告)号：EP2480552A1
公开(公告)日：2012-08-01
申请号：EP10763083.2
申请日：2010-09-20
申请人： Gilead Sciences, Inc.
发明人： CHO, Aesop , KIM, Choung, U. , METOBO, Samuel, E. , RAY, Adrian, S. , XU, Jie
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo(1,2-f][ 1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2' position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.

50. 发明公开

EP2396340A1 CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT 有权
标题翻译：卡巴 - 核苷类似物用于抗病毒治疗
公开(公告)号：EP2396340A1
公开(公告)日：2011-12-21
申请号：EP10704068.5
申请日：2010-02-09
申请人： Gilead Sciences, Inc.
发明人： BUTLER, Thomas , CHO, Aesop , KIM, Choung, U. , XU, Jie
IPC分类号： C07H19/24 , A61K31/7064 , A61P31/14
CPC分类号： C07D495/04
摘要： Provided are thieno[3,4-d]pyrimidin-7-yI and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful for the treatment of
Flaviviridae virus infections.
摘要翻译：提供了噻吩并[3,4-d]嘧啶-7-基和呋喃并[3,4-d]嘧啶-7-基核糖苷，核苷磷酸酯及其前药以及中间体和制备方法。所提供的化合物，组合物和方法可用于治疗黄病毒科病毒感染。

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