N4-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine - CAS号 140859-16-1

物化性质

密度：

1.23±0.1 g/cm3(Predicted)

计算性质

辛醇/水分配系数(LogP)：

3.62
重原子数：

35
可旋转键数：

6
环数：

3.0
sp3杂化的碳原子比例：

0.74
拓扑面积：

116
氢给体数：

1
氢受体数：

7

上下游信息

上游原料

中文名称	英文名称	CAS号	化学式	分子量
N-乙酰基-3',5'-O-[1,1,3,3-四(异丙基)-1,3-二硅氧烷二基]胞苷	N4-acetyl-3',5'-O-(tetraisopropyldisiloxane-1,3-diyl)cytidine	85335-73-5	C₂₃H₄₁N₃O₇Si₂	527.765
(+)-3’,5’-O-(1,1,3,3-四异丙基-1,3-二硅氧烷)胞苷	3',5'-O-[(1,1,3,3-tetraisopropyl)-1,3-disiloxanediyl]cytidine	69304-42-3	C₂₁H₃₉N₃O₆Si₂	485.728
胞苷	CYTIDINE	65-46-3	C₉H₁₃N₃O₅	243.219
尿嘧啶核苷	uridine	58-96-8	C₉H₁₂N₂O₆	244.204

下游产品

中文名称	英文名称	CAS号	化学式	分子量
——	N-[1-[(6aR,8R,9aS)-9-methylidene-2,2,4,4-tetra(propan-2-yl)-6a,9a-dihydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	170112-37-5	C₂₄H₄₁N₃O₆Si₂	523.777
——	N-[1-[(6aR,8R,9R,9aS)-9-cyano-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403250-61-2	C₂₅H₄₂N₄O₆Si₂	550.803
——	N-[1-[(2R,3R,4S,5R)-3-cyano-4-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1491025-66-1	C₂₅H₄₄N₄O₇Si₂	568.818
——	N-[1-[(6aR,8R,9R,9aR)-9-methyl-9-methylsulfanyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-55-7	C₂₅H₄₅N₃O₆SSi₂	571.886
——	N-[1-[(6aR,8R,9R,9aS)-9-azido-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-53-5	C₂₄H₄₂N₆O₆Si₂	566.805
——	1-[(6aR,8R,9R,9aS)-9-amino-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-67-1	C₂₂H₄₂N₄O₅Si₂	498.77
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-5-(hydroxymethyl)-3-methyloxolane-3-carbonitrile	1491025-69-4	C₂₃H₄₂N₄O₆Si₂	526.781
——	1-[(6aR,8R,9R,9aR)-9-chloro-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-59-1	C₂₂H₄₀ClN₃O₅Si₂	518.201
——	N-[1-[(6aR,8R,9R,9aR)-9-methyl-9-methylsulfonyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-62-6	C₂₅H₄₅N₃O₈SSi₂	603.885
——	1-[(6aR,8R,9R,9aS)-9-azido-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-66-0	C₂₂H₄₀N₆O₅Si₂	524.768
——	N-[(6aR,8R,9R,9aS)-8-(4-amino-2-oxopyrimidin-1-yl)-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-9-yl]acetamide	1403249-68-2	C₂₄H₄₄N₄O₆Si₂	540.808
——	N-[1-[(6aR,8R,9R,9aS)-9-methyl-2,2,4,4-tetra(propan-2-yl)-9-(triazol-1-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-64-8	C₂₆H₄₄N₆O₆Si₂	592.843
——	2-methylpropyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1491026-66-4	C₃₆H₆₀N₅O₁₀PSi₂	810.045
——	N-[1-[(2R,3S,4R,5R)-3-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1610022-46-2	C₁₃H₁₅N₃O₆	309.279
——	N⁴-acetyl-1-<2-C-cyano-2-deoxy-5-O-(dimethoxytrityl)-β-D-arabinofuranosyl>cytosine	140859-05-8	C₃₃H₃₂N₄O₇	596.64
——	N⁴-acetyl-1-(2-C-cyano-2-deoxy-β-D-arabinofuranosyl)cytosine	135598-72-0	C₁₂H₁₄N₄O₅	294.267
——	[(2R,3S,4R,5R)-4-azido-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-89-3	C₃₀H₄₂N₇O₁₀P	691.678
——	N-[1-[(2R,3R,4S,5R)-3-cyano-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1491021-51-2	C₁₃H₁₆N₄O₅	308.294
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-azido-3-hydroxy-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1605283-90-6	C₂₆H₃₆N₇O₉P	621.587
——	N-[1-[(2R,3R,4S,5R)-3-azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1403567-97-4	C₁₂H₁₆N₆O₅	324.296
——	[(2R,3S,4R,5R)-4-cyano-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-84-8	C₃₁H₄₂N₅O₁₀P	675.676
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-cyano-3-hydroxy-4-methyl-5-[2-oxo-4-(2-propylpentanoylamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1605283-80-4	C₃₁H₄₄N₅O₉P	661.692
——	methyl (2S)-2-[[[(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyl-4-methylsulfanyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403249-81-9	C₂₁H₂₉N₄O₈PS	528.523
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-4-methyl-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-86-0	C₂₆H₃₆N₇O₉P	621.587
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403574-71-9	C₂₂H₃₀N₇O₈P	551.496
——	methyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403568-00-2	C₂₀H₂₆N₇O₈P	523.442
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-amino-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403250-92-9	C₂₂H₃₂N₅O₈P	525.499
——	butyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-naphthalen-1-yloxyphosphoryl]amino]propanoate	1491021-88-5	C₂₈H₃₄N₅O₈P	599.58
——	methyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyl-4-(triazol-1-yl)oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403249-80-8	C₂₂H₂₈N₇O₈P	549.48
——	2-methylpropyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1491026-71-1	C₂₄H₃₂N₅O₈P	549.521
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-4-methyl-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-propylpentanoate	1605283-78-0	C₃₁H₄₄N₅O₉P	661.692
——	1-[(4aR,6R,7R,7aS)-7-azido-7-methyl-2-oxo-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinin-6-yl]-4-aminopyrimidin-2-one	1403250-40-7	C₁₃H₁₉N₆O₆P	386.304
——	4-amino-1-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-methylsulfonyloxolan-2-yl]pyrimidin-2-one	1403249-63-7	C₁₁H₁₇N₃O₆S	319.338
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methyl (2-chlorophenyl) propan-2-yl phosphate	1403250-39-4	C₁₉H₂₄ClN₆O₇P	514.862
——	1-[(4aR,6R,7R,7aS)-7-amino-7-methyl-2-oxo-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinin-6-yl]-4-aminopyrimidin-2-one	1403250-41-8	C₁₃H₂₁N₄O₆P	360.307
——	N-[(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-3-yl]acetamide	1403249-69-3	C₁₂H₁₈N₄O₅	298.299
——	4-amino-1-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-methylsulfanyloxolan-2-yl]pyrimidin-2-one	1403249-56-8	C₁₁H₁₇N₃O₄S	287.34
——	4-amino-1-[(2R,3R,4S,5R)-3-azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one	1403249-54-6	C₁₀H₁₄N₆O₄	282.259
——	(4aR,6R,7R,7aS)-6-(4-amino-2-oxopyrimidin-1-yl)-7-methyl-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinine-7-carbonitrile	1491023-16-5	C₁₄H₁₉N₄O₅P	354.302
——	N⁴-acetyl-2'-C-cyano-2',3'-didehydro-2',3'-dideoxycytidine	140858-97-5	C₁₂H₁₂N₄O₄	276.252
——	4-amino-1-[(2R,3R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-(triazol-1-yl)oxolan-2-yl]pyrimidin-2-one	1403249-65-9	C₁₂H₁₆N₆O₄	308.297
——	4-amino-1-[(2R,3R,4S,5R)-3-amino-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one	1403249-61-5	C₁₀H₁₆N₄O₄	256.261
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolane-3-carboxamide	1403250-62-3	C₁₁H₁₆N₄O₅	284.272
——	[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1491023-69-8	C₁₁H₁₇N₄O₁₃P₃	506.196
4-氨基-1-(2-氰基-2-脱氧-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮	1-(2-cyano-2-deoxy-beta-D-arabinofuranosyl)cytosine	135598-68-4	C₁₀H₁₂N₄O₄	252.23
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolane-3-carbonitrile	1491021-53-4	C₁₁H₁₄N₄O₄	266.257

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反应信息

作为反应物：

描述：

N⁴-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine 在 Carreira’s cobalt catalyst 对甲苯磺酰叠氮、双(三甲基硅烷基)氨基钾作用下，以四氢呋喃为溶剂，反应 23.94h，生成 N-[1-[(6aR,8R,9R,9aS)-9-methyl-2,2,4,4-tetra(propan-2-yl)-9-(triazol-1-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide

参考文献：

名称：

[EN] 2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
[FR] DÉRIVÉS DE NUCLÉOSIDE 2'-SUBSTITUÉS ET PROCÉDÉS D'UTILISATION DE CEUX-CI POUR LE TRAITEMENT DE MALADIES VIRALES

摘要：

本发明涉及式(I)的2'-取代核苷衍生物及其药学上可接受的盐，其中A、B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-取代核苷衍生物的组合物，以及使用这些2'-取代核苷衍生物治疗或预防患者HCV感染的方法。

公开号：

WO2012142085A1
作为产物：

描述：

胞苷在吡啶、戴斯-马丁氧化剂作用下，以乙醇、二氯甲烷为溶剂，反应 33.0h，生成 N⁴-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine

参考文献：

名称：

[EN] 2'-METHYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
[FR] DÉRIVÉS DE NUCLÉOSIDES 2'-MÉTHYLE SUBSTITUÉS ET LEURS PROCÉDÉS D'UTILISATION DANS LE TRAITEMENT DE MALADIES VIRALES

摘要：

本发明涉及式(I)的2'-甲基取代核苷衍生物及其药学上可接受的盐，其中R、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-甲基取代核苷衍生物的组合物，以及使用这些2'-甲基取代核苷衍生物治疗或预防患者HCV感染的方法。

公开号：

WO2014062596A1

点击查看最新优质反应信息

文献信息

2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

申请人：Girijavallabhan Vinay

公开号：US20140206640A1

公开（公告）日：2014-07-24

The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及式(I)的2'-叠氮基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-叠氮基取代核苷衍生物的组合物，以及使用这些2'-叠氮基取代核苷衍生物治疗或预防患者HCV感染的方法。
2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES

申请人：Girijavallabhan Vinay

公开号：US20140161770A1

公开（公告）日：2014-06-12

The present invention relates to 2′-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Cyano Substituted Nucleoside Derivative, and methods of using the 2′-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及式(I)的2'-氰基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-氰基取代核苷衍生物的组合物，以及使用这些2'-氰基取代核苷衍生物治疗或预防患者HCV感染的方法。
[EN] PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHEIS OF 2'-CYANO-2'-DEOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE [FR] PRÉPARATION D'INTERMÉDIAIRES UTILES DANS LA SYNTHÈSE DE 2'-CYANO-2'-DÉSOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE

申请人：CYCLACEL LTD

公开号：WO2009136158A1

公开（公告）日：2009-11-12

The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2'; (ii) converting said compound of formula 682-2' into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.

本发明涉及一种制备式682-4化合物的方法，该方法包括以下步骤：(i)将式682-1化合物转化为式682-2'化合物；(ii)将所述式682-2'化合物转化为式682-3化合物；以及(iii)将所述式682-3化合物转化为式682-4化合物。该发明的进一步方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯莫呋核苷的用途，这是一种嘧啶核苷，对治疗和/或预防癌症具有治疗作用。
[EN] INTERMEDIATE AND PROCESSES INVOLVED IN THE PREPARATION OF 2 ' -CYANO-2 ' -DE0XY-N4-PALMIT0YL-1-BETA-ARABIN0FURAN0SYLCYTOSINE [FR] INTERMÉDIAIRE ET PROCÉDÉS ASSOCIÉS À LA PRÉPARATION DE 2'-CYANO-2'-DÉSOXY-N4-PALMITOYL-1-BÊTA-ARABINOFURANOSYLCYTOSINE

申请人：CYCLACEL LTD

公开号：WO2009136162A1

公开（公告）日：2009-11-12

The present invention relates to a process for preparing a compound of formula (682-6'), said process comprising the steps of: formula (682-4), (682-5), (682-6'): (i) converting a compound of formula (682-4) into a compound of formula (682-5); and (ii) converting said compound of formula (682-5) into a compound of formula (682- 6'). Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4-palmitoyl-l-β-D-arabinofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.

本发明涉及一种制备式（682-6'）化合物的方法，该方法包括以下步骤：式（682-4）、（682-5）、（682-6'）：（i）将式（682-4）化合物转化为式（682-5）化合物；以及（ii）将所述式（682-5）化合物转化为式（682-6'）化合物。该发明的进一步方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯呋喃核苷胞嘧啶中的应用，该核苷是治疗和/或预防癌症中具有治疗作用的。
[EN] 2 -ALKYNYL SUBSTITUTED NUCLEOSIDE DERIVATIVES FOR TREATING VIRAL DISEASES [FR] DÉRIVÉS DE NUCLÉOSIDE À SUBSTITUTION ALKYNYLE EN POSITION 2 POUR LE TRAITEMENT DE MALADIES VIRALES

申请人：MERCK SHARP & DOHME

公开号：WO2014078463A1

公开（公告）日：2014-05-22

The present invention relates to 2'-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2'-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及具有以下结构式(I)的2'-炔基取代核苷衍生物及其药用可接受的盐，其中B、X、R1、R2、R3和R4如本文所定义。本发明还涉及包含至少一种2'-炔基取代核苷衍生物的组合物，以及使用这些2'-炔基取代核苷衍生物治疗或预防患者HCV感染的方法。

N⁴-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine | 140859-16-1

分子结构分类

物化性质

计算性质

上下游信息

反应信息

文献信息

同类化合物

相关结构分类

热门分子

N4-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine | 140859-16-1

分子结构分类

物化性质

计算性质

上下游信息

反应信息

文献信息

同类化合物

相关结构分类

热门分子

N⁴-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine | 140859-16-1