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1. 发明申请

WO2006037028A3 METHODS AND COMPOSITIONS FOR TREATING FLAVIVIRUSES, PESTIVIRUSES AND HEPACIVIRUS 审中-公开
公开(公告)号：WO2006037028A3
公开(公告)日：2006-04-06
申请号：PCT/US2005/034786
申请日：2005-09-26
申请人： IDENIX (CAYMAN) LIMITED , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , SOMMADOSSI, Jean-Pierre , GOSSELIN, Gilles , STORER, Richard , EGAN, James
发明人： SOMMADOSSI, Jean-Pierre , GOSSELIN, Gilles , STORER, Richard , EGAN, James
IPC分类号： A61K31/70 , C07H19/00 , C07H19/048
摘要： A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective flavivirus, pestivirus or hepacivirus treatment amount of a described base-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

2. 发明申请

WO0240021A3 METHODS FOR INHIBITING THE TRANSMISSION OF HIV USING TOPICALLY APPLIED SUBSTITUTED 6-BENZYL-4-OXOPYRIMIDINES 审中-公开
标题翻译：使用局部应用的取代的6-苄基-4-氧代嘧啶抑制HIV传播的方法
公开(公告)号：WO0240021A3
公开(公告)日：2002-08-22
申请号：PCT/US0145652
申请日：2001-11-19
申请人： NOVIRIO PHARMACEUTICALS LTD , UNIV CAGLIARI , SOMMADOSSI JEAN-PIERRE , LA COLLA PAULO , ARTICO MARINO , BRYANT MARTIN L
发明人： SOMMADOSSI JEAN-PIERRE , LA COLLA PAULO , ARTICO MARINO , BRYANT MARTIN L
IPC分类号： A61K9/00 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/513 , A61K45/06 , A61P31/18 , C07D239/47 , C07D239/52 , C07D239/56 , C07D403/04
CPC分类号： A61K31/381 , A61K9/0031 , A61K9/0034 , A61K9/1271 , A61K31/44 , A61K31/505 , A61K31/513 , A61K45/06 , C07D333/16 , C07D333/56 , C07D409/10 , C07D493/04 , A61K2300/00
摘要： A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor ("NNRTI")that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 uM. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).
摘要翻译：一种抑制HIV的性传播的方法，包括向人的皮肤或上皮组织局部施用包含能够抑制病毒复制的非核苷逆转录酶抑制剂（“NNRTI”）的组合物超过12,24或甚至36天，浓度甚至低于10μM。在一个实施方案中，NNRTI是二氢 - 烷氧基 - 苄基 - 氧代嘧啶（DABO）。

3. 发明申请

WO1997049717A1 3'-OXIMINO-2',3'-DIDEOXYNUCLEOSIDES AND DERIVATIVES OF THE SAME 审中-公开
标题翻译： 3'-氧亚氨基-2'，3'-二脱氧核苷酸及其衍生物
公开(公告)号：WO1997049717A1
公开(公告)日：1997-12-31
申请号：PCT/RU1997000201
申请日：1997-06-24
申请人： FEDOROV, Ivan Igorevich , GOSSELIN, Gilles , DE CLERCQ, Eric , BALZARINI, Jan , SOMMADOSSI, Jean-Pierre , IMBACH, Jean-Louis , KAZMINA, Ema Maximovna , ARZAMASTSEV, Alexandr Pavlovich , GURSKAYA, Galina Viktorovna , YASKO, Maxim Vladimirovich , FARAJ, Abdesslem
IPC分类号： C07H19/073
CPC分类号： C07H19/04 , Y02P20/55
摘要： The present invention relates to new 3'-oximino-2',3'-dideoxynucleoside derivatives corresponding to formula (I) where B is substituted or unsubstituted thymin-1-yl, uracyl-1-yl, cytosin-1-yl, adenin-9-yl or guanin-9-yl and R is C1-C6 alkyl or C1-C6 acyl. This invention may be used to produce substances of this class having an increased activity. The 3'-oximino-2',3'-dideoxynucleosides are synthesised from naturally occurring nucleosides that contain a 2-deoxyribofuranose as their hydrocarbon compound. The position 5' of said 2-deoxyribofuranose is protected by a monomethoxytrityl, dimethoxytrityl or tributyldimethylsilyl group. The hydroxyl group is then oxidised at position 3' in the keto-group using an oxidiser such as pyridine dichromate or a Dess-Martin reagent, and further oximised in situ (hydroxylamine hydrochloride in pyridine) before suppressing the protecting group at position 5', the yield ranging from 30 to 70 %. Virological tests showed that 3'-oximino-2',3'-dideoxynucleosides and more precisely 3'-oximino-2',3'-dideoxythymidine are active against the human immunodeficiency virus (HIV), the B hepatitis virus and the herpes simplex virus (HSV). These compounds show anti-HIV activity in cells deficient in thymidinekynase, as well as an activity against HSV strains deficient in thymidinekynase.
摘要翻译：本发明涉及对应于式（I）的新的3'-肟基-2'，3'-二脱氧核苷衍生物，其中B为取代或未取代的甲氨基-1-基，尿嘧啶-1-基，胞嘧啶-1-基，腺嘌呤 -9-基或guanin-9-基，R是C 1 -C 6烷基或C 1 -C 6酰基。本发明可用于产生具有增加活性的该类物质。 3'-肟基-2'，3'-二脱氧核苷由天然存在的含有2-脱氧呋喃核糖作为其烃化合物的核苷合成。所述2-脱氧呋喃核糖的位置5'由单甲氧基三苯甲基，二甲氧基三苯甲基或三丁基二甲基甲硅烷基保护。然后使用氧化剂如吡啶重铬酸盐或Dess-Martin试剂将羟基在酮基的3'位置进行氧化，并在抑制位置5'处的保护基之前，进一步进行原位氧化（吡啶中的盐酸羟胺）产量从30％到70％不等。病毒学检测显示，3'-肟基-2'，3'-二脱氧核苷和3'-肟基-2'，3'-二脱氧胸苷对人免疫缺陷病毒（HIV），B型肝炎病毒和单纯疱疹病毒病毒（HSV）。这些化合物在胸苷激酶缺乏的细胞中显示抗HIV活性，以及针对缺乏胸苷激酶的HSV毒株的活性。

4. 发明申请

WO1995007287A1 2' OR 3'-DEOXY AND 2'-DIDEOXY-'beta'-L-PENTAFURANONUCLEOSIDE COMPOUNDS, METHOD OF PREPARATION AND APPLICATION IN THERARY, ESPECIALLY AS ANTI-VIRAL AGENTS 审中-公开
标题翻译： 2'或3'-脱氧和2'-二脱氧-β-L-蓬特壬烷砜化合物，其制备方法及其应用，特别是作为抗病毒剂
公开(公告)号：WO1995007287A1
公开(公告)日：1995-03-16
申请号：PCT/FR1994001066
申请日：1994-09-09
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , GOSSELIN, Gilles , IMBACH, Jean-Louis , AUBERTIN, Anne-Marie , SOMMADOSSI, Jean-Pierre , SCHINAZI, Raymond, F.
发明人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
IPC分类号： C07H19/04
CPC分类号： C07D473/00 , C07D405/04 , C07H19/04
摘要： Method for the stereospecific preparation of 2' or 3' deoxy and 2', 3'-dideoxy- beta -L-pentafuanonucleoside compounds. 2' or 3' deoxy and 2', 3'-dideoxy- beta -L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of these compounds, and particularly 2', 3' dideoxy- beta -L-5-fluorocytidine, as drugs, and especially as anti-viral agents.
摘要翻译： 2'或3'脱氧和2'，3'-二脱氧-β-L-戊酮核苷化合物的立体特异性制备方法。还描述了2'或3'脱氧和2'，3'-二脱氧-β-L-呋喃核糖核苷化合物。最后，本发明涉及这些化合物，特别是2'，3'-二脱氧-β-1-L-5-氟胞嘧啶作为药物，特别是作为抗病毒剂的用途。

5. 发明申请

WO2005020884A3 NUCLEOSIDES FOR TREATMENT OF INFECTION BY CORONA VIRUSES, TOGA VIRUSES AND PICORNA VIRUSES 审中-公开
公开(公告)号：WO2005020884A3
公开(公告)日：2005-03-10
申请号：PCT/US2004/015395
申请日：2004-05-14
申请人： IDENIX (CAYMAN) LIMITED , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITA DEGLI STUDI DI CAGLIARI , SOMMADOSSI, Jean-Pierre , GOSSELIN, Gilles , LA COLLA, Paolo , STORER, Richard
发明人： SOMMADOSSI, Jean-Pierre , GOSSELIN, Gilles , LA COLLA, Paolo , STORER, Richard
IPC分类号： A61K31/70 , A61K31/665
摘要： This invention is in the area of methods and pharmaceutical compositions for treating a host, especially a human, infected with a coronavirus, togavirus or picornavirus, comprising administering to that host an effective amount of a compound described herein or its salt, ester or prodrug. The compound can be administered alone or in combination with another optionally substituted pentofuranonucleoside or in combination with another anti-coronavirus, anti-togavirus and/or anti-picornavirus agent.

6. 发明申请

WO2004046331A2 2'-BRANCHED NUCLEOSIDES AND FLAVIVIRIDAE MUTATION 审中-公开
标题翻译： 2分支核苷酸和FLAVIVIRIDAE突变
公开(公告)号：WO2004046331A2
公开(公告)日：2004-06-03
申请号：PCT/US0336714
申请日：2003-11-17
申请人： IDENIX CAYMAN LTD , UNIV CAGLIARI , SOMMADOSSI JEAN-PIERRE , LA COLLA PAOLO , STANDRING DAVID , BICHKO VADIM , QU LIN
发明人： SOMMADOSSI JEAN-PIERRE , LA COLLA PAOLO , STANDRING DAVID , BICHKO VADIM , QU LIN
IPC分类号： A61K31/7052 , A61K38/21 , A61K45/06 , C07H19/06 , C07H19/16 , C07K14/18 , C12Q1/70 , C12N
CPC分类号： A61K31/7072 , A61K31/7052 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K45/06 , C07H19/06 , C07H19/16 , C07K14/005 , C12N2770/24022 , C12N2770/24122 , C12N2770/24222 , C12Q1/04 , C12Q1/18 , C12Q1/701 , C12Q1/707 , C12Q2600/156 , C12Q2600/158 , G01N2333/186 , A61K2300/00
摘要： The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2'-branched nucleoside, or a pharmaceutically acceptable prodrug and/or salt thereof, to a human in need of therapy in combination or alternation with a drug that directly or indirectly induces a mutation in the viral genome at a location other than a mutation of a nucleotide that results in a change from serine to a different amino acid in the highly conserved consensus sequence, XRXSGXXXT, of domain B of the RNA polymerase region, or is associated with such a mutation. The invention also includes a method to detect a mutant strain of Flaviviridae and a method for its treatment.
摘要翻译：本发明公开了一种治疗黄病毒科感染的方法，其包括将2支支链核苷或其药学上可接受的前药和/或盐给予需要与药物组合或替代的药物，直接或间接地诱导病毒基因组中突变的位置，其不是导致在RNA聚合酶区域B的高度保守的共有序列XRXSGXXXT中从丝氨酸到不同氨基酸的变化的突变，或与这种突变有关。本发明还包括检测黄病毒科突变菌株的方法及其治疗方法。

7. 发明申请

WO2004014364A1 SUBSTITUTED PHENYLINDOLES FOR THE TREATMENT OF HIV 审中-公开
标题翻译：用于治疗艾滋病毒的替代苯乙醇
公开(公告)号：WO2004014364A1
公开(公告)日：2004-02-19
申请号：PCT/US2003/024957
申请日：2003-08-07
申请人： IDENIX (CAYMAN) LIMITED , UNIVERSITA DEGLI STUDI DI CAGLIARI , SOMMADOSSI, Jean-Pierre , LA COLLA, Paolo , ARTICO, Marino , STORER, Richard , MOUSSA, Adel, M.
发明人： SOMMADOSSI, Jean-Pierre , LA COLLA, Paolo , ARTICO, Marino , STORER, Richard , MOUSSA, Adel, M.
IPC分类号： A61K31/404
CPC分类号： C07D403/04 , C07D209/42 , C07D403/12
摘要： This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4' and 5', 5' and 6' or the 5' and 7' positions, optionally in combination with disubstitution at positions 3" and 5" on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF 3 , methoxy, CN, and NO 2 .
摘要翻译：本发明在可用于治疗HIV感染的苯基吲哚的区域中，特别是对抗HIV抗性菌株显示出显着活性的苯基吲哚。苯吲哚在吲哚官能团的苯并环上具有至少两个除氢以外的取代基，优选在4'和5'，5'和6'或5'和7'位置，任选地与3位的取代基组合 “和5”，化合物的吲哚基上的位置-2的含羧酰胺的部分。甲基是在苯环上取代的优选基团。吲哚官能团的苯并环的优选取代基包括但不限于氯，氟，溴，碘，CF 3，甲氧基，CN和NO 2。

8. 发明申请

WO0191737A3 METHODS FOR TREATING HEPATITIS DELTA VIRUS INFECTION WITH BETA-L-2' DEOXY-NUCLEOSIDES 审中-公开
标题翻译：用BETA-L-2'脱氧核糖核酸治疗肝炎病毒感染的方法
公开(公告)号：WO0191737A3
公开(公告)日：2002-05-30
申请号：PCT/US0117301
申请日：2001-05-29
申请人： NOVIRIO PHARMACEUTICALS LTD , SOMMADOSSI JEAN PIERRE , BRYANT MARTIN L
发明人： SOMMADOSSI JEAN-PIERRE , BRYANT MARTIN L
IPC分类号： C07H19/073 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/00 , A61K45/06 , A61P31/12 , A61P31/20 , C07H19/173 , A61K31/706 , A61K31/70 , A61K31/7064
CPC分类号： A61K45/06 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , Y10S514/894 , A61K2300/00
摘要： A method and composition for treating a host infected with hepatitis D comprising administering an effective hepatitis D treatment amount of a described 2'-deoxy- beta -L-erythropentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译：用于治疗感染了丙型肝炎的宿主的方法和组合物，其包括施用有效的丙型肝炎治疗量的所述2'-脱氧-β-L-赤式呋喃核苷或其药学上可接受的盐或前药。

9. 发明申请

WO0190121A3 METHODS AND COMPOSITIONS FOR TREATING HEPATITIS C VIRUS 审中-公开
标题翻译：治疗乙型肝炎病毒的方法和组合物
公开(公告)号：WO0190121A3
公开(公告)日：2002-05-02
申请号：PCT/US0116671
申请日：2001-05-23
申请人： NOVIRIO PHARMACEUTICALS LTD , UNIV CAGLIARI , SOMMADOSSI JEAN PIERRE , LACOLLA PAULO
发明人： SOMMADOSSI JEAN-PIERRE , LACOLLA PAULO
IPC分类号： C07D473/18 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P1/16 , A61P31/12 , A61P31/14 , C07D405/04 , C07D473/30 , C07D473/34 , C07H19/04 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20
CPC分类号： A61K31/708 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21 , A61K45/06 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , G03C1/0051
摘要： A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1', 2' or 3'-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
摘要翻译：提供用于治疗感染丙型肝炎的宿主的方法和组合物，其包括施用有效的丙型肝炎治疗量的所述1'，2'或3'-修饰的核苷或其药学上可接受的盐或前药。

10. 发明申请

WO2008082602A2 COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF LIVER DISORDERS 审中-公开
标题翻译：用于治疗肝病的化合物和药物组合物
公开(公告)号：WO2008082602A2
公开(公告)日：2008-07-10
申请号：PCT/US2007/026409
申请日：2007-12-28
申请人： IDENIX PHARMACEUTICALS, INC. , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , L'UNIVERSITE MONTPELLIER II , SOMMADOSSI, Jean-pierre , GOSSELIN, Gilles , PIERRA, Claire , PERIGAUD, Christian , PEYROTTES, Suzanne
发明人： SOMMADOSSI, Jean-pierre , GOSSELIN, Gilles , PIERRA, Claire , PERIGAUD, Christian , PEYROTTES, Suzanne
IPC分类号： A61K31/664
CPC分类号： C07H17/02 , A61K31/675 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07F9/65586 , C07F9/65616 , C07H19/00
摘要： Provided herein are compounds, compositions and methods for the treatment of liver disorders, including liver cancer and metabolic diseases, such as diabetes, hyperlipidemia, atherosclerosis, and obesity. Specifically, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents.
摘要翻译：本文提供了用于治疗肝病的化合物，组合物和方法，所述肝病包括肝癌和代谢疾病，例如糖尿病，高脂血症，动脉粥样硬化和肥胖症。具体而言，公开了核苷衍生物的化合物和组合物，其可以单独或与其他抗癌剂联合给药。

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