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1. 发明申请

WO2007006707A1 1- [2' , 3' -DIDEOXY-3' C- (HYDROXYMETHYL) - BETA-D-ERYTHRO-PENTOFURANOSYL] CYTOSINE DERIVATIVES AS HIV INHIBITORS 审中-公开
标题翻译：作为艾滋病毒抑制剂的1- [2'，3'-二氧代-3'C-（羟甲基） - β-D-呋喃基 - 戊氧羰基]胞嘧啶衍生物
公开(公告)号：WO2007006707A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063919
申请日：2006-07-05
申请人： MEDIVIR AB , ZHOU, Xiao-Xiong , SAHLBERG, Christer
发明人： ZHOU, Xiao-Xiong , SAHLBERG, Christer
IPC分类号： C07D493/04 , A61K31/513 , A61P31/18
CPC分类号： C07D493/04
摘要： Compounds of the formula (I) wherein: R 1 is independently H 1 -OR 3 , -NHR 4 ; C 1 -C 4 alkyl; or, when n is 2, adjacent R 1 together define an olefin ic bond; R 2 is H; or when the gem R 1 is C 1 -C 4 alkyl, that R 2 may also be C 1 -C 4 alkyl; or when the gem R 1 is -OR 3 , that R 2 may also be -C(=O)OH or a pharmaceutically acceptable ester thereof; R 3 is independently H, or a pharmaceutically acceptable ester thereof; R 4 is independently H or a pharmaceutically acceptable amide thereof; R 5 and R6 are H or an amine prodrug moiety n is 1 , 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
摘要翻译：式（I）的化合物其中：R 1独立地是H 1 - ， - 3， - NHR 4， ; C 1 -C 4烷基; 或者当n为2时，相邻的R 1一起限定了烯烃键; R 2是H; 或者当R 1是C 1 -C 4烷基时，R 2也可以是C 1 -C 4烷基， C 1 -C 4烷基; 或当Gem R 1为-OR 3时，R 2还可以是-C（= O）OH或药学上可接受的酯物; R 3独立地为H或其药学上可接受的酯; R 4独立地是H或其药学上可接受的酰胺; R 5和R 6是H或胺前体药物部分n是1,2或3; 及其药学上可接受的盐; 在治疗或预防艾滋病毒方面具有实用价值，特别是逆转录酶突变体，其允许通过ATP或焦磷酸盐介导的切除从核心DNA链上切除核苷或磷酸核苷酸。

2. 发明申请

WO2005066180A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2005066180A1
公开(公告)日：2005-07-21
申请号：PCT/GB2005/050003
申请日：2005-01-06
申请人： MEDIVIR AB , NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
发明人： NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
IPC分类号： A61K31/407 , C07D491/04
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula (II) wherein one of R 1 and R 2 is halo and the other is H or halo; R 3 is C 1 -C 4 straight or branched chain, optionally fluorinated, alkyl; R 4 is H; or R 3 together with R 4 and the adjoining backbone carbon defines: a spiro-C 5 -C 7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl; or optionally bridged with a methylene group; or a C 4 -C 6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O) 2 ; where Ra is H, C 1 -C 4 alkyl or CH 3 C(=O); R 5 is independently selected from H or methyl; E is -C(=O)-, -S(=O) m -, -NR 5 S(=O) m -, -NR 5 C(=O)-, -OC(=O)-, R 6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：其中R 1和R 2之一为卤素且另一个为H或卤素的式（II）化合物; R 3是C 1 -C 4直链或支链，任选氟化的烷基; R 4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R 5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O） - ，R 6是稳定的，任选取代的单环或双环碳环或hetorocycle; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

3. 发明申请

WO1997030051A1 ACYCLIC NUCLEOSIDE DERIVATIVES 审中-公开
公开(公告)号：WO1997030051A1
公开(公告)日：1997-08-21
申请号：PCT/SE1997000241
申请日：1997-02-14
申请人： MEDIVIR AB
发明人： MEDIVIR AB , ENGELHARDT, Per , HÖGBERG, Marita , ZHOU, Xiao-Xiong , LINDBORG, Björn , JOHANSSON, Nils, Gunnar
IPC分类号： C07D473/18
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： Compounds of formula (I) where one of R1 and R2 is -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2; the other of R1 and R2 is -C(=O)C3-C21 saturated or monounsaturated, optionally substituted alkyl; and R3 is OH or H; and pharmaceutically acceptable salts thereof have utility as enhanced bioavailability antivirals against herpes and retroviral infections.
摘要翻译：其中R 1和R 2中的一个是-C（O）CH（CH（CH 3）2）NH 2或-C（O）CH（CH（CH 3）CH 2 CH 3）NH 2; R 1和R 2中的另一个是-C（= O）C 3 -C 21饱和或单不饱和，任选取代的烷基; 并且R 3是OH或H; 其药学上可接受的盐具有用于抗疱疹和逆转录病毒感染的增强的生物利用度抗病毒剂的效用。

4. 发明申请

WO1997030052A1 SYNTHESIS OF ACYCLIC NUCLEOSIDES 审中-公开
标题翻译： ACYCLIC NUCLEOSIDES的合成
公开(公告)号：WO1997030052A1
公开(公告)日：1997-08-21
申请号：PCT/SE1997000242
申请日：1997-02-14
申请人： MEDIVIR AB
发明人： MEDIVIR AB , ENGELHARDT, Per , HÖGBERG, Marita , ZHOU, Xiao-Xiong , LINDBORG, Björn , JOHANSSON, Nils, Gunnar
IPC分类号： C07D473/18
CPC分类号： C07D473/00 , C07D473/18 , Y02P20/55
摘要： A method for preparing enhanced bioavailability antiviral compounds of formula (I) where one of R1 and R2 is -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 and the other of R1 and R2 is -C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl; and R3 is OH or H, the method comprising: A) the monodeacylation of a diacylated compound corresponding to formula (I) wherein R1 and R2 are both -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 (which are optionally N-protected) or R1 and R2 are both -C(=O)C3-C21, saturated or monounsaturated, optionally substituted alkyl; B) acylating the thus liberated side chain 4-hydroxy or side chain 2-hydroxymethyl group with the corresponding -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 or -C(=O)C3-C21, saturated or monounsaturated, optionally substituted alkyl to thereby produce a compound of formula (I); and C) deprotecting as necessary.
摘要翻译：制备式（I）的增强的生物利用度抗病毒化合物的方法，其中R 1和R 2之一是-C（O）CH（CH（CH 3）2）NH 2或-C（O）CH（CH（CH 3）CH 2 CH 3）NH 2和 R1和R2中的另一个是-C（O）C 3 -C 21饱和或单不饱和的，任选取代的烷基; 并且R 3是OH或H，所述方法包括：A）对应于式（I）的二酰化化合物的单脱甲酰化，其中R 1和R 2都是-C（O）CH（CH（CH 3）2）NH 2或-C ）CH（CH（CH 3）CH 2 CH 3）NH 2（其任选地被N-保护的）或R 1和R 2都是-C（= O）C 3 -C 21，饱和或单不饱和，任选取代的烷基; B）用相应的-C（O）CH（CH（CH 3）2）NH 2或-C（O）CH（CH（CH 3）CH 2 CH 3）NH 2酰化由此释放的侧链4-羟基或侧链2-羟甲基或-C（= O）C 3 -C 21，饱和或单不饱和的任选取代的烷基，从而产生式（I）化合物; 和C）根据需要脱保护。

5. 发明公开

EP0988304A1 NUCLEOSIDES ANALOGUES, SUCH AS ANTIVIRALS INCLUDING INHIBITORS OF RETROVIRAL REVERSE TRANSCRIPTASE AND THE DNA POLYMERASE OF HEPATITIS B VIRUS (HBV) 有权
标题翻译： ANALOG核苷作为抗病毒药包括LICH抑制剂逆转录病毒逆转录酶和DNA聚合酶乙型肝炎病毒
公开(公告)号：EP0988304A1
公开(公告)日：2000-03-29
申请号：EP98939041.4
申请日：1998-08-14
申请人： MEDIVIR AB
发明人： ZHOU, Xiao-Xiong , JOHANSSON, Nils-Gunnar , WÄHLING, Horst
IPC分类号： C07D473/00 , C07D473/18 , C07D473/32 , C07H19/16 , C07H19/167 , C07H19/173 , A61K31/52 , A61K31/70
CPC分类号： C07D213/80 , C07D213/85 , C07D307/68 , C07D473/00 , C07D473/18 , C07D473/32 , C07D513/04 , C07H17/08 , C07H19/04 , C07H19/16 , C40B40/00
摘要： A compound of the formula (I), wherein: nuc is the residue of a nucleoside analogue bonded through its single hydroxy group on the cyclic or acyclic saccharide moiety, R1 is hydroxy, amino or carboxy; optionally having esterified/amide bonded thereon; a C4-C22 saturated or unsaturated, optionally substituted fatty acid or alcohol, or an aliphatic L-amino acid; R2 is the residue of an aliphatic L-amino acid; L1 is a trifunctional linker group; L2 is absent or a difunctional linker group; and pharmaceutically acceptable salts thereof have favourable pharmacological properties and are antivirally active.

6. 发明公开

EP1899352A1 1- [2' , 3' -DIDEOXY-3' C- (HYDROXYMETHYL) - BETA-D-ERYTHRO-PENTOFURANOSYL] CYTOSINE DERIVATIVES AS HIV INHIBITORS 有权
标题翻译： 1- [2'，3'-DIDESOXY-3'-C（羟甲基）-B-D-呋喃基 - 戊氧羰基] CYPOSINDERIVATE ALS HIV-INHIBITOREN
公开(公告)号：EP1899352A1
公开(公告)日：2008-03-19
申请号：EP06777595.7
申请日：2006-07-05
申请人： MEDIVIR AB
发明人： ZHOU, Xiao-Xiong , SAHLBERG, Christer
IPC分类号： C07D493/04 , A61K31/513 , A61P31/18
CPC分类号： C07D493/04
摘要： Compounds of the formula (I) wherein: R1 is independently H1 -OR3, -NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefin ic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is -OR3, that R2 may also be -C(=O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1 , 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.

7. 发明公开

EP1150956A1 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷类逆转录酶抑制剂
公开(公告)号：EP1150956A1
公开(公告)日：2001-11-07
申请号：EP99943591.0
申请日：1999-08-18
申请人： MEDIVIR AB
发明人： ZHOU, Xiao-Xiong , JOHANSSON, Nils-Gunnar , WÄHLING, Horst , SUND, Christian , SALVADOR, Lourdes , LINDSTRÖM, Stefan , WALLBERG, Hans , SAHLBERG, Christer
IPC分类号： C07D213/85 , A61K31/44
摘要： Non-nucleoside reverse transcriptase inhibitors of formula (P-1) wherein: Ar1 is an unsaturated, optionally substituted, mono or bicyclic ring structure comprising 0 to 3 hetero atoms selected from S, O and N; Ar2 is an aromatic, optionally substituted, monocyclic ring structure comprising at least one nitrogen hetero atom and zero to two further hetero atoms selected from S, O and N; R4 and R5 are independently H or C3-C8 cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C8 alkynyl, C1-C5 alkoxy, C1-C4 alkanoyloxy, C1-C4 alkylthio, amino, carboxy, carbamoyl, cyano, halo, hydroxy, aminomethyl, hydroxymethyl, carboxymethyl, or halo substituted C1-C6 alkyl mercapto, nitro; or R4 and R5 join to form a 3-6 membered, optionally substituted ring structure; R6 is O or S; Rx is the residue of a natural or unnatural amino acid; and L* is a linker moiety which is ether-, carbonate- or ester-bound to the adjacent oxygen and ester linked to Rx; and pharmaceutically acceptable salts thereof are anti-HIV agents with favourable pharmacokinetic properties.

8. 发明公开

EP1121366A1 PRODRUGS OF PHOSPHOROUS-CONTAINING PHARMACEUTICALS 审中-公开
标题翻译：含磷制药药物前体
公开(公告)号：EP1121366A1
公开(公告)日：2001-08-08
申请号：EP99921327.5
申请日：1999-03-30
申请人： MEDIVIR AB
发明人： ZHOU, Xiao-Xiong , JOHANSSON, Nils, Gunnar , WÄHLING, Horst , SUND, Christian , WALLBERG, Hans , SALVADOR, Lourdes , LINDSTRÖM, Stefan
IPC分类号： C07F9/38 , C07H19/06 , C07H19/16 , C07D473/32
摘要： Pharmaceutical compounds with the formula: Drug-P(=O)-O-Linker(-R2')k-R2 where Drug-P(=O)-O- is the residue of a drug comprising a phosphonate, phosphinate or phosphoryl function, such as alendronate or foscarnet, R2 and R2' (if present) are independently the acyl residue of an aliphatic amino acid; Linker is an at least difunctional moiety comprising a first function ester-bonded to the phosphonate, phosphinate or phosphoryl function spaced from a second function ester-bonded to R2; and k is 1 or zero; have enhanced bioavailability or other pharmacokinetic performance relative to the parent drug.

9. 发明公开

EP1058687A1 NUCLEOSIDES 有权
标题翻译：核苷
公开(公告)号：EP1058687A1
公开(公告)日：2000-12-13
申请号：EP99932499.9
申请日：1999-02-12
申请人： MEDIVIR AB
发明人： WÄHLING, Horst , ZHOU, Xiao-Xiong
IPC分类号： C07H19/16 , C07H19/167 , A61K31/70 , C07K5/00
CPC分类号： C07D213/80 , C07D213/85 , C07D307/68 , C07D473/32 , C07D513/04 , C07H17/08 , C07H19/16 , C40B40/00
摘要： Compounds of formula (I) wherein R is independently H or -CH3 and pharmaceutically acceptable salts thereof have favourable pharmacological properties and are antivirally active against HBV and HIV.

10. 发明公开

EP1054891A1 PRODRUGS 审中-公开
标题翻译：药物前体
公开(公告)号：EP1054891A1
公开(公告)日：2000-11-29
申请号：EP99932500.4
申请日：1999-02-15
申请人： MEDIVIR AB
发明人： JOHANSSON, Nils, Gunnar , ZHOU, Xiao-Xiong , WÄHLING, Horst , SUND, Christian , WALLBERG, Hans , SALVADOR, Lourdes , LINDSTRÖM, Stefan
IPC分类号： C07K5/00 , C07D473/32 , C07D473/00 , C07H19/16 , C07D501/34 , C07D211/34
CPC分类号： C07D213/80 , C07C271/22 , C07D213/85 , C07D307/68 , C07D473/32 , C07D513/04 , C07F9/4006 , C07F9/404 , C07F9/4075 , C07F9/5721 , C07H17/08 , C07H19/00 , C07H19/16 , C40B40/00
摘要： A pharmaceutical compound or an intermediate therefor, having the formula: D*-Linker*(R2')k-R2, where R2 and R2' (if present) is the amide or ester residue of an aliphatic amino acid, k is 0 or 1, D* is a Drug residue bearing an accessible function selected from amine, hydroxy and carboxy, or a group amenable to attachment to said accessible function, Linker* is an at least bifunctional linker comprising a first function bound to said accessible function spaced from a second function forming an amide or acyl bond with the aliphatic amino acid; wherein the compound is free from long chain fatty acid esters; and with the provisos that Linker* does not consist solely of alkoxy when the Drug comprises a lactamcarboxy or enolic hydroxy function and that the Drug is not a monohydric nucleoside.

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