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公开(公告)号:US20090247512A1
公开(公告)日:2009-10-01
申请号:US11995869
申请日:2008-01-16
申请人: Kenneth Alan Simmen , Herman Augustinus De Kock , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Susana Ayesa Alvarez , Bjorn Olof Classon , Hans Kristian Wallberg
发明人: Kenneth Alan Simmen , Herman Augustinus De Kock , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Susana Ayesa Alvarez , Bjorn Olof Classon , Hans Kristian Wallberg
IPC分类号: A61K31/427 , C07D245/04 , A61K31/4709 , A61K31/538 , A61P31/04
CPC分类号: C07D403/12 , C07D401/12 , C07D413/12 , C07D487/04
摘要: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 substituents pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译: 式(I)的HCV复制抑制剂及其N-氧化物,盐或立体异构体,其中每个虚线表示任选的双键; X为N,CH,X为双键,C为C; R1是-OR6,-NH-SO2R7; R2是氢,并且其中X是C或CH,R2也可以是C1-6烷基; R 3是氢,C 1-6烷基,C 1-6烷氧基C 1-6烷基或C 3-7环烷基; n为3,4,5或6; R4和R5与它们所连接的氮原子一起形成双环体系,其选自其中所述环系可以任选被1-3个取代基取代; R6是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基,芳基或与Het取代的C 1-6烷基; R7是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基,芳基或与Het取代的C 1-6烷基; 芳基是苯基或萘基,每个可以任选被1-3个取代基取代; Het是含有1至4个独立地选自N,O或S的杂原子的5或6元饱和的,部分不饱和的或完全不饱和的杂环,并且任选被1-3个取代基取代,含有化合物(I)的药物组合物和 制备化合物(I)。 还提供了式(I)的HCV抑制剂与利托那韦的生物可利用组合。
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公开(公告)号:US20090105302A1
公开(公告)日:2009-04-23
申请号:US11995827
申请日:2006-07-28
申请人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Oden , Susana Ayesa Alvarez , Bjorn Olof Classon
发明人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Oden , Susana Ayesa Alvarez , Bjorn Olof Classon
IPC分类号: A61K31/427 , A61P31/14 , C07D401/12 , A61K31/4523 , A61K31/407 , C07D417/12 , A61K31/4155 , A61K31/395
CPC分类号: C07D401/12 , C07D225/04 , C07D245/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译: 式(I)的HCV复制抑制剂及其N-氧化物,盐或立体异构体,其中每个虚线(由 - - - - 表示)表示任选的双键; X为N,CH,X为双键,C为C; R1是-OR6,-NH-SO2R7; R2是氢,并且其中X是C或CH,R2也可以是C1-6烷基; R 3是氢,C 1-6烷基,C 1-6烷氧基C 1-6烷基或C 3-7环烷基; n为3,4,5或6; R 4和R 5彼此独立地是氢,卤素,羟基,硝基,氰基,羧基,C 1-6烷基,C 1-6烷氧基,C 1-6烷氧基C 1-6烷基,C 1-6烷基羰基,C 1-6烷氧基羰基,氨基,叠氮基,巯基, C 1-6烷硫基,多卤代C 1-6烷基,芳基或Het; W是芳基或Het; R6是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基,芳基或与Het取代的C 1-6烷基; R7是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基,芳基或与Het取代的C 1-6烷基; 芳基是苯基或萘基,各自任选被1-3个取代基取代; Het是含有1-4个杂原子的5或6元饱和的,部分不饱和的或完全不饱和的杂环,各自独立地选自N,O或S,并且任选被1-3个取代基取代; 含有化合物(I)的药物组合物和制备化合物(I)的方法。 还提供了式(I)的HCV抑制剂与利托那韦的生物可利用组合。
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公开(公告)号:US20090118312A1
公开(公告)日:2009-05-07
申请号:US11995900
申请日:2006-07-28
申请人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindstrom , Anna Karin Gertrud Linnea Belfrage , Horst Jurgen Wahling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Bjorn Olof Classon
发明人: Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindstrom , Anna Karin Gertrud Linnea Belfrage , Horst Jurgen Wahling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Bjorn Olof Classon
IPC分类号: A61K31/517 , C07D403/12 , A61P31/12
CPC分类号: C07D487/10 , C07D245/04
摘要: Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; — denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV
摘要翻译: 式I的化合物及其N-氧化物,盐和立体异构体,其中A是OR 1,NHS(-O)p R 2; 其中; R 1是氢,C 1 -C 6烷基,C 0 -C 3亚烷基环羰基,C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基,C 0 -C 3亚烷基环羰基,C 0 -C 3亚烷基杂环基; p独立地为1或2; n为3,4,5或6; - 表示任选的双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq为H或当L为CRz时,Rq也可为C1-C6烷基; Rr是喹唑啉基,任选地被一个两个或三个独立地选自C 1 -C 6烷基,C 1 -C 6烷氧基,羟基,卤素,卤代C 1 -C 6烷基,氨基,单或二烷基氨基,单或二烷基氨基羰基,C 1 -C 6烷基 - 羰基氨基 ,C 0 -C 3亚烷基环基和C 0 -C 3亚烷基杂环基; R 5是氢,C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C 7环烷基; R 6是氢,C 1 -C 6烷基,C 1 -C 6烷氧基,C 0 -C 3亚烷基环羰基,C 0 -C 3亚烷基 - 杂环基,羟基,溴,氯或氟可用于治疗或预防黄病毒感染如HCV
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公开(公告)号:US5747473A
公开(公告)日:1998-05-05
申请号:US516551
申请日:1995-08-18
申请人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
发明人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
IPC分类号: A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号: A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要: ##STR1## Novel antiviral compounds of formulae (1A) and (1B), wherein X and R
1 -R
4 are as stated in claim 1 in the form of an α- or β-anomer or a mixture thereof, and pharmaceutically acceptable salts thereof, are disclosed, as well as a new method for preparation thereof. Said compounds can be used for treatment of infections caused by viruses requiring reverse transcriptase for replication, such as HIV and hepatitis B virus.摘要翻译: (1A)式(1A)和(1B)的新型抗病毒化合物,其中X和R 1 -R 4如权利要求1中所述,为α-或β-甘油基或 其混合物及其药学上可接受的盐,以及其制备方法。 所述化合物可用于治疗由需要逆转录酶复制的病毒引起的感染,例如HIV和乙型肝炎病毒。
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公开(公告)号:US6121431A
公开(公告)日:2000-09-19
申请号:US334756
申请日:1999-06-17
申请人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
发明人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
IPC分类号: A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号: A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要: ##STR1## Novel antiviral compounds of formulae (1A) and (1B), wherein X and R
1 -R
4 are as stated in claim 1 in the form of an α- or β-anomer or a mixture thereof, and pharmaceutically acceptable salts thereof, are disclosed, as well as a new method for preparation thereof. Said compounds can be used for treatment of infections caused by viruses requiring reverse transcriptase for replication, such as HIV and hepatitis B virus.摘要翻译: 公开了式(1A)和(1B)的新型抗病毒化合物,其中X和R 1 -R 4如α-或β-戊内酯或其混合物形式的权利要求1所述及其药学上可接受的盐, 以及其制备方法。 所述化合物可用于治疗由需要逆转录酶复制的病毒引起的感染,例如HIV和乙型肝炎病毒。
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公开(公告)号:US5952500A
公开(公告)日:1999-09-14
申请号:US41135
申请日:1998-03-12
申请人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
发明人: Bjorn Olof Classon , Bengt Bertil Samuelsson , Ingemar Sven-Anders Kvarnstrom , Lars Goran Svansson , Stefan Carl Tore Svensson
IPC分类号: A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
CPC分类号: A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要: The instant disclosure is directed to cyclopentyl analogues of .alpha.- and .beta.-L-2', 3'-dideoxypurine ribonucleosides wherein the 3- and 4-cyclopentyl substituents may be either --H or --CH.sub.2 --OH.
摘要翻译: 本公开涉及α-和β-L'2',3'-脱氨基嘌呤核糖核苷的环戊基类似物,其中3-和4-环戊基取代基可以是-H或-CH 2 -OH。
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