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公开(公告)号:US4942166A
公开(公告)日:1990-07-17
申请号:US374628
申请日:1989-06-30
IPC分类号: C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/00
CPC分类号: C07D473/00
摘要: A crystalline monohydrate of the compound of formula (A) or a crystalline sodium salt monohydrate of the compound of formula (A): ##STR1## having antiviral activity, processes for their preparation and their use as pharmaceuticals.
摘要翻译: 式(A)化合物的结晶一水合物或具有抗病毒活性的式(A)化合物的结晶钠盐一水合物:其制备方法及其作为药物的用途。
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公开(公告)号:US5075445A
公开(公告)日:1991-12-24
申请号:US85216
申请日:1987-08-12
IPC分类号: A61K31/52 , A61K31/522 , A61K31/675 , A61P31/12 , A61P31/22 , C07C31/22 , C07C43/178 , C07C69/007 , C07D319/06 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/22 , C07D473/24 , C07D473/40 , C07F9/6561 , C07F9/6574
CPC分类号: C07D473/00 , C07C31/22 , C07C43/1782 , C07C69/007 , C07D319/06 , C07F9/65616
摘要: A compound of formula (I) ##STR1## or a salt or acyl derivative thereof, in which X represents chlorine, C.sub.1-6 alkoxy, phenoxy, phenyl C.sub.1-6 alkoxy, NH.sub.2, --OH or --SH, is useful in treating viral infections.
摘要翻译: 其中X代表氯,C1-6烷氧基,苯氧基,苯基C1-6烷氧基,NH2,-OH或-SH的式(I)化合物或其盐或酰基衍生物是有用的 治疗病毒感染。
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公开(公告)号:US5250688A
公开(公告)日:1993-10-05
申请号:US825440
申请日:1992-01-22
IPC分类号: C07C69/007 , C07D473/00 , C07F9/6561 , C07D473/34 , A61K31/52
CPC分类号: C07D473/00 , C07C69/007 , C07F9/65616
摘要: A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group.Processes for preparing these compounds and their use in therapy is also described.
摘要翻译: 式(I)化合物或其盐,其中R 1和R 2各自独立地为氢,酰基或磷酸酯,条件是当R 1或R 2中的一个为磷酸酯时,另一个为氢; 或R 1和R 2连接在一起形成环状缩醛基,环状碳酸酯基或环状磷酸酯基。 还描述了制备这些化合物及其在治疗中的用途的方法。
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公开(公告)号:US5246937A
公开(公告)日:1993-09-21
申请号:US824131
申请日:1992-01-22
IPC分类号: C07C69/007 , C07D473/00
CPC分类号: C07D473/00 , C07C69/007
摘要: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.
摘要翻译: 本发明提供式(I)的抗病毒化合物:由其制备的药物组合物,以及用其治疗病毒感染的方法。
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公开(公告)号:US4736029A
公开(公告)日:1988-04-05
申请号:US844520
申请日:1986-03-21
IPC分类号: B01J31/00 , B01J31/02 , C07B61/00 , C07D473/40 , A61K31/52
CPC分类号: C07D473/40
摘要: A process for the preparation of the compound of formula (I): ##STR1## which process comprises reacting the compound of formula (II): ##STR2## with a chlorinating agent in the presence of a phase transfer catalyst containing chloride ions.
摘要翻译: 制备式(I)化合物的方法:该方法包括使式(II)化合物:(II)与氯化剂在相转移催化剂存在下反应 含氯离子。
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公开(公告)号:US5247085A
公开(公告)日:1993-09-21
申请号:US892601
申请日:1992-05-29
IPC分类号: C07F9/40 , C07F9/6506 , C07F9/6512 , C07F9/6561 , C07F9/6571
CPC分类号: C07F9/657181 , C07F9/4006 , C07F9/65061 , C07F9/65127 , C07F9/65616
摘要: Compounds of formula (I), and pharmaceutically acceptable salts thereof ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 whereinR.sub.7 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two substituents selected from halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sub.2 is amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is a group of formula: ##STR2## R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; orR.sub.3 and R.sub.4 together are: ##STR3## wherein R.sub.6 is as defined above;having antiviral activity, to processes for their preparation and their use as pharmaceuticals.
摘要翻译: 式(I)化合物及其药学上可接受的盐其中R 1是羟基,氨基,氯或OR 7,其中R 7是C 1-6烷基,苯基或苯基C 1-2烷基,其中苯基部分可以是 被一个或两个选自卤素,C 1-4烷基或C 1-4烷氧基的取代基取代; R2是氨基,或当R1是羟基或氨基时,R2也可以是氢; R3是氢,羟甲基或酰氧基甲基; R 4是下式的基团:R 5和R 6独立地选自氢,C 1-6烷基和任选取代的苯基; 或者R 3和R 4一起是:其中R 6如上定义; 具有抗病毒活性,其制备方法及其作为药物的用途。
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7.
公开(公告)号:US5252575A
公开(公告)日:1993-10-12
申请号:US886710
申请日:1992-05-21
IPC分类号: C07D473/18 , C07D473/32 , A61K31/52 , C07D473/26
CPC分类号: C07D473/32 , C07D473/18
摘要: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; andR.sub.2 is C.sub.1-6 alkyl;which are pro-drugs for 9-(3-hydroxyprop-1-oxy)guanine having antiviral activity, a process for their preparation and their use as pharmaceuticals.
摘要翻译: 式(I)化合物及其药学上可接受的盐:其中R 1是氢或羟基; 和R 2是C 1-6烷基; 其为具有抗病毒活性的9-(3-羟基丙-1-氧)鸟嘌呤的前药,其制备方法及其作为药物的用途。
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公开(公告)号:US4965270A
公开(公告)日:1990-10-23
申请号:US433011
申请日:1989-11-07
申请人: Michael R. Harnden , Paul G. Wyatt , Stuart Bailey
发明人: Michael R. Harnden , Paul G. Wyatt , Stuart Bailey
IPC分类号: C07D473/16 , C07D473/18 , C07D473/32
CPC分类号: C07D473/18 , C07D473/16 , C07D473/32
摘要: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or CH.sub.2 OH;R.sub.2 is hydrogen or, when R.sub.1 is hydrogen, hydroxy or CH.sub.2 OH;R.sub.3 is CH.sub.2 OH or, when R.sub.1 and R.sub.2 are both hydrogen, CH(OH)CH.sub.2 OH;R.sub.4 is hydrogen, hydroxy, amino or OR.sub.5 whereinR.sub.5 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy groups;and in which any OH groups in R.sub.1, R.sub.2 and R.sub.3 may be in the form of O-acyl, phosphate, cyclic acetal or cyclic carbonate derivatives thereof; having antiviral activity.
摘要翻译: 式(I)化合物及其药学上可接受的盐:其中R 1是氢或CH 2 OH; R2是氢或当R1是氢时羟基或CH2OH; R 3是CH 2 OH,或当R 1和R 2均为氢时,CH(OH)CH 2 OH; R4是氢,羟基,氨基或OR5,其中R5是C1-6烷基,苯基或苯基C1-2烷基,其中苯基部分可以被一个或两个卤素,C1-4烷基或C1-4烷氧基取代; 其中R 1,R 2和R 3中的任何OH基可以是O-酰基,磷酸酯,环状缩醛或环状碳酸酯衍生物的形式; 具有抗病毒活性。
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公开(公告)号:US5356886A
公开(公告)日:1994-10-18
申请号:US965260
申请日:1993-01-19
IPC分类号: A61K31/52 , A61P31/12 , C07D473/16 , C07F9/6561 , A61K31/675
CPC分类号: C07F9/65616
摘要: The present invention provides antiviral compounds of Formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein X is --CH.sub.2 O or --CH.sub.2 ;R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl, wherein the acyl group of said acyloxymethyl is selected from the group consisting of C.sub.1-7 alkanoyl and benzoyl optionally substituted in the phenyl ring by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, wherein the alkyl moiety of said C.sub.1-4 alkyl and C.sub.1-4 alkoxy substituents is selected from the group consisting of methyl, ethyl, n- and iso-propyl, n-, sec-, iso- and tert-butyl,R.sub.4 is a group of formula: ##STR2## wherein R.sub.5 and R.sub.6 are independent selected from hydrogen, C.sub.1-6 alkyl and phenyl optionally substituted by one, two or three substituents selected from the group consisting of fluoro, chloro, bromo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, wherein the alkyl moiety of said C.sub.1-4 alkyl and C.sub.1-4 alkoxy substituents is selected from the group consisting of methyl, ethyl, n- and iso-propyl, n-, sec-, iso- and tert-butyl.
摘要翻译: PCT No.PCT / GB91 / 01171 Sec。 371日期:1993年1月19日 102(e)日期1993年1月19日PCT PCT 1991年7月15日PCT公布。 出版物WO92 / 01698 本发明提供式(I)的抗病毒化合物及其药学上可接受的盐:其中X是-CH 2 O或-CH 2; R1是羟基或氨基; R2是氢或氨基; R3是氢,羟甲基或酰氧基甲基,其中所述酰氧基甲基的酰基选自C1-7烷酰基和任选在苯环中被苯基取代的苯甲酰基中的一个,两个或三个选自氟,氯 ,溴,C 1-4烷基和C 1-4烷氧基,其中所述C 1-4烷基和C 1-4烷氧基取代基的烷基部分选自甲基,乙基,正和异丙基,正,正,正 - ,异 - 和叔丁基,R 4是下式的基团:其中R 5和R 6独立地选自氢,C 1-6烷基和任选被一个,两个或三个选自以下的取代基取代的苯基: 氟,氯,溴,C 1-4烷基和C 1-4烷氧基,其中所述C 1-4烷基和C 1-4烷氧基取代基的烷基部分选自甲基,乙基,正和异丙基, 正,仲,异,叔丁基。
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公开(公告)号:US5166198A
公开(公告)日:1992-11-24
申请号:US500718
申请日:1990-03-28
IPC分类号: C07D487/04 , A61K31/505 , A61P31/12 , C07F9/6561
CPC分类号: C07F9/65616
摘要: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is hydrogen or (when R.sub.3 =H and Z is a bond or CH.sub.2) hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;Z is a bond, or a group CHR.sub.8 wherein R.sub.8 is hydrogen, or (when R.sub.3 =R.sub.4 =H), R.sub.8 is hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;R.sub.5 is a group of formula: ##STR2## wherein R.sub.6 and R.sub.7 are independently selected from hydrogen,C.sub.1-6 alkyl and optionally substituted phenyl.
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