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1. 发明申请

WO1991001319A1 SYNTHESIS OF CYCLOPENTENE DERIVATIVES 审中-公开
标题翻译：环己基衍生物的合成
公开(公告)号：WO1991001319A1
公开(公告)日：1991-02-07
申请号：PCT/EP1990001200
申请日：1990-07-18
申请人： GLAXO GROUP LIMITED , MYERS, Peter, Leslie , STORER, Richard , WILLIAMSON, Christopher , JONES, Martin, Francis , PATERNOSTER, Ian, Leonard , BIGGADYKE, Keith
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D473/18
CPC分类号： C07D473/00 , Y02P20/55
摘要： A process is described for the preparation of the 1R-cis isomer of carbovir, [1'R,4'S]-2-amino-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-1,9-dihydro -6H-purin-6-one and its physiologically acceptable salts from a compound of formula (II) (wherein R is a hydroxyl protecting group) via a compound of formula (III) (wherein R is a hydroxyl protecting group). The 1R-cis isomer of carbovir is an antiviral agent with potent activity against human immunodeficiency virus (HIV).
摘要翻译：描述了制备羰基维生素的1R-顺式异构体的方法，[1'R，4'S] -2-氨基-9- [4-（羟甲基）-2-环戊烯-1-基] 二氢-6H-嘌呤-6-酮及其生理学上可接受的盐通过式（III）化合物（其中R 1是一个羟基保护基）的式（II）化合物（其中R 1是羟基保护基）羟基保护基）。 carbovir的1R-顺式异构体是对人类免疫缺陷病毒（HIV）具有强烈活性的抗病毒剂。

2. 发明申请

WO1991001318A1 SYNTHESIS OF CYCLOPENTENE DERIVATIVES 审中-公开
标题翻译：环己基衍生物的合成
公开(公告)号：WO1991001318A1
公开(公告)日：1991-02-07
申请号：PCT/EP1990001199
申请日：1990-07-18
申请人： GLAXO GROUP LIMITED , MYERS, Peter, Leslie , STORER, Richard , WILLIAMSON, Christopher , JONES, Martin, Francis
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , Y02P20/55
摘要： A process is described for the preparation of the 1R-cis isomer of carbovir, [1'R,4'S]-2-amino-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-1,9-dihydro -6H-purin-one and its physiologically acceptable salts from a compound of formula (II) (where L represents a leaving group, R represents a hydrogen atom or a hydroxyl protecting group and R represents OH, NH2 or a protected hydroxyl group). The 1R-cis isomer of carbovir is an antiviral agent with potent activity against human immunodeficiency virus (HIV).
摘要翻译：描述了制备羰基维生素的1R-顺式异构体的方法，[1'R，4'S] -2-氨基-9- [4-（羟甲基）-2-环戊烯-1-基] （II）化合物（其中L表示离去基团，R 1表示氢原子或羟基保护基团，并且R 2表示OH，NH 2）的化学式及其生理上可接受的盐或被保护的羟基）。 carbovir的1R-顺式异构体是对人类免疫缺陷病毒（HIV）具有强烈活性的抗病毒剂。

3. 发明申请

WO1991001317A1 SYNTHESIS OF CYCLOPENTENE DERIVATIVES 审中-公开
标题翻译：环己基衍生物的合成
公开(公告)号：WO1991001317A1
公开(公告)日：1991-02-07
申请号：PCT/EP1990001198
申请日：1990-07-18
申请人： GLAXO GROUP LIMITED , MYERS, Peter, Leslie , STORER, Richard , WILLIAMSON, Christopher
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , Y02P20/55
摘要： A process is described for the preparation of the 1R-cis isomer of carbovir, [1'R,4'R]-2-amino-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-1,9-dihydro -6H-purin-6-one from carbocyclic guanosine via a cyclic orthoester of formula (III) (where R is a protecting group and R is a C1-6 alkyl group). The 1R-cis isomer of carbovir is an antiviral agent with potent activity against human immunodeficiency virus (HIV).
摘要翻译：描述了制备碳水化合物的1R-顺式异构体的方法，[1'R，4'R] -2-氨基-9- [4-（羟基甲基）-2-环戊烯-1-基] 通过式（III）的环状原酸酯（其中R是保护基，R 1是C 1-6烷基），通过碳环鸟苷来制备9-二氢-6H-嘌呤-6-酮。 carbovir的1R-顺式异构体是对人类免疫缺陷病毒（HIV）具有强烈活性的抗病毒剂。

4. 发明申请

WO1999021861A1 PROCESS FOR PREPARING A CHIRAL NUCLEOSIDE ANALOGUE 审中-公开
标题翻译：制备核苷类似物的方法
公开(公告)号：WO1999021861A1
公开(公告)日：1999-05-06
申请号：PCT/EP1997005872
申请日：1997-10-24
申请人： GLAXO GROUP LIMITED , WALLIS, Christopher, John , JONES, Martin, Francis , XIE, Shiping
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00
摘要： A new process for the preparation of the chiral nucleoside analogue (1S,4R)-4-[2-amino-6-(cyclopropylamino)-9Hpurin-9-yl]-2-cyclopentene-1-methanol comprising reacting a compound of formula (II) or (III), wherein X is H or a blocking group and Y is H or an activating group, with 2-amino-6-(cyclopropylamino) purine in the presence of a catalyst.
摘要翻译：该方法用于制备手性核苷类似物（1S，4R）-4- [2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基] -2-环戊烯-1-甲醇，其包括使式（II）或（III），其中X为H或封闭基团，Y为H或活化基团，与2-氨基-6-（环丙基氨基）嘌呤在催化剂存在下反应。

5. 发明申请

WO1999024431A1 PROCESS FOR PREPARING A CHIRAL NUCLEOSIDE ANALOGUE 审中-公开
标题翻译：制备核苷类似物的方法
公开(公告)号：WO1999024431A1
公开(公告)日：1999-05-20
申请号：PCT/EP1997006379
申请日：1997-11-12
申请人： GLAXO GROUP LIMITED , WALLIS, Christopher, John , JONES, Martin, Francis , XIE, Shiping
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D473/00
CPC分类号： C07D473/00
摘要： A new process for the preparation of the chiral nucleoside analogue (1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H purin-9-yl]-2-cyclopentene-1-methanol comprising reacting a compound of formula (II) or (III), wherein X is H or a blocking group and Y is H or an activating group, with 2-amino-6-(cyclopropylamino)purine in the presence of a catalyst.
摘要翻译：该方法用于制备手性核苷类似物（1S，4R）-4- [2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基] -2-环戊烯-1-甲醇，其包括使式（II）或（III）其中X为H或封闭基团，Y为H或活化基团，与2-氨基-6-（环丙基氨基）嘌呤在催化剂存在下反应。

6. 发明申请

WO1995001170A2 USE OF PHENETHANOLAMINE DERIVATIVES IN THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：苯乙醇胺衍生物在治疗胃肠疾病中的应用
公开(公告)号：WO1995001170A2
公开(公告)日：1995-01-12
申请号：PCT/EP1994002106
申请日：1994-06-29
申请人： GLAXO GROUP LIMITED , STORER, Richard , FOXTON, Michael, Walter , HARTLEY, Charles, David , GREEN, Richard, Howard , TRAVERS, Stuart
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/165
CPC分类号： A61K31/195 , A61K31/135
摘要： The use of compounds of formula (I) in which: R is hydrogen, methyl or hydroxymethyl; R is substituted alkyl; R and R are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl group, or substituted alkyl; X is oxygen or sulphur; and Ar is optionally substituted phenyl or naphtyl; and pharmaceutically acceptable salts thereof in the treatment of gastrointestinal disorders is described.
摘要翻译：式（I）化合物的用途，其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自为氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代的烷基; X是氧或硫; 和Ar是任选取代的苯基或萘基; 和其药学上可接受的盐在治疗胃肠道疾病中的用途。

7. 发明申请

WO1993001174A1 THIAZOLIDINE DERIVATIVES AND THEIR USE AS ANTI-VIRAL COMPOUNDS 审中-公开
标题翻译：噻唑烷衍生物及其作为抗病毒化合物的用途
公开(公告)号：WO1993001174A1
公开(公告)日：1993-01-21
申请号：PCT/EP1992001494
申请日：1992-07-03
申请人： GLAXO GROUP LIMITED , KITCHIN, John , HOLMES, Duncan, Stuart , HUMBER, David, Cedric , STORER, Richard , DOLAN, Simon, Charles , HANN, Michael, Menteith , MCMEEKIN, Peter , MURRAY-RUST, Peter , PATEL, Binakumari , WEINGARTEN, Gordon, Gad
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D217/06
CPC分类号： C07D417/12 , C07D277/06 , C07D417/14
摘要： The present invention provides compounds of formula (I), wherein R is hydrogen, alkyl or CH2alkyl where the alkyl portion is substituted by OH; A represents either a group CHR CHR OH or a group (II), where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen, alkyl, cycloalkylalkyl, aralkyl, CHR CONR R (where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen or methyl and R is hydrogen, alkyl optionnally substituted by one or two hydroxyl groups, aryl, heteroaryl, cycloalkylalkyl, Aralkyl wherein the alkyl portion is optionnally substituted by hydroxymethyl, or Hetalkyl) or CHR NHCOR (where R is alkyl, cycloalkylalkyl or an aralkyl), R is alkoxy or NR R (where R is hydrogen or methyl and R is hydrogen, alkyl, aryl, aralkyl or cycloalkylalkyl); X is a group -CHR (CHR )r(CHR )sCHR -, where R and R are hydrogen, r is 1, s is zero and R is hydroxyl or hydroxymethyl, or R and R are hydrogen, r and s are 1 and R and R are each hydrogen or hydroxyl provided that at least one of R and R is hydroxyl, or one of R and R is hydrogen and the other is hydroxymethyl and r and s are zero; useful in chemotherapy, particularly of viral infections.
摘要翻译：本发明提供式（I）化合物，其中R 1是氢，烷基或C 2烷基，其中烷基部分被OH取代; A代表基团CHR 21 CHR 22 OH或基团（II），其中R 21是氢，烷基，环烷基烷基或芳烷基，R 22是氢，烷基，环烷基烷基，芳烷基，CHR 24 R CONR 25 R 26（其中R 24是氢，烷基，环烷基烷基或芳烷基，R 25是氢或甲基，R 26是氢，烷基选择性地被一个或两个羟基取代，芳基，杂芳基，环烷基烷基，芳烷基，其中烷基部分选择性地被羟甲基或Hetalkyl取代）或CHR 24 NHCOR 27（其中R 27是烷基，环烷基烷基或芳烷基），R 23是烷氧基或NR 28 R 29（其中R 28是氢或甲基，R 29是氢，烷基，芳基，芳烷基或环烷基烷基）; X是基团-CHR 30（CHR 31）r（CHR 32）s CHR 33，其中R 30和R 33是氢，r是1，s是0，R 31是羟基或羟甲基，或R 30和R 33是氢，r和s是1，R 31和R 32各自是氢或羟基，条件是R 31中至少有一个且R 32为羟基，R 30和R 33之一为氢，另一个为羟甲基，r和s为0; 可用于化疗，特别是病毒感染。

8. 发明申请

WO1992020665A1 THIAZOLIDINE DERIVATIVES AND THEIR USE IN THERAPY 审中-公开
标题翻译：噻唑啶衍生物及其在治疗中的应用
公开(公告)号：WO1992020665A1
公开(公告)日：1992-11-26
申请号：PCT/GB1992000840
申请日：1992-05-08
申请人： GLAXO GROUP LIMITED , HUMBER, Dai, Cedric , WEINGARTEN, Gordon, Gad , STORER, Richard , KITCHIN, John , HANN, Michael, Menteith
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D277/06
CPC分类号： C07D417/14 , C07D277/06 , C07D499/00
摘要： The present invention provides compounds of formula (I), wherein x is zero, 1 or 2; R and R are each independently hydrogen, C1-4alkyl or CH2C1-3alkyl where the C1-3alkyl portion is substituted by OH; R , R , R and R are each independently hydrogen, methyl, ethyl, CH2OH,CH2NH2 or COOH when x is zero, or R , R , R and R are each independently hydrogen, methyl or CH2OH when x is 1 or 2; R and R are each independently hydrogen, C1-10alkyl, C3-8cycloalkyl, ArC1-4alkyl, HetC1-4alkyl, COAr, COHet, COCH2R , COCH(OH)Ar, COCH(OH)Het, COCH=CHPh, COR , CO2CH2Ar, CO2CH2Het, SO2Ar, SO2Het,SO2CH2R , SO2CH=CHPh or SO2R [where R and R each independently represent hydrogen, C1-6alkyl, aryl, heteroaryl, ArC1-4alkyl, HetC1-4alkyl, aryloxy, heteroaryloxy, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, (CH2)nCO2R (where n is zero or 1 and R is hydrogen or C1-6alkyl), (CH2)mNR R (where m is zero, 1, 2, 3, 4 or 5 and R are each independently hydrogen or C1-4alkyl or together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group), and R and R each independently represent C3-8cycloalkyl substituted by phenyl]; R and R are each independently hydrogen, C1-6alkyl, COOR (where R is hydrogen, C1-6alkyl or ArC1-4alkyl) or CONR R [where R is hydrogen or C1-4alkyl and R is hydrogen, OH, aryl, heteroaryl, ArC1-4alkyl (wherein the C1-4alkyl portion is optionally substituted by hydroxymethyl), HetC1-4alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, (CH2pR (where p is zero or 1 and R is CF3 or CO2R where R is hydrogen or C1-6alkyl), (CH2)qNR R (where q is zero, 1, 2, 3, 4, or 5 and R and R are each independently hydrogen, C1-4alkyl or aryl or together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group), CHArCO2R , CHHet CO2R (where R and R are each independently hydrogen or C1-6alkyl) or C1-6alkyl optionally substituted by OH, or R and R together with the nitrogen atom to which they are attached form a saturated heterocyclic amino group]; R and R are each independently hydrogen, hydroxy or acetoxy; and physiologically acceptable salts and solvates thereof. Also described are the use of the compounds as antiviral agents, pharmaceutical compositions containing them and methods for their preparation.
摘要翻译：本发明提供式（I）化合物，其中x为0,1或2; R 1和R 6各自独立地为氢，C 1-4烷基或C 2 -C 1-3烷基，其中C 1-3烷基部分被OH取代; 当x为零时，R 2，R 3，R 4和R 5各自独立地为氢，甲基，乙基，CH 2 OH，CH 2 NH 2或COOH，或R 2，R 3，R 当x为1或2时，R 4和R 5各自独立地为氢，甲基或CH 2 OH; R 7和R 9各自独立地为氢，C 1-10烷基，C 3-8环烷基，Ar C 1-4烷基，Het C 1-4烷基，COAr，COHet，COCH 2 R 13，COCH（OH）Ar，COCH（OH）Het ，COCH = CHPh，COR 14，CO 2 CH 2 Ar，CO 2 CH 2 Het，SO 2 Ar，SO 2 Het，SO 2 CH 2 R 15，SO 2 CH = CHPh或SO 2 R 16 [其中R 13和R 15各自独立地表示氢，C 1-6烷基，芳基，杂芳基，ArC 1-4烷基，HetC 1-4烷基，芳氧基，杂芳氧基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，（CH 2）n CO 2 R 17（其中n为0或1，R 17为氢或C 1 烷基），（CH 2）m NR R 18 R（其中m为0,1,2,3,4或5，R 19各自独立地为氢或C 1-4烷基或与氮原子一起它们连接形成饱和杂环氨基），R 14和R 16各自独立地表示被苯基取代的C 3-8环烷基; R 8和R 10各自独立地为氢，C 1-6烷基，COOR 20（其中R 20为氢，C 1-6烷基或ArC 1-4烷基）或CONR 21 R 22 [其中 R 21是氢或C 1-4烷基，R 22是氢，OH，芳基，杂芳基，ArC 1-4烷基（其中C 1-4烷基部分任选被羟甲基取代），HetC 1-4烷基，C 3-8环烷基，C 3 -8环烷基C 1-4烷基，（CH 2 p R 23）（其中p为0或1，R 23为CF 3或CO 2 R 24，其中R 24为氢或C 1-6烷基），（CH 2）q NR R R <26>（其中q为零，1,2,3,4或5，R 25和R 26各自独立地为氢，C 1-4烷基或芳基，或与它们相连的氮原子一起形成饱和杂环氨基），CHArCO 2 R 27，CHHet CO 2 R 28（其中R 27和R 28各自独立地为氢或C 1-6烷基）或任选被OH取代的C 1-6烷基， 21>和R 22与它们所连接的氮原子一起形成饱和杂环氨基]; R 11和R 12各自独立地为氢羟基或乙酰氧基; 及其生理上可接受的盐和溶剂合物。还描述了化合物作为抗病毒剂的用途，含有它们的药物组合物及其制备方法。

9. 发明申请

WO1995000503A1 PROCESS FOR THE PREPARATION OF N-ACETYL NEURAMINIC ACID DERIVATIVES 审中-公开
标题翻译：制备N-乙酰神经氨酸衍生物的方法
公开(公告)号：WO1995000503A1
公开(公告)日：1995-01-05
申请号：PCT/EP1994001940
申请日：1994-06-15
申请人： GLAXO GROUP LIMITED , SEARLE, Andrew, David , WILLIAMSON, Christopher
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D309/28
CPC分类号： C07D309/28 , Y02P20/55
摘要： A method for the preparation of 5-acetamido-4-amino-2,3,4,5-tetradeoxy-D &cir& _-glycero-D &cir& _-galacto-non-2-enopyranosonic acid is described.
摘要翻译：描述了制备5-乙酰氨基-4-氨基-2,3,4,5-四脱氧-D-半乳糖 - 甘油基-D-半乳糖 - 非-2-吡喃糖酸的方法。

10. 发明申请

WO1986001205A1 PYRIMIDINONE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO1986001205A1
公开(公告)日：1986-02-27
申请号：PCT/GB1985000360
申请日：1985-08-13
申请人： GLAXO GROUP LIMITED , PHILLIPPS, Gordon, Hanley , UNDHEIM, Kjell , WILLIAMSON, Christopher , STEEPLES, Ian, Philip , BAIN, Brian, MacDonald , BORELLA, Raymond, Andrew
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D239/22
CPC分类号： C07D239/56 , C07D409/06 , C07D417/06
摘要： Bisulphite adducts of compounds of formula (I) wherein R represents a group formula (II), R represents a halogen atom or a trifluoromethyl group; R represents a hydrogen atom or a C1-4 alkyl, C6-10 aryl or benzoyl group; R represents a hydrogen atom or, together with R , represents a -CH2- or -CH2-CH2- chain; and formula (III) represents a C6-10 carbocyclic aromatic group or a carbon-attached heterocyclic group containing a 5- or 6- membered unsaturated heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused carbocyclic ring, which carbocyclic or heterocyclic group may carry one or more substituents selected from halogen atoms, C1-4 alkyl, C1-4 alkanoyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, C1-4 alkylthio, hydroxyl, nitro, cyano and formyl groups, -NR R groups (where R is a hydrogen atom or a C1-4 alkyl group, and R is a hydrogen atom or a C1-4 alkyl, C1-4 alkanoyl or aroyl group) and C1-4 alkyl groups substituted by one or more hydroxy or -NR R groups and halogen atoms; and salts of such adducts have metaphase arrest abilities and desirably good water solubilities and may be useful in combatting abnormal cell proliferation.
摘要翻译：式（I）化合物的亚硫酸氢盐加合物，其中R表示基团式（II），R 1表示卤素原子或三氟甲基; R 2表示氢原子或C 1-4烷基，C 6-10芳基或苯甲酰基; R 3表示氢原子，或与R 2一起代表-CH 2 - 或-CH 2 -CH-链; 并且式（III）表示含有5-或6-元不饱和杂环的C 6-10碳环芳基或含碳连接的杂环基，该环含有一个或多个选自O，N和S的杂原子，并且任选携带稠合碳环，其中碳环或杂环基可以携带一个或多个选自卤素原子，C 1-4烷基，C 1-4烷酰基，C 1-4烷氧基，C 1-4烷氧基羰基，C 1-4烷硫基，羟基，硝基，氰基和甲酰基，-NR 4 R 5基团（其中R 4是氢原子或C 1-4烷基，R 5是氢原子或C 1-4烷基，C 1-4 烷酰基或芳酰基）和被一个或多个羟基或-NR 4 R 5基团和卤素原子取代的C 1-4烷基; 并且这种加合物的盐具有中期阻滞能力和期望的良好的水溶性，并且可用于对抗异常细胞增殖。

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