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1. 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。

2. 发明申请

WO1997021665A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 审中-公开
标题翻译：芳香胺衍生物及其作为原子反应的激动剂使用
公开(公告)号：WO1997021665A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005469
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED , GREEN, Richard, Howard , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C229/42
CPC分类号： C07D209/08 , C07C217/84 , C07C229/42 , C07D215/04
摘要： The present invention relates to phenethanolamine derivatives of formula (I) wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the ring is substituted by one to four further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; or R represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents ZCH2CO2H wherein Z represents a bond, or O; Y represents (CH2)n where n is 1-3; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基; R 2表示氢或C 1-6烷基; R 3表示其中环被1-4个其它取代基取代的基团（A），所述取代基选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基; 或R 3表示其中芳环任选被至多三个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的其它取代基取代的基团（B）; R 4表示氢或C 1-6烷基; R 5表示ZCH 2 CO 2 H，其中Z表示键或O; Y表示（CH2）n，其中n为1-3; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

3. 发明申请

WO1997021666A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 审中-公开
标题翻译：芳香胺衍生物及其作为原子反应的激动剂使用
公开(公告)号：WO1997021666A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005470
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , CARTER, Malcolm, Clive , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C229/42
CPC分类号： C07D257/04 , C07C229/42 , C07C229/46 , C07C237/20 , C07C275/40 , C07C309/24 , C07C311/35 , C07C2601/08 , C07F9/3882
摘要： The present invention relates to phenethanolamine derivatives of formula (I), wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the aromatic ring may be optionally substituted by up to four substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents CO2R , C1-6alkylCO2R , CONR R , NHCONR R , SO2NHR , P(O)(OR )2, SO3H, C1-6alkylSO3H, NHSO2R , NHCOR or tetrazol-5-yl; R and R independently represent hydrogen, C1-6alkyl, trifluoromethyl, CN, OH, CO2R , CH2CO2R , or R and R form a 5-6 membered cycloalkyl ring; R represents hydrogen, or C1-6alkyl; R represents hydrogen, C1-6alkyl, or C1-6alkylOR ; R , R , R , R -R , and R -R each independently represent hydrogen, or C1-6alkyl; R represents C1-6alkyl or trifluoromethyl; R represents C1-6alkyl or trifluoromethyl; with the proviso that when R and R are both hydrogen, R is other than hydrogen; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基 ; R 2表示氢或C 1-6烷基; R 3表示芳基可以任选被至多四个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的取代基取代的基团（A）; R 4表示氢或C 1-6烷基; R 5表示CO 2 R 8，C 1-6烷基CO 2 R 16，CONR 9 R 10，NHCONR 11 R 12，SO 2 NHR 13，P（O）（OR 14） 2，SO 3 H，C 1-6烷基SO 3 H，NHSO 2 R 15，NHCOR 17或四唑-5-基; R 6和R 7独立地表示氢，C 1-6烷基，三氟甲基，CN，OH，CO 2 R 18，CH 2 CO 2 R 19或R 6和R 7形成5-6元环烷基环; R 8表示氢或C 1-6烷基; R 9表示氢，C 1-6烷基或C 1-6烷基OR 20; R 10，R 11，R 12，R 14 -R 16和R 18 -R 20各自独立地表示氢或C 1-6烷基; R 13表示C 1-6烷基或三氟甲基; R 17表示C 1-6烷基或三氟甲基; 条件是当R 6和R 7都是氢时，R 8不是氢; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

4. 发明申请

WO1995033724A1 PHENETHANOLAMINE DERIVATIVES AND THEIR USE AS ATYPICAL BETA-ADRENOCEPTOR AGONISTS 审中-公开
标题翻译：苯乙醇胺衍生物及其作为原位β-受体激动剂的用途
公开(公告)号：WO1995033724A1
公开(公告)日：1995-12-14
申请号：PCT/EP1995002133
申请日：1995-06-06
申请人： GLAXO GROUP LIMITED , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07C229/42 , C07C2601/02 , C07D231/38 , C07D277/42 , C07D317/68
摘要： The present invention relates to phenethanolamine derivatives of formula (I), wherein: R represents an aryl group optionally substituted by one or more substituents selected from halo, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents H or C1-6alkyl; R represents a phenyl or heteroaryl group substituted by R and R ; R and R each independently represent H or C1-6alkyl or, R and R together form a C3-6cycloalkyl group; R represents ZCH2CO2H and R represents H or ZCH2CO2H, or R and R together represent a group (a), wherein each Z may be the same or different and is selected from a bond, CH2, O, S or NR , R is H or CO2H and R is H or C1-6alkyl; X represents(CH2)n where n is 1 or 2; and pharmaceutically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中：R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基; R 2表示H或C 1-6烷基; R 3表示被R 6和R 7取代的苯基或杂芳基; R 4和R 5各自独立地表示H或C 1-6烷基，或者R 4和R 5一起形成C 3-6环烷基; R 6表示ZCH 2 CO 2 H，R 7表示H或ZCH 2 CO 2 H，或R 6和R 7一起表示基团（a），其中每个Z可以相同或不同，并且选自键， CH 2，O，S或NR 9，R 8是H或CO 2 H，R 9是H或C 1-6烷基; X表示（CH 2）n，其中n为1或2; 及其药学上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

5. 发明申请

WO1993025548A1 5-(1,2,4-TRIAZOL-1-YLMETHYL)-3H-ISOBENZOFURAN-1-ONE DERIVATIVES, THEIR PREPARATION AND USE AS AROMATASE INHIBITORS 审中-公开
标题翻译： 5-（1,2,4-TRIAZOL-1-YLMETHYL）-3H-ISOBENZOFURAN-1-ONE衍生物，其制备和用作芳香酶抑制剂
公开(公告)号：WO1993025548A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001520
申请日：1993-06-14
申请人： GLAXO GROUP LIMITED , CHERRY, Peter, Clive , FOXTON, Michael, Walter , MERRITT, Andrew, Thomas
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention relates to heterocyclic compounds which are inhibitors of the enzyme aromatase, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Particular compounds of the invention are compounds of formula (I) wherein R represents a cyano or nitro group; R represents hydrogen or one or more halogen atoms; R represents a C1-6alkyl group and R represents hydrogen or a C1-6alkyl group or R and R together represent a C3-6cycloalkyl group; and R represents hydrogen or one or more halogen atoms or C1-6alkoxy groups and pharmaceutically acceptable salts and solvates thereof.
摘要翻译：本发明涉及作为芳香酶的抑制剂，其制备方法的杂环化合物，含有它们的药物组合物及其在医药中的用途。本发明的具体化合物是式（I）的化合物，其中R 1表示氰基或硝基; R 2表示氢或一个或多个卤素原子; R 3表示C 1-6烷基，R 4表示氢或C 1-6烷基，或者R 3和R 4一起表示C 3-6环烷基; R 5表示氢或一个或多个卤素原子或C 1-6烷氧基及其药学上可接受的盐和溶剂化物。

6. 发明申请

WO1992012160A1 BRIDGED CYCLIC KETAL DERIVATIVES 审中-公开
标题翻译： BRIDGED循环酮衍生物
公开(公告)号：WO1992012160A1
公开(公告)日：1992-07-23
申请号：PCT/EP1992000019
申请日：1992-01-07
申请人： GLAXO GROUP LIMITED , SIDEBOTTOM, Philip, James , HARTLEY, Charles, David , PROCOPIOU, Panayiotis, Alexandrou , LESTER, Michael, George , WATSON, Nigel, Stephen , KIRK, Barrie, Edward , COX, Brian , ROBERTS, Suzanne, Elaine , ROSS, Barry, Clive
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D493/08
CPC分类号： C07D493/08 , C07H9/04 , C07H19/01 , C12P17/181
摘要： These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

7. 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。

8. 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。

9. 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。

10. 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。

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