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1. 发明申请

WO1995016680A1 CRYSTALLINE N-ACETYL NEURAMINIC ACID DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：晶型N-乙酰神经氨酸衍生物及其制备方法
公开(公告)号：WO1995016680A1
公开(公告)日：1995-06-22
申请号：PCT/EP1994004154
申请日：1994-12-15
申请人： GLAXO GROUP LIMITED , WILLIAMSON, Christopher , WHITE, William, James , PATEL, Vipulkumar
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D309/28
CPC分类号： C07D309/28
摘要： Acetamido-2,3,4,5-tetradeoxy-4-guanidino- D -glycero- D -gal acto-non-2-enopyranosonic acid in crystalline form, particularly in the form of a hydrate which exists as crystals having a low aspect ratio, or in the form of a hydrate which exists as crystals having a high aspect ratio.
摘要翻译：具有结晶形式的乙酰氨基-2,3,4,5-四脱氧-4-胍基-N， - 甘油-D-脯氨酸 - 非-2-吡喃葡萄糖酸，特别是以水合物的形式存在，作为具有低纵横比的晶体，或以具有高纵横比的晶体存在的水合物的形式存在。

2. 发明申请

WO1997022589A1 BENZAMIDE DERIVATIVES AS THROMBIN INHIBITORS 审中-公开
标题翻译：苯扎林衍生物作为抑制剂
公开(公告)号：WO1997022589A1
公开(公告)日：1997-06-26
申请号：PCT/EP1996005743
申请日：1996-12-13
申请人： GLAXO GROUP LIMITED , WATSON, Nigel, Stephen , PASS, Martin , PATEL, Vipulkumar
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , A61K31/4409 , A61K31/4439 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to a novel class of amide derivatives which act as thrombin inhibitors as described by formula (I), where R and R , independently represent a group (a) or R and R together form a C3-7 heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C1-6 alkyl, C1-4 alkoxy, halogen, carboxylic acid or a C1-4 carboxylic acid ester group; R represents hydrogen, C1-3 alkyl, halogen, or C1-2 alkoxy; R , R and R independently represent hydrogen, or halogen; R represents hydrogen or C1-6 alkyl; R represents hydrogen, C3-7 cycloalkyl, C3-7 cycloalkenyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkenyl, aryl or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR R , NHCOR , NHSO2R , COR , CO2R , CONR R , and SO2NHR ; X represents a bond, a C1-6 alkyl chain, or a C3-6 alkenyl chain, where one or two nitrogen, oxygen, or sulfur atoms may be optionally contained within each chain, and the chains are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6alkyl, C1-6alkoxy, C1-6acyloxy, NR R , NHCOR , NHSO2R , COR , CO2R , CONR R , and SO2NHR ; R -R represent hydrogen, C1-6 alkyl, or R and R or R and R form a C3-7 heterocycloalkyl ring, or R additionally may represent trifluoromethyl; and pharmaceutically acceptable derivatives or solvates threreof, to processes for their preparation; and their use in the treatment of clinical conditions susceptible to amelioration by administration of a thrombin inhibitor.
摘要翻译：本发明涉及作为如式（I）所述的凝血酶抑制剂的新一类酰胺衍生物，其中R 1和R 2独立地表示基团（a）或R 1和R 2 >一起形成可以被C 1-6烷基，C 1-4烷氧基，卤素，羧酸或C 1-4羧酸酯基团任选取代的C 3-7杂环烷基或杂环烯基; R 3表示氢，C 1-3烷基，卤素或C 1-2烷氧基; R 4，R 5和R 6独立地表示氢或卤素; R 7表示氢或C 1-6烷基; R 8表示氢，C 3-7环烷基，C 3-7环烯基，C 3-7杂环烷基，C 3-7杂链烯基，芳基或杂芳基，这些基团任选被一个或多个选自卤素，羟基，CN，C 1 -6烷基，C 1-6烷氧基，C 1-6酰氧基，NR 9 R 10，NHCOR 11，NHSO 2 R 12，COR 13，CO 2 R 14，CONR 15 R 16 >和SO2NHR17; X表示键，C 1-6烷基链或C 3-6烯基链，其中每个链中可任选地含有一个或两个氮，氧或硫原子，并且该链任选被一个或多个基团取代选自卤素，羟基，CN，C 1-6烷基，C 1-6烷氧基，C 1-6酰氧基，NR 9 R 10，NHCOR 11，NHSO 2 R 12，COR 13，CO 2 R 14，CONR <15> R 16，和SO 2 NHR 17; R 9 -R 17代表氢，C 1-6烷基或R 9和R 10或R 15和R 16形成C 3-7杂环烷基环，或R 12 另外可以表示三氟甲基; 和其药学上可接受的衍生物或溶剂合物，用于制备它们的方法; 以及它们在治疗通过施用凝血酶抑制剂而易于改善的临床病症中的用途。

3. 发明申请

WO1994007886A1 SYNTHESIS OF N-ACETYL NEURAMINIC ACID DERIVATIVES 审中-公开
标题翻译： N-乙酰神经氨酸衍生物的合成
公开(公告)号：WO1994007886A1
公开(公告)日：1994-04-14
申请号：PCT/EP1993002575
申请日：1993-09-23
申请人： GLAXO GROUP LIMITED , PATEL, Vipulkumar
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D309/28
CPC分类号： C07D309/28
摘要： A method for the preparation of 5-acetamido-2,3,4,5-tetradeoxy-4-guanidino-D &cir& _-glycero-D &cir& _-galacto-non-2-eno-pyranosonic acid by reaction of 5-acetamido-2,3,4,5-tetradeoxy-4-amino-D &cir& _-glycero-D &cir& _-galacto-non-2-eno-pyranosonic acid with pyrazole-1H-carboxamidine or a derivative thereof in aqueous medium.
摘要翻译： 5-乙酰氨基-2,3,4,5-四脱氧-4-胍基-N，N-甘油基-D-半乳糖 - 非-2-烯 - 吡喃糖酸的制备方法 -2,3,4,5-四脱氧-4-氨基-D-环丙基-D-胆甾 - 壬-2-酮 - 吡喃酮酸与吡唑-1H-甲脒或其衍生物在水性介质中反应。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明申请

WO1998057980A1 PEPTIDES AND COMPOUNDS THAT BIND TO THE IL-5 RECEPTOR 审中-公开
标题翻译：与IL-5受体结合的肽和化合物
公开(公告)号：WO1998057980A1
公开(公告)日：1998-12-23
申请号：PCT/GB1997001618
申请日：1997-06-16
申请人： GLAXO GROUP LIMITED , BARRETT, Ronald, William , ENGLAND, Bruce, Padon , SCHATZ, Peter, Joseph , SLOAN, Derek, Dean , CHEN, Min-Jia
发明人： GLAXO GROUP LIMITED
IPC分类号： C07K07/08
CPC分类号： C40B40/02 , A61K38/00 , C07K7/08 , C07K14/7155 , C12N15/1037
摘要： Described are peptides and peptide mimetics that bind to the IL-5 receptor. Such peptides and peptide mimetics are useful in methods for treating disorders that involve improper production of or response to IL-5 and or the production and accumulation of eosinophils, such as asthma, as well as in diagnostic methods employing labeled peptides and peptide mimetics.
摘要翻译：描述了结合IL-5受体的肽和肽模拟物。这样的肽和肽模拟物可用于治疗涉及IL-5的不适当产生或应答以及嗜酸性粒细胞（例如哮喘）的产生和积累以及使用标记肽和肽模拟物的诊断方法的疾病的方法。

10. 发明申请

WO1998024741A2 PROCESS FOR RESOLVING MIXTURES OF CARBOCYCLIC STEREOISOMERS 审中-公开
标题翻译：用于分解碳化硅立体异构体混合物的方法
公开(公告)号：WO1998024741A2
公开(公告)日：1998-06-11
申请号：PCT/EP1997006782
申请日：1997-12-04
申请人： GLAXO GROUP LIMITED , SICKLES, Barry, Riddle , INGOLD, Kenneth, James , WALLIS, Christopher, John
发明人： GLAXO GROUP LIMITED
IPC分类号： C07B57/00
CPC分类号： C07D209/52 , C07C229/48 , Y02P20/55
摘要： A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilising fractional crystallisation of salts formed with a chiral base; a reducing agent; a protecting group removing agent or a protecting group providing agent.
摘要翻译：制备式（I），（I'），（IIA'），（IIB'），（VA'）和（VB'）的碳环立体异构体的方法，包括对映体纯（IIA'），（I）和（I'）利用与手性碱形成的盐的分级结晶; 还原剂; 保护基团除去剂或保护基团提供剂。

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