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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO1998017382A1 SYSTEM AND METHODS FOR PARALLEL SYNTHESIS OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物并行合成的系统与方法
公开(公告)号：WO1998017382A1
公开(公告)日：1998-04-30
申请号：PCT/EP1997005827
申请日：1997-10-22
申请人： GLAXO GROUP LIMITED , ANTONENKO, Valery Viktorovich , KULIKOV, Nicolay Valintovich , JACOBS, Jeffrey, William
发明人： GLAXO GROUP LIMITED
IPC分类号： B01J19/00
CPC分类号： B01L3/5025 , B01J19/0046 , B01J2219/00286 , B01J2219/00308 , B01J2219/0031 , B01J2219/00313 , B01J2219/00315 , B01J2219/00319 , B01J2219/00351 , B01J2219/00416 , B01J2219/00418 , B01J2219/00423 , B01J2219/00454 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , Y10T436/25 , Y10T436/255
摘要： The invention provides systems, devices and methods for synthesizing various chemicals onto solid supports, cleaving the synthesized compounds and preparing samples for analysis. In one exemplary embodiment, the invention provides a device (10) comprising a housing (12) which defines an enclosure (18). A plate (20) having a plurality of wells (22) has a bottom end (26) and at least some of the wells (22) have a hole in the bottom end. A pressure source is in fluid communication with the holes in the bottom ends (26) of the wells (22). In this manner, a fluid may be maintained within the wells (22) by application of pressure from the pressure source.
摘要翻译：本发明提供了用于将各种化学物质合成到固体支持物上的裂解合成化合物并制备用于分析的样品的系统，装置和方法。在一个示例性实施例中，本发明提供一种包括限定外壳（18）的壳体（12）的装置（10）。具有多个孔（22）的板（20）具有底端（26），并且至少一些井（22）在底端具有孔。压力源与孔（22）的底端（26）中的孔流体连通。以这种方式，通过施加来自压力源的压力，可以在孔（22）内保持流体。

6. 发明申请

WO1998002438A1 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：双相异构化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：WO1998002438A1
公开(公告)日：1998-01-22
申请号：PCT/EP1997003674
申请日：1997-07-11
申请人： GLAXO GROUP LIMITED , COCKERILL, George, Stuart , CARTER, Malcolm, Clive , GUNTRIP, Stephen, Barry , SMITH, Kathryn, Jane
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D493/08 , C07D209/08 , C07D231/56 , C07D235/08 , C07D401/06 , C07D407/12 , C07D471/04
摘要： Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R group and is optionally substituted by at least one indepenently selected R group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是式（I）的取代的双环杂芳族化合物，其中X是N或CH; A表示稠合的5,6或7元杂环，其含有1至5个可以相同或不同的杂原子，并且其选自N，O或S（O）m，其中m如上定义，杂环包含总共1,2或3个双键，包括其所融合的吡啶或嘧啶环中的键，条件是杂环不形成嘌呤的一部分，并且稠合杂环不含两个相邻的O或S（O）m原子。 U表示5至10元单环或双环系，其中一个或多个碳原子任选被独立地选自N，O和S（O）m的杂原子取代，其中m为0,1或2，以及其中所述环系被至少一个独立选择的R 6基团取代，并且任选地被至少一个独立选择的R 4基团取代，条件是U不表示苯基; 是蛋白酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

7. 发明申请

WO1997049411A1 COMBINATIONS COMPRISING VX478, ZIDOVUDINE, FTC AND/OR 3TC FOR USE IN THE TREATMENT OF HIV 审中-公开
标题翻译：包含VX478，ZIDOVUDINE，FTC和/或3TC用于治疗艾滋病毒的组合
公开(公告)号：WO1997049411A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003247
申请日：1997-06-23
申请人： GLAXO GROUP LIMITED , ST. CLAIR, Martha, Heider , BARRY, David, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/70
CPC分类号： A61K31/506 , A61K31/34 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： The present invention relates to therapeutic combinations of 3S-[3R*(1R*,2S*)-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phenyl-methyl)propyl]carbamic acid, tetrahydro-3-furanyl ester (141W94), 3'-azido-3'-déoxythymidine (zidovudine) and (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (3TC) (or, alternatively to 3TC, (2R,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (FTC)) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.
摘要翻译：本发明涉及3S- [3R *（1R *，2S *） - [3 - [[（4-氨基苯基）磺酰基]（2-甲基丙基） - 氨基] -2-羟基-1-苯基 - 甲基）丙基]氨基甲酸，四氢-3-呋喃基酯（141W94），3'-叠氮基-3'-二氧基胸苷（齐多夫定）和（2R，顺式）-4-氨基-1-（2-羟甲基-1,3 - 亚硫杂环戊烷-5-基） - （1H） - 嘧啶-2-酮（3TC）（或者替代为3TC，（2R，顺式）-4-氨基-5-氟-1-（2-羟甲基-1,1- 3-氧硫杂环戊烷-5-基） - （1H） - 嘧啶-2-酮（FTC）），其具有抗HIV活性。本发明还涉及含有所述组合的药物组合物及其在治疗HIV感染中的用途，包括具有对核苷和/或非核苷抑制剂具有抗性的HIV突变体的感染。

8. 发明申请

WO1997046238A1 MEDICAMENTS FOR AMELIORATING ENDOTHELIAL CELL ACTIVATION 审中-公开
标题翻译：用于改善内皮细胞活化的药物
公开(公告)号：WO1997046238A1
公开(公告)日：1997-12-11
申请号：PCT/GB1997001521
申请日：1997-06-06
申请人： GLAXO GROUP LIMITED , COMINACINI, Luciano
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/425
CPC分类号： A61K31/427
摘要： The use of a compound of formula (I) in which: R and R are the same or different and each represents a hydrogen atom or a C1 - C5 alkyl group; R represents a hydrogen atom, a C1 - C6 aliphatic acyl group, a (C5 - C7 cycloalkane) carbonyl group, an aromatic acyl group which is a benzoyl or naphthoyl group optionally with one or more nitro, amino, alkylamino, dialkylamino, alkoxy, halo, alkyl or hydroxy substituents, a heterocyclic acyl group having one or more oxygen, sulphur or nitrogen hetero atoms and with 4 to 7 ring atoms, an optionally halo-substituted phenylacetyl or phenylpropionyl group, a cinnamoyl group, a (C1 - C6 alkoxy) carbonyl group or a benzoyloxycarbonyl group; R and R are the same or different and each represents a hydrogen atom, a C1 - C5 alkyl group or a C1 - C5 alkoxy group, or R and R together represent a C1 - C4 alkylenedioxy group; n is 1, 2 or 3; W represents the -CH2, > CO or > CH-OR group (in which R represents any one of the atoms or groups defined for R and may by the same as or different from R ); and Y and Z are the same or different and each represents an oxygen atom or an imino (=NH) group; or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the amelioration of inappropriate endothelial cell activation.
摘要翻译：使用式（I）化合物，其中：R 1和R 2相同或不同，各自表示氢原子或C 1 -C 5烷基; R 3表示氢原子，C 1 -C 6脂族酰基，（C 5 -C 7环烷烃）羰基，任选具有一个或多个硝基，氨基，烷基氨基，二烷基氨基的苯甲酰基或萘甲酰基的芳族酰基烷氧基，卤素，烷基或羟基取代基，具有一个或多个氧，硫或氮杂原子和具有4至7个环原子的杂环酰基，任选的卤代取代的苯乙酰基或苯基丙酰基，肉桂酰基，（C1 C6烷氧基）羰基或苯甲酰氧基羰基; R 4和R 5相同或不同，各自表示氢原子，C 1 -C 5烷基或C 1 -C 5烷氧基，或者R 4和R 5一起代表C1- C4亚烷基二氧基; n为1,2或3; W表示-CH 2，> CO或> CH-OR 6基团（其中R 6表示对R 3定义的任何一个原子或基团，并且可以与R 3相同或不同） >）; Y和Z相同或不同，各自表示氧原子或亚氨基（= NH）基团; 或其药学上可接受的盐，用于制备用于改善不适当的内皮细胞活化的药物。

9. 发明申请

WO1997043300A1 ADENOSINE DERIVATIVES 审中-公开
标题翻译：腺苷衍生物
公开(公告)号：WO1997043300A1
公开(公告)日：1997-11-20
申请号：PCT/EP1997002403
申请日：1997-05-13
申请人： GLAXO GROUP LIMITED , ELLIS, Frank , SWANSON, Stephen , COUSINS, Richard, Peter, Charles , COX, Brian , PENNELL, Andrew, Michael, Kenneth , ELDRED, Colin, David
发明人： GLAXO GROUP LIMITED
IPC分类号： C07H19/16
CPC分类号： C07H15/04 , C07H19/16
摘要： A compound of formula (I) wherein R represents phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, -CO2R , -CONR R , -COR , -SOR , -SO2R , -SO3H, -SO2NR R , -OR , -NHSO2R , -NHCOR and -NR R ; R represents a C1-6alkyl or C3-6alkenyl group; R represents C1-3alkyl; R and R may each independently represent hydrogen or C1-3alkyl or, when -NR R is directly attached to said phenyl, R and R together with the nitrogen atom may form a 5- or 6- membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C1-3alkyl; R represents C1-3alkyl; and salts and solvates thereof.
摘要翻译：式（I）化合物，其中R 1表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R a，-CONR a R a，，-COR a，-SOR c，-SO 2 R c，-SO 3 H，-SO 2 NR a R b，-OR a，-NHSO 2 R c，-NHCOR a和 -NR - [R的; R 2表示C 1-6烷基或C 3-6烯基; R 3表示C 1-3烷基; R a和R b可各自独立地表示氢或C 1-3烷基，或当-NR a R a直接连接到所述苯基时，R a和R b与氮原子可以形成任选地含有选自氧或氮的第二杂原子的5-或6-元杂环，该第二氮杂原子可以任选地被氢或C 1-3烷基进一步取代; R c表示C 1-3烷基; 及其盐和溶剂合物。

10. 发明申请

WO1997042337A1 GENE EXPRESSION IN MONOCYTES AND MACROPHAGES 审中-公开
标题翻译：基因表达在单核细胞和巨噬细胞中的表达
公开(公告)号：WO1997042337A1
公开(公告)日：1997-11-13
申请号：PCT/GB1997001209
申请日：1997-05-02
申请人： GLAXO GROUP LIMITED , GREAVES, David, Robert
发明人： GLAXO GROUP LIMITED
IPC分类号： C12N15/86
CPC分类号： C12N15/85 , C07K14/70596 , C12N2830/00 , C12N2830/85
摘要： The invention provides a cloned polynucleotide having the function of a transcriptional regulatory sequence (trs) and comprising: (a) a polynucleotide fragment having at least 70 % identity to the polynucleotide of SEQ ID NO. 2; (b) a polynucleotide which is complementary to the polynucleotide of (a); or (c) a polynucleotide comprising at least 15 sequential bases of the polynucleotide of (a) or (b).
摘要翻译：本发明提供了具有转录调节序列（trs）功能的克隆多核苷酸，其包含：（a）与SEQ ID NO：1的多核苷酸具有至少70％同一性的多核苷酸片段。 2; （b）与（a）的多核苷酸互补的多核苷酸; 或（c）包含（a）或（b）的多核苷酸的至少15个连续碱基的多核苷酸。

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