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    • 5. 发明申请
    • BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
    • 双相异构化合物作为蛋白酪氨酸激酶抑制剂
    • WO1998002438A1
    • 1998-01-22
    • PCT/EP1997003674
    • 1997-07-11
    • GLAXO GROUP LIMITEDCOCKERILL, George, StuartCARTER, Malcolm, CliveGUNTRIP, Stephen, BarrySMITH, Kathryn, Jane
    • GLAXO GROUP LIMITED
    • C07D471/04
    • C07D493/08C07D209/08C07D231/56C07D235/08C07D401/06C07D407/12C07D471/04
    • 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.
    • 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。
    • 6. 发明申请
    • COMBINATIONS COMPRISING VX478, ZIDOVUDINE, FTC AND/OR 3TC FOR USE IN THE TREATMENT OF HIV
    • 包含VX478,ZIDOVUDINE,FTC和/或3TC用于治疗艾滋病毒的组合
    • WO1997049411A1
    • 1997-12-31
    • PCT/EP1997003247
    • 1997-06-23
    • GLAXO GROUP LIMITEDST. CLAIR, Martha, HeiderBARRY, David, Walter
    • GLAXO GROUP LIMITED
    • A61K31/70
    • A61K31/506A61K31/34A61K31/7072A61K45/06A61K2300/00
    • 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.
    • 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。
    • 7. 发明申请
    • MEDICAMENTS FOR AMELIORATING ENDOTHELIAL CELL ACTIVATION
    • 用于改善内皮细胞活化的药物
    • WO1997046238A1
    • 1997-12-11
    • PCT/GB1997001521
    • 1997-06-06
    • GLAXO GROUP LIMITEDCOMINACINI, Luciano
    • GLAXO GROUP LIMITED
    • A61K31/425
    • A61K31/427
    • 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.
    • 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。