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    • 47. 发明申请
    • STABILISED DYE COMPOSITION
    • 稳定的染料组合物
    • WO1997003132A1
    • 1997-01-30
    • PCT/GB1996001561
    • 1996-06-28
    • ZENECA LIMITEDGREGORY, PeterKENYON, Ronald, WynfordWIGHT, Paul
    • ZENECA LIMITED
    • C09B67/24
    • C09B31/08C09B67/0072
    • A composition of a water-soluble bis-azo dye of formula (1) and an oxidising agent, wherein A is optionally substituted phenyl or optionally substituted naphthyl; B is optionally substituted phenylene or optionally substituted naphthylene; R is H or sulpho; R is H, optionally substituted alkyl, optionally substituted aryl or optionally substituted acyl; R is H, optionally substituted aryl, optionally substituted alkyl or a group, -D-E; D is optionally substituted C2-6-alkylene; and E is a group of formula (1a); R & R each independently is H or optionally substituted alkyl; and R is H, optionally substituted alkyl, optionally substituted aryl or optionally substituted acyl.
    • 式(1)的水溶性双偶氮染料和氧化剂的组合物,其中A是任选取代的苯基或任选取代的萘基; B是任选取代的亚苯基或任选取代的亚萘基; R 1是H或磺基; R 2是H,任选取代的烷基,任选取代的芳基或任选取代的酰基; R 3是H,任选取代的芳基,任选取代的烷基或基团,-D-E; D是任选取代的C 2-6 - 亚烷基; 和E是式(1a)的一组; R 4和R 5各自独立地为H或任选取代的烷基; 且R 6为H,任选取代的烷基,任选取代的芳基或任选取代的酰基。
    • 48. 发明申请
    • PEPTIDE INHIBITORS OF FIBRONECTINE
    • 纤维蛋白抑肽酶
    • WO1997002289A1
    • 1997-01-23
    • PCT/GB1996001580
    • 1996-07-02
    • ZENECA LIMITEDDUTTA, Anand, Swaroop
    • ZENECA LIMITED
    • C07K14/78
    • C07K7/56A61K38/00
    • Cyclic dimeric peptides of formula (1) wherein: peptide 1 and peptide 2 independently represent a tetrapeptide of formula -AA1-AA2-AA3-AA4- juxtaposed in parallel or antiparallel orientation; AA1 is an L or D amino acid selected from Ile, Leu and amino analogues thereof selected from Pro, Gly, Tic and Phe; AA2 is an L amino acid selected from Leu and amino acid analogues thereof selected from Ile, Phe and Val; AA3 is an L amino acid selected from Asp, Glu and amino acid analogues thereof; AA4 is an L amino acid selected from Val and amino acid analogues thereof selected from Leu, Ile, Phe and Cha (cyclohexylalanine); L1 and L2 independently represent linking moieties for linking peptides 1 and 2 to form a cyclic dipeptide; or salts thereof. The cyclic dipeptides inhibit the interaction of vascular cell adhesion molecule-1 and fibronectin with integrin very late antigen 4 and have therapeutic applications such as in rheumatoid arthritis, asthma or multiple sclerosis.
    • 式(1)的环状二聚肽其中:肽1和肽2独立地表示并​​列或反平行取向并入的式-AA1-AA2-AA3-AA4的四肽; AA1是选自Ile,Leu及其选自Pro,Gly,Tic和Phe的氨基类似物的L或D或D 氨基酸; AA2是选自Leu和其选自Ile,Phe和Val的氨基酸类似物的L9氨基酸; AA3是选自Asp,Glu及其氨基酸类似物的一种氨基酸; AA4是选自Val和其氨基酸类似物的选自Leu,Ile,Phe和Cha(环己基丙氨酸)的L9A氨基酸; L1和L2独立地表示用于连接肽1和2的连接部分以形成环状二肽; 或其盐。 环状二肽抑制血管细胞粘附分子-1和纤连蛋白与整联蛋白非常晚的抗原4的相互作用,并具有治疗应用,例如类风湿性关节炎,哮喘或多发性硬化。
    • 49. 发明申请
    • AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 芳香化合物和含有它们的药物组合物
    • WO1997000864A1
    • 1997-01-09
    • PCT/GB1996001443
    • 1996-06-17
    • ZENECA LIMITEDBREAULT, Gloria, Anne
    • ZENECA LIMITED
    • C07D237/24
    • C07D213/80C07D213/82C07D237/18C07D237/24C07D401/04C07D403/04C07D413/04C07D413/12C07D417/12
    • The invention relates to compounds of formula (I), wherein A is an optionally substituted, ring system provided that the -CH(R )N(R )B-R and -OD groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OD linking group (and therefore in the 3-position relative to the -CHR NR linking group) is not substituted; B is an optionally substituted ring system; R is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R )N(R )- linking group and is as defined in the description; R is hydrogen, C1-6alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), (C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R is hydrogen, methyl or ethyl; D is hydrogen, an optionally substituted 5-7 membered carbocyclic ring containing one double bond, C1-3alkyl substituted by an optionally substituted 5-7 membered carbocyclic ring containing one double bond or D is of the formula -(CH2)nCH(R )C(R )=C(R )R and N-oxides of -NR where chemically possible; and S-oxides of sulphur containing rings where chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof; excluding 4-[5-carboxy-2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzoic acid, 5-[2-hydroxybenzylamino]-2-hydroxybenzoic acid, 3-[2,5-dihydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzenecarboxamide, 3-[2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]-2-hydroxybenzoic acid, 4-[hydroxybenzylamino]-2-hydroxybenzoic acid and 4[2-hydroxybenzylamino]benzoic acid. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
    • 本发明涉及式(I)化合物,其中A是任选取代的环系,条件是-CH(R 3)N(R 2)BR 1和-OD基团位于 在环碳原子上彼此相关,并且位于-OD连接基团(因此相对于-CHR 3 NR 2连接基团的3位)的环原子未被取代 ; B是任选取代的环系; R 1与-CH(R 3)N(R 2) - 连接基以1,3或1,4个关系位于环B上,并且如说明书中所定义; R 2是氢,任选被羟基,氰基或三氟甲基取代的C 1-6烷基,C 2-6烯基(提供双键不在1-位),(C 2-6炔基(条件是三键不在 1-位),苯基C 1-3烷基或吡啶基C 1-3烷基; R 3是氢,甲基或乙基; D是氢,任选取代的含有一个双键的5-7元碳环,被任选取代的C 1-3烷基 含有一个双键的5-7元碳环或D具有式 - (CH 2)n CH(R 4)C(R 5)= C(R 6)R 7和N-氧化物 其中化学上可能的是-NR 2,和其中化学可能的含硫环的S-氧化物;及其药学上可接受的盐和体内可水解的酯和酰胺;不包括4- [5-羧基-2-羟基苄基氨基]苯甲酸, 4- [2,5-二羟基苄基氨基]苯甲酸,5- [2-羟基苄基氨基] -2-羟基苯甲酸,3- [2,5-二羟基苄基氨基]苯甲酸,4- [2,5-二羟基苄基氨基]苯甲醛 de,3- [2-羟基苄基氨基]苯甲酸,4- [2,5-二羟基苄基氨基] -2-羟基苯甲酸,4- [羟基苄基氨基] -2-羟基苯甲酸和4 [2-羟基苄基氨基]苯甲酸。 其制备方法,制备中的中间体,作为治疗剂的用途和含有它们的药物组合物。