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    • 111. 发明申请
    • RAF KINASE INHIBITORS
    • RAF激酶抑制剂
    • WO1998022103A1
    • 1998-05-28
    • PCT/GB1997003102
    • 1997-11-12
    • ZENECA LIMITEDHEDGE, Philip, JohnBOYLE, Francis, Thomas
    • ZENECA LIMITED
    • A61K31/165
    • A61K31/222A61K31/167A61K31/235C07C235/56
    • The present invention relates to pharmaceutical compositions comprising inhibitors of raf kinase of formula (I) wherein: R and R are substituents on the phenyl rings; p, which may take the same or different values for R and R , is 0-3, and when p is 2 or 3 each group may be the same or different; R is C1-4alkyl; q is 0-4; R is aryl or cycloalkyl wherein R is optionally substituted with up to 3 substituents or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof and a pharmaceutically acceptable carrier with the proviso that N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-hydroxybenzamide, N -[5-(3-cyclopentylpropionylamino)-2-methylphenyl]-4-acetoxybenzamide, N -[5-(3-phenylpropionylamino)-2-methylphenyl]-4-acetoxybenzamide, N -[5-(4-cyclohexylbutyrylamino)-2-methylphenyl]-4-acetoxybenzamide, N -[5-(2-cyclohexylacetylamino)-2-methylphenyl]-4-acetoxybenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-aminobenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-nitrobenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-hydroxymethylbenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-methoxycarbonylbenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-2-hydroxybenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-3-hydroxybenzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]benzamide, N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-acetoxybenzamide and N -[5-(3-cyclohexylpropionylamino)-2-methylphenyl]-4-hydroxybenzamide are excluded. Processes for their preparation and their use as therapeutic agents. A particular use is in cancer therapy.
    • 本发明涉及包含式(I)的raf激酶抑制剂的药物组合物,其中:R 1和R 2是苯环上的取代基; 对于R 1和R 2可以具有相同或不同的值的p为0-3,当p为2或3时,每个基团可以相同或不同; R 3是C 1-4烷基; q为0-4; R 4是芳基或环烷基,其中R 4任选被至多3个取代基或其药学上可接受的盐或体内可水解的酯和药学上可接受的载体取代,条件是N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -4-羟基苯甲酰胺,N - [5-(3-环戊基丙酰基氨基)-2-甲基苯基] -4-乙酰氧基苯甲酰胺, [5-(3-苯基丙酰基氨基)-2-甲基苯基] -4-乙酰氧基苯甲酰胺,N - [5-(4-环己基丁酰基氨基)-2-甲基苯基] -4-乙酰氧基苯甲酰胺, N - [5-(2-环己基乙酰基氨基)-2-甲基苯基] -4-乙酰氧基苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -4 - 氨基苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -4-硝基苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2- 甲基苯基] -4-羟甲基苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -4-甲氧基羰基苯甲酰胺,N - [5-(3-环己基丙酰基氨基 )-2-甲基苯基] -2- hydroxybenzami de,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -3-羟基苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基 ]苯甲酰胺,N - [5-(3-环己基丙酰基氨基)-2-甲基苯基] -4-乙酰氧基苯甲酰胺和N - [5-(3-环己基丙酰基氨基)-2- 甲基苯基] -4-羟基苯甲酰胺。 其制备方法及其用作治疗剂。 一个特别的用途是癌症治疗。
    • 112. 发明申请
    • DISPERSANTS
    • 分散剂
    • WO1998019784A1
    • 1998-05-14
    • PCT/GB1997002698
    • 1997-10-01
    • ZENECA LIMITEDTHETFORD, DeanSCHOFIELD, John, DavidSUNDERLAND, Patrick, John
    • ZENECA LIMITED
    • B01F17/00
    • C08G63/08B01F17/0028B01F17/005B01F17/0057B01F17/0064C09D7/45C09D17/002
    • A dispersant of general Formula (1) wherein T is hydrogen or a polymerisation terminating group; Z is an acidic or basic group or a moiety containing either an acidic or basic group; A and B are each, independently, oxyalkylene carbonyl groups derivable from delta -valerolactone, ELEMENT -caprolactone or alkyl substituted ELEMENT -caprolactone provided that both are not ELEMENT -caprolactone or delta -valerolactone; n and p are integers; and n + p is from 2 to 100; including salts thereof. Specific examples of dispersants are the reaction product of lauric acid, ELEMENT -caprolactone, 7-methyl- ELEMENT -caprolactone with PEI, the reaction product of lauric acid, ELEMENT -caprolactone, delta -valerolactone with PEI and the phosphate of the reaction product of dodecanol, ELEMENT -caprolactone and delta -valerolactone.
    • 通式(1)的分散剂,其中T是氢或聚合端基; Z是酸性或碱性基团或含有酸性或碱性基团的部分; A和B各自独立地是衍生自δ-戊内酯,ELEMENT-己内酯或烷基取代的ELEMENT-己内酯的氧化烯羰基,条件是两者都不是ELEMENT-己内酯或δ-戊内酯; n和p是整数; n + p为2〜100; 包括其盐。 分散剂的具体实例是月桂酸,ELEMENT-己内酯,7-甲基-1-己内酯与PEI的反应产物,月桂酸,ELEMENT-己内酯,δ-戊内酯与PEI的反应产物和反应产物的磷酸酯 十二烷醇,ELEMENT-己内酯和δ-戊内酯。
    • 115. 发明申请
    • SULFONAMIDES
    • 磺胺类药物
    • WO1998007742A1
    • 1998-02-26
    • PCT/GB1997002222
    • 1997-08-19
    • ZENECA LIMITEDZENECA-PHARMA S.A.BARLAAM, Bernard, Christophe
    • ZENECA LIMITEDZENECA-PHARMA S.A.
    • C07K05/06
    • C07D213/70C07C311/19C07C311/29C07C311/42C07C311/46C07D209/34C07D215/36C07D217/02C07D233/84C07D239/88C07D261/10C07D271/12C07D277/54C07D333/34C07D409/04
    • Compounds of formula (I) wherein R is aryl, heterocyclyl or heteroaryl; R is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R is C1-6alkyl, C2-6alkenyl, aryl, C1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R is hydrogen or C1-6alkyl; or R and R together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R -R , is optionally substituted; or pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumor Necrosis Factor and/or one or more matrix metalloproteinase enzymes. Compositions containing them and their preparation are also described.
    • 式(I)的化合物,其中R 1是芳基,杂环基或杂芳基; R 2是氢,C 1-8烷基,C 2-6烯基,C 2-6炔基,C 3-8环烷基,杂芳基,杂环基,芳基C 1-6烷基,杂芳基C 1-6烷基,杂环基C 1-6烷基或C 3-8环烷基C 1-6烷基; R 3是C 1-6烷基,C 2-6烯基,芳基,C 1-6烷基,杂芳基C 1-6烷基或天然存在的氨基酸的侧链; R 4是氢,C 1-6烷基,C 3-8环烷基,C 4-8环烯基,芳基C 1-6烷基,杂芳基C 1-6烷基或杂环基C 1-6烷基; R 5是氢或C 1-6烷基; 或R 4和R 5与它们所连接的氮原子一起形成杂环; 其中R 1 -R 5中的任何基团或环任选被取代; 或其药学上可接受的盐或体内可水解的酯被描述为产生肿瘤坏死因子和/或一种或多种基质金属蛋白酶的抑制剂。 还描述了含有它们的组合物及其制备方法。
    • 116. 发明申请
    • CELL ADHESION INHIBITING COMPOUNDS
    • 细胞粘附抑制化合物
    • WO1997049731A1
    • 1997-12-31
    • PCT/GB1997001641
    • 1997-06-18
    • ZENECA LIMITEDDUTTA, Anand, Swaroop
    • ZENECA LIMITED
    • C07K14/78
    • C07K14/78A61K38/00Y10S514/863
    • Cyclic peptide of formula (I) where Xaa1 is selected from L-amino acids selected from Phe, Lys and Arg; D-amino acids selected from Phe and Met, the L- and D-amino acid optionally substituted on its alpha -carbon or its alpha -amino group with a C1-4 alkyl group; and MeIle; Xaa2, Xaa3 et Xaa4 are respectively Leu, Asp and Val, optionally substituted on their alpha -carbon or alpha -amino group with a C1-4 alkyl group; X is selected from D-amino acids selected from Ala, Phe, Arg, Lys, Trp, hArg(Et)2, Orn(CHMe2), Orn(Me2), Lys(CHMe2) and Arg(Pmc), optionally substituted on their alpha -carbon or alpha -amino group with a C1-4 alkyl group; Formula (II); NH(CH2)5CO; and NH(CH2)2S(CH2)yCO, where y is 1 or 2; X is selected from D-amino acids selected from Ala, Arg, Lys, His, hArg(Et)2, Orn(CHMe2), and Orn(Me2), optionally substituted on their alpha -carbon or alpha -amino group with a C1-4 alkyl group; NH(CH2)2SCH2CO; and NH(CH2)xCO, where x is 2 or 3; Xaa5 and Xaa6 are each independently a D-amino acid selected from Ala and Arg, optionally substituted on its alpha -carbon or alpha -amino group with a C1-4 alkyl group; p is 0 or 1; and q is 0 or when p is 1, q is 0 or 1; or a salt thereof. The cyclic peptides inhibit the interaction of vascular cell adhesion molecule-1 and fibronectin with integrin very late antigen 4 ( alpha 4 beta 1) and of mucosal addressin cell adhesion molecule -1 (MAdCAM-1) with integrin alpha 4 beta 7. They have therapeutic applications such as in rheumatoid arthritis, multiple sclerosis, asthma, psoriasis, inflammatory bowel disease and insulin-dependent diabetes.
    • 式(I)的环肽,其中Xaa1选自Phe,Lys和Arg的L-氨基酸; 选自Phe和Met的D-氨基酸,任选地在其α-碳或其α-氨基上被C 1-4烷基取代的L-和D-氨基酸; 和MeIle; Xaa2,Xaa3和Xaa4分别为Leu,Asp和Val,任选地在其具有C 1-4烷基的α-碳或α-氨基上取代; X 1选自Ala,Phe,Arg,Lys,Trp,hArg(Et)2,Orn(CHMe2),Orn(Me2),Lys(CHMe2)和Arg(Pmc)中的D-氨基酸, 在其α-碳或α-氨基上被C 1-4烷基取代; 式(II); NH(CH2)5CO; 和NH(CH 2)2 S(CH 2)y CO,其中y为1或2; X 2选自选自Ala,Arg,Lys,His,hArg(Et)2,Orn(CHMe2)和Orn(Me2)的D-氨基酸,任选地在它们的α-碳或α-氨基上取代 与C 1-4烷基; NH(CH 2)2SCH2CO; 和NH(CH 2)x CO,其中x为2或3; Xaa5和Xaa6各自独立地是选自Ala和Arg的D-氨基酸,任选地在其α-碳或α-氨基上被C 1-4烷基取代; p为0或1; q为0或当p为1时,q为0或1; 或其盐。 环肽可以抑制血管细胞粘附分子-1与纤维连接蛋白与整合素非常晚的抗原4(α4β1)和粘膜定位素细胞粘附分子-1(MAdCAM-1)与整合素α4β7的相互作用。它们具有 治疗应用如类风湿性关节炎,多发性硬化,哮喘,牛皮癣,炎性肠病和胰岛素依赖性糖尿病。
    • 118. 发明申请
    • MICROENCAPSULATED COMPOSITIONS
    • 微胶囊化组合物
    • WO1997044125A1
    • 1997-11-27
    • PCT/GB1997001370
    • 1997-05-19
    • ZENECA LIMITED
    • ZENECA LIMITEDCHEN, Jin, LingLEE, Kuo-ShinRODSON, MariusSCHER, Herbert, Benson
    • B01J13/16
    • A01N43/40A01N25/28A01N53/00A01N2300/00
    • Polyurea microcapsules particularly suitable for foliar application are prepared by an interfacial polymerization process in which the polyurea is formed from an aromatic diisocyanate and optionally an aromatic polyisocyanate having 3 or more isocyanate groups, in a weight ratio (when both types of isocyanate are present) of polyisocyanate:diisocyanate of from about 1:100 to about 1:15, and in which the microcapsules are produced having an average particle size of from about 1 to about 5 microns. As compared to conventional liquid (e.g., emulsifiable concentrate) compositions of pesticides, the microcapsules can provide safer handling and higher loading of active ingredients, while providing substantially equivalent biological activity to the liquid compositions.
    • 特别适用于叶面施用的聚脲微胶囊通过界面聚合方法制备,其中聚脲由芳族二异氰酸酯和任选的具有3个或更多个异氰酸酯基团的芳族多异氰酸酯形成,其重量比(当存在两种类型的异氰酸酯时)为 多异氰酸酯:约1:100至约1:15的二异氰酸酯,其中制备平均粒度为约1至约5微米的微胶囊。 与常规液体(例如可乳化浓缩物)农药组合物相比,微胶囊可以提供更安全的处理和更高的活性成分负载,同时为液体组合物提供基本相同的生物活性。
    • 120. 发明申请
    • QUINAZOLINE DERIVATIVES
    • 喹诺酮衍生物
    • WO1997038994A1
    • 1997-10-23
    • PCT/GB1997000970
    • 1997-04-08
    • ZENECA LIMITED
    • ZENECA LIMITEDGIBSON, Keith, Hopkinson
    • C07D405/12
    • C07D405/12
    • The invention concerns quinazoline derivatives of formula (I) wherein n is 1, 2 or 3 and each R is independently halogeno, trifluoromethyl or (1-4C)alkyl; R is (1-4C)alkoxy; A is (1-4C)alkylene; and Q is a saturated, monocyclic 4-, 5-, 6- or 7-membered heterocyclic ring containing one or two oxygen heteroatoms, which ring optionally bears up to four (1-4C)alkyl substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
    • 本发明涉及式(I)的喹唑啉衍生物,其中n为1,2或3,并且每个R 2独立地为卤代,三氟甲基或(1-4C)烷基; R 1是(1-4C)烷氧基; A是(1-4C)亚烷基; 并且Q是含有一个或两个氧杂原子的饱和的单环4-,5-,6-或7-元杂环,其任选地带有多达四个(1-4C)烷基取代基; 或其药学上可接受的盐; 其制备方法,含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。