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111. 发明申请

WO1993020807A1 AMINES AS INHIBITORS OF SQUALENE SYNTHASE 审中-公开
标题翻译：作为平均合成酶的抑制剂的氨基酸
公开(公告)号：WO1993020807A1
公开(公告)日：1993-10-28
申请号：PCT/GB1993000742
申请日：1993-04-08
申请人： HARRISON, Alison +hf , ZENECA LIMITED , BROWN, George, Robert , EAKIN, Murdoch, Allan , MALLION, Keith, Blakeney
发明人： HARRISON, Alison +hf , ZENECA LIMITED , HARRISON, Peter, John +di
IPC分类号： A61K31/135
CPC分类号： C07D295/088 , A61K31/135 , C07C217/18 , C07C217/20 , C07C217/22 , C07C233/25 , C07C235/34 , C07C251/48 , C07C255/54 , C07C275/34 , C07C311/29 , C07C317/22 , C07C323/20 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , Y10S514/824
摘要： Compounds of formula (I), and their pharmaceutically acceptable salts, in which R and R are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR R is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthase and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1和R 2是氢，烷基，环烷基，环烷基烷基，苯基烷基或烯基; 或NR 1 R 2是杂环基; A是任选被烷基取代的三亚甲基，苯环任选被取代基如卤代，烯基，氨基，氰基，脲基，烷基，氨基甲酰基烷基，烷酰基氨基，烷氧基羰基，N-烷基 - 烷酰基氨基，烷酰基及其胺取代; 是角鲨烯合酶的抑制剂，因此可用于治疗胆固醇降低的疾病。除了在医药中使用这些化合物之外，还提及了新化合物，其制备方法和药物组合物。

112. 发明申请

WO1993018000A1 REGIOSELECTIVE SULPHONYLATION OF SUBSTITUTED AROMATIC COMPOUNDS 审中-公开
标题翻译：取代芳族化合物的选择性磺酰化
公开(公告)号：WO1993018000A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000330
申请日：1993-02-17
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , DALEY, Stephen, Trevor, Adrian, Kitchener , RANDLES, Kenneth, Richard , GOTT, Brian, David
IPC分类号： C07C315/04
CPC分类号： C07C315/04 , C07C317/22
摘要： A process for preparing a compound comprising a monocyclic aromatic ring having at least a first substituent and a substituted sulphonyl group at the position para to said first substituent, the process comprising mixing a reactant comprising the monocyclic aromatic ring with said first substituent and hydrogen in the position of the ring para to said first substituent, with a sulphonic acid halide derivative in the presence of a naturally occurring or synthetic zeolite capable of catalysing a sulphonylation reaction between said reactant and said sulphonic acid halide, under conditions in which said reaction will occur.
摘要翻译：一种制备包含在所述第一取代基的对位具有至少第一取代基和取代的磺酰基的单环芳环的化合物的方法，该方法包括将包含单环芳香环的反应物与所述第一取代基和在所述反应将发生的条件下，在存在可在所述反应物和所述磺酸卤化物之间进行磺酰化反应的天然存在或合成的沸石的存在下，所述第一取代基的环对位的位置与磺酸卤衍生物反应。

113. 发明申请

WO1993015078A1 CARBAPENEMS CONTAINING A CARBOXY SUBSTITUTED PHENYL GROUP, PROCESSES FOR THEIR PREPARATION, INTERMEDIATES AND USE AS ANTIBIOTICS 审中-公开
标题翻译：含有羧基取代苯基的碳水化合物，其制备方法，中间体和用作抗生素
公开(公告)号：WO1993015078A1
公开(公告)日：1993-08-05
申请号：PCT/GB1993000217
申请日：1993-02-02
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BETTS, Michael, John , DAVIES, Gareth, Morse , SWAIN, Michael, Lingard
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , A61K31/40 , A61K31/407 , A61K31/41 , C07D207/16 , C07D403/12 , C07F9/568
摘要： The present invention relates to carbapenems and provides a compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; R and R are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N-C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n- wherein n is zero, one or two; with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to -NR -. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及碳青霉烯并提供式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中：R 1是1-羟基乙基，1-氟乙基或羟甲基; R 2是氢或C 1-4烷基; R 3是氢或C 1-4烷基; R 4和R 5相同或不同，选自氢，卤素，氰基，C 1-4烷基，硝基，羟基，羧基，C 1-4烷氧基，C 1-4烷氧基羰基，氨基磺酰基，C 1-4烷基氨基磺酰基， C 1-4烷基氨基磺酰基，氨基甲酰基，C 1-4烷基氨基甲酰基，二-C 1-4烷基氨基甲酰基，三氟甲基，磺酸，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，C 1-4烷酰基氨基，C 1-4烷酰基（N-C 1-4烷基）氨基，C 1 -4烷基磺酰氨基和C 1-4烷基S（O）n - ，其中n为0，一个或两个; 条件是在与-NR 3 - 的连接相邻的位置处不存在羟基或羧基取代基。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。

114. 发明申请

WO1993014212A1 TRANSGENIC PLANTS WITH INCREASED SOLIDS CONTENT 审中-公开
标题翻译：具有增加固体含量的转基因植物
公开(公告)号：WO1993014212A1
公开(公告)日：1993-07-22
申请号：PCT/GB1993000021
申请日：1993-01-08
申请人： ZENECA LIMITED , BIRD, Colin, Roger , BONIWELL, Jeremy, Michael
发明人： ZENECA LIMITED
IPC分类号： C12N15/82
CPC分类号： C12N15/8249 , A01H5/08 , A23L19/03 , A23L19/09 , C07K14/415
摘要： A method is provided for making fruit (particularly tomatoes) having increased solids content which comprises cultivating fruit-bearing plants in which expression of genes homologous to pTOM36 is at least partially inhibited. For this purpose the fruit may be transformed with DNA constructs comprising a DNA sequence homologous to some or all of the genes encoded by the clone pTOM36. The clone is adapted to generate sense or antisense RNA under control of a plant promoter.
摘要翻译：提供了一种用于制备具有增加的固体含量的水果（特别是西红柿）的方法，其包括培育其中与pTOM36同源的基因的表达至少部分被抑制的含果实植物。为此，可以用包含与由克隆pTOM36编码的一些或全部基因同源的DNA序列的DNA构建体来转化果实。该克隆适于在植物启动子的控制下产生正义或反义RNA。

115. 发明申请

WO2001007639A2 SELECTABLE MARKER GENE 审中-公开
标题翻译：可选标记基因
公开(公告)号：WO2001007639A2
公开(公告)日：2001-02-01
申请号：PCT/GB2000002673
申请日：2000-07-12
申请人： ZENECA LIMITED , SKIPSEY, Mark , EDWARDS, Robert
发明人： ZENECA LIMITED
IPC分类号： C12Q1/00
CPC分类号： C12N15/8274 , C12N9/88 , C12N15/8209
摘要： A method of selecting transformed cells comprising stably transforming the genome of the cell with a nucleic acid encoding a glyoxalase I protein and subjecting the cell to a selective agent comprising a normally toxic agent which is toxic to untransformed cells but is capable of being degraded by the glyoxalase thereby eliminating the toxicity of the agent to the transformed cell.
摘要翻译：一种选择转化细胞的方法，包括用编码乙二醛酶I蛋白质的核酸稳定转化细胞基因组，并对细胞进行选择性试剂，该选择剂包含对未转化细胞有毒的正常毒性试剂，但能够被乙二醛酶，从而消除了药剂对转化细胞的毒性。

116. 发明申请

WO1998028283A1 PROCESS FOR MAKING BENZISOTHIAZOLIN-3-ONES 审中-公开
标题翻译：制备苯扎氯唑啉-3-酮的方法
公开(公告)号：WO1998028283A1
公开(公告)日：1998-07-02
申请号：PCT/GB1997003130
申请日：1997-11-13
申请人： ZENECA LIMITED , COX, Brian, Geoffrey , GRAY, Thomas
发明人： ZENECA LIMITED
IPC分类号： C07D275/04
CPC分类号： C07D275/04
摘要： A process for making a 1,2-benzisothiazolin-3-one by cycling a bisamide precursor under alkaline conditions in the presence of oxygen or an oxygen-release compound in the presence of a nitrogen, sulphur or phosphorus nucleophile. Preferred nucleophiles are ammonia, primary, secondary and tertiary amines, amides, pyridines and quinolines.
摘要翻译：在氮，硫或磷亲核试剂存在下，在氧气或脱氧化合物存在下，在碱性条件下循环双酰胺前体，制备1,2-苯并异噻唑啉-3-酮的方法。优选的亲核试剂是氨，伯，仲和叔胺，酰胺，吡啶和喹啉。

117. 发明申请

WO1998025890A1 PROCESS FOR THE PRODUCTION OF SULPHONAMIDES 审中-公开
标题翻译：生产磺化胺的方法
公开(公告)号：WO1998025890A1
公开(公告)日：1998-06-18
申请号：PCT/GB1997003272
申请日：1997-11-27
申请人： ZENECA LIMITED , BROWN, Stephen, Martin , MUXWORTHY, James, Peter , GOTT, Brian, David
发明人： ZENECA LIMITED
IPC分类号： C07C303/38
CPC分类号： C07C303/38 , C07C311/03
摘要： A process for the preparation of a sulphonamide of formula: RSO2NR R wherein R represents C1-C10 alkyl or C6-C10 aryl; and R and R independently represent hydrogen, C1-C10 alkyl or C6-C10 aryl; which comprises reacting the corresponding alkane- or arenesulphonyl halide of formula: RSO2Hal wherein Hal represents halogen; with the corresponding compound of formula: NHR R in an aqueous solvent and extracting the sulphonamide from the resulting mixture into a polar organic solvent.
摘要翻译：一种制备下式的磺酰胺的方法：其中R代表C1-C10烷基或C6-C10芳基; R 1和R 2独立地表示氢，C 1 -C 10烷基或C 6 -C 10芳基; 其包括使相应的式：RSO 2 Hal的烷烃或芳烃磺酰卤反应，其中Hal表示卤素; 与相应的式NHR 1 R 2化合物反应，并将所得混合物中的磺酰胺萃取到极性有机溶剂中。

118. 发明申请

WO1998022103A1 RAF KINASE INHIBITORS 审中-公开
标题翻译： RAF激酶抑制剂
公开(公告)号：WO1998022103A1
公开(公告)日：1998-05-28
申请号：PCT/GB1997003102
申请日：1997-11-12
申请人： ZENECA LIMITED , HEDGE, Philip, John , BOYLE, Francis, Thomas
发明人： ZENECA LIMITED
IPC分类号： A61K31/165
CPC分类号： A61K31/222 , A61K31/167 , A61K31/235 , C07C235/56
摘要： 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.
摘要翻译：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。

119. 发明申请

WO1998019784A1 DISPERSANTS 审中-公开
标题翻译：分散剂
公开(公告)号：WO1998019784A1
公开(公告)日：1998-05-14
申请号：PCT/GB1997002698
申请日：1997-10-01
申请人： ZENECA LIMITED , THETFORD, Dean , SCHOFIELD, John, David , SUNDERLAND, Patrick, John
发明人： ZENECA LIMITED
IPC分类号： B01F17/00
CPC分类号： C08G63/08 , B01F17/0028 , B01F17/005 , B01F17/0057 , B01F17/0064 , C09D7/45 , C09D17/002
摘要： 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.
摘要翻译：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。

120. 发明申请

WO1998017680A1 PEPTIDE ANALOGUES CONTAINING A 7-MEMBERED LACTAM RING 审中-公开
标题翻译：含有7个成员的LACTAM环的肽类似物
公开(公告)号：WO1998017680A1
公开(公告)日：1998-04-30
申请号：PCT/GB1997002837
申请日：1997-10-14
申请人： ZENECA LIMITED , LUKE, Richard, William, Arthur , COTTON, Ronald
发明人： ZENECA LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , Y10S424/81
摘要： The invention concerns pharmaceutically useful peptide derivatives of the formula (I), P-R -R -R -R , in which P, R , R , R , and R have the various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.
摘要翻译：本发明涉及式（I）PR 1 -R 2 -R 3 -R 4的药用有用肽衍生物，其中P，R 1，R 2，R 3， 3＆gt;和R 4具有本文定义的各种含义及其药学上可接受的盐和含有它们的药物组合物。新型肽衍生物在治疗MHC II类依赖性T细胞介导的自身免疫性或炎性疾病如类风湿性关节炎中是有价值的。本发明还涉及制备新型肽衍生物的方法和该化合物在医疗中的用途。

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