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151. 发明申请

WO1996037483A1 PROCESS FOR THE PREPARATION OF SUBSTITUTED 5-HYDROXY-OXAZOLIDIN-4-ONE 审中-公开
标题翻译：制备取代的5-羟基 - 恶唑烷-4-酮的方法
公开(公告)号：WO1996037483A1
公开(公告)日：1996-11-28
申请号：PCT/GB1996001149
申请日：1996-05-13
申请人： ZENECA LIMITED , COX, John, Michael , PEARSON, David, Philip, John , KOZAKIEWICZ, Anthony, Marian , MOORE, Richard, Butler , MITCHELL, Glynn , LANGTON, David, William , ELLIS, Russel, Martin
发明人： ZENECA LIMITED
IPC分类号： C07D263/18
CPC分类号： C07D263/18 , C07D263/28
摘要： A process for the synthesis of a compound of general formula (II), wherein: R and R are each independently hydrogen or C1-C4 alkyl; A is an aromatic or heteroaromatic ring system optionally substituted with one or more substituents selected from: halogen or C1-C10 hydrocarbyl, -O(C1-C10 hydrocarbyl), -S(C1-C10 hydrocarbyl), -SO(C1-C10 hydrocarbyl) or -SO2(C1-C10 hydrocarbyl), cyano, nitro, SCN, SiR 3 (where each R is independently C1-C4 alkyl or phenyl), COR , CR NOR , NHOH, ONR R , SF5, COOR , SO2NR R , OR or NR R ; and in which any ring nitrogen atom may be quaternised or oxidised; alternatively, any two substituents of the group A may combine to form a fused 5- or 6-membered saturated or partially saturated carbocyclic or heterocyclic ring in which any carbon or quaternised nitrogen atom may be substituted with any of the groups mentioned above for A or in which a ring carbon atom may be oxidised; R and R are each independently hydrogen or C1-C10 hydrocarbyl; R is hydrogen, C1-C10 hydrocarbyl, SO2(C1-C10 hydrocarbyl), CHO, CO(C1-C10 hydrocarbyl), COO(C1-C10 hydrocarbyl) or CONR R ; R and R are each independently hydrogen, C1-C10 hydrocarbyl, O(C1-C10 hydrocarbyl), SO2(C1-C10 hydrocarbyl), CHO, CO(C1-C10 hydrocarbyl), COO(C1-C10 hydrocarbyl) or CONR R ; any of the hydrocarbyl groups within the group A may optionally be substituted with halogen (i.e. chlorine, bromine, fluorine or iodine), hydroxy, SO2NR R (where R and R are independently H or C1-C6 alkyl), cyano, nitro, amino, mono- and dialkylamino in which the alkyl groups have from 1 to 6 or more carbon atoms, acylamino, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 alkylsulphinyl, C1-C6 alkylsulphonyl, carboxy, carboxyamide, in which the groups attached to the N atom may be hydrogen or lower hydrocarbyl optionally substituted with halogen; alkoxy carbonyl wherein the alkoxy group may have from 1 to 6 or more carbon atoms, or aryl such as phenyl; the process comprising cyclising a compound of general formula (VII); wherein A, R and R are as defined for general formula (II), R is hydrogen, benzyl or benzyl substituted with up to five substituents selected from halo, C1-C6 alkyl, O(C1-C6 alkyl) or nitro and R is C1-C8 alkyl, benzyl or benzyl substituted with up to five of the substituents mentioned above for R .
摘要翻译：一种合成通式（II）化合物的方法，其中：R 2和R 3各自独立地为氢或C 1 -C 4烷基; A是任选被一个或多个选自以下的取代基取代的芳族或杂芳族环系：卤素或C 1 -C 10烃基，-O（C 1 -C 10烃基），-S（C 1 -C 10烃基）， - （C 1 -C 10烃基）或-SO 2（C 1 -C 10烃基），氰基，硝基，SCN，SiR c 3（其中每个R c独立地为C 1 -C 4烷基或苯基），COR 7， 8，NHOH，ONR 7 R 8，SF 5，COOR 7，SO 2 NR 7 R 8，OR 9或NR 10 R 11; 并且其中任何环氮原子可被季铵化或氧化; 可选地，基团A的任何两个取代基可以结合形成稠合的5或6元饱和或部分饱和的碳环或杂环，其中任何碳或季铵化的氮原子可被上述任何A或其中环碳原子可被氧化; R 7和R 8各自独立地为氢或C 1 -C 10烃基; R 9是氢，C 1 -C 10烃基，SO 2（C 1 -C 10烃基），CHO，CO（C 1 -C 10烃基），COO（C 1 -C 10烃基）或CONR 7 R 8; R 10和R 11各自独立地为氢，C 1 -C 10烃基，O（C 1 -C 10烃基），SO 2（C 1 -C 10烃基），CHO，CO（C 1 -C 10烃基）烃基）或CONR 7 R 8; 基团A中的任何烃基可以任选地被卤素（即氯，溴，氟或碘），羟基，SO 2 NR a R b（其中R a和R b独立地是H 或C 1 -C 6烷基），氰基，硝基，氨基，一烷基氨基和二烷基氨基，其中烷基具有1至6个或更多个碳原子，酰基氨基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷硫基，C 1 -C 6烷基亚磺酰基，C 1 -C 6烷基磺酰基，羧基，羧酰胺，其中与N原子连接的基团可以是氢或任选被卤素取代的低级烃基; 烷氧基羰基，其中烷氧基可以具有1至6个或更多个碳原子，或芳基如苯基; 该方法包括环化通式（VII）的化合物; 其中A，R 2和R 3如通式（II）所定义，R 20是氢，被至多5个选自卤素，C 1 -C 6烷基，O（C 1 -C 6） -C 1-6烷基）或硝基，R 21是C 1 -C 8烷基，被至多五个上述R 20取代基取代的苄基或苄基。

152. 发明申请

WO1996036435A1 COMPOSITION OF MATTER 审中-公开
标题翻译：物质组成
公开(公告)号：WO1996036435A1
公开(公告)日：1996-11-21
申请号：PCT/GB1996001127
申请日：1996-05-13
申请人： ZENECA LIMITED , LINDOY, Leonard, Francis , ATKINSON, Ian, Murray , TASKER, Peter, Anthony , THORP, Derek
发明人： ZENECA LIMITED
IPC分类号： B01J45/00
CPC分类号： B01J39/12 , B01J45/00 , C22B3/42 , Y02P10/234
摘要： A composition of matter is provided in which a phosphonic acid or phosphonic acid ester group is linked through a thioether residue to a silicon atom which is further covalently bonded to a solid inorganic support. The compositions can be employed to selectively separate metal ions having high cationic charge from a solution containing lower-charged cations, and also to selectively separate highly charged cations having a relatively high charge density from cations having the same charge, but a lower charge density.
摘要翻译：提供了一种物质组合物，其中膦酸或膦酸酯基通过硫醚残基连接到进一步共价键合到固体无机载体上的硅原子上。该组合物可用于从含有较低电荷的阳离子的溶液中选择性分离具有高阳离子电荷的金属离子，并且还可选择性地从具有相同电荷但电荷密度较低的阳离子分离具有较高电荷密度的高电荷阳离子。

153. 发明申请

WO1996034919A1 INK JET PRINTING INK 审中-公开
标题翻译：喷墨打印墨水
公开(公告)号：WO1996034919A1
公开(公告)日：1996-11-07
申请号：PCT/GB1996000995
申请日：1996-04-26
申请人： ZENECA LIMITED , GUNN, Janet , HOLBROOK, Mark , LAVERY, Aidan, Joseph
发明人： ZENECA LIMITED
IPC分类号： C09D11/00
CPC分类号： C09D11/38
摘要： Ink compositions comprising an aqueous medium containing: (1) at least one water-soluble dye; (2) at least one cyclic ester or amide of formula (1), wherein m is a whole number from 3 to 5 and X represents -O- or -N(R)- in which R represents hydrogen, alkyl or substituted alkyl; (3) at least one hydroxy compound selected from polyhydroxy compounds having at least four hydroxy groups, optionally substituted cycloalkanols, cyclohexane dimethanol, benzyl alcohol, benzene dimethanol, phenol and polyhydroxybenzenes, and (4) at least one water-soluble organic solvent selected from alkanediols, alkanetriols, ether glycols and thioether glycols and suitable for use in ink jet printing processes for coloration of substrates such as paper or overhead projector slides.
摘要翻译：包含水性介质的油墨组合物含有：（1）至少一种水溶性染料; （2）至少一种式（1）的环酯或酰胺，其中m是3至5的整数，X表示-O-或-N（R） - ，其中R表示氢，烷基或取代的烷基; （3）选自具有至少四个羟基的多羟基化合物，任选取代的环烷醇，环己烷二甲醇，苄醇，苯二甲醇，苯酚和多羟基苯的至少一种羟基化合物，和（4）至少一种选自以下的水溶性有机溶剂：链烷二醇，烷三醇，醚二醇和硫醚二醇，适用于喷墨印刷工艺，用于着色诸如纸或高架投影仪载玻片的基材。

154. 发明申请

WO1996033980A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1996033980A1
公开(公告)日：1996-10-31
申请号：PCT/GB1996000961
申请日：1996-04-23
申请人： ZENECA LIMITED , GIBSON, Keith, Hopkinson
发明人： ZENECA LIMITED
IPC分类号： C07D239/94
CPC分类号： C07D403/12 , C07D239/94
摘要： The invention concerns quinazoline derivatives of the 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; and R is di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-[(1-4C)alkoxy-(2-4C)alkoxyl]amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R substituents comprising a CH2 (methylene) group which is not attached to a N or O atom optionally bears on said CH2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
摘要翻译：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 3为（1-4C）烷氧基; 并且R 1是二 - [（1-4C）烷基]氨基 - （2-4C）烷氧基，吡咯烷-1-基 - （2-4C）烷氧基，哌啶子基 - （2-4C）烷氧基，吗啉代 2-4C）烷氧基，哌嗪-1-基 - （2-4C）烷氧基，4-（1-4C）烷基哌嗪-1-基 - （2-4C）烷氧基，咪唑-1-基 - （2-4C）烷氧基，二 - [（1-4C）烷氧基 - （2-4C）烷氧基]氨基 - （2-4C）烷氧基，硫代吗啉代 - （2-4C）烷氧基，1-氧硫代吗啉代 - （2-4C）（2-4C）烷氧基，并且其中包含未连接到N或O原子上的CH2（亚甲基）基团的任何上述R 1取代基任选地在所述CH 2基团上带有羟基取代基 ; 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以及该化合物的受体酪氨酸激酶抑制性质用于治疗增殖性疾病例如癌症的用途。

155. 发明申请

WO1996033979A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1996033979A1
公开(公告)日：1996-10-31
申请号：PCT/GB1996000960
申请日：1996-04-23
申请人： ZENECA LIMITED , BARKER, Andrew, John
发明人： ZENECA LIMITED
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The invention concerns quinazoline derivatives of formula (I) wherein n is 1, 2 or 3 and each R is independently halogeno; and R is (1-4C)alkoxy-(2-4C)alkylamino; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
摘要翻译：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; 和R 1是（1-4C）烷氧基 - （2-4C）烷基氨基; 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以及该化合物的受体酪氨酸激酶抑制性质用于治疗增殖性疾病例如癌症的用途。

156. 发明申请

WO1996032488A1 S-ADENOSYL-L-HOMOCYSTEIN HYDROLYSE PROMOTER 审中-公开
公开(公告)号：WO1996032488A1
公开(公告)日：1996-10-17
申请号：PCT/GB1996000882
申请日：1996-04-10
申请人： ZENECA LIMITED , GREENLAND, Andrew, James , DRAPER, John , WARNER, Simon , SKIPSEY, Marc
发明人： ZENECA LIMITED
IPC分类号： C12N15/82
CPC分类号： C12N15/8216 , C12N9/14 , C12N15/8243 , C12N15/8282
摘要： A promoter derived from an SHH gene, especially the SHH gene of Arabidopsis thaliana which is capable of directing expression of a variety of operator genes in both monocotyledonous and dicotyledonous plants. The promoter of the invention may be used for directing expression of pathogen resistance genes to disease or wound sites.
摘要翻译：衍生自SHH基因，特别是拟南芥的SHH基因的启动子，其能够指导单子叶植物和双子叶植物中多种操纵基因的表达。本发明的启动子可用于将病原体抗性基因的表达指导到疾病或伤口部位。

157. 发明申请

WO1996031124A1 HERBICIDAL AZA BISPHOSPHONIC ACIDS AND COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：除草AZA二磷酸及其组合物
公开(公告)号：WO1996031124A1
公开(公告)日：1996-10-10
申请号：PCT/US1996004869
申请日：1996-04-08
申请人： ZENECA LIMITED , FISHER, Karl, J. , WOOLARD, Frank, X. , LEADBETTER, Michael, R. , GERDES, John, M.
发明人： ZENECA LIMITED
IPC分类号： A01N57/18
CPC分类号： C07F9/5532 , A01N57/18 , C07F9/3873 , C07F9/405 , C07F9/568 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/65031 , C07F9/6506 , C07F9/6512 , C07F9/6518 , C07F9/6533
摘要： Herbicidal compositions containing a bisphosphonic acid compound of formula (I) wherein n is 1, 2, 3, 4, 5 or 6, or an agrochemically acceptable salt or hydrolyzable ester thereof and methods of controlling undesirable plant growth using these bisphosphonic acid containing compositions. The herbicidal compositions exhibit desirable efficacy when applied to plants post-emergence, but exhibit little significant activity when applied to plants pre-emergence. Novel aza-bisphosphonic acid compounds are also disclosed.
摘要翻译：含有其中n为1,2,3,4,5或6的式（I）的双膦酸化合物或其农业化学上可接受的盐或可水解的酯的除草组合物以及使用这些含二膦酸的组合物来控制不期望的植物生长的方法。当施用于植物出苗后，除草组合物表现出期望的功效，但当施用于植物出苗前显示出很小的显着活性。还公开了新的氮杂双膦酸化合物。

158. 发明申请

WO1996029410A1 IN VIVO GENERATION OF ANTIBODIES AGAINST ANTIGENS SECRETED IN A HOST BY TRANSFECTED MEL CELLS 审中-公开
标题翻译：在转基因细胞中分泌抗原的抗体生物体内
公开(公告)号：WO1996029410A1
公开(公告)日：1996-09-26
申请号：PCT/GB1996000616
申请日：1996-03-18
申请人： ZENECA LIMITED , NEEDHAM, Maurice, Ronald, Charles , HOLLIS, Melvyn
发明人： ZENECA LIMITED
IPC分类号： C12N15/13
CPC分类号： C07K16/00 , A61K39/00 , A61K48/00 , C07K14/52 , C07K14/70542
摘要： A method for the generation in a mammalian host of antibodies to a biological of interest which method comprises incorporating murine erythroleukemia (MEL) cell comprising DNA encoding the biological of interest into the mammalian host, allowing the MEL cells to express and secrete the biological of interest, allowing the host to raise antibodies thereto, and isolating said antibodies from the host.
摘要翻译：在哺乳动物宿主中产生感兴趣的生物学抗体的方法包括将包含编码目的生物学信息的DNA的鼠红白血病（MEL）细胞掺入到哺乳动物宿主中，允许MEL细胞表达和分泌感兴趣的生物学，允许宿主产生抗体，并从宿主中分离所述抗体。

159. 发明申请

WO1996028762A1 LIQUID PHOTOCURABLE COMPOSITIONS 审中-公开
标题翻译：液体光电组合物
公开(公告)号：WO1996028762A1
公开(公告)日：1996-09-19
申请号：PCT/GB1996000517
申请日：1996-03-06
申请人： ZENECA LIMITED , POPAT, Ajay, Haridas , LAWSON, John, Robert , MCLEAN, Colin, Henry
发明人： ZENECA LIMITED
IPC分类号： G03F07/027
CPC分类号： G03F7/0037 , G03F7/027
摘要： A liquid composition comprising: a) 5 to 25 parts of a monomeric aliphatic or cycloaliphatic di(meth)acrylate having a MW of not more than 800; b) 2 to 20 parts of a monomeric poly(meth)acrylate having a functionality of at least 3 and a MW of at least 610; c) 12 to 40 parts of a urethane(meth)acrylate having a functionality of 2 to 4 and a MW of 400 to 10,000; d) 35 to 70 parts of a monomeric or oligomeric di(meth)acrylate based on bisphenol A or bisphenol F; and e) 0.1 to 10 parts of a photoinitiator; wherein all parts are by weight, the total number of parts of a) + b) does not exceed 30 and the total number of parts of a) + b) + c) + d) + e) add up to 100. The compositions are suitable for the stereolighographic production of three-dimensional solid articles such as mechanical parts and models of body parts.
摘要翻译：一种液体组合物，其包含：a）5〜25份MW不大于800的单体脂族或脂环族二（甲基）丙烯酸酯; b）2至20份官能度至少为3且MW至少为610的单体聚（甲基）丙烯酸酯; c）12〜40份官能度为2〜4，MW为400〜10,000的氨基甲酸酯（甲基）丙烯酸酯; d）35〜70份基于双酚A或双酚F的单体或低聚二（甲基）丙烯酸酯; 和e）0.1至10份光引发剂; 其中所有部分都是重量比，a）+ b）的部分总数不超过30，a）+ b）+ c）+ d）+ e）的总数量加到100上。组合物适用于三维固体制品如机械零件和车身部件型号的立体定向生产。

160. 发明申请

WO1996028151A2 USE OF A PYRUVATE DEHYDROGENASE ACTIVATOR FOR THE TREATMENT OF ISCHAEMIA IN LIMBS 审中-公开
标题翻译：用于治疗肢体血浆的吡啶类脱氢酶活化剂
公开(公告)号：WO1996028151A2
公开(公告)日：1996-09-19
申请号：PCT/GB1996000555
申请日：1996-03-11
申请人： ZENECA LIMITED , CONSTANTIN-TEODOSIU, Dumitru , TIMMONS, James, Archibald , GREENHAFF, Paul, Leonard , POUCHER, Simon, Martin
发明人： ZENECA LIMITED
IPC分类号： A61K31/22
CPC分类号： A61K31/222 , A61K31/00 , A61K31/19 , A61K31/22
摘要： Agents which inhibit PDH kinase such as dichloroacetic acid, its salts and derivatives are described as being useful in the treatment of ischaemia in limbs. In particular, dichloroacetic acid and its salts are useful in treating intermittent claudification. Pharmaceutical compositions are also described.
摘要翻译：抑制PDH激酶如二氯乙酸，其盐和衍生物的药物被描述为可用于治疗肢体中的局部缺血。特别地，二氯乙酸及其盐可用于治疗间歇性跛行。还描述了药物组合物。

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