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1. 发明申请

WO1997047621A1 PROCESS FOR THE PREPARATION OF CARBAPENEM DERIVATIVES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备碳氢化合物衍生物及其中间体的方法
公开(公告)号：WO1997047621A1
公开(公告)日：1997-12-18
申请号：PCT/GB1997001560
申请日：1997-06-10
申请人： ZENECA LIMITED , GALLAGHER, Timothy, Charles , HALES, Neil, James , BRADBURY, Robert, Hugh , WISEDALE, Richard , MARTEL, Sarah, Ruth
发明人： ZENECA LIMITED
IPC分类号： C07D477/04
CPC分类号： C07D205/10 , C07D477/04 , Y02P20/55
摘要： The invention provides a process for the preparation of compounds of formula (I) wherein R , R , R R and R are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which process includes the step of reacting the intermediate formed by heating a compound of formula (II) in an inert solvent, with a compound of the formula R --R wherein R , R , R , R and R are as defined in the specification and functional groups are optionally protected; and thereinafter, if necessary, removing any protecting groups. The compounds of formula (I) are useful as intermediates in the preparation of DELTA carbapenems and may possess antibacterial properties and/or inhibit beta -lactamase.
摘要翻译：本发明提供了制备式（I）化合物的方法，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义; 并且其中任选的官能团被保护; 及其盐; 该方法包括使通过在惰性溶剂中加热式（II）化合物形成的中间体与式R 3 -R 4的化合物反应的步骤，其中R 1，R 2， R 3，R 4和R 5如说明书中所定义，并且官能团任选被保护; 并且如果需要，移除任何保护组。式（I）化合物可用作制备DELTA 2碳青霉烯类的中间体，并且可具有抗菌性和/或抑制β-内酰胺酶。

2. 发明申请

WO1998000429A1 PROCESS FOR THE PREPARATION OF PENAM AND PENEM DERIVATIVES 审中-公开
标题翻译：制备PENAM和PENEM衍生物的方法
公开(公告)号：WO1998000429A1
公开(公告)日：1998-01-08
申请号：PCT/GB1997001714
申请日：1997-06-24
申请人： ZENECA LIMITED , GALLAGHER, Timothy, Charles , HALES, Neil, James , WISEDALE, Richard , PLANCHENAULT, Denis
发明人： ZENECA LIMITED
IPC分类号： C07D499/04
CPC分类号： C07D499/88 , C07D499/00 , Y02P20/55
摘要： The invention provides a process for the preparation of compounds of formula (I) wherein R , R , R , R and R are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which process includes the step of reacting the intermediate formed by heating a compound of formula (II), in an inert solvent, with a compound of the formula S=C(R )R wherein R , R , R , R and R are as defined in the specification and functional groups are optionally protected; and thereinafter, if necessary, removing any protecting groups. The compounds of the formula (I) are useful as intermediates in the preparation of penems and may possess antibacterial properties and/or inhibit beta -lactamase in their own right.
摘要翻译：本发明提供了制备式（I）化合物的方法，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义; 并且其中任选的官能团被保护; 及其盐; 该方法包括使在惰性溶剂中加热式（II）化合物形成的中间体与式S = C（R 3）R 4的化合物反应的步骤，其中R 1， R 2，R 3，R 4和R 5如说明书中所定义，官能团任选地被保护; 并且如果需要，移除任何保护组。式（I）的化合物可用作制备青霉烯的中间体，并且可以具有本身的抗菌性和/或抑制β-内酰胺酶。

3. 发明申请

WO1996032642A1 AFFINITY CHROMATOGRAPHIC METHOD FOR SCREENING COMBINATORIAL LIBRARIES 审中-公开
标题翻译：用于筛选组合图书馆的亲属色谱方法
公开(公告)号：WO1996032642A1
公开(公告)日：1996-10-17
申请号：PCT/GB1996000790
申请日：1996-04-01
申请人： ZENECA LIMITED , HALES, Neil, James , CLAYTON, Edward
发明人： ZENECA LIMITED
IPC分类号： G01N33/538
CPC分类号： G01N33/68 , G01N33/538
摘要： An assay method for determining the affinity of low molecular weight ligands for a biological of interest under physiologically relevant conditions, which method comprises immobilising the biological of interest on a solid phase matrix, contacting this with a mixture comprising the ligands, removing any unbound ligands from the matrix, eluting the ligands from the matrix and establishing their affinity for the biological of interest by reference to their order of retention on the column.
摘要翻译：用于在生理相关条件下测定低分子量配体对感兴趣的生物学的亲和力的测定方法，该方法包括将感兴趣的生物学固定在固相基质上，使其与包含配体的混合物接触，从而除去任何未结合的配体基质，从基质中洗脱配体并通过参考其在柱上的保留顺序来确定它们对感兴趣的生物学的亲和力。

4. 发明申请

WO1995026957A1 N-HETEROCYCLYL SULPHONAMIDE DERIVATIVES AND THEIR USE AS ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译： N-环己基磺酰胺衍生物及其作为内皮素拮抗剂的用途
公开(公告)号：WO1995026957A1
公开(公告)日：1995-10-12
申请号：PCT/GB1995000702
申请日：1995-03-29
申请人： ZENECA LIMITED , BRADBURY, Robert, Hugh
发明人： ZENECA LIMITED
IPC分类号： C07D237/20
CPC分类号： C07D213/76 , C07D237/20 , C07D239/69 , C07D241/20 , C07D241/22
摘要： The invention concerns pharmaceutically useful compounds of formula (I), wherein Q is a naphthyl or biphenyl group; W, X, Y and Z are independently selected from nitrogen and CR such that two or three of W, X, Y and Z are nitrogen and the remainder are CR or X is nitrogen and W, Y and Z are CR ; A , A , A and R have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译：本发明涉及药用有用的式（I）化合物，其中Q是萘基或联苯基; W，X，Y和Z独立地选自氮和CR 2，使得W，X，Y和Z中的两个或三个为氮，其余为CR 2或X为氮，W，Y和Z 是CR <2>; A 1，A 2，A 3和R 1具有本文定义的任何含义及其药学上可接受的盐和含有它们的药物组合物。新化合物具有内皮素受体拮抗剂活性，可用于治疗高血糖或异常水平的内皮素起重要作用的疾病或医学病症。本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。

5. 发明公开

EP0639173A1 CERTAIN 2-(2'METHYL-3',4'-TRISUBSTITUTED BENZOYL)-1,3-CYCLOHEXANEDIONES 失效
标题翻译： 2-（2'-甲基-3”，4'-三取代苯甲酰基）-1,3-环己二酮。
公开(公告)号：EP0639173A1
公开(公告)日：1995-02-22
申请号：EP92903536.0
申请日：1991-12-19
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED
IPC分类号： A01N35 , A01N39 , A01N41 , C07C49 , C07C65 , C07C205 , C07C317 , C07C323
CPC分类号： A01N41/10 , A01N39/00 , C07C49/84 , C07C65/03 , C07C65/21 , C07C205/45 , C07C205/59 , C07C317/46 , C07C323/62 , C07C2601/14
摘要： Herbicidal compounds of structural formula (I), wherein R1 is hydrogen or C¿1?-C4 alkyl; R?2¿ is hydrogen or C¿1?-C4 alkyl; R?3¿ is hydrogen or C¿1?-C4 alkyl; R4 is hydroxy, hydrogen or C1-C4 alkyl; or R?3 and R4¿ together are carbonyl (=O) with the proviso that R?1, R2, R5 and R6¿ are C¿1?-C4 alkyl; R?5¿ is hydrogen or C¿1?-C4 alkyl; R?6¿ is hydrogen, C¿1?-C4 alkyl, C1-C4 alkylthio, or C1-C4 alkylsulfonyl, with the proviso that when R?6 is C¿1-C4 alkylthio or C1-C4 alkylsulfonyl, then R3 and R4 are not together carbonyl; R7 is methyl or ethyl; and R8 is (1) halogen; (2) nitro; or (3) RbSOn- wherein n is the integer 0 or 2, and Rb is (a) C¿1?-C4 alkyl; and its salts.

6. 发明公开

EP0584227A1 HERBICIDAL SUBSTITUTED CYCLOHEXANEDIONE AND NITROGEN FERTILISER COMPOSITIONS AND METHOD 失效
标题翻译：方法和除草剂的组合物取代的氮化肥和环己二酮包括在内。
公开(公告)号：EP0584227A1
公开(公告)日：1994-03-02
申请号：EP92912147.0
申请日：1992-04-27
申请人： ZENECA LIMITED , THOAMS, David, A.
发明人： ZENECA LIMITED , THOAMS, David, A.
IPC分类号： A01N35 , A01N41
CPC分类号： A01N35/06 , A01N41/10 , A01N47/28 , A01N59/00 , A01N2300/00
摘要： Composition herbicide contenant une cyclohexanedione substituée en quantités produisant un effet herbicide et ayant la formule (I) où R représente halogène; alkyle C1-C2, de préférence méthyle; alcoxy C1-C2, de préférence méthoxy; nitro; cyano; haloalkyle C1-C2, de préférence trifluorométhyle; ou RaSOn-, où n vaut 0 ou 2, de préférence 2, et Ra représente de préférence alkyle C1-C2, de préférence méthyle. R représente de préférence chlore, brome, alkyle C1-C2, alcoxy_C1-C2, cyano, nitro, alkylthio C1-C2, ou alkylsulfonyle C1-C2; ou idéalement, chlorine, nitro, méthyle, trifluorométhyle ou méthylsulfonyle; R1, R2, R3, R4, R5 et R6 représentent indépendamment hydrogène; alkyle C1-C4, de préférence alkyle C1-C2, idéalement méthyle ou hydrogène; R7 et R8 représentent indépendamment (1) hydrogène; (2) halogène, de préférence chlore, fluor ou brome; (3) alkyle C1-C4, de préférence méthyle; (4) alcoxy C1-C4, de préférence méthoxy ou éthoxy; (5) trifluorométhoxy; (6) cyano; (7) nitro; (8) haloalkyle C1-C4, de préférence trifluorométhyle; (9) RbSOn- où n représente le nombre entier 0, 1 ou 2, de préférence 0 ou 2; et Rb représente (a) alkyle C1-C4, de préférence méthyle; ou (b) alkyle C1-C4 à substitution d'halogène, de préférence chlorométhyle ou trifluorométhyle; (10) -NRcRd, où Rc et Rd représentent indépendamment hydrogène ou alkyle C1-C4; (11) ReC(O)- où Re représente alkyle C1-C4 ou alcoxy C1-C4; (12) -SO2NRcRd, où Rc et Rd représentent les éléments définis ci-dessus; (13) -N(Rc)C(O)Rd, où Rc et Rd sont tels que définis ci-dessus; et (14) -CH2CH2OCH3 ou -CH2CH2OC2H5; la composition comprenant au moins un engrais azoté présent en une quantité susceptible de renforcer l'activité herbicide de ladite cyclohexanedione substituée; et un ou plusieurs adjuvants.

7. 发明公开

EP0565654A1 PREPARATION OF TRISUBSTITUTED BENZENE INTERMEDIATES 失效
标题翻译：用于生产TRIPLE苯衍生物作为中间体。
公开(公告)号：EP0565654A1
公开(公告)日：1993-10-20
申请号：EP92918679.0
申请日：1992-01-23
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED
IPC分类号： C07C317
CPC分类号： C07C317/14
摘要： Procédé de préparation de 2-nitro-4-(alkylsulfonyle C1-C4) toluène ou de 2-nitro-4-(alkylsulfonyl C1-C4) éthylbenzène par alkylsulfonylation de 2-nitrotoluène ou 2-nitro éthylbenzène.

8. 发明申请

WO1998029507A1 PLASTISOL COMPOSITIONS 审中-公开
标题翻译： PLASTISOL组合物
公开(公告)号：WO1998029507A1
公开(公告)日：1998-07-09
申请号：PCT/GB1996003246
申请日：1996-12-31
申请人： ZENECA LIMITED , OVEREND, Andrew, Stuart , PADGET, John, Christopher , COOPER, David, Henry
发明人： ZENECA LIMITED
IPC分类号： C08L33/06
CPC分类号： C08L33/06 , B29C2793/0081 , B29D2030/1685 , C09D133/06 , C08L2666/02 , C08L2666/28
摘要： Acrylic plastisol composition comprising a plasticiser component, a plasticiser compatible acrylic polymer powder component of primary particle size >/=0.4 mu m and preferably not more than 30 mu m, and Tg >/=65 DEG C, and a plasticiser incompatible polymer powder component, where both polymers are preformed, are present in the weight ratio 95:5 to 40:60, and in combination are compatibly formulated with the plasticiser component.
摘要翻译：丙烯酸增塑剂组合物，其包含增塑剂组分，一次粒径≥0.4μm，优选不大于30μm，Tg> = 65℃的增塑剂相容的丙烯酸类聚合物粉末组分和增塑剂不相容的聚合物粉末组分，其中两种聚合物都被预先形成，其重量比为95:5至40:60，并且与增塑剂组分配合使用。

9. 发明申请

WO1998028306A1 PROCESS FOR THE PREPARATION OF AN ORGANOZINC REAGENT 审中-公开
标题翻译：制备有机原料试剂的方法
公开(公告)号：WO1998028306A1
公开(公告)日：1998-07-02
申请号：PCT/GB1997003443
申请日：1997-12-15
申请人： ZENECA LIMITED , BLACKER, Andrew, John , FIELDEN, Jan, Michael
发明人： ZENECA LIMITED
IPC分类号： C07F03/06
CPC分类号： C07D213/30 , C07B53/00 , C07B2200/07 , C07C29/40 , C07F3/06 , C07C33/22 , C07C33/46 , C07C33/20
摘要： A process for the preparation of an aromatic organozinc compound is provided. The process comprises reacting a zinc chloride, bromide or iodide and an organometallic compoud of another metal comprising an aromatic moiety, producing a reaction product comprising an organozinc compound and a halide salt of the other metal. The reaction product is then contacted with a liquid hydrocarbon, in which the organozinc compound is soluble and the halide salt of the other metal is of low solubility. The halide salt of the other metal is separated from the hydrocarbon, and the organozinc compound can be recovered from the hydrocarbon. Organozinc compounds produced by this process can be employed to generate chiral centres in suitable substrates.
摘要翻译：提供了一种制备芳香族有机锌化合物的方法。该方法包括使氯化锌，溴化物或碘化物与包含芳族部分的另一种金属的有机金属化合物反应，产生包含有机锌化合物和另一种金属的卤化物盐的反应产物。然后使反应产物与液态烃接触，其中有机锌化合物是可溶的，另一种金属的卤化物盐的溶解度低。另一种金属的卤化物盐与烃分离，有机锌化合物可以从烃中回收。通过该方法制备的有机锌化合物可用于在合适的底物中产生手性中心。

10. 发明申请

WO1998025924A1 8-AZABICYCLO[3.2.1]OCTANE-, 8-AZABICYCLO[3.2.1]OCT-6-ENE-, 9-AZABICYCLO[3.3.1]NONANE-, 9-AZA-3-OXABICYCLO[3.3.1]NONANE- AND 9-AZA-3-THIABICYCLO[3.3.1]NONANE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INSECTICIDES 审中-公开
标题翻译： 8-亚氨基双环[3.2.1]十八烷，8-亚氨基二环[3.2.1] OCT-6-ENE-，9-异亚氨基[3.3.1] NONANE-，9-亚氨基-3-氧代羰基[3.3.1] NONANE - 和9-氨基-3-噻唑啉[3.3.1] NONANE衍生物，其制备及其作为杀虫剂的用途
公开(公告)号：WO1998025924A1
公开(公告)日：1998-06-18
申请号：PCT/GB1997003054
申请日：1997-11-06
申请人： ZENECA LIMITED , URCH, Christopher, John , LEWIS, Terence , SUNLEY, Raymond, Leo , SALMON, Raymond , GODFREY, Christopher, Richard, Ayles , BRIGHTWELL, Christopher, Ian , HOTSON, Matthew, Brian
发明人： ZENECA LIMITED
IPC分类号： C07D451/14
CPC分类号： C07D451/02 , A01N43/90 , A01N47/16 , A01N47/18 , C07D451/04 , C07D451/06 , C07D451/14
摘要： A compound of formula (I) wherein A represents a bidentate group of the formula -CH2-X-CH2- (wherein X is methylene, sulfur or oxygen), X'C=CY or X'WC-CYZ (wherein X', W, Y and Z are independently hydrogen, hydroxy, acyloxy, alkoxy, alkylsilyloxy, cyano or halogen, or X' and W or Y and Z together with the carbon to which they are attached form a carbonyl group), provided that A is not CH2-CH2; Ar is an optionally substituted phenyl or 5- or 6-membered heterocyclic ring system containing from 1 to 3 heteroatoms individualy selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, wherein the substituents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups, any of which groups contain up to six carbon atoms; R is hydrogen or cyano or a group selected from alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkenyloxycarbonyl, aralkylocycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl or X''R (where X'' represents oxygen or a group NR ), provided that when R is alkenyl, aralkenyl or alkynyl said group does not have an unsaturated carbon atom bonding directly to the ring nitrogen of formula (I); R is hydrogen, cyano, hydroxy, alkyl, alkoxy, amino, nitro, isocyanato, acylamino, hydroxyalkyl, optionally substituted heteroaryl, alkoxyalkyl, haloalkyl, halohydroxyalkyl, aralkyloxyalkyl, acyloxyalkyl, amidoximido, sulfonyloxyalkyl, aminoalkyl, alkoxycarbonylamino, acylaminoalkyl, cyanoalkyl, imino, formyl, acyl or carboxylic acid or an ester or amide thereof, or alkenyl or alkynyl either of which is optionally substituted by halogen, alkoxy, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or cyano; R and R are, independently, hydrogen, alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, heterocyclylalkyl, alkoxycarbonyl or carboxylic acyl; alkyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from, halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, amino, acylamino, imidate and phosphonato groups; aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkanyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from, halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, haloalkyl, alkyl, amino, acylamino, imidate and phosphonato groups; or an acid addition salt, quaternary ammonium salt or N -oxide derived therefrom; an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor; a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.
摘要翻译：式（I）的化合物，其中A表示式-CH 2 -X-CH 2 - （其中X是亚甲基，硫或氧），X'C = CY或X'WC-CYZ（其中X'， W，Y和Z独立地是氢，羟基，酰氧基，烷氧基，烷基甲硅烷氧基，氰基或卤素，或X'和W或Y和Z与它们所连接的碳一起形成羰基），条件是A不是 CH2-CH2; Ar是任选取代的苯基或含有1至3个选自氮，氧和硫原子的杂原子的5或6元杂环系，以及环中相邻原子之间的至少一个不饱和键（双键），所述杂环任选地与苯环稠合，其中取代基（如果存在的话）选自卤素原子，氰基，烷基，烯基，炔基，烷氧基，卤代烷基，卤代烯基，烷硫基和烷基氨基，其中任何一个基团含有最多六个碳原子 R是氢或氰基或选自烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，链烷磺酰基，芳烃磺酰基，烯氧基羰基，芳烷基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，二硫代羧基或X'R （其中X“表示氧或基团NR 4），条件是当R是烯基时，所述基团不具有与式（I）的环氮直接键合的不饱和碳原子; R 1是氢，氰基，羟基，烷基，烷氧基，氨基，硝基，异氰酸根合，酰氨基，羟烷基，任选取代的杂芳基，烷氧基烷基，卤代烷基，卤代羟烷基，芳烷氧基烷基，酰氧基烷基，酰氨基亚氨基，磺酰氧基烷基，氨基烷基，烷氧基羰基氨基，酰基氨基烷基，酰基或羧酸或其酯或酰胺，或任选被卤素，烷氧基，环烷基，任选取代的芳基，任选取代的杂芳基或氰基取代的链烯基或炔基; R 3和R 4独立地是氢，烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，杂环基烷基，烷氧基羰基或羧基酰基。 R 3，R 3和R 4的烷基部分含有1至15个碳原子，并且任选地被一个或多个选自卤素，氰基，羧基，羧酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基，羟基，硝基，氨基，酰氨基，亚氨基和膦酸基; 芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，烷磺酰基，芳烃磺酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，R 3，R 3和R 4的二硫代羧基部分包含1至15个碳任选被一个或多个选自卤素，氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基，羟基，硝基，卤代烷基，烷基，氨基，酰氨基，亚氨酸酯基和膦酸基的取代基取代。或由其衍生的酸加成盐，季铵盐或N，N-氧化物; 杀虫杀螨或杀线虫组合物，其包含式（I）化合物及其合适的载体或稀释剂; 一种防治昆虫，螨虫或线虫害虫的方法，包括用有效量的式（I）化合物或上述组合物处理害虫或害虫的场所。

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