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91. 发明申请

WO1994010249A1 PIGMENT MANUFACTURING PROCESS 审中-公开
标题翻译：颜料制造工艺
公开(公告)号：WO1994010249A1
公开(公告)日：1994-05-11
申请号：PCT/GB1993002157
申请日：1993-10-20
申请人： ZENECA LIMITED , PIKE, Leslie, Clark , WOOLLVEN, Peter
发明人： ZENECA LIMITED
IPC分类号： C09B48/00
CPC分类号： C07D471/04 , C07C67/343 , C07C249/02 , C09B48/00 , C07C69/757
摘要： A process of preparing a quinacridone of formula (VII), wherein X is methyl, chloro or fluoro, and n is 0, 1 or 2, which comprises : (a) treating a dialkylsuccinate of formula (II), wherein R is alkyl of 1 to 3 carbons atoms, with at least the stoichiometric amount of a solution of a sodium alkoxide NaOR in an alcohol ROH, in a reaction medium principally comprising one or more aliphatic polyethers of the formula R [O(CH2)m]nOR wherein R is C1-4-alkyl, m is 2 or 3, and n is 1, 2, 3 or 4, at a temperature of 70 DEG C to 120 DEG C, and maintaining the reaction mixture at a temperature of from 90 DEG C to 150 DEG C for a period sufficient to complete the formation of the dialkylsuccinylsuccinate (III), cooling the reaction mixture; (b) adding an aniline of formula (IV), wherein X is methyl, chloro or fluoro, and n is 0, 1 or 2, acidifying the reaction mixture, heating it to 60 DEG C to 100 DEG C to convert the dialkylsuccinylsuccinate (III) in the dihydro dianilinoterephthalic ester (V) wherein X and n are as defined for formula (IV), cooling the reaction mixture and neutralising it; (c) heating the reaction mixture under a vacuum to distil off water, alcohol ROH, and any unreacted aniline, placing the reaction mixture under an inert atmosphere, optionally adding more aliphatic polyether, and heating the reaction mixture to a temperature of 225-300 DEG C, whereby the dihydro dianilinoterephthalic ester (V) is converted to the dihydroquinacridone (VI); and (d) adding a mono-, di- or tri-ethanolamine or a 2-alkoxyethanol of formula F OCH2CH2OH wherein R is C1-4-alkyl, making the reaction mixture alkaline, oxidising the dihydroquinacridone (VI) to form the quinacridone (VII), and recovering the quinacridone from the reaction mixture.
摘要翻译：制备式（VII）的喹吖啶酮的方法，其中X是甲基，氯或氟，n是0,1或2，其包括：（a）处理式（II）的二烷基琥珀酸酯，其中R是 1至3个碳原子，至少化学计量量为醇ROH中的醇钠NaOR溶液，主要包含一种或多种式R 1 [O（CH 2）m]的脂族聚醚的反应介质中， nOR 1其中R 1为C 1-4 - 烷基，m为2或3，n为1,2,3或4，温度为70℃至120℃，并保持反应混合物在90℃至150℃的温度下，足以完成二烷基琥珀酰基琥珀酸盐（III）的形成，冷却反应混合物; （b）加入式（Ⅳ）的苯胺，其中X是甲基，氯或氟，n是0,1或2，酸化反应混合物，将其加热到60℃至100℃，将二烷基琥珀酰基琥珀酸酯 III）在二氢二苯胺基对苯二甲酸酯（V）中，其中X和n如式（IV）所定义，冷却反应混合物并中和; （c）在真空下加热反应混合物以蒸馏出水，醇ROH和任何未反应的苯胺，将反应混合物置于惰性气氛下，任选加入更多的脂族聚醚，并将反应混合物加热至225-300℃ 将二氢二苯胺基对苯二甲酸酯（V）转化为二氢喹吖啶酮（VI）; 和（d）加入式F 2 OCH 2 CH 2 OH的单 - ，二 - 或三 - 乙醇胺或2-烷氧基乙醇，其中R 2是C 1-4 - 烷基，使反应混合物碱性，氧化二氢喹吖啶酮）以形成喹吖啶酮（VII），并从反应混合物中回收喹吖啶酮。

92. 发明申请

WO1994010159A1 OXA- AND THIADIAZOLE DERIVATIVES USED AS INSECTICIDES AND FUNGICIDES 审中-公开
标题翻译：用作杀虫剂和杀真菌剂的OXA-和噻二唑衍生物
公开(公告)号：WO1994010159A1
公开(公告)日：1994-05-11
申请号：PCT/GB1993002097
申请日：1993-10-11
申请人： ZENECA LIMITED , MATTHEWS, Ian, Richard
发明人： ZENECA LIMITED
IPC分类号： C07D271/06
CPC分类号： C07D271/07 , A01N43/82 , C07D271/113 , C07D285/08 , C07D285/13 , C07D413/04 , C07D417/04
摘要： Fungicidal and insecticidal compounds having general formula (I), or a stereoisomer thereof, wherein A is CH or N; B is OCH3 or NHCH3; one of L and M is N and the other is S or O; X is an optionally substituted carbocyclic or heterocyclic group; and n is 0 or 1.
摘要翻译：具有通式（I）的杀真菌剂和杀虫剂化合物或其立体异构体，其中A为CH或N; B是OCH 3或NHCH 3; L和M之一是N，另一个是S或O; X是任选取代的碳环或杂环基; n为0或1。

93. 发明申请

WO1994008948A2 PROCESS FOR THE PREPARATION OF OXIME DERIVATIVES, CERTAIN INTERMEDIATES AND THE USE OF THE OXIME DERIVATIVES AS FUNGICIDES 审中-公开
标题翻译：氧化衍生物的制备方法，某些中间体和使用衍生物作为杀真菌剂
公开(公告)号：WO1994008948A2
公开(公告)日：1994-04-28
申请号：PCT/GB1993001979
申请日：1993-09-21
申请人： ZENECA LIMITED , WORTHINGTON, Paul, Anthony , ASPINALL, Ian, Henry
发明人： ZENECA LIMITED
IPC分类号： C07C249/12
CPC分类号： C07D213/64 , A01N37/36 , A01N39/00 , A01N43/06 , A01N43/40 , A01N43/50 , A01N43/52 , A01N43/54 , A01N43/653 , A01N43/713 , A01N43/76 , C07C249/12 , C07C251/60 , C07C255/54 , C07D213/70 , C07D213/89 , C07D215/26 , C07D233/42 , C07D235/26 , C07D235/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/56 , C07D249/12 , C07D257/04 , C07D263/58 , C07D277/68 , C07D277/70 , C07D333/34
摘要： A process for the preparation of a compound of formula (I), wherein Y is O, S(O)n (wherein n is 0, 1 or 2) or NR ; W is CH3O.CH=C.CO2CH3, CH3O.CH=C.CONR R , CH3O.N=C.CO2CH3 or CH3O.N=C.CONR R ; R is hydrogen, C1-4 alkyl, C1-4 haloalkyl or cyano; R , R , R , R and R are independently hydrogen or C1-4 alkyl; p is 1; and R is hydrogen, C1-10 alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl or optionally substitued heteroarylalkyl; the process comprising reacting a compound of formula (II), wherein W, R , R and R are as previously defined and L is a leaving group, with a compound of formula (III), wherein R and Y are as previously defined.
摘要翻译：制备式（I）化合物的方法，其中Y为O，S（O）n（其中n为0,1或2）或NR 5; W是CH 3 O，CH = C.CO 2 CH 3，CH 3 O，CH = C.CONR 6 R 7，CH 3 O，N = C.CO 2 CH 3或CH 3 O.N = C.CONR 6 R 7; R 1是氢，C 1-4烷基，C 1-4卤代烷基或氰基; R 2，R 3，R 5，R 6和R 7独立地是氢或C 1-4烷基; p为1; 和R 4是氢，C 1-10烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳基烷基或任选取代的杂芳基烷基; 所述方法包括使式（II）化合物（其中W，R 1，R 2和R 3如前所定义，L是离去基团）与式（III）化合物反应，其中 R 4和Y如前所定义。

94. 发明申请

WO1994005662A1 INDOLIZINES AS HERBICIDES 审中-公开
标题翻译：不溶于除草剂
公开(公告)号：WO1994005662A1
公开(公告)日：1994-03-17
申请号：PCT/EP1993002132
申请日：1993-08-12
申请人： ZENECA LIMITED , MITCHELL, Glynn , SMITH, Stephen, Christopher , CLARKE, Eric, Daniel
发明人： ZENECA LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A01N43/90 , C07D471/14
摘要： A herbicidal composition comprising a compound of formula (I) or a tautomer or a quaternised derivative thereof where Y is a group of formula -CR1=CR2-CO- and R1, R2, R3, R4 and R5 are independently selected from hydrogen; optionally substituted alkyl; optionally alkenyl; optionally substituted alkynyl; optionally substituted aryl; optionally substituted aromatic heterocyclic; halo; nitro; cyano; a group OR6 where R6 is hydrogen or a salt thereof, carboxy or an ester thereof, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or optionally substituted aryl; carboxy or a salt, ester or amide derivative thereof; S(O)nR7 where n is 0, 1 or 2 and R7 is optionally alkyl, optionally substituted alkenyl, optionally substituted alkynyl or optionally substituted aryl; NR8R9 where R8 and R9 are independently selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or optionally substituted aryl and R9 may additionally be acyl, or R8 and R9 together with the nitrogen atom to which they are attached form a heterocyclic ring; or R1 and R2 and/or any adjacent two of R3, R4 and R5 together with the carbon atoms to which they are attached form an optionally substituted fused saturated or unsaturated carbocyclic or heterocyclic ring; in combination with a carrier or diluent.
摘要翻译：一种除草组合物，其包含式（I）化合物或其互变异构体或其季铵化衍生物，其中Y为式-CR1 = CR2-CO-基团，R1，R2，R3，R4和R5独立地选自氢; 任选取代的烷基; 烯基; 任选取代的炔基; 任选取代的芳基; 任选取代的芳族杂环; 光环; 硝基; 氰基; 任选取代的烷基，任选取代的烯基，任选取代的炔基或任选取代的芳基;其中R 6为氢或其盐，羧基或其酯，任选取代的烷基，任选取代的烯基，羧基或其盐，酯或酰胺衍生物; S（O）n R 7，其中n为0,1或2，R 7为任选烷基，任选取代的烯基，任选取代的炔基或任选取代的芳基; NR 8 R 9，其中R 8和R 9独立地选自氢，任选取代的烷基，任选取代的烯基，任选取代的炔基或任选取代的芳基，R 9可以另外是酰基，或者R 8和R 9与它们所连接的氮原子一起形成杂环环; 或R 1和R 2和/或R 3，R 4和R 5中的任何相邻的两个与它们所连接的碳原子一起形成任选取代的稠合饱和或不饱和碳环或杂环; 与载体或稀释剂组合。

95. 发明申请

WO1994005660A1 QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为平均合成酶抑制剂
公开(公告)号：WO1994005660A1
公开(公告)日：1994-03-17
申请号：PCT/GB1993001802
申请日：1993-08-24
申请人： ZENECA LIMITED , BROWN, George, Robert , MALLION, Keith, Blakeney , WHITTAMORE, Paul, Robert, Owen , BRITTAIN, David, Robert
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts in which R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR -CR is a double bond; X is selected from -CH2CH2-, -CH=CH-, -C=C-, -CH2O-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S- and -SCH2-; Ar is a phenylene moiety; Ar is a heteroaryl moiety; and wherein one or both of Ar and Ar may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R is hydroxy, X is not selected from -NHCH2- and -SCH2-; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial, such as hypercholesterolemia and atherosclerosis. Processes for preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1是氢或羟基; R 2是氢; 或R 1和R 2连接在一起，使得CR 1 -CR 2是双键; X选自-CH 2 CH 2 - ， - CH = CH - ， - C = C - ， - CH 2 O - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 CO-，-COCH 2 - ， - CH 2 S-和-SCH 2 - Ar 1是亚苯基; Ar 2是杂芳基部分; 并且其中Ar 1和Ar 2中的一个或两个可任选地具有一个或多个独立地选自卤素，羟基，氨基，硝基，氰基，羧基，氨基甲酰基，烷基，烯基，炔基，烷氧基，烷基氨基，二 - 烷基氨基，N-烷基氨基甲酰基，二-N，N-烷基氨基甲酰基，烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代 - 烷基，羧基烷基和烷酰基氨基; 条件是当R 1是羟基时，X不选自-NHCH 2 - 和-SCH 2 - ; 是角鲨烯合酶的抑制剂，因此可用于治疗胆固醇降低有益的医学病症，例如高胆固醇血症和动脉粥样硬化。制备这些衍生物的方法，含有它们的药物组合物也与其在医药中的用途一起被描述。

96. 发明申请

WO1994002020A1 PESTICIDAL COMPOSITIONS 审中-公开
标题翻译：农药组合物
公开(公告)号：WO1994002020A1
公开(公告)日：1994-02-03
申请号：PCT/GB1993001445
申请日：1993-07-12
申请人： ZENECA LIMITED , ICI PROTECTION DE L'AGRICULTURE S.A. , FLECHEL, Brigitte
发明人： ZENECA LIMITED , ICI PROTECTION DE L'AGRICULTURE S.A.
IPC分类号： A01N53/00
CPC分类号： A01N53/00 , A01N47/38 , A01N43/653 , A01N25/30 , A01N25/02 , A01N2300/00
摘要： A pesticidal composition in the form of an emulsifiable concentrate comprising as active ingredient the insecticide lambda-cyhalothrin in combination with an emulsifier and a diluent characterized in that the emulsifier is as defined in the description and the diluent is a solvent blend consisting mainly of alkylnaphthalenes having a high flash point and optionally comprising an oil-soluble dyestuff.
摘要翻译：可乳化浓缩物形式的杀虫组合物，其包含与乳化剂和稀释剂组合的杀虫剂λ-氯氟氰菊酯作为活性成分，其特征在于乳化剂如说明书中所定义，稀释剂是主要由烷基萘组成的溶剂混合物，其中烷基萘具有高闪点且任选地包含油溶性染料。

97. 发明申请

WO1994001500A1 POWDER COATING COMPOSITION 审中-公开
标题翻译：粉末涂料组合物
公开(公告)号：WO1994001500A1
公开(公告)日：1994-01-20
申请号：PCT/GB1993001423
申请日：1993-07-07
申请人： ZENECA LIMITED , SATGURUNATHAN, Rajasingham , HINDE, David, Charles , PADGET, John, Christopher , YEATES, Stephen, George
发明人： ZENECA LIMITED
IPC分类号： C09D05/03
CPC分类号： C09D151/00 , C09D5/03
摘要： Powder coating composition which comprises a hybrid polymer system in granular form of a polymer A formable from monomer(s) by aqueous suspension polymerisation and a polymer B, different to A, which polymer system has been obtained using a process which comprises dissolving polymer B in monomeric material to be used in the formation of polymer A, polymerising the monomer(s) to form polymer A using an aqueous suspension polymerisation process, and removing the aqueous phase to form a hybrid of the polymers A and B in granular form, and wherein polymer A and polymer B bear functional groups for imparting curability to the hybrid polymer system, and wherein further the hybrid polymer system has a number average molecular weight within the range of from 1,500 to 15,000.
摘要翻译：粉末涂料组合物，其包含通过水悬浮聚合可从单体形成的聚合物A的颗粒形式的混合聚合物体系和与A不同的聚合物B，该聚合物体系已经使用包括将聚合物B溶解在用于形成聚合物A的单体材料，使用水悬浮聚合方法聚合单体以形成聚合物A，并除去水相以形成颗粒形式的聚合物A和B的杂化物，其中聚合物A和聚合物B具有赋予混合聚合物体系固化性的官能团，并且其中该混合聚合物体系的数均分子量在1,500至15,000范围内。

98. 发明申请

WO1993024519A1 LACTAM DIPEPTIDES HAVING HLE INHIBITING ACTIVITY 审中-公开
标题翻译：具有HLE抑制活性的LACTAM插入物
公开(公告)号：WO1993024519A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001176
申请日：1993-06-03
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , VEALE, Chris, Allan , WARNER, Peter , WOLANIN, Donald, John
IPC分类号： C07K05/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to certain novel amide derivatives which are pyrido(3,4-b)indol-2-ylacetamides of formula (I) which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.
摘要翻译：本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂的也称为人嗜中性粒细胞弹性蛋白酶（HNE）的式（I）的吡啶并（3,4-b）吲哚-2-基乙酰胺的某些新型酰胺衍生物，使其在需要这种抑制时有用，例如用于药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。本发明还包括可用于合成这些酰胺衍生物的中间体，制备酰胺衍生物的方法，含有这种酰胺衍生物的药物组合物及其使用方法。

99. 发明申请

WO1993024486A1 QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHETASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为平均合成酶抑制剂
公开(公告)号：WO1993024486A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001165
申请日：1993-06-02
申请人： ZENECA LIMITED , MALLION, Keith, Blakeney
发明人： ZENECA LIMITED
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Quinuclidine derivatives of formula (I), and their pharmaceutically acceptable salts, in which R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR -CR is a double bond; Ar is a phenylene moiety; Ar is a 6-membered heteroaryl moiety containing one or two nitrogen atoms; and wherein one or both of Ar and Ar may optionally bear one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oxime derivatives; inhibit squalene synthetase and are therefore useful in treating diseases and medical conditions where inhibition of squalene synthetase is desirable, for exemple in treating hypercholesterolemia and atherosclerosis. Processes for the preparation of these derivatives and pharmaceutical compositions containing them are also referred to as well as their use in medicine.
摘要翻译：式（I）的奎宁环衍生物及其药学上可接受的盐，其中R 1是氢或羟基; R 2是氢; 或R 1和R 2连接在一起，使得CR 1 -CR 2是双键; Ar 1是亚苯基; Ar 2是含有一个或两个氮原子的6元杂芳基部分; Ar 1和Ar 2中的一个或两个可以任选地具有一个或多个取代基，例如卤代，羟基，氨基，硝基，氰基，羧基，氨基甲酰基，烷基，烯基，炔基，烷氧基，烷基氨基，烷基氨基，N-烷基氨基甲酰基，二-N，N-烷基氨基甲酰基，烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代烷基，烷酰基氨基，亚烷基二氧基，烷酰基和肟衍生物和所述肟衍生物的O-烷基醚; 抑制角鲨烯合成酶，因此可用于治疗需要抑制角鲨烯合成酶的疾病和医学病症，例如治疗高胆固醇血症和动脉粥样硬化。制备这些衍生物和含有它们的药物组合物的方法也被称为它们在医学中的用途。

100. 发明申请

WO1993021210A1 PYRIMIDINYL ACETAMIDES AS ELASTASE INHIBITORS 审中-公开
标题翻译：吡咯烷酮乙酸酯作为弹性酶抑制剂
公开(公告)号：WO1993021210A1
公开(公告)日：1993-10-28
申请号：PCT/GB1993000797
申请日：1993-04-15
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , BERNSTEIN, Peter, Robert , EDWARDS, Philip, Duke , SHAW, Andrew , THOMAS, Royston, Martin , VEALE, Chris, Allan , WARNER, Peter , WOLANIN, Donald, John
IPC分类号： C07K05/02
CPC分类号： C07K5/0205 , A61K38/00 , C07K5/06191
摘要： The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula (I), set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which (HLE) is implicated. The invention also includes intermediates useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.
摘要翻译：本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的本文所列的式（I）的1-嘧啶基乙酰胺衍生物的某些新型取代的酮，使得它们有用这样的抑制是期望的，例如用于药理学，诊断和相关研究中的研究工具以及涉及（HLE）的哺乳动物中的疾病的治疗。本发明还包括可用于合成这些取代酮的中间体，用于制备含取代酮的取代酮药物组合物的方法及其使用方法。

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