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    • 198. 发明申请
    • VIABLE BACTERIA
    • 可视细菌
    • WO1994025564A1
    • 1994-11-10
    • PCT/GB1994000811
    • 1994-04-18
    • ZENECA LIMITEDRODHAM, David, KirkCANTWELL, John, Burnett
    • ZENECA LIMITED
    • C12N01/04
    • C12N1/04C12N11/04
    • Microbial cells are stabilised for storage in the form of a dried composition in a stasis state suspended in a collapsed matrix. The composition is prepared by mixing the microbial cells, for example Gram-negative bacterial cells such as Pseudomonas fluorescens, with an aqueous composition comprising a polyhydroxy compound, preferably a saccharide, from which the matrix will be derived, and drying the mixture under conditions such that viscous flow of the polyhydroxy compound occurs and the matrix collapses but does not unduly damage the cells. The glass transition temperature of the matrix is ideally above the temperature at which the composition is stored.
    • 稳定的微生物细胞以悬浮在收缩基质中的停滞状态的干燥组合物的形式存储。 通过将微生物细胞,例如革兰氏阴性细菌细胞,例如荧光假单胞菌(Pseudomonas fluorescens)与包含多羟基化合物(优选糖)的水性组合物混合来制备组合物,从其中衍生基质,并在下列条件下干燥该混合物: 发生多羟基化合物的粘性流动,并且基质崩溃,但不会不适当地损伤细胞。 基质的玻璃化转变温度理想地高于组合物储存温度。
    • 199. 发明申请
    • HETEROCYCLIC DERIVATIVES
    • 杂环衍生物
    • WO1994025459A1
    • 1994-11-10
    • PCT/GB1994000910
    • 1994-04-28
    • ZENECA LIMITEDBROWN, George, RobertWHITTAMORE, Paul, Robert, OwenBRITTAIN, David, Robert
    • ZENECA LIMITED
    • C07D453/02
    • C07D453/02
    • Compounds of formula (I) wherein 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-, -CC-, -CH2O-, -OCH2-, CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S(O)n- and -S(O)nCH2- (wherein n is 0, 1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, (1-6C)alkoxycarbonyl(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, carbamoyl, (1-6C) alkylcarbamoyl, di-[(1-6C)alkyl]carbamoyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oximes, (1-6C)alkylthio, (1-6C)alkylsulphinyl and (1-6C)alkylsulphonyl when substituted by one or more groups selected from (1-6C)alkoxycarbonyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives, (1-6C)alkanoylamino, (1-6C)alkanoyloxy, (1-6C)alkanoyloxy(1-6C)alkyl, carbamoyl, N-(1-6C)alkylcarbamoyl, N,N-di[(1-6C)alkyl]carbamoyl, amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, (1-6C)alkoxy, (2-6C)alkenyloxy, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno(1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, phenoxy, cyano, nitro, hydroxy and carboxy; and wherein Ar may bear further substituents; and their pharmaceutically acceptable salts inhibit squalene synthese and are hence useful in lowering cholesterol levels in blood plasma. Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.
    • 式(I)的化合物,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 - , - CH 2 O - , - OCH 2 - ,CH 2 NH-,-NHCH 2 - , - CH 2 CO-,-COCH 2 - , - CH 2 S(O) S(O)n CH 2 - (其中n为0,1或2); Ar是含有一个或多个独立地选自(1-6C)烷基,(2-6C)烯基,(2-6C)炔基,(1-6C)烷氧基,(1-6C)烷氧羰基,(1-6C) (1-6C)烷基,(1-6C)烷氧基(1-6C)烷基,(1-6C)烷基氨基,二 - [(1-6C)烷基]氨基,氨基甲酰基,(1-6C )烷基氨基甲酰基,二 - [(1-6C)烷基]氨基甲酰基,(1-6C)烷酰基和肟衍生物和所述肟的(1-6C)烷基醚,(1-6C)烷硫基,(1-6C )(1-6C)烷氧基羰基,(1-6C)烷酰基及其肟衍生物和所述肟衍生物的O-(1-6C)烷基醚取代的(1-6C)烷基磺酰基, (1-6C)烷酰氨基,(1-6C)烷酰氧基,(1-6C)烷酰氧基(1-6C)烷基,氨基甲酰基,N-(1-6C)烷基氨基甲酰基,N,N-二[(1-6C) 氨基,(1-6C)烷基氨基,二 - [(1-6C)烷基]氨基,(1-6C)烷氧基,(2-6C)烯氧基,(1-6C)烷硫基,(1-6C) 烷基亚磺酰基,(1-6C)烷基磺酰基,卤代(1-6C)烷基,(2-6C)烯基,(2-6C)炔基,苯基,苯氧基,氰基, 硝基,羟基和羧基; 并且其中Ar可以带有其它取代基; 其药学上可接受的盐抑制角鲨烯合成物,因此可用于降低血浆中的胆固醇水平。 制备式(I)化合物的方法也被称为含有它们的药物组合物及其在医药中的用途。
    • 200. 发明申请
    • 4-ARYL-4-HYDROXY-TETRAHYDROPYRANS AND 3-ARYL-3-HYDROXY-TETRAHYDROFURANS AS 5-LIPOXYGENASE INHIBITORS
    • 4-亚氨基-4-羟基四氢吡喃酮和3-氰基-3-羟基四氢呋喃作为5-LIPOXYGENASE抑制剂
    • WO1994025453A1
    • 1994-11-10
    • PCT/EP1994001277
    • 1994-04-25
    • ZENECA LIMITEDZENECA-PHARMA S.A.
    • ZENECA LIMITEDZENECA-PHARMA S.A.BIRD, Thomas, Geoffrey, ColerickCRAWLEY, Graham, CharlesLARGE, Michael, StewartPLE, Patrick
    • C07D405/12
    • C07D405/12C07D409/14C07D417/14C07D493/08
    • The invention concerns ether derivatives of the formula (I): Q -X-Ar-Q , wherein Q is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q is selected from the groups of formulae (II) and (III), wherein R is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R is (1-4C)alkyl; and R is hydrogen or (1-4C)alkyl; or R and R are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    • 本发明涉及式(I)的醚衍生物:Q 1 -X-Ar -Q 2,其中Q 1是任选取代的9,10或11元双环杂环部分,其含有一个或多个 两个氮杂原子和任选地含有另外的选自氮,氧和硫的杂原子; X是氧基,硫基,亚磺酰基或磺酰基; Ar是任选取代的亚苯基,吡啶二基,嘧啶二基,噻吩二基,呋喃二基,噻唑二基,恶唑二基,噻二唑二基或恶二唑二基。 和Q 2选自式(II)和(III)的基团,其中R 1是氢,(2-5C)烷酰基或任选取代的苯甲酰基; R 2是(1-4C)烷基; 和R 3是氢或(1-4C)烷基; 或R 2和R 3连接形成亚甲基,亚乙烯基,亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。