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43 条记录 (耗时 0.038 秒)

    Benzanilide derivatives
    6.
    发明授权
    Benzanilide derivatives 失效
    苯甲酰苯胺衍生物

    公开(公告)号：US5510350A

    公开(公告)日：1996-04-23

    申请号：US237297

    申请日：1994-05-03

    申请人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

    发明人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

    IPC分类号： A61K31/495 ,  A61K20060101 ,  A61K31/165 ,  A61K31/41 ,  A61K31/496 ,  A61K31/53 ,  A61P5/00 ,  A61P9/12 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D249/04 ,  C07D249/06 ,  C07D249/08 ,  C07D249/14 ,  C07D271/06 ,  C07D271/07 ,  C07D271/08 ,  C07D271/10 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/12 ,  C07D285/125 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D249/08 ,  C07D249/06 ,  C07D271/06 ,  C07D271/07 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/12

    摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl and C.sub.1-6 alkoxy;R.sup.2 represents a phenyl group substituted by a group selected from ##STR2## and optionally further substituted by one or two substituents selected from halogen atoms, C.sub.1-6 alkoxy, hydroxy, and C.sub.1-6 alkyl;R.sup.3 represents the group ##STR3## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C.sub.1-6 alkoxy and C.sub.1-6 alkyl;R.sup.6 represents a hydrogen atom or a group selected from --NR.sup.9 R.sup.10 and a C.sub.1-6 alkyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 acyloxy and --SO.sub.2 R.sup.11 ;R.sup.7, R.sup.8 and R.sup.9, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-6 alkyl group;R.sup.10 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.1-6 acyl, benzoyl and --SO.sub.2 R.sup.11 ;R.sup.11 represents a C.sub.1-6 alkyl group or a phenyl group;Z represents an oxygen atom or a group selected from NR.sup.8 and S(O).sub.k ; andk represents zero, 1 or 2.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

    摘要翻译： 本发明提供式（I）化合物：其中R 1表示氢原子或卤素原子或选自C 1-6烷基和C 1-6烷氧基的基团;或其生理学上可接受的盐或溶剂化物。 R 2表示被选自下列基团取代的苯基，并任选进一步被一个或两个选自卤素原子，C 1-6烷氧基，羟基和C 1-6烷基的取代基取代; R 3表示基团R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或选自羟基，C 1-6烷氧基和C 1-6烷基的基团。 R6表示氢原子或选自-NR9R10和任选被一个或两个选自C 1-6烷氧基，C 1-6酰氧基和-SO 2 R 11的取代基取代的C 1-6烷基的基团; R 7，R 8和R 9可以相同或不同，各自独立地表示氢原子或C 1-6烷基; R 10表示氢原子或选自C 1-6烷基，C 1-6酰基，苯甲酰基和-SO 2 R 11的基团; R11表示C1-6烷基或苯基; Z表示氧原子或选自NR8和S（O）k的基团; 并且k代表0,1或2.化合物可用于治疗或预防抑郁症和其它CNS疾病。

    1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine H.sub.2 -antagonists
    8.
    发明授权
    1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine H.sub.2 -antagonists 失效

    公开(公告)号：US4442110A

    公开(公告)日：1984-04-10

    申请号：US324440

    申请日：1981-11-24

    申请人： John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon ,  Barry J. Price ,  Michael Martin-Smith ,  Duncan B. Judd

    发明人： John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon ,  Barry J. Price ,  Michael Martin-Smith ,  Duncan B. Judd

    IPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  A01N43/64

    CPC分类号： C07D209/48 ,  C07D249/14 ,  C07D307/52 ,  C07D317/12 ,  Y10S514/926 ,  Y10S514/927

    摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered alicyclic heterocyclic ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5-positions, the furan ring optionally bearing a further substituent R.sub.7 adjacent to the group R.sub.1 R.sub.2 N-Alk-, or Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions;R.sub.7 represents halogen or C.sub.1-4 alkyl which may be substituted by hydroxy or C.sub.1-4 alkoxy;X represents --CH.sub.2 --, ##STR2## --O-- or --S-- whereR.sub.6 represents hydrogen or methyl;n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl having at least two carbon atoms, alkoxyalkyl or aryl; andR.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl or R.sub.4 and R.sub.5 may together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain another heteroatom, or the group ##STR3## or R.sub.4 and R.sub.5 taken together may represent the group .dbd.CR.sub.8 R.sub.9 where R.sub.8 represents aryl or heteroaryl and R.sub.9 represents hydrogen or alkyl.Preferably when X represents an oxygen atom or ##STR4## and n is zero, then Q only represents a benzene ring. The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    Substituted furan compounds and pharmaceutical compositions containing them
    9.
    发明授权
    Substituted furan compounds and pharmaceutical compositions containing them 失效
    取代的呋喃化合物和含有它们的药物组合物

    公开(公告)号：US4288443A

    公开(公告)日：1981-09-08

    申请号：US124115

    申请日：1980-02-25

    申请人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    发明人： Duncan B. Judd ,  John W. Clitherow ,  Barry J. Price ,  John Bradshaw

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P1/04 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D307/54

    CPC分类号： C07D307/56 ,  C07D307/52 ,  C07D307/68

    摘要： The invention relates to compounds of the general formula ##STR1## and physiologically acceptable salts and N-oxides, hydrates and bioprecursors thereof, in which R.sub.1 and R.sub.2 which may be the same or different each represent hydrogen, C.sub.1-8 alkyl, C.sub.4-8 cycloalkyl, C.sub.3-6 alkenyl, aralkyl with 1 to 4 carbon atoms in the alkyl residue or C.sub.1-8 alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.5 represents hydrogen or C.sub.1-8 alkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7 membered heterocyclic ring which may additionally contain the heterofunction O or ##STR3## R.sub.3 represents straight or branched chain C.sub.1-8 alkyl, alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkoxycarbonyl, alkyl thioalkyl with 1 to 8 carbon atoms in each alkyl residue, halogen or aryl;R.sub.4 represents hydrogen, C.sub.1-8 alkyl, C.sub.3-6 alkenyl or alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue;X represents --O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHNO.sub.2 where R.sub.6 represents hydrogen, nitro, cyano, C.sub.1-8 alkyl, aryl, C.sub.1-8 alkylsulphonyl or arylsulphonyl;m represents an integer from 2 to 4 inclusive; andn represents an integer which is 1 or 2, or additionally when X is --S-- n may also be zero.The invention also relates to processes for the production of such compounds, pharmaceutical compositions containing them and certain novel intermediates used in their production, i.e. amines of the formula ##STR4## and alcohols of the formula ##STR5## The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译： 本发明涉及通式为（I）的化合物及其生理上可接受的盐和N-氧化物，水合物和生物前体，其中可以相同或不同的R 1和R 2各自表示氢，C 1-8烷基， C4-8环烷基，C3-6烯基，在烷基中具有1至4个碳原子的芳烷基或被氧原子间断的C1-8烷基或其中R5表示氢或C1-8烷基的基团，或R1 并且R 2可以与它们所连接的氮原子一起形成饱和的单环5至7元杂环，其可另外含有杂官能O，或者R 3表示直链或支链C 1-8烷基，烷氧基烷基与1至 每个烷基残基中的8个碳原子，C 1-8羟基烷基，C 1-8烷氧基羰基，每个烷基残基中具有1至8个碳原子的烷基硫代烷基，卤素或芳基; R4表示氢，C1-8烷基，C3-6烯基或每个烷基残基具有1至8个碳原子的烷氧基烷基; X表示-O-或-S-; Y表示= S，= O，= NR6或= CHNO2，其中R6表示氢，硝基，氰基，C1-8烷基，芳基，C1-8烷基磺酰基或芳基磺酰基; m表示2〜4的整数， 并且n表示1或2的整数，或者当X是-S-n时也可以为零。 本发明还涉及生产这种化合物的方法，含有它们的药物组合物和它们生产中使用的某些新型中间体，即式（III）的胺和式的醇（VIII）。化合物 式（I）表示作为选择性组胺H2拮抗剂的药理学活性。

    Calibrating dispensing device performance for complex and/or non-aqueous liquids
    10.
    发明申请
    Calibrating dispensing device performance for complex and/or non-aqueous liquids 有权
    为复合和/或非水性液体校准分配装置性能

    公开(公告)号：US20070141709A1

    公开(公告)日：2007-06-21

    申请号：US11305301

    申请日：2005-12-16

    申请人： Keith Albert ,  John Bradshaw ,  Alex Rogers

    发明人： Keith Albert ,  John Bradshaw ,  Alex Rogers

    IPC分类号： G01N31/00 ,  G06F19/00

    CPC分类号： G01N35/1016 ,  G01F25/0092 ,  G01N1/38 ,  G01N21/25 ,  Y10T436/10 ,  Y10T436/25 ,  Y10T436/25625

    摘要： A method for precisely and accurately determining the volume of a test liquid aliquot which can be used to calibrate a liquid delivery device. The method is particularly useful for determining the volume of an aliquot of a test liquid which is complex or non-aqueous, or is both complex and non-aqueous. The test-stock mixture contains at least the test liquid and a stock solution including a first dye, the first dye having absorbance characteristics which are measurably distinguishable from the absorbance characteristics of a second dye. The test-stock mixture is mixed with a diluent including the second dye to form a sample solution to be used to measure absorbances of the first dye and the second dye. The volume of the test-stock mixture aliquot is calculated by using a formula based on the Beer-Lambert law which incorporates the measured absorbance values and a dilution characteristic of the test-stock mixture. The test liquid and the stock solution are combined gravimetrically in a controlled ratio so that the flow characteristics of the test-stock mixture correspond to the flow characteristics of the test liquid and without affecting the ability to distinguish the absorbance characteristics between the first dye and the second dye.

    摘要翻译： 用于精确和准确地确定可用于校准液体输送装置的测试液体等分试样的体积的方法。 该方法特别可用于测定复合物或非水性的测试液体的等分试样的体积，或者是复合的和非水性的。 试料混合物至少包含测试液体和包含第一染料的原液，所述第一染料具有与第二染料的吸光度特性可测量的吸光度特性。 将试料混合物与包括第二染料的稀释剂混合以形成用于测量第一染料和第二染料的吸光度的样品溶液。 通过使用基于Beer-Lambert定律的公式计算测试样品混合物等分试样的体积，其中包含测量的吸光度值和测试样品混合物的稀释特性。 测试液体和储备溶液以受控比例重量分数组合，使得测试液体的流动特性对应于测试液体的流动特性，并且不影响区分第一染料和 第二染料。