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    Quinolone sulphonamides useful as antihypertensive agents
    5.
    发明授权
    Quinolone sulphonamides useful as antihypertensive agents 失效
    喹诺酮磺酰胺可用作抗高血压药

    公开(公告)号：US4772614A

    公开(公告)日：1988-09-20

    申请号：US874217

    申请日：1986-06-13

    申请人： Roy V. Davies ,  James Fraser ,  Kenneth J. Nichol

    发明人： Roy V. Davies ,  James Fraser ,  Kenneth J. Nichol

    IPC分类号： C07D209/38 ,  A61K31/47 ,  A61P9/10 ,  A61P9/12 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C303/40 ,  C07C311/35 ,  C07D215/22 ,  C07D215/36 ,  C07D215/56

    CPC分类号： C07D215/36

    摘要： Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel.Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.

    摘要翻译： 具有抗高血压活性的喹诺酮具有通式I，其中X是任选取代的苯环的残基; R为低级烷基; R3是氢或低级烷基; R 1和R 2可以相同或不同，为氢，低级烷基，或与它们相连的氮原子一起形成任选地含有另外的杂原子的5至7元饱和杂环，该杂原子选自氮， 氧和硫，并任选被一个或多个低级烷基取代; 并且喹诺酮核的位置2和3之间的虚线表示任选的键。 该化合物可用作抗高血压药。 它们也被用于治疗心力衰竭和缺血性心脏病。 除了三种化合物之外，1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺，1，N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和6,7-二甲氧基 - 甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺，式I的喹诺酮是新的。 描述含有式I化合物的药物组合物。 还描述了制备新喹诺酮类的方法。

    POTASSIUM ION CHANNEL MODULATORS AND USES THEREOF
    6.
    发明申请
    POTASSIUM ION CHANNEL MODULATORS AND USES THEREOF 失效
    钾离子通道调节剂及其用途

    公开(公告)号：US20120065270A1

    公开(公告)日：2012-03-15

    申请号：US12746524

    申请日：2008-12-05

    申请人： Simon David Edwards ,  Meriel Ruth Kimberly ,  Kanesalingam Suthaharan ,  Nawaz Mohammed Khan ,  Geoff Lawton

    发明人： Simon David Edwards ,  Meriel Ruth Kimberly ,  Kanesalingam Suthaharan ,  Nawaz Mohammed Khan ,  Geoff Lawton

    IPC分类号： A61K31/18 ,  A61P13/02 ,  A61P25/22 ,  A61P25/08 ,  A61P29/00 ,  A61P9/00 ,  A61P27/16 ,  A61P25/06 ,  A61P25/28 ,  A61P3/00 ,  A61P35/00 ,  A61P21/00 ,  A61P25/00 ,  A61P37/00 ,  C07C311/39 ,  C07C311/35

    CPC分类号： C07C311/35 ,  C07C311/40

    摘要： Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs wherein: Ar1 and Ar2=aryl or heteroaryl; a=0 to 5; R1=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R1 is the same or different; b=0 to 5; R2=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and where b is >1, each R2 is the same or different; V=(CR3aR3b)pSO2N(R3b)X and (CR3aR3b)pN(R3b)SO2(X); W=NR4a, O, S, S═O, SO2 and C(R4aR4b)2; X=hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with ≧1 NR8R9 groups wherein R8 and R9+nitrogen atom form a saturated or partially unsaturated heterocyclic group which is optionally further substituted by ≧1 substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monoalkylamino, dialkylamino and hydroxyl; Y and Z each ═(CR5aR5b)n1, C═O, SO2, C(═O)NR5a, C(═O)NR5aSO2 or C═O(R5aR5b)n2; R3a, R3b, R4a, R4b, R5a and R5b each=hydrogen, alkyl, cycloalkyl, aryl or heteroaryl; n1 and n2 each =0 to 2; and p=0 to 2; are excellent selective modulators of potassium ion flux through KCNQ2, KCNQ3 and/or KCNQ2/3 channels, making them of use in treating and preventing a number of conditions including pain and lower urinary tract disorders.

    摘要翻译： 式（I）化合物及其药理学上可接受的盐和前药，其中：Ar1和Ar2 =芳基或杂芳基; a = 0〜5; R 1 =烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基和氰基，其中a≥1，每个R 1相同或不同; b = 0〜5; R 2 =烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基和氰基，其中b≥1，各自相同或不同; V =（CR3aR3b）pSO2N（R3b）X和（CR3aR3b）pN（R3b）SO2（X）; W = NR4a，O，S，S = O，SO2和C（R4aR4b）2; X =羟基烷基，烷氧基烷基，卤代烷氧基烷基，芳氧基烷基，聚亚烷基二醇残基，氨基烷基，单烷基氨基烷基，二烷基氨基烷基和被1个NR8R9基团取代的烷基，其中R8和R9 +氮原子形成饱和或部分不饱和的杂环基，其任选进一步被≧ 1个选自烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，硝基，氨基，单烷基氨基，二烷基氨基和羟基的取代基; Y和Z各自为（CR5aR5b）n1，C = O，SO2，C（= O）NR5a，C（= O）NR5aSO2或C = O（R5aR5b）n2; R3a，R3b，R4a，R4b，R5a和R5b各自为氢，烷基，环烷基，芳基或杂芳基; n1和n2各自= 0至2; 和p = 0至2; 是通过KCNQ2，KCNQ3和/或KCNQ2 / 3通道的钾离子通量的优异选择性调节剂，可用于治疗和预防许多病症，包括疼痛和下尿路疾病。

    Triazole methine compounds
    9.
    发明授权
    Triazole methine compounds 失效
    三唑次甲基化合物

    公开(公告)号：US5068348A

    公开(公告)日：1991-11-26

    申请号：US454087

    申请日：1989-12-20

    申请人： Max A. Weaver ,  Wayner P. Pruett ,  Samuel D. Hilbert

    发明人： Max A. Weaver ,  Wayner P. Pruett ,  Samuel D. Hilbert

    IPC分类号： C07C229/44 ,  C07C255/34 ,  C07C311/35 ,  C07C311/42 ,  C07C317/44 ,  C07C323/60 ,  C07D249/12 ,  C08G63/685 ,  C08G64/04 ,  C08K5/00 ,  C08K5/315

    CPC分类号： C07C317/44 ,  C07C229/44 ,  C07C255/34 ,  C07C311/35 ,  C07C311/42 ,  C07C323/60 ,  C08G63/6858 ,  C08G64/045 ,  C08K5/005 ,  C08K5/315

    摘要： A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.0 to about 100,000 ppm, of the reactant residue moieties of one or more of such bis- or tris-methine compounds.

    摘要翻译： 可用于掺入用于食品包装等的聚合物组合物中的组合物，其包含具有结构式为“IMAGE”的双或三 - 次甲基化合物，其中A选自基团 其中R'和R“各自选自氯，溴，氟，烷基，烷氧基，芳基，芳氧基和芳硫基; 每个n独立地为0,1,2; R1选自各种基团，例如环烷基，苯基，可被取代的直链或支链烷基; R2是亚烷基等; R3，R4和R5各自选自氢和烷基; 并且P和Q以及P1和Q1选自氰基，烷氧基，碳酰氧基，卡巴尔基氧基等。 本发明组合物特别适用于成型或纤维级缩聚物; 最优选地，其中共聚有总共为1.0至约100,000ppm的一种或多种这样的双 - 或三 - 次甲基化合物的反应物残余部分的这种聚合物。