Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as
inhibitors of leukotriene biosynthesis
    1.
    发明授权
    Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    对称双杂芳基 - 甲氧基 - 苯基烷基羧酸盐作为白三烯生物合成的抑制剂

    公开(公告)号:US5795900A

    公开(公告)日:1998-08-18

    申请号:US703441

    申请日:1996-09-17

    摘要: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.9, (e)-NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.

    摘要翻译: 具有下式的化合物:其中W在每次出现时相同,并且选自任选取代的喹啉基,任选取代的苯并噻唑基,任选取代的苯并恶唑基,任选取代的苯并咪唑基,任选取代的喹喔啉基,任选取代的吡啶基,任选取代的嘧啶基, 取代的噻唑基; R 1和R 2独立地选自氢,烷基,卤代烷基,烷氧基,卤素; R3是价键或选自氢和烷基; X是价键或选自亚烷基,烯基和亚炔基; 并且Z选自(a)COM,(b)CH = NOA-COM,(c)CH2-ON = A-COM其中A选自亚烷基和亚环烷基,M选自(a)药学上可接受的代谢 可裂解基团,(b)-OR6,(c)-NR7R8,(d)-NR6SO2R9,(e)-NH-四唑基,(f)甘氨酰抑制白三烯生物合成,可用于治疗过敏性和炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

    Iminoxyderivatives of fenamates as inhibitors of prostaglandin
biosynthesis
    3.
    发明授权
    Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
    作为前列腺素生物合成抑制剂的灭火剂的亚硝基衍生物

    公开(公告)号:US5863946A

    公开(公告)日:1999-01-26

    申请号:US660046

    申请日:1996-06-06

    CPC分类号: C07D257/04 C07C251/58

    摘要: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; X is absent or is alkylene; A is absent or is selected from optionally substituted alkylene, optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, optionally substituted alkenylene, and ##STR2## or R.sup.2 and A together define a saturated 5- to 8-membered optionally substituted carbocyclic or heterocyclic ring to which the group Z is attached; Z is selected from (a) hydrogen, (b) COM wherein M is selected from the group consisting of --OR.sup.5, a pharmaceutically acceptable cation, --NR.sup.7 R.sup.8, and a pharmaceutically acceptable, metabolically cleavable group, (c) --OR.sup.3, (d) tetrazolyl, (e) --CH(OR.sup.3)--CH.sub.2 OR.sup.9, (f) --CH(OR.sup.3)--CH.sub.2 --CH.sub.2 OR.sup.9, (g) --CH(OR.sup.3)--CH(OR.sup.9)--CH.sub.2 OR.sup.10, and (h) .dbd.N--OR.sup.3 ; and R.sup.1, R.sup.2, R.sup.3, R.sup.9, and R.sup.10 are independently selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译: 具有式“IMAGE”的化合物或其药学上可接受的盐,其中Y选自卤素,烷基和卤代烷基; n为0,1,2或3; X不存在或是亚烷基; A不存在或选自任选取代的亚烷基,任选取代的亚环烷基,任选取代的亚环烷基,其中一个或两个碳原子被一个或两个独立地选自O,S和N的杂原子,任选取代的亚烯基取代,以及

    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds
having lipoxygenase inhibitory activity
    4.
    发明授权
    N-substituted-furylalkenyl hydroxamic acid and N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
    N-取代呋喃基异羟肟酸和具有脂氧合酶抑制活性的N-羟基脲化合物

    公开(公告)号:US5169854A

    公开(公告)日:1992-12-08

    申请号:US841968

    申请日:1992-02-26

    摘要: Compounds useful in inhibiting the biosynthesis of leukotrienes have the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group, R.sup.4 is alkyl, cycloalkyl or --NR.sup.5 R.sup.6, where R.sup.5 and R.sup.6 are hydrogen, alkyl, cycloalkyl or alkanoyl, where A is a valence bond or is a straight or branched divalent alkylene group of from one to twelve carbon atoms, R.sup.2 and R.sup.3 are independently selected from hydrogen, straight or branched alkyl of from one to twelve carbon atoms, halogen, or trifluoroalkyl, and R.sup.1 is selected from phenoxy, phenylthio, 2-, 3-, or 4-pyridyloxy, 1 or 2-naphthyloxy, or 2,4,5, or 8-quinolyloxy, all optionally substituted with alkyl, haloalkyl, alkoxy, hydroxy or halogen.

    摘要翻译: 可用于抑制白细胞三烯生物合成的化合物具有其中M是氢,药学上可接受的阳离子或代谢可裂解基团的结构,R 4是烷基,环烷基或-NR 5 R 6,其中R 5和R 6是氢,烷基,环烷基或 烷酰基,其中A是价键或是具有1至12个碳原子的直链或支链二价亚烷基,R 2和R 3独立地选自氢,具有1至12个碳原子的直链或支链烷基,卤素或三氟烷基 ,R1选自苯氧基,苯硫基,2-,3-或4-吡啶氧基,1或2-萘氧基或2,4,5或8-喹啉氧基,全部任选被烷基,卤代烷基,烷氧基,羟基 或卤素。

    Real time sensor for therapeutic radiation delivery
    8.
    发明授权
    Real time sensor for therapeutic radiation delivery 失效
    实时传感器用于治疗辐射传播

    公开(公告)号:US5704890A

    公开(公告)日:1998-01-06

    申请号:US455586

    申请日:1995-05-31

    IPC分类号: A61N5/10 G01T5/08 A61N5/00

    摘要: The invention is a real time sensor for therapeutic radiation. A probe is placed in or near the patient that senses in real time the dose at the location of the probe. The strength of the dose is determined by either an insertion or an exit probe. The location is determined by a series of vertical and horizontal sensing elements that gives the operator a real time read out dose location relative to placement of the patient. The increased accuracy prevents serious tissue damage to the patient by preventing overdose or delivery of a dose to a wrong location within the body.

    摘要翻译: 本发明是用于治疗辐射的实时传感器。 将探针放置在患者体内或附近,实时感测探针位置处的剂量。 剂量的强度由插入或出口探针确定。 该位置由一系列垂直和水平感测元件确定,其给予操作者相对于患者的放置的实时读出剂量位置。 提高的准确性通过防止剂量过量或递送到身体内的错误位置来防止对患者的严重组织损伤。