Hydroisoquinoline derivatives
    13.
    发明授权
    Hydroisoquinoline derivatives 失效
    氢异喹啉衍生物

    公开(公告)号:US5441956A

    公开(公告)日:1995-08-15

    申请号:US175371

    申请日:1994-01-05

    摘要: ##STR1## Compounds of formula (I) in which, R is linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, aralkyl or furan-2-yl alkyl; R
    1 and R
    2 , which may be the same or different, are each hydrogen, hydroxy, alkoxy, or halogen; R
    3 is hydrogen, hydroxy or alkoxy; "Het" is optionally substituted single or fused heteroxyclic ring, containing from 5 to 10 ring atoms and comprising up to four heteratoms in the or each ring, selected from oxygen, nitrogen and sulphur; R
    4 and R
    5 , which may be the same or different, are each hydrogen alkyl, halogen, nitro; CF, cyano, alkoxy carbonyl, NH, alkylcarbonylamino, hydroxy, alkoxy, or benzyl, are selective delta receptor agonists and are useful in the treatment of pain.

    摘要翻译: PCT No.PCT / EP92 / 01483第 371日期1994年1月5日 102(e)日期1994年1月5日PCT提交1992年7月1日PCT公布。 公开号WO93 / 01186 (I)其中R为直链或支链烷基,环烷基,环烷基烷基,烯基,芳基,芳烷基或呋喃-2-基烷基的式(I)化合物; R 1和R 2可以相同或不同,分别为氢,羟基,烷氧基或卤素; R3是氢,羟基或烷氧基; “Het”是任选取代的单或稠环氧环,其含有5至10个环原子,并且在该环或每个环中包含至多四个杂原子,选自氧,氮和硫; R 4和R 5可以相同或不同,分别为氢烷基,卤素,硝基; CF,氰基,烷氧基羰基,NH,烷基羰基氨基,羟基,烷氧基或苄基是选择性δ受体激动剂,可用于治疗疼痛。

    Substituted isoquinoline compounds, pharmaceutical composition and
method of use in treating pain in mammals
    14.
    发明授权
    Substituted isoquinoline compounds, pharmaceutical composition and method of use in treating pain in mammals 失效
    取代的异喹啉化合物,药物组合物和用于治疗哺乳动物疼痛的方法

    公开(公告)号:US5254564A

    公开(公告)日:1993-10-19

    申请号:US553723

    申请日:1990-07-16

    摘要: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.sub.1-6 alkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are not simultaneously hydrogen;R.sub.8 and R.sub.9, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.10, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.12, --NHSO.sub.2 R.sub.13, --CH.sub.2 SO.sub.2 NR.sub.14 R.sub.15, in which each of R.sub.10 to R.sub.15 is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl, is useful for the treatment of pain, and or hyponatraemic disease states and/or cerebral ischaemia.

    Method for the treatment of a hyponatremic disease
    16.
    发明授权
    Method for the treatment of a hyponatremic disease 失效
    治疗高血压疾病的方法

    公开(公告)号:US5087630A

    公开(公告)日:1992-02-11

    申请号:US422122

    申请日:1989-10-16

    摘要: Compounds of formula (Ia), or pharmaceutically acceptable salts or solvates thereof, ##STR1## in which A, together with the nitrogen atom, represents --(CH.sub.2)p--, where p is an integer from 3 to 6, or an optionally substituted tetrahydroisoquinoline ring system;each of R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl, or together form a C.sub.2-6 polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.x is hydrogen, C.sub.1-6 alkyl or phenyl, or together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group; and R comprises a substituted or unsubstituted carbocyclic or heterocyclic aromatic group;and compounds of formula (Ib) ##STR2## in which: R, R.sub.1, R.sub.2 and X are as defined in formula (Ia)R.sub.a is C.sub.1-6 alkyl or phenyl;R.sub.b is hydrogen or together with R.sub.a forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and`Het` is an optionally substituted single or fused ring heterocyclic group containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring, selected from oxygen, nitrogen and sulphur,are useful as diuretic agents.

    Azolyl-derivatives having fungicidal activity
    17.
    发明授权
    Azolyl-derivatives having fungicidal activity 失效
    具有杀真菌活性的唑基衍生物

    公开(公告)号:US4810718A

    公开(公告)日:1989-03-07

    申请号:US74352

    申请日:1987-07-16

    摘要: Compounds having the formula: ##STR1## wherein: m=1 or 2;q=1 or 2;Y=a haloethylene or haloethenyl group;X is oxygen or sulfur;A=N or CH;R is H, CH.sub.3 or F;R.sub.1 is selected from the group comprising chlorine, bromine, fluorine CF.sub.3, phenyl, C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 haloalkoxy, alkylthio, haloalkylthio radical, wherein the halogen is Cl, Br or F;R.sub.2 is selected from the group comprising H, chlorine, bromine or fluorine; andR.sub.f is a C.sub.1 -C.sub.5 polyfluoroalkyl or a C.sub.2 -C.sub.4 polyfluoroalkenyl radical containing at least 3 fluorine atoms and, optionally, other halogen atoms selected from the group comprising Cl and Br. These compounds have good fungicidal activity.

    摘要翻译: 具有下式的化合物:其中:m = 1或2; q = 1或2; Y =卤代乙烯基或卤代乙烯基; X是氧或硫; A = N或CH; R为H,CH 3或F; R 1选自氯,溴,氟CF 3,苯基,C 1 -C 2烷氧基,C 1 -C 2卤代烷氧基,烷硫基,卤代烷硫基,其中卤素是Cl,Br或F; R2选自H,氯,溴或氟; 并且Rf是含有至少3个氟原子的C1-C5多氟烷基或C2-C4多氟烯基,以及任选的选自Cl和Br的其它卤素原子。 这些化合物具有良好的杀真菌活性。