Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity
    81.
    发明公开
    Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity 失效
    胍类取代基杂环衍生物组蛋白-H-2拮抗剂Wirkung。

    公开(公告)号:EP0059597A2

    公开(公告)日:1982-09-08

    申请号:EP82300946.9

    申请日:1982-02-24

    摘要: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I:-
    in which R' and R 2 , same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R 1 and R 2 is halogen substituted, or R 2 is hydrogen and R 1 is R 5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO. SO 2 or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R 6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R 2 is H and R 1 is H, 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups: D is O or S; R 4 is H or 1-6C alkyl; R 3 is H or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

    摘要翻译: 本发明涉及作为组胺H-2拮抗剂并抑制胃酸分泌的羰基衍生物。 根据本发明,其中提供了式I的胍衍生物:其中R1和R2相同或不同,为氢或1-10C烷基,3-8C环烷基或4-14C环烷基烷基,每个烷基, 任选地携带一个或多个F,Cl或Br原子的环烷基或环烷基烷基,条件是R 1和R 2中的一个是卤素取代的,或者R 2是氢,R 1是其中W是任选被1或2取代的2-6C亚烷基的R 5-EW 1-4C烷基,E是O,S,SO,SO2或NR6,其中R6是H或1-6C烷基,R5是H或任选被1或2个1-4C烷基取代的1-6C烷基,或R5和R6 连接形成吡咯烷,哌啶,吗啉,哌嗪或N-甲基哌嗪环,或R 2为H,R 1为H,1-10C烷基,3-8C环烷基,4-14C环烷基烷基,3-6C烯基,3-6C 炔基,1-6C烷酰基,6-10C芳基,7-11C芳烷基或7-11C芳酰基; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基,或其中任选插入一个或两个基团的1-8C亚烷基; D为O或S; R4是H或1-6C烷基; R3是H或本说明书中描述的各种基团及其药学上可接受的酸加成盐。 还描述了制造方法和药物组合物。

    In-mold coating compositions containing a non-isocyanate-reactive unsaturated resin, a non-isocyanate-reactive monomer and a free isocyanate-containing compound
    84.
    发明公开
    In-mold coating compositions containing a non-isocyanate-reactive unsaturated resin, a non-isocyanate-reactive monomer and a free isocyanate-containing compound 失效
    模内涂布组合物,包含不与异氰酸酯反应的不饱和树脂,单体不与异氰酸酯反应,和一个自由异氰酸酯基的化合物。

    公开(公告)号:EP0048117A2

    公开(公告)日:1982-03-24

    申请号:EP81304043.3

    申请日:1981-09-04

    申请人: ICI AMERICAS INC.

    发明人: Kuehn, Erich

    摘要: Fully cured reinforced molded resins such as polyester, polyurea-urethane, polyurea, polyurethane, polyisocyanurate, polyepoxy and polycarbonate resins can be in-mold coated to cover surface defects such as sink marks and microcracks with an improved coating composition comprising 5-94% by weight of an ethylenically unsaturated base resin free of groups reactive with isocyanate radicals; 5-94% by weight of an ethylenically unsaturated monomer free of groups reactive with isocyanate radicals; and 1-20% by weight of isocyanate-containing compounds or compounds which decompose to form free isocyanate-containing compounds. Such coatings unexpectedly have improved adherence to molded articles over those obtained from similar compositions which contain no free isocyanate. The compositions may contain minor amounts of emulsifiers, fillers, catalysts, cross-linking agents, dryers and pigments. In particular, the coatings obtained when the compositions contain electroconductive fillers can be painted by standard electrostatic paint techniques.

    摘要翻译: 完全固化的增强的成型体的树脂:例如聚酯,聚脲 - 氨基甲酸酯,聚脲,聚氨酯,聚异氰脲,聚环氧和聚碳酸酯树脂可以是在模内涂覆,以覆盖表面缺陷:如凹痕,并在改进的涂层组合物的微裂纹与包含5-94%的 重量的游离的异氰酸酯与自由基反应性基团的烯属不饱和树脂基体材料; 通过自由与异氰酸酯自由基反应性基团的烯属不饱和单体的5-94%重量; 和按重量计能分解生成自由含异氰酸酯化合物含异氰酸酯的化合物或化合物的1-20%。 搜索涂料出人意料地提高了坚持对那些从不含游离异氰酸酯类似的组合物获得的模塑制品。 组合物可以含有乳化剂,填料,催化剂,交联剂,颜料和干衣机的少量。 特别是涂料时获得的组合物含有导电填料,可通过静电涂料标准技术来画。

    Guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them
    86.
    发明公开
    Guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them 失效
    胍衍生物,其制备方法和含有它们的药物组合物。

    公开(公告)号:EP0030092A1

    公开(公告)日:1981-06-10

    申请号:EP80304023.7

    申请日:1980-11-11

    摘要: The invention relates to a guanidine of the formula:-
    in which R 1 and R 2 are H, Ci-io alkyl, C 3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C 1-6 and the cycloalkyl part is C 3-8 , each of the alkyl, cycloalkyl and cycloalkylal- kyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R' and R' is a halogen substituted alkyl, cycloalkyl or cycloalkyl-alkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen;

    ring X is phenyl carrying 1 or 2 optional substitutents or a 5- or 6-membered heterocyclic aromatic ring containing 1, 2 or 3 hetero atoms selected from 0, N and S, which heterocyclic ring may, carry a single optional substituent selected from F, Cl, Br, I, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, trifluoromethyl, hydroxy and amino;
    Y is 0, S, a direct bond, methylene, vinylene, SO or NR 4 in which R 4 is H or C 1-6 alkyl;
    m is 0 to 4 and n is 1 to 5, provided that when Y is 0, SO or NR 4 , n is 2 to 5;
    R 3 has various significances; and the pharmaceutically-acceptable acid-addition salts thereof.
    Manufacturing processes and pharmaceutical compositions are also described.

    摘要翻译: 本发明涉及下式的胍: - ... ...其中R <2>为H <1>和R,C 1-10烷基,C 3-8环烷基或环烷基烷基,其中烷基部分是C 1-6 和环烷基部分是C 3-8,每一个烷基,环烷基和环烷基烷基通过选自F,Cl和Br中的一种或多种卤素任选substituiertem的,提供并 - [R <1>和R的<2>的至少一个是一个 卤素取代的烷基,环烷基或环烷基 - 烷基和提供thatthere是上连接到氮直接的碳上没有卤素取代基; ...环X是苯基携带1个或2个取代基任选的或5-或6元杂芳环含有1 ,2或3个杂原子选自O,N和S,选择该杂环可以,携带选自F,Cl,溴,我所选择的单一的任选取代基,C1-6烷基,C1-6烷氧基,C1-6烷硫基,三氟甲基 ,羟基和氨基; ... Y是O,S,直接键合,亚甲基,亚乙烯基,SO或NR <4>中R <4>是H或C 1-6烷基; ...... m是0至4和 n为1至5,只要没当Y是O,SO或NR <4>中,n为2至5; ... [R <3>具有多种意义; ...和药学上可接受的酸加成盐。 所以... 制造工艺和药物组合物进行说明。

    Electrostatic safety element for an electric initiator
    87.
    发明公开
    Electrostatic safety element for an electric initiator 失效
    Elektrostatisches Sicherheitselementfüreinen elektrischenInitialzünder。

    公开(公告)号:EP0029671A1

    公开(公告)日:1981-06-03

    申请号:EP80303920.5

    申请日:1980-11-04

    申请人: ICI AMERICAS INC.

    IPC分类号: F42B3/18

    CPC分类号: F42B3/18

    摘要: An electrostatic safety element within an electric initiator having the form of a disc (40) surrounding lead wires for preventing accidental ignition due to static electricity. It comprises a non-conductive circular substrate (42) having a slotted opening (44) for the lead wires, and a conductive coating layer (46) on at least one face of the substrate to conduct electricity from the leads to the metallic initiator casing in the event of electrostatic discharge. This conductive layer (46) should be in electrical contact with the casing but not with the lead wires; to that end the substrate (42) is left uncoated in the immediate vicinity of the opening (44).

    摘要翻译: 电引发器内的静电安全元件,其具有围绕引线的盘(40)的形式,用于防止由静电引起的意外点火。 它包括一个非导电圆形基底(42),它具有用于导线的开槽开口(44)和在该基片的至少一个表面上的导电涂层(46),以将导线从导线传导到金属引导器外壳 在静电放电的情况下。 该导电层(46)应与壳体电接触而不与导线接触; 为此,衬底(42)在开口(44)的紧邻附近未被涂覆。