Pharmacologically active amine boranes
    61.
    发明授权
    Pharmacologically active amine boranes 失效
    药理活性胺硼烷

    公开(公告)号:US4312989A

    公开(公告)日:1982-01-26

    申请号:US68356

    申请日:1979-08-21

    IPC分类号: C07F5/00 C07F5/02 A61K31/69

    CPC分类号: C07F5/006 C07F5/027

    摘要: The use of amine boranes to inhibit the inflammation process is disclosed. These boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz, 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.

    摘要翻译: 公开了使用胺硼烷来抑制炎症过程。 这些硼烷是α-氨基酸的硼类似物,有效地阻断了以下:一般炎症,诱发的关节炎和与炎症疼痛相关的扭动反射。 与胸膜炎相关的炎症也受到抑制。 硼类似物在体外显示以抑制溶酶体酶从肝脏和多形核嗜中性粒细胞(PMN)的释放。 此外,前列腺素合成被这些化合物以低浓度(即10-6M)阻断。 肝氧化磷酸化过程也被这些化合物解偶联,但PMN迁移在10-4M不变。 PMN中环磷酸腺苷的升高与体内抗关节炎活性呈正相关。 啮齿动物的研究表明,这些硼类似物可以以安全的治疗剂量使用。 本发明的范围包括几种化合物本身。

    Caged boron-nitrogen compounds containing ester substitution
    62.
    发明授权
    Caged boron-nitrogen compounds containing ester substitution 失效
    含有异氰酸酯的硝酸化合物

    公开(公告)号:US3755388A

    公开(公告)日:1973-08-28

    申请号:US3755388D

    申请日:1971-05-18

    发明人: LUDWIG J WITSKEN K

    CPC分类号: C07F5/006 C07F5/04 C08K5/55

    摘要: CAGED BORON-NITROGEN COMPOUNDS HAVING THE FORMULA:

    (-O-(CXR2X)-N(-(CYR2Y)-O(-))-(CZR2Z)-O-)>B(-) WHERE O

    AND B ARE JOINED

    CERTAIN OF THE COMPOUNDS OF THIS INVENTION CONTAIN AT LEAST ONE RING SUBSTITUENT WHEREAS WITH OTHERS AT LEAST TWO OF THE RINGS OF THE COMPOUNDS ARE SUBSTITUTED, WITH AT LEAST ONE OF THE RINGS BEING SUBSTITUTED WITH A HYDROXYALKYL, AMINOALKYL, ARYLALKYL, ARYL, ESTER, AMIDO OR ETHER RADICAL, AND AT LEAST ONE OF THE REMAINING RINGS BEING SUBSTITUTED WITH ONE OF THESE RADICALS OR AN ALKYL RADICAL, BUT ONE RING NEED BE SUBSTITUTED WHEN THE SUBSTITUENT IS A HIGHER C8-C22 ALKYL RADICAL, A HYDROXYL GROUP, A HIGHER C8-C22 ETHER OR ESTER, OR AN ALKYL HIGHER (C8-C22) ETHER OR ESTER. EXEMPLARY OF THESE COMPOUNDS ARE 3,7,10-TRIHYDROXYMETHYL-2, 8,9-TROXA - 5 - AZA - 1 - BORATRICYCLO(3.3.3.0)UNDECANE; 3MEHTYL-7,10-DIPHENYL-2,8,9-TRIOXA-5-AZA - 1 - BORATRICYCLO (3.3.3.0)UNDECANE; AND 3-HYDROXYMETHYL-7,10-DIMETHYL-2, 8,9-TRIOXA-5-AZA-1-BORATRICYCLO(3.3.3.0)UNDECANE STEARATE. THE COMPOUNDS ARE USEFUL AS ANTISTATIC AGENTS IN NATURAL AND SYNTHETIC, POLYMERIC FIBERS AND FILMS, AND AS COLOR IMPROVING AGENTS FOR FATTY ACID DISTILLATIONS.

    Azaborolidine compounds
    63.
    发明授权
    Azaborolidine compounds 失效
    氮杂吲哚化合物

    公开(公告)号:US3696103A

    公开(公告)日:1972-10-03

    申请号:US3696103D

    申请日:1970-02-02

    申请人: RHONE POULENC SA

    CPC分类号: C07F5/02 C07F5/006

    摘要: The new azaborolidine compounds of the formula:
    WHEREIN R1 and R2 represent alkyl of one through four carbon atoms, or R1 and R2 together with the nitrogen atom collectively represent a mononuclear 5- or 6-membered heterocyclic group, X represents hydrogen, halogen, alkyl, alkoxy or alkylthio of one through four carbon atoms, or trifluoromethyl or dimethylsulphamoyl, and at least one of the carbon atoms of the trimethylene chain linking the nitrogen and boron atoms can be substituted by alkyl of one through four carbon atoms, possess fungicidal, insecticidal acaricidal and herbicidal properties.

    摘要翻译: 新的具有下式的氮杂硼烷化合物:

    Benzidene boron complex and process for preparing the same
    69.
    发明授权
    Benzidene boron complex and process for preparing the same 失效
    亚苄基硼络合物及其制备方法

    公开(公告)号:US3362995A

    公开(公告)日:1968-01-09

    申请号:US33197263

    申请日:1963-12-19

    IPC分类号: C06B47/10 C07F5/00

    CPC分类号: C06B47/10 C07F5/006

    摘要: A solid fuel block characterized in that it is produced by the agglomeration of one or more powdered solid fuels containing boron, carbon, hydrogen and nitrogen, obtained by the action, at a temperature at most equal to ordinary temperature, of diborane on phenylhydrazine and/or 1,1-dimethyl hydrazine, together with a binder, for example cellulose triacetate, polyvinyl chloride, polyethylene, "Stratyl" (a Trade Mark relating to a mixture of polyesters and styrene), an elastomer, such as natural rubber, or paratolyl borazane. The agglomeration may be effected at a pressure ranging from 50 to 1000 kgs/cm.2 The solid fuel block has a hypergolic character with respect to some oxidizers such as nitric acid, nitrogen peroxide, fluorine or chlorine trifluoride.ALSO:The invention comprises boron, carbon, hydrogen and nitrogen containing compounds which are solid at 60 DEG C. resulting from the action, at a temperature at most equal to ordinary temperature, of diborane on phenylhydrazine and/or 1,1-dimethyl hydrazine. The solid product is advantageously agglomerated under pressure, e.g. 50 to 1000 kg./cm.2 at ordinary or moderate temperature.ALSO:A solid fuel comprises a complex obtained by the action of diborane on phenyl hydrazine and/or 1,1-dimethyl hydrazine agglomerated with polyvinyl chloride or polyethylene as a binder.

    Composition and process for separation of trialkylaluminum compounds
    70.
    发明授权
    Composition and process for separation of trialkylaluminum compounds 失效
    用于分离三烷基铝化合物的组合物和方法

    公开(公告)号:US3328446A

    公开(公告)日:1967-06-27

    申请号:US23758862

    申请日:1962-11-14

    IPC分类号: C07C2/88 C07F5/00 C07F5/06

    摘要: To either (A) a displacement product containing low molecular weight trialkyl aluminium and a -olefin or (B) a mixture of non-olefin hydrocarbon and a low molecular weight trialkyl aluminium or (C) a mixture of a dialkyl aluminium alkoxide and a low molecular weight trialkyl aluminium or (D) mixtures of any of these is added a complexing agent for the low molecular weight trialkylaluminium comprising either a compound RnMX or a complex of RnMX and low molecular weight trialkyl aluminium in a 1 : 1 ratio, in an amount sufficient to form a complex having a 2 : 1 ratio of trialkyl aluminium to RnMX with substantially all of the trialkyl aluminium, and separating the 2 : 1 complex. R is an alkyl radical, M is nitrogen, arsenic, phosphorus, sulphur, selenium or tellurium, X is halogen and n is 3 or 4. The complexing agent is preferably a tetra-alkyl ammonium halide or a 1 : 1 complex thereof with low molecular weight tri-alkyl aluminium, and complexes a (R13Al)R4NCl, wherein R1 i an alkyl radical containing 2-5 carbon atoms, R contains 1-5 carbon atoms, and a is 1 or 2 are claimed per se. The complexing reaction takes place at 50-150 DEG C., suitably at atmospheric pressure during a time of 0.25-30 minutes. In the formation of the 1 : 1 complex, equimolar amounts of the reactants or a slight excess of trialkyl aluminium are employed. In the reaction between the 1 : 1 complex and trialkyl aluminium, preferably an excess, e.g. 1.05 to 1.2 moles of 1 : 1 complex per mole of trialkyl aluminium is employed. The displacement product may be that obtained by treating a high molecular weight trialkyl aluminium in which the alkyl radicals have an average of 4 to 30 carbon atoms with an a -olefin containing 2 to 5 carbon atoms and this may be treated with a 1 : 1 complex of a tetra-alkyl ammonium halide in which the alkyl radicals have an average of 1 to 5 carbon atoms and a trialkyl aluminium in which the alkyl radicals have an average of 2 to 5 carbon atoms. A lower layer of 2 : 1 complex so produced is separated and washed with a paraffinic hydrocarbon containing 5-12 carbon atoms. The 2 : 1 complex may be decomposed at least partly to 1 : 1 complex and trialkyl aluminium by heating at subatmospheric pressure, but decomposition is preferably achieved by contacting the complex with a non-reactive extraction solvent, e.g. a hydrocarbon having 4 to 20 carbon atoms, at 100-200 DEG C. under atmospheric pressure. The hydrocarbon is conveniently the same as that used in the growth reaction, e.g. kerosene. In a continuous reaction the complex and 1 to 40 volumes of solvent are contacted in countercurrent in an extraction zone during a residence time of 1 to 60 minutes and extraction solvent enriched in trialkyl aluminium and complex material enriched in 1 : 1 complex are withdrawn from the zone. Part of the latter may be returned to the extraction zone. The remainder is recycled to the complexing stage.