11-aza, 11-thia and 11-oxa sterol compounds and compositions
    3.
    发明授权
    11-aza, 11-thia and 11-oxa sterol compounds and compositions 失效
    11-氮杂,11-硫杂和11-氧杂甾醇化合物和组合物

    公开(公告)号:US08541600B2

    公开(公告)日:2013-09-24

    申请号:US13183275

    申请日:2011-07-14

    申请人: James M. Frincke

    发明人: James M. Frincke

    IPC分类号: C07D221/18 C07D227/08

    摘要: The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

    摘要翻译: 本发明提供包含式1类固醇的组合物,例如16α-溴-3β-羟基-5α-雄甾烷-17-酮半水合物和一种或多种赋形剂,包括包含低于约3%v / v水的液体制剂的组合物 。 该组合物可用于制备改进的药物制剂。 本发明还提供了类固醇化合物如16α-溴-3β-羟基-5α-雄甾烷-17-型的类似物的间歇给药方法和用于该给药方案的组合物。 本发明进一步提供抑制病原体复制,改善与免疫调节异常有关的症状并使用该化合物调节受试者的免疫应答的组合物和方法。 本发明还提供了制备和使用这些免疫调节组合物和制剂的方法。

    N-substituted acyl-lactam compound
    4.
    发明授权
    N-substituted acyl-lactam compound 失效
    N-取代的酰基 - 内酰胺化合物

    公开(公告)号:US4692521A

    公开(公告)日:1987-09-08

    申请号:US808558

    申请日:1985-12-13

    摘要: The invention relates to N-substitutecd acyl lactam compounds of the formula ##STR1## where R is a polyol residue originating from a polyol with the formula R-(OH).sub.x where x is a number.ltoreq.2R' a bivalent cyclic or non-cyclic alkyl, aralkyl, alkaryl or aryl radicalR" a bivalent radical having the following general formula ##STR2## wherein R'" is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl,R.sup.iv is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl whereR"' and R.sup.iv may jointly form a substituted or non-substituted cycloalkyl residuen is 0 or 1 and(-L) represents a non-opened lactam ring of the formula ##STR3## wherein Y is hydrocarbon residue with 3-11 carbon atoms. It has been found that this group of compounds is very suitable as activator in the preparation of nylon block copolymers, more specifically in the RIM or RRIM systems.

    摘要翻译: 本发明涉及式(IMAGE)的N-取代的酰基内酰胺化合物,其中R是衍生自具有式R-(OH)x的多元醇的多元醇残基,其中x是二价环状的数字, 非环烷基,芳烷基,烷芳基或芳基R“具有以下通式的二价基团,其中R”'是H,烷基,环烷基,芳基,烷芳基或芳烷基,Riv是H,烷基,环烷基 ,芳基,烷芳基或芳烷基,其中R“'和Riv可以共同形成取代或未取代的环烷基残基n为0或1,(-L)表示式”IMAGE“的未开封的内酰胺环,其中Y为 具有3-11个碳原子的烃残基。 已经发现,这组化合物在制备尼龙嵌段共聚物中非常适合作为活化剂,更具体地说在RIM或RRIM系统中。

    Salts of aminic organic peroxides
    10.
    发明授权
    Salts of aminic organic peroxides 失效
    胺类有机过氧化物的盐

    公开(公告)号:US4499273A

    公开(公告)日:1985-02-12

    申请号:US451882

    申请日:1982-12-21

    摘要: There are disclosed new organic peroxides having two peroxy functional groups and containing in their molecule an atom of salified aminic nitrogen, having the general formula: ##STR1## in which: R.sub.1, R.sub.2 are each an alkyl radical having 1 to 8 carbon atoms, optionally aryl-substituted, preferably a tertiary alkyl group such as t.butyl, t.amyl, t.octyl and cumyl;R.sub.3 is a hydrogen, an alkyl radical having 1 to 8 carbon atoms, a cycloalkyl having 5-6 carbon atoms in the ring, an aryl, an arylalkyl optionally halogen, alkoxy-, carboalkoxy-, alkyl-, mono- or poly-substituted;R.sub.4 is the methylene, ethylene or trimethylene radical, optionally halogen-, alkoxy-, carboalkoxy-, aryl-, alkyl-, mono- or poly-substituted;R.sub.5 is the methylene or ethylene radical optionally halogen-, alkoxy-, carboalkoxy-, alkyl-, aryl-, mono- or poly-substituted;X is an anion or an inorganic or organic acid in which one or more acid hydrogens are substituted by the aminic cation;n is 1, 2 or 3 and represents the number of hydrogen atoms which are salified.The peroxides so salified are employed in the crosslinking of plastomers, natural and synthetic elastomers and thermosetting resins.This invention relates to salts of amino organic peroxides and, more particularly, to new organic peroxides having the peroxy functional groups, containing in their molecule an atom of salified aminic nitrogen, as well as to the use thereof in the cross-linking of plastomers, natural and synthetic elastomers and thermosetting resins.

    摘要翻译: 公开了具有两个过氧官能团的新的有机过氧化物,并且在其分子中含有盐化的氨基氮原子,具有以下通式:其中:R 1,R 2各自为具有1至8个碳原子的烷基,任选地 芳基取代的,优选叔烷基如叔丁基,叔戊基,辛基和枯基; R3是氢,具有1至8个碳原子的烷基,环中具有5-6个碳原子的环烷基,芳基,任选卤素的芳烷基,烷氧基 - ,烷氧基 - ,烷基 - ,单 - 或多取代 ; R4是亚甲基,亚乙基或三亚甲基,任选是卤素,烷氧基,烷氧基,芳基,烷基,单或多取代的; R5是任选卤素,烷氧基,烷氧基,烷基,芳基,单取代或多取代的亚甲基或亚乙基; X是其中一个或多个酸氢被氨基阳离子取代的阴离子或无机或有机酸; n为1,2或3,表示成盐的氢原子数。 如此成盐的过氧化物用于塑性体,天然和合成弹性体和热固性树脂的交联。 本发明涉及氨基有机过氧化物的盐,更具体地说,涉及具有过氧官能团的新型有机过氧化物,其分子中含有盐化氨基氮的原子,以及其在塑性体交联中的用途, 天然和合成弹性体和热固性树脂。