Phosphorus-containing cyclic nitroxide free radicals
    41.
    发明授权
    Phosphorus-containing cyclic nitroxide free radicals 失效
    含磷环状氮氧自由基

    公开(公告)号:US5006663A

    公开(公告)日:1991-04-09

    申请号:US433597

    申请日:1989-11-08

    摘要: A nitroxide radical of the formula (I) or (II): ##STR1## in which R.sub.1 and R.sub.2 are independently chosen from among the optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, H, D or Cl; R.sub.3, R.sub.8 and R.sub.9 are independently chosen from among the optionally deuterated alkyl, alkoxyl and phenyl radicals; R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently chosen from among the optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, COOH, OH, OD, H, D, a halogen, COOR (in which R is an alkyl radical); R.sub.10 and R.sub.11 are independently chosen from among optionally deuterated alkyl, alkoxyl, dialkylaminyl and phenyl radicals, COOH, OH, OD, H, D, a halogen, COOR (in which R is an alkyl radical) or represent an oxygen atom linked with the cycle of the radical by a double bond is described.

    摘要翻译: 式(I)或(II)的氮氧自由基:其中R 1和R 2独立地选自任选的氘代烷基,烷氧基,二烷基氨基和苯基,H, D或Cl; R3,R8和R9独立地选自任选的氘代烷基,烷氧基和苯基; R 4,R 5,R 6和R 7独立地选自任选的氘代烷基,烷氧基,二烷基氨基和苯基,COOH,OH,OD,H,D,卤素,COOR(其中R是烷基) R 10和R 11独立地选自氘代烷基,烷氧基,二烷基氨基和苯基,COOH,OH,OD,H,D,卤素,COOR(其中R是烷基)或代表与 描述了基团的双键循环。

    Pharmaceuticals, phosphorus-containing 2-isoxazolines and isoxazoles
contained therein
    42.
    发明授权
    Pharmaceuticals, phosphorus-containing 2-isoxazolines and isoxazoles contained therein 失效
    药物,其中含有含磷的2-异恶唑啉和异恶唑

    公开(公告)号:US5006515A

    公开(公告)日:1991-04-09

    申请号:US262635

    申请日:1988-10-26

    CPC分类号: C07F9/653 A61K31/675

    摘要: Pharmaceuticals containing or composed of at least one compound of the formula I and/or one of its physiologically tolerated salts where appropriate, where the compounds of the formula I can, where appropriate, be in the form of pure stereoisomers or mixtures thereof; formula I is: ##STR1## in which R.sup.1 =organic radical or halogen,A=C,C single or C,C double bond,n=0, 1 or 2, and ##STR2## R.sup.2 and R.sup.3 =H or optionally substituted aliphatic radical. The pharmaceuticals are suitable for the prophylaxis and/or treatment of diseases of the immune system, especially of tumors, infections and/or autoimmune diseases of the human or animal body and for use as adjuvants for vaccines.Some of the compounds of the formula I are new; the compounds can be prepared by special processes.

    摘要翻译: 含有或由至少一种式I化合物和/或其适当的生理学耐受盐组成的药物,其中式I化合物在适当时可以是纯立体异构体或其混合物的形式; 式I是:其中R 1 =有机基团或卤素,A = C,C单或C,C双键,n = 0,1或2,X和Y =烷基或= OR 2 或具有R2和R3 = H的NR2R3或任选取代的脂族基团。 该药物适用于预防和/或治疗免疫系统疾病,特别是人或动物体的肿瘤,感染和/或自身免疫性疾病的疾病,并且可用作疫苗佐剂。 一些式I的化合物是新的; 该化合物可以通过特殊方法制备。

    Certain 1-hydroxyethane, 1,1-di-phosphonic acid derivatives useful in
treating calcium metabolism disturbances
    45.
    发明授权
    Certain 1-hydroxyethane, 1,1-di-phosphonic acid derivatives useful in treating calcium metabolism disturbances 失效
    某些用于治疗钙代谢紊乱的1-羟基乙烷,1,1-二膦酸衍生物

    公开(公告)号:US4687767A

    公开(公告)日:1987-08-18

    申请号:US759608

    申请日:1985-07-26

    摘要: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.

    摘要翻译: 本发明提供了以下通式的二膦酸盐:其中Het是咪唑,恶唑,异恶唑,噻唑,吡啶,1,2,3-三唑,1,2,4-三唑或苯并咪唑基,其中 烷氧基,卤素,羟基,羧基,任选被烷基或烷酰基取代的氨基或任选被烷基,硝基,氨基或氨基烷基取代的苄基,A是直链或支链,饱和或 含有2至8个碳原子的不饱和烃链,X是任选被烷酰基取代的氢原子或任选被烷基或烷酰基取代的氨基,R是氢原子或烷基; 及其药理学上可接受的盐。 本发明还提供了制备这些二膦酸盐和含有它们的药物组合物的方法。