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    Diphosphonate derivatives, pharmaceutical compositions and methods of use
    4.
    发明授权
    Diphosphonate derivatives, pharmaceutical compositions and methods of use 失效
    二膦酸衍生物，药物组合物和使用方法

    公开(公告)号：US4927814A

    公开(公告)日：1990-05-22

    申请号：US71471

    申请日：1987-07-09

    申请人： Rudi Gall ,  Elmar Bosies

    发明人： Rudi Gall ,  Elmar Bosies

    IPC分类号： A61K31/66 ,  A61P3/00 ,  A61P3/14 ,  A61P29/00 ,  A61P43/00 ,  C07F9/38 ,  C07F9/40

    CPC分类号： C07F9/405 ,  C07F9/3873

    摘要： The present invention provides disphosphonates of the general formula: ##STR1## wherein R.sub.1 is a straight-chain or branched, saturated or unsaturated aliphatic hydrocarbon radical of 1-9 carbon atoms which is optionally substituted by phenyl or cyclohexyl, R.sub.2 is cyclohexyl or cyclohexylmethyl, benzyl or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon of 4 to 18 carbon atoms which is optionally substituted by phenyl or oxygen wherein the oxygen can be esterified or etherified, R.sub.3 is hydrogen or a straight-chain or branched alkyl of 1-4 carbon atoms, X is a straight-chain or branched alkylene chain of 1-6 carbon atoms and Y is hydrogen, hydroxyl or an amino group optionally substituted by alkyl radicals of 1-6 carbon atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonic acid derivatives and pharmaceutical compositions containing them for the prophyllaxis treatment of diseases or disturbances of calcium metabolism such as osteoporsis, Pagets disease, Bechterew's disease, bone metastases, urolithiasis, heterotropic ossifications, rheumatoid arthritis, osteoarthritis and degenerative arthrosis.

    摘要翻译： 本发明提供以下通式的分解膦酸盐：其中R 1是1-9个碳原子的直链或支链，饱和或不饱和脂族烃基，其任选被苯基或环己基取代，R 2是环己基 或环己基甲基，苄基或具有4至18个碳原子的直链或支链，饱和或不饱和的脂族烃，其任选被苯基或氧取代，其中氧可被酯化或醚化，R 3是氢或直链或支链 1-4个碳原子的烷基，X是1-6个碳原子的直链或支链亚烷基链，Y是氢，羟基或任选被1-6个碳原子的烷基取代的氨基; 以及其药理学上可接受的盐。 本发明还提供制备这些二膦酸衍生物的方法和含有它们的药物组合物，用于预防性治疗钙代谢疾病或紊乱，例如骨质疏松症，佩吉特氏病，贝克特尔病，骨转移，尿石症，异质性骨化，类风湿性关节炎 ，骨关节炎和退行性关节病。

    1-Aziridine carboxylic acid derivatives with immunostimulant activity
    5.
    发明授权
    1-Aziridine carboxylic acid derivatives with immunostimulant activity 失效
    具有免疫刺激活性的1-氮杂环丁烷羧酸衍生物

    公开(公告)号：US4376731A

    公开(公告)日：1983-03-15

    申请号：US859633

    申请日：1978-01-31

    申请人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

    发明人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

    IPC分类号： C07D203/20 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/395

    CPC分类号： C07D403/12 ,  C07D203/20 ,  C07D405/12 ,  C07D409/12

    摘要： 2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula ##STR1## wherein X is a carbamoyl or alkoxycarbonyl radical, andR.sup.1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R.sup.1 is as above, except for ethyl, are also new.

    摘要翻译： 2-取代的1-氮丙啶 - 羧酸酯，其具有免疫刺激活性，并且具有下式：其中X是氨基甲酰基或烷氧基羰基，R1是任选被卤素，烷氧基，氨基，氨基甲酰氧基取代的脂族烃基， 环烷基，羟基，亚氨基或杂环基，环烷基; 芳基，芳烷基，芳氧基烷基或芳硫基烷基，其中芳基部分任选被卤素，烷基，烷氧基，羟基，氨基，硝基，氰基，酰基，烷氧基，硫代烷基，烷基磺酰基，苯基或三氟甲基取代。 对应物，其中X为-CN和R1如上所述，除乙基以外，也是新的。

    N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation
    6.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation 失效
    N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激

    公开(公告)号：US4321194A

    公开(公告)日：1982-03-23

    申请号：US59863

    申请日：1979-07-23

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D203/10 ,  C07D203/12 ,  C07D203/14

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.

    摘要翻译： 其中X是羧基，腈，烷氧基羰基或氨基甲酰基的氮杂环丁烷-2-羧酸衍生物，R和R 1是各种有机基团或其药理学上可接受的盐，具有显着的免疫刺激活性，特别是与 添加化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素。 那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。

    Amidine group containing monocycloheteracyclic or bicycloheterocyclic diphosphonic acid derivatives and medicaments containing these compounds
    8.
    发明授权
    Amidine group containing monocycloheteracyclic or bicycloheterocyclic diphosphonic acid derivatives and medicaments containing these compounds 失效
    含有单环杂环或双环杂环二膦酸衍生物的脒基和含有这些化合物的药物

    公开(公告)号：US5366969A

    公开(公告)日：1994-11-22

    申请号：US829019

    申请日：1992-03-06

    申请人： Elmar Bosies ,  Harald Zilch

    发明人： Elmar Bosies ,  Harald Zilch

    IPC分类号： A61K31/675 ,  A61P3/00 ,  C07F9/6512 ,  C07F9/6561 ,  A61K31/66 ,  C07F9/38 ,  C07F9/40

    CPC分类号： C07F9/65126 ,  C07F9/6561

    摘要： Compounds of the formula I ##STR1## in which R can be hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.1 hydrogen, C.sub.1 -C.sub.6 -alkyl, aryl, aryl-C.sub.1 -C.sub.4 -alkyl, amino-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -dialkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.7 -alkenyl, R.sup.2 R.sup.1 or C.sub.2 -C.sub.7 -alkenyl, C.sub.1 -C.sub.6 -alkylmercapto, C.sub.1 -C.sub.6 -alkoxy, phenoxy-C.sub.1 -C.sub.4 -alkyl,amino, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, morpholino, thiomorpholino, pyrrolidino, piperidino, hexamethyleneimino, pyrasolino, imidazolino, n 0, 1 or 2 and R.sup.1 and R.sup.2, together with the carbon and the nitrogen atom to which they are attached, can form a heterocyclic five-, six- or seven-membered ring with 1-4 heteroatoms, whereby the heteroatoms can be the same or different and signify oxygen, nitrogen or sulphur and the annelated ring can possibly be substituted by one or more C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylmercapto groups, hydroxyl, amino, nitro, halogen or halomethyl, as well as their pharmacologically acceptable salts, processes for their preparation, as well as medicaments which contain these compounds for the treatment of calcium metabolism disturbances.

    摘要翻译： 其中R可以是氢或C 1 -C 4烷基，R 1氢，C 1 -C 6烷基，芳基，芳基-C 1 -C 4烷基，氨基-C 1 -C 6烷基，C 1 -C 4烷基， C 1-6 - 烷基氨基-C 1 -C 4 - 烷基，C 1 -C 6 - 二烷基氨基-C 1 -C 4烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷硫基-C 1 -C 4烷基，C 3 -C 7 - 烯基，R 2 R 1或C 2 -C 7 - 烯基，C 1 -C 6烷基巯基，C 1 -C 6 - 烷氧基，苯氧基-C 1 -C 4烷基，氨基，C 1 -C 4烷基氨基，二-C 1 -C 4烷基氨基，吗啉代， 硫代吗啉代，吡咯烷子基，哌啶子基，六亚甲基亚氨基，吡咯烷基，咪唑啉，n 0,1或者2，并且R 1和R 2与它们所连接的碳原子和氮原子一起可以形成杂环的五，六或七元 具有1-4个杂原子的环，其中杂原子可以相同或不同，表示氧，氮或硫，并且环状环可以被一个或多个C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基巯基，羟基，氨基，硝基，卤素或卤代甲基，以及它们的药理学上可接受的盐， 其制备方法以及含有这些化合物用于治疗钙代谢紊乱的药物。

    Diphosphonic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
    10.
    发明授权
    Diphosphonic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them 失效
    二膦酸衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4719203A

    公开(公告)日：1988-01-12

    申请号：US930331

    申请日：1986-11-12

    申请人： Elmar Bosies ,  Rudi Gall

    发明人： Elmar Bosies ,  Rudi Gall

    IPC分类号： A61K31/665 ,  A61K31/66 ,  A61P3/00 ,  A61P3/02 ,  A61P3/14 ,  C07F9/38 ,  C07F9/40 ,  A61K31/045 ,  A61K31/13 ,  A61K31/185

    CPC分类号： C07F9/405 ,  C07F9/3873

    摘要： Diphosphonate compounds, processes for their preparation and pharmaceutical compositions containing them and being useful for treating calcium metabolism disorders. The diphosphonates are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, acyl or alkyl which can be substituted by aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl or R.sub.3 and R.sub.4 together represent lower alkylene, R.sub.5 is a hydrogen atom or alkyl, X is a valency bond or alkylene, Y is a valency bond, alkylene or substituted alkylene, Z is hydrogen, hydroxyl or amino group optionally substituted by alkyl and n is 1, 2 or 3; and including the pharmacologically acceptable salts thereof.

    摘要翻译： 二膦酸酯化合物，其制备方法和含有它们的药物组合物，并且可用于治疗钙代谢紊乱。 二膦酸酯具有下式（I）其中R 1和R 2是氢，可被芳基取代的酰基或烷基，R 3和R 4是氢或烷基或R 3和R 4一起代表低级亚烷基，R 5是氢原子 或烷基，X是价键或亚烷基，Y是价键，亚烷基或取代的亚烷基，Z是氢，任选被烷基取代的羟基或氨基，n是1,2或3; 并包括其药理学上可接受的盐。