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    Diphosphonate derivatives, pharmaceutical compositions and methods of use
    1.
    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
    2.
    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。

    Diphosphonic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
    3.
    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。

    Triazole containing diphosphonate compounds and the use thereof
    4.
    发明授权
    Triazole containing diphosphonate compounds and the use thereof 失效
    含三唑的二膦酸盐化合物及其用途

    公开(公告)号：US4784993A

    公开(公告)日：1988-11-15

    申请号：US76706

    申请日：1987-07-23

    申请人： Elmar Bosies ,  Rudi Gall

    发明人： Elmar Bosies ,  Rudi Gall

    IPC分类号： A61K31/675 ,  A61P3/00 ,  A61P3/14 ,  C07F9/38 ,  C07F9/553 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/6515 ,  C07F9/6518 ,  C07F9/653 ,  A61K31/41 ,  C07F9/65

    CPC分类号： C07F9/3839 ,  C07F9/582 ,  C07F9/65062 ,  C07F9/65182 ,  C07F9/653

    摘要： The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is 1,2,3-triazole, or 1,2,4-triazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or acyl radicals or is 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 acyl, or an amino group optionally substituted by alkyl or acyl 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为1,2,3-三唑或1,2,4-三唑基，其任选被烷基，烷氧基，卤素，羟基， 羧基，任选被烷基或酰基取代的氨基，或是任选被烷基，硝基，氨基或氨基烷基取代的苄基，A是含有2-8个碳原子的直链或支链，饱和或不饱和烃链，X 是任选被酰基取代的氢原子或任选被烷基或酰基取代的氨基，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。

    Diphosphonate derivatives, pharmaceutical compositions and methods of use for calcium disturbances
    5.
    发明授权
    Diphosphonate derivatives, pharmaceutical compositions and methods of use for calcium disturbances 失效
    二膦酸衍生物，药物组合物和钙紊乱的使用方法

    公开(公告)号：US4777163A

    公开(公告)日：1988-10-11

    申请号：US77228

    申请日：1987-07-24

    申请人： Elmar Bosies ,  Rudi Gall

    发明人： Elmar Bosies ,  Rudi Gall

    IPC分类号： A61K31/66 ,  A61K31/675 ,  A61P3/00 ,  A61P3/14 ,  A61P43/00 ,  C07F9/38 ,  C07F9/6506 ,  C07F9/6518 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/6541 ,  C07F9/6544 ,  C07F9/65

    CPC分类号： C07F9/6539 ,  C07F9/65062 ,  C07F9/65181 ,  C07F9/65182 ,  C07F9/653 ,  C07F9/65324 ,  C07F9/6541

    摘要： The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the prepearation of these compounds and pharmaceutical compositions containing them useful for the treatment or prophylaxis of calcium metabolism disturbances or disease as for example osteoporosis, Bechterew's disease, bone metastases, urolithiasis, heterotropic ossifications, rheumatoid arthritis osteoarthritis or degenerative arthrosis.

    摘要翻译： 本发明产生以下通式的烷基二膦酸衍生物：其中Het是含有3个杂原子的杂芳族五元环，其可以被部分氢化并任选地被烷基，烷氧基，苯基， 环己基，环己基甲基，卤素或氨基，两个相邻的烷基取代基可一起形成环，Y为氢原子或低级烷基，X为氢原子，羟基或任选被低级烷基取代的氨基， R是氢原子或低级烷基，条件是Het不是吡唑环; 以及其药理学上可接受的盐。 本发明还提供了这些化合物的预切方法和含有它们的药物组合物的方法，所述方法可用于治疗或预防钙代谢紊乱或疾病，例如骨质疏松症，Bechterew氏病，骨转移，尿石症，异质性骨化，类风湿性关节炎骨关节炎或退行性 关节。

    Phospholipid compound
    6.
    发明授权
    Phospholipid compound 失效

    公开(公告)号：US4492659A

    公开(公告)日：1985-01-08

    申请号：US395954

    申请日：1982-07-07

    申请人： Elmar Bosies ,  Rudi Gall ,  Gunter Weimann ,  Uwe Bicker ,  Wulf Pahlke

    发明人： Elmar Bosies ,  Rudi Gall ,  Gunter Weimann ,  Uwe Bicker ,  Wulf Pahlke

    IPC分类号： A61K31/66 ,  A61P35/00 ,  C07F9/09 ,  C07F9/10 ,  C07F9/02

    CPC分类号： C07F9/10 ,  C07F9/091

    摘要： The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.3 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, which can also be part of a cycloalkane ring system and is optionally substituted one or more times by hydroxyl, halogen, alkylthio, alkanesulphinyl, alkanesulfonyl, nitrile, alkoxycarbonyl, carboxamido optionally substituted by alkyl radicals, cycoalkyl, optionally substituted phenyl or alkoxy, which in turn is optionally substituted by phenyl, hydroxyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, optionally acylated amino, alkoxycarbonyl, nitrile or carboxamido optionally substituted by alkyl radicals, Z is an oxygen or sulfur atom, R.sub.4 is a straight-chained or branched alkylene radical containing 2 to 5 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl radical, with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together represent an unsubstituted, straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon chain containing up to 18 carbon atoms, Y, R.sub.4 and R.sub.5 have the above-given meanings and Z is an oxygen atom, R.sub.3 cannot be a propylene or 2-methylpropylene chain optionally substituted by hydroxyl, alkoxy or benzyloxy and with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together signify an alkyl radical containing up to 18 carbon atoms and substituted by halogen or phenyl, Y and Z are oxygen atoms and R.sub.4 and R.sub.5 have the above-given meanings, R.sub.3 cannot be a propylene or 2-hydroxypropylene chain; and the pharmacologically acceptable salts thereof.The invention also provides pharmaceutical compositions containing such compounds, having cancerostatic action without inducing thrombocyte aggregation.

    Certain 1-hydroxyethane, 1,1-di-phosphonic acid derivatives useful in treating calcium metabolism disturbances
    9.
    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

    申请人： Elmar Bosies ,  Rudi Gall

    发明人： Elmar Bosies ,  Rudi Gall

    IPC分类号： A61K31/675 ,  A61P3/00 ,  A61P3/14 ,  C07F9/38 ,  C07F9/553 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/6515 ,  C07F9/6518 ,  C07F9/653 ,  C07F9/65 ,  A61K31/44 ,  A61K31/415

    CPC分类号： C07F9/3839 ,  C07F9/582 ,  C07F9/65062 ,  C07F9/65182 ,  C07F9/653

    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。

    Diphosphonic acid derivatives
    10.
    发明授权
    Diphosphonic acid derivatives 失效
    二膦酸衍生物

    公开(公告)号：US4666895A

    公开(公告)日：1987-05-19

    申请号：US846250

    申请日：1986-03-31

    申请人： Elmar Bosies ,  Rudi Gall

    发明人： Elmar Bosies ,  Rudi Gall

    IPC分类号： A61K31/66 ,  A61K38/00 ,  A61P3/00 ,  A61P3/02 ,  A61P3/14 ,  C07F9/38 ,  C07F9/40 ,  C07K5/00 ,  C07K5/06 ,  C07K5/08 ,  A61K31/045 ,  A61K31/16

    CPC分类号： C07K5/06191 ,  C07F9/3873 ,  C07F9/405 ,  C07K5/00 ,  C07K5/0827 ,  A61K38/00

    摘要： The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another or also together, signify hydrogen atoms or lower alkyl radicals, whereby R.sub.1 and X or R.sub.3 and Y or R.sub.4 and Z, together with the nitrogen atom to which they are attached, can form a five- or six-membered ring, X and Y, which can be the same or different, represent a straight-chained or branched alkylene chain with up to 6 carbon atoms which can optionally be substituted by aromatic or heteroaromatic radicals, Z is a straight-chained or branched alkylene chain with up to 6 carbon atoms, which can be interrupted by heteroatoms and can optionally also be substituted by aromatic or heteroaromatic radicals, n is 0, 1 or 2 and A is a hydrogen atom or a hydroxyl group, and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these new diphosphonic acid derivatives and pharmaceutical compositions containing them for the treatment of calcium metabolism disturbances.

    摘要翻译： 本发明提供了以下通式的二膦酸衍生物：其中R 1，R 2，R 3，R 4和R 5彼此独立地或一起表示氢原子或低级烷基，其中R1和X或 R3和Y或R4和Z与它们所连接的氮原子一起可以形成五元或六元环，X和Y可以相同或不同，表示直链或支链亚烷基 具有多达6个碳原子的链，其可以任选地被芳族或杂芳族基团取代，Z是具有至多6个碳原子的直链或支链亚烷基链，其可以被杂原子中断，并且还可以任选地被芳族或 杂芳基，n为0,1或2，A为氢原子或羟基，以及其药理学上可接受的盐。 本发明还提供制备这些新的二膦酸衍生物的方法和含有它们的用于治疗钙代谢紊乱的药物组合物。