Osteoblast-specific mitogens and drugs containing such compounds
    1.
    发明授权
    Osteoblast-specific mitogens and drugs containing such compounds 失效
    成骨细胞特异性有丝分裂原和含有此类化合物的药物

    公开(公告)号:US06911553B1

    公开(公告)日:2005-06-28

    申请号:US09675943

    申请日:2000-09-29

    IPC分类号: C07F9/09 C07F9/06

    CPC分类号: C07F9/091

    摘要: The invention is directed to compounds of formula (I) wherein R1 alkyl, alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; and the physiologically safe salts, esters, optically active forms, racemates and derivatives thereof which can be metabolized in vivo to yield compounds of general formula (I), methods of preparing same, and drugs containing said compounds, for treating bone metabolic disorders.

    摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,R 2,R 2, n = 0-12; X =氧或NH; 以及其可在体内代谢产生通式(I)的化合物,其制备方法和含有所述化合物的药物用于治疗骨代谢紊乱的生理上安全的盐,酯,光学活性形式,外消旋体及其衍生物。

    Osteoblast-specific mitogens and drugs containing such compounds
    3.
    发明申请
    Osteoblast-specific mitogens and drugs containing such compounds 审中-公开
    成骨细胞特异性有丝分裂原和含有此类化合物的药物

    公开(公告)号:US20050014723A1

    公开(公告)日:2005-01-20

    申请号:US10893426

    申请日:2004-07-16

    IPC分类号: C07F9/09 A61K31/685 A61K31/66

    CPC分类号: C07F9/091

    摘要: Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. Novel compounds for this treatment include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds.

    摘要翻译: 成骨细胞特异性有丝分裂原和含有此类化合物的药物可用于治疗代谢性骨病。 用于该处理的新型化合物包括选自下式的化合物的溶血磷脂酰衍生物:其中R 1 =具有6至24个碳原子的链烯基或炔基; n = 0-12; X =氧; 化合物(全顺式-5,8,11,14) - 二十碳四烯酸2-羟基-3-膦酰氧丙基酯; 顺式-9,顺式-12-十八碳二烯酸2-羟基-3-膦酰氧基丙基酯; (全顺式-9,12,15) - 十八碳三烯酸2-羟基-3-膦酰氧丙基酯; 顺-9-十八碳烯酸2-羟基-3-膦酰氧基丙酯; 和芥酸2-羟基-3-膦酰氧基丙基酯,以及所述化合物的生理上可耐受的盐,酯,旋光形式和外消旋体。

    Osteoblast-specific mitogens and drugs containing such compounds
    5.
    发明授权
    Osteoblast-specific mitogens and drugs containing such compounds 有权
    成骨细胞特异性有丝分裂原和含有此类化合物的药物

    公开(公告)号:US06197759B1

    公开(公告)日:2001-03-06

    申请号:US09508714

    申请日:2000-04-11

    IPC分类号: A61K31661

    CPC分类号: C07F9/091

    摘要: Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. These compounds include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds, and derivatives of said compounds, salts, esters, optically active forms and racemates which can be metabolized in vivo to yield the corresponding compound of formula (I).

    摘要翻译: 成骨细胞特异性有丝分裂原和含有此类化合物的药物可用于治疗代谢性骨病。 这些化合物包括选自下式的化合物的溶血磷脂酰衍生物:其中R1 =具有6至24个碳原子的烯基或炔基; n = 0-12; X =氧或NH;化合物(全顺式-5, 8,11,14) - 二十碳四烯酸2-羟基-3-膦酰氧基丙基酯; 顺式-9,顺式-12-十八碳二烯酸2-羟基-3-膦酰氧基丙基酯; (全顺式-9,12,15) - 十八碳三烯酸2-羟基-3-膦酰氧丙基酯; 顺-9-十八碳烯酸2-羟基-3-膦酰氧基丙酯; 和芥酸2-羟基-3-膦酰氧基丙基酯,以及所述化合物的生理上可耐受的盐,酯,旋光形式和外消旋物,以及所述化合物的衍生物,盐,酯,旋光活性物质和可被代谢的外消旋体 在体内产生相应的式(I)化合物。

    Rhodanine carboxylic acid derivatives for the treatment and prevention of metabolic bone disorders
    6.
    发明授权
    Rhodanine carboxylic acid derivatives for the treatment and prevention of metabolic bone disorders 失效
    用于治疗和预防代谢性骨骼疾病的罗丹明羧酸衍生物

    公开(公告)号:US06673816B1

    公开(公告)日:2004-01-06

    申请号:US09787917

    申请日:2001-06-21

    IPC分类号: A61K31426

    摘要: Compounds of general formula (I), in which m is 0-8, q is a 0-8, a is 0-4, A signifies a single or double bond, R1, R2 signify hydrogen or lower alkyl and, when m signifies 2-8, R1 and R2 in the group CR1═CR2 can have various significances within the following sequence, R3 signifies hydrogen or lower alkyl, X signifies hydrogen or —(CH2)b—COR4 with b=0-4, Y signifies hydrogen, —COR4, phenyl or indolyl residue R4 signifies hydroxyl, lower alkoxy or the NR1R2 residue, W signifies an optionally mono- or polysubstituted saturated or unsaturated mono-, bi- or tricycle which can contain hetero atoms, as well physiologically compatible salts, esters, optically active forms, racemates, tautomers, and derivatives which can be metabolized in vivo to compounds of general formula (I).

    摘要翻译: 通式(I)的化合物,其中m为0-8,q为0-8,a为0-4,A表示单键或双键,R1,R2表示氢或低级烷基,当m表示 2-8中,基团CR1 = CR2中的R1和R2可以在以下序列中具有各种含义,R3表示氢或低级烷基,X表示氢或 - (CH2)b-COR4,其中b = 0-4,Y表示氢 ,-COR 4,苯基或吲哚基残基R 4表示羟基,低级烷氧基或NR 1 R 2残基,W表示可以含有杂原子的任选的单取代或多取代的饱和或不饱和单 - ,二 - 或三环,以及生理上相容的盐,酯 ,光学活性形式,外消旋体,互变异构体和衍生物,其可以在体内被代谢为通式(I)的化合物。

    2,4-diphosphonoglutaric acid derivatives, processes for their production
and pharmaceutical agents containing these compounds
    7.
    发明授权
    2,4-diphosphonoglutaric acid derivatives, processes for their production and pharmaceutical agents containing these compounds 失效
    2,4-二膦酸葡萄糖酸衍生物,其制备方法和含有这些化合物的药剂

    公开(公告)号:US5698541A

    公开(公告)日:1997-12-16

    申请号:US714076

    申请日:1996-09-25

    摘要: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl, their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.

    摘要翻译: PCT No.PCT / EP95 / 01062 Sec。 371日期1996年9月25日 102(e)日期1996年9月25日PCT提交1995年3月22日PCT公布。 公开号WO95 / 26358 日期1995年10月5日本发明涉及通式Ⅰ(I)的化合物,其中R表示可以被羟基,烷氧基,氨基,二烷基氨基,烷基巯基,烷基亚磺酰基,烷基磺酰基,环烷基, 芳基或杂环,或者表示低级烯基,环烷基,环烯基,芳基或杂环,并且R 1和R 2可以彼此独立地为氢,低级烷基,环烷基,芳基或芳甲基,它们的光学活性盐 作为其药理学上可接受的盐,其生产方法以及含有这些化合物用于治疗钙代谢疾病的药剂。 此外,本发明涉及式II化合物作为制备式I化合物的中间产物。

    Active hedgehog protein conjugate
    8.
    发明申请
    Active hedgehog protein conjugate 审中-公开
    活性刺猬蛋白结合物

    公开(公告)号:US20070191274A1

    公开(公告)日:2007-08-16

    申请号:US11645014

    申请日:2006-12-22

    摘要: A hedgehog conjugate which is characterized in that it contains: a) a polypeptide composed of 10 to 30 hydrophobic amino acids and/or amino acids which form transmembrane helices and are positively charged, b) 1 to 4 aliphatic, saturated or unsaturated hydrocarbon residues with a chain length of 10 to 24 C atoms and with a hydrophobic action or c) a hydrophobic thio compound covalently bound to a hedgehog protein and which has a several-fold increased activity and is suitable as a pharmaceutical agent.

    摘要翻译: 一种刺猬蛋白缀合物,其特征在于其包含:a)由10至30个疏水氨基酸和/或氨基酸组成的多肽,其形成跨膜螺旋并带正电荷,b)1至4个脂族,饱和或不饱和的烃残基, 链长为10至24个C原子并具有疏水作用,或c)与猬蛋白共价结合的疏水性硫代化合物,并且其具有几倍增加的活性并且适于作为药剂。

    Active hedgehog protein conjugate
    10.
    发明授权
    Active hedgehog protein conjugate 失效
    活性刺猬蛋白结合物

    公开(公告)号:US06468978B1

    公开(公告)日:2002-10-22

    申请号:US09301199

    申请日:1999-04-28

    IPC分类号: A61K3817

    摘要: A hedgehog conjugate which is characterized in that it contains: a) a polypeptide composed of 10 to 30 hydrophobic amino acids and/or amino acids which form transmembrane helices and are positively charged, b) 1 to 4 aliphatic, saturated or unsaturated hydrocarbon residues with a chain length of 10 to 24 C atoms and with a hydrophobic action or c) a hydrophobic thio compound covalently bound to a hedgehog protein and which has a several-fold increased activity and is suitable as a pharmaceutical agent.

    摘要翻译: 一种刺猬蛋白缀合物,其特征在于其包含:a)由10至30个疏水氨基酸和/或氨基酸组成的多肽,其形成跨膜螺旋并带正电荷,b)1至4个脂族,饱和或不饱和的烃残基, 链长为10至24个C原子并具有疏水作用,或c)与猬蛋白共价结合的疏水性硫代化合物,并且其具有几倍增加的活性并且适于作为药剂。