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    4-Aminopyridines and medicaments containing the same
    1.
    发明授权
    4-Aminopyridines and medicaments containing the same 失效
    4-氨基吡啶和含有它们的药物

    公开(公告)号：US4289765A

    公开(公告)日：1981-09-15

    申请号：US109913

    申请日：1980-01-07

    申请人： Wilfried Greve ,  Heinzgeorg von Schuh ,  Hiristo Anagnostopulos

    发明人： Wilfried Greve ,  Heinzgeorg von Schuh ,  Hiristo Anagnostopulos

    IPC分类号： A61K31/44 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P11/14 ,  C07D213/74 ,  C07D213/85 ,  C07D405/12 ,  C07D417/04 ,  C07D213/61 ,  C07D413/04

    CPC分类号： C07D213/74 ,  C07D213/85

    摘要： 4-Aminopyridines of the formula ##STR1## in which R.sup.1 is hydrogen or alkyl of up to 6 carbon atoms andR.sup.2 represents (a) alkyl of up to 6 carbon atoms substituted up to three times with at least one radical from the group of halogen and hydroxyl, with formyl acetalized with an alcohol of up to 3 carbon atoms, alkylthio of up to 3 carbon atoms, phenylthio or the corresponding alkyl- and phenyl-sulfoxy and sulfone groups, the phenyl ring optionally carrying in each case up to three substituents from the group of alkyl, alkyl halide, alkoxy, mono- or dialkylamino having each up to 4 carbon atoms in each alkyl radical, halogen, nitro, amino and hydroxy, or (b) phenylalkyl or diphenyl-alkyl of up to 6 carbon atoms in the linear or branched alkyl moiety, the phenyl rings optionally being substituted up to three times with at least one radical from the group of alkyl, alkoxy, alkyl halide with up to 4 carbon atoms each, halogen, amino, hydroxy, nitro, the sulfamoyl group and the methylene dioxy radical, orR.sup.1 and R.sup.2, together with the nitrogen atom present in the 4-position, form a five- to seven-membered heterocyclic ring optionally substituted with alkyl of up to 2 carbon atoms and including up to two hetero-atoms, the second hetero-atom being oxygen, sulfur optionally carrying up to two oxygen atoms, or nitrogen, andR.sup.3 and R.sup.4 which may be identical or different, each represent alkyl of up to 9 carbon atoms, one of the two radicals optionally also being hydrogen,Y is a nitro or a cyano group, andZ stands for hydrogen or halogen,and the physiologically acceptable salts of these compounds, processes for their preparation and medicaments made thereof.

    摘要翻译： 其中R 1是氢或至多6个碳原子的烷基，R 2代表（a）至多6个碳原子的烷基，至少被一个取代基的一个基团取代至多三次的4-氨基吡啶 和羟基，用最多3个碳原子的醇缩醛化，最多3个碳原子的烷硫基，苯硫基或相应的烷基 - 和苯基 - 磺氧基和砜基团，苯环任选地带有至多三个取代基 在烷基，卤素，硝基，氨基和羟基中具有至多4个碳原子的烷基，烷基卤，烷氧基，一或二烷基氨基，或（b）至多6个碳原子的苯基烷基或二苯基 - 烷基 在直链或支链烷基部分中，苯基环任选被至少一个基团取代至多三次，所述基团为烷基，烷氧基，烷基卤，各自具有至多4个碳原子，卤素，氨基，羟基，硝基， 氨磺酰基和亚甲基二氧基 基团或R 1和R 2与存在于4-位的氮原子一起形成任选被至多2个碳原子的烷基并且包含至多两个杂原子的5至7元杂环，第二个 杂原子是氧，任选带有两个氧原子的硫，或氮，可以相同或不同的R 3和R 4各自代表至多9个碳原子的烷基，两个基团中的一个任选地也​​可以是氢，Y 是硝基或氰基，Z表示氢或卤素，这些化合物的生理上可接受的盐，其制备方法和由其制得的药物。

    Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals
    3.
    发明授权
    Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals 失效
    烷基黄嘌呤膦酸盐和烷基黄嘌呤膦氧化物及其作为药物的用途

    公开(公告)号：US5728686A

    公开(公告)日：1998-03-17

    申请号：US741591

    申请日：1996-10-31

    申请人： Gunter Billen ,  Ismahan Okyayuz-Baklouti ,  Hiristo Anagnostopulos ,  Stefan Mullner

    发明人： Gunter Billen ,  Ismahan Okyayuz-Baklouti ,  Hiristo Anagnostopulos ,  Stefan Mullner

    IPC分类号： A61K31/675 ,  A61P3/00 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P33/02 ,  A61P35/00 ,  A61P43/00 ,  C07F9/6561 ,  C07F9/6512

    CPC分类号： C07F9/65616

    摘要： Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals A compound of the formula ##STR1## where R.sup.1 and R.sup.3 are identical or different and at least one of the radicals R.sup.1 and R.sup.3 is a radical of the formula XI ##STR2## in which E is a covalent bond or a (C.sub.1 -C.sub.5)-alkyl, are suitable for the production of pharmaceuticals for the treatment of muscular atrophy, cachexia, muscular dystrophy, sepsis, septic shock, endotoxic shock, systemic inflammation response syndrome, adult respiratory distress syndrome, cerebral malaria, chronic pneumonia, pulmonary sarcoidosis, reperfusion damage, scar formation, inflammation of the bowel and ulcerative colitis, as a result of infections, acquired immune deficiency syndrome, cancer, trauma and other disorders having increased protein loss, peripheral circulatory disorders, disorders having altered leucocyte adhesion, and also disorders which are accompanied by an increased or unregulated tumor necrosis factor production such as rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis and other arthritic disorders.

    摘要翻译： 烷基黄嘌呤膦酸盐和烷基黄嘌呤膦氧化物及其作为药物的用途下式化合物其中R 1和R 3相同或不同，R 1和R 3中的至少一个是式XI的基团。 （XI）其中E是共价键或（C1-C5） - 烷基，适用于制备用于治疗肌肉萎缩，恶病质，肌营养不良症，败血症，败血性休克，内毒素性休克，全身炎症反应的药物 综合征，成人呼吸窘迫综合征，脑疟疾，慢性肺炎，肺结节病，再灌注损伤，瘢痕形成，肠炎和溃疡性结肠炎，由于感染，获得性免疫缺陷综合征，癌症，创伤和其他具有增加的蛋白质的疾病 损失，外周循环障碍，具有改变的白细胞粘附的病症，以及伴有增加或不调节的肿瘤坏死因子p 类风湿关节炎，类风湿性脊柱炎，骨关节炎和其他关节炎疾病。

    Cyclic derivatives of alkyl dihydroxyalkylxanthenes
    8.
    发明授权
    Cyclic derivatives of alkyl dihydroxyalkylxanthenes 失效
    烷基二羟基烷基呫吨的环状衍生物

    公开(公告)号：US4713455A

    公开(公告)日：1987-12-15

    申请号：US848139

    申请日：1986-04-04

    申请人： Harald Furrer ,  Hiristo Anagnostopulos ,  Ulrich Gebert

    发明人： Harald Furrer ,  Hiristo Anagnostopulos ,  Ulrich Gebert

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P11/08 ,  C07C21/04 ,  C07C29/10 ,  C07C31/42 ,  C07D303/08 ,  C07D317/16 ,  C07D317/20 ,  C07D473/06 ,  C07D473/08 ,  C07D473/10 ,  C07D405/06

    CPC分类号： C07D473/08 ,  C07C29/10 ,  C07C31/42 ,  C07D303/08 ,  C07D317/16 ,  C07D317/20 ,  C07D473/06

    摘要： Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.

    摘要翻译： 式（I）的化合物其中基团R 1，R 2或R 3中的一个表示具有4至8个C原子的直链烷基和ω，ω-1或ω-1中的两个邻位羟基， ω-2位，另外两个基团表示在R 2和R 3的位置具有至多12个C原子的直链或支链烷基，R2的位置中具有至多4个C原子的直链或支链烷基，这两个基团中的C原子总数 通过氧化相应的链烯基黄嘌呤并通过引入二羟基烷基或其前体的化合物进行烷基化来制备最多14个的烷基取代基。 二羟基烷基二烷基黄嘌呤适用于治疗阻塞性呼吸道疾病。

    Pyridine compounds, pharaceutical compositions, their use in allergy therapy
    10.
    发明授权
    Pyridine compounds, pharaceutical compositions, their use in allergy therapy 失效
    吡啶化合物，药物组合物，它们在过敏疗法中的应用

    公开(公告)号：US4792554A

    公开(公告)日：1988-12-20

    申请号：US933532

    申请日：1986-11-21

    申请人： Ulrich Elben ,  Hiristo Anagnostopulos ,  Robert R. Bartlett

    发明人： Ulrich Elben ,  Hiristo Anagnostopulos ,  Robert R. Bartlett

    IPC分类号： A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61P37/08 ,  C07D213/74 ,  C07D213/80 ,  C07D213/85 ,  C07D213/89 ,  C07D401/12 ,  A61K31/44 ,  C07D295/12

    CPC分类号： C07D213/74 ,  C07D213/80 ,  C07D213/85 ,  C07D213/89 ,  C07D401/12

    摘要： A pyridine compound of the formula I ##STR1## in which R.sup.1 and R.sup.2 independently of each other represent hydrogen or alkyl having from 1 to 4 carbon atoms,R.sup.3 represents hydrogen or alkyl having up to 2 carbon atoms andA represents alkylene having 2 to 4 carbon atoms, n is O or 1,Z is a group of the formula Za, Zb or Zc ##STR2## in which either R.sup.4 is hydrogen andR.sup.5 is phenyl or cinnamyl orR.sup.4, R.sup.5, R.sup.7 and R.sup.8 independently of each other are pyridyl, phenyl or phenyl which is substituted by up to 2 equal or different substituents from the group halogen and alkoxy having up to 2 carbon atoms,R.sup.6 is hydrogen or hydroxy andX is hydrogen, a cyano, amino or nitro group or the group --CO--R.sup.9, in whcih R.sup.9 is hydroxy or alkoxy having from 1 to 4 carbon atoms,and the physiologically tolerable salts of these compounds. The invention also relates to a process for the manufacture of such compounds and to their use in pharmaceutical compositions.

    摘要翻译： 其中R 1和R 2彼此独立地表示氢或具有1至4个碳原子的烷基，R 3表示氢或具有至多2个碳原子的烷基，并且A表示具有至少2个碳原子的烷基的式I的吡啶化合物 2至4个碳原子，n为0或1，Z为式Za，Zb或Zc的基团，其中R4为氢，R5为苯基或肉桂基，R4，R5，R7和R8分别为 另外是吡啶基，苯基或苯基，其被至多2个相同或不同的取代基取代为卤素和具有至多2个碳原子的烷氧基，R6是氢或羟基，X是氢，氰基，氨基或硝基或 基团-CO-R9，其中R9是具有1至4个碳原子的羟基或烷氧基，以及这些化合物的生理上可耐受的盐。 本发明还涉及制备这些化合物及其在药物组合物中的用途的方法。