Cephem compounds
    42.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号:US4861769A

    公开(公告)日:1989-08-29

    申请号:US828527

    申请日:1986-02-12

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, lower alkylthio, lower alkenyl, lower alkenylthio, lower alkynyl, heterocyclicthio or a heterocyclic group, in which lower alkylthio, lower alkenyl, lower alkenylthio, heterocyclicthio and a heterocyclic group may have suitable substituent(s),R.sup.4 and R.sup.5 are each hydrogen, halogen or arylthio,A is lower alkylene, andn is an integer of 0 or 1,and a pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical composition comprising the same.

    摘要翻译: 下式的化合物,其中R 1是低级烷基,低级烷酰基,芳基,芳(低级)烷基或杂环基,其各自可以具有合适的取代基,R 2是羧基或被保护的羧基,R 3是 氢,卤素,羟基,低级烷氧基,酰氧基,低级烷硫基,低级烯基,低级链烯硫基,低级炔基,杂环硫基或杂环基,其中低级烷硫基,低级烯基,低级链烯硫基,杂环硫基和杂环基可具有合适的取代基 s)中,R 4和R 5各自为氢,卤素或芳硫基,A为低级亚烷基,n为0或1的整数,及其药学上可接受的盐,其制备方法和包含其的药物组合物。

    Cephem compounds
    44.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号:US4420477A

    公开(公告)日:1983-12-13

    申请号:US209988

    申请日:1980-11-24

    摘要: This invention relates to novel cephem compounds of high antimicrobial activity, said compounds being of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or a protected amino group; and R.sup.6 is lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cyclo(lower)alkenyl, aryl, ar(lower)alkyl, or halogen-substituted ar(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group;A is hydroxy(lower)alkylene, amino(lower)alkylene, protected amino(lower)alkylene, lower alkenylene, hydroxyimino(lower)alkylene, lower alkoxyimino(lower)alkylene, or lower alkenyloxyimino(lower)alkylene; andR.sup.3 is carboxy or a protected carboxy group, and pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明涉及高抗微生物活性的新型头孢烯化合物,所述化合物具有下式:其中R 1是下式的基团:其中R 5是氨基或被保护的氨基; 低级烯基,低级炔基,环烷基,环(低级)烯基,芳基,芳(低级)烷基或卤素取代的芳(低级)烷基; R2是羧基或被保护的羧基; A是羟基(低级)亚烷基,氨基(低级)亚烷基,保护的氨基(低级)亚烷基,低级亚烯基,肟基(低级)亚烷基,低级烷氧基亚氨基(低级)亚烷基或低级烯氧基亚氨基(低级) 且R 3为羧基或被保护的羧基,及其药学上可接受的盐。

    Process for making fluorinated 4-azasteroid derivatives
    46.
    发明申请
    Process for making fluorinated 4-azasteroid derivatives 失效
    氟化4-氮灰石衍生物的制备方法

    公开(公告)号:US20060252937A1

    公开(公告)日:2006-11-09

    申请号:US11410179

    申请日:2006-04-24

    IPC分类号: C07D471/02 C07D221/18

    摘要: The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.

    摘要翻译: 本发明涉及可用于制备调节雄激素受体并且用于治疗由雄激素缺乏或雄激素受体多动症引起的疾病的合成方法,例如骨质疏松症,牙周病,骨折,虚弱, 勃起功能障碍,性欲丧失,雄激素依赖性癌症和肌肉减少症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。

    Amine salts of an integrin receptor antagonist
    47.
    发明授权
    Amine salts of an integrin receptor antagonist 失效
    整合素受体拮抗剂的胺盐

    公开(公告)号:US07074930B2

    公开(公告)日:2006-07-11

    申请号:US10494760

    申请日:2002-11-01

    IPC分类号: C07D471/04 A61K31/44

    CPC分类号: C07C215/10 C07D471/04

    摘要: Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin αvβ3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.

    摘要翻译: 3- {2-氧代-3- [3-(5,6,7,8-四氢[1,8]萘啶-2-基) - 丙基]咪唑烷-1-基} -3-(6 - 甲氧基 - 吡啶-3-基)丙酸是整联蛋白α2受体的有效拮抗剂,可用于预防和/或治疗骨质疏松症和血管再狭窄,以及与过度血管生成相关的病症,如黄斑变性,糖尿病 视网膜病变,动脉粥样硬化,炎性关节炎,癌症和转移性肿瘤生长。 本发明还涉及制备新型盐的方法以及含有盐的药物组合物和使用该盐的方法。