CRYSTALLINE FORMS OF ATORVASTATIN 4-(NITROOXY) BUTYL ESTER
    1.
    发明申请
    CRYSTALLINE FORMS OF ATORVASTATIN 4-(NITROOXY) BUTYL ESTER 审中-公开
    4-(硝基)丁酯酯的结晶形式

    公开(公告)号:US20100152274A1

    公开(公告)日:2010-06-17

    申请号:US12594511

    申请日:2008-03-19

    CPC分类号: C07D207/34

    摘要: The present invention relates to two crystalline forms designated as form A and form B, of (βR,δR)-2(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbon-yl]-1H-pyrrole-1-heptanoic acid 4-(nitrooxy)butyl ester (atorvastatin 4-(nitrooxy)butyl ester), represented by the formula (I), The invention also relates to processes for the preparation of the forms A and B, to pharmaceutical compositions comprising the two forms, and to their use for treating and/or preventing acute coronary syndromes, stroke, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis.

    摘要翻译: 本发明涉及两种结晶形式,其命名为(&bgr; R,δR)-2(4-氟苯基) - ,b-,δ-二羟基-5-(1-甲基乙基)-3-苯基的形式A和形式B -4 - [(苯基氨基)碳基] -1H-吡咯-1-庚酸4-(硝基氧基)丁酯(阿托伐他汀4-(硝基氧基)丁酯),由式(I)表示,本发明还涉及 用于制备形式A和B的方法,包含两种形式的药物组合物及其用于治疗和/或预防急性冠状动脉综合征,中风,神经变性疾病如阿尔茨海默病和帕金森病以及自身免疫疾病的用途 ,如多发性硬化症。

    Nitric oxide releasing steroids
    10.
    发明授权
    Nitric oxide releasing steroids 有权
    一氧化氮释放类固醇

    公开(公告)号:US08933062B2

    公开(公告)日:2015-01-13

    申请号:US12525970

    申请日:2008-01-28

    CPC分类号: C07J41/005

    摘要: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx  (I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position α or β; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

    摘要翻译: 本发明涉及通式(I)的糖皮质激素及其药学上可接受的盐或立体异构体的硝基氧基衍生物R-(Z)a-Rx(I)其中R是式(II)的皮质类固醇残基:其中:R1是OH,R2 -CH 3或R 1和R 2一起形成式(III)的基团,R 3为Cl或F; R4是H或F; 其中R 1,R 2,R 3和R 4可以连接到甾族结构在位置α或bgr中的相应碳原子。 条件是:当R 1和R 2是式(III)的基团时,R 3是F且R 4是H或F; 该化合物可用于治疗呼吸系统疾病,炎性疾病,皮肤病和眼部疾病。