Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same
    2.
    发明授权
    Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same 失效
    固体形式的大环内酯类化合物,其制备方法和含有该化合物的药物组合物

    公开(公告)号:US07790887B2

    公开(公告)日:2010-09-07

    申请号:US12021184

    申请日:2008-01-28

    IPC分类号: C07D411/14

    CPC分类号: C07D407/06

    摘要: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

    摘要翻译: 本发明提供了固体形式的式(I)化合物,其作为药物制造的大量药物是均匀的,具有高纯度,并且易于加工。 本发明还提供了制备该化合物的方法和含有该化合物的药物组合物。 (8E,12E,14E)-7 - {(4-环庚基哌嗪-1-基)羰基}氧-3,6,16,21-四羟基-6,10,12,16,20-五甲基 - 开发了具有统一规格并且易于使用的18,19-环氧树脂-8,12,14-三烯-11-硼化物。

    METHOD FOR PRODUCING PYRAZOLE FUSED RING DERIVATIVE
    3.
    发明申请
    METHOD FOR PRODUCING PYRAZOLE FUSED RING DERIVATIVE 审中-公开
    用于生产吡唑熔融衍生物的方法

    公开(公告)号:US20100217001A1

    公开(公告)日:2010-08-26

    申请号:US12738514

    申请日:2008-10-17

    IPC分类号: C07D471/04 C07F5/02

    CPC分类号: C07D471/04 C07F5/025

    摘要: Disclosed is a commercially advantageous method for producing a pyrazole fused ring derivative (such as a 7-phenylpyrazolo[1,5-a]pyridine derivative). Specifically disclosed is a method for producing a compound (I) represented by the formula (I) below or a salt thereof, which comprises a step A wherein a hydroxy group in a compound (IV) represented by the formula (IV) below is converted into a methoxy group, thereby obtaining a compound (I) or a salt thereof:

    摘要翻译: 公开了用于制备吡唑稠环衍生物(如7-苯基吡唑并[1,5-a]吡啶衍生物)的商业上有利的方法。 具体公开的是制备下述式(I)表示的化合物(I)或其盐的方法,其包括步骤A,其中由下式(IV)表示的化合物(IV)中的羟基转化为 形成甲氧基,从而得到化合物(I)或其盐:

    MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
    5.
    发明申请
    MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
    固体形式的MACROLIDE化合物,其制备方法和含有该化合物的药物组合物

    公开(公告)号:US20080214564A1

    公开(公告)日:2008-09-04

    申请号:US12021184

    申请日:2008-01-28

    IPC分类号: A61K31/497 C07D405/12

    CPC分类号: C07D407/06

    摘要: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

    摘要翻译: 本发明提供了固体形式的式(I)化合物,其作为药物制造的大量药物是均匀的,具有高纯度,并且易于加工。 本发明还提供了制备该化合物的方法和含有该化合物的药物组合物。 (8E,12E,14E)-7 - {(4-环庚基哌嗪-1-基)羰基}氧-3,6,16,21-四羟基-6,10,12,16,20-五甲基 - 开发了具有统一规格并且易于使用的18,19-环氧树脂-8,12,14-三烯-11-硼化物。

    Process for preparation of water-soluble azole prodrugs
    7.
    发明授权
    Process for preparation of water-soluble azole prodrugs 有权
    制备水溶性唑前体药物的方法

    公开(公告)号:US07803949B2

    公开(公告)日:2010-09-28

    申请号:US12097244

    申请日:2006-12-20

    IPC分类号: C07F9/06

    CPC分类号: C07F9/65583

    摘要: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.

    摘要翻译: 本发明的目的是提供一种适于工业化有效的脱保护反应而不使用有毒溶剂的方法,以及提供一种制备水溶性唑类药物的方法等。 。 本发明提供由式(I)表示的盐的制备方法。 (其中X表示在苯基的第4位或第5位键合的氟原子),包括以下步骤:(a)进行式(II)表示的化合物的脱保护反应; (其中X表示在苯基的4位或5位键合的氟原子)在碳阳离子清除剂存在下进行。

    PROCESS FOR PRODUCTION OF LIPID A ANALOGUE
    8.
    发明申请
    PROCESS FOR PRODUCTION OF LIPID A ANALOGUE 审中-公开
    生产脂类似物的方法

    公开(公告)号:US20090149647A1

    公开(公告)日:2009-06-11

    申请号:US12064450

    申请日:2006-08-29

    IPC分类号: C07H1/00

    CPC分类号: C07H15/04 C07H1/02

    摘要: Discloses is a process for producing α-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-β-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source.

    摘要翻译: 公开了制备α-D-吡喃葡萄糖,3-O-癸基-2-脱氧-6-O- [2-脱氧-3-O - [(3R)-3-甲氧基癸基] -6-O-甲基 -2 - [(11Z)-1-氧代-11-十八碳烯基]氨基] -4-O-膦酰基-β-D-吡喃葡萄糖基] -2 - [(1,3-二氧代十四烷基)氨基] - 或1- 磷酸盐)四钠盐,其可用作其合成的药物或中间体的活性成分,其环境友好并且安全性,操作性和再现性优异。 一种制备由式(I)表示的化合物的方法,包括以下步骤:使式(VIII)表示的化合物与钯催化剂在一种核仁类药剂的存在下反应并用钠源处理该产物。

    Apparatus, method, and storage medium for file management
    9.
    发明授权
    Apparatus, method, and storage medium for file management 失效
    用于文件管理的装置,方法和存储介质

    公开(公告)号:US06795834B2

    公开(公告)日:2004-09-21

    申请号:US09748372

    申请日:2000-12-27

    IPC分类号: G06F1200

    摘要: When a sweeping process and a backup process are performed on an electronic library file in an electronic library, a file storing a history of the sweeping process or a history of a backup process is generated, and the sweeping and the backup processes are managed. Thus, a user can easily manage as to which medium an original document has been swept to or where a backup copy of the original document is. If the uniqueness of the original document shown in a sweep history and a backup history can be secured, the problem that there can be a plurality of original documents on the storage media of a plurality of electronic libraries can be avoided.

    摘要翻译: 当在电子图书馆的电子图书馆文件中执行扫描处理和备份处理时,生成存储扫描处理的历史或备份处理的历史的文件,并且管理扫描和备份处理。 因此,用户可以容易地管理原始文档被扫描到哪个媒体或原始文档的备份副本的位置。 如果可以确保扫描历史和备份历史中所示的原始文档的唯一性,则可以避免在多个电子图书馆的存储介质上存在多个原始文档的问题。

    Heterocyclic-ring condensed benzothiazine compound
    10.
    发明授权
    Heterocyclic-ring condensed benzothiazine compound 失效
    杂环稠合苯并噻嗪化合物

    公开(公告)号:US06583138B1

    公开(公告)日:2003-06-24

    申请号:US09622458

    申请日:2001-01-04

    IPC分类号: C07D51304

    CPC分类号: C07D513/04

    摘要: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula: In the formula, the ring Het represents an unsaturated heterocyclic ring; R1 and R2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula —NR20R2 (in the formula, R20 and R21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R20 and R21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.

    摘要翻译: 本发明提供一种新颖的杂环稠合苯并噻嗪化合物,其对组胺,白细胞三烯等参与的疾病的预防或治疗有效。 本发明的杂环稠合苯并噻嗪化合物或其药理学上可接受的盐对于预防或治疗其中化学介质如组胺,白三烯等参与的疾病是有效的,例如哮喘,过敏性鼻炎, 特应性皮炎,荨麻疹,花粉症,胃肠道过敏,食物过敏等。 此外,本发明的杂环稠合苯并噻嗪化合物,其药理学上可接受的盐或其水合物由下式表示:式中,环Het表示不饱和杂环; R1和R2彼此相同或不同,各自表示卤素原子,可以被卤素原子取代的低级烷基,可被卤素原子取代的低级烷氧基,低级烷基低级烷氧基 基团,氰基; D表示可以具有取代基的低级亚烷基等; Q表示例如式-NR20R2(式中,R20和R21彼此相同或不同,各自表示氢原子,可被卤素原子取代的低级烷基,芳基 可以具有取代基的芳基烷基,可以具有取代基的芳基烷基,可以具有取代基的杂芳基或可以具有取代基的杂芳基烷基,或者R20和R21可以与 氮原子); x表示1〜2的整数。