METHOD FOR SEPARATING GEOMETRICAL ISOMER
    1.
    发明公开

    公开(公告)号:US20240010615A1

    公开(公告)日:2024-01-11

    申请号:US18253137

    申请日:2021-12-20

    IPC分类号: C07C405/00

    摘要: The present invention provides a method for separating a compound represented by Formula (1) or (2) [in the formula, P1 is a hydrogen atom or a protective group of a hydroxyl group, R1 is a linear or branched C1-6 alkyl group that may be substituted with a phenyl group, A is an alkenylene group, and R2 is a hydroxyl group, a C1-3 alkoxy group, a mono(C1-3 alkyl)amino group, or a di(C1-3 alkyl)amino group] from a geometrical isomer thereof, in which the geometrical isomer is a geometrical isomer in a double bond included in A, the method including processing a mixture containing the compound and the geometrical isomer thereof by a chromatographic method using an acidic functional group-modified silica gel as a stationary phase.

    NOVEL PROCESSES FOR THE PREPARATION OF PROSTAGLANDIN AMIDES
    6.
    发明申请
    NOVEL PROCESSES FOR THE PREPARATION OF PROSTAGLANDIN AMIDES 审中-公开
    制备前列腺素的新方法

    公开(公告)号:US20160137602A1

    公开(公告)日:2016-05-19

    申请号:US14965489

    申请日:2015-12-10

    申请人: CHINOIN ZRT

    摘要: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula, the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5, 6 and 13, 14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.

    摘要翻译: 本发明的主题是制备通式I的前列腺素酰胺的方法,其中在该式中,用虚线标记的键可以是单键或双键,在5,6位的双重界限的情况下, 13,14可以是顺式或反向取代,Q表示羟基,Z表示羟基或氧代基,R1和R2独立地表示氢原子或直链或支链C1-10烷基或 任选被-ONO 2基团取代的芳烷基,或含有杂原子的芳烷基 - 或芳基,R 3表示直链或支链,饱和或不饱和的C 4-6烃基或C 4-10烷基环烷基 - 或环烷基 - 基团或任选具有烷基或卤素原子取代的苯基 - ,C7-10烷基芳基或杂芳基,Y表示(CH 2)n基团或O原子或S原子,并且其中n = 0-3。

    POLYMER CONJUGATED PROSTAGLANDIN ANALOGUES
    10.
    发明申请
    POLYMER CONJUGATED PROSTAGLANDIN ANALOGUES 审中-公开
    聚合物共聚物PROSTAGLANDIN ANALOGUES

    公开(公告)号:US20140120058A1

    公开(公告)日:2014-05-01

    申请号:US14111408

    申请日:2012-04-12

    IPC分类号: A61K47/48

    CPC分类号: A61K47/595 C07C405/00

    摘要: The present invention relates in general to polymer-drug conjugates. In particular, the invention relates to polymer-drug conjugates wherein the conjugated drugs are selected from prostaglandins and substituted prostaglandins, to a method of delivering such prostaglandin drugs to a subject, to a sustained drug delivery system comprising the polymer-drug conjugates, to a method of preparing the polymer-drug conjugates, and to an implant comprising the polymer-drug conjugates. The polymer-drug conjugates may be useful for delivering prostaglandins and substituted prostaglandins for the treatment of glaucoma.

    摘要翻译: 本发明一般涉及聚合物 - 药物共轭物。 特别地,本发明涉及其中所述共轭药物选自前列腺素和取代的前列腺素的聚合物 - 药物偶联物,涉及将这种前列腺素药物递送至受试者的方法,包括所述聚合物 - 药物共轭物的持续药物递送系统, 制备聚合物 - 药物共轭物的方法,以及包含聚合物 - 药物共轭物的植入物。 聚合物 - 药物共轭物可用于递送前列腺素和替代的前列腺素用于治疗青光眼。