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    Method for preparing dihydroquercetin
    1.
    发明授权
    Method for preparing dihydroquercetin 有权

    公开(公告)号：US11753389B2

    公开(公告)日：2023-09-12

    申请号：US18008044

    申请日：2022-05-07

    Applicant: HEFEI LIFEON PHARMACEUTICAL CO., LTD.

    Inventor： Junqiu Ji ,  Xiaochang Li ,  Bing Li ,  Qiao Li ,  Qing Miao ,  Limei Liu ,  Jinping Liu

    IPC: C07D311/32 ,  C07D311/40

    CPC classification number: C07D311/32 ,  C07D311/40

    Abstract: The present disclosure provides a preparation method of dihydroquercetin, belonging to the field of synthesis of drugs. The method includes steps of: adjusting reaction solvent water to be alkaline with an alkalizing reagent, to obtain an alkaline aqueous solution; dissolving quercetin dihydrate in the alkaline aqueous solution, and adding a sulfite binary combined reducing agent to carry out reduction reaction, to obtain an endpoint reduction reaction solution; diluting the endpoint reduction reaction solution with water, and then acidizing, aging, and filtering the resultant to obtain a filtrate and a filter cake; subjecting the filtrate to extraction, washing, drying, and vacuum concentration to obtain a concentrated crude product; and repeatedly crystallizing the concentrated crude product to obtain dihydroquercetin. The preparation method of the present disclosure has readily available raw materials, a simple process, and low production costs, and is particularly suitable for industrial production.

    T-TYPE CALCIUM CHANNEL INHIBITOR
    7.
    发明申请
    T-TYPE CALCIUM CHANNEL INHIBITOR 审中-公开
    T型钙通道抑制剂

    公开(公告)号：US20160096815A1

    公开(公告)日：2016-04-07

    申请号：US14892392

    申请日：2014-05-16

    Applicant: KINKI UNIVERSITY ,  FUSO PHARMACEUTICAL INDUSTRIES, LTD.

    Inventor： Atsufumi KAWABATA ,  Hideaki MATSUDA ,  Fumiko SEKIGUCHI ,  Kazuya MURATA ,  Hiroyuki NISHIKAWA

    IPC: C07D311/32

    CPC classification number: C07D311/32 ,  A61K31/352

    Abstract: The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R1 and R2 independently represents H, —OH or —OR11, wherein R11 represents a C1-3 alkyl group; each of R3 and R4 independently represents H, —OH or —OR12, wherein R12 represents a C1-3 alkyl group; and each of R5 and R6 independently represents H, a halogen atom, a C1-10 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a phenyl group (which may be substituted by a C1-6 alkoxy group or a halogen atom), a —C1-3 alkyl-phenyl group (which may be substituted by a C1-6 alkyloxy group or a halogen atom) or a C10-50 prenyl group.)

    Abstract translation: 本发明提供了由式（1）表示的化合物，该化合物的药学上可接受的盐或该化合物的溶剂化物的T型钙通道抑制剂。 本发明还提供：该T型钙通道抑制剂; 含有该T型钙通道抑制剂的药物; 以及用于疾病的治疗剂或预防剂，其有效作用是T型钙通道抑制作用。 （式（1）中，R 1和R 2各自独立地表示H，-OH或-OR 11，其中R 11表示C 1-3烷基; R 3和R 4各自独立地表示H，-OH或-OR 12，其中R 12表示 C 1-3烷基; R 5和R 6各自独立地表示H，卤素原子，C 1-10烷基，C 2-6烯基，C 2-6炔基，苯基（可以被取代 通过C 1-6烷氧基或卤素原子），-C 1-3烷基 - 苯基（其可以被C 1-6烷氧基或卤素原子取代）或C10-50异戊烯基）。

    Compounds and Mixtures Influencing Inflammatory States
    9.
    发明申请
    Compounds and Mixtures Influencing Inflammatory States 审中-公开
    影响炎症状态的化合物和混合物

    公开(公告)号：US20130251730A1

    公开(公告)日：2013-09-26

    申请号：US13782391

    申请日：2013-03-01

    Applicant: SYMRISE AG

    Inventor： Jakob Ley ,  Katharina Reichelt ,  Marcus Götz ,  Maria Blings ,  Veronika Somoza ,  Jessica Walker ,  Joel Michael Walker

    IPC: A61K31/192 ,  C07D311/58 ,  A23L1/30 ,  C07D311/32 ,  A61K45/06 ,  C07C65/40 ,  A61K31/353

    CPC classification number: A61K31/192 ,  A23L33/105 ,  A61K8/365 ,  A61K8/498 ,  A61K31/352 ,  A61K31/353 ,  A61K45/06 ,  A61K2800/10 ,  A61Q19/00 ,  C07C65/40 ,  C07D311/32 ,  C07D311/58 ,  A61K2300/00

    Abstract: Suggested is a compound of the formula (X) or any salt of a compound of the formula (X) or any mixture containing or consisting of two or more different compounds of the formula (X), two or more different salts of compounds of the formula (X) or one or more different compounds of the formula (X) and one or more different salts of compounds of the formula (X), wherein for R1, R2 and R3 independently of one another in every compound of the formula (X) the following applies: R1 means hydrogen or methyl, R2 means an organic residue with 5 carbon atoms and one oxygen atom or none and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, or R1 and R2 together with the carbon atoms in positions 4 and 5 and the oxygen atom bound to the carbon atom in position 4 form a ring and comprise 5 carbon atoms and one oxygen atom or none, and R3 means an organic residue with 10 carbon atoms and one or more oxygen atoms, for use in a method for the prophylaxis and/or treatment of inflammation.

    Abstract translation: 建议式（X）的化合物或式（X）化合物的任何盐或含有两种或更多种不同式（X）化合物的任何混合物或两种或更多种不同的 式（X）或一种或多种不同的式（X）化合物和一种或多种式（X）化合物的不同盐，其中对于R 1，R 2和R 3在每个式（X ）适用：R 1表示氢或甲基，R 2表示具有5个碳原子和一个氧原子的有机残基或不表示R 3表示具有10个碳原子和一个或多个氧原子的有机残基，或R 1和R 2与 位置4和5中的碳原子和结合到位置4的碳原子的氧原子形成环，并且包含5个碳原子和一个氧原子或不存在，并且R 3表示具有10个碳原子和一个或多个氧原子的有机残基 ，用于预防和/或治疗的方法 炎症。

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