A METHOD FOR THE PREPARATION OF INDOLE-3-CARBOXYLIC ACID DERIVATIVES

    公开(公告)号:WO2023067628A1

    公开(公告)日:2023-04-27

    申请号:PCT/IN2022/050940

    申请日:2022-10-20

    Abstract: The present invention provides a new synthetic method for the preparation of building block indole-3-carboxylic acid (ICA) derivatives used as a key starting material to produce several artificial drugs. An efficient, safe, operationally simple, cost-effective method for the preparation of several ICA derivatives has been introduced in a very simple way. Utilizing easily available starting material, reagent, and solvent several key starting materials of ICA derivatives have been synthesized rapidly indicates the novel method is functional group tolerable. The preparation process does not involve use of any reducing agents or transition metals in the economically viable and operationally simple condition in one pot. ICA derivatives have been generated from isatin derivative in one step and this methodology is important with a wide range of applications from the drug development and material synthesis point of view.

    METHODS FOR TREATING CENTRAL NERVOUS SYSTEM DISORDERS WITH MUSCARINIC RECEPTOR ACTIVATION AND ANTIPSYCHOTICS

    公开(公告)号:WO2022246405A1

    公开(公告)日:2022-11-24

    申请号:PCT/US2022/072374

    申请日:2022-05-17

    Abstract: Provided is a method of treating a central nervous system disorder in a patient in need thereof, the method comprising co-administering a first composition comprising xanomeline and/or a salt thereof and a second composition comprising an antipsychotic. In certain embodiments, a method of treating schizophrenia in a patient in need thereof is provided. For example, the method comprises co-administering a first composition comprising xanomeline and/or a salt thereof and a second composition comprising risperidone or aripiprazole. In certain embodiments, the first composition comprising xanomeline and/or a salt thereof further comprises an anticholinergic agent, such as a muscarinic antagonist.

    PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE OR DEMENTIA

    公开(公告)号:WO2022189366A1

    公开(公告)日:2022-09-15

    申请号:PCT/EP2022/055775

    申请日:2022-03-07

    Inventor: TASKER, Tim

    Abstract: This invention relates to the use of compounds which are agonists of the muscarinic M1 receptor and M4 receptor, their salts and pharmaceutical compositions containing them in therapy of the human body. In particular, the invention is directed to compounds, which are useful in the treatment of diseases mediated by the muscarinic M1/M4 receptors, including neurodegenerative disorders (i.e. Alzheimer's disease) and neuropsychiatric disorders (Schizophrenia).

    苯并噻唑类化合物的新晶型及其制备方法

    公开(公告)号:WO2021233461A1

    公开(公告)日:2021-11-25

    申请号:PCT/CN2021/098056

    申请日:2021-06-03

    Inventor: 鲁霞 张晓宇

    Abstract: 本发明涉及苯并噻唑类化合物的新晶型及其制备方法。本发明提供了式(I)化合物的晶型A及其制备方法和用途。本发明提供的式(I)化合物晶型A,在溶解度、熔点、稳定性、溶出度、引湿性、黏附性、流动性、生物有效性以及加工性能、提纯作用、制剂生产、安全性等方面中的至少一方面上存在优势,为含式(I)化合物的药物制剂的制备提供了新的更好的选择,对于药物开发具有非常重要的意义。

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