176445-80-0Relevant articles and documents
KRAS G12D INHIBITORS
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Paragraph 0344-0345, (2022/02/15)
The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
Preparation method of heterocyclic compound and salt thereof
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, (2019/07/01)
The invention belongs to the field of organic chemistry and specifically relates to a preparation method of a heterocyclic compound as shown in the formula I and salt thereof. In comparison with the prior art, the invention has the following beneficial effects: the use of the extremely toxic substance cyanide is avoided; there is no cyanide ion residue in the reaction product and the reaction waste such that environmental burden is greatly reduced. In addition, the price of the reaction materials is low; the preparation method is simple; the yield is high; and the preparation method is suitable for large-scale industrial production. It is found unexpectedly that by the adoption of the method of the scheme 4, such as use of a reducing agent and under the acidic condition, the compound VIIIcan be obtained by one-step reaction and the off-protecting group, alkylation and cyano group reduction are realized to obtain the target product. The defect that polystep reactions are required in the prior art is greatly improved.
NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
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Paragraph 0147; 0148; 0149; 0150, (2014/11/27)
Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
