1672665-49-4

Usage

Uses

Used in Pharmaceutical Industry:
PT-2385 is used as a HIF-2α antagonist for targeting the HIF-2α protein, which plays a crucial role in various cellular processes and is implicated in several diseases. Its high specificity and potency make it a promising candidate for the development of novel therapeutics.
Used in Cancer Research:
In the field of cancer research, PT-2385 is used as a research tool to study the role of HIF-2α in tumor growth and progression. Its ability to inhibit HIF-2α activity can provide valuable insights into the development of targeted cancer therapies.
Used in Drug Development:
PT-2385 is utilized in drug development as a lead compound for the creation of new medications that can potentially treat diseases associated with HIF-2α dysregulation. Its specificity and potency make it an attractive starting point for the design and synthesis of more effective and targeted drugs.

Upstream product

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Relevant academic research and scientific papers

Method for preparing HIF-2 alpha inhibitor PT2385

The invention relates to a preparation method of HIF-2 alpha inhibitor PT2385. To the method, difluorobenzene is taken as a raw material, and reacted with 3 - chloropropionyl chloride to generate an intermediate II which reacts with sodium methoxide to generate an intermediate III which is subsequently oxidized. The intermediate VII is obtained through an oxidation reaction, and the intermediate VIII is obtained by reaction with n-butylamine to obtain compound IX which is subjected to fluorination reaction and hydrolysis to obtain intermediate X which is finally subjected to asymmetric reduction reaction to obtain final product PT2385. Compared with the existing synthetic method, the process route provided by the invention has the obvious advantages of cheap and easily available raw materials, simple operation, few reaction steps, high total yield of 47.6%, avoidance of multi-step high-temperature reaction and easiness in industrial production. .

METHODS OF REDUCING INFLAMMATION OF THE DIGESTIVE SYSTEM WITH INHIBITORS OF HIF-2-ALPHA

The present disclosure provides methods of reducing inflammation of the digestive system in a subject in need thereof, including subjects suffering from inflammatory bowel disease. Compositions for use in these methods are also provided.

COMBINATION THERAPY OF A HIF-2-ALPHA INHIBITOR AND AN IMMUNOTHERAPEUTIC AGENT AND USES THEREOF

The present invention provides methods and pharmaceutical compositions for treating proliferative disorders. The method involves step of administering to said subject a HIF-2alpha inhibitor and an immunotherapeutic agent.

COMPOSITIONS FOR USE IN TREATING PULMONARY ARTERIAL HYPERTENSION

The present disclosure provides methods of treating pulmonary arterial hypertension (PAH) in a subject in need thereof. Compositions for use in these methods are also provided.

HIF-2-ALPHA INHIBITOR POLYMORPHS

Chemical compounds that modulate HIF-2α activity, their polymorphs, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with HIF-2α, are described herein.

HIF-2α INHIBITORS FOR TREATING IRON OVERLOAD DISORDERS

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating iron overload disorders. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and reduced liver iron accumulation and serum iron parameters in both prophylactic and treatment mouse models.

COMPOSITIONS FOR USE IN TREATING GLIOBLASTOMA

The present disclosure provides methods of treating glioblastoma multiform (GBM) in a subject in need thereof. Compositions for use in these methods are also provided.