1022158-35-5

Usage

Uses

Used in Pharmaceutical Development:
4-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole is used as a pharmacological agent for the development of therapeutics targeting the CB2 receptor. Its high selectivity for this receptor makes it a valuable tool in creating medications aimed at managing pain, inflammation, and neurodegenerative diseases by modulating the endocannabinoid system.
Used in Research Applications:
In the field of scientific research, 4-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole serves as a research chemical to study the function and role of the CB2 receptor in various physiological and pathological processes. This helps in understanding the receptor's potential in treating different conditions and contributes to the advancement of medical knowledge in endocannabinoid system research.
Used in Drug Discovery:
4-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole is utilized as a lead compound in drug discovery for the identification and optimization of new molecules that can selectively target the CB2 receptor. This selective targeting is crucial for developing drugs with fewer side effects and increased efficacy in treating specific diseases.
Used in Neurodegenerative Disease Treatment:
In the medical industry, 4-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole is considered for use as a therapeutic agent for neurodegenerative diseases. Its interaction with the CB2 receptor suggests potential benefits in managing the symptoms and progression of such conditions, offering new avenues for treatment development.

Upstream product

• 110-87-2 3,4-dihydro-2H-pyran 
• 360575-28-6 2-bromo-6-fluorobenzaldehyde 
• 1073-06-9 3-fluorobromobenzene 
• 55289-36-6 3-bromo-2-methylaniline 
• 186407-74-9 4-bromoindazole 

Downstream Products

• 1022158-36-6 1-(tetrahydro-2H-pyran-2-yl)-1H-indazole-4-carbaldehyde 
• 1053655-57-4 1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-4-amine 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of thieno[3,2-d]pyrimidine derivatives containing aroyl hydrazone or aryl hydrazide moieties for PI3K and mTOR dual inhibition

Recently, PI3K and mTOR have been regarded as promising targets for cancer treatment. Herein, we designed and synthesized four series of novel thieno[3,2-d]pyrimidine derivatives that containing aroyl hydrazone or aryl hydrazide moieties. These derivatives act as PI3K/mTOR dual inhibitors, suggesting that they can be used as cancer therapeutic agents. All compounds were tested for anti-proliferative activity against four cancer cell lines. The structure-activity relationship (SAR) studies were conducted by varying the moieties at the C-6 and C-2 positions of the thieno[3,2-d]pyrimidine core. It indicated that aryl hydrazide at C-6 position and 2-aminopyrimidine at C-2 position are optimal fragments. Compound 18b showed the most potent in vitro activity (PI3Kα IC50 = 0.46 nM, mTOR IC50 = 12 nM), as well as good inhibition against PC-3 (human prostate cancer), HCT-116 (human colorectal cancer), A549 (human lung adenocarcinoma) and MDA-MB-231 (human breast cancer) cell lines. Furthermore, Annexin-V and propidium iodide (PI) double staining confirmed that 18b induces apoptosis in cytotoxic HCT-116 cells. Moreover, the influence of 18b on cell cycle distribution was assessed on the HCT-116 cell line, and a cell cycle arrest was observed at the G1/S phases.

INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE

Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.

POLYHETEROCYCLIC COMPOUNDS AS METTL3 INHIBITORS

The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity is implicated.

RAS INHIBITORS AND METHODS OF USING THE SAME

Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.

Application of C-H Functionalization in the Development of a Concise and Convergent Route to the Phosphatidylinositol-3-kinase Delta Inhibitor Nemiralisib

This paper describes the development of an improved and scalable method for the manufacture of nemiralisib, a phosphatidylinositol-3-kinase delta inhibitor. Incorporation of three consecutive catalytic reactions, including a palladium-catalyzed C-H functionalization and an iridium-catalyzed borylation, significantly simplified and shortened the synthetic sequence. The revised route was successfully implemented in a pilot plant on a multikilogram scale to deliver >100 kg of product.

METTL3 INHIBITORY COMPOUNDS

The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z5 (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity 10 is implicated.

Preparation method of thienopyrimidine compounds and application thereof

The invention relates to thienopyrimidine derivatives as shown in a general formula I, pharmaceutically acceptable salts or prodrugs and a preparation method thereof, which belong to the technical field of medicinal chemistry. In the general formula I, substituent groups L and R2 have meanings given in the specification. The invention also relates to a compound shown in the general formula I, which has a strong effect of inhibiting PI3K. The invention also relates to an application of the compounds and pharmaceutically acceptable salts, solvates or prodrugs thereof in preparation of drugs fortreating and/or preventing diseases caused by abnormal high expression of PI3K, especially the application in preparation of drugs for treating and/or preventing cancers.

ANTIBODY DRUG CONJUGATES (ADCS) WITH NAMPT INHIBITORS

Conjugate of a binder having formula: (A) wherein AB stands for a binder, Z' stands for a linker and D stands for an active component of Formula (I): and its use as pharmaceuticals.

CHEMICAL COMPOUNDS

The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.

INDAZOLE DERIVATIVES THAT DOWN-REGULATE THE ESTROGEN RECEPTOR AND POSSESS ANTI-CANCER ACTIVITY

The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.