91446-15-0

Usage

Uses

As the specific properties and uses of 4-chloro-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyriMidine have not been extensively studied or documented, its applications are currently not well-defined. However, given the general biological activities associated with pyrazolo[3,4-d]pyrimidines, potential uses in the following areas could be explored:
Used in Pharmaceutical Industry:
4-chloro-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyriMidine could be used as a pharmaceutical agent for its potential anti-inflammatory, antiviral, and antitumor properties, pending further research and development.
Used in Medicinal Chemistry Research:
4-chloro-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyriMidine may serve as a starting point for medicinal chemistry research aimed at developing new drugs with improved efficacy and selectivity, based on its structural features and the biological activities of related pyrazolo[3,4-d]pyrimidines.

InChI:InChI=1/C10H11ClN4O/c11-9-7-5-14-15(10(7)13-6-12-9)8-3-1-2-4-16-8/h5-6,8H,1-4H2

Upstream product

• 76-26-6 camphor-10-sulfonic acid 
• 5399-92-8 4-chloro-1H-pyrazolo[3,4-d]pyrimidine 
• 110-87-2 3,4-dihydro-2H-pyran 

Downstream Products

• 1196486-96-0 4-(4-methanesulfonyl-phenoxy)-1-(tetrahydro-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine 
• 1423126-48-0 1-(4-((1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)phenyl)-3-(2,3-dimethylphenyl)urea 

Relevant academic research and scientific papers

Bisarylureas based on 1H-Pyrazolo[3,4-d]pyrimidine Scaffold as Novel Pan-RAF inhibitors with potent anti-proliferative activities: Structure-based design, synthesis, biological evaluation & molecular modelling studies

RAF (Ras activating factor) kinases are important and attractive targets for cancer therapy. With the aim of discovering RAF inhibitors that bind to DFG-out inactive conformation created by the movement of Asp-Phe-Gly (DFG), we conducted structure-based drug design using the X-ray cocrystal structures of BRAF (v-raf murine sarcoma viral oncogene homolog B1), starting from bisarylurea derivative based on 1H-pyrazolo[3,4-d]pyrimidine scaffold 1a. Most of the synthesized compounds showed good to excellent inhibitory activities against BRAFV600E kinase, possessed moderate to potent anti-proliferative activities against four tumor cell lines (A375, HT-29, PC-3 and A549) and good selectivity towards cancer cells rather normal cells (Madin-Darby canine kidney, MDCK). The most promising compound, 1v, exhibited potent inhibitory activity against not only BRAFV600E (half maximal inhibitory concentration, IC50 = 23.6 nM) but also wild-Type BRAF (IC50 = 51.5 nM) and C-RAF (IC50 = 8.5 nM), and effective cellular anti-proliferative activities against A375, HT-29, PC-3 and A549 cell lines as well as a very good selectivity profile. Moreover, compound 1v mainly arrested the A375 cell line in the G0/G1 stage, and showed significant suppression of MEK (mitogen-Activated protein kinase kinase) phosphorylation in A375 and HT-29 cell lines. Taken together, the optimal compound 1v showed excellent in vitro potency as a pan-RAF inhibitor. In addition, the promise of compound 1v was further confirmed by molecular dynamics simulation and binding free energy calculations.

1-(2-tetrahydropyrane)-1H-pyrazole[3, 4-d] pyrimidine compound having anti-tumor activity and preparation method thereof

The invention discloses a 1-(2-tetrahydropyrane)-1H-pyrazole[3, 4-d] pyrimidine compound having anti-tumor activity. A general formula of the compound is shown as follows. The invention further discloses a synthesis method of the compound and a medicinal composition containing the compound. The invention further discloses application of the medicinal composition in treating diseases caused by protein kinase activity abnormality. The pyrazole [3, 4-d] pyrimidine compound which is novel in structure and remarkable in anti-tumor activity is developed. The compound can be used as a double-target inhibitor of BRAF/VEGFR-2 kinase and has good effect and wide application prospect in the aspect of treating the diseases caused by protein kinase activity abnormality.

Protein kinase inhibitor and its composition and use thereof

The invention relates to compounds as shown in the general formula (I), pharmaceutical compositions containing the compounds, a method for treating diseases and disease symptoms related to abnormal activity of protein kinase by using the compounds, and medicinal use of the compounds.

3,3-DIFLUORO-PIPERIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS

Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).

N-PYRIDINYL ACETAMIDE DERIVATIVES AS WNT SIGNALLING PATHWAY INHIBITORS

This invention relates to compounds. More specifically, the invention relates to compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

SUBSTITUTED QUINOXALINES AND BENZOTRIAZINE P70S6 KINASE INHIBITORS

The invention provides compounds that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (0), or a salt, tautomer or N-oxide thereof; wherein: X1 is N or N+(0-); X2 is N or CH; Q1 is an optionally substituted C1-8 alkylene; Q2 is a bond or an optionally substituted C1-8 alkylene group; R1 is selected from hydrogen and a group Cy1; Cy1 is an optionally substituted 4 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic group containing 0, 1 or 2 heteroatom ring members selected from O and S and oxidised forms of S; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine, C1-2 alkyl and C1-2 alkoxy, wherein each C1-2 alkyl and C1-2 alkoxy is optionally substituted with two or more fluorine atoms; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring Ar2 is an optionally substituted bicyclic 8 to 1 1 -membered heteroaryl group containing 1, 2, 3 or 4 heteroatom ring members selected from O, N and S. The compounds are useful in medicine, for example in the treatment of a disease or condition selected from cancers (e.g. triple negative breast cancer, brain tumours and brain metastases arising from non-brain cancers), neurodevelopmental diseases (e.g. Fragile X syndrome) and neurodegenerative diseases.

DIFLUOROETHYLPYRIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS

Disclosed are chemical entities of formula (I) wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

KINASE MODULATING COMPOUNDS, COMPOSITIONS CONTAINING THE SAME AND USE THEREOF

The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.

GPR119 Receptor Agonists

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.