862730-04-9

Usage

Uses

Used in Medicinal Chemistry:
3-Iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine is used as a chemical intermediate for the development of new pharmaceuticals. Its unique structure and potential biological activity make it a promising candidate for the creation of novel therapeutic agents.
Used in Drug Development:
In the pharmaceutical industry, 3-Iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine is utilized as a key component in the synthesis of various drug molecules. Its presence in these compounds may enhance their efficacy and selectivity, leading to improved treatments for a range of medical conditions.
Used in Research Laboratories:
3-Iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine is employed as a research tool in academic and industrial laboratories. It aids scientists in understanding the mechanisms of action of various biological processes and in the discovery of new drug targets.

Upstream product

• 75-29-6 isopropyl chloride 
• 151266-23-8 4-amino-3-iodo-pyrazolo[3,4-d]pyrimidine 
• 64834-00-0 4-aminopyrazolo[3,4-d]pyrimidine 
• 151266-23-8 4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidine 
• 2380-63-4 4-Aminopyrazolo<3,4-d>pyrimidin 
• 75-30-9 2-iodo-propane 
• 75-26-3 isopropyl bromide 

Downstream Products

• 1189793-15-4 4-amino-1-isopropyl-3-(4-phenethyl-1H-1,2,3-triazol-1-yl)-1H-pyrazolo[3,4-d]pyrimidine 
• 1189793-14-3 4-amino-3-(4-benzyl-1H-1,2,3-triazol-1-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidine 

Relevant academic research and scientific papers

Substituted aromatic fused ring derivative, composition containing same and application

The invention provides a substituted aromatic fused ring derivative, a composition containing the compound and application. The substituted aromatic fused ring derivative is a compound shown in a formula (I) or a tautomer, a stereoisomer, a prodrug, a cry

A Fluorescent Kinase Inhibitor that Exhibits Diagnostic Changes in Emission upon Binding

The development of a fluorescent LCK inhibitor that exhibits favourable solvatochromic properties upon binding the kinase is described. Fluorescent properties were realised through the inclusion of a prodan-derived fluorophore into the pharmacophore of an ATP-competitive kinase inhibitor. Fluorescence titration experiments demonstrate the solvatochromic properties of the inhibitor, in which dramatic increase in emission intensity and hypsochromic shift in emission maxima are clearly observed upon binding LCK. Microscopy experiments in cellular contexts together with flow cytometry show that the fluorescence intensity of the inhibitor correlates with the LCK concentration. Furthermore, multiphoton microscopy experiments demonstrate both the rapid cellular uptake of the inhibitor and that the two-photon cross section of the inhibitor is amenable for excitation at 700 nm.

SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS

Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1 and R2 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases

One effective means to achieve inhibitor specificity for RAF kinases, an important family of cancer drug targets, has been to target the monomeric inactive state conformation of the kinase domain, which, unlike most other kinases, can accommodate sulfonamide-containing drugs such as vemurafenib and dabrafenib because of the presence of a unique pocket specific to inactive RAF kinases. We previously reported an alternate strategy whereby rigidification of a nonselective pyrazolo[3,4-d]pyrimidine-based inhibitor through ring closure afforded moderate but appreciable increases in selectivity for RAF kinases. Here, we show that a further application of the rigidification strategy to a different pyrazolopyrimidine-based scaffold dramatically improved selectivity for RAF kinases. Crystal structure analysis confirmed our inhibitor design hypothesis revealing that 2l engages an active-like state conformation of BRAF normally associated with poorly discriminating inhibitors. When screened against a panel of distinct cancer cell lines, the optimized inhibitor 2l primarily inhibited the proliferation of the expected BRAFV600E-harboring cell lines consistent with its kinome selectivity profile. These results suggest that rigidification could be a general and powerful strategy for enhancing inhibitor selectivity against protein kinases, which may open up therapeutic opportunities not afforded by other approaches.

PYRAZOLOPYRIMIDINE DERIVATIVES AS BTK INHIBITORS FOR THE TREATMENT OF CANCER

This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of t

3-ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USES THEREOF

The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors.

MTOR MODULATORS AND USES THEREOF

The present invention provides methods and compositions for selective modulation of certain protein kinases, and especially mTor complexes. The methods and compositions are particularly useful in inhibiting mTor selectively for therapeutic applications.

Benzothiazole Kinase Inhibitors and Methods of Use

The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.

Preparation of 3-substituted-1-isopropyl-1 H-pyrazolo[3,4-d]pyrimidin-4- amines as RET kinase inhibitors

A series of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines have been designed, synthesized, and evaluated as RET protein kinase inhibitors. On the basis of docking results, a small library of pyrazolopyrimidine compounds with an extended hydrophobic side arm was synthesized. The most promising of the compounds (7a) displayed efficient inhibition in vitro and good selectivity when tested on a panel of kinases. Furthermore, 7a inhibited GDNF-induced RET phosphorylation of ERK1/2 in MCF-7 breast cancer cells at concentrations as low as 100 nM.

COMPOSITIONS AND METHODS FOR TREATING TOXOPLASMOSIS. CRYPTOSPORIDIOSIS AND OTHER APICOMPLEXAN PROTOZOAN RELATED DISEASES

Compositions and methods for the treatment of toxoplasmosis-, caused by the infectious eukaryotic parasite Toxoplasma gondii (T, gondii) and for the treatment of ciyptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C parvuai) and Cnγtosporidium homimus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpDPKS) using pyrazolopyriinidine and/or imidazo[l,5-a]pyraziαe inhibitors, of the formula.(I), wherein the variables X. Y, Z, L. R1. and R3 are defined herein.