216661-87-9

Usage

Uses

Used in Pharmaceutical Industry:
4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE is used as a reactant for the synthesis of various pharmaceutical products. Its unique molecular structure allows it to form stable complexes with other molecules, making it a valuable component in the development of new drugs and therapeutic agents.
4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE is used as a building block for the creation of novel drug candidates. Its ability to form stable complexes with other molecules enables the design of drugs with improved pharmacological properties, such as enhanced potency, selectivity, and bioavailability.
4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE is also used in the development of prodrugs. Prodrugs are biologically inactive compounds that are converted into active drugs within the body. The use of 4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE in prodrug design can improve the pharmacokinetic properties of the final drug, such as absorption, distribution, metabolism, and excretion.
Furthermore, 4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE can be used in the synthesis of drug conjugates. Drug conjugates are hybrid molecules that combine the therapeutic effects of two or more different drugs. The use of 4-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE in drug conjugate synthesis can lead to the development of multi-targeted therapies, which can be more effective in treating complex diseases.

InChI:InChI=1/C8H8N4/c9-8-7(5-11-12-8)6-1-3-10-4-2-6/h1-5H,(H3,9,11,12)

Upstream product

• 13121-99-8 pyridin-4-ylacetonitrile 
• 103851-89-4 3-(dimethylamino)-2-(4-pyridyl)prop-2-enenitrile 
• 69512-60-3 cyano-pyridin-4-yl-acetic acid ethyl ester 
• 10445-91-7 4-(Chloromethyl)pyridine 
• 493038-83-8 (Z)-3-(dimethylamino)-2-(4-pyridyl)prop-2-enenitrile 
• 92333-25-0 pyridin-4-ylacetonitrile hydrochloride 

Downstream Products

• 216661-58-4 3-(pyridin-4-yl)-6-(4-methoxyphenyl)-pyrazolo(1,5-A)pyrimidine 
• 866405-64-3 dorsomorphin 
• 1062368-41-5 6-{4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl}-3-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine 
• 515880-87-2 6-(4-hydroxyphenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine 
• 597544-21-3 4-(2-(4-(3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-6-yl)phenoxy)ethyl)morpholine 

Relevant academic research and scientific papers

HERBICIDAL COMPOUNDS

Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.

Inhibitor of heat shock factor 1, and preparation method and application of inhibitor

The invention provides an inhibitor of a heat shock factor 1 (HSF1) and an application of the inhibitor, particularly a compound as shown in a formula I or pharmaceutically-acceptable salt of the compound. The compound has excellent HSF1 restraining activity and tumor resisting effects. The invention further provides a medical composition containing the compound and an application of the medical composition in the respect of restraining HSF1.

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

INHIBITORS OF THE BMP SIGNALING PATHWAY

The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.

Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors

A structure-activity relationship study of dorsomorphin, a previously identified inhibitor of SMAD 1/5/8 phosphorylation by bone morphogenetic protein (BMP) type 1 receptors ALK2, 3, and 6, revealed that increased inhibitory activity could be accomplished by replacing the pendent 4-pyridine ring with 4-quinoline. The activity contributions of various nitrogen atoms in the core pyrazolo[1,5-a]pyrimidine ring were also examined by preparing and evaluating pyrrolo[1,2-a]pyrimidine and pyrazolo[1,5-a]pyridine derivatives. In addition, increased mouse liver microsome stability was achieved by replacing the ether substituent on the pendent phenyl ring with piperazine. Finally, an optimized compound 13 (LDN-193189 or DM-3189) demonstrated moderate pharmacokinetic characteristics (e.g., plasma t1/2 = 1.6 h) following intraperitoneal administration in mice. These studies provide useful molecular probes for examining the in vivo pharmacology of BMP signaling inhibition.

Microwave-assisted protocols for the expedited synthesis of pyrazolo[1,5-a] and [3,4-d]pyrimidines

General, high-yielding MAOS protocols for the expedited synthesis of functionalized pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyrimidines, as well as their pyrazole precursors, are described amenable to an iterative analogue library synthesis strategy for lead optimization.

Methods for inhibiting protein kinases

The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevent

PYRAZOLO AND IMIDAZO-PYRIMIDINE DERIVATIVES

The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula (I) wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined in the description and claims and to processes for their preparation, pharmaceutical compositions containing said derivatives and their use in the prevention and treatment of diseases.

Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: A new class of KDR kinase inhibitors

We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC50=19 nM), respectively. The synthesis and SAR of these compounds are described.