91912-53-7

Basic information

• Product Name: 5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE
• Synonyms: 5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE;1H-Pyrazol-3-amine, 5-(4-pyridinyl)-;5-(4-pyridinyl)-1H-pyrazol-3-amine(SALTDATA: 1.3HCl);5-(pyridin-4-yl)-1H-pyrazol-3-aMine;3-Amino-5-(pyridin-4-yl)-1H-pyrazole
• CAS NO: 91912-53-7
• Molecular Formula: C₈H₈N₄
• Molecular Weight: 160.18
• Mol File: 91912-53-7.mol

Chemical Properties

• Melting Point: 192-193 °C
• Boiling Point: 465.369 °C at 760 mmHg
• Flash Point: 266.32 °C
• Appearance: /
• Density: 1.315 g/cm³
• Vapor Pressure: 0mmHg at 25°C
• Refractive Index: 1.674
• Storage Temp.: 2-8°C
• PKA: 13.12±0.10(Predicted)
• CAS DataBase Reference: 5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE(CAS DataBase Reference)
• NIST Chemistry Reference: 5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE(91912-53-7)
• EPA Substance Registry System: 5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE(91912-53-7)

Safety Data

• Hazard Codes: Xn
• Statements: 22
• Hazardous Substances Data: 91912-53-7(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
5-PYRIDIN-4-YL-2H-PYRAZOL-3-YLAMINE is used as a reagent for the preparation of small molecule inhibitors, specifically targeting the IL-12/23 pathway. This application is crucial in the development of treatments for autoimmune and autoinflammatory diseases, as modulating the IL-12/23 pathway can help regulate immune responses and alleviate disease symptoms.

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

Upstream product

• 23821-37-6 3-oxo-3-(pyridin-4-yl)propanenitrile 
• 1570-45-2 isonicotinic acid ethylester 
• 4114-31-2 ethylhydrazine carboxylate 
• 92163-27-4 3-(6-methoxy-naphthalen-2-yl)-3-oxo-propionitrile 
• 2459-09-8 4-pyridinecarboxylic acid, methyl ester 
• 75-05-8 acetonitrile 
• 569656-00-4 N-(5-pyridin-4-yl-2H-pyrazol-3-yl)acetamide 

Downstream Products

• 950739-42-1 7-(3-nitrophenyl)-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidine 
• 1240521-55-4 tert-butyl (S)-(1-oxo-3-phenyl-1-((3-(pyridin-4-yl)-1H-pyrazol-5-yl)amino)propan-2-yl)carbamate 
• 1232221-74-7 N-(3-methylbenzylidene)-N'-(7-morpholin-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine 
• 1232221-92-9 N-(4-methoxy-3-methyl-benzylidene)-N'-(7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232222-68-2 N-(3-fluoro-benzylidene)-N'-(7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232222-82-0 N-(3-vinyl-benzylidene)-N'-(7-morpholin-4-yl-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine 
• 1459140-16-9 1-(3,4-dichlorophenyl)-3-(3-(pyridin-4-yl)-1H-pyrazol-5-yl)urea 
• 1186334-57-5 7-(4-bromophenyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine 
• 1186421-98-6 N,N-dimethyl-3-(2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)benzenesulfonamide 
• 950738-70-2 5-methyl-7-(3-nitro-phenyl)-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine 

Relevant articles and documents

SUBSTITUTED PYRIDINE DERIVATIVES AS SARM1 INHIBITORS

This disclosure is drawn to substituted pyridine compounds and compositions, and associated methods, useful for inhibition of SARM1 activity and/or for treating or preventing a neurological diseases.

SUBSTITUTED PYRAZOLO-PYRIMIDINES AND USES THEREOF

The present disclosure provides compounds that are inhibitors of PIKfyve kinases useful for the treatment of neurological diseases treatable by inhibition of PIKfyve. Also provided are pharmaceutical compositions containing such compounds, and methods of

Polysubstituted heterocyclic derivative, preparation method thereof and application of polysubstituted heterocyclic derivative in medicine

The invention provides a polysubstituted heterocyclic derivative, a preparation method thereof and application of the polysubstituted heterocyclic derivative in medicine, and belongs to the technical field of medicinal chemistry. The polysubstituted heterocyclic derivative is a compound shown in a general formula I or II, a pharmaceutically acceptable salt or a solvate of the compound, and the compound can inhibit mRNA demethylase on the protease level and is used for treating diseases related to mRNA demethylase functions.

5- OR 7-AZAINDAZOLES AS BETA-LACTAMASE INHIBITORS

The present invention relates to β-lactamase inhibitors having the following general formula (I): wherein R1-R4 and X1-X2 are defined in the specification, pharmaceutical composition thereof, and use thereof for the treatment of a bacterial infection, alone or in combination with β-lactam antibiotics and/or other antibiotics and/or other β-lactamase inhibitors.

NOVEL PYRAZOLO-PYRROLO-PYRIMIDINE-DIONE DERIVATIVES AS P2X3 INHIBITORS

The present invention covers substituted Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.

SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND 2,3-DIHYDRO-1H-IMIDAZO[1,2-b]PYRAZOLE DERIVATIVES AS ROS1 INHIBITORS

The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives of formula (I) and also compounds of formula (I') wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201

Interleukin-12 (IL-12) and IL-23 are proinflammatory cytokines and therapeutic targets for inflammatory and autoimmune diseases, including inflammatory bowel diseases, psoriasis, rheumatoid arthritis, and multiple sclerosis. We describe the discovery of APY0201, a unique small molecular IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an experimental model of colitis. Through a chemical proteomics approach using a highly sensitive direct nanoflow LC-MS/MS system and bait compounds equipped with the FLAG epitope associated regulator of PIKfyve (ArPIKfyve) was detected. Further study identified its associated protein phosphoinositide kinase, FYVE finger-containing (PIKfyve), as the target protein of APY0201, which was characterized as a potent, highly selective, ATP-competitive PIKfyve inhibitor that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2. These results elucidate the function of PIKfyve kinase in the IL-12/23 production pathway and in IL-12/23-driven inflammatory disease pathologies to provide a compelling rationale for targeting PIKfyve kinase in inflammatory and autoimmune diseases.

TETRAHYDROPYRAZOLOPYRIMIDINE COMPOUNDS

Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis

Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H- pyrazol-3-yl] amide (SEN15924, WAY-361789)

Alpha-7 nicotinic acetylcholine receptors (α7 nAChR) are implicated in the modulation of many cognitive functions such as attention, working memory, and episodic memory. For this reason, α7 nAChR agonists represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer's disease (AD) and schizophrenia. A medicinal chemistry effort, around our previously reported chemical series, permitted the discovery of a novel class of α7 nAChR agonists with improved selectivity, in particular against the α3 receptor subtype and better ADME profile. The exploration of this series led to the identification of 5-(4-acetyl[1,4] diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (25, SEN15924, WAY-361789), a novel, full agonist of the α7 nAChR that was evaluated in vitro and in vivo. Compound 25 proved to be potent and selective, and it demonstrated a fair pharmacokinetic profile accompanied by efficacy in rodent behavioral cognition models (novel object recognition and auditory sensory gating).

PYRAZOLO-PYRIMIDINE COMPOUNDS

The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.