530144-72-0

Usage

Uses

Used in Pharmaceutical Industry:
1H-Pyrazole-1-carboxylic acid, 4-(bromomethyl)-, 1,1-dimethylethyl ester is used as an intermediate in the synthesis of various pharmaceutical compounds. Its unique chemical structure allows it to be a versatile building block for the development of new drugs with potential therapeutic applications.
Used in Chemical Research:
In the field of chemical research, 1H-Pyrazole-1-carboxylic acid, 4-(bromomethyl)-, 1,1-dimethylethyl ester serves as a valuable compound for studying the properties and reactivity of pyrazole carboxylic acid esters. It can be used to explore new reaction pathways and develop innovative synthetic methods.
Used in the Preparation of Benzophenone Derivatives:
1H-Pyrazole-1-carboxylic acid, 4-(bromomethyl)-, 1,1-dimethylethyl ester is used in the preparation of benzophenone derivatives that act as AP-1 inhibitors. These derivatives have potential applications in the treatment of arthritis, as they can help regulate the expression of genes involved in the inflammatory response and reduce the associated pain and swelling.

Upstream product

• 121669-69-0 tert-butyl 4-methyl-1H-pyrazole-1-carboxylate 
• 199003-22-0 tert-butyl 4-(hydroxymethyl)-1H-pyrazole-1-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 128-08-5 N-Bromosuccinimide 

Relevant academic research and scientific papers

Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO)

Myeloperoxidase (MPO), a critical enzyme in antimicrobial host-defense, has been implicated in chronic inflammatory diseases such as coronary artery disease. The design and evaluation of MPO inhibitors for the treatment of cardiovascular disease are reported herein. Starting with the MPO and triazolopyridine 3 crystal structure, novel inhibitors were designed incorporating a substituted pyrazole, which allowed for substituents to interact with hydrophobic and hydrophilic patches in the active site. SAR exploration of the substituted pyrazoles led to piperidine 17, which inhibited HOCl production from activated neutrophils with an IC50 value of 2.4 μM and had selectivity against thyroid peroxidase (TPO). Optimization of alkylation chemistry on the pyrazole nitrogen facilitated the preparation of many analogs, including macrocycles designed to bridge two hydrophobic regions of the active site. Multiple macrocyclization strategies were pursued to prepare analogs that optimally bound to the active site, leading to potent macrocyclic MPO inhibitors with TPO selectivity, such as compound 30.

TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE

The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE

The present invention provides compounds of Formula (I). wherein A and Z are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and may be useful for for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS

Disclosed in the present application is a compound of formula (I) as defined herein as well as a pharmaceutical composition comprising said compound. Further disclosed in the present application is the use of such pharmaceutical compositions for treating diseases, namely inter alia for use in the treatment of cancer, metabolic, inflammatory, autoimmune and viral diseases. The compounds disclosed herein are inhibitors of MNK1 and/or MNK2 kinases.

PROBES FOR IMAGING HUNTINGTIN PROTEIN

Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.

NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME

The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).

NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVE AND A PRODUCTION METHOD FOR SAME

The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).

CARBACEPHEM BETA-LACTAM ANTIBIOTICS

Carbacephem β-lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, X, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.

HETEROCYCLIC ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS

Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such an

SUBSTITUTED PYRIDINONES

Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.