401647-24-3

Usage

Uses

Used in Pharmaceutical Industry:
1-BENZYL-1H-PYRAZOLE-4-CARBOXYLIC ACID is used as a building block in organic synthesis for the development of new drugs and pharmaceuticals. Its versatile chemical structure allows for the creation of a variety of compounds with potential therapeutic applications.
Used in Anti-inflammatory Applications:
1-BENZYL-1H-PYRAZOLE-4-CARBOXYLIC ACID is used as a potential anti-inflammatory agent, leveraging its pharmacological properties to modulate inflammatory responses and alleviate symptoms associated with inflammation.
Used in Analgesic Applications:
1-BENZYL-1H-PYRAZOLE-4-CARBOXYLIC ACID is used as a potential analgesic agent, providing pain relief through its interaction with pain signaling pathways and contributing to the management of acute and chronic pain conditions.
Used in Drug Development:
1-BENZYL-1H-PYRAZOLE-4-CARBOXYLIC ACID is used in drug development for its potential to contribute to the creation of novel therapeutic agents. Its unique structure and properties make it a valuable component in the design and synthesis of new pharmaceutical compounds with diverse applications in medicine.

InChI:InChI=1/C11H10N2O2/c14-11(15)10-6-12-13(8-10)7-9-4-2-1-3-5-9/h1-6,8H,7H2,(H,14,15)

Upstream product

• 121358-86-9 1-benzyl-1H-pyrazole-4-carbonitrile 
• 150559-94-7 ethyl 1‐benzyl‐1H‐pyrazole‐4‐carboxylate 
• 10199-67-4 1-benzylpyrazole 
• 50877-41-3 1-benzyl-4-bromo-1H-pyrazole 
• 63874-95-3 1-benzyl-1H-pyrazole-4carboxaldehyde 
• 861135-90-2 methyl 1-benzylpyrazole-4-carboxylate 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 

Downstream Products

• 37718-11-9 1H-pyrazole-4-carboxylic acid 
• 1073486-51-7 C₁₈H₂₀N₆O₃ 
• 1073495-05-2 C₂₀H₂₄N₆O₃ 
• 1056638-89-1 N-[6-amino-3-(cyclopropylmethyl)-1-methyl-2,4-dioxo(1,3-dihydropyrimidin-5-yl)][1-(benzylpyrazol-4-yl)]carboxamide 
• 1073496-62-4 C₂₀H₂₄N₆O₃ 
• 1073493-40-9 C₁₉H₂₂N₆O₃ 
• 1056639-19-0 C₂₀H₂₄N₆O₃ 
• 531506-36-2 8-(1-benzylpyrazol-4-yl)-1,3-dipropyl-1,3,7-trihydropurine-2,6-dione 
• 1056639-11-2 1-benzyl-1H-pyrazole-4-carboxylic acid (6-amino-2,4-dioxo-3-propyl-1,2,3,4-tetrahydro-pyrimidin-5-yl)-amide 

Relevant academic research and scientific papers

CRYSTALLINE FORMS OF PLASMA KALLIKREIN INHIBITORS

Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.

PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS

A process for preparing and purifying a compound of Formula I is provided: or a salt thereof, wherein the subscript m is an integer of from 0 to 3;each Ra is independently selected from the group consisting of (C3-C8)cyclo

Design, synthesis, biological evaluation and in silico studies of pyrazole‐based nh2‐acyl oseltamivir analogues as potent neuraminidase inhibitors

Oseltamivir represents one of the most successful neuraminidase (NA) inhibitors in the current anti‐influenza therapy. The 150‐cavity of NA was identified as an additional binding pocket, and novel NA inhibitors have been designed to occupy the 150‐cavity

Development of inhibitors against mycobacterium abscessus tRNA (m1G37) Methyltransferase (TrmD) Using Fragment-Based Approaches

Mycobacterium abscessus (Mab) is a rapidly growing species of multidrug-resistant nontuberculous mycobacteria that has emerged as a growing threat to individuals with cystic fibrosis and other pre-existing chronic lung diseases. Mab pulmonary infections are difficult, or sometimes impossible, to treat and result in accelerated lung function decline and premature death. There is therefore an urgent need to develop novel antibiotics with improved efficacy. tRNA (m1G37) methyltransferase (TrmD) is a promising target for novel antibiotics. It is essential in Mab and other mycobacteria, improving reading frame maintenance on the ribosome to prevent frameshift errors. In this work, a fragment-based approach was employed with the merging of two fragments bound to the active site, followed by structure-guided elaboration to design potent nanomolar inhibitors against Mab TrmD. Several of these compounds exhibit promising activity against mycobacterial species, including Mycobacterium tuberculosis and Mycobacterium leprae in addition to Mab, supporting the use of TrmD as a target for the development of antimycobacterial compounds.

COMPOUNDS AND USES THEREOF

The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

Oxidation of imidazole- and pyrazole-derived aldehydes by plant aldehyde dehydrogenases from the family 2 and 10

Plant cytosolic aldehyde dehydrogenases from family 2 (ALDH2s, EC 1.2.1.3) are non-specific enzymes and participate for example in the metabolism of acetaldehyde or biosynthesis of phenylpropanoids. Plant aminoaldehyde dehydrogenases (AMADHs, ALDH10 family, EC 1.2.1.19) are broadly specific and play an important role in polyamine degradation or production of osmoprotectants. We have tested imidazole and pyrazole carbaldehydes and their alkyl-, allyl-, benzyl-, phenyl-, pyrimidinyl- or thienyl-derivatives as possible substrates of plant ALDH2 and ALDH10 enzymes. Imidazole represents a building block of histidine, histamine as well as certain alkaloids. It also appears in synthetic pharmaceuticals such as imidazole antifungals. Biological compounds containing pyrazole are rare (e.g. pyrazole-1-alanine and pyrazofurin antibiotics) but the ring is often found as a constituent of many synthetic drugs and pesticides. The aim was to evaluate whether aldehyde compounds based on azole heterocycles are oxidized by the enzymes, which would further support their expected role as detoxifying aldehyde scavengers. The analyzed imidazole and pyrazole carbaldehydes were only slowly converted by ALDH10s but well oxidized by cytosolic maize ALDH2 isoforms (particularly by ALDH2C1). In the latter case, the respective Km values were in the range of 10–2000 μmol l?1; the kcat values appeared mostly between 0.1 and 1.0 s?1. The carbaldehyde group at the position 4 of imidazole was oxidized faster than that at the position 2. Such a difference was not observed for pyrazole carbaldehydes. Aldehydes with an aromatic substituent on their heterocyclic ring were oxidized faster than those with an aliphatic substituent. The most efficient of the tested substrates were comparable to benzaldehyde and p-anisaldehyde known as the best aromatic aldehyde substrates of plant cytosolic ALDH2s in vitro.

FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.

FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

GLUCOCORTICOID RECEPTOR ANTAGONISTS

The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucoc