425379-93-7

Upstream product

• 369-34-6 3,4-difluoronitrobenzene 
• 226220-35-5 3-fluoro-1-nitro-4-(1H-pyrazol-1-yl)benzene 

Downstream Products

• 797783-98-3 4-azidomethyl-1-(3-fluoro-4-pyrazol-1-yl-phenyl)-1H-[1,2,3]triazole 
• 797783-66-5 [1-(3-fluoro-4-pyrazol-1-ylphenyl)-1H-[1,2,3]triazol-5-yl]-methanol 
• 797783-99-4 C-[1-(3-fluoro-4-pyrazol-1-yl-phenyl)-1H-[1,2,3]triazol-4-yl]methylamine 
• 1542257-89-5 3-(3-fluoro-4-(1H-pyrazol-1-yl)phenyl)-2,6-dimethylpyrimidine-4(3H)-one 
• 226220-37-7 Methanesulfonic acid (R)-3-(3-fluoro-4-pyrazol-1-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl ester 
• 181997-05-7 (R)-5-Azidomethyl-3-(3-fluoro-4-pyrazol-1-yl-phenyl)-oxazolidin-2-one 
• 343880-91-1 (S)-5-aminomethyl-3-[3-fluoro-4-(1-pyrazolyl)phenyl]oxazolidine-2-one 
• 226220-36-6 [3-[3-fluoro-4-(1H-pyrazol-1-yl)phenyl]-2-oxo-5-oxazolidinyl]methanol 
• 797783-64-3 1-(4-azido-2-fluorophenyl)-1H-pyrazole 
• 181997-07-9 3-fluoro-1-(phenylmethoxycarbonylamino)-4-(1H-pyrazol-1-yl)benzene 

Relevant academic research and scientific papers

NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS

The invention relates to the field of medicine, discloses new nitrogen heterocyclic derivatives, preparation method thereof and as medicament in particular as the treatment and prevention of treating tissue fibrosis of the medicament. The invention also discloses a pharmaceutically acceptable compound of the present invention comprise a pharmaceutical composition and methods for using the composition for the treatment of the human or animal tissue fibrosis of diseases, in particular for treating the human or animal renal interstitial fibrosis, glomerular sclerosis, hepatic fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, skin fibrosis, after the operation of adhering, benign prostate hypertrophy, bone-myocardial, scleroderma, multiple sclerosis, pancreas fibrosis, liver cirrhosis, myosarcoma, neurofibromatosis, interstitial pulmonary fibrosis, diabetic nephropathy, Alzheimer's disease or vascular fibrosis disease in use. (by machine translation)

Nitrogenous Heterocyclic Derivatives And Their Application In Drugs

The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.

NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS

The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.

Design and synthesis of novel 5-acetylthiomethyl oxazolidinone analogs

The oxazolidinone class of antimicrobial agents represents a promising advance in the fight against resistant Gram-positive bacterial infections. To improve antibacterial activity and expand the spectrum of activity including Gram-negative bacteria, a series of novel 5-acetylthiomethyl oxazolidinone analogs were designed and synthesized based on the structure-activity relationship studies. The structures of the target compounds and main intermediates were confirmed by 1H NMR, 13C NMR, infrared (IR), mass spectra (MS), and elemental analysis.

PIPERAZINE COMPOUNDS FOR THE INHIBITION OF HAEMATOPOIETIC PROSTAGLANDIN D SYNTHASE

The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnoea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.

ANTIINFECTIVE 1,2,3-TRIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The present invention relates to novel triazole compounds of formula (I), thie pharmaceutically acceptable salts and their pharmaceutical compositions, where all symbols have meaning as defined in the description, for use in the treatment of bacterial inf

Substituent effects on the antibacterial activity of nitrogen-carbon- linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis

A series of new nitrogen-carbon-linked (azolylphenyl)oxazolidinone antibacterial agents has been prepared in an effort to expand the spectrum of activity of this class of antibiotics to include Gram-negative organisms. Pyrrole, pyrazole, imidazole, triazole, and tetrazole moieties have been used to replace the morpholine ring of linezolid (2). These changes resulted in the preparation of compounds with good activity against the fastidious Gram- negative organisms Haemophilus influenzae and Moraxella catarrhalis. The unsubstituted pyrrolyl analogue 3 and the 1H-1,2,3-triazolyl analogue 6 have MICs against H. influenzae = 4 μg/mL and M. catarrhalis = 2 μg/mL. Various substituents were also placed on the azole moieties in order to study their effects on antibacterial activity in vitro and in vivo. Interesting differences in activity were observed for many analogues that cannot be rationalized solely on the basis of sterics and position/number of nitrogen atoms in the azole ring. Differences in activity rely strongly on subtle changes in the electronic character of the overall azole systems. Aldehyde, aldoxime, and cyano azoles generally led to dramatic improvements in activity against both Gram-positive and Gram-negative bacteria relative to unsubstituted counterparts. However, amide, ester, amino, hydroxy, alkoxy, and alkyl substituents resulted in no improvement or a loss in antibacterial activity. The placement of a cyano moiety on the azole often generates analogues with interesting antibacterial activity in vitro and in vivo. In particular, the 3-cyanopyrrole, 4-cyanopyrazole, and 4-cyano-1H-1,2,3- triazole congeners 28, 50, and 90 had S. aureus MICs ≤ 0.5-1 μg/mL and H. influenzae and M. catarrhalis MICs = 2-4 μg/mL. These analogues are also very effective versus S. aureus and S. pneumoniae in mouse models of human infection with ED50s in the range of 1.2-1.9 mg/kg versus 2.8-4.0 mg/kg for the eperezolid (1) control.