1295583-21-9

Upstream product

• 67-56-1 methanol 
• 689251-97-6 (E)-3-(1-methyl-1H-pyrazol-4-yl)acrylic acid 
• 5927-18-4 trimethyl phosphonoacetate 
• 35344-95-7 1H-pyrazole-4-carbaldehyde 
• 25016-11-9 1-methylpyrazole-4-carbaldehyde 

Downstream Products

• 224776-32-3 methyl 3-(1-methyl-1H-pyrazol-4-yl)propanoate 
• 1380427-95-1 2-((3-methoxy-4-(3-(trifluoromethyl)phenoxy)benzyl)thio)-5-((1-methyl-1H-pyrazol-4-yl)methyl)pyrimidin-4(1H)-one 
• 1380427-97-3 C₂HF₃O₂*C₂₅H₂₃F₃N₄O₃S 
• 1380428-00-1 5-[2-({5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4-oxo-1,4-dihydro-2-pyrimidinyl}thio)ethyl]-2-{[3-(trifluoromethyl)phenyl]oxy}benzonitrile 
• 1380428-06-7 2-((4-(4-chloro-3-(trifluoromethyl)phenoxy)phenethyl)thio)-5-((1-methyl-1H-pyrazol-4-yl)methyl)pyrimidin-4(1H)-one 
• 1380428-07-8 2-{[2-(4-{[4-chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)ethyl]thio}-1-methyl-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380428-20-5 5-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-{[2-(4-{[4-(trifluoromethyl)phenyl]oxy}phenyl)ethyl]oxy}-4(1H)-pyrimidinone 
• 1380426-85-6 2-{[2-(4-{[4-chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)ethyl]amino}-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380428-36-3 5-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-{[2-(4-{[6-(trifluoromethyl)-3-pyridinyl]oxy}phenyl)ethyl]oxy}-4(1H)-pyrimidinone 
• 1380428-49-8 2-[(2-{4-[(3-chloro-4-methylphenyl)oxy]phenyl}ethyl)oxy]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380428-52-3 2-[(2-{4-[(4-chloro-3-methylphenyl)oxy]phenyl}ethyl)oxy]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380428-56-7 2-[(2-{4-[(3-fluoro-4-methylphenyl)oxy]phenyl}ethyl)oxy]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380426-88-9 2-{[2-(4-{[4-chloro-3-(trifluoromethyl)phenyl]oxy}phenyl)ethyl]amino}-1-methyl-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4(1H)-pyrimidinone 
• 1380428-59-0 5-[(1-methyl-1H-pyrazol-4-yl)methyl]-2-[(2-{4-[(6-methyl-2-pyridinyl)oxy]phenyl}ethyl)oxy]-4(1H)-pyrimidinone 

Relevant academic research and scientific papers

Synthesis of 1-hetaryl-2,2-difluorocyclopropane-derived building blocks: The case of pyrazoles

An approach to 1-hetaryl-2,2-difluorocyclopropane building blocks compatible with the current criteria of lead-oriented synthesis was developed and implemented for the case of 3-, 4- and 5-subsituted pyrazole derivatives. The method implied 6–9 synthetic steps, including difluorocyclopropanation with the TMSCF3–NaI system as the key transformation, and provided the title compounds on up to gram scale. The scope of the procedures towards substitution in the pyrazole ring and typical functional groups (i.e. COOH, NH2, CH2NH2, CH2OH) was established. The results obtained allowed formulation of preliminary guidelines for the synthetic feasibility of various functionalized 1-hetaryl-2,2-difluorocyclopropanes. 2018 Elsevier Ltd. All rights reserved.

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.

Histone Deacetylase Inhibitors

This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP - PLA2

The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema (I).

HISTONE DEACETYLASE INHIBITORS

This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).