18755-53-8

Upstream product

• 50-00-0 formaldehyd 
• 1817-47-6 4-nitrocumene 
• 18755-52-7 (2-acetoxy-1,1-dimethylethyl)benzene 
• 59115-08-1 methyl 2-methyl-2-(4-nitrophenyl)propanoate 
• 83397-45-9 ethyl 2-methyl-2-(4-nitrophenyl)propanoate 
• 74002-19-0 2-methyl-2-(4-nitrophenyl)propanamide 
• 42206-47-3 2-methyl-2-(4-nitro-phenyl)-propionic acid 
• 71825-51-9 4-(2-cyanoprop-2-yl)-1-nitrobenzene 
• 408306-81-0 ethyl 1,4-dimethylpiperidine-4-carboxylate 

Downstream Products

• 74401-33-5 2-methyl-2-(4-nitrophenyl)propyl tosylate 
• 18755-55-0 2-(p-nitrophenyl)-2-methylpropyl p-bromobenzenesulfonate 
• 954424-98-7 tert-butyl-dimethyl-[2-methyl-2-(4-nitro-phenyl)-propoxy]-silane 
• 453562-77-1 2-methyl-2-(4-nitrophenyl)propionaldehyde 
• 1021439-61-1 1-(2-methoxy-1,1-dimethyl-ethyl)-4-nitro-benzene 
• 91133-58-3 3-methyl-3-(4-nitrophenyl)-butan-1-one 
• 1067193-11-6 {3-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-3-methyl-butyl}-carbamic acid tert-butyl ester 
• 1067191-56-3 N-(4-(4-acetamido-2-methylbutan-2-yl)phenyl)-3,4-dimethoxybenzamide 
• 1067193-12-7 N-[4-(3-amino-1,1-dimethyl-propyl)-phenyl]-3,4-dimethoxy-benzamide 
• 1067192-93-1 N-[3-methyl-3-(4-nitro-phenyl)-butyl]-acetamide 
• 1067192-96-4 N-(3-(4-aminophenyl)-3-methylbutyl)acetamide 
• 1067192-92-0 3-methyl-3-(4-nitro-phenyl)-butylamine 

Relevant academic research and scientific papers

Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity

Pyruvate dehydrogenase kinases (PDKs) are promising therapeutic targets that have received increasing attentions in cancer metabolism. In this paper, we report the synthesis and biological evaluation of a series of novel dichloroacetophenones as potent PDKs inhibitors. Structure-activity relationship analysis enabled us to identify a potent compound 6u, which inhibited PDKs with an EC50 value of 0.09 μM, and reduced various cancer cells proliferation with IC50 values ranging from 1.1 to 3.8 μM, while show weak effect against non-cancerous L02 cell (IC50 > 10 μM). In the A375 xenograft model, 6u displayed an obvious antitumor activity at a dose of 5 mg/kg, but with no negative effect to the mice weight. Molecular docking suggested that 6u formed direct hydrogen bond interactions with Ser75 and Gln61 in PDK1, and meanwhile the aniline skeleton in 6u was sandwiched by the conserved hydrophobic residues Phe78 and Phe65, which contribute to the biochemical activity improvement. Moreover, 6u induced A375 cell apoptosis and cell arrest in G1 phase, and inhibited cancer cell migration. In addition, 6u altered glucose metabolic pathway in A375 cell by decreasing lactate formation and increasing ROS production and OCR consumption, which could serve as a potential modulator to reprogram the glycolysis pathway in cancer cell.

QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS

Compounds of formula (Ι') that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors

Structure-activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase selectivity, particularly over KIT. Potent compound 17r (FMS IC50 0.7 nM, FMS cell IC50 6.1 nM) was discovered that had good PK properties and a greater than fivefold improvement in selectivity for FMS over KIT kinase in a cellular assay relative to the previously reported clinical candidate 4. This improved selectivity was manifested in vivo by no observed decrease in circulating reticulocytes, a measure of bone safety, at the highest studied dose. Compound 17r was highly active in a mouse pharmacodynamic model and demonstrated disease-modifying effects in a dose-dependent manner in a strep cell wall-induced arthritis model of rheumatoid arthritis in rats.

IMIDAZOPYRAZINE SYK INHIBITORS

Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suf-fering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or dis-order are provided.

Anti-Viral Compounds

Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

INDOLE ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS

The present invention provides indole compounds of Formula (I) or (II) or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X3, X4, R6, and R15 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

NOVEL BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE

The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1 nare defined as in formula I; invention compounds are modulators of follicle-stimulating hormone - ("FSH") which are useful for male and female contraception as well as other disorders modulated by FSH receptor.

INHIBITORS OF C-FMS KINASE

The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.