872882-98-9

Upstream product

• 14062-25-0 Ethyl 4-bromophenylacetate 
• 5798-75-4 Ethyl 4-bromobenzoate 
• 1609-47-8 diethyl dicarbonate 
• 74-88-4 methyl iodide 
• 93139-85-6 2-(4-bromophenyl)malonic acid diethyl ester 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 609-08-5 Diethyl methylmalonate 

Downstream Products

• 53578-00-0 2-(4-Bromophenyl)-2,2-dimethoxyethane 
• 66810-01-3 2-(4-bromophenyl)-2-methylpropane-1,3-diol 
• 872882-97-8 3-(4-bromophenyl)-3-methyloxetane 
• 1431616-23-7 6-(4-(3-methyloxetan-3-yl)phenyl)nicotinonitrile 
• 1431616-42-0 (4-(3-methyloxetan-3-yl)phenyl)boronic acid 

Relevant academic research and scientific papers

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

Metabolically stable tert-butyl replacement

Susceptibility to metabolism is a common issue with the tert-butyl group on compounds of medicinal interest. We demonstrate an approach of removing all the fully sp3 C-Hs from a tert-butyl group: replacing some C-Hs with C-Fs and increasing the s-character of the remaining C-Hs. This approach gave a trifluoromethylcyclopropyl group, which increased metabolic stability. Trifluoromethylcyclopropyl-containing analogues had consistently higher metabolic stability in vitro and in vivo compared to their tert-butyl-containing counterparts.

COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES

The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

Modulators of ATP-binding cassette transporters

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Pyridyl piperazines for the treatment of CNS disorders

This invention is directed to compounds of Formula I and to pharmaceutical compositions comprising the compound of Formula I. where the dashed line represents an optional double bond; and where n is 1 or 2, and Ar1, Ar2, . . . and Z

PYRIDIL-LACTAMS AND THEIR USE 5 -HTl RECEPTORS LIGAN

The present invention relates to novel pyridyl-lactams, compounds of the formula (I), wherein R1 is a group of the formula G1, G2, G3 or G4 depicted below, and R3, Y, R6, R7, R8, R13, a, n and m are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions, their preparation and intermediates therefrom, and their use in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1B antagonist is indicated.

Heterocyclic compounds

The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.