90221-50-4

Upstream product

• 54582-26-2 α-6-bromo-3-nitro-acetophenone oxime 
• 10403-47-1 2-bromo 5-nitroaniline 
• 108-24-7 acetic anhydride 
• 60-29-7 diethyl ether 
• 10026-13-8 phosphorus pentachloride 
• 75-36-5 acetyl chloride 
• 99-09-2 3-nitro-aniline 
• 64-19-7 acetic acid 

Downstream Products

• 21762-74-3 6-nitro-3,4-dihydro-3-oxo-2H(1,4)benzothiazine 
• 2941-66-4 2-methyl-5-nitrobenzothiazole 
• 32046-51-8 2-methyl-5-nitro-1,3-benzoxazole 
• 68867-15-2 N-(2-methyl-1,3-benzothiazol-5-yl)acetamide 
• 453562-71-5 1-(6-amino-3,3-dimethyl-2,3-dihydroindol-1-yl)ethanone 
• 453562-67-9 N-(2-bromo-5-nitrophenyl)-N-(2-methylprop-2-enyl)-acetamide 
• 38463-33-1 2-Methylthiazolochinolin 
• 13382-43-9 2-methyl-5-aminobenzothiazole 
• 116529-42-1 2-bromo-4,5-dinitro-aniline 
• 453562-68-0 1-(3,3-dimethyl-6-nitro-2,3-dihydro-indol-1-yl)-ethanone 

Relevant academic research and scientific papers

Synthesis of dibenzothiophene, dibenzofuran and carbazole donor-acceptor chromophores

We present efficient synthetic protocols for functionalizing dibenzothiophene, dibenzofuran, and carbazole with hydroxy and nitro or cyano groups. The synthesis of these donor-acceptor chromophores is based on a key Suzuki-Miyaura coupling using an approp

Iridium-catalyzed intramolecular C–N and C–O/S cross-coupling reactions: Preparation of benzoazole derivatives

The irdium-catalyzed intramolecular arylcarbon-hetero cross-coupling reactions with o-haloarylamides or o-haloarylamidine have been effectively achieved using KOAc and just 1 mol% catalyst. The [Ir(cod)Cl]2 was proved to be more potential for smoothly assembling functional structures benzimidazoles, benzoxazoles and benzothiazoles, which was superior to Cu- and Pd-catalyzed systems. Simultaneously, a concise and efficient synthesis of tafamidis was developed in 5-g scale.

PRODRUGS FOR NITROREDUCTASE BASED CANCER THERAPY- 2: Novel amide/Ntr combinations targeting PC3 cancer cells

The use of nitroreductases (NTR) that catalyze the reduction of nitro compounds by using NAD(P)H in GDEPT (Gene-directed enzyme prodrug therapy) studies which minimize toxicity at healthy cells and increases concentration of drugs at cancer cells is remarkable. Discovery of new prodrug/NTR combinations is necessary to be an alternative to known prodrug candidates such as CB1954, SN23862, PR-104A. For this aim, nitro containing aromatic amides (A1-A23) were designed, synthesized, performed in silico ADMET and molecular docking techniques in this study. Prodrug candidates were studied on reduction potentials with Ssap-NtrB by HPLC system. Also, cyototoxic properties and prodrug ability of these amides were investigated using different cancer cell lines such as Hep3B and PC3. As a result of theoretical and biological studies, combinations of A5, A6 and A20 with Ssap-NtrB can be suggested as potential prodrugs/enzyme combinations at NTR based cancer therapy compared with CB1954/NfsB.

Synthesis and Photophysical, Electrochemical and Theoretical Study of Thiazole-Annelated Phthalocyanines

Phthalocyanines with annelated thiazole rings were synthesised by cyclotetramerisation of benzothiazoledicarbonitriles. Three types of these dicarbonitriles with ortho-configuration were prepared from disubstituted anilines and their cyclisation led to al

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.

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.

Highly effective Pd-catalyzed ortho olefination of acetanilides: Broad substrate scope and high tolerability

Bring it on! An effective Pd-catalyzed ortho olefination of various acetanilides has been developed. This transformation has a broad substrate scope and wide functional-group tolerability, regardless of the electronic and steric properties of acetanilide substrates, providing a straightforward access to highly functionalized arenes.

Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors

Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.

COMPOUNDS 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.

SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE

The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.