187396-78-7

Upstream product

• 79-37-8 oxalyl dichloride 
• 3438-16-2 5-chloro-2-methoxybenzoic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 30289-28-2 N-methoxy-N-methylcarbamoyl chloride 
• 29568-33-0 2-methoxy-5-chlorobenzoyl chloride 

Downstream Products

• 329945-56-4 (3-bromo-5-methylphenyl)(5-chloro-2-methoxyphenyl)methanone 
• 329946-54-5 [3-bromo-5-(trifluoromethyl)phenyl][5-chloro-2-(methyloxy)phenyl]methanone 
• 329944-59-4 (3-bromo-5-chlorophenyl)(5-chloro-2-methoxyphenyl)methanone 
• 329944-74-3 [5-chloro-2-(methyloxy)phenyl](3-chloro-5-methylphenyl)methanone 
• 329946-44-3 [4-chloro-2-(3-chloro-5-cyano-benzoyl)-phenoxy]-acetic acid ethyl ester 
• 329945-72-4 [4-chloro-2-(3-cyano-5-methyl-benzoyl)-phenoxy]-acetic acid ethyl ester 
• 329946-46-5 ({4-chloro-2-[(3-chloro-5-cyanophenyl)carbonyl]phenyl}oxy)acetic acid 
• 874889-42-6 [4-chloro-2-(3-chloro-5-cyanobenzoyl)phenoxy]acetyl chloride 
• 329945-74-6 [4-chloro-2-(3-cyano-5-methyl-benzoyl)-phenoxy]-acetic acid 
• 329946-56-7 3-{[5-chloro-2-(methyloxy)phenyl]carbonyl}-5-(trifluoromethyl)benzonitrile 

Relevant academic research and scientific papers

Benzoic acid derivatives as non nucleoside reverse transcriptase inhibitors

Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are

Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor

Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clinically relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clinical resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clinical resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in intravenous pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clinical studies.

Alkynyl compounds as non nucleoside reverse transcriptase inhibitors

Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table. R1R2R4Rs

1,3,8-TRIAZA- AND 3,8-DIAZA-1-OXASPIRO[4,5] DECANE DERIVATIVES

Heterocyclic compounds of Formula I: STR1 in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R 4); Y and Z are independently C(O), C(S) or CH 2 (provided that Y and Z are not both CH 2); R 1, R. sup.2, R 3, and R 4 are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis.