104066-80-0

Upstream product

• 588-16-9 m-methoxyacetanilide 
• 19056-40-7 4-bromo-3-methoxyaniline 
• 108-24-7 acetic anhydride 
• 75-36-5 acetyl chloride 
• 591-33-3 3-ethoxyacetanilide 
• 536-90-3 m-Anisidine 

Downstream Products

• 565227-62-5 N-{4-bromo-2-[(3-bromo-1-phenylsulfonyl-1H-indol-2-yl)methyl]-5-methoxyphenyl}acetamide 
• 619297-21-1 N-[2-(1-benzenesulfonyl-3-phenylsulfanyl-1H-indol-2-ylmethyl)-4-bromo-5-methoxy-phenyl]-acetamide 
• 173312-35-1 4'-bromo-5'-methoxy-2'-nitroacetanilide 
• 1307885-48-8 N-(4-(7-(3,4-dichlorophenyl)-1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)-3-methoxyphenyl)acetamide 
• 1022983-61-4 N-[4-bromo-2-(4-ethyl-benzoyl)-5-methoxy-phenyl]-acetamide 
• 619297-32-4 N-[2-(1-benzenesulfonyl-3-bromo-1H-indole-2-carbonyl)-4-bromo-5-methoxy-phenyl]-acetamide 
• 7251-09-4 4-amino-2-methoxybenzonitrile 
• 84954-08-5 4-cyano-3-methoxyphenyl isocyanate 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUNDS AND USES THEREOF

In recognition of the unmet need to develop novel therapeutic agents, the present invention discloses a novel class of heterocycles as dual inhibitors of BRD4 and class I PI3Ks. The compounds claimed herein could be used alone or in combination therapies

BICYCLIC HETEROCYCLE DERIVATIVES AS BROMODOMAIN INHIBITORS

The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1,Cy2, R1,R2 and L have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are usefulas bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.

BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS

The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.

BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS

The present invention provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n and dotted line are have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Mild C - H halogenation of anilides and the isolation of an unusual palladium(I)-palladium(II) species

Reducing the load: A facile palladium-catalyzed ortho-selective bromination and chlorination of anilides occurs under aerobic conditions at room temperature when N-halosuccinimides (NXS) are used in the presence of p-toluenesulfonic acid (PTSA). The orthopalladated PTSA complex is not only catalytically competent but also undergoes a reductive process to yield an unusual PdI-PdII tetramer (see structure; Pdgreen, Ored, Syellow, Cgray). Copyright

GAMMA SECRETASE MODULATORS

The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions conta

Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors

The synthesis and structure-activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded compounds with improved enzymatic and cellular potency.

GLUCOPYRANOSYL-SUBSTITUTED BENZYL-BENZONITRILE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR MANUFACTURE

Glucopyranosyl-substituted benzyl-benzonitrile derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators

Pharmacokinetic studies in cynomolgus monkeys with a novel prototype selective androgen receptor modulator revealed trace amounts of an aniline fragment released through hydrolytic metabolism. This aniline fragment was determined to be mutagenic in an Ames assay. Subsequent concurrent optimization for target activity and avoidance of mutagenicity led to the identification of a pharmacologically superior clinical candidate without mutagenic potential.

HETEROCYCLIC KINASE INHIBITORS

Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.