193902-99-7

Upstream product

• 1046790-71-9 tert-butyl 4-(3,4-dinitrophenyl)piperazine-1-carboxylate 
• 1635-61-6 5-chloro-2-nitroaniline 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 364-53-4 4-fluoro-1,2-dinitro-benzene 
• 2369-11-1 5-fluoro-2-nitroaniline 
• 1581275-04-8 tert-butyl 4-(4-acetylamino-3-nitrophenyl)piperazine-1-carboxylate 
• 881-50-5 N-(4-bromo-2-nitrophenyl)acetamide 
• 1581275-05-9 tert-butyl 4-(4-amino-3-nitrophenyl)piperazine-1-carboxylate 
• 193902-98-6 4-(3-amino-4-nitrophenyl)piperazine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 1581275-12-8 5-(4-(biphenyl-4-ylmethyl)piperazin-1-yl)-1H-benzo[d]imidazol-2(3H)-one 
• 1581275-13-9 5-(4-((4'-fluorobiphenyl-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazol-2(3H)-one 
• 1581275-14-0 5-(4-((5-phenylpyridin-3-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazol-2(3H)-one 
• 1581275-15-1 5-(4-((5-(4-fluorophenyl)pyridin-3-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazol-2(3H)-one 
• 1581275-16-2 5-(4-(3-(cyclopentenyl)benzyl)piperazin-1-yl)-1H-benzo[d]imidazol-2(3H)-one 
• 1621399-81-2 tert-butyl 4-(2-(2-(tert-butoxycarbonylamino)-4-fluorophenylcarbamoyl)-quinoxalin-6-yl)-piperazine-1-carboxylate 
• 1621399-59-4 C₁₉H₁₉FN₆O 
• 1621399-82-3 tert-butyl 4-(2-(2-amino-5-fluorophenylcarbamoyl)quinoxalin-6-yl)piperazine-1-carboxylate 
• 1621399-60-7 C₁₉H₁₉FN₆O 

Relevant academic research and scientific papers

SMALL MOLECULE INHIBITORS OF GALECTIN-3

The present disclosure relates to compounds of Formula (I), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions. (Formula (I))

DIHYDROBENZIMIDAZOLONES

The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

HPK1 INHIBITORS AND METHODS OF USING SAME

Thienopyridinone compounds of Formula (I) and pharmaceutically acceptable salts thereof are described. In these compounds, one of X1; X2, and X3 is S and the other two are each independently CR, wherein R and all other variables are as defined herein. The compounds are shown to inhibit HPK1 kinase activity and to have in vivo antitumor activity. The compounds can be effectively combined with pharmaceutically acceptable carriers and also with other immunomodulatory approaches, such as checkpoint inhibition or inhibitors of tryptophan oxidation. Formula (I).

NOVEL 5-HYDROXYTRYPTAMINE RECEPTOR 7 ACTIVITY MODULATORS AND THEIR METHOD OF USE

Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

NOVEL SIGMA-2 RECEPTOR BINDERS AND THEIR METHOD OF USE

Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.

SELECTIVE HDAC3 INHIBITORS

Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.

Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones

A series of new 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)- ones have been synthesized and evaluated for dual D2 and 5-HT1A receptor binding affinities. The synthesized ligands are structurally related to bifeprunox, a potential atypical antipsychotic, having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. The Suzuki-Miyaura reaction of cyclic vinyl boronate with appropriate aryl halide yielded arylpiperidine, which was eventually transformed to piperidinyl-1H-benzo[d]imidazol-2(3H)-one. The reductive amination of the latter with appropriate biarylaldehdyes rendered the synthesis of 5-piperidinyl-1H-benzo[d]imidazol-2(3H)-ones. Likewise, the Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halide and subsequent removal of the boc group rendered arylpiperazine. The reductive amination of the latter with appropriate biarylaldehdyes accomplished the synthesis of 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The structure-activity relationship studies showed that cyclopentenylpyridine and cyclopentenylbenzyl groups contribute significantly to the dual D2 and 5-HT1A receptor binding affinities of these compounds.

2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor

Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as endometriosis, prostate cancer and others. Traditional therapy has been limited to peptide agonists and

JAK-2 MODULATORS AND METHODS OF USE

This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention

Identification of novel benzimidazole series of potent and selective ORL1 antagonists

Structure-activity studies on benzimidazole lead 1 obtained from library screening led to the discovery of potent and selective ORL1 antagonist 28, 5-chloro-2-[(1-ethyl-1-methylpropyl)thio]-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1H-benzimidazole, which is s