55439-73-1

Upstream product

• 3622-35-3 benzothiazole-6-carboxylic acid 
• 79-37-8 oxalyl dichloride 

Downstream Products

• 101084-51-9 benzothiazole-6-carboxamide 
• 55439-58-2 benzothiazole-6-carboxylic acid N'-(3-methyl-benzoyl)-hydrazide 
• 55439-56-0 benzothiazole-6-carboxylic acid N'-benzoyl-hydrazide 
• 55439-57-1 benzothiazole-6-carboxylic acid N'-(4-chloro-benzoyl)-hydrazide 
• 55439-62-8 6-(5-phenyl-[1,3,4]oxadiazol-2-yl)-benzothiazole 
• 55439-64-0 6-(5-m-tolyl-[1,3,4]oxadiazol-2-yl)-benzothiazole 
• 55439-63-9 6-[5-(4-chloro-phenyl)-[1,3,4]oxadiazol-2-yl]-benzothiazole 
• 55439-68-4 6-(5-phenyl-[1,3,4]thiadiazol-2-yl)-benzothiazole 
• 55439-70-8 6-(5-m-tolyl-[1,3,4]thiadiazol-2-yl)-benzothiazole 
• 55439-69-5 6-[5-(4-chloro-phenyl)-[1,3,4]thiadiazol-2-yl]-benzothiazole 
• 1147130-49-1 N-(4-phenoxy-2-butynyl)-benzothiazole-6-carboxamide 
• 1147130-48-0 N-(4-phenoxy-2-butenyl)-benzothiazole-6-carboxamide 
• 1392323-22-6 C₁₇H₁₄N₂OS 

Relevant academic research and scientific papers

APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS AND METHODS OF USE THEREOF

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).

Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

METHODS FOR THE TREATMENT OF BACTERIAL INFECTIONS

This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.

Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease

Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic effects, it has been suggested that the CB1 receptors in the periphery could play a significant role in reducing reflux. A moderately potent and highly lipophilic series of 2-aminobenzamides was identified through focused screening of GPCR libraries. Development of this series focused on improving potency and efficacy at the CB1 receptor, reducing lipophilicity and limiting the central nervous system (CNS) exposure while maintaining good oral absorption. Improvement of the series led to compounds having excellent potency at the CB1 receptor and high levels of agonism, good physical and pharmacokinetic properties, and low penetration into the CNS. A range of compounds demonstrated a dose-dependent inhibition of transient lower esophageal sphincter relaxations in a dog model.

Enantioselective halocyclization using reagents tailored for chiral anion phase-transfer catalysis

A chiral anion phase-transfer system for enantioselective halogenation is described. Highly insoluble, ionic reagents were developed as electrophilic bromine and iodine sources, and application of this system to o-anilidostyrenes afforded halogenated 4H-3,1-benzoxazines with excellent yield and enantioselectivity.

Synthesis and evaluation of 5-fluoro-2-aryloxazolo[5,4- b ]pyridines as β-amyloid PET ligands and identification of MK-3328

5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential 18F containing β-amyloid PET ligands. In competition binding assays using human AD brain homogenates, compounds 14b, 16b, and 17b were identified as having favorable potency versus human β-amyloid plaque and were radiolabeled for further evaluation in in vitro binding and in vivo PET imaging experiments. These studies led to the identification of 17b (MK-3328) as a candidate PET ligand for the clinical assessment of β-amyloid plaque load.

Heteroaromatic ester inhibitors of hepatitis A virus 3C proteinase: Evaluation of mode of action

The related 3C and 3C-like proteinase (3Cpro and 3CLpro) of picornaviruses and coronaviruses, respectively, are good drug targets. As part of an effort to generate broad-spectrum inhibitors of these enzymes, we screened a library of inhibitors based on a halopyridinyl ester from a previous study of the severe acute respiratory syndrome (SARS) 3CL proteinase against Hepatitis A virus (HAV) 3Cpro. Three of the compounds, which also had furan rings, inhibited the cleavage activity of HAV 3Cpro with Kics of 120-240 nM. HPLC-based assays revealed that the inhibitors were slowly hydrolyzed by both HAV 3Cpro and SARS 3CLpro, confirming the identity of the expected products. Mass spectrometric analyses indicated that this hydrolysis proceeded via an acyl-enzyme intermediate. Modeling studies indicated that the halopyridinyl moiety of the inhibitor fits tightly into the S1-binding pocket, consistent with the lack of tolerance of the inhibitors to modification in this portion of the molecule. These compounds are among the most potent non-peptidic inhibitors reported to date against a 3Cpro.

CONDENSED IMIDAZOLE COMPOUND AND USE THEREOF

The present invention relates to a compound represented by the formula [I] wherein X1, X2 and X3 are each an optionally substituted CH or a nitrogen atom, and any one of X1, X2 and X3 is a nitrogen atom, X4 is an optionally substituted CH, R1 is an optionally substituted phenyl group or an optionally substituted heterocyclic group, and R2 is an optionally substituted pyridin-4-yl group, an optionally substituted pyridine-N-oxide-4-yl group or an optionally substituted pyrimidin-4-yl group, or a salt thereof. The compound has superior p38 MAP kinase inhibitory activity and MMP-13 production inhibitory activity, and is useful as an agent for the prophylaxis or treatment and the like of an inflammatory disease, an autoimmune disease, a debilitating disease, an osteoarticular degenerative disease, a neurodegenerative disease, a vascular disease, a neoplastic disease or an infectious disease.

Pyrrolobenzodiazepine carboxyamide vasopressin agonists

The present invention provides compounds of the formula: wherein: X, Y and Z are independently selected from O, S, CH, CH2, N, or NR4; W is moiety selected from (CH2)n; n=1-2; R1, R2are independently, hydrogen, straight chain alkyl (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), halogen, straight or branched chain alkoxy (C1-C6), hydroxy, CF3, or perfluoroalkyl (C2-C6); R3is hydrogen or a straight chain alkyl group (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), or hydroxyalkyl (C1-C6); R4is selected from hydrogen, or (lower alkyl (C1-C6); and R5is selected from halogen or hydrogen; or a pharmaceutically acceptable salt thereof: as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Heterocyclic N-acetonylbenzamides and their use as fungicides

Certain N-acetonylbenzamides and their use as fungicides are disclosed. The N-acetonylbenzamides disclosed contain a heterocyclic ring fused to an aromatic ring. These compounds are particularly effective against phytopathogenic fungi of the class Oomycetes. Also disclosed is a method for controlling phytopathogenic fungi by applying one or more of the heterocyclic N-acetonylbenzamides of the present invention, optionally with one or more additional fungicidal compounds.