915100-66-2

Upstream product

• 75-52-5 nitromethane 
• 165047-24-5 2,4,5-trifluorobenzaldehyde 
• 956924-25-7 2-nitro-1-(2,4,5-trifluorophenyl)ethanol 

Downstream Products

• 936482-23-4 (R)-diethyl 2-(2-nitro-1-(2,4,5-trifluorophenyl)ethyl)malonate 
• 1384175-50-1 8-nitro-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-3-carbonitrile 
• 1384175-49-8 8-amino-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-3-carbonitrile 
• 1384175-52-3 (R)-N-((7R,8S)-3-cyano-7-(2,4.5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridin-8-yl)-2-hydroxy-2-phenylacetamide 
• 1384175-56-7 (7R,8S)-8-amino-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 
• 1384175-66-9 8-nitro-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 
• 1384175-67-0 8-amino-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 
• 1384175-69-2 (R)-N-((7R,8S)-4-cyano-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridin-8-yl)-2-hydroxy-2-phenylacetamide 
• 1384175-71-6 (7R,8S)-8-((tert-butoxycarbonyl)amino)-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carboxylic acid 
• 1384175-80-7 (7R,8S)-8-amino-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-4-carboxamide 
• 1384175-53-4 (7R,8S)-8-amino-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyridine-3-carbonitrile 
• 1384126-50-4 7-nitro-8-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine 
• 1384126-46-8 2-bromo-4-nitro-5-(2,4,5-trifluorophenyl)cyclohexanone 

Relevant academic research and scientific papers

Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes

Poor medication adherence is one of the leading causes of suboptimal glycaemic control in approximately half of the patients with type 2 diabetes mellitus (T2DM). Long-acting antidiabetic drugs are clinically needed for improving patients' compliance. Dipeptidyl peptidase-4 (DPP-4) inhibitors play an increasingly important role in the treatment of T2DM because of their favorable properties of weight neutrality and hypoglycemia avoidance. Herein, we report the successful discovery and scale-up synthesis of compound 5, a structurally novel, potent, and long-acting DPP-4 inhibitor for the once-weekly treatment of T2DM. Inhibitor 5 has fast-associating and slow-dissociating binding kinetics profiles as well as slow clearance rate and long terminal half-life pharmacokinetic properties. A single-dose oral administration of 5 (3 mg/kg) inhibited >80% of DPP-4 activity for more than 7 days in diabetic mice. The long-term antidiabetic efficacies of 5 (10 mg/kg, qw) were better than those of the once-weekly trelagliptin and omarigliptin, especially in decreasing the hemoglobin A1c level.

Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a clinically validated target for the treatment of type 2 diabetes mellitus (T2DM). To discover novel and potent DPP-4 inhibitors, three series of compounds were designed and synthesized in this study based on our previou

Preparation method of 2,3-dihydro-1H-benzo[f] chromane-2-amine derivative

The invention provides a preparation method of a (2S, 3R)-2-amidogen-3-(2,4,5-trifluorophenyl)-9-methoxyl-2,3-dihydro-1H-benzo[f] chromane-8 bit substitutive derivative shown as a formula I shown in the accompanying drawing, wherein R is selected from H, OCH3, CN, SO2CH3 and NHSO2CH3. The method has the advantages that the yield is high; the purification is convenient; the cost is low, and the like.

Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes

Starting from the lead isodaphnetin, a natural product inhibitor of DPP-4 discovered through a target fishing docking based approach, a series of novel 2-phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine derivatives as potent DPP-4 inhibitors are rationally designed utilizing highly efficient 3D molecular similarity based scaffold hopping as well as electrostatic complementary methods. Those ingenious drug design strategies bring us approximate 7400-fold boost in potency. Compounds 22a and 24a are the most potent ones (IC50 ≈ 2.0 nM) with good pharmacokinetic profiles. Compound 22a demonstrated stable pharmacological effect. A 3 mg/kg oral dose provided >80% inhibition of DPP-4 activity within 24 h, which is comparable to the performance of the long-acting control omarigliptin. Moreover, the efficacy of 22a in improving the glucose tolerance is also comparable with omarigliptin. In this study, not only promising DPP-4 inhibitors as long acting antidiabetic that are clinically on demand are identified, but the target fish docking and medicinal chemistry strategies were successfully implemented.

Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative

The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.

CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS

Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.

CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS

Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.

PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to pyrrolidine derivatives of formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives

1,4 DISUBSTITUTED PYRROLIDINE - 3 - YL -AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS

Therapeutic compounds are disclosed having the general formula (I) that are useful for the treatment of metabolic disorders, including type II diabetes. The compounds have activity as agonists of GPR1 19. Compounds having stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.

CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS

Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.