52397-82-7

Upstream product

• 1201-99-6 trans-2,4-dichlorocinnamic acid 
• 79-37-8 oxalyl dichloride 
• 55144-92-8 3-(2,4-dichlorophenyl)propionic acid 

Downstream Products

• 1215279-81-4 (1aS,6aR)-3,5-dichloro-6,6a-di-hydro-1aH-1-oxa-cyclopropa[a]indene 
• 1188143-94-3 4,6-dichloroindan-1-ol 
• 1215273-25-8 (S)-1-[(1S,2S)-4,6-dichloro-1-(4-methanesulfonylphenoxy)indan-2-yl]-3-fluoropyrrolidine 
• 1215272-30-2 (R)-1-[(1S,2S)-4,6-dichloro-1-(4-methanesulfonylphenoxy)indan-2-yl]-3-fluoropyrrolidine 
• 1623130-92-6 (1H-1,2,4-triazol-1-yl)methyl 3-(2,4-dichlorophenyl)propanoate 
• 52397-81-6 4,6-dichloroindan-1-one 
• 55144-55-3 2-bromo-4,6-dichloroindan-1-one 

Relevant academic research and scientific papers

Synthesis of Conformationally Locked and C-Linked Analogues of Imidazole-Based Ketene Dithioacetal Fungicides

First examples with the unknown tricyclic 4,8 b -dihydro-3 aH -indeno[1,2- d ][1,3]dithiole ring system have been prepared. Also, imidazoles linked in ring position 5 to a ketene dithioacetal and 1,3-dithiane derivatives with an exocyclic cyano- and imidazole-substituted C-C double bond are completely new. All these compounds are either conformationally locked, C-linked or six-ring analogues of the antifungal agent luliconazole. Synthesis and fungicidal activity of these sterol biosynthesis inhibitors are reported.

Discovery and Optimization of 1-Phenoxy-2-aminoindanes as Potent, Selective, and Orally Bioavailable Inhibitors of the Na+/H+ Exchanger Type 3 (NHE3)

The design, synthesis, and structure-activity relationship of 1-phenoxy-2-aminoindanes as inhibitors of the Na+/H+ exchanger type 3 (NHE3) are described based on a hit from high-throughput screening (HTS). The chemical optimization resulted in the discovery of potent, selective, and orally bioavailable NHE3 inhibitors with 13d as best compound, showing high in vitro permeability and lacking CYP2D6 inhibition as main optimization parameters. Aligning 1-phenoxy-2-aminoindanes onto the X-ray structure of 13d then provided 3D-QSAR models for NHE3 inhibition capturing guidelines for optimization. These models showed good correlation coefficients and allowed for activity estimation. In silico ADMET models for Caco-2 permeability and CYP2D6 inhibition were also successfully applied for this series. Moreover, docking into the CYP2D6 X-ray structure provided a reliable alignment for 3D-QSAR models. Finally 13d, renamed as SAR197, was characterized in vitro and by in vivo pharmacokinetic (PK) and pharmacological studies to unveil its potential for reduction of obstructive sleep apneas.

Synthesis, structure and biological activities of novel triazole compounds containing Ester Group

Novel triazole compounds containing ester group were synthesized. Their structure were confirmed by means of IR, 1H NMR and elemental analysis. The single crystal structure of compound (1H-1,2,4-triazol-1-yl)methyl 3-(2,4-dichlorophenyl)propanoate (compound 3c) was determined via X-ray diffraction. It crystallizes in a monoclinic system with space group P2(1)/c, a = 1.0814(2) nm, b = 0.64514(13) nm, c = 1.8698(4) nm, β = 101.05(3)°, Z = 4, V = 1.2802(5) nm3, Dc = 1.557 Mg/m3, μ = 0.508 mm-1, F(000) = 616 and final R1 = 0.0700. Intermolecular hydrogen-bond and φ-φ stacking interactions exit in the lattice, facilitating the stabilization of crystal structure. The results of the biological test show that these compounds have some fungicidal activity.

Indanylidenes. 2. Design and synthesis of (E)-2-(4-chloro-6-fluoro-1-indanylidene)-N-methylacetamide, a potent antiinflammatory and analgesic agent without centrally acting muscle relaxant activity

Extension of the structure-activity relationship studies that led to the discovery of the nonsedating potent muscle relaxant, antiinflammatory, and analgesic agent (E)-2-(4,6-difluoro-1-indanylidene)acetamide, 1, has given rise to (E)-2-(4-chloro-6-fluoro

METHOD FOR TREATING MENIERE'S DISEASE

A method for the treatment of Meniere's disease comprising the administration of a medicament which modulates the IKs channel of the ear and thereby reducing endolymph production.

Antiarrhythmic benzodiazepines

Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: STR1

METHODS OF TREATING CARDIAC ARRHYTHMIA

Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.