59280-70-5

Upstream product

• 57946-56-2 2-fluoro-4-chloroaniline 
• 108-24-7 acetic anhydride 
• 75-36-5 acetyl chloride 
• 399-31-5 N-(2-fluorophenyl)acetamide 
• 64-19-7 acetic acid 

Downstream Products

• 95635-45-3 N-(4-chloro-2-fluoro-5-nitrophenyl)acetamide 
• 1442470-80-5 N-(4-chloro-2-fluoro-3-(hydroxymethyl)phenyl)acetamide 
• 1442470-82-7 3-acetamido-6-chloro-2-fluorobenzyl methanesulfonate 
• 1442470-84-9 N-(4-chloro-3-(cyanomethyl)-2-fluorophenyl)acetamide 
• 1379666-58-6 (E)-3-(3-acetamido-6-chloro-2-fluorophenyl)acrylic acid 
• 1379666-59-7 3-(3-acetamido-2-fluorophenyl)propanoic acid 
• 1379666-61-1 5-(benzylamino)-4-fluoro-2,3-dihydro-1H-inden-1-one 
• 1379666-62-2 2-(benzyl(4-fluoro-1-oxo-2,3-dihydro-1H-inden-5-yl)amino)-N,N-diethylacetamide 
• 1000590-86-2 N-(4-chloro-2-fluoro-3-iodophenyl)acetamide 
• 50739-39-4 2-(bromomethyl)-6-chloro-1,3-benzothiazole 
• 1379666-56-4 N-(4-chloro-2-fluoro-3-formylphenyl)acetamide 
• 1442472-19-6 1-(4-chloro-3-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea 
• 1442470-89-4 3-(3-amino-6-chloro-2-fluorophenyl)-1-ethyl-7-(methylamino)-1,6-naphthyridin-2(1H)-one 
• 1442470-88-3 3-(3-amino-6-chloro-2-fluorophenyl)-7-chloro-1-ethyl-1,6-naphthyridin-2(1H)-one 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUND

Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Imidazolium Salt Catalyzed para -Selective Halogenation of Electron-Rich Arenes

A highly para-selective halogenation of arenes bearing coordinating groups in the presence of a dimidazolium salt as a catalyst is reported. A series of electron-rich p-haloarenes were prepared in good yields and good to excellent selectivities. We also propose a plausible mechanism for the catalytic reaction.

CYCLOPENTYLBENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PSYCHOTIC AND COGNITIVE DISORDERS

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, Ra, Rb, R1, R2 and R3 their preparation, pharmaceutical compositions containing them and their use in therapy.

NOVEL COMPOUND, AND KINESIN SPINDLE PROTEIN INHIBITOR AND APPLICATION THEREOF

A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.

COMPOUND, KINESIN SPINDLE PROTEIN INHIBITOR, AND APPLICATION THEREOF

A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.

Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases

The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.

DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.

Facile synthesis and herbicidal activities of new isoxazole derivatives via 1,3-dipolar cycloaddition reaction

A series of cycloadducts via 1,3-dipolar cycloaddition reactions of generated nitrile oxides with N-(4-chloro-2-fluorophenyl) maleimides were described. The reaction of N-(4-chloro-2-fluorophenyl) maleimides with nitrile oxides gave 3,5-diaryl-3a,6a-dihydropyrroio[3,4-d]isoxazole-4,6-diones through syn-addition pattern. The title compounds were characterized by 1H NMR, IR, MS, and elemental analysis or HRMS. The single crystal structure of 6i was determined by X-ray diffraction. The herbicidal activities of the title compounds were evaluated. Some of them exhibited certain herbicidal activities against barnyardgrass and rape.

PHENYLACETIC ACID DERIVATIVES

Compounds of formula (I) pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications

Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective 3-[(benzothiazol-2-yl)methyl]indole-N-alkanoic acid aldose reductase inhibitors. The lead candidate, 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat, 9) inhibits aldose reductase with an IC50 of 5 nM, while being 5400 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes. It lowers nerve and lens sorbitol levels with ED50's of 1.9 and 4.5 mg/kg/d po, respectively, in the 5-day STZ-induced diabetic rat model. In a 3-month diabetic intervention model (1 month of diabetes followed by 2 months of drug treatment at 5 mg/kg/d po), it normalizes polyols and reduces the motor nerve conduction velocity deficit by 59% relative to diabetic controls. It has a favorable pharmacokinetic profile (F, 82%; t1/2, 5.6 h; Vd, 0.694 L/kg) with good drug penetration in target tissues (Cmax in sciatic nerve and eye are 2.36 and 1.45 μg equiv/g, respectively, when dosed with [14C] lidorestat at 10 mg/kg po).