536975-36-7

Upstream product

• 115933-49-8 4-benzyloxy-3-trifluoromethylbenzoic acid methyl ester 
• 942399-25-9 4-benzyloxy-3-trifluoromethylbenzoic acid benzyl ester 
• 100-51-6 benzyl alcohol 
• 67515-55-3 4-fluoro-3-(trifluoromethyl)benzoic acid 
• 536975-35-6 4-benzyloxy-3-trifluoromethyl benzoic acid 

Downstream Products

• 536975-37-8 1-benzyloxy-4-chloromethyl-2-trifluoromethylbenzene 
• 957204-71-6 5-(4-benzyloxy-3-trifluoromethylbenzyloxy)-1-(tert-butoxycarbonyl)indoline 
• 773871-37-7 4-hydroxy-3-trifluoromethylbenzyl alcohol 
• 537683-42-4 4-[(4-benzyloxy-3-trifluoromethylbenzyl)[1,2,4]triazol-4-ylamino]benzonitrile 

Relevant academic research and scientific papers

AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF

Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.

HETEROARYLAMIDE LOWER CARBOXYLIC ACID DERIVATIVE

To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, -O-, or - CH2-; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3) : (1) -G1-, (2) -G2-N(R2) -G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents -CH2-O- or the like, and Y represents a group represented by foumula 3, a salt thereof, or a solvate thereof.

AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(=O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH=CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5 - 8.

Dual aromatase-steroid sulfatase inhibitors

By introducting the steroid sulfatase inhibitory pharmacophore into aromatase inhibitor 1 (YM511), two series of single agent dual aromatase-sulfatase inhibitors (DASIs) were generated. The best DASIs in'vitro (JEG-3 cells) are 5, (IC50(aromatase) = 0.82 nM; IC 50(sulfatase) = 39 nM), and 14, (IC50(aromatase) = 0.77 nM; IC50(sulfatase) = 590 nM). X-ray crystallography of 5, and docking studies of selected compounds into an aromatase homology model and the steroid sulfatase crystal structure are presented. Both 5 and 14 inhibit aromatase and sulfatase in PMSG pretreated adult female Wistar rats potently 3 h after a single oral 10 mg/kg dose. Almost complete dual inhibition is observed for 5 but the levels were reduced to 85% (aromatase) and 72% (sulfatase) after 24 h. DASI 5 did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed.