669080-79-9

Upstream product

• 261952-04-9 3-methyl-5-(trifluoromethyl)benzonitrile 
• 569370-38-3 3-(hydroxymethyl)-5-(trifluoromethyl)benzonitrile 

Downstream Products

• 1616670-61-1 3-(4-methylpiperazin-1-ylmethyl)-5-trifluoromethylbenzonitrile 
• 1616670-62-2 3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)benzoic acid 
• 1006599-04-7 3-{1-[({3-[(cyclopentylmethyl)(ethyl)amino]-6-methoxypyridin-2-yl}methyl){5-[2-(methylthio)ethoxy]pyrimidin-2-yl}amino]methyl}-5-(trifluoromethyl)benzonitrile 
• 866400-64-8 (2R,4S)-4-[(5-bromopyrimidin-2-yl)-(3-cyano-5-trifluoromethylbenzyl)]-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester 
• 693250-09-8 3-aminomethyl-5-trifluoromethyl-benzonitrile 

Relevant academic research and scientific papers

Pharmacophore-based design of novel oxadiazoles as selective sphingosine-1-phosphate (S1P) receptor agonists with in vivo efficacy

Sphingosine-1-phosphate (S1P) receptor agonists have shown promise as therapeutic agents for multiple sclerosis (MS) due to their regulatory roles within the immune, central nervous system, and cardiovascular system. Here, the design and optimization of novel [1,2,4]oxadiazole derivatives as selective S1P receptor agonists are described. The structure-activity relationship exploration was carried out on the three dominant segments of the series: modification of the polar head group (P), replacement of the oxadiazole linker (L) with different five-membered heterocycles, and the use of diverse 2,2′-disubstituted biphenyl moieties as the hydrophobic tail (H). All three segments have a significant impact on potency, S1P receptor subtype selectivity, physicochemical properties, and in vitro absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of the compounds. From these optimization studies, a selective S1P1 agonist, N-methyl-N-(4-{5-[2-methyl-2′-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (45), and a dual S1P1,5 agonist, N-methyl-N-(3-{5-[2′-methyl-2-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (49), emerged as frontrunners. These compounds distribute predominantly in lymph nodes and brain over plasma and induce long lasting decreases in lymphocyte count after oral administration. When evaluated head-to-head in an experimental autoimmune encephalomyelitis mouse model, together with the marketed drug fingolimod, a pan-S1P receptor agonist, S1P1,5 agonist 49 demonstrated comparable efficacy while S1P1-selective agonist 45 was less potent. Compound 49 is not a prodrug, and its improved property profile should translate into a safer treatment of relapsing forms of MS.

AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus a

NK-1 AND SEROTONIN TRANSPORTER INHIBITORS

The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.

Dibenzyl Amine Compounds and Derivatives

Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

TRISUBSTITUTED AMINE COMPOUND

The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES

The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.

Dibenzylamine compound and medicinal use thereof

A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.