102392-07-4

Upstream product

• 1978-39-8 5-fluoro-2-methoxy-aniline 
• 821-48-7 bis-(2-chloroethyl)amine hydrochloride 
• 452-08-4 2-bromo-4-fluoro-1-methoxybenzene 

Downstream Products

• 102392-08-5 N-[3-[4-(3-fluoro-6-methoxyphenyl)-1-piperazinyl]propyl]-phthalimide 
• 178974-44-2 1-(8-aza-bicyclo[3.2.1]oct-8-yl)-4-[4-(5-fluoro-2-methoxy-phenyl)-piperazin-1-yl]-2-phenyl-butan-1-one 

Relevant academic research and scientific papers

Identification of novel GLUT inhibitors

The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.

1-ARYL-4-SUBSTITUTED PIPERAZINES DERIVATIVES FOR USE AS CCR1 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATION AND IMMUNE DISORDERS

Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

ISOINDOLINYL-ALKYL-PIPERAZINES

The invention is generally concerned with isoindolinyl-alkylpiperazine compounds generally characterized by the formula STR1 wherein X is halogen or trifluoromethyl; n is an integer ranging from 2 to 5; Y is STR2 in which R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, cyano; R 2 is hydrogen, halogen, lower alkyl, lower alkoxy; and R 3 is hydrogen, cyano. These compounds are useful as diuretic and/or antihypertensive agents.