147247-29-8

Upstream product

• 622-47-9 4-tolylacetic acid 
• 68682-48-4 methyl 2-methyl-2-(4-methylphenyl)propanoate 
• 79443-97-3 methyl 2-(4-methylphenyl)propanoate 
• 938-94-3 (R,S)-2-(4'-methylphenyl) propionic acid 

Downstream Products

• 1247008-47-4 [1-[[4-(2-methoxy-1,1-dimethyl-2-oxoethyl)phenyl]methyl]-4-piperidinyl]methyl 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxylate 
• 1606974-89-3 2-(4-((2-(3-chlorophenyl)-6-ethylpyrimidin-4-yl)methyl)phenyl)-2-methylpropan-1-ol 
• 1606974-88-2 2-(4-((2-(3-chlorophenyl)-6-ethylpyrimidin-4-yl)methyl)phenyl)-2-methylpropanamide 
• 1606977-29-0 2-(4-((2-(3-chlorophenyl)-6-ethylpyrimidin-4-yl)methyl)phenyl)-2-methylpropanoic acid 
• 1606977-28-9 methyl 2-(4-((2-(3-chlorophenyl)-6-ethylpyrimidin-4-yl)methyl)phenyl)-2-methylpropanoate 
• 1247008-25-8 [1-[[4-[1,1-dimethyl-2-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy]-2-oxoethyl]phenyl]methyl]-4-piperidinyl]methyl 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxylate 
• 1247008-27-0 [1-[[4-[1,1-dimethyl-2-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy]-2-oxoethyl]phenyl]methyl]-4-piperidinyl]methyl 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxylate hydrochloride 
• 1247008-23-6 2-[4-[[4-(3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carbonyloxymethyl)-1-piperidinyl]methyl]phenyl]-2-methylpropanoic acid 
• 879484-59-0 methyl 2-methyl-2-{4-[(4-methyl-1-piperazinyl)methyl]phenyl}propanoate 

Relevant academic research and scientific papers

Development of Fluorine-18 Labeled Metabolically Activated Tracers for Imaging of Drug Efflux Transporters with Positron Emission Tomography

Increased activity of efflux transporters, e.g., P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), at the blood-brain barrier is a pathological hallmark of many neurological diseases, and the resulting multiple drug resistance represents a major clinical challenge. Noninvasive imaging of transporter activity can help to clarify the underlying mechanisms of drug resistance and facilitate diagnosis, patient stratification, and treatment monitoring. We have developed a metabolically activated radiotracer for functional imaging of P-gp/BCRP activity with positron emission tomography (PET). In preclinical studies, the tracer showed excellent initial brain uptake and clean conversion to the desired metabolite, although at a sluggish rate. Blocking with P-gp/BCRP modulators led to increased levels of brain radioactivity; however, dynamic PET did not show differential clearance rates between treatment and control groups. Our results provide proof-of-concept for development of prodrug tracers for imaging of P-gp/BCRP function in vivo but also highlight some challenges associated with this strategy.

HETEROARYL INHIBITORS OF PDE4

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist

5-HT4 receptor antagonists have been suggested to have clinical potential in treatment of atrial fibrillation, diarrhea-prone irritable bowel syndrome and urinary incontinence. Recently, the use of 5-HT4 antagonists has been suggeste

FXR AGONISTS

Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.

2,4-SUBSTITUTED PYRIMIDINES AS CYSTEINE PROTEASE INHIBITORS

Substituted heteroaryl nitrile derivatives of Formula (I) processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.

NOVEL ADENINE COMPOUND AND USE THEREOF

A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene; etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents -COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

Piperazine compounds and medicinal use thereof

The present invention relates to a piperazine compound of the formula wherein R1and R2are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4and R5are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6and R7are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8and R9are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.