346617-98-9

Upstream product

• 540-38-5 p-Iodophenol 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 352-34-1 4-fluoro-1-iodobenzene 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 346617-99-0 4-[4-(4-methoxy-phenylsulfanyl)-phenoxy]-piperidine-1-carboxylic acid tert-butyl ester 
• 203445-38-9 4-[4-(benzo[1,3]dioxol-5-ylsulfanyl)-phenoxy]-piperidine-1-carboxylic acid tert-butyl ester 
• 955360-28-8 4-[(4-iodophenyl)oxy]piperidine trifluoroacetate 
• 889865-34-3 4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy]piperidine-1-carboxylic acid tert-butyl ester 
• 921616-50-4 phenylmethyl 4-{4-[(1-{[(1,1-dimethylethyl)oxy]carbonyl}-4-piperidinyl)oxy]phenyl}-3-oxo-1-piperazinecarboxylate 
• 1012330-94-7 tert-butyl 4-(4-(3-hydroxyprop-1-ynyl)phenoxy)piperidine-1-carboxylate 
• 1033055-22-9 tert-butyl 4-{-4-[4-(ethoxycarbonyl)-1H-pyrazol-1-yl]phenoxy}piperidine-1-carboxylate 
• 1033055-20-7 tert-butyl 4-{-4-[4-(pyrrolidin-1-ylcarbonyl)-1H-pyrazol-1-yl]phenoxy}piperidine-1-carboxylate 
• 684249-46-5 4-[(4-iodophenyl)oxy]-1-(1-methylethyl)piperidine 
• 1373010-41-3 1-isopropyl-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy)piperidine 
• 1220019-83-9 4-(4-iodophenoxy)piperidine hydrochloride 
• 955360-30-2 4-{4-[(1-cyclobutyl-4-piperidinyl)oxy]phenyl}-3-butyn-1-ol 
• 955360-31-3 4-{4-[(1-cyclobutyl-4-piperidinyl)oxy]phenyl}-1-butanol 
• 955360-29-9 1-cyclobutyl-4-(4-iodophenoxy)piperidine 

Relevant academic research and scientific papers

RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

MULTIPLE D2 A(NTA)GONISTS/H3 ANTAGONISTS FOR TREATMENT OF CNS-RELATED DISORDERS

The present invention relates to compounds compound according to Formula (III); and pharmaceutically acceptable salts, hydrates and solvates thereof. These compounds have D2receptor antagonist/(partial) agonist effects and H3antagonistic effects, pharmaceutical compositions thereof, and methods of using them for application in the prophylaxis or treatment of CNS disorders.

PLK-4 INHIBITORS AND METHOD OF TREATING CANCER WITH SAME

The invention is directed to a compound represented by the following Structural Formula (I) and (II) and pharmaceutically acceptable salts thereof: (Formula (I)); (Formula (IV)). Compounds represented by this structural formula are kinase inhibitors and are, therefore, disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.

PYRAZOLE DERIVATIVE

A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect: or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention

Optimization of α-ketooxazole inhibitors of fatty acid amide hydrolase

A series of α-ketooxazoles containing conformational constraints in the flexible C2 acyl side chain of 2 (OL-135) and representative oxazole C5 substituents were prepared and examined as inhibitors of fatty acid amide hydrolase (FAAH). Exceptionally potent and selective FAAH inhibitors emerged from the series (e.g., 6, Ki = 200 and 260 pM for rat and rhFAAH). With simple and small C5 oxazole substituents, each series bearing a biphenylethyl, phenoxyphenethyl, or (phenoxymethyl)phenethyl C2 side chain was found to follow a well-defined linear relationship between -log Ki and Hammett σp of a magnitude (ρ = 2.7-3.0) that indicates that the substituent electronic effect dominates, confirming its fundamental importance to the series and further establishing its predictive value. Just as significantly, the nature of the C5 oxazole substituent substantially impacts the selectivity of the inhibitors whereas the effect of the C2 acyl chain was more subtle but still significant even in the small series examined. Combination of these independent features, which display generalized trends across a range of inhibitor series, simultaneously improves FAAH potency and selectivity and can provide exquisitely selective and potent FAAH inhibitors.

4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists

A series of ketopiperazines were prepared and evaluated for their activity as histamine H3 antagonists. From investigation of the tertiary basic center in the aminopropyloxyphenyl template, the 2(R)-methylpyrrolidine was identified as the most

PIPERAZINONE DERIVATIVES USEFUL AS HISTAMINE H3 RECEPTOR ANTAGONISTS AND/OR INVERSE AGONISTS

The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis, wherein R1 and

2-SUBSTITUTED 4-BENZYLPHTHALAZINONE DERIVATIVES AS HISTAMINE H1 AND H3 ANTAGONISTS

The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.

Reversible red fluorescent molecular switches

I see red, I see red, I see red: Optically switchable compounds were synthesized whose visible fluorescence can be quenched down to 6% with light at 360-400 nm and then restored with red light from a diode laser. The molecular switch offers potential applications in data storage and far-field microscopy with spatial resolution far below the diffraction limit. (Chemical Equation Presented).

SUBSTITUTED PIPERAZINES, (1,4) DIASZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS

The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.