54824-07-6

Upstream product

• 67-56-1 methanol 
• 7664-93-9 sulfuric acid 
• 76854-15-4 C₂₀H₂₃NO₂ 
• 200052-48-8 4-phenyl-piperidine-4-carboxylic acid 4-toluene sulfonate 
• 101-41-7 benzeneacetic acid methyl ester 
• 167262-47-7 1-tert-butyloxycarbonyl-4-phenyl-piperidine-4-carboxylic acid methyl ester 
• 24476-55-9 N-(p-tosyl)-4-phenyl-4-cyano-piperidine 

Downstream Products

• 166809-18-3 3-[4-methoxycarbonyl-4-phenyl piperidin-1-yl]propylamine 
• 200052-24-0 1-benzyl-4-[4-methoxycarbonyl-4-phenylpiperidin-1-yl]piperidine 
• 252001-97-1 3-(4-methoxycarbonyl-4-phenylpiperidin-1-yl)-3-methylpropionitrile 
• 758672-26-3 1-(4-Cyano-4,4-diphenylbutyl)-4-phenyl-4-piperidinecarboxylic acid, methyl ester 
• 200052-59-1 2-[4-methoxycarbonyl-4-phenylpiperidin-1-yl]ethylamine 
• 216310-98-4 5-benzyloxycarbonyl-6-(2,4-difluorophenyl)-1,6-dihydro-1-(5-(4-methoxycarbonyl-4-phenylpiperidin-1-yl)pent-1-yl)-2,4-dimethylpyrimidine 
• 749913-39-1 4-phenyl-1-[5-(1-pyrrolidinylcarbonyl)-2-pyridinyl]-4-piperidinecarboxylic acid, methyl ester 
• 875831-88-2 C₁₃H₁₆N₂O₃ 
• 1246390-30-6 1-[4-(3-methyl-[1,2,4]oxadiazol-5-yl)-benzoyl]-4-phenyl-piperidine-4-carboxylic acid methyl ester 
• 103166-95-6 1-(3-cyano-3,3-diphenyl-propyl)-4-phenyl-piperidine-4-carboxylic acid methyl ester 
• 3627-45-0 4-phenyl-piperidine-4-carboxylic acid 
• 166808-36-2 5-[3-(4-methoxycarbonyl-4-phenyl-piperidin-1-yl)-propylcarbamoyl]-2,6-dimethyl-4-(4-nitro-phenyl)-1,4-dihydro-pyridine-3-carboxylic acid 2-cyano-ethyl ester 

Relevant academic research and scientific papers

Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class i HDAC Enzymes and Cancer Cell Proliferation

AR-42 is an orally active inhibitor of histone deacetylases (HDACs) in clinical trials for multiple myeloma, leukemia, and lymphoma. It has few hydrogen bond donors and acceptors but is a chiral 2-arylbutyrate and potentially prone to racemization. We report achiral AR-42 analogues incorporating a cycloalkyl group linked via a quaternary carbon atom, with up to 40-fold increased potency against human class I HDACs (e.g., JT86, IC50 0.7 nM, HDAC1), 25-fold increased cytotoxicity against five human cancer cell lines, and up to 70-fold less toxicity in normal human cells. JT86 was ninefold more potent than racAR-42 in promoting accumulation of acetylated histone H4 in MM96L melanoma cells. Molecular modeling and structure-activity relationships support binding to HDAC1 with tetrahydropyran acting as a hydrophobic shield from water at the enzyme surface. Such potent inhibitors of class I HDACs may show benefits in diseases (cancers, parasitic infections, inflammatory conditions) where AR-42 is active.

SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES

The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS

The present application relates to compounds of formula (I) wherein the definitions are as described in claim 1. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Pa

A facile method for preparation of [2H3]-sufentanil and its metabolites

An improved process for the synthesis of sufentanil with an overall yield of 26% is described. The reactive and high yielding N-debenzylation of the piperidine intermediate 7 using a mixture of Pd/C and Pd(OH)2 was applied to other drug intermediates affording free amines in short reaction times. The deuterium-labeled sufentanil and the metabolite desmethylsufentanil were synthesized applying the optimized process.

PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY

The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.

5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines

This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human α1Areceptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the α1Areceptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

MORPHOLINONE AND MORPHOLINE DERIVATIVES AND USES THEREOF

This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human α 1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the α 1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Oxazolidinones as alpha 1A receptor antagonists

This invention is directed to oxazolidinone compounds which are selective antagonists for human alpha 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the alpha 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Phenylacetamides as selective α-1A adrenergic receptor antagonists

A novel class of potent and selective α-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known α-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described. (C) 2000 Elsevier Science Ltd. All rights reserved.

5-(HETEROCYCLIC ALKYL)-6-ARYL-DIHYDROPYRIMIDINES

This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1C receptors and which have the structure: STR1 wherein A is aryl; R 1, R 2 and R. sub.3 are alkyl or heteroalkyl; R 4 is heterocyclic alkyl; and X is S, O or NR 3. This invention also relates to use of these compounds for the treatment of benign prostatic hyperplasia and other diseases where antagonism of the human α 1C receptor is useful. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of such a compound and a pharmaceutically acceptable carrier.