79098-88-7

Upstream product

• 29608-05-7 1-(4-aminobenzyl)piperidine 
• 530-62-1 1,1'-carbonyldiimidazole 
• 552-89-6 2-nitro-benzaldehyde 
• 4403-69-4 2-amino-1-benzylamine 
• 68790-38-5 2-(tert-butyloxycarbonylamino)benzoic acid 
• 83425-16-5 2-amino-N-(1-benzyl-piperidin-4-yl)-benzamide 
• 50541-93-0 4-amino-1-benzylpiperidine 
• 98754-28-0 (1-benzyl-piperidin-4-yl)-(2-nitro-benzyl)-amine 
• 79099-03-9 2-amino-N-[1-(phenylmethyl)-4-piperidinyl]-benzenemethanamine 
• 79098-87-6 1-benzyl-4-(2-nitrophenylmethyl)aminopiperidine*2HCl 
• 1205-72-7 1-benzyl-4-amino-piperidine dihydrochloride 
• 79106-75-5 1-benzyl-4-(2-aminophenylmethyl)aminopiperidine*3HCl 

Downstream Products

• 79098-75-2 3-piperidin-4-yl-3,4-dihydro-1H-quinazoline-2-one 
• 1443256-63-0 3-(1-benzyl-piperidin-4-yl)-1-methyl-3,4-dihydro-1H-quinazolin-2-one 
• 79122-21-7 threo-1-<2-hydroxy-2-(3,4-dimethoxyphenyl)-1-methylethyl>-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl)piperidine 
• 79122-21-7 erythro-1-<2-hydroxy-2-(3,4-dimethoxyphenyl)-1-methylethyl>-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl)piperidine 
• 79106-29-9 1-[2-(3,4-Dimethoxyphenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79106-31-3 1-<2-oxo-2-(3,4-dimethoxyphenyl)-1-methylethyl>-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl)piperidine 
• 79106-47-1 1-[2-(3,4-Dichlorophenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79106-27-7 1-(3,4-dimethoxybenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79106-46-0 1-[2-(4-Methoxyphenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79106-45-9 1-<2-(4-chlorophenyl)-2-hydroxyethyl>-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl)piperidine 
• 79106-44-8 1-[2-(3-Chlorophenyl)-2-hydroxyethyl]-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79098-78-5 1-(3,4-dichlorobenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 79106-42-6 1-(4-Methoxybenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine 
• 85350-65-8 1-(3-phenyl-3-hydroxypropyl)-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl)piperidine 

Relevant academic research and scientific papers

NOVEL HETEROCYCLIC COMPOUNDS AND USE THEREOF IN MEDICINE AND IN COSMETICS

The invention relates to novel heterocyclic compounds of general formula (I), as well as their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to the use thereof as a medicinal product, preferably in the prevention and/or treatment of inflammatory diseases with a neurogenic component or use thereof as a cosmetic. The compounds of the present invention act as antagonists of the CGRP-R receptor.

An efficient synthesis of the piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant

Olcegepant is one of the most potent and selective small molecule CGRP antagonists for the treatment of migraine headaches. Herein, we describe a new and efficient synthesis of the key piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant. PDQ plays a key role in the activity of CGRP antagonists. Primary improvements over existing methods include a high-yielding reductive amination step, greater overall yield, and operational simplicity. Coupling of PDQ to a D-tyrosine derivative effectively produced over one half of the total molecular structure of olcegepant. A unique tandem deprotection-nucleophilic addition sequence was also applied to the coupling of Fmoc-PDQ with phenyl isocyanate.

1,2,4 -TRIAZOLES AS ALLOSTERIC MODULATORS OF MGLU5 RECEPTOR ACTIVITY FOR THE TREATMENT OF SCHIZOPHRENIA OF DEMENTIA

This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.

NOVEL COMPOUNDS

This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.

Process for preparing 1- [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine

The present application relates to a process for preparing the CGRP-antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine of formula by means of which this compound can be prepared in large amounts, in high yields and with high purity.

METHOD FOR THE PRODUCTION OF 1-[N2-[3,5-DIBROMO-N-[[4-(3,4-DIHYDRO-2(1H)-OXOQUINAZOLINE-3-YL)-1-PIPERIDINYL]CARBONYL]-D-TYROSYL]-L-LYSYL]-4-(4-PYRIDINYL)-PIPERAZINE

The invention relates to a method for producing the CGRP antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazoline-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-Iysyl]-4-(4-pyridinyl)-piperazine of formula (I). The disclosed method allows said compound to be produced in great quantities, at great yields, and at a high degree of purity.

Synthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents

A series of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines were synthesized and tested for antihypertensive activity. Among the compounds tested, 1-(2-hydroxy-2-phenethyl)-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl) piperidine derivatives were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model. Of these, 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(1,2,3,4-tetrahydro-2-oxo-3- quinazolinyl)piperidine (KF5908) seemed the most promising.

Piperidine derivatives and pharmaceutical compositions containing same

A new piperidine derivative represented by the formula: STR1 wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); m and n are 0 or 1, and are