866087-24-3

Basic information

• Product Name: 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester
• Synonyms: 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester
• CAS NO: 866087-24-3
• Molecular Weight: 571.673
• Mol File: 866087-24-3.mol

Chemical Properties

• CAS DataBase Reference: 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester(866087-24-3)
• EPA Substance Registry System: 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester(866087-24-3)

Safety Data

• Hazardous Substances Data: 866087-24-3(Hazardous Substances Data)

Upstream product

• 100-44-7 benzyl chloride 
• 1117699-25-8 (2Z)-3-(4-benzyloxy-3,5-dimethyl-phenyl)-2-(tetrahydro-pyran-2-yloxy)acrylic acid monopotassium salt 
• 1117699-24-7 ethyl (2Z)-3-(4-benzyloxy-3,5-dimethyl-phenyl)-2-(tetrahydropyran-2-yloxy)acrylate 
• 866087-23-2 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-benzyloxy-3,5-dimethyl-phenyl)-1-methoxycarbonyl-ethyl ester 
• 1007587-76-9 1-(1H-imidazol-1-yl-carbonyl)-4-(1,2,4,5-tetrahydro-2-oxo-3H-1,3-benzodiazepin-3-yl)-piperidine 
• 1007587-75-8 (αR)-α-hydroxy-3,5-dimethyl-4-(phenylmethoxy)-phenylpropionic acid monosodium salt 
• 910575-44-9 (R)-3-(4-benzyloxy-3,5-dimethyl-phenyl)-2-hydroxy-propionic acid 
• 866087-19-6 (Z,E)-2-acetylamino-3-(4-benzyloxy-3,5-dimethyl-phenyl)-acrylic acid methyl ester 
• 866087-20-9 3-(4-benzyloxy-3,5-dimethyl-phenyl)-2-oxo-propionic acid 
• 866087-22-1 (R)-3-(4-Benzyloxy-3,5-dimethyl-phenyl)-2-hydroxy-propionic acid methyl ester 
• 168196-87-0 2-benzyloxy-5-bromo-1,3-dimethylbenzene 

Downstream Products

• 866087-25-4 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-hydroxy-3,5-dimethyl-phenyl)-1-carboxy-ethyl ester 
• 930604-23-2 (R)-1-(4-benzyloxy-3,5-dimethyl-benzyl)-2-(4-ethoxycarbonylmethoxy-1,4'-bipiperidinyl-1'-yl)-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate 
• 930604-18-5 (R)-1-(4-benzyloxy-3,5-dimethyl-benzyl)-2-(1'-ethoxycarbonylmethyl-4,4'-bipiperidinyl-1-yl)-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate 
• 910575-45-0 4-(2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-piperidine-1-carboxylic acid (R)-2-(4-hydroxy-3,5-dimethyl-phenyl)-1-methoxycarbonyl-ethyl ester 

Relevant articles and documents

NOVEL PREPARATION PROCESS

A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.

SYNTHESIS OF INTERMEDIATES USEFUL FOR THE PRODUCTION OF CERTAIN CGRP INHIBITORS AND INTERMEDIATES USED IN SUCH SYNTHESIS

A method for making the compound of the formula (I), (IV), (VI), (VII) and (VIII), wherein R1 is C-1-5-alkyl, C(O)-O benzyl, C(O)-O-tert.butyl or benzyl; and R2 is C1-C6 alkyl.

Selected Cgrp-Antagonists, Processes for Preparing Them and Their Use as Pharmaceutical Compositions

The invention relates to CGRP-antagonists of general formula (I), wherein R1, R2, R3, R4 and R5 are defined in claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures salts and salt hydrates thereof, in particular to 10 salts thereof, which are physiologically compatible with acids or inorganic or organic bases and to compounds of general formula (I), wherein one or several hydrogen atoms are substituted by deuterium. Drugs containing said compounds, the use thereof and a method for the production thereof are also disclosed.

Production Method

The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.

Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions

The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

CGRP ANTAGONISTS, METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE AS MEDICAMENTS

The invention relates to CGRP antagonists of general formula (I) in which: R1, R2, R3, R4 and X are defined as in Claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts as well as the hydrates of the salts, in particular, their physiologically compatible salts with inorganic or organic acids and bases, and those compounds of general formula (I) in which one or more hydrogen atoms are replaced by deuterium. The invention also relates to medicaments containing these compounds, the use thereof, and to methods for producing them.

2-OXO-1,2,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-3-YL-PIPERIDINES USED AS CGRP ANTAGONISTS

The invention relates to novel CGRP antagonists of general formula (I), in which B, R1 and R2 are defined as cited in claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts, in addition to the hydrates of their salts, in particular their physiologically compatible salts, with inorganic or organic acids or bases. The invention also relates to medicaments containing said compounds, to their use and to a method for their production.

SELECTED CGRP ANTAGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICAMENTS

The invention relates to CGRP antagonists of general formula (I), in which A, X, D, E, G, M, Q and R1 to R3 are defined as in Claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and their salts as well as the hydrates of the salts, particularly their physiologically compatible salts having inorganic or organic acids, to medicaments containing these compounds, to their use, and to methods for the production thereof.