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1. WO2015038022 - PROCESSES FOR PREPARING MEDICAMENTS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES AND INTERMEDIATES FOR USE THEREIN

Publication Number WO/2015/038022
Publication Date 19.03.2015
International Application No. PCT/PT2014/000061
International Filing Date 12.09.2014
IPC
C07D 311/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
06with oxygen or sulfur atoms directly attached in position 2
08not hydrogenated in the hetero ring
12substituted in position 3 and unsubstituted in position 7
C07D 311/20 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
06with oxygen or sulfur atoms directly attached in position 2
20hydrogenated in the hetero ring
CPC
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
C07C 51/41
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
51Preparation of carboxylic acids or their salts, halides or anhydrides
41Preparation of salts of carboxylic acids
C07D 311/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
06with oxygen or sulfur atoms directly attached in position 2
08not hydrogenated in the hetero ring
12substituted in position 3 and unsubstituted in position 7
C07D 311/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
06with oxygen or sulfur atoms directly attached in position 2
20hydrogenated in the hetero ring
C07D 311/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
58other than with oxygen or sulfur atoms in positions 2 or 4
Applicants
  • BIAL - PORTELA & CA., S.A. [PT]/[PT]
Inventors
  • RUSSO, Domenico
  • WAHNON, Jorge
  • MATON, William
  • WEBER, Beat T.
  • JERÓNIMO, Paula
  • SOUSA, Luísa
  • BARROCAS, Pedro
  • PIRES, Rita
  • LIMA, Ricardo
  • VASCONCELOS, Teófilo
Agents
  • MOREIRA, Pedro Alves
Priority Data
1316410.813.09.2013GB
1320366.618.11.2013GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES FOR PREPARING MEDICAMENTS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES AND INTERMEDIATES FOR USE THEREIN
(FR) PROCÉDÉS DE PRÉPARATION DE MÉDICAMENTS POUR LE TRAITEMENT DE MALADIES CARDIOVASCULAIRES ET INTERMÉDIAIRES PRÉVUS À CET EFFET
Abstract
(EN) The present invention provides a compound of formula N wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-ß-hydroxylase.
(FR) Cette invention concerne un composé de formule N où : X est CH2, un atome d'oxygène ou de soufre; R1, R2 et R3 sont identiques ou différents et désignent des atomes d'hydrogène, des atomes d'halogène, ou un groupe alkyle, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino ou dialkylamino, N étant sous la forme de l'énantiomère R et S individuel ou d'un mélange de l'énantiomère (R) et (S). La présente invention concerne également un composé de formule MA. Des procédés de préparation des composés ci-dessus, et des procédés impliquant leur utilisation sont en outre décrits. Les composés selon l'invention sont particulièrement utiles en tant qu'intermédiaires dans la synthèse d'inhibiteurs sélectifs au niveau périphérique de dopamine-ß-hydroxylase.
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