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1. WO2000002859 - N-SUBSTITUTED NAPHTHALENE CARBOXAMIDES AS NEUROKININ-RECEPTOR ANTAGONISTS

Publication Number WO/2000/002859
Publication Date 20.01.2000
International Application No. PCT/GB1999/002178
International Filing Date 07.07.1999
Chapter 2 Demand Filed 19.01.2000
IPC
C07C 235/66 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
66with carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
C07C 255/57 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
49having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
57containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
C07D 211/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 211/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
20with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
22by oxygen atoms
C07D 211/24 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
20with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
24by sulfur atoms to which a second hetero atom is attached
C07D 211/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
26with hydrocarbon radicals, substituted by nitrogen atoms
CPC
A61P 1/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
08for nausea, cinetosis or vertigo; Antiemetics
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 25/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
22Anxiolytics
A61P 25/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
24Antidepressants
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
C07C 235/66
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
66with carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
Applicants
  • ASTRAZENECA AB [SE]/[SE] (AllExceptUS)
  • BERNSTEIN, Peter, Robert [US]/[US] (UsOnly)
  • DEDINAS, Robert, Frank [US]/[US] (UsOnly)
  • RUSSELL, Keith [GB]/[US] (UsOnly)
  • SHENVI, Ashokkumar, Bhikkappa [US]/[US] (UsOnly)
Inventors
  • BERNSTEIN, Peter, Robert
  • DEDINAS, Robert, Frank
  • RUSSELL, Keith
  • SHENVI, Ashokkumar, Bhikkappa
Agents
  • DENERLEY, Paul, Millington
Priority Data
9814886.910.07.1998GB
9821699.707.10.1998GB
9821703.707.10.1998GB
9909840.230.04.1999GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) N-SUBSTITUTED NAPHTHALENE CARBOXAMIDES AS NEUROKININ-RECEPTOR ANTAGONISTS
(FR) NAPHTALENE CARBOXAMIDES N-SUBSTITUES EN TANT QU'ANTAGONISTES DE RECEPTEURS DES NEUROKININES
Abstract
(EN)
A compound of formula (I) wherein: R is alkyl; R1 is optionally substituted phenyl, 2-oxo-tetrahydro-1(2H)-pyrimidinyl, or 2-oxo-1-piperidinyl; R2 is hydrogen, alkoxy, alkanoyloxy, alkoxycarbonyl, alkanoylamino, acyl, alkyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl where the alkyl groups are the same or different, hydroxy, thioacyl, thiocarbamoyl, N-alkylthiocarbamoyl, or N,N-dialkylthiocarbamoyl where the alkyl groups are the same or different. X1 and X2 are independently hydrogen or halo, provided that at least one of X1 or X2 is halo; and R3, R4, R5, and R6 are independently hydrogen, cyano, nitro, trifluoromethoxy, trifluoromethyl, or alkylsulfonyl are antagonists of at least one tachykinin receptor and are useful in the treatment of depression, anxiety, asthma, pain, inflammation, urinary incontinence and other disease conditions. Processes for their preparation are described, as are compositions containing them and their use.
(FR)
L'invention concerne un composé de formule (I) dans laquelle R désigne un alkyle; R1 désigne un phényle éventuellement substitué, 2-oxo-tétrahydro-1(2H)- pryimidinyle ou 2-oxo-1-pipéridinyle; R2 désigne un hydrogène, alcoxy, alcanoyloxy, alcoxycarbonyle, alcanoylamino, aclye, alkyle, carbamoyle, N-alkylcarbamoyle, N,N-dialkylcarbamoyle où les groupes alkyles, identiques ou différents, désignent un hydroxy, thioacyle, thiocarbamoyle, N-alkylthiocarbamoyle ou N,N-dialkylthiocarbamoyle. X1 et X2 désignent indépendamment un hydrogène ou halo, à condition qu'au mois un des X1 ou X2 désigne un halo; et R3, R4, R5 et R6 désignent indépendamment un hydrogène, cyano, nitro, tribluorométhoxy, trifluorométhyle ou alkylesulfonyle, désignent des antagonistes d'au moins un récepteur de la tachykinine et sont utiles dans le traitement de la dépression, l'anxiété, l'asthme, la douleur, les inflammations, l'incontinence urinaire et d'autres pathologies. Font aussi l'objet de cette invention leurs procédés de préparation et les compositions les contenant ainsi que leur utilisation.
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