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1. WO1997045111 - PHENYL DERIVATIVES USEFUL AS BLOCKERS OF CHLORIDE CHANNELS

Publication Number WO/1997/045111
Publication Date 04.12.1997
International Application No. PCT/EP1997/002724
International Filing Date 26.05.1997
Chapter 2 Demand Filed 23.12.1997
IPC
A61K 31/155 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
155Amidines , e.g. guanidine , isourea , isothiourea
A61K 31/17 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
17having the group N-C(O)-N or N-C(S)-N, e.g. urea, thiourea, carmustine
C07C 233/55 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
45having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
53with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
55having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
C07C 271/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
40having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
58with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
C07C 275/40 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
275Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
40being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 309/51 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
309Sulfonic acids; Halides, esters, or anhydrides thereof
01Sulfonic acids
28having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
45containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
51at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
CPC
A61K 31/155
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
A61K 31/17
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
17having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
A61P 1/00
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
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/12
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
12Antidiarrhoeals
A61P 27/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
Applicants
  • NEUROSEARCH A/S [DK]/[DK] (AllExceptUS)
  • CHRISTOPHERSEN, Palle [DK]/[DK] (UsOnly)
  • PEDERSEN, Ove [DK]/[DK] (UsOnly)
Inventors
  • CHRISTOPHERSEN, Palle
  • PEDERSEN, Ove
Agents
  • GRÜNECKER, KINKELDEY, STOCKMAIR & SCHWANHÄUSSER
Priority Data
0602/9624.05.1996DK
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PHENYL DERIVATIVES USEFUL AS BLOCKERS OF CHLORIDE CHANNELS
(FR) DERIVES PHENYLIQUES SERVANT D'ANTAGONISTES DES CANAUX CHLORURE
Abstract
(EN)
The present invention relates to a method for the treatment of a disorder or disease of a living animal body, including a human, which disorder or disease is responsive to the blockade of chloride channels, comprising administering to a living animal body in need thereof a therapeutically effective amount of a compound having formula (I) or a pharmaceutically acceptable salt thereof wherein R2, R3, R4 and R5 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl or heteroaryl group may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4 to 7 membered carbocyclic ring which may be unsaturated, or partially or fully saturated while the other substituents R2, R3, R4 and R5 is as defined above; Y is -CO-, -CS-, -SO2-, or -C(=N-R8)-, wherein R8 is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, -SO2-NH-, or -CH2-; Z is -NR6-, -O-, -CH=CH-, -N=CH-, -CH=N-, or -NR6-CH2-, wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl or heteroaryl group may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 and R13, R13 and R14 or R14 and R15 together form a fused 4 to 7 membered carbocyclic ring which may be unsaturated, or partially or fully saturated while the other substituents R11, R12, R13, R14 and R15 is as defined above.
(FR)
La présente invention concerne une méthode pour traiter les troubles ou les affections du corps d'un animal vivant, y compris un être humain, lesdits troubles ou affections réagissant au blocage des canaux chlorure. Ladite méthode consiste à administrer à un animal vivant nécessitant un tel traitement, une quantité efficace sur le plan thérapeutique d'un composé de formule (I), ou d'un sel pharmaceutiquement acceptable dudit composé. Dans la formule, R2, R3, R4 et R5 sont sélectionnés indépendamment l'un de l'autre parmi: hydrogène, alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, alcoxy, hydroxy, halogène, trifluorométhyle, trifluorométhoxy, cyano, nitro, amino, et aryle, aralkyle, arylamino, aryloxy, aryl-CO-, ou hétéroaryle, où le groupe aryle ou hétéroaryle peut être substitué une ou plusieurs fois par des substituants sélectionnés parmi alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, hydroxy, alcoxy, halogène, trifluorométhyle, trifluorométhoxy, cyano, nitro et amino; où R3 et R4 ou R4 et R5 forment conjointement un noyau carbocyclique condensé comportant 4 à 7 chaînons, pouvant être insaturé, ou partiellement ou totalement saturé, tandis que les autres substituants R2, R3, R4 et R5 ont la signification mentionnée ci-dessus; Y représente -CO-, -CS-, -SO2-, ou -C(=N-R8)-, où R8 représente hydrogène, alkyle ou cyano; X représente -NH-, -CH2-NH-, -SO2-NH-, ou -CH2-; Z représente -NR6-, -O-, -CH=CH-, -N=CH-, -CH=N-, ou -NR6-CH2-, où R6 représente hydrogène ou alkyle; R11, R12, R13, R14 et R15 sont sélectionnés indépendamment l'un de l'autre parmi: hydrogène, alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, alcoxy, hydroxy, halogène, trifluorométhyle, trifluorométhoxy, cyano, nitro, amino, et aryle, aralkyle, arylamino, aryloxy, aryl-CO-, ou hétéroaryle, où le groupe aryle ou hétéroaryle peut être substitué une ou plusieurs fois par des substituants sélectionnés parmi alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, hydroxy, alcoxy, halogène, trifluorométhyle, trifluorométhoxy; cyano; nitro et amino; où l'un des éléments R11 et R12, ou R12 et R13, R13 et R14, ou R14 et R15 forment conjointement un noyau carbocyclique condensé comportant 4 à 7 chaînons, pouvant être insaturé, ou partiellement ou totalement saturé, tandis que les autres substituants R11, R12, R13, R14 et R15 ont la signification mentionnée ci-dessus.
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