Processing

Please wait...

Settings

Settings

Goto Application

1. EP0882051 - THIOPHENOPYRIMIDINES

Office
European Patent Office
Application Number 97904368
Application Date 30.01.1997
Publication Number 0882051
Publication Date 09.12.1998
Publication Kind B1
IPC
A61P 5/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
02of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
04for decreasing, blocking or antagonising the activity of the hypothalamic hormones
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61P 5/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
02of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
04for decreasing, blocking or antagonising the activity of the hypothalamic hormones
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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
C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants JANSSEN PHARMACEUTICA NV
NEUROCRINE BIOSCIENCES INC
Inventors CHEN CHEN
WEBB THOMAS R
MCCARTHY JAMES R
MORAN TERENCE J
Designated States
Priority Data 9700457 30.01.1997 EP
1127496 07.02.1996 US
2768996 08.10.1996 US
Title
(DE) THIOPHENOPYRIMIDINE
(EN) THIOPHENOPYRIMIDINES
(FR) THIOPHENOPYRIMIDINES
Abstract
(EN)
This invention concerns compounds of formula (I) including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6 alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of the formula: -Alk-O-CO-Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is a phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

(FR)
L'invention concerne des composés représentés par la formule (I) comprenant les stéréoisomères, ainsi que leurs sels d'addition d'acide acceptables sur le plan pharmaceutique, dans laquelle X représente S, SO ou SO2; R1 représente NR4R5 ou OR5; R2 représente alkyle C1-6, alkyloxy C1-6 ou alkylthio C1-6; R3 représente hydrogène, alkyle C1-6, alkylsulfonyle C1-6, alkylsulfoxy C1-6 ou alkylthio C1-6; R4 représente hydrogène, alkyle C1-6, mono- ou di(cycloalkyle C3-6)méthyle, cycloalkyle C3-6, alcényle C3-6, hydroxyalkyle C1-6, alkyl C1-6 carbonyloxyalkyle C1-6 ou alkyl C1-6 oxyalkyle C1-6; R5 représente alkyle C1-8, mono- ou di(cycloalkyle C3-6)méthyle, Ar1CH2, alkyl C1-6 oxyalkyle C1-6, hydroxyalkyle C1-6, alcényle C3-6, thiénylméthyle, furanylméthyle, alkyl C1-6 thioalkyl C1-6, morpholinyle, mono- ou di(alkyle C1-6) aminoalkyle C1-6, di(alkyle C1-6)amino, alkyl C1-6 carbonylalkyle C1-6, alkyle C1-6 substitué par imidazolyle; ou un radical représenté par la formule -Alk-O-CO-Ar1; ou R4 et R5 avec l'atome d'azote auquel ils sont fixés peuvent constituer conjointement un groupe pyrrolidinyle, pipéridinyle, homopipéridinyle ou morpholinyle éventuellement substitué; Ar représente phényle, phényle substitué, pyridinyle ou pyridinyle substitué; ces composés possédant des propriétés antagonistes du récepteur de CRF; l'invention concerne également des compositions pharmaceutiques contenant ces composés en tant qu'ingrédients actifs ainsi que des procédés servant à traiter des maladies relatives à l'hypersécrétion de CRF, telles que la dépression, l'anxiété, la toxicomanie, au moyen de l'administration d'une quantité efficace d'un composé représenté par la formule (I).