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1. MYPI 97000490 - THIOPHENOPYRIMIDINES

Office
Malaysia
Application Number PI 97000490
Application Date 06.02.1997
Publication Number PI 97000490
Publication Date 10.04.2008
Publication Kind A
IPC
A61K 31/505
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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 N.V.
NEUROCRINE BIOSCIENCES INC.
Inventors JAMES R. MCCARTHY
CHEN CHEN
TERENCE J. MORAN
THOMAS R. WEBB
Agents DATO' V.L. KANDAN
Priority Data 60/011274 07.02.1996 US
60/027689 08.10.1996 US
Title
(EN) THIOPHENOPYRIMIDINES
Abstract
(EN)
THIS INVENTION CONCERNS COMPOUNDS OF FORMULA( FORMULA 1 )INCLUDING THE STEREOISOMERS AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT FORMS THEREOF, WHEREIN X IS S, SO OR SO2; R1 IS NR4R5 OROR5; 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-C1-6ALKYLOXY-C1-6ALKYL, HYDROXYC1-6ALKYL,C3-6ALKENYL, THIENYLMETHYL, FURANYLMETHYL, C1-6ALKYLTHIOC1-6ALKYL, MORPHOLINYL, MONO- OR DI(C1-6ALKYL)AMINOC1-6ALKYL, DI(C1-6ALKYL)AMINO, C1-6ALKYLCARBONYLC1-6ALKYL, C1-6ALKYL SUBSTITUTED WITH IMIDAZOLYL; OR A RADICAL OF 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 PHENYL, SUBSTITUTED PHENYL, PYRIDNYL OR SUBSTITUTED PYRIDINYL; HAVING CRF RECEPTOR ANTAGONISTIC PROPERTIES; PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS AS ACTIVE INGREDIENTS; METHOD OF TREATING DISORDERS RELATED TO HYPERSECRETION OF CRF SUCH ASD DEPRESSION, ANXIETY, SUBSTANCE ABUSE, BY ADMINISTERING AN EFFECTIVE AMOUNT OF A COMPOUND OF FORMULA (I).