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Application filed by Yamanouchi Pharmaceutical Co., Ltd.filedCriticalYamanouchi Pharmaceutical Co., Ltd.
Priority claimed from YU19890Aexternal-prioritypatent/YU47555B/en
Publication of SI9010198ApublicationCriticalpatent/SI9010198A/en
Publication of SI9010198BpublicationCriticalpatent/SI9010198B/en
Pharmaceuticals Containing Other Organic And Inorganic Compounds
(AREA)
Claims (8)
PATENTNI ZAHTEVKI 1. Tetrahidrobenzimidazolni derivat, označen s tem, da ima formulo (I): IIA tetrahydrobenzimidazole derivative characterized in that it has the formula (I): IIo kjer Het pomeni člana, izbranega iz skupine, ki jo sestavljajo pirolidin, piperidin, piperazin, morfolin, pirol, furan, tiofen, imidazol, oksazol, tiazol, pirazol, izoksazol, izotiazol, triazol, tiadiazol, oksadiazol, piridin, piridazin, pirimidin, pirazin, 4H-ciklopentatiazol, indol, izoindol, 2,3-dihidroindol, (indolin), izoindolin, hidroksiindol, indazol, indolizin, benzotiofen, benzofuran, benzotiazol, benzimidazol, benzooksazol, 4,5,6,7-tetrahidrobenzotiofen, 2,3-dihidrobenzimidazol-2-on, kinolin, izokinolin, 1,2,3,4-tetrahidrokinolin, 1,2,3,4-tetrahidroizokinolin, 1,4-benzoksazin, fenotiazin, karbazol in /3-karbolin in kjer je Het lahko substituiran z enim do tri substituenti, izbranimi iz skupine, ki jo sestavljajo nižji alkil, nižji alkenil, nižji alkinil, cikloalkil-nižji alkil, ar alkil, nižji alkoksi, nitro, hidroksil, nižji alkoksikarbonil in halo; in X pomeni enojno vez ali -ΝΗ-, ki je vezan na atom ogljika ali dušika heterocikličnega obroča navedenega Het, ali njegova farmacevtsko sprejemljiva sol.o wherein Het means a member selected from the group consisting of pyrrolidine, piperidine, piperazine, morpholine, pyrrole, furan, thiophene, imidazole, oxazole, thiazole, pyrazole, isoxazole, isothiazole, triazole, thiadiazole, oxadiazole, pyridine, pyridine, pyridine , pyrazine, 4H-cyclopentathiazole, indole, isoindole, 2,3-dihydroindole, (indoline), isoindoline, hydroxyindole, indazole, indolizine, benzothiophene, benzofuran, benzothiazole, benzimidazole, benzooxazole, 4,5,6,7-tetrahydrobenzo , 3-dihydrobenzimidazol-2-one, quinoline, isoquinoline, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroisoquinoline, 1,4-benzoxazine, phenothiazine, carbazole and N-carboline, and wherein Het may be substituted with one to three substituents selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl-lower alkyl, aryl alkyl, lower alkoxy, nitro, hydroxyl, lower alkoxycarbonyl and halo; and X represents a single bond or -ΝΗ- which is attached to a carbon or nitrogen atom of the heterocyclic ring of said Het, or a pharmaceutically acceptable salt thereof.2. Spojina po zahtevku 1, označena s tem, da ima Het formulo:Compound according to Claim 1, characterized in that Het has the formula:kjer R1 pomeni vodik, nižji alkil, nižji alkenil, nižji alkinil, cikloalkil-nižji alkil ali aralkil; R2 pomeni vodik, nižji alkil ali aralkil; in R1 pomeni vodik, nižji alkoksi, nitro, hidroksil, nižji alkoksikarbonil ali halo; in X pomeni enojno vez. 1 Spojina po zahtevku 1, označena s tem, da Het pomeni heterociklično skupino, ki vsebuje dušik in je X enojna vez, vezana na atom dušika heterocikličnega obroča, ki vsebuje dušik.wherein R 1 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl-lower alkyl or aralkyl; R 2 represents hydrogen, lower alkyl or aralkyl; and R 1 represents hydrogen, lower alkoxy, nitro, hydroxyl, lower alkoxycarbonyl or halo; and X represents a single bond. Compound according to Claim 1, characterized in that Het represents a nitrogen-containing heterocyclic group and X is a single bond attached to the nitrogen atom of the nitrogen-containing heterocyclic ring.4. Spojina po zahtevku 2, označena s tem, da je 5-[(l-metilindol-3-il)karbonil]-4,5,6,7-tetrahidrobenzimidazol.Compound according to Claim 2, characterized in that 5 - [(1-methylindol-3-yl) carbonyl] -4,5,6,7-tetrahydrobenzimidazole.5. Spojina po zahtevku 4, označena s tem, daje (R)-spojina.Compound according to Claim 4, characterized in that it is an (R) -compound.6. Spojina po zahtevku 4, označena s tem, da je (S)-spojina.Compound according to Claim 4, characterized in that it is an (S) -compound.7. Spojina po zahtevku 2, označena s tem, da je 5-[[l-(2-propinil)indol-3-il]karbonil]-4,5,6,7-tetrahidrobenzimidazol.A compound according to claim 2, characterized in that 5 - [[1- (2-propynyl) indol-3-yl] carbonyl] -4,5,6,7-tetrahydrobenzimidazole.8. Spojina po zahtevku 3, označena s tem, da je 5-[(2,3-dihidroindol-l-il)karbonil]-4,5,6,7-tetrahidrobenzimidazol.Compound according to Claim 3, characterized in that 5 - [(2,3-dihydroindol-1-yl) carbonyl] -4,5,6,7-tetrahydrobenzimidazole.9. Spojina po zahtevku 3, označena s tem, daje l-[(4,5,6,7-tetrahidrobenzimidazol--5-il)karbonil]-2,3-dihidrobenzimidazol-2-on. Za YAMANOUCHIPHARMACEUTICAL CO., Ltd.:Compound according to Claim 3, characterized in that 1 - [(4,5,6,7-tetrahydrobenzimidazol-5-yl) carbonyl] -2,3-dihydrobenzimidazol-2-one. For YAMANOUCHIPHARMACEUTICAL CO., Ltd .:PATENTNA PISARNA, d.o.o. LJUBLJANA, ČOPOVA 14PATENT OFFICE, d.o.o. LJUBLJANA, ČOPOVA 14
SI9010198A1989-02-021990-02-02Derivatives of tetrahydrobenzimidazole and process for their preparation
SI9010198B
(en)
1-Aryl-3-tetrahydropyridyl, 1-aryl-3-piperidyl or 1-aryl-3-piperazinyl-indole derivatives, process for their preparation and pharmaceutical compositions containing these compounds
Piperidin-3-yl or (1,2,5,6-tetrahydro-pyrid-3-yl) -substituted heterocyclic compounds, pharmaceutical compositions thereof, and methods for their preparation
METHOD FOR INHIBITING ONE OR MORE ACTIVITIES OF PROTEINIC KINASE, COMPOSED OF 2 - PIRAZOLIN-5-ONA PROTEINIC QUINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION THAT INCLUDES IT
indol derivative or a pharmaceutically acceptable salt thereof, pharmaceutical composition, use of a (indol-3-yl) heterocycle derivative, and method of treating pain