Patent ID: 8835653
Filing Date: 2014-09-16
Classification: A61P,C07D

Abstract:
1. A compound of formula Ia, wherein is a thiophenyl residue, X is halogen; R1 and R3 are selected from H, halogen, (C R2 is a 5- or 6-membered lactam ring optionally substituted one, two, or three times by R8; R4 and R5 are the same or different and are independently of one another 1) hydrogen atom, 2) —(C 3) —(C 4) —SO 5) —(C 6) —(C 7) —O—(C 8) —(C R4 and R5 together with the nitrogen atom to which they are bonded form a 4- to 10-membered mono- or bicyclic heterocyclic ring selected from 2-oxa-5-aza-bicyclo[2.2.1]heptane, azepane, azepine, azetidine, 2,5-diaza-bicyclo[2.2.1]heptane, 1,4-diazepane, 1,2-diazepine, 1,3-diazepine, 1,4-diazepine, 2,3-dihydro-1H-isoindole, 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine, 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine, 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole, dioxazole, dioxazine, imidazole, imidazoline, imidazolidine, isothiazole, isothiazolidine, isothiazoline, isoxazole, isoxazoline, isoxazolidine, 2-isoxazoline, morpholine, octahydro-pyrido[1,2-a]pyrazine, octahydro-pyrrolo[3,4-b]pyridine, octahydro-pyrrolo[1,2-a]pyrazine, [1,4]oxazepane, 1,4-oxazepine, oxazole, piperazine, piperidine, piperidinone, pyrazine, pyrazole, pyrazoline, pyrazolidine, pyridazine, pyridine, pyridone, pyrimidine, pyrrole, pyrrolidine, pyrrolidinone, pyrroline, 4,5,6,7-tetrahydro-1H-imidazo[4,3-c]pyridine, tetrahydropyridine, 1,4,5,6-tetrahydro-pyrrolo[3,4-c]pyrazole, 4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine, tetrazine, tetrazole, thiazole, thiadiazole, thiazolidine, thiazoline, thiomorpholine, thiophene, 1,2,3-triazine, 1,2,4-triazine, 1,3,5-triazine, 1,2,3-triazole and 1,2,4-triazole, wherein said heterocyclic ring is unsubstituted or mono-, di- or trisubstituted independently of one another by R7; R6 is: 1) heterocyclyl, wherein heterocyclyl is as defined above and is un-substituted or mono-, di- or tri substituted independently of one another by R8, or R7 is halogen, —NO R8 is halogen, —NO R10 and R20 are the same or different and are independently of one another hydrogen atom, halogen, —(C R16 is selected from hydrogen atom, —OH, and —O—(C or a stereoisomeric form thereof, or a physiologically tolerable salt of any of these.