Abstract:
The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.
Abstract:
Die vorliegende Erfindung betrifft Guanidinverbindungen der allgemeinen Formel (I) entsprechende enantiomere, diastereomere und/oder tautomere Formen davon sowie pharmazeutisch annehmbare Salze davon. Weiterhin betrifft die vorliegende Verbincaung die Verwendung von Guanidinverbindungen als Bindungspartner für 5-HT5-Rezeptoren zur Behandlung von Krankheiten, die durch eine 5-HT5-Rezeptoraktivität moduliert werden, insbesondere zur Behandlung von neurodegenerativen und neuropsychiatrischen Störungen sowie den damit zusammenhängenden Anzeichen, Symptomen und Fehlfunktionen.
Abstract:
The invention describes compounds of formula (I), where A is an oxygen atom or a NH group; B is the radical -Zm-(CHQ)p-(CH=CH)q-(CH2)r-P, where Z is a -CO- group or -SO2-group, m is 0 or 1, p is 0, 1 or 2, q is 0, 1 or 2, r is 0, 1 or 2, Q is a hydrogen atom, a C1-4 alkyl radical, a carboxyl-, carboxamido- or carboxy-C1-4 alkyl group, and P is a hydrogen atom, an indolyl radical, or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkyl groups, and/or a C1-2 alkylenedioxy group; D is an amino-, hydroxy-, C1-4 alkoxy, C1-4 alkylamino-, aryl-C1-4 alkylenoxy- or aryl-C1-4 alkyleneamino, where the aryl radicals represent a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; X is a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; Y is a hydrogen atom, a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group, or X and Y together represent a -(CH2)s group, where s is 3, 4 or 5, and 1 or 2 hydrogen atoms can be replaced by methyl groups, and n is 0 or 1, and possibly their salts with physiologically tolerable acids and bases. The compounds can be used to combat diseases.
Abstract:
Die vorliegende Erfindung betrifft neue Carbamat-substituierte Oxindol-Derivate der Formel (I), diese enthaltende pharmazeutische Mittel und ihre Verwendung zur Behandlung von Vasopressin-abhängigen Erkrankungen, worin R 1 für Wasserstoff, Methoxy oder Ethoxy steht; R 2 für Wasserstoff oder Methoxy steht; R 3 für Wasserstoff, Methyl, Ethyl, n-Propyl oder Isopropyl steht; X 1 und X 2 für N oder CH stehen, unter der Maßgabe, dass X 1 und X 2 nicht gleichzeitig für N stehen.
Abstract translation:本发明涉及式(I)的新的氨基甲酸酯取代的羟吲哚衍生物,含有它们和它们用于治疗加压素依赖性疾病的方法,其中R1是氢,甲氧基或乙氧基的药物组合物; R 2是氢或甲氧基; R3是氢,甲基,乙基,正丙基或异丙基; X1和X2是N或CH,条件是X1和X2不同时为N.条件
Abstract:
The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. formula (I) wherein R is a moiety of the formula (R) wherein A, R 1 to R 4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; R a , R b are independently selected from the group consisting of halogen, CN, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C(O)R aa , C(O)NR cc R bb and NR cc R bb ; X is CH 2 , C(O), S, S(O) or S(O) 2 ; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar 1 , Ar 2 -Ar 3 or Ar 2 -O-Ar 3 , wherein Ar 1 , Ar 2 and Ar 3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents R x , wherein and physiologically tolerated acid addition salts and the N-oxides thereof.
Abstract:
The present invention relates to novel oxindole derivatives of the formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.
Abstract:
Die vorliegende Erfindung betrifft neue Oxindol-Derivate der allgemeinen Formel (I), worin die Substituenten R 1 , R 2 , A, B und Y wie in Anspruch 1 definiert sind, diese enthaltende Arzneimittel und deren Verwendung zur Prophylaxe und/oder Behandlung von Vasopressin-abhängigen und/oder Oxytocin-abhängigen Krankheiten.
Abstract:
The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.
Abstract:
Die Erfindung betrifft 5-Ring-Heteroaromaten-Verbindungen der allgemeinen Formel (I) deren Verwendung zur Behandlung und/oder Prophylaxe von Krankheiten, und diese enthaltende Arzneimittel.
Abstract:
Die vorliegende Erfindung betrifft neue Oxindol-Derivate der allgemeinen Formel (I), worin die Substituenten R 1 , R 2 , A, B und Y wie in Anspruch 1 definiert sind, diese enthaltende Arzneimittel und deren Verwendung zur Prophylaxe und/oder Behandlung von Vasopressin-abhängigen und/oder Oxytocin-abhängigen Krankheiten.