C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/218, 260/242
C07D 471/14 (2006.01) C07D 487/04 (2006.01) C07D 487/14 (2006.01) C07D 491/14 (2006.01) C07D 495/14 (2006.01)
Patent
CA 1288097
21489-7012 4-15519/1+2/CGC 1151 2-SUBSTITUTED-e-FUSED[1,2,4]TRIAZOLO[1,5-c]PYRIMIDINES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF Abstract of the Disclosure Compounds of the formulae Ia, Ib and Ic Image (Ia) (Ib) (Ic) wherein X is O, S, NH or NR; R is alkyl, alkenyl, alkynyl, cycloalkyl, aromatic-ring-alkyl all of which may be optionally interrupted by a herero atom; OH; an aromatic ring; or the group -C(=NH)-NH2; R1 is optionally substituted and selected from a carboxylic aromatic and a heterocyclic group which heterocyclic group is aromatic, partially saturated or fully saturated, the optional substituent of R2 being halogen, alkyl, haloalkyl, OH, alkoxy, hydroxyalkyl, amino, mono- or di-alkylamino, carbalkoxy, carbamoyl and alkylcarbamoyl; R2 is H, alkyl, hydroxy-C2-C4-alkyl, alkenyl, arylalkyl, or arylalkenyl; A is a bivalent bridging group containing chain atoms selected from C, O, N and S thus forming together with the two adjacent carbon atoms to which the chain is attached a mono- or bicyclic carbocyclic or heterocyclic group with the proviso that a monocyclic group formed by A is saturated or partially saturated and that the ring moiety adjacent to the triazolopyrimidine structure in a bicyclic, carbo- cyclic or heterocyclic group is other than carbocyclic aromatic, and A 21489-7012 is optionally substituted by substituents from the group consisting of alkyl, alkoxy, hydroxy, halogen, haloalkyl, NO2, NH2, lower alkylthio, lower alkylsulfonyl, lower alkylsulfinyl, aryl-lower alkyl, amido, carbamoyl, carbalkoxy or aroyl; and pharmaceutically acceptable salts thereof are benzodiazepine agonists/antagonists and anxiomodulating agents, especially those wherein X represents 0, and in addition are adenosine antagonists, anti-asthmatic agents and central nervous stimulating agents, especially those wherein X represents NH or NR. The compounds differ from known triazolo[1,5-c]pyrimidines in the definition of X, R1 or the bridging group A.
519161
Francis John E.
Gelotte Karl O.
Ciba-Geigy Investments Ltd.
Fetherstonhaugh & Co.
Francis John E.
Gelotte Karl O.
LandOfFree
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