Pyrazolo(1,5a)pyrimidines, their preparation and their use

Details Pyrazolo(1,5a)pyrimidines, their preparation and their use Pyrazolo(1,5a)pyrimidines, their preparation and their use

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A01N 43/90 (2006.01)

Patent

CA 2217778

Pyrazolo-(1,5a)-pyrimidines have formula (I), in which the indexes and substituents have the following meanings: n equals 0 or 1; Y stands for 0, S, NRa, OCH2*, SCH2*, NRaCH2*, CH2O*, CH2S*, CH2NRa*, CH2CH2, CRa=Rb or CC, the positions with an * indicating the bond to the phenyl ring; R' stands for H3CO- CO-o=CHOCH3, H3CNH-CO-o=CHOCH3, H3CO-CO-o=NOCH3, H3CNH-CO-o=NOCH3, H2N-CO- o=NOCH3, HO-CO-o=NOCH3, H3CO-CO-o=CHCH3, H3CO-CO-o=CHCH2CH3, H3C-CO-o=CHOCH3, H3C-CO-o=NOCH3, H3CCH2-CO-o=NOCH3, in which o indicates a C atom bound to the phenyl ring, N(OCH3)-CO2CH3, N(CH3)-CO2CH3, N(CH2CH3)-CO2CH3, or a group R'.1- o=NOCH3, R'.2-o=NOCH3, R'.3-o=NOCH3 or R'.4-o=NOCH3; m equals 0, 1, 2 or 3; the residues R" may be different when m is greater than 1; R" stands for cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; R1, R3 stand for hydrogen, cyano, nitro, hydroxy, amino, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkylthio halide, aryl, arylalkyl, aryloxy, arylalkoxy, arylthio, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, heteroarylthio or NRcRd, NRcNRdRe, CO-Rc, CO2-Rc, CO-NRcRd, O-CO-Rc, O-CO2-Rc, O-CO-NRcRd, NRc-CO-Rd, NRc-CO2-Rd or NRc-CO-NRdRe; R2 stands for hydrogen, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, aryl, aryloxy, heteroaryl, heteroaryloxy, CO- Rc, CO2-Rc or CRf=NORg; R4 stands for hydrogen, cyano, nitro, nitroso, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkylthio halide, aryl, arylalkyl, aryloxy, arylalkoxy, arylthio, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, heteroarylthio or NRcRd, CO- Rc, CO2-Rc or CRf=NORg; Ra, Rb stand for hydrogen, halogen, C1-C4 alkyl or C1- C4 alkyl halide; Rc, Rd and Re stand for hydrogen, alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; Rf stands for hydrogen, cyano, halogen, or optionally substituted alkyl, alkyloxy, alkylthio, alkenyl, alkenyloxy, alkenylthio, alkinyl, alkinyloxy, alkinylthio, cycloalkyl, cycloalkyloxy, cycloalkylthio, heterocyclyl, heterocyclyloxy, heterocyclylthio, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy or heteroarylthio; Rg stands for hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, heterocyclyl, aryl or heteroaryl. Also disclosed are a process for preparing the same and their use.

Les pyrazolo-(1,5a)-pyrimidines décrites ont la formule (I), dans laquelle les indices et substituants ont la notation suivante: n vaut 0 ou 1; Y désigne O, S, Nr?a¿, OCH¿2?*, SCH¿2?*, NR?a¿CH¿2?*, CH¿2?O*, CH¿2?S*, CH¿2?NR?a¿*, CH¿2?CH¿2?, CR?a¿=R?b¿ ou C?C, les positions signalées par un * représentant la liaison avec le cycle phényle; R' désigne H¿3?CO-CO-o=CHOCH¿3?, H¿3?CNH-CO-o=CHOCH¿3?, H¿3?CO-CO-o=NOCH¿3?, H¿3?CNH-CO-o=NOCH¿3?, H¿2?N-CO-o=NOCH¿3?, HO-CO-o=NOCH¿3?, H¿3?CO-CO-o=CHCH¿3?, H¿3?CO-CO-o=CHCH¿2?CH¿3?, H¿3?C-CO-o=CHOCH¿3?, H¿3?C-CO-o=NOCH¿3?, H¿3?CCH¿2?-CO-o=NOCH¿3?, le symbole o désignant un atome de carbone lié au cycle phényle, N(OCH¿3?)-CO¿2?CH¿3?, N(CH¿3?)-CO¿2?CH¿3?, N(CH¿2?CH¿3?)-CO¿2?CH¿3?, ou un groupe R'.1-o=NOCH¿3?, R'.2-o=NOCH¿3?, R'.3-o=NOCH¿3? ou R'.4-o=NOCH¿3?; m vaut 0, 1, 2 ou 3, les résidus R" pouvant être différents lorsque m est supérieur à 1; R" désigne cyano, halogène, alkyle, haloalkyle, alcoxy, haloalcoxy, alkylthio ou haloalkylthio; R?1¿, R?3¿ désignent hydrogène, cyano, nitro, hydroxy, amino, halogène, alkyle, halogénure d'alkyle, alcoxy, halogénure d'alcoxy, alkylthio, halogénure d'alkylthio, aryle, arylalkyle, aryloxy, arylalcoxy, arylthio, hétéroaryle, hétéroarylalkyle, hétéroaryloxy, hétéroarylalcoxy, hétéroarylthio ou NR?c¿R?d¿, NR?c¿NR?d¿R?e¿, CO-R?c¿, CO¿2?-R?c¿, CO-NR?c¿R?d¿, O-CO-R?c¿, O-CO¿2?-R?c¿, O-CO-NR?c¿R?d¿, NR?c¿-CO-R?d¿, NR?c¿-CO¿2?-R?d¿ ou NR?c¿-CO-NR?d¿R?e¿; R?2¿ désigne hydrogène, halogène, alkyle, halogénure d'alkyle, alcoxy, halogénure d'alcoxy, aryle, aryloxy, hétéroaryle, hétéroaryloxy, CO-R?c¿, CO¿2?-R?c¿ ou CR?f¿=NOR?g¿; R?4¿ désigne hydrogène, cyano, nitro, nitroso, halogène, alkyle, halogénure d'alkyle, alcoxy, halogénure d'alcoxy, alkylthio, halogénure d'alkylthio, aryle, arylalkyle, aryloxy, arylalcoxy, arylthio, hétéroaryle, hétéroarylalkyle, hétéroaryloxy, hétéroarylalcoxy, hétéroarylthio ou NR?c¿R?d¿, CO-R?c¿, CO¿2?-R?c¿ ou CR?f¿=NOR?g¿; R?a¿, R?b¿ désignent hydrogène, halogène, alkyle C¿1?-C¿4? ou halogénure d'alkyle C¿1?-C¿4?; R?c¿, R?d¿ et R?e¿ désignent hydrogène, alkyle, alcényle, alcinyle, aryle, arylalkyle, hétéroaryle ou hétéroarylalkyle; R?f¿ désigne hydrogène, cyano, halogène, ou alkyle, alkyloxy, alkylthio, alcényle, alcényloxy, alcénylthio, alcinyle, alcinyloxy, alcinylthio, cycloalkyle, cycloalkyloxycycloalkylthio, hétérocyclyle, hétérocyclyloxy, hétérocyclylthio, aryle, aryloxy, arylthio, hétéroaryle, hétéroaryloxy ou hétéroarylthio le cas échéant substitués; R?g¿ désigne hydrogène ou alkyle, alcényle, alcinyle, cycloalkyle, hétérocyclyle, aryle ou hétéroaryle le cas échéant substitués. L'invention concerne également leur préparation et leur utilisation.

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