Patent ID: 6306847
Filing Date: 2001-10-23
Classification: A61P,C07D

Abstract:
A condensed purine derivative or a pharmacologically acceptable salt thereof, represented by the following formula (I): ##STR56##wherein R.sup.1 represents(I) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl, or(II) an aromatic heterocyclic group unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl;R.sup.2 represents(I) hydrogen,(II) lower alkyl,(III) alicyclic alkyl,(IV) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl,(V) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl, or(VI) an aromatic heterocyclic group unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl;R.sup.3 represents(I) hydrogen,(II) lower alkyl, or(III) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl;X.sup.1 and X.sup.2 are the same or different and each represents(I) hydrogen,(II) lower alkyl,(III) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl, or(IV) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of (i) lower alkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (ii) lower alkenyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iii) lower alkynyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (iv) aralkyl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (v) aryl unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (vi) hydroxy, (vii) lower alkoxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of carboxy, sulfo, lower alkyl esters, aralkyl esters or aryl esters thereof, hydroxy, and halogen, (viii) aralkyloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (ix) aryloxy unsubstituted or substituted with 1 to 3 substituents which are the same or different, and are selected from the group consisting of lower alkyl, hydroxy, and halogen, (x) lower alkoxycarbonyl, (xi) lower alkylthio, (xii) lower alkylsulfonyl, (xiii) carboxy, (xiv) carbamoyl, (xv) lower alkanoyl, (xvi) aroyl, (xvii) halogen, (xviii) nitro, (xix) amino, (xx) mono- or di-lower alkylamine, (xxi) cyano, and (xxii) trifluoromethyl; and n represents an integer of 0 to 3.