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1. (WO1997018212) ARYL AND HETEROARYL PURINE COMPOUNDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018212 International Application No.: PCT/EP1996/004460
Publication Date: 22.05.1997 International Filing Date: 14.10.1996
IPC:
C07D 471/04 (2006.01) ,C07D 473/00 (2006.01) ,C07D 473/30 (2006.01) ,C07D 473/34 (2006.01) ,C07D 473/38 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
28
Oxygen atom
30
attached in position 6, e.g. hypoxanthine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32
Nitrogen atom
34
attached in position 6, e.g. adenine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
36
Sulfur atom
38
attached in position 6
Applicants:
PHARMACIA & UPJOHN S.P.A. [IT/IT]; Via Robert Koch, 1.2 I-20152 Milan, IT (AllExceptUS)
BUZZETTI, Franco [IT/IT]; IT (UsOnly)
BRASCA, Maria, Gabriella [IT/IT]; IT (UsOnly)
LONGO, Antonio [IT/IT]; IT (UsOnly)
BALLINARI, Dario [IT/IT]; IT (UsOnly)
Inventors:
BUZZETTI, Franco; IT
BRASCA, Maria, Gabriella; IT
LONGO, Antonio; IT
BALLINARI, Dario; IT
Priority Data:
9523242.714.11.1995GB
9524131.124.11.1995GB
Title (EN) ARYL AND HETEROARYL PURINE COMPOUNDS
(FR) COMPOSES D'ARYLPURINE ET D'HETEROARYLPURINE
Abstract:
(EN) Novel bicyclic condensed pyrimidine compounds having general formula (I) wherein X is -CH2-, -NH-(CH2)n-, -O-(CH2)n- or -S-(CH2)n- in which n is zero or 1; A is a 4,5-fused imidazole ring N-substituted by R3 which is hydrogen, C1-C4 alkyl or benzyl, or A is a 2,3-fused pyridine ring C-substituted by R4 which is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or NR5R6 in which each of R5 and R6 independently is H or C1-C4 alkyl; B is a bicyclic ring chosen from tetralin, indane and 2-oxindole; each of R1 and R2, independently, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof; and wherein, when at the same time, A is pyridine and B is a tetralin ring, R4 is H, C1-C4 alkyl, C1-C4 alkoxy or halogen and X is as defined above, then each of R1 and R2 is other than H; and wherein, when at the same time, A is imidazole, X is -NH-(CH2)n- as defined above, and B is an indan ring unsubstituted or substituted by one or more of halogen, hydroxy, C1-C4 alkoxy and nitro, then R3 is other than C1-C4 alkyl or benzyl, are provided.
(FR) On décrit des nouveaux composés de pyrimidine condensés bicycliques, répondant à la formule générale (I), ainsi que des sels de ceux-ci, acceptables sur le plan pharmacologique. Dans cette formule, X représente -CH2-, -NH-(CH2)n, -O-(CH2)n-, ou -S-(CH2)n- où n vaut zéro ou 1; A représente un noyau imidazole fusionné en 4,5, substitué en N par R3, lequel représente hydrogène, alkyle C1-C4 ou benzyle, ou bien A représente un noyau pyridine fusionné en 2,3, substitué en C par R4, lequel représente hydrogène, alkyle C1-C4, alcoxy C1-C4, halogène ou NR5R6, où R5 et R6 représentent chacun indépendamment H ou alkyle C1-C4, B représente un noyau bicyclique choisi parmi tétraline, indane et 2-indoxyle, R1 et R2 représentent chacun indépendamment hydrogène, alkyle C1-C4, halogène, hydroxy, alcoxy C1-C4, alcoxycarbonyle C1-C4, nitro, cyano ou CF3. Cette formule est caractérisée en ce que si, en même temps, A représente pyridine, B représente un noyau tétraline, R4 représente H, alkyle C1-C4, alcoxy C1-C4, alcoxy C1-C4 ou halogène, et X est tel que défini ci-dessus, alors R1 et R2 ne peuvent être H, et en ce que si, en même temps, A représente imidazole, X représente -NH-(CH2)n-, tel que défini ci-dessus, et B représente un noyau indane non substitué ou substitué par un ou plusieurs substituants choisis parmi halogène, hydroxy, alcoxy C1-C4 et nitro, alors R3 ne peut être alkyle C1-C4 ou benzyle.
Designated States: AU, BG, BR, BY, CA, CN, CZ, EE, HU, IL, JP, KR, KZ, LT, LV, MX, NO, NZ, PL, RU, SG, SI, TR, UA, US
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
NO19973198NZ320219MXPA/a/1997/005010EP0802914US5965563JPH10512896
CN1168138CA2209598EA199700107AU1996072920