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US 5,292,738 AGranted
Anti-virally active pyridazinamines
AssigneeJanssen Pharmaceutica NV
InventorsRaymond A. Stokbroekx, Marcel J. M. Van der Aa, Joannes J. M. Willems, Marcel G. M. Luyckx
Life of this patent
Estimating the term…
Abstract
Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.
Claims8
A compound of the formula:
- ##STR194## a pharmaceutically acceptable acid-addition salt or a stereoisomeric form or a tautomeric form thereof, wherein:
- R.sup.1 is a member selected from the group consisting of hydrogen, halo, 1H-imidazol-1-yl, lower alkyloxy, aryloxy, aryllower alkyloxy, lower alkylthio, arylthio, hydroxy, mercapto, amino, lower alkylsulfinyl, lower alkylsulfonyl, cyano, lower alkyloxycarbonyl, lower alkylcarbonyl, and lower alkyl;
- and
- A.sup.2 is a bivalent radical of the formula:
- --C.sub.m H.sub.2m --C(R.sup.5)(R.sup.6)--C.sub.n H.sub.2n --(c);
- or
- --C.sub.m-1 H.sub.2(m-1) --C(R.sup.7).dbd.C(R.sup.8)--C.sub.n H.sub.2n --(d);
- wherein one of the hydrogen atoms within the radical C.sub.m H.sub.2m, C.sub.m-1 H.sub.2(m-1), or C.sub.n H.sub.2n may be replaced by lower alkyl or aryl;
- m is the integer 1 or 2 and n is the integer 2;
- R.sup.5 is hydrogen, aryl, arylamino, (aryl)(lower alkyl)amino, hydroxy, or indolyl;
- R.sup.6 is hydrogen, aryl, arylcarbonyl, or (arylcarbonyl)lower alkyl;
- and
- R.sup.7 and R.sup.8 are, each independently, members selected from the group consisting of hydrogen, lower alkyl, aryl, aryllower alkyl, and pyridinyl;
- wherein aryl is phenyl, being optionally substituted with up to 3 substituents, each independently selected from the group consisting of halo, lower alkyl, trifluoromethyl, nitro, amino, lower alkyloxy, hydroxy and lower alkyloxycarbonyl;
- thienyl;
- and naphthalenyl,
- provided that when A.sup.2 is a radical of formula (c) and one of R.sup.5 and R.sup.6 is hydrogen, then the other of R.sup.5 and R.sup.6 cannot be hydrogen, hydroxy, or lower alkyl.
14 more elements
An anti-rhinoviral composition consisting essentially of an inert carrier and as an active ingredient an anti-rhinovirally effective amount of a compound of the formula:
- ##STR195## a pharmaceutically acceptable acid-addition salt or a stereoisomeric form or a tautomeric form thereof, wherein:
- R.sup.1 is a member selected from the group consisting of hydrogen, halo, 1H-imidazol-1-yl, lower alkyloxy, aryloxy, aryllower alkyloxy, lower alkylthio, arylthio, hydroxy, mercapto, amino, lower alkylsulfinyl, lower alkylsulfonyl, cyano, lower alkyloxycarbonyl, lower alkylcarbonyl, and lower alkyl;
- and
- A.sup.2 is a bivalent radical of the formula:
- --C.sub.m H.sub.2m --C(R.sup.5)(R.sup.6)--C.sub.n H.sub.2n --(c);
- or
- --C.sub.m-1 H.sub.2(m-1) --C(R.sup.7).dbd.C(R.sup.8)--C.sub.n H.sub.2n --(d);
- wherein one of the hydrogen atoms within the radical C.sub.m H.sub.2m, C.sub.m-1 H.sub.2(m-1), or C.sub.n H.sub.2n may be replaced by lower alkyl or aryl;
- m is the integer 1 or 2 and n is the integer 2;
- R.sup.5 is hydrogen, aryl, arylamino, (aryl)(lower alkyl)amino, hydroxy, or indolyl;
- R.sup.6 is hydrogen, aryl, arylcarbonyl, or (arylcarbonyl)lower alkyl;
- and
- R.sup.7 and R.sup.8 are, each independently, members selected from the group consisting of hydrogen, lower alkyl, aryl, aryllower alkyl, and pyridinyl;
- wherein aryl is phenyl, being optionally substituted with up to 3 substituents, each independently selected from the group consisting of halo, lower alkyl, trifluoromethyl, nitro, amino, lower alkyloxy, hydroxy and lower alkyloxycarbonyl;
- thienyl;
- and naphthalenyl,
- provided that when A.sup.2 is a radical of formula (c) and one of R.sup.5 and R.sup.6 is hydrogen, then the other of R.sup.5 and R.sup.6 cannot be hydrogen, hydroxy, or lower alkyl.
14 more elements
Dependencies are inferred from the claim text.