Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1988-06-10
1990-06-19
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142362, 514326, 514422, 544132, 546210, 548518, 5482622, C07D24908, A61K 3141
Patent
active
049354370
ABSTRACT:
A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.
REFERENCES:
patent: 4226878 (1980-10-01), Iizuka et al.
patent: 4271170 (1981-06-01), Tanouchi et al.
patent: 4713387 (1987-12-01), Watanabe et al.
patent: 4749713 (1988-06-01), Bowman et al.
patent: 4755526 (1988-07-01), Hirsch et al.
Iizuka et al., J. Med. Chem., 1981, 24, 1139-1148.
Tanouchi et al., J. Med. Chem., 1981, 24, 1149-1155.
Chem. Abstr., 99, 139652b, Mitsubishi Chemical.
J. Org. Chem., 1987, 52(5), 946-8, (Eq. to Chem. Abstr., 106, 102640).
Chem. Abstr., 106, 50050u.
Chemical Abstracts, vol. 107, No. 21, Nov. 23, 1987, Columbus, Ohio, U.S.A., Wickings, E. J.; Middleton, M. C., "Non-Steroidal Inhibition of Granulosa Cell Aromatase Activity in Vitro", p. 88, col. 2, Abstract No. 191 136j.
Edwards Philip N.
Large Michael S.
Hollrah Glennon H.
Imperial Chemical Industries plc
Morris Patricia L.
LandOfFree
(Substituted aralkyl) heterocyclic compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with (Substituted aralkyl) heterocyclic compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and (Substituted aralkyl) heterocyclic compounds will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2260605