Substituted benzyl pyrimidines

Details Substituted benzyl pyrimidines Substituted benzyl pyrimidines

1997-05-21

1998-06-09

Gupta, Yogendra N.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514256, 544324, 544325, A61K 31505, C07D23948

Patent

active

057634505

DESCRIPTION:

BRIEF SUMMARY
The present invention is concerned with substituted 5-benzyl-2,4-diaminopyrimidines of the general formula ##STR2## in which R.sup.1 represents lower alkoxy, R.sup.2 represents bromine or lower alkoxy and R.sup.3 represents aryl, heteroaryl or a group --Q--R.sup.30, wherein Q signifies ethylene, vinylene or ethynylene and R.sup.30 signifies aryl, heteroaryl, lower alkoxycarbonyl or carbamoyl, pharmaceutically acceptable salts of these compounds.
These compounds are novel and possess valuable antibiotic properties. They can be used in the control or prevention of infectious diseases. In particular, they exhibit a pronounced antibacterial activity not only against multi-resistant gram-positive strains, but also against opportunistic pathogens such as e.g. Pneumocystis carinii. These compounds can also be administered in combination with known antibacterially active substances and then exhibit a synergistic effect. Typical combination partners are e.g. sulphonamides, which can be admixed with the compounds of formula I or their salts in various ratios.
Objects of the present invention are compounds of formula I, their readily hydrolyzable esters and pharmaceutically acceptable salts per se and for use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.
The term "lower" denotes residues and compounds with up to 7, preferably up to 4, carbon atoms. Alkyl and alkoxy residues can be straight-chain or branched, such as e.g. methyl, ethyl, n-propyl, isopropyl and t-butyl and, respectively, methoxy, ethoxy, n-propoxy, isopropoxy and t-butoxy. The same applies to "lower alkyl" as a component of other groups such as lower lower-alkanoyl.
"Aryl" denotes 6-membered aromatic groups which have one or more rings and which preferably have 6-14 carbon atoms. Phenyl, naphthyl, anthryl and phenanthryl are examples. These groups can be substituted, e.g. by phenyl; lower alkyl (e.g. methyl); C.sub.3-6 cycloalkyl (e.g. cyclopropyl); halogen (e.g. bromine, fluorine); trifluoromethyl; lower alkenyl (e.g. 1-pentenyl); lower alkoxy (e.g. methoxy, n-butoxy); carboxy; lower alkoxycarbonyl (e.g. methoxycarbonyl); hydroxy; oxo; lower alkanoyloxy (e.g. acetoxy); amino; lower alkylamino (e.g. methylamino); di-(lower alkyl)-amino (e.g. dimethylamino, diethylamino); lower alkoxycarbonyl-lower alkylamino (e.g. methoxycarbonylethylamino); carboxy-lower alkylamino (e.g. carboxyethylamino); lower alkanoylamino (e.g. acetylamino); lower alkoxycarbonyl-lower alkanoylamino (e.g. 2-ethoxycarbonyl-acetylamino, 4-methoxycarbonyl-n-butyrylamino); lower alkoxycarbonylbenzoylamino (e.g. 4-methoxycarbonylbenzoylamino); hydroxybenzoylamino; carboxy-lower alkanoylamino (e.g. 2-carboxyacetylamino, 4-carboxy-n-butyrylamino); carboxybenzoylamino (e.g. 4-carboxybenzoylamino); mono- or di-(heterocyclylcarbonyl)amino (e.g. furan-2-carbonylamino); aminobenzenesulphonyl (e.g. 4-aminobenzenesulphonyl); sulphamoyl; hydroxyiminomethyl; aminobenzenesulphonylamino (e.g. 4-aminobenzenesulphonylamino); aryl-lower alkyl (e.g. benzyl); heteroaryl-lower alkyl (e.g. 2,4-diamino-pyrimidin-5-ylmethyl); arylamino (e.g. 3-chloro-1,4-dioxo-1,4-dihydro-naphthalen-2-ylamino); nitro-lower-alkylamino, e.g. (2-nitro-ethyl)amino; carboxy-lower-alkenyl, e.g. 2-carboxyvinyl; lower-alkyloxycarbonyl-lower-alkenyl, e.g. 2-methoxycarbonylvinyl; formyl, cyano, hydroxy-lower-alkyl, e.g. hydroxymethyl; di-(lower-alkoxycarbonyl)-lower-alkenyl, e.g. di-(ethoxycarbonyl)vinyl; --C(O)C(CH-lower-alkoxy)COOH; --C(O)C(NOH)COOH; --C(O)C(NOH)CO--O-lower-alkyl; --C(O)C(NO-trityl)CO--O-lower-alkyl; --C(O)C(NO-lower-alkyl)COO-lower-alkyl; --C(O)C(NO-lower-alkoxy-lower-alkyl)CO-O-lower-alkyl; --C(O)C(CHN-(lower-alkyl).sub.2)CO--O-lower-alkyl; mono- or di-(lower-alkyl or cyclo

REFERENCES:
CA121: 271337, 1993.
CA94: 170109, 1980.

Affiliated with

Also associated with

Rating

Substituted benzyl pyrimidines 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 benzyl pyrimidines, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted benzyl pyrimidines will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2199418