Abbott Laboratories Corporation

Sharps Associates

Cheuk M Lee

Harold Elmer Zaugg

Jacob J Plattner

Daniel T Chu

Anthony K Fung

Qun Li

Curt S Cooper

Raymond John Michaels

Zhenkun Ma

Wei-Bo Wang

Louis Selig Harris

Nicholas Plotnikoff

Carroll Wayne Ours

James A Parks

Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein

Quinolizinone type compounds

Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds wherein A is .dbd.CR.sup.6 --; R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; and R.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Described are compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently of one another denote hydrogen or loweralkyl; A is CO, CH.sub.2, O, S, SO or CHOH; X is hydrogen, halo, loweralkyl, or --CH.sub.2 NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are as defined above; W is COOR wherein R is hydrogen or alkyl of 1-10 carbon atoms, CH.sub.2 OH, CONR.sub.1 R.sub.2 or CH.sub.2 NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are as defined above; Z.sub.1 and Z.sub.2 independently of one another denote hydrogen, halo or loweralkyl; and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents.

5-Substituted 2,3-dihydrobenzofuran-2-carboxylic acids and their use in

Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,

Hydroxyaminomethyl derivatives of benzoyl di-substituted

5H-[1]Benzopyrano[3,4-d]pyridines represented by the formula ##STR1## wherein each R.sub.1 is loweralkyl, R.sub.2 is alkyl, cycloalkyl or ##STR2## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms and each R.sub.4, R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and R.sub.3 is hydroxy, acyloxy, loweralkoxy, loweralkenyloxy, loweralkynyloxy or ##STR3## X is a straight or branched chain alkylene group having from one to eight carbon atoms, and wherein R.sub.7 and R.sub.8 are the same or different members of the group consisting of hydrogen or loweralkyl, or ##STR4## wherein X is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.sub.10 with R.sub.10 being hydrogen or loweralkyl, with the limitation that when Z is O or S, the sum of a and b is 3 or 4; and when Z is NR.sub.10, the sum of a and b is 3-5; R.sub.9 is hydrogen or loweralkyl, and the pharmaceutically acceptable salts thereof.

5H-[1]Benzopyrano[3,4-d]pyridines

A compound of the formula ##STR1## wherein R.sub.1 is H or loweralkyl; R.sub.2 is H, loweralkyl, phenyl or substituted phenyl; R is C.sub.3 -C.sub.20 alkyl, phenyl alkyl or substituted phenyl alkyl; R.sub.3 is H or ##STR2## where X is a straight or branched chain alkylene group of 3 to 4 carbon atoms, and R.sub.4 and R.sub.5 are the same or different members of the group consisting of H or loweralkyl; or R.sub.4 and R.sub.5 taken together form a 6- or 6- member heterocyclic ring and containing no more than one additional heterocyclic atom, with or without .alpha.-loweralkyl substituents, and the acid addition salts thereof. The compounds of this invention are useful as analgesics, tranquilizers, sedative-hypnotics and anti-glaucoma agents.

(8-Substituted-10-hydroxy-5,5-dimethyl-1,2

A compound of the formula ##STR1## wherein n is 1 or 2; R is C.sub.3 -C.sub.20 alkyl or arylalkyl; R.sub.1 is OH, loweralkoxy or NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 each are H, lower-alkyl or aryl. The compounds of this invention are useful as tranquilizers, analgesics, and sedative-hypnotics.

2,8-Disubtituted-10-hydroxy-5,5-dimethyl-1,2,3,4-tetrahydro-5H-[1]be

A compound of the formula ##STR1## wherein n is 1 or 2; R is C.sub.3 -C.sub.20 alkyl, phenyl alkyl or substituted phenyl alkyl; R.sub.1 is NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 each are H, loweralkyl or phenyl or substituted phenyl. The compounds of this invention are useful as tranquilizers, analgesics, and sedative-hypnotics.

2,8-Disubstituted-10-hydroxy-5,5-dimethyl-1,2,3,4-tetrahydro-5H

Compounds of the formula ##STR1## wherein R.sub.1 is methyl or R.sub.1 R.sub.1 is oxygen; R.sub.2 is alkyl or halogen substituted phenyl alkyl; and R.sub.3 is hydrogen, loweralkyl, loweralkenyl or loweralkynyl.

9-Hydroxy-7,8,9,10-tetrahydro-6H-dibenzo[b][d]pyranones

This invention provides compounds of the structure ##STR1## where R.sub.1 is C.sub.3 -C.sub.20 alkyl or arylalkyl; R.sub.2 is hydrogen, loweralkanoyl, loweralkylsulfonyl, loweralkoxycarbonyl, carbamoyl or ##STR2## wherein X is an alkylene group having from 2 to 4 carbon atoms; and R.sub.3 and R.sub.4 are the same or different members of the group consisting of hydrogen or loweralkyl, or R.sub.3 and R.sub.4 taken together form a 5-, 6-, or 7-member heterocyclic ring; and the pharmaceutically acceptable acid addition salts thereof. The compounds of this invention are useful as analgesics, tranquilizers and sedative-hypnotics.

10-Amino-5H-[1]benzopyrano[4,3-c]pyridines

A compound of the formula ##STR1## wherein R is a C.sub.6 -C.sub.20 alkyl, arylalkyl or cycloalkyl alkyl; R' is phenyl or substituted phenyl; and X is H, halogen,

2-(.alpha.-Amidobenzyl)-5-alkylresorcinols

Compounds of the formula ##STR1## wherein R.sub.1 is methyl or R.sub.1 R.sub.1 is oxygen; R.sub.2 is alkyl or halogen substituted phenyl alkyl; and R.sub.3 is hydrogen, loweralkyl, loweralkenyl or loweralkynyl. The compounds of this invention are useful as analgesics and tranquilizers.

9-Hydroxy-7,8,9,10-tetrahydro-6H, dibenzo[b][d] pyrans and pyranones

Covers 2-substituted-5-alkyl resorcinols represented by the formula ##STR1## wherein R.sub.1 is hydrogen or lower-alkanoyl; R.sub.2 is a straight or branched chain alkyl of 1 to 20 carbon atoms; and X is nitrogen or C-methyl. The compounds of this invention are useful as tranquilizers, analgesics, sedative-hypnotics and anticonvulsants.

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Libertyville, IL, United States of America

Cheuk M Lee