Abbott Laboratories Corporation

Andre G Pernet

Naoyasu Ishizuka

Hiromasa Nakamoto

Anthony K Fung

Jacob J Plattner

Daniel T Chu

Stephen Hanessian

Curt S Cooper

Alex M Nadzan

Leslie A Freiberg

Gerard Yvon Paris

Nathan L Shipkowitz

Mina D Perlin

Donald E Morrison

Howard E Gracey

New 7-substituted 6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids or esters having a substituted or unsubstituted phenyl radical, an aromatic heterocyclic radical, an alkyl or cycloalkyl radical in the 1-position are antibacterial agents.

7-(3-Substituted imino-1-pyrrolidinyl)-quinolone-3-carboxylic acids

An erythromycin A derivative with high antimicrobial activity and improved pharmacokinetics is disclosed. 4'-Deoxyerythromycin A 11,12-carbonate and derivatives show superior in vitro and in vivo antimicrobial activity compared to erythromycin A, and when administered to animals has a serum half-life much prolonged over that of erythromycin A.

Erythromycin A 11,12-carbonate and method of use

This invention relates to a product which will provide a high caloric source upon I.V. administration. More particularly, this invention relates to glucosyl esters of malonic acids and substituted malonic acid derivatives which will permit the assimilation of glucose into the body at high concentrations but with low toxicity.

High caloric product for I.V. administration

Described are compounds of the formula ##STR1## wherein R is hydrogen, loweralkyl, aminomethyl or halo, R.sub.1 is hydroxy or NHX where X is H, loweralkyl, phenyl, substituted phenyl, acetyl, benzyl and substituted benzyl, and Y is hydrogen, loweralkyl or halo and may be the same or different, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents.

Benzophenone derivatives

Certain 1-substituted-3-loweralkyl-5-(substituted)phenyl-6-aminopyrazolo[3,4-b]pyr azines are provided. They have useful activity as antivirals.

Antiviral pyrazolopyrazines

By condensation of anisoyl chloride with 2,3-dichloroanisole under proper conditions, 2,3-dichloro-4-(hydroxybenzoyl)phenol is obtained directly.

Synthesis for 2,3-dichloro-4-(hydroxybenzoyl)phenol

Prostaglandin type compounds of the formula ##STR1## where X is CH.sub.2 --CH.sub.2, CH.dbd.CH cis or C.tbd.C; Y is CH.sub.2 or O; Z is H, OH, CH.sub.3 or CH.sub.2 OH and R is a linear, branched or cyclo alkyl chain of 3 to 7 carbon atoms, can be prepared by essentially a one-step reaction from a new intermediate of the formula ##STR2## where R represents a linear, branched or cyclo alkyl group of 3 to 7 carbon atoms; P is a removable protective group and z is H, OP,CH.sub.3 or CH.sub.2 OP. The intermediate is useful in making known and new PGEs useful as antihypertensives, gastric acid secretion inhibitors and smooth muscle stimulants.

Prostaglandin derivatives

Prostaglandin type compounds of the formula ##STR1## where X is CH.sub.2 --CH.sub.2, CH.dbd.CH or C.tbd.C; Y is CH.sub.2 or O; Z is OH, CH.sub.3 or CH.sub.2 OH, R' is H or loweralkyl and R is a linear, branched or cyclic alkyl group of 3 to 7 carbon atoms, can be prepared by essentially a one-step reaction from a new intermediate of the formula ##STR2## wherein R' is hydrogen, R and Z are the same as shown above, and P is a removable protective group. The new compounds are useful as antihypertensives, gastric acid secretion inhibitors and smooth muscle stimulants.

Prostaglandin type compounds of the formula ##STR1## wherein X is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-cis or--C.tbd.C--; Y is CH.sub.2 or O; Q is--CH.sub.2 --CH.sub.2 --or --CH.dbd.CH--; Z is H, OH, CH.sub.3 or CH.sub.2 OH, R is a linear, branched or cyclo alkyl chain of 3 to 7 carbon atoms or certain other moieties, and R' and R'''are H or CH.sub.3. These compounds are prepared by essentially a one-step reaction from a new intermediate of the formula ##STR2## wherein Z, R, R' and Q have the above meaning and P is a removable protective group by condensation with a reactive moiety introducing the entire .alpha.-chain (R'''=CH.sub.3). If desired, the carbonyl function is subsequently reduced to W= --CH(OH)--. The intermediate is useful in making known and new PGEs useful as antihypertensives, gastric acid secretion inhibitors and smooth muscle stimulants.

Growing community of inventors

Lake Bluff, IL, United States of America

Andre G Pernet