Abbott Laboratories Corporation

University of Kansas

Adria Laboratories Inc.

Pathogenesis Corporation

The Ohio State University

The Kansas University Endowment Association

Lester A Mitscher

George W Clark, Iii

Daniel T Chu

William R Baker

Gordon Herman Bokelman

Carl F Nathan

Jeffrey Aube

Frank John Schoenen

Paul Hanson

William R Groskopf

Gregg T Williams

Robert Smith

Paul B Hudson

Jose Alexander

Daniel Lednicer

Chunjing Liu

Ben S Gold

Maneesh Pingle

Beimar N Iriarte

This invention provides cephalosporin derivatives for killing or inhibiting the spread of microorganisms such as non-replicatingand in the treatment of infectious disease.

Cephalosporin derivatives and methods of use

Aqueous solutions of steroid compounds which have biological activity and have a tendency to oxidative degradation at temperatures between 2.degree. and 8.degree. C. on storage in excess of several months are stabilized by the addition of cyclodextrin.

Stabilized aqueous steroid immunoassay standards with cyclodextrins

Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using indolo[2,1-b]quinazoline-6,12-dione compounds of the formula (I): ##STR1## wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofloxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).

Indolo[2,1-biquinazoline-6,12-dione antibacterial compounds and methods

Methods, compounds and compositions are provided for inhibiting the growth of mycobacteria and gram-positive organisms in vitro and of treatment of mycobacterial and gram-positive infections in vivo using compounds of the formula (I) or (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, amino or loweralkyl; and R.sub.2 is selected from the group consisting of --CONR.sub.4 R.sub.5, --(CH.sub.2).sub.n- NR.sub.4 R.sub.5, --NHCO--NR.sub.4 R.sub.5 and --NHCO.sub.2 R.sub.4, wherein R.sub.4 and R.sub.5 are selected from hydrogen, loweralkyl, alkoxy, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, arylalkylaryl, arylaryl, aryoxy, aryloxyaryl, aryloxyarylalkyl, arylalkoxy, arylalkoxyaryl, arylalkoxyarylalkyl, arylalkoxyaryl, alkenyl, alkynyl and heterocycle, or R.sub.4 and R.sub.5 are connected to form a ring and produce cycloalkyl or heterocycle; and n is 0, 1, 2, or 3; or a pharmaceutically acceptable salt thereof processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and a method of treating disorders resulting from mycobacterial or MRSA infections. The methods, compounds and compositions are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofioxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).

Isoflavonoid antibacterial compounds, compositions and use

A process for producing racemic or optically active compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 to C.sub.6 alkyl or benzyl; and Z is amino or substituted amino. Also disclosed are intermediates useful in the process and methods for producing the intermediates.

Intermediates for preparation of racemate and optically active ofloxacin

Process for preparation of racemate and optically active ofloxacin and

Chemically simplified versions of intermediates on the identified biosynthetic pathway to daunomycin are bioconverted to active analogues of naturally occurring antibiotics.

Biosynthesis of simplified anthracyclines

A synthesis of 5,12-dihydroxy-1,3,4-trihydro-2,6,11-tetracenetrione and its derivatives from leucoquinizarin or a derivative of leucoquinizarin. The tetracenetriones are well-known intermediates in the synthesis of compounds related to doxorubicin.

Anthracycline synthesis

A regiospecific synthesis for anthracyclinones asymmetric is disclosed. The synthesis is based upon a regiospecific bromination of the C-7 position of the .alpha.-tetralone which after transposing the keto group to the .beta.-position and reaction with an organo-lithium compound is condensed with a phthalate ester.

Regiospecific synthesis of anthracyclinone compounds such as

A process for synthesizing the 7-substituted or unsubstituted 5,12-dihydroxy-1,2,3,4,6,11-hexahydro-2,6,11-trioxonaphthacene precursors for doxorubicin and related compounds from butadiene and p-benzoquinone and intermediates useful in the synthesis.

The compound of the formula ##STR1## has been found to be an important and practical intermediate with the proper stereo-isomerism for the preparation of numerous prostaglandin derivatives. It can easily be converted to 4.alpha.-acetoxy-2-cyclopentenone by a variety of processes.

Intermediate for prostaglandins and process for preparing the

A process for synthesizing doxorubicin and related compounds from aloe-emodin is disclosed. Intermediates useful in the preparation of doxorubicin and related compounds are also disclosed.

This invention provides intermediates which are essential for a new chemical method which converts terrein, a fungal metabolite, to an intermediate which is known to be useful for the preparation of prostaglandins of the C series and analogs of other prostaglandins.

Growing community of inventors

Lawrence, KS, United States of America

Lester A Mitscher