The Upjohn Co.

Pharmacia & Upjohn Company

Ronald B Gammill

Michael R Barbachyn

Gordon L Bundy

Joseph Walter Strohbach

Paul A Aristoff

Harvey I Skulnick

Suvit Thaisrivongs

David John Anderson

Paul D Johnson

Steven Ronald Turner

Joel Morris

Karen Rene Romines

Thomas M Judge

Sharon N Bisaha

Kyoung S Kim

Douglas K Hutchinson

Steven J Brickner

Ruben Alberto Tommasi

Louis L Skaletzky

Joseph M Timko

Frank P Bell

George P Luke

Theresa M Schwartz

Mahesh V Patel

Richard Charles Thomas

Ruth Elizabeth TenBrink

E Jon Jacobsen

Paul K Tomich

Tomi K Sawyer

Michael John Bohanon

Chih-Ping Yang

Lee S Banitt

Qingwei Zhang

The present invention relates to compounds of formula I and II which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl&lsqb;b&rsqb;pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.

Compounds useful to treat retroviral infections

Pyranone compounds useful to treat retroviral infections

This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.

Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and

A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

Oxazolidinone antimicrobials containing substituted diazine moieties

4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl�b!pyran-2-ones

Imidazo-benzoxazines of Formula (I) and pharmaceutically acceptable salts thereof. ##STR1## where Q is selected from (A) through (H) ##STR2## or pharmaceutically acceptable salts thereof wherein the R groups are as defined herein. The imidazo-benzoxazines, Formula (I), of the present invention are useful as anxiolytics and sedatives.

4-oxo- and 4H-imidazo(5,1-c)(1,4)benzoxazines useful as benzodiazepine

A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is chosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

An invention relating to Imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group and which are useful as anxiolytic and sedative/hypnotic agents.

Imidazo[1,5-A]quinoxalines

A quinolone compound of Formula (I) ##STR1## as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial infections in animals including humans.

Antibacterial quinolone compounds

Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.

Bivalent ligands effective for blocking ACAT enzyme for lowering plasma

The present invention provides novel peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 containing a novel (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety of the formula XL.sub.2c at the E.sub.10 -F.sub.11 -position, X is a terminal group, and the remaining variables are amino acid residues. The present invention also provides novel intermediate compounds. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodificiency disease syndrome (AIDS). ##STR1##

Peptides containing a (1-amino-2-hydroxy-2-heterocyclic)ethyl moiety

The present invention particularly provides novel benzofuran compounds which are useful in the synthesis of khellin and antiatherosclerotic furochromones.

Intermediates for antiatherosclerotic furochromones

The present invention particularly provides novel furochromones and intermediates for their preparation.

Antiatherosclerotic furochromones and intermediates therefor

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Portage, MI, United States of America

Ronald B Gammill