The Upjohn Co.

Pharmacia & Upjohn Company

Upjohn

Pah P&u LLC

John R Palmer

John M McCall

Donald E Ayer

Frederick J VanDoornik

Harold A Karnes

E Jon Jacobsen

Donna Lee Romero

Michael R Barbachyn

Arthur Glenn Romero

Peter Laurence Toogood

Dennis Joseph McNamara

Alexander Ross Hurd

Lisa Marie Thomasco

Debra Ann Sherry

J Craig Ruble

Paul Joseph Dobrowolski

E Jonathan Jacobsen

Paul A Aristoff

Gordon L Bundy

Herman W Smith

Valerie Ann Vaillancourt

Richard Charles Thomas

Mark E Schnute

Martin Gall

Fred L Ciske

Gordan L Bundy

Gary E Martin

Frederick J Van Doornik

The present invention is directed to tricyclic tetrahydroquinoline compounds of formula I, and pharmaceutically acceptable salts thereof wherein the variables R, R, R, R, R, Rand X are as described herein and to pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.

Tricyclic tetrahydroquinoline antibacterial agents

The invention includes tetrahydroquinoline and related compounds of formula I and pharmaceutical compositions thereof, that exhibit useful antibacterial activity again a wide range of human and veterinary pathogens 

The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens 

The present invention provides a compound of formula Iwhich is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Heterocycle carboxamides as antiviral agents

Pyrimido�4,5-B!indoles

Substituted indoles of formula (I) ##STR1## are useful anti-AIDS pharmaceuticals.

Pyridyl piperazine compound

The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.

Diaromatic substituted compounds as anti-HIV-1 agents

Disclosed are amino substituted steroids (XI) which contain an imidazolylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.

Imidazolylpiperazinyl steroids

The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).

Anti-aids piperazines

Disclosed are amino substituted steroids (XI) which contain a pyridinylpiperazinyl group group attached to the terminal carbon atom of the C.sub.17 -side chain of the steroid which are useful as pharmaceutical agents for treating a number of conditions.

Pyridinylpiperazinyl steroids

Disclosed are amino substituted steroids (XI) which contain 4-[1,3,5-triazin-2-yl]- or 4-[1,2,4-triazin-3-yl]- 1-piperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.

Triazinylpiperazinyl steroids

Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Piperazine compounds which are substituted

The claimed invention is to triazin-2-yl and triazin-3-yl piperazines which are useful intermediates in the preparation of amino substituted steroid (XI) which are useful pharmaceutical agents.

Triazinylpiperazinyl amine intermediates

Pharmaceutically active pyrimidinylpiperazinylsterioids

The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).

Growing community of inventors

Kalamazoo, MI, United States of America

John R Palmer