Abstract: A process for preparing a compound of the formula I:
or pharmaceutical acceptable salts thereof wherein X is —NR1—, —S(O)g—, or —O—; R1 is —H, C1-6 alkyl optionally substituted with one or more —OH, —CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is —H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are the same or different and are —H or halo; R6 is —H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy. The compounds are useful antimicrobial agents.
Type:
Grant
Filed:
March 3, 2000
Date of Patent:
November 6, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Dalton Ennis, Robert Louis Hoffman, Douglas K. Hutchinson, David John Anderson, Toni-Jo Poel, Richard Charles Thomas
Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA
These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
Type:
Grant
Filed:
September 5, 1997
Date of Patent:
October 30, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Valerie Ann Vaillancourt, Karen Rene Romines, Arthur Glenn Romero, John Alan Tucker, Joseph Walter Strohbach, Olivier Bezencon, Suvit Thaisrivongs
Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I
wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
Abstract: Anti-microbial oxazolidinone antibiotics are provided having formula I and formula II wherein R1 is methyl, ethyl, cyclopropyl, or dichloromethyl; R2 and R3 are independently hydrogen or fluoro; R4 is ethyl or dichloromethyl.
The oxazolidinone antibiotics have minimum inhibitory activity for monoamine oxidase. An assay for detecting such oxazolidinone antibiotics is carried out by incubating a potential oxazolidinone inhibitor with a monoamine oxidase, then adding 1-methyl-4-(1-methyl-2-pyrryl)-1,2,3,6-tetrahydropyridine and determining inhibitory activity of the antibiotic.
Abstract: The present invention provides compounds of Formula 1
or pharmaceutical acceptable salts thereof wherein A, G and R, are as defined in the claims which are antibacterial agents.
Type:
Grant
Filed:
November 27, 1998
Date of Patent:
July 3, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jackson B. Hester, Jr., Eldon George Nidy, Salvatore Charles Perricone, Toni-Jo Poel
Abstract: The present invention provides methods and compositions for enhancing the effectiveness of oxazolidinone antibacterial agents against gram-negative organisms infection by using an arginine derivative.
Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA
These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
Abstract: The present invention provides a compound of formula I
which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
June 19, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Steven Ronald Turner, Joseph Walter Strohbach, Suvit Thaisrivongs, Valerie A. Vaillancourt, Mark E. Schnute, John Alan Tucker
Abstract: The present invention provides a compound of formula I
Wherein R1 is C1-7 alkyl, optionally substituted by hydroxy or NR4R5; R2 is C1-7 alkyl substituted by hydroxy or NR4R5; R3 is H, F or C1-7 alkoxy; R4 and R5 together with N are a 5- or 6-membered heterocyclic moiety having 1-3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur in which sulfur may be substituted by one (1) or two (2) oxygen atoms; and pharmaceutically acceptable salts thereof Compounds of formula I of the present invention are useful as antiviral agents.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
June 19, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Steven Ronald Turner, Joseph Walter Strohbach, Suvit Thaisrivongs, Valerie A. Vaillancourt, Mark E. Schnute, Allen Scott
Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
January 22, 1999
Date of Patent:
May 29, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular amount of basic amine which comprises a pyranone compound as a pharmaceutically active agent, a basic amine in an amount of from about 0.1% to about 10% by weight of the total composition, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. In addition, the composition may further comprises one or more pharmaceutically acceptable oils. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic pyranone compounds.
Abstract: The present invention provides compounds of Formula 1
or pharmaceutical acceptable salts thereof wherein A, G and R1 are as defined in the claims which are antibacterial agents.
Type:
Grant
Filed:
May 18, 1998
Date of Patent:
April 17, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Jackson B. Hester, Jr., Eldon George Nidy, Salvatore Charges Perricone, Toni-Jo Poel
Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula III
These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
April 3, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Karen Rene Romines, John Alan Tucker, Arthur Glenn Romero
Abstract: The present invention provides a method of topically administering antimicrobial agents such as premafloxacin, premafloxacin-like compound, premafloxacin ester, ciprofloxacin, enrofloxacin, cefquinome, cefpodoxime, gentamicin or erythromycin for the treatment of systemic bacterial diseases in mammals.
Abstract: 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[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.
Type:
Grant
Filed:
November 9, 1998
Date of Patent:
January 2, 2001
Assignee:
Pharmacia & Upjohn Company
Inventors:
Karen Rene Romines, Gordon L. Bundy, Theresa M. Schwartz, Ruben A. Tommasi, Joseph W. Strohbach, Steven Ronald Turner, Suvit Thaisrivongs, Paul Adrian Aristoff, Paul D. Johnson, Harvey Irving Skulnick, Louis L. Skaletzky, David John Anderson, Joel Morris, Ronald B. Gammill, George P. Luke
Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1 ; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.
Type:
Grant
Filed:
August 24, 1998
Date of Patent:
December 26, 2000
Assignees:
Pharmacia, Upjohn Company
Inventors:
Richard C. Thomas, Toni-Jo Poel, Michael D. Ennis, David J. Anderson, Robert L. Hoffman
Abstract: The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).
Type:
Grant
Filed:
March 16, 1999
Date of Patent:
November 21, 2000
Assignee:
Pharmacia & Upjohn Company
Inventors:
Suvit Thaisrivongs, Steven Ronald Turner
Abstract: The present invention relates to a novel method for improving the pharmacokinetics of tipranavir, comprising administering to a human in need of such treatment a combination of a therapeutically effective amount of tipranavir or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of ritonavir or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 29, 1999
Date of Patent:
November 14, 2000
Assignee:
Pharmacia & Upjohn Company
Inventors:
James J. Ferry, John R. Baldwin, Marie T. Borin
Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.
Type:
Grant
Filed:
May 11, 1999
Date of Patent:
November 14, 2000
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Robert Barbachyn, Fred L. Homa, Antonio Monge, Esteban Santiago, Juan J. Martinez-Irujo, Maria Font