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: 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.
Type:
Grant
Filed:
August 8, 1988
Date of Patent:
March 24, 1992
Assignee:
Upjohn Company
Inventors:
John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
Abstract: The present invention is a process for the production of a ketolactone of formula III ##STR1## which comprises contacting an aldehyde lactone of formula I ##STR2## with a .beta.-ketophosphonate (X.sub.1 --O--).sub.2 --PO--CH.sub.2 --CO--X.sub.15 (II). The ketolactone (III) is a useful intermediate in the synthesis of prostaglandins.
Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.
Type:
Grant
Filed:
October 3, 1986
Date of Patent:
April 30, 1991
Assignee:
Upjohn Company
Inventors:
Douglas L. Rector, George A. Conder, Sylvester D. Folz