Abstract: A 5-oximino-25-substituted avermectin B1 or B2 monosaccharide of formula I herein has use in the treatment of parasitic infections in animals and humans. The compounds may be prepared from corresponding 5-keto substituted derivatives.
Type:
Grant
Filed:
May 9, 1997
Date of Patent:
November 9, 1999
Assignee:
Pfizer Inc.
Inventors:
Bernard Frank Bishop, Michael Stephen Pacey, David Austen Perry
Abstract: A compound of formula (I), wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
Abstract: A compound of the formula ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4 R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and Ar are as defined above, useful in the treatment of a condition seiected from the group consisting of arthritis, cancer, tisuue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other disease characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.
Abstract: A process for preparing a compound of formula (I): ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or benzyl, and wherein the phenyl moiety of said benzyl group is optionally substituted with one or two substituents each independently selected from halo, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino and trifluoromethyl, which comprises treating a solution of a compound of formula (II): ##STR2## wherein R is as defined for formula (I), and a halonitromethane in a first organic solvent, with a quaternary ammonium fluoride of formula (III):R.sup.1 R.sup.2 R.sup.3 F.sup.4 N.sup.+ F.sup.- (III)wherein R.sup.1,R.sup.2,R.sup.3 and R.sup.4 are each independently selected from C.sub.1 -C.sub.8 alkyl and benzyl, optionally in solution in a second organic solvent.
Abstract: Aqueous pharmaceutical solutions suitable for injection into a host, having improved injection site toleration, comprise danofloxacin or its pharmaceutically acceptable salts and a magnesium or zinc compound. The zinc compound in addition requires the presence of a co-solvent.
Abstract: The anhydrate of 7-(?1.alpha.,5.alpha.,6.alpha.!-6-amino-3-azabicyclo?3.1.0!hex-3-yl)-6-flu oro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt has advantageous stability for formulation as an antibacterial agent.
Type:
Grant
Filed:
May 21, 1997
Date of Patent:
June 9, 1998
Assignee:
Pfizer, Inc.
Inventors:
Lynne A. Handanyan, Thomas A. Morris, Robert L. Hendrickson, Phillip J. Johnson, Timothy Norris
Abstract: Antiparasitic compounds of the formula (I) ##STR1## where the broken lines between the 3-4 and 4-5 positions represent optional bonds and either (i) the 3-4 optional bond is present; the 4-5 optional bond is absent, R.sup.7 is absent and R.sup.6 is halogen atom, an isothiocyanate group, a diazo group, a thioureido group of formula NHCSNR.sup.15 R.sup.16 where R.sup.15 and R.sup.16 are independently H, C.sub.1 -C.sub.8 alkyl, cycloalkyl, aryl or aralkyl groups, an azido group or a C.sub.1 -C.sub.8 alkylcarbonyl-thio group, or (ii) the 4-5 optional bond is present, the 3-4 optional bond is absent, R.sup.6 is absent and R.sup.7 is a mercapto, C.sub.1 -C.sub.8 alkylthio, oxo, optionally substituted oximino or C.sub.1 -C.sub.8 alkylcarbonylthio group; or R.sup.7 is absent and R.sup.6 is CN, with the provisos that the compounds where R.sup.6 is .alpha.-fluoro and R.sup.2 is CH(CH.sub.3).sub.2, CH(CH.sub.3)C.sub.2 H.sub.5, C(CH.sub.3).dbd.CHCH.sub.3, C(CH.sub.3).dbd.CHC.sub.2 H.sub.5 and C(CH.sub.3).dbd.CHCH(CH.sub.
Abstract: An infection with Helicobacter may successfully be treated with a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl and R.sub.2 is hydrogen or L-alanine-L-alanyl, and the pharmaceutically acceptable acid additive salts thereof. These compounds are useful in the treatment of gastric and duodenal ulcers.
Abstract: Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
Abstract: Compound of formula (I) or salts thereof wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4 represents hydrogen or up to four substituents; X is S, SO, SO.sub.2 or CH.sub.2 ; Y is O, S, SO or SO.sub.2 ; n is 0 or 1; m is 1 or 2; and wherein in the (a) ring system the dotted line indicates that one pair of adjacent ring carbon atoms is joined by a C.dbd.C double bond. These compounds have antibacterial activity.
Type:
Grant
Filed:
January 25, 1995
Date of Patent:
June 3, 1997
Assignee:
Pfizer Inc.
Inventors:
George Burton, John H. Bateson, Richard L. Elliott, Stephen C. M. Fell
Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.
Type:
Grant
Filed:
March 1, 1995
Date of Patent:
April 29, 1997
Assignee:
Pfizer Inc.
Inventors:
Bingwei Yang, Joyce Sutcliffe, Chris J. Dutton
Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2 ; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkyl substituted with 1, 2 or 3 halogen atoms; R.sup.2 is selected from the group consisting of phenyl, substituted phenyl, heterocyclic groups, and substituted heterocyclic groups, said substituted phenyl and substituted heterocyclic groups being substituted with 1 or 2 substituents independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl, trifuluoromethyl, and halogen; R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, or R.sup.3 and R.sup.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
April 29, 1997
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, Joseph G. Lombardino, James M. McManus
Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof; wherein X.sub.1, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock etc.
Abstract: Avermectin and milbemycin derivatives of formula (I) ##STR1## having a double bond at the 3-4 position and a cyano substituent at the 3-position have outstanding anthelmintic properties. They may be prepared by allowing an avermectin or milbemycin derivative having a leaving group at the 5-position, or having double bonds at the 2-3 and 4-5 positions and no substituent at the 5-position, to react with an ionic cyanide.
Abstract: Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
Abstract: The invention relates to benzopyran leukotriene B.sub.4 (LTB.sub.4) antagonists and pharmaceutical compositions containing the compounds. The compounds inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders.
Type:
Grant
Filed:
September 30, 1994
Date of Patent:
August 27, 1996
Assignee:
Pfizer Inc.
Inventors:
Kevin Koch, Lawrence S. Melvin, Jr., Lawrence A. Reiter, Sally G. Ruggeri
Abstract: An improved device for repairing fractured bones is provided, the device comprising a specially designed connector, which is especially useful in combination with a plate having a tab cut out, a stop, a flat portion and a bore portion and with a compression screw and a lag screw.
Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof; wherein X.sub.1, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock etc.
Abstract: The present invention relates to novel substituted oxindoles of the formula I as defined below and related compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as inhibitors of phosphodiesterase ("PDE") type IV. The compounds of this invention are useful in the treatment of AIDS, asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, atopic, dermatitis, shock, other inflammatory diseases, and other conditions where the action of phosphodiesterase type IV is implicated.