Abstract: Immunoregulatory N-(S-3-alkyl-4-heptenoyl)- and N-(S-3-alkylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine and esters thereof are synthesized via R-trans-2-hexen-4-ols, R-3-alkyl-4-heptanoic acid and S-3-alkylheptanoic acid.
Abstract: An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1-yl]acetic acid esters.
Abstract: Improved means for constraining a rumen drug delivery device in a rolled configuration, said means comprising a laminate, which may be perforated, comprising a water-permeable material having a low friction surface in the presence of water, said material being bonded by means of a water-dispersible pressure sensitive adhesive to a repulpable tape, said tape having said water-dispersible pressure sensitive adhesive on both its surfaces; a laminate comprising a flexible, water-permeable polymeric material bonded between the low friction surface material and the repulpable tape; and devices constrained by said means.
Abstract: A series of novel 3-phenyl-3-[1-(cyclicalkyl)pyrrolidin-3-yl]glutarimide derivatives have been prepared, including their pharmaceutically acceptable salts. The cyclic moiety present in these compounds is derived from either benzene or a heteroaryl such as benzofuran or 2,3-dihydrobenzofuran, or it is derived from an aromatic heterocyclic such as pyridine, pyrazine or thiophene, and it is attached to the adjacent alkyl group of the molecule by means of one of the available ring carbon atoms situated in the aromatic ring of the aforementioned cyclic ring moiety. These particular compounds are useful in therapy as selective muscarinic receptor antagonists, which are selective for smooth muscle muscarinic sites over cardiac muscarinic sites and therefore, are of value in the treatment of diseases associated with altered motility and/or smooth muscle tone as found in the gut, trachea and bladder. Methods for preparing these compounds from known starting materials are provided.
Abstract: This invention relates to a process for resolving racemic or optically enriched 2-benzyl-4-piperidone-succinic acid, comprising reacting such compound with (+)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylamine, (-)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylamine or (+)-dehydroabietylamine.
Abstract: The invention provide antifungal compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.
Abstract: There is disclosed a bone cement composition comprising (a) a liquid component comprising a monomer of an acrylic ester and (b) a powdered component comprising a terpolymer of methyl methacrylate, butyl methacrylate, and styrene. A prepared terpolymer, based on the weight of the powdered component, has between 55 to 89.5% methyl methacrylate, 10 to 40% butyl methacrylate and 0.5 to 5% styrene.
Abstract: Certain 1-substituted 4-(1,2-benzisoxazolyl)-piperidine compounds exhibit neuroleptic activity and are useful in the treatment of psychosis and anxiety.
Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
Abstract: Process for the pancreatic lipase mediated transesterification method for the optical resolution of endo-norborneol; derived optically active 5-(3-(exo-bicyclo[2.2.1]hept-2-yloxy)-4-methoxyphenyl)-3,4,5,6-tetrahydrop yrimidin-2(1H)-ones; and stepwise process and intermediate therefor.
Abstract: A form of calcium carbonate having a blocky[-six-sided] rhombohedral crystal [habit ] structure and [a morphology, with] properties including a surface area of from about 3 to about 15 m.sup.2 /g, an average discrete particle size of from about 0.2 to about 0.9 micron, wherein the discrete particles have an aspect ratio less than 2, and a particle size distribution such that at least about 60 weight percent of the particles have a size within 50 percent of the equivalent discrete particle spherical diameter, suitable for use as a filler material in papermaking to improve the optical properties of the resulting paper, is disclosed.
Abstract: Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.
Type:
Grant
Filed:
January 26, 1993
Date of Patent:
December 14, 1993
Assignee:
Pfizer, Inc.
Inventors:
Wayne E. Barth, Kelvin Cooper, Edward F. Kleinman, Lawrence A. Reiter, Ralph P. Robinson
Abstract: A method of relieving erectile impotence in a human male. The method comprises administering to the male an erectile impotence relieving amount of a compound selected from the group consisting of U.K. 52,046, Amlodipine, Doxazosin and the pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
March 11, 1993
Date of Patent:
December 14, 1993
Assignee:
Pfizer Inc.
Inventors:
George M. Milne, Jr., Michael G. Wyllie
Abstract: Human insulin analogs are disclosed. These analogs are tissue-selective. Accordingly, pharmaceutical formulations containing the analogs of the invention provide superior clinical benefits as compared to human insulin when used in the treatment of patients suffering from diabetes. The analogs are modified at amino residue A12, A15 or A19, are different from the naturally occurring residue at said position, and are hepatoselective. Also disclosed are human insulin analogs modified at amino acid residues A12 or A14 or amino acid residues A10 and A13 different from naturally occurring residues or residues at said position or positions and are peripheral selective. DNA sequences and microorganisms comprising sequences coding for human insulin analogs are also provided. Processes for preparing the human insulin analogs are described.
Abstract: A method of modifying salts of alginic acid in situ for prevention and treatment of various intra-articular and extra-articular (spine) complications modifies the alginate in situ to an insoluble gel. This in situ modification provides a final product which can be compressed within the intra-articular space thus remaining localized. The modified material can have varied mechanical strengths and thus varied degradation times and can serve as a matrix for localizing and slowly releasing therapeutic agents. The modified material is biocompatible and biodegradable, thus requiring no reoperation for removal.
Type:
Grant
Filed:
June 30, 1992
Date of Patent:
November 30, 1993
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
James J. Barry, Paul A. Higham, Harold M. Aberman
Abstract: An implantable material for promoting bone growth has a microporous structure exhibiting an average pore size of at least 30 .ANG.. The porous biomaterial is capable of retaining macromolecules having a molecular weight of at least 15,000 and up to 500,000.
Type:
Grant
Filed:
November 20, 1992
Date of Patent:
November 23, 1993
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Qi-Bin Bao, John H. Dumbleton, Paul A. Higham