Abstract: The present invention comprises a process of preparing a solution of an enhanced efficacy aluminum antiperspirant salt in a polyhydric alcohol by(a) providing an aqueous solution consisting essentially of about 5% to about 18% by weight of an enhanced efficacy aluminum antiperspirant salt in water, the enhanced efficacy aluminum antiperspirant salt having been prepared in situ without having been dried to a solid powder;(b) mixing the aqueous solution with a sufficient amount of a liquid polyhydric alcohol to provide a mixed solution which has an antiperspirant salt to polyhydric alcohol ratio of about 1:4 to about 1.2:1; and(c) rapidly evaporating the water from the mixed solution under vacuum to provide a final liquid polyhydric alcohol solution containing about 20 to 50% enhanced efficacy aluminum antiperspirant salt and about 2 to 16% water, with the balance being polyhydric alcohol.
Type:
Grant
Filed:
June 13, 1997
Date of Patent:
August 17, 1999
Inventors:
Stephen J. Provancal, Angel L. Carrillo, Thomas J. Fluhler, Richard Oryszczak, Jayant N. Sane
Abstract: This invention relates to a novel quinolone- or naphthyridone-carboxylic acid derivative or its salt useful as an antibacterial agent, said derivative has a substituent represented by the following formula at the 7 position: ##STR1## wherein preferably R.sup.3 represents at least one member selected from the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl, lower alkoxy or lower alkylthio group, a nitro group, a cyano group, a protected or unprotected hydroxyl group and a protected or unprotected amino group; R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkylidene group and a group forming a cycloalkane ring together with the carbon atom to which R.sup.4 is bonded; and R.sup.5 represents a hydrogen atom or a substituted or unsubstituted lower alkyl or cycloalkyl group.
Abstract: The invention relates to a process for producing a carboxamide of the formula ##STR1## which comprises reacting ##STR2## with an excess of urea in water, wherein the variables in the above formulae are as described herein.
Abstract: The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein the group R.sup.2 is ##STR2## and R.sup.1, A, G, Y, Z and m have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.
Type:
Grant
Filed:
May 27, 1997
Date of Patent:
July 13, 1999
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Brigit Jung, Erich Burger, Georg Speck
Abstract: Compounds of formula (I) wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 14 CR.sup.2 is a double bond; X is selected from --Ch.sub.2 CH.sub.2 --, --C.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2, CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.
Type:
Grant
Filed:
October 26, 1995
Date of Patent:
July 6, 1999
Assignee:
Zeneca Limited
Inventors:
George Robert Brown, Paul Robert Owen Whittamore, David Robert Brittain
Abstract: N,N'-bridged bistetramethylpiperidinyl compounds, which are produced by reacting tetramethylpiperidinyl compounds with a cyclic carbonate, and are useful as light stabilizers for organic material.
Abstract: The present invention provides a method for treating a viral infection in a subject. The method comprises administering to the subject an amount of 5-aminolevulinic acid and an iron-chelating agent to cause virus-infected cells to accumulate protoporphyrin in amounts such that upon application of a sufficient dose of red light, the virus-infected, protoporphyrin-accumulated cells will be destroyed; and applying a sufficient dose of red light to the virus-infected, protoporphyrin-accumulated cells to destroy the virus-infected, protoporphyrin-accumulated cells.
Abstract: The present invention provides cholinesterase inhibitors of general formula (I): ##STR1## wherein R is H or (C.sub.1 -C.sub.4)alkyl, Y is a linking group and Z is an aryl group, and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
May 15, 1997
Date of Patent:
March 23, 1999
Assignee:
Mayo Foundation For Medical Education and Research
Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.
Abstract: 6,7-propylene-, butylene-, or pentylene-bridged imidazopyridin-4-amines that induce interferon (.alpha.) biosynthesis in human cells. Also disclosed are pharmaceutical compositions containing such compounds and methods of inducing interferon (.alpha.) biosynthesis and treating viral infections involving the use of such compounds.
Type:
Grant
Filed:
March 6, 1997
Date of Patent:
March 23, 1999
Assignee:
Minnesota Mining and Manufacturing Company
Abstract: A series of novel polyamine-linked acridine dimers and derivatives thereof are described. The polyamine-linked acridine dimers and derivatives are potential anti-cancer agents.
Abstract: The present invention are marefortines and paraherquamides where the 7-member oxygenated ring has been modified to produce 25-methylene compounds (VII) and 24,25-epoxy compounds (VIII) all of which are useful as antiparasitic agents against endo and ecto parasites, particularly helminths and arthropods.
Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
Type:
Grant
Filed:
July 21, 1997
Date of Patent:
March 16, 1999
Assignee:
Bristol-Myers Squibb Company
Inventors:
Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino, John E. Lawson, Henry M. Holava, Richard A. Partyka
Abstract: A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.
Abstract: Disclosed is a stable and effective formulation of a taxane analog, preferably paclitaxel. The formulation comprises a dimethylacetamide and polyethylene glycol solution of the drug that is diluted into an aqueous lipid emulsion prior to use. The formulation is effective as a parenterel drug against taxane sensitive tumors.
Type:
Grant
Filed:
June 28, 1996
Date of Patent:
March 2, 1999
Assignee:
Board of Regents, The University of Texas System
Abstract: A 2-silyloxy-4,5,6,7-tetrahydrothieno?3,2-c!pyridine represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent an alkyl group having 1 to 10 carbon atoms or an aryl group,and a salt thereof and a process for preparing the same, and a 5-alkyl-2-silyloxy-4,5,6,7-tetrahydrothieno?3,2-c!-pyridine represented by the formula (IV): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 represent the same meanings as described above; R.sup.4 represents a hydrogen atom, an alkoxycarbonyl group having 2 to 10 carbon atoms, an acyl group having 2 to 10 carbon atoms or a cyclo-alkylcarbonyl group having 4 to 10 carbon atoms; andR.sup.5 represents a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms,which is useful as a synthetic intermediate of an antiplatelet medicine and an elastase inhibitor, etc., and a process for preparing the same.
Abstract: "Novel compounds, such as: ##STR1## are disclosed. Also disclosed are methods for inhibiting the abnormal growth of cells, for inhibiting farnesyl protein transferase and for treating cancers using the novel compounds.
Type:
Grant
Filed:
December 12, 1996
Date of Patent:
February 23, 1999
Assignee:
Schering-Plough Corporation
Inventors:
Ronald J. Doll, Joseph M. Kelly, Alan K. Mallams, F. George Njoroge, Stacy W. Remiszewski, Arthur G. Taveras
Abstract: 1-Oxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)isoindolines and 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)isoindolines reduce the levels of TNF.alpha. in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindoline.
Type:
Grant
Filed:
November 18, 1997
Date of Patent:
February 23, 1999
Assignee:
Celgene Corporation
Inventors:
George W. Muller, David I. Stirling, Roger Shen-Chu Chen, Hon-Wah Man
Abstract: A compound which inhibits human thrombin and which has the general structure ##STR1##
Type:
Grant
Filed:
September 10, 1997
Date of Patent:
February 16, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Adel M. Naylor-Olsen, Gerald S. Ponticello, Joseph P. Vacca, Randall W. Hungate, Craig Coburn, Brian T. Phillips, S. D. Lewis, Mark E. Fraley
Abstract: An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. ##STR1## (symbols in the formula have the following meanings; R.sup.1 : a hydrogen atom or a group represented by the formula --A--W--R.sup.4,A: a group represented by the formula ##STR2## a group represented by the formula ##STR3## or a group represented by the formula --SO.sub.2 --, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula --NR.sup.5 --, R.sup.4 : a hydroxyl group, a lower alkoxy group, etc., R.sup.5 : a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R.sup.2 : a lower alkyl group, R.sup.