Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
July 11, 1997
Date of Patent:
January 19, 1999
Assignee:
Merck Frosst Canad, Inc.
Inventors:
Daniel Dube, Richard Friesen, Rejean Fortin, Zhaoyin Wang, Jacques Yves Gauthier
Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
Type:
Grant
Filed:
June 10, 1997
Date of Patent:
January 19, 1999
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter Losel, Otto Roos
Abstract: There is described a novel process of polymerizing 4-vinyl pyridine monomer in an aqueous polymerization system which comprises preparing an aqueous solution of polyvinyl alcohol, and contacting said aqueous solution of a polyvinyl alcohol with less than about 10% by weight of 4-vinyl pyridine monomer and a water-soluble initiator capable of decomposing to give free radicals.The resultant dispersion of the novel polymerization process comprises a homogeneous, i.e., weight average molecular weight and particle size, poly-4-vinylpyridine, with no appreciable residual 4-vinyl pyridine monomer.The resultant dispersion may be used to coat image- and ink-receiving layers of image-recording materials and ink jet recording sheets, respectively.
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 12, 1999
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Vincent J. Kalish, Siegfried H. Reich, John H. Tatlock, Michael J. Rodriguez
Abstract: A method of fluorinating a heterocyclic organic compound comprises the step of reacting a heterocyclic compound with elemental fluorine in the presence of another halogen. The reaction may be conducted in the presence of a base.
Type:
Grant
Filed:
June 20, 1997
Date of Patent:
January 12, 1999
Assignee:
F2 Chemicals Ltd.
Inventors:
Richard Dickinson Chambers, Graham Sandford
Abstract: An alpha-tocopherol is disclosed as a polymerization inhibitor effective against vinyl monomer polymerization. Alpha-tocopherol was found to inhibit polymerization of acrylonitrile and diolefines such as isoprene and butadiene. Alpha-tocopherol was found to interact synergistically with hydroquinone in inhibiting polymerization of acrylonitrile.
Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains N-phosphonoglycine derivatives which are systemic herbicides in combination with chemotherapeutic agents for treatment of cancers and tumors. N-phosphonoglycine derivatives can be used to treat viral infections, particularly herpes infections. Optionally potentiators can be included.
Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2)n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.
Abstract: The present invention is directed to compounds of formula (I), and the pharmaceutically acceptable acid addition salts thereof, wherein R is selected from the group consisting of F,--CF.sub.3, --OCH.sub.3, --O(C.sub.1)alkyl substituted with 1 to 3 fluoro atoms. --O(C.sub.2) substituted with 1 to 5 fluoro atoms, and --O(C.sub.3)alkyl substituted with 1 to 7 fluoro atoms. The compounds of formula (I) are useful in the treatment of stroke, traumatic brain injury and central nervous system degenerative diseases.
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 22, 1998
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Type:
Grant
Filed:
December 5, 1996
Date of Patent:
December 15, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Lin Chu, Thomas F. Walsh, Michael H. Fisher, Narindar N. Girotra, Matthew J. Wyvratt, Peter Lin, Wallace T. Ashton
Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
Type:
Grant
Filed:
November 2, 1995
Date of Patent:
December 15, 1998
Assignees:
GD Searle & Co., Monsanto Co.
Inventors:
Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
Abstract: A method and apparatus for treating a surface on a glass article with a fluid. The article is surrounded by a containment system for the treating fluid and the fluid is continuously agitated by an agitator.
Type:
Grant
Filed:
September 5, 1996
Date of Patent:
December 8, 1998
Assignee:
Corning Incorporated
Inventors:
Stephen P. Edwards, Donald B. Kloeber, Joseph W. Neubert, Stephen R. Ormsby
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
Type:
Grant
Filed:
February 28, 1997
Date of Patent:
December 8, 1998
Assignee:
GPI NIL Holdings, Inc.
Inventors:
Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
Abstract: Products prepared by reacting polyisocyanates with alkenyl or alkynyl compounds; then with perfluoroalkyl iodides & dehydroiodinating the product.
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 8, 1998
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
Abstract: N-Heteroaryl-N'-(pyrid-2-yl-sulfonyl)ureas, processes for their preparation, and their use as herbicides and plant growth regulatorsCompounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, A, n, m and w are as defined in claim 1, are suitable as herbicides for controlling harmful plants and can be prepared, inter alia, from the sulfonamides of the formula (II) ##STR2## by reacting them with carbamates R*O--CO--NR.sup.4 --A.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
December 8, 1998
Assignee:
Hoechst Schering AgrEvo GmbH
Inventors:
Rainer Schutze, Heinz Kehne, Klaus Bauer, Hermann Bieringer
Abstract: The present invention provides an industrially advantageous process for the preparation of an optically active 2-halo-1-(substituted phenyl)ethanol useful as medicines, agricultural chemicals or as intermediates thereof; and a simple process for the preparation of an optically active substituted styrene oxide or 2-amino-1-(substituted phenyl)ethanol useful as medicines, agricultural chemicals or intermediates thereof. A 2-halo-1-(substituted phenyl)ethanol represented by the following general formula (I) is allowed to contact, in the presence of a carboxylic anhydride, with an enzyme stereoselectively catalyzing ester interchange to produce an optically active 2-halo-1-(substituted phenyl)ethanol: ##STR1## (wherein X represents a chlorine atom or a bromine atom, and R.sup.1, R.sup.2 and R.sup.3 may be the same or different and each represent a hydrogen atom, a halogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 haloalkyl group, a C.sub.
Abstract: The present invention relates to a process of preparing quinacridone by oxidizing a 6,13-dihydroquinacridone salt corresponding to the quinacridone pigment with hydrogen peroxide as the oxidizing agent. The inventive process is economical and environmentally friendly and yields high performance quinacridone pigments in a high yield.