Abstract: A method of preparing a thiophene comprises reacting an organic compound containing a chain of at least 4 C atoms linked by single or double bonds with a source of sulphur in the vapor phase, in the presence of a supported catalyst, the catalyst having the composition(Fe.sub.0-1 M.sub.1-0)O.sub.nwherein M is a metal of Group VA, VIA or VIIA; and n is an appropriate value.
Type:
Grant
Filed:
June 24, 1996
Date of Patent:
March 10, 1998
Assignee:
Shell Research Limited
Inventors:
Graham John Hutchings, Richard William Joyner, Barry William Luke Southward, Russel Andrew Stewart, Lance Svend Fuller
Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.
Type:
Grant
Filed:
October 11, 1996
Date of Patent:
March 10, 1998
Assignee:
Adir et Compagnie
Inventors:
Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
Abstract: A method of producing optically active tert-leucinol (formula I) of high enantiomeric purity ##STR1## by converting racemic (RS)-tert-leucinol into a diastereomeric salt pair by reaction with an optically active acid, removing the salt pair from solution by fractionated crystallization and separating therefrom the optically active acid to release the optically active tert-leucinol from the salt. The optically active acid used is an N-acylated tert-leucine of general formula VIII: ##STR2## in which R can be hydrogen or an alkyl-, arylalkyl- or aryl group with up to 20 C atoms and * signifies a chirality center.
Type:
Grant
Filed:
February 21, 1996
Date of Patent:
March 3, 1998
Assignee:
Degussa Aktiengesellschaft
Inventors:
Karlheinz Drauz, Wilfried Jahn, Michael Schwarm
Abstract: A process for preparing an aliphatic thioamide entails reacting a nitrile compound of the general formulaR.sub.1 R.sub.2 R.sub.3 C--CN,wherein R.sub.1 denotes a hydrogen atom, an alkyl radical containing from 1 to 5 carbon atoms or an aryl radical and R.sub.2 and R.sub.3 each denotes a hydrogen atom containing from 1 to 5 carbon atoms, with hydrogen sulphide, in the presence as catalyst of an aliphatic amine of the general formulaR.sub.4 R.sub.5 R.sub.6 N,wherein R.sub.4 denotes an alkyl radical containing 1 to 5 carbon atoms and R.sub.5 and R.sub.6 each denotes a hydrogen atom or an alkyl radical containing 1 to 5 carbon atoms, in a water-miscible polar solvent.
Type:
Grant
Filed:
August 8, 1995
Date of Patent:
March 3, 1998
Assignee:
Fine Organics, Ltd.
Inventors:
Arthur Jackson, Graham Heyes, David Holmes, Craig Morgan
Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
Type:
Grant
Filed:
June 23, 1997
Date of Patent:
March 3, 1998
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Joseph M. Karpinski
Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth are disclosed. The method comprises administering a nitroso or nitrone spin trap such as N-t-butyl-.alpha.-phenylnitrone (PBN) to the affected tissue.
Abstract: This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon residue; R.sup.2 is an optionally esterified carboxyl group; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R.sup.2 ; and Y is a bond, --O--, --S(O)m-- (wherein m is 0, 1 or 2) or --N(R.sup.4)-- (wherein R.sup.4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.
Abstract: Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
Type:
Grant
Filed:
November 8, 1996
Date of Patent:
February 17, 1998
Assignee:
Glaxo Wellcome Inc.
Inventors:
Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth is disclosed. The method comprises administering 2,2-disubstituted-4,4-dimethyl-3-oxazolidinyloxy (DOXYL) to the affected tissue.
Abstract: Described are preferred suicide inhibitors of phosphatase or phosphodiesterase enzymes, and methods for preparing halo enol phosphates which can serve as such suicide inhibitors.
Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth is disclosed. The method comprises administering substituted or unsubstituted 2,2,5,5-tetramethyl-1-pyrrolidinyloxyl (PROXYL) to the affected tissue.
Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth are disclosed. The method comprises administering a spin label such as 2-(acetoxymercuri)-4,4,5,5-tetramethyl-2-imidazolin-1-yloxy-3-oxide, 3-carbamoyl-2,5-dihydro-2,2,5,5,-tetramethyl-1H-pyrrol-1-yloxy, or 3-(?ethoxycarbonyl!-oxycarbonyl)-2,5-dihydro-2,2,5,5-tetramethyl-1H-pyrrol -1-yloxy to the affected tissue.
Abstract: A process for preparing thioxanthone and derivatives thereof is disclosed. In the process, an aromatic compound, such as cumene, is reacted with thiosalicylic acid (TSA) or dithiosalicylic acid (DTSA) in the presence of sulfuric acid. The reaction mixture, which includes thioxanthone or a derivative thereof, is thereafter distilled under reduced pressure to recover the thioxanthone compound.
Type:
Grant
Filed:
April 29, 1996
Date of Patent:
January 27, 1998
Assignee:
First Chemical Corporation
Inventors:
Amy Lisa Bearson, John Robert Ira Eubanks, Alan Daniel Farmer, Franklin Dewitt Ford, Diana Boney Haydel, August John Muller
Abstract: The present invention provides processes for preparing compounds of formula I ##STR1## and for preparing compounds of formula VII ##STR2## Also provided are processes for preparing compounds of formula VII in addition to intermediates of formula IX ##STR3## wherein R.sup.1' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; andZ is bromo, iodo, triflate, or --B(OH).sub.2.
Type:
Grant
Filed:
October 27, 1995
Date of Patent:
January 27, 1998
Assignee:
Eli Lilly and Company
Inventors:
Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
Abstract: The present invention relates to compounds of the formula I ##STR1## wherein A, Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.
Type:
Grant
Filed:
July 11, 1994
Date of Patent:
January 27, 1998
Assignee:
Abbott Laboratories
Inventors:
Karl-Heinz Budt, Bernd Stowasser, Dieter Ruppert, Christoph Meichsner, Arnold Paessens, Jutta Hansen, Jochen Knolle
Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 20, 1998
Assignee:
Sugen, Inc.
Inventors:
Peng Cho Tang, Asaad S. Nematalla, Gerald McMahon
Abstract: The present invention provides useful intermediates for preparing 2-(substituted phenyl)benzothiophenes compounds said intermediates having the structure ##STR1## wherein R.sup.1 ' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; andZ is bromo, iodo, triflate, or --B(OH).sub.2 with the proviso that when Z is bromo or iodo, R1' is not alkoxy.
Type:
Grant
Filed:
October 27, 1995
Date of Patent:
January 20, 1998
Assignee:
Eli Lilly and Company
Inventors:
Kenneth L. Hauser, Alan D. Palkowitz, Daniel J. Sall, Kenneth J. Thrasher
Abstract: A compound of formula (I), wherein R.sup.1 and R.sup.2 are independently selected from chloro, fluoro, bromo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 haloalkyl provided that both R.sup.1 and R.sup.2 are not fluoro; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.
Abstract: Tri- and tetra substituted thiepane and compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 6, 1998
Assignee:
Gilead Sciences, Inc.
Inventors:
Lawrence R. McGee, Choung U. Kim, Norbert W. Bischofberger, Steven Krawczyk
Abstract: 1. A method of producing flowable R,S-thioctic acid, R,S-thioctic acid and its use.2.1. Known methods of preparing flowable thioctic acid which can be galenically further processed by pressing to highly-concentrated, solid presentations with active-substance contents of more than 200 mg pure substance require the mixing of the thioctic-acid forms of different origins and/or a spraying on of galenic adjuvants from aqueous solution and a subsequent grinding process in order to arrive at a pressable granulate.2.2.
Type:
Grant
Filed:
March 20, 1996
Date of Patent:
January 6, 1998
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Horst Bethge, Kurt Klostermann, Roland Moller, Gerhard Sator