Abstract: The invention relates to a process for the enantioselective preparation of L-phosphinothricin (L-Ptc) and derivatives of the formula I ##STR1## in which R.sup.1 is H, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.4)-haloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl or (subst.) phenyl-(C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen, formyl, [(C.sub.1 -C.sub.6)alkyl]carbonyl, [(C.sub.1 -C.sub.6)alkoxy]carbonyl, (subst.) benzyloxycarbonyl, (C.sub.1 -C.sub.6)-alkylsulfonyl or (subst.) (C.sub.6 -C.sub.10)-arylsulfonyl, and R.sup.3 is OH, NH.sub.2 or (C.sub.1 -C.sub.6)-alkoxy, or their salts with acids or bases.
Abstract: A process for the continuous reaction of halogenopyrimidines with amines, a halogenopyrimidine and an aqueous amine solution or suspension being passed into a reactor and the reaction product being subsequently conducted away, is described, characterized in that the starting materials are introduced into the reactor simultaneously and continuously with intensive mixing.
Type:
Grant
Filed:
February 22, 1994
Date of Patent:
May 30, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Siegbert Arnold, Hans-Georg Frosch, Manfred Hoppe, Wolfgang Mullers, Richard Sommer
Abstract: This invention provides a process for producing a cyclic carbonate compound represented by the following formula (5): ##STR1## or the like which is useful as a dissolution inhibitor for use in a chemically amplified positive photoresist, as well as a positive photoresist composition comprising said cyclic carbonate compound, an alkali-soluble resin and a photo-induced acid precursor. This composition gives a positive photoresist excellent in performances such as resolution, profile, sensitivity, etc.
Abstract: A reactive dye comprising a 1,3,5-s-triazine group having a chromophoric group at two of the 2-, 4- and 6-positions and a substituent at the remaining 2-, 4- or 6-position selected from H, optionally substituted alkyl, optionally substituted phenyl, --CH(CO.sub.2 R.sup.1).sub.2, --NR.sup.1 SO.sub.2 R.sup.2, and --SO.sub.2 R.sup.2, wherein each R.sup.1 is H or alkyl and R.sup.2 is alkyl. The reactive dyes may be used for the coloration of textile materials.
Abstract: A class of 4-hydroxy-2(1H)-pyrrolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
Type:
Grant
Filed:
May 10, 1993
Date of Patent:
May 30, 1995
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
Abstract: Phsophonate esters can be synthesized in high yields by condensations of alcohols with methyl phosphonates followed by selective demethylation. The reaction is general, relativly insensitive to steric constraints of hindered phosphonic acids, and can also be carried out on a solid support to synthesize large collections of compounds to screen for pharmacological activity.
Abstract: Benzyl derivatives of the formula I ##STR1## where A isCH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B isOH, alkylthio, alkoxy or alkylamino,U, V, W arehydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' ishydrogen or alkyl andR ishydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.
Abstract: Provided is a long chain carboxylic acid imide ester (I) represented by the following general formula (I) ##STR1## wherein W is a divalent long chain hydrocarbon group which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen atom, a sulfur atom, and a group of --N(R.sup.1)-- (R.sup.1 being a lower alkyl group) and X represents a divalent hydrocarbon group which may optionally be substituted, or salts thereof. The above long chain carboxylic acid imide ester or its salts is useful for modifying enzymes or proteins having biological activities to give their derivatives which have, while retaining most of the original biological activities, an extremely prolonged plasma half-life as compared with the proteins and have no antigenecities and can be administered to animals.
Abstract: Novel compounds of the formula I and formula II ##STR1## in which R and R.sub.1, independently of one another, are hydrogen or C.sub.1 -C.sub.4 alkyl or together with the carbon atom to which they are attached form a 3,4-dehydrocyclohexylidene ring,R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.3 is C.sub.1 -C.sub.8 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4, R.sub.5 and R.sub.6, independently of one another, are hydrogen or C.sub.1 -C.sub.4 alkyl, when alkyl, R.sub.4, R.sub.5 and R.sub.6 together containing 1 to 4 carbon atoms, andR.sub.7 and R.sub.8 are hydrogen or together an additional direct bond, are described for use as stabilizers for organic materials against thermal, oxidative or light-induced degradation.
Abstract: Dialkyl carbonates can be prepared by reaction of carbon monoxide with alkyl nitrites in a continuous gas-phase reaction using a platinum metal catalyst on a metal phosphate support and adding hydrogen halide stepwise or continuously during the course of the reaction in almost quantitative selectivity; the corresponding dialkyl oxalates are formed in such small amounts that in most cases they cannot be detected.
Type:
Grant
Filed:
April 22, 1994
Date of Patent:
May 9, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Joerg-Dietrich Jentsch, Alexander Klausener, Heinz Landscheidt, Erich Wolters, Eberhard Zirngiebl
Abstract: Disclosed herein are an azole derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 respectively represent a (C.sub.1 -C.sub.5) alkyl group or a hydrogen atom; X represents a halogen atom, a (C.sub.1-C.sub.5) alkyl group or a phenyl group; n represents an integer of from 0 to 2 and A represents a nitrogen atom or a CH, provided that R.sup.1 is not a hydrogen atom when R.sup.2 is a hydrogen atom, a process for producing the azole derivative represented by the formula (I), and an agricultural and horticultural composition containing the azole derivative represented by the formula (I).
Abstract: A process for preparing compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined herein,R.sub.2, R.sub.3, and R.sub.4 are each independently straight or branched chain (C.sub.1-4)alkyl,and pharmaceutically acceptable salts, physiological hydrolyzable esters, and pro-drug forms thereof, which are useful as hypoglycemic agents.
Abstract: The reactive dyestuffs of the formula ##STR1## wherein the substituents have the meaning given in the description, are particularly suitable for dyeing naturally occurring and synthetic materials containing OH groups and/or amide groups.
Type:
Grant
Filed:
January 26, 1993
Date of Patent:
May 2, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Thomas Eizenhofer, Wolfgang Harms, Karl-Josef Herd
Abstract: Substituted pyrroloanthracenes are prepared by reacting either furanoanthracenes or N-unsubstituted pyrroloanthracenes with appropriately substituted alkylamines. The compounds can be employed as active ingredients in medicaments, in particular as immunomodulators.
Type:
Grant
Filed:
December 9, 1993
Date of Patent:
May 2, 1995
Assignee:
Bayer Aktiengesellschaft
Inventors:
Eckhard Schwenner, Gaetan Ladouceur, Hans-Joachim Kabbe, Thomas M. Aune
Abstract: The present invention relates to substituted 2, 5-diaryl-4-isothiazolin-3-ones, pharmaceutical preparations containing them, and their use in the treatment of, thrombosis and, especially inflammation.
Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.
Type:
Grant
Filed:
May 27, 1994
Date of Patent:
May 2, 1995
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
Abstract: These acrylic and methacrylic compounds are chosen from those of the formula: ##STR1## in which R.sup.1 is H or CH.sub.3 ; A is (CH.sub.2).sub.n or n is an integer from 2 to 12 or --(CH.sub.2 CH.sub.2 O).sub.d --CH.sub.2 CH.sub.2 --, d is an integer from 1 to 20; X is S or O; Y is S or O, under the condition that X is S and Y is O when A is --(CH.sub.2 CH.sub.2 O).sub.d --CH.sub.2 CH.sub.2 --; R is C.sub.1 --C.sub.20 alkyl or --(CH.sub.2).sub.p SR.sup.3 where p is an integer from 3 to 12 and R.sup.3 is C.sub.1 -C.sub.20 -alkyl; m is an integer from 1 to 3; and Z is H, R.sup.2 QH, or R.sup.2 is C.sub.2 -C.sub.12 -alkyl and Q is O or S, and the atoms of the metals from Groups IA, IIA, IIIA, IB, IIB, VIB, VIIB and VIII of the Periodic Table, on condition that Z is H or R.sup.2 OH when m is 1 and m is the valence of Z when Z is a metal.
Type:
Grant
Filed:
December 14, 1992
Date of Patent:
May 2, 1995
Assignee:
Elf Atochem S.A.
Inventors:
Martine Cerf, Jean-Luc Mieloszynski, Daniel Paquer
Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Abstract: New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line "- - - -" is two double bonds or saturated single bonds).These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.
Abstract: A new compound, which we have named Leustroducsin H, has formula (I): ##STR1## and pharmaceutically acceptable salts thereof. This compound may be prepared by hydrolysis of naturally occurring Leustroducsins and the compound may be used for the treatment or prophylaxis of thrombocytopenia.