Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.
Type:
Application
Filed:
January 19, 2001
Publication date:
September 13, 2001
Applicant:
De Montfort University
Inventors:
Gerald Andrew Potter, Lawrence Hylton Patterson, Michael Danny Burke
Abstract: Acylsulfamoylbenzamides of the formula I and crop protection compositions comprising them are described. In this formula I, R1, R2, R3, R4 and R5 are various organic radicals and X is CH or N.
Type:
Grant
Filed:
September 25, 1998
Date of Patent:
June 26, 2001
Assignee:
Hoechst Schering AgrEvo GmbH
Inventors:
Frank Ziemer, Lothar Willms, Thomas Auler, Hermann Bieringer, Christopher Rosinger
Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
Type:
Application
Filed:
December 26, 2000
Publication date:
June 7, 2001
Applicant:
AstraZeneca UK Limited
Inventors:
Andrew Baxter, Thomas Mcinally, Michael Mortimore, David Cladingooel
Abstract: The present invention provides dihalopropene compounds of the general formula:
wherein R1 is C1-C10 alkyl or the like; L is C(═O)NH or the like; R2, R3 and R4 are independently halogen or the like; R5, R6 and R7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
Abstract: Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula:
in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue.
Type:
Grant
Filed:
June 21, 1999
Date of Patent:
January 23, 2001
Assignee:
Instituto Biochimico Pavese Pharma S.p.A.
Inventors:
Pierre Paul Vanlemmens, Denis Ghislain Postel, Pierig Emmanuel Germain, Ren{acute over (e)} Jean-Marie Julien, Jean-Pierre Constant Petit, Gino Lino Ronco, Pierre Joseph Villa
Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
Abstract: Pyridyl-thiazoles of the formula ##STR1## intermediates of the formulae ##STR2## and their salts and acid adducts suitable for the protection of plants against attack by undesirable microorganisms are disclosed.
Type:
Grant
Filed:
May 24, 1999
Date of Patent:
December 12, 2000
Assignee:
Bayer Aktiengesellschaft
Inventors:
Bernd Gallenkamp, Klaus Stenzel, Gerd Hanssler, Stefan Dutzmann, Heinz-Wilhelm Dehne
Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.
Type:
Grant
Filed:
November 13, 1997
Date of Patent:
November 28, 2000
Assignee:
Euro-Celtique, S.A.
Inventors:
David J. Cavalla, Mark Chasin, Lloyd Dolby
Abstract: The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I): ##STR1## that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Grant
Filed:
June 21, 1999
Date of Patent:
November 21, 2000
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
David Mark Rotstein, Eric Brian Sjogren
Abstract: A platinum complex useful as a catalyst for converting nitrites into amides comprises a platinum complex of dialkyl phosphine of stoichiometric formula: PtX(R.sub.2 POHOPR.sub.2)(PR.sub.2 OH) where R is an alkyl, alicyclic, chiral, alkylaryl group or substituted alkyl, alicyclic, chiral, alkaryl group or the two R groups attached to one phosphorous atom can form a heterocyclic ring with the phosphorous atom and X is H or a halide. The conversion takes place under reflux conditions to give a high yield of the amide.
Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
Abstract: An antiproliferative, antiinflammatory, antiinfective, immunization agent of a metal ion chelating agent such as picolinic acid or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes required for growth, replication or inflammatory response. The preparations can be administered systemically or for topical use. The preparations have antineoplastic, antiviral, antiinflammatory and antiproliferative effects and are used in the treatment of warts, psoriasis, acne, skin cancers, sunburn and other proliferative diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS. The agents also can be used to induce autologous immunological response.
Abstract: The present invention relates to a malondialdehyde-acetaldehyde adduct which acts as a specific immune-enhancing factor. In addition to its highly specific and immunogenic properties, the factor is highly fluorescent. It has an excitation frequency of about 398 nanometers and an absorbance of about 460 nanometers. The factor is also highly reactive and is also adducted to antigens including complex proteins, lipids, carbohydrates or DNA.
Type:
Grant
Filed:
May 27, 1997
Date of Patent:
September 19, 2000
Assignee:
The Board of Regents of the University of Nebraska
Inventors:
Geoffrey M. Thiele, Thomas L. McDonald, Dean J. Tuma, Lynell W. Klassen, Michael F. Sorrell
Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters 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:
December 22, 1997
Date of Patent:
September 19, 2000
Assignee:
GPI NIL Holdings, Inc
Inventors:
Gregory S. Hamilton, Jai-He Li, Wei Huang
Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
Type:
Grant
Filed:
July 15, 1997
Date of Patent:
July 4, 2000
Assignees:
ICAgen, Inc., Eli Lilly & Company
Inventors:
Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
Abstract: The present application describes 6-membered aromatics of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein D may be CH.sub.2 NH.sub.2 or C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
May 9, 2000
Assignee:
Dupont Pharmaceuticals
Inventors:
James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Ruth Richmond Wexler
Abstract: This invention relates to a process for preparing 2-substituted pyridines via metal halogen exchange with sec-butyllithium on optionally substituted 2-bromo or 2-iodopyridines. The resulting lithopyridine intermediate is reacted with an electrophile to provide the desired 2-substituted pyridine. The substitution of sec-butyllithium for n-butyllithium in such a process results in an enhanced yield and purity of the desired 2-substituted pyridine.
Type:
Grant
Filed:
May 5, 1999
Date of Patent:
April 25, 2000
Assignee:
Rohm and Haas Company
Inventors:
Martha Jean Kelly, Damian Gerard Weaver
Abstract: This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
Type:
Grant
Filed:
December 9, 1998
Date of Patent:
April 25, 2000
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
Abstract: A compound expressed by the following formula (1) and a liquid crystalline composition with using it are provided: ##STR1## wherein, either one of rings A, B and C denotes ##STR2## remaining two of them denote each independently ##STR3## R denotes an alkyl group or an alkoxy group with 4-16 carbon atoms, R* denotes ##STR4## in which, R.sub.1 denotes CH.sub.3, CF.sub.3, CH.sub.2 F or CHF.sub.2, R.sub.2 denotes an alkyl group with 1-10 carbon atoms and m denotes 2-12.The said compound exhibits a ferroelectric liquid crystalline phase and an antiferroelectric liquid crystalline phase by itself.
Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.
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. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
October 29, 1998
Date of Patent:
December 14, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
Abstract: Pyridylacetic acid compounds of the formula I ##STR1## where X is NOCH.sub.3. CHOCH.sub.3, CHCH.sub.3 or CHCH.sub.2 CH.sub.3 ; andY is oxygen or NR', and salts thereof,processes and intermediates for their preparation and compositions containing them which are used for controlling animal pests and fungi.
Type:
Grant
Filed:
April 29, 1998
Date of Patent:
October 12, 1999
Assignee:
BASF Aktiengesellschaft
Inventors:
Bernd Muller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Rohl, Norbert Gotz, Michael Rack, Ruth Muller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
Type:
Grant
Filed:
October 28, 1997
Date of Patent:
July 6, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
Abstract: Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R.sup.1.sub.(m) represents up to 6 substituents, K represents --O--, --S--, --CH.sub.2 --, --N(R.sup.2)-- or --N(COR.sup.2)--, in which R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, W is a carbonyl, sulfonyl or sulfinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description, and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors.
Type:
Grant
Filed:
April 23, 1998
Date of Patent:
July 6, 1999
Assignee:
James Black Foundation Limited
Inventors:
Sarkis Barret Kalindjian, Katherine Isobel Mary Steel, Michael John Pether, Jonathan Michael Richard Davies, Caroline Minli Rachel Low, Martin Lyn Hudson, Ildiko Maria Buck, Iain Mair McDonald, David John Dunstone, Matthew John Tozer
Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein A is N or CH; V is O or NH; m and n are integers 0 and 1 provided that m+n is 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4) alkoxy;R is independently selected from, (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic moieties;R is independently selected from (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic;R.sub.1 and R.sub.2 are independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halo(C.sub.1 -C.sub.
Type:
Grant
Filed:
June 2, 1997
Date of Patent:
March 16, 1999
Assignee:
Rohm and Haas Company
Inventors:
Ronald Ross, Ted Tsutomu Fujimoto, Steven Howard Shaber
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, 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 possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
Type:
Grant
Filed:
October 27, 1994
Date of Patent:
January 26, 1999
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Siegfried H. Reich, Kathleen Lewis, Michael Melnick, Mary Ann M. Fuhry, Stephen Warren Kaldor
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: The present invention is directed to substituted bicycloheptanedion e derivatives represented by a general formula ?I!; ##STR1## wherein R represents C.sub.1 -C.sub.4 alkyl, R.sup.1 represents hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aralkyl, C.sub.2 -C.sub.4 haloalkynyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 haloalkenyl, etc. and R.sup.2 represents optionally substituted phenyl or optionally substituted pyridyl, the salts thereof and herbicides comprising the same as the active ingredient.
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:
October 20, 1998
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
Abstract: Substituted 2-phenylpyridines I ##STR1## where substituents have the meaning described in the specification and their use as herbicides; for the desiccation/defoliation of plants.
Type:
Grant
Filed:
July 3, 1997
Date of Patent:
May 5, 1998
Assignee:
BASF Aktiengesellschaft
Inventors:
Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
Abstract: Vulcanization accelerators constituted by compounds belonging to the class of dihydropyridines having the general formula (I): ##STR1## and their use in natural or synthetic rubbers.
Type:
Grant
Filed:
February 20, 1997
Date of Patent:
May 5, 1998
Assignee:
Great Lakes Chemical Italia S.r.l.
Inventors:
Fabio Broussard, Mauro Adovasio, Jose Roncalli
Abstract: Substituted 2-phenylpyridines I ##STR1## where the substituents have the meaning given in the specification and their use.
Type:
Grant
Filed:
July 3, 1997
Date of Patent:
March 31, 1998
Assignee:
BASF Aktiengesellschaft
Inventors:
Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Hartmann Konig, Albrecht Harreus, Norbert Gotz, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
Abstract: HIV protease inhibitors, obtainable by chemical synthesis, 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 possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
Type:
Grant
Filed:
October 27, 1994
Date of Patent:
February 3, 1998
Assignee:
Agouron Pharmaceuticals
Inventors:
Siegfried H. Reich, Mark J. Pino, Dzuy T. Nguyen, Anthony J. Trippe
Abstract: The reaction of cyanoolefins, aminocarbonylolefins or hydroxyiminoolefins with a Vilsmeier reagent leads to 2-halogenopyridines which bear aldehyde groups in the 3 and/or 5 position. These pyridinealdehydes are valuable intermediates for the preparation of pharmaceuticals and crop protection agents.
Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.
Type:
Grant
Filed:
December 28, 1994
Date of Patent:
January 6, 1998
Assignee:
Monsanto Company
Inventors:
Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.
Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 21, 1997
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are, for example, an alkyl chain,A is a mesogenic group, andM is a spacer group,are highly suitable as components of liquid-crystal mixtures.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
October 21, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Claus Escher, Gerhard Illian, Hubert Schlosser, Rainer Wingen
Abstract: Patients susceptible to or suffering from central nervous system are treated by administering an effective amount of an aryl substituted olefinic amine compound, such as (E)-metanicotine. (E)-metanicotine is provided from nicotine. Nicotine is reacted with ethyl chloroformate to produce ethyl N-methyl-N-[4-chloro-4-(3-pyridyl)butyl]carbamate, which then is reacted in the presence of potassium tert-butoxide, tetrahydrofuran and dimethylformamide to produce (E)-metanicotine N-ethyl carbamate, which then is subjected to hydrolysis using hydrochloric acid to produce a reaction mixture containing (E)-metanicotine. The reaction mixture containing (E)-metanicotine is adjusted to a slightly basic pH, and then contacted with dichloromethane. The resulting water immiscible phase then is separated from the aqueous phase. The aqueous phase, then is adjusted to a very basic pH, and then contacted with methyl tert-butyl ether.
Abstract: A process for preparing a compound of general formula ##STR1## where Ar represents an optionally substituted aromatic or heteroaromatic group, the process comprising reacting a compound of general formulaAr--C(L.sup.1).sub.2 Cl (II)where each L.sup.1 independently represents a leaving group (preferably a chlorine atom), with water in the presence of a Lewis acid and a chlorocarbon solvent which includes at least two chlorine atoms, is disclosed.
Type:
Grant
Filed:
October 3, 1994
Date of Patent:
June 17, 1997
Assignee:
American Cyanamid Co.
Inventors:
Michael John Bull, John Warcup Cornforth
Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I
in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
Type:
Grant
Filed:
June 20, 1991
Date of Patent:
March 6, 2001
Assignee:
Schering Aktiengesellschaft
Inventors:
Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles