Abstract: The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.
Type:
Grant
Filed:
August 4, 1988
Date of Patent:
June 19, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Philippe Bey, David M. Stemerick, Michael L. Edwards, Alan J. Bitonti
Abstract: A compound of the formula: ##STR1## wherein R is a C.sub.2 -C.sub.3 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, or a C.sub.3 -C.sub.4 alkynyl group, and X is a chlorine or bromine atom, is disclosed. These compounds are useful as intermediates in the production of herbicidal 3-chlorotetrahydroindazoles.
Type:
Grant
Filed:
August 3, 1989
Date of Patent:
June 12, 1990
Assignee:
Sumitomo Chemical Company, Limited
Inventors:
Toru Haga, Eiki Nagano, Ryo Sato, Ryo Yoshida
Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
Type:
Grant
Filed:
August 1, 1988
Date of Patent:
May 15, 1990
Assignee:
Boots Company, PLC
Inventors:
John R. Housley, James E. Jeffery, David N. Johnston, Bruce J. Sargent
Abstract: This invention relates to an improved process for the preparation of polynuclear aromatic polyamines in which the reaction product is prepared by condensing aniline with formaldehyde in the presence of water and acidic catalysts and is worked up by extraction with a hydrophobic solvent. The acid catalyst that accumulates in the aqueous phase during the extraction process is reused.
Type:
Grant
Filed:
April 6, 1989
Date of Patent:
May 8, 1990
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hartmut Knofel, Michael Brockelt, Marcel Petinaux, Rudolf Uchdorf
Abstract: The invention is directed to 1-(2,6-Dimethyl-Phenyl-amino)-2-Dimethyl-amino-Propane and the pharmaceutical composition thereof useful for the treatment of cardiac rhythm disorders.
Abstract: The optically active isomer of S(-)-N-(1'methyl-2'-methoxyethyl)-N-chloroacetyl-2,6-dimethylaniline has improved action against problem weeds over the racemic mixture of isomers.
Abstract: The present invention is directed to a new chemical compound, 1,5-diaminoheptanol-6, which corresponds to the formula ##STR1## The present invention is additionally directed to a process for the preparation of 1,5-diaminoheptanol-6 by reacting L-lysine in its free form and/or in the form of its HCl salt, with acetic acid anhydride in the presence of a tertiary organic amino base and with the addition of a 4-aminopyridine derivative, hydrogenating the resulting 1,5-bisacetaminohepthanone-6 to 1,5-bisacetaminoheptanol-6, forming a salt of 1,5-diaminoheptanol-6 by treating 1,5-bisacetaminoheptanone-6 with a mineral acid and isolating the free amine by treating the 1,5-diaminoheptanol-6 salt of a mineral acid with a strong base.Finally, the present invention is directed to the use of 1,5-diaminoheptanol-6 as at least a portion of the chain lengthening agent for the preparation of polyurethane plastics by the isocyanate polyaddition process.
Abstract: The invention relates to the use of the fungus Amphobotrys ricini as a mycoherbicide to control texasweed (Caperonia palustris). Amphobotrys ricini has been found to infect and kill texasweed when applied to the plant and is considered effective at all stages of plant development.
Abstract: A process of forming N,N-dialkylhydroxylamines (a class of compounds useful as oxygen scavengers in boiler water feed) by contacting an N-alkylhydroxylamine with an alkyl carbonyl compound to form a nitrone in situ or, alternatively, using previously formed alkylnitrone which is subjected to H.sub.2 and a hydrogenation catalyst.
Type:
Grant
Filed:
December 14, 1987
Date of Patent:
March 20, 1990
Assignee:
W. R. Grace & Co.-Conn.
Inventors:
Nelson S. Marans, Stephen G. Harsy, Herbert S. Harris
Abstract: A process for preparing a 2,2,6,6-tetrahalocyclohexanimine derivative (I) which comprises reacting a 2,2,6,6-tetrahalocyclohexanone with a primary amine or ammonia in the presence of a Lewis acid, a process for preparing a 2,6-dihaloaniline derivative (II) which comprises subjecting the 2,2,6,6-tetrahalocyclohexaneimine derivative (I) to dehydrohalogenation in the presence or absence of a catalyst, and an N-phenyl-2,2,6,6-tetrahalocyclohexaneimine. According to the process of the present invention, the 2,2,6,6-tetrahalocyclohexaneimine derivative (I) can be prepared from inexpensive starting materials in high yield through a few steps. Also, the 2,6-dihaloaniline derivative (II) can be prepared from inexpensive starting materials in high yield and high purity through a few steps. Further, the N-phenyl-2,2,6,6-tetrahalocyclohexaneimine is very useful in the preparation of N-phenyl-2,6-dihaloaniline.
Abstract: When making an a amide by hydrolysis of a nitrile in an aqueous medium containing a Raney copper catalyst, the yield of amide can be increased and the yield of impurities can be decreased by including vanadium metal in the catalyst. The vanadium may be present as Raney vanadium often as an alloy in the Raney copper.
Type:
Grant
Filed:
May 19, 1987
Date of Patent:
March 6, 1990
Assignee:
Allied Colloids Ltd.
Inventors:
Gerald P. Benn, David Farrar, Seraj A. M. Karolia
Abstract: The present invention relates to a process for the preparation of alpha alkyl amino aldehydes of formula ##STR1## in which R is alkyl or aralkyl possibly substituted, characterized in that N,O-dimethylhydroxylamine is reacted, in a basic medium, on a blocked amine ester of an amino acid of formula ##STR2## and in that the product obtained is reduced with the aid of a hydride such as the double hydride of lithium-aluminum.
Abstract: Compounds of formula I wherein R.sup.1 and R.sup.2 are haloalkyl or halo, X is O, S, S(O), SO.sub.2 or NR.sub.4 where R.sub.4 is H or alkyl, R.sup.3 is alkyl and n is 1 to 4, and compositions comprising them, useful as insecticides.
Abstract: The present invention relates to a process for the treatment of depression comprising administering to a human in need thereof an antidepressant amount of a compound selected from 1-(2-fluorophenyl)-2-tertiobutylamino-1-ethanol and an addition salt thereof.
Abstract: This invention relates to sulfur-substituted phenylacetamides of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are H or CH.sub.3 ; R.sub.4 is SR.sub.5, ##STR2## R.sub.5 and R.sub.6 may be the same or different and are lower alkyl containing 1-4 carbon atoms and R.sub.5 and R.sub.6 may be taken together with S to form a 5-7 member ring; and X.sup.- is a pharmaceutically acceptable anion, which exhibit arrhythmia activity.
Abstract: Disclosed is a process for the preparation of monomethylhydrazine which comprises reacting hydrazine monohydrochloride with methanol in the presence of hydrazine dihydrochloride or methyl chloride and recovering free monomethylhydrazine from the formed monomethylhydrazine hydrochloride.According to this process, monomethylhydrazine can be prepared at a high selectivity very easily while controlling formation of by-products.
Abstract: High molecular weight amines having reduced low molecular weight amine contents are obtained by reacting a mixture of (1) a high molecular weight amine and (2) a low molecular weight amine with (3) an isocyanate in quantities such that from 0.5 to 10 equivalents of isocyanate are present for each equivalent of low molecular weight amine. The product of high molecular weight amines is particularly useful in the production of isocyanate addition products such as polyurethane plastics and foams.
Type:
Grant
Filed:
September 23, 1985
Date of Patent:
August 8, 1989
Assignee:
Bayer Aktiengesellschaft
Inventors:
Werner Rasshofer, Ernst Grigat, Gerhard Grogler, Heinrich Hess, Richard Kopp
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Type:
Grant
Filed:
August 27, 1982
Date of Patent:
August 8, 1989
Assignee:
Hoechst-Roussel Pharmaceuticals, Inc.
Inventors:
Lawrence L. Martin, Manfred Worm, Charles A. Crishlow