Abstract: This invention concerns a process for killing internal parasites, especially nematodes, trematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I. ##STR1## The compounds are readily prepared by conventional chemical reactions.
Type:
Grant
Filed:
January 30, 1990
Date of Patent:
September 17, 1991
Assignee:
The Upjohn Company
Inventors:
Douglas L. Rector, George A. Conder, Sylvester D. Folz
Abstract: A 5-fluorouracil derivative represented by the formula (1): ##STR1## wherein A represents a group represented by ##STR2## wherein R.sup.1 represents a hydrogen atom or OR.sup.5 group, R.sup.2, R.sup.3 and R.sup.5 may be the same or different and each represents a hydrogen atom or a group represented by the following formula (2): ##STR3## wherein R.sup.6 represents an acyl group, R.sup.7 represents a hydrogen atom, a straight or branched alkyl group, a cycloalkyl group, an aralkyl group, a lower alkenyl group or a phenyl group, and n is an integer of 0 to 6,provided that at least one of R.sup.2, R.sup.3 and R.sup.5 is a group represented by the formula (2), and the case whereinR.sup.2 and R.sup.5 are both hydrogen atoms is excluded,R.sup.4 represents a group represented by the formula (2), and X represents an alkylene group or a cycloalkylene group,and an antitumor agent containing the same as an active ingredient.
Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
Type:
Grant
Filed:
May 2, 1990
Date of Patent:
September 10, 1991
Assignee:
Warner-Lambert Co.
Inventors:
Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
Abstract: Compounds of the formula I ##STR1## in which Me is Ti, Zr or Hf, R.sub.1 is a group transferable to aldehyde, keto or imine groups, for example methyl, allyl, vinyl or the radical of an enol or enamine, R.sub.2 is, for example, cyclopentadienyl, R.sub.3 and R.sub.4 are, for example, H or alkyl, R.sub.5 is, for example, phenyl and the C(1) and C(2) atoms are chiral and have predominantly one configuration, are suitable for use as chiral reactants for aldehydes, ketones and imines for the preparation of both enantiomers of secondary or tertiary alcohols or tertiary amines.
Type:
Grant
Filed:
February 16, 1990
Date of Patent:
September 10, 1991
Assignee:
Ciba-Geigy Corporation
Inventors:
Andreas Hafner, Rudolf Duthaler, Guido Bold
Abstract: Highly pure 3,3',4,4'-biphenyltetracarboxylic acid (BPTA) and dianhydride thereof (BPDA) are produced by heating crude BPTA to give BPDA, treating the BPDA with hot water to give highly pure BPTA, and in the case of highly pure BPDA, heat treating the pure BPTA to give highly pure BPDA.
Type:
Grant
Filed:
March 9, 1990
Date of Patent:
September 10, 1991
Assignees:
Hitachi, Ltd., Japan Carlit Co., Ltd., Kanto Koatsu
Abstract: This invention relates to N'-alkyl-spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical perparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes melitus associated complications.
Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.
Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two,provided that when R.sup.
Type:
Grant
Filed:
October 21, 1988
Date of Patent:
August 27, 1991
Assignee:
Syntex Pharmaceuticals, Ltd.
Inventors:
Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. Macfarlane, Serge Beranger, Robert J. Dow
Abstract: Compounds of the formula ##STR1## in which R is alkyl, arylalkyl or substituted arylkalkyl, or alkenyl containing one or more olephinic bonds; X is O, NH or NR.sub.1, where R.sub.1 is alkyl of 1 to 20 carbons or arylalkyl; and Y is H, alkyl of 1 to 20 carbons, arylalkyl, aryl, substituted aryl, substituted arylalkyl, alkenyl containing one or more olephinic bonds PO(OH).sub.2, PO(OH)OR.sub.2, PO(OH)R.sub.2 PO(OR.sub.2).sub.2, where R.sub.2 is independently alkyl of 1 to 20 carbons, phenyl, or substituted phenyl, further Y is CO--R.sub.3, CO--OR.sub.3, CONHR.sub.3, SO.sub.2 R.sub.3, SO.sub.2 NHR.sub.3, (CH.sub.2).sub.n --O--R.sub.3, or (CH.sub.2).sub.n --O--(CH.sub.2).sub.m --O--R.sub.3, where n, and m, are integers and are independently 1 to 20 and R.sub.3 is H, alkyl, alkenyl containing one or more olephinic bonds, aryl, substituted aryl, arylalkyl or substituted arylalkyl, with the proviso that when Y is CO--R.sub.3, CO--OR.sub.3, and CONHR.sub.3 then R.sub.3 is not hydrogen, are disclosed.
Abstract: The present invention relates to amino acid esters of pyrimidine and purine nucleosides containing an acyclic side chain, and their use in medical therapy, particularly the treatment of herpes virus infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.
Abstract: Glycol bisphosphate compounds are formed by first hydrolytically condensing a dihydrocarbylhalophosphate to form a tetrahyrocarbyl pyrophosphate and then reacting the pyrophosphate with a cyclic ether to form the glycol bisphosphate.
Abstract: The present invention is concerned with heterocyclic compounds, namely 3-aryluracils of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q are as described herein, as well as salts thereof and their manufacture, weed control compositions.
Type:
Grant
Filed:
June 16, 1989
Date of Patent:
August 20, 1991
Assignee:
Ciba-Geigy Corporation
Inventors:
Milos Suchy, Jean Wenger, Paul Winternitz, Martin Zeller
Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.
Abstract: This invention relates to 3-[1-thiazolidinylbutyl-4-piperazinyl]-1H-indazoles of the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane or cycloheptane ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane or cycloheptane ring; R.sub.5 is hydrogen, loweralkyl, alkanoyl or aroyl; X is hydrogen, halogen, loweralkyl or alkoxy; m is an integer of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and where applicable, the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention are useful as antipsychotic agents.
Abstract: Quaternary ammonium salts such as the benzalkonium chlorides and cetylpyridinium chloride can prevent the transmission of AIDS-causing virus through blood transfusions and through the use of blood products prepared using the blood of an AIDS infected individual.
Abstract: This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihal ophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl ]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.
Type:
Grant
Filed:
May 11, 1990
Date of Patent:
August 13, 1991
Assignee:
Schering Corporation
Inventors:
Anil K. Saksena, Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Dinanath F. Rane
Abstract: Preparation of novel symmetrical and unsymmetrical chromogenic di-[bis-(indolyl)ethylenyl]tetrahalophthalides is disclosed. Specifically these compounds are chromogenic di-[bis-(indolyl)ethylenyl]tetrahalophthalides of the formula ##STR1## wherein L and X are as hereinafter defined. The process disclosed involves condensing bis(indolyl)ethylenes with tetrahalophthalic anhydride in acetic anhydride, in the presence of an electron acceptor or preferably an acetate of Group I or II of the Periodic Table. Optionally, and preferably, where unsymmetrical di-[bis-(indolyl)ethylenyl]tetrahalophthalides are desired, indoles are reacted with an acylindole in the presence of a Vilsmeier reagent to form the starting bis(indolyl)ethylene.
Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
Abstract: Compounds of the formula ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1.sup.* CO--O--R.sub.1.sup.* CO--NH--R.sub.1.sup.* or PO(OR.sub.1.sup.*).sub.2 or PO(OR.sub.1.sup.*)R.sub.1.sup.* where R.sub.1.sup.* independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; X is O, S, SO--, SO.sub.2, NH--, or NR.sub.2 where R.sub.2 is phenyl, substituted phenyl or alkyl of 1 to 20 carbons, and Y is alkyl having at least 6 carbon atoms, arylalkyl, aryl, substituted aryl, substituted arylalkyl, alkenyl containing one or more olephinic bonds and at least 6 carbon atoms, CO--R.sub.3, CO--OR.sub.3, CONHR.sub.3, SO.sub.2 R.sub.3, SO.sub.2 NHR.sub.3 where R.sub.3 is aryl, substituted aryl, substituted arylalkyl, alkyl, alkenyl containing one or more olephinic bonds, further Y is (CH.sub.2).sub.n --O--R.sub.4, or (CH.sub.2).sub.n --O--(CH.sub.2).sub.m --O--R.sub.4, where n, and m, are integers and are independently 1 to 25 and R.sub.
Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a hydroxyl group or a methoxy radical, R.sub.2 is a hydrogen atom or a hyroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group, with the proviso that R.sub.2 and R.sub.3 are not simultaneously hydrogen atoms when R.sub.1 is a methoxy radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
Type:
Grant
Filed:
June 6, 1990
Date of Patent:
August 6, 1991
Assignee:
Boehringer Mannheim GmbH
Inventors:
Gisbert Sponer, Harald D. Borbe-Volmer, Jurgen Engel, Bernhard Kutscher, Georg Niebch, Marianne Siebert-Weigel