Abstract: An odorless sterilizing and disinfecting solution is described which has a pH of from 3 to 9 and which contains an effective amount of phthalaldehyde. The solution is used to sterilize or to disinfect a surface in need of such treatment.
Type:
Grant
Filed:
May 10, 1989
Date of Patent:
November 20, 1990
Assignee:
Johnson & Johnson Medical, Inc.
Inventors:
Norman I. Bruckner, Michael D. Gordon, Ronald G. Howell
Abstract: A compound of the formula (I):ArCH.sub.2 R.sup.1where Ar is ##STR1## where Z is NH, NCH.sub.3 or NEt and R.sup.1 is an hydroxyalkylamino group and pharmaceutically acceptable salts thereof. The compounds are useful as antitumor agents.
Abstract: A substituted 1,2,4-triazinedione of the formula ##STR1## in which R.sup.1 stands for an unsubstituted or substituted heteroaromatic radicals bonded via carbon,X stands for one or more, identical or different radicals selected from the group consisting of hydrogen, halogen, nitro, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy and halogenoalkylthio.R.sup.3 stands for hydrogen, unsubstituted or substituted alkyl, alkenyl, alkinyl or aralkyl. The substituted 1,2,4-triazinedione is useful to combat parasitic protozoa in warmblooded animals.
Abstract: Novel enantiomeric and diastereoisomeric forms of decahydroquinolines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom to which they are connected form a 5 to 6 member heterocycle optionally including another heteroatom and optionally substituted, A is selected from the group consisting of --(CH.sub.2).sub.n -- and alkylene substituted with an alkyl and having 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, naphthyl indenyl, monocyclic heterocycle of 5 to 6 members and a bicyclic heterocycle all being unsubstituted or substituted by one or more substituents and their non-toxic, pharmaceuically acceptable acid addition salts and quaternary ammonium salts having central analgesic properties.
Type:
Grant
Filed:
July 11, 1988
Date of Patent:
November 6, 1990
Assignee:
Roussel Uclaf
Inventors:
Francois Clemence, Michel Fortin, Odile Le Martret, Francoise Delevallee
Abstract: The present invention relates to novel 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime-O-sulfonic acid compound, processes for producing said compounds, intermediate compounds to produce said compounds and compositions containing said compounds with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites.The present invention is based on the selection of 1-acyl-7-halo-2,3-dihydro-4(1H)-quinolinone-4-oxime-O-sulfonic acid compounds, namely heterocyclic-or fused heterocyclic- carbonyl derivatives at 1 position.The compounds of the present invention containing these substituents have potent hypotensive, antioedematous and diuretic effect as well as an activity to remove ascites and are extremely useful for the treatment of diseases and disorders mentioned above.
Type:
Grant
Filed:
October 28, 1988
Date of Patent:
November 6, 1990
Assignees:
Mochida Pharmaceutical Co., Ltd., Hodogaya Chemical Co., Ltd.
Abstract: To prepare the compound (I), a lithiation of the compound (II) is performed, an aldehyde (IV) is reacted with the compound (III) formed, leading to the secondary alcohol (V) which is subjected to a reduction leading to the compound (VI), which is then subjected to a hydrolysis (of the dioxolane group)/cyclization/dehydration reaction. The procedure may be followed by a nucleophilic substitution reaction of the chlorine. The compounds (a) below exhibit antitumor activity. ##STR1## R=C.sub.1 -C.sub.3 alkyl; Ar=aromatic or polycyclic aromatic group; R.sub.1 and r.sub.2 =H or C.sub.1 -C.sub.3 alkyl; and n=2 to 4. No drawing.
Type:
Grant
Filed:
November 14, 1988
Date of Patent:
October 30, 1990
Assignee:
Centre National de la Recherche Scientifique (C.N.R.S.)
Inventors:
Emile R. B. Bisagni, Marilys Greletepouse Rautureau
Abstract: Pyrrole derivatives of the general formula I ##STR1## wherein R denotes alkyl which is substituted by --NH.sub.2 or acylamino, R.sup.1 and R.sup.2 independently of one another denote hydrogen or alkyl having 1 to 4 carbon atoms, R.sup.3 denotes hydrogen, alkyl having 1 to 4 carbon atoms or a carboxylic acid grouping, R.sup.
Type:
Grant
Filed:
May 23, 1989
Date of Patent:
October 30, 1990
Assignee:
Cassella Aktiengesellschaft
Inventors:
Gerhard Zoller, Rudi Beyerle, Ursula Schindler
Abstract: The use of the naturally occurring and readily synthesized alkaloid compound eupolauridine as an antimicrobial agent and particularly against Candida albicans organism .
Abstract: Novel pheophorbide derivatives of the general formula: ##STR1## [wherein Z is O or NH; n is an integer of 1 to 6; Y is NR'R" or ##STR2## wherein R', R" and R'" are the same or different or each represents a C.sub.1 to C.sub.4 lower alkyl group; X.sup.- is a halogen or organic acid ion); R.sub.1 is an ethenyl group; C.sub.1 to C.sub.4 lower alkyl group or ##STR3## (wherein m is an integer of 0 to 6; R.sub.6 is H or a C.sub.1 to C.sub.4 lower alkyl group); R.sub.2 is CH.sub.3, CHO or CH.sub.2 OH; either of R.sub.3 and R.sub.4 is H, with the other being OH, or both of them combine to represent .dbd.O; R.sub.5 is H or CO.sub.2 CH.sub.3) are provided.When administered to a cancer-carrying animal, the derivatives accumulate specifically in cancer tissues and emit characteristic fluorescent spectrum under irradiation of light, which enables one to detect the cancer tissues.
Abstract: Pure dimer compounds prepared and shown to be effective photosensitizing agents are of the formula ##STR1## wherein one R is vinyl and the other R is hydroxyethyl or vinyl and the pharmaceutically acceptable esters and salts thereof in isolated form.
Abstract: A thienotriazolodiazepine compound of the formula: ##STR1## wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl; R.sup.1 and R.sup.3 are the same or different and each is hydrogen, alkyl having 1 to 4 carbon atoms; R.sup.2 is hydrogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl; R.sup.4 is straight or branched chain alkyl, alkenyl or alkynyl having 6 to 18 carbon atoms, or a thienodiazepine compound of the formula: ##STR2## wherein Ar, R.sup.1, R.sup.2 and R.sup.4 are as defined above, and pharmaceutically acceptable acid addition salt thereof.These compounds are useful as drugs for the treatment of circulatory diseases and various PAF-induced diseases. The compound (II) is also useful as an intermediate for preparing the compound (I).
Abstract: There are disclosed compounds of the formula ##STR1## wherein A is alkyl of 3-19 carbon atoms, diloweralkyl allyl, dihaloallyl, diphenylallyl, lower alkynyl, ##STR2## X is N or CR; Z is ##STR3## R is hydrogen or lower alkyl; R.sup.1 is hydrogen, lower alkyl or phenyl;R.sup.2 is hydrogen or loweralkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.
Type:
Grant
Filed:
May 12, 1989
Date of Patent:
October 2, 1990
Assignee:
American Home Products Corporation
Inventors:
Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak
Abstract: Compounds of the formula ##STR1## where R is hydrogen, hydroxy, amino or lwer-alkyl; R.sup.1 is lower-alkyl, lower-alkenyl, cycloalkyl, pyridinyl, phenyl or substituted phenyl; R.sup.2 is hydrogen, amino or hydroxy; R.sup.6 is hydrogen or fluoro; and R.sup.7 is phenyl, pyridinyl or selected other heterocycles, have antiviral acitivity against herpes virus.The compounds are prepared from the corresponding carboxylic acids or ester, or by a tin-coupling reaction on the corresponding 7-halo compounds.
Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## comprising in a first reaction step reacting an enamine of the formula ##STR2## in an anhydrous, aprotic solvent with one equivalent of a base, at a temperature from 80.degree. C. to 180.degree. C., to give a 4-quinolone-3-carboxylic acid derivative of the formula ##STR3## and, in a second reaction step, reacting that with another equivalent of a base, to give the 1,8-bridged 4-quinolone-3-carboxylic acid derivative of the formula (I) and optionally converting the group Y into a carboxyl group or salt thereof. Both steps may be effected simultaneously in a one-pot process without intermediate isolation of the compound II. Some of the compounds are new. The old and new compounds are antibacterials and promote animal growth.
Abstract: There are provided gastric antiulcer and cytoprotective substituted N-phenyl-2-pyridinecarbothioamides. The process for their production and formulation is disclosed.
Abstract: Antimicrobial polymeric bisbiguanides capped with alkylene pyrrolidonyl groups having the formula: ##STR1## where X is C.sub.2 -C.sub.4 alkylene; Y is a bivalent bridging group; and n is at least 2; and acid addition salts thereof.
Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
Type:
Grant
Filed:
July 14, 1989
Date of Patent:
September 4, 1990
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 alkenyl group, a C.sub.3 -C.sub.7 alkynyl group, a halo(C.sub.1 -C.sub.5)alkyl group, a halo(C.sub.3 -C.sub.4) alkenyl group, a halo(C.sub.3 -C.sub.4)alkynyl group, a C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.2)alkyl group, a C.sub.1 -C.sub.2 alkylthio(C.sub.1 -C.sub.2)alkyl group and R.sup.2 is a hydrogen atom or a methyl group, which is useful as a herbicide.
Abstract: The present invention relates to a pharmaceutical composition for the prophylaxis and treatment of ischemic disorder in mammalian organs which contains, as an ingredient, a compound of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the methyl group or a hydrogen atom, or a salt thereof.