Abstract: The compounds according to the invention have the formulae Ia or Ib ##STR1## in which Y is a divalent organic radical and Z is --NH.sub.2, --NH-alkyl having 1-4 C atoms, --OH, --COOH, --COCl, --O--CO--CH.dbd.CH.sub.2, ##STR2## --COO--CH.dbd.CH.sub.2 or --O--CH.dbd.CH.sub.2. These novel 3- or 4-azidophthalic acid derivatives may be used for the preparation of photo-crosslinkable polymers. Compared to corresponding photosensitive polymers of the prior art, these novel polymers have the advantages that they are even more photosensitive and that they also absorb in the long wavelength UV region (at wavelengths greater than 320 nm).
Type:
Grant
Filed:
October 5, 1978
Date of Patent:
February 10, 1981
Assignee:
Ciba-Geigy Corporation
Inventors:
Vratislav Kvita, Hans Zweifel, Gerd Greber
Abstract: Piperazine derivatives having the formula (I) ##STR1## wherein R.sub.1 is C.sub.1-5 alkyl group which can have a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl, phenyl which can have one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituents, or C.sub.2-5 alkoxycarbonyl;R.sub.2 is hydrogen or C.sub.1-4 alkyl; andR.sub.3 is furyl or a C.sub.5-6 cycloalkyl having a C.sub.1-4 alkoxy substituent, and acid addition salts or quaternary salts thereof with anti-arrhythmic and coronary dilatating pharmaceutical effects.
Type:
Grant
Filed:
December 28, 1978
Date of Patent:
February 10, 1981
Assignee:
Richter Gedeon Vegyeszeti Gyar R.T.
Inventors:
Karoly Felfoldi, Jozsef Apjok, Mihaly Bartok, Jozsef Czombos, Arpad Molnar, Ferenc Noteisz, Egon Karpati, Laszlo Szporny
Abstract: Red colors having the anthraquinone structure ##STR1## are disclosed wherein R.sub.1 and R.sub.2 are independently selected from among hydrogen, halos, lower alkyls, lower alkoxies, nitros, and sulfonates, and R.sub.3 and R.sub.4 are independently selected from hydrogens, alkyls and alkylsulfonates. Precursors are disclosed as well. In a preferred embodiment R.sub.4 is an alkyl-containing polymer linking a plurality of anthraquinones into a polymeric colorant especially useful as a nonabsorbable colorant for edibles.
Abstract: Novel high purity crystalline forms of dialkylgermaazaspirodiones, their preparation and their use in an improved process for the preparation of high purity dialkylgermaazaspiranes and their acid addition salts is disclosed.
Type:
Grant
Filed:
April 26, 1979
Date of Patent:
February 3, 1981
Assignee:
The Norac Company, Inc.
Inventors:
Chester M. McCloskey, James R. Fischer, Leonard F. Scott
Abstract: A process for preparing beta or gamma crystals of linear quinacridone, substituted quinacridone or solid solutions thereof by contacting premilled quinacridone with 45-60% by weight sulfuric acid and 0-10% by weight of a surfactant based on the quinacridone at a weight ratio of acid to quinacridone of 3:1-6:1 to form a slurry, agitating said slurry for a period of time at 45.degree.-75.degree. C., adding water to form a dilute slurry, agitating said dilute slurry for a period of time at 75.degree.-95.degree. C. and separating quinacridone from the liquid of the dilute slurry.
Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR2## R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy, and ##STR3## wherein R.sub.1 is selected from the group consisting of lower alkyl; R.sub.8 is selected from the group consisting of --O--(CH.sub.2).sub.n --wherein n is 2 to 20, ##STR4## and R.sub.6 is selected from the group consisting of hydrogen or lower alkoxy and racemates thereof.There are also disclosed processes and intermediate utilized to produce the end products.The end products have utility as agents exhibiting both .alpha. and selective .beta. adrenergic blocking action.
Type:
Grant
Filed:
September 6, 1979
Date of Patent:
January 27, 1981
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Kenneth E. Fahrenholtz, Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
Abstract: The present invention relates to a new organic heterocyclic isocyanate which is the reaction product of an organic diisocyanate and an amino or hydroxy nitrile. The invention also relates to a process of producing such isocyanates by reacting an excess of the diisocyanate with the nitrile under conditions under which the nitrile will not decompose and then maintaining the reaction mixture at an elevated temperature until the isocyanate nitrile adduct cyclizes. The reaction may be carried out in the presence of a catalyst for isocyanate addition reactions. Additionally, the invention relates to a process for the production of polyurethane by the reaction of the heterocyclic isocyanates with compounds carrying at least two isocyanate reactive hydrogen atoms per molecule.
Type:
Grant
Filed:
June 11, 1979
Date of Patent:
January 27, 1981
Assignee:
Bayer Aktiengesellschaft
Inventors:
Kurt Findeisen, Kuno Wagner, Walter Uerdingen
Abstract: A phase transfer catalyzed "soft ion synthesis" is disclosed in which the presence of a "soft ion" generated in situ by a soft ion catalyst has a directive effect which favors the formation of a polysubstituted 2-keto-1,4-diazacycloalkane isomer having substituents on both N.sup.4 -adjacent carbon atoms ("C atoms") of its diaza ring; this isomer is formed at the expense of isomers in which an N.sup.4 -adjacent C atom is not substituted. Such an isomer which has substituents on each N.sup.4 -adjacent C atom is generally more effective as a u-v light stabilizer than an isomer which has an unsubstituted N.sup.4 -adjacent C atom, and therefore the former is more desirable.
Abstract: 9-Phenyl(or benzyl)acridines, 9-phenyl(or benzyl)-9-acridinols and acridinium compounds, useful as trypanosomacidal and antibacterial agents, are prepared from aminoalkoxy substituted 9-acridinones via reaction with the appropriate Grignard reagents or aryllithium. The intermediate aminoalkoxy substituted 9-acridinones, prepared from the corresponding halo or hydroxy substituted 9-acridinones, are useful as antiviral agents.
Abstract: This disclosure describes novel 4-[(monosubstituted-alkyl)amino]benzoic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.
Abstract: Techniques for the preparation of 3-fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(b,f) thiepins and their addition salts with organic and inorganic acids are disclosed. The described compositions evidence psychotropic activity and low toxicity and are characterized as neuroliptics with a high degree of cataleptic, anti-apomorphine and central depressant action.
Type:
Grant
Filed:
December 22, 1978
Date of Patent:
January 6, 1981
Assignee:
SPOFA, spojene podniky pro zdravotnickou vyrobu
Inventors:
Miroslav Protiva, Miroslav Rajsner, Karel Sindelar, Jiri Jilek, Vaclav Bartl, Jirina Metysova, Antonin Dlabac, Leon Langsadl, Josef Pomykacek, Frantisek Miksik
Abstract: 1,2,4-Oxadiazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 =H, halogen or alkyl, or two of them represent the --CH.dbd.CH--CH.dbd.CH-- group required to form a fused benzene ring and R=an amino radical NR'R" or --N.dbd.CR'.sub.3 --NR'.sub.1 R'.sub.2, in which R', R", R'.sub.1 and R'.sub.2 =alkyl, hydroxyalkyl or N,N-dialkylaminoalkyl or NRR' or NR'.sub.1 R'.sub.2 =heterocyclic ring, and R' R" can also be H, dialkylaminoalkylcarbonyl and pyridinoalkyl, (at least two of R.sub.1 to R.sub.5 being other than H when R' and R"=H), are pharmaceutically useful as anti-hypertensive agents.
Abstract: Novel derivatives of morphine having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are certain specified values, and their pharmaceutically acceptable salts.The compounds exhibit activity in the central nervous system and may be presented in the form of pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable diluent or carrier.
Type:
Grant
Filed:
March 15, 1978
Date of Patent:
December 23, 1980
Assignee:
Reckitt & Colman Products Limited
Inventors:
Ryszard J. Kobylecki, Ian G. Guest, John W. Lewis, Gordon W. Kirby
Abstract: 2-(o-Hydroxyphenyl)-pyrrole and a process for its preparation, wherein o-benzyloxybenzoic acid allylamide is reacted with phosgene in an inert solvent, the resulting imide-chloride is cyclized in the presence of a strong sterically hindered base and the benzyl protective group is then removed by hydrogenolysis.2-(o-Hydroxyphenyl)-pyrrole is a valuable intermediate for the synthesis of drugs. In particular, alkylamino-hydroxypropyl ethers thereof can, because of their .beta.-sympatholytic actions, be used for the treatment of coronary cardiac diseases, cardiac arrhythmias and hypertonia.
Type:
Grant
Filed:
August 8, 1979
Date of Patent:
December 23, 1980
Assignee:
BASF Aktiengesellschaft
Inventors:
Horst Koenig, Albrecht Franke, Fritz-Frieder Frickel, Wolfgang Steglich, Norbert Engel
Abstract: Novel derivatives of morphine having the general formula: ##STR1## wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are certain specified values, and their pharmaceutically acceptable salts.The compounds exhibit activity in the central nervous system and may be presented in the form of pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable diluent or carrier.
Type:
Grant
Filed:
March 15, 1978
Date of Patent:
December 23, 1980
Assignee:
Reckitt & Colman Products Limited
Inventors:
Ryszard J. Kobylecki, Ian G. Guest, John W. Lewis, Gordon W. Kirby
Abstract: Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.
Type:
Grant
Filed:
January 6, 1976
Date of Patent:
December 9, 1980
Assignee:
SPOFA, United Pharmaceutical Works
Inventors:
Miroslav Protiva, Karel Sindelar, Irena Cervena, Jirina Metysova
Abstract: A process for the removal of oxazole from acrylonitrile by contacting oxazole-containing acrylonitrile with a substantially dry cation exchange resin. The process exhibits the advantage of up to 40 percent or greater increase in the oxazole removal capacity than a corresponding process employing a water-wet cation exchange resin.
Abstract: Novel compounds of the following general formula are useful in the preparation of 4-aminohex-5-enoic acid and 4-aminohex-5-ynoic acid which are useful pharmacological agents: ##STR1## wherein R.sub.1 is hydroxy, amino, or tert-butoxy.