Abstract: A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.
Abstract: 5H-[1]Benzopyrano[3,4-d]pyridines represented by the formula ##STR1## wherein each R.sub.1 is loweralkyl, R.sub.2 is alkyl, cycloalkyl or ##STR2## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms and each R.sub.4, R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and R.sub.3 is hydroxy, acyloxy, loweralkoxy, loweralkenyloxy, loweralkynyloxy or ##STR3## X is a straight or branched chain alkylene group having from one to eight carbon atoms, and wherein R.sub.7 and R.sub.8 are the same or different members of the group consisting of hydrogen or loweralkyl, or ##STR4## wherein X is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.sub.10 with R.sub.10 being hydrogen or loweralkyl, with the limitation that when Z is O or S, the sum of a and b is 3 or 4; and when Z is NR.sub.
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: 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: Novel 3-substituted-4-aminoalkoxy-5,6-condensed ring-2-pyranones are disclosed as having utility as pharmacologically active compounds, in particular vasodilatory, hypotensive, anti-ischemic and anti-tussive activity. The compounds may be 3-phenyl-4-morpholinoalkoxy-coumarins. Administration may be by the oral or parenteral route. Intermediates useful in the production of these compounds are also disclosed.
Abstract: 9-(.beta.-hydroxyethyl) piperazinyl-carbonyl-2-trifluoromethyl-10, 11-dihydrodibenzo[b,f]thiepin is prepared and disclosed as having antiinflamatory action.
Abstract: A compound of the formula ##STR1## wherein Q is CH.sub.2, C.dbd.O, CHOH or CHCH.sub.2 OH; M is O or NR.sub.6 ; where R.sub.6 is hydrogen, or certain alkyl, aralkyl, acyl or carboalkoxy substituted alkyl groups; R.sub.1 is hydrogen, or certain alkanoyl or amino substituted alkanoyl groups; R.sub.4 and R.sub.5 are each hydrogen or alkyl having from 1 to 4 carbon atoms; Z is alkylene having from 1 to 9 carbon atoms or --(alk.sub.1)--X--(alk.sub.2).sub.n -- where (alk.sub.1) and (alk.sub.2) are certain alkylene groups and X is O, S, SO or SO.sub.2 ; W is a methyl, phenyl, substituted phenyl, pyridyl, piperidyl, cycloalkyl or substituted cycloalkyl group and the pharmaceutically acceptable and addition salts of said compounds having a basic nitrogen atoms. Said compounds are useful as analgesics and as intermediates therefore.
Abstract: The present invention provides 5-hydroxy-PGI.sub.1, piperazinylamides, which are useful pharmacological agents. These analogs of prostaglandin I.sub.1 are useful for the stimulation of mammalian smooth muscle tissues.
Abstract: Antiviral compositions and methods of inhibiting or inactivating viruses by administering to hosts an effective quantity of an active ingredient are disclosed herein. The active ingredients are those compounds having the formula ##STR1## wherein A is a straight or branched alkylene chain of from 1 to 6 carbon atoms and each Y is the group(A) ##STR2## wherein R.sup.1 and R.sup.2 are each individually selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, cycloalkyl of from 3 to 6 carbon atoms, alkenyl of from 3 to 6 carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group; or(B) ##STR3## wherein n is a whole integer of 4, 5 or 6 and R.sup.3 is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl and can be attached to any one of the carbon atoms of the heterocyclic group; or(C) ##STR4## wherein X is oxygen or N--R.sup.4 and R.sup.
Abstract: 9-Hydroxydibenzo[b,d]pyrans useful as analgesics, hypotensives, immunosuppressants, tranquilizers; as anti-secretory and anti-anxiety drugs; intermediates therefor and derivatives thereof having the formulae ##STR1## wherein R is hydrogen or alkanoyl having from one to five carbon atoms; R.sub.1 is hydrogen, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.P --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from one to four carbon atoms in the alkyl group;Each of R.sub.4 and R.sub.5 is hydrogen, methyl or ethyl;R.sub.0 is oxo or alkylenedioxy having from two to four carbon atoms;Z is(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.
Abstract: The invention relates to novel piperazine derivatives having the formula (I), ##STR1## wherein R.sub.1 represents a C.sub.1-5 alkyl group having optionally a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl group, a phenyl group having optionally one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituent(s), or a C.sub.2-5 alkoxycarbonyl group,R.sub.2 represents hydrogen or a C.sub.1-4 alkyl group, andR.sub.3 represents furyl group, 9-xanthenyl group or a C.sub.5-6 cycloalkyl group having a C.sub.1-4 alkoxy substituent,Or acid addition salts or quaternary salts thereof.The invention also relates to pharmaceutical compositions containing the above compounds, furthermore to a process for the preparation of the novel compounds and pharmaceutical compositions.The novel compounds according to the invention possess anti-arrhythmic and coronary dilatating effects.
Type:
Grant
Filed:
December 12, 1977
Date of Patent:
February 20, 1979
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Karoly Felfoldi, Jozsef Apjok, Mihaly Bartok, Jozsef Czombos, Arpad Molnar, Ferenc Noteisz, Egon Karpati, Laszlo Szporny
Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.
Type:
Grant
Filed:
July 28, 1977
Date of Patent:
January 9, 1979
Assignees:
Mitsubishi Chemical Industries Ltd., Shosuke Okamoto
Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.
Type:
Grant
Filed:
April 13, 1977
Date of Patent:
September 19, 1978
Assignee:
Lilly Industries Limited
Inventors:
Jiban Kumar Chakrabarti, David Edward Tupper
Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.
Type:
Grant
Filed:
June 1, 1977
Date of Patent:
September 19, 1978
Assignee:
Lilly Industries Limited
Inventors:
Jiban Kumar Chakrabarti, David Edward Tupper
Abstract: Novel dibenzo[b.f]thiepin and oxepin compounds of the formula and the pharmaceutically acceptable esters and salts thereof, wherein R is hydrogen or methyl; X is oxygen or S(O).sub.n in which n is the integer 0, 1 or 2 and Z is a single or double bond, provided that when Z is a double bond X is not SO, and when R is methyl the compounds are (dl) mixtures, and methods for the production thereof.
Abstract: Dihydrodibenzo[b,f]thiepin compounds of formula (I) and process for making them. These compounds have antiinflammatory action. ##STR1## wherein R represents a hydrogen, fluorine atom, a trifluoromethyl, 1-5C lower alkoxy, hydroxy, hydroxyethoxy, aminoethoxy group or the group of the formula --OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OH, Y represents a hydroxy group or the group of the formula ##STR2## (R.sub.3 and R.sub.4 represent a 1-4C lower alkyl group or R.sub.3 and R.sub.4 may jointly form a heterocyclic group together with an adjacent nitrogen atom.