Plural Chalcogens Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/425)
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Patent number: 4663319Abstract: Novel thioketene derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y;Y is a nitrogen-containing monocyclic heterocyclic group or a substituted or unsubstituted phenyl group;B is a straight or branched lower alkylene group;R.sup.2 and R.sup.3 are both a lower alkyl group or are combined together to form a group of the formula: --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sup.4 is hydrogen atom, a lower alkyl group or a (lower alkoxy)carbonyl group;A is a group of the formula: --(CH.sub.2).sub.n -- or --CH(COOR.sup.5)--;n is an integer of 0, 1 or 2 andR.sup.5 is a lower alkyl group,are disclosed. The compound (I) is useful as an agent for treating and protecting various liver diseases.Type: GrantFiled: January 7, 1985Date of Patent: May 5, 1987Assignee: Tanabe Seiysku Co., Ltd.Inventors: Ikuo Iijima, Koichi Homma, Yutaka Saiga, Yuzo Matsuoka, Mamoru Matsumoto
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Patent number: 4656034Abstract: The absorption of a scavenger of oxygen free radicals generated at the time of reperfusion or the absorption of an agent preventing the cytotoxic effects on healthy cells in a mammal. e.g. superoxide dismutase or S-aminotrimethyleneaminoethyl thiophosphate is enhanced by substantially simultaneously administering an absorption enhancing agent therefore, e.g. hydroxylamine or a non-toxic salt thereof. It is also part of the invention to inject WR-2721 intravenously or intramuscularly as a scavenger of oxygen free radicals even in the absence of an absorption enhancing agent.Type: GrantFiled: May 20, 1985Date of Patent: April 7, 1987Assignee: Survival Technology, Inc.Inventor: Stanley J. Sarnoff
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Patent number: 4649204Abstract: Dialkanolamines and nontoxic pharmaceutically-acceptable acid-addition salts of the compounds of the following formula ##STR1## wherein R.sub.1 is hydrogen lower alkyl, or fluoro; R.sub.2 is hydrogen or lower alkyl; R.sub.3 and R.sub.4 are the same or different and selected from the group consisting of hydrogen or lower alkyl or R.sub.3 and R.sub.4 together define a chemical bond directly linking the two alkanol chains so as to form a pyrrolidine ring; Ar, is phenyl or thienyl or phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo; and Ar.sub.2 is phenyl and phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo which have antidepressant activity.Type: GrantFiled: September 30, 1985Date of Patent: March 10, 1987Assignee: McNeilab, Inc.Inventor: Bruce E. Maryanoff
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Patent number: 4649152Abstract: A method for making a composition containing a fatty acid or fatty ester compound and potassium. The compositions produced by the method. Administration of these compositions to a patient to increase the potassium content of cells or tissue having a potassium deficiency or to treat at least some of the symptoms of diseases or adverse effects caused by this potassium deficiency.Type: GrantFiled: October 1, 1985Date of Patent: March 10, 1987Assignee: Elena AvramInventor: Emanuel Revici
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Patent number: 4645776Abstract: The new compound N-(dichlorofluoromethylthio)-3,4-dimethylmaleimide can be prepared by reacting 3,4-dimethylmaleimide with dichlorofluoromethanesulphenyl chloride in the presence of an acid-binding agent. N-(dichlorofluoromethylthio)-3,4-dimethylmaleimide is an active compound in microbicidal agents.Type: GrantFiled: April 9, 1985Date of Patent: February 24, 1987Assignee: Bayer AktiengesellschaftInventors: Engelbert Kuhle, Wilfried Paulus, Hermann Genth
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Patent number: 4634717Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.Type: GrantFiled: May 1, 1984Date of Patent: January 6, 1987Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4620973Abstract: The invention relates to the use of nootropics, particularly Piracetam.RTM., in connection with the treatment of cancer with cytostatically effective preparations, for the prevention or mitigation of side effects which are caused by cytostatics.Type: GrantFiled: June 14, 1985Date of Patent: November 4, 1986Assignee: Ciba Geigy CorporationInventor: Peter Truog
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Patent number: 4605663Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.Type: GrantFiled: May 1, 1984Date of Patent: August 12, 1986Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4605664Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.Type: GrantFiled: May 1, 1984Date of Patent: August 12, 1986Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4604403Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.Type: GrantFiled: May 1, 1984Date of Patent: August 5, 1986Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4596821Abstract: The invention relates to novel substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, their analogs and their salts. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections and various brain concussions.Type: GrantFiled: May 1, 1984Date of Patent: June 24, 1986Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4594096Abstract: The aqueous mixed dispersions, according to the invention, of pesticides, which contain an active compound concentrate, based on (C.sub.1 -C.sub.12)-alkyl phthalates as the solvent, of one or more active compounds melting below 70.degree. C., in combination with an aqueous suspension concentrate of one or more active compounds melting above 70.degree. C., possess surprisingly high stability on storage.Type: GrantFiled: January 24, 1984Date of Patent: June 10, 1986Assignee: Hoechst AktiengesellschaftInventors: Konrad Albrecht, Gerhard Frisch
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Patent number: 4594239Abstract: A technique is described for neutralizing unishiol. The technique involves contacting urushiol with a chlorine-containing compound in a liquid medium. In one embodiment the chlorine-containing compound is sodium or calcium hypochlorite in an aqueous solution. In another embodiment the chlorine-containing compound is a chloramine in a liquid organic medium.Type: GrantFiled: March 14, 1984Date of Patent: June 10, 1986Inventor: Arthur W. Pluim, Jr.
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Patent number: 4585785Abstract: Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, phenylalkyl, benzyloxycarbonyl, carbamoyl, N-loweralkylcarbamoyl, N-diloweralkylcarbamoyl and parafluorobenzoyl-lower-alkyl; Ar is phenyl, substituted phenyl, 1-naphthyl, 2-naphthyl, 1-indenyl and 2-indenyl and pharmaceutically acceptable acid addition and quaternary salts thereof. The compounds have antidepressant, antihypertensive and antiarrythmic activity in animals.Type: GrantFiled: March 10, 1980Date of Patent: April 29, 1986Assignee: A. H. Robins Company, Inc.Inventors: David A. Walsh, William J. Welstead, Jr.
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Patent number: 4582849Abstract: Fungicidally active substituted maleic acid amides of the formula ##STR1## in which X is hydrogen, chlorine or bromine,X.sup.1 is chlorine or bromine,R is alkyl, optionally substituted aryl or optionally substituted aralkyl,R.sup.1 to R.sup.5 each independently is hydrogen, alkyl, optionally substituted aryl or optionally substituted aralkyl,R.sup.6 each independently is halogen, alkyl, optionally substituted aryl, optionally substituted cycloalkyl, alkoxy, sulphonylamine, halogenoalkyl, nitro, cyano, alkoxycarbonyl, alkylsulphonyl or carboxylamine,n is 0, 1, 2 or 3,m is 0, 1, 2 or 3,m+n is 0, 1, 2 or 3, andy is 0, 1, 2, 3, 4 or 5,with the exception of the compound in whichX and X.sup.1 are chlorine,m and y are 0,n is 1,R.sup.1, R.sup.4 and R.sup.5 are hydrogen, andR is methyl,and the compound in whichX and X.sup.1 are chlorine,m, n and y are 0,R.sup.1 is hydrogen, andR is phenyl.Type: GrantFiled: May 27, 1983Date of Patent: April 15, 1986Assignee: Bayer AktiengesellschaftInventors: Gerhard Marzolph, Heinz U. Blank, Paul Reinecke, Wilhelm Brandes, Hans Scheinpflug
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Patent number: 4575489Abstract: Novel peptide B-52653 having the formula: ##STR1## which is produced by cultivating a microorganism belonging to the genus Streptomyces and being capable of producing B-52653 in a culture medium, whereby B-52653 is elaborated and accumulated in the cultured broth and is recovered.B-52653 is useful as a germicide or disinfectant, and a possibility of the present substance as an antifibrotic agent is suggested.Type: GrantFiled: September 8, 1981Date of Patent: March 11, 1986Assignee: Takeda Chemical Industries, Ltd.Inventors: Eiji Higashide, Satoshi Horii
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Patent number: 4552890Abstract: A method of combatting fungi which comprises applying to fungi or a fungus habitat a fungicidally effective amount of at least one maleic acid N-aralkyl-imide of the formula ##STR1## in which X is hydrogen or halogen,Hal is halogen, andm is 2,3 or 4.Those compounds are new in whichHal is chlorine or bromine, andX is hydrogen or bromine if m is 2, orX is chlorine if m is 4.Type: GrantFiled: February 8, 1984Date of Patent: November 12, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Marzolph, Heinz U. Blank, Paul Reinecke, Wilhelm Brandes, Gerd Hanssler
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Patent number: 4537897Abstract: Novel 3-(1,2-propadienyl)-cyclopropane-carboxylates of the formula ##STR1## wherein R is alcohol used in pyrethrinoid synthesis, X and Y are both hydrogen or individually halogen or X is hydrogen or halogen and Y is alkyl of 1 to 18 carbon atoms or halogen or X is hydrogen or halogen or alkyl of 1 to 18 carbon atoms and Y is --COOR' or --CN or ##STR2## R' is alkyl of 1 to 18 carbon atoms, R.sub.2 and R.sub.3 are individually hydrogen or alkyl of 1 to 18 carbon atoms or R.sub.2 and R.sub.3 together with the nitrogen atom form a heterocycle having pesticidal properties.Type: GrantFiled: September 15, 1983Date of Patent: August 27, 1985Assignee: Roussel UclafInventors: Jean Tessier, Jean-Pierre Demoute, Joseph Cadiergue
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Patent number: 4537902Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.Type: GrantFiled: June 11, 1979Date of Patent: August 27, 1985Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
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Patent number: 4530933Abstract: Biologically active 8-aza-13-thiaprostanoids having the formula: ##STR1## wherein A is CH.dbd.CH (cis or trans), C.tbd.C, CH.sub.2 CH.sub.2, ##STR2## or CHOHCH.sub.2 ; R is H, C.sub.1 to C.sub.12 n-alkyl, branched chain alkyl, or cycloalkyl, or a physiologically acceptable metal or amine salt cation;R.sup.1 is H, CH.sub.3 or C.sub.2 H.sub.5 ;R.sup.2 is CH.sub.3 or CF.sub.3 ; andn is an integer from 4 to 9.Type: GrantFiled: December 27, 1982Date of Patent: July 23, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chia-Lin J. Wang
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Patent number: 4517185Abstract: The present invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are unsubstituted or substituted aromatic rings, Alk is a straight-chained or branched lower hydrocarbon chain and Z is a hydrogen atom, with the proviso that when Alk is a straight-chained hydrocarbon chain, Z can also be a lower alkylamino radical of the general formula II ##STR2## in which R.sup.3 and R.sup.4 are the same or different and are hydrogen atoms or straight-chained or branched lower alkyl radicals or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, can also form a ring optionally containing further hetero atoms; and the pharmacologically acceptable salts thereof.The present invention also provides an inventive process for preparing these compounds, as well as pharmaceutical compositions containing them. The compounds I may be used in the therapy of inflammations and they are free of gastrointestinal side effects.Type: GrantFiled: March 25, 1983Date of Patent: May 14, 1985Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Edgar Fritschi, Volker Ganser, Johannes Hartenstein, Manfred Herrmann, Gerhard Satzinger
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Patent number: 4511576Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.Type: GrantFiled: August 10, 1982Date of Patent: April 16, 1985Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4507291Abstract: This invention relates to a method of using compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl or alkenyl; R.sup.2 is hydrogen, alkyl, cycloalkyl or mononuclear aryl or R.sup.1 and R.sup.2, taken together with the carbon atom to which they are attached, form a cycloalkyl or cycloalkoxyalkyl; R.sup.3 is hydroxy, alkyl, alkoxycarbonyl, hydroxy lower alkyl or a radical of the formula: --C(.dbd.Y)NR.sup.4 R.sup.5 wherein R.sup.4 is hydrogen, alkyl, alkenyl, R.sup.5 is alkyl, alkenyl, alkoxyalkyl, carbalkoxy, mononuclear aryl, or R.sup.4 and R.sup.5 may be joined together with the nitrogen atom to which they are attached to form a 5 to 7 membered heterocyclic ring having from 1 to 3 hetero atoms; Y is O or S; X is alkyl, alkoxycarbonylalkyl or cyano; m is an integer of 0 to 2 and n and n' are integers each having a value of 1 to 2 and the dotted line indicates an optional double bond anywhere in the ring, compositions containing said compounds as insect repellents and to novel compounds.Type: GrantFiled: July 15, 1982Date of Patent: March 26, 1985Assignee: Rohm and Haas CompanyInventor: Joel R. Smolanoff
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Patent number: 4499089Abstract: 2-Alkylthio-1-aminoalkyl-2-pyrroline-3-carbonitriles and pharmaceutically acceptable acid addition salts, processes for their preparation and formulation into pharmaceutical compositions as well as their activity as thrombocyte aggregation-inhibitors are described. The compounds are thus useful for the prophylaxis and therapy of thrombotic states.Type: GrantFiled: May 10, 1984Date of Patent: February 12, 1985Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Johannes Hartenstein, Gerhard Satzinger, Edgar Fritschi, Volker Ganser, Horst-Dietmar Tauschel, Gunter Wolf
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Patent number: RE32393Abstract: According to the invention, the parenteral administration of water-insoluble pharmacologically active agents is enhanced wherein the agents are administered in the lipoid phase of a carrier emulsion comprising a microemulsion of a finely dispersed lipoid in an aqueous phase. The lipoid preferably has a mean particle size below 1 micron. This makes it possible to administer water-insoluble agents in high concentrations, and thus a lower dose, whereby a rapid onset of the pharmacological effect is accompanied by a markedly reduced incidence of injury to body tissues.Type: GrantFiled: August 14, 1984Date of Patent: April 7, 1987Assignee: KabiVitrum ABInventors: Karl A. J. Wretlind, Stellan Ljungberg, Ivan Hakansson, Bengt M. Ajaxon