Plural Chalcogens Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/425)
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Patent number: 5102905Abstract: The invention concerns heterocyclic nitromethane derivatives of the formula 1 as defined hereinafter (and their non-toxic salts) wherein the heterocyclic moiety Q is thienyl, benzothienyl or dibenzothienyl and may bear a wide variety of optional substituents, together with pharmaceutical compositions containing them. The nitromethane derivatives are inhibitors of the enzyme aldose reductase and are of value in the treatment of certain complications of diabetes and galactosemia.Type: GrantFiled: April 28, 1989Date of Patent: April 7, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey Morris, John Preston
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5098927Abstract: Pyrroline compounds of the formulae (I) and (II) are effective in the treatment of retroviral infection and lymphadenopathy.Type: GrantFiled: January 10, 1991Date of Patent: March 24, 1992Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Takatsuki, Yohsuke Maeda, Toshio Hattori, Tsutomu Kaizu, Masanori Okamoto, Yoshiko Yokota, Katsuya Nakamura, Hiroshi Kayakiri
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Patent number: 5089520Abstract: A group of five- and six-membered heterocyclic compounds having a nitrogen in the ring and 2 to 3 hydroxyl substituents on the ring are effective inhibitory agents of human immunodeficiency virus.Type: GrantFiled: September 20, 1990Date of Patent: February 18, 1992Assignee: Monsanto CompanyInventors: George W. J. Fleet, Thomas W. Rademacher, Raymond A. Dwek
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Patent number: 5081130Abstract: Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.Type: GrantFiled: September 19, 1990Date of Patent: January 14, 1992Assignee: Roussel UclafInventors: Giulio Galliani, Fernando Barzaghi, Michel Fortin, Carlo Gorini, Emilio Toja
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Patent number: 5066651Abstract: New pyrrolidone compounds of the formula: ##STR1## in which: R is OR", SR" or N (R.sub.3 R.sub.4)R' is optionally substituted alkyl or aryl, andthe carbon in the 5-position of the pyrrolidone ring, which is substituted by CH.sub.2 R has the R or S configuration.These new compounds and their physiologically tolerable salts may be used therapeutically especially in the treatment of asthenias, ischaemic syndromes and nervous disorders associated with normal or pathological ageing.Type: GrantFiled: May 17, 1990Date of Patent: November 19, 1991Assignee: Adir et CompagnieInventors: Gilbert Regnir, Alain Dhainaut, Jean Lepagnol, Jean Lepagnol
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5049584Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.Type: GrantFiled: November 6, 1990Date of Patent: September 17, 1991Assignee: Molecular Design InternationalInventors: William P. Purcell, Harlie A. Parish, Jr.
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Patent number: 5045560Abstract: Insecticidal, acaricidal, herbicidal and antimycotic 3-aryl-pyrrolidine-2,4-diones of the formula ##STR1## in which X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number from 0-3,R represents hydrogen or represents the groups --CO--R.sup.1 or --CO--O--R.sup.2, in whichR.sup.1 represents alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl which can be interrupted by hetero atoms, each of which radicals is optionally substituted by halogen, or represents optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl or substituted hetaryloxyalkyl, or represents optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl and substituted hetaryloxyalkyl, andR.sup.Type: GrantFiled: January 2, 1990Date of Patent: September 3, 1991Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Bernd Baasner, Hermann Hagemann, Andreas Krebs, Albrecht Marhold, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen, Benedikt Becker, Klaus Schaller, Harry Strang
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Patent number: 5039696Abstract: A maleimide derivative useful as an active agent for a fungicide for agriculture and horticulture, having the formula (I): ##STR1## wherein X and Y each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group or a trifluoromethyl group,Z represents a chlorine atom or bromine atom,and R represents a straight or branched alkyl group having 1 to 15 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, an alkynyl group having 2 to 5 carbon atoms, an alkoxyalkyl group having 2 to 5 carbon atoms, an oxoalkyl group having 3 to 6 carbon atoms or a phenyl group or a phenyl alkyl group which may be substituted.Type: GrantFiled: February 1, 1990Date of Patent: August 13, 1991Assignee: Suntory LimitedInventors: Shinjiro Niwata, Harukazu Fukami, Masaki Hashimoto, Norio Ohtsuka, Fumio Fujita
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Patent number: 5039703Abstract: A method for the treatment of inflammatory bowel disorders, together with a pharmaceutical composition comprising short chain fatty acids that is useful therein, is described in this invention. The administration of short chain fatty acids of about 2 to about 6 carbon-length to patients afflicated with inflammatory bowel disorders is shown to effectively alleviate the symptoms of the treated disorder.Type: GrantFiled: November 16, 1989Date of Patent: August 13, 1991Inventor: Richard I. Breuer
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Patent number: 5034402Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups,enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.Type: GrantFiled: April 12, 1990Date of Patent: July 23, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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Microbiocidal compositions comprising an aryl alkanol and a microbiocidal compound dissolved therein
Patent number: 5028619Abstract: Provided are microbiocidal solutions comprising an aryl alkanol solvent and a microbiocidal compound dissolved therein. The solutions may be used to impart microbiocidal properties to polymer compositions.Type: GrantFiled: January 25, 1989Date of Patent: July 2, 1991Assignee: Morton International, Inc.Inventors: Nuno M. Rei, Ronald C. Wilson -
Patent number: 5001115Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.Type: GrantFiled: May 17, 1989Date of Patent: March 19, 1991Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4994491Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.Type: GrantFiled: December 14, 1988Date of Patent: February 19, 1991Assignee: Molecular Design InternationalInventors: William P. Purcell, Harlie A. Parish, Jr.
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Patent number: 4990513Abstract: The antihypoxic drug with verebroprotective and hepatoprotective action contains piracetam and orotic acid or their pharmaceutically tolerable salts in a weight ratio of from 500:1 to 1:2. This combined drug is administered for the treatment of acute and chronic diseases and exogenic intoxications in daily doses respectively from 0.150 to 50 g and from 0.030 to 0.30 g of both components. The synergistic effect of the combination is shown in the antihypoxic action as confirmed by clinical data. The drug can be administered orally or parenterally. The oral therapy comprises tablets, capsules, pills, solutions and emulsions and is applied in slight forms of exogenic intoxications, whereas the parenterally therapy is suitable in case of severe diseases and acute exogenic intoxications leading to complex injuries of the organism.Type: GrantFiled: February 3, 1987Date of Patent: February 5, 1991Assignee: S O "Pharmachim"Inventors: Ani I. Genova, Milka P. Nikolova, Maria G. Todorova, Alexander P. Monov, Nikola G. Alexandrov, Rumen K. Nikolov, Violeta H. Andonova, Nadejda I. Zoneva, Yosif N. Nisimov, Snejana G. Vitkova, Nikola G. Boyadjiev, Anastasia M. Stoyanova, Keranka N. Savova, Nevena L. Firkova, Slava N. Spasova
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Patent number: 4990531Abstract: Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitrogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.Type: GrantFiled: February 24, 1989Date of Patent: February 5, 1991Assignee: Roussel UclafInventors: Giulio Galliani, Fernando Barzaghi, Michel Fortin, Carlo Gorini, Emilio Toja
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Patent number: 4977183Abstract: The invention concerns fungicidal compounds of the formula ##STR1## wherein R signifies a chlorine, bromine or iodine atom, n 0, 1, 2 or 3 and X, X', Y and Z have the meanings given in the description.Type: GrantFiled: September 12, 1989Date of Patent: December 11, 1990Assignee: The Dow Chemical CompanyInventors: Norman Haberle, Anneliese Reutter
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Patent number: 4975441Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a chemical inhibitor of glycosidase activity chosen from lactams having the structure: ##STR1## where A.sup.1 and A.sup.6 are --H, --CH.sub.3, ##STR2## --CH.sub.2 OT or ##STR3## A.sup.1 and A.sup.6 being the same or different, and at least one of which being the group: ##STR4## in a lactam ring; and where Q is --OT', --NHT' or a lactam linkage to A.sup.1 or A.sup.6 ;the Q groups being the same or different, and at least one of which is involved in a lactam linkage;and where T is the same or different and is chosen from --H, --C.sub.p H.sub.2p+1 or a metal ion,T' is --H or --COC.sub.p H.sub.2p+1, andp is an integer of from 1 to 22;provided that:where any of the Q groups is --OT' or --NHT',then that group or groups can be of either stereochemical configuration with respect to the plane of the ring; and(ii) a cosmetically acceptable vehicle for the chemical inhibitor.Type: GrantFiled: March 22, 1989Date of Patent: December 4, 1990Assignee: Unilever Patent Holdings B.V.Inventor: Walter T. Gibson
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Patent number: 4973602Abstract: Novel N-aryl derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol and their acylated derivatives are disclosed. These compounds have useful antiviral activity.Type: GrantFiled: September 26, 1989Date of Patent: November 27, 1990Assignee: G. D. Searle & Co.Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
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Patent number: 4952580Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.Type: GrantFiled: November 9, 1988Date of Patent: August 28, 1990Assignee: FMC CorporationInventors: Anthony J. Martinez, Thomas G. Cullen
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Patent number: 4945104Abstract: A maleimide derivative having the formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group which may be substituted, or an aralkyl group having 7 to 10 carbon atoms, and X.sub.1 and X.sub.2 independently represent a hydrogen atom or a halogen atom, and a production process thereof as well as a agricultural and horticultural fungicide containing, as an active ingredient, the maleimide derivative.Type: GrantFiled: June 23, 1989Date of Patent: July 31, 1990Assignee: Suntory LimitedInventors: Harukazu Fukami, Masaki Hashimoto, Shinjiro Niwata, Norio Ohtsuka, Fumio Fujita
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Patent number: 4927844Abstract: New N-substituted dichloromaleimides of the general formula (I) ##STR1## in which R stands for hydrogen or alkylAr stands for optionally substituted aryl,A.sup.1 and A.sup.2 independently of one another each stand for optionally substituted alkylene andn stands for a number 0 or 1,with the exception of the compound 2-(dichloromaleimido)acetanilide, have been found. These compounds are useful as pesticides, especially as fungicides and bactericides.Type: GrantFiled: November 10, 1988Date of Patent: May 22, 1990Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Wolfgang Kramer, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler
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Patent number: 4925867Abstract: Compounds of formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R represents a hydrocarbon group, X represents oxygen or sulphur, and R and --NH.sub.2 are cis; are of use in the treatment and/or prevention of neurodegenerative disorders, and are also useful as anticonvulsant agents and muscle relaxants.Type: GrantFiled: September 29, 1989Date of Patent: May 15, 1990Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Paul D. Leeson, Tamara Ludduwahetty, Brian J. Williams
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Patent number: 4925868Abstract: The present invention relates to a compound of the formula: ##STR1## wherein X is sulfur or optionally substituted imino group; Y is a bond, oxygen, phenylene, phenyleneoxy, or oxyphenyleneoxy; R.sup.1 is hydrogen or optionally substituted hydrocarbon residue; R.sup.2 is optionally substituted hydrocarbon residue; and R.sup.1 may form, together with the imino-nitrogen atom as X, a nitrogen-containing 5- to 7-membered ring, production and use thereof.The compound (I) of the present invention has an anti-oxidation activity and activities of preventing or improving functional disorders due to biologically active oxygen species, thus being useful as a pharmaceutical agent for prophylaxis and therapy of disorders in the circulatory system.Type: GrantFiled: August 12, 1987Date of Patent: May 15, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Minoru Hirata
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Patent number: 4914126Type: GrantFiled: September 23, 1987Date of Patent: April 3, 1990Assignee: Fisons plcInventors: John Dixon, Francis Ince
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Patent number: 4913721Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: October 31, 1988Date of Patent: April 3, 1990Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
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Patent number: 4897414Abstract: Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or mental strain of the formula (I) ##STR1## in which R' represents hydrogen, linear, branched or cyclic alkyl containing up to 8 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms and R represents aryl containing up to 14 carbon atoms, possibly substituted, or a mono- or polycyclic heterocyclic aromatic radical possibly substituted; also process and intermediates for their preparation, therapeutic compositions containing those compounds and method of use.Type: GrantFiled: June 27, 1988Date of Patent: January 30, 1990Assignee: Roussel UCAFInventors: Emilio Toja, Carlo Zirotti, Fernando Barzaghi, Giulio Galliani
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Patent number: 4886545Abstract: This invention provides compositions comprising a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen. The invention also provides compositions comprising a physiologically-active agent and the hereinabove recited 1-substituted azacycloalkane compound in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: July 23, 1987Date of Patent: December 12, 1989Assignee: Nelson Research & Development CompanyInventors: James V. Peck, Gevork Minaskanian
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Patent number: 4885306Abstract: Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or mental strain of the formula (I) ##STR1## in which R' and R.sub.2, being identical or different, represent hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms, R.sub.1 represents a possibly substituted aryl containing up to 14 carbon atoms, or a possibly substituted mono- or polycyclic heterocyclic aromatic radical; also therapeutic compositions containing those compounds and method of use.Type: GrantFiled: June 2, 1988Date of Patent: December 5, 1989Assignee: Roussel UclafInventors: Emilio Toja, Carlo Gorini, Fernando Barzaghi, Giulio Galliani
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Patent number: 4885307Abstract: Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or mental strain of the formula (I) ##STR1## in which R' represents hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms and R represents aryl containing up to 14 carbon atoms, possibly substituted, or a mono- or polycyclic heterocyclic aromatic radical, possibly substituted; also thereapeutic compositions containing those compounds and method of use.Type: GrantFiled: June 13, 1988Date of Patent: December 5, 1989Assignee: Roussel UclafInventors: Emilio Toja, Carlo Gorini, Fernando Barzaghi, Giulio Galliani
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Patent number: 4885311Abstract: Esters and amides of 13-trans-retinoic acid are disclosed which are used for the treatment of acne and skin diseases.Type: GrantFiled: June 29, 1987Date of Patent: December 5, 1989Assignee: Molecular Design InternationalInventors: Harlie A. Parish, William P. Purcell
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Patent number: 4882350Abstract: Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or metal strain of the formula (I) ##STR1## in which R' represents hydrogen, linear, branched or cyclic alkyl containing up to 12 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms and R represents aryl containing up to 14 carbon atoms, possibly substituted, or a mono- or polycyclic heterocyclic aromatic radical possibly substituted, provided that if R is unsubstituted phenyl, R' does not represent methyl or ethyl; also therapeutic compositions containing those compounds and method of use.Type: GrantFiled: June 24, 1988Date of Patent: November 21, 1989Assignee: Roussel UclafInventors: Emilio Toja, Carlo Gorini, Fernando Barzaghi, Giulio Galliani
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Patent number: 4876268Abstract: Acylated derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol and their N-alkyl and N-hydroxyalkyl derivatives in which all the free hydroxyl groups are acylated with acyl groups having from one to six carbon atoms and in which the N-alkyl substituents in the N-alkyl and N-hydroxyalkyl derivatives contain from one to fourteen carbon atoms are disclosed.Type: GrantFiled: November 3, 1988Date of Patent: October 24, 1989Assignee: G. D. Searle & Co.Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
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Patent number: 4863953Abstract: The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I: ##STR1## or pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of neurodegenerative disorders.Type: GrantFiled: November 18, 1988Date of Patent: September 5, 1989Assignee: Merck & Co., Inc.Inventors: Paul D. Leeson, Brian J. Williams
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Patent number: 4855289Abstract: The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.Type: GrantFiled: July 30, 1987Date of Patent: August 8, 1989Inventors: Per O. Wester, Thomas R. Dyckner
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Patent number: 4851421Abstract: The invention relates to a biocidal fine powder with increased biocidal activity and an agricultural suspension containing the biocidal fine powder and an adjuvant selected from the group consisting of polyoxyalkylene-type nonionic surface active agents and polyoxyalkylene alkyl or alkylaryl ether phosphates or their salts.Type: GrantFiled: December 22, 1986Date of Patent: July 25, 1989Assignee: Kao CorporationInventors: Tetsuji Iwasaki, Yasushi Kamihisa
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Patent number: 4849444Abstract: Compounds of the formula I ##STR1## with R.sup.1 equal to H or (cyclo)alk(en)yl, R.sup.2 equal to H or alkyl, R.sup.3 equal to alkyl, R.sup.4 /R.sup.5 equal to H, alkyl or acyl, and Y equal to H, alkyl, CF.sub.3 or Hal, are described, as are processes for the preparation thereof.They are effective diuretics and antihypertensive agents with a lipid-lowering action.Type: GrantFiled: April 22, 1988Date of Patent: July 18, 1989Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Max Hropot, Ernold Granzer, Bela Kerekjarto
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Patent number: 4847285Abstract: Substituted 1-phenyl-3-methyl-pyrrolidinediones of the general formula: ##STR1## in which R may represent fluorine, chlorine, bromine, iodine, CN, SCN or methanesulfonyl, Z represents one or more of the same or different substituents selected from fluorine, chlorine, bromine, iodine, NO.sub.2, CN, SCN, sulfamoyl, phenoxy, an alkyl having from 1 to 3 carbon atoms, a halogenalkyl having from 1 to 3 carbon atoms and 1 to 7 halogen atoms selected from fluorine, chlorine or bromine, an alkyloxy having from 1 to 3 carbon atoms, a halogenalkoxy having from 1 to 3 carbon atoms and 1 to 4 halogen atoms selected from the group consisting of fluorine, chlorine and bromine, an allyloxy or ethoxycarbonyl, and n is 0 or an integer from 1 to 4 with the following types of substitutions: 2-, 4-, 2,3-, 2,4-, 2,5-, 2,6-, 3,4-, 2,3,4-, 2,3,5-, 2,3,6-, 2,4,5-, 2,4,6-, 3,4,5-, 2,3,4,5-, 2,4,5,6- and 2,3,5,6-. The invention also relates to a process for making the compounds, which are active ingredients of fungicidal agents.Type: GrantFiled: April 27, 1988Date of Patent: July 11, 1989Assignee: The Dow Chemical CompanyInventors: Norman Haberle, Anneliese Reutter, Peter Kinzel
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Patent number: 4833160Abstract: 3-(3,5-di-tert-butyl-4-hydroxy-benzylidene)-2-pyrrolidone and N-substituted derivatives thereof are described. The substituent includes alkyl, alkoxy, alkynyl phenyl-alkylene, hydroxy-alkylene and amino-alkylene. They are effective as an anti-inflammatory, analgesic and antithermic agent, and they have a low toxicity.Type: GrantFiled: April 23, 1986Date of Patent: May 23, 1989Assignee: Eisai Co., Ltd.Inventors: Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Isao Yamatsu, Seiichi Kobayashi, Hiroshi Shirota, Kouichi Katayama
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Patent number: 4829079Abstract: Memory enhancing 1-(benzenesulfonyl)-2-oxo-5-alkoxy-pyrrolidines are prepared by alkylation of the corresponding pyrrolidones or pyrrolidone precursors.Type: GrantFiled: December 29, 1986Date of Patent: May 9, 1989Assignee: Roussel UclafInventors: Emilio Toja, Carlo Gorini, Carlo Zirotti, Fernando Barzaghi, Giulio Galliani
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Patent number: 4824861Abstract: The invention relates to 4-hydroxy pyrrolidone derivatives which help restore learning and memory difficulties associated with ageing. A compound of the invention is 2-(4-hydroxy-2-oxo-1-pyrrolidineacetamido)acetamide.Type: GrantFiled: December 11, 1987Date of Patent: April 25, 1989Assignee: ISF Societa Per AzioniInventors: Mario Pinza, Carlo Farina, Silvano Banfi, Ugo Pfeiffer
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Patent number: 4810722Abstract: The therapeutic compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures or old age and excessive intellectual fatigue having the formula (I): ##STR1## in which R.sub.1 represents an alkyl radical, linear or branched, containing up to 8 carbons atoms, an acyl radical containing from 1 to 6 carbon atoms or a cycloalkyl radical containing from 3 to 6 carbon atoms and R represents an aryl radical containing up to 14 carbon atoms, unsubstituted or substituted, or a mono- or polycyclic heterocyclic radical, unsubstituted or substituted. Also, therapeutic compositions containing the compound, method of preparing the compound and method of use.Type: GrantFiled: March 26, 1987Date of Patent: March 7, 1989Assignee: Roussel UclafInventors: Emilio Toja, Carlo Zirotti, Giulio Galliani, Fernando Barzaghi
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Patent number: 4802913Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.Type: GrantFiled: August 5, 1986Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventors: John Clough, Christopher R. A. Godfrey
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Patent number: 4801603Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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Patent number: 4761423Abstract: Fungicidal or insecticidal seed dressings characterized by a water content substantially greater than that of the carrier vehicle providing homogeneous coating.Type: GrantFiled: October 24, 1985Date of Patent: August 2, 1988Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Andras Szego, Jozsef Sos, Ferenc Kovats, Istvan Petroczi, Gyorgy Kis, Jozsef Karsai, Sandor ngyan, Istvan Racz, Katalin Marmarosi
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Patent number: 4760077Abstract: There is described the use of pyrrothine derivatives of the general formula I ##STR1## wherein R.sub.1 and R.sub.3 signify hydrogen or methyl, R.sub.2 hydrogen, methyl or an acyl group with 1 to 5 carbon atoms and X and Y signify hydrogen, an equivalent of a physiolgically acceptable cation or together a single bond, for the inhibition of the allergen-induced degranulation of peripheral leukocytes.Type: GrantFiled: May 15, 1986Date of Patent: July 26, 1988Assignee: Boehringer Mannheim GmbHInventors: Peter Stahl, Hans Seidel, Herbert Von der Eltz, Otto-Henning Wilhelms, Androniki Roesch
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Patent number: 4745113Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sub.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.Type: GrantFiled: September 10, 1986Date of Patent: May 17, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Martin Anderson, Anthony G. Brinnand
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Patent number: 4677120Abstract: Esters and amides of 13-cis-retinoic acid are disclosed which are used for the treatment of acne and skin diseases.Type: GrantFiled: July 31, 1985Date of Patent: June 30, 1987Assignee: Molecular Design InternationalInventors: Harlie A. Parish, William P. Purcell
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Patent number: 4665089Abstract: Cataract in mammalian lenses can be prevented or reversed by applying a solution of an imidoester, a N-hydroxysuccinimide-ester or hydrogen peroxide to the lens under conditions that permit the solution to interact with the lens constituents.Type: GrantFiled: March 21, 1985Date of Patent: May 12, 1987Assignee: Massachusetts Institute of TechnologyInventors: Roelant J. Siezen, Christophe M. Coppin, George B. Benedek