Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
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Patent number: 5093360Abstract: Therapeutic as well as preventive measures to improve cosmetic conditions and to alleviate the symptoms of dermatologic disorders with retinal and its derivatives is disclosed. Cosmetic conditions and dermatologic disorders in humans and domestic animals in which retinal and its derivatives may be useful include age spots, wrinkles, warts, eczema, seborrheic keratoses, acne, oily skin, psoriasis, dandruff, xerosis, inflammatory and pruritic skin, disturbed keratinization skin changes associated with aging and possibly viral infections. Retinal and its derivatives include their stereoisomers, for example, all-trans, 13-cis, 11-cis, 9-cis, 7-cis, 11,13-cis and 9,13-cis vitamin A aldehydes, their hydrate, hemiacetal and acetal forms, and their adduct compounds. Compositions containing retinal or its derivative may be administered systemically such as orally, or topically to the affected areas of the skin.Type: GrantFiled: April 7, 1989Date of Patent: March 3, 1992Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 5043008Abstract: A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.Type: GrantFiled: October 25, 1989Date of Patent: August 27, 1991Assignee: Kao CorporationInventor: Tetsuji Iwasaki
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Patent number: 5039700Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.Type: GrantFiled: March 19, 1990Date of Patent: August 13, 1991Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain, Marcel Descamps, Dino Nisato, Henri Inion, Jean Lucchetti, Jean-Marie Mahaux, Jean-Noel Vallat
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Patent number: 5030629Abstract: A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I: ##STR1## wherein R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms, alkoxyalkyl, haloalkyl, specifically trifluoromethyl, alkoxy, amino, alkylamino and acylamino; R' and R" are hydrogen, alkyl, trifluoromethyl, alkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, carboxy, carbalkoxy, hydroxyalkyl or lower alkyl ester thereof; X is O or NR.sub.1 wherein R.sub.Type: GrantFiled: August 11, 1989Date of Patent: July 9, 1991Inventor: Vithal J. Rajadhyaksha
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Patent number: 5021430Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: June 29, 1987Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 5019395Abstract: Penetration of various drugs through living membranes is improved by their use in transdermal compositions containing certain penetration-enhancing systems. A new delivery device is also described.Type: GrantFiled: August 9, 1989Date of Patent: May 28, 1991Assignee: Warner-Lambert CompanyInventors: Majid Mahjour, Bernadette Mauser, Zahra Rashidbaigi, Edwards E. Linn
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Patent number: 5017618Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.Type: GrantFiled: September 18, 1989Date of Patent: May 21, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4970233Abstract: There is disclosed a method of treating inflammatory viral infections of Acquired Immunodeficiency Syndrome (AIDS) HTLV-111/LAV virus and Acquired Immunodeficiency Syndrome (AIDS) Related Complex (ARC) in humans by stimulating and increasing the rate of Prostaglandin Biosynthesis to levels many times higher than that now occurring naturally thereby enhancing and reconstituting the Immune System, comprising the oral administration of an effective dosage of 3,3-Bis(p-hydroxyphenyl) phthalide (phenolphthalein) by itself or in composition with, or in combination with a Prostaglandin Synthetase inhibitor Aspirin or Indomethacin. Comprising the oral administration of an effective dosage of 3,3-Bis(p-hydroxyphenyl) phthalide (phenolphthalein) by itself or in composition with, or in combination with a Prostaglandins Synthetase inhibitor Aspirin or Indomethacin.Type: GrantFiled: August 4, 1987Date of Patent: November 13, 1990Inventor: John E. McHugh
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Patent number: 4960771Abstract: Compositions for carrying physiologically active agents through body membranes having the structural formula I: ##STR1## where: R=H, Alkyl group containing from 1-18 carbon atoms, cycloalkyl, aryl, aralkyl, alkoxy, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;X=O and NR.sub.1, where R.sub.1 is selected from H, alkyl, aralkyl acyl group containing from 1-18 carbon atoms, cycloalkyl, hydroxyalkyl, alkoyloxyalkyl acyloxyalkyl and alkoxyalkyl;Y=O and NR.sub.2, where R.sub.2 is selected from H, alkyl, aralkyl, cycloalkyl, acyl group containing from 1-18 carbon atoms, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;m=2-4; andn=0-4,are disclosed.Type: GrantFiled: July 12, 1988Date of Patent: October 2, 1990Inventor: Vithal J. Rajadhyaksha
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Patent number: 4956384Abstract: Isosorbide 2- and 5-mononitrate esters with aliphatic, aryl, or cynnamic acids or diacids, or with alkylcarbonyloxy substituents optionally containing an isosorbide 2- or 5-mononitrate group, are useful in human therapy.Type: GrantFiled: May 4, 1988Date of Patent: September 11, 1990Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Vittorino Servadio
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Patent number: 4952599Abstract: Novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl which is substituted by one or more halogen atoms and/or C.sub.1 -C.sub.4 alkyl groups; C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, di(C.sub.3 -C.sub.8)cycloalkyl-C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 phenylalkyl or C.sub.1 -C.sub.4 phenylalkyl which is substituted in the phenyl nucleus by one or more members selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and/or C.sub.1 -C.sub.4 haloalkyl; or is C.sub.5 -C.sub.6 cycloalkenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.Type: GrantFiled: July 20, 1988Date of Patent: August 28, 1990Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Manfred Boger, Jozef Drabek
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Patent number: 4943307Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.Type: GrantFiled: July 15, 1988Date of Patent: July 24, 1990Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
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Patent number: 4939141Abstract: A (fused) benz(thio)amides of the general ##STR1## (wherein, symbol A represents a single bond or a group of methylene, ethylene, trimethylene, tetramethylene, vinylene, propenylene, butenylene, butadienylene or ethynylene group optionally being substituted by one, two or three of straight or branched alkyl groups(s) of from 1 to 10 carbon atom(s) and/or phenyl group(s);Symbol B represents(i) a heterocyclic ring of from 4 to 8 members containing one, two or three hetero atoms selected from oxygen, nitrogen and/or sulphur atom(s), wherein the ring may optionally be substituted by group(s) of oxo, thioxo and/or hydroxy group(s) with the exclusion of a ring of the formula: ##STR2## Symbol T represents an oxygen atom or a sulphur atom; R.sup.1 represents a group of general formula:(i) ##STR3## (ii) ##STR4## or (iii) ##STR5## or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s);(wherein R.sup.5 and R.sup.Type: GrantFiled: April 4, 1989Date of Patent: July 3, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
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Patent number: 4937263Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: July 17, 1989Date of Patent: June 26, 1990Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Robert L. Smith, Clarence S. Rooney
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Patent number: 4937264Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: June 30, 1989Date of Patent: June 26, 1990Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
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Patent number: 4918092Abstract: Compounds having the formula I: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.Type: GrantFiled: January 15, 1988Date of Patent: April 17, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Robert N. Young, Masatoshi Kakushima
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Patent number: 4912131Abstract: 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.Type: GrantFiled: October 11, 1988Date of Patent: March 27, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Julian Adams, Yvan Guindon
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Patent number: 4891373Abstract: Novel aminopropanol derivatives of 1,4:3,6-dianhydro-hexitol nitrates of the general formula I ##STR1## in which X has the meaning given in the specification, processes for their preparation and their use in preventing and treating angina pectoris, systemic hypertension and pulmonary hypertension in mammals.Type: GrantFiled: November 23, 1988Date of Patent: January 2, 1990Assignee: Pfizer Inc.Inventors: Peter Stoss, Matyas Leitold, Rodney Yeates
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Patent number: 4888351Abstract: This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.Type: GrantFiled: November 7, 1988Date of Patent: December 19, 1989Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
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Dihydropyridine combination product comprising a dihydropyridine compound and a cardioactive nitrate
Patent number: 4886820Abstract: A solid medicament formulation which can be administered orally, comprising 1 to 40 mg of a dihydropyridine of the formula ##STR1## in which R.sup.1 and R.sup.3 are always different from one another and represent alkyl which has 1 to 12 carbon atoms and which is optionally substituted once or several times by fluorine or chlorine or which is optionally interrupted by an oxygen atom in the chain, andA represents the radical ##STR2## R.sup.2 representing one or two substituents from the group consisting of nitro, chlorine and trifluoromethyl, or represents and 0.1 to 100 mg of a cardioactive nitrate. The composition is cardio-active and the patient's tendency toward nitrate tolerance is reduced.Type: GrantFiled: November 3, 1988Date of Patent: December 12, 1989Assignee: Bayer AktiengesellschaftInventors: Rainer Gross, Matthias Schramm -
Patent number: 4885299Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.Type: GrantFiled: January 17, 1989Date of Patent: December 5, 1989Assignee: ADIR Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4883813Abstract: Treatment of inflammation in mammals utilizing selected ketobutyrolactones and furylbutyrolactones. Treatment is applicable to both acute or chronic inflammation. Antiviral activity of methylfurylbutyrolactone is also disclosed.Type: GrantFiled: August 24, 1988Date of Patent: November 28, 1989Assignee: American Biotechnology CompanyInventors: Peter E. Maxim, Robert W. Veltri
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Patent number: 4873259Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.Type: GrantFiled: January 11, 1988Date of Patent: October 10, 1989Assignee: Abbott LaboratoriesInventors: James B. Summers, Jr., Bruce P. Gunn, Dee W. Brooks
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Patent number: 4868179Abstract: A method of reducing mortality associated with chronic congestive heart failure in a patient with impaired cardiac function and concomitant reduced exercise tolerance, comprising the oral administration to said patient in need of the same of a combination of (a) between about 75 and about 300 milligrams of hydralazine, per day and (b) between about 40 and about 160 milligrams of isosorbide dinitrate, per day.Type: GrantFiled: April 22, 1987Date of Patent: September 19, 1989Inventor: Jay N. Cohn
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Patent number: 4868153Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.Type: GrantFiled: August 17, 1988Date of Patent: September 19, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
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Patent number: 4863949Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.Type: GrantFiled: September 21, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Herbert Simon, Helmut Michel, Wolfgang Bartsch, Klaus Strein
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Patent number: 4859700Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.Type: GrantFiled: February 12, 1988Date of Patent: August 22, 1989Assignee: ADIR Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4847286Abstract: Cromoglycic acid derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (for ester bonding) whose amino group may optionally be substituted by at least one lower alkyl group, and R.sup.2 and R.sup.3 each independently is a lower alkyloxy-substituted or an unsubstituted lower alkyl group, an 1-alkanoyloxyalkyl group, an 1-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1,3-dioxol-2-on-4-ylmethyl group; nontoxic salts thereof; and pharmaceutical compositions containing such compounds. Since the compounds have antiallergic activity and are readily absorbable into the blood stream, they are useful as oral antiallergic agents.Type: GrantFiled: March 27, 1987Date of Patent: July 11, 1989Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Satoshi Tamaki, Masaru Kitagawa, Hirokazu Tsuda, Susumu Nishizawa, Nobuhara Kakeya, Kazuhiko Kitao
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Patent number: 4845123Abstract: A method for the reduction in vivo of the inappropriate levels of endogenous and environmental-derived compounds by inhibiting the activity of .beta.-glucuronidase in a mammal which comprises the administration to the mammal of an effective amount of a water insoluble, or sparingly soluble, sustained release precursor of glucarolactone or its analog is disclosed. The sustained release precursor of glucarolactone compound is selected from the group consisting of D-glucaric acid, D-galactaric acid, and L-idaric acid or derivatives or analogs. An orally administrable preparation of the sustained release precursor of glucarolactone compound is provided in the form of a capsule tablet, such that the glucarolactone or its analog is slowly released in the stomach of the treated animal or human.Type: GrantFiled: August 5, 1985Date of Patent: July 4, 1989Assignee: The Ohio State UniversityInventors: Zbigniew Walaszek, Malgorzata Hanausek-Walaszek, Thomas E. Webb, John P. Minton
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Patent number: 4816481Abstract: Disclosed herein is a cerebral-circulation-metabolism-function-improving agent which contains a 2,6-diphenyl-3,7-dioxabicyclo[3.3.0]octane derivative represented by the following formula as the effective ingredient: ##STR1## wherein, each of R.sub.1, R.sub.3, R.sub.4 and R.sub.6 represents a hydrogen atom or a lower alkoxyl group; each of R.sub.2 and R.sub.5 represents a hydrogen atom, a .beta.-D-glucosyl group or a hydroxyl group; and each of R.sub.7 and R.sub.8 represents an oxygen atom or two hydrogen atoms.Type: GrantFiled: July 21, 1987Date of Patent: March 28, 1989Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Naoyuki Takasugi, Mitsuyasu Ushijima, Satoshi Inoue, Terukage Hirata
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Patent number: 4812469Abstract: The invention relates to new acetamides derived from 2,3-dihydro-3-phenyl-2-benzofuranone, of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen or halogen atom,R.sub.2 and R.sub.3, which may be identical or different, each denote a hydrogen atom or a linear or branched alkyl radical containing 1 to 4 carbon atoms, a benzyl radical optionally substituted with a halogen atom, with an alkoxy radical containing 1 to 4 carbon atoms or with an alkyl radical having 1 to 4 carbon atoms, or a 3,4-methylenedioxybenzyl radical, or form, together with the nitrogen to which they are attached, a 4-morpholinyl radical or a 1-piperazinyl radical.Type: GrantFiled: February 12, 1988Date of Patent: March 14, 1989Assignee: Adir Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4791123Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Treatment of allograft rejection with mycophenolic acid morpholinoethylester and derivatives thereof
Patent number: 4786637Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.Type: GrantFiled: January 22, 1988Date of Patent: November 22, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee -
Patent number: 4784856Abstract: A percutaneous administration type pharmaceutical preparation in tape form comprising a flexible backing, which is not permeable by the active ingredient, and an adhesive base layer formed on said flexible backing; said adhesive base layer consisting essentially of an adhesive base material and an active ingredient compatible with said adhesive base material, wherein said adhesive base material is a copolymer containing 2-ethylhexyl acrylate (EHA) in a concentration of 45 mole% or more and N-vinyl-2-pyrrolidone (VP) in a concentration of 20 to 55 mole%, and said active ingredient is isosorbide dinitrate (ISDN) which is contained in a concentration of 10% by weight or more in said adhesive base material.Type: GrantFiled: August 10, 1987Date of Patent: November 15, 1988Assignee: Sekisui Kagaku Kogyo Kabushiki KaishaInventors: Mutsumi Fukuda, Takashi Nakagawa, Takaji Kishi, Michiharu Ando, Masahachi Yoshioka
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Patent number: 4778805Abstract: 4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention.Type: GrantFiled: June 18, 1987Date of Patent: October 18, 1988Assignee: Merck Frosst CanadaInventors: Julian Adams, Yvan Guindon, Patrice C. Belanger, Michel L. Belley, Joshua Rokach
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Patent number: 4769379Abstract: Dianhydrohexites of the formula ##STR1## wherein R.sup.1 is hydrogen or benzyl, R.sub.2 is alkyl or omega-theophyllin-7-yl-alkyl, and R.sup.1 and R.sub.2 together with the nitrogen atom to which they are attached form a bicyclic group and R.sup.3 is hydrogen, acyl, pyridylcarbonyl, nitro or a hydroxylamino group, are formed by an analogous method and used as pharmaceuticals in the treatment of heart and circulatory diseases.Type: GrantFiled: July 2, 1985Date of Patent: September 6, 1988Assignee: Heinrich Mack Nachf.Inventors: Matyas Leitold, Peter Stoss
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Patent number: 4749714Abstract: A solid medicament formulation which can be administered orally comprising 5 to 30 mg of nifedipine and 10 to 40 mg of isosorbide 5-mononitrate. Oral administration of such cardioactive formulation reduces the time tolerance to the isosorbide 5-mononitrate alone.Type: GrantFiled: September 18, 1987Date of Patent: June 7, 1988Assignee: Bayer AktiengesellschaftInventors: Rainer Gross, Matthias Schramm
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Patent number: 4742077Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## whereby R.sub.4 and R.sub.5 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and X represents oxygen, sulfur, imino, lower alkylimino, --(CH.sub.2)--, --(S.CH.sub.2)-- or --(O.CH.sub.2)--,R.sub.2 represents hydrogen or lower alkyl,R.sub.3 represents a group of formula ##STR3## whereby R.sub.6, R.sub.7 and R.sub.8 are the same or different and represent hydrogen or alkyl or R.sub.6 together with R.sub.7 or R.sub.7 together with R.sub.8 represent --(CH.sub.2).sub.m -- wherein m is 3 to 6,R.sub.9 represents alkyl, alkenyl, trialkylsilyl or alkyl substituted by hydroxy, lower alkoxy, lower halogenalkyl or aryl andn stands for 1, 2 or 3,which possess pharmaceutical in particular antimycotic activity as well as activity against phytopathogenic fungi.Type: GrantFiled: September 8, 1986Date of Patent: May 3, 1988Assignee: Sandoz Ltd.Inventor: Anton Stutz
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Patent number: 4734280Abstract: The present invention relates to the treatment of PAF Acether-induced maladies. The treatment comprises the administration of a ginkgolide or a ginkgolide derivative. Ginkgolide B has been found to be the most effective. The ginkgolides may be introduced orally, intraveneously or by spray inhalation.Type: GrantFiled: January 23, 1985Date of Patent: March 29, 1988Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventor: Pierre Braquet
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Patent number: 4731385Abstract: An insecticidal and fungicidal composition comprising (1) An insecticidally effective amount of a nitromethylene derivative of the formula ##STR1## in which X is a lower alkyl group, a lower alkoxy group, or a halogen atom,n is 0, 1 or 2 andm is 2 or 3,and a fungicidally effective amount of at least one fungicide selected from the group consisting of(2) O-ethyl S,S-diphenyl phosphorodithioate,(3) 4,5,6,7-tetrachlorophthalide,(4) 1-(4-chlorobenzyl)-1-cyclopentyl-3-phenylurea,(5) Validamycin A, 3'-iso-propoxy-2-methylbenzenilide, o-trifluoromethyl-m'-isopropoxybenzoylanilide or 6-(3,5-dichloro-4-methylphenyl-3(2H)pyridazinone, and(6) di-isopropyl-1,3-dithiolan-2-ylidenemalonate, 5-methyl-1,2,4-triazo[3,4-b]-benzothiazole, 3-allyloxy-1,2-benzisothiazole 1,1-dioxide, and 1,2,5,6-tetrahydro-4H-pyrrolo-[3,2,1-i,j]quinolin-4-one, [5-amino-2-methyl-6-(2,3,4,5,6-pentahydroxycyclohexyloxy)tetrahydropyran-3 -yl]amino-.alpha.-iminoacetic acid or S-benzyl diisopropylphosphorothiolate.Type: GrantFiled: October 21, 1986Date of Patent: March 15, 1988Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Shinichi Tsuboi, Shoko Sasaki, Yumi Hattori, Yoshio Kurahashi, Shinji Sakawa, Toshihito Kondo
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Patent number: 4727086Abstract: The invention relates to 2,3-dihydrobenzofuran derivatives of the general formula: ##STR1## in which: each of X.sub.1 and X.sub.2, which are identical or different, represents a hydrogen or halogen atom or an alkoxy radical containing from 1 to 4 carbon atoms,X.sub.3 represents a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms,Y represents a hydrogen atom or a hydroxy radical, each of R.sub.1 and R.sub.2, which are identical or different, represents an alkyl radical having from 1 to 4 carbon atoms,or R.sub.1 represents a methyl radical and R.sub.2 represents a phenylalkyl grouping or a 2-indanyl grouping, each of which may be substituted or unsubstituted,or R.sub.1 and R.sub.2 together form, with the nitrogen atom to which they are attached, a piperazinyl radical, a tetrahydroisoquinolyl radical, a morpholinyl radical or a tetrahydrothienopyridinyl radical. The compounds are useful in the treatment of hypertension.Type: GrantFiled: June 30, 1986Date of Patent: February 23, 1988Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Yves-Michel Gargouil, Jean-Paul Vilaine
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Patent number: 4722925Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: March 3, 1987Date of Patent: February 2, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4720503Abstract: N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e.g., methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e.g., methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products.Type: GrantFiled: August 2, 1985Date of Patent: January 19, 1988Assignee: Merck & Co., Inc.Inventors: Bruce E. Witzel, Allan N. Tischler, Debra L. Allison
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Patent number: 4713393Abstract: Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent anti-inflammatory agents.Type: GrantFiled: April 25, 1985Date of Patent: December 15, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Kathryn L. Thompson, David A. Boulton
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Patent number: 4684661Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 independently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2, CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u, in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.Type: GrantFiled: November 20, 1985Date of Patent: August 4, 1987Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 4675320Abstract: Antimicrobial 2-nitro-3-phenylbenzofurans wherein the benzo or the 3-phenyl portion of the molecule is bonded to an alkylene or an oxyalkylene group which is in turn bonded to a basic nitrogen atom or to the nitrogen atom of an (N-lower alkanoyl)amino group.Type: GrantFiled: May 15, 1985Date of Patent: June 23, 1987Assignee: Riker Laboratories, Inc.Inventors: Robert A. Scherrer, Richard M. Stern, Walton J. Hammar
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Patent number: 4670457Abstract: 2H-Benzofuran-3-one derivatives, process for their preparation and pharmaceutical compositions containing them. The compounds and compositions are useful in the treatment of allergies.Type: GrantFiled: July 19, 1979Date of Patent: June 2, 1987Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Gianfederico Doria, Ciriaco Romeo, Maria L. Corno
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Patent number: 4666931Abstract: A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.Type: GrantFiled: December 27, 1985Date of Patent: May 19, 1987Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoshitaka Ohishi, Michiko Nagahara, Norio Kajikawa, Motoyuki Yajima, Katsumi Nogimori, Shigeki Kurokawa
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Patent number: 4659709Abstract: Highly effective diuretic antihypertensives, i.e., 2,3-dihydrobenzofuran-5-sulfonamide derivatives which is classified to loop diuretics with less adverse side-effects and can be administered orally at a daily dosage of 0.5-200 mg or parenterally of 0.01-50 mg.Type: GrantFiled: August 12, 1985Date of Patent: April 21, 1987Assignee: Shionogi & Co.Inventors: Hiroshi Harada, Yoshihiro Matsushita, Masuhisa Nakamura, Yukio Yonetani
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Patent number: 4656163Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms,Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin which M denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation, for prolonging the duration of a high activity in agents for combating soil pests.Type: GrantFiled: November 14, 1985Date of Patent: April 7, 1987Assignees: Bayer Aktiengesellschaft, Mobay CorporationInventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet