Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
  • Patent number: 5093360
    Abstract: 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: Grant
    Filed: April 7, 1989
    Date of Patent: March 3, 1992
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5043008
    Abstract: 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: Grant
    Filed: October 25, 1989
    Date of Patent: August 27, 1991
    Assignee: Kao Corporation
    Inventor: Tetsuji Iwasaki
  • Patent number: 5039700
    Abstract: 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: Grant
    Filed: March 19, 1990
    Date of Patent: August 13, 1991
    Assignee: Sanofi
    Inventors: Jean Gubin, Pierre Chatelain, Marcel Descamps, Dino Nisato, Henri Inion, Jean Lucchetti, Jean-Marie Mahaux, Jean-Noel Vallat
  • Patent number: 5030629
    Abstract: 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: Grant
    Filed: August 11, 1989
    Date of Patent: July 9, 1991
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 5021430
    Abstract: 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: Grant
    Filed: June 29, 1987
    Date of Patent: June 4, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Gary M. Ksander
  • Patent number: 5019395
    Abstract: 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: Grant
    Filed: August 9, 1989
    Date of Patent: May 28, 1991
    Assignee: Warner-Lambert Company
    Inventors: Majid Mahjour, Bernadette Mauser, Zahra Rashidbaigi, Edwards E. Linn
  • Patent number: 5017618
    Abstract: 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: Grant
    Filed: September 18, 1989
    Date of Patent: May 21, 1991
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4970233
    Abstract: 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: Grant
    Filed: August 4, 1987
    Date of Patent: November 13, 1990
    Inventor: John E. McHugh
  • Patent number: 4960771
    Abstract: 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: Grant
    Filed: July 12, 1988
    Date of Patent: October 2, 1990
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4956384
    Abstract: 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: Grant
    Filed: May 4, 1988
    Date of Patent: September 11, 1990
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Vittorino Servadio
  • Patent number: 4952599
    Abstract: 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: Grant
    Filed: July 20, 1988
    Date of Patent: August 28, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Josef Ehrenfreund, Manfred Boger, Jozef Drabek
  • Patent number: 4943307
    Abstract: 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: Grant
    Filed: July 15, 1988
    Date of Patent: July 24, 1990
    Assignee: 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
  • Patent number: 4939141
    Abstract: 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: Grant
    Filed: April 4, 1989
    Date of Patent: July 3, 1990
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
  • Patent number: 4937263
    Abstract: 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: Grant
    Filed: July 17, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta J. Lee, Robert L. Smith, Clarence S. Rooney
  • Patent number: 4937264
    Abstract: 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: Grant
    Filed: June 30, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
  • Patent number: 4918092
    Abstract: 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: Grant
    Filed: January 15, 1988
    Date of Patent: April 17, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Frenette, Robert N. Young, Masatoshi Kakushima
  • Patent number: 4912131
    Abstract: 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: Grant
    Filed: October 11, 1988
    Date of Patent: March 27, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Julian Adams, Yvan Guindon
  • Patent number: 4891373
    Abstract: 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: Grant
    Filed: November 23, 1988
    Date of Patent: January 2, 1990
    Assignee: Pfizer Inc.
    Inventors: Peter Stoss, Matyas Leitold, Rodney Yeates
  • Patent number: 4888351
    Abstract: 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: Grant
    Filed: November 7, 1988
    Date of Patent: December 19, 1989
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 4886820
    Abstract: 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: Grant
    Filed: November 3, 1988
    Date of Patent: December 12, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rainer Gross, Matthias Schramm
  • Patent number: 4885299
    Abstract: 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: Grant
    Filed: January 17, 1989
    Date of Patent: December 5, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4883813
    Abstract: 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: Grant
    Filed: August 24, 1988
    Date of Patent: November 28, 1989
    Assignee: American Biotechnology Company
    Inventors: Peter E. Maxim, Robert W. Veltri
  • Patent number: 4873259
    Abstract: 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: Grant
    Filed: January 11, 1988
    Date of Patent: October 10, 1989
    Assignee: Abbott Laboratories
    Inventors: James B. Summers, Jr., Bruce P. Gunn, Dee W. Brooks
  • Patent number: 4868179
    Abstract: 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: Grant
    Filed: April 22, 1987
    Date of Patent: September 19, 1989
    Inventor: Jay N. Cohn
  • Patent number: 4868153
    Abstract: 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: Grant
    Filed: August 17, 1988
    Date of Patent: September 19, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
  • Patent number: 4863949
    Abstract: 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: Grant
    Filed: September 21, 1987
    Date of Patent: September 5, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Herbert Simon, Helmut Michel, Wolfgang Bartsch, Klaus Strein
  • Patent number: 4859700
    Abstract: 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: Grant
    Filed: February 12, 1988
    Date of Patent: August 22, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4847286
    Abstract: 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: Grant
    Filed: March 27, 1987
    Date of Patent: July 11, 1989
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Satoshi Tamaki, Masaru Kitagawa, Hirokazu Tsuda, Susumu Nishizawa, Nobuhara Kakeya, Kazuhiko Kitao
  • Patent number: 4845123
    Abstract: 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: Grant
    Filed: August 5, 1985
    Date of Patent: July 4, 1989
    Assignee: The Ohio State University
    Inventors: Zbigniew Walaszek, Malgorzata Hanausek-Walaszek, Thomas E. Webb, John P. Minton
  • Patent number: 4816481
    Abstract: 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: Grant
    Filed: July 21, 1987
    Date of Patent: March 28, 1989
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Naoyuki Takasugi, Mitsuyasu Ushijima, Satoshi Inoue, Terukage Hirata
  • Patent number: 4812469
    Abstract: 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: Grant
    Filed: February 12, 1988
    Date of Patent: March 14, 1989
    Assignee: Adir Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4791123
    Abstract: 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: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4786637
    Abstract: 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: Grant
    Filed: January 22, 1988
    Date of Patent: November 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
  • Patent number: 4784856
    Abstract: 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: Grant
    Filed: August 10, 1987
    Date of Patent: November 15, 1988
    Assignee: Sekisui Kagaku Kogyo Kabushiki Kaisha
    Inventors: Mutsumi Fukuda, Takashi Nakagawa, Takaji Kishi, Michiharu Ando, Masahachi Yoshioka
  • Patent number: 4778805
    Abstract: 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: Grant
    Filed: June 18, 1987
    Date of Patent: October 18, 1988
    Assignee: Merck Frosst Canada
    Inventors: Julian Adams, Yvan Guindon, Patrice C. Belanger, Michel L. Belley, Joshua Rokach
  • Patent number: 4769379
    Abstract: 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: Grant
    Filed: July 2, 1985
    Date of Patent: September 6, 1988
    Assignee: Heinrich Mack Nachf.
    Inventors: Matyas Leitold, Peter Stoss
  • Patent number: 4749714
    Abstract: 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: Grant
    Filed: September 18, 1987
    Date of Patent: June 7, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rainer Gross, Matthias Schramm
  • Patent number: 4742077
    Abstract: 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: Grant
    Filed: September 8, 1986
    Date of Patent: May 3, 1988
    Assignee: Sandoz Ltd.
    Inventor: Anton Stutz
  • Patent number: 4734280
    Abstract: 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: Grant
    Filed: January 23, 1985
    Date of Patent: March 29, 1988
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventor: Pierre Braquet
  • Patent number: 4731385
    Abstract: 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: Grant
    Filed: October 21, 1986
    Date of Patent: March 15, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Shinichi Tsuboi, Shoko Sasaki, Yumi Hattori, Yoshio Kurahashi, Shinji Sakawa, Toshihito Kondo
  • Patent number: 4727086
    Abstract: 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: Grant
    Filed: June 30, 1986
    Date of Patent: February 23, 1988
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Yves-Michel Gargouil, Jean-Paul Vilaine
  • Patent number: 4722925
    Abstract: 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: Grant
    Filed: March 3, 1987
    Date of Patent: February 2, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
  • Patent number: 4720503
    Abstract: 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: Grant
    Filed: August 2, 1985
    Date of Patent: January 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Allan N. Tischler, Debra L. Allison
  • Patent number: 4713393
    Abstract: 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: Grant
    Filed: April 25, 1985
    Date of Patent: December 15, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Kathryn L. Thompson, David A. Boulton
  • Patent number: 4684661
    Abstract: 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: Grant
    Filed: November 20, 1985
    Date of Patent: August 4, 1987
    Assignee: Sandoz Ltd.
    Inventor: Anton Stuetz
  • Patent number: 4675320
    Abstract: 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: Grant
    Filed: May 15, 1985
    Date of Patent: June 23, 1987
    Assignee: Riker Laboratories, Inc.
    Inventors: Robert A. Scherrer, Richard M. Stern, Walton J. Hammar
  • Patent number: 4670457
    Abstract: 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: Grant
    Filed: July 19, 1979
    Date of Patent: June 2, 1987
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Maria L. Corno
  • Patent number: 4666931
    Abstract: 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: Grant
    Filed: December 27, 1985
    Date of Patent: May 19, 1987
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoshitaka Ohishi, Michiko Nagahara, Norio Kajikawa, Motoyuki Yajima, Katsumi Nogimori, Shigeki Kurokawa
  • Patent number: 4659709
    Abstract: 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: Grant
    Filed: August 12, 1985
    Date of Patent: April 21, 1987
    Assignee: Shionogi & Co.
    Inventors: Hiroshi Harada, Yoshihiro Matsushita, Masuhisa Nakamura, Yukio Yonetani
  • Patent number: 4656163
    Abstract: 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: Grant
    Filed: November 14, 1985
    Date of Patent: April 7, 1987
    Assignees: Bayer Aktiengesellschaft, Mobay Corporation
    Inventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet