Ulcer Treatment Patents (Class 514/925)
  • Patent number: 5120533
    Abstract: Dimethylpolysiloxane is effective in the treatment of ulcers of the gastrointestinal tract.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: June 9, 1992
    Assignee: Steigerwald Arzneimittelwerk GmbH
    Inventors: Alfred Schmidt, Hans-Jurgen Upmeyer
  • Patent number: 5114953
    Abstract: Compounds of the formulas ##STR1## wherein R.sup.1 is H and R.sup.2 is alkyl (3-8C) or wherein R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.n -- wherein n=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is a substituted or unsubstituted fused or conjugated bicycloaryl methylene;X is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amineare useful for treating or preventing ulceration of tissue, especially cornea.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: May 19, 1992
    Assignee: University of Florida
    Inventors: Richard E. Galardy, Damian Grobelny, Gregory Schultz
  • Patent number: 5109023
    Abstract: The invention provides a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.
    Type: Grant
    Filed: December 5, 1990
    Date of Patent: April 28, 1992
    Assignee: Glaxo Group Limited
    Inventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
  • Patent number: 5096891
    Abstract: An ointment comprising an adenosine 3',5'-cyclic phosphate derivative as an active ingrediment, an ointment base having water-absorbing and drying properties, a saccharide and/or inorganic high polymer is disclosed. The ointment exhibits improved stability of the adenosine 3',5'-cyclic phosphate derivative.
    Type: Grant
    Filed: March 30, 1989
    Date of Patent: March 17, 1992
    Assignee: Daiichi Seiyaku Co., Ltd.
    Inventors: Sadao Hirota, Hitoshi Yamauchi
  • Patent number: 5093132
    Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: March 3, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-ichiro Hirai
  • Patent number: 5091547
    Abstract: A pharmaceutical phenylacetic acid derivative of the following formula (I): ##STR1## with the process of obtention which includes reacting 2-(2,6-dichloroaniline)-phenylacetic acid with zinc oxide, zinc hydroxides, zinc carbonates or zinc salts or reacting an ammonium salt, an alkali metal salt or an alkaline earth metal salt of 2-(2,6-dichloroaniline)-phenylacetic acid with a zinc salt, e.g. zinc chloride, in a nonpolar solvent. The compound of formula I is novel and has improved pharmaceutical properties in anti-inflammatory preparations.
    Type: Grant
    Filed: May 17, 1990
    Date of Patent: February 25, 1992
    Assignee: Laboratorias Vinas, S.A.
    Inventor: Antonio Buxade
  • Patent number: 5089639
    Abstract: N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur,R2 is lower alkyl,R3 is hydrogen or lower alkyl,m has the value of 1 or 2,R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5,R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, andQ represents an ethylene-1,2-diyl group --CH.dbd.
    Type: Grant
    Filed: January 24, 1991
    Date of Patent: February 18, 1992
    Assignee: Jouveinal S.A.
    Inventors: Gilbert G. Aubard, Alain P. Calvet, Jean-Pierre Defaux, Claude J. Gouret, Agnes M. Grouhel, Henry L. Jacobelli, Jean-Louis Junien, Xavier B. Pascaud, Francois F. Roman, James P. Hudspeth, Yuan Lin
  • Patent number: 5081154
    Abstract: The present invention relates to metoprolol succinate, a new therapeutically active compound, and pharmaceutical preparations comprising this new compound.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: January 14, 1992
    Assignee: Aktiebolaget Hassle
    Inventors: Curt H. Appelgren, Eva C. Eskilsson
  • Patent number: 5081157
    Abstract: A film-forming composition for topical application of medicaments to body tissues. The film-forming composition includes hydroxypropyl cellulose; a non-toxic volatile solvent for said hydroxypropyl cellulose and said reaction product, and an esterification agent which reacts with the hydroxypropyl cellulose to form a reaction product which is soluble in the solvent. The medicinal compound is selected from the group consisting of hydrocortisone, hydrocortisone acetate, betamethasone dipropionate, triamainolone acetonide, lidocaine hydrochloride, dibucaine hydrochloride.
    Type: Grant
    Filed: February 6, 1991
    Date of Patent: January 14, 1992
    Assignee: Zila Pharmaceuticals, Inc.
    Inventor: Edwin Pomerantz
  • Patent number: 5081158
    Abstract: Medicated protective films are formed in situ on body tissue by applying a composition comprising (a) hydroxypropyl cellulose; (b) an esterification agent which reacts with the hydroxypropyl cellulose to form a reaction product which is soluble in the solvent of (c), but insoluble in body fluids at body temperatures; and (c) a nontoxic volatile solvent for said hydroxypropyl cellulose and said reaction products; and (d) a separate medicinal component. The films are tough, resilient and adhesive to body tissue including the mucosa.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: January 14, 1992
    Assignee: Zila Pharmaceuticals, Inc.
    Inventor: Edwin Pomerantz
  • Patent number: 5066496
    Abstract: Ganglioside mixtures and/or lipid mixtures e.g. from brain and omentum, are found to be effective to treat peptic ulcers.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: November 19, 1991
    Assignees: Angio-Medical Corporation, Trustees of Boston University
    Inventors: Sandor Szabo, Meryl S. A. Rubin, Michael Klibaner, Ahmad R. Kamarei, Robert S. Sinn, Nicholas Catsimpoolas
  • Patent number: 5049567
    Abstract: Substituted 4-aminoquinazoline derivatives which are inhibitors of gastric acid secretion. A compound of the invention is ethyl 8-methoxy-4-(4-methyl-3-thinenylamino)quinoline-3-carboxylate.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: September 17, 1991
    Assignee: SmithKline Beckman Intercredit B.V.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 5045321
    Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylaklyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt of magnesium and/or a basic inorganic salt of calcium, is physically stable.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: September 3, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-ichiro Hirai
  • Patent number: 5043329
    Abstract: Disclosed are compositions composed of unique mixtures of phospholipids and neutral lipids and methods of employing such compositions to treat the luminal lining of the gastrointestinal tract in the prevention or treatment of ulcerogenic processes such as peptic ulcer disease and inflammatory bowel disease. Compositions including mixtures of saturated or unsaturated phospholipids, together with saturated or unsaturated triglycerides and/or sterols, are shown to provide a surprising ulcer protective efficacy in experimental models. Further enhancement of activity is found upon the addition of a polyvalent cation or antioxidant to the various lipid mixtures.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: August 27, 1991
    Assignee: Board of Regents, University of Texas System
    Inventor: Lenard M. Lichtenberger
  • Patent number: 5039699
    Abstract: An anti-peptic ulcer agent comprising (a) a powdery material which includes tocopheryl retinoate, light silicic anhydride, and an antioxidant; (b) a low substituted hydroxypropylcellulose; and (c) polyvinylpyrrolidone which is orally administrable.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 13, 1991
    Assignee: Lederle (Japan), Ltd.
    Inventors: Masaaki Kurihara, Keiichiro Ohta
  • Patent number: 5026560
    Abstract: The spherical granules having a core coated with spraying powder containing a drug and low substituted hydroxypropylcellulose, because of their excellent hardness, can be coated further evenly, (e.g. sustained release coating, gastric coating, enteric coating), and at the time the granules are excellent in disintegration.
    Type: Grant
    Filed: January 14, 1988
    Date of Patent: June 25, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-ichiro Hirai
  • Patent number: 5021597
    Abstract: Novel acrylic acid salts of formula ##STR1## wherein R represents a hydrogen or a halogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group,M represents a cation derived from bismuth, zinc or a pharmaceutically acceptable organic base,X represents an inorganic anion,n is an integer of from 0 to 2,m is an integer of from 1 to 3,p is 0 or 1, andr is an integer of from 0 to 6having cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: June 4, 1991
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Tamas Fodor, Janos Fischer, Laszlo Dobay, Ferenc Trischler, Elemer Ezer, Judit Matuz, Katalin Saghy, Laszlo Szporny, Gyorgy Hajos
  • Patent number: 5013743
    Abstract: The compound represented by the formula; ##STR1## [wherein R.sup.1 stands for hydrogen, methoxy or trifluoromethyl; R.sup.2 and R.sup.3, being the same or different from each other, stand for hydrogen or methyl; R.sup.4 stands for optionally substituted hydrocarbon residue; and n denotes 0 or 1] or a salt thereof show excellent antibacterial activities, against the genus Campylobacter, especially against Campylobacter pylori, and they are used for preventing or treating infectious diseases caused by the said bacteria.
    Type: Grant
    Filed: February 12, 1990
    Date of Patent: May 7, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tomoyuki Iwahi, Hiroshi Satoh
  • Patent number: 5006509
    Abstract: A new indication for human growth hormone is described. Mixed with an ointment or other based the growth hormone causes an accelerated healing of ulcers. Described is further a method for the treatment of ulcers comprising applying an effective amount of the growth hormone in an ointment or other base as well as a preparation for use in the above method.
    Type: Grant
    Filed: June 24, 1988
    Date of Patent: April 9, 1991
    Inventor: Harald Waago
  • Patent number: 5004741
    Abstract: Methods of antagonizing gastrin and/or cholecystokinin (CCK) with benzodiazepine analogs are disclosed, as well as related pharmaceutical compositions, which are useful in treating disorders of the gastrointestinal tract, central nervous system, and of the appetite.
    Type: Grant
    Filed: November 9, 1988
    Date of Patent: April 2, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Mark G. Bock, Roger M. Freidinger
  • Patent number: 5001152
    Abstract: The invention is concerned with the new use of known catechol derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms; X is nitro, halogen or cyano and R.sub.3 is chlorine, nitro, cyano or a radical of the formula ##STR2## wherein R.sub.4 is hydrogen, cyano, alkyl having 1 to 4 carbon atoms or alkanoyl having 2 to 5 carbon atoms and R.sub.5 is cyano, alkanoyl having 2 to 5 carbon atoms, hydroxyalkyl having 1 to 4 carbon atoms, carboxyl or phenylcarbonyl unsubstituted or substituted with one to three methoxy groups or pharmaceutically acceptable salt thereof. The new use is the treatment and prophylaxis of ulcers and lesions in the gastrointestinal tract.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: March 19, 1991
    Assignee: Orion Corporation Ltd.
    Inventors: Paivi A. Aho, Pentti Pohto, Inge-Britt Y. Linden, Reijo J. Backstrom, Erkki J. Honkanen, Erkki A. O. Nissenen
  • Patent number: 4994457
    Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of a non-steroidal antiinflammatory agent such as piroxicam, or a pharmaceutically acceptable salt thereof, with 5'-guanylic acid or N-acetyl-L-methionine, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 19, 1987
    Date of Patent: February 19, 1991
    Assignee: Pfizer Inc.
    Inventors: Thomas C. Crawford, David L. Larson, Joseph G. Lombardino
  • Patent number: 4965269
    Abstract: The novel compounds of the formula I ##STR1## wherein Cl is in 5 or 6 position and whereby R is the group --CH.sub.2 OCOOR.sup.1, wherein R.sup.1 is a straight or branched alkyl containing 1-6 carbon atoms or benzyl,or R.sup.1 is the group --(CH.sub.2).sub.n ##STR2## --(CH.sub.2).sub.n COOH or --(CH.sub.2).sub.n SO.sub.3 H wherein n is 1-6 and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
    Type: Grant
    Filed: December 20, 1989
    Date of Patent: October 23, 1990
    Assignee: AB Hassle
    Inventors: Arne E. Brandstrom, Per L. Lindberg, Carl I. Starke, Gunnel E. Sunden
  • Patent number: 4957741
    Abstract: Lipid material or ganglioside from mammalian sources e.g. bovine and porcine brain or omentum is used to treat peptic ulcers.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: September 18, 1990
    Assignee: Angio-Medical Corp.
    Inventors: Ahmad R. Kamarei, Nicholas Catsimpoolas, Robert McCluer, Takashi Mise, Robert S. Sinn
  • Patent number: 4956350
    Abstract: Wound filling compositions containing: (a) chitosan, (b) at least one compatible hydrocolloid material other than chitosan, and (c) water, exhibit a variety of properties desirable for use in filling large wound such as dermal ulcers, yet do not exhibit syneresis. Preferably compositions exhibit antimicrobial activity, would healing capability, a viscosity suitable to allow them to be applied to and remain in an open wound, and are able to absorb wound exudate.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: September 11, 1990
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Deral T. Mosbey
  • Patent number: 4954512
    Abstract: An anti-peptic ulcer composition containing, as an active ingredient, a therapeutically effective amount of a compound having the formula (I): ##STR1## wherein A represents H.sub.2 NCH.sub.2 --, ##STR2## B represents ##STR3## D and E each independently represent H, R,--R'CO.sub.2 R,--R'(OH)CO.sub.2 R, ##STR4## wherein X represents H, CONR.sub.2, CONHR, CONH.sub.2, CO.sub.2 H, CO.sub.2 R, or COR or --R'(CO.sub.2 R)--; R' represents a lower alkylene group and R represents a lower alkyl group; F represents H, ##STR5## or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: November 23, 1988
    Date of Patent: September 4, 1990
    Assignees: Shosuke Okamoto, Showa Denko Kabushiki Kaisha
    Inventors: Katsunori Oguro, Hiroshi Nojima, Nobuyuki Hashizume, Norio Ohno, Taketoshi Naito
  • Patent number: 4950656
    Abstract: Disclosed are compositions composed of unique mixtures of phospholipids and neutral lipids and methods of employing such compositions to treat the luminal lining of the gastrointestinal tract in the prevention or treatment of ulcerogenic processes such as peptic ulcer disease and inflammatory bowel disease. Compositions including mixtures of saturated or unsaturated phospholipids, together with saturated or unsaturated triglycerides and/or sterols, are shown to provide a surprising ulcer protective efficacy in experimental models. Further enhancement of activity is found upon the addition of a polyvalent cation or antioxidant to the various lipid mixtures.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: August 21, 1990
    Assignee: Board of Regents, The University of Texas System
    Inventor: Lenard M. Lichtenberger
  • Patent number: 4940695
    Abstract: Pharmaceutical compositions suitable for oral administration comprising: (a) pharmaceutically-acceptable bismuth-containing agents such as bismuth subsalicylate; (b) pharmaceutically-acceptable non-ionic cellulose ether polymers such as methylcellulose; and (c) magnesium aluminum silicate. The ratio of bismuth to non-ionic cellulose ether polymer is greater than about 1.5:1. Compositions in the form of liquids containing water are preferred.This invention also relates to methods for treating or preventing disturbances of the gastrointestinal tract in humans or lower animals by orally administering a composition of the present invention.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: July 10, 1990
    Assignee: The Procter & Gamble Company
    Inventors: Leila D. Coveney, Linda C. Jones, Jerry R. Maney
  • Patent number: 4918063
    Abstract: Disclosed are compositions composed of unique mixtures of phospholipids and neutral lipids and methods of employing such compositions to treat the luminal lining of the gastrointestinal tract in the prevention or treatment of ulcerogenic processes such as peptic ulcer disease and inflammatory bowel disease. Compositions including mixtures of saturated or unsaturated phospholipids, together with saturated or unsaturated triglycerides and/or sterols, are shown to provide a surprising ulcer protective efficacy in experimental models. Further enhancement of activity is found upon the addition of a polyvalent cation or antioxidant to the various lipid mixtures.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: April 17, 1990
    Assignee: Board of Regents, The University of Texas System
    Inventor: Lenard M. Lichtenberger
  • Patent number: 4910204
    Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen; R.sup.2 is (C.sub.1 -C.sub.15) alkyl, (C.sub.3 -C.sub.15)alkenyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.20)-phenylalkyl, or substituted (C.sub.7 -C.sub.20)phenylalkyl wherein the substituents on the substituted phenyl and substituted phenylalkyl are independently one or two of fluoro, chloro, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3 alkoxy, and trifluoromethyl; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a pyrrolodinyl, substituted pyrrolidinyl, piperidyl or substituted piperidyl group, wherein the substituents on said substituted pyrrolidinyl and piperidyl groups are independently one of (C.sub.1 -C.sub.6)alkyl, phenyl, and (C.sub.7 -C.sub.9)phenylalkyl; and R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.9)phenylalkyl, or substituted (C.sub.7 -C.sub.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: March 20, 1990
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Walker, John L. LaMattina, Brian T. O'Neill
  • Patent number: 4891356
    Abstract: A method of treating gastrointgestinal ulcer disease is provided which involves administration of a proteinase inhibitor or analogue to patients suffering from same. Of particular interest is the use of inhibitors of serine, cysteine, carboxyl, and metallo proteinases.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: January 2, 1990
    Assignee: Brigham & Women's Hospital
    Inventor: Sandor Szabo
  • Patent number: 4873261
    Abstract: A method for treating ulcerative large intestinal diseases with a pharmcautical composition containing, as the active ingredient, a sesquiterpene compound or a salt thereof.
    Type: Grant
    Filed: February 10, 1988
    Date of Patent: October 10, 1989
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Wasei Miyazaki, Yasuhiko Inoue
  • Patent number: 4866039
    Abstract: Peptides comprising, in sequence, units selected from the amino acid residues 17 to 24 of VIP, and consisting at least of the amino acid residues 18 to 23, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid; having anti-ulcer activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: September 12, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Gordon Wootton, Eric A. Watts, Christine Summers
  • Patent number: 4851523
    Abstract: Compounds of the general formula (1) ##STR1## in which n is 1 or 2;m is 2-5 and X is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; or m is 1-4 and X is --CH.dbd.C.dbd.CH--;R.sup.1 is phenyl, substituted phenyl or naphthyl;Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl.These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: July 25, 1989
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Harry Finch
  • Patent number: 4847370
    Abstract: Compounds are described of formula ##STR1## wherein n is 1 or 2;m is 2-5 and X is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; or m is 1-4 and x is --CH.dbd.C.dbd.CH--;Z is --CH.sub.2 OH, --CHO or --CONHR.sup.1 [where R.sup.1 is a hydrogen atom or C.sub.1-4 alkyl, aryl, --COR.sup.2 (where R.sup.2 is a hydrogen atom or a C.sub.1-4 alkyl or aryl group) or --SO.sub.2 R.sup.3 (where R.sup.3 is a C.sub.1-4 alkyl or aryl group)];Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl.These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: July 11, 1989
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Harry Finch, Duncan B. Judd, James D. Meadows
  • Patent number: 4820690
    Abstract: Pharmaceutical compositions for oral administration comprise human urogastrone or a urogastrone fragment as active ingredient and such an active ingredient may be used for the manufacture of a medicament for promoting healing of a damaged alimentary tract.
    Type: Grant
    Filed: July 2, 1987
    Date of Patent: April 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Harold Gregory, Keith G. McCullagh
  • Patent number: 4806548
    Abstract: This invention relates to an improved anti-ulcer composition for prophylaxis and treatment of stomach and duodenum ulcers, including stress ulcers. The composition provides potent anti-ulcer activity with a dramatic reduction in toxicity and harmful side effects. The composition comprises a histamine H.sub.2 antagonist based on a guanidine derivative, preferably [N-cyano-H'-methyl-N"]-2(4-methyl-imidazolyl)-methylthio-[ethylguanidine]; and at least one 4-phenyl-tetrahydroisoquinoline antidepressant, preferably the [+] isomer of 4-phenyl-2-methyl-8-amino-1,2,3,4-tetrahydroisoquinoline hydrogen maleate. The composition may also contain a spasmolytic agent, preferably 2-metoxycarbonyl-4-(beta-piperidino ethyl) -metoxycarbonyl-4-(beta-peperidinoethyl) benzophenone. The ratio of antagonist to antidepressant ranges from 2:1 to 60:1, and the ratio of their sum to the spasmolytic agent, when used, ranges from 2.2:1 to 42.5:1.
    Type: Grant
    Filed: August 4, 1987
    Date of Patent: February 21, 1989
    Assignee: T P O Pharmachim
    Inventors: Nedyalka S. Ivanova, Tshavdar B. Ivanov, Margarita D. Dryanska, Orhideya B. Zabunova, Lilyana D. Dalleva, Milka P. Nikolova, Nikolina D. Berova, Rossitza S. Rakovska, Maria S. Stoyanova, Sascha R. Mihaylova, Milka A. Luna, Jossif N. Nissimou, Snejana G. Vitkova, Vladimir K. Matov, Boris K. Dimitrov, Grigor M. Metshkov
  • Patent number: 4801608
    Abstract: A new solid bismuth containing composition which is colloidally soluble in water is obtained by spray drying an aqueous ammoniacal colloidal solution of bismuth citrate. The new composition is effective for the treatment of peptic ulcers.
    Type: Grant
    Filed: December 6, 1983
    Date of Patent: January 31, 1989
    Assignee: Gist-Brocades N. V.
    Inventors: Petrus J. H. Bos, Dirk J. C. Engel, Hayo de Jonge
  • Patent number: 4753942
    Abstract: A method of treating arthritis and rheumatism in human patients comprises the topical application to an affected part of the patient's body of at least one zwitterionic aminosulfonic acid of the kind commonly known as Good buffers. The acid is preferably made up as a pharmaceutical composition such as a cream, and applied at a dosage of 50 .mu.g - 50 mg of the acid per day for at least 5 days, but usually several weeks.
    Type: Grant
    Filed: December 16, 1986
    Date of Patent: June 28, 1988
    Inventor: Donncha O'Sullivan
  • Patent number: 4749572
    Abstract: A pharmaceutical preparation for the treatment of, e.g. ulcers, burns and skin diseases contains, as essential ingredients, from 5 to 25% by weight of Peru Balsam and from 0.01 to 0.20% by weight of silver nitrate. The preparation may be administered enterally or topically.
    Type: Grant
    Filed: August 21, 1985
    Date of Patent: June 7, 1988
    Assignee: Pharmaceutical Holdings Limited
    Inventor: Mahmoud Ahari
  • Patent number: 4749683
    Abstract: Secretion of gastric acid in the stomach of mammals is inhibited by parenteral administration of alpha-transforming growth factor.
    Type: Grant
    Filed: October 3, 1986
    Date of Patent: June 7, 1988
    Assignee: President and Fellows of Harvard College
    Inventors: Richard A. Murphy, James A. Rhodes
  • Patent number: 4748157
    Abstract: Fab or Fc fragment of human IgG which is obtainable by enzymatic digestion of the human IgG is reduced by a reducing agent to sever an interchain of disulfide bonds therein and then blocked the SH radicals formed with alkyl group which may contain other group. The resulting alkylated Fab and Fc fragments display therapeutic and prophylactic action for gastrointestinal ulcers by the oral or parenteral administration.
    Type: Grant
    Filed: February 4, 1986
    Date of Patent: May 31, 1988
    Assignee: The Green Cross Corporation
    Inventors: Masakazu Iwai, Kazumasa Yokoyama, Tsunekazu Fukushima
  • Patent number: 4732760
    Abstract: A curative and preventive agent for ulcers of digestive organs comprising as the main constituent an active component having anti-ulcer activity derived from a hot-water, an alcohol or a water-alcohol mixed solution extract of cassia buds.
    Type: Grant
    Filed: June 20, 1986
    Date of Patent: March 22, 1988
    Assignee: The Green Cross Corporation
    Inventors: Yoshiro Iga, Kanemichi Okano, Toshiaki Akira
  • Patent number: 4719111
    Abstract: A composition for treatment of decubitus ulcers comprising an admixture of from about 10 to about 50 parts lecithin, from about 10 to about 50 parts goldenseal root or rhizome, and from about 10 to about 50 parts myrrh gum.
    Type: Grant
    Filed: June 14, 1985
    Date of Patent: January 12, 1988
    Inventor: Lynn M. Wilson
  • Patent number: 4689229
    Abstract: Gastrointestinal compositions containing from 99 to 70 percent by weight of plantago and from 1 to 30 percent by weight of pectin, useful for inhibiting the occurrence of gastroduodenal ulcers and for preventing their recurrence, for reducing the incidence and severity of undesirable side effects caused by anti-ulcer drugs, and for alleviating discomfort occasioned by gastroesophageal reflux. Methods for their preparation and use are also disclosed.
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: August 25, 1987
    Inventor: Upendra Banik
  • Patent number: 4684632
    Abstract: Pharmaceutical formulations for the treatment of gastrointestinal disorders, which contain as the active component an effective gastrointestinal disorder alleviating amount of a 1,2-diacylglycero-3-phosphocholine in which 75-86% by weight of the acyl radicals are unsaturated fatty acid radicals having a chain length of 16, 18 or 20 carbon atoms. The mixtures of fatty acid radicals in the acyl groups in the 1- and 2-positions preferably have different compositions. The formulations can also contain other active compounds, in particular those which display injurious gastrointestinal side effects.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: August 4, 1987
    Assignee: A. Nattermann & CIE. GmbH
    Inventors: Volker Schulz, Sigurd Leyck, Manfred Durr, Miklos Ghyczy, Armin Wendel, Jorg Hager
  • Patent number: 4631292
    Abstract: A series of new 1,3-dioxane derivatives are disclosed. These compounds have an outstanding anti-peptic ulcerative activity and are useful as novel anti-peptic ulcer agents. Such compounds are synthesized by reacting a 1,3-butanediol derivative with suitable ketone.
    Type: Grant
    Filed: July 31, 1984
    Date of Patent: December 23, 1986
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama
  • Patent number: 4577022
    Abstract: The invention provides new silyl derivatives of 5,6,7,8-tetrahydroquinolines and related compounds. The tetrahydroquinolines are substiuted at the 8-position by the group SiR.sub.3 where R may be one of various hydrocarbon groups or an electron donating substituent. The 8-position may also carry a lithium, sodium or potassium atom. The new silyl derivatives may be prepared by treating a corresponding 8-lithio, sodio or potassio tetrahydroquinoline with a silyl halide R.sub.3 SiHal followed by a metal compound R*M where M is sodium, potassium or lithium and R* is alkyl, cycloalkyl, aralkyl or aryl or an amine residue. The new silyl derivatives are useful intermediates for the preparation of known 5,6,7,8-tetrahydroquinline-8-nitriles, amides and thioamides employing an alkyl silyl isothiocyanate or cyanate. The nitriles and thioamides are anti-ulcer agents. The related compounds may be made by analogous methods.
    Type: Grant
    Filed: June 21, 1983
    Date of Patent: March 18, 1986
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Roger Crossley, Robin G. Shepherd
  • Patent number: 4557754
    Abstract: A novel compound bis-(N,N-dimethyl-N-carbodecyloxymethyl-N-ethyleneammonium)-sulphide dichloride of the formula ##STR1## A method for preparing said novel compound comprising quaternization of bis-(.beta.-dimethylaminoethyl)-sulphide with monochloroacetic acid decyl ester, molar ratio of said reagents being not more than 1:2.A chemotherapeutic antimicrobial preparation comprising said novel compound as an active principle in combination with a pharmaceutical carrier.A plant growth regulator in the form of an aqueous solution of said novel compound in a concentration of from 0.0001 to 0.1 wt. %.
    Type: Grant
    Filed: August 13, 1980
    Date of Patent: December 10, 1985
    Assignee: Institut Organicheskoi Khimii
    Inventors: Georgy A. Golik, Yaroslav P. Demchenko, Miron O. Lozinsky, Vladlen V. Malovik, Valery Y. Semeny
  • Patent number: 4548944
    Abstract: Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms;tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
    Type: Grant
    Filed: February 10, 1983
    Date of Patent: October 22, 1985
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Piero del Soldato, Antonio Giachetti, Rosamaria Micheletti