Peptic Patents (Class 514/927)
  • 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: 5091422
    Abstract: Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8;n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at B.sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.
    Type: Grant
    Filed: June 21, 1990
    Date of Patent: February 25, 1992
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor
  • 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: 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: 5053498
    Abstract: A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or .dbd.O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.5 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;X represents group (A);.dbd.C.dbd.CH--COR.sub.8 (A)or group (B): ##STR2## wherein R.sub.8 represents alkyl, and R.sub.9 and R.sub.10 each represents hydrogen or an organic residue; with the proviso that when X represents group (A), then R.sub.1 and R.sub.3 both represent hydrogen, R.sub.2 represents --OR.sub.5, R.sub.4 represents OR.sub.7 and the bond between the carbon atom to which X is attached and the carbon atom to which R.sub.4 is attached is a single bond, and when X represents group (B), then R.sub.1 represents .dbd.O, R.sub.2 represents hydrogen, R.sub.3 represents --OR.sub.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: October 1, 1991
    Assignee: Green Cross Corporation
    Inventors: Yusei Shiraga, Chikara Fukaya, Toshiaki Akira, Masakazu Iwai, Kazumasa Yokoyama, Mamoru Tabata, Hiroshi Fukui, Shigeo Tanaka, Yoshiro Iga, Tadakazu Suyama, Kanemichi Okano
  • 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: 5043358
    Abstract: A pharmaceutical composition and process for administering non-steroidal anti-inflammatory drugs which are protected against injury to gastrointestinal tract by beta adrenergic agonists.
    Type: Grant
    Filed: September 4, 1990
    Date of Patent: August 27, 1991
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alison B. Lukacsko, Randy J. Koslo
  • Patent number: 5041442
    Abstract: This invention is directed to compounds of formula (I): ##STR1## wherein R.sup.1 is thiocyano, --CH.sub.2 CN, --NH.sub.2, --NHR.sup.5, or --CH.sub.2 OR.sup.5 where R.sup.5 is lower alkyl;R.sup.2 is hydrogen, halo, lower alkyl, or lower alkylthio;R.sup.3 is hydrogen, halo, lower alkyl, lower alkylthio, or thiocyano;R.sup.4 is hydrogen, halo, lower alkyl, lower alkoxy, lower alkylthio, or lower alkylsulfonyl; andY is --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.dbd.CH--, or --(CH.sub.2).sub.n -- where n is 0, 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof. These compounds are useful in treating mammals having disease-states characterized by excessive gastric acid secretion.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: August 20, 1991
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Ruth S. Romero, Fidencio Franco, Armando C. Castaneda, Joseph M. Muchowski
  • 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: 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: 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: 4985423
    Abstract: The invention relates to a group of new 1,4-diazepine derivatives of the formula ##STR1## wherein A represents a group of the formulae 2-10 ##STR2## These compounds have a strong anti-ulcer activity after oral administration.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: January 15, 1991
    Assignee: Duphar International Research B.V.
    Inventors: Jacobus A. J. den Hartog, Herman H. van Stuivenberg, Ineke van Wijngaarden
  • Patent number: 4983723
    Abstract: A cycloalkane derivative represented by the formula (I): ##STR1## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, Z, and n are as defined in the specification. The compounds of formula (I) exhibit activities against peptic ulcers and are useful as therapeutic and prophylactic agents for peptic ulcers.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: January 8, 1991
    Assignee: Green Cross Corporation
    Inventors: Hitoshi Yasuda, Chikara Fukaya, Kanemichi Okano, Kazumasa Yokoyama
  • Patent number: 4983584
    Abstract: A therapeutic and prophylactic agent for peptic ulcers comprising as an effective ingredient a cyclohexane derivative represented by general formula (I): ##STR1## wherein A represents a group shown by formula, >CH.sub.2, ##STR2## wherein X represents ethynylene, vinylene or ethylene, Y represents oxo or a hydroxy group; R.sup.1, R.sup.3, R.sup.4 and R.sup.5 each represents a hydrogen atom or alkyl; R.sup.2 represents a hydrogen atom, alkyl or a group shown by --OR.sup.8 ;R.sup.6 represents a hydrogen atom, oxo or a group shown by --OR.sup.8 ; and R.sup.7 represents a hydrogen atom or a group shown by --OR.sup.8, wherein R.sup.8 represents a hydrogen atom or an organic residue.
    Type: Grant
    Filed: November 23, 1987
    Date of Patent: January 8, 1991
    Assignee: Green Cross Corporation
    Inventors: Chikara Fukaya, Hitoshi Yasuda, Toshiaki Akira, Masakazu Iwai, Kanemichi Okano, Kazumasa Yokoyama
  • Patent number: 4978536
    Abstract: Disclosed is use of a synthetic aluminum silicate as antacid and anti-ulcer preparation, anti-obesity preparation and acne curing preparation. This aluminum silicate is obtained by reacting an aluminum compound and silicic acid or water glass at a weight ratio Al.sub.2 O.sub.3 : SiO.sub.2 of 4.5:1.0-6.0:1.0 in a strongly acidic aqueous solution having an initial pH of 1.0-3.0, then adding thereto a basic substance to reach excess in alkali and then neutralizing the reaction mixture to pH 5.0-7.0 with an acid.
    Type: Grant
    Filed: May 17, 1988
    Date of Patent: December 18, 1990
    Assignee: Yakurigaku Chuo Kenkyusho
    Inventor: Hidehiko Takahashi
  • Patent number: 4959369
    Abstract: The present invention relates to a combination for use in improving the condition of skin and mucosa which combination comprises an S-methyl substituted ternary sulphonium derivative of methionine and cysteine. The present invention also extends to methods of treatment and prophylaxis of stress, gastric and peptic ulcers and deterioration of skin.
    Type: Grant
    Filed: February 1, 1988
    Date of Patent: September 25, 1990
    Inventor: Aws S. M. Salim
  • Patent number: 4959384
    Abstract: The invention involves methods for the treatment and prophylaxis of human or animal subjects having infectious gastrointestinal disorders of the upper gastrointestinal tract caused or mediated by Campylobacter-like organisms comprising the step of administering to the subjects safe and effective amounts of nitrofurantoin.
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: September 25, 1990
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: William G. Kraft, Donna R. Morgan
  • 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: 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: 4925870
    Abstract: There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.
    Type: Grant
    Filed: May 25, 1989
    Date of Patent: May 15, 1990
    Assignees: Inverni Della Beffa SpA, Societe de Recherches Industrielles Sori
    Inventors: Bruno Gabetta, Maria J. Magistretti, Philippe Dostert
  • Patent number: 4891384
    Abstract: The use of valepotriate hydrins in the prevention and treatment of disorders of the gastrointestinal tract is described, together with pharmaceutical compositions containing valepotriate hydrins and certain novel valepotriate hydrins per se.
    Type: Grant
    Filed: May 3, 1988
    Date of Patent: January 2, 1990
    Assignee: Kali-Chemic Pharma GmbH
    Inventors: Peter W. Thies, Samuel David, Insa Hell, Klau U. Wolf
  • 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: 4888417
    Abstract: A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or =O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.6 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;X represents group (A):.dbd.C.dbd.CH--COR.sub.8 (A)or group (B): ##STR2## wherein R.sub.8 represents alkyl, and R.sub.9 and R.sub.10 each represents hydrogen or an organic residue; with the proviso that when X represents group (A), then R.sub.1 and R.sub.3 both represent hydrogen, R.sub.2 represents --OR.sub.5 ; R.sub.4 represents OR.sub.7 and the bond between the carbon atoms to which X is attached and the carbon atom to which R.sub.4 is attached is a single bond, and when X represents group (B), then R.sub.1 represents .dbd.O, R.sub.2 represents hydrogen, R.sub.3 represents --OR.sub.
    Type: Grant
    Filed: May 27, 1986
    Date of Patent: December 19, 1989
    Assignee: Green Cross Corporation
    Inventors: Yusei Shiraga, Chikara Fukaya, Toshiaki Akira, Masakazu Iwai, Kazumasa Yokoyama, Mamoru Tabata, Hiroshi Fukui, Shigeo Tanaka, Yoshiro Iga, Tadakazu Suyama, Kanemichi Okano
  • Patent number: 4888329
    Abstract: A composition comprising a compound of the following formula or a salt thereof ##STR1## wherein R.sub.1 and R.sub.2 each represent a hydrogen atom or a methyl group. The composition is highly safe and useful as an antiulcer agent.
    Type: Grant
    Filed: April 27, 1988
    Date of Patent: December 19, 1989
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Ogawa, Takahiro Sakaue
  • Patent number: 4863956
    Abstract: There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: September 5, 1989
    Assignees: Inverni Della Beffa SpA, Societe de Recherches Industrielles Sori
    Inventors: Bruno Gabetta, Maria J. Magistretti, Philippe Dostert
  • Patent number: 4859709
    Abstract: A pharmaceutical composition comprising a freely flowable powder, the powder comprising a porous, high absorption silica or silicate having absorbed therein at least 10% by volume of a liquid, pharmaceutically active composition, based on the weight of powder plus liquid, provided that when the liquid pharmaceutically active composition is a corticoid solution the silica or silicate has a mean particle size of at least 10 .mu.m in diameter.
    Type: Grant
    Filed: October 26, 1987
    Date of Patent: August 22, 1989
    Assignee: Beecham Group plc
    Inventor: David A. Rawlins
  • Patent number: 4849404
    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 groups. The resulting alkylated Fab and Fc fragments display therapeutic and prophylactic action for gastrointestinal ulcers by the oral or parenteral administration.
    Type: Grant
    Filed: March 3, 1988
    Date of Patent: July 18, 1989
    Assignee: The Green Cross Corporation
    Inventors: Masakazu Iwai, Kazumasa Yokoyama, Tsunekazu Fukushima
  • Patent number: 4839385
    Abstract: Compounds derived form the marine sponge Laffariella variabilis and known by the name manoalide, and its derivatives, modify calcium homeostasis.
    Type: Grant
    Filed: August 25, 1987
    Date of Patent: June 13, 1989
    Assignees: The Regents of the University of California, Allergan, Inc.
    Inventors: Shmuel Maullem, George Sachs, Larry Wheeler
  • Patent number: 4833157
    Abstract: A therapeutic method for inhibiting gastric secretion in an individual for whom such therapy is indicated is disclosed. The method comprises administering to such an individual an effective inhibitory amount of certain derivatives of 15-deoxy-16-hydroxy-prostaglandin E.sub.1 esters.
    Type: Grant
    Filed: January 4, 1988
    Date of Patent: May 23, 1989
    Assignee: Miles Inc.
    Inventors: Harold C. Kluender, Warren D. Woessner, William G. Biddlecom
  • Patent number: 4831040
    Abstract: Disclosed is a method for prophylactic and therapeutic treatment of peptic ulcers which comprises the administration of a pharmaceutical composition containing a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereon, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminolakyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formuloximino, tetrazolyl, carbalkoxyalky or caboxyalkyl, andm is 0 or 1,in admixture or in association with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 1, 1988
    Date of Patent: May 16, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Dennis L. Decktor, Leo R. Fitzpatrick, Henry F. Campbell
  • Patent number: 4814348
    Abstract: The present invention relates to therapeutic compositions for the treatment of gastric disorders, said compositions containing a compound of the formula ##STR1## in which R is a mono- or poly-cyclic heterocyclic radical, possibly substituted, containing an oxygen atom, R' is a hydrogen atom or a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 18 carbon atoms, and,either A represents a hydrogen atom and B represents a hydroxyl radicalor A and B together form a carbon-carbon double bond, as well as the pharmaceutically acceptable alkaline, alkaline-earth or amine salts thereof.
    Type: Grant
    Filed: May 22, 1987
    Date of Patent: March 21, 1989
    Assignee: Roussel Uclaf
    Inventors: Mario Bianchi, Fernando Barzaghi
  • Patent number: 4760075
    Abstract: N-alkyl-N'-(2-aminomethyl-4-thiazolylmethylthio)alkyl guanidines, thioureas, ethenediamines and related compounds, H.sub.2 -receptor antagonists, useful in inhibiting gastric acid secretion in mammals.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: July 26, 1988
    Assignee: Eli Lilly and Company
    Inventor: Richard P. Pioch
  • 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: 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: 4728658
    Abstract: Pyridine derivatives having the formula I ##STR1## and their pharmaceutically acceptable salts (where n is 0 or 1; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is an aromatic group) exhibit anti-secretory activity and may be used as anti-secretory agents and/or as anti-ulcer agents.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: March 1, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Ian A. Cliffe
  • Patent number: 4707495
    Abstract: A method of treating peptic ulcer disease by topical application of a prostaglandin analog is described.
    Type: Grant
    Filed: October 28, 1985
    Date of Patent: November 17, 1987
    Assignee: Ortho Pharmaceutical
    Inventors: Marvin E. Rosenthale, David A. Shriver, Laurence B. Katz
  • Patent number: 4694019
    Abstract: The present invention relates to therapeutic compositions for the treatment of gastric disorders, said compositions containing a compound of the formula ##STR1## in which R is a mono- or poly-cyclic heterocyclic radical, possibly substituted, containing an oxygen atom, R' is a hydrogen atom or a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 18 carbon atoms, and,either A represents a hydrogen atom and B represents a hydroxyl radicalor A and B together form a carbon-carbon double bond, as well as the pharmaceutically acceptable alkaline, alkaline-earth or amine salts thereof.
    Type: Grant
    Filed: August 14, 1985
    Date of Patent: September 15, 1987
    Assignee: Roussel UCLAF
    Inventors: Mario Bianchi, deceased, Fernando Barzaghi
  • 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: 4681895
    Abstract: Novel N-phenyl-trans-4-guanidinomethylcyclohexanecarboxamide compounds of the formula: ##STR1## wherein R is hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which have excellent anti-ulcer activities and hence are useful as an anti-ulcer drug, and a pharmaceutical composition useful for the treatment and prophylaxis of peptic ulcers which comprises as an active ingredient the compound as set forth above in admixture with a conventional pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: March 6, 1986
    Date of Patent: July 21, 1987
    Assignee: Kanebo, Ltd.
    Inventors: Toshio Satoh, Goro Tsukamoto
  • Patent number: 4677107
    Abstract: Use of a compound of the formula: ##STR1## wherein R is hydrogen atom or ethyl group, or a pharmaceutically acceptable salt thereof for prophylaxis and/or treatment of peptic ulcer, and a method for prophylaxis and/or treatment of peptic ulcer disease which comprises administering an effective amount of the above-mentioned compound to warm blooded aninal, especially human. Said active compounds have excellent pharmacological activities such as inhibition of ulceration and inhibition of gastric secretion, and hence, are useful as an anti-peptic ulcer agent.
    Type: Grant
    Filed: October 4, 1985
    Date of Patent: June 30, 1987
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Toshiaki Kadokawa, Katsuyoshi Kawashima, Hitoshi Uno, Katsuhiko Hino
  • Patent number: 4673677
    Abstract: A method for the treatment of gastrointestinal disorders in a patient which comprises administering to the patient a gastric anti-secretory effective amount of a 2-amino-5-hydroxy-4-methylpyrimidine or a substituted amino derivative thereof, optionally in admixture with an additional gastric anti-secretory agent.
    Type: Grant
    Filed: August 9, 1985
    Date of Patent: June 16, 1987
    Assignee: Pfizer Inc.
    Inventor: John L. LaMattina
  • Patent number: 4666912
    Abstract: The invention relates to a process for the restoration and prevention of gastrointestinal injuries, which comprises treating a patient with an effective dose of racemic or optically active 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrimido[1,2-a]pyrimidine-3-c arboxamide.
    Type: Grant
    Filed: March 22, 1985
    Date of Patent: May 19, 1987
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termeker Gyara RT
    Inventors: Zoltan Meszaros, Jozse Knoll, Istvan Hurmecz, Peter Szentmiklosi, Agnes Horvath, Lelle Vasvari nee Debreczy, Gabor Kovacs, Klara Gyires, Sandor Virag
  • Patent number: 4642314
    Abstract: An antiulcer composition, containing, as active ingredient, an antiulcer effective amount of an isoprene derivative as herein defined, is described.
    Type: Grant
    Filed: November 14, 1984
    Date of Patent: February 10, 1987
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Yoshiyuki Tahara, Michiko Nagai, Katsura Kogure, Shigeo Kawase, Teruhito Yamaguchi
  • Patent number: 4600780
    Abstract: New N-cyano-formamidine are disclosed of the formula I: ##STR1## wherein R is 2-[[(5-methyl-1H-Imidazol-4-yl)methyl]thio]ethyl, 2-[[[5-[dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl, 2-[[[2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl or 3-[3-(1-piperidinylmethyl)phenoxy]propyl, as well as a process for its production, and pharmaceutical preparations containing the same. The compounds possess histamine--induced gastric acid secretion--inhibiting activity, and are indicated for use in the treatment of peptic ulcer and other pathologies caused or stimulated by gastric acidity.
    Type: Grant
    Filed: March 20, 1984
    Date of Patent: July 15, 1986
    Assignee: Ferrer International, S.A.
    Inventors: Rafael Foguet, Luis Anglada, Manuel M. Raga, Jose A. Ortiz, Aurelio Sacristan, Jose M. Castello
  • 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: 4510149
    Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond; Z completes a single bond or is a --CH.sub.2 -- group; each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5- tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')-COR and --X-C(R') (R")-COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: July 1, 1983
    Date of Patent: April 9, 1985
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Paolo Cozzi, Germano Carganico, Antonio Pillan, Umberto Branzoli
  • Patent number: 4507321
    Abstract: Disclosed herein are compositions containing aliphatic di- and polyamine, or agmatine which are useful to regulate, i.e., stimulate or inhibit, epithelial cell growth. The compositions containing low concentrations of these compounds, by virtue of their epithelial cell growth stimulating activity, are useful in promoting wound healing, treating burns, treating ischemic, debubitus and peptic ulcers, plastic and reconstructive surgery, dermatological disorders, promoting autograft and homograft growth, stimulating organ and tissue regeneration in vitro and in vivo, as a component in defined (serum protein-free) media for cultured cells.Compositions containing these compounds in higher concentrations are useful in the inhibition of cell growth and are useful in the treatment of psoriasis and in retardation of fibrosis after injuries to the spinal cord and nervous system. Also disclosed are various methodologies for utilizing such compositions.
    Type: Grant
    Filed: February 17, 1982
    Date of Patent: March 26, 1985
    Assignee: The Research Foundation of State University of New York
    Inventor: Ilene H. Raisfeld