Peptic Patents (Class 514/927)
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Patent number: 5109023Abstract: 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: GrantFiled: December 5, 1990Date of Patent: April 28, 1992Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5091422Abstract: 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: GrantFiled: June 21, 1990Date of Patent: February 25, 1992Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor
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Patent number: 5089639Abstract: 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: GrantFiled: January 24, 1991Date of Patent: February 18, 1992Assignee: 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
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Patent number: 5066496Abstract: Ganglioside mixtures and/or lipid mixtures e.g. from brain and omentum, are found to be effective to treat peptic ulcers.Type: GrantFiled: August 3, 1988Date of Patent: November 19, 1991Assignees: Angio-Medical Corporation, Trustees of Boston UniversityInventors: Sandor Szabo, Meryl S. A. Rubin, Michael Klibaner, Ahmad R. Kamarei, Robert S. Sinn, Nicholas Catsimpoolas
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Patent number: 5053498Abstract: 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: GrantFiled: October 16, 1989Date of Patent: October 1, 1991Assignee: Green Cross CorporationInventors: Yusei Shiraga, Chikara Fukaya, Toshiaki Akira, Masakazu Iwai, Kazumasa Yokoyama, Mamoru Tabata, Hiroshi Fukui, Shigeo Tanaka, Yoshiro Iga, Tadakazu Suyama, Kanemichi Okano
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Patent number: 5045321Abstract: 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: GrantFiled: February 13, 1987Date of Patent: September 3, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadashi Makino, Tetsuro Tabata, Shin-ichiro Hirai
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Patent number: 5043358Abstract: 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: GrantFiled: September 4, 1990Date of Patent: August 27, 1991Assignee: Bristol-Myers Squibb CompanyInventors: Alison B. Lukacsko, Randy J. Koslo
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Patent number: 5041442Abstract: 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: GrantFiled: July 31, 1990Date of Patent: August 20, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Ruth S. Romero, Fidencio Franco, Armando C. Castaneda, Joseph M. Muchowski
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Patent number: 5039699Abstract: 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: GrantFiled: March 27, 1989Date of Patent: August 13, 1991Assignee: Lederle (Japan), Ltd.Inventors: Masaaki Kurihara, Keiichiro Ohta
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Patent number: 5021597Abstract: 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: GrantFiled: July 11, 1990Date of Patent: June 4, 1991Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Tamas Fodor, Janos Fischer, Laszlo Dobay, Ferenc Trischler, Elemer Ezer, Judit Matuz, Katalin Saghy, Laszlo Szporny, Gyorgy Hajos
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Patent number: 5004741Abstract: 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: GrantFiled: November 9, 1988Date of Patent: April 2, 1991Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Mark G. Bock, Roger M. Freidinger
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Patent number: 5001152Abstract: 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: GrantFiled: December 23, 1988Date of Patent: March 19, 1991Assignee: Orion Corporation Ltd.Inventors: Paivi A. Aho, Pentti Pohto, Inge-Britt Y. Linden, Reijo J. Backstrom, Erkki J. Honkanen, Erkki A. O. Nissenen
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Patent number: 4994457Abstract: 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: GrantFiled: May 19, 1987Date of Patent: February 19, 1991Assignee: Pfizer Inc.Inventors: Thomas C. Crawford, David L. Larson, Joseph G. Lombardino
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Patent number: 4985423Abstract: 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: GrantFiled: July 3, 1989Date of Patent: January 15, 1991Assignee: Duphar International Research B.V.Inventors: Jacobus A. J. den Hartog, Herman H. van Stuivenberg, Ineke van Wijngaarden
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Patent number: 4983723Abstract: 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: GrantFiled: December 7, 1987Date of Patent: January 8, 1991Assignee: Green Cross CorporationInventors: Hitoshi Yasuda, Chikara Fukaya, Kanemichi Okano, Kazumasa Yokoyama
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Patent number: 4983584Abstract: 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: GrantFiled: November 23, 1987Date of Patent: January 8, 1991Assignee: Green Cross CorporationInventors: Chikara Fukaya, Hitoshi Yasuda, Toshiaki Akira, Masakazu Iwai, Kanemichi Okano, Kazumasa Yokoyama
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Patent number: 4978536Abstract: 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: GrantFiled: May 17, 1988Date of Patent: December 18, 1990Assignee: Yakurigaku Chuo KenkyushoInventor: Hidehiko Takahashi
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Patent number: 4959369Abstract: 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: GrantFiled: February 1, 1988Date of Patent: September 25, 1990Inventor: Aws S. M. Salim
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Patent number: 4959384Abstract: 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: GrantFiled: October 24, 1985Date of Patent: September 25, 1990Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: William G. Kraft, Donna R. Morgan
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Patent number: 4957741Abstract: Lipid material or ganglioside from mammalian sources e.g. bovine and porcine brain or omentum is used to treat peptic ulcers.Type: GrantFiled: August 2, 1988Date of Patent: September 18, 1990Assignee: Angio-Medical Corp.Inventors: Ahmad R. Kamarei, Nicholas Catsimpoolas, Robert McCluer, Takashi Mise, Robert S. Sinn
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Patent number: 4954512Abstract: 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: GrantFiled: November 23, 1988Date of Patent: September 4, 1990Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Katsunori Oguro, Hiroshi Nojima, Nobuyuki Hashizume, Norio Ohno, Taketoshi Naito
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Patent number: 4950656Abstract: 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: GrantFiled: November 2, 1988Date of Patent: August 21, 1990Assignee: Board of Regents, The University of Texas SystemInventor: Lenard M. Lichtenberger
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Patent number: 4925870Abstract: 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: GrantFiled: May 25, 1989Date of Patent: May 15, 1990Assignees: Inverni Della Beffa SpA, Societe de Recherches Industrielles SoriInventors: Bruno Gabetta, Maria J. Magistretti, Philippe Dostert
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Patent number: 4891384Abstract: 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: GrantFiled: May 3, 1988Date of Patent: January 2, 1990Assignee: Kali-Chemic Pharma GmbHInventors: Peter W. Thies, Samuel David, Insa Hell, Klau U. Wolf
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Patent number: 4891356Abstract: 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: GrantFiled: July 15, 1987Date of Patent: January 2, 1990Assignee: Brigham & Women's HospitalInventor: Sandor Szabo
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Patent number: 4888417Abstract: 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: GrantFiled: May 27, 1986Date of Patent: December 19, 1989Assignee: Green Cross CorporationInventors: Yusei Shiraga, Chikara Fukaya, Toshiaki Akira, Masakazu Iwai, Kazumasa Yokoyama, Mamoru Tabata, Hiroshi Fukui, Shigeo Tanaka, Yoshiro Iga, Tadakazu Suyama, Kanemichi Okano
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Patent number: 4888329Abstract: 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: GrantFiled: April 27, 1988Date of Patent: December 19, 1989Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Ogawa, Takahiro Sakaue
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Patent number: 4863956Abstract: 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: GrantFiled: July 18, 1986Date of Patent: September 5, 1989Assignees: Inverni Della Beffa SpA, Societe de Recherches Industrielles SoriInventors: Bruno Gabetta, Maria J. Magistretti, Philippe Dostert
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Patent number: 4859709Abstract: 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: GrantFiled: October 26, 1987Date of Patent: August 22, 1989Assignee: Beecham Group plcInventor: David A. Rawlins
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Patent number: 4849404Abstract: 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: GrantFiled: March 3, 1988Date of Patent: July 18, 1989Assignee: The Green Cross CorporationInventors: Masakazu Iwai, Kazumasa Yokoyama, Tsunekazu Fukushima
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Patent number: 4839385Abstract: Compounds derived form the marine sponge Laffariella variabilis and known by the name manoalide, and its derivatives, modify calcium homeostasis.Type: GrantFiled: August 25, 1987Date of Patent: June 13, 1989Assignees: The Regents of the University of California, Allergan, Inc.Inventors: Shmuel Maullem, George Sachs, Larry Wheeler
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Patent number: 4833157Abstract: 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: GrantFiled: January 4, 1988Date of Patent: May 23, 1989Assignee: Miles Inc.Inventors: Harold C. Kluender, Warren D. Woessner, William G. Biddlecom
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Patent number: 4831040Abstract: 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: GrantFiled: February 1, 1988Date of Patent: May 16, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Dennis L. Decktor, Leo R. Fitzpatrick, Henry F. Campbell
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Patent number: 4814348Abstract: 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: GrantFiled: May 22, 1987Date of Patent: March 21, 1989Assignee: Roussel UclafInventors: Mario Bianchi, Fernando Barzaghi
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Patent number: 4760075Abstract: 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: GrantFiled: December 23, 1985Date of Patent: July 26, 1988Assignee: Eli Lilly and CompanyInventor: Richard P. Pioch
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Patent number: 4749572Abstract: 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: GrantFiled: August 21, 1985Date of Patent: June 7, 1988Assignee: Pharmaceutical Holdings LimitedInventor: Mahmoud Ahari
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Patent number: 4748157Abstract: 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: GrantFiled: February 4, 1986Date of Patent: May 31, 1988Assignee: The Green Cross CorporationInventors: Masakazu Iwai, Kazumasa Yokoyama, Tsunekazu Fukushima
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Patent number: 4728658Abstract: 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: GrantFiled: September 3, 1985Date of Patent: March 1, 1988Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Ian A. Cliffe
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Patent number: 4707495Abstract: A method of treating peptic ulcer disease by topical application of a prostaglandin analog is described.Type: GrantFiled: October 28, 1985Date of Patent: November 17, 1987Assignee: Ortho PharmaceuticalInventors: Marvin E. Rosenthale, David A. Shriver, Laurence B. Katz
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Patent number: 4694019Abstract: 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: GrantFiled: August 14, 1985Date of Patent: September 15, 1987Assignee: Roussel UCLAFInventors: Mario Bianchi, deceased, Fernando Barzaghi
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Patent number: 4684632Abstract: 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: GrantFiled: December 21, 1984Date of Patent: August 4, 1987Assignee: A. Nattermann & CIE. GmbHInventors: Volker Schulz, Sigurd Leyck, Manfred Durr, Miklos Ghyczy, Armin Wendel, Jorg Hager
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Patent number: 4681895Abstract: 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: GrantFiled: March 6, 1986Date of Patent: July 21, 1987Assignee: Kanebo, Ltd.Inventors: Toshio Satoh, Goro Tsukamoto
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Patent number: 4677107Abstract: 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: GrantFiled: October 4, 1985Date of Patent: June 30, 1987Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Toshiaki Kadokawa, Katsuyoshi Kawashima, Hitoshi Uno, Katsuhiko Hino
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Patent number: 4673677Abstract: 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: GrantFiled: August 9, 1985Date of Patent: June 16, 1987Assignee: Pfizer Inc.Inventor: John L. LaMattina
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Patent number: 4666912Abstract: 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: GrantFiled: March 22, 1985Date of Patent: May 19, 1987Assignee: Chinoin Gyogyszer es Vegyeszeti Termeker Gyara RTInventors: Zoltan Meszaros, Jozse Knoll, Istvan Hurmecz, Peter Szentmiklosi, Agnes Horvath, Lelle Vasvari nee Debreczy, Gabor Kovacs, Klara Gyires, Sandor Virag
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Patent number: 4642314Abstract: An antiulcer composition, containing, as active ingredient, an antiulcer effective amount of an isoprene derivative as herein defined, is described.Type: GrantFiled: November 14, 1984Date of Patent: February 10, 1987Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Yoshiyuki Tahara, Michiko Nagai, Katsura Kogure, Shigeo Kawase, Teruhito Yamaguchi
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Patent number: 4600780Abstract: 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: GrantFiled: March 20, 1984Date of Patent: July 15, 1986Assignee: Ferrer International, S.A.Inventors: Rafael Foguet, Luis Anglada, Manuel M. Raga, Jose A. Ortiz, Aurelio Sacristan, Jose M. Castello
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Patent number: 4577022Abstract: 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: GrantFiled: June 21, 1983Date of Patent: March 18, 1986Assignee: John Wyeth & Brother, Ltd.Inventors: Roger Crossley, Robin G. Shepherd
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Patent number: 4510149Abstract: 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: GrantFiled: July 1, 1983Date of Patent: April 9, 1985Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Paolo Cozzi, Germano Carganico, Antonio Pillan, Umberto Branzoli
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Patent number: 4507321Abstract: 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: GrantFiled: February 17, 1982Date of Patent: March 26, 1985Assignee: The Research Foundation of State University of New YorkInventor: Ilene H. Raisfeld