Abstract: N-acyl derivatives of aminoalcohols with bicarboxylic or tricarboxylic acids able to modulate the degranulation process consequent to the mast cells activation in inflammatory processes caused by supramaximal stimuli of neurogenic and immunogenic origin.
Type:
Grant
Filed:
June 24, 1994
Date of Patent:
April 8, 1997
Assignee:
Lifegroup S.p.A.
Inventors:
Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
Abstract: The present invention relates to a process for the preparation of 2,5-di-phenylamino-terephthalic acid and its dialkyl esters of the formula ##STR1## in which R is a hydrogen atom or a methyl or an ethyl group, by reaction of a succinic acid dialkyl ester with a sodium alcoholate in xylene, treatment of the resulting 2,5-dihydroxy-cyclohexadiene-1,4-di-carboxylic acid dialkyl ester with acid and aniline, dehydrogenation of the resulting 2,5-di-phenylamino-dihydro-(3,6)-terephthalic acid dialkyl ester by means of oxygen, if appropriate hydrolysis of the 2,5-di-phenylamino-terephthalic acid dialkyl ester formed and liberation of the 2,5-di-phenylamino-terephthalic acid from the di-sodium salt formed. The 2,5-di-phenylamino-dihydro-(3,6)-terephthalic acid dialkyl ester is reacted with pure oxygen in the presence of an alkali metal ion and/or an alkaline earth metal ion. This significantly decreases undesirable impurities.
Abstract: Compositions and method for the minimization or prevention of adhesion formation, whereby an effective amount of at least one lazaroid compound, preferably one of general formula I, is administered for a period of time sufficient to permit tissue repair. The compound of general formulae I or II is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, biodegradable polymer films, lipid-based delivery systems such as liposomes and lipid foams, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at an effective level.
Abstract: The orally administrable pharmaceutical compositions containing a slightly water-soluble drug, characterized by improved stability and improved absorption of the drug from digestive tract into blood. The use of the compositions of the present invention enables decrease of the dose amount of a slightly water-soluble drug, which eventually leads to alleviation of pains and side effects on the part of patients.
Abstract: A method of treating skeletal muscle fibrosis in mammals. The novel method is effective for reducing the extent of skeletal muscle fibrosis in an individual who suffers from a disorder which targets skeletal muscle tissue, such as Duchenne's and Becker's muscular dystrophy and denervation atrophy induced by either trauma or neuromuscular disease. The treatment includes administering to the individual an effective amount of a metalloporphyrin compound, especially hemin, heme arginate, cobalt protoporphyrin IX chloride and cobalt protoporphyrin IX arginate.
Abstract: A stably storable and readily water soluble composition for use in preparing injections and containing Cefditoren, namely a cephalosporin of the formula ##STR1## is now provided, which composition comprises a physical mixture of Cefditoren or a non-toxic salt thereof with a proportion of arginine and/or lysine and/or a non-toxic salt thereof. This new composition of Cefditoren can be stored for long periods of time without discoloration and without undesirable reduction in the antibacterial activity, and the composition can be dissolved completely and quickly in water.
Abstract: The present invention relates to a method for the synthesis of foscarnet, i.e. trisodium phosphonoformate hexahydrate, comprising the steps of adding sodium hydroxide to water, heating the aqueous sodium hydroxide solution to 50.degree. C., adding triethyl phosphonoformate to said solution at 50.degree. C., heating the reaction mixture to reflux for about 1 hour, cooling of the reaction mixture and filtering-off of the product.
Abstract: Use of a medicament with a content of metanolone and/or Oral Turinabol for increasing and optimizing the degree of activation of the central nervous system and/or for prophylaxis and therapy of osteoporosis.
Abstract: A process of preparing purified alkanesulfonic acid from crude aqueous alkanesulfonic acid containing oxidizable impurities wherein the crude material is treated with a sufficient amount of chlorine to convert the oxidizable impurities to alkanesulfonyl chloride and then hydrolyzing said alkanesulfonyl chloride to alkanesulfonic acid by heating.
Type:
Grant
Filed:
March 27, 1991
Date of Patent:
December 10, 1996
Inventors:
Phyllis A. Henderson, Steven G. Schon, Carl Postuma
Abstract: This invention relates to parenteral preparations of antiestrogens such as toremifene, desmethyl toremifene, tamoxifen or desmethyltamoxifen. The preparations can be emulsions, liposomes or aqueous solutions of cyclodextrin-drug complexes. Particularly the invention relates to a parenteral drug formulation comprising a complex having a 2-hydroxypropyl cyclodextrin component and including an active drug substance selected from the group consisting of toremifene, desmethyl toremifene, tamoxifen and desmethyltamoxifen or a pharmaceutically acceptable non-toxic salt thereof, said complex being present either in an aqueous solution or emulsion or loaded into a liposome.
Type:
Grant
Filed:
July 7, 1994
Date of Patent:
November 5, 1996
Assignee:
Orion-yhtyma Oy
Inventors:
Harry G. Jalonen, Terttu M. Heikkila, Hannu U. Jalonen, Lauri V. M. Kangas, Risto A. S. Lammintausta, Kauko O. A. Kurkela
Abstract: The invention is directed to improved methods for modulating the human sexual response by administering a vasodilator to the circulation by a route of administration that avoids the "first-pass" effect.
Type:
Grant
Filed:
August 9, 1994
Date of Patent:
October 15, 1996
Assignee:
Zonagen, Inc.
Inventors:
Diane-Marie Gioco, Adrian Zorgniotti, deceased
Abstract: Cyanoquinoline compounds Ia or Ib ##STR1## where R.sup.1 is CH.dbd.C(CN).sub.2 ; CH.dbd.N--N.dbd.CH--(5-quinolyl); methylsulfonyl; CH.dbd.NOH; halogen; hydroxyl; nitro; cyano; unsubstituted or substituted C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkylthio, pyrrolidinyl; piperidinyl; morpholinyl; thiomorpholinyl; unsubstituted or substituted phenyl, phenoxy, phenylthio, phenyldithiolyl, phenylsulfonyl or pyrrolyl;m is 0, 1, 2 or 3;R.sup.2 is hydrogen; hydroxyl; halogen; C.sub.1 -C.sub.4 -alkoxy; --NR.sup.3 R.sup.4 ; --NR.sup.5 --CXR.sup.6 or --N.dbd.CR.sup.7 R.sup.8 ;R.sup.3 is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.4 -alkyl;R.sup.4 is a radical R.sup.3 ; C.sub.1 -C.sub.4 -alkylamino; di-C.sub.1 -C.sub.4 -alkylamino; substituted C.sub.1 -C.sub.4 -alkyl; CH.dbd.N--(3-cyano-2-quinolinyl); or R.sup.3 and R.sup.4 together form C.sub.4 - or C.sub.3 -alkylene which may be interrupted by a hetero atom, or unsubstituted or substituted 1,3-butadienyl;R.sup.5 and R.sup.
Type:
Grant
Filed:
April 17, 1995
Date of Patent:
October 15, 1996
Assignee:
BASF Aktiengesellschaft
Inventors:
Helmut Hagen, Juergen Pfister, Gunter Brill, Gerhard Nilz, Bruno Wuerzer, Karl-Otto Westphalen
Abstract: Substituted 5-2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles having the structural formula: ##STR1## wherein R4, R5, R6, R7, and R8 are as hereinafter defined, are .beta.3-adrenergic agonists useful in the treatment of elevated intraocular pressure and glaucoma.
Abstract: The present invention relates to pharmaceutical compositions for the treatment of infections caused by Microsporidia comprising treating an animal with 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt thereof.
Type:
Grant
Filed:
June 9, 1995
Date of Patent:
October 1, 1996
Assignee:
Glaxo Wellcome Inc.
Inventors:
Winston E. Gutteridge, Alan T. Hudson, Victoria S. Latter, Mary Pudney
Abstract: The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Mircosporidia comprising 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other functional derivative thereof as active ingredient and to a method of treating or preventing siad protozoal infections in an animal which comprises administering to said animal an effective amount of siad compound.
Type:
Grant
Filed:
November 8, 1994
Date of Patent:
September 24, 1996
Assignee:
Glaxo Wellcome, Inc.
Inventors:
Winston E. Gutteridge, Alan T. Hudson, Victoria S. Latter, Mary Pudney
Abstract: A medicament for immediately treating painful, inflammatory and/or febrile acute diseases contains flurbiprofen as a racemate, a mixture of a racemate with its enantiomers, a pseudoracemate (mixtures of equal parts of S- and R-flurbiprofen) or as a mixture of different parts of S- and R-flurbiprofen in the range extending between pure S and pure R-flurbiprofen as active substance in the form of a pharmaceutically applicable nanosol. This medicament satisfies all requirements of an immediate-effect pharmaceutic form.
Type:
Grant
Filed:
September 16, 1994
Date of Patent:
September 17, 1996
Assignee:
Alfatec Pharma GMBH
Inventors:
Jens-Christian Wunderlich, Otto Schuster, Helmut Lukas, Ursula Schick
Abstract: An ophthalmic suspension comprising difluprednate as an active ingredient. The ophthalmic suspension of the present invention shows superior antiinflammatory action and antiallergic action by local administration. Accordingly, the suspension of the present invention is useful for the treatment and prevention of disorders of the eye, such as allergic conjunctivitis, vernal conjunctivitis, blepharitis marginalis, catarrhal conjunctivitis and uveitis.
Type:
Grant
Filed:
December 20, 1994
Date of Patent:
September 17, 1996
Assignees:
Senju Pharmaceutical Co., Ltd., Mitsubishi Chemical Corporation
Abstract: A dental product is provided in a dual-compartment dispenser that includes a first and second composition in respective compartments thereof. The first composition includes a zinc salt while the second composition includes a bicarbonate salt. Preferably the first composition also contains a peroxygen compound or a C.sub.2 -C.sub.20 carboxylic acid. The zinc salt in combination with the bicarbonate salt achieves an enhanced antitartar effect.
Type:
Grant
Filed:
April 11, 1995
Date of Patent:
September 10, 1996
Assignee:
Chesebrough-Pond's USA Co., Division of Conopco, Inc.
Inventors:
David R. Williams, Christine W. Ryles, Stephen R. Barrow
Abstract: Low viscosity, highly concentrated surfactant suspensions for replacement therapy In diseases of the respiratory tract are described. The suspensions are characterised in that they contain calcium and/or magnesium ions bound to the surfactant and unbound in the suspension agent, as well as containing a certain amount of common salt.
Type:
Grant
Filed:
May 1, 1995
Date of Patent:
September 3, 1996
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Bernd Disse, Eberhard Weller, Robert Becker