Guanidines (i.e., N=c(-n)-n) Patents (Class 514/634)
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Patent number: 6153604Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 28, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6150415Abstract: Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 ##STR1## wherein X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R.sub.1 -R.sub.4 is hydrogen, R.sub.2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R.sub.4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R.sub.1 and R.sub.3 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloalkyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.Type: GrantFiled: February 18, 1999Date of Patent: November 21, 2000Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Christophe H. Morisseau, Jiang Zheng, Marvin H. Goodrow, Tonya Severson, James Sanborn
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Patent number: 6150419Abstract: A treatment and composition for neuropathic pain by administering an effective amount of agmatine.Type: GrantFiled: February 10, 2000Date of Patent: November 21, 2000Inventors: Carolyn A. Fairbanks, George L. Wilcox, Kristin Schreiber, Tinna Marie Laughlin
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Patent number: 6150382Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6149822Abstract: A process is provided for both removing and controlling biofilms present in industrial cooling and process waters. The process provides a composition which includes the reaction products of an amino base, a formaldehyde, an alkylenepolyamine, and the ammonium salt of an inorganic or organic acid. The composition may be used to remove existing biofilms from process water equipment. Further, lower maintenance dosages may be used to maintain the equipment in a substantially biofilm-free condition.Type: GrantFiled: March 1, 1999Date of Patent: November 21, 2000Assignee: Polymer Ventures, Inc.Inventors: Jon O. Fabri, Walter D. Heslep
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Patent number: 6146622Abstract: Anionic amino acid based surfactants are used to enhance antimicrobial effectiveness in topically administrable pharmaceutical compositions containing at least one active ingredient, a cationic preservative and an anionic polyelectrolyte, such as carboxyvinyl polymers, xanthan gum, polystyrene sulfonic acid polymers and cationic exchange resins.Type: GrantFiled: September 21, 1999Date of Patent: November 14, 2000Assignee: Alcon Laboratories, Inc.Inventors: Ernesto J. Castillo, Steven Howard Gerson, Wesley Wehsin Han
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Patent number: 6147063Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6143791Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 7, 1995Date of Patent: November 7, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Hu Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6143790Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
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Patent number: 6140350Abstract: A method for controlling ectoparasites systemically through host animal blood which comprises administering at least one neonocotinoid compound among those defined in the specification to the host animal.Type: GrantFiled: April 23, 1999Date of Patent: October 31, 2000Assignee: Sumitomo Chemical Company, LimitedInventor: Satoshi Sembo
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Patent number: 6133320Abstract: Primary and secondary osteoporosis in a female or a male mammal is treated by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally; in further combination with one or more of an estrogen, a progestin, an anabolic steroid. Nitric oxide substrate or donor also can be combined with one or more of other medications acting on bone, such as bisphosphonate, calcitonin, fluoride, androgen and other novel therapeutic agents. Either nitric oxide donor or substrate by itself or combination with other medications as described above can be used in both women and men, (preferably human) for prevention and treatment of osteoporosis and other metabolic bone disorders.Type: GrantFiled: October 22, 1998Date of Patent: October 17, 2000Assignee: Board of Regents, The University of Texas SystemInventors: Chandrasekhar Yallampalli, Sunil J. Wimalawansa
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Patent number: 6114393Abstract: Inhibitors of the sodium-hydrogen exchanger are suitable on their own or in combination with other classes of active compound for the production of a medicament for the treament of diseases which are caused by protozoa; thus of diseases which are caused by animal- and human-pathogenic protozoa, such as by intracellularly active parasites of the classes Apicomplexa and Zoomastigophorea, in particular trypanosomes, plasmodia (malaria pathogens), leishmanias, babesias and theilerias, cryptosporidiidae, sarcocystidae, amoebae, coccidia and trichomonads.Type: GrantFiled: August 26, 1998Date of Patent: September 5, 2000Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Hans Jochen Lang, Michael Lanzer, Jochen Wiesner, Cecilia Sanchez, Stefan Wunsch
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6103768Abstract: The invention described here concerns the unique utility of fatty acids and their derivatives to eradicate existing fungal and bacterial infections in plants. Also, described herein are combination treatments whereby fatty acids are used to enhance or augment the activity of fungicides, bactericides, and biological control agents.Type: GrantFiled: September 8, 1997Date of Patent: August 15, 2000Assignee: Mycogen CorporationInventors: Steven D. Savage, Steven L. Evans, Robert A. Haygood, Paul S. Zorner, Keith Jones
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Patent number: 6093746Abstract: An object of the present invention is to provide safe therapeutic agents for asthma inhibiting the delayed type asthmatic reaction in bronchial asthma and having no side effect. The present invention is a therapeutic agents for asthma containing a compound represented by the under chemical formula or a physiologically acceptable base thereof as an effective ingredient, and the drug containing creatine or a physiologically acceptable base thereof as an effective ingredient.Type: GrantFiled: June 16, 1998Date of Patent: July 25, 2000Assignees: Yoshiyuki Uchida, Immuno-Bio Japan Co., Ltd.Inventors: Yoshiyuki Uchida, Haruhiko Sueoka
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Patent number: 6093745Abstract: Methods and a compositions are provided for treating a skin proliferation disease such as psoriasis to inhibit the proliferation of epidermal cells, particularly keratinocytes and to reduce the symptoms of erythematous scales associated with the disease. The method comprises administering to a mammalian host with a skin proliferation disease a composition comprising an effective amount of an aminoguanidine composition, generally in a pharmaceutically acceptable carrier. The invention also provides a composition comprising an aminoguanidine composition which can be formulated in a pharmaceutically acceptable carrier, in a topical application form or for oral administration. The composition finds use in alleviating symptoms associated with the disease, such as reducing size, thickness or scales of a psoriatic lesion, reducing erthema, decreasing itching and decreasing induration.Type: GrantFiled: November 25, 1997Date of Patent: July 25, 2000Assignee: PsoRx, L.L.C.Inventors: Hans-Peter Hammes, Michael Brownlee
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Patent number: 6075054Abstract: Benzoylguanidines of formula I ##STR1## with R(1) to R(4) as defined in the specification, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment of angina pectoris.They inhibit, in a preventive manner, the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: February 24, 1998Date of Patent: June 13, 2000Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 6071969Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: June 6, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 6066673Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications.In particular, the present invention relates to compounds having the structure: ##STR1## and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L.sub.1, L.sub.2, L.sub.3, L.sub.4, Z, X, B.sub.1, and B.sub.2 are defined herein.Type: GrantFiled: March 12, 1998Date of Patent: May 23, 2000Assignee: The Procter & Gamble CompanyInventors: John McMillan McIver, Todd Laurence Underiner, Timothy Bates
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Patent number: 6063819Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.Type: GrantFiled: February 18, 1998Date of Patent: May 16, 2000Assignee: Cypros Pharmaceutical Corp.Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
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Patent number: 6060471Abstract: Mammalian hair growth is reduced by applying to the skin an inhibitor of hypusine biosynthetic pathway.Type: GrantFiled: January 21, 1998Date of Patent: May 9, 2000Inventors: Peter Styczynski, Gurpreet S. Ahluwalia, Douglas Shander
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Patent number: 6060484Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Stephen W. Kaldor, Jeffrey A. Kyle, John E. Munroe
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Patent number: 6043268Abstract: A method for treatment of viral infections which comprises administering to the patients being suffering from said viral infections an effective amount of one or more substances selected from the group consisting of nitric oxide scavengers and nitric oxide synthase inhibitors. Said method for treatment of viral infections is useful in viral infections induced by influenza virus, herpes virus, hepatitis virus, cytomegalovirus, human immunodeficiency virus, etc.Type: GrantFiled: December 24, 1996Date of Patent: March 28, 2000Assignee: Hiroshi MaedaInventors: Hiroshi Maeda, Takaaki Akaike
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Patent number: 6034080Abstract: Inhibitors of the Maillard reaction are useful in the treatment or prophylaxis of amyloidosis-based disease, particularly Alzheimer's disease. Particular examples include aminoguanidine and amphotericin B.Type: GrantFiled: December 4, 1998Date of Patent: March 7, 2000Assignee: Quadrant Holdings Cambridge LimitedInventors: Camilo Colaco, Bruce Joseph Roser
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Patent number: 6022900Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: February 8, 2000Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6013675Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: January 11, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 6011059Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.Type: GrantFiled: November 23, 1998Date of Patent: January 4, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Karnail S. Atwal, Sundeep Dugar
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Patent number: 5990174Abstract: A aqueous medium containing a biguanide, particularly a biguanide oligomer, and having a pH of less than 5. The biguanide oligomer may be a poly(hexamethylene biguanide) having up to 15 repeat units. The medium has improved storage stability compared to commercially available systems and is at least as effective as a biocide.Type: GrantFiled: May 19, 1993Date of Patent: November 23, 1999Assignee: Zeneca LimitedInventor: William John Henry
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Patent number: 5985931Abstract: The present invention relates to antimicrobial compositons comprising (i) less than or equal to two percent by weight chlorhexidine or chlorhexidine salt; (ii) less than or equal to 1 percent by weight of a quaternary ammonium compound, such as benzalkonium chloride; and (iii) less than or equal to two percent by weight of parachlorometaxylenol. The antimicrobial compositions of the invention may be utilized in antimicrobial deterents, soaps, creams rinses, and emulsions for use in the medical community as well as general public use.Type: GrantFiled: June 2, 1998Date of Patent: November 16, 1999Assignee: The Trustees of Columbia University in the city of New YorkInventors: Shanta Modak, Lester Sampath
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Patent number: 5985917Abstract: This invention is directed to a pharmacologically acceptable composition for inhibiting nitric oxide synthase in a mammal, which includes a mercapto or seleno derivative and a pharmaceutically acceptable carrier. The invention also concerns a method of inhibiting nitric oxide synthase, selectively inhibiting the inducible isoform of nitric oxide synthase, and treating various conditions where there is an advantage in inhibiting nitric oxide biosynthesis. The method includes the step of administering to a mammal a mercapto or seleno derivative in pure form or in a pharmaceutically acceptable carrier.Type: GrantFiled: March 29, 1999Date of Patent: November 16, 1999Assignee: Children's Hospital Medical CenterInventors: Garry J. Southan, Andrew L. Salzman, Csaba Szabo
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Patent number: 5972940Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and --NO.sub.2, E is --O-- or a covalent bond, n is an integer from 1 to 12, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms or taken together with the nitrogen to which they are attached form an optionally unsaturated 5 to 6-member ring of the formula --NX and X is selected from the group consisting of oxygen, sulfur, methylene and >N--R', R' being hydrogen or an alkyl of 1 to 6 carbon atoms, and their pharmaceutically acceptable acid addition salts useful to inhibit --NO synthase.Type: GrantFiled: September 10, 1997Date of Patent: October 26, 1999Assignee: Societe de Conseils Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Colette Broquet, Pierre Etienne Chabrier De Lassauniere
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Patent number: 5965529Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.Type: GrantFiled: June 6, 1995Date of Patent: October 12, 1999Assignees: The Board of Regents, University of Texas, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
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Patent number: 5955632Abstract: New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system.Type: GrantFiled: July 10, 1997Date of Patent: September 21, 1999Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Gobbini, Sergio De Munari, Giorgio Fedrizzi, Patrizia Ferrari, Piero Melloni, Marco Santagostino, Marco Torri
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Patent number: 5955507Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: September 21, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5952385Abstract: This invention is directed to a pharmacologically acceptable composition for inhibiting nitric oxide synthase in a mammal, which includes a mercapto derivative and a pharmaceutically acceptable carrier. The invention also concerns a method of inhibiting nitric oxide synthase, selectively inhibiting the inducible isoform of nitric oxide synthase, and treating various conditions where there is an advantage in inhibiting nitric oxide biosynthesis. The method includes the step of administering to a mammal a mercapto derivative in pure form or in a pharmaceutically acceptable carrier.Type: GrantFiled: July 8, 1997Date of Patent: September 14, 1999Assignee: Children's Hospital Medical CenterInventors: Garry J. Southan, Andrew L. Salzman, Csaba Szabo
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Patent number: 5945455Abstract: Use of amine and amidine containing compounds of formula (I) such as galegine and related substituted amine and amidine containing compounds as agents for reducing weight in mammals, pharmaceutical formulations containing a compound of formula (I) and methods of attaining weight reduction in mammals.Type: GrantFiled: April 15, 1998Date of Patent: August 31, 1999Assignee: University of StrathclydeInventors: Piali Palit, Brian Laurence Furman, Alexander Irvine Gray, Roger David Waigh
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Patent number: 5939078Abstract: A wrinkle-care product, an aging-preventive cosmetic and a skin cosmetic each comprising a guanidine derivative of formula (I) or an acid addition salt thereof: ##STR1## wherein R1 represents a hydrogen atom, a lower alkyl group or --(AO).sub.m --(BO).sub.n --D--E ?wherein A and B may be the same or different and each represents an alkylene group having 2 to 8 carbon atoms; D represents a binding hand, --CO--, or an unsubstituted or substituted alkylene group having 1 to 6 carbon atoms; E represents a hydrogen atom, a lower alkyl group, an aralkyl group or an unsubstituted or substituted aryl group; m is a number of from 1 to 6; and n is a number of from 0 to 6!; k is a number of from 1 to 10; and G represents a hydrogen atom, a hydroxyl group, a carboxyl group, a sulfonate group or a phosphate group. These products are excellent in the effects of inhibiting wrinkling and smoothing wrinkles without damaging the physiological conditions of the skin.Type: GrantFiled: November 18, 1996Date of Patent: August 17, 1999Assignee: Kao CorporationInventors: Tsutomu Fujimura, Ayumi Ogawa, Kazue Tsukahara, Yoshinori Takema, Minoru Nagai, Toshiya Ono
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Patent number: 5929120Abstract: Compounds of the following general structureX--Y--Z-Aryl-A--B, ##STR1## which inhibit osteoclast mediated bone resorption.Type: GrantFiled: January 30, 1998Date of Patent: July 27, 1999Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan, William F. Hoffman, Nathan C. Ihle
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Patent number: 5929055Abstract: A method for treating diabetes in a mammal by moderately controlling blood glucose concentration in the mammal together with administering to the mammal an amount of a tetracycline compound effective to reduce complications associated with diabetic hyperglycemia. The method enables long term management of diabetes by avoiding the problems associated with tight control of blood glucose concentrations, i.e., hypoglycemia tolerance and seizures, while simultaneously avoiding the problems associated with conventional moderate control of blood glucose concentrations, i.e., pathological complications associated with hyperglycemia, such as nephropathy, retinopathy, etc. Blood glucose concentration can be controlled by moderate administration (e.g.Type: GrantFiled: June 23, 1997Date of Patent: July 27, 1999Assignee: The Research Foundation of State University of New YorkInventors: Maria Emanuel Ryan, Lorne M. Golub, Nungavaram S. Ramamurthy, Thomas F. McNamara
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Patent number: 5922769Abstract: Non-insulin dependent diabetes mellitus in cases of secondary failure is treated with a combination of glibenclamide and metformin.Type: GrantFiled: May 13, 1998Date of Patent: July 13, 1999Assignee: Abiogen Pharma s.r.l.Inventors: Giulio Barelli, Massimo De Regis
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Patent number: 5922693Abstract: The present invention relates to an aqueous cleaning composition containing(a) 1 to 10 weight % of at least one surfactant selected from the group consisting of anionic surfactants and ethoxylated nonionic surfactants and mixtures thereof;(b) 0.2 to 10 weight % of a biostatic agent such as a C.sub.2 -C.sub.20 alkyl trimethyl ammonium halide, a C.sub.8 -C.sub.16 alkyl dimethyl benzyl ammonium halide, a polyhexamethylene biguanide hydrochloride, a 3-(trialkoxysilyl)propyl C.sub.14 -C.sub.20 alkyl dimethyl ammonium halide, ketoconazole, and zinc-bis(2-pyridinethiol 1-oxide); and(c) the balance being water; wherein said liquid cleaning composition does not contain a pigment, a chlorine containing bleach, peroxygen bleach, hydrogen peroxide, builder, water soluble or water dispersible organic binding agent, sequestering agent, acid dye, C.sub.8 -C.sub.18 fatty acid monoester of diglycerol, C.sub.8 -C.sub.Type: GrantFiled: February 20, 1998Date of Patent: July 13, 1999Assignee: Colgate-Palmolive Co.Inventor: Louis Oldenhove
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Patent number: 5922772Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: July 13, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5891873Abstract: Inhibitors of the Maillard reaction are useful in the treatment or prophylaxis of amyloidosis-based disease, particularly Alzheimer's disease. Particular examples include aminoguanidine and amphotericin B.Type: GrantFiled: January 16, 1997Date of Patent: April 6, 1999Assignee: Quadrant Holdings Cambridge LimitedInventors: Camilo Colaco, Bruce Joseph Roser
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Patent number: 5886040Abstract: An organic salt formed between creatine and pyruvic acid and their attendant salts and analogs, is water soluble and possesses improved palatability. The creatine is in a chemical form which increases its resistance to aqueous acid hydrolysis. The creatine cation provides the additional energy which the demands of a pyruvate induced metabolic state require. The result is a salt, which, when ingested results in increased energy and an enhanced metabolic rate.Type: GrantFiled: June 17, 1997Date of Patent: March 23, 1999Assignee: AMT Labs, Inc.Inventor: Sen-Maw Fang
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Patent number: 5883133Abstract: Compounds of the formula I ##STR1## are described in which at least one of the substituents R(1), R(2), R(3), R(4) and R(5) is a nitrogen-containing heterocyclic radical. They are outstanding cardiovascular therapeutic agents. They are obtained by reaction of a compound II ##STR2## with guanidine.Type: GrantFiled: July 24, 1996Date of Patent: March 16, 1999Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Udo Albus, Wolfgang Scholz
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Patent number: 5869531Abstract: Disclosed are 4-(2'-trifluoromethylethyl)benzoylguanidine and 3-methylsulfonyl-4-(2'-trifluoromethylethyl)benzoylguanidine. Also disclosed are pharmaceutical compositions and the use of the compounds in the treatment of disorders induced by ischemia.Type: GrantFiled: September 8, 1995Date of Patent: February 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5869534Abstract: The in vivo oxidation of lipids and lipid-containing molecules has been discovered to be initiated by the concurrent reaction of such lipid materials with reducing sugars such as glucose, advanced glycosylation endproducts such as AGE-peptides, or a compound which forms advanced glycosylation endproducts, to form materials or particles known as AGE-lipids. AGE-lipids have been implicated in the aging process, the abnormal formation of lipofuscin and in various disease states such as diabetes and atherosclerosis. Diagnostic methods are contemplated, extending in utility from the detection of the onset and course of conditions in which variations in lipid oxidation, AGE-lipid levels, LDL levels, apolipoprotein levels, apolipoprotein receptor binding the like, may be measured, to drug discovery assays.Type: GrantFiled: March 11, 1993Date of Patent: February 9, 1999Assignee: The Picower Institute for Medical ResearchInventors: Richard J. Bucala, Helen Vlassara, Anthony Cerami
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Patent number: 5869073Abstract: A liquid composition for applying a non-leachable antimicrobial coating on a surface. The liquid composition consists of a solution, dispersion or suspension of a biguanide polymer reacted with a cross-linking agent to form an adduct, and an antimicrobial metal material. The resulting antimicrobial coating does not release biocidal levels of leachables into surrounding solution.Type: GrantFiled: December 13, 1996Date of Patent: February 9, 1999Assignees: Biopolymerix, Inc, Surfacine Development Company, Inc.Inventors: Samuel P. Sawan, Tadmor Shalon, Sundar Subramanyam, Alexander Yurkovetskiy
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Patent number: 5859062Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: January 12, 1999Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5856344Abstract: Benzoylguanidines of the formula I ##STR1## in which R(1) to R(6) have the meanings stated in the claims, are antiarrhythmic pharmaceuticals which have excellent activity and a cardioprotective component and are highly suitable for the prophylaxis of infarcts and the treatment of infarcts, and for the treatment of angina pectoris, in which case they also preventively inhibit or greatly reduce the pathophysiological processes in the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: GrantFiled: October 31, 1996Date of Patent: January 5, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz