2-imidazolines Patents (Class 514/401)
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Patent number: 5464857Abstract: (1) The imidazoline derivative represented by the following general formula (1) ##STR1## where R.sup.1 is a substituent endowed with water solubility or fat solubility, particularly carboxyl group or carboxymethoxy group or a pharmaceutically acceptable salt thereof, (2) The method for producing the above-mentioned compound, and (3) A therapeutic agent containing as its active ingredient the above-mentioned imidazoline derivative or an imidazoline derivative wherein R.sup.1 indicated in the formula (1) is hydrogen atom. The imidazoline derivative set forth under (1) above is a novel substance; and this compound itself and its derivative having R.sup.1 as indicated in the general formula (1) is hydrogen atom are useful as a therapeutic agent for treatment of shock from the fall in blood pressure by virtue of their ability to remove excess NO which is the vascular endothelium-derived relaxing factor (EDRF).Type: GrantFiled: November 21, 1994Date of Patent: November 7, 1995Assignee: Hiroshi MaedaInventors: Hiroshi Maeda, Yoichi Miyamoto, Takaaki Akaike
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Patent number: 5459157Abstract: A pharmaceutical aqueous solution for ophthalmic use comprising a nonsteroidal anti-inflammatory drug, having a carboxylic group, a decongestant drug and a mixture of a polysorbate and a poloxamer.Type: GrantFiled: March 21, 1994Date of Patent: October 17, 1995Assignee: Zambon Group S.p.A.Inventors: Federico Stroppolo, Daniele Bonadeo, Luigi Virgano', Annibale Gazzaniga
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Patent number: 5453428Abstract: In accordance with the present invention, neuropsychiatric symptoms of apathy-amotivation syndrome and particularly those symptoms in: Alzheimer's disease, multiple sclerosis, Huntington's chorea, frontal lobe lesions, and AIDS dementia can be ameliorated by treating a patient with a histamine H.sub.2 -antagonist that passes the blood-brain barrier. Suitable H.sub.2 -antagonists include famotidine and ranitidine. The H.sub.2 -antagonists may be co-administered with other compounds which are known to be useful in the treatment of the above neuropsychiatric conditions, and in one aspect of the invention can be formulated with such other compounds into a therapeutic composition.Type: GrantFiled: September 7, 1993Date of Patent: September 26, 1995Assignee: The Mount Sinai School of Medicine of the City of New YorkInventor: Ram Kaminski
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Patent number: 5444082Abstract: 3,9-disubstituted-spiro[5.5]undecanes and ##STR1## wherein, R, Y, A, B and n are defined in the specification, pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension, are disclosed.Type: GrantFiled: June 28, 1993Date of Patent: August 22, 1995Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Marco Frigerio, Patrizia Ferrari, Piero Melloni, Giuliana Salani
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Patent number: 5444069Abstract: The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT.sub.2 receptors to treat memory loss.Type: GrantFiled: April 13, 1994Date of Patent: August 22, 1995Assignee: Warner-Lambert CompanyInventors: David T. Dudley, John C. Hodges, Thomas A. Pugsley, Michael D. Taylor
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Patent number: 5430063Abstract: The invention concerns a phenoxyphenyl compound having the formula ##STR1## wherein R is one or two halogen atoms; andA is CH.sub.2 NR.sub.1 R.sub.2 or 4,5-dihydro-1H-imidazole, in which R.sub.1 and R.sub.2 are independently selected from hydrogen and lower alkyl; ora pharmaceutically acceptable salt thereof.The compounds have long half-lives and can be used against depression.Type: GrantFiled: February 3, 1993Date of Patent: July 4, 1995Assignee: Akzo N.V.Inventors: Gerardus S. F. Ruigt, Dirk Leysen, Johannes H. Wieringa
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Patent number: 5428041Abstract: Provided are bis-trifluoromethyl-substituted imidazolines as inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and therapeutic methods for their use as antihypercholesterolemic or antiatherosclerotic agents.Type: GrantFiled: March 4, 1992Date of Patent: June 27, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Jeffrey T. Billheimer, George A. Boswell, Jr., Indawati De Lucca, Spencer Drummond, Jr., Peter J. Gillies, James M. Trzaskos
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Patent number: 5428013Abstract: Differential diagnosis of diverse GH-deficient states may be effectively established by cojointly administering an alpha-2-adrenergic agonist, such as clonidine, and a growth hormone releasing peptide such as GHRH. In addition, some children with short stature and showing a positive response to this test may effectively be treated with such administration.Type: GrantFiled: September 18, 1992Date of Patent: June 27, 1995Inventor: Jesus D. Mugica
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Patent number: 5407954Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.Type: GrantFiled: February 9, 1994Date of Patent: April 18, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jules Freedman, Bruce M. Baron, Mark W. Dudley
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Patent number: 5338744Abstract: The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT.sub.2 receptors.Type: GrantFiled: August 19, 1992Date of Patent: August 16, 1994Assignee: Warner-Lambert CompanyInventors: David T. Dudley, John C. Hodges, Thomas A. Pugsley, Michael D. Taylor
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Patent number: 5334610Abstract: The present invention relates to novel .alpha.-aryl-.alpha.-hydroxy-.beta.-imidazolinyl-propionamides of the general formula (I) ##STR1## in which n, R.sup.1 to R.sup.4 and X have the meaning indicated in the description, to a process for their preparation and to their use in medicaments.Type: GrantFiled: January 14, 1993Date of Patent: August 2, 1994Assignee: Bayer AktiengesellschaftInventors: Wilfried Draber, Hilmar Bischoff
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Patent number: 5298242Abstract: The invention relates to compounds of formula: ##STR1## in which: w is 0, 1 or 2;x is between 2 and 10;y is between 0 and 5;R denotes a methyl, ethyl, hydroxyethyl or benzyl radical;X.crclbar. denotes an inorganic or organic anion; andn is an integer or decimal number between 1 and 15;the [C.sub.5 H.sub.6 N.sub.2 R.sup.+ ] group representing the following structures, taken as a mixture or individually: ##STR2## as well as their use as a biocidal agent or preservative.Type: GrantFiled: June 23, 1992Date of Patent: March 29, 1994Assignee: L'OrealInventors: Guy Vanlerberghe, Eric Bollens, Claude Mahieu, Henri Sebag
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Patent number: 5296498Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: January 19, 1993Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5296493Abstract: The present patent application discloses compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1-10 saturated or unsaturated alkyl; or ##STR2## wherein R'" is H or ##STR3## R.sup.2 is phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; benzyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; or cyclohexyl;R.sup.3 phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; naphthyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; C.sub.1-6 unsaturated alkyl; furanyl;R.sup.4 is H, C.sub.Type: GrantFiled: May 23, 1991Date of Patent: March 22, 1994Assignee: NeuroSearch A/SInventors: Peter Moldt, Elsebet O. Nielsen
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Patent number: 5292756Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
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Patent number: 5281607Abstract: The treatment of neurodegenerative diseases by the stimulation of endogenous or recombinant expression in vivo of nerve growth factor in the central nervous system by administration of a therapeutically effective amount of an .alpha..sub.2 -antagonist.Type: GrantFiled: October 8, 1992Date of Patent: January 25, 1994Assignee: New York UniversityInventors: Eric A. Stone, Guoying Bing
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Patent number: 5278184Abstract: Antirhinoviral compounds having the formula ##STR1## wherein R is hetrocyclic, particularly pyrrole or pyrrolidine, X is H.sub.2 or O, n IS 3 to 7, and R.sub.1 is substituted phenyl are disclosed.Type: GrantFiled: April 17, 1992Date of Patent: January 11, 1994Assignee: Repla Chemical Ltd.Inventors: Marino Artico, Federico Corelli, Silvio Massa, Antonello Mai, Enzo Tramontano
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Patent number: 5256674Abstract: An imidazolidine derivative having the formula (I) or its salt: ##STR1## wherein X is an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, ##STR2## (in which each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently a hydrogen atom or an alkyl group, R.sup.5 is an alkyl group which may be substituted with a halogen atom, a cycloalkyl group which may be substituted or a phenyl group which may be substituted, W is an oxygen atom or a sulfur atom, and each of k, l, m and n is independently 0 or 1, provided that (a) case where all of k, l and m are 0 at the same time and (b) case where m and n are 0 at the same time and R.sup.5 is an alkyl group which may be substituted with a halogen atom, are excluded), or ##STR3## group (in which each of R.sup.6 and R.sup.7 is independently a hydrogen atom or an alkyl group, each of R.sup.8 and R.sup.9 is independently an alkyl gorup, R.sup.Type: GrantFiled: December 21, 1990Date of Patent: October 26, 1993Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Masato Omatsu, Hiroshi Sasaki, Masayuki Morita, Kiyomitsu Yoshida
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Patent number: 5250286Abstract: A method of using an imidazoline compound, which is a vasodilator and an alpha-adrenergic blocking agent, for the treatment of symptoms of chronic obstructive pulmonary diseases (COPD), including cystic fibrosis, chronic bronchitis and emphysema, or COPD where it is associated with asthma, comprises administering the imidazoline to a patient by inhalation. Preferably, the imidazoline compound employed is tolazoline. The presentation of an imidazoline compound in a device for the administration of an aerosol is disclosed.Type: GrantFiled: November 27, 1991Date of Patent: October 5, 1993Assignee: Aegis Technology, Inc.Inventor: Alvaro H. Skupin
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Patent number: 5246936Abstract: The present invention describes a composition for enhanced pesticidal activity comprising a pesticide or a mixture of pesticides and a potentiating amount of a stilbene compound. This invention further describes a method for enhancing pesticide toxicity against an insect, an acarina, a mollusk or a nematode which employs the sequential or concurrent application of a pesticide and a stilbene compound.Type: GrantFiled: December 20, 1991Date of Patent: September 21, 1993Assignee: American Cyanamid CompanyInventors: Michael F. Treacy, Bruce C. Black, Stephen F. Donovan
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Patent number: 5244653Abstract: The use of glycine anhydride dimethylol, also known as 1,4-bis(hydroxymethyl)-2,5-piperazinedione, comprising the formula ##STR1## to kill microorganisms present in or on a host substance and to preserve products susceptible to contamination by a variety of microorganisms is disclosed.Type: GrantFiled: May 1, 1991Date of Patent: September 14, 1993Assignee: ISP Chemicals Inc.Inventors: Philip A. Berke, William E. Rosen
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Patent number: 5231112Abstract: Methods and compositions are described for the preparation of bioactive agents entrapped in lipid vesicles the bilayers of which comprise a salt form of an organic acid derivative of a sterol, such as the tris-salt form of a sterol hemisuccinate, and to bompositions comprising a mixture of tris(hydroxymethyl)aminomethane salt of cholesteryl hemisuccinate with either an antifungal compound or a peptide. These compositions have various applications in vivo.Type: GrantFiled: October 23, 1989Date of Patent: July 27, 1993Assignee: The Liposome Company, Inc.Inventors: Andrew S. Janoff, Mircea C. Popescu, Alan L. Weiner, Lois E. Bolcsak, Paul A. Tremblay, Christine E. Swenson
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Patent number: 5216008Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.Type: GrantFiled: February 6, 1992Date of Patent: June 1, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jules Freedman, Bruce M. Baron, Mark W. Dudley
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Patent number: 5196432Abstract: Ruminal lactic acidosis develops in ruminant animals following the ingestion of large amounts of unaccustomed feeds that are rich in readily fermentable carbohydrates. Characteristics symptoms of this disease include systemic acidosis, ruminal acidosis, forestomach stasis or forestomach hypomotility, inappetence, depression and hemoconcentration. Alpha-2 adrenoceptor antagonists have been found to be capable of re-establishing forestomach motility that has been lost or severely diminished in ruminants suffering from ruminal lactic acidosis. These antagonist compounds have also been found to be effective in the treatment of ruminants experiencing ruminal lactic acidosis.Type: GrantFiled: February 14, 1990Date of Patent: March 23, 1993Inventor: Eugene C. Crichlow
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Patent number: 5190965Abstract: The invention concerns a phenoxyphenyl derivative having the formula ##STR1## wherein R is one or two halogen atoms; andA is CH.sub.2 NR.sub.1 R.sub.2 or 4,5-dihydro-1H-imidazole, in which R.sub.1 and R.sub.2 are independently selected from hydrogen and lower alkyl; ora pharmaceutically acceptable salt thereof.The compounds have long half-lives and can be used against depression.Type: GrantFiled: May 29, 1992Date of Patent: March 2, 1993Assignee: AKZO N.V.Inventors: Gerardus S. F. Ruigt, Dirk Leysen, Johannes H. Wieringa
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Patent number: 5189065Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.Type: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
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Patent number: 5180721Abstract: Methods and pharmaceutical formulations of alpha.sub.2 agonists and alpha.sub.3 antagonists which are useful in lowering intraocular pressure (IOP) and treatment of intraocular hypertension. Co-administration of a therapeutic amount of alpha.sub.2 agonist with a potentiating amount of alpha.sub.3 agonist is effective in lowering IOP and treatment of intraocular hypertension.Type: GrantFiled: May 30, 1991Date of Patent: January 19, 1993Assignee: Allergan, Inc.Inventor: James A. Burke
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Patent number: 5162361Abstract: The present invention relates to a method of treating diseases associated with elevated levels of interleukin 1 (IL-1) including inflammatory diseases such as arthritis, skin hypersensitivity and endotoxemia. More specifically, the invention relates to a method for the treatment of such diseases in warm-blooded animals, such as humans, which comprises the administration of a therapeutically effective amount of an aromatic diamidine, sufficient to inhibit IL-1 release from IL-1 producing cells. The aromatic diamidine can also be used to block interleukin 6 (IL-6) and tumor necrosis factor from cells producing these cytokines.Type: GrantFiled: April 10, 1990Date of Patent: November 10, 1992Assignee: The United States of America as represented by the Secretary, Department of Health and Human ServicesInventors: Gary J. Rosenthal, Yasuhida Kouchi, Emanuela Corsini, Benny Blaylock, Christine Comment, Michael Luster, William Craig, Michael Taylor
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Patent number: 5134154Abstract: The present invention is directed to a new class of phenoxy-heterocyclic compounds and to their use as anti-depressants and as anxiolytics.Type: GrantFiled: March 5, 1991Date of Patent: July 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jules Freedman, Mark W. Dudley
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Patent number: 5128361Abstract: The present invention relates to agents for systemic combating of ectoperasites in host animals, containing a compound of the formul I ##STR1## in which R.sup.1 denotes hydrogen, (C.sub.1 -C.sub.5)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkyl or halogen;R.sup.2 and R.sup.3 independently of one another denote (c.sub.1 -C.sub.5)-alkyl, (C.sub.2 -C.sub.5)-alkenyl, (C.sub.2 -C.sub.5)-alkynyl, (C.sub.3 -C.sub.7)-cycloalkyl, (C.sub.3 -C.sub.7)-cycloalkenyl, (C.sub.1 -C.sub.3)-halogenoalkyl, halogen, cyano, nitro, (C.sub.1 -C.sub.5)-alkoxy, (C.sub.1 -C.sub.3)-alkoxy-C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkoxy or (C.sub.1 -C.sub.3)-alkylthio, or R.sup.2 and R.sup.3 together form a polymethylene chain having 2 to 5 carbon atoms:R.sup.4 denotes hydrogen, (c.sub.1 -C.sub.10)-alkyl, (C.sub.2 -C.sub.5)-alkenyl or (C.sub.3 -C.sub.7)-cycloalkyl;R.sup.5 denotes hydrogen, (C.sub.1 -C.sub.10)-alkyl, (C.sub.3 -C.sub.5)-alkenyl, C.sub.3 -C.sub.5)-alkynyl, (C.sub.3 -C.sub.7)- cycloalkyl, (C.sub.3 -C.sub.Type: GrantFiled: December 18, 1989Date of Patent: July 7, 1992Assignee: Hoechst AktiengesellschaftInventors: Herbert Stark, Gerhard Salbeck, Werner Bonin
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Patent number: 5120713Abstract: Obese patients may be effectively treated by cojointly administering an alpha-2-adrenergic agonist, such as clonidine, and a growth hormone releasing peptide, such as GHRH, to restore or substantially enhance growth hormone release in such patients.Type: GrantFiled: September 10, 1990Date of Patent: June 9, 1992Assignee: Applied Research Systems ARS Holding N.V.Inventor: Jesus D. Mugica
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Patent number: 5110824Abstract: The invention relates to the use of benzamide derivatives of the formula: ##STR1## in which: A is a diethylaminoethyl group or a group of the formula II: ##STR2## where R is a C.sub.1 -C.sub.3 alkyl, allyl, cyclopropylmethyl or cyclohexenylmethyl group,X is a chlorine or bromine atom, andZ is --NH-- or --O-- with the following condition: when Z is --O--, A is a diethylaminoethyl group, and their pharmacologically acceptable salts for the preparation of medicinal products which are useful in the treatment and prevention of disorders of the cognitive function.Type: GrantFiled: April 12, 1990Date of Patent: May 5, 1992Assignee: Societe d'Etudes Scientifiques et Industrielles de L'Ile-de-FranceInventors: Jacques Acher, Jean-Claude Monier, Jean-Paul Schmitt, Renee Gardaix-Luthereau, Brenda Costall, Robert Naylor
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Patent number: 5106845Abstract: The present invention is directed to a new class of cyclic guanidines of the formula: ##STR1## in which Q is represented by a substituent selected from the group consisting of (CH.sub.2).sub.n in which n is an integer from 2-10, ##STR2## A is a substituent selected from the group consisting of --NH--(CH.sub.2).sub.m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar.sub.1 are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and trifluoromethyl; and R is represented by either hydrogen or a C.sub.1-4 alkyl; R.sub.1 is represented by hydrogen or a C.sub.1-4 alkyl; the optional isomers and tautomers thereof; and the pharmaceutically acceptable acid addition salts thereof, and their use as calcium antagonists.Type: GrantFiled: January 10, 1990Date of Patent: April 21, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Hsien C. Cheng, John M. Kane
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Patent number: 5106407Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.Type: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
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Patent number: 5096916Abstract: A method of using an imidazoline compound, which is a vasodilator and an alpha-adrenergic blocking agent, for the treatment of symptoms of chronic obstructive pulmonary diseases (COPD), including cystic fibrosis, chronic bronchitis and emphysema, or COPD where it is associated with asthma, comprises administering the imidazoline to a patient by inhalation. Preferably, the imidazoline compound employed is tolazoline. The presentation of an imidazoline compound in a device for the administration of an aerosol is disclosed.Type: GrantFiled: May 7, 1990Date of Patent: March 17, 1992Assignee: Aegis Technology, Inc.Inventor: Alvaro H. Skupin
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Patent number: 5091404Abstract: The use of cyclocreatine to preserve and/or restore the physiological functionality of muscle tissue subject to ischemia.Type: GrantFiled: October 5, 1990Date of Patent: February 25, 1992Inventor: Salwa A. Elgebaly
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Patent number: 5068240Abstract: A pharmaceutical composition and process for preparing the same is provided, wherein the active ingredient of the said composition is one or more compounds of the general formula /I/ ##STR1## In the formula R is longer aliphatic hydrocarbon radical which may contain one or more unsaturation,R.sub.1 is hydrogen or longer aliphatic acyl radical which may contain one or more unsaturation,X is oxygen and Y is hydrogen, orX and Y, when taken together, form a radical of the formula .dbd.N--CH.sub.2 --CH.sub.2 --,z is 1 to 5, andq is 1 to 4.The use of the above compounds in the therapy of tumorous diseases and for regenerating tumorous cells and tissues is also claimed.Type: GrantFiled: June 4, 1990Date of Patent: November 26, 1991Inventor: Adam Kovacs
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Patent number: 5051441Abstract: Imidazoline derivative of the formula: ##STR1## wherein R is a halogenophenyl group or a pyridyl group and X.sup.1 and X.sup.2 are a hydrogen atom or a lower alkoxy group, or a pharmaceutically acceptable salt thereof, which is useful as an immunomodulator and as an agent for the treatment and/or prophylaxis of rheumathoid arthritis, multiple sclerosis, systemic lupus erythemathodes, rheumatic fever and the like, a process for the preparation thereof, and a pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: October 4, 1989Date of Patent: September 24, 1991Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kazuo Matsumoto, Mamoru Suzuki, Kozo Yamamoto, Isao Takata, Yoshio Iwasawa
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Patent number: 5049315Abstract: The present invention provides polycarboxylic acid imidazolines of the general formula: ##STR1## wherein X is --Cl, --OH, --O--SO.sub.3 H, --O--PO.sub.3 H.sub.2, --O--CH.sub.2 --CH.sub.2 --COOH, --NH.sub.2, --NHalk or --N(alk).sub.2, alk being an alkyl radical containing up to 6 carbon atoms, n is a whole number of from 2 to 4, R is a C.sub.8 -C.sub.18 hydrocarbon radical which is straight-chained, branched, saturated or one to three times unsaturated, m is a whole number of from 2 to 5, R' is a hydrogen atom or a carboxyl group and R" is a hydrogen atom or a methyl radical. The present invention also provides a process for the preparation of these compounds and cleaning agents containing them.Type: GrantFiled: June 8, 1990Date of Patent: September 17, 1991Assignees: Chemisches Instutut Schaefer AG, Joh. A. Benskiser GmbHInventors: Hans Hitz, Rolf Schaefer, Heinrich Baust, Wolfgang Gross
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Patent number: 5025015Abstract: Formamidine compounds of general formula I ##STR1## in which: R.sub.1 represents H or C.sub.1-4 alkyl,R.sub.2 represents benzoyl, benzyl, or alphahydroxybenzyl, the aromatic ring being optionally substituted by a halogen atom,R.sub.3 and R.sub.4, which are identical or different, represent hydrogen, lower-alkyl, or lower-alkenyl, or form between them with the formamidine function a heterocycle,R.sub.5 represents hydrogen or C.sub.1-4 lower-alkyl or forms with R.sub.4 a double bond (--N.dbd.R.sub.4) in the case of pseudoaromatic heterocycles,n equals 0 or 1,A represents a linear or branched C.sub.1-4 alkylene chain,X represents hydrogen, halogen, C.sub.1-4 lower-alkyl, C.sub.1-4 lower-alkoxy, or nitro, and pharmaceutically-acceptable salts thereof, are disclosed.The compounds and pharmaceutical compositions thereof are used, optionally in combination with other active principles, as drugs for the treatment of gastrointestinal ailments, especially as gastric antisecretory and antiulcer agents.Type: GrantFiled: September 7, 1989Date of Patent: June 18, 1991Assignee: Pierre Fabre MedicamentInventors: Jean F. Patoiseau, Jean-Marie Autin, Henri Cousse, Veronique Sales, Jacky Tisne-Versailles, Jean-Pierre Bali
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Patent number: 5013750Abstract: The glycocyamidine derivatives of the present invention are represented by the following formula (I): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, is hydrogen or a lower alkyl group, preferably a straight or branched alkyl group having 1 to 3 carbon atoms, such as methyl, ethyl, propyl or isopropyl, and R represents hydrogen or an acetyl group,which are useful as test reagents for diagnosis of renal failure.Type: GrantFiled: July 11, 1990Date of Patent: May 7, 1991Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Ko Nakamura, Kazuharu Ienaga
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Patent number: 5006523Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.Type: GrantFiled: October 26, 1989Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5001141Abstract: N-[2-(2-oxo-1-imidazolidinyl)ethyl]-3-phenylurea and analogs are useful for protecting against oxygen-derived free radical damage in mammals, by inducing endogenous antioxidant enzymes, including superoxide dismutase, in mammals.Type: GrantFiled: August 4, 1989Date of Patent: March 19, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Janet S. Kerr, George A. Boswell
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Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4973592Abstract: New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: September 13, 1988Date of Patent: November 27, 1990Assignee: Istituto de AngeliInventors: Massimo Nicola, Arturo Donetti, Enzo Cereda, Marco Turconi, Giovanni B. Schiavi, Rosamaria Micheletti
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Patent number: 4970208Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilization of fodder and the ratio of muscle to fat in favour of the proportion of muscle and protein.Type: GrantFiled: October 25, 1988Date of Patent: November 13, 1990Assignee: Boehringer Ingelheim GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4940723Abstract: A method of treating arthritis, and/or bone marrow hyperplasia, osteitis and synovitis, and/or granulomatosis including of the liver and spleen, which comprises administering to a patient an effective amount of BABIM and a pharmaceutically acceptable carrier.Type: GrantFiled: October 20, 1988Date of Patent: July 10, 1990Assignee: University of North Carolina, Chapel HillInventors: Richard R. Tidwell, Joachim D. Geratz, John H. Schwab, Katherine B. Pryzwansky, Sonia K. Anderle
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Patent number: 4910215Abstract: The use of 2,6-dichlorophenyl compounds as active principles in pharmaceutical formulations designed to stimulate the secretion or release of somatotropic hormone in man and animals is described.Type: GrantFiled: April 12, 1988Date of Patent: March 20, 1990Inventor: Eugenio Muller
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Patent number: 4897411Abstract: A method of using clonidine for the treatment of Premenstrual Syndrome (PMS) in selective subjects to reduce or alleviate subject's manifestation of psychiatric symptoms associated with PMS.Type: GrantFiled: February 13, 1989Date of Patent: January 30, 1990Inventor: A. James Giannini
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Patent number: 4897412Abstract: Antiglaucoma compounds having beta adrenoreceptor antagonist properties and alpha adrenoreceptor antagonist properties are described. The compounds comprise a beta blocker-derived moiety designed to provide beta antagonist properties and an imidazolidine moiety designed to provide alpha-antagonist properties. Methods of synthesizing the compounds are also described. The compounds are useful in the treatment of glaucoma due to their ability to lower elevated intraocular pressure.Type: GrantFiled: January 19, 1989Date of Patent: January 30, 1990Assignee: Laboratories Alcon S.A.Inventors: Gerard LeClerc, Didier Huber, Jacques Himber, Guy Andermann