2-imidazolines Patents (Class 514/401)
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Patent number: 4889868Abstract: This invention relates to chemical compounds which possess valuable therapeutic activity particularly as lipoxygenase and phospholipase C inhibitors and as platelet-activating factor receptor antagonists. The compounds posses anti-inflammatory anti-asthmatic and anti-allergic properties and are additionally useful for the treatment of myocardial infarctions.Type: GrantFiled: December 16, 1985Date of Patent: December 26, 1989Assignee: Rorer Pharmaceutical CorporationInventor: Fu-chih Huang
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Patent number: 4876266Abstract: Disclosed are novel substituted 3-aralkylimidazolines of the structure. ##STR1## processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy in particular as dopamine-.beta.-hydroxylase inhibitors.Type: GrantFiled: December 31, 1987Date of Patent: October 24, 1989Assignee: SmithKline Beckman CorporationInventors: Lawrence I. Kruse, Thomas B. Leonard, Stephen T. Ross
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Patent number: 4871760Abstract: The invention relates to the use of 2-[N-(2,6-dichlorophenyl)-N-allylamino]-2-imidazoline as a cytoprotective agent.Type: GrantFiled: June 18, 1987Date of Patent: October 3, 1989Assignee: Boehringer Ingelheim KGInventors: Dietrich Arndts, Gunter Schingnitz, Ilse Streller, Alexander Walland
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4853402Abstract: 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 utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.Type: GrantFiled: February 26, 1987Date of Patent: August 1, 1989Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4847250Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.Type: GrantFiled: July 18, 1988Date of Patent: July 11, 1989Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Takeru Higuchi
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Patent number: 4800209Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of drug withdrawal, pre-menstrual tension and peri-menopausal flushing is disclosed.Type: GrantFiled: May 18, 1987Date of Patent: January 24, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Albert Sjoerdsma
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Patent number: 4789681Abstract: Compounds of the general formula I ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 and R.sub.3, which are the same or different, represent hydrogen or methyl, or taken together, form the amidine system to which an imidazole or imidazoline ring is bound;R.sub.4 is a linear or branched C.sub.1 -C.sub.10 alkyl group; cycloalkyl, aryl, aralkyl or hetaryl group;R.sub.5 is hydrogen or methyl;A is a propylene chain optionally substituted by one or two methyl groups in one or more of the positions thereof; a chain of formula --HN--CH.sub.2 --CH.sub.2 -- or of formula --N.dbd.CH--CH.sub.2 --; a 1,4-cyclohexylene group optionally substituted by one or more methyl groups; a 1,4- phenylene group optionally substituted by one or more halogen atoms, alkyl groups or C.sub.1 -C.sub.4 alkoxy group with the proviso that, when R.sub.4 is methyl or ethyl and R.sub.1 =R.sub.2 =R.sub.3 =R.sub.Type: GrantFiled: December 22, 1986Date of Patent: December 6, 1988Assignee: Italfarmaco S.p.A.Inventors: Giancarlo Sportoletti, Pietro Cremonesi, Moniquet Sarret
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Patent number: 4788189Abstract: Administering divided dose of oral Clonidine potentiated by an intramuscular tricyclic antidepressant alleviates the abstinence syndrome resulting from withdrawal of nicotine by smoking cessation. Patient response to the Clonidine/tricyclic serves as the basis for titrating the dosages of transdermal Clonidine and oral buspar administered daily for two weeks following the office visit. Behavioral counseling, supported by written and audio materials on diet, nutrition, exercise, stress management, and habit control, are provided to the patient. Following up support groups are also made available.Type: GrantFiled: February 29, 1988Date of Patent: November 29, 1988Inventor: Howard I. Glazer
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Patent number: 4785014Abstract: Disclosed is a method of treating cognitive decline in a normal aged primate by administering thereto a therapeutically effective amount of 2-[(2,6-dichlorophenyl)-amino]-2-imidazoline or a nontoxic, pharmaceutically acceptable salt thereof. Administration is preferably in amounts of at least about 0.001 mg/day.Type: GrantFiled: November 6, 1986Date of Patent: November 15, 1988Assignee: Yale UniversityInventors: Patricia S. Goldman-Rakic, Amy F. T. Arnsten
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Patent number: 4783457Abstract: The invention relates to an invertebrate pest controlling composition comprising an invertebrate pest-controlling amount of a non-formamidine octopamine against having substantial activity toward an octopamine receptor present in an invertebrate pest and a pesticidally inert carrier.Type: GrantFiled: March 17, 1987Date of Patent: November 8, 1988Assignee: The General Hospital CorporationInventor: James A. Nathanson
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Patent number: 4778807Abstract: Described are compounds of the formula: ##STR1## wherein Y denotes dimethylamino, methylpropynylamino, pyrrolidino, piperidino, or morpholino; R.sub.1 and R.sub.2 independently of each other denote hydrogen or loweralkyl; and X denotes loweralkyl, loweralkoxy, or halo; and n is and integer from 1 to 3 inclusive, or pharmaceutically acceptable salts thereof.The compounds exhibit antiarrhythmic activity without unwanted sympathomimetic effects.Type: GrantFiled: October 13, 1987Date of Patent: October 18, 1988Assignee: E. I. Du Pont de Nemours & CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4746660Abstract: The invention relates to a new process for the treatment of hypertension and thromboembolic diseases in humans by simultaneous administration of (.+-.)- or (-)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene hydrochloride on the one side, and 4,5-dihydro-6-[4-(1-imidazolyl)-phenyl]-5-methyl-3(2H)-pyridazinone or 4,5-dihydro-6-[4-(1-imidazolyl)-thien-2-yl]-5-methyl-3(2H)-pyridazinone, on the other side, as the active substances.Type: GrantFiled: January 21, 1987Date of Patent: May 24, 1988Assignee: A. Natternabb & CIE GmbHInventors: Jurgen Biedermann, Harald Borbe, Erich Graf, Gerd Hilboll, Gerrit Prop
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Patent number: 4742054Abstract: A method, and compositions, for treating an animal with an injured spinal cord, causing loss to sensory function and motor control, to regain such function and control. The method comprises the administration of at least 1 .alpha..sub.2 -adrenergic receptor agonist or a serotonergic receptor agonist or a dopaminergic receptor agonist, and preferably a combination with an anti-desensitization agent, such as a xanthine, a .beta.-adrenergic receptor agonist or a vascular skeletal muscle dilator. The composition comprises at least 1 receptor agonist and a second compound acting in conjunction therewith or preventing desensitization thereof.Type: GrantFiled: January 16, 1985Date of Patent: May 3, 1988Inventor: Nosrat E. Naftchi
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Patent number: 4728664Abstract: There is disclosed a substituted nitroimidazole compound, 1-methyl-2-methylsulfonyl-4-nitroimidazole which is an antiprotozoal and bactericidal compound with the unique and surprising property of being totally non-mutagenic and thus of a much higher degree of safety than is found with other nitroimidazoles. Compositions and methods for the antiprotozoal and bactericidal uses of such compounds are also disclosed.Type: GrantFiled: August 28, 1985Date of Patent: March 1, 1988Assignee: Merck & Co., Inc.Inventors: Edward S. Bagan, Gerald T. Miwa
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Patent number: 4721794Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: July 30, 1986Date of Patent: January 26, 1988Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4678775Abstract: A method of controlling a pest which comprises bringing into contact with the pest a pest-controlling amount of an agent selected from the group consisting of(1) a non-formamidine -p-octopamine agonist having substantial activity toward an octopamine receptor present in the pest;(2) a compound directly and substantially stimulating the enzyme, adenylate cyclase; and(3) a cyclic adenosine monophosphate (cAMP) analogue.Type: GrantFiled: May 1, 1984Date of Patent: July 7, 1987Inventor: James A. Nathanson
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Patent number: 4670459Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of drug withdrawal, pre-menstrual tension and peri-menopausal flushing is disclosed.Type: GrantFiled: January 23, 1986Date of Patent: June 2, 1987Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Albert Sjoerdsma
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Patent number: 4665095Abstract: Disclosed herein are alpha adrenergic and nasal decongestant compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, each being the same or different, are halogens, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: December 11, 1985Date of Patent: May 12, 1987Assignee: Abbott LaboratoriesInventors: Martin Winn, John F. Debernardis
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Patent number: 4663340Abstract: The present invention relates to imidazolines of general formula (I) ##STR1## and the addition salts formed therefrom with the pharmaceutically acceptable mineral or organic acids, possibly having their own specific pharmacological properties.The invention further relates to the preparation of these products, to their use as new medicines and to the medicinal compositions containing them.Type: GrantFiled: July 3, 1985Date of Patent: May 5, 1987Inventors: Henry Najer, Jean-Francois Giudicelli, Jean-Claude Dufour
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Patent number: 4661487Abstract: The invention relates to a new process for the treatment of hypertension and thromboembolic diseases in humans by simultaneous administration of (.+-.)- or (-)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene hydrochloride on the one side, and 4,5-dihydro-6-[4-(1-imidazolyl)-phenyl]-5-methyl-3(2H)-pyridazinone or 4,5-dihydro-6-[4-(1-imidazolyl)-thien-2-yl]-5-methyl-3(2H)-pyridazinone, on the other side, as the active substances.Type: GrantFiled: February 26, 1985Date of Patent: April 28, 1987Assignee: A. Nattermann & Cie GmbHInventors: Jurgen Biedermann, Harald Borbe, Erich Graf, Gerd Hilboll, Gerrit Prop
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Patent number: 4659714Abstract: Improved methods of anesthesia for mammals, especially humans, are provided wherein the prolonging effect upon local anesthesia which is exhibited by co-administration of vasoconstrictors, especially vasoconstrictors believed to act upon alpha adrenoreceptor sites on blood vessel walls, are provided. In accordance with a preferred embodiment, alpha adrenoreceptor blocking agents are aministered subsequent to the performance of surgery or dentistry under local anesthesia accomplished through co-administration of anesthesia and vasoconstrictor to cause reduction of prolonged anesthetic effect. Seriatim procedures are facilitated under local anesthesia through employment of the present invention. Improved patient aesthetics, diminution of self-inflicted trauma, and increased sensory feedback from patients are among the benefits conferred by the present invention.Type: GrantFiled: March 27, 1984Date of Patent: April 21, 1987Assignee: Dentsply, Ltd.Inventor: Stephen R. Watt-Smith
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Patent number: 4649150Abstract: Compounds of the formula ##STR1## wherein R represents substituents of various types;R.sub.1 and R.sub.2 are each independently hydrogen or lower alkyl;R.sub.3 represents substituents of various types; andR.sub.4 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halogen, cyano or carbamoyl;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics.Type: GrantFiled: May 16, 1984Date of Patent: March 10, 1987Assignee: Istituto de Angeli, S.p.A.Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Antonio Giachetti, Ferdinando Pagani
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Patent number: 4647557Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.Type: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
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Patent number: 4634705Abstract: Disclosed herein are adrenergic compounds represented by the formula ##STR1## wherein m is 0, 1 or 2; R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO.sub.2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R.sub.1, R.sub.2, R.sub.3 and R.sub.7 cannot simultaneously be hydrogen or halo, and provided that when one of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 is halo, the others cannot simultaneously be hydrogen and when two of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are halo, the other two cannot simultaneously be hydrogen and provided that R.sub.1 and R.sub.7 cannot simultaneously be methoxy each when R.sub.2 and R.sub.3 are hydrogen; R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.7 taken together can form a methylenedioxy or ethylenedioxy bridge; or R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.Type: GrantFiled: March 7, 1986Date of Patent: January 6, 1987Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Fatima Z. Basha
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Patent number: 4624960Abstract: The invention relates to the use of a substance as a sedative with an analgesic and bradycardiac effect in warm-blooded animals. The possible applications are, for example, in the field of veterinary medicine for general tranquilizing and for producing analgesia.Type: GrantFiled: October 11, 1985Date of Patent: November 25, 1986Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Otto Kern, Franz Wilhelm
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Patent number: 4610999Abstract: The present invention relates to 4-substituted .DELTA.2-imidazolinyl-thioethers and to intermediates and processes for their preparation. The components according to the invention are distinguished in particular by their platelet aggregation-inhibiting and hypotensive action.Type: GrantFiled: October 11, 1984Date of Patent: September 9, 1986Assignee: Hoechst AktiengesellschaftInventors: Gerhard Beck, Wilhelm Bartmann, Hans-Hermann Lau, Gunther Wess
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Patent number: 4611000Abstract: The present invention relates to 5-substituted .DELTA.2-imidazolinyl-thioethers and to intermediates and processes for their preparation. The components according to the invention are distinguished in particular by their platelet aggregation-inhibiting and hypotensive action.Type: GrantFiled: October 11, 1984Date of Patent: September 9, 1986Assignee: Hoechst AktiengesellschaftInventors: Gerhard Beck, Wilhelm Bartmann, Hans-Hermann Lau, Gunther Wess
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Patent number: 4598077Abstract: Amidine derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R.sub.1 and R.sub.2 together with an intermediary carbon atom and/or hetero atom may form a ring; X represents ##STR2## (wherein R.sub.8 represents a hydrogen atom, a lower alkyl group, or --CH.sub.2 COOR.sub.9, where R.sub.9 represents a hydrogen atom or a lower alkyl group; Z represents a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--); R.sub.3 represents a hydrogen or chlorine atom, methoxy group, nitro group, or amino group; Y represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, or --OCH.sub.2 --; R.sub.4 represents a hydrogen atom, methoxy group, benzoyl group, nitro group, or amino group; and R.sub.5, R.sub.6 and R.sub.Type: GrantFiled: December 14, 1984Date of Patent: July 1, 1986Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takuo Sato, Hiroyuki Kawamura, Takashi Yaegashi, Masateru Kurumi, Takuo Aoyama
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Patent number: 4596818Abstract: A compound of formula (I): ##STR1## or a salt thereof wherein R.sup.1 is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxyR.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxyR.sup.3 and R.sup.4 are the same or different and each is hydrogen, C.sub.1-4 alkyl or acyl andR.sup.5 is either (i) ##STR2## wherein R.sup.6, R.sup.7 and R.sup.8 are the same or different and each is selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, mercapto, mercaptoalkyl, amino, aminoalkyl, nitro, cyano, carboxy or a salt, ester or amide of carboxy provided that at least one of R.sup.6, R.sup.7 and R.sup.8 is other than hydrogen or (ii) ##STR3## wherein R.sup.9, R.sup.10 and R.sup.11 are the same or different and each is selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, mercapto, mercaptoalkyl, amino, aminoalkyl, nitro, cyano, carboxy or a salt, ester or amide of carboxyand X is --CH.sub.2 -- or --CH.dbd.CH-- or (iii) ##STR4## wherein R.sup.12 and R.sup.Type: GrantFiled: February 16, 1984Date of Patent: June 24, 1986Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Lee J. Beeley, Stephen F. Moss, Geoffrey H. Baker
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Patent number: 4588739Abstract: In human subjects accustomed to smoking tobacco the withdrawal symptoms associated with the cessation or reduction of tobacco smoking may be prevented by administering to the subject an effective amount of an alpha-2 adrenergic agonist such as clonidine hydrochloride for a suitable period of time.Alternatively, such withdrawal symptoms may be prevented by administering to such a person an effective amount of alprazolam.Type: GrantFiled: March 2, 1984Date of Patent: May 13, 1986Assignee: Research Foundation for Mental Hygiene, Inc.Inventor: Alexander H. Glassman
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Patent number: 4575510Abstract: The use of lofexidine and its pharmaceutically acceptable salts in alleviating the adverse symptoms of tobacco withdrawal is disclosed.Type: GrantFiled: October 3, 1984Date of Patent: March 11, 1986Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Albert Sjoerdsma
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Patent number: 4567181Abstract: Compounds of the formula: ##STR1## in which: R.sub.1 and R.sub.2 each represent, independently of one another, hydrogen, halogen, alkyl or alkoxy having from 1 to 4 carbon atoms, sulphonamide possibly substituted by an alkyl radical having from 1 to 4 carbon atoms; or together methylenedioxy, n is 0 or 1,in racemic form or in the form of optical isomers, and also their salts of addition with pharmaceutically acceptable acids. Useful in the treatment of ailments and/or conditions which are adrenoreceptor-related, such relationship being well known in the art.Type: GrantFiled: April 5, 1984Date of Patent: January 28, 1986Assignee: ADIR, s.a.r.l.Inventors: Charles Malen, Jean-Louis Peglion, Michel Laubie, Jean-Claude Poignant
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Patent number: 4559356Abstract: Compounds of the general formula (I) ##STR1## in which R.sub.1 is a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl, benzyl, phenethyl or methoxy group and R.sub.2 is a hydrogen atom or a methyl group, and their addition salts with pharmaceutically acceptable acids are useful, as such or in pharmaceutical compositions containing them in association with excipients, as .alpha..sub.2 -antagonists.Type: GrantFiled: March 16, 1984Date of Patent: December 17, 1985Assignee: SynthelaboInventors: Dennis Bigg, Jacques Menin
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Patent number: 4558063Abstract: Compounds A--B--C wherein A is 2 imidazolinyl or N-alkyl derivative thereof, B is oxygen, sulphur, CR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 are hydrogen or alkyl, or NR.sup.3 wherein R.sup.3 is hydrogen or alkyl, and C is a 5- or 6- membered carbo- or heterocyclic group having a nitrogen containing substituent and up to two other substituents, are useful in treatment of diarrhoea or scours. Certain compounds A--B--C are novel.Type: GrantFiled: February 27, 1984Date of Patent: December 10, 1985Assignee: Beecham Group p.l.c.Inventors: Lee J. Beeley, Peter M. Newsome
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Patent number: 4540705Abstract: 2-(2-Naphthalenyl)alkyl-4,5-dihydro-1H-imidazoles and -tetrahydropyrimidines, the corresponding 3,4-dihydronaphthalenyl and 1,2,3,4-tetrahydronaphthalenyl compounds; and the corresponding indene and indane derivatives, useful as antidepressant or diuretic agents, are prepared by reacting the appropriate 2-(cyanoalkyl)naphthalene or -indane derivative (or the corresponding ester or imino-ether) with an alkylenediamine.Type: GrantFiled: March 14, 1983Date of Patent: September 10, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4532135Abstract: A treatment method and substances have been found to reduce the risk of incurring renal damage or failure. Vasodilators useful for the treatment of hypertension have been found to lower cholesterol levels and prevent renal failure or damage. These substances are administered alone or in combination with other substances useful in the treatment of hyperlipidemia such as phenoxyacetic acid derivatives. Suitable vasodilators include: hydralazine hydrochloride and functionally similar agents such as endralazine, trimazosin, minoxidil, and diazoxide; prazosin hydrochloride and functionally similar agents such as doxazosin, triodazosin, phentolamine hydrochloride, phenoxybenzamine hydrochloride, benextramine, indoramine, and yohimbine; clonidine HCl and functionally similar agents such as guanabenz, guanfacine, lofexidine, and UK No. 14,304; labetalol and other combined alpha and beta blocking agents such as prizidolol and peroxidil.Type: GrantFiled: September 27, 1982Date of Patent: July 30, 1985Inventor: K. David G. Edwards
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Patent number: 4520014Abstract: Vasoconstrictor .alpha.-adrenergic agonists of formula (I)A-B-C (I)wherein, A is a 2-imidazoline group or a guanidine group; B is a chemical bond or a linking group one or two atoms in length; and C is a C.sub.6-10 mono- or bi-cyclic group which is either an aromatic group, a heteroaromatic group containing only one hetero-atom, or a group containing an aromatic moiety; and which group C may be substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or hydroxyl; or salts thereof, are useful in the treatment and prevention of diarrhoea in livestock. Compositions of these compounds are described.Type: GrantFiled: February 19, 1982Date of Patent: May 28, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan