Additional Hetero Ring Patents (Class 514/402)
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Patent number: 6090811Abstract: A novel use for the class of biologically active bis-heterocyclic, e.g., bis-indole alkaloid compounds, which have been named topsentins, bromotopsentins, homocarbonyltopsentins, nortopsentins, hamacanthins, bis-indole ethylamines, or dragmacidins, pharmaceutical compositions containing the compounds, methods of producing the compounds, and methods of using the compounds are disclosed. Specifically, the novel utility pertains to the anti-neurogenic inflammatory properties exhibited by the bis-indole compounds and their analogs.Type: GrantFiled: July 16, 1999Date of Patent: July 18, 2000Assignees: Harbor Branch Oceanographic Institution, Inc., Regents of the Univ. of CaliforniaInventors: Robert S. Jacobs, Shirley A. Pomponi, Sarath P. Gunasekera, Amy E. Wright
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Patent number: 6080769Abstract: The present invention relates to compounds of formula 1 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein Z, R, R.sup.3 and R.sup.4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to said mammal.Type: GrantFiled: December 28, 1998Date of Patent: June 27, 2000Assignee: Pfizer Inc.Inventors: Joseph P. Lyssikatos, Bingwei V. Yang
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Patent number: 5972964Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.Type: GrantFiled: October 22, 1997Date of Patent: October 26, 1999Assignee: H. Lundbeck A/SInventor: Jens Perregaard
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Patent number: 5965579Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.Type: GrantFiled: November 21, 1997Date of Patent: October 12, 1999Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5955462Abstract: A novel use for the class of biologically active bis-heterocyclic, e.g., bis-indole alkaloid compounds, which have been named topsentins, bromotopsentins, homocarbonyltopsentins, nortopsentins, hamacanthins, bis-indole ethylamines, or dragmacidins, pharmaceutical compositions containing the compounds, methods of producing the compounds, and methods of using the compounds are disclosed. Specifically, the novel utility pertains to the anti-neurogenicinflammatory properties exhibited by the bis-indole compounds and their analogs.Type: GrantFiled: October 31, 1997Date of Patent: September 21, 1999Assignees: Harbor Branch Oceanographic Institution, Inc., Regents of the Univ. of CaliforniaInventors: Robert S. Jacobs, Shirley A. Pomponi, Sarath P. Gunasekera, Amy E. Wright
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Patent number: 5952361Abstract: The present invention involves the novel use of various classes of drugs, such as H.sub.2 and H.sub.3 agonists, as erectogenic agents in the treatment of male and female sexual dysfunction.Type: GrantFiled: March 9, 1998Date of Patent: September 14, 1999Inventor: Cesar Roberto Dias Nahoum
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Patent number: 5939449Abstract: The invention relates to compounds of the formula: ##STR1## The compounds have great affinity for the neurotensin receptors.Type: GrantFiled: November 24, 1997Date of Patent: August 17, 1999Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5919488Abstract: Disclosed is a novel aqueous suspension of an antimicrobial compound having high stability of the suspension despite the use of such a very small amount of a suspending agent as not to cause any adverse influences on the inherent activity of the active ingredient. The suspending agent is a biocellulose as a microbial products of certain acetic bacteria which is not used in the prior art as a suspending agent in the prior art due to susceptibility to putrefaction while this defect of the biocellulose can be solved in the antimicrobial aqueous suspension by the use of an antimicrobial compound such as 2-methoxycarbonylamino benzimidazole, 2-pyridinethiol zinc-1-oxide and 2-(4-thiazolyl) benzimidazole.Type: GrantFiled: February 2, 1998Date of Patent: July 6, 1999Assignee: SOMAR CorporationInventor: Munetoshi Yamaji
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Patent number: 5914343Abstract: The present invention features compounds and methods for inhibiting hyper-proliferative cell growth. The compounds and method are preferably used to treat patients having a hyperproliferative cell disorder.Type: GrantFiled: November 14, 1997Date of Patent: June 22, 1999Assignee: Sugen, Inc.Inventor: Peng Cho Tang
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Patent number: 5912261Abstract: Carboxyalkyl heterocyclic derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (A): ##STR1## The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibiting aldehyde reductase.Type: GrantFiled: December 19, 1995Date of Patent: June 15, 1999Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Takayuki Kotani, Kaoru Okamoto, Yasuhiro Nagaki
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Patent number: 5910507Abstract: A method is provided for controlling the proliferation of molluscs in target habitat by applying to the habitat a compound or mixture of compounds which are amines, ethoxylated amines, quaternary amines, ethoxylated quaternary amines and cyclic amines.Type: GrantFiled: April 22, 1997Date of Patent: June 8, 1999Assignee: Electric Power Research Institute, Inc.Inventors: Billy D. Fellers, Arthur J. Freedman, Thomas M. Laronge
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Patent number: 5795880Abstract: The invention describes a method and composition for treating obesity or related disorders in animals using an anorectic agent and dehydroepiandrosterone (DHEA). The composition effectively diminishes caloric intake, may alter metabolism, weight gain, or a combination thereof.Type: GrantFiled: December 30, 1996Date of Patent: August 18, 1998Assignee: Louisiana State University Medical Center FoundationInventors: Frank Svec, Johnny Porter
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Patent number: 5780497Abstract: The present invention relates to new 2-Phenyl-1-?4-(amino-1-yl-alk-1-ynyl)benzyl!-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below.Type: GrantFiled: April 14, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran
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Patent number: 5780492Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: March 27, 1997Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Theresa M. Williams
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Patent number: 5756527Abstract: The present invention relates to imidazole derivatives having formula 1 ##STR1## wherein: R.sub.1 is selected from the group consisting of: mono-,di-,and tri-substituted phenyl or thienyl, the substituents are selected from the group consisting of:(i) substituted C.sub.1-6 alkyl, substituted C.sub.2-6 alkyloxy, wherein the substituents are selected from the group consisting of hydrogen or C.sub.1-6 alkoxy;(ii) C.sub.1-11 CO.sub.2 R.sub.5, trans-CH.dbd.CHCO.sub.2 R.sub.5, wherein R.sub.5 is C.sub.1-11 alkyl, or phenyl C.sub.1-11 alkyl;R.sub.2 and R.sub.3 are mono-, di, and tri-substituted phenyl wherein the substituents are independently selected from:(i) halo;(ii) C.sub.1-6 alkyl-amino, or di(C.sub.1-6 alkyl)amino, and R.sub.4 is hydrogen.These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents.Type: GrantFiled: April 25, 1997Date of Patent: May 26, 1998Assignee: Ontogen CorporationInventors: Adnan M. M. Mjalli, Sepehr Sarshar
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Patent number: 5731337Abstract: A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.Type: GrantFiled: October 3, 1995Date of Patent: March 24, 1998Assignee: AllerganInventors: Stephen A. Munk, Michael E. Garst, James A. Burke
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Patent number: 5721266Abstract: Methods of treating proliferative diseases or viral, inflammatory, allergic and cardiovascular diseases, and restenosis are disclosed. The present invention demonstrates the use of N,N'-piperazinylbis-?2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylene-bis?2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with a substrate regulatory protein. The present invention also demonstrates the use of pharmaceutical compositions employing N,N'-piperazinylbis?2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylenebis-?2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with substrate regulatory protein. The present invention also relates to novel N,N'-piperazinylbis?2-amino-1-imidazolin-2-yl)-2-imidazolines!.Type: GrantFiled: September 26, 1994Date of Patent: February 24, 1998Assignee: Warner-Lambert CompanyInventors: Stuart James Decker, David William Fry, James Marino Hamby, Alan Robert Saltiel
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Patent number: 5677283Abstract: Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine;R.sub.1 is selected from the group consisting of N-?4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-?4-(pyridyl)methyl!, N-?4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-?4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-?2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; andR.sub.8, R.sub.9 and R.sub.10 are as defined below.Type: GrantFiled: October 16, 1996Date of Patent: October 14, 1997Assignee: SanofiInventors: Roland E. Dolle, Jasbir Singh, David A. Whipple, Catherine Prouty, Prasad V. Chaturvedula, Stanley J. Schmidt, Mohamed M. A. Awad, Denton W. Hoyer, Tina Morgan Ross
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Patent number: 5662940Abstract: Improved biocidal composition and method for controlling biofouling and microorganism population levels in recirculating water systems such as cooling towers, swimming pools or spas is disclosed and claimed. The composition comprises a hypochlorite donor and a bromide ion donor in proportions selected to maintain a mole ratio of the sum of all bromine containing species to the sum of all hypohalite species in the recirculating water of about 0.2 to about 20. The method comprises introducing into the recirculating water a mixture or combination of a hypochlorite donor and a bromide ion donor in an amount sufficient to maintain a ratio of the sum of all bromine containing species to the sum of all species in the recirculating water in the range of about 0.2 to about 20.Type: GrantFiled: June 7, 1995Date of Patent: September 2, 1997Assignee: University of HoustonInventors: Terry V. T. Hight, Jack V. Matson, Lawrence F. Rakestraw, Zhihe Zhang, Thomas C. Kuechler
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Patent number: 5663167Abstract: A method for treating a serious psychotic mental illness includes the step of administering to a patient in need of such treatment a combination of (i) an .alpha..sub.2 -adrenergic receptor antagonist and (ii) a D.sub.2 dopamine receptor antagonist. A pharmaceutical composition useful in the novel method includes an effective amount of the combination of the foregoing two ingredients together with a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: September 2, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: David Pickar, Robert E. Litman, William Z. Potter
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Patent number: 5661172Abstract: The present invention relates to the use of efaroxan and derivatives for the treatment of Alzheimer's disease.Type: GrantFiled: January 11, 1996Date of Patent: August 26, 1997Assignee: Pierre Fabre MedicamentInventors: Francis Colpaert, Michael Briley, Thierry Imbert
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Patent number: 5610174Abstract: The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the following structure: ##STR1## wherein each of the substiutents for the compound is as defined in the specification.Type: GrantFiled: June 2, 1995Date of Patent: March 11, 1997Assignee: Synaptic Pharmaceutical CorporationInventors: Douglas A. Craig, Carlos C. Forray, Charles Gluchowski, Theresa A. Branchek
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Patent number: 5602163Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
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Patent number: 5527788Abstract: The invention describes a method and composition for treating obesity or related disorders in animals using an anorectic agent and dehydroepiandrosterone (DHEA). The composition effectively diminishes caloric intake, may alter metabolism, weight gain, or a combination thereof.Type: GrantFiled: January 18, 1994Date of Patent: June 18, 1996Assignee: Louisiana State Univ. Medical Center FoundationInventors: Frank Svec, Johnny Porter
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Patent number: 5519023Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.Type: GrantFiled: July 2, 1993Date of Patent: May 21, 1996Assignee: Adir et CompagnieInventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5492907Abstract: A method for treating a serious psychotic mental illness includes the step of administering to a patient in need of such treatment a combination of (i) an .alpha..sub.2 -adrenergic receptor antagonist and (ii) a D.sub.2 dopamine receptor antagonist, A pharmaceutical composition useful in the novel method includes an effective amount of the combination of the foregoing two ingredients together with a pharmaceutically acceptable carrier.Type: GrantFiled: December 9, 1992Date of Patent: February 20, 1996Assignee: The United States of America as represented by the Department of Health & Human ServicesInventors: David Pickar, Robert E. Litman, William Z. Potter
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Patent number: 5486532Abstract: Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.5 --,R.sub.1 represents halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl or linear or branched (C.sub.1 -C.sub.6) alkoxy,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.4 represents hydrogen or amino (unsubstituted or substituted)R.sub.5 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,or alternativelyR.sub.1 and R.sub.Type: GrantFiled: July 19, 1994Date of Patent: January 23, 1996Assignee: Adir et CompagnieInventors: Alex Cordi, Jean-Michel Lacoste, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes, Mark Millan
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Patent number: 5476670Abstract: Improved biocidal composition and method for controlling biofouling and microorganism population levels in recirculating water systems such as cooling towers, swimming pools or spas is disclosed and claimed. The composition comprises a hypochlorite donor and a bromide ion donor in proportions selected to maintain a mole ratio of the sum of all bromine containing species to the sum of all hypohalite species in the recirculating water of about 0.2 to about 20. The method comprises introducing into the recirculating water a mixture or combination of a hypochlorite donor and a bromide ion donor in an amount sufficient to maintain a ratio of the sum of all bromine containing species to the sum of all species in the recirculating water in the range of about 0.2 to about 20.Type: GrantFiled: June 13, 1994Date of Patent: December 19, 1995Assignee: The University of HoustonInventors: Terry V. T. Hight, Jack V. Matson, Lawrence F. Rakestraw, Zhihe Zhang, Thomas C. Kuechler
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Patent number: 5470867Abstract: Imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.Type: GrantFiled: October 17, 1994Date of Patent: November 28, 1995Assignee: Roussel-UclafInventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
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Patent number: 5464859Abstract: Compounds of formula (I): ##STR1## wherein: --X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,--R.sub.1 represents hydrogen or halogen or linear or branched (C.sub.1 -C.sub.6)alkoxy,--R.sub.2 represents linear or branched (C.sub.1 -C.sub.6)alkoxy or linear or branched (C.sub.1 -C.sub.6)alkylthio,their isomers and their addition salts with a pharmaceutically acceptable acid, and medicinal product containing the same are useful as .alpha..sub.1 adrenergic agonist.Type: GrantFiled: July 19, 1994Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Alex Cordi, Jean-Michel Lacoste, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
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Patent number: 5453435Abstract: A preservative system for ophthalmic solutions, particularly contact lens solutions, comprises:(a) chlorhexidine or a water-soluble salt thereof; and(b) polyhexamethylene biguanide or a water-soluble salt thereof.Type: GrantFiled: January 13, 1994Date of Patent: September 26, 1995Assignee: Polymer Technology CorporationInventors: Manohar K. Raheja, Stanley J. Wrobel
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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: 5430048Abstract: Spiro- [4H- 1 -benzopyran-4,4'-5'H-imidazol]-5'-ones of the Formula 1: ##STR1## wherein R.sup.1 is H, R.sup.2 F, Cl, Br, CF.sub.3, CF.sub.3 O, CN, NO.sub.2, R.sup.2 SO.sub.2, R.sup.2 NHSO.sub.2, R.sup.2 O, R.sup.2 CO, R.sup.2 OCO, or R.sup.2 NHCO. R.sup.2 is a C.sub.1 -C.sub.10 branched or linear alkyl, a C.sub.3-8 cycloalkyl, phenyl, or benzyl. X can be S, O, or NH. Both enantiomers are included in this invention as well as salts and tautomeric forms of these compounds. The subject compounds are useful in the treatment of hypertension, alopecia, and erectile dysfunction.Type: GrantFiled: February 10, 1994Date of Patent: July 4, 1995Assignee: The Upjohn CompanyInventor: Robert C. Gadwood
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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: 5393762Abstract: The present invention relates to a method of treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.Type: GrantFiled: June 4, 1993Date of Patent: February 28, 1995Assignee: Pfizer Inc.Inventors: Manoj C. Desai, John A. Lowe, III, John W. Watson
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Patent number: 5385919Abstract: The invention relates to compound of formula I: ##STR1## wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen or methyl; and R is 2-pyridyl, 3-pyridyl or --C.sub.6 H.sub.4 --R.sup.4, where R.sup.4 is hydrogen or hydroxy, or a non-toxic salt thereof, which are useful in the treatment of diabetes.Type: GrantFiled: May 5, 1993Date of Patent: January 31, 1995Assignee: Reckitt & Colman Products LimitedInventors: Christopher B. Chapleo, Gay P. Fagan
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Patent number: 5376659Abstract: The present invention relates to novel substituted guanidine and amidine compounds, their preparation and their use in the kill and control of fungal organisms which infest plants.Type: GrantFiled: January 14, 1992Date of Patent: December 27, 1994Assignee: DowElancoInventors: John W. Liebeschuetz, Michel J. Jung
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Patent number: 5346914Abstract: Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, inhibit the biosynthesis of leukotrienes.Type: GrantFiled: May 14, 1993Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Dorn, Wendy Lee
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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: 5310750Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 and R.sup.2 may each represent hydrogen or alkyl providing that at least one of R.sup.1 or R.sup.2 represents alkyl;R.sup.3 and R.sup.4 each represent hydrogen or R.sup.3 and R.sup.4 together represent a bond;n represents an integer 1 or 2;and m represents an integer 1 or 2; a composition containing such a compound and the method of using such compounds and compositions in medicine.Type: GrantFiled: March 1, 1991Date of Patent: May 10, 1994Assignee: Beecham Group P.L.C.Inventors: John M. Berge, Michael A. Cawthorne
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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: 5262430Abstract: The invention relates to novel substituted 2-imidazolines (I) having a lowering effect on blood glucose in mammals, to their preparation, to pharmaceutical compostions containing them and to their use.Type: GrantFiled: December 16, 1991Date of Patent: November 16, 1993Assignee: Novo Nordisk A/SInventors: Poul Borrevang, Henrik S. Andersen
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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: 5240930Abstract: A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine precursor or an inhibitor of aromatic L-amino acid decarboxylase, preferably carbidopa. The compositions can be used for treatment of endogenous depression or low blood pressure.Type: GrantFiled: February 22, 1991Date of Patent: August 31, 1993Assignee: National Research Development CorporationInventor: Saad Al-Damluji
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Patent number: 5206236Abstract: A method for treating malaria which comprises to an afflicted host patient a therapeutically effective amount of a compound have the structure of formula I: ##STR1## wherein X is O or NH; R.sub.1 is H or two R.sub.1 groups on the same amidine group together represents --(CH.sub.2).sub.m --, wherein m=2, 3 or 4; R.sub.2 is H, NH.sub.2, Cl, NO.sub.2 ; R.sub.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3 and n=2-6 or a pharmaceutically acceptable salt thereof provided that when X is O, both R.sub.2 and both R.sub.3 can not be H.Type: GrantFiled: September 5, 1991Date of Patent: April 27, 1993Inventors: Richard R. Tidwell, J. Dieter Geratz, James E. Hall, Dennis E. Kyle, Max Grogl, Kwasi A. Ohemeng
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Patent number: 5202320Abstract: This invention relates to a method for treating leishmaniasis which comprises administering to an afflicted host patient, a therapeutically effective amount of a compound having the following structure; ##STR1## wherein X is O or NH; R.sub.1 is H or two R.sub.1 of the same amidine group together represent --(CH.sub.2).sub.m -- wherein m=2, 3 or 4; R.sub.2 is H, NH.sub.2, OCH.sub.3, Cl or NO.sub.2 ; R.sub.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3 and n=2-6 or a pharmaceutical acceptable salt thereof provided that X is O both R.sub.2 and both R.sub.3 cannot be H.Type: GrantFiled: April 6, 1989Date of Patent: April 13, 1993Inventors: Richard R. Tidwell, J. Dieter Geratz, James E. Hall, Dennis E. Kyle, Max Grogl, Kwasi A. Ohemeng
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Patent number: 5202424Abstract: The present invention relates to a method and associated agents for measuring the presence and amount of advanced glycosylation endproducts in cells and fluids. The methods take advantage of the existence of receptors and receptor complexes for AGEs and include receptor-containing ligands comprising whole mesangial and other cells, mesangial cellular fragments and protein extracts therefrom. Competitive assays, sandwich assays and assays involving AGE antisera are disclosed. Numerous diagnostic applications are defined and test kits are also contemplated.Type: GrantFiled: August 23, 1991Date of Patent: April 13, 1993Assignee: The Rockefeller UniversityInventors: Helen Vlassara, Anthony Cerami
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Patent number: 5175182Abstract: The invention relates to acryloyl substituted pyrrole derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, --CN, --NO.sub.2, C.sub.1 -C.sub.4 alkyl, or a group ##STR2## R.sub.3 is hydrogen, halogen, --CN, or --NO.sub.2 ; each R.sub.4 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;A is a bond, a group ##STR3## or a group --NH--Het--CO--, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; andB is a group ##STR4## in which m is 1, 2 or 3 and each R.sub.5 is, independently, a C.sub.1 -C.sub.4 alkyl group, and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.Type: GrantFiled: November 5, 1990Date of Patent: December 29, 1992Assignee: Farmitalia Carlo Erba SrlInventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
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Patent number: RE35465Abstract: The present invention relates to a method and associated agents for the inhibition and treatment of protein aging in animals by stimulating the bodies of the animals to increase their recognition and affinity for advanced glycosylation end products. Specifically, the method contemplates the administration of certain agents such as advanced glycosylation endproducts, such endproducts as are bound to the carrier, monokines that stimulate phagocytic cells to increase their activity toward advanced glycosylation endproducts, and mixtures of these materials either alone, or in conjunction with other co-stimulatory agents. Numerous diagnostic and therapeutic applications are defined, and pharmaceutical compositions are also contemplated.Type: GrantFiled: May 9, 1995Date of Patent: February 25, 1997Assignee: The Rockefeller UniversityInventors: Helen Vlassara, Michael Brownlee, Anthony Cerami