Polycyclo Ring System Patents (Class 514/656)
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Patent number: 6245774Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12Type: GrantFiled: June 20, 1995Date of Patent: June 12, 2001Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
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Patent number: 6211171Abstract: When administered locally, tricyclic, second generation and third generation antidepressants, such as amitriptyline and desipramine, have been shown to produce analgesia in a subject having a site of local discomfort. The analgesic effect of such antidepressants, when administered locally is equal to that achieved by systemic administration and lasts longer. The invention provides compositions containing tricyclic, second generation, and third generation antidepressants for local administration, such as those formulated for topical application, or for injection in slow release delivery vehicles, and methods for their use for producing local analgesia.Type: GrantFiled: May 19, 1998Date of Patent: April 3, 2001Assignee: Dalhousie UniversityInventors: Jana Sawynok, Mike Esser, Allison Reid
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Patent number: 6143795Abstract: An aqueous solution of from about 1 mg/ml to about 5 mg/ml mitoxantrone.HCl, from about 0.01% wt. to about 0.15% wt. based on the solution of sodium edetate, sodium chloride, sodium acetate, and acetic acid, and a process for preparing the same.Type: GrantFiled: April 26, 1999Date of Patent: November 7, 2000Assignee: Arzneimittelwerk Dresden GmbHInventors: Katrin Moschner, Mario Weingart, Michael Pieroth, Wolfgang Morick, Elisabeth Wolf-Heuss
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Patent number: 6127422Abstract: A method of inhibiting an envelope virus selected from the group consisting of influenza bovine diarrheal, hepatitis C and tick borne encephalitis virus that udergoes hemagglutinin-mediated fusion with a host cell is disclosed which comprises administering to a virus-infected cell, a cell susceptible of infection or a mammal in need thereof, an effective amount of a compound as defined by Formula I in the specification.Type: GrantFiled: January 6, 1999Date of Patent: October 3, 2000Assignee: Eli Lilly and CompanyInventors: Joseph M. Colacino, William J. Hornback, Scott C. Mauldin, John E. Munroe, Joseph C. Tang
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Patent number: 6127426Abstract: Therapeutic compositions comprising 1,8-dihyroxy-9(10H) anthracenones substituted at position 10 thereof with phenylalkylidene or arylacyl blacking moieties, said compounds having substantial therapeutic activity and minimal inflammatory effect.Type: GrantFiled: November 19, 1998Date of Patent: October 3, 2000Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Klaus Muller, Wolfgang Wiegrebe, Dieter Gurster, Susanne Peters, nee Piwek
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Patent number: 6127424Abstract: Use of aryl-substituted cyclobutylalkylamines and their pharmaceutically suitable salts for treating obesity and its accompanying disorders are disclosed.Type: GrantFiled: April 27, 1998Date of Patent: October 3, 2000Assignee: Knoll AktiengesesllschaftInventors: Keith Frank Martin, David John Heal
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Patent number: 6103700Abstract: Compounds of formula (A), wherein R.sub.1, R.sub.2, R.sub.3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.Type: GrantFiled: December 24, 1998Date of Patent: August 15, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Tiziano Bandiera, Daniele Fancelli, Michele Caruso, Jacqueline Lansen, Antonino Suarato
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Patent number: 6069176Abstract: The present invention relates to phenylethanolamine compounds represented by general formula [I]: ##STR1## (where R.sub.1 represents hydrogen or halogen; R.sub.2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted with lower alkylaminocarbonyl which may be substituted with lower alkoxy, lower alkoxy substituted with cyclic aminocarbonyl of 4 to 6 carbon atoms, lower alkoxycarbonyl or carboxy; R.sub.3 represents hydrogen, hydroxy, lower alkoxy or lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups; R.sub.2 and R.sub.3 may be bonded to each other to form methylenedioxy substituted with carboxy or lower alkoxycarbonyl; and m and n are 0 or 1), and their pharmacologically acceptable salts, which have a potent .beta.3 adrenergic stimulating effect and high .beta.3 adrenergic receptor selectivity, as well as to processes for their production and intermediates in their production.Type: GrantFiled: April 24, 1998Date of Patent: May 30, 2000Assignee: Mitsubishi-Tokyo Pharmaceuticals, Inc.Inventors: Susumu Tsuchiya, Nobuyuki Yasuda, Toshifumi Matsumoto, Kozo Hiratsuka, Hiroyuki Iizuka, Atsusi Hukuzaki, Kouichi Matsunaga
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Patent number: 5981600Abstract: A compound selected from the group having the general formula ##STR1## wherein Z is a divalent moiety selected from linear or branched, saturated or unsaturated alkylene group, and the O.dbd.C(R) group contains one of a quaternary ammonium group and a sugar moiety, or the O.dbd.C(R) group is part of a neuraminic acid moiety, and their pharmacologically acceptable acid addition salts. Also a medical preparate with antineoplastic effects utilizing such a compound.Type: GrantFiled: August 26, 1997Date of Patent: November 9, 1999Inventor: Fikret Baykut
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Patent number: 5968987Abstract: The present invention relates to the use of halofantrine free base in the treatment of malarial infections. In particular, lipid-based formulations for oral and injectable use are disclosed.Type: GrantFiled: October 15, 1997Date of Patent: October 19, 1999Assignee: Smithkline Beecham p.l.c.Inventors: William Neil Charman, Christopher John Hamilton Porter
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Patent number: 5945566Abstract: New amino compounds of formula: ##STR1## wherein n and Y are as defined in the description, in racemic form or in the form of optical isomers.and addition salts thereof with pharmaceutically acceptable acids.Those compounds may be used as medicaments.Type: GrantFiled: April 9, 1998Date of Patent: August 31, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Mark Millan
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Patent number: 5922774Abstract: Method for repelling insect herbivores from plant surfaces and deterring them from feeding on plant surfaces by applying an aqueous dispersion of polycyclic quinone or precursor thereof to the foliage of the plant and/or to the surrounding soil in which the plant is rooted.Type: GrantFiled: October 22, 1996Date of Patent: July 13, 1999Assignee: DCV, Inc.Inventor: Anna Louise Winslow
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Patent number: 5880120Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.Type: GrantFiled: September 11, 1997Date of Patent: March 9, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventor: Mark W. Dudley
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Patent number: 5844004Abstract: Therapeutic compositions comprising 1,8-dihyroxy-9(10H) anthracenones substituted at position 10 thereof with phenylalkylidene or arylacyl blocking moieties, said compounds having substantial therapeutic activity and minimal inflammatory effect.Type: GrantFiled: March 27, 1997Date of Patent: December 1, 1998Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Klaus Muller, Wolfgang Wiegrebe, Dieter Gurster, Susanne Peters, nee Piwek
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Patent number: 5834521Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.Type: GrantFiled: August 5, 1996Date of Patent: November 10, 1998Assignee: Ortho Pharmaceutical CorporationInventors: John H. Dodd, Lisa A. Dixon, James L. Bullington, Charles F. Schwender
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Patent number: 5731313Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.Type: GrantFiled: April 4, 1996Date of Patent: March 24, 1998Assignee: Pharmacia & Upjohn S.P.A.Inventors: Antonino Suarato, Jacqueline Lansen, Michele Caruso, Dario Ballinari, Tiziano Bandiera
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Patent number: 5726208Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.Type: GrantFiled: October 11, 1996Date of Patent: March 10, 1998Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
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Patent number: 5705533Abstract: 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones, therapeutic compositions containing at least one of the 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones of the invention and methods of treating inflammatory conditions are provided.Type: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Klaus Muller, Hsu-Shan Huang, Wolfgang Wiegrebe
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Patent number: 5681846Abstract: The present invention is directed to improved pharmaceutical compositions employing paclitaxel that are formulated to increase stability and solubility. These improved formulations are useful in long-term, multi-day continuous infusion protocols, and have the advantage of reducing the number of infusion system breaks during the entire period of drug administration. Also disclosed are kits for use in preparing paclitaxel for long-term infusion and enhanced solubility.Type: GrantFiled: March 17, 1995Date of Patent: October 28, 1997Assignee: Board of Regents, The University of Texas SystemInventor: Lawrence A. Trissel
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Patent number: 5679715Abstract: The invention relates to a method of treating multiple sclerosis comprising administering an effective amount of (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine alone or in conjunction with an effective amount of interferon beta or an effective amount of amantadine.Type: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Inventor: Richard Y. Harris
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Patent number: 5629045Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.Type: GrantFiled: October 7, 1993Date of Patent: May 13, 1997Assignee: Richard L. VeechInventor: Richard L. Veech
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Patent number: 5618803Abstract: The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)-C.sub.r H.sub.2r -- wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.Type: GrantFiled: November 15, 1994Date of Patent: April 8, 1997Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5596020Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: December 7, 1994Date of Patent: January 21, 1997Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
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Patent number: 5567723Abstract: Compounds having the structural formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl; R.sup.1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.1 -C.sub.4 haloalkyl and nitro; and R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkoxyalkyl. The compounds of this invention are effective for controlling mites and nematodes.Type: GrantFiled: July 5, 1995Date of Patent: October 22, 1996Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Mark A. Dekeyser, Derek J. McPhee, Paul T. McDonald
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Patent number: 5538986Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.Type: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5478862Abstract: The invention is drawn to 17-oxo-15,16-seco-19-nor steroids which are useful as intermediates in the production of various 15,16-seco-19-nor progestins. These progestins display elevated progestational activity with a minimum of ancillary hormonal activity and are thus useful in the suppression of ovulation in the human female.Type: GrantFiled: May 13, 1994Date of Patent: December 26, 1995Assignee: SRI InternationalInventors: Richard H. Peters, Masato Tanabe
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Patent number: 5459163Abstract: A pharmaceutical composition for use in the treatment of chronic Graft-versus-host diseases as well as autoimmune diseases, in particular for the treatment of systemic lupus erythematosus containing as an active ingredient at least one compound of the formulae 1 or 2 ##STR1## the latter being present per se or in the form of a physiologically tolerable salt.The invention also relates to a dosage unit form of said pharmaceutical composition and a method of treating chronic Graft-versus host diseases as well as autoimmune diseases, in particular systemic lupus erythematosus.Type: GrantFiled: September 13, 1993Date of Patent: October 17, 1995Assignee: Hoechst AktiengesellschaftInventors: Robert R. Bartlett, Rudolph Schleyerbach, Friedrich-Johannes Kammerer
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Patent number: 5449720Abstract: The invention relates to the oral delivery of peptide and protein pharmaceuticals using the vitamin B.sub.12 (VB.sub.12) uptake system, with the delivery being amplified using polymers. More particularly, the invention concerns a complex having the general formula:(V--Q).sub.n --P--(Q'--A).sub.mwhere, V is a carrier which will bind to natural intrinsic factor (IF) selected from vitamin B.sub.12 or an analogue thereof, n is the molar substitution ratio of V in the complex, and is a number from 1.0 to about 10, P is a pharmaceutically acceptable polymer, A is a pharmaceutically active substance, m is the molar substitution ratio of A in the complex, and is a number greater than 1.0 to about 1000, Q and Q' are independently a covalent bond, or a spacer compound linking V, P and A by covalent bonds.Type: GrantFiled: May 24, 1993Date of Patent: September 12, 1995Assignee: Biotech Australia PTY LimitedInventors: Gregory J. Russell-Jones, Steven W. Westwood, Alison R. Gould, Bernard V. McInerney
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Patent number: 5389687Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: April 11, 1991Date of Patent: February 14, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 5364843Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are piperazinyl benzyl compounds such as 1-[.alpha.-(4-Chlorophenyl)-3-methoxybenzyl]-4-allylpiperazine dihydrochloride.Type: GrantFiled: June 10, 1992Date of Patent: November 15, 1994Assignee: Burroughs Wellcome Co.Inventor: Ann C. King
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Patent number: 5356935Abstract: A series of dihydrophenanthreneones and tetrahydrophenanthreneones are useful as inhibitors of 5.alpha.-reductase, and a series of hexahydrophenanthreneones are useful as intermediates for preparing such pharmaceuticals.Type: GrantFiled: December 13, 1993Date of Patent: October 18, 1994Assignee: Eli Lilly and CompanyInventors: James E. Audia, Thomas C. Britton, Patrick G. Spinazze
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Patent number: 5346897Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are acrivastine esters and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 10, 1992Date of Patent: September 13, 1994Assignee: Burroughs Wellcome Co.Inventor: Ann C. King
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Patent number: 5318768Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and a crystalline contrast agent in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.Type: GrantFiled: February 17, 1993Date of Patent: June 7, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Eugene R. Cooper
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Patent number: 5276053Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5252608Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.Type: GrantFiled: June 10, 1992Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Philippe Bey, Ian A. McDonald
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Patent number: 5208238Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are 2-(aminoethylamino) pyridines such as (E)-3-(6-(N-(2-Dimethylaminoethyl)-4-methoxybenzylamino)-2-pyridyl)acrylic acid.Type: GrantFiled: June 10, 1992Date of Patent: May 4, 1993Assignee: Burroughs Wellcome CompanyInventor: Ann C. King
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Patent number: 5204370Abstract: The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.Type: GrantFiled: November 5, 1990Date of Patent: April 20, 1993Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
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Patent number: 5190949Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are acrivastine esters and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 10, 1992Date of Patent: March 2, 1993Assignee: Burroughs Wellcome CompanyInventor: Ann C. King
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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: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5166173Abstract: A method of inhibiting cell infection by herpes simplex virus-1 or -2. The method includes contacting the virus with a macrocyclic chromotropic acid compound, in an amount effective to inhibit cell infectivity of the virus.Type: GrantFiled: January 29, 1991Date of Patent: November 24, 1992Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
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Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5071853Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 5055468Abstract: Certain bridged tricyclic amine compounds are described as being therapeutically effective in treatments of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Compounds of particular interest for use as neuroprotective agents are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R.sup.1 through R.sup.7 is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R.sup.Type: GrantFiled: October 30, 1989Date of Patent: October 8, 1991Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Patricia C. Contreras
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Patent number: 5053431Abstract: The present invention concerns compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further provides a method of inhibiting topoisomerase II using a compound having the structure: ##STR2## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a halogen, secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further concerns pharmaceutical compositions which comprise the above-identified compound or the acid salts thereof, and the use of the compound or compositions for treating a malignancy in a subject.Type: GrantFiled: June 26, 1990Date of Patent: October 1, 1991Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Kyoichi A. Watanabe, Masao Koyama, Ting-Chao Chou
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Patent number: 5036106Abstract: Methods are described to utilize synergistic interactions by various combinations of (1) bethanidine and various tricyclic compounds, (2) bethanidine and bretylium tosylate, (3) bretylium tosylate and various tricyclic compounds, and (4) debrisoquin sulfate and various tricyclic compounds, preferably in a single injectable or oral dosage form, to prevent, treat, and reduce the vulnerability of the heart to ventricular fibrillation and other ventricular arrhythmias in animals, both human and otherwise. Also, the use of bethanidine and bretylium tosylate in combination, and the use of debrisoquin sulfate for the resuscitation of pulseless beings, the use of debrisoquin sulfate for the suppression of ventricular fibrillation and ventricular tachycardia, and the use of bethanidine as an antidote to tricyclic antidepressant toxicity are disclosed.Type: GrantFiled: September 5, 1989Date of Patent: July 30, 1991Inventor: Marvin B. Bacaner
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Patent number: 4996235Abstract: The present invention provides 3,4-diphenylbutanamines capable of selectively inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: November 25, 1987Date of Patent: February 26, 1991Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong
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Patent number: 4966918Abstract: The present invention concerns compounds of the formula: ##STR1## wherein R.sup.1 hydrogen, a hydroxyl group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a halogen, a secondary amino group or a tertiary amino group; andZ is hydrogen or a halogen.The invention further concerns pharmaceutical compositions which comprises the above-identified compound or the acid salts thereof, and the use of the compound or compositions for treating a malignancy in a subject.Type: GrantFiled: January 27, 1989Date of Patent: October 30, 1990Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Kyoichi A. Watanabe, Masao Koyama
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Patent number: 4956361Abstract: The invention relates to combination products with a synergistic action and antidepressant activity, containing substances having antidepressant activity and compounds having antagonistic activity and belonging to the class of dihydropyridines, and to the use of the dihydropyridines in antidepressants.Type: GrantFiled: June 23, 1989Date of Patent: September 11, 1990Assignee: Troponwerke GmbH & Co. KGInventors: Jorg Traber, Harald Horstmann
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Patent number: 4908388Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.Type: GrantFiled: January 20, 1988Date of Patent: March 13, 1990Assignee: National Research Development CorporationInventors: John A. Pickett, Ewen D. M. Macaulay