The Aryl Ring Or Aryl Ring System And Amino Nitrogen Are Bonded Directly To The Same Acylic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 514/655)
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Patent number: 6022894Abstract: The present invention features calcilytic compounds. "Calcilytic compounds" refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: GrantFiled: April 4, 1997Date of Patent: February 8, 2000Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, Corp., SmithKline Beecham, PLCInventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6011069Abstract: There is disclosed a multidrug resistance inhibitor for overcoming a multidrug resistance of cancer, or an agent for enhancing the activity of anti-cancer agents, which comprises as an active ingredient a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein n is an integer of 5 to 12,R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen, and/or by methylenedioxy, with the proviso that R.sub.1 and R.sub.Type: GrantFiled: December 17, 1996Date of Patent: January 4, 2000Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Kohei Inomata, Toshihiro Takahashi, Hitoshi Inoue, Makoto Yanai, Hiroyuki Yamazaki, Masashi Suzuki, Tsutomu Takasawa, Kouji Kawamura, Norio Oshida, Hiroyuki Ikemoto, Takao Kishiye
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Patent number: 5985906Abstract: Use of a combination of the squalene epoxidase inhibitor terbinafine and an azole 14-alpha-methyldemethylase inhibitor (fluconazole or itraconazole) in mycotic infections caused by azole-resistant fungal strains, and corresponding pharmaceutical compositions, process and method.Type: GrantFiled: November 12, 1997Date of Patent: November 16, 1999Assignee: Novartis AGInventors: Josef Gottfried Meingassner, Neil Stewart Ryder
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Patent number: 5981599Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.Type: GrantFiled: April 30, 1997Date of Patent: November 9, 1999Assignee: NPS Pharmaceuticals, Inc.Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
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Patent number: 5939458Abstract: Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.Type: GrantFiled: September 22, 1997Date of Patent: August 17, 1999Inventors: James P. Henry, Gurpreet S. Ahluwalia
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Patent number: 5935998Abstract: Use of compounds of formula (I), wherein R has various significances, in free base form or in pharmaceutically acceptable salt form, as agents against H. pylori infection and associated diseases.Type: GrantFiled: January 6, 1998Date of Patent: August 10, 1999Assignee: Novartis AGInventors: Ivan James Dalton Lindley, Neil Stewart Ryder
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Patent number: 5922744Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.Type: GrantFiled: January 12, 1998Date of Patent: July 13, 1999Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Andrew Pate Owens
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Patent number: 5906996Abstract: 2,3,2 Tetramine (3,7-diazanonane-1,9-diamine) is propounded for the treatment of Parkinson's Disease and dementias characterized by mitochondrial damage in view of this compound's ability to completely neutralize the dopainine-depriving effect of MPTP in laboratory animals up to 12 hours post MPTP injection, and to retain partial protection at suboptimal tissue levels for up to 36 hours.Type: GrantFiled: August 21, 1997Date of Patent: May 25, 1999Inventor: Michael A. Murphy
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Patent number: 5898035Abstract: The present invention pertains to the field of pain management in medicine. Methods for treating reflex sympathetic dystrophy (including causalgia) are provided, in which a haloalkylamine a adrenergic blocking agent and a local anesthetic are administered to the affected limb by intravenous regional block. Formulations which can be used in these methods are also provided. In a preferred embodiment, phenoxybenzamine and either lidocaine or procaine are administered to the affected limb using a Bier block procedure.Type: GrantFiled: October 22, 1996Date of Patent: April 27, 1999Assignee: New York Medical CollegeInventors: Mario Inchiosa, Kamil Mustafa
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Patent number: 5877218Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: June 7, 1995Date of Patent: March 2, 1999Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Yaacov Herzig, Jeff Sterling, Alex Veinberg, Benjamin Sklarz, Ramy Lidor, Eliezer Bahar
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Patent number: 5827894Abstract: An anti-viral, anti-psoriasis or anti-retroviral therapy based on the administration of a compound having one of the formulae: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are alkyl having from 1 to 12 carbon atoms or hydrocarbyl aralkyl having up to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive; or(III) a salt thereof with a pharmaceutically acceptable acid.Type: GrantFiled: September 18, 1996Date of Patent: October 27, 1998Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5827870Abstract: Antimicrobial compositions useful in the treatment of microbial infections and as general cleansers are provided along with methods for their administration. The antimicrobial compositions are aqueous based and preferably contain a quaternary ammonium compound as a antimicrobial agent. The antimicrobial compositions also preferably contain a surfactant such as a cationic, nonionic, or amphoteric surfactant or mixtures thereof. A keratolytic agent, such as allantoin, is also preferably blended into the antimicrobial compositions. The antimicrobial compositions are ideally suited for subcutaneous, cutaneous, or mucosal membrane administration.Type: GrantFiled: December 3, 1996Date of Patent: October 27, 1998Assignee: Woodward Laboratories, Inc.Inventor: Daniel Frank Chodosh
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Patent number: 5792799Abstract: Methods of treating Parkinson's disease in a human by administering an effective amount of at least one monoamine oxidase (MAO) A inhibitor by a nasal, intrapulmonary or parenteral routes are disclosed. Reversible or irreversible MAO A inhibitors, or non-selective MAO inhibitors, can be used, and more than one MAO A inhibitor can be administered concurrently. The MAO A inhibitor can be administered in conjunction with other drugs, such as MAO B inhibitors.Type: GrantFiled: October 10, 1996Date of Patent: August 11, 1998Assignee: Athena Neurosciences, Inc.Inventor: Rivka Sherman-Gold
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Patent number: 5786386Abstract: The present invention provides an antibacterial and fungicidal agent containing an amino compound of formula (1) or a salt thereof. The invention also provides a method for imparting antibacterial and fungicidal properties to a variety of objects using the compound. ##STR1## wherein .phi. represents a phenyl group, a substituted phenyl group (wherein the substituents are 1-5 members arbitrarily selected from the group consisting of a hydroxyl group, halogen atoms, lower alkoxyl groups, trifluoromethyl group, an amino group, and a methylenedioxy group), or an imidazolyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; and R.sup.2 represents a C6-C12 alkyl group. The amino compound of formula (1) or a salt thereof exhibits excellent antibacterial effects and fungicidal effects, and when it is applied to a variety of articles used in industry, commodities, etc., enhanced antibacterial effects and fungicidal effects are obtained.Type: GrantFiled: July 15, 1996Date of Patent: July 28, 1998Assignee: Takasago International CorporationInventors: Kenya Ishida, Kazutoshi Sakurai
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Patent number: 5780505Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.Type: GrantFiled: July 7, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5763474Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: June 9, 1998Assignee: American Home Products CorporationInventors: David R. Herbst, Madelene M. Antane, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5756475Abstract: Isoprene derivatives of formula (I) ##STR1## wherein m is an integer of 0 to 3,n is an integer of 5 to 12,A is cyclo(C.sub.3 -C.sub.6)alkylene, phenylene, fluorenylene, pyrrolidinylene, piperazinylene, 9-aza-3-oxabicyclo?3.3.1!-nonylene,R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from the group consisting of hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen,X is a single bond or a divalent radical of --(CH.sub.2).sub.p NH--,p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. Those compounds are useful as multidrug resistance inhibitors for overcoming multidrug resistance of cancer and agents for enhancing an activity of anti-cancer agents.Type: GrantFiled: January 30, 1997Date of Patent: May 26, 1998Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Kohei Inomata, Toshihiro Takahashi, Hitoshi Inoue, Makoto Yanai, Hiroyuki Yamazaki, Masashi Suzuki, Tsutomu Takasawa, Kouji Kawamura, Norio Oshida, Hiroyuki Ikemoto, Takao Kishiye
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Patent number: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5753714Abstract: This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.Type: GrantFiled: March 15, 1994Date of Patent: May 19, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: David M. Stemerick, Alan J. Bitonti, Michael L. Edwards, Peter P. McCann, Albert Sjoerdsma
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Patent number: 5750574Abstract: A compound of the general formula (I) ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 is F, perfluoroalkyl group of 1 to 10 carbon atoms or perfluoroalkoxy of 1 to 10 carbon atoms; or a pharmaceutically acceptable salt thereof relax smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: May 12, 1998Assignee: American Home Products CorporationInventor: Adam M. Gilbert
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Patent number: 5719192Abstract: A method of use comprising administering terbinafine for the primary and secondary prophylaxis and treatment of Pneumocystis carinii pneumonia, including oral administration of terbinafine at does of 3 to 20 mg/kg/day, to a subject suffering from this type of pneumonia is disclosed.Type: GrantFiled: September 12, 1995Date of Patent: February 17, 1998Assignee: Mendes s.r.l.Inventors: Claudio De Simone, Carlo Contini, Sonia Tzoutzoglou
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Patent number: 5677350Abstract: The present invention relates to the inhibition of cancer cell growth, proliferation, and metastasis by contacting cells with an N,N'-dibenzyl .alpha.,.omega.-diaminoalkane, a derivative of naturally-occurring putrescine. More specifically, the present invention relates to the treatment of cancer in humans by administration of a cancer cell growth-inhibiting amount of an N,N'-dibenzyl .alpha.,.omega.-diaminoalkane to a human cancer patient.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Wisconsin Alumni Research FoundationInventor: Benjamin J. Frydman
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Patent number: 5677351Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5656671Abstract: Polyamines having the formula: ##STR1## wherein R.sup.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; ora salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5648396Abstract: A method and composition are utilizing the pure R(-) isomer of fluoxetine which is a potent antidepressant and appetite suppressant substantially free of adverse effects. In addition, a method and composition are disclosed utilizing the pure R(-) isomer of fluoxetine which is useful to treat migraine headaches, pain, in particular chronic pain, psychoactive substance abuse disorders and obsessive compulsive disorders.Type: GrantFiled: June 7, 1995Date of Patent: July 15, 1997Assignee: Sepracor Inc.Inventors: James W. Young, Timothy J. Barberich, Martin H. Teicher
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Patent number: 5637324Abstract: A medical food having the below listed components is administered for several days as the sole source or as a substantial source of the daily caloric intake of a patient suffering from metabolic poisoning: 45 to 65% protein concentrate; 2.5 to 17.5% of grain syrup solids containing 50% dextran; 2.5 to 17.5% of grain syrup solids containing 50% of maltose; 3 to 12% of oil containing 20% of oleic acid, 1 to 11% medium chain triglycerides; magnesium ions; buffering agent; soluble calcium salt; ascorbic acid; 0.40 to 0.65% of .beta. carotene; D-.alpha.-tocopherol; chromium ions in the trivalent or hexavalent form, 0.008 to 0.022% glutathione, 0.08 to 0.22% N-acetylcysteine; L-lysine hydrochloride; 0.08 to 0.22% L-threonine, and 0.08 to 0.22% of L-cysteine.Type: GrantFiled: June 6, 1995Date of Patent: June 10, 1997Inventor: Jeffrey S. Bland
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Patent number: 5629023Abstract: A medical food having the below listed components is administered for several days as the sole source or as a substantial source of the daily caloric intake of a patient suffering from metabolic poisoning: 45 to 65% protein concentrate; 2.5 to 17.5% of grain syrup solids containing 50% dextran; 2.5 to 17.5% of grain syrup solids containing 50% of maltose; 3 to 12% of oil containing 20% of oleic acid, 1 to 11% medium chain triglycerides; magnesium ions; buffering agent; soluble calcium salt; ascorbic acid; 0.40 to 0.65% of .beta. carotene; D-.alpha.-tocopherol; chromium ions in the trivalent or hexavalent form, 0.008 to 0.022% glutathione, 0.08 to 0.22% N-acetylcysteine; L-lysine hydrochloride; 0.08 to 0.22% L-threonine, and 0.08 to 0.22% of L-cysteine.Type: GrantFiled: November 22, 1993Date of Patent: May 13, 1997Inventor: Jeffrey S. Bland
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Patent number: 5605916Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.Type: GrantFiled: March 6, 1995Date of Patent: February 25, 1997Assignee: Astra ABInventors: Ronald C. Griffith, James J. Napier
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Patent number: 5554656Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.Type: GrantFiled: February 25, 1994Date of Patent: September 10, 1996Assignee: Reckitt & Colman Inc.Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
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Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes
Patent number: 5552444Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: March 14, 1995Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus -
Patent number: 5519033Abstract: The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of azabiaglo and related compounds.Type: GrantFiled: May 31, 1994Date of Patent: May 21, 1996Assignee: Pfizer Inc.Inventors: Terry J. Rosen, Manoj C. Desai, John A. Lowe, III
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Patent number: 5508306Abstract: This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z.sup.1 and Z.sup.2 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, OH, F, Cl, Br, I, NO.sub.2, CN, SO.sub.2 NHR.sup.3, NR.sup.4.sub.2, CONR.sup.3.sub.2, COR.sup.5 ; where each R.sup.1 and R.sup.2 is independently H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH.sub.2, NR.sup.4, S, S.dbd.O, SO.sub.2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where R.sup.4 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or COR.sup.3 ; and where R.sup.5 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl, C.sub.1 -C.sub.6 straight or branched chain alkoxy or OH.Type: GrantFiled: September 9, 1993Date of Patent: April 16, 1996Assignee: Synaptic Pharmaceutical CorporationInventors: George Chiu, Charles Gluchowski
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Patent number: 5508280Abstract: This invention relates to novel derivatives of 5H-dibenzo (a,d)cycloheptenes, to the processes for their preparation, to their muscarinic receptor antagonist properties and to their end-use application for treating Parkinson's Disease, tardive dyskinesia, and motion sickness.Type: GrantFiled: January 30, 1995Date of Patent: April 16, 1996Assignee: Merrell Pharmaceuticals, Inc.Inventors: Marcel Hibert, Luc Van Hijfte, Mary Richards, Paul Moser
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Patent number: 5484588Abstract: There are provided attracting and ingestion-stimulating agents for cockroach comprising as the active ingredient one or more compounds represented by the formula ##STR1## wherein R represents an amino group or an aminomethyl group. The attracting and ingestion-stimulating agents for cockroach exhibit a very potent attracting and ingestion-stimulating activity in the known species of house cockroach, both male and female.Type: GrantFiled: February 2, 1993Date of Patent: January 16, 1996Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kazumasa Ogino, Haruo Shimamura, Kazuyuki Tomisawa, Fumio Urushizaki, Masami Nemoto, Tuguchika Yoshida
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Patent number: 5462970Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn is an integer from 3 to 6, inclusive; or(IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.Type: GrantFiled: January 3, 1995Date of Patent: October 31, 1995Assignee: University of Florida Research Foundation, Inc.Inventors: Raymond J. Bergeron, Jr., Charles A. Sninsky
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Patent number: 5455276Abstract: Pharmaceutical compositions for treating psychiatric disorders are provided. The compositions include 2-phenylethylamine ("PEA") and at least one inhibitor of monoamine oxidase B. Methods for the treatment of psychiatric disorders, including depression, using the disclosed pharmaceutical compositions are also provided.Type: GrantFiled: May 20, 1993Date of Patent: October 3, 1995Inventor: Hector C. Sabelli
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Patent number: 5434179Abstract: An aminoketone compound of the formula ##STR1## wherein ring A' means a five through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O, S, N, as the ring-constituents; R.sup.1' means a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.2' means a hydrogen atom or a lower alkyl group; R.sup.3' means an aromatic group which may be substituted; R.sup.4' means a hydrogen atom, a lower alkyl group or aromatic group which may be substituted; n' means an integer of 2 to 7, or a salt thereof, is useful as an cholinesterase inhibitors and a cerebral function ameliorating agent.Type: GrantFiled: March 22, 1994Date of Patent: July 18, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
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Patent number: 5430044Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.Type: GrantFiled: July 16, 1992Date of Patent: July 4, 1995Assignee: Fisons CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 5428065Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 27, 1995Assignee: Lilly Industries LimitedInventors: Barry P. Clark, Graham H. Timms
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Patent number: 5397385Abstract: An anti-fouling coating utilizes capsaicin as an anti-fouling agent. In a preferred embodiment, finely divided capsaicin, an oleoresin capsaicin liquid solution, or crystalized capsaicin, is mixed with a suitable corrosion resistant epoxy resin which is then mixed with a hardening catalyst and applied to the surface to be treated. In some applications, finely divided inert particles may be added to impart additional desirable characteristic to the surface. The capsaicin constituent used in the coating preferably has a rating of from about 100,000 to about 1,500,000 Scoville Heat Units. The capsaicin may be mixed with a silicon dioxide and then solubilized into a free-flowing homogeneous liquid oleoresin composition by adding a solvent to increase solubility and facilitate mixing. The capsaicin may also be formed into crystals which are mixed with the coating material.Type: GrantFiled: March 28, 1994Date of Patent: March 14, 1995Inventor: James L. Watts
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Patent number: 5393786Abstract: Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.Type: GrantFiled: December 2, 1993Date of Patent: February 28, 1995Assignee: Eli Lilly and CompanyInventors: James A. Clemens, Jill A. Panetta
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Patent number: 5387614Abstract: A method of stimulation salivary secretion comprising oral administration of certain sigma ligands which may be generally described as N,N-disubstituted phenylalkylamines.Type: GrantFiled: July 27, 1993Date of Patent: February 7, 1995Assignee: University of Iowa Research FoundationInventors: Ronald D. Schoenwald, Charles F. Barfknecht
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Patent number: 5380761Abstract: An anhydrous transdermal composition is disclosed comprising in a 20 to 100% lyotropic liquid crystalline arrangement:5 to 15 weight % of optically active or racemic N-methyl-N-(1-phenyl-2-propyl)-2-propynylamine or N-methyl-N-{1-(4-fluorophenyl)-2-propyl}-2-propynylamine or a pharmaceutically acceptable salt thereof;40 to 70% by weight of liquid polyethylene glycol;10 to 20% by weight of solid polyethylene glycol;2 to 30% by weight of a nonionic surface active agent;2 to 20% by weight of propylene glycol, and if desired,0.5 to 2% by weight of a polymer, the a value of which is greater than 0.6, andoptionally, in an amount needed up to 100% an emulsifying agent.Type: GrantFiled: October 20, 1993Date of Patent: January 10, 1995Assignee: Chinoin Gyogyszer- ES Vegyeszeti Termekek Gyara RT.Inventors: Szabo Anna Z., Gabriella Szabo nee Ujhelyi, Antal Toth, Tamas Szuts, Kalman Magyar, Jozsef Lengyel, Janos Pinter, Anna Szekely, Andras Szego, Katalin Marmarosi nee Kellner
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Patent number: 5354782Abstract: The present invention relates to certain polyamine phenols which are useful as radioprotective agents.Type: GrantFiled: August 30, 1993Date of Patent: October 11, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael L. Edwards, Ronald D. Snyder
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Patent number: 5334628Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.Type: GrantFiled: December 31, 1992Date of Patent: August 2, 1994Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
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Patent number: 5300527Abstract: This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula ##STR1## where Ar is aryl of the formula ##STR2## where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF.sub.3, NO.sub.2 and u is an integer of 1 to 3; X and Y are independently CH.sub.2 --, --CF.sub.2 -- or --CHF--; Z and W are independently --CH.sub.2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1; R.sub.1 is H or loweralkyl; R.sub.2 and R.sub.3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: October 13, 1992Date of Patent: April 5, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: R. Richard L. Hamer, Brian Freed, Richard C. Allen
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Patent number: 5294638Abstract: Pharmacologically active compounds corresponding to the general formula I: ##STR1## wherein m represents 1-4,n represents 2-5,R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy or halogen, orR.sup.2 and R.sup.3 are linked to adjacent carbon atoms and together form an alkylenedioxy group with 1-2 carbon atoms,R.sup.4 represents a saturated monocyclic or bicyclic hydrocarbon radical derived from terpenes and having 10 or 11 hydrocarbon atoms, andZ represents oxygen, an N--R.sup.5 group, wherein R.sup.5 is lower alkyl, or if R.sup.4 is a dihydronopyl radical, Z may also be sulfur,and their acid addition salts.Type: GrantFiled: January 19, 1993Date of Patent: March 15, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Insa Hell, Ulf Preuschoff, Hermann Kraehling, Samuel David, Ivan Ban, Marie-Odile Christen
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5286753Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: April 16, 1993Date of Patent: February 15, 1994Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
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Patent number: 5281623Abstract: Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.Type: GrantFiled: August 27, 1990Date of Patent: January 25, 1994Assignee: Eli Lilly and CompanyInventors: James A. Clemens, Jill A. Panetta