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)
  • Patent number: 6022894
    Abstract: 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: Grant
    Filed: April 4, 1997
    Date of Patent: February 8, 2000
    Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, Corp., SmithKline Beecham, PLC
    Inventors: 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
  • Patent number: 6011069
    Abstract: 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: Grant
    Filed: December 17, 1996
    Date of Patent: January 4, 2000
    Assignee: 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
  • Patent number: 5985906
    Abstract: 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: Grant
    Filed: November 12, 1997
    Date of Patent: November 16, 1999
    Assignee: Novartis AG
    Inventors: Josef Gottfried Meingassner, Neil Stewart Ryder
  • Patent number: 5981599
    Abstract: 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: Grant
    Filed: April 30, 1997
    Date of Patent: November 9, 1999
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
  • Patent number: 5939458
    Abstract: Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: August 17, 1999
    Inventors: James P. Henry, Gurpreet S. Ahluwalia
  • Patent number: 5935998
    Abstract: 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: Grant
    Filed: January 6, 1998
    Date of Patent: August 10, 1999
    Assignee: Novartis AG
    Inventors: Ivan James Dalton Lindley, Neil Stewart Ryder
  • Patent number: 5922744
    Abstract: 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: Grant
    Filed: January 12, 1998
    Date of Patent: July 13, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Andrew Pate Owens
  • Patent number: 5906996
    Abstract: 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: Grant
    Filed: August 21, 1997
    Date of Patent: May 25, 1999
    Inventor: Michael A. Murphy
  • Patent number: 5898035
    Abstract: 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: Grant
    Filed: October 22, 1996
    Date of Patent: April 27, 1999
    Assignee: New York Medical College
    Inventors: Mario Inchiosa, Kamil Mustafa
  • Patent number: 5877218
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: March 2, 1999
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Yaacov Herzig, Jeff Sterling, Alex Veinberg, Benjamin Sklarz, Ramy Lidor, Eliezer Bahar
  • Patent number: 5827894
    Abstract: 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: Grant
    Filed: September 18, 1996
    Date of Patent: October 27, 1998
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron
  • Patent number: 5827870
    Abstract: 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: Grant
    Filed: December 3, 1996
    Date of Patent: October 27, 1998
    Assignee: Woodward Laboratories, Inc.
    Inventor: Daniel Frank Chodosh
  • Patent number: 5792799
    Abstract: 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: Grant
    Filed: October 10, 1996
    Date of Patent: August 11, 1998
    Assignee: Athena Neurosciences, Inc.
    Inventor: Rivka Sherman-Gold
  • Patent number: 5786386
    Abstract: 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: Grant
    Filed: July 15, 1996
    Date of Patent: July 28, 1998
    Assignee: Takasago International Corporation
    Inventors: Kenya Ishida, Kazutoshi Sakurai
  • Patent number: 5780505
    Abstract: 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: Grant
    Filed: July 7, 1997
    Date of Patent: July 14, 1998
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5763474
    Abstract: 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: Grant
    Filed: July 7, 1997
    Date of Patent: June 9, 1998
    Assignee: American Home Products Corporation
    Inventors: David R. Herbst, Madelene M. Antane, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5756475
    Abstract: 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: Grant
    Filed: January 30, 1997
    Date of Patent: May 26, 1998
    Assignee: 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
  • Patent number: 5753715
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: May 19, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
  • Patent number: 5753714
    Abstract: 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: Grant
    Filed: March 15, 1994
    Date of Patent: May 19, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: David M. Stemerick, Alan J. Bitonti, Michael L. Edwards, Peter P. McCann, Albert Sjoerdsma
  • Patent number: 5750574
    Abstract: 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: Grant
    Filed: July 7, 1997
    Date of Patent: May 12, 1998
    Assignee: American Home Products Corporation
    Inventor: Adam M. Gilbert
  • Patent number: 5719192
    Abstract: 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: Grant
    Filed: September 12, 1995
    Date of Patent: February 17, 1998
    Assignee: Mendes s.r.l.
    Inventors: Claudio De Simone, Carlo Contini, Sonia Tzoutzoglou
  • Patent number: 5677350
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Benjamin J. Frydman
  • Patent number: 5677351
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5656671
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: August 12, 1997
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5648396
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: July 15, 1997
    Assignee: Sepracor Inc.
    Inventors: James W. Young, Timothy J. Barberich, Martin H. Teicher
  • Patent number: 5637324
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: June 10, 1997
    Inventor: Jeffrey S. Bland
  • Patent number: 5629023
    Abstract: 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: Grant
    Filed: November 22, 1993
    Date of Patent: May 13, 1997
    Inventor: Jeffrey S. Bland
  • Patent number: 5605916
    Abstract: 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: Grant
    Filed: March 6, 1995
    Date of Patent: February 25, 1997
    Assignee: Astra AB
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 5554656
    Abstract: 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: Grant
    Filed: February 25, 1994
    Date of Patent: September 10, 1996
    Assignee: Reckitt & Colman Inc.
    Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
  • Patent number: 5552444
    Abstract: 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: Grant
    Filed: March 14, 1995
    Date of Patent: September 3, 1996
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5519033
    Abstract: 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: Grant
    Filed: May 31, 1994
    Date of Patent: May 21, 1996
    Assignee: Pfizer Inc.
    Inventors: Terry J. Rosen, Manoj C. Desai, John A. Lowe, III
  • Patent number: 5508306
    Abstract: 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: Grant
    Filed: September 9, 1993
    Date of Patent: April 16, 1996
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: George Chiu, Charles Gluchowski
  • Patent number: 5508280
    Abstract: 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: Grant
    Filed: January 30, 1995
    Date of Patent: April 16, 1996
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Marcel Hibert, Luc Van Hijfte, Mary Richards, Paul Moser
  • Patent number: 5484588
    Abstract: 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: Grant
    Filed: February 2, 1993
    Date of Patent: January 16, 1996
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Kazumasa Ogino, Haruo Shimamura, Kazuyuki Tomisawa, Fumio Urushizaki, Masami Nemoto, Tuguchika Yoshida
  • Patent number: 5462970
    Abstract: 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: Grant
    Filed: January 3, 1995
    Date of Patent: October 31, 1995
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Raymond J. Bergeron, Jr., Charles A. Sninsky
  • Patent number: 5455276
    Abstract: 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: Grant
    Filed: May 20, 1993
    Date of Patent: October 3, 1995
    Inventor: Hector C. Sabelli
  • Patent number: 5434179
    Abstract: 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: Grant
    Filed: March 22, 1994
    Date of Patent: July 18, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
  • Patent number: 5430044
    Abstract: 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: Grant
    Filed: July 16, 1992
    Date of Patent: July 4, 1995
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 5428065
    Abstract: 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: Grant
    Filed: September 27, 1994
    Date of Patent: June 27, 1995
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, Graham H. Timms
  • Patent number: 5397385
    Abstract: 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: Grant
    Filed: March 28, 1994
    Date of Patent: March 14, 1995
    Inventor: James L. Watts
  • Patent number: 5393786
    Abstract: Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.
    Type: Grant
    Filed: December 2, 1993
    Date of Patent: February 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: James A. Clemens, Jill A. Panetta
  • Patent number: 5387614
    Abstract: A method of stimulation salivary secretion comprising oral administration of certain sigma ligands which may be generally described as N,N-disubstituted phenylalkylamines.
    Type: Grant
    Filed: July 27, 1993
    Date of Patent: February 7, 1995
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 5380761
    Abstract: 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: Grant
    Filed: October 20, 1993
    Date of Patent: January 10, 1995
    Assignee: 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
  • Patent number: 5354782
    Abstract: The present invention relates to certain polyamine phenols which are useful as radioprotective agents.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: October 11, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael L. Edwards, Ronald D. Snyder
  • Patent number: 5334628
    Abstract: 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: Grant
    Filed: December 31, 1992
    Date of Patent: August 2, 1994
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
  • Patent number: 5300527
    Abstract: 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: Grant
    Filed: October 13, 1992
    Date of Patent: April 5, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: R. Richard L. Hamer, Brian Freed, Richard C. Allen
  • Patent number: 5294638
    Abstract: 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: Grant
    Filed: January 19, 1993
    Date of Patent: March 15, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Insa Hell, Ulf Preuschoff, Hermann Kraehling, Samuel David, Ivan Ban, Marie-Odile Christen
  • Patent number: 5288749
    Abstract: 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: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5286753
    Abstract: 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: Grant
    Filed: April 16, 1993
    Date of Patent: February 15, 1994
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5281623
    Abstract: Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: January 25, 1994
    Assignee: Eli Lilly and Company
    Inventors: James A. Clemens, Jill A. Panetta