Bicyclo Ring System Patents (Class 514/657)
  • Patent number: 6159971
    Abstract: The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT.sub.1B antagonist or partial agonist having the formula I ##STR1## wherein X is CH.sub.2, O; Y is CONH, NHCO;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen;R.sub.3 is ##STR2## R.sub.4 and R.sub.5 independently are H or C.sub.1 -C.sub.4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: December 12, 2000
    Assignee: Astrazeneca AB
    Inventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
  • Patent number: 6147072
    Abstract: The invention relates to a method of treating psychosis, acute mania, mild anxiety states or depression in combination with psychotic episodes by administering to a patient a combination of an atypical antipsychotic and a serotonin reuptake inhibitor.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: November 14, 2000
    Assignee: Eli Lilly and Company
    Inventors: Franklin P. Bymaster, Kenneth W. Perry, Gary D. Tollefson
  • Patent number: 6127424
    Abstract: Use of aryl-substituted cyclobutylalkylamines and their pharmaceutically suitable salts for treating obesity and its accompanying disorders are disclosed.
    Type: Grant
    Filed: April 27, 1998
    Date of Patent: October 3, 2000
    Assignee: Knoll Aktiengesesllschaft
    Inventors: Keith Frank Martin, David John Heal
  • Patent number: 6114394
    Abstract: The present invention relates to polyamine derivatives of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof which are useful as radioprotective agents. It relates also to the use of polyamines of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NH-(CH.sub.2).sub.m -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof as radioprotective agents.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: September 5, 2000
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Michael L. Edwards, Ronald D. Snyder
  • Patent number: 6107345
    Abstract: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: August 22, 2000
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
  • Patent number: 6103760
    Abstract: Left ventricular dysfunction is treated by a process, comprising:administering to a subject suffering from left ventricular remodeling a therapeutically effective amount of 5,6-dihydroxy-2-methylaminotetralin, or 5,6-diisobutyroyl-oxy-2-methyl-aminotetralin, or a pharmaceutically acceptable salt thereof in combination with an angiotensin-converting enzyme inhibitor.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: August 15, 2000
    Assignee: Chiesi Farmaceuticals S.p.A.
    Inventors: Paolo Chiesi, Stefano Bongrani, Roberta Razzetti, Maurizio Civelli, Alberto Umile
  • Patent number: 6075044
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: June 13, 2000
    Assignee: The Regents of the University of California
    Inventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
  • Patent number: 6071918
    Abstract: The invention relates to a method of treating alcoholism and alcohol dependence in a mammal comprising administering to the mammal a therapeutically effective amount of a synergistic combination of: (i) at least one opioid antagonist, and (ii) at least one selective serotonin reuptake inhibitor. The invention also relates to compositions and kits containing the same.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: June 6, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventor: Leonard Cook
  • Patent number: 6034091
    Abstract: Disclosed herein is a method for treating depression associated with alcoholism in a patient comprising administering to the patient a pharmacologically effective dose of an opioid antagonist, and a pharmacologically effective dose of at least one drug compound selected from the group consisting of a tricyclic antidepressant, an a-typical antidepressant, and lithium.
    Type: Grant
    Filed: October 2, 1998
    Date of Patent: March 7, 2000
    Assignee: John S. Nagle
    Inventor: Lee G. Dante
  • Patent number: 6020369
    Abstract: Respiratory viral infections may be effectively prevented or treated by administering an aerosol spray comprising a polyoxometalate to the lungs.
    Type: Grant
    Filed: July 7, 1998
    Date of Patent: February 1, 2000
    Inventors: Raymond F. Schinazi, Craig L. Hill
  • Patent number: 6013678
    Abstract: A method of treating congestive heart failure is diclosed comprising administering 5,6-dihydroxy- or 5,6-diisobutyroyloxy-2-methylaminotetralin or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: January 11, 2000
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Stefano Bongrani, Roberta Razzetti, Maurizio Civelli, Alberto Umile
  • Patent number: 6011054
    Abstract: The present invention relates to a method of treatment of depression in a human being identified as having depression. This method comprises the administration of a therapeutically effective depression treatment amount of N-acetyl-serotonin (NAS), also referred to as N-acetyl-5-hydroxytryptamine, to a human being identified as having depression. The NAS may be administered alone or in combination with other agents, e.g., Ca.sup.++ antagonists.
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: January 4, 2000
    Assignee: St. Elizabeth's Medical Center of Boston
    Inventors: Gregory F. Oxenkrug, Pura J. Requintina
  • Patent number: 6011070
    Abstract: Disclosed is a method of treating an individual who abuses cocaine by administering to the individual a therapeutically effective amount of an N,N-dialkyl 3-phenyl-1-indanamine or a mixture of N,N-dialkyl 3-phenyl-1-indanamines. Also disclosed is a method of treating an individual with Parkinson's disease or attention deficit hyperactivity disorder by administering to the individual a therapeutically effective amount of an N,N-dialkyl 3-phenyl-1-indanamine or a mixture of N,N-dialkyl 3-phenyl-1-indanamines.
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: January 4, 2000
    Assignee: Allelix-Pharm-Eco L.P.
    Inventors: Mark Froimowitz, Kuo-Ming Wu
  • Patent number: 5994408
    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: October 16, 1997
    Date of Patent: November 30, 1999
    Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research & Development Foundation, Ltd.
    Inventors: Sasson Cohen, Yaacov Herzig, Ruth Levy, Tzipora Speiser, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
  • 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: 5977147
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: April 24, 1996
    Date of Patent: November 2, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: John Joseph Tegeler, Barbara Seavey Rauckman, Russell Richard Lee Hamer, Brian Scott Freed, Gregory Harold Merriman
  • Patent number: 5977187
    Abstract: Novel 4-substituted-1,2-naphthoquinones, pharmaceutical unit dosage forms containing 4-substituted-1,2-naphthoquinones, and uses of 4-substituted-1,2-naphthoquinones to inhibit the growth of cancer cells are disclosed.
    Type: Grant
    Filed: October 14, 1998
    Date of Patent: November 2, 1999
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Benjamin J. Frydman, Donald T. Witiak, Laurence J. Marton, Karen Neder, M. Eileen Dolan
  • Patent number: 5932195
    Abstract: Arylaminomethylenecamphor derivatives of the formula (1) ##STR1## where the C.dbd.C double bond is in the Z or E configuration, and the variables have the following meanings:R.sup.1 H, CH.sub.3,R.sup.2 H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkenyl, aryl or substituted aryl,R.sup.3 H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, aryl, substituted aryl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.8 -acyl,Ar aryl, substituted aryl, hetaryl or substituted hetaryl,are used as sunscreen agents, especially in cosmetic and pharmaceutical formulations.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: August 3, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Drogemuller, Volker Bomm, Volker Schehlmann, Horst Westenfelder
  • Patent number: 5922774
    Abstract: 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: Grant
    Filed: October 22, 1996
    Date of Patent: July 13, 1999
    Assignee: DCV, Inc.
    Inventor: Anna Louise Winslow
  • Patent number: 5891923
    Abstract: This invention relates to the use of R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof for the treatment of dementia.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 6, 1999
    Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation, Ltd.
    Inventors: Moussa B.H. Youdim, John P.M. Finberg, Ruth Levy, Haim Yellin
  • Patent number: 5889039
    Abstract: A topical pharmaceutical composition having penetration enhancing properties for treating fungal dermatological conditions, comprising a pharmaceutically active topical antifungal agent selected from sulconazole and naftifine with an acetate penetration enhancing compound is disclosed.
    Type: Grant
    Filed: July 28, 1997
    Date of Patent: March 30, 1999
    Inventor: W. Roy Knowles
  • Patent number: 5885976
    Abstract: A composition is described which is useful for treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in humans the composition being administered in combination with a sufficient amount of an AC pulsed magnetic field alone or in conjunction with a DC magnetic field and a sufficient amount of random noise to the brain of a human in need of such treatment which composition comprises an effective amount of a composition which increases serotonin transmission to the human to be treated.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: March 23, 1999
    Inventor: Reuven Sandyk
  • 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: 5874477
    Abstract: The invention provides a method of preventing or treating malaria comprising administering a therapeutically effective amount of serotonin receptor ligand to reduce the pathological consequences of malaria infection in a patient, said serotonin receptor ligand characterized by an ability to displace an identifying ligand which defines the serotonin receptor subtype 5HT1a or 5HT2/5HT1c.In addition, the invention provides a method of identifying a serotonin receptor ligand capable of reducing the pathological consequences of malarial infection in a patient comprising the step of sequentially assaying potential ligands to identify a ligand characterized by an ability to displace an identifying ligand which defines the serotonin receptor subtype 5HT1a or 5HT2/5HT1c.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: February 23, 1999
    Assignee: The University of Hawaii
    Inventors: Bruce McConnell, Christopher P. Locher
  • Patent number: 5863952
    Abstract: The single enantiomers of formula (I) and salts thereof ##STR1## are calcium channel antagonists useful in the treatment of ischaemic conditions e.g., stroke.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: January 26, 1999
    Assignee: SmithKline Beecham plc
    Inventors: Barry Sidney Orlek, John David Harling
  • Patent number: 5840756
    Abstract: The present invention provides a pharmaceutical composition contains a thpeutically effective amount of L-DOPA ethyl ester and a carrier which comprises from 5.5 to 98.5% hydroxypropylmethyl cellulose, from 0.25 to 4.5% hydroxypropyl cellulose, and from 1 to 90% of a carboxyvinyl polymer.
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: November 24, 1998
    Assignees: Teva Pharmaceutical Industries Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Sasson Cohen, Sela Yoram, Ruth Levy, Nava Shterman, Eldad Melamed, Dafna Atlas
  • Patent number: 5817665
    Abstract: This invention relates to a composition and method for treating depression by administering to a patient a pharmacologically effective dose of an opioid antagonist having a pentacyclic nucleus structurally analogous to naltrexone, and a pharmacologically effective dose of a nontricyclic antidepressant
    Type: Grant
    Filed: November 20, 1995
    Date of Patent: October 6, 1998
    Assignee: John S. Nagle
    Inventor: Lee G. Dante
  • Patent number: 5807897
    Abstract: The invention relates to aminotetralin derivatives of the formula I: ##STR1## wherein: R.sup.1 is methyl or ethyl; R.sup.2 is hydrogen, halogen, lower-alkoxy or thiolower-alkyl; R.sup.3 is hydrogen, halogen, lower-alkoxy or lower-alkyl; and the chiral center * is in the (S)(-) form; or a pharmaceutically acceptable acid-addition salt thereof, with the proviso that when R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 must be methyl; to pharmaceutical compositions containing them and to methods for the treatment or prevention of movement disorders utilizing them.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: September 15, 1998
    Assignee: Zeneca Limited
    Inventors: Edward John Warawa, Bernard Migler
  • Patent number: 5789449
    Abstract: There is disclosed a method for treating certain psychiatric symptoms including anger, rejection sensitivity and a lack of mental or physical energy with administration of a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is fluoxetine or norfluoxetine.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: August 4, 1998
    Inventor: Michael J. Norden
  • Patent number: 5786390
    Abstract: The subject invention relates to pharmaceutical composition of R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 28, 1998
    Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation Ltd.
    Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin, Alex Veinberg
  • Patent number: 5773463
    Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: June 30, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: John David Harling, Barry Sidney Orlek
  • Patent number: 5744501
    Abstract: There is disclosed a method for treating Late Luteal Phase Dysphoric Disorder with administration of a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is fluoxetine or norfluoxetine.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: April 28, 1998
    Inventor: Michael J. Norden
  • Patent number: 5698571
    Abstract: The present invention provides a method for the treatment of migraine with compounds or compositions that are selective agonists of 5-HT.sub.1F receptors relative to other serotonin receptors that produce unwanted effects like vasoconstriction. The neurogenic meningeal extravasation that leads to the pain of migraine is inhibited.
    Type: Grant
    Filed: October 5, 1994
    Date of Patent: December 16, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Marlene L. Cohen, Kirk W. Johnson, Lee A. Phebus, Theresa Branchek
  • Patent number: 5691324
    Abstract: A composition is described which is useful for treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in humans the composition being administered in combination with a sufficient amount of an AC pulsed magnetic field alone or in combination with a sufficient amount of a DC magnetic field to the brain of a human in need of such treatment which composition comprises an effective amount of a composition which increases serotonin transmission to the human to be treated.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: November 25, 1997
    Inventor: Reuven Sandyk
  • Patent number: 5691325
    Abstract: A method of retarding the aging process and improving the symptoms of age-related disease conditions in humans which result from diminished pineal melatonin functions and reduced serotonin neurotransmission is described which comprises administering to a human in need thereof an effective amount of a composition which increases serotonin transmission to said human followed by the application to the brain of the human an effective amount of an AC pulsed magnetic field of proper intensity, frequency and waveform. Preferably the composition is supplemented by an effective amount of a dietary composition rich in the amino-acid tryptophan. Optionally an effective amount of an agent which provides growth hormone release is also administered prior to the application of the AC pulsed magnetic field.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: November 25, 1997
    Inventor: Reuven Sandyk
  • Patent number: 5684035
    Abstract: The invention is directed to a method of killing or inhibiting the growth of the malaria-causing pathogen Plasmodium falciparum by exposing the pathogen to an effective amount of a preparation comprising a compound selected from the group consisting of:a) a compound of formula I: ##STR1## where ##STR2## b) a compound of formula II; ##STR3## where each R' is --H or each R' is --OH; and c) a compound of formula III; ##STR4## where R" is --NH.sub.2, --H, or --SO.sub.3 M, and where M is H, Na, or K.
    Type: Grant
    Filed: July 17, 1996
    Date of Patent: November 4, 1997
    Inventor: Govind J. Kapadia
  • Patent number: 5670143
    Abstract: The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geomentry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of AIDS and ARC.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: September 23, 1997
    Assignees: Merrell Pharmaceuticals Inc., The Dow Chemical Company
    Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
  • Patent number: 5668181
    Abstract: This invention relates to the use of R(+)-N-propargyl-1-aminoindan.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 16, 1997
    Assignees: Teva Pharmaceutical Industries Ltd., Techion Research and Development Foundation Ltd.
    Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin
  • 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: 5652270
    Abstract: The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: July 29, 1997
    Assignee: Egis Gyogyszergyar RT
    Inventors: Zoltan Budai, Istvan Gacsalyi, Gabor Szenasi, Tibor Mezei, Aniko Kovacs, Gabor Blasko, Katalin Szemeredi, Gyula Simig, Lujza Petocz, Klara Reiter nee Esses
  • Patent number: 5652256
    Abstract: A topical pharmaceutical composition having penetration enhancing properties for treating fungal dermatological conditions comprising a pharmaceutically active topical antifungal agent selected from the group consisting of sulconazole and natifine with an acetate penetration enhancing compound.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 29, 1997
    Inventor: W. Roy Knowles
  • Patent number: 5652271
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which m is 0, 1 or 2; n is 2, 3, 4 or 5; X is carbonyl or a group of formula II ##STR2## in which R.sub.5 is H or alkyl; Y is an alkylene chain optionally substituted by one or more alkyl groups; Z is an alkylene chain containing 2 to 5 carbon atoms optionally substituted by one or more alkyl groups; R is phenyl optionally substituted by one or more halo substituents or R is naphthyl; and R.sub.1 and R.sub.2, which are the same or different, are H, alkyl, or arylalkyl, provided that when R.sub.1 is benzyl, R.sub.2 is H or methyl;have utility in the treatment of depression, anxiety, Parkinson's disease, obesity, cognitive disorders, seizures, neurological disorders such as epilepsy, and as neuroprotective agents to protect against conditions such as stroke.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: July 29, 1997
    Assignee: Knoll Aktiengesellschaft
    Inventors: Paul John Harris, David John Heal
  • Patent number: 5648087
    Abstract: The present invention relates to an anaesthetic veterinary pharmaceutical composition, comprising a general anaesthetic selected from phencyclidine derivatives such as ketamine or tiletamine, as well as 0.015 to 1.25 molar equivalents of selegiline, combined in a single pharmaceutical composition or presented separately.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: July 15, 1997
    Assignee: Sanofi Sante Nutrition Animale
    Inventors: Patricia Ovaert, Eliane Boivin
  • Patent number: 5646188
    Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.
    Type: Grant
    Filed: July 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
  • Patent number: 5637624
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.
    Type: Grant
    Filed: March 9, 1993
    Date of Patent: June 10, 1997
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Robert D. Titus
  • Patent number: 5635537
    Abstract: A compound of the formula ##STR1## Z is hydrogen or halogen, Q is COR.sup.1 or 5-or 6-membered aryl which may contain 1 or 2 heteroatoms selected from N, 0 or S and may be substituted or fused wherein R is hydrogen or C.sub.1 -methyl (cis-configuration), R.sup.1 is C.sub.1 -C.sub.6 alkyl or an aromatic ring which may contain heteroatoms selected from O and S and may be substituted or fused to an optionally substituted benzene ring, R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.3 may be different groups defined in claim 1, and enantiomers/salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: June 3, 1997
    Assignee: Astra Aktiebolag
    Inventors: Nils-Erik Anden, Berit C. E. Backlund Hook, Anna L. Bjork, Uli A. Hacksell, Sven-Erik Hillver, Ye Liu, Eva C. Mellin, Eva M. Persson, Karl J. Vallg.ang.rda, Hong Yu
  • Patent number: 5597826
    Abstract: The present invention relates to novel compositions containing the serotonin selective re-uptake inhibitor (SSRI), preferably (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine, and an agonist or antagonist of the serotonin 1 (5-HT.sub.
    Type: Grant
    Filed: September 14, 1994
    Date of Patent: January 28, 1997
    Assignee: Pfizer Inc.
    Inventors: Harry R. Howard, John E. Macor, Bertrand L. Chenard, Jeffrey S. Sprouse, David W. Schulz
  • Patent number: 5594034
    Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: January 14, 1997
    Assignee: Eli Lilly and Company
    Inventors: Jaswant S. Gidda, John M. Schaus
  • Patent number: 5591777
    Abstract: The use of 6,7-substituted-2-aminotetralines (e.g. 2-amino-6-fluoro-7-methoxytetraline) is disclosed for preparing pharmaceutical compositions useful for the treatment of septic shock and having antiinflammatory and antipyretic activities.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: January 7, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Piero Foresta, Vito Ruggiero
  • Patent number: 5589512
    Abstract: There is disclosed a method for treating borderline personality disorder in a patient by administering a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is fluoxetine or norfluoxetine.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: December 31, 1996
    Inventor: Michael J. Norden