Bicyclo Ring System Patents (Class 514/657)
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Patent number: 6159971Abstract: 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: GrantFiled: October 21, 1998Date of Patent: December 12, 2000Assignee: Astrazeneca ABInventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
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Patent number: 6147072Abstract: 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: GrantFiled: September 23, 1997Date of Patent: November 14, 2000Assignee: Eli Lilly and CompanyInventors: Franklin P. Bymaster, Kenneth W. Perry, Gary D. Tollefson
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Patent number: 6127424Abstract: Use of aryl-substituted cyclobutylalkylamines and their pharmaceutically suitable salts for treating obesity and its accompanying disorders are disclosed.Type: GrantFiled: April 27, 1998Date of Patent: October 3, 2000Assignee: Knoll AktiengesesllschaftInventors: Keith Frank Martin, David John Heal
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Patent number: 6114394Abstract: 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: GrantFiled: October 14, 1997Date of Patent: September 5, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Michael L. Edwards, Ronald D. Snyder
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Patent number: 6107345Abstract: 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: GrantFiled: March 3, 1999Date of Patent: August 22, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
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Patent number: 6103760Abstract: 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: GrantFiled: June 9, 1999Date of Patent: August 15, 2000Assignee: Chiesi Farmaceuticals S.p.A.Inventors: Paolo Chiesi, Stefano Bongrani, Roberta Razzetti, Maurizio Civelli, Alberto Umile
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Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
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Patent number: 6071918Abstract: 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: GrantFiled: July 21, 1999Date of Patent: June 6, 2000Assignee: Dupont Pharmaceuticals CompanyInventor: Leonard Cook
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Patent number: 6034091Abstract: 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: GrantFiled: October 2, 1998Date of Patent: March 7, 2000Assignee: John S. NagleInventor: Lee G. Dante
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Patent number: 6020369Abstract: Respiratory viral infections may be effectively prevented or treated by administering an aerosol spray comprising a polyoxometalate to the lungs.Type: GrantFiled: July 7, 1998Date of Patent: February 1, 2000Inventors: Raymond F. Schinazi, Craig L. Hill
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Patent number: 6013678Abstract: 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: GrantFiled: October 14, 1997Date of Patent: January 11, 2000Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Stefano Bongrani, Roberta Razzetti, Maurizio Civelli, Alberto Umile
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Patent number: 6011054Abstract: 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: GrantFiled: November 4, 1998Date of Patent: January 4, 2000Assignee: St. Elizabeth's Medical Center of BostonInventors: Gregory F. Oxenkrug, Pura J. Requintina
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Patent number: 6011070Abstract: 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: GrantFiled: August 15, 1997Date of Patent: January 4, 2000Assignee: Allelix-Pharm-Eco L.P.Inventors: Mark Froimowitz, Kuo-Ming Wu
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Patent number: 5994408Abstract: 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: October 16, 1997Date of Patent: November 30, 1999Assignees: 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
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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: 5977147Abstract: 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: GrantFiled: April 24, 1996Date of Patent: November 2, 1999Assignee: Hoechst Marion RousselInventors: John Joseph Tegeler, Barbara Seavey Rauckman, Russell Richard Lee Hamer, Brian Scott Freed, Gregory Harold Merriman
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Patent number: 5977187Abstract: 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: GrantFiled: October 14, 1998Date of Patent: November 2, 1999Assignee: Wisconsin Alumni Research FoundationInventors: Benjamin J. Frydman, Donald T. Witiak, Laurence J. Marton, Karen Neder, M. Eileen Dolan
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Patent number: 5932195Abstract: 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: GrantFiled: January 13, 1998Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: Michael Drogemuller, Volker Bomm, Volker Schehlmann, Horst Westenfelder
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Patent number: 5922774Abstract: Method for repelling insect herbivores from plant surfaces and deterring them from feeding on plant surfaces by applying an aqueous dispersion of polycyclic quinone or precursor thereof to the foliage of the plant and/or to the surrounding soil in which the plant is rooted.Type: GrantFiled: October 22, 1996Date of Patent: July 13, 1999Assignee: DCV, Inc.Inventor: Anna Louise Winslow
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Patent number: 5891923Abstract: This invention relates to the use of R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof for the treatment of dementia.Type: GrantFiled: June 6, 1995Date of Patent: April 6, 1999Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation, Ltd.Inventors: Moussa B.H. Youdim, John P.M. Finberg, Ruth Levy, Haim Yellin
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Patent number: 5889039Abstract: 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: GrantFiled: July 28, 1997Date of Patent: March 30, 1999Inventor: W. Roy Knowles
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Patent number: 5885976Abstract: 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: GrantFiled: November 25, 1997Date of Patent: March 23, 1999Inventor: Reuven Sandyk
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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: 5874477Abstract: 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: GrantFiled: August 12, 1994Date of Patent: February 23, 1999Assignee: The University of HawaiiInventors: Bruce McConnell, Christopher P. Locher
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Patent number: 5863952Abstract: 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: GrantFiled: July 11, 1997Date of Patent: January 26, 1999Assignee: SmithKline Beecham plcInventors: Barry Sidney Orlek, John David Harling
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Patent number: 5840756Abstract: 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: GrantFiled: July 11, 1996Date of Patent: November 24, 1998Assignees: Teva Pharmaceutical Industries Ltd., Yissum Research Development Company of the Hebrew University of JerusalemInventors: Sasson Cohen, Sela Yoram, Ruth Levy, Nava Shterman, Eldad Melamed, Dafna Atlas
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Patent number: 5817665Abstract: 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 antidepressantType: GrantFiled: November 20, 1995Date of Patent: October 6, 1998Assignee: John S. NagleInventor: Lee G. Dante
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Patent number: 5807897Abstract: 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: GrantFiled: February 21, 1997Date of Patent: September 15, 1998Assignee: Zeneca LimitedInventors: Edward John Warawa, Bernard Migler
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Patent number: 5789449Abstract: 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: GrantFiled: September 19, 1996Date of Patent: August 4, 1998Inventor: Michael J. Norden
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Patent number: 5786390Abstract: The subject invention relates to pharmaceutical composition of R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1995Date of Patent: July 28, 1998Assignees: 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
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Patent number: 5773463Abstract: 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: GrantFiled: January 22, 1996Date of Patent: June 30, 1998Assignee: SmithKline Beecham p.l.c.Inventors: John David Harling, Barry Sidney Orlek
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Patent number: 5744501Abstract: 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: GrantFiled: March 11, 1997Date of Patent: April 28, 1998Inventor: Michael J. Norden
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Patent number: 5698571Abstract: 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: GrantFiled: October 5, 1994Date of Patent: December 16, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Marlene L. Cohen, Kirk W. Johnson, Lee A. Phebus, Theresa Branchek
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Patent number: 5691324Abstract: 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: GrantFiled: May 8, 1995Date of Patent: November 25, 1997Inventor: Reuven Sandyk
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Patent number: 5691325Abstract: 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: GrantFiled: May 8, 1995Date of Patent: November 25, 1997Inventor: Reuven Sandyk
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Patent number: 5684035Abstract: 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: GrantFiled: July 17, 1996Date of Patent: November 4, 1997Inventor: Govind J. Kapadia
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Patent number: 5670143Abstract: 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: GrantFiled: May 19, 1995Date of Patent: September 23, 1997Assignees: Merrell Pharmaceuticals Inc., The Dow Chemical CompanyInventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Patent number: 5668181Abstract: This invention relates to the use of R(+)-N-propargyl-1-aminoindan.Type: GrantFiled: June 2, 1995Date of Patent: September 16, 1997Assignees: 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
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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: 5652270Abstract: 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: GrantFiled: June 17, 1996Date of Patent: July 29, 1997Assignee: Egis Gyogyszergyar RTInventors: Zoltan Budai, Istvan Gacsalyi, Gabor Szenasi, Tibor Mezei, Aniko Kovacs, Gabor Blasko, Katalin Szemeredi, Gyula Simig, Lujza Petocz, Klara Reiter nee Esses
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Patent number: 5652256Abstract: 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: GrantFiled: June 6, 1995Date of Patent: July 29, 1997Inventor: W. Roy Knowles
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Patent number: 5652271Abstract: 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: GrantFiled: December 22, 1995Date of Patent: July 29, 1997Assignee: Knoll AktiengesellschaftInventors: Paul John Harris, David John Heal
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Patent number: 5648087Abstract: 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: GrantFiled: March 4, 1994Date of Patent: July 15, 1997Assignee: Sanofi Sante Nutrition AnimaleInventors: Patricia Ovaert, Eliane Boivin
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Patent number: 5646188Abstract: 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: GrantFiled: July 5, 1995Date of Patent: July 8, 1997Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
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Patent number: 5637624Abstract: 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: GrantFiled: March 9, 1993Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 5635537Abstract: 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: GrantFiled: March 18, 1993Date of Patent: June 3, 1997Assignee: Astra AktiebolagInventors: 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
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Patent number: 5597826Abstract: 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: GrantFiled: September 14, 1994Date of Patent: January 28, 1997Assignee: Pfizer Inc.Inventors: Harry R. Howard, John E. Macor, Bertrand L. Chenard, Jeffrey S. Sprouse, David W. Schulz
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Patent number: 5594034Abstract: 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: GrantFiled: April 7, 1995Date of Patent: January 14, 1997Assignee: Eli Lilly and CompanyInventors: Jaswant S. Gidda, John M. Schaus
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Patent number: 5591777Abstract: 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: GrantFiled: February 27, 1996Date of Patent: January 7, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero
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Patent number: 5589512Abstract: 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: GrantFiled: January 25, 1994Date of Patent: December 31, 1996Inventor: Michael J. Norden