Bicyclo Ring System Patents (Class 514/657)
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Patent number: 5567712Abstract: The present invention provides pharmaceutically active compounds formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3; andor a pharmaceutically acceptable salt thereof.Also provided are compounds of formula II ##STR2## wherein R.sup.1a is --H or --OR.sup.5 in which R.sup.5 is a hydroxy protecting group.R.sup.2a is --H, halo, or --OR.sup.6 in which R.sup.6 is a hydroxy protecting group; andR.sup.4 is --OH or --CHO;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5561152Abstract: The present invention provides novel aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake.Type: GrantFiled: December 6, 1994Date of Patent: October 1, 1996Assignee: Merrell Pharmaceuticals Inc.Inventor: Jules Freedman
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Patent number: 5554656Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.Type: GrantFiled: February 25, 1994Date of Patent: September 10, 1996Assignee: Reckitt & Colman Inc.Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
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Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes
Patent number: 5552444Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: March 14, 1995Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus -
Patent number: 5521183Abstract: The present invention is based on the finding that 5-HT receptor ligands are useful in treating experimental models of clinically encountered pruritus (itch). A 5-HT ligand as used in this specification is a compound capable of binding with some selectivity to one or more of the 5-HT receptor sites. Systemic administration of 5-HT agonists and antagonists causes a reduction in the number of itch-scratch responses to an ocular challenge by allergenic antigens. Therefore, the present invention relates to a method for treating pruritus by administering systemically a therapeutically effective amount of a 5-HT agonist or antagonist to a mammal afflicted with pruritus. The 5-HT ligands may, for example, be selected from the group consisting of 5-HT.sub.1, 5-HT.sub.2, 5-HT.sub.3, and 5-HT.sub.4 agonists, partial agonists and antagonists.Type: GrantFiled: August 30, 1994Date of Patent: May 28, 1996Assignee: AllerganInventors: David F. Woodward, Amelia L. Nieves
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Patent number: 5519062Abstract: 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: May 23, 1994Date of Patent: May 21, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5486541Abstract: N-propargyl-1-amonoindan monofluorinated in the phenyl ring and their use as selective inhibitors of monoamine oxidase (MAO).There are provided several processes for the preparation of these novel compounds. There are also provided as novel compounds 1-aminoindans monofluorinated in the phenyl ring, which serve as intermediates in the preparation of the corresponding novel N-propargyl derivatives.Type: GrantFiled: September 22, 1994Date of Patent: January 23, 1996Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Jeff Sterling, Ruth Levy, Alex Veinberg, Willy Goldenberg, John Finberg, Musa Youdim, Arieh Gutman
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Patent number: 5484588Abstract: There are provided attracting and ingestion-stimulating agents for cockroach comprising as the active ingredient one or more compounds represented by the formula ##STR1## wherein R represents an amino group or an aminomethyl group. The attracting and ingestion-stimulating agents for cockroach exhibit a very potent attracting and ingestion-stimulating activity in the known species of house cockroach, both male and female.Type: GrantFiled: February 2, 1993Date of Patent: January 16, 1996Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kazumasa Ogino, Haruo Shimamura, Kazuyuki Tomisawa, Fumio Urushizaki, Masami Nemoto, Tuguchika Yoshida
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Patent number: 5470846Abstract: A method of treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in humans is described which comprises administering to a human in need thereof an effective amount of a composition which increases serotonin transmission to the patient to be treated followed by the application to the brain of the patient of a sufficient amount of an AC pulsed magnetic field of proper intensity and frequency to treat the disorder.Type: GrantFiled: January 14, 1994Date of Patent: November 28, 1995Inventor: Reuven Sandyk
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Patent number: 5439891Abstract: A new pharmaceutical composition for the treatment of tuberculosis and leprosy, said composition comprising piperine in combination with known antituberculosis or antileprosy drugs or the mixtures thereof.Type: GrantFiled: October 29, 1993Date of Patent: August 8, 1995Inventors: Randhir S. Kapil, Usha Zutshi, Kasturi L. Bedi, Gurbax Singh, Ramesh K. Johri, Santosh K. Dhar, Jawahar L. Kaul, Subhash C. Sharma, Gurcharan S. Pahwa, Naveen Kapoor, Ashok K. Tickoo, Manoj K. Tickoo, Uma Kaul, Surjeet Singh, Ram K. Zutshi, Rajinder Singh
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Patent number: 5420158Abstract: The invention relates to a compound selected from those of general formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable base.Medicinal product which is useful in the treatment of disorders linked to abnormal melatonin activity.Type: GrantFiled: March 23, 1993Date of Patent: May 30, 1995Assignee: Adir et CompagnieInventors: Said Yous, Daniel Lesieur, Patrick Depreux, Beatrice Guardiola-Lemaitre, Gerard Adam, Pierre Renard, Daniel H. Caignard
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Patent number: 5389687Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: April 11, 1991Date of Patent: February 14, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 5382596Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.2 is OA and R.sub.3 is selected from the group consisting of H and OA; where A is H or is selected from the group consisting of hydrocarbyl radicals comprising between 1 and 3 carbon atoms, as well as ##STR2## with the proviso that when R.sub.3 is OA, then R.sub.2 and R.sub.3 may be bonded together to form the group R.sub.4 is selected from the group consisting of alkyl and aromatic residues having from 1 to 20, preferably from 1 to 12, carbon atoms, for example, alkyl, optionally substituted with aromatic residues, and aromatic residues optionally substituted with alkyl radicals; n is an integer from 1 to 4; R.sub.5 is an unbranched alkyl chain comprising from 1 and 3 carbon atoms or a cyclopropylmethyl radical; R.sub.1 is alkoxy, cycloalkoxy and a cyclic ether of the formula ##STR3## where m is an integer from 3 to 5; with the proviso that when R.sub.1 is alkoxy, then R.sub.Type: GrantFiled: August 5, 1993Date of Patent: January 17, 1995Assignee: Whitby Research, Inc.Inventors: Mark C. Sleevi, Gevork Minaskanian, L. Meredith Moses
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Patent number: 5376687Abstract: A compound of formula (I), wherein X is O, CH.sub.2, S, SO or SO.sub.2 ; R is F or Cl; R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl; R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl; R.sub.3 is H, C.sub.1 -C.sub.6, alkyl, a pharmaceutically acceptable salt thereof, an enantiomer thereof, and a pharmaceutically acceptable salt of said enantiomer for use in therapy. A pharmaceutical preparation containing as active ingredient any one of said compounds. A process for the preparation of a compound of formula (I).Type: GrantFiled: August 7, 1991Date of Patent: December 27, 1994Assignee: Aktiebolaget AstraInventors: Uli A. Hacksell, Sven-Erik Hillver
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Patent number: 5374654Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.Type: GrantFiled: April 21, 1993Date of Patent: December 20, 1994Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
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Patent number: 5326784Abstract: New cycloalkylalkylamines which are sigma-receptor ligands of formule (I) ##STR1## in which: R.sub.1 is H or lower alkyl; X and Y are H, OH, lower alkyl, lower alkoxy, halogen or nitrile; V.sub.1 and V.sub.2 together form a double bond attached to an oxygen atom or to a hydroxyimino radical, or are linked as an ethylenedioxy chain; A represents a valency bond, an oxygen atom, a methylene or an ethylene group; m is equal to 0, 1 or 2; n has the value of an integer from 1 to 5. Psychotropic drug which is also useful in gastroenterology.Type: GrantFiled: July 29, 1993Date of Patent: July 5, 1994Assignee: Institut de Recherche JouveinalInventors: Jean-Louis Junien, Alain Calvet, Henri Jacobelli, Francois Roman
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Patent number: 5286747Abstract: Compounds of the formula ##STR1## wherein R.sup.3 and the NR.sup.1 R.sup.2 group are in a cis-position to each other and wherein Y is OH, R.sup.4 COO, (R.sup.5).sub.2 NCOO or R.sup.6 O either in position 5 or position 7, whereby R.sup.4 is an alkyl group having 1-5 carbon atoms or a possibly substituted phenyl group, R.sup.5 is an alkyl group having 1-5 carbon atoms and R.sup.6 is an allyl or benzyl group, R.sup.1 is hydrogen or an alkyl group having 1-3 carbon atoms, R.sup.2 is an alkyl group having 1-6 carbon atoms, a phenylalkyl- or m-hydroxyphenylalkyl group with 2-4 carbon atoms in the alkyl part, or an alkenyl group with 3-6 carbon atoms other than 1-alkenyl, and R.sup.3 is an alkyl group having 1-3 carbon atoms, processes and intermediates for their preparation, pharmaceutical preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.Type: GrantFiled: September 29, 1989Date of Patent: February 15, 1994Assignee: Per A. E. CarlssonInventors: Folke L. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Anette M. Johansson, Per L. Lindberg, John L. G. Nilsson, Domingo Sanchez, H.ang.kan V. Wikstrom
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Patent number: 5286753Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: April 16, 1993Date of Patent: February 15, 1994Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
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Patent number: 5268385Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.Type: GrantFiled: November 18, 1991Date of Patent: December 7, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
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Patent number: 5264206Abstract: A nail lacquer containing at least one film-former which is insoluble in water and at least one substance which has antimycotic activity and is from the group comprising tioconazole, econazole, oxiconazole, miconazole, tolnaftate and naftifine hydrochloride.Type: GrantFiled: June 14, 1988Date of Patent: November 23, 1993Assignee: Hoechst AktiengesellschaftInventors: Manfred Bohn, Walter Dittmar, Karl Kraemer, Heinz G. Peil, Eberhard Futterer
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Patent number: 5262441Abstract: An aromatic compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.3 -C.sub.8 alkyl group, a C.sub.3 -C.sub.8 alkoxy group, an alkoxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkenyloxy group, an alkenyloxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 haloalkyl group, a C.sub.3 -C.sub.8 alkoxy group, a haloalkoxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 haloalkenyl group, a C.sub.3 -C.sub.8 haloalkenyloxy group, a haloalkenyloxyalkyl group having 3 to 8 carbon atoms or a C.sub.3 -C.sub.8 alkynyloxy group; R.sup.2 is a halogen atom; R.sup.3 is, the same or different, a hydrogen atom, a halogen atom or a methyl group; R.sup.4 is a hydrogen atom or a methyl group R.sup.5 is, the same or different, a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 haloalkoxy group, a C.sub.1 -C.sub.4 alkylthio group, a C.sub.1 -C.sub.Type: GrantFiled: September 28, 1992Date of Patent: November 16, 1993Assignee: Sumitomo Chemical Company LimitedInventors: Akira Shuto, Noriyasu Sakamoto, Hirosi Kisida, Hiroaki Fujimoto, Kimitoshi Umeda, Noritada Matsuo
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Patent number: 5252608Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.Type: GrantFiled: June 10, 1992Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Philippe Bey, Ian A. McDonald
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Patent number: 5236951Abstract: A method of prophylaxis and/or of treatment of ocular disorders, mainly of controlling intraocular hypertension and treating glaucoma, which comprises administering, preferably topically, a prophylactically and/or therapeutically effective amount of a phenylethanolamine derivative.Type: GrantFiled: June 12, 1990Date of Patent: August 17, 1993Assignee: SanofiInventor: Luciano Manara
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Patent number: 5234945Abstract: This invention provides a method for treating the symptoms of obesity which comprises administering to a human or other mammal suffering from the symptoms of obesity an effective amount of a compound selected from the group consisting of the optically active compounds especially the (-) negative stereoisomers represented by the formula: ##STR1## wherein R.sub.1 R.sub.2,R.sub.3,R.sub.4,R.sub.5 and R.sub.6 are defined by the specification substituted or unsubstituted phenyls, pyridyl, hydroxyphenyl, ##STR2## X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3,R.sub.2, R.sub.3 and R.sub.Type: GrantFiled: January 4, 1991Date of Patent: August 10, 1993Assignee: Whitby Research, Inc.Inventor: James D. Belluzzi
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Patent number: 5214156Abstract: This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein YR.sub.1 is OR.sub.1 at the 8 position where R.sub.1 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.4 is hydrogen, C.sub.1-8 alkyl, --CH.sub.2 --(C.sub.3-4 cycloalkyl), --(CH.sub.2).sub.m --R.sub.5 or --CH.sub.2 --CH.sub.2 --X--(CH.sub.2).sub.n CH.sub.3 ; n is zero to 3 and m is 2 or 3; X is oxygen or sulfur;R.sub.5 is phenyl, C.sub.1-3 alkoxy, C.sub.1-3 alkyl, 2-thiophene, 3-thiophene, or phenyl substituted with one or two substituent groups selected from chlorine, bromine or fluorine; and with the proviso that when R.sub.3 contains more than four carbon atoms and R.sub.4 is alkyl, said alkyl contains from 1 to 3 carbon atoms.Alternatively, --YR.sub.1 is --S--(C.sub.1-3 alkyl) at the 5, 6, 7 or 8 position of the aromatic ring or OR.sub.1 at the 8 position where R.sub.Type: GrantFiled: April 10, 1992Date of Patent: May 25, 1993Assignee: The Upjohn CompanyInventors: Bengt R. Andersson, Per Arvid E. Carlsson, Kjell A. I. Svensson, Hakan V. Wikstrom
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Patent number: 5189037Abstract: Combinations having synergistic anxiolytic activity which comprise a first component selected from the group consisting of 8-hydroxy-2-(dipropylamino)-1,2,3,4-tetrahydronaphthalene, gepirone, ipsapirone, tandospirone, (7S,9S)-2-(2-pyrimidyl)-7-(succinimidomethyl)-perhydro-1H-pyrido[1,2-a]pyr azine, or chlordiazepoxide; and a second component selected from the group consisting of 1-(2-pyrimidyl)pyrazine and idazoxan.Type: GrantFiled: April 2, 1992Date of Patent: February 23, 1993Assignee: Pfizer IncInventor: Patricia A. Seymour
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Patent number: 5166181Abstract: Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, ##STR1## wherein R.sub.1 to R.sub.8 are as defined in the description, are useful as acetylcholinesterase inhibitors.Type: GrantFiled: August 15, 1990Date of Patent: November 24, 1992Assignee: Sandoz Ltd.Inventor: Sylvain Cottens
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Patent number: 5162353Abstract: The invention relates to carbacyclin derivatives with general formula I: ##STR1## in which Y.sub.1 stands for the radical --CH.sub.2 --X--(CH.sub.2).sub.n --R.sub.1 or the radical ##STR2## n, 1 or 3, R.sub.1, the radical ##STR3## the radical ##STR4## R.sub.9 stands for the radical --(CH.sub.2).sub.m --R.sub.6 or the radical --(CH.sub.2).sub.m-o --[Z.sub.1 --(CH.sub.2).sub.m-p ].sub.x --[Z.sub.2 --(CH.sub.2).sub.m-q ].sub.y --R.sub.6,m=2-20,o, p, and q are less than or equal to 19,x, y=0, 1 or 2,Z.sub.1 stands for a cis--CH.dbd.CH group, a trans--CH.dbd.CH group of a --C.dbd.C group, and each of these groups must be separated at least by a methylene group from the C-9 carbon atom of the carbacyclin bicyclic compound,Z.sub.2 stands for oxygen, sulfur, an NH or an N methyl group,R.sub.6 stands for amino, methylamino, hydroxy, carboxy or mercapto,X an oxygen atom or a methylene group,Y.sub.2 hydrogen or fluorine,A a --CH.sub.2 --CH.sub.2, trans--CH.dbd.CH or --C.dbd.Type: GrantFiled: August 21, 1990Date of Patent: November 10, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher
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Patent number: 5162375Abstract: A method for the treatment and/or prophylaxis of disorders associated with neuronal degeneration resulting from ischaemic events, in mammals, such as humans, which comprises administering to the mammal in need of such treatment an effective amount of a 5-HT1.sub.A agonist.Type: GrantFiled: February 28, 1991Date of Patent: November 10, 1992Assignee: Beecham Group p.l.c.Inventors: Charles D. Nicholson, Johannes Jukna
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Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5134168Abstract: Drug-resistant protozoal infection, particularly, drug-resistant malarial infection in humans, can be effectively treated with standard antiprotozoal agents if administered in conjunction with a phenoxyamino-substituted benzocycloalkane derivative.Type: GrantFiled: March 13, 1991Date of Patent: July 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan J. Bitonti, Jules Freedman
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Patent number: 5086073Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.Type: GrantFiled: May 30, 1990Date of Patent: February 4, 1992Assignee: John Wyeth & Brother LimitedInventors: John F. White, Michael C. Warren, Christine Ennis
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Patent number: 5086074Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.Type: GrantFiled: March 26, 1990Date of Patent: February 4, 1992Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
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Patent number: 5079245Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.Type: GrantFiled: July 5, 1989Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
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Patent number: 5061728Abstract: 4-Phenyl-1,2,3,4-tetrahydro-1-napthalenamine derivatives have been found useful for the treatment of psychosis, inflammation and as immunosuppressants.Type: GrantFiled: December 5, 1990Date of Patent: October 29, 1991Assignee: Pfizer Inc.Inventor: B. Kenneth Koe
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Patent number: 5051409Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.Type: GrantFiled: November 1, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5049588Abstract: A method for the treatment and/or prophylaxis of disorders associated with neuronal degeneration resulting from ischaemic events, in mammals, such as humans, which comprises administering to the mammal in need of such treatment an effective amount of a 5-HTl.sub.A agonist.Type: GrantFiled: May 8, 1989Date of Patent: September 17, 1991Assignee: Beecham Group p.l.c.Inventors: Charles D. Nicholson, Johannes Jukna
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Patent number: 5047433Abstract: N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.Type: GrantFiled: December 21, 1987Date of Patent: September 10, 1991Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Marzi, Maria O. Tinti, Romano Di Fabio, Domenico Misiti
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Patent number: 5047422Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: July 13, 1990Date of Patent: September 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5032616Abstract: 4-trans-substituted cyclohexylamine derivatives of the formula ##STR1## where R.sup.1 is the group CR.sup.5 R.sup.6 R.sup.7, in which R.sup.5, R.sup.6 and R.sup.7 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that not more than one of the substituents R.sup.5, R.sup.6 and R.sup.7 may by hydrogen, or in which R.sup.6 and R.sup.7 together with the included carbon atom form a three-membered to six-membered carbocyclic aliphatic ring,R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl or alkynyl or cycloalkyl or cycloalkenyl, which in turn may be substituted, with the proviso that the sum of the carbon atoms and hetero atoms (O, S and halogen) of R.sup.2 and R.sup.3 together is not less than 8,R.sup.4 is hydrogen, alkyl, cycloalkyl or alkoxy, and m is 1 to 4, and the bond is a single or a double bond,salts thereof, and their use as fungicides.Type: GrantFiled: August 28, 1987Date of Patent: July 16, 1991Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4981870Abstract: 4-Phenyl-1,2,3,4-tetrahydro-1-naphthalenamine derivatives have been found useful for the treatment of psychosis, inflammation and as immunosuppressants.Type: GrantFiled: March 7, 1989Date of Patent: January 1, 1991Assignee: Pfizer Inc.Inventor: B. Kenneth Koe
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Patent number: 4980354Abstract: The invention relates to tetrahydronaphthalene and indane derivatives with the general formula I: ##STR1## wherein R.sup.1 represents zero to four substituents, which may be the same or different and are selected from OH, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and unsubstituted or C.sub.1 -C.sub.4 alkyl substituted amino;R.sup.2 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkenyl and C.sub.1 -C.sub.4 alkynyl which may be substituted by halogen;R.sup.3 and R.sup.4 represent independently H, C.sub.1 -C.sub.4 alkyl or form together with the nitrogen atom a 5- or 6-membered ring;n has the value 0 or 1;ALK is an aliphatic hydrocarbon with 1-8 carbon atoms and their pharmaceutically acceptable salts.These new compounds are typical monoamine reuptake blockers with additional .alpha..sub.2 antagonist activity and show strong anti-depressant activity without being sedative.Type: GrantFiled: September 14, 1989Date of Patent: December 25, 1990Assignee: Akzo N.V.Inventors: James Cairns, Duncan R. Rae
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Patent number: 4975461Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0, 1 or 2; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 may be the same or different and are H, hydroxy or alkoxy; R.sup.3 is H, lower alkyl, alkanoyl or aroyl and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof.These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.Type: GrantFiled: June 19, 1986Date of Patent: December 4, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4971987Abstract: The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.Type: GrantFiled: March 7, 1988Date of Patent: November 20, 1990Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher, Ulrich Klar
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4952401Abstract: A composition and a method of using the same wherein said composition comprises a rodenticide and an additive selected from the group consisting of1. polyoxyalkylated alkyl phenols;2. sorbitan fatty acids and polyoxyalkylated derivatives thereof;3. polyoxyalkylated fatty amines;4. polyoxyalkylated branched or linear alcohols, diols or polyols;5. polyoxyalkylated branched or linear mercaptans;6. polyoxyalkylated esters; and7. polyoxyalkylated amines.The composition may optionally include an organic solvent and/or a dye. The rodenticide may be selected from a wide host of compounds, including brodifacoum, bromadiolone, diphacinone, chlorodiphacinone, monofluoroacetatic acid, bromethalin, calciferol, flocoumafen, and salts of such compounds.Type: GrantFiled: June 12, 1990Date of Patent: August 28, 1990Assignee: ICI Americas Inc.Inventor: David G. Hobbs
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Patent number: 4943428Abstract: A method for the alleviation of both motion sickness and chemically-induced emesis is provided which includes the administration of a nontoxic, therapeutically effective amount of a composition which stimulates serotonin-1A receptors in a mammal in need of such treatment. The preferred compounds for use are buspirone and 8-hydroxy-2(di-n-propylamino)-tetralin (8-OH-DPAT).Type: GrantFiled: February 16, 1988Date of Patent: July 24, 1990Assignee: Wright State UniversityInventors: James B. Lucot, George H. Crampton
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Patent number: 4940731Abstract: A method of treating premature ejaculation comprising administering to a human in need of such treatment an amount of the compound (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine, also known by the generic name sertraline, or a pharmaceutically acceptable salt thereof, effective in delaying ejaculation.Type: GrantFiled: August 30, 1989Date of Patent: July 10, 1990Assignee: Pfizer Inc.Inventor: Peter A. Bick
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Patent number: 4920112Abstract: Novel fungicidal compositions comprising a 25-azasterol compound and a squalene epoxidase inhibitor compound are disclosed.Type: GrantFiled: April 18, 1988Date of Patent: April 24, 1990Assignee: Merck & Co., Inc.Inventors: Janet C. Onishi, Arthur A. Patchett
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Patent number: 4910208Abstract: A method is provided for inhibiting leukotriene biosynthesis and thus treating asthma, psoriasis or inflammation by oral administration of p-aminophenols having the structure ##STR1## wherein m is 0 to 5; X is CH or N; R.sup.1 and R.sup.2 may be the same or different and are H, lower alkyl, aryl, hydroxy, hydroxyalkyleneoxy, alkylthio, alkoxy, alkanoyloxy, aryloxy, halo, carboxy, alkoxycarbonyl or amido; R.sup.3 is H, lower alkyl, alkanoyl or aroyl; and R.sup.4 is H, lower alkyl, benzoyl or alkanoyl, and including acid-addition salts thereof, with the proviso that when R.sup.4 is benzoyl, R.sup.2 is other than H.Type: GrantFiled: February 19, 1988Date of Patent: March 20, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra