Bicyclo Ring System Patents (Class 514/657)
  • Patent number: 5567712
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 22, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5561152
    Abstract: The present invention provides novel aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake.
    Type: Grant
    Filed: December 6, 1994
    Date of Patent: October 1, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Jules Freedman
  • Patent number: 5554656
    Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: September 10, 1996
    Assignee: Reckitt & Colman Inc.
    Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
  • Patent number: 5552444
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: September 3, 1996
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5521183
    Abstract: 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: Grant
    Filed: August 30, 1994
    Date of Patent: May 28, 1996
    Assignee: Allergan
    Inventors: David F. Woodward, Amelia L. Nieves
  • Patent number: 5519062
    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: May 23, 1994
    Date of Patent: May 21, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5486541
    Abstract: 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: Grant
    Filed: September 22, 1994
    Date of Patent: January 23, 1996
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Jeff Sterling, Ruth Levy, Alex Veinberg, Willy Goldenberg, John Finberg, Musa Youdim, Arieh Gutman
  • Patent number: 5484588
    Abstract: There are provided attracting and ingestion-stimulating agents for cockroach comprising as the active ingredient one or more compounds represented by the formula ##STR1## wherein R represents an amino group or an aminomethyl group. The attracting and ingestion-stimulating agents for cockroach exhibit a very potent attracting and ingestion-stimulating activity in the known species of house cockroach, both male and female.
    Type: Grant
    Filed: February 2, 1993
    Date of Patent: January 16, 1996
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Kazumasa Ogino, Haruo Shimamura, Kazuyuki Tomisawa, Fumio Urushizaki, Masami Nemoto, Tuguchika Yoshida
  • Patent number: 5470846
    Abstract: 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: Grant
    Filed: January 14, 1994
    Date of Patent: November 28, 1995
    Inventor: Reuven Sandyk
  • Patent number: 5439891
    Abstract: 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: Grant
    Filed: October 29, 1993
    Date of Patent: August 8, 1995
    Inventors: 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
  • Patent number: 5420158
    Abstract: 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: Grant
    Filed: March 23, 1993
    Date of Patent: May 30, 1995
    Assignee: Adir et Compagnie
    Inventors: Said Yous, Daniel Lesieur, Patrick Depreux, Beatrice Guardiola-Lemaitre, Gerard Adam, Pierre Renard, Daniel H. Caignard
  • Patent number: 5389687
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which exhibit binding activity at the serotonin 1A receptor.
    Type: Grant
    Filed: April 11, 1991
    Date of Patent: February 14, 1995
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Robert D. Titus
  • Patent number: 5382596
    Abstract: 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: Grant
    Filed: August 5, 1993
    Date of Patent: January 17, 1995
    Assignee: Whitby Research, Inc.
    Inventors: Mark C. Sleevi, Gevork Minaskanian, L. Meredith Moses
  • Patent number: 5376687
    Abstract: 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: Grant
    Filed: August 7, 1991
    Date of Patent: December 27, 1994
    Assignee: Aktiebolaget Astra
    Inventors: Uli A. Hacksell, Sven-Erik Hillver
  • Patent number: 5374654
    Abstract: 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: Grant
    Filed: April 21, 1993
    Date of Patent: December 20, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
  • Patent number: 5326784
    Abstract: 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: Grant
    Filed: July 29, 1993
    Date of Patent: July 5, 1994
    Assignee: Institut de Recherche Jouveinal
    Inventors: Jean-Louis Junien, Alain Calvet, Henri Jacobelli, Francois Roman
  • Patent number: 5286747
    Abstract: 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: Grant
    Filed: September 29, 1989
    Date of Patent: February 15, 1994
    Assignee: Per A. E. Carlsson
    Inventors: 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
  • Patent number: 5286753
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 15, 1994
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5268385
    Abstract: 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: Grant
    Filed: November 18, 1991
    Date of Patent: December 7, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5264206
    Abstract: 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: Grant
    Filed: June 14, 1988
    Date of Patent: November 23, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Manfred Bohn, Walter Dittmar, Karl Kraemer, Heinz G. Peil, Eberhard Futterer
  • Patent number: 5262441
    Abstract: 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: Grant
    Filed: September 28, 1992
    Date of Patent: November 16, 1993
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Akira Shuto, Noriyasu Sakamoto, Hirosi Kisida, Hiroaki Fujimoto, Kimitoshi Umeda, Noritada Matsuo
  • Patent number: 5252608
    Abstract: 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: Grant
    Filed: June 10, 1992
    Date of Patent: October 12, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael G. Palfreyman, Philippe Bey, Ian A. McDonald
  • Patent number: 5236951
    Abstract: 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: Grant
    Filed: June 12, 1990
    Date of Patent: August 17, 1993
    Assignee: Sanofi
    Inventor: Luciano Manara
  • Patent number: 5234945
    Abstract: 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: Grant
    Filed: January 4, 1991
    Date of Patent: August 10, 1993
    Assignee: Whitby Research, Inc.
    Inventor: James D. Belluzzi
  • Patent number: 5214156
    Abstract: 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: Grant
    Filed: April 10, 1992
    Date of Patent: May 25, 1993
    Assignee: The Upjohn Company
    Inventors: Bengt R. Andersson, Per Arvid E. Carlsson, Kjell A. I. Svensson, Hakan V. Wikstrom
  • Patent number: 5189037
    Abstract: 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: Grant
    Filed: April 2, 1992
    Date of Patent: February 23, 1993
    Assignee: Pfizer Inc
    Inventor: Patricia A. Seymour
  • Patent number: 5166181
    Abstract: 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: Grant
    Filed: August 15, 1990
    Date of Patent: November 24, 1992
    Assignee: Sandoz Ltd.
    Inventor: Sylvain Cottens
  • Patent number: 5162353
    Abstract: 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: Grant
    Filed: August 21, 1990
    Date of Patent: November 10, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher
  • Patent number: 5162375
    Abstract: 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: Grant
    Filed: February 28, 1991
    Date of Patent: November 10, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Charles D. Nicholson, Johannes Jukna
  • Patent number: 5153227
    Abstract: 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: Grant
    Filed: February 6, 1989
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
  • Patent number: 5134168
    Abstract: 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: Grant
    Filed: March 13, 1991
    Date of Patent: July 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Alan J. Bitonti, Jules Freedman
  • Patent number: 5086073
    Abstract: 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: Grant
    Filed: May 30, 1990
    Date of Patent: February 4, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. White, Michael C. Warren, Christine Ennis
  • Patent number: 5086074
    Abstract: 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: Grant
    Filed: March 26, 1990
    Date of Patent: February 4, 1992
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
  • Patent number: 5079245
    Abstract: 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: Grant
    Filed: July 5, 1989
    Date of Patent: January 7, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
  • Patent number: 5061728
    Abstract: 4-Phenyl-1,2,3,4-tetrahydro-1-napthalenamine derivatives have been found useful for the treatment of psychosis, inflammation and as immunosuppressants.
    Type: Grant
    Filed: December 5, 1990
    Date of Patent: October 29, 1991
    Assignee: Pfizer Inc.
    Inventor: B. Kenneth Koe
  • Patent number: 5051409
    Abstract: 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: Grant
    Filed: November 1, 1989
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5049588
    Abstract: 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: Grant
    Filed: May 8, 1989
    Date of Patent: September 17, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Charles D. Nicholson, Johannes Jukna
  • Patent number: 5047433
    Abstract: 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: Grant
    Filed: December 21, 1987
    Date of Patent: September 10, 1991
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mauro Marzi, Maria O. Tinti, Romano Di Fabio, Domenico Misiti
  • Patent number: 5047422
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: July 13, 1990
    Date of Patent: September 10, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 5032616
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: July 16, 1991
    Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4981870
    Abstract: 4-Phenyl-1,2,3,4-tetrahydro-1-naphthalenamine derivatives have been found useful for the treatment of psychosis, inflammation and as immunosuppressants.
    Type: Grant
    Filed: March 7, 1989
    Date of Patent: January 1, 1991
    Assignee: Pfizer Inc.
    Inventor: B. Kenneth Koe
  • Patent number: 4980354
    Abstract: 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: Grant
    Filed: September 14, 1989
    Date of Patent: December 25, 1990
    Assignee: Akzo N.V.
    Inventors: James Cairns, Duncan R. Rae
  • Patent number: 4975461
    Abstract: 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: Grant
    Filed: June 19, 1986
    Date of Patent: December 4, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Patent number: 4971987
    Abstract: 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: Grant
    Filed: March 7, 1988
    Date of Patent: November 20, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher, Ulrich Klar
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4952401
    Abstract: 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: Grant
    Filed: June 12, 1990
    Date of Patent: August 28, 1990
    Assignee: ICI Americas Inc.
    Inventor: David G. Hobbs
  • Patent number: 4943428
    Abstract: 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: Grant
    Filed: February 16, 1988
    Date of Patent: July 24, 1990
    Assignee: Wright State University
    Inventors: James B. Lucot, George H. Crampton
  • Patent number: 4940731
    Abstract: 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: Grant
    Filed: August 30, 1989
    Date of Patent: July 10, 1990
    Assignee: Pfizer Inc.
    Inventor: Peter A. Bick
  • Patent number: 4920112
    Abstract: Novel fungicidal compositions comprising a 25-azasterol compound and a squalene epoxidase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4910208
    Abstract: 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: Grant
    Filed: February 19, 1988
    Date of Patent: March 20, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra