Benzo Is The Other Cyclo Patents (Class 544/62)
  • Patent number: 5109135
    Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: April 28, 1992
    Assignee: Sterling Drug Inc.
    Inventors: Thomas E. D'Ambra, Malcolm R. Bell
  • Patent number: 5089043
    Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: February 18, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
  • Patent number: 5071841
    Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
  • Patent number: 5070090
    Abstract: Novel (thio)morpholinyl and piperazinyl alkylphenol ethers having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting, combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.
    Type: Grant
    Filed: April 25, 1990
    Date of Patent: December 3, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
  • Patent number: 5061813
    Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: October 29, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5037825
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: August 6, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5028711
    Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 2, 1991
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5021413
    Abstract: Analgesic compounds are of the general formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: June 4, 1991
    Assignee: Sankyo Company Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5017576
    Abstract: Quinoline derivatives of formula: ##STR1## in which either R.sub.1 denotes trifluoromethyl, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, morpholino and R.sub.4 denotes a 4-methylphenyl, 4-chlorophenyl, 2-, 3- or 4-fluorophenyl, 4-methoxyphenyl, 4-methyl-3-fluorophenyl, 2,4-difluorophenyl or 4-aminophenyl,or R.sub.1 denotes trifluoromethyl, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, thiomorpholino, or R.sub.2 denotes methyl and R.sub.3 denotes 2-methoxyethyl and R.sub.4 denotes 4-methylphenyl,or R.sub.1 denotes chlorine fluorine, or methoxy, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, morpholino, and R.sub.4 denotes 4-methylphenyl, are useful as anxiolytics, hypnotics, anticonvulsants and antiepileptics.
    Type: Grant
    Filed: September 11, 1989
    Date of Patent: May 21, 1991
    Assignee: Rhone-Poulenc Sante
    Inventors: Marie-Christine Dubroeucq, Jean-Marc Paris, Christian Renault
  • Patent number: 5013732
    Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: May 7, 1991
    Assignee: Sterling Drug Inc.
    Inventor: Malcolm R. Bell
  • Patent number: 5000777
    Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.
    Type: Grant
    Filed: November 21, 1989
    Date of Patent: March 19, 1991
    Assignees: Ciba-Geigy Corporation, Janssen Pharmaceutica
    Inventors: Henry Szczepanski, Lourens Wals
  • Patent number: 4996328
    Abstract: Novel bis-(indolyl)ethylenes, process for their production and record systems utilizing such bis-(indolyl)ethylene chromogens are described.Bis-(indolyl)ethylenes of the following general formula are prepared: ##STR1## wherein each L.sup.1 and L.sup.2 is the same or different and is each independently selected from indole moieties (J1) through (J4) (L.sup.1 need not be the same as L.sup.2), ##STR2## wherein in (J1) through (J4) above, each of R.sup.5, R.sup.6, R.sup.13, R.sup.14, R.sup.21, R.sup.22, R.sup.29 and R.sup.30 need not be the same and is each independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, alkylaroxy, alkylalkoxy, and substituted or unsubstituted aryl, such as phenyl, naphthyl, or heterocyclyl.Each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.23, R.sup.24, R.sup.25, Rphu 26, R.sup.27, and R.sup.
    Type: Grant
    Filed: March 8, 1989
    Date of Patent: February 26, 1991
    Assignee: Appleton Papers Inc.
    Inventor: Ponnampalam Mathiaparanam
  • Patent number: 4975455
    Abstract: Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: December 4, 1990
    Assignee: Adir et Cie
    Inventors: Jean-Daniel Brion, Guillaume Le Baut, Patrick Ducrey, Sylvie Piessard-Robert, Claude Cudennec, Genevieve Seurre
  • Patent number: 4973590
    Abstract: Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an acid, allowing the solution to stand for about 0.15 to 150 hours at a temperature from room temperature to the boiling point of the solution, filtering the solution, precipitating the active compound from the solution using a basic reagent, and converting the precipitated active compound into a form which can be administered parenterally.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: November 27, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Preiss, Ulrich Schorsch, Arthur Haaf, Paul Naab, Rudolf Zerbes
  • Patent number: 4970308
    Abstract: Chromogenic di-[bis-(indolyl)ethylenyl] tetrahalophthalides are disclosed of the formula ##STR1## wherein each X.sup.1, X.sup.2, X.sup.3, and X.sup.4 is independently selected from chlorine or bromine;wherein each of R.sup.1 and R.sup.7 is independently selected from cycloalkyl, aralkyl, alkoxyalkyl, or aroxyalkyl;wherein each of R.sup.2 and R.sup.8 is independently selected from alkyl (C.sub.1 -C.sub.8) or aryl (substituted or unsubstituted);wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 is independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, aryl (substituted or unsubstituted), halogen, alkoxy (C.sub.1 -C.sub.8), aroxy, cycloalkoxy, dialkylamino including symmetrical and unsymmetrical (C.sub.1 -C.sub.
    Type: Grant
    Filed: August 23, 1989
    Date of Patent: November 13, 1990
    Assignee: Appleton Papers Inc.
    Inventor: Ponnampalam Mathiaparanam
  • Patent number: 4959379
    Abstract: Fungicidal 7-substituted 2-carboxamido-benzothiazole 3-oxides of the formula ##STR1## in which n stands for the numbers 0, 1, 2 or 3,R.sup.1 stands for hydrogen or optionally substituted alkyl,R.sup.2 stands for hydrogen, hydroxyl, ureido or for an optionally substituted radical from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, aralkoxy, aralkyl, aryl, heterocyclyl and heterocyclylakyl, orR.sup.1 and R.sup.2 together stand for an alkylene chain which is optionally substituted and optionally interrupted by hetero atoms,R.sup.3 stands for halogen, alkyl or halogenoalkyl andR.sup.4 stands for halogen, alkyl or halogenoalykl.The intermediates of the formula ##STR2## are also new.
    Type: Grant
    Filed: March 21, 1989
    Date of Patent: September 25, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Wagner, Gerd Hanssler
  • Patent number: 4954509
    Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: September 4, 1990
    Assignee: Dr. Lo. Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina
  • Patent number: 4925840
    Abstract: The invention relates to novel 3-phenyl-4-cyanopyrrole derivatives of the general formula ##STR1## wherein X has the following meanings:A: hydrogen or CO--R.sub.1, wherein R.sub.1 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, or C.sub.1 -C.sub.6 alkoxy which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 cycloalkyl, or tetrahydrofur-2-yl;B: S--R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.3 haloalkyl;C: CH(Y)R.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.8 haloalkyl and Y is hydroxy, halogen or OC(O)R.sub.4, wherein R.sub.4 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxycarbonyl; orD: CH.sub.2 --Z, wherein Z is the group ##STR2## wherein each of R.sub.7 and R.sub.8 independently of the other is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: May 15, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert Nyfeler, Josef Ehrenfraund
  • Patent number: 4923861
    Abstract: Novel 6-[2-[2-(substituted amino)-3-quinolinyl]-ethenyl and ethyl]tetrahydro-4-hydroxypyran-2-ones and/or oxides and the corresponding dihydroxy ring opened acids and esters are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are thus useful hypolipidemic and hypocholesterolemic agents.
    Type: Grant
    Filed: February 7, 1989
    Date of Patent: May 8, 1990
    Assignee: Warner-Lambert Company
    Inventors: Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 4868300
    Abstract: Compounds of the formula ##STR1## wherein: z is O or I;X is ##STR2## a and b are 0, 1, or 2 and a+b=0, 1 or 2; R, R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, alkyl or aralkyl;R.sub.n is hydrogen, alkyl, aralkyl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl or amidino;R.sup.5 groups on vicinal carbon atoms may together form a carbon-carbon double bond when a or b=2;R groups on vicinal carbon atoms may together form a carbon-carbon double bond when R.sub.n is hydrogen and z=1;R.sup.4 and R.sup.5 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;R.sup.5 and R.sup.6 groups may together form a carbon-nitrogen double bond when R.sub.3 is hydrogen and a+b=1;R.sup.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;Y is hydrogen, --O--R.alpha., --S-R.alpha. or ##STR3## R.alpha. is hydrogen, alkyl, cycloalkyl or acyl; R.beta. is hydrogen or alkyl; andR.alpha. and R.beta.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: September 19, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
  • Patent number: 4845118
    Abstract: The invention relates to compounds of the formula ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, and R.sup.1 to R.sup.9 have the meanings given in the description, to a process for their preparation, to pharmaceutical compositions containing them, and to their use as inhibitors of gastric acid secretion.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: July 4, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Robert Rippel, Andreas W. Herling, Klaus Weidmann
  • Patent number: 4845094
    Abstract: 2-phenylbenzoxepin derivatives having a hypoglycemic activity, hypotensive activity, and platelet coagulation inhibiting activity, a process for production of the derivatives, and pharmaceutical compositions containing the derivatives.
    Type: Grant
    Filed: June 19, 1987
    Date of Patent: July 4, 1989
    Assignee: Suntory Limited
    Inventors: Toshio Tatsuoka, Kayoko Nomura, Fumio Satoh, Takafumi Ishihara, Seiji Miyano, Kunihiro Sumoto
  • Patent number: 4831151
    Abstract: Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Helmut Link, Marc Montavon, Eva M. Karpitschka, Wilhelm Klotzer, Renate Mussner
  • Patent number: 4826976
    Abstract: This invention relates to a color-shifted dye compounds containing at least one thermally unstable carbamate moiety which are useful in thermal imaging. These compounds may be represented by the formula [M--(X).sub.q ].sub.p D wherein M is a carbamate moiety; X is --N.dbd., --SO.sub.2 -- or --CH.sub.2 --; D taken with X and M represents the radical of a color-shifted organic dye, said carbamate moiety M comprising a tert-alkoxycarbonyl group, ##STR1## wherein R' is halomethyl or alkyl.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: May 2, 1989
    Assignee: Polaroid Corporation
    Inventors: Alan L. Borror, Ernest W. Ellis, Donald A. McGowan
  • Patent number: 4826836
    Abstract: Fungicidally active novel saccharine salts of aminomethyl heterocyclic compounds of the formula ##STR1## in which R represents optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted thienyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl or alkinyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms,X represents oxygen or sulphur,Y represents oxygen, sulphur or the methylene group,m represents 0 or 1 andn represents 0 or 1.
    Type: Grant
    Filed: November 5, 1987
    Date of Patent: May 2, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Wolfgang Kramer, Paul Reinecke, Gerd Hanssler
  • Patent number: 4818755
    Abstract: Cardiotonic fused aromatic bicyclic ring substituted thiazole compounds and their salts, methods for increasing cardiac contractility in humans and other mammals by the use of said compounds, pharmaceutical compositions including said compounds and methods for compound preparation.
    Type: Grant
    Filed: July 28, 1986
    Date of Patent: April 4, 1989
    Assignee: Rorer Pharmaceutical Corporaton
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Bruce F. Molino
  • Patent number: 4814345
    Abstract: Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.
    Type: Grant
    Filed: November 20, 1987
    Date of Patent: March 21, 1989
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuhl, Gerd Buschmann, Stephen J. Magda
  • Patent number: 4808718
    Abstract: Novel fused polycyclic and bridged compounds are disclosed which are useful as calcium entry blockers.
    Type: Grant
    Filed: May 6, 1986
    Date of Patent: February 28, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko, Brian T. Phillips
  • Patent number: 4803198
    Abstract: New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl.
    Type: Grant
    Filed: July 15, 1986
    Date of Patent: February 7, 1989
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuehl, Gerd Buschmann, Stephen J. Magda
  • Patent number: 4794116
    Abstract: Esters, acetal ethers, thioethers and nitrogen substituted derivatives of certain bicyclic compounds are disclosed which are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents and in treatment of hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: December 27, 1988
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Ho-Jane Shue
  • Patent number: 4777168
    Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting parmacological activity, including anti-secretory and anti-ulcerogenic activity, pharaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: January 7, 1988
    Date of Patent: October 11, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
  • Patent number: 4774246
    Abstract: Quinoline compounds having the formula: ##STR1## wherein R is a phenyl or substituted phenyl group or an aromatic heterocyclic group, R.sub.1 is a hydrogen or a carboxy-protecting group and Z is an amine group or an aliphatic heterocyclic group. The compounds have antibacterial activity.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: September 27, 1988
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu
  • Patent number: 4772622
    Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: September 20, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, William C. Lumma, Jr.
  • Patent number: 4772706
    Abstract: An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.
    Type: Grant
    Filed: January 13, 1986
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventors: James N. Wemple, James R. Zeller, John M. Domagala
  • Patent number: 4767762
    Abstract: This invention relates to novel isoxazolo-naphthyridine, isoxazolo-quinoline, isothiazolo-naphthyridine, and isothiazolo-quinoline, derivatives having antibacterial properties.
    Type: Grant
    Filed: December 11, 1986
    Date of Patent: August 30, 1988
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu
  • Patent number: 4766211
    Abstract: Chromogenic quinazolines of formula ##STR1## wherein R is an aryl radical or a heterocyclic radical,Z.sub.1 is oxygen or sulfur,Z.sub.2 is oxygen, sulfur or ##STR2## R' is hydrogen, alkyl which is unsubstituted or substituted by halogen, cyano or lower alkoxy, or is cycloalkyl, phenyl, benzyl, phenethyl or acyl, or --NRR' is a 5- or 6-membered heterocyclic radical,Q is an aliphatic radical which may be interrupted by a further member Z.sub.2,Y is the radical of a couplable compound, and the ringA is unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy or lower alkoxycarbonyl.These quinazolines are exceedingly fast to sublimation and are particularly suitable color formers in pressure-sensitive or heat-sensitive recording materials and give strong and lightfast yellow and orange colorations.
    Type: Grant
    Filed: August 27, 1986
    Date of Patent: August 23, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Rudolf Zink, Ian J. Fletcher
  • Patent number: 4748182
    Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.
    Type: Grant
    Filed: March 5, 1986
    Date of Patent: May 31, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Marcel Hibert, Maurice W. Gittos
  • Patent number: 4743609
    Abstract: This invention provides a class of new indole derivatives which are useful as medicinal compounds having a mild inhibitory effect on the gastric acid secretion as well as a remarkably cytoprotective effects on gastric muscosa, and which are represented by the general formula: ##STR1##
    Type: Grant
    Filed: February 10, 1986
    Date of Patent: May 10, 1988
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Masaaki Hosoi, Fumio Nakano, Kenji Matsuyama, Hiroshi Takeshita, Kenji Niiyama, Susumu Nakagawa
  • Patent number: 4743601
    Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: May 10, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4731364
    Abstract: 2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C.sub.1 -C.sub.2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: March 15, 1988
    Assignee: Schering Corporation
    Inventors: Dinanath F. Rane, Russell E. Pike
  • Patent number: 4728647
    Abstract: Compounds of formula: ##STR1## in which V and W are H, halogen, alkyl (1-4C) or alkoxy (1-4C), amino, or acylamino,Z is phenyl, optionally substituted, thienyl, or pyridyl,R.sub.1 is alkyl (1-6C), alkoxyalkyl, cycloalkyl (3-6C), phenyl, phenylalkyl, or cycloalkylalkyl,R.sub.2 is alkyl (1-6C), alkoxyalkyl, cycloalkyl (3-6C), phenyl, phenylalkyl, cycloalkylalkyl, or morpholino, andNR.sub.1 R.sub.2 can also be pyrrolidino, optionally substituted piperidino, optionally substituted morpholino, thiomorpholino, optionally substituted piperazino, or an optionally substituted piperazinone, are useful as anxiolytic agents.
    Type: Grant
    Filed: May 28, 1986
    Date of Patent: March 1, 1988
    Assignee: Rhone-Poulenc Sante
    Inventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard Le Fur, Christian Renault
  • Patent number: 4705788
    Abstract: Novel antibacterially active 7-amino-1-(substituted cyclopropyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the formula ##STR1## in which X.sup.1 and X.sup.2 can be identical or different and represent hydrogen or halogen,R.sub.1, R.sub.2 and R.sub.3 represent hydrogen, methyl, chlorine or fluorine, the radicals R.sub.1 -R.sub.3 never all being identical, andR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring which may be substituted.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: November 10, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4692445
    Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: November 12, 1986
    Date of Patent: September 8, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4673682
    Abstract: Isoquinoline-4-carboxylic acid derivatives of the formula I ##STR1## in which m, n, R.sup.1, R.sup.2, R.sup.3, A and X have the meansings indicated, and physiologically acceptable acid addition salts thereof, a process for their preparation, pharmaceutical formulations based on these compounds and the use thereof as antiarrythmic agents.
    Type: Grant
    Filed: September 7, 1983
    Date of Patent: June 16, 1987
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Elmar Konz, Joachim Kaiser
  • Patent number: 4672062
    Abstract: 3-amino-2,3-dihydro-1-benzoxepine compounds corresponding to the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 may each be hydrogen, halogen, lower alkyl or lower alkoxy, or if one of R.sub.1 and R.sub.2 is hydrogen, the other may also be nitro or trifluoromethyl, R.sub.3 represents hydrogen or a lower alkyl group which optionally may be substituted by hydroxy, lower alnoxy, an optionally substituted phenyl group or an optionally substituted amino group, and R.sub.4 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 member heterocycle. The compounds exhibit pharmacological, especially antidepressive, activity.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: June 9, 1987
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Heinrich-Wilhelm Ohlendorf, Michael Ruhland, Klaus-Ullrich Wolf
  • Patent number: 4668673
    Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: July 2, 1986
    Date of Patent: May 26, 1987
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
  • Patent number: 4666920
    Abstract: Antibacterially effective 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)quinolinecarboxylic acids of the formula ##STR1## in which A is nitrogen or C--R.sup.1,R.sup.1 is nitro or halogen,R.sup.2 and R.sup.3 each independently is C.sub.1 -C.sub.3 -alkyl, or together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring, which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 -- or .dbd.N--R.sup.4 as a ring member and can optionally be mono-, di- or tri-substituted on the carbon atoms by C.sub.1 -C.sub.3 -alkyl, hydroxyl, alkoxy with 1-3 carbon atoms, amino, methylamino or ethylamino,R.sup.
    Type: Grant
    Filed: March 15, 1985
    Date of Patent: May 19, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4665202
    Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X.sub.1 and X.sub.2, independently of each other, represent hydrogen, halogen, unsubstituted or substituted amino or a quaternary ammonium salt; etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; nitro; functionally modified formyl; free or functionally modified carboxyl; acyl; an unsubstituted or substituted hydrocarbon radical, or an unsubstituted or substituted heterocyclic radical; with the proviso that at least one of the radicals X.sub.1 and X.sub.2 is bonded by a carbon atom to the ring system and with the proviso that X.sub.1 and X.sub.2 cannot be together halogen and formyl; in which Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be sulfur, sulfinyl or sulfonyl, if X.sub.1 is hydrogen and X.sub.
    Type: Grant
    Filed: August 24, 1984
    Date of Patent: May 12, 1987
    Assignee: Zyma SA
    Inventors: Christian G. Rimbault, Philippe M. Narbel
  • Patent number: 4659708
    Abstract: The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidine erivatives have the formula: ##STR1## wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O).sub.2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R" substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R'"; R" represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'" represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.
    Type: Grant
    Filed: August 20, 1981
    Date of Patent: April 21, 1987
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Leslie M. Werbel, Edgar A. Steck
  • Patent number: RE32761
    Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: October 4, 1988
    Assignee: Sterling Drug Inc.
    Inventor: Malcolm R. Bell