Patents Examined by E. Bernhardt
  • Patent number: 5008264
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is loweralkyl, arylloweralkyl, diarylloweralkyl or --CH.sub.2 CHOHCH.sub.2 OR.sub.5, R.sub.5 being aryl, or alternatively --NR.sub.1 R.sub.2 taken together is ##STR2## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## and R.sub.3 and R.sub.4 are each independently methoxy or hydroxy, which compounds are useful as analgesic and hypotensive agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: April 16, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Larry Davis
  • Patent number: 5006534
    Abstract: Substituted benzyl ethers, benzyl thioethers, and benzylamines of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, sulphonylalkyl, halogenoalkoxy, halogenoalkylthio, aralkoxy, aralkylthio, halogen, nitro, cyano or hydroxyl, or represent a group of the formula ##STR2## wherein R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or acyl,R.sup.3 represents a group of the formula ##STR3## in which R.sup.6 represents hydrogen, alkyl or acyl,R.sup.7 represents hydrogen or alkyl andn represents a number from 3 to 10,B represents --CH.sub.2 --X-- or --X--CH.sub.2 --,wherein X represents O, S or NR.sup.7,and wherein R.sup.7 has the abovementioned meaning and the group ##STR4## represents a benzo-fused heterocyclic system, A in the heterocyclic radical being 3-, 4- or 5-membered and containing nitrogen, oxygen and/or sulphur as hetero-atoms.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: April 9, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer
  • Patent number: 5006659
    Abstract: 7-Chloroquinoline-8-carboxylic acids of the formula (I) ##STR1## where R is hydrogen, chlorine or methyl, are prepared by direct oxidation of the corresponding 8-methylqunoline compound with nitric acid or nitrogen oxide in the presence of sulfuric acid and a heavy metal catalyst.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: April 9, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Hagen, Jacques Dupuis, Heinz Eilingsfeld
  • Patent number: 5002950
    Abstract: The present invention is various 7-deazaguanines having activity as immunomodulators. Also included are pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: February 1, 1990
    Date of Patent: March 26, 1991
    Assignee: Warner-Lambert CO.
    Inventors: Thomas C. Malone, Jagadish C. Sircar
  • Patent number: 5002960
    Abstract: Compounds of the formulas: ##STR1## wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed. Also disclosed are novel intermediates, N-halo-alkyl-4-(isoxazol-5-yl)alkoxybenzamides, also useful as antiviral agents.
    Type: Grant
    Filed: June 12, 1989
    Date of Patent: March 26, 1991
    Assignee: Sterling Drug, Inc.
    Inventor: Guy D. Diana
  • Patent number: 5001130
    Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.
    Type: Grant
    Filed: February 18, 1988
    Date of Patent: March 19, 1991
    Assignee: Bristol-Myers Company
    Inventors: James S. New, William L. Christopher
  • Patent number: 4999355
    Abstract: Compounds of formula: ##STR1## in which: either R.sub.1 represents 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl or 4-(4-fluorophenyl)-1,2,3,6-tetrahydro-1-pyridyl, R.sub.2 represents hydrogen, alkoxy of 1 or 2 carbon atoms, hydroxyl, alkyl, alkylthio, alkylcarbonyloxy, phenylalkylcarbonyloxy, phenylalkyl or --NR.sub.4 R.sub.5 in which R.sub.4 represents hydrogen or alkyl and R.sub.5 represents alkyl, phenyl, monohalogenated phenyl or pyridyl, and R.sub.3 represents a hydrogen atom, or else R.sub.2 represent phenyl and R.sub.3 represents hydrogen or hydroxyl;or R.sub.1 represnets 4-phenyl-1-piperazinyl whose phenyl nucleus has a substituent halogen atom or hydroxyl radical in the 4-position, R.sub.2 represents alkoxy and R.sub.3 represents hydrogen;it being understood that when R.sub.1 represents the 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl radical, R.sub.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: March 12, 1991
    Assignee: Rhone-Poulenc
    Inventors: Marie-Therese Comte, Claude Gueremy, Gerard Ponsinet
  • Patent number: 4996208
    Abstract: Fungicidal thiazolopyrimidine derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen or alkyl,R.sup.2 stands for hydrogen, alkyl or optionally substituted aryl,R.sup.3 stands in each case for optionally substituted alkyl, cycloalkyl, aryl, arylcarbonyl or arylsulphonyl, andX stands for oxygen or sulphur.
    Type: Grant
    Filed: June 19, 1989
    Date of Patent: February 26, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Lindner, Wilhelm Brandes
  • Patent number: 4995899
    Abstract: Diazabicycloalkane derivatives of the formula ##STR1## where R is alkyl, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are identical or different and independently of one another are each hydrogen or methyl, X is chlorine or bromine, m is 0 or 1, n is 1 or 2, and p and q are each 0, 1 or 2, the carbon atom functioning as bridgehead having an R configuration, and herbicidal agents containing acetanilides as herbididally active compounds and diazabicycloalkane derivatives as antagonistic agents.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: February 26, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Scholz, Adolf Zeidler, Bruno Wuerzer, Norbert Meyer
  • Patent number: 4996206
    Abstract: N-(Acyl)glutamic acid derivatives in which the acyl group is substituted with 4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl group are antineoplastic agents. A typical embodiment is N-[4-(2-{4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-glutamic acid.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: February 26, 1991
    Assignee: The Trustees of Princeton University
    Inventors: Edward C. Taylor, Dietmar G. Kuhnt, Chuan Shih, Gerald B. Grindey
  • Patent number: 4994571
    Abstract: This invention relates to a process for producing a compound of the formula (I) as shown below. ##STR1## wherein Q is a condensed heterocyclic group having a nitrogen atom in the bridgehead position which may optionally be substituted, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, or a salt thereof.The compound (I) or a salt thereof is novel and of value as agricultural chemicals.According to the process of this invention the compound (I) or a salt thereof can be produced in good yield and high purity.
    Type: Grant
    Filed: August 26, 1988
    Date of Patent: February 19, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Miki, Yasuo Ishida
  • Patent number: 4992091
    Abstract: Novel compounds, e.g. 3-cyano-5,7-dimethyl-N-(2,6-dichlorophenyl)pyrazolo]1,5-a]pyrimidine-2-sul fonamide and their use as herbicides and/or for the suppression of nitrification of ammonium nitrogen in soil.
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: February 12, 1991
    Assignee: The Dow Chemical Company
    Inventors: Anna P. Vinogradoff, William A. Kleschick
  • Patent number: 4992449
    Abstract: Novel antibacterial compounds of the formula: ##STR1## in which R.sub.1 is alkyl (C.sub.1 -C.sub.4), cycloalkyl (C.sub.3 -C.sub.6), alkoxy (C.sub.1 -C.sub.4), alkylamino (C.sub.1 -C.sub.3), vinyl, phenyl, benzyl, --CH.sub.2 CH.sub.2 F or mono or polysubstituted phenyl (wherein the substituent is halogen, CF.sub.3 or OCH.sub.2 F); n is an integer of from 1 to 4; and R.sub.2 is cis or trans hydroxy, amino, mono or disubstituted alkyl (C.sub.1 -C.sub.3) amino and the pharmacologically accepted salts thereof are described.
    Type: Grant
    Filed: February 1, 1990
    Date of Patent: February 12, 1991
    Assignee: American Cyanamid Company
    Inventors: Panayota Bitha, Yang-I Lin
  • Patent number: 4988702
    Abstract: The present invention is novel derivatives of pyrrolo[3,2-d]pyrimidines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.
    Type: Grant
    Filed: February 12, 1990
    Date of Patent: January 29, 1991
    Assignee: Warner-Lambert Company
    Inventors: Catherine R. Kostlan, Jagadish C. Sircar
  • Patent number: 4988695
    Abstract: Pyrrolo- and dihydropyrrolocinnolines, and their use as inhibitors of gastric acid secretion. A compound of the invention is 1-(2-methylphenyl)-2,3-dihydropyrrolo-[3,2-c]-cinnoline.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: January 29, 1991
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Peter Blurton
  • Patent number: 4987133
    Abstract: New salicylic acid derivatives of the general formula I ##STR1## in which R.sup.1 is H or CH.sub.3,R.sup.2 is 4-(4-methyl-2-thiazolyl)-piperazino, 4-(tetrahydro-2-furoyl)-piperazino, 4-(4-methyl-2-thiazolyl)-homopiperazino, 4-benzamidopiperidino, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolino, 1-imidazolyl, tribromo-1-imidazolyl or 2-(3-indolyl-1,1-dimethyl-ethylamino andR.sup.3 is alkoxy having 1-C atoms, NH.sub.2 or alkylamino having 1-4 C atoms,as well as the physiologically acceptable acid addition salts thereof, exhibit effects on the circulation, especially effects lowering the blood pressure and relieving the heart, and diuretic effects.
    Type: Grant
    Filed: April 17, 1989
    Date of Patent: January 22, 1991
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Adolf Kurmeier, Wolf-Dietrich Weber, Hans-Eckart Radunz, Hans-Jochen Schliep
  • Patent number: 4985560
    Abstract: The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: January 15, 1991
    Assignee: American Home Products Corporation
    Inventors: Annmarie L. Sabb, Magid A. Abou-Gharbia, Gervais Dionne
  • Patent number: 4983210
    Abstract: Isoxazolines of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted phenyl, or a saturated or unsaturated 5- or 6-membered heterocycle;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl andR.sup.7 is substituted or unsubstituted C.sub.2 -C.sub.6 -alkenyl, C.sub.5 -C.sub.7 -cycloalkenyl, phenyl, naphthyl or thienyl,processes for their manufacture, and their use.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: January 8, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Karl Eicken, Hans Theobald, Thomas Kuekenhoehner, Karl-Otto Westphalen, Bruno Wuerzer, Juergen Frank, Norbert Meyer
  • Patent number: 4983603
    Abstract: The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors.These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: January 8, 1991
    Assignee: Societe Anonyme: SANOFI
    Inventors: Camille G. Wermuth, Paul Worms, Jean-Jacques Bourguignon, Roger Brodin
  • Patent number: 4980365
    Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or loweralkyl; R.sub.2 is loweralkyl, arylloweralkyl, diarylloweralkyl or --CH.sub.2 CHOHCH.sub.2 OR.sub.5, R.sub.5 being aryl, or alternatively --NR.sub.1 R.sub.2 taken together is ##STR2## R.sub.6 being aryl, arylloweralkyl, diarylloweralkyl, ##STR3## and R.sub.3 and R.sub.4 are each independently methoxy or hydroxy, which compounds are useful as analgesic and hypotensive agents.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: December 25, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Larry Davis