Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly Or Indirectly To The Tricyclo Ring System By Nonionic Bonding Patents (Class 546/99)
  • Patent number: 5510486
    Abstract: This invention relates to a process for preparing 2-(1-azabicyclo 2.2.2!oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-benz de!isoquin olin-1-one, particularly 2-(1-azabicyclo 2.2.2!oct-3S-yl)-2,3,3aS,4,5,6-tetrahydro-1H-benz de!isoqu inolin-1-one, and to intermediates useful in such process.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: April 23, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James Robinson, III, John C. Rohloff, Bruce A. Kowalczyk
  • Patent number: 5492914
    Abstract: This invention relates to 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[de ]isoquinolin-1-one and 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1H-ben z[de]isoquinolin-1-one and their individual stereoisomers and uses and the processes for their making.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: February 20, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Paul E. Weller, Douglas L. Wren
  • Patent number: 5491236
    Abstract: This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein R, R.sub.1 and A are as defined in claim 1. These compounds are useful to treat central nervous system disorders.
    Type: Grant
    Filed: December 4, 1991
    Date of Patent: February 13, 1996
    Assignee: The Upjohn Company
    Inventor: Chiu-Hong Lin
  • Patent number: 5420234
    Abstract: Bis-N-aminoimides of formula (III): ##STR1## wherein m is 0 or 1 and ##STR2## is a mono- or polycyclic aromatic radical, can be employed to produce a variety of polymers of the type produced from diamines, including polyimides having an N--N linkage; polymers can be produced having exceptionally high glass transition temperatures, but which are also soluble in organic solvents; colored polymers and electroconductive polymers and photoconductive polymers can also be produced.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: May 30, 1995
    Inventors: Allan S. Hay, Hossein Ghassemi
  • Patent number: 5397708
    Abstract: A method for determining the concentration of sulfide in a process stream. The method comprises the steps of adding to a process stream a sulfide scavenger (probe) that changes electronic properties when it reacts with sulfide. One can then monitor the electronic properties of the sulfide scavenger in the process stream to determine the concentration of sulfide present. In a preferred embodiment, the sulfide scavenger is either fluorescent and when it reacts with sulfide becomes inactive or is inactive and when it reacts with sulfide becomes fluorescent.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: March 14, 1995
    Assignee: Nalco Chemical Company
    Inventors: Ronald B. Lessard, Manian Ramesh
  • Patent number: 5376664
    Abstract: This invention relates to unsymmetrical mono-3-nitro bis-naphthalimides of formula ##STR1## including (R,R)-2-{2-[2-((2-(1,3-dioxo-1H-benz[de]isoquinolin-2-(3H)-yl)-propylamino ))ethylamino]-1-methylethyl}-5-nitro-1H-benz[de]isoquinolin-1,3-(2H)-dione, processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer, particularly solid tumor carcinomas, in mammals.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: December 27, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Robert F. Kaltenbach, III, Jung-Hui Sun, Robert J. Cherney, Steven P. Seitz
  • Patent number: 5359092
    Abstract: Bis-N-aminoimides of formula (III): ##STR1## wherein m is 0 or 1 and is a mono- or polycyclic aromatic radical, can be employed to produce a variety of polymers of the type produced from diamines, including polyimides having an N--N linkage; polymers can be produced having exceptionally high glass transition temperatures, but which are also soluble in organic solvents; coloured polymers and electroconductive polymers and photoconductive polymers can also be produced.
    Type: Grant
    Filed: June 2, 1993
    Date of Patent: October 25, 1994
    Inventors: Allan S. Hay, Hossein Ghassemi
  • Patent number: 5306720
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: April 26, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5292881
    Abstract: New naphthalimides, useful as additives in toners for controlling the charge and conductivity, of the formula ##STR1## in which R represents C.sub.1 - to C.sub.22 -alkyl,R.sup.1 and R.sup.2 independently of one another in each case represent C.sub.1 - to C.sub.4 -alkyl, or R.sup.1 and R.sup.2, together with the nitrogen atom in between, form a pyrrolidine, piperidine or morpholine ring,n represents 2 or 3 andX.sup..crclbar. represent one equivalentof a benzoate or naphthoate, which is optionally substituted by chlorine, bromine, methyl, methoxy, hydroxyl, cyano and/or hydroxycarbonyl,of a benzenesulphonate which is substituted by hydroxyl, amino or nitro,of a naphthalenesulphonate which is optionally substituted by hydroxyl, amino or a sulphonic acid group, orof a fluorine-substituted anion of a C.sub.4 - to C.sub.18 -alkanecarboxylic or -alkanesulphonic acid.
    Type: Grant
    Filed: February 19, 1992
    Date of Patent: March 8, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Berneth, Horst Harnisch, Roderich Raue, Jurgen-Rolf Hassdenteufel, Matthias Kocher
  • Patent number: 5235045
    Abstract: A class of predominantly hydrophobic non-azo N-substituted 1,8-naphthalimide compounds, each bearing, at its 3-position, a nucleofuge and, at its 4-position, a heteroatomic electron-releasing group. The heteroatomic electron-releasing group is being characterized as having a heteroatom directly linked to the 4-position of the ring, and having at least one hydrogen directly attached to the heteroatom. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species initiate chemical changes in lipid bilayer membranes of viruses and other target cells. These changes can eradicate viruses and other target cells. The activated species can also cause structural changes in lipid and any associated proteins and polypeptides at a level beneath the surface of the membrane, leading to polymerization and crosslinking.
    Type: Grant
    Filed: March 19, 1992
    Date of Patent: August 10, 1993
    Assignee: MicroBioMed Corporation
    Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
  • Patent number: 5206249
    Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 11, 1991
    Date of Patent: April 27, 1993
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Jung-Hui Sun
  • Patent number: 5206250
    Abstract: There are provided novel bis-naphthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing such compounds.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: April 27, 1993
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Jung-Hui Sun
  • Patent number: 5202333
    Abstract: The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: April 13, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
  • Patent number: 5202318
    Abstract: Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: April 13, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
  • Patent number: 5162335
    Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.
    Type: Grant
    Filed: November 27, 1989
    Date of Patent: November 10, 1992
    Assignee: Duphar International Research B.V.
    Inventors: Maurits E. A. Vandewalle, Johan T. A. Van der Eycken, Ineke van Wijngaarden, Roelof van Hes, Antonius Hulkenberg, Christophorus M. J. F. Keet
  • Patent number: 5118684
    Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: April 3, 1991
    Date of Patent: June 2, 1992
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5097034
    Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5095119
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alkyl, phenyl, benzyl or phenethyl; Y is --CH.sub.2--, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: March 10, 1992
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger
  • Patent number: 5086059
    Abstract: There are provided novel bis-napthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing intermediates to such compounds.
    Type: Grant
    Filed: June 7, 1990
    Date of Patent: February 4, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Robert J. Ardecky, Arthur D. Patten, Jung-Hui Sun
  • Patent number: 5076831
    Abstract: Substituted 1,8-naphthalenedicarboximides of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, and Z have the meanings recited in the disclosure are disclosed as new compounds suitable for use as antidotes in herbicidal compositions.
    Type: Grant
    Filed: November 20, 1990
    Date of Patent: December 31, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Saupe, Norbert Meyer, Peter Plath, Ulrich Schirmer, Bruno Wuerzer, Karl-Otto Westphalen, Manfred Patsch, Juergen Pfister
  • Patent number: 5066800
    Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: November 19, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Masami Okabe
  • Patent number: 5064965
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alky, phenyl, benzyl or phenylethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or O; b is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylakyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: November 12, 1991
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger
  • Patent number: 5039681
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: August 13, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5023338
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alky, phenyl, benzyl or phenethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: June 11, 1991
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger
  • Patent number: 5017702
    Abstract: Useful stabilizers for organic material, in particular plastics and paints, and metal ion deactivators are amides of the formula ##STR1## where R.sup.1 and R.sup.2 are singly methyl or together tetramethylene or pentamethylene, R.sup.3 is hydrogen, alkyl, alkoxycarbonyl, alkanoyl, benzyl, hydroxyethyl, cyanomethyl or aminomethyl, n is 1, 2 or 3 and--when n is 1--R.sup.4 is hydrogen and R.sup.5 is --CO--R.sup.6 is H, alkyl, cycloalkyl, aralkyl, phenoxyalkyl, aryl, a 5- or 6-membered heterocycle, alkoxy, aryloxy, cycloalkyloxy, phenylalkoxy, carbamoyl or --SO.sub.2 --R.sup.8 where R.sup.8 is alkyl or phenyl or ##STR2## is a phthalimide group or--when n is 2--R.sup.4 is H and R.sup.5 is --CO--Z--CO-- where Z is a chemical bond, C.sub.1 -C.sub.8 -alkylene, oxaalkylene, phenylene, cyclohexylene, biphenylene, biphenylene oxide, dioxyphenylene, diaminophenylene, diaminocyclohexylene, 1-.OMEGA.-diiminoalkylene or a 2-valent heterocycle or ##STR3## is a pyromellimide group or--when n is 3--R.sup.4 is H and R.sup.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: May 21, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
  • Patent number: 5011840
    Abstract: A series of novel 5-substituted imidazolidinedione derivatives and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. 5-Naphthalimido-imidazolidine-2,4-dione and 5-[3-(4'-bromo-2'-fluorobenzyl)-3,4-dihydro-4-oxophthalazin-1-yl]-imidazol idine-2,4-dione represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.
    Type: Grant
    Filed: May 5, 1989
    Date of Patent: April 30, 1991
    Assignee: Pfizer Inc.
    Inventor: Reinhard Sarges
  • Patent number: 4942169
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: March 10, 1989
    Date of Patent: July 17, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4927926
    Abstract: The present invention relates to new heterocyclic compounds, derivatives of 7-(1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids, characterized in that they correspond to formula (I) ##STR1## The invention also relates to the preparation of these compounds and their applications as medicines.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: May 22, 1990
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Juan P. Corominas, Jordi F. Constansa, Augusto C. Pinol
  • Patent number: 4922020
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## B is a group of the formula: ##STR3## when B is of Formula III, X is of Formula III;when B is of Formula IV,X is selected from H, phenyl, substituted phenyl, naphthyl, substituted naphthyl, thienyl, substituted thienyl, thiazol-5-yl and substituted thiazol-5-yl in which the substituents are selected from NR.sup.7 R.sup.8, NO.sub.2, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyl, halogen, cyano and phenyl;each Q is independently selected from H, C.sub.1-4 -alkyl, phenyl and benzyl;and wherein each benzene ring in Formulae II, III and IV has no further substituents or carries 1 or 2 further substituents selected from halogen, C.sub.1-4 -alkyl and C.sub.1-4 -alkoxy.The compound is suitable for use as a charge transport material in organic photoconductors, as a charge control agent in electroreprographic toners and as a color former in pressure sensitive recording materials.
    Type: Grant
    Filed: March 17, 1988
    Date of Patent: May 1, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter Gregory, Nigel Hughes
  • Patent number: 4919848
    Abstract: To quench the fluorescence generated by anionic optical brighteners, virtually colourless, water-soluble, cationic compounds are used which contain at least one cationic group per molecule or per repeating structural unit and at least two nitro group-free naphthalene-peridicarboxylic acid imide groups per molecule or at least one such group per repeating structural unit.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: April 24, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventor: Horst Harnisch
  • Patent number: 4892973
    Abstract: Disclosed herein is a novel process for producing 1,1-diphenylalkenes, comprising contacting lead peroxide with 1,1-diphenylalkanes having the structure wherein a nitrogen atom of a tertiary amino group is bonded to the para-position of each of the two benzene rings of the 1,1-diphenylalkane, thereby obtaining the corresponding 1,1-diphenylalkenes.
    Type: Grant
    Filed: August 31, 1988
    Date of Patent: January 9, 1990
    Assignee: Yamada Chemical Co., Ltd.
    Inventors: Kozo Mizuno, Hideaki Fujisaki, Yoshinori Uda, Tadashi Imai, Katsuhiko Tsunemitsu
  • Patent number: 4892950
    Abstract: Process for the preparation of naphthalene-1,8-dicarboximide which is optionally substituted in the naphthalene ring, characterized in that naphthalene-1,8-dicarboxylic anhydride which is optionally substituted in the naphthalene ring is reacted with an ammonium salt in an aqueous medium at a pH near to the neutral point, the reaction mixture is then acidified to a pH of 1 to 4 and the pH is subsequently adjusted to a value near to the neutral point.
    Type: Grant
    Filed: June 9, 1988
    Date of Patent: January 9, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Detlef-Ingo Schutze, Klaus Wunderlich, Karl-Heinz Reinhardt, Martin Wienkenhover
  • Patent number: 4849431
    Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: July 18, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4841052
    Abstract: Positively charged electrophotographic toners contain, in addition to conventional resin and pigment particles, an additive reinforcing the cationic charge, of the general formula ##STR1## in which R.sup.1 and R.sup.2 each represent hydrogen, chlorine,bromine, hydroxyl, C.sub.1 -C.sub.4 -alkoxy or carboxyl,A represents C.sub.1 -C.sub.5 -alkylene or --C.sub.6 H.sub.4 --CH.sub.2 -- (m or p),m represents 0 or 1,n represents 1 or 2K.sup..sym. represents ##STR2## R.sup.3 represents C.sub.1 -C.sub.18 -alkyl, carbamoyl-C.sub.1 -C.sub.2 -alkyl, C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.2 -alkyl, benzyl, cyclohexyl or allyl,R.sup.4 represents C.sub.1 -C.sub.4 -alkyl or a single bond linked to D,R.sup.5 represents C.sub.1 -C.sub.4 -alkyl,D represents --CH.sub.2, --CH.sub.2 --CO--, --CH.sub.2 --CO--NH-- orW represents ##STR3## --CO-- or a single bond,Z represents --CH.sub.2 --, ##STR4## --O--, --S--, --SO.sub.2 -- or a single bond and An.sup..crclbar. represents an anion.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: June 20, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Harnisch, Roderich Raue
  • Patent number: 4782064
    Abstract: This invention concerns novel 2-heteroarylalkyl-1H-benz[de]isoquinoline-1,3(2H)-diones which are useful as inhibitors of thromboxane synthetase and/or as hypotensive agents in the treatment of hypertension and myocardial ischemia.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: November 1, 1988
    Assignee: American Cyanamid Co.
    Inventors: William B. Wright, Jr., Andrew S. Tomcufcik, Nancy H. Eudy
  • Patent number: 4614820
    Abstract: Chemical compounds are provided that are novel 3,6-disubstituted-1,8-naphthalimides (I), as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents. ##STR1## .
    Type: Grant
    Filed: February 13, 1986
    Date of Patent: September 30, 1986
    Assignee: Warner-Lambert Co.
    Inventors: Robert K. Zee-Cheng, Chia C. Cheng
  • Patent number: 4595756
    Abstract: Cationic compounds of the formula (1) ##STR1## in which R denotes alkyl, hydroxyalkyl, alkoxyalkyl, phenylalkyl, or phenoxyalkyl,R' denotes alkyl, hydroxyalkyl, benzyl, or allyl andX.sup.(-) denotes a colorless anion, process for their manufacture and their use.
    Type: Grant
    Filed: May 24, 1984
    Date of Patent: June 17, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Norbert Schonberger, Erich Schinzel, Thomas Martini, Gunter Rosch
  • Patent number: 4578474
    Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: March 25, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Peter C. Wade
  • Patent number: 4530929
    Abstract: A class of novel fused-ring, benzotricyclic, nitrogen-containing diones useful as agents in reversing electroconvulsive shock-induced amnesia. A method of preparing the compounds, pharmaceutical compositions including the compounds, and a method of reversing electroconvulsive shock-induced amnesia are disclosed.
    Type: Grant
    Filed: February 2, 1984
    Date of Patent: July 23, 1985
    Assignee: Warner-Lambert Company
    Inventors: Donald E. Butler, Michael R. Pavia, Fred M. Hershenson
  • Patent number: 4508900
    Abstract: Cationic compounds of the formula (1) ##STR1## in which R denotes alkyl, hydroxyalkyl, alkoxyalkyl, phenylalkyl, or phenoxyalkyl,R' denotes alkyl, hydroxyalkyl, benzyl, or allyl andX.sup.(-) denotes a colorless anion,process for their manufacture and their use.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: April 2, 1985
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Norbert Schonberger, Erich Schinzel, Thomas Martini, Gunter Rosch
  • Patent number: 4499266
    Abstract: Chemical compounds are provided that are novel 3,6-dinitro-1,8-naphthalimides (I), as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents.
    Type: Grant
    Filed: April 1, 1983
    Date of Patent: February 12, 1985
    Assignee: Warner-Lambert Company
    Inventors: Chia C. Cheng, Robert K. Zee-Cheng
  • Patent number: 4497953
    Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
    Type: Grant
    Filed: January 3, 1983
    Date of Patent: February 5, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Peter C. Wade
  • Patent number: 4432886
    Abstract: Cationic fluorescent whitening agents of the formula ##STR1## wherein B is a fluorescent whitening agent containing basic tertiary amino groups, m is the number of basic amino groups, and each of R.sub.1, R.sub.2 and R.sub.3 is alkyl of 1 to 4 carbon atoms which is unsubstituted or substituted by non-chromophoric groups, or is alkenyl of 2 to 4 carbon atoms which is unsubstituted or substituted by non-chromophoric groups. These compounds have good solubility in water and they make it possible to prepare concentrated solutions and can be used for whitening organic material.
    Type: Grant
    Filed: September 22, 1982
    Date of Patent: February 21, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans R. Meyer
  • Patent number: 4384121
    Abstract: Cationic fluorescent whitening agents of the formula ##STR1## wherein B is a fluorescent whitening agent containing basic tertiary amino groups, m is the number of basic amino groups, and each of R.sub.1, R.sub.2 and R.sub.3 is alkyl of 1 to 4 carbon atoms which is unsubstituted or substituted by non-chromophoric groups, or is alkenyl of 2 to 4 carbon atoms which is unsubstituted or substituted by non-chromophoric groups. These compounds have good solubility in water and they make it possible to prepare concentrated solutions and can be used for whitening organic material.
    Type: Grant
    Filed: October 27, 1980
    Date of Patent: May 17, 1983
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans R. Meyer
  • Patent number: 4220777
    Abstract: Naphthalimide derivatives of the general formula ##STR1## where R.sup.1 is hydrogen or C.sub.1 - to C.sub.4 -alkyl,R.sup.2 is nitrile or a radical containing a carbonyl group or an acetalized carbonyl group andR.sup.3 and R.sup.4 are unsubstituted or substituted alkyl.The compounds are excellent optical brighteners, especially for synthetic fibers.
    Type: Grant
    Filed: November 17, 1978
    Date of Patent: September 2, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochen Karg, Manfred Patsch, Walter Himmele
  • Patent number: 4204063
    Abstract: N-substituted-3-substituted naphthalimides are prepared by reacting 3-substituted naphthalic acid with a compound having a primary amino group. The naphthalimides possess cytotoxic properties.
    Type: Grant
    Filed: June 2, 1978
    Date of Patent: May 20, 1980
    Assignee: Laboratorios Made, S.A.
    Inventors: Miguel F. Brana, Antonio M. Sanz, Rafael P. Alvarez-Ossorio, Cristobal M. Roldan, Cristina R. Fernandez de Gamboa
  • Patent number: 4180579
    Abstract: Compounds of the following formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, nitro, cyano, and trifluoromethyl, and R is selected from a triacetyl substituted pentose, pentose, a tetraacetyl substituted hexose, hexose, a hydroxy substituted cycloalkyl of 5 to 7 carbons, ##STR2## wherein n is 1 or 2 and R.sup.3 is hydrogen, an alkali metal or alkaline earth metal ion; are disclosed. These compounds possess useful anti-inflammatory activity.
    Type: Grant
    Filed: July 12, 1978
    Date of Patent: December 25, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter C. Wade, Berthold R. Vogt
  • Patent number: 4170651
    Abstract: Compounds of the following formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, nitro, cyano, and trifluoromethyl, and R is selected from a triacetyl substituted pentose, pentose, a tetraacetyl substituted hexose, hexose, a hydroxy substituted cycloalkyl of 5 to 7 carbons, ##STR2## wherein n is 1 or 2 and R.sup.3 is hydrogen, an alkali metal or alkaline earth metal ion; are disclosed. These compounds possess useful anti-inflammatory activity.
    Type: Grant
    Filed: July 12, 1978
    Date of Patent: October 9, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter C. Wade, Berthold R. Vogt
  • Patent number: 4150025
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group; R.sub.2 and R.sub.5, independently from each other, represent a hydrogen atom, a halogen atom or a lower alkyl group; one of R.sub.3 and R.sub.4 represents an imido group of the formula ##STR2## in which Y represents a 1,2-phenylene, 1,2-naphthylene, 2,3-naphthylene or 1,8-naphtylene group optionally containing at least one substituent, and the other represents a hydrogen atom, a halogen atom or a lower alkyl group; R.sub.6 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and X represents a halogen atom; with the proviso that when R.sub.3 represents the imido group, R.sub.2 represents a hydrogen or halogen atom. This compound can be prepared by reacting a corresponding quinaldine derivative with a tetrahalophthalic acid or a reactive derivative thereof. A yellow organic pigment comprising this compound as a coloring ingredient is useful for coloring polymeric materials.
    Type: Grant
    Filed: February 10, 1977
    Date of Patent: April 17, 1979
    Assignee: Teijin Limited
    Inventors: Keizo Shimada, Toshiaki Harada, Masahiro Koga
  • Patent number: 4146720
    Abstract: Compounds having the formula ##STR1## wherein Y is 2-dimethylaminoethyl, 2-diethylaminoethyl, 2-(N-pyrrolidino)ethyl or 2-(N-piperidino)ethyl. The compounds are prepared by reacting 3-nitronaphthalic acid, or corresponding anhydride, with the corresponding primary amine. The compounds possess cytostatic and raticide properties.
    Type: Grant
    Filed: September 19, 1977
    Date of Patent: March 27, 1979
    Assignee: Laboratorios Made, S.A.
    Inventors: Cristobal M. Roldan, Miguel F. Brana, Jose M. C. Berlanga