Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly Or Indirectly To The Tricyclo Ring System By Nonionic Bonding Patents (Class 546/99)
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Patent number: 5510486Abstract: 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: GrantFiled: July 26, 1994Date of Patent: April 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: James Robinson, III, John C. Rohloff, Bruce A. Kowalczyk
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Patent number: 5492914Abstract: 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: GrantFiled: July 28, 1994Date of Patent: February 20, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Paul E. Weller, Douglas L. Wren
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Patent number: 5491236Abstract: 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: GrantFiled: December 4, 1991Date of Patent: February 13, 1996Assignee: The Upjohn CompanyInventor: Chiu-Hong Lin
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Patent number: 5420234Abstract: 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: GrantFiled: July 26, 1994Date of Patent: May 30, 1995Inventors: Allan S. Hay, Hossein Ghassemi
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Patent number: 5397708Abstract: 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: GrantFiled: May 13, 1993Date of Patent: March 14, 1995Assignee: Nalco Chemical CompanyInventors: Ronald B. Lessard, Manian Ramesh
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Patent number: 5376664Abstract: 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: GrantFiled: February 11, 1993Date of Patent: December 27, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Robert F. Kaltenbach, III, Jung-Hui Sun, Robert J. Cherney, Steven P. Seitz
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Patent number: 5359092Abstract: 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: GrantFiled: June 2, 1993Date of Patent: October 25, 1994Inventors: Allan S. Hay, Hossein Ghassemi
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Patent number: 5306720Abstract: 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: GrantFiled: December 20, 1991Date of Patent: April 26, 1994Assignee: 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
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Patent number: 5292881Abstract: 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: GrantFiled: February 19, 1992Date of Patent: March 8, 1994Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Horst Harnisch, Roderich Raue, Jurgen-Rolf Hassdenteufel, Matthias Kocher
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Patent number: 5235045Abstract: 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: GrantFiled: March 19, 1992Date of Patent: August 10, 1993Assignee: MicroBioMed CorporationInventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
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Patent number: 5206249Abstract: 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: GrantFiled: December 11, 1991Date of Patent: April 27, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Jung-Hui Sun
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Patent number: 5206250Abstract: There are provided novel bis-naphthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing such compounds.Type: GrantFiled: March 27, 1991Date of Patent: April 27, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Jung-Hui Sun
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Patent number: 5202333Abstract: 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: GrantFiled: May 22, 1991Date of Patent: April 13, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
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Patent number: 5202318Abstract: 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: GrantFiled: May 28, 1991Date of Patent: April 13, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark, Richard M. Eglen, William L. Smith, Klaus K. Weinhardt
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Patent number: 5162335Abstract: 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: GrantFiled: November 27, 1989Date of Patent: November 10, 1992Assignee: 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
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Patent number: 5118684Abstract: 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: GrantFiled: April 3, 1991Date of Patent: June 2, 1992Assignee: 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
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Patent number: 5097034Abstract: 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: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5095119Abstract: 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: GrantFiled: November 16, 1990Date of Patent: March 10, 1992Assignee: American Home Products CorporationInventors: Timothy D. Ocain, David D. Deininger
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Patent number: 5086059Abstract: There are provided novel bis-napthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing intermediates to such compounds.Type: GrantFiled: June 7, 1990Date of Patent: February 4, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Robert J. Ardecky, Arthur D. Patten, Jung-Hui Sun
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Patent number: 5076831Abstract: 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: GrantFiled: November 20, 1990Date of Patent: December 31, 1991Assignee: BASF AktiengesellschaftInventors: Thomas Saupe, Norbert Meyer, Peter Plath, Ulrich Schirmer, Bruno Wuerzer, Karl-Otto Westphalen, Manfred Patsch, Juergen Pfister
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Patent number: 5066800Abstract: 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: GrantFiled: April 27, 1990Date of Patent: November 19, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Masami Okabe
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Patent number: 5064965Abstract: 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: GrantFiled: November 16, 1990Date of Patent: November 12, 1991Assignee: American Home Products CorporationInventors: Timothy D. Ocain, David D. Deininger
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Patent number: 5039681Abstract: 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: GrantFiled: February 14, 1990Date of Patent: August 13, 1991Assignee: 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
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Patent number: 5023338Abstract: 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: GrantFiled: March 8, 1990Date of Patent: June 11, 1991Assignee: American Home Products CorporationInventors: Timothy D. Ocain, David D. Deininger
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Patent number: 5017702Abstract: 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: GrantFiled: July 6, 1989Date of Patent: May 21, 1991Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
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Patent number: 5011840Abstract: 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: GrantFiled: May 5, 1989Date of Patent: April 30, 1991Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4942169Abstract: 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: GrantFiled: March 10, 1989Date of Patent: July 17, 1990Assignee: 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
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Patent number: 4927926Abstract: 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: GrantFiled: December 27, 1988Date of Patent: May 22, 1990Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Juan P. Corominas, Jordi F. Constansa, Augusto C. Pinol
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Patent number: 4922020Abstract: 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: GrantFiled: March 17, 1988Date of Patent: May 1, 1990Assignee: Imperial Chemical Industries PLCInventors: Peter Gregory, Nigel Hughes
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Patent number: 4919848Abstract: 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: GrantFiled: September 30, 1986Date of Patent: April 24, 1990Assignee: Bayer AktiengesellschaftInventor: Horst Harnisch
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Patent number: 4892973Abstract: 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: GrantFiled: August 31, 1988Date of Patent: January 9, 1990Assignee: Yamada Chemical Co., Ltd.Inventors: Kozo Mizuno, Hideaki Fujisaki, Yoshinori Uda, Tadashi Imai, Katsuhiko Tsunemitsu
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Patent number: 4892950Abstract: 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: GrantFiled: June 9, 1988Date of Patent: January 9, 1990Assignee: Bayer AktiengesellschaftInventors: Detlef-Ingo Schutze, Klaus Wunderlich, Karl-Heinz Reinhardt, Martin Wienkenhover
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Patent number: 4849431Abstract: 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: GrantFiled: December 24, 1986Date of Patent: July 18, 1989Assignee: 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
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Patent number: 4841052Abstract: 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: GrantFiled: July 28, 1988Date of Patent: June 20, 1989Assignee: Bayer AktiengesellschaftInventors: Horst Harnisch, Roderich Raue
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Patent number: 4782064Abstract: 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: GrantFiled: July 21, 1986Date of Patent: November 1, 1988Assignee: American Cyanamid Co.Inventors: William B. Wright, Jr., Andrew S. Tomcufcik, Nancy H. Eudy
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Patent number: 4614820Abstract: 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: GrantFiled: February 13, 1986Date of Patent: September 30, 1986Assignee: Warner-Lambert Co.Inventors: Robert K. Zee-Cheng, Chia C. Cheng
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Patent number: 4595756Abstract: 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: GrantFiled: May 24, 1984Date of Patent: June 17, 1986Assignee: Hoechst AktiengesellschaftInventors: Norbert Schonberger, Erich Schinzel, Thomas Martini, Gunter Rosch
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Patent number: 4578474Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.Type: GrantFiled: November 19, 1984Date of Patent: March 25, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Peter C. Wade
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Patent number: 4530929Abstract: 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: GrantFiled: February 2, 1984Date of Patent: July 23, 1985Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Michael R. Pavia, Fred M. Hershenson
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Patent number: 4508900Abstract: 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: GrantFiled: September 13, 1982Date of Patent: April 2, 1985Assignee: Hoechst AktiengesellschaftInventors: Norbert Schonberger, Erich Schinzel, Thomas Martini, Gunter Rosch
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Patent number: 4499266Abstract: 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: GrantFiled: April 1, 1983Date of Patent: February 12, 1985Assignee: Warner-Lambert CompanyInventors: Chia C. Cheng, Robert K. Zee-Cheng
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Patent number: 4497953Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.Type: GrantFiled: January 3, 1983Date of Patent: February 5, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Peter C. Wade
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Patent number: 4432886Abstract: 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: GrantFiled: September 22, 1982Date of Patent: February 21, 1984Assignee: Ciba-Geigy CorporationInventor: Hans R. Meyer
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Patent number: 4384121Abstract: 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: GrantFiled: October 27, 1980Date of Patent: May 17, 1983Assignee: Ciba-Geigy CorporationInventor: Hans R. Meyer
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Patent number: 4220777Abstract: 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: GrantFiled: November 17, 1978Date of Patent: September 2, 1980Assignee: BASF AktiengesellschaftInventors: Jochen Karg, Manfred Patsch, Walter Himmele
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Patent number: 4204063Abstract: 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: GrantFiled: June 2, 1978Date of Patent: May 20, 1980Assignee: Laboratorios Made, S.A.Inventors: Miguel F. Brana, Antonio M. Sanz, Rafael P. Alvarez-Ossorio, Cristobal M. Roldan, Cristina R. Fernandez de Gamboa
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Patent number: 4180579Abstract: 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: GrantFiled: July 12, 1978Date of Patent: December 25, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Peter C. Wade, Berthold R. Vogt
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Patent number: 4170651Abstract: 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: GrantFiled: July 12, 1978Date of Patent: October 9, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Peter C. Wade, Berthold R. Vogt
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Patent number: 4150025Abstract: 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: GrantFiled: February 10, 1977Date of Patent: April 17, 1979Assignee: Teijin LimitedInventors: Keizo Shimada, Toshiaki Harada, Masahiro Koga
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Patent number: 4146720Abstract: 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: GrantFiled: September 19, 1977Date of Patent: March 27, 1979Assignee: Laboratorios Made, S.A.Inventors: Cristobal M. Roldan, Miguel F. Brana, Jose M. C. Berlanga