The Nitrogen Is Bonded Directly To A Carbocyclic Ring Of The Tricyclo Ring System Patents (Class 546/100)
  • Patent number: 5637710
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: June 10, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5633265
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5629326
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Hoechst-Marion-Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5624927
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 29, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5614543
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 25, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
  • Patent number: 5612343
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5612342
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5607945
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5602158
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5602159
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5599821
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5597842
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 28, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5591745
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5589495
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 31, 1996
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5585497
    Abstract: The invention relates to substituted 1-naphyl-3-pyrazolecarboxamides of formula I: ##STR1## These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: December 17, 1996
    Assignee: Sanofi
    Inventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
  • Patent number: 5580890
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5580879
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5578624
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 26, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5571803
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5552544
    Abstract: An antitumor 5-nitrobenzo[de]isoquinoline-1,3-dione of the formula I ##STR1## where n is 1 or 2, R.sup.1 and R.sup.2 are identical or different and are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -hydroxyalkyl, pyrrolidinyl, morpholino, piperidinyl or piperacinyl and R.sup.3 and R.sup.4 are identical or different and are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -acyl, C.sub.2 --C.sub.7 -alkoxycarbonyl, ureyl, aminocarbonyl or C.sub.2 -C.sub.7 -alkylaminocarbonyl, and its salts with physiologically tolerated acids, are described.
    Type: Grant
    Filed: June 4, 1990
    Date of Patent: September 3, 1996
    Inventors: Miguel F. Bra na, Jos e M. Castellano Berlanga, Marina Mor an Moset, Erich Schlick, Gerhard Keilhauer
  • Patent number: 5502059
    Abstract: The invention relates to substituted 1-naphthyl-3-pyrazolecarboxamides of formula I: ##STR1## Application: These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: March 26, 1996
    Assignee: Sanofi
    Inventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
  • Patent number: 5488110
    Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis(methylimino-2,1-ethanediyl)]-bis[5-nitro-1H-benz[d e]isoquinoline-1,3(2H)-dione], 2-[2-[N-methyl-N-[2-[[2-(5-nitro-1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-y l)ethyl]amino]ethyl]amino]ethyl]-5-nitro-1H-benz[de]isoquinoline-1,3(2H)-di one, 2,2'-[1,2-ethanediylbis(imino-2,1-ethanediyl)]-bis[5-nitro-1H-benz[de]isoq uinoline-1,3(2H)-dione], pharmaceutical compositions containing them, and methods of using them to treat solid tumor carcinomas in mammals.
    Type: Grant
    Filed: March 29, 1994
    Date of Patent: January 30, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Jung-Hui Sun
  • Patent number: 5420137
    Abstract: The monohydrochloride and the monomethanesulfonate of amonafide are described. The salts have good pharmaceutical properties besides their antitumor action.
    Type: Grant
    Filed: June 20, 1994
    Date of Patent: May 30, 1995
    Assignee: Knoll AG
    Inventors: Miguel F. Brana, Jose M. C. Berlanga, Reinhard Spengler, Christine Tetzner
  • Patent number: 5420136
    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: August 9, 1993
    Date of Patent: May 30, 1995
    Assignee: MicroBioMed Corporation
    Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
  • Patent number: 5308773
    Abstract: The use of a class of non-azo 1,8-naphthalimide dyes for the detection and quantitation of a paramagnetic metal cation in a non-aqueous medium and some of the dyes that will complex with a paramagnetic metal cation. The concentration of the paramagnetic metal cation is determined by monitoring differences in the detected fluorescent emission spectra of the non-azo 1,8-naphthalimide dye solution when it is mixed with paramagnetic metal cations present in the non-aqueous medium. The detected fluorescent emission spectra will vary in relation to the presence or amount of the paramagnetic metal cation in the mixture.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: May 3, 1994
    Assignee: MicroBioMed Corp.
    Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
  • Patent number: 5283355
    Abstract: Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted alkyl, alkoxy, Cl or Br;R is a group of Formula (3) ##STR2## R.sup.1 and R.sup.2 are each independently alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form an optionally substituted 4, 5 or 6 membered alicyclic or heterocyclic ring;R.sup.3 is H;Z is Cl, Br or A--NH; andA is H or the residue of a primary amine.
    Type: Grant
    Filed: October 22, 1991
    Date of Patent: February 1, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventor: William J. E. Norris
  • Patent number: 5266569
    Abstract: Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.
    Type: Grant
    Filed: February 2, 1993
    Date of Patent: November 30, 1993
    Assignee: Pfizer Inc.
    Inventor: Katherine E. Brighty
  • 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: 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: 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: 5183821
    Abstract: N-(2-dimethylaminoethyl)-3-amino-1,8-naphthalimide (amonafide) is an effective agent for the treatment of leukemias and solid tumors.
    Type: Grant
    Filed: July 8, 1991
    Date of Patent: February 2, 1993
    Assignee: Laboratories Knoll, S.A.
    Inventors: Miguel F. Brana, Antonio M. Sanz, Rafael P. Alvarez-Ossorio, Cristobal M. Roldan, Cristina R. F. De Gamboa, Jesus G. Garcia, Jose M. C. Berlanga
  • 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: 5082938
    Abstract: Enhanced branched chain hydroxyl compounds are provided of formulaY--(Z).sub.1-6wherein Y is the residue of a nucleophile devoid of conjugated divalent linking moieties, and each Z is a poly(oxyalkylene) moiety having a molecular weight of from about 200-10,000 and containing at least one glycidol residue, wherein at least one of the primary oxy sites of said glycidol residue is linked preferably directly to a first epoxide residue of three or more carbons, and wherein said first epoxide residue is linked through a secondary oxy site preferably directly to a second epoxide reside having a primary terminal hydroxyl.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: January 21, 1992
    Assignee: Milliken Research Corporation
    Inventors: Edward W. Kluger, David J. Moody
  • 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: 5061712
    Abstract: Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce a compound of the formula ##STR4## reacting the compound of the formula (III) with a compound of the formula ##STR5## to give a compound of the formula ##STR6## and then eliminating the amino-protective group ##STR7##
    Type: Grant
    Filed: May 25, 1990
    Date of Patent: October 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • Patent number: 4990517
    Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1, and addition products thereof.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: February 5, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • 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: 4874863
    Abstract: Bisnaphthalimides of the formula I ##STR1## where X.sup.1 to X.sup.4 and R have the meanings stated in the description, and their preparation are described. The compounds are cytotoxic towards human cells in vitro.
    Type: Grant
    Filed: March 1, 1988
    Date of Patent: October 17, 1989
    Assignee: Knoll AG
    Inventors: Miguel F. Brana, Jose M. C. Berlanga, Gerhard Keilhauer, Erich Schlick
  • Patent number: 4816453
    Abstract: Compounds of formula (i) and pharmaceutically acceptable salts thereof: ##STR1## wherein: m and n are independently 1 or 2 and p is 0, 1 or 2 such that m+n+p.gtoreq.3;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein either R.sub.3 is hydrogen or C.sub.1-7 alkanoyl; and X is chloro, bromo, methylthio or nitro; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation, and their use as pharmaceuticals.
    Type: Grant
    Filed: September 17, 1986
    Date of Patent: March 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Eric A. Watts
  • 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: 4473693
    Abstract: Fluorescent yellow dyes of the aminonaphthalimide type which have the following structures: ##STR1## In the formula above alk (alkali metal) may be substituted for Li.sup.+ and thus alk may be Li.sup.+, Na.sup.+, or K.sup.+, but the preferable structure is Li.sup.+. These dyes have shown superior activity in intracellular use in vivo in tissues such as turtle retina and wholemount tissue observation.
    Type: Grant
    Filed: August 4, 1978
    Date of Patent: September 25, 1984
    Inventor: Walter W. Stewart
  • Patent number: 4371694
    Abstract: Compounds of Formula I or Formula II ##STR1## where A is an electron withdrawing group and B is a secondary or tertiary amino group or the group OD where D is H, aryl or an aliphatic group are made by reacting a corresponding compound of Formula Ia or Formula IIa ##STR2## in a solvent with a reagent selected from organic primary and secondary amines and compounds of the formula MOD where M is an alkali metal and A and D are as defined above. In this process the nitro group and the group B in Formula I and Ia are in the 2- or 4- position and the compounds of Formula I, Ia, II and IIa may optionally be further substituted. Preferably a primary or secondary amine is reacted with a compound of formula Ia, preferably using dimethylformamide as solvent. The process can result in the production of novel compounds, including (1) Compounds of Formula III wherein each group A is CO.sub.
    Type: Grant
    Filed: July 1, 1980
    Date of Patent: February 1, 1983
    Assignee: Brent Chemicals International Limited
    Inventors: Michael S. Alexiou, Philip I. Brittain, John H. P. Tyman
  • Patent number: 4302399
    Abstract: Acetylation of residual primary and secondary alkyl amine groups in polymeric colorants, when said colorants are in the form of a crude preparation reaction mixture, is disclosed. The acetylation improves the colorants' water solubility.
    Type: Grant
    Filed: March 10, 1980
    Date of Patent: November 24, 1981
    Assignee: Dynapol
    Inventors: Daniel J. Dawson, Robert E. Wingard, Guy A. Crosby
  • Patent number: 4207107
    Abstract: Ortho-quinone diazide compounds of the formula ##STR1## wherein R is an organic radical are useful sensitizers for photoresist compositions and intermediates for novel dyes.
    Type: Grant
    Filed: August 23, 1978
    Date of Patent: June 10, 1980
    Assignee: RCA Corporation
    Inventor: Daniel L. Ross
  • 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: 4200752
    Abstract: The present disclosure is directed to novel quenchable, fluorescent dyestuffs which are substantially soluble in low surface tension, substantially non-polar oily solvents, e.g., refined kerosene, and are trisubstituted 4-aminonaphthalimides having the structure formula: ##STR1## wherein R.sub.1 is a member selected from the group consisting of:(a) alkyl groups having from two to twelve carbon atoms,(b) substituted akyl groups having at least two carbon atoms,(c) phenylalkyl groups whose alkyl moiety has from one to four carbon atoms and(d) alicyclic rings having from five to six carbon atoms in the alicyclic ring;R.sub.2 and R.sub.
    Type: Grant
    Filed: February 16, 1978
    Date of Patent: April 29, 1980
    Inventor: Robert C. Bertelson
  • Patent number: 4172202
    Abstract: N-substituted amides or optionally N-substituted hydrazides of 4-amino-naphthalic acids which may be substituted in 3-position by a sulfo group are obtained by reacting 4-halo-1,8-naphthalic anhydride with a primary amine or an optionally N-substituted hydrazine having a pK.sub.a -value of at least 8, exchanging in the so-obtained 4-halo-naphthalimide the halogen for the amino group by reacting it with ammonia and, optionally, subsequent sulfonation. The products are dyeing matters useful for the coloration of synthetic fibers, plastics, oils, waxes, resins, paper, printing pastes, lacquers or natural polyamides, especially for daylight-fluorescence pigments.
    Type: Grant
    Filed: January 9, 1978
    Date of Patent: October 23, 1979
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Theodor Papenfuhs
  • Patent number: 4169203
    Abstract: Acetylation of residual primary and secondary alkyl amine groups present in the structure of polymeric colorants and the acetylated colorant products are disclosed. The acetylation is a post production step. The acetylation improves the colorants' water solubility.
    Type: Grant
    Filed: November 18, 1976
    Date of Patent: September 25, 1979
    Assignee: Dynapol
    Inventors: Robert E. Wingard, Daniel J. Dawson