The Nitrogen Is Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/105)
  • Patent number: 10350299
    Abstract: The present invention relates to complexes of transcription factor decoys, their delivery to bacteria and their formulation. In particular, the present invention resides in an antibacterial complex comprising a nucleic acid sequence and one or more delivery moieties selected from quaternary amine compounds; bis-aminoalkanes and unsaturated derivatives thereof, wherein the amino component of the aminoalkane is an amino group forming part of a heterocyclic ring; and an antibacterial peptide.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: July 16, 2019
    Assignee: PROCARTA BIOSYSTEMS LTD.
    Inventor: Michael McArthur
  • Patent number: 8765781
    Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an antitumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, said rings being linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: July 1, 2014
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Dmity A. Androsov
  • Publication number: 20140148451
    Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 29, 2014
    Applicants: Translational Genomics Research Institute, Van Andel Research Institute
    Inventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
  • Patent number: 8722701
    Abstract: Disclosed are 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine and the salt thereof, as well as the preparation method and medical use thereof. The compound can be useful for the preparation of medicaments for treating cardiovascular diseases, especially arrhythmia.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 13, 2014
    Assignees: Changchun Huayang High Technology, Inc., Jiangsu Shen ER Yang High Technology Co., Ltd.
    Inventor: Tonghui Wang
  • Publication number: 20140058099
    Abstract: The compounds represented fey the following general formula is is thermally stable and has excellent characteristics as a charge transport material [Ar1 represents a single bond, a benzene ring, etc.; X1 represents a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; either one of L1 and L2, and L3 and L4 bond to each other to represent a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; the other of L1 and L2, and L3 and L4 represent a hydrogen atom or a substituent; Y1 represents a linking group that links via a nitrogen atom, a boron atom or a phosphorus atom; R1, R2, R5 to R7 and R10 to R12 represent a hydrogen atom or a substituent; and n1 indicates an integer of 2 or more.].
    Type: Application
    Filed: March 2, 2012
    Publication date: February 27, 2014
    Applicant: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION
    Inventors: Atsushi Wakamiya, Hidetaka Nishimura, Yasujiro Murata, Tatsuya Fukushima, Hironori Kaji
  • Patent number: 8530496
    Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 10, 2013
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Justin M. Lopchuk
  • Publication number: 20130225517
    Abstract: The invention provides compounds of formula I: or salts thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I and therapeutic methods for treating cancer.
    Type: Application
    Filed: February 22, 2013
    Publication date: August 29, 2013
    Applicant: University of Iowa Research Foundation
    Inventor: University of Iowa Research Foundation
  • Publication number: 20130158065
    Abstract: Disclosed are 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine and the salt thereof, as well as the preparation method and medical use thereof. The compound can be useful for the preparation of medicaments for treating cardiovascular diseases, especially arrhythmia.
    Type: Application
    Filed: September 2, 2011
    Publication date: June 20, 2013
    Applicants: JIANGSU SHEN ER YANG HIGH TECHNOLOGY CO., LTD, CHANGCHUN HUAYANG HIGH TECHNOLOGY CO., LTD
    Inventor: Tonghui Wang
  • Publication number: 20130035351
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: August 3, 2011
    Publication date: February 7, 2013
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20120220537
    Abstract: N-substituted 9-aminoacridine and bis-acridino derivatives containing electron-withdrawing groups (EWG) or electron-donating groups (EDG), including amino acid residues, and one-pot methods for their synthesis are disclosed. The derivatives are potential candidates for cancer treatment.
    Type: Application
    Filed: November 1, 2010
    Publication date: August 30, 2012
    Applicant: ARIEL-UNIVERSITY RESEARCH AND DEVELOPMENT COMPANY LTD.
    Inventor: Gary Gellerman
  • Patent number: 8063062
    Abstract: Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: November 22, 2011
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Belal Shadid
  • Patent number: 8057990
    Abstract: The present invention provides a medicament for preventing/treating cancer, comprising a tacrine compound, or a compound promoting the binding between the tacrine compound and a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1.
    Type: Grant
    Filed: March 7, 2006
    Date of Patent: November 15, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masaaki Mori, Kimiko Kanehashi
  • Patent number: 7910739
    Abstract: The invention provides compounds of formula: which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the ?-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer's disease.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: March 22, 2011
    Assignee: Noscira, S.A.
    Inventors: Ana Martinez Gil, Isabel Dorronsoro Diaz, Laura Rubio Arrieta, Diana Alonso Gordillo, Ana Fuertes Huerta, Susana Morales-Alcelay, Maria Del Monte Millan, Esther Garcia Palomero, Paola Usan Egea, Celia De Austria, Miguel Medina Padilla, Pilar Munoz Ruiz
  • Publication number: 20100055682
    Abstract: This application concerns methods and compositions that can be used for detecting the Alzheimer disease in mammals, particularly in humans. It describes in particular serum markers for Alzheimer's disease and the way they are used for diagnostic procedures. It also concerns tools and/or kits that can be used for applying these procedures (reagents, probes, primers, antibodies, chips, cells, etc.) with the preparation thereof and the way to use them. The invention can be used to detect the presence or the progression of Alzheimer illness in mammals, including at early stages of the disease.
    Type: Application
    Filed: May 14, 2007
    Publication date: March 4, 2010
    Inventors: Fabien Schweighoffer, Laurent Bracco
  • Patent number: 7622478
    Abstract: The invention is directed to 1-nitroacridine derivative(s)/tumor inhibitor(s) compositions as well as methods for using said compositions for inhibiting or preventing tumor growth, particularly, prostate cancer cell growth and metastases.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: November 24, 2009
    Inventors: Raj Tiwari, Daniel Miller, Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela
  • Publication number: 20090226940
    Abstract: The present invention relates to fluorescent dyes based on acridine derivatives and use of such dyes, for example, in biochemical and/or cell based assays. A preferred feature of some of the dyes described is their long fluorescence lifetimes and their use to label biological molecules.
    Type: Application
    Filed: October 27, 2006
    Publication date: September 10, 2009
    Applicant: ITI Scotland Limited
    Inventors: Robert Ramage, Beatrice Maltman, Graham Cotton, Sarah Claire Monique Couturier, Robert Austin Simms McMordie
  • Publication number: 20080319001
    Abstract: The present invention relates to a 3,6,9 acridine compound and optionally substituted derivatives thereof that may be useful in the treatment of cancer. The invention also provides compositions comprising the compounds and uses thereof. Formula (I) wherein each of R1, R2, R3, R4 and R5 is either fluorine or is not present (i.e. represents a hydrogen atom); n represents 1 or 2.
    Type: Application
    Filed: March 2, 2006
    Publication date: December 25, 2008
    Inventors: Christina Martins, Stephen Neidle, Mekala Gunaratnam, John Stuart, Lloyd Kelland
  • Publication number: 20080176308
    Abstract: Novel heterodimers of tetrahydroacridines and tetrahydroquinolinones are disclosed. The heterodimers are capable of acting as both acetylcholinesterase inhibitors and N-methyl-D-aspartate (NMDA) receptor antagonists. The heterodimers may be used to improve cognitive defects via treatment or prevention in both humans and non-humans.
    Type: Application
    Filed: January 22, 2007
    Publication date: July 24, 2008
    Applicant: BIOTECHNOLOGY RESEARCH CORPORATION LIMITED
    Inventors: Nancy Y. IP, Fanny Chui Fun IP, Yueqing Hu, Yifan Han, Sookja Kim Chung
  • Publication number: 20080171765
    Abstract: New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines and quinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydrazineurea, hydrazinecarbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.
    Type: Application
    Filed: January 11, 2008
    Publication date: July 17, 2008
    Applicant: Academia Sinica
    Inventors: Tsann-Long Su, Ting-Chao Chou
  • Patent number: 7300930
    Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptabl
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: November 27, 2007
    Assignee: Cancer Research Technology Limited
    Inventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
  • Patent number: 7230105
    Abstract: The present invention relates to a new 9-aminoacridine derivative which exhibits prominent antitumor activity and low toxicity.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: June 12, 2007
    Assignee: Samjin Pharmaceutical Co., Ltd.
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang
  • Patent number: 7160896
    Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable sal
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: January 9, 2007
    Assignee: Cancer Research Technology Limited
    Inventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reskza
  • Patent number: 7041674
    Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: May 9, 2006
    Assignee: Boehringer Ingelhiem Pharma GmbH & Co. KG
    Inventors: Steffen Breitfelder, Matthias Hoffmann, Matthias Grauert, Michael P. Pieper, Georg Speck
  • Patent number: 6858742
    Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: February 22, 2005
    Assignee: AsiaGEN Corporation
    Inventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
  • Patent number: 6821983
    Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: November 23, 2004
    Assignee: Academia Sinica
    Inventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
  • Publication number: 20040219564
    Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.
    Type: Application
    Filed: October 22, 2003
    Publication date: November 4, 2004
    Applicant: AsiaGEN Corporation
    Inventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
  • Publication number: 20040132747
    Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
    Type: Application
    Filed: December 19, 2003
    Publication date: July 8, 2004
    Inventors: Peter Emig, Eckhard Gunther, Jurgen Schmidt, Bernd Nickel, Bernhard Kutscher
  • Patent number: 6743817
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Neurogen Corporation
    Inventors: George Maynard, LingHong Xie, Stanislaw Rachwal
  • Patent number: 6620936
    Abstract: The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrogen or (II) (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, —N═CHR′(wherein R′ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (III) (wherein R″ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower al
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: September 16, 2003
    Assignee: Samjin Pharmaceutical Co., Ltd.
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang, Jeong-Ho Joo
  • Patent number: 6589961
    Abstract: The invention is directed to novel 9-hydroxyalkylamino-, 9-alkoxyalkylamino-1-nitroacridine derivatives. Methods of preparation, pharmaceutical compositions comprising said derivatives and their medical uses are also encompassed by this invention.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: July 8, 2003
    Assignee: New York Medical College
    Inventors: Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela, Raj Tiwari
  • Patent number: 6489336
    Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: December 3, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Mitsuaki Miyamoto, Tatsuya Yoshiuchi, Keizo Sato, Makoto Kaino, Masayuki Tanaka, Motohiro Soejima, Katsuhiro Moriya, Yoshinori Sakuma, Koji Yamada, Kokichi Harada, Yukio Nishizawa, Seiichi Kobayashi, Makoto Okita, Koichi Katayama
  • Patent number: 6479504
    Abstract: The present invention relates generally to the field of immunology. More particularly it concerns compositions and methods for inhibiting stimulation of the immune system. The compounds and methods comprise compounds that are analogs and derivatives of chloroquine, such as 4-aminoquinolines, and other weak bases. They can be used in preventative and therapeutic treatments of autoimmune diseases and phenomena, transplant rejection such as host-versus-graft disease, and sepsis.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: November 12, 2002
    Assignees: The University of Iowa Research Foundation, Georgia State University Research Foundation, Inc., The United States of America as represented by the Department of Veterans Affairs
    Inventors: Donald E. Macfarlane, Lucjan Strekowski, Lori Manzel, Fyaz M. D. Ismail, Gordon B. Barlin
  • Publication number: 20020111491
    Abstract: The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrogen or (II) (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, -N═CHR′(wherein R′ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (III) (wherein R″ is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkylcar
    Type: Application
    Filed: May 16, 2001
    Publication date: August 15, 2002
    Applicant: Samjin Pharmaceutical Co., Ltd.
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang, Jeong-Ho Joo
  • Publication number: 20020099211
    Abstract: The invention is directed to novel 9-hydroxyalkylamino-, 9-alkoxyalkylamino-1- nitroacridine derivatives. Methods of preparation, pharmaceutical compositions comprising said derivatives and their medical uses are also encompassed by this invention.
    Type: Application
    Filed: August 22, 2001
    Publication date: July 25, 2002
    Inventors: Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela, Raj Tiwari
  • Patent number: 6248750
    Abstract: There are disclosed compounds having the formula wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, —SH, loweralkylthio, —NHCOR2 or —NR3R4 where R2 is hydrogen or loweralkyl, and R3 and R4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: June 19, 2001
    Assignee: Hoechst Roussel Pharmaceuticals
    Inventors: Gregory Michael Shutske, Kevin James Kapples
  • Patent number: 6221877
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: April 24, 2001
    Assignee: Regents of the University of California
    Inventors: Alex M. Aronov, Narsimha R. Munagala, Paul R. Ortiz de Montellano, Irwin D. Kuntz, Ching C. Wang
  • Patent number: 6207673
    Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII  (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: March 27, 2001
    Assignees: The University of North Carolina at Chapel Hill, Yale University
    Inventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Xin Guo, Kenneth F. Bastow, Hui-Kang Wang
  • Patent number: 6130228
    Abstract: Compounds of Formula (I), methods for their preparation, pharmaceutical formulations and use thereof.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: October 10, 2000
    Assignee: University of Strathclyde
    Inventors: George Rennet Proctor, Alan Lang Harvey, Maureen Theresa McKenna, Steven John Mullins
  • Patent number: 6111109
    Abstract: A process for producing an acridine carboxamide of formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.5 and R.sup.6, which may be the same or different, is H or an organic subsituent, x is from 1 to 6 and Y is N(R)2 wherein R is C.sub.1 -C.sub.6 alkyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: August 29, 2000
    Assignee: Xenova Limited
    Inventors: William Alexander Denny, Swarnalatha Akuratiya Gamage, Julie Ann Spicer, Michael Wright, David Frank Hayman
  • Patent number: 6075144
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: June 13, 2000
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory Michael Shutske, Kevin James Kapples
  • Patent number: 6020131
    Abstract: The present invention has an object to provide an easy method for detecting a nucleic acid polymer in aqueous phase.The present invention provides a method for detecting the amount of nucleic acid polymer, which comprises the steps of modifying an intercalator to be amphiphilic by using a hydrophobic group, spreading the amphiphilic intercalator on an aqueous solution containing a nucleic acid polymer to form a monolayer of said nucleic acid polymer and said amphiphilic intercalator at the gas-water interface, and measuring surface pressures per unit area of said monolayer.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: February 1, 2000
    Assignee: Research Development Corporation of Japan
    Inventors: Kunihara Ijiro, Masatsugu Shimomura
  • Patent number: 6015902
    Abstract: Intercalator compounds of formula I-T.sub.m as defined herein are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: January 18, 2000
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Jeffrey Bruce Huff, Denis R. Henrard
  • Patent number: 5886007
    Abstract: The present invention provides cholinesterase inhibitors of general formula (I): ##STR1## wherein R is H or (C.sub.1 -C.sub.4)alkyl, Y is a linking group and Z is an aryl group, and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: March 23, 1999
    Assignee: Mayo Foundation For Medical Education and Research
    Inventors: Yuan-Ping Pang, Stephen Brimijoin
  • Patent number: 5861411
    Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.
    Type: Grant
    Filed: April 10, 1996
    Date of Patent: January 19, 1999
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
  • Patent number: 5840980
    Abstract: A diamine compound of the following formula (1): ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group, each of A.sub.1, A.sub.2 and A.sub.3 which are independent of one another, is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a group of the following formula (2): ##STR2## wherein R.sub.1 is as defined above, and X is a substituted or unsubstituted arylene group or a substituted or unsubstituted heterocyclic bivalent group.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: November 24, 1998
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Mitsutoshi Anzai, Atsushi Takesue, Takanobu Watanabe, Chieko Inayoshi
  • Patent number: 5767126
    Abstract: Polyhydroxylated and dehydrogenated metabolites of 9-amino-1,2,3,4-tetrahydro-acridine (Tacrine) in which attached to at least two of the carbon atoms numbered 1,2,3 and 4 is a hydroxyl group and to the others either hydrogen, hydroxyl or double bonded oxygen the residual valencies being occupied by hydrogen or double bonds between carbon atoms 1 and 2 and/or 3 and 4 are disclosed as being useful medicaments for enhancing memory and cognitive function in Alzheimer's disease because they have retained the anticholinesterase activity of their metabolic precursor while circumventing its hepatotoxicity. Related compounds to which this disclosure also applies include those in which the aromatic ring is substituted with lower alkyl, lower alkoxy, halogen, hydroxy, nitro, trifluoromethyl, alkyl-N-substituted carboxamides and where the 9-amino group is mono or di-substituted independently.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: June 16, 1998
    Inventor: Roger Michael Marchbanks
  • Patent number: 5672707
    Abstract: "Derivatives of 9-aminoacridine characterized by psychothropic, antiamnestic and lipid-regulating activities".New chemical compounds derived of 9-aminoacridine with a general formula are presented: ##STR1## where R=H or CH.sub.3 R.sup.1 =H, CH.sub.3, or BrR.sup.2 =H, CH.sub.3R.sup.3 =--C.sub.1 -C.sub.5 alkyl phenylmethyl, substituted phenylmethyl or diethylaminoethylX=C=O, or CHOH, Y=CH.sub.2 orX+Y=CH=CHand their salts with organic and inorganic acids.The target compounds were obtained by a reaction of substituted nitriles of anthranilic acid with dimedone and subsequent cyclization of intermediate enaminonitriles to the corresponding 9-amino-3,4-dihydroacridine-1(2H)-ones. The reduction of the compounds or their alkylated or aralkylated at 9-aminogroupe derivatives results in corresponding alkanols, which on dehydratation give 9-amino-3,4-dihydroacridines.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: September 30, 1997
    Assignee: Vserossiisky Nauchny Tsentr Po Bezopasnosti Biologicheski Aktivnykh veschestv (Vntsbav)
    Inventors: Yury Valentinovich Burov, Sergei Borisovich Goncharenko, Tatyana Nikolaevna Robakidze, Jury Nikolaevich Portnov, Ljubov Vladislavovna Kadysheva, Ilmar Kharievich Penke, Eduard Maximovich Peganov, Svetlana Alexeevna Sukhanova, Galina Vasilievna Tananova, Anatoly Evgenievich Voronin, Anatoly Alexeevich Kotlobai, Yanis Fritsevich Oshis, Lidia Evgenievna Pchelintseva
  • Patent number: 5567716
    Abstract: Traumatic acid salts, wherein B is a cation selected from:a) a quaternary ammonium,b) a cation of a linear or branched C.sub.1 -C.sub.20 mono-, di- or trialkanolamine,c) a cation of a biologically active primary, secondary or tertiary amine,d) silver or zinc cation,and relative pharmaceutical compositions administrable by topical or parenteral route For the therapeutic treatment of cutaneous pathologies in which it is important to associate an a bacteriostatic, antibiotic, antifungal or an antiviral activity, to the cicatrizant effect, typical of traumatic acid.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 22, 1996
    Assignee: Lifegroup S.p.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
  • Patent number: 5536728
    Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: July 16, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka