The Nitrogen Is Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/105)
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Patent number: 11932620Abstract: An ethyl 2-[9-(6-fluoro-2-hydroxyquinolin-3-yl)-1,8-dioxo-3,4,9,10-tetrahydroacridine-10-yl]-acetate compound, its synthesis, and its use as an antimicrobial agent.Type: GrantFiled: November 2, 2023Date of Patent: March 19, 2024Assignee: KING FAISAL UNIVERSITYInventors: Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed
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Patent number: 10350299Abstract: 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: GrantFiled: June 1, 2017Date of Patent: July 16, 2019Assignee: PROCARTA BIOSYSTEMS LTD.Inventor: Michael McArthur
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Patent number: 8765781Abstract: 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: GrantFiled: July 2, 2009Date of Patent: July 1, 2014Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmity A. Androsov
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Publication number: 20140148451Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.Type: ApplicationFiled: May 9, 2012Publication date: May 29, 2014Applicants: Translational Genomics Research Institute, Van Andel Research InstituteInventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
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Patent number: 8722701Abstract: 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: GrantFiled: September 2, 2011Date of Patent: May 13, 2014Assignees: Changchun Huayang High Technology, Inc., Jiangsu Shen ER Yang High Technology Co., Ltd.Inventor: Tonghui Wang
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Publication number: 20140058099Abstract: 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: ApplicationFiled: March 2, 2012Publication date: February 27, 2014Applicant: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATIONInventors: Atsushi Wakamiya, Hidetaka Nishimura, Yasujiro Murata, Tatsuya Fukushima, Hironori Kaji
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Patent number: 8530496Abstract: 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: GrantFiled: September 20, 2011Date of Patent: September 10, 2013Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Justin M. Lopchuk
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Publication number: 20130225517Abstract: 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: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: University of Iowa Research FoundationInventor: University of Iowa Research Foundation
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Publication number: 20130158065Abstract: 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: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Applicants: JIANGSU SHEN ER YANG HIGH TECHNOLOGY CO., LTD, CHANGCHUN HUAYANG HIGH TECHNOLOGY CO., LTDInventor: Tonghui Wang
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Publication number: 20130035351Abstract: 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: ApplicationFiled: August 3, 2011Publication date: February 7, 2013Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Publication number: 20120220537Abstract: 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: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Applicant: ARIEL-UNIVERSITY RESEARCH AND DEVELOPMENT COMPANY LTD.Inventor: Gary Gellerman
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Patent number: 8063062Abstract: 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: GrantFiled: December 17, 2007Date of Patent: November 22, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Belal Shadid
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Patent number: 8057990Abstract: 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: GrantFiled: March 7, 2006Date of Patent: November 15, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Masaaki Mori, Kimiko Kanehashi
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Patent number: 7910739Abstract: 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: GrantFiled: July 9, 2004Date of Patent: March 22, 2011Assignee: 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
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Publication number: 20100055682Abstract: 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: ApplicationFiled: May 14, 2007Publication date: March 4, 2010Inventors: Fabien Schweighoffer, Laurent Bracco
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Patent number: 7622478Abstract: 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: GrantFiled: February 16, 2001Date of Patent: November 24, 2009Inventors: Raj Tiwari, Daniel Miller, Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela
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Publication number: 20090226940Abstract: 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: ApplicationFiled: October 27, 2006Publication date: September 10, 2009Applicant: ITI Scotland LimitedInventors: Robert Ramage, Beatrice Maltman, Graham Cotton, Sarah Claire Monique Couturier, Robert Austin Simms McMordie
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Publication number: 20080319001Abstract: 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: ApplicationFiled: March 2, 2006Publication date: December 25, 2008Inventors: Christina Martins, Stephen Neidle, Mekala Gunaratnam, John Stuart, Lloyd Kelland
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Publication number: 20080176308Abstract: 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: ApplicationFiled: January 22, 2007Publication date: July 24, 2008Applicant: BIOTECHNOLOGY RESEARCH CORPORATION LIMITEDInventors: Nancy Y. IP, Fanny Chui Fun IP, Yueqing Hu, Yifan Han, Sookja Kim Chung
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Publication number: 20080171765Abstract: 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: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: Academia SinicaInventors: Tsann-Long Su, Ting-Chao Chou
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Patent number: 7300930Abstract: 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 acceptablType: GrantFiled: June 22, 2005Date of Patent: November 27, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 7230105Abstract: The present invention relates to a new 9-aminoacridine derivative which exhibits prominent antitumor activity and low toxicity.Type: GrantFiled: March 7, 2002Date of Patent: June 12, 2007Assignee: Samjin Pharmaceutical Co., Ltd.Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang
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Patent number: 7160896Abstract: 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 salType: GrantFiled: July 6, 2001Date of Patent: January 9, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reskza
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Patent number: 7041674Abstract: 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: GrantFiled: November 20, 2003Date of Patent: May 9, 2006Assignee: Boehringer Ingelhiem Pharma GmbH & Co. KGInventors: Steffen Breitfelder, Matthias Hoffmann, Matthias Grauert, Michael P. Pieper, Georg Speck
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Patent number: 6858742Abstract: 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: GrantFiled: October 22, 2003Date of Patent: February 22, 2005Assignee: AsiaGEN CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Patent number: 6821983Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.Type: GrantFiled: July 30, 2003Date of Patent: November 23, 2004Assignee: Academia SinicaInventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
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Publication number: 20040219564Abstract: 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: ApplicationFiled: October 22, 2003Publication date: November 4, 2004Applicant: AsiaGEN CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Publication number: 20040132747Abstract: 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: ApplicationFiled: December 19, 2003Publication date: July 8, 2004Inventors: Peter Emig, Eckhard Gunther, Jurgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6743817Abstract: 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: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6620936Abstract: 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 alType: GrantFiled: May 16, 2001Date of Patent: September 16, 2003Assignee: Samjin Pharmaceutical Co., Ltd.Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang, Jeong-Ho Joo
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Patent number: 6589961Abstract: 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: GrantFiled: August 22, 2001Date of Patent: July 8, 2003Assignee: New York Medical CollegeInventors: Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela, Raj Tiwari
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Patent number: 6489336Abstract: 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: GrantFiled: November 2, 2001Date of Patent: December 3, 2002Assignee: 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
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Patent number: 6479504Abstract: 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: GrantFiled: June 16, 2000Date of Patent: November 12, 2002Assignees: The University of Iowa Research Foundation, Georgia State University Research Foundation, Inc., The United States of America as represented by the Department of Veterans AffairsInventors: Donald E. Macfarlane, Lucjan Strekowski, Lori Manzel, Fyaz M. D. Ismail, Gordon B. Barlin
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Publication number: 20020111491Abstract: 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 alkylcarType: ApplicationFiled: May 16, 2001Publication date: August 15, 2002Applicant: Samjin Pharmaceutical Co., Ltd.Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang, Jeong-Ho Joo
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Publication number: 20020099211Abstract: 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: ApplicationFiled: August 22, 2001Publication date: July 25, 2002Inventors: Jerzy Kazimierz Konopa, Barbara Wysocka-Skrzela, Raj Tiwari
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Patent number: 6248750Abstract: 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: GrantFiled: March 24, 2000Date of Patent: June 19, 2001Assignee: Hoechst Roussel PharmaceuticalsInventors: Gregory Michael Shutske, Kevin James Kapples
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Patent number: 6221877Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: April 12, 2000Date of Patent: April 24, 2001Assignee: Regents of the University of CaliforniaInventors: Alex M. Aronov, Narsimha R. Munagala, Paul R. Ortiz de Montellano, Irwin D. Kuntz, Ching C. Wang
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Patent number: 6207673Abstract: 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: GrantFiled: March 12, 1997Date of Patent: March 27, 2001Assignees: The University of North Carolina at Chapel Hill, Yale UniversityInventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Xin Guo, Kenneth F. Bastow, Hui-Kang Wang
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Patent number: 6130228Abstract: Compounds of Formula (I), methods for their preparation, pharmaceutical formulations and use thereof.Type: GrantFiled: August 25, 1998Date of Patent: October 10, 2000Assignee: University of StrathclydeInventors: George Rennet Proctor, Alan Lang Harvey, Maureen Theresa McKenna, Steven John Mullins
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Patent number: 6111109Abstract: 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: GrantFiled: June 18, 1999Date of Patent: August 29, 2000Assignee: Xenova LimitedInventors: William Alexander Denny, Swarnalatha Akuratiya Gamage, Julie Ann Spicer, Michael Wright, David Frank Hayman
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Patent number: 6075144Abstract: 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: GrantFiled: June 13, 1994Date of Patent: June 13, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory Michael Shutske, Kevin James Kapples
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Patent number: 6020131Abstract: 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: GrantFiled: November 7, 1997Date of Patent: February 1, 2000Assignee: Research Development Corporation of JapanInventors: Kunihara Ijiro, Masatsugu Shimomura
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Patent number: 6015902Abstract: 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: GrantFiled: October 21, 1996Date of Patent: January 18, 2000Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Jeffrey Bruce Huff, Denis R. Henrard
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Patent number: 5886007Abstract: 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: GrantFiled: May 15, 1997Date of Patent: March 23, 1999Assignee: Mayo Foundation For Medical Education and ResearchInventors: Yuan-Ping Pang, Stephen Brimijoin
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Patent number: 5861411Abstract: 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: GrantFiled: April 10, 1996Date of Patent: January 19, 1999Assignee: Mitsubishi Chemical CorporationInventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
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Patent number: 5840980Abstract: 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: GrantFiled: July 24, 1997Date of Patent: November 24, 1998Assignee: Hodogaya Chemical Co., Ltd.Inventors: Mitsutoshi Anzai, Atsushi Takesue, Takanobu Watanabe, Chieko Inayoshi
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Patent number: 5767126Abstract: 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: GrantFiled: October 18, 1994Date of Patent: June 16, 1998Inventor: Roger Michael Marchbanks
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Patent number: 5672707Abstract: "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: GrantFiled: October 29, 1993Date of Patent: September 30, 1997Assignee: 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
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Patent number: 5567716Abstract: 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: GrantFiled: November 19, 1993Date of Patent: October 22, 1996Assignee: Lifegroup S.p.A.Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
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Patent number: 5536728Abstract: 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: GrantFiled: December 8, 1994Date of Patent: July 16, 1996Assignee: Mitsubishi Chemical CorporationInventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada