Nitrogen Or Halogen Bonded Directly To The Polycyclo Ring System Patents (Class 552/297)
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Patent number: 9783513Abstract: In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: August 16, 2013Date of Patent: October 10, 2017Assignees: Ohio State Innovation Foundation, Research Institute at Nationwide Children's HospitalInventors: Chenglong Li, Wenying Yu, Jiayuh Lin
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Patent number: 8937193Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.Type: GrantFiled: October 7, 2010Date of Patent: January 20, 2015Assignee: Sanford-Burnham Medical Research InstituteInventors: Maurizio Pellecchia, Jun Wei
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Publication number: 20130102650Abstract: The present invention relates to a compound having formula (I) wherein: R1 is chosen from the group consisting of: phenyl group, possibly substituted, —CH2—C6H4—R?1 group, R?1 being chosen from the group consisting of: H, —OH, halogen, alkyl, aryl, CHO, —CN, —NO2, —SR?, —OR?, —NR?R?, —CONR?R?, —COOR?, and —NHCOR?, R? and R? representing independently from each other H, an alkyl group or an aryl group, R?1 being preferably in para position, and —CH2—CO—R? group, R? representing an aryl or heteroaryl group, said aryl and heteroaryl groups being possibly substituted, R2 is chosen from the group consisting of: —OH and halogen, and R3, R4, R5 and R6 are in particular H, for its use for the prevention and/or the treatment of bacterial infections.Type: ApplicationFiled: April 8, 2011Publication date: April 25, 2013Inventors: Yap Jean-Bertrand Boum, II, Tamara Basta-Le-Berre, Ursula Liebl, Hannu Myllykallio
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Publication number: 20110144347Abstract: Provided is a process for the epimerization of the cis isomer of atovaquone, atovaquone intermediates and isomeric mixtures thereof into their corresponding trans-isomers resulting in higher yield of pure atovaquone.Type: ApplicationFiled: June 30, 2008Publication date: June 16, 2011Applicant: CHEMAGIS LTD.Inventors: Fuqiang Zhu, Michel Bekhazi
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Patent number: 7829555Abstract: The invention provides a method of targeting a drug to areas of hypoxic and/or ischemic tissue within the body in which the desired drug species is linked to a non-cytotoxic bioreductive carrier. Also provided by the invention are novel bioreductive conjugates comprising a non-cytotoxic bioreductive moiety with linked-thereto at least one therapeutic agent. The compounds of the invention are particularly suitable for the treatment of rheumatoid arthritis and other arthritic conditions, diabetes, atherosclerosis, stroke, sepsis, Alzheimer's disease and other neurological disorders, cancer, kidney disease, digestive diseases, liver disease, chronic periodontitis or ischemia following tissue transplantation.Type: GrantFiled: February 13, 1998Date of Patent: November 9, 2010Assignee: The University of ManchesterInventors: David Blake, Declan Naughton, Ged Adams, Margaret Adams, legal representative, Ian Stratford, Christopher Morris, Mohammed Jaffar, Matthew Naylor
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Publication number: 20090253709Abstract: An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a nitro group, a hydroxyl group, a C1-C12 alkyl group, a C1-C12 alkyl halide group (—(CH2)nX), a C3-C12 cycloalkyl group, a benzyl group, a C1-C12 alkylamino group, a C5-C12 nitrocycloalkyl group and a heterocyclic group, n satisfies 1?n?12 and X is an atom selected from a group consisting of a fluoride (F), a chloride (Cl), a bromide (Br) and an iodine (I). The preparation method of the 2,7-disubstituted anthraquinone derivatives includes the steps of acetylating 2,7-diaminoanthraquinone to be one 2,7-disubstituted anthraquinone derivative, which can be further aminated to be another 2,7-disubstituted anthraquinone derivative.Type: ApplicationFiled: August 15, 2008Publication date: October 8, 2009Applicant: NATIONAL DEFENSE MEDICAL CENTERInventor: Hsu-Shan HUANG
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Publication number: 20040171616Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: February 19, 2003Publication date: September 2, 2004Inventors: Michael S. South, John J. Parlow
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Publication number: 20030232801Abstract: The invention features compounds for the treatment of cancer and other proliferative diseases. These compounds were identified in screening assays that contact candidate compounds with a cell containing a nucleic acid that includes a HER2 regulatory element and a reporter sequence. The invention further features compounds structurally related to those identified by the screening assays. Finally, the invention features methods of treating or preventing a proliferative disease using the compounds of the invention.Type: ApplicationFiled: April 15, 2003Publication date: December 18, 2003Inventors: Michael Alan Sturgess, Ke Yang
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Publication number: 20030225086Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: February 19, 2003Publication date: December 4, 2003Inventors: Michael S. South, John J. Parlow
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Publication number: 20020128499Abstract: The invention comprises a process for preparing a compound having the formula comprising: 1Type: ApplicationFiled: December 5, 2001Publication date: September 12, 2002Inventors: Otto William Maender, Charles John Rostek, Alan Roy Katritzky, Herman Howard Odens, Michael Victor Voronkov
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Publication number: 20020091163Abstract: This invention provides analogs of triptycene which are useful as anticancer drugs, as well as for other uses. The potency of these compounds is in a similar magnitude as daunomycin, a currently used anticancer drug. Each compound of the invention produces one or more desired effects (blocking nucleoside transport, inhibiting nucleic acid or protein syntheses, decreasing the proliferation and viability of cancer cells, inducing DNA fragmentation or retaining their effectiveness against multidrug-resistant tumor cells).Type: ApplicationFiled: October 9, 2001Publication date: July 11, 2002Inventors: Duy Hua, Jean-Pierre Perchellet
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Patent number: 5744623Abstract: Terpene-quinone with antitumor activity defined from a cyclocondensation reaction of Diels-Alder, used to obtain families or series of said compounds having a new structure and presenting a cytotoxic activity to cellular cultures P-388, A-549, HT-29 and MEL-28, with levels of IC.sub.50 lower than 1 microgram per unit of milliliter.Type: GrantFiled: October 4, 1996Date of Patent: April 28, 1998Assignee: Pharma Mar, s.a.Inventors: M.sup.a Dolores Garcia Gravalos, Marina Gordaliza Escobar, Santana Jose M.sup.a Miguel Del Corral, Ma del Mar Mahiques Bujanda, Arturo San Feliciano Martin
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Patent number: 5679808Abstract: The present invention discloses a tertiary non-linear optical material comprising a quinone derivative expressed by any one of the general formulas: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined above, or the formula: ##STR2## The tertiary non-linear material enables the co-existence of large tertiary non-linear optical susceptibility and high-speed response.Type: GrantFiled: January 26, 1995Date of Patent: October 21, 1997Assignee: Sumitomo Electric Industries, Ltd.Inventors: Akira Mizoguchi, Yasuhiro Hattori, Michiru Kubata
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Patent number: 5639718Abstract: An oil-soluble lubricating oil and fuel additive, useful as a multifunctional viscosity modifier comprising succinimide and other amine-containing polymers reacted with a quinone or substituted quinone adducts. Suitable polymers are those containing primary or secondary amine groups such as EPSA-PAM and EPDM-amine polymers. The multifunctional viscosity modifier additive provides improved dispersancy and antioxidancy to a lubricating oil or fuel composition.Type: GrantFiled: November 23, 1994Date of Patent: June 17, 1997Assignee: Exxon Chemical Patents Inc.Inventor: Abhimanyu O. Patil
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Patent number: 5175319Abstract: Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described.Type: GrantFiled: September 12, 1991Date of Patent: December 29, 1992Assignee: Burroughs Wellcome Co.Inventors: Alan T. Hudson, Anthony W. Randall
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Patent number: 5175318Abstract: Phenols are oxidated to quinones with hydrogen peroxide in the presence of catalytic amounts of bromine, iodine, hydrogen bromide and hydrogen iodide.Type: GrantFiled: April 7, 1992Date of Patent: December 29, 1992Assignees: Consiglio Nazionale Della Ricerche, Enicham Synthesis, Brichima, S.p.A.Inventors: Francesco Minisci, Attilio Citterio, Elena Vismara, Silvia De Bernardinis, Carlo Neri, Luciano Pallini, Mariano Correale
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Patent number: 4933489Abstract: An improved process for the manufacture of the antipsoriatic agent, 6-chloro-1,4-diacetoxy-2,3-dimethoxynaphthalene, is herein described which involves in situ Diels-Alder coupling of 2,3-dimethoxybenzo-1,4-quinone with a 3-chloro-1-alkoxy-1,3-butadiene; 1,4-elimination of the alcohol with aromatization of the chlorine-bearing ring, and acetylation.Type: GrantFiled: October 24, 1985Date of Patent: June 12, 1990Assignee: Warner-Lambert CompanyInventor: Daniel L. Flynn
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Patent number: 4880571Abstract: A process for the preparation of 5-nitro-1,4-naphthoquinones of formula ##STR1## wherein R is hydrogen, a C.sub.1 -C.sub.4 alkyl radical or a C.sub.1 -C.sub.4 alkoxy radical, by oxidation of 1-nitronaphthalene or a suitably substituted 1-nitronaphthalene, which process comprises carrying out the reaction with manganese(III) sulfate as oxidizing agent or a mixture of manganese(III) sulfate and cerium sulfate.The maganese(III) sulfate consumed can be regenerated electrolytically with good current yield. The process is environmentally safe, as the oxidizing agent and the solvent, if any, can be reused.Type: GrantFiled: October 22, 1986Date of Patent: November 14, 1989Assignee: Ciba-Geigy CorporationInventors: Christos Comninellis, Robert U. Osterwalder, Eric Plattner, Gottfried Seifert