Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/473)
  • Patent number: 11198670
    Abstract: The invention provides a novel hydrocarbon-containing carboxylic acid, hydrocarbon-containing sulfonic acid, hydrocarbon-containing sulfuric acid ester, or a salt thereof, and a surfactant. Each of them is a compound represented by the following formula (1): CR1R2R4—CR3R5—X-A wherein R1 to R5 are each H or a monovalent substituent; at least one of R1 or R3 is a group represented by the formula: —Y—R6; at least one of R2 or R5 is a group represented by the formula: —X-A or a group represented by the formula: —Y—R6; and As at the respective appearances are the same as or different from each other, and are each —COOM, —SO3M, or —OSO3M.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: December 14, 2021
    Assignee: DAIKIN INDUSTRIES, LTD.
    Inventors: Masahiro Higashi, Satoru Yoneda, Akiyoshi Yamauchi, Sumi Ishihara, Yosuke Kishikawa, Hirokazu Aoyama
  • Patent number: 10407418
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: where R, L, X1, X2, X3, X4, X5, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: September 10, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Aleksandra Rudnitskaya, David R. Lancia, Jr.
  • Publication number: 20140323718
    Abstract: The present invention relates to compounds that are useful as metal ligands and which can be bound to a biological entity such as a molecular recognition moiety and methods of making these compounds. Once the compounds that are bound to a biological entity are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Paul Donnelly, Brett Paterson
  • Publication number: 20140323717
    Abstract: Special C-functionalized cyclic bisaminal compounds having formula (I) or (II), their salts or solvates, methods for their preparation, their uses, and methods for preparing functional tetraazacycloalkane compounds implementing such cyclic bisaminal compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 30, 2014
    Inventors: Raphael Tripier, Nathalie Camus
  • Patent number: 8722881
    Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: May 13, 2014
    Assignee: Board of Trustees of the University of Arkansas
    Inventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
  • Patent number: 8420626
    Abstract: The present invention relates to arene connected polyamine macrocyclic derivatives represented by general formula I, pharmaceutically acceptable salts or hydrates thereof which have anti-HIV activities, in which the definitions of substituents are as defined in the description; to preparation methods of the compounds of formula I; to pharmaceutical compositions containing the compounds of formula I or their pharmaceutically acceptable salts or hydrates; to the use of the compounds of formula I or their pharmaceutically acceptable salts or hydrates for the preparation of a medicament for the treatment and prevention of HIV-associated diseases.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: April 16, 2013
    Assignee: Beijing Molecule Science and Technology Co., Ltd.
    Inventors: Song Li, Jing Su, Yao Liu, Junhai Xiao, Lili Wang, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Guoming Zhao, Xiaokui Wang, Xinbo Zhou, Hongying Liu
  • Publication number: 20130053380
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: February 28, 2011
    Publication date: February 28, 2013
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Olaf Kinzel, Christoph Steeneck, Gerald Klaymann, Michael Albers, Thomas Hoffman, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
  • Patent number: 8222257
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
  • Publication number: 20120178915
    Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.
    Type: Application
    Filed: December 24, 2009
    Publication date: July 12, 2012
    Inventor: Lifeng Xu
  • Patent number: 8034800
    Abstract: A compound of Formulae (1), (2) or (3), A1-Ph (1) or A1-Ar-A2 (2) or A1-(A2)A?-A3 (3) wherein A1, A2 and A3 are selected from Formulae 4, 5 and 6: or a salt whereof; wherein Ar is selected from the group consisting of 1,2-phenyl, 1,3-phenyl and 1,4-phenyl optionally substituted with one or more methyl groups; m and n are independently integers from 0 to 1; Ph is phenyl, optionally substituted with one or more methyl groups; Ar1 is trisubstituted phenyl optionally substituted with one or more phenyl groups; and R1, R2 and R3 are independently selected from the group consisting of H, Me and linear chain C2-C4 alkyl.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: October 11, 2011
    Assignee: University of Hull
    Inventors: Stephen James Archibald, Elizabeth Amie Lewis, Timothy J. Hubin
  • Patent number: 7951791
    Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 31, 2011
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Kevin B. Sippy, Jianguo Ji, Tao Li, Jennifer M. Frost, Clark A. Briggs, William H. Bunnelle
  • Patent number: 7935692
    Abstract: Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed.
    Type: Grant
    Filed: November 8, 2005
    Date of Patent: May 3, 2011
    Assignee: Genzyme Corporation
    Inventors: Gary J. Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald Trevor MacFarland, Gary B. Calandra, Hal E. Broxmeyer, David C. Dale
  • Patent number: 7897590
    Abstract: Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: March 1, 2011
    Assignee: Genzyme Corporation
    Inventors: Gary J. Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald Trevor MacFarland, Gary B. Calandra, Hal E. Broxmeyer, David C. Dale
  • Publication number: 20090286827
    Abstract: The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
    Type: Application
    Filed: April 2, 2007
    Publication date: November 19, 2009
    Inventors: Ralf Glatthar, David Carcache, Carsten Spanka, Ivan-toma Vranesic, Thomas J. Troxler
  • Patent number: 7582280
    Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
    Type: Grant
    Filed: July 8, 2008
    Date of Patent: September 1, 2009
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
  • Publication number: 20090042912
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.
    Type: Application
    Filed: October 7, 2008
    Publication date: February 12, 2009
    Applicant: Wyeth
    Inventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Keith Douglas Barnes, Matthew Robert Johnson, Yu Hui
  • Patent number: 7368100
    Abstract: Backbone-substituted 1,4,7,10-tetraaza cyclododecane-N,N?,N?,N??-tetraacetic acid compounds, metal complexes thereof, compositions thereof, conjugates thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: May 6, 2008
    Assignee: The United States of America, represented by the Secretary, Department of Health and Human Services
    Inventors: Martin W. Brechbiel, Hyun-Soon Chong
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7211241
    Abstract: Described are new cascade polymer complexes, compositions containing them and use of the complexes in diagnosis and therapy, particularly for magnetic resonance imaging and computer tomography imaging.
    Type: Grant
    Filed: October 17, 2003
    Date of Patent: May 1, 2007
    Assignee: Schering Aktiengesellschaft
    Inventors: Heribert Schmitt-Willich, Johannes Platzek, Bernd Radüchel, Andreas Mühler, Thomas Frenzel
  • Patent number: 7060818
    Abstract: An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: June 13, 2006
    Assignee: Carnegie Mellon University
    Inventors: Colin P. Horwitz, Anindya Ghosh
  • Patent number: 7053214
    Abstract: Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A?, B, X, Y, R2, R3, R4 and R5 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are tryptase antagonists.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: May 30, 2006
    Assignee: Myriad Genetics, Inc.
    Inventors: Cyprian O. Ogbu, Hwa-Ok Kim, Mark A Blaskovich
  • Patent number: 7030238
    Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: April 18, 2006
    Assignee: Duke University
    Inventors: Jonathan S. Stamler, Eric J. Toone
  • Patent number: 6987102
    Abstract: Certain nitrogen-containing compounds that bind the chemokine receptor CXCR4 are able to mobilize progenitor and/or stem cells into the peripheral blood to permit harvesting them for stem cell transplantation.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: January 17, 2006
    Assignee: Anormed, Inc.
    Inventors: Gary J. Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald Trevor MacFarland, Gary B. Calandra, Hal E. Broxmeyer, David C. Dale
  • Patent number: 6942966
    Abstract: Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: September 13, 2005
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventor: Phillip Dan Cook
  • Patent number: 6916805
    Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: July 12, 2005
    Assignee: Warner-Lambert Company LLC
    Inventors: Danette Andrea Dudley, Jeremy John Edmunds
  • Patent number: 6900222
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6818149
    Abstract: The present invention provides a bleaching composition comprising a [3.3.1] bicyclo compound carrying at least one tertiary amine group the bleaching composition substantially devoid of a peroxygen source.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: November 16, 2004
    Assignee: Unilever Home & Personal Care USA, division of Conopco, Inc.
    Inventors: Heidi Boerzel, Peter Comba, Ronald Hage, Marion Kerscher, Joachim Lienke, Michael Merz
  • Patent number: 6696435
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: February 24, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6670354
    Abstract: Methods to elevate white blood cell counts in animal subjects using compounds of formula (1) are disclosed.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: December 30, 2003
    Assignee: AnorMed, Inc.
    Inventors: Ronald Trevor MacFarland, Andrew W. Millar, Gary Bridger, Michael J. Abrams, Geoffrey W. Henson
  • Patent number: 6656930
    Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: December 2, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne D Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 6576760
    Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: June 10, 2003
    Assignee: Chelator LLC
    Inventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
  • Patent number: 6552012
    Abstract: The present invention relates to novel heteroaryl diazabicycloalkane derivatives represented by general formula (I), any of its enantiomers or any mixture thereof, an N oxide thereof, a pharmaceutically acceptable salt thereof, in a labelled or un-labelled form, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: April 22, 2003
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Simon Feldbaek Nielsen, Gunnar M. Olsen, Elsebet Ostergaard Nielsen
  • Publication number: 20020173644
    Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.
    Type: Application
    Filed: May 9, 2002
    Publication date: November 21, 2002
    Inventors: George Douglas Hiler, Christopher Mark Perkins
  • Patent number: 6469162
    Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: October 22, 2002
    Assignee: Concat, Ltd.
    Inventors: Harry S. Winchell, Joseph Y. Klein, Elliot D. Simhon, Rosa L. Cyjon, Ofer Klein, Haim Zaklad
  • Patent number: 6455519
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N- disubstituted fused-heterocyclo amines.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: September 24, 2002
    Assignee: G.D. SEarle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6413963
    Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: July 2, 2002
    Assignee: Molecumetics, Ltd.
    Inventors: Michael Kahn, Masakatsu Eguchi, Hwa-Ok Kim, Marcin Stasiak
  • Patent number: 6395725
    Abstract: Synthetic low molecular weight catalysts for the dismutation of superoxide are potent analgesics that are effective in elevating the pain threshold in hyperalgesic conditions such as arthritis, and also operate to prevent or reverse tolerance to opioid analgesics.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: May 28, 2002
    Assignee: G.D. Searle & Co.
    Inventor: Daniela Salvemini
  • Patent number: 6369220
    Abstract: A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.
    Type: Grant
    Filed: October 2, 2000
    Date of Patent: April 9, 2002
    Inventors: Jinglin (James T.) Li, Ching-Cheng Wang, David B. Reitz, Victor Snieckus, Horng-Chih Huang, Andrew J. Carpenter
  • Patent number: 6365583
    Abstract: Methods to elevate white blood cell counts in animal subjects using compounds of formula (1) are disclosed.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: April 2, 2002
    Assignee: AnorMED, Inc.
    Inventors: Ronald Trevor MacFarland, Andrew W. Millar, Gary Bridger, Michael J. Abrams, Geoffrey W. Henson
  • Patent number: 6248306
    Abstract: Cascade polymer complexes containing a) complexing ligands of general formula I A—{X—[Y—(Z—( W—Kw)z)y]x}a  (I)  in which A stands for a nitrogen-containing cascade nucleus of base multiplicity a, X and Y, independently of one another, stand for a direct bond or a cascade reproduction unit of reproduction multiplicity x or y, Z and W, independently of one another, stand for a cascade reproduction unit of reproduction multiplicity z or w, K stands for the radical of a complexing agent, a stands for numbers 2 to 12, x, y, z and w, independently of one another, stand for numbers 1 to 4, provided that at least two reproduction units are different and that 16≦a·x·y·z·w≦64 holds true for the product of the multiplicities, b) at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83 and c) optionally cations of inorganic and/or organic bases, amino acids or amino acid amides are valuab
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 19, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Heribert Schmitt-Willich, Johannes Platzek, Ulrich Niedballa, Bernd Raduchel, Andreas Muhler, Thomas Frenzel, Wolfgang Ebert
  • Patent number: 6214817
    Abstract: The present invention relates to compounds which are effective as catalysts for dismutating superoxide and, more particularly, the manganese or iron complexes of substituted, unsaturated heterocyclic pentaazacyclopentadecane ligands which catalytically dismutate superoxide.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: April 10, 2001
    Assignee: Monsanto Company
    Inventors: Dennis P. Riley, William L. Neumann, Susan L. Henke, Patrick Lennon, Karl W. Aston, Daniela Salvemini, James A. Sikorski, Yvette M. Fobian, Margaret Lanahan Grapperhaus, Carrie L. Kusturin
  • Patent number: 6207826
    Abstract: Novel macrocyclic compounds are constructed to include a ring or ring system having two bridgehead atoms with a bridge extending between the bridgehead atoms. Located in at least the bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring or ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: March 27, 2001
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Phillip Dan Cook, Charles J. Guinosso, Pei-Pei Kung, Allister S. Fraser
  • Patent number: 6166200
    Abstract: Cascade polymer complexes that containa) complexing ligands of general formula IA--{X--[Y--(Z--W--K.sub.W .sub.z).sub.y ].sub.x}.sub.a (I),in whichA stands for a nitrogen-containing cascade nucleus of base multiplicity a,X and Y, independently of one another, stand for a direct bond or a cascade reproduction unit of reproduction multiplicity x or y,Z and W, independently of one another, stand for a cascade reproduction unit of reproduction multiplicity z or w,K stands for the radical of a complexing agent,a stands for numbers 2 to 12,x, y, z and w, independently of one another, stand for numbers 1 to 4,provides that at least two reproduction units are different and that for the product of the multiplicities,16.ltoreq.a.multidot.x.multidot.y.multidot.z.multidot.w.ltoreq.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: December 26, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Heribert Schmitt-Willich, Johannes Platzek, Bernd Raduchel, Andreas Muhler, Thomas Frenzel
  • Patent number: 6162912
    Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles .
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: December 19, 2000
    Assignee: Dibra S.p.A.
    Inventors: Maria Argese, Giorgio Ripa
  • Patent number: 6069114
    Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: May 30, 2000
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6063361
    Abstract: Cascade polymer complexes having a complexing ligand with at least two different reproduction units and having a complexing agent which is a macrocyclic group having an amide grouping or a linear DTPA-type group having a linkage to the polymer through the central nitrogen.
    Type: Grant
    Filed: March 18, 1998
    Date of Patent: May 16, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Heribert Schmitt-Willich, Johannes Platzek, Bernd Raduchel, Andreas Muhler, Thomas Frenzel
  • Patent number: 6048980
    Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: April 11, 2000
    Assignee: Dibra S.p.A
    Inventors: Maria Argese, Giorgio Ripa
  • Patent number: 6028193
    Abstract: A method for producing aryl alkyl hydroperoxides which comprises selectively oxidizing an aryl alkyl hydrocarbon having the formula: ##STR1## wherein P and Q are hydrogen or an alkyl and may be the same or different from each other; x is an integer of 1-3; and Ar is an aromatic hydrocarbon group having a valence of x, with an oxygen-containing gas in the presence of a transition metal complex which contains, as a ligand, a cyclic polyfunctional amine compound having at least three nitrogen atoms in the ring forming molecular chain or an open chain polyfunctional amine compound having at least three nitrogen atoms in the main chain of the molecule.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: February 22, 2000
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Terunori Fujita, Shigekazu Matsui, Toshihiro Takai, Hideto Matsuoka, Akifumi Kagayama, Hiroshi Kuroda, Masayasu Ishibashi, Hiroshi Iwasaki, Nobuya Hirokane
  • Patent number: 6028194
    Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles and the mono and diacetic acid derivatives.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: February 22, 2000
    Assignee: Dibra S.p.A.
    Inventors: Maria Argese, Giorgio Ripa
  • Patent number: 6020485
    Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: February 1, 2000
    Assignee: Dibra S.p.A.
    Inventors: Maria Argese, Giorgio Ripa