Tetracyclo Naphthacene Configured Ring System Having At Least One Double Bond Between Ring Members And Having Oxygen Bonded Directly To A Carbon Of An Interior Ring Which Carbon Is A Member Of One Ring Only Patents (Class 552/200)
  • Patent number: 8992896
    Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Foamix Pharmaceuticals Ltd.
    Inventors: Dov Tamarkin, Elana Gazal, Irakliy Papiashvili, Yohan Hazot, David Schuz, Rita Keynan
  • Patent number: 8871184
    Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents; and the amount of viscosity modifying agents can optionally be reduced by at least an amount by weight that would have increased the viscosity of the carrier without the tetracycline antibiotic by at least 30%; wherein the tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: October 28, 2014
    Assignee: Foamix Ltd.
    Inventors: Dov Tamarkin, Elana Gazal, Yohan Hazot, David Schuz, Rita Keynan, Nukri Papiashvili
  • Patent number: 8865139
    Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: October 21, 2014
    Assignee: Foamix Pharmaceuticals Ltd.
    Inventors: Dov Tamarkin, Elana Gazal, Irakliy Papiashvili, Yohan Hazot, David Schuz, Rita Keynan
  • Publication number: 20130196953
    Abstract: The invention relates to tetracycline products produced by genetically engineered cells, and to therapeutic methods using such tetracyclines. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway.
    Type: Application
    Filed: January 28, 2013
    Publication date: August 1, 2013
    Applicant: UNIVERZA V LJUBLJANI
    Inventor: UNIVERZA V LJUBLJANI
  • Publication number: 20130123217
    Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.
    Type: Application
    Filed: December 13, 2012
    Publication date: May 16, 2013
    Applicant: NEUMEDICS
    Inventor: Neumedics
  • Publication number: 20130012481
    Abstract: The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament.
    Type: Application
    Filed: July 17, 2012
    Publication date: January 10, 2013
    Applicant: SANDOZ AG
    Inventors: Josef Wieser, Andreas Hotter, Arthur Pichler
  • Publication number: 20100255117
    Abstract: The instant invention provides methods and compositions for the treatment of cancer.
    Type: Application
    Filed: April 6, 2008
    Publication date: October 7, 2010
    Applicant: The Johns Hopkins University
    Inventors: Shyam Biswal, Anju Singh, Deepti Malhotra
  • Patent number: 7786099
    Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.
    Type: Grant
    Filed: January 18, 2005
    Date of Patent: August 31, 2010
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventor: Mark L. Nelson
  • Publication number: 20090054379
    Abstract: A compound of formula (I): wherein: A represents an aromatic 5 membered heterocycle, optionally containing, in addition to the nitrogen atom indicated in formula (I), one to three additional nitrogen atoms and optionally substituted by one or more groups “R” selected from halogen, —NRaRb, C1-6 alkyl, C2-6 alkenyl, C3-6 alkynyl, aryl, heteroaryl, hydroxy, —OC1-6 alkyl, formyl, cyano, trifluoromethyl, —CHNORa, —CO2Ra, —CONRaRb, —NRaC(O)Ra, —NRaC(O)ORa, —OC(O)NRaRb, —OC(O)Ra, —OC(O)ORa, or a C1-6 alkyl group substituted by one or more groups selected from hydroxy, —NRaRb, —OC1-6 alkyl, —SRa, —CHNORa, —CO2Ra, —CONRaRb, —NRaC(O)Ra, —NRaC(O)ORa, —OC(O)NRaRb, —OC(O)Ra, —OC(O)ORa X represents —NRxRy or —OC1-6 alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, amino and trifluoromethyl.
    Type: Application
    Filed: December 3, 2007
    Publication date: February 26, 2009
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Fiandor, Roger Frechette
  • Publication number: 20040043388
    Abstract: The invention provides compositions and methods for isolating ligand binding polypeptides for a user-specified ligand, and for isolating small molecule ligands for a user-specified target polypeptide using an improved class of hybrid ligand compounds.
    Type: Application
    Filed: September 3, 2002
    Publication date: March 4, 2004
    Inventors: Jon H. Come, Frank Becker, Nikolai A. Kley, Christoph Reichel
  • Publication number: 20030125348
    Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 29, 2001
    Publication date: July 3, 2003
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Jimmy Dumornay, Glen Rennie, Gui Liu, Darrell Koza, Paul Sheahan, Karen Stapleton, Paul Hawkins, Beena Bhatia, Atul K. Verma, Laura McIntyre, Tadeusz Warchol, David Messersmith
  • Publication number: 20020160987
    Abstract: The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted with aryl, alkenyl, or alkynyl groups. The 7, 8, and/or 9 positions and methods for preparing such compounds. Other tetracycline compounds include the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N—NH-Alkyl group substituted at the C4 position as well as C2 Mannich derivatives. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified tetracycline compounds.
    Type: Application
    Filed: July 24, 2001
    Publication date: October 31, 2002
    Inventors: Robert Ashley, Joseph J. Hlavka
  • Patent number: 6410695
    Abstract: The present invention relates to a conjugate comprising an active substance and a compound having a binding site for metallic compounds. In addition, this invention relates to a process for the preparation of such a conjugate and its use.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: June 25, 2002
    Assignee: Deutsches Krebsforschungszentrum Stiftung Des Öffentlichen Rechts
    Inventors: Hannsjörg Sinn, Wolfgang Maier-Borst, Hans-Hermann Schrenk, Gerd Stehle
  • Patent number: 6359113
    Abstract: The protective group having the following formula (I): Ar—L—  (I) wherein Ar represents a substantially planar, fused ring system containing at least 4 aromatic rings, and L represents a group containing at least one carbon atom which is capable of bonding to a group to be protected.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: March 19, 2002
    Assignee: Rhodia Chimie
    Inventors: Robert Ramage, Gilles Raphy
  • Patent number: 6184397
    Abstract: The present invention provides a method for the direct esterification of stanols and sterols with catalyst, which can be acidic or basic, in the presence of a color deactivating agent to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: February 6, 2001
    Assignee: McNeil-PPC, Inc.
    Inventors: Allan Roden, James L. Williams, Ruey Bruce, Frank Detrano, Marie H. Boyer, John D. Higgins, III
  • Patent number: 5804563
    Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier.
    Type: Grant
    Filed: April 8, 1996
    Date of Patent: September 8, 1998
    Assignee: The Trustees of Columbia University in The City of New York
    Inventors: W. Clark Still, Ge Li
  • Patent number: 5663386
    Abstract: The invention discloses the use of anthraquinones of the formula ##STR1## where R.sup.3 is unsubstituted or substituted C.sub.1 -C.sub.18 -alkyl or unsubstituted or substituted phenyl for marking mineral oils. Also disclosed are the marked mineral oils and a method of detecting the anthraquinones in mineral oils.
    Type: Grant
    Filed: September 18, 1995
    Date of Patent: September 2, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Friedrich-Wilhelm Raulfs, Christos Vamvakaris
  • Patent number: 5488119
    Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: January 30, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer-Reimann, Walter Fischer
  • Patent number: 5407885
    Abstract: Compounds of formula I or V or mixtures thereof ##STR1## wherein R is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.5, and R.sub.5 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, and at least one of the substituents R.sub.1 to R.sub.4 is --F, --Cl or --Br, or is independently the group RO--, and the other substituents R.sub.1 to R.sub.4 are H, --F, --Cl or --Br, are reversible photochromic systems which can be used for contrast formation, light absorption or for the reversible optical storage of information.
    Type: Grant
    Filed: February 1, 1993
    Date of Patent: April 18, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Jurgen Finter, Heinz Spahni
  • Patent number: 5300663
    Abstract: Compounds of formula V, ##STR1## wherein R is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthiol, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.5, and R.sub.5 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, and at least one of the substituents R.sub.1 to R.sub.4 is an organic thiol, sulfoxyl or sulfonyl group, and the other members R.sub.1 to R.sub.4 are H, F, Cl or Br, are reversible photochromic systems which can be used for contrast formation or light absorption.
    Type: Grant
    Filed: January 11, 1993
    Date of Patent: April 5, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Evelyn Fischer, Ernst Minder, Manfred Hofmann, Jurgen Finter, Heinz Spahni
  • Patent number: 5208354
    Abstract: Compounds of formula I or V or mixtures thereof ##STR1## whereinR is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.5, and R.sub.5 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, and at least one of the substituents R.sub.1 to R.sub.4 is --F, --Cl or --Br, or is independently the group RO--, and the other substituents R.sub.1 to R.sub.4 are H, --F, --Cl or --Br, are reversible photochromic systems which can be used for contrast formation, light absorption or for the reversible optical storage of information.
    Type: Grant
    Filed: December 2, 1991
    Date of Patent: May 4, 1993
    Assignee: Ciba-Geigy Corp.
    Inventors: Walter Fischer, Jurgen Finter, Heinz Spahni