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)
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Patent number: 8992896Abstract: 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: GrantFiled: August 27, 2014Date of Patent: March 31, 2015Assignee: Foamix Pharmaceuticals Ltd.Inventors: Dov Tamarkin, Elana Gazal, Irakliy Papiashvili, Yohan Hazot, David Schuz, Rita Keynan
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Patent number: 8871184Abstract: 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 tetracyclineType: GrantFiled: October 1, 2010Date of Patent: October 28, 2014Assignee: Foamix Ltd.Inventors: Dov Tamarkin, Elana Gazal, Yohan Hazot, David Schuz, Rita Keynan, Nukri Papiashvili
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Patent number: 8865139Abstract: 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: GrantFiled: July 9, 2014Date of Patent: October 21, 2014Assignee: Foamix Pharmaceuticals Ltd.Inventors: Dov Tamarkin, Elana Gazal, Irakliy Papiashvili, Yohan Hazot, David Schuz, Rita Keynan
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Publication number: 20130196953Abstract: 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: ApplicationFiled: January 28, 2013Publication date: August 1, 2013Applicant: UNIVERZA V LJUBLJANIInventor: UNIVERZA V LJUBLJANI
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Publication number: 20130123217Abstract: 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: ApplicationFiled: December 13, 2012Publication date: May 16, 2013Applicant: NEUMEDICSInventor: Neumedics
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Publication number: 20130012481Abstract: 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: ApplicationFiled: July 17, 2012Publication date: January 10, 2013Applicant: SANDOZ AGInventors: Josef Wieser, Andreas Hotter, Arthur Pichler
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Publication number: 20100255117Abstract: The instant invention provides methods and compositions for the treatment of cancer.Type: ApplicationFiled: April 6, 2008Publication date: October 7, 2010Applicant: The Johns Hopkins UniversityInventors: Shyam Biswal, Anju Singh, Deepti Malhotra
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Patent number: 7786099Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.Type: GrantFiled: January 18, 2005Date of Patent: August 31, 2010Assignee: Paratek Pharmaceuticals, Inc.Inventor: Mark L. Nelson
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Publication number: 20090054379Abstract: 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: ApplicationFiled: December 3, 2007Publication date: February 26, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Fiandor, Roger Frechette
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Publication number: 20040043388Abstract: 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: ApplicationFiled: September 3, 2002Publication date: March 4, 2004Inventors: Jon H. Come, Frank Becker, Nikolai A. Kley, Christoph Reichel
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Publication number: 20030125348Abstract: 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: ApplicationFiled: June 29, 2001Publication date: July 3, 2003Inventors: 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
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Publication number: 20020160987Abstract: 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: ApplicationFiled: July 24, 2001Publication date: October 31, 2002Inventors: Robert Ashley, Joseph J. Hlavka
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Patent number: 6410695Abstract: 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: GrantFiled: February 9, 1998Date of Patent: June 25, 2002Assignee: Deutsches Krebsforschungszentrum Stiftung Des Öffentlichen RechtsInventors: Hannsjörg Sinn, Wolfgang Maier-Borst, Hans-Hermann Schrenk, Gerd Stehle
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Patent number: 6359113Abstract: 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: GrantFiled: September 30, 1998Date of Patent: March 19, 2002Assignee: Rhodia ChimieInventors: Robert Ramage, Gilles Raphy
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Patent number: 6184397Abstract: 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: GrantFiled: June 21, 1999Date of Patent: February 6, 2001Assignee: McNeil-PPC, Inc.Inventors: Allan Roden, James L. Williams, Ruey Bruce, Frank Detrano, Marie H. Boyer, John D. Higgins, III
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Patent number: 5804563Abstract: 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: GrantFiled: April 8, 1996Date of Patent: September 8, 1998Assignee: The Trustees of Columbia University in The City of New YorkInventors: W. Clark Still, Ge Li
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Patent number: 5663386Abstract: 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: GrantFiled: September 18, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Friedrich-Wilhelm Raulfs, Christos Vamvakaris
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Patent number: 5488119Abstract: 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: GrantFiled: October 12, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer-Reimann, Walter Fischer
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Patent number: 5407885Abstract: 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: GrantFiled: February 1, 1993Date of Patent: April 18, 1995Assignee: Ciba-Geigy CorporationInventors: Walter Fischer, Jurgen Finter, Heinz Spahni
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Patent number: 5300663Abstract: 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: GrantFiled: January 11, 1993Date of Patent: April 5, 1994Assignee: Ciba-Geigy CorporationInventors: Walter Fischer, Evelyn Fischer, Ernst Minder, Manfred Hofmann, Jurgen Finter, Heinz Spahni
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Patent number: 5208354Abstract: 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: GrantFiled: December 2, 1991Date of Patent: May 4, 1993Assignee: Ciba-Geigy Corp.Inventors: Walter Fischer, Jurgen Finter, Heinz Spahni