Daunomycin Or Derivative Patents (Class 536/6.4)
  • Patent number: 10954261
    Abstract: The invention relates to a method for producing aqueous preparations of complexes of platinum group metals (PGM) Pt, Pd, Rh and Ir having the general formula [MA/MB/MC(L)a (H2O)b (O2—)c(OH?)d] (OH—)e(H+)f, wherein MA=PtII or PdII, MB=PtIV, MC=Rh or Ir, L is a neutral monodentate or bidentate donor ligand, and a is an integer between 1 and 4 (or 2) and/or between 1 and 6 (or 3), b is an integer between 0 and 3 (or 5), c is an integer between 0 and 3 (or 4), d is an integer between 0 and 3 (or 5), e is an integer between 0 and 2 (or 3 or 4) and f is an integer between 0 and 4 (or 5). In the method according to the invention, the hydroxo complexes H2Pd(OH)4 (in the case of MA=PdII), H2Pt(OH)6 (in the case of MA=PtII and MB=PtIV) or H3MC(OH)6 (for MC=RhIII IrIII) are converted in the presence of the donor ligands, wherein at least one hydroxo group of the hydro complex is exchanged. Preferably, the reaction occurs at temperatures in the range of 40 to 110° C.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: March 23, 2021
    Inventors: Eileen Woerner, Ralf Karch, Andreas Rivas-Nass, Angelino Doppiu
  • Patent number: 9492553
    Abstract: The present invention relates to antibody-drug conjugate compounds of Formula I: Ab-(L-D)p??I where one or more nemorubicin metabolite or analog drug moieties (D) are covalently attached by a linker (L) to an antibody (Ab) which binds to one or more tumor-associated antigens or cell-surface receptors. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: November 15, 2016
    Assignee: GENENTECH, INC.
    Inventors: Robert L. Cohen, Edward HyungSuk Ha, Mark E. Reynolds
  • Patent number: 9434756
    Abstract: 4?-epidaunorubicin hydrochloride is provided in a crystalline form which is stable and readily soluble. A process of producing the crystalline form includes crystallizing 4?-epidaunorubicin hydrochloride in a solvent system including (a) solvent A selected from C1 and C2 halogenated solvents and mixtures thereof, (b) solvent B selected from C1-C5 straight and branched alcohols and mixtures thereof, and (c) solvent C selected from C1-C5 straight and branched alcohols and mixtures thereof, wherein solvent C is selected to provide lower solubility to 4?-epidaunorubicin hydrochloride than solvent B. A method of producing an anthracycline using crystalline 4?-epidaunorubicin hydrochloride is also provided.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: September 6, 2016
    Assignee: medac Gesellschaft für klinische Spezialpräparate mbH
    Inventors: Tero Kunnari, Holger Bindernagel, Sascha Weiser, Andrew Lupton, Stefan Wallert
  • Patent number: 9371302
    Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: June 21, 2016
    Assignee: AvoScience, LLC
    Inventor: Richard Huber
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Publication number: 20150141359
    Abstract: Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.
    Type: Application
    Filed: January 19, 2015
    Publication date: May 21, 2015
    Inventors: Justin Scot Hanes, Peter Anthony Campochiaro, Jie Fu
  • Publication number: 20150118248
    Abstract: The application describes a method of screening for breast cancer by testing fro the amount of HAGE (Helicase antigen) in a sample of breast tissue. Methods of prognosis of samples of breast cancer tumours are also provided. HAGE+ ER? (estrogen receptor-) cancers are indicated as being amenable to chemotherapy. Methods of treating breast cancers with HAGE-specific CTA antigen or HAGE-specific antibodies are also provided.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 30, 2015
    Inventors: Adam Linley, Morgan Mathieu, Stephanie Mcardle, Chungui Lu, Robert Rees
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Publication number: 20150072946
    Abstract: A process for the preparation of nanoparticles from polysaccharides and derivatives thereof, by their specific partial oxidation to produce aldehyde groups and attachment of compounds with amino or other group with the R—NH2 bond which react with aldehyde groups, and a nanoparticle produced by such process.
    Type: Application
    Filed: September 12, 2014
    Publication date: March 12, 2015
    Inventors: Tomasz CIACH, Iga WASIAK
  • Patent number: 8962577
    Abstract: Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: February 24, 2015
    Assignee: The Johns Hopkins University
    Inventors: Justin Scot Hanes, Peter Anthony Campochiaro, Jie Fu
  • Publication number: 20150032045
    Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 29, 2015
    Inventors: Rafael Yuste, Roberto Etchenique, Luis Baraldo
  • Publication number: 20150017246
    Abstract: The invention provides novel chemical entities based on sugar alcohols. These new chemical entities are biocompatible and biodegradable. The molecules can be made in a single and pure form. The molecular weights of these molecules range from small (<1000 Da) to large (1000-120,000 Da). The sugar alcohol-based molecules can have functional groups throughout the molecule for crosslinking compounds, such as the preparation of antibody-drug conjugates, or to facilitate the delivery of therapeutic proteins, peptides, siRNA, and chemotherapeutic drugs. Also provided are new conjugate entities prepared through sugar alcohol molecules. Methods of synthesizing sugar alcohol-based molecules and conjugates are also within the scope of the invention.
    Type: Application
    Filed: January 15, 2014
    Publication date: January 15, 2015
    Applicant: CellMosaic, Inc.
    Inventor: Yumei Huang
  • Publication number: 20150011492
    Abstract: The present invention relates generally to the pathology of restenosis. In particular, provided herein are devices comprising a compound that selectively decreasing smooth muscle cell proliferation without a substantial decrease in endothelial cell proliferation. Also provided are methods of using such devices to treat, prevent, or reduce vascular disease or the likelihood of restenosis following angioplasty.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Inventors: F. Michael Hoffmann, K. Craig Kent, Shakti Goel, Lian-Wang Guo, Toshio Takayama
  • Publication number: 20140378673
    Abstract: Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.
    Type: Application
    Filed: February 13, 2013
    Publication date: December 25, 2014
    Inventors: Yukio Nagasaki, Yutaka Ikeda, Hikaru Hisano
  • Publication number: 20140364359
    Abstract: The invention provides di-peptide conjugated antitumor agents, pharmaceutical compositions and methods for preparation and use thereof for treating various cancer and inflammation-related diseases and conditions. The present invention addresses the shortcomings of the existing anti-tumor and anti-inflammatory drugs, particularly in that the anti-tumor agents of the invention that selectively kill cancer cells with minimal damage to normal cells.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 11, 2014
    Inventor: Raymond A FIRESTONE
  • Publication number: 20140357848
    Abstract: 4?-epidaunorubicin hydrochloride is provided in a crystalline form which is stable and readily soluble. A process of producing the crystalline form includes crystallizing 4?-epidaunorubicin hydrochloride in a solvent system including (a) solvent A selected from C1 and C2 halogenated solvents and mixtures thereof, (b) solvent B selected from C1-C5 straight and branched alcohols and mixtures thereof, and (c) solvent C selected from C1-C5 straight and branched alcohols and mixtures thereof, wherein solvent C is selected to provide lower solubility to 4?-epidaunorubicin hydrochloride than solvent B. A method of producing an anthracycline using crystalline 4?-epidaunorubicin hydrochloride is also provided.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Tero KUNNARI, Holger BINDERNAGEL, Sascha WEISER, Andrew LUPTON, Stefan WALLERT
  • Publication number: 20140350230
    Abstract: The present invention relates to a multi-functional nucleic acid-based anti-cancer drug in which the anti-cancer drug is physically bound to a linear nucleic acid having a thiol group at 5? terminal thereof and then gold nanoparticles and aptamers are chemically bound. The present invention also relates to a method for preparing the anti-cancer drug and to an anti-cancer composition comprising the anti-cancer drug. The multi-functional nucleic acid-based anti-cancer drug according to the present invention uses A10 aptamer to achieve high targeting properties, and uses high-concentration anti-cancer drugs and gold nanoparticles to enable dual therapy of thermal therapy/chemical therapy, and may have less side effects and be more effective in anti-cancer therapy compared to existing anti-cancer drugs.
    Type: Application
    Filed: September 21, 2012
    Publication date: November 27, 2014
    Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY
    Inventors: Soong Ho Um, A Ra Kim
  • Patent number: 8895725
    Abstract: Use of 9,10-anthraquinone compounds of formula (I) or pharmaceutical salts thereof or plant extracts containing said compounds in the preparation of anti-HCV medicaments is disclosed, in which Y1 are Y2 are independently hydrogen, hydroxyl or groups of formula (II); and R1, R2, R3, R4, R5 and R6 are independently hydrogen, hydroxyl, carboxyl, cyano group, nitro group, groups of formula (III) or groups selected from those substituted or unsubstituted groups: amino, C1-C6 aliphatic hydrocarbon, C3-C7 cyclic aliphatic hydrocarbon, C1-C6 alkoxy, C2-C7 carbalkoxy, C1-C4 acyloxy, C6-C20 aryl, or 5 to 7 members heterocyclic or benzoheterocyclic thereof; or R5 and R6 form the group of formula (IV). The compounds of present invention are cheap, safe and effective because that they mostly come from traditional Chinese medicines and have better anti-HCV effects and lighter side effects.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: November 25, 2014
    Assignees: Shanghai Institute of Pharmaceutical Industry, Institute Pasteur of Shanghai, Chinese Academy of Sciences
    Inventors: Shuguang Wang, Jin Zhong, Deyun Kong, Jue Hu, Bo Li, Wen Gao, Chunyan Gai, Changlong Zhuang, Haitao Mao
  • Publication number: 20140343261
    Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic application.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 20, 2014
    Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
  • Publication number: 20140335132
    Abstract: This invention describes nanocrystalline cellulose (NCC) for use as a drug delivery excipient. NCC binds significant quantities of water soluble, ionizable drugs, e.g., tetratcycline and doxorubicin, which are released rapidly over a one day period. A surfactant such as cetyl trimethylammonium bromide (CTAB) can bind to the surface of NCC and increase the zeta potential in a concentration-dependent manner from ?55 to 0 mV. NCC with CTAB modified surfaces can bind significant quantities of the hydrophobic drugs such as anticancer drugs docetaxel, paclitaxel and etoposide. These drugs were released in a controlled manner over a 2-day period. The NCC-CTAB nanocomplexes were found to bind to KU-7 cells and evidence of cellular uptake was observed.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 13, 2014
    Inventors: Helen Mary Burt, John Kevin Jackson, Wadood Yasser Hamad
  • Patent number: 8877720
    Abstract: Disclosed are compounds represented by formula (I), pharmaceutically acceptable salts thereof, solvates thereof, and solvates of the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, W and are as defined in the present application.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: November 4, 2014
    Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 8865130
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20140308234
    Abstract: Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as cisplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
    Type: Application
    Filed: April 9, 2014
    Publication date: October 16, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: Jeremiah A. Johnson, Longyan Liao
  • Publication number: 20140294851
    Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.
    Type: Application
    Filed: April 1, 2013
    Publication date: October 2, 2014
    Inventor: MARK QUANG NGUYEN
  • Patent number: 8846882
    Abstract: The present invention relates to a method for the synthesis of 4-demethoxydaunorubicin (idarubicin) having the chemical structure of formula (I), which involves the demethylation of 3?-Prot-daunorubicin in the presence of a soft Lewis acid. The method of the present invention does not comprise cleavage of the glycosidic linkage at carbon C7, thus resulting in a faster synthesis cycle and an improved yield of the final product.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: September 30, 2014
    Assignee: Synbias Pharma AG
    Inventors: Alexander Zabudkin, Victor Matvienko, Alexey Matvyeyev
  • Patent number: 8822658
    Abstract: 4?-epidaunorubicin hydrochloride is provided in a crystalline form which is stable and readily soluble. A process of producing the crystalline form includes crystallizing 4?-epidaunorubicin hydrochloride in a solvent system including (a) solvent A selected from C1 and C2 halogenated solvents and mixtures thereof, (b) solvent B selected from C1-C5 straight and branched alcohols and mixtures thereof, and (c) solvent C selected from C1-C5 straight and branched alcohols and mixtures thereof, wherein solvent C is selected to provide lower solubility to 4?-epidaunorubicin hydrochloride than solvent B. A method of producing an anthracycline using crystalline 4?-epidaunorubicin hydrochloride is also provided.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: September 2, 2014
    Assignee: Heraeus Precious Metals GmbH & Co. KG
    Inventors: Tero Kunnari, Holger Bindernagel, Sascha Weiser, Andrew Lupton, Stefan Wallert
  • Publication number: 20140236071
    Abstract: Conjugates are provided which comprise a membrane permeable drug linked to a moiety that is not membrane permeable. Attachment of the moiety that is not membrane permeable prevents the drug from crossing cell membranes and entering cells. However, exposure to light either i) breaks the linkage, releasing the drug and allowing it to enter cells; or ii) converts the non-membrane permeable moiety to a membrane permeable form, allowing the entire conjugate to enter the cell, where the drug is released from the conjugate by cleavage. The membrane permeable drugs are thus delivered to cells at locations of interest, e.g. cancer cells in a tumor, in a temporally and spatially controlled manner.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 21, 2014
    Inventors: Matthew Hartman, Martin Michael Dcona, Deboleena Mitra
  • Publication number: 20140228311
    Abstract: A method is provided for production of crystalline idarubicin hydrochloride, the method including the steps of: (i) producing a mixture containing (a) idarubicin hydrochloride, (b) at least one alcohol selected from 1-butanol, 2-butanol, and 1-pentanol, and (c) water; and (ii) crystallizing idarubicin hydrochloride from this mixture. A crystalline idarubicin hydrochloride is also provided characterized by a powder x-ray diffraction pattern in which at least reflexes at diffraction angles occur in the following ranges (in 2?): 7.2-7.7; 11.7-12.2; 16.2-16.7; 16.7-17.2; 19.6-20.1; 19.8-20.3; 22.2-22.7, and 22.9-23.4.
    Type: Application
    Filed: September 4, 2012
    Publication date: August 14, 2014
    Applicant: HERAEUS PRECIOUS METALS GMBH & CO. KG
    Inventor: Tero Kunnari
  • Patent number: 8802830
    Abstract: A method of preparing an anthracyclin such as epirubicin from a starting material comprising 13-dihydrodaunorubicine (13-daunorubicinol). The method comprises producing N-Trifluoroacetyl-13-daunorubicinol from 13-daunorubicinol by acylation. The N-Trifluoroacetyl-13-daunorubicinol is reacted with an aprotic solvent and an acylating agent to produce an intermediate sulfoxy salt which is treated with a strong base to produce 4?-keto-N-Trifluoroacetyldaunorubicin. The 4?-keto-N-Trifluoroacetyldaunorubicin is reacted with a reducing agent, such as borohydride of an alkaline metal, to produce N-Trifluoroacetyl-4?-epi-daunorubicin. The N-Trifluoroacetyl-4?-epi-daunorubicin is hydrolyzed in a basic solution to produce an intermediate compound. The intermediate compound is reacted with a halogenizing agent to produce a 14-Hal-derivative. The 14-Hal derivative is hydrolized in the presence of a formate of an alkaline metal to produce the desired final compound.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: August 12, 2014
    Assignee: Solux Corporation
    Inventors: Alexander F. Zabudkin, Victor Matvienko, Aleksandr M. Itkin, Alexey Matveev
  • Patent number: 8802831
    Abstract: This invention is in the field of anthracycline family of drugs. More particularly, it concerns converting daunorubicin hydrochloride to an orotate salt and providing methods of improving the tolerability of daunorubicin in animals by reducing the adverse effects and toxicity in noncancerous tissues. Daunorubicin orotate provides a safer treatment for specific types of leukemias and neuroblastomas in adults and in pediatric patients.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: August 12, 2014
    Assignee: Savvipharm Inc
    Inventor: Rashida A. Karmali
  • Patent number: 8785406
    Abstract: The present invention provides a lyophilized amrubicin formulation and a process thereof. In the process, the concentration of the aqueous solution before lyophilization is controlled to about 7.5 mg(potency)/mL or more. Thus, the formulation decreases the production of desaccharified compound and is stable to storage for a long period. The formulation is useful as a cancer chemotherapeutic agent.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: July 22, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Hajimu Hirofuji, Hotaka Hashimoto, Kazunari Tanaka
  • Publication number: 20140199331
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Application
    Filed: May 16, 2012
    Publication date: July 17, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
  • Patent number: 8778914
    Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: July 15, 2014
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: Felix Kratz, Katrin Hochdoerffer
  • Patent number: 8778897
    Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 15, 2014
    Assignee: The Regents of the University of California
    Inventor: Paul C. Simpson, Jr.
  • Publication number: 20140171629
    Abstract: Provided is a medicinal agent for medical applications, which can act on the function of a target cell specifically. The medicinal agent for medical applications comprises: a cell-incorporated substance that can be incorporated into a target cell specifically; and an acting substance that can act on the function of the target cell and is bound to the cell-incorporated substance.
    Type: Application
    Filed: August 9, 2012
    Publication date: June 19, 2014
    Applicants: HITACHI ALOKA MEDICAL, LTD., THE NIPPON DENTAL UNIVERSITY
    Inventors: Minako Suzuki, Taka Nakahara, Hiroshi Ishikawa, Akihiro Oyama
  • Publication number: 20140148587
    Abstract: 4?-epidaunorubicin hydrochloride is provided in a crystalline form which is stable and readily soluble. A process of producing the crystalline form includes crystallizing 4?-epidaunorubicin hydrochloride in a solvent system including (a) solvent A selected from C1 and C2 halogenated solvents and mixtures thereof, (b) solvent B selected from C1-C5 straight and branched alcohols and mixtures thereof, and (c) solvent C selected from C1-C5 straight and branched alcohols and mixtures thereof, wherein solvent C is selected to provide lower solubility to 4?-epidaunorubicin hydrochloride than solvent B. A method of producing an anthracycline using crystalline 4?-epidaunorubicin hydrochloride is also provided.
    Type: Application
    Filed: February 4, 2014
    Publication date: May 29, 2014
    Applicant: HERAEUS PRECIOUS METALS GMBH & CO. KG
    Inventors: Tero KUNNARI, Holger BINDERNAGEL, Sascha WEISER, Andrew LUPTON, Stefan WALLERT
  • Publication number: 20140093522
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 3, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
  • Publication number: 20140086843
    Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 27, 2014
    Applicant: ATLANTHERA
    Inventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
  • Publication number: 20140079636
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20140051623
    Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.
    Type: Application
    Filed: February 24, 2012
    Publication date: February 20, 2014
    Applicant: KTB Tumorforschungsgesellschaft mbH
    Inventors: Felix Kratz, Katrin Hochdoerffer
  • Publication number: 20140046021
    Abstract: The molecular structures of metal-salen complexes which exerts pharmacological effects are clarified and the metal-salen complexes having such molecular structures and their derivatives are provided. A metal-salen complex compound is characterized in that a metal atom part in each of multiple molecules of the metal-salen complex or its derivative is multimerized via water.
    Type: Application
    Filed: January 19, 2012
    Publication date: February 13, 2014
    Applicants: IHI CORPORATION
    Inventors: Yoshihiro Ishikawa, Haruki Eguchi
  • Publication number: 20140044646
    Abstract: Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin ?v?3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin ?v?3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.
    Type: Application
    Filed: July 26, 2013
    Publication date: February 13, 2014
    Applicant: The Methodist Hospital Research Institute
    Inventors: King Chuen Li, Zheng Li, Feng Li
  • Publication number: 20140017322
    Abstract: Disclosed are nanoparticles, such as carbon nanotubes or other graphitic sheet materials having extended aromatic surfaces, which are used to deliver active agents such as drugs, labels or dyes (termed for convenience a “drug”) to the interior of cells. The nanoparticles are functionalized by a hydrophilic polymer or adsorption of an amphiphilic molecule to render them stable in suspension. The drug is therefore capable of release in the cell exterior. The drug is more rapidly released at lower pH, as found e.g., in tumor cells. The drug may also be linked to a branched chain hydrophilic polymer, so that each polymer molecule carries more than one drug bound by a cleavable linker.
    Type: Application
    Filed: September 16, 2013
    Publication date: January 16, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Hongjie Dai, Zhuang Liu, Xiaolin Li, Xiaoming Sun
  • Publication number: 20130337065
    Abstract: A delivery device for an active agent comprises nanoparticles based on a biopolymer such as starch. The delivery device may also be in the form of an aptamer-biopolymer-active agent conjugate wherein the aptamer targets the device for the treatment of specific disorders. The nanoparticles may be made by applying a high shear force in the presence of a crosslinker. The particles may be predominantly in the range of 50-150 nm and form a colloidal dispersion of crosslinked hydrogel particles in water. The biopolymer may be functionalized. The aptamer may be conjugated directly to the cross-linked biopolymers. The active agent may be a drug useful for the treatment of cancer. The delivery device survives for a period of time in the body sufficient to allow for the sustained release of a drug and for the transportation and uptake of the conjugate into targeted cells. However, the biopolymer is biocompatible and resorbable.
    Type: Application
    Filed: December 2, 2011
    Publication date: December 19, 2013
    Applicant: ECOSYNTHETIX LTD.
    Inventors: Steven Bloembergen, Ian J. McLennan, Nathan Jones, Ryan Wagner, Aareet Ganesh Shermon, Abdel Rahman Elsayed, Juewen Liu
  • Patent number: 8609135
    Abstract: Anthracycline derivatives are suitable for use in cancer therapy and diagnosis. These anthracycline derivatives can be radiolabelled and used as an imaging agent in cancer diagnosis. The radiolabelled anthracycline derivatives can also be used together with a drug delivery system, in particular including a two-step targeting strategy, for treating solid and disseminated tumors. These drug delivery system can advantageously be used for treatment and diagnosis of breast cancer.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: December 17, 2013
    Assignee: Nuclisome AB
    Inventors: Katarina Edwards, Stefan Sjöberg, Jörgen Carlsson, Lars Gedda
  • Publication number: 20130331764
    Abstract: The present invention relates to a method for effectively delivering an anticancer drug into cancer cells by binding the anticancer drug to pH-sensitive metal nanoparticles so as to be separated from cancer cells. The pH-sensitive metal nanoparticles according to the present invention may be heated by photothermal therapy, thereby effectively killing cancer cells in conjunction with the isolated anticancer drug.
    Type: Application
    Filed: April 7, 2011
    Publication date: December 12, 2013
    Inventors: Sungjee Kim, Jutaek Nam
  • Patent number: 8603990
    Abstract: A polymeric drug, in which a cancerostatic connected via spacers containing hydrolytically cleavable hydrazone bonds is bound to a water-soluble polymeric carrier prepared on the basis of a N-(2-hydroxypropyl)methacrylamide copolymer, wherein the structure of the polymeric drug consists of the main chain of N-(2-hydroxypropyl)methacrylamide carrying the cancerostatic and another chain of N-(2-hydroxypropyl)methacrylamide—a graft, which may also carry a cancerostatic, said grafts being bound to the main chain by a bond that is stable in the body and/or by a bond cleavable in the body, especially by an oligopeptide spacer selected from the series of GlyLeuGly (SEQ ID. NO. 1), GlyPheGly (SEQ ID. NO. 2), GlyPheLeuGly (SEQ ID. NO. 3) and GlyLeuPheGly (SEQ ID. NO. 4), and a method of its preparation.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: December 10, 2013
    Assignee: Zentiva k.s.
    Inventors: Tomas Etrych, Petr Chytil, Karel Ulbrich, Tomas Mrkvan, Blanka Rihova
  • Publication number: 20130324706
    Abstract: The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 5, 2013
    Inventors: Laurent Ducry, Bernhard Stump, Heilam Wong, Jin She, Gayle Phillips
  • Patent number: 8575359
    Abstract: The invention is in general directed to acid-sensitive linkers, and methods of use thereof, such as, for example, in drug delivery methods.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: November 5, 2013
    Assignee: The Regents of the University of California
    Inventors: Jerry Yang, Seong Deok Kong, Alice Luong, Stephen Howell
  • Patent number: RE47873
    Abstract: Embolic compositions comprising macromers having a backbone comprising a polymeric backbone comprising units with a 1,2-diol or 1,3-diol structure, such as polyvinyl alcohol, and pendant chains bearing crosslinkable groups and, optionally, other modifiers. When crosslinked, the macromers form hydrogels having many properties advantageous for use as embolic agents to block and fill lumens and spaces. The embolic compositions can be used as liquid embolic agents and crosslinked in situ or as preformed embolic articles, such as microspheres.
    Type: Grant
    Filed: March 16, 2015
    Date of Patent: February 25, 2020
    Assignee: BIOCOMPATIBLES UK LIMITED
    Inventors: Dennis W. Goupil, Hassan Chaouk, Troy Holland, Bruktawit T. Asfaw, Stephen D. Goodrich, Lucas Latini