Daunomycin Or Derivative Patents (Class 536/6.4)
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Patent number: 11730822Abstract: The present invention provides improved processes for the preparation of drug-linkers with a ?-glucuronide cleavable unit, as well as intermediates thereof.Type: GrantFiled: March 23, 2018Date of Patent: August 22, 2023Assignee: Seagen Inc.Inventors: Yunyu Mao, Philip Moquist, Anusuya Choudhury, Wendel Doubleday
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Patent number: 11666589Abstract: The present invention relates to compositions comprising at least one of pivarubicin and benzarubicin, or a pharmaceutically acceptable salt thereof, and methods for using the compositions in the treatment of triple negative breast cancer (TNBC) by administering an effective amount of the compositions to a subject. In some instances, the subject is a mammal, including at least one of human, feline, and canine mammals.Type: GrantFiled: March 2, 2021Date of Patent: June 6, 2023Inventors: Leonard Lothstein, Judith Soberman, Tiffany N. Seagroves
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Patent number: 10954261Abstract: 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: GrantFiled: December 29, 2017Date of Patent: March 23, 2021Inventors: Eileen Woerner, Ralf Karch, Andreas Rivas-Nass, Angelino Doppiu
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Patent number: 9492553Abstract: 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: GrantFiled: April 16, 2014Date of Patent: November 15, 2016Assignee: GENENTECH, INC.Inventors: Robert L. Cohen, Edward HyungSuk Ha, Mark E. Reynolds
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Patent number: 9434756Abstract: 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: GrantFiled: August 14, 2014Date of Patent: September 6, 2016Assignee: medac Gesellschaft für klinische Spezialpräparate mbHInventors: Tero Kunnari, Holger Bindernagel, Sascha Weiser, Andrew Lupton, Stefan Wallert
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Patent number: 9371302Abstract: 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: GrantFiled: March 28, 2014Date of Patent: June 21, 2016Assignee: AvoScience, LLCInventor: Richard Huber
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Publication number: 20150141359Abstract: 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: ApplicationFiled: January 19, 2015Publication date: May 21, 2015Inventors: Justin Scot Hanes, Peter Anthony Campochiaro, Jie Fu
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Publication number: 20150139905Abstract: 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: ApplicationFiled: October 9, 2014Publication date: May 21, 2015Inventors: Dinesh Chimmanamada, Weiwen Ying
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Publication number: 20150118248Abstract: 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: ApplicationFiled: March 27, 2013Publication date: April 30, 2015Inventors: Adam Linley, Morgan Mathieu, Stephanie Mcardle, Chungui Lu, Robert Rees
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Publication number: 20150072946Abstract: 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: ApplicationFiled: September 12, 2014Publication date: March 12, 2015Inventors: Tomasz CIACH, Iga WASIAK
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Publication number: 20150072396Abstract: 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: ApplicationFiled: March 1, 2012Publication date: March 12, 2015Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
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Patent number: 8962577Abstract: 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: GrantFiled: March 12, 2013Date of Patent: February 24, 2015Assignee: The Johns Hopkins UniversityInventors: Justin Scot Hanes, Peter Anthony Campochiaro, Jie Fu
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Publication number: 20150032045Abstract: 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: ApplicationFiled: December 21, 2012Publication date: January 29, 2015Inventors: Rafael Yuste, Roberto Etchenique, Luis Baraldo
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Publication number: 20150017246Abstract: 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: ApplicationFiled: January 15, 2014Publication date: January 15, 2015Applicant: CellMosaic, Inc.Inventor: Yumei Huang
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Publication number: 20150011492Abstract: 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: ApplicationFiled: July 2, 2014Publication date: January 8, 2015Inventors: F. Michael Hoffmann, K. Craig Kent, Shakti Goel, Lian-Wang Guo, Toshio Takayama
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Publication number: 20140378673Abstract: 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: ApplicationFiled: February 13, 2013Publication date: December 25, 2014Inventors: Yukio Nagasaki, Yutaka Ikeda, Hikaru Hisano
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Publication number: 20140364359Abstract: 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: ApplicationFiled: January 17, 2013Publication date: December 11, 2014Inventor: Raymond A FIRESTONE
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Publication number: 20140357848Abstract: 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: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Inventors: Tero KUNNARI, Holger BINDERNAGEL, Sascha WEISER, Andrew LUPTON, Stefan WALLERT
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Publication number: 20140350230Abstract: 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: ApplicationFiled: September 21, 2012Publication date: November 27, 2014Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITYInventors: Soong Ho Um, A Ra Kim
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Patent number: 8895725Abstract: 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: GrantFiled: November 23, 2009Date of Patent: November 25, 2014Assignees: Shanghai Institute of Pharmaceutical Industry, Institute Pasteur of Shanghai, Chinese Academy of SciencesInventors: Shuguang Wang, Jin Zhong, Deyun Kong, Jue Hu, Bo Li, Wen Gao, Chunyan Gai, Changlong Zhuang, Haitao Mao
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Publication number: 20140343261Abstract: 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: ApplicationFiled: September 17, 2012Publication date: November 20, 2014Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
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Publication number: 20140335132Abstract: 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: ApplicationFiled: November 22, 2011Publication date: November 13, 2014Inventors: Helen Mary Burt, John Kevin Jackson, Wadood Yasser Hamad
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Patent number: 8877720Abstract: 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: GrantFiled: November 3, 2010Date of Patent: November 4, 2014Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.Inventor: Hesheng Zhang
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Patent number: 8865130Abstract: 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: GrantFiled: March 27, 2012Date of Patent: October 21, 2014Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Publication number: 20140308234Abstract: 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: ApplicationFiled: April 9, 2014Publication date: October 16, 2014Applicant: Massachusetts Institute of TechnologyInventors: Jeremiah A. Johnson, Longyan Liao
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Publication number: 20140294851Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.Type: ApplicationFiled: April 1, 2013Publication date: October 2, 2014Inventor: MARK QUANG NGUYEN
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Patent number: 8846882Abstract: 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: GrantFiled: April 29, 2011Date of Patent: September 30, 2014Assignee: Synbias Pharma AGInventors: Alexander Zabudkin, Victor Matvienko, Alexey Matvyeyev
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Patent number: 8822658Abstract: 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: GrantFiled: February 4, 2014Date of Patent: September 2, 2014Assignee: Heraeus Precious Metals GmbH & Co. KGInventors: Tero Kunnari, Holger Bindernagel, Sascha Weiser, Andrew Lupton, Stefan Wallert
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Publication number: 20140236071Abstract: 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: ApplicationFiled: September 28, 2012Publication date: August 21, 2014Inventors: Matthew Hartman, Martin Michael Dcona, Deboleena Mitra
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Publication number: 20140228311Abstract: 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: ApplicationFiled: September 4, 2012Publication date: August 14, 2014Applicant: HERAEUS PRECIOUS METALS GMBH & CO. KGInventor: Tero Kunnari
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Patent number: 8802830Abstract: 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: GrantFiled: December 18, 2006Date of Patent: August 12, 2014Assignee: Solux CorporationInventors: Alexander F. Zabudkin, Victor Matvienko, Aleksandr M. Itkin, Alexey Matveev
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Patent number: 8802831Abstract: 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: GrantFiled: February 27, 2012Date of Patent: August 12, 2014Assignee: Savvipharm IncInventor: Rashida A. Karmali
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Patent number: 8785406Abstract: 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: GrantFiled: May 27, 2009Date of Patent: July 22, 2014Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hajimu Hirofuji, Hotaka Hashimoto, Kazunari Tanaka
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Publication number: 20140199331Abstract: 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: ApplicationFiled: May 16, 2012Publication date: July 17, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Patent number: 8778914Abstract: 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: GrantFiled: August 24, 2010Date of Patent: July 15, 2014Assignee: KTB Tumorforschungsgesellschaft mbHInventors: Felix Kratz, Katrin Hochdoerffer
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Patent number: 8778897Abstract: 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: GrantFiled: September 7, 2012Date of Patent: July 15, 2014Assignee: The Regents of the University of CaliforniaInventor: Paul C. Simpson, Jr.
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Publication number: 20140171629Abstract: 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: ApplicationFiled: August 9, 2012Publication date: June 19, 2014Applicants: HITACHI ALOKA MEDICAL, LTD., THE NIPPON DENTAL UNIVERSITYInventors: Minako Suzuki, Taka Nakahara, Hiroshi Ishikawa, Akihiro Oyama
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Publication number: 20140148587Abstract: 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: ApplicationFiled: February 4, 2014Publication date: May 29, 2014Applicant: HERAEUS PRECIOUS METALS GMBH & CO. KGInventors: Tero KUNNARI, Holger BINDERNAGEL, Sascha WEISER, Andrew LUPTON, Stefan WALLERT
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Publication number: 20140093522Abstract: 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: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Publication number: 20140086843Abstract: 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: ApplicationFiled: March 28, 2012Publication date: March 27, 2014Applicant: ATLANTHERAInventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
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Publication number: 20140079636Abstract: 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: ApplicationFiled: March 15, 2013Publication date: March 20, 2014Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140051623Abstract: 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: ApplicationFiled: February 24, 2012Publication date: February 20, 2014Applicant: KTB Tumorforschungsgesellschaft mbHInventors: Felix Kratz, Katrin Hochdoerffer
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Publication number: 20140046021Abstract: 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: ApplicationFiled: January 19, 2012Publication date: February 13, 2014Applicants: IHI CORPORATIONInventors: Yoshihiro Ishikawa, Haruki Eguchi
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Publication number: 20140044646Abstract: 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: ApplicationFiled: July 26, 2013Publication date: February 13, 2014Applicant: The Methodist Hospital Research InstituteInventors: King Chuen Li, Zheng Li, Feng Li
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Publication number: 20140017322Abstract: 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: ApplicationFiled: September 16, 2013Publication date: January 16, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Hongjie Dai, Zhuang Liu, Xiaolin Li, Xiaoming Sun
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Publication number: 20130337065Abstract: 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: ApplicationFiled: December 2, 2011Publication date: December 19, 2013Applicant: ECOSYNTHETIX LTD.Inventors: Steven Bloembergen, Ian J. McLennan, Nathan Jones, Ryan Wagner, Aareet Ganesh Shermon, Abdel Rahman Elsayed, Juewen Liu
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Patent number: 8609135Abstract: 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: GrantFiled: October 13, 2009Date of Patent: December 17, 2013Assignee: Nuclisome ABInventors: Katarina Edwards, Stefan Sjöberg, Jörgen Carlsson, Lars Gedda
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Publication number: 20130331764Abstract: 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: ApplicationFiled: April 7, 2011Publication date: December 12, 2013Inventors: Sungjee Kim, Jutaek Nam
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Patent number: 8603990Abstract: 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: GrantFiled: September 18, 2007Date of Patent: December 10, 2013Assignee: Zentiva k.s.Inventors: Tomas Etrych, Petr Chytil, Karel Ulbrich, Tomas Mrkvan, Blanka Rihova
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Patent number: RE47873Abstract: 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: GrantFiled: March 16, 2015Date of Patent: February 25, 2020Assignee: BIOCOMPATIBLES UK LIMITEDInventors: Dennis W. Goupil, Hassan Chaouk, Troy Holland, Bruktawit T. Asfaw, Stephen D. Goodrich, Lucas Latini