Ring Nitrogen In The Pentacyclo Ring System Is Shared By Five-membered Cyclo And Six-membered Cyclo (e.g., Vincamine, Etc.) Patents (Class 514/283)
  • Publication number: 20140323514
    Abstract: Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
    Type: Application
    Filed: July 3, 2014
    Publication date: October 30, 2014
    Inventors: Xuan Zhao, Michael David Bentley, Zhongxu Ren, Tacey X. Viegas
  • Publication number: 20140323513
    Abstract: Disclosed are compound for targeting chemotherapeutic agents to mammalian mitochondria. Also disclosed are monoamine oxidase-specific compositions, and methods of using them for the selective therapy of mammalian cancers, and in particular, in the treatment of human gliomas. Also disclosed are methods employing the novel targeted chemotherapeutics with one or more conventional anti-cancer therapies, including, for example, radiotherapy, or multi-drug regimens.
    Type: Application
    Filed: April 30, 2014
    Publication date: October 30, 2014
    Inventors: David S. Baskin, Martyn Alun Sharpe
  • Patent number: 8871253
    Abstract: A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase contains sulfobutyl ether cyclodextrin and active compound. Said sulfobutyl ether cyclodextrin is sulfobutyl ether ?-cyclodextrin, sulfobutyl ether ?-cyclodextrin, or sulfobutyl ether ?-cyclodextrin.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: October 28, 2014
    Assignee: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.
    Inventors: Chunlei Li, Lan Zhang, Caixia Wang, Li Zhang, Dongmin Shen, Yanhui Li, Xian Xiu, Min Liang, Yongfeng Li
  • Publication number: 20140314750
    Abstract: Described herein are methods of predicting the risk of developing ovarian cancer recurrence of a subject comprising the steps of detecting the expression levels of at least four of the six genes selected from the group consisting of AKT2, KRAS, RAC1, CALM3, RPS6KA2 and YWHAB or the gene products thereof, wherein the presence of increased expression levels of the genes or the gene products is predictive of the increased risk of developing ovarian cancer recurrence in the subject. Kits for practicing the methods are also disclosed.
    Type: Application
    Filed: April 11, 2014
    Publication date: October 23, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Christina Kendziorski Newton, Kevin Hasegawa Eng
  • Publication number: 20140314664
    Abstract: Symmetrically and asymmetrically branched homopolymers are modified at the surface level with functional groups that enable forming aggregates with water insoluble or poorly water soluble pharmaceutically active agents (PAA). The aggregates formed are specifically induced by interaction of PAA and homopolymer and are different from aggregates that are formed by the polymer alone in the absence of the PAA or by the PAA alone in the absence of the polymer. Such aggregates can be used to improve drug solubility, stability, delivery and efficacy.
    Type: Application
    Filed: January 6, 2012
    Publication date: October 23, 2014
    Applicant: ANP Technologies, Inc.
    Inventors: Dujie Qin, Ray Yin, Jing Pan, Yubei Zhang
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Publication number: 20140308336
    Abstract: Drug-eluting devices and methods for the treatment of tumors of the pancreas, biliary system, gallbladder, liver, small bowel, or colon, are provided. Methods include deploying a drug-eluting device having a film which includes a mixture of a degradable polymer and a chemotherapeutic drug, wherein the film has a thickness from about 2 ?m to about 1000 ?m, into a tissue site and releasing a therapeutically effective amount of the chemotherapeutic drug from the film to treat the tumor, wherein the release of the therapeutically effective amount of the drug from the film is controlled by in vivo degradation of the polymer at the tissue site.
    Type: Application
    Filed: April 10, 2014
    Publication date: October 16, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Laura Indolfi, Elazer R. Edelman, Robert S. Langer, Jeffrey W. Clark, David T. Ting, Cristina Rosa Annamaria Ferrone, Matteo Ligorio
  • Publication number: 20140308370
    Abstract: Compositions and methods for determining circulating biomolecules before, during, and/or after treatment of a patient with an anti-cancer or anti-tumor drug (or putative drug) are described. Methods of treatments based on the compositions and methods described herein are also provided. Noninvasive methods and kits are provided for assessing the efficacy of an anti-cancer therapy for killing or damaging cancer cells. Embodiments are used to determine the cancer-killing efficacy of an anti-cancer drug in a patient, to optimize the selection of an anti-cancer drug for treatment of a patient, to adjust the dosage of an anti-cancer drug for treatment of a particular cancer in a patient and for identifying useful anti-cancer therapeutics for any one particular type of cancer.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 16, 2014
    Inventors: David Frendewey, Gavin Thurston, George D. Yancopoulos, Matthew Koss, Gustavo Droguett
  • Publication number: 20140302173
    Abstract: A method for treating side effects of anticancer agent includes administering to a subject in need thereof a prophylactic and/or therapeutic agent containing a therapeutically effective amount of a compound shown by the following Formula (1): R1—NHCH2COCH2CH2COOR2 ??(I) wherein R1 represents a hydrogen atom or an acyl group, and R2 represents a hydrogen atom, a linear or branched alkyl group, a cycloalkyl group, an aryl group, or an aralkyl group, or a salt thereof.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION KOCHI UNIVERSITY, SBI PHARMACEUTICALS CO., LTD.
    Inventors: Tohru Tanaka, Kyoko Tsuchiya, Masahiro Ishizuka, Motowo Nakajima, Hitoshi Nakagawa, Taro Shuin, Keiji Inoue, Hideo Fukuhara, Masayuki Tsuda, Mutsuo Furihata
  • Patent number: 8853233
    Abstract: A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: October 7, 2014
    Assignees: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Istituto Nazionale per lo Studio e la Cura dei Tumori
    Inventors: Claudio Pisano, Loredana Vesci, Franco Zunino
  • Patent number: 8853151
    Abstract: The present invention provides methods, compositions and applications for efficient, site-specific drug delivery using pro-drug complexes comprising one or more functional groups (e.g., imaging agents, targeting agents, and trigger agents) conjugated with a therapeutic agent (e.g., a chemotherapeutic agent), methods of synthesizing the same, as well as systems and methods utilizing the therapeutic and diagnostic compositions (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.))). Trigger agents include an indolequinone; attachment groups include a triazole ring; and therapeutic agents include camptothecin.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: October 7, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Baohua M. Huang, Thommey P. Thomas
  • Publication number: 20140296278
    Abstract: Provided herein are compositions for lowering intracellular pH in a cell or population of cells from a subject comprising contacting the cell or population of cells with a therapeutically effective amount of 5-nonyloxytryptamine or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivatives thereof. These compounds are useful for acidification of cells, including cancer cells, which induces apoptosis and cell necrosis. Methods of use of these compounds, including in pharmaceutical compositions in conjunction with other biologically active agents, in treatment of cancers, including glioblastoma and related neuronal cancers are also included.
    Type: Application
    Filed: October 25, 2012
    Publication date: October 2, 2014
    Inventor: Eli Eliyahu Bar
  • Publication number: 20140294973
    Abstract: The present invention provides a pharmaceutical composition comprising at least one hydrophobic camptothecin derivative or a pharmaceutically acceptable salt of said derivative and a polyethylene glycol (PEG) conjugated phospholipid. Also provided is a method to inhibit cancer cells in a subject in need thereof by administering the pharmaceutical composition of the present invention.
    Type: Application
    Filed: November 2, 2012
    Publication date: October 2, 2014
    Inventors: Pei Kan, ChiaHung Hung, Kee-lung Hong, Yun-Long Tseng, Yun-Hsu Chan
  • Publication number: 20140294818
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a PGAM1 mediated condition such as cancer or tumor growth comprising administering an effective amount of PGAM1 inhibitor, for example, an anthracene-9,10-dione derivative to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, head and neck cancer, and leukemia, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 2, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Jing Chen, Taro Hitosugi, Sumin Kang
  • Publication number: 20140286938
    Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.
    Type: Application
    Filed: March 21, 2014
    Publication date: September 25, 2014
    Applicant: EcoBiotics Ltd
    Inventors: Paul Warren Reddell, Victoria Anne Gordon
  • Publication number: 20140287063
    Abstract: Provided are methods of determining a response to a chemotherapeutic agent in a subject with ovarian cancer, comprising: determining a RNA integrity value of a sample comprising ovarian cancer cell RNA from the subject after the subject has received one or more doses of the chemotherapeutic agent; wherein a low RNA integrity value and/or RNA degradation of the cancer cell RNA is indicative that the cancer is responding to the chemotherapeutic agent and/or a high RNA integrity value and/or stable RNA integrity of the ovarian cancer cell RNA is indicative that the cancer is resistant to the chemotherapeutic agent.
    Type: Application
    Filed: August 10, 2011
    Publication date: September 25, 2014
    Applicants: RNA DIAGNOSTICS INC., LAURENTIAN UNIVERSITY OF SUDBURY
    Inventors: Amadeo Mark Parissenti, Baoqing Guo, Kenneth Pritzker, Laura Pritzker
  • Patent number: 8835482
    Abstract: The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: September 16, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: François Paul Bischoff, Henricus Jacobus Maria Gijsen, Serge Maria Aloysius Pieters, Garrett Berlond Minne
  • Publication number: 20140256619
    Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.
    Type: Application
    Filed: October 18, 2012
    Publication date: September 11, 2014
    Inventors: Anne Lespine, Roger Prichard, Cecile Menez
  • Publication number: 20140255348
    Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 11, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: David Proia
  • Publication number: 20140255502
    Abstract: A pharmaceutical composition is provided. The pharmaceutical composition includes a nanoparticle, a shell and a drug, wherein the nanoparticle has an outer surface and the drug is mixed with the shell and is formed on the outer surface.
    Type: Application
    Filed: September 25, 2013
    Publication date: September 11, 2014
    Applicant: National Chiao Tung University
    Inventors: San-Yuan Chen, Wei-Ming Li
  • Patent number: 8829021
    Abstract: A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: September 9, 2014
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Claudio Pisano, Loredana Vesci, Paolo Carminati
  • Publication number: 20140249203
    Abstract: Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 4, 2014
    Inventors: Mark E. Davis, Han Han
  • Patent number: 8822491
    Abstract: The present invention provides compounds (such as compounds of formula I-a) that induce ? globin expression and pharmaceutical compositions thereof. Such compounds may have beneficial therapeutic effects. Compounds and compositions described herein may be used to treat hemoglobinopathies such as ?-thalassemia and sickle cell anemia.
    Type: Grant
    Filed: January 3, 2012
    Date of Patent: September 2, 2014
    Assignee: Academia Sinica
    Inventors: Che-kun James Shen, Yu-Chi Chou
  • Publication number: 20140242026
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Publication number: 20140234295
    Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.
    Type: Application
    Filed: November 1, 2011
    Publication date: August 21, 2014
    Applicant: MARSHALL EDWARDS, INC.
    Inventors: George Jeoffreys, Alison Johnson, Andrew Heaton, Ofir Moreno
  • Patent number: 8809362
    Abstract: To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. The marker for determining sensitivity to an anti-cancer agent is formed of one or more substances selected from the group consisting of a substance or a fragment thereof detected as an anion at m/z of 149.05 to 149.06, a substance or a fragment thereof detected as an anion at m/z of 152.99 to 153.00, a substance or a fragment thereof detected as a cation at m/z of 724.34 to 724.35, the peaks being determined by means of a mass spectrometer, glycerol 3-phosphate, dihydrobiopterin, GABA, lactic acid, asparagine, aspartic acid, 2-methylbutyroylcarnitine, 1-methyladenosine, and glutathione, and a substance involved in a metabolic pathway of any of these substances.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: August 19, 2014
    Assignees: Keio University, Kabushiki Kaisha Yakult Honsha
    Inventors: Yusuke Tanigawara, Tetsuya Suzuki, Akito Nishimuta, Shinji Sugimoto, Yoshiaki Igarashi
  • Patent number: 8802240
    Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: August 12, 2014
    Assignee: Nanopharmaceuticals LLC
    Inventors: Paul J. Davis, Shaker A. Mousa
  • Patent number: 8802692
    Abstract: This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: August 12, 2014
    Assignee: Exelixis, Inc.
    Inventors: Geetha Shankar, Frauke Bentzien, Peter Lamb, David Matthews
  • Publication number: 20140220112
    Abstract: Sparingly water-soluble agents can be formulated as cyclodextrin complexes, however, these water-soluble drug-cyclodextrin complexes dissociate when the complex is administered into patients. The dilution of the complex in the patient leads to the drug being released from the complex, so the drug is not effectively targeted. In contrast, drugs encapsulated in the aqueous core of a lipid vesicles are not released when the liposome is diluted in blood. This invention describes compositions and methods whereby cyclodextrin or polyanionic beta-cyclodextrin drug-complexes are mixed with a preformed liposome containing the amine salts of an acidic compound. This results in the drug cyclodextrin complex being transferred into the liposome where it is stably retained. The liposome-encapsulated drug can then be injected into a patient.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Inventors: Francis C. SZOKA, JR., Charles O. Noble, Mark E. Hayes
  • Publication number: 20140212480
    Abstract: Described herein are pharmaceutical compositions according to aspects of the present invention which include one or more hydrophilic antineoplastic chemotherapeutics, such as vinca alkyloid antineoplastic chemotherapeutics, encapsulated in ceramide anionic liposomes. Methods of treatment of a subject having cancer using the pharmaceutical compositions are described, along with methods of making ceramide anionic liposomes which encapsulate one or more hydrophilic antineoplastic chemotherapeutics in the aqueous interior of the ceramide anionic liposomes.
    Type: Application
    Filed: April 3, 2014
    Publication date: July 31, 2014
    Applicant: The Penn State Research Foundation
    Inventors: Mark Kester, Sriram S. Shanmugavelandy, Todd Fox
  • Publication number: 20140205595
    Abstract: It is an object of the present invention that the novel nicotinic receptor antagonists disclosed herein may be used in a broad array of clinical or medicinal facets. For example, it is a contemplated use of the present invention that the novel nicotinic receptor antagonists be used to inhibit the growth cycle of non-small cell lung cancer cells. Without being bound by theory, it is an object of the present invention that the nicotinic receptor antagonists disclosed herein are believed to possess reversible binding properties. Moreover, the compounds of the present invention are selective for 0.7 nAChR. For example, the compounds of the present invention are not believed to bind to 0.4 (32 nAChR neuromuscular receptors. It is also contemplated that the nicotinic receptor antagonists of the present invention will be used as a counter measure to treat exposure, or potential exposure, to a wide array of potential neurotoxins.
    Type: Application
    Filed: June 22, 2012
    Publication date: July 24, 2014
    Inventors: Youyi Peng, Lawrence P. Wennogle, Qing Zhang, John Tomesch
  • Publication number: 20140205596
    Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.
    Type: Application
    Filed: June 22, 2012
    Publication date: July 24, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Youyi Peng, John Tomesch, Lawrence P. Wennogle, Qiang Zhang
  • Patent number: 8785470
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: July 22, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • 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
  • Publication number: 20140194458
    Abstract: Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, aryl substituted C1-6 alkyl, phosphate substituted C1-6 alkyl, amino-substituted C1-6 alkyl, carboxyl substituted C1-6 alkyl, hydroxyl substituted C1-6 alkyl, and amide- substituted C1-6 alkyl; R1 is selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and the use thereof in anti-tumor drug preparation.
    Type: Application
    Filed: June 15, 2012
    Publication date: July 10, 2014
    Applicant: Northeast Forestry University
    Inventors: Yang Wang, Xiufeng Yan, Lijia Jing, Weimin Ding, Jian Zheng, Qiuying Pang, Tao Yu
  • Publication number: 20140193519
    Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.
    Type: Application
    Filed: August 2, 2013
    Publication date: July 10, 2014
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: Barbara P. Wallner, Brian Eric Schwartz, Philip B. Komarnitsky, Gerald Bacher, Bernhard Kutscher, Gerhard Raab
  • Publication number: 20140186367
    Abstract: Embodiments of the invention are directed to methods of determining the prognosis of a breast cancer patient by evaluating the activity of the glucocorticoid receptor in tumor cells. Other embodiment include methods of treating breast cancer cells, particularly, chemo-resistant cells, with a glucocorticoid receptor antagonist and an anticancer agent or compound.
    Type: Application
    Filed: February 4, 2014
    Publication date: July 3, 2014
    Applicant: The University of Chicago
    Inventors: Deng PAN, Masha Kocherginsky, Suzanne D. Conzen
  • Patent number: 8765173
    Abstract: A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises poorly water soluble nanoparticles formed by the API together with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: July 1, 2014
    Assignee: Ardenia Investments, Ltd.
    Inventors: Julian Aleksov, Igor Lokot
  • Patent number: 8765432
    Abstract: The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: July 1, 2014
    Assignee: Oligasis, LLC
    Inventors: Stephen A. Charles, D. Victor Perlroth
  • Publication number: 20140178354
    Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: The Regents of the University of California
    Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
  • Patent number: 8758830
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: June 24, 2014
    Assignee: Array BioPharma, Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Patent number: 8759375
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: June 24, 2014
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Patent number: 8754121
    Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: June 17, 2014
    Assignee: Academia Sinica
    Inventors: Lie-Fen Shyur, Wen-Wan Chao, Ya-Wen Cheng
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Publication number: 20140162969
    Abstract: There is provided a new use of microspheres comprising a water-insoluble, water-swellable polymer which is anionically charged at pH7, and electrostatically associated with the polymer, in releasable form, a cationically charged chemotherapeutic agent, in the manufacture of a composition for use in the treatment of a brain tumour, wherein in the treatment the composition is introduced into the brain and the chemotherapeutic agent is released from the microspheres, wherein the microspheres, when equilibrated in water at 37° C., comprise at least 40 wt % water based on weight of polymer plus water. Compositions comprising the microspheres and methods for the treatment of brain tumours are also provided.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicant: BIOCOMPATIBLES UK LIMITED
    Inventors: Andrew Lennard LEWIS, Yiqing TANG, Peter William STRATFORD
  • Publication number: 20140162996
    Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
    Type: Application
    Filed: July 29, 2013
    Publication date: June 12, 2014
    Applicant: CITY OF HOPE
    Inventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
  • Patent number: 8747891
    Abstract: Described herein are pharmaceutical compositions according to aspects of the present invention which include one or more hydrophilic antineoplastic chemotherapeutics, such as vinca alkyloid antineoplastic chemotherapeutics, encapsulated in ceramide anionic liposomes. Methods of treatment of a subject having cancer using the pharmaceutical compositions are described, along with methods of making ceramide anionic liposomes which encapsulate one or more hydrophilic antineoplastic chemotherapeutics in the aqueous interior of the ceramide anionic liposomes.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: June 10, 2014
    Assignee: The Penn State Research Foundation
    Inventors: Mark Kester, Sriram S. Shanmugavelandy, Todd Fox
  • Patent number: 8748449
    Abstract: Polyols stabilize polymorphous form of rifaximin, in particular the ? form. When polyols having at least two hydroxy groups are added to rifaximin powder, polymorph ? is stable and remains stable in time independently from the environment humidity. In this invention a method to prepare formulations constituted by pure and stable polymorphous forms able to give a pharmaceutical product is described.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: June 10, 2014
    Assignee: Alfa Wassermann S.p.A.
    Inventors: Paola Maffei, Milena Bachetti, Giuseppe Bottoni, Giuseppe Claudio Viscomi
  • Patent number: 8735394
    Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents (such as an anti-VEGF antibody), or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: May 27, 2014
    Assignee: Abraxis BioScience, LLC
    Inventors: Neil P. Desai, Patrick Soon-Shiong
  • Publication number: 20140140931
    Abstract: This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and anti-oxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and/or drugs.
    Type: Application
    Filed: July 27, 2012
    Publication date: May 22, 2014
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: John S. Yu, Bong Seop Lee