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)
  • Patent number: 11090299
    Abstract: An oral solid formulation includes irinotecan or a pharmaceutically acceptable salt thereof as an active ingredient, and an acidifying agent.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: August 17, 2021
    Assignee: HANMI PHARM. CO., LTD.
    Inventors: Caleb Hyung Min Park, Myeong Ki Jung, Jin Cheul Kim, Yong Il Kim, Jae Hyun Park, Jong Soo Woo
  • Patent number: 11058679
    Abstract: The present invention relates to a dosage form comprising an aqueous solution of a vinca alkaloid drug or its pharmaceutically acceptable salt in a flexible infusion container, and a light protective secondary packaging containing the flexible infusion container, wherein the dosage form is ready-to-infuse and wherein the aqueous solution is stable at room temperature.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: July 13, 2021
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: Subhas Balaram Bhowmick, Prashant Kane, Samarth Kumar, Ramaji Karshanbhai Varu, Nisarg Bipinchandra Mistry, Swapnil Ramesh Patil
  • Patent number: 10980796
    Abstract: The present invention relates to a drug delivery system having a double core-shell structure and, specifically, to a double nano-drug delivery system having an inner core-shell containing a poorly soluble camptothecin compound and a water-soluble camptothecin compound inside and an amphiphilic polymer shell, and to a manufacturing method therefor. The double core-shell structured particles manufactured by the present invention form very stable particles and show a mono-distribution of particles before and after freeze-drying. The particles of the present invention show excellent results compared with existing monolayer micelles in animal efficacy tests and pharmacokinetic tests, and do not use a surfactant causing hypersensitivity, and thus the use of the particles of the present invention can provide a pharmaceutical composition or a drug delivery system platform, which are safe for the human body.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: April 20, 2021
    Assignee: SN BIOSCIENCE INC.
    Inventors: Young Hwan Park, Il Hyun Lee
  • Patent number: 10976319
    Abstract: A cell response assay for cancer is provided. In the assay, the levels of a cancer cell type biomarker, a chemo resistance biomarker and a metastatic potential biomarker are simultaneously measured in a biological sample.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: April 13, 2021
    Assignee: Siemens Healthcare Diagnostics Inc.
    Inventor: Michael Pugia
  • Patent number: 10857147
    Abstract: The present invention provides SN-38 compositions for treating cancer.
    Type: Grant
    Filed: November 19, 2018
    Date of Patent: December 8, 2020
    Assignee: Intezyne Technologies, Inc.
    Inventors: Kevin N. Sill, Adam Carie
  • Patent number: 10799495
    Abstract: A benzodiazepine alkaloid compound and a pharmaceutically acceptable salt thereof, the structure of the compound being shown in general formula (I). in the formula (I), R1, R2 and R3 independently are hydrogen, C1-4 alkyl or C1-4 alkanoyl; one from among R4 and R5 is a benzene ring or a substituted benzene ring, while the other is hydrogen, a benzene ring or a substituted benzene ring, wherein a substituent group on the substituted benzene ring is hydroxyl, cyano, amino, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylamine, C1-4 alkanoyl or C1-4 alkoxyacyl. A method for synthesizing the compound and a use in the preparation of anti-tumor drugs. The compound shown in formula (I) may be used for preparing anti-tumor, especially anti-lung cancer, drugs as well as anti-fungal drugs.
    Type: Grant
    Filed: July 28, 2017
    Date of Patent: October 13, 2020
    Assignee: RENJI HOSPITAL, SHANGHAI JIAO TONG UNIVERSITY SCHOOL OF MEDICINE
    Inventors: Houwen Lin, Fan Yang
  • Patent number: 10739333
    Abstract: In various aspects the invention provides methods of predicting sensitivity of a cancer cell to a therapeutic agent by contacting a test cell population BH3 domain peptide; measuring the amount of BH3 domain peptide induced mitochondrial outer membrane permeabilization in the test cell population; and comparing the amount of BH3 domain peptide induced mitochondrial outer membrane permeabilization in the test cell population to a control cell population that has not been contacted with the therapeutic agent. An increase in mitochondrial membrane permeabilization in the test cell population compared to the control cell population indicates the cell is sensitive to the therapeutic agent.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: August 11, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Jeremy Ryan, Anthony Letai
  • Patent number: 10722463
    Abstract: A method of delivering a pharmaceutical agent into a target organ protected by a blood barrier is provided. The method comprising administering to a subject in need thereof an amount of liposomes which comprise the pharmaceutical agent, the amount and the liposomes are selected such that the liposomes accumulate in cells of an immune system of the subject to thereby generate liposome loaded immune cells, the liposome loaded immune cells become activated and cross the blood barrier, and an effective amount of the pharmaceutical agent is released from the liposomes in the target organ of the subject.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: July 28, 2020
    Assignee: Zuli Holdings Ltd.
    Inventors: Gershon Golomb, Hila Epstein, Eyal Afergan
  • Patent number: 10689381
    Abstract: A vinca alkaloid compound substituted at the 20?-position with a carboxamido group is disclosed. The carbonyl of the carboxamido group is bonded to a 20?-amino group and to a ring system that contains up to three 5-, 6- or 7-membered rings that are fused or otherwise bonded together. Each ring can be carbocyclic or heterocyclic, with a heterocyclic ring containing up to three hetero ring atoms that are the same or different and are selected from nitrogen, oxygen and sulfur. The ring system can include up to four substituent groups other than hydrogen that are discussed within. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using d compound. A particularly preferred compound has an activity in specified cancer cell growth inhibition assays that is the same or better than its parental, unsubstituted vinca compound and is not subject to Pgp-mediated efflux.
    Type: Grant
    Filed: August 1, 2018
    Date of Patent: June 23, 2020
    Assignee: The Scripps Research Institute
    Inventor: Dale Boger
  • Patent number: 10172943
    Abstract: Provided is an irinotecan-loaded dual-reverse thermosensitive formulation, which is a dual-reverse thermosensitive hydrogel composition including nanoparticles including irinotecan and lipids; a hydrogel; and a stabilizer.
    Type: Grant
    Filed: January 21, 2016
    Date of Patent: January 8, 2019
    Assignee: INDUSTRY—UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY ERICA CAMPUS
    Inventors: Han-Gon Choi, Fakhar Ud Din, Dong Wuk Kim, Dong Shik Kim, Chul Soon Yong, Jong Oh Kim, Yu-Kyoung Oh
  • Patent number: 10172581
    Abstract: The present invention provides method of assessing tumor growth.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: January 8, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Mizuki Nishino, Bruce E. Johnson, Hiroto Hatabu, Suzanne E. Dahlberg
  • Patent number: 10155757
    Abstract: The invention relates to novel co-crystals of a drug substance and their use to treat respiratory diseases such as asthma and COPD.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: December 18, 2018
    Assignee: Vectura Limited
    Inventor: Joanne Holland
  • Patent number: 10143689
    Abstract: The present invention provides SN-38 compositions for treating cancer.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: December 4, 2018
    Assignee: Interzyne Technologies, Inc.
    Inventors: Kevin N. Sill, Adam Carie
  • Patent number: 10098813
    Abstract: The present invention relates to a method for enabling hospitals or clinics to administer a dose of a drug to patients in need thereof while avoiding steps of manipulation, dilution, reconstitution, dispensing, sterilization, transfer, handling or compounding before intravenous administration. The present invention further relates to a perfusion system comprising different sets of perfusion containers, each container comprising a ready-to-infuse, stable, sterile, aqueous perfusion solution of a drug, wherein the set of perfusion containers alone or in combination provides for direct intravenous administration of a desired dose of the drug to a patient in need thereof, such that the delivered dose is equal to or within ±5% of the calculated dose.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: October 16, 2018
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITED
    Inventors: Samarth Kumar, Prashant Kane, Balaram Subhas Bhowmick, Kirti Ganorkar, Nishit Patel, Anilrao Ashish Dubewar, Mukeshbhai Umeshkumar Patel
  • Patent number: 10052392
    Abstract: Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: August 21, 2018
    Assignee: JENKEM TECHNOLOGY CO., LTD. (TIANJIN)
    Inventors: Lihua Xu, Xuan Zhao, Zewang Feng, Jinliang Wang, Zhen'guo Wang
  • Patent number: 10052391
    Abstract: Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: August 21, 2018
    Assignee: JENKEM TECHNOLOGY CO., LTD. (TIANJIN)
    Inventors: Lihua Xu, Xuan Zhao, Zewang Feng, Jinliang Wang, Zhen'guo Wang
  • Patent number: 10034948
    Abstract: Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: July 31, 2018
    Assignee: JENKEM TECHNOLOGY CO., LTD.
    Inventors: Lihua Xu, Xuan Zhao, Zewang Feng, Jinliang Wang, Zhen'guo Wang
  • Patent number: 9962452
    Abstract: The present invention provides novel, non-covalently bound complexes of serum albumin and analogs of poorly soluble drugs, such as camptothecin. The novel complexes are significantly more water-soluble than the camptothecin analogs and are useful as prodrug forms of the camptothecin analogs for the treatment of mammalian cell proliferative diseases, such as cancer.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: May 8, 2018
    Assignee: Zhuhai Beihai Biotech Co., Ltd.
    Inventor: Qun Sun
  • Patent number: 9943609
    Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: April 17, 2018
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Aleksandr V. Yurkovetskiy, Mao Yin, Timothy B. Lowinger, Joshua D. Thomas, Charles E. Hammond, Cheri A. Stevenson, Natalya D. Bodyak, Patrick R. Conlon, Dimitry R. Gumerov
  • Patent number: 9919027
    Abstract: A lipid nanoparticle that includes at least one antibiotic from the polymyxin family, a lipid fraction, and one or more surfactants. The lipid nanoparticle is useful in the prevention and/or treatment of respiratory tree infections.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: March 20, 2018
    Assignees: Biopraxis Research Aie, Praxis Pharmaceutical, S.A., Fundacio D'Investigacio Sanitaria De Les Illes Balears, Universidad Del Pais Vasco/Euskal Herriko Unibertsitatea, Universidad De Barcelona, Consejo Superior De Investigaciones Cientificas
    Inventors: Eusebio Gainza Lafuente, Angel Del Pozo Perez, Garazi Gainza Lucea, Oihane Ibarrola Moreno, Silvia Villullas Rincon, Raul Fernandez Plagaro, Daniel Bachiller Perez, Jose Luis Pedraz Munoz, Amaya Esquisabel Alegria, Marta Pastor Navarro, Ester Fuste Dominguez, Eulalia Sans Serramit Jana, Iraida Gil Martin
  • Patent number: 9808430
    Abstract: The present invention relates to compositions and methods comprising resveratrol and uses thereof. Some embodiments include compositions and methods with increased bioavailability of resveratrol. Certain embodiments include compositions comprising resveratrol and a solubilizer. Particular embodiments include transmucosal delivery of resveratrol from the composition.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: November 7, 2017
    Assignee: WILMORE LABS LLC
    Inventor: Otis L. Blanchard
  • Patent number: 9789198
    Abstract: Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: October 17, 2017
    Assignee: JENKEM TECHNOLOGY CO., LTD. (TIANJIN)
    Inventors: Lihua Xu, Xuan Zhao, Zewang Feng, Jinliang Wang, Zhenguo Wang
  • Patent number: 9782401
    Abstract: A method of isolating at least one phenanthroindolizidine alkaloid, in particular with HIF-1 inhibitory activity, from Tylophora atrofolliculata is used to isolate and obtain for example about 22 phenanthroindolizidine alkaloids, including at least 11 new phenanthroindolizidine alkaloids which have not been previously isolated. Experimental tests confirmed an exceptional HIF-1 inhibitory activity of the phenanthroindolizidine alkaloids isolated. A pharmaceutical composition includes at least one phenanthroindolizidine alkaloid and at least one pharmaceutical tolerable excipient. A method of treating a subject suffering from cancer includes administering at least one phenanthroindolizidine alkaloid isolated from Tylophora atrofolliculata. A method of treating a subject suffering from cancer includes administering at least one phenanthroindolizidine alkaloid to the subject.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: October 10, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Zhi-Hong Jiang, Jing-Rong Wang, Cheng-Yu Chen, Guo-Yuan Zhu
  • Patent number: 9733256
    Abstract: To provide an anti-cancer agent sensitivity determination marker, which marker can determine whether or not the patient has a therapeutic response to the anti-cancer agent, and novel cancer therapeutic means employing the marker. The anti-cancer agent sensitivity determination marker, the anti-cancer agent including oxaliplatin or a salt thereof and fluorouracil or a salt thereof, contains one or more substances selected from among an amino-acid-metabolism-related substance, a nucleic-acid-metabolism-related substance, a substance in the pentose phosphate pathway, a substance in the glycolytic pathway, a substance in the TCA cycle, a polyamine-metabolism-related substance, 7,8-dihydrobiopterin, 6-phosphogluconic acid, butyric acid, triethanolamine, 1-methylnicotinamide, NADH, NAD+, and a substance involved in the metabolism of any of these substances.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: August 15, 2017
    Assignees: KEIO UNIVERSITY, KABUSHIKI KAISHA YAKULT HONSHA
    Inventors: Yusuke Tanigawara, Akito Nishimuta, Junya Tsuzaki, Hiroyuki Takahashi
  • Patent number: 9694073
    Abstract: The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: July 4, 2017
    Assignees: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA, ALBERTA HEALTH SERVICES
    Inventors: Michael Weinfeld, Dennis G. Hall, Feridoun Karimi-Busheri, Gary Kenneth Freschauf, Todd Randall Mereniuk
  • Patent number: 9675609
    Abstract: A pharmaceutical composition is provided having particles of a physical mixture that contain at least one 20-camptothecin or a derivative thereof, at least one surfactant, at least one stabilizer, and at least one diluent. The particles have a mean particle size of less than about 2500 nm. The pharmaceutical composition can be nano- or micro-sized particles containing the 20-camptothecin esters or derivatives thereof as part of a physical mixture, which can provide the active compound in a water-soluble/dispersible, bioavailable form. The particles can be used as an oral pharmaceutical composition which comprises the nano- or micro-sized form of 20-camptothecin esters or derivatives, such as in an oral suspension (e.g., an aqueous suspension), or capsules, or caplets. The pharmaceutical composition can be used in the treatment of a cancer or malignant tumor in a patient by oral administration thereof in a therapeutically effective amount.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: June 13, 2017
    Assignee: Cao Pharmaceuticals Inc.
    Inventors: Wenhao Chen, Jiyao Zhang, Zhisong Cao
  • Patent number: 9643975
    Abstract: A method for preparing 9-allylcamptothecin derivatives using compound 14 as an essential intermediate. The total yield of the method is high.
    Type: Grant
    Filed: December 31, 2014
    Date of Patent: May 9, 2017
    Assignee: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD
    Inventors: Lei Jiang, Lei Liu, Lei Li
  • Patent number: 9636351
    Abstract: This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: May 2, 2017
    Assignee: Pop Test Oncology Limited Liability Company
    Inventors: Randice Lisa Altschul, Neil David Theise, Myron Rapkin, Rebecca O'Brien
  • Patent number: 9561219
    Abstract: The present invention discloses a method of treating cancer comprising administering an effective amount of an alkaloid, in which the alkaloid is liensinine, isoliensinine, dauricine, cepharanthine, hernandezine or thalidezine and isolated from the traditional Chinese medicinal herbs. The use of the alkaloid in treating neurodegenerative disorder is also disclosed.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: February 7, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Kam Wai Wong, Yuen Kwan Law, Liang Liu, Jingrong Wang
  • Patent number: 9556192
    Abstract: The present disclosure is directed to a compound of formula (I) wherein L is null or a conditionally-cleavable moiety; W is null or a self-immolative system, comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid —peptidic and non peptidic—linker; RM is null or a reactive moiety that can be attached to one or more of L, W or Z groups, or RM is attached to oxygen when L, W and Z are all null; provided that at least one of L, W, Z and RM is not null; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: January 31, 2017
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Matteo Salsa, Daniela Faiardi
  • Patent number: 9498469
    Abstract: Compositions and methods are provided that enhance cognition in a human to which the composition is orally administered. Remarkably, clinical studies have proven that contemplated compositions achieved the desired effects using a minimal number of active ingredients at or near threshold active dosages, wherein such compositions almost exclusively comprise huperzine A, vinpocetine or rhodiola, and acetyl-L-carnitine, and optionally further include alpha lipoic acid, rhodiola, and biotin.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: November 22, 2016
    Assignee: KeyView Labs, Inc.
    Inventor: Josh Reynolds
  • Patent number: 9493766
    Abstract: The present disclosure relates to buffers containing polyols for use with affinity-binding and/or magnetically susceptible thermoplastic particles and methods of making and use thereof.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: November 15, 2016
    Assignee: Corning Incorporated
    Inventors: Jinlin Peng, Thomas Mark Leslie
  • Patent number: 9387257
    Abstract: A conjugate is disclosed. The conjugate comprises (a) an isolated or a synthetic targeting peptide of less than 15 amino acid residues in length, comprising an amino acid sequence having at least 90% identity to a sequence selected from the group consisting of SEQ ID NOs: 1-8; and (b) a component conjugated to the targeting peptide, the component being selected from the group consisting of a drug delivery vehicle, an anti-cancer drug, a micelle, a nanoparticle, a liposome, a polymer, a lipid, an oligonucleotide, a peptide, a polypeptide, a protein, a cell, an imaging agent, and a labeling agent. Methods of treating lung cancer and detecting lung cancer cells are also disclosed.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: July 12, 2016
    Assignee: ACADEMIA SINICA
    Inventors: Han-Chung Wu, Yi-Hsuan Chi
  • Patent number: 9342657
    Abstract: Methods, systems, and computer program products that predict an individual's treatment outcome from a sampling of a group of patients' biological profiles. Biological profile information is received from patients who had a medical condition and who received a treatment. Treatment outcome information regarding the patients who had the medical condition and who received the treatment is also received. A discriminant analysis-based pattern recognition process is then performed on the biological profile information and the treatment outcome information, thereby generating a model that correlates between the biological profile information and the treatment outcome information. The model can be used for, among other things, predicting treatment outcome for the new patient for the treatment.
    Type: Grant
    Filed: March 24, 2003
    Date of Patent: May 17, 2016
    Inventor: Nien-Chih Wei
  • Patent number: 9333256
    Abstract: The present invention provides compositions and methods useful for promoting or reducing T-cell trafficking to a target tissue. Also provided are compositions and methods useful for promoting or inhibiting antigen-presenting cell (APC) activation. The invention is related to discovery of functional characteristics of TIM-3, a molecule that is preferentially expressed on the surface of Th1 cells. The methods are useful for treating disorders including cancer, infectious disease, allergy, asthma, and autoimmune disease.
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: May 10, 2016
    Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute
    Inventors: Vijay K. Kuchroo, Laurent Monney, Jason L. Gaglia, Edward A. Greenfield, Gordon J. Freeman, Hanspeter Waldner
  • Patent number: 9266911
    Abstract: The present invention relates to a camptothecin derivative having a structure as represented by Formula (II), in which Xn+ is selected from H+, K+, Na+, Li+, Mg2+, Ca2+, Zn2+, Fe3+, and ammonium ion, while R1, R2, R3, and R4 independently represent a hydrogen, a hydroxyl group, a nitro group, a cyano group, a halogen, a carboxyl group, an optionally substituted amino group, a silicon-containing group, a monocyclic aryloxy group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkylcarbonyl group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C3-C6 cycloalkyl group; alternatively, R1 and R2 are connected via one to three other atoms to form a heterocyclic ring; and in another embodiment, R3 and R4 are oxygen atoms and connected via —O—(CH2)n—O—, forming a ring, in which n=I or 2. The compound has great water-solubility, chemical stability, and great efficacy in treatment on cancer.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: February 23, 2016
    Inventors: Wenqiang Zhou, Jing Deng
  • Patent number: 9254339
    Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: February 9, 2016
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Aleksandr Yurkovetskiy, Mao Yin, Timothy B. Lowinger, Joshua D. Thomas, Charles E. Hammond, Cheri A. Stevenson, Natalya D. Bodyak, Patrick R. Conlon, Dmitry R. Gumerov
  • Patent number: 9226969
    Abstract: Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: January 5, 2016
    Assignee: Nektar Therapeutics
    Inventors: Anthony O. Chong, Seoju Lee, Bhalchandra V. Joshi, Brian Bray, Shaoyong Nie, Patrick L. Spence, Antoni Kozlowski, Samuel P. McManus, Sachin Tipnis, David Swallow, John R. Handley, Anthony G. Schaefer
  • Patent number: 9220714
    Abstract: The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: December 29, 2015
    Assignees: Brown University, Women and Infants' Hospital Rhode Island
    Inventors: Giselle L. Saulnier Sholler, Narasimha Swamy, Stayan Kalkunte, Rakesh K. Singh, Laurent Brard, Kyu Kwang Kim
  • Patent number: 9211258
    Abstract: A stable, taste-masked, ready-to-use suspension comprising rifaximin dispersed in a suspension base and one or more pharmaceutically acceptable additive(s). Also provided is a process for preparing a stable, taste-masked, ready-to-use suspension of rifaximin comprising the steps of mixing rifaximin with the suspension base and further sizing the particles of rifaximin by milling the suspension to obtain a homogenously dispersed rifaximin suspension.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: December 15, 2015
    Assignee: LUPIN LIMITED
    Inventors: Harshal Anil Jahagirdar, Kishore Kumar Konda, Satish Kumar Dalal, Shirishkumar Kulkarni
  • Patent number: 9206192
    Abstract: Disclosed is a trolox derivative-modified fat-soluble anti-cancer pharmaceutical compound having a structure as represented by formula I or II. An active moiety of the anti-cancer pharmaceutical compound, camptothecin or a camptothecin derivative, is covalently bonded to a lipophilic moiety, a trolox ester or a trolox amide, by a linking group to form the fat-soluble anti-cancer pharmaceutical compound. Also disclosed are a preparation, preparing method and use of the pharmaceutical compound.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 8, 2015
    Assignee: Jiangsu Chiatei Tianqing Pharmaceutical Co., LTd
    Inventor: Yuehua Zhang
  • Patent number: 9173938
    Abstract: The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol. Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: November 3, 2015
    Assignee: Cyclacel Limited
    Inventors: Simon Green, Sheelagh Frame, Ian Fleming
  • Patent number: 9173842
    Abstract: Stable pharmaceutical composition consisting of a hydrosoluble vinflunine salt and at least one diluent and one lubricant, said composition being in the form of a solid intended for oral administration. The hydrosoluble vinflunine salt is preferably Vinflunine ditartrate. The pharmaceutical composition is advantageously in the form of a capsule or tablet. The invention also concerns a method of treating cancer pathology comprising the oral administration of the pharmaceutical composition of the invention.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: November 3, 2015
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Bruno Paillard, Jean-Louis Avan, Joël Bougaret
  • Patent number: 9150585
    Abstract: The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell proliferative diseases, such as cancer.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: October 6, 2015
    Assignee: FL Therapeutics LLC
    Inventor: Qun Sun
  • Patent number: 9144615
    Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ?5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
    Type: Grant
    Filed: August 12, 2014
    Date of Patent: September 29, 2015
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Aleksandr Yurkovetskiy, Mao Yin, Timothy B. Lowinger, Joshua D. Thomas, Charles E. Hammond, Cheri A. Stevenson, Natalya D. Bodyak, Patrick R. Conlon, Dmitry R. Gumerov
  • Patent number: 9125858
    Abstract: The present invention relates to compositions and methods comprising resveratrol and uses thereof. Some embodiments include compositions and methods with increased bioavailability of resveratrol. Certain embodiments include compositions comprising resveratrol and a solubilizer. Particular embodiments include transmucosal delivery of resveratrol from the composition.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: September 8, 2015
    Assignee: WILMORE LABS L.L.C.
    Inventors: Otis L. Blanchard, Tina C. Blanchard
  • Patent number: 9115406
    Abstract: There is described herein compounds, compositions and methods for inducing synthetic lethality in a cancer cell(s).
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: August 25, 2015
    Assignees: THE GOVENORS OF THE UNIVERSITY OF ALBERTA, ALBERTA HEALTH SERVICES
    Inventors: Michael Weinfeld, Todd Randall Mereniuk, Edan Foley, Dennis G. Hall
  • Patent number: 9095565
    Abstract: Methods of treating blood disorders are described.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: August 4, 2015
    Assignee: Phoenicia Biosciences, Inc.
    Inventor: Susan P. Perrine
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150148369
    Abstract: The current application relates to the use of a compound selected from the group consisting of camptothecin and its analog, 10-hydroxy camptothecin, topotecan, irinotecan, 18-beta-glycyrrhetinic acid and its analog, carbinoxolone, etoposide, topoisomerase inhibitors, and combinations thereof, for the treatment of a synucleinopathy disease or disorder such as Parkinson's disease.
    Type: Application
    Filed: May 31, 2013
    Publication date: May 28, 2015
    Applicant: OXALYS PHARMACEUTICALS
    Inventors: Katharine Julia Sepp, Joost Schulte