Three Or More Ring Hetero Atoms In The Pentacyclo Ring System Patents (Class 546/48)
  • Patent number: 10301303
    Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: May 28, 2019
    Assignee: Shenzhen HighTide Biopharmaceutical, Ltd.
    Inventor: Liping Liu
  • Patent number: 10265409
    Abstract: A macromolecule includes i) a dendrimer with a core and at least one generation of lysine residue building units, the outermost generation of building units having surface amino groups, ii) a first terminal group covalently attached to a first surface amino group of a building unit, which includes a residue of docetaxel (DTX), and iii) a second terminal group covalently attached to a second surface amino group of a building unit, which includes a pharmacokinetic modifying agent. The pharmacokinetic modifying agent can be a polyethylene glycol (PEG). The first terminal group can be covalently attached to the surface amino group of the dendrimer through a diacid linker. The diacid linker can include a 2,2?-thiodiacetic acid residue. The diacid linker can form an ester bond with a hydroxyl group of the DTX and an amide bond with the surface amino group. A pharmaceutically acceptable salt of the macromolecule can be prepared.
    Type: Grant
    Filed: August 28, 2017
    Date of Patent: April 23, 2019
    Assignee: STARPHARMA PTY LTD
    Inventors: David Owen, Brian Devlin Kelly, Peter Karellas
  • Patent number: 9504755
    Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: November 29, 2016
    Assignee: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Samuel P. McManus, Jennifer Riggs-Sauthier, Xiaoming Shen, Wen Zhang
  • Patent number: 9067879
    Abstract: Improved processes are described for making trialkyl esters and acylated trialkyl esters of carboxylic acids, as well as epoxidized trialkyl esters and acylated trialkyl carboxylate esters, such as are used in developing plasticized PVC compositions. In particular, processes are described for conducting the esterification and acylation steps involved in making the acylated trialkyl esters in a single vessel without an intermediate purification step, by means of a Lewis acid metal triflate catalyst.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: June 30, 2015
    Assignee: Archer Daniels Midland Company
    Inventor: Stephen Howard
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Patent number: 9035042
    Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: May 19, 2015
    Assignee: ATTO-TEC GmbH
    Inventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
  • Patent number: 9034894
    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: Grant
    Filed: June 15, 2012
    Date of Patent: May 19, 2015
    Assignee: NORTHEAST FORESTRY UNIVERSITY
    Inventors: Yang Wang, Xiufeng Yan, Lijia Jing, Weimin Ding, Jian Zheng, Qiuying Pang, Tao Yu
  • Publication number: 20150133445
    Abstract: The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Mark S. CUSHMAN, Trung X. Nguyen, Martin M. Conda-Sheridan, Yves George Pommier
  • Publication number: 20150119415
    Abstract: A method and a composition for improving gut micro biota structure, selectively increase a first gut microbiota population while simultaneously decrease a second gut micro biota population in a subject. The first gut micro biota population includes a short-chain fatty acid (SCFA)-producing bacterium and the second gut microbiota population includes an endotoxin-producing bacterium.
    Type: Application
    Filed: June 4, 2013
    Publication date: April 30, 2015
    Inventors: Liping Zhao, Xu Zhang, Menghui Zhang, Yufeng Zhao, Xiaoyan Pang, Xiaojun Zhang, Linghua Wang, Guang Ning, Xiaoying Li, Yifei Zhang
  • Publication number: 20150119388
    Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 30, 2015
    Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIA
    Inventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
  • Patent number: 9018226
    Abstract: The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic-D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10-demethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and ?-yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: April 28, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Santosh Kumar Srivastava, Ashok Kumar Agrawal, Subhash Chandra Singh, Vinay Kumar Khanna, Janardan Singh, Chandeshwar Nath, Madan Mohan Gupta, Shikha Gupta, Ram Kishor Verma, Anirban Pal, Dnyaneshwar Umrao Bawankule, Dharmendra Saikia, Anil Kumar Gupta, Anupam Maurya, Suman Preet Singh Khanuja
  • Patent number: 9006439
    Abstract: Disclosed are novel camptothecin derivatives having anti-tumor activity (the basic structure thereof is as shown in the figure) and compositions of such compounds and use thereof. The compounds according to the present invention exhibit very good water solubility and stability, show good selectivity among drugs of the same category, and have a very high therapeutic index. Such compounds are promising as therapeutic agents for treating tumors.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: April 14, 2015
    Assignee: Ningbo Team Pharmaceutical Co., Ltd
    Inventors: Xiaoguang Lei, Xiuguo Zhang
  • Patent number: 9006437
    Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: April 14, 2015
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Publication number: 20150031717
    Abstract: Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same.
    Type: Application
    Filed: October 24, 2012
    Publication date: January 29, 2015
    Applicant: Institute of Materia Medica, Chinese Academy of Medical Sciences
    Inventors: Hailin Qin, Wenjie Wang, Zhihui Zhang, Lianqiu Wu, Anjun Deng, Jinqian Yu, Zhihong Li
  • Publication number: 20150031644
    Abstract: The invention provides novel amphiphilic drug-drug conjugates useful as cancer therapeutics, and compositions and methods thereof.
    Type: Application
    Filed: March 11, 2014
    Publication date: January 29, 2015
    Inventors: Deyue Yan, Ping Huang, Xinyuan Zhu, Wei Huang, Yongfeng Zhou
  • Patent number: 8940338
    Abstract: Formulations containing sanguinarine or chelerythrine or the salts thereof or extracts containing them in admixture with suitable carriers and/or excipients for the treatment and/or prevention of mucositis.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: January 27, 2015
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana
  • Patent number: 8937180
    Abstract: Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to a taxane. The method involves, among other things, a step of reacting a taxane with a polyethylene glycol polymer comprising a functional group reactive with a functional group within said taxane in the presence of a coupling reagent and DPTS. The result of the reacting step is the formation of a polyethylene glycol-taxane conjugate.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: January 20, 2015
    Assignee: Nektar Therapeutics
    Inventor: Wen Zhang
  • Publication number: 20140371258
    Abstract: Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 18, 2014
    Applicant: Nektar Therapeutics
    Inventors: Xuyuan Gu, Jennifer Riggs-Sauthier, Michael D. Bentley, Tacey X. Viegas
  • Patent number: 8901139
    Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Srikanth Venkatraman, Anilkumar Gopinadhan Nair, Kevin X. Chen, Francisco Velazquez, Qingbei Zeng, Duan Liu, Yueheng Jiang, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Stephen J. Gavalas, Patrick A. Pinto, Oleg B. Selyutin, Bancha Vibulbhan
  • Patent number: 8900722
    Abstract: The invention provides an OLED device containing certain alkali metal cluster compounds with mixed ligands, such compounds, and methods of making them. In particular, the cluster compound is a neutrally charged mixed cluster compound comprising first and second subunits with the first subunit comprising an alkali metal salt of a nitrogen containing a heterocyclic ligand bearing a anionic hydroxy group and the second subunit consisting of an organic alkali metal salt different than the first subunit.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: December 2, 2014
    Assignee: Global OLED Technology LLC
    Inventors: William J. Begley, Manju Rajeswaran, Tukaram K. Hatwar, Natasha Andrievsky
  • Publication number: 20140343088
    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: Application
    Filed: October 18, 2012
    Publication date: November 20, 2014
    Applicant: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventor: Yuehua Zhang
  • 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: 8865130
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20140308234
    Abstract: Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as cisplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
    Type: Application
    Filed: April 9, 2014
    Publication date: October 16, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: Jeremiah A. Johnson, Longyan Liao
  • 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: 20140255920
    Abstract: The present invention relates to new rhodamine compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.
    Type: Application
    Filed: May 2, 2014
    Publication date: September 11, 2014
    Applicant: ILLUMINA CAMBRIDGE LIMITED
    Inventors: Nikolai Nikolaevich Romanov, Xiaohai Liu
  • Publication number: 20140243512
    Abstract: In a first embodiment the present invention relates to a sorbent comprising a porous inorganic solid support material having on its surface a film of a crosslinked polyvinylamine comprising derivatized amine groups and amine groups binding to the surface of the support material via electron donor/acceptor interactions. In a second embodiment 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 sorbents according to the invention for the purification of organic molecules, in particular pharmaceutical active compounds, preferably in chromatographic applications.
    Type: Application
    Filed: September 17, 2012
    Publication date: August 28, 2014
    Applicant: INSTRACTION GMBH
    Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
  • 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
  • Publication number: 20140227180
    Abstract: The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6 or less, most preferably 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 14, 2014
    Applicant: Immunomedics, Inc.
    Inventors: Serengulam V. Govindan, Jonathan B. Gale, Nicholas J. Holman, David M. Goldenberg
  • Patent number: 8785637
    Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: July 22, 2014
    Assignee: Atto-Tec GmbH
    Inventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
  • Publication number: 20140200226
    Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.
    Type: Application
    Filed: December 12, 2013
    Publication date: July 17, 2014
    Applicants: Florida Atlantic University, University of Central Florida Research Foundation, Inc.
    Inventors: Debopam Chakrabarti, Amy Wright
  • Patent number: 8779138
    Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: July 15, 2014
    Assignees: Sutter West Bay Hospital, Catholic Healthcare West
    Inventor: Li-Xi Yang
  • 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
  • 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: 20140174537
    Abstract: The present invention relates to new naphthalene carbodiimide (NTCDI) derivatives, and organic electronic device using the same and especially to an organic solar cell. The new NTCDI derivatives are used as acceptor, electron transport material, and doped electron transport materials.
    Type: Application
    Filed: June 7, 2012
    Publication date: June 26, 2014
    Applicant: Novaled AG
    Inventor: Omrane Fadhel
  • 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
  • Patent number: 8754190
    Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: June 17, 2014
    Assignee: Prolynx LLC
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8748014
    Abstract: The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2); and an organic electroluminescent device having a pair of electrodes and at least one organic layer interposed therebetween, in which the compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2), is used as a constituent material of the aforementioned at least one organic layer.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: June 10, 2014
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Norimasa Yokoyama, Shuichi Hayashi, Kouki Kase, Hiroshi Ohkuma, Eiji Takahashi, Daizou Kanda
  • Publication number: 20140155577
    Abstract: Disclosed are conjugates of hydrophobic drugs linked to protected or unprotected amino acids or peptides. The disclosed conjugates are amphiphilic and can self assemble into nanotubes. Nanotubes comprising the conjugates are also described and can have high loading of the drug and protect it from degradation or elimination. The nanotubes are well suited to deliver hydrophobic and unstable drugs to individuals.
    Type: Application
    Filed: December 3, 2013
    Publication date: June 5, 2014
    Applicant: Ohio State Innovation Foundation
    Inventors: Jonathan R. Parquette, Se Hye Kim, Mark W. Grinstaff, Jonah A. Kaplan
  • Publication number: 20140141025
    Abstract: The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 22, 2014
    Applicant: REDWOOD BIOSCIENCE, INC.
    Inventors: Romas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
  • Publication number: 20140135356
    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: Application
    Filed: November 11, 2013
    Publication date: May 15, 2014
    Applicant: FL Therapeutics, LLC
    Inventor: Qun Sun
  • Publication number: 20140135486
    Abstract: A multi-arm polyethylene glycol (I) having different kinds of reactive groups and the uses thereof are disclosed, which is formed by polymerizing ethylene oxide with oligo-pentaerythritol as an initiator, wherein, PEG is same or different and is —(CH2CH2O)m—, the average value of m is an integer of 2-250; l is an integer of 1 or more. The method for producing the multi-arm polyethylene glycol having different kinds of reactive groups, the multi-arm polyethylene glycol active derivatives comprising linking groups X attached to PEG and terminal reactive groups F attached to X, the gels formed by the multi-arm polyethylene glycol active derivatives, the drug conjugates formed by the multi-arm polyethylene glycol active derivatives and drug molecules, and the uses thereof in preparing drugs are also disclosed.
    Type: Application
    Filed: January 21, 2014
    Publication date: May 15, 2014
    Applicant: JENKEM TECHNOLOGY CO., LTD, TIANJIN BRANCH
    Inventors: Xuan Zhao, Meina Lin
  • Publication number: 20140128272
    Abstract: Provided are a method for retaining in a dormant state a cancer tissue-derived cell mass that can reflect accurately the in vivo behavior of cancer cells, and an evaluation method for examining the sensitivity to various treatments including a drug sensitivity test by using a cancer tissue-derived cell mass in such a dormant state. The cancer tissue-derived cell mass is prepared from an individual. Such a cancer tissue-derived cell mass is cultured in vitro under the conditions of hypoxia and low levels of growth factors. Furthermore, a treatment with a drug, etc. is applied in vitro to the cancer tissue-derived cell mass in the dormant state so that evaluation is achieved by examination of its proliferation state, determination of life and death, and analysis of signals.
    Type: Application
    Filed: February 15, 2013
    Publication date: May 8, 2014
    Inventor: Masahiro Inoue
  • Publication number: 20140128421
    Abstract: Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 8, 2014
    Applicants: EAST CHINA NORMAL UNIVERSITY, NANJING LUYESKIE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Wei Lv, Shanbao Yu, Yu Luo, Yi Chen, Jian Ding
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Patent number: 8710071
    Abstract: The present technology relates to compounds of Formulas (V) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: April 29, 2014
    Assignee: CVI Pharmaceuticals Limited
    Inventors: Haiyan Liu, Gaoping Li, Junbo Wang, Jingwen Liu
  • Patent number: 8685997
    Abstract: New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
    Type: Grant
    Filed: January 17, 2007
    Date of Patent: April 1, 2014
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Wei Lu, Jian Ding, Heyong Gao, Liping Lin, Yi Chen
  • Patent number: 8686146
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: April 1, 2014
    Assignee: Purdue Research Foundation
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell