Nitrogen Attached Directly Or Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/546)
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Patent number: 8188145Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.Type: GrantFiled: April 18, 2005Date of Patent: May 29, 2012Assignee: Magnachem International Laboratories, Inc.Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
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Publication number: 20120077988Abstract: A branched hetero polyethylene glycol according to the present invention is represented by the formula [1]: wherein X and Y represent each an atomic group containing at least a functional group which reacts with a functional group present in a bio-functional molecule to form a covalent bond and the functional group contained in the atomic group X and the functional group contained in the atomic group Y are different from each other; s is an integer of 2 to 8, which represents the number of polyethylene glycol chains; n is the number of average added moles for the polyethylene glycol chain and 20?n?2000; and E is a branching linker moiety having s-valent bonding valency for the polyethylene glycol chains and having monovalent bonding valency for the functional group Y.Type: ApplicationFiled: June 24, 2011Publication date: March 29, 2012Applicant: NOF CORPORATIONInventors: Yuji Yamamoto, Hiroki Yoshioka, Fumiaki Manabe
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Patent number: 8138182Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: GrantFiled: September 24, 2009Date of Patent: March 20, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
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Publication number: 20120045848Abstract: The invention provides a novel class of reactive fluorescent agents that are based on a pyrene sulfonic acid nucleus. The agents are readily incorporated into conjugates with other species by reacting the reactive group with a group of complementary reactivity on the other species of the conjugate. Also provided are methods of using the compounds of the invention to detect and/or quantify an analyte in a sample. In an exemplary embodiment, the invention provides multi-color assays incorporating the compounds of the invention.Type: ApplicationFiled: May 31, 2011Publication date: February 23, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Richard Haugland, Wai-Yee Leung, Jixiang Liu
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Publication number: 20120027680Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for treating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.Type: ApplicationFiled: July 28, 2011Publication date: February 2, 2012Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Publication number: 20110305632Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).Type: ApplicationFiled: December 11, 2009Publication date: December 15, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Brett Michael Paterson
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Publication number: 20110288076Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: EXELIXIS, INC.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20110263457Abstract: We describe herein a cell-based multiplexing technique called detectable cell barcoding (DCB). In DCB, each individual sample is labeled with a different DCB signature that distinguishes each sample by one or both of detected intensity or type of detection characteristic. The samples are then combined and analyzed for a detectable characteristic of interest (e.g., presence of an analyte). By employing multiple distinct DCB labels at varying concentrations, one can perform multiplex analyses on up to hundreds or thousands (or more) of cell samples in a single reaction tube. DCB reduces reagent consumption by factors of 100-fold or more, significantly reduces data acquisition times and allows for stringent control sample analysis.Type: ApplicationFiled: July 1, 2011Publication date: October 27, 2011Inventors: Peter O. Krutzik, Garry Nolan
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Publication number: 20110256549Abstract: Described herein are methods, compositions and articles of manufacture involving neutral conjugated polymers including methods for synthesis of neutral conjugated water-soluble polymers with linkers along the polymer main chain structure and terminal end capping units. Such polymers may serve in the fabrication of novel optoelectronic devices and in the development of highly efficient biosensors. The invention further relates to the application of these polymers in assay methods.Type: ApplicationFiled: March 17, 2011Publication date: October 20, 2011Applicant: Sirigen, Inc.Inventors: Brent S. Gaylord, Jean M. Wheeler, Glenn P. Bartholomew, Frank Peter Uckert, Janice W. Hong, William H. Huisman
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Publication number: 20110245509Abstract: A polyfunctional polyoxyalkylene compound represented by the following formula (1): wherein Z represents a hydroxyl group-removed residue of pentaerythritol or dipentaerythritol, R represents a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 represent an oxyalkylene group having 2 to 4 carbon atoms, L1 and L2 represent an alkylene group which may have an ester bond or the like in the alkylene chain or at the terminal end, and X represents a functional group capable of reacting chemically; R, OA1, OA2, L1, and L2 are the same or different from one another in one molecule, m and n are an average number of moles of the oxyalkylene group added, m represents 5 to 1,000, and n represents 0 to 1,000; p and q represent 0 or 1; r1+r2=4 or 6; and r1 and r2 are an integer of 2 or more.Type: ApplicationFiled: July 6, 2010Publication date: October 6, 2011Applicant: NOF CORPORATIONInventors: Ken-ichiro NAKAMOTO, Masaki KAMIYA, Tsuyoshi TAKEHANA
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Publication number: 20110213123Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).Type: ApplicationFiled: August 30, 2010Publication date: September 1, 2011Inventors: Carolyn R. Bertozzi, Nicholas J. Agard, Jennifer A. Prescher, Jeremy Michael Baskin
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110111477Abstract: The invention relates to a long-acting formulation of biopharmaceutical, more specifically an aptamer therapeutics. A branched PEGylated aptamer or a hyaluronic acid (HA) derivative of which degradation in vivo is regulated is linked by the bioconjugation with biopharmaceutical to produce the long-action formulation.Type: ApplicationFiled: April 13, 2009Publication date: May 12, 2011Inventors: Sei-Kwang HAHN, Hyun-Gu Kang, Sung-Ho Ryu, Jung-Kyu Park, Eun-Ju Oh
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Patent number: 7923562Abstract: Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.Type: GrantFiled: June 16, 2009Date of Patent: April 12, 2011Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Surajit Sinha, Ilya Shestopalov, Xiaohu Ouyang
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Patent number: 7915228Abstract: The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the pharmaceutical composition.Type: GrantFiled: June 2, 2008Date of Patent: March 29, 2011Assignee: Tioga Pharmaceuticals, Inc.Inventors: Matthias Wiesner, Christoph Seyfried
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Patent number: 7910618Abstract: The present invention provides an albumin-binding compound essentially of the following elements: a spacer group, a water-soluble bridging group, a fatty acid chain and an acidic group characterised in that the acidic group is attached to the distal end of the fatty acid chain. The invention also provides an albumin-binding compound to which one or more biologically active moieties are attached.Type: GrantFiled: May 25, 2005Date of Patent: March 22, 2011Assignee: UCB Pharma S.A.Inventors: Michael Anthony Eaton, Timothy John Norman, John Robert Porter
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Publication number: 20110053819Abstract: The present invention relates to compositions comprising polyaspartic acid (PAS) derivatives and the use of said compositions in washing processes, especially in automatic dishwashing.Type: ApplicationFiled: January 23, 2009Publication date: March 3, 2011Inventors: Judith Preuschen, Ralf Wiedemann
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Publication number: 20110028364Abstract: A bis-type alkenyl-substituted succinimide which is prepared by reaction of succinic anhydride substituted with 2-alkenyl group having a branch structure in ?-position with alkylenepolyamine and its derivatives derived from the bis-type alkenyl-substituted succinimide by post-treatment are of value as friction modifiers, particularly for incorporation into lubricating oils for automatic transmissions.Type: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Inventors: Kedar Shanker Shrestha, Michio Shiga, Masami Fuchi, Takahiro Nakagawa
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Publication number: 20110021761Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.Type: ApplicationFiled: October 5, 2010Publication date: January 27, 2011Applicant: Nektar TherapeuticsInventors: Antoni Kozlowski, Xiaoming Shen, Michael D. Bentley, Zhihao Fang, Tony L. Sander
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Publication number: 20100280252Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.Type: ApplicationFiled: February 17, 2010Publication date: November 4, 2010Applicant: Intezyne TechnologiesInventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
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Publication number: 20100261245Abstract: The invention relates to a long-acting formulation of biopharmaceutical, more specifically an aptamer therapeutics. A branched PEGylated aptamer or a hyaluronic acid (HA) derivative of which degradation in vivo is regulated is linked by the bioconjugation with biopharmaceutical to produce the long-action formulation.Type: ApplicationFiled: April 13, 2009Publication date: October 14, 2010Inventors: Sei-Kwang HAHN, Hyun-Gu Kang, Sung-Ho Ryu, Jung-Kyu Park, Eun-Ju Oh
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Patent number: 7812178Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: GrantFiled: November 3, 2008Date of Patent: October 12, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi
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Patent number: 7807846Abstract: There is provided a method for producing a succinimide compound. The method for producing a succinimide compound of formula (3) comprises reacting an aminomalonic ester compound of formula (1) with a compound of formula (2) in a solvent in the presence of a base, wherein an alcohol is used as the solvent and an alkali metal alkoxide is used as the base. (where R1 and R4 independently represent an alkyl group having 1 to 12 carbon atom(s) which may be a straight chain, branched or cyclic, etc., R2 and R3 independently represent a hydrogen atom, etc., R5 represents an alkyl group having 1 to 12 carbon atom(s) which may be straight chain, branched or cyclic, etc.).Type: GrantFiled: September 26, 2007Date of Patent: October 5, 2010Assignees: Nissan Chemical Industries, Ltd., DaiNippon Sumitomo Pharma Co., Ltd.Inventors: Masami Kozawa, Hideki Musashi
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Publication number: 20100233190Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: ApplicationFiled: March 12, 2009Publication date: September 16, 2010Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong ZHAO, Maria Belen RUBIO, Pasanna Reddy
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Publication number: 20100183532Abstract: UV-absorbing compounds are disclosed that are derived from at least: (a) a UV absorber having at least one hydroxyl group, primary amine group, or secondary amine group, (b) a coupling agent having anhydride functionality, and (c) a graft host comprising an unsaturated fatty acid. These compounds absorb, scatter, deflect, or scatter ultraviolet radiation in a variety of personal care and performance chemical applications. W? and R?? are alkyl or alkenyl groups that naturally occur in oil.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Inventors: Osama M. Musa, Jenn S. Shih
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Publication number: 20100160409Abstract: The invention relates to compounds, which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, in addition to conjugates from the compounds comprising biomolecules or pharmaceutically active substances. The inventive compounds are highly cross-linked and can be formed in a simple manner by using a central cross-linking module. The invention also relates to the use of conjugates as an improved formulation of pharmaceuticals and to the production thereof.Type: ApplicationFiled: August 31, 2006Publication date: June 24, 2010Inventors: Ralf Krahmer, Frank Leenders
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Publication number: 20100107478Abstract: The present invention relates to oxazolidines derived from polyalkyl or polyalkenyl N-hydroxyalkyl succinimides, the obtainment process thereof, and their use to prevent and control the formation of deposits in internal combustion engines, primarily in formulations of additives to be applied to hydrocarbon fuels.Type: ApplicationFiled: April 15, 2008Publication date: May 6, 2010Applicant: INSTITUTO MEXICANO DEL PETROLEOInventors: Luis Silvestre Zamudio Rivera, Eugenio Alejandro Flores Oropeza, Marcelo Lozada y Cassou, Hiram Issac Beltran Conde, Eduardo Buenrostro Gonzalez, Youri Douda, Mario Alberto Guzman Vega, Adela Morales Pacheco, Violeta Yasmin Mena Cervantes, Raul Hernandez Altamirano
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Patent number: 7678913Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: GrantFiled: December 7, 2005Date of Patent: March 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Bing-Yan Zhu, Shumei Wang, Chhaya Bhakta, Robert M. Scarborough
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Publication number: 20100056776Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: ApplicationFiled: November 6, 2007Publication date: March 4, 2010Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Publication number: 20100016550Abstract: The present invention relates to methods for the chemo-selective pegylation of the cysteine residue having unoxidized sulfhydryl side-chain and free ?-amino group in proteins, peptides and other molecules. Similar methods are provided for the chemo-selective pegylation of the homocysteine, selenocysteine, penicillamine, and N-methyl-cysteine residues.Type: ApplicationFiled: May 25, 2007Publication date: January 21, 2010Inventors: Zheng Xin Dong, John S. Eynon
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Publication number: 20100004464Abstract: There is provided a method for producing a succinimide compound. The method for producing a succinimide compound of formula (3) comprises reacting an aminomalonic ester compound of formula (1) with a compound of formula (2) in a solvent in the presence of a base, wherein an alcohol is used as the solvent and an alkali metal alkoxide is used as the base. (where R1 and R4 independently represent an alkyl group having 1 to 12 carbon atom(s) which may be a straight chain, branched or cyclic, etc., R2 and R3 independently represent a hydrogen atom, etc., R5 represents an alkyl group having 1 to 12 carbon atom(s) which may be straight chain, branched or cyclic, etc.Type: ApplicationFiled: September 26, 2007Publication date: January 7, 2010Applicants: NISSAN CHEMICAL INDUSTRIES, LTD., DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Masami Kozawa, Hideki Musashi
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Publication number: 20090324621Abstract: Drug-Linker-Ligand Conjugates are disclosed in which a Drug is linked to a Ligand via a peptide-based Linker unit. In one embodiment, the Ligand is an Antibody. Drug-Linker compounds and Drug compounds are also disclosed. Methods for treating cancer, an autoimmune disease or an infectious disease using the compounds and compositions of the invention are also disclosed.Type: ApplicationFiled: March 20, 2009Publication date: December 31, 2009Applicant: Seattle Genetics, Inc.Inventors: Peter D. Senter, Svetlana O. Doronina, Brian E. Toki
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Publication number: 20090312530Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.Type: ApplicationFiled: August 17, 2009Publication date: December 17, 2009Applicant: WyethInventors: Justin Keith Moran, Jianxin Gu
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Patent number: 7629433Abstract: The invention relates to compounds of formula (I) which contain aldimine, and to the use thereof. Said compounds which contain aldimines are characterized in that they are odor-less and during hydrolysis the odor-free aldehydes are separated. They are used, therefor, as sources for aldehydes. They can also be used in cross-linking reactions.Type: GrantFiled: September 29, 2006Date of Patent: December 8, 2009Assignee: Sika Technology AGInventor: Urs Burckhardt
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Publication number: 20090253917Abstract: The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, wherein R3 is a tert-C4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3?-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.Type: ApplicationFiled: June 13, 2007Publication date: October 8, 2009Inventor: Daisuke Tanaka
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Publication number: 20090253672Abstract: This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, X and Y are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritisType: ApplicationFiled: October 10, 2006Publication date: October 8, 2009Inventors: Serge Leger, Christopher Bayly, Jean-Francois Truchon
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Publication number: 20090208410Abstract: The present invention relates to a method for stratifying tumor cells comprising the steps: (a) providing a sample comprising tumor cells to be analysed, (b) contacting said sample with an ED-B fibronectin-specific molecule and assessing the binding thereof to tumor cells in said sample, and (c) stratifying said tumor cells based on the assessment of step (b).Type: ApplicationFiled: September 16, 2008Publication date: August 20, 2009Inventors: Dietmar BERNDORFF, Ludger Dinkelborg, Tobias Heinrich
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Publication number: 20090203706Abstract: The present invention provides polymeric linkers containing branching moieties. Methods of making the polymeric linkers and methods of making conjugates using the same are also disclosed.Type: ApplicationFiled: March 12, 2009Publication date: August 13, 2009Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong Zhao, Prasanna Reddy
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Publication number: 20090156485Abstract: The invention relates to a method of producing keratin-binding effector molecules and to intermediates and end-products of the method according to the invention and to the use of the keratin-binding effector molecules produced according to the invention in dermocosmetics.Type: ApplicationFiled: November 15, 2006Publication date: June 18, 2009Applicant: BASE SEInventors: Heiko Barg, Burghard Liebmann, Martin Volkert, Arne Ptock, Heike Reents
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Patent number: 7547765Abstract: The present invention provides a branched polyalkylene glycol wherein three or more single-chain polyalkylene glycols and a group having reactivity with an amino acid side chain, the N-terminal amino group or the C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity are bound; and a physiologically active polypeptide modified with the branched polyalkylene glycol.Type: GrantFiled: October 23, 2007Date of Patent: June 16, 2009Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Motoo Yamasaki, Toshiyuki Suzawa, Tatsuya Murakami, Noriko Sukurai, Kinya Yamashita, Mayumi Mukai, Takashi Kuwabara
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Patent number: 7544709Abstract: The invention relates to compounds of general formula (I), to a method for the production thereof, to pharmaceutical compositions containing them, and to their use in the treatment and/or prophlaxis of diseases in humans or animals, particularly bacterial infections diseases. The compounds are derivatives of the natural substances andrimide and moiramide B.Type: GrantFiled: November 7, 2002Date of Patent: June 9, 2009Assignee: Bayer Healthcare AGInventors: Nina Brunner, Christoph Freiberg, Thomas Lampe, Ben Newton, Michael Otteneder, Josef Pernerstorfer, Jens Pohlmann, Guido Schiffer, Mitsuyuki Shimada
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Publication number: 20090105256Abstract: Prodrugs of ion channeling modulating compounds, including, for example, prodrugs of the ion channel modulating compound of the following formula: are described herein, as well as methods of making and using such prodrugs and pharmaceutical compositions containing such prodrugs.Type: ApplicationFiled: March 31, 2005Publication date: April 23, 2009Applicant: Cardiome Pharma Corp.Inventors: Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Adewale Eniale, Bertrand M.C. Plouvier
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Publication number: 20090099333Abstract: The invention relates to compounds of formula (I) which contain aldimine, and to the use thereof. Said compounds which contain aldimines are characterised in that they are odour-less and during hydrolysis the odour-free aldehydes are separated. They are used, therefor, as sources for aldehydes. They can also be used in cross-linking reactions.Type: ApplicationFiled: September 29, 2006Publication date: April 16, 2009Applicant: SIKA TECHNOLOGY AGInventor: Urs Burckhardt
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Publication number: 20090098076Abstract: The invention relates to a method of producing keratin-binding effector molecules, and to intermediates and end-products of the method according to the invention and to the use of the keratin-binding effector molecules produced according to the invention in dermocosmetics. In addition, the invention relates to a method of applying dermocosmetically active ingredients to skin and/or hair and to a method of increasing the residence time of an active ingredient on skin and hair.Type: ApplicationFiled: November 15, 2006Publication date: April 16, 2009Applicant: BASF SEInventors: Heiko Barg, Burghard Liebmann, Martin Volkert, Arne Ptock, Heike Reents
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Publication number: 20090017004Abstract: The present invention provides polymeric delivery systems including an aromatic allyllic acyl group. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: ApplicationFiled: July 11, 2008Publication date: January 15, 2009Applicant: ENZON PHARMACEUTICALS, INC.Inventor: Hong ZHAO
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Publication number: 20090005542Abstract: The invention relates to Fmoc (9-fluorenyl-methoxycarbonyl)-based polymeric conjugates. These conjugates are useful for extending the in-vivo circulation of protein and peptide drugs.Type: ApplicationFiled: June 25, 2008Publication date: January 1, 2009Applicants: Baxter International Inc., Baxter Healthcare SAInventors: Peter Turecek, Juergen Siekmann
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Publication number: 20080305986Abstract: Described are compounds useful for trimerising chemical entities, methods of trimerising chemical entities, and trimerised entities. In one aspect, the entities are peptides.Type: ApplicationFiled: August 16, 2005Publication date: December 11, 2008Inventors: Killian Waldemar Conde Fieboes, Birgitte Urs, Lars Fogh Iversen
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Publication number: 20080293920Abstract: The present invention relates to novel arginine analogs, and methods for their synthesis and use. Such analogs are designed to provide a protected or free thiol (—SH) group, thereby providing a convenient linkage chemistry for coupling to a suitable group on a target such as a protein, polypeptide, detectable label or solid phase, and at a site distal to the guanidino group. Arginine analog conjugates are useful for generating antibodies that can bind specifically with dimethylarginine, which can be detected using such antibodies in immunoassays.Type: ApplicationFiled: January 19, 2006Publication date: November 27, 2008Inventors: Kenneth F. Buechler, Mariusz G. Banaszczyk, Joseph Barry Noar, Violeta Dinauer
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Patent number: 7402678Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.Type: GrantFiled: December 17, 2004Date of Patent: July 22, 2008Assignee: 3M Innovative Properties CompanyInventors: Karl E. Benson, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. I. Moore, Rahul Shah
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Patent number: 7348357Abstract: The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis of diseases in people or animals, especially diseases of bacterial infection.Type: GrantFiled: July 28, 2003Date of Patent: March 25, 2008Assignee: Bayer HealthCare AGInventors: Nina Brunner, Christoph Freiberg, Thomas Lampe, Peter Nell, Ben Newton, Michael Otteneder, Josef Pernerstorfer, Jens Pohlmann, Guido Schiffer, Mitsuyuki Shimada, Niels Svenstrup, Rainer Endermann