| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 41 | Electrochemical synthesis of chloro-chitosan | US14374948 | 2013-02-01 | US09518077B2 | 2016-12-13 | Gary P. Halada; Prashant Kumar Jha |
| The present disclosure provides methods for producing chitosan derivatives and the derivatives formed by these methods. The processes of the present disclosure utilize electrochemical methods to functionalize and/or modify amine and/or hydroxyl groups present on chitosan, to form new derivatives. In embodiments, a chloro-chitosan derivative may be prepared. The altered cationic affinity of these derivatives make them excellent candidates for biomedical applications, including pharmaceuticals, as well as food applications. | ||||||
| 42 | Polysaccharides comprising carboxyl functional groups substituted by a hydrophobic alcohol derivative | US12588149 | 2009-10-06 | US20100167991A1 | 2010-07-01 | Remi Soula; Olivier Soula; Gerard Soula; Richard Charvet |
| The invention relates to a polysaccharide comprising carboxyl functional groups, one at least of which is substituted by a derivative of a hydrophobic alcohol. The invention also relates to a pharmaceutical composition comprising one of the polysaccharides according to the invention and at least one active principle. It also relates to a pharmaceutical composition, wherein the active principle is chosen from the group consisting of proteins, glycoproteins, peptides and nonpeptide therapeutic molecules. The invention also relates to the use of the functionalized polysaccharides according to the invention in the preparation of pharmaceutical compositions as described above. | ||||||
| 43 | ENZYMATIC SUBSTRATES FOR MULTIPLE DETECTION SYSTEMS | US12403790 | 2009-03-13 | US20090253117A1 | 2009-10-08 | Blas Cerda; Mark Norman Bobrow |
| An inventive substrate is provided which includes a substrate compound of formula A-B1-B2-B3-B4: wherein A is a sugar moiety; B1 is a linker moiety allowing the conjugation of moiety A and the remaining structure of the substrate; B2 is a linker moiety with a free reactive amino group so as to be available for reaction with carboxylic acids or detectable tags; B3 contains a permanently charged element such as a quaternary ammonium group so as to increase sensitivity for mass spectrometry analysis; and B4 of various carbon length conferring specificity amongst individual substrates in detection methods. Also provided is a molecule of the formula B1-B2-B3-B4, with similar structural characteristics to an enzymatic product produced by the action of a target enzyme on an inventive substrate. Further provided are methods for using inventive substrates for detecting enzymatic activity. | ||||||
| 44 | Gene encoding a DNA repair enzyme and methods of use thereof | US11739558 | 2007-04-24 | US07491807B2 | 2009-02-17 | Alfonso Bellacosa |
| An isolated nucleic acid molecule encoding a human DNA repair enzyme, MED1, is disclosed. Like other mismatch repair genes which are mutated in certain cancers, MED1, encoding nucleic acids, proteins and antibodies thereto may be used to advantage in genetic or cancer screening assays. MED1, which recognizes and cleaves DNA, may also be used for the diagnostic detection of mutations and genetic variants. | ||||||
| 45 | Micelles | US10204227 | 2001-02-20 | US06906042B2 | 2005-06-14 | James McShane; Tori Arens; Kazuhiro Kaneko; Tomohiro Watanabe; Kazuhide Ashizawa |
| The invention provides micelles, pharmaceutical formulations comprising micells, solutions comprising micells, methods for preparing micells, methods for delivering micells to patients, and methods for treating sepsis, endotoxemia, septic shock and systemic inflamatory response syndrome in patients by adiministering micelles. The micelles comprises compounds of Forumala (A): wherein the substituents are as defined herein. | ||||||
| 46 | Prodrugs and conjugates of thiol- and selenol-containing compounds and methods of use thereof | US10051463 | 2002-01-18 | US06841536B2 | 2005-01-11 | Jeannette C. Roberts; Britta H. Wilmore; Pamela B. Cassidy; Pamela K. Dominick; Megan D. Short |
| Disclosed is a prodrug of the formula: where A is a sulfur or a selenium, and R is derived from a mono- di- or oligo- saccharide. Also disclosed is a prodrug of the formula: where A is sulfur or selenium, R′ is derived from a sugar and R′ has the formula (CHOH)nCH2OH, where n is 1 to 5, or R′ is an alkyl or aryl group, or R′ is ═O, and the R″ groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine.Also disclosed is a prodrug of the formula; where A is sulfur or selenium, and R′ is derived from a sugar and R′ has the formula (CHOH)nCH2OH, where n is 1 to 5, or R′ is also be an alkyl or aryl group, or R′ is ═O, and R‡ is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula: where R is COOH or H, and R′ is derived from a sugar and R′ has the formula (CHOH)nCH2OH,where n is 1 to 5, or R′ is an alkyl or aryl group, or R′ is ═O. | ||||||
| 47 | 3,4-di-O,N-Protected-4-amino-2,4,6-trideoxy-2-fluoro-L-manno-pyranosyl halide and a process for its preparation | US282200 | 1999-03-31 | US6075135A | 2000-06-13 | Tomio Takeuchi; Sumio Umezawa; Tsutomu Tsuchiya; Yasushi Takagi |
| 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-.alpha.-L-mannopyranosyl)-daunomycinone or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1## wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent. | ||||||
| 48 | Preparation of glucosaminyl muramic acid derivatives | US539292 | 1995-10-04 | US5750665A | 1998-05-12 | Gerald J. Vosika; Fanfeng Ma |
| The present invention provides a method for the preparation of disaccharides, such as glucosaminyl muramic acids peptides and derivatives. The method includes condensing a protected muramic acid ester with a 1-organothio- or 1-fluoroglucosamine derivative in the presence of a suitable promoter to produce a protected glucosaminyl muramic acid ester. The protected glucosaminyl muramic acid ester may be used to prepare disaccharide peptides, such as N-acetylglucosaminyl-N-acetylmuramyl dipeptides, which have demonstrated immunological activity. Protected muramic acid esters and 1-organothio- or 1-fluoro- glucosamine compounds which may be employed as intermediates in the method are also provided. | ||||||
| 49 | Substituted liposaccharides useful in the treatment and prevention of endotoxemia | US461675 | 1995-06-05 | US5750664A | 1998-05-12 | William J. Christ; Daniel P. Rossignol; Seiichi Kobayashi; Tsutomu Kawata |
| Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein. | ||||||
| 50 | Process for preparing macrolide derivatives | US846446 | 1986-03-31 | US4921947A | 1990-05-01 | Eddie V. P. Tao; Jeffrey T. Vicenzi |
| This invention provides an improvement in the process for preparing C-20-amino-substituted derivatives of the macrolide antibiotics of the tylosin type by reductively aminating the C-20 aldehyde group in the parent antibiotic. The improvement comprises using formic acid as the reducing agent. The new process is less expensive and more amenable to scale-up than previously used processes, but is still selective. | ||||||
| 51 | Treatment of malignant tumors with 2-(.beta.-D-ribofuranosylthiazole-4-carboxamide related compounds | US706084 | 1985-02-27 | US4680285A | 1987-07-14 | Roland K. Robins |
| The compound 2-.beta.-D-ribofuranosylthiazole-4-carboxamide is used to treat malignant tumors in warm blooded animals. Esters of this compound such as 2-(2,3,5-tri-O-acetyl-.beta.-D-ribofuranosyl)thiazole-4-carboxamide and 2-(5-O-phosphoryl-.beta.-D-ribofuranosyl)thiazole-4-carboxamide are also useful for treating tumors in warm blooded animals. | ||||||
| 52 | 2-.beta.-D-ribofuranosylselenazole-4-carboxamide compounds and methods for their production | US612078 | 1984-07-23 | US4594416A | 1986-06-10 | Roland K. Robins; Prem C. Srivastava |
| A class of novel 2-.beta.-D-ribofuranosylselenazole-4-carboxamide nucleoside and nucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties, especially antitumor and antiviral properties, and are well tolerated, being useful, for example, in treating tumors and viral infections in warm blooded animals. | ||||||
| 53 | Novel antifugal antibiotic substance, process for production of the same, and agricultural and horticultural fungicidal composition containing said substance | US272217 | 1972-07-17 | US3956276A | 1976-05-11 | Toju Hata; Satoshi Omura; Michiko Katagiri; Juichi Awaya; Shimpei Kuyama; Shizuo Higashikawa; Kazuomi Yasui; Haruko Terada |
| The antifungal antibiotic substance "F-1028" having the following formula, ##EQU1## or an acid salt thereof, a process for the production of the same by fermentation, and a fungicidal composition useful for agricultural and horticultural use. | ||||||
| 54 | Mannose-Based mRNA Targeted Delivery System and Use Thereof | US18329015 | 2023-06-05 | US20230355776A1 | 2023-11-09 | Yong Hu; Miaomiao Zhang |
| The present invention provides a mannose-based mRNA targeted delivery system and use thereof. The mRNA can encode one or more target polypeptides and contains at least one mannose modification. The technical solution of the present invention modifies the mRNA molecule with a mannose, so that the mRNA can be directly and efficiently coupled with the mannose, and the targeted delivery of the mRNA is realized without the need for a carrier. | ||||||
| 55 | INHIBITORS OF SODIUM GLUCOSE COTRANSPORTER 1 | US15601175 | 2017-05-22 | US20180244708A1 | 2018-08-30 | Kenneth Gordon CARSON; Nicole Cathleen GOODWIN; Bryce Alden HARRISON; David Brent RAWLINS; Eric STROBEL; Brian ZAMBROWICZ |
| Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein. | ||||||
| 56 | Stabilisation of radiopharmaceutical precursors | US11721563 | 2005-11-18 | US10000518B2 | 2018-06-19 | Lill Torild Wickstrom; Dirk-Jan in't Veld; Nigel John Osborn; Julian Grigg; Anthony Wilson |
| The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-ß-D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed. | ||||||
| 57 | Cell-permeable probes for identification and imaging of sialidases | US14422310 | 2013-08-16 | US09914956B2 | 2018-03-13 | Chi-Huey Wong; Jim-Min Fang; Yih-Shyun E. Cheng; Charng-Sheng Tsai |
| Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions. | ||||||
| 58 | Inhibitors of sodium glucose cotransporter 1 | US14943505 | 2015-11-17 | US09688710B2 | 2017-06-27 | Kenneth Gordon Carson; Nicole Cathleen Goodwin; Bryce Alden Harrison; David Brent Rawlins; Eric Strobel; Brian Zambrowicz |
| Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein. | ||||||
| 59 | Inhibitors of sodium glucose cotransporter 1 | US14082786 | 2013-11-18 | US09200025B2 | 2015-12-01 | Kenneth Gordon Carson; Nicole Cathleen Goodwin; Bryce Alden Harrison; David Brent Rawlins; Eric Strobel; Brian Zambrowicz |
| Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein. | ||||||
| 60 | ELECTROCHEMICAL SYNTHESIS OF CHLORO-CHITOSAN | US14374948 | 2013-02-01 | US20150011742A1 | 2015-01-08 | Gary P. Halada; Prashant Kumar Jha |
| The present disclosure provides methods for producing chitosan derivatives and the derivatives formed by these methods. The processes of the present disclosure utilize electrochemical methods to functionalize and/or modify amine and/or hydroxyl groups present on chitosan, to form new derivatives. In embodiments, a chloro-chitosan derivative may be prepared. The altered cationic affinity of these derivatives make them excellent candidates for biomedical applications, including pharmaceuticals, as well as food applications. | ||||||
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