| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 101 | SELENOGALACTOSIDE COMPOUNDS FOR THE TREATMENT OF SYSTEMIC INSULIN RESISTANCE DISORDERS AND THE USE THEREOF | PCT/US2018/032321 | 2018-05-11 | WO2019089080A9 | 2019-05-09 | TRABER, Peter G.; ZOMER, Eliezer; SLATE, Deirdre; JOHNSON, Joseph M.; GEORGE, Ryan; SHECHTER, Sharon; NIR, Raphael |
Aspects of the invention relate to novel synthetic compounds having a binding affinity with galectin proteins for the treatment of systemic insulin resistance disorders. |
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| 102 | PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES | PCT/EP2010/005199 | 2010-08-25 | WO2011023374A1 | 2011-03-03 | FRANZEN, Manuela; NOTI, Christian |
Enantiomerically enriched (1 S,4R)-2-oxa-3-azabicyclo[2.2.1]hept-5-ene of formula wherein PG1 is an amino-protective group, are prepared from cyclopentadiene via hetero-Diels-Alder cycloaddition with protected 1-C-nitroso-β-D-ribofuranosyl halides of formula wherein X is a halogen atom selected from fluorine, chlorine, bromine and iodine, PG2 is a hydroxyl-protective group and PG3 is a 1,2-diol-protective group. |
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| 103 | GENERATION OF PHOSPHORUS OXYCHLORIDE AS BY-PRODUCT FROM PHOSPHORUS PENTACHLORIDE AND DMF AND ITS USE FOR CHLORINATION REACTION BY CONVERTING INTO VILSMEIER-HAACK REAGENT. | PCT/IN2006000151 | 2006-04-28 | WO2007017891A3 | 2009-04-09 | RATNAM RAKESH; SUNDEEP AURORA; MOFIZUDDIN MOHAMMED |
| A process is described wherein after formation of first crop of Vilsmeier-Haack reagent by reacting Phosphorus Pentachloride with N,N-dimethylformamide to form a first crop of Vilsmeier reagent as insoluble crystals, a by-product of this reaction, the Phosphorus Oxy-Chloride, reacts with N,N-dimethylformamide to give a second crop of Vilsmeier reagent. This second crop of Vilsmeier reagent is soluble in DIV1F. This process makes it possible to double the yield of chlorinated substrate, such as sucrose-6-acetate or sucrose-6-benzoate, from the same quantity of Phosphorus Pentachloride. | ||||||
| 104 | STABILIZATION OF TRIFLATED COMPOUNDS | PCT/US2006/022757 | 2006-06-08 | WO2006133448A1 | 2006-12-14 | MAJOR, Michael; PETERSON, Robert; KOSINSKI, Szymon |
Described are novel processes for the synthesis triflated sugars. These sugars are useful for the production of compounds, such as D-1-deoxynojirimycin (DNJ) and D-1-deoxygalactonojirimycin (DGJ). In particular, described is a multi- kilogram scale stabilization method for the synthesis of imino sugars. |
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| 105 | STABILISATION OF RADIOPHARMACEUTICAL PRECURSORS | PCT/GB2005/004448 | 2005-11-18 | WO2006067366A1 | 2006-06-29 | WICKSTROM, Lill, Torild; VELD, Dirk in't; OSBORN, Nigel, John; GRIGGS, Julian; WILSON, Anthony |
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. |
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| 106 | IMPROVED SUCRALOSE COMPOSITION AND PROCESS FOR ITS PREPARATION | PCT/US2001/043491 | 2001-11-16 | WO02040495A2 | 2002-05-23 | |
| The present invention provides an improved form of sucralose and a process for making it. | ||||||
| 107 | PRODRUGS AND CONJUGATES OF THIOL- AND SELENOL- CONTAINING COMPOUNDS AND METHODS OF USE THEREOF | PCT/US1998/016324 | 1998-08-06 | WO99007719A1 | 1999-02-18 | |
| Disclosed is a prodrugs of the formula (I) where A is a sulfur or a selenium, and R is derived from a mono- di- or oligosaccharide. Also disclosed is a prodrug of the formulas (II); 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 (III); 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 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 (IV) 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. | ||||||
| 108 | ANTIVIRAL ACTIVITY AND RESOLUTION OF 2-HYDROXYMETHYL-5-(5-FLUOROCYTOSIN-1-YL)-1,3-OXATHIOLANE | PCT/US9201339 | 1992-02-20 | WO9214743A3 | 1992-10-29 | LIOTTA DENNIS C; SCHINAZI RAYMOND F; CHOI WOO-BAEG |
| Enantiomerically enriched cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimidin-2-one, derivatives and pharmaceutical compositions thereof. | ||||||
| 109 | ARYL GLUCOSIDE DERIVATIVE AND USE THEREOF IN DRUG | EP20935900.9 | 2020-11-24 | EP4119550A1 | 2023-01-18 | DU, Fengtian; WANG, Haibo; ZHANG, Qiang |
A compound inhibiting a sodium-glucose cotransporter 1, and a pharmaceutically acceptable salt and a stereoisomer thereof. The compound is used in a pharmaceutical composition. Also disclosed are methods for preparing and using the pharmaceutical composition, and an application in preparing a drug and a composition of the compound for treating and improving diabetes,cardiovascular and cerebrovascular diseases, weight reduction, fatty liver, astriction, and metabolism-related diseases, and cancer therapy. |
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| 110 | INHIBITORS OF SODIUM GLUCOSE COTRANSPORTER 1 | EP18213751.3 | 2013-11-18 | EP3489226B1 | 2021-02-17 | CARSON, Kenneth Gordon; GOODWIN, Nicole Cathleen; HARRISON, Bryce Alden; RAWLINS, David Brent; STROBEL, Eric; ZAMBROWICZ, Brian |
| 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. | ||||||
| 111 | STABILISATION OF RADIOPHARMACEUTICAL PRECURSORS | EP05814407.2 | 2005-11-18 | EP1843792B1 | 2017-01-04 | WICKSTROM, Lill Torild, Amersham Health AS; VELD, Dirk in't, Amersham Health AS; OSBORN, Nigel John, GE Healthcare Limited; GRIGG, Julian, GE Healthcare Limited; WILSON, Anthony, GE Healthcare Limited |
| 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-beta-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. | ||||||
| 112 | PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES | EP10747830.7 | 2010-08-25 | EP2473492B1 | 2015-10-07 | FRANZEN, Manuela; NOTI, Christian |
| 113 | CORONA-LIKE (GUANIDYL)-OLIGOSACCHARIDIC DERIVATIVES AS CELL-PENETRATING ENHANCERS FOR INTRACELLULAR DELIVERY OF COLLOIDAL THERAPEUTIC SYSTEMS | EP11709656.0 | 2011-01-21 | EP2665736A1 | 2013-11-27 | CALICETI, Paolo; SALMASO, Stefano; BERSANI, Sara |
| A novel class of cell-penetrating enhancers with unusual chemical structure is herein disclosed. Said cell-penetrating enhancers are non-linear and non peptidic (guanidyl)-oligosaccharidic derivatives, which can be easily obtained according to simple and reproducible synthetic steps. A wide array of cell penetration enhancers can be obtained by slight modification of the main structure oligosaccharidic backbone and in order to provide for their conjugation or physical combination with a variety of therapeutic systems. These molecules can be designed for conjugation to proteins or polymer therapeutics or for surface decoration of liposomes or nanoparticles. Finally, the cationic features and the penetration enhancer properties of the corona-like (guanidyl)-oligosaccharidic derivatives can be exploited for oligonucleotide, namely siRNA, or gene delivery. | ||||||
| 114 | 17 HUMAN SECRETED PROTEINS | EP01984565 | 2001-01-17 | EP1317472A4 | 2005-04-27 | ROSEN CRAIG A; KOMATSOULIS GEORGE A; BAKER KEVIN P; BIRSE CHARLES E; SOPPET DANIEL R; OLSEN HENRIK S; MOORE PAUL A; WEI PING; EBNER REINHARD; DUAN ROXANNE D; SHI YANGGU; CHOI GIL H; FISCELLA MICHELE; NI JIAN |
| 115 | 17 HUMAN SECRETED PROTEINS | EP01984565.0 | 2001-01-17 | EP1317472A1 | 2003-06-11 | ROSEN, Craig, A.; KOMATSOULIS, George, A.; BAKER, Kevin, P.; BIRSE, Charles, E.; SOPPET, Daniel, R.; OLSEN, Henrik, S.; MOORE, Paul, A.; WEI, Ping; EBNER, Reinhard; DUAN, Roxanne, D.; SHI, Yanggu; CHOI, Gil, H.; FISCELLA, Michele; NI, Jian |
| The present invention relates to novel human secreted proteins and isolated nucleic acids containing the coding regions of the genes encoding such proteins. Also provided are vectors, host cells, antibodies, and recombinant methods for producing human secreted proteins. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating diseases, disorders, and/or conditions related to these novel human secreted proteins. | ||||||
| 116 | A COMBINATORIAL LIBRARY OF MOENOMYCIN ANALOGS AND METHODS OF PRODUCING SAME | EP98960228.9 | 1998-11-17 | EP1047703A1 | 2000-11-02 | ALLANSON, Nigel, Mark; CHAN, Tin, Yau; HATZENBUHLER, Nicole, T.; JAIN, Rakesh, K.; KAKARLA, Ramesh; LIANG, Rui; LIU, Dashan; SILVA, Domingos; SOFIA, Michael |
| A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has formula (I) wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes. | ||||||
| 117 | NEW CARBOHYDRATE-BASED ANTI-INFLAMMATORY AGENTS | EP91916053 | 1991-07-30 | EP0541719A4 | 1995-09-06 | BRANDLEY BRIAN K; TIEMEYER MICHAEL; SWIEDLER STUART J; MORELAND MARGARET; SCHWEINGRUBER HANS |
| 118 | Process for the manufacture of 2-deoxy-D-threo-pentofuranosides, intermediates for their manufacture and their use | EP91105231.4 | 1991-04-03 | EP0450585A2 | 1991-10-09 | Saischek, Gerald, Dipl.-Ing.; Fuchs, Franz; Dax, Karl, Dr.; Billiani, Gertrude, Dr. |
Disclosed is a process for the manufacture of 2-Deoxy-D-threo-pentofuranosides of formula 1
Furtheron disclosed are a process for the manufacture of 3-substituted 2-deoxy-D-erythro-pentofuranosides using these compounds and novel and substituted and unsubstituted 2-deoxy-D-pentofuranosides and their use for the manufacture of 3'-substituted 2'-deoxynucleosides. |
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| 119 | Isolation of unreduced oligosaccharides | EP86870123.6 | 1986-09-05 | EP0215766B1 | 1991-10-09 | Dwek, Raymond Allen; Rademacher, Thomas William |
| 120 | ARYL GLUCOSIDE DERIVATIVE | EP20935121.2 | 2020-11-24 | EP4166547A1 | 2023-04-19 | WANG, Haibo; DU, Fengtian; ZHANG, Qiang; GUO, Na |
Provided in the present invention are a compound for inhibiting sodium glucose cotransporter 1, and a pharmaceutically acceptable salt and a stereoisomer of the compound. The compound is used for a pharmaceutical composition, and further provided is a method for preparing and using same, comprising the use of the drug or the composition in the preparation for the treatment and improvement of diabetes, cardiovascular and cerebrovascular diseases, weight loss, fatty liver, constipation, metabolism-related diseases and in the treatment of tumors. |
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