Substituted saccharide compounds and dental compositions

Substituted saccharide compounds, dental compositions comprising substituted saccharide compounds, and methods of using dental compositions are described. In one embodiment, the substituted saccharide amide compound comprises a hydrophobic group and at least one free-radically polymerizable group with the proviso that the hydrophobic group is not bonded to the ethylenically unsaturated carbon atom of the free-radically polymerizable group. The hydrophobic group is typically bonded to a nitrogen atom of a saccharide amine residue or a carbonyl moiety of saccharide amide residue.

Photoacid generator, photoresist, coated substrate, and method of forming an electronic device

A photoacid generator has the formula (I): wherein R 1 , R 2 , R 3 , L 1 , L 2 , L 3 X, Z + , a, b, c, d, p, q, and r, are defined herein. A photoresist comprises the photoacid generator, and a coated article comprises the photoresist. The photoresist can be used to form an electronic device.

Dibenzo[B,F][1,4]Oxazepin-11-yl-N-Hydroxybenzamides as HDAC Inhibitors

This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) 225.-. (canceled) This application claims the benefit of U.S. application Ser. No. 11/925,151, filed Oct. 26, 2007, which claims the benefit of U.S. provisional application 60/884,287, filed Jan. 10, 2007, and U.S. provisional application 60/863,347, filed Oct. 28, 2006.1. Field of the InventionThis invention relates to compounds for the inhibition of histone deacetylase.2. Description of Related ArtIn eukaryotic cells, nuclear DNA associates with histones to form a compact complex called chromatin. The histones constitute a family of basic proteins which are generally highly conserved across eukaryotic species. The core histones, termed H2A, H2B, H3, and H4, associate to form a protein core. DNA winds around this protein core, with the basic amino acids of the histones interacting with the negatively charged phosphate groups of the DNA. Approximately 146 base pairs of DNA wrap around a histone core to make up a nucleosome particle, the repeating structural motif of chromatin.Csordas, 286: 23-38 (1990) teaches that histones are subject to posttranslational acetylation of the N-terminal lysine residues, a reaction that is catalyzed by histone acetyl transferase (HAT1). Acetylation neutralizes the positive charge of the lysine side chain, and is thought to impact chromatin structure. Indeed, Taunton et al., 272: 408-411 (1996), teaches that access of transcription factors to chromatin templates is enhanced by histone hyperacetylation. Taunton et al. further teaches that an enrichment in underacetylated histone H4 has been found in transcriptionally silent regions of the genome.Histone acetylation is a reversible modification, with deacetylation being catalyzed by a family of enzymes termed histone deacetylases (HDACs). The molecular cloning of gene sequences encoding proteins with HDAC activity has established the ...

POLYPHOSPHATE AND PYROPHOSPHATE DERIVATIVE OF SACCHARIDES

The present invention provides, among other things, phosphorylated and pyrophosphate derivatives of mono-, di- and oligosaccharides, as well as structural derivatives of these compounds. These compounds have a variety of uses including for pharmaceutical applications. Also provided are methods of use in the treatment of disease, including diseases related to oxygen delivery. 1. A pharmaceutical composition comprising a compound that is a polyphosphate or pyrophosphate derivative of a mono- , di- or oligosaccharide containing a pyranose or furanose unit , or a pharmaceutically acceptable salt thereof.2. The pharmaceutical composition of claim 1 , wherein the compound is a phosphate or polyphosphate derivative of glucose claim 1 , mannose claim 1 , or galactose.3. The pharmaceutical composition of or claim 1 , wherein the pyranose is part of an oligosaccharide comprising from 2 to 4 monosaccharide units.4. The pharmaceutical composition of claim 3 , wherein the oligosaccharide is a phosphate or polyphosphate derivative of sucrose or lactose.5. The pharmaceutical composition of any one of to claim 3 , wherein the compound comprises from 2 to about 10 phosphate or polyphosphate groups.6. The pharmaceutical composition of any one of to claim 3 , wherein the compound comprises 2 to about 10 pyrophosphate groups.7. The pharmaceutical composition of any one of to claim 3 , wherein the composition comprises at least one pyrophosphate that is an internal pyrophosphate ring.8. The pharmaceutical composition of any one of to claim 3 , wherein the pyranose further comprises a derivatized hydroxyl selected from alkoxy (—OR) or acyloxy (—OCOR) claim 3 , where R is selected from alkyl claim 3 , aryl claim 3 , acyl claim 3 , aralkyl claim 3 , alkenyl claim 3 , alkynyl claim 3 , heterocyclyl claim 3 , polycyclyl claim 3 , carbocycle claim 3 , amino claim 3 , acylamino claim 3 , amido claim 3 , alkylthio claim 3 , carbonyl claim 3 , sulfonate claim 3 , alkoxyl claim 3 , sulfonyl claim ...

FGF RECEPTOR-ACTIVATING 3-O-ALKYL OLIGOSACCHARIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

The invention relates to the FGF receptor-activating oligosaccharides corresponding to formula (I): 2. The compound according to claim 1 , in which n=1 and m=0 or n=0 and m=1.3. The compound according to claim 1 , in which Rrepresents an —O-alkyl group claim 1 , where said alkyl group contains from 1 to 8 carbon atoms and is optionally substituted with 1 or 2 groups claim 1 , which may be identical or different claim 1 , selected from aryl groups.4. The compound according to claim 1 , in which Rrepresents an —O-methyl or —O-pentyl group and is optionally substituted with 1 or 2 phenyl groups.5. The compound according to claim 1 , in which R claim 1 , R claim 1 , R claim 1 , Rand R claim 1 , which may be identical to or different from one another claim 1 , represent an —OSO group or a hydroxyl group claim 1 , on the condition that at least one group among R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents an —OSO group.6. The compound according to claim 1 , in which R claim 1 , R claim 1 , R claim 1 , Rand Rall represent —OSO groups.7. The compound according to claim 1 , in which at least one of the groups R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents an —OSO group claim 1 , and at least one of the groups R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents a hydroxyl group.8. The compound according to claim 1 , in which R claim 1 , Rand Rrepresent —OSO groups claim 1 , and Rand Rrepresent hydroxyl groups.9. The compound according to claim 1 , in which Rrepresents an —NH—CO-alkyl group claim 1 , where said alkyl group comprises from 1 to 4 carbon atoms.10. The compound according to claim 1 , in which R represents a methoxy group.11. The compound according to claim 1 , selected from the following compounds:{'smallcaps': L', 'D', 'L', 'D', 'L', 'D, 'sub': '2', 'methyl (sodium 3-O-methyl-2-O-sodium sulphonato-α--idopyranosyluronate)-(1→4)-(2-acetamido-2-deoxy-3-O-methyl-6-O-sodium sulphonato-α--glucopyranosyl)-(1→4)-[(sodium 3-O-methyl-2-O-sodium sulphonato-α-- ...

Protected Monomer and Method of Final Deprotection for RNA Synthesis

A method of deprotecting a solid support bound polynucleotide includes the step of contacting the polynucleotide with a composition comprising a diamine under conditions sufficient to deprotect the 2′-protected ribonucleotide residue. The solid support bound polynucleotide has at least one 2′-protected ribonucleotide residue, which has the following structure: wherein B P is a protected or unprotected heterocycle; R 12 is a protecting group selected from a hydrocarbyl, a substituted hydrocarbyl, an aryl, and a substituted aryl; X is O or S; and PG is a thionocarbamate protecting group.

Large scale preparation of pseudo-trisaccharide aminoglycosides and of intermediates thereof

Synthetic pathways for preparing pseudo-trisaccharide aminoglycoside compounds represented by Formula I or Ia as defined in the specification and donor and acceptor compounds useful for preparing such compounds are provided. A process of stereoselectively preparing compounds represented by Formula III as defined in the specification, while avoiding chromatographic separation of stereoisomers are also provided. Compounds prepared by the described processes and uses thereof are also provided.

Liposomes Useful for Drug Delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS

The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: 172-. (canceled)74. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is suitable for oral administration.75. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a capsule.76. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a tablet.77. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a pill.78. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a lozenge claim 73 , cachet claim 73 , dragee claim 73 , granules claim 73 , emulsion claim 73 , elixir claim 73 , or syrup.79. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a suspension.80. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a solution.81. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a powder.82. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 95% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.83. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 30% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.84. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 10% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.85. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.1 to about 10% by weight of the ...

CELL LABELING AGENT AND CELL LABELING KIT

The cell labeling agent includes a monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells. Among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives, at least one group that does not change, even when metabolized by the sialic acid biosynthetic pathway, includes a ring structure with a carbon-carbon double bond or triple bond. 16-. (canceled)7. A cell labeling agent , comprising monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells ,wherein at least one group in the monosaccharide derivatives that does not change even when metabolized by the sialic acid biosynthetic pathway, comprises a ring structure with a carbon-carbon double bond or triple bond among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives.14. A cell labeling kit comprising:{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'the cell labeling agent according to , and'}a reporter substance that binds to the sialic acid by reacting with the group presented outside the cell, wherein the group is not changed when metabolized by the sialic acid biosynthetic pathway. The present disclosure relates to a cell labeling agent and a cell labeling kit.Metabolic labeling methods are known to use the metabolism of monosaccharides by the sialic acid biosynthetic pathway to label sugar chains on the cell surface. In the metabolic labeling method, for example, a derivative of N-acetyl mannosamine (ManNAc) with an azide group (peracetylated N-azidoacetyl mannosamine, AcManNAz) is used. AcManNAz taken up into the cell is enzymatically deacetylated in the cytoplasm and is metabolized to the corresponding N-azidoacetylsialic acid (SiaNAz). SiaNAz is incorporated into the sialo sugar complex and then is presented to the cell surface along with ...

CONJUGATED ANTISENSE COMPOUNDS AND THEIR USE

Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the gomeric compounds are conjugated to N-Acetylgalactosamine or to N-Acetylgalactosamine anaologues. 1243-. (canceled)247. The compound of claim 245 , wherein Qis CH.248. The compound of claim 244 , wherein Ris CHN.249. The compound of claim 248 , wherein Qis CH.252. The compound of claim 250 , wherein Ris CHOH.254. The compound of wherein L comprises a phosphorus linking group claim 244 , NH claim 244 , or N(CH).256. The compound of claim 244 , wherein the oligomer is a modified oligonucleotide comprising at least one modified nucleoside comprising a modified base and/or a modified sugar moiety.257. The compound of having at least one modified nucleoside comprising a modified sugar moiety selected from a bicyclic sugar moiety and a 2′-substituted sugar moiety.258. The compound of claim 257 , comprising at least one 4′-C(CH)H—O-2′ or 4′-CH—O-2′bridged bicyclic sugar moiety.259. The compound of comprising at least one 2′-O(CH)OCHsubstituted sugar moiety.260. The compound of claim 244 , wherein the conjugate group is attached to the 5′-terminal nucleoside of the oligomer.261. The compound of claim 244 , wherein the conjugate group is attached to the 3′-terminal nucleoside of the oligomer.262. The compound of claim 244 , wherein the oligomer is an oligonucleotide and has a sugar motif comprising:a 5′-region consisting of 2-8 linked 5′-region nucleosides, wherein at least two 5′-region nucleosides are modified nucleosides and wherein the 3′-most 5′-region nucleoside is a modified nucleoside;a 3′-region consisting of 2-8 linked 3′-region nucleosides, wherein at least two 3′-region nucleosides are modified nucleosides and wherein the 5′-most 3′-region nucleoside is a modified nucleoside; anda central region between the 5′-region and the 3′-region consisting of 5-10 linked central region nucleosides, each independently selected from among: a modified nucleoside and an unmodified ...

2,3-Fluorinated Glycosides as Neuraminidase Inhibitors and Their Use as Anti-Virals

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza. 3. The compound of claim 1 , wherein T is COOH or COOR claim 1 ,{'sup': '1', 'sub': '1-10', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO, and'}wherein zero to five backbone carbons of the optionally substituted alkyl group are optionally and independently substituted with O, N or S.4. The compound of claim 1 , wherein T is C(O)OCH claim 1 , C(O)OCHCH claim 1 , C(O)OCHCHCH claim 1 , C(O)OCHCHCHCH claim 1 , C(O)OCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCHCH claim 1 , or COOH.5. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO.6. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , and OR claim 1 ,{'sup': '3', 'sub': '1-10', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}7. The compound of claim 1 , wherein A is F or Cl.8. The compound of claim 1 , wherein A is F.9. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO claim 1 , provided A and D are not both H.10. The compound of claim 1 , wherein D is selected from the group ...

Azacitidine process and polymorphs

Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form I and mixtures of azacitidine crystalline Forms I and II.

Liposomes Useful for Drug Delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

Improved peptide pharmaceuticals for insulin resistance

Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.

MOENOMYCIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF

The present invention provides compounds of Formula (I); or a pharmaceutically acceptable form thereof; wherein RR,R,R,R,R,R, and Rare as defined herein, and G is a group of Formula (a), (b), or (c): Formula (II), wherein X; X, X, X, X, X, X, Y, R, R, R, a, d, e, x, n, and m are as defined herein. The present invention further provides pharmaceutical compositions comprising a compound of Formula (I), kits comprising such compositions, methods of use and treatment, and preparative methods. 5. The compound of wherein G is a group of Formula (a).7. The compound of wherein G is a group of Formula (b).8. The compound of wherein at least one of X claim 7 , X claim 7 , X claim 7 , X claim 7 , X claim 7 , X claim 7 , and Xis halogen.9. The compound of wherein Xand Xare each hydrogen claim 7 , Xand Xare each fluoro claim 7 , and X claim 7 , X claim 7 , and Xare each fluoro.11. The compound of wherein G is a group of Formula (c).14. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or pharmaceutically acceptable form thereof claim 1 , and optionally a pharmaceutically acceptable excipient.15. A method of treating or preventing a bacterial infection comprising administering to a subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable form thereof.16. The method of claim 15 , wherein the bacterial infection being treated or prevented is caused by Gram-positive bacteria.17. (canceled)18. The method of claim 15 , wherein bacterial infection being treated or prevented is caused by Gram-negative bacteria.19. (canceled)20. The method of claim 15 , wherein bacterial infection being treated or prevented is caused by vancomycin-resistant bacteria.21. (canceled)22. The method of claim 15 , wherein bacterial infection being treated or prevented is caused by methicillin-resistant bacteria.23. (canceled)24. An in vitro method of inhibiting bacterial growth by contacting a bacterium with an effective amount of a compound ...

Liposomes Useful for Drug Delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention. 120-. (canceled)21. A pharmaceutical composition comprising irinotecan liposomes encapsulating irinotecan and a polyphosphate having 13-18 phosphate units per polyphosphate molecule , said composition having a molar ratio of irinotecan to total lipids ranging from 0.15:1 to 1.5:1.22. The composition of claim 21 , comprising a lecithin and cholesterol.23. The composition of claim 22 , wherein the lecithin:cholesterol molar ratio is 3:2.24. The composition of claim 21 , comprising DSPC and cholesterol in a 3:2 molar ratio.25. The composition of claim 21 , comprising DSPC claim 21 , cholesterol claim 21 , and an amphipathic polymer comprising a polyethylene glycol-lipid.26. The composition of claim 25 , comprising a polyethylene glycol phosphatidylethanolamine.27. The composition of claim 26 , wherein the polyethylene glycol phosphatidylethanolamine comprises a poly(ethylene glycol) moiety having a molecular weight ranging from about 250 to about 20 claim 26 ,000.28. The composition of claim 21 , comprising DSPC claim 21 , cholesterol claim 21 , and N-(methoxy-poly(ethylene glycol)-oxycarbonyl)-distearoylphosphatidylethanolamine claim 21 , in a molar ratio of 3:2:0.015.29. The composition of claim 21 , comprising DSPC claim 21 , cholesterol claim 21 , and methoxy-PEG (2000)-DSPE claim 21 , in a molar ratio of 3:2:0.015.30. The composition of claim 21 , comprising one or more phospholipids claim 21 , and wherein the liposomes encapsulate irinotecan and a polyphosphate having 13-18 phosphate units per polyphosphate molecule claim 21 , and the ratio of grams of irinotecan to moles of total phospholipids is (134.4±9.3):1.31. The composition of claim 21 , comprising one or more phospholipids claim 21 ...

USE OF CO2 FOR THE SYNTHESIS OF CYCLIC GLYCOCARBONATES AND LINEAR POLYGLYCOCARBONATES BY POLYCONDENSATION FROM GLYCANS

Provided herein are methods for synthesizing cyclic carbonates, glycocarbonates, and polyglycocarbonates by reacting polyol glycans with carbon dioxide. Synthesis can include selective polycondensation of polyol glycan hydroxyl moieties. 1. A method for making glycocarbonates , the method comprising reacting a polyol glycan with carbon dioxide , wherein the glycan comprises a closed chain structure.2. The method of claim 1 , wherein the polyol glycan comprises hexose.3. The method of claim 1 , wherein the polyol glycan comprises a pyranose moiety.4. The method of claim 1 , wherein the polyol glycan comprises a pyranoside.5. The method of claim 1 , wherein the polyol glycan comprises a polysaccharide moiety.6. The method of claim 1 , wherein the polyol glycan comprises a glycan derivative.7. The method of claim 1 , wherein reaction occurs in the presence of one or more solvents.8. The method of claim 7 , wherein the solvents are one or more of dibromomethane claim 7 , dimethylformamide claim 7 , and an ionic liquid.9. The method of claim 8 , wherein the ionic liquid comprises 1-Butyl-3-methylimidazolium hexafluorophosphate.10. The method of claim 1 , further comprising selectively protecting one or more hydroxyl moieties of the polyol glycan before reacting claim 1 , wherein the polyol glycan comprises at least three hydroxyl moieties.11. The method of claim 10 , wherein protecting comprises methylating.12. The method of claim 1 , wherein reacting is conducted in the presence of a catalyst.13. The method of claim 12 , wherein the catalyst comprises 1 claim 12 ,8-diazabicyclo [5.4.0] undec-7-ene.14. The method of claim 1 , wherein the method is free of phosgene claim 1 , phosgene derivatives claim 1 , and isocyanates.15. The method of claim 1 , wherein reacting is conducted at a pressure between about 1 bar and about 20 bar.16. The method of claim 1 , wherein reacting is conducted at a temperature of between about 60° F. and 80° F.17. The method of claim 1 , wherein ...

Sialic acid analogs

The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.

5-ALA DERIVATIVES AND USE THEREOF

The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis. 131-. (canceled)33. The derivative according to wherein n is 1.34. The derivative according to wherein n is 0.36. The 5-Aminolevulinic derivative according to wherein B is a biocompatible non-peptidic moiety cleavable by phosphatases or glycosidases.37. The derivative according to wherein B is a phosphate group.38. The derivative according to wherein B is at least one glucuronic acid group.40. The derivative according to wherein B is a group B1.41. The derivative according to claim 32 , wherein Ris H.42. The derivative according to claim 32 , wherein Ris an optionally substituted phenyl.43. The derivative according to claim 32 , wherein Ris a lipid group.44. The derivative according to wherein Ris a squalene.45. The derivative according to claim 32 , wherein B is a group B2.47. The derivative according to selected from the group consisting of:triethylammonium salt of hexyl 5-((hydroxy(phenoxy)phosphoryl)amino)-4-oxopentanoate;triethylammonium salt of methyl 5-((hydroxy(phenoxy)phosphoryl) amino)-4-oxopentanoatetriethylammonium salt of benzyl 5-((hydroxy(phenoxy)phosphoryl) amino)-4-oxopentanoate;hexyl 5-((hydroxy(((4E,8E,12E,16E)-4,8,13,17,21-pentamethyldocosa-4,8,12,16,20-pentaen-1-yl)oxy)phosphoryl)amino)-4-oxopentanoate;Bis(hexyl) 5-((hydroxy(phenoxy)phosphoryl)bis(amino)-4-oxopentanoate);Bis-hexyl 5-((hydroxy(((4E,8E,12E,16E)-4,8,13,17,21-pentamethyldocosa-4,8,12,16,20-pentaen-1-yl)oxy)phosphoryl)bis-amino)-4-oxopentanoate;hexyl 4-oxo-5-((((phosphonooxy)methoxy)carbonyl)amino)pentanoate;(2S,3S,4S,5R,6R)-6-(((4-((((5-(hexyloxy)-2,5-dioxopentyl)carbamoyl)oxy)methyl) phenyl)carbamoyl ...

SIALIC ACID ANALOGS

The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies. 177-. (canceled)92. A sustained release pharmaceutical composition comprising a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 , wherein:a) the release of the compound is over a period of about four hours or more; and/orb) the pharmacological effect from the compound lasts about four hours or more upon administration of the composition.93. A sustained release pharmaceutical composition comprising a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 ,wherein the composition, upon administration, provides a therapeutically effective amount of the compound for about 4 hours or more.94. A method for treating a sialic acid deficiency in a patient in need thereof comprising administering an effective amount of a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof.95. A method for treating a sialic acid deficiency in a patient in need thereof comprising administering a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof; wherein upon administration claim 78 , the compound claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 , continuously provides a therapeutically effective amount of sialic acid for about 4 hours to about 24 hours.96. The method of claim 94 , wherein the sialic acid deficiency is myopathy associated with sialic acid deficiency.97. The method of claim 96 , wherein the myopathy associated with sialic acid deficiency is Hereditary Inclusion Body Myopathy (HIBM) claim 96 , Nonaka myopathy claim 96 , or Distal Myopathy with Rimmed Vacuoles (DMRV). This application is a continuation of U.S. patent application Ser. No. 16/050,343, filed on Jul. 31, 2018, which is a continuation of U.S. patent application Ser. No. 14/944,779, filed on Nov. 18, 2015, now U.S. Pat. No. 10,065,981, ...

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. 2. The method of wherein said disorder is selected from the group consisting of pulmonary fibrosis claim 1 , liver fibrosis claim 1 , kidney fibrosis claim 1 , cancers claim 1 , autoimmune diseases claim 1 , metabolic disorders claim 1 , heart disease claim 1 , heart failure claim 1 , liver disorders claim 1 , and non-alcoholic steatohepatitis.3. The method of wherein said disorder is selected from the group consisting of carcinomas claim 1 , sarcomas claim 1 , leukemias claim 1 , lymphomas claim 1 , T-cell lymphomas claim 1 , and metastasising cancers.4. The method of wherein said disorder is selected from the group consisting of interstitial lung fibrosis claim 1 , liver cirrhosis claim 1 , autoimmune cirrhosis claim 1 , primary biliary cirrhosis claim 1 , hepatic impairment claim 1 , moderate hepatic impairment claim 1 , cardiovascular disorders claim 1 , cardiac fibrosis claim 1 , cardiac failure claim 1 , aortic stenosis claim 1 , and aortic stiffness.5. The method of wherein the mammal is a human.6. The method of wherein the compound of formula I is in amorphous form.7. The method of wherein the compound of formula I is administered in a pharmaceutical composition selected from tablets or capsules. This application is a continuation of U.S. patent application Ser. No. 17/018,713, filed Sep. 11, 2020, which is a continuation of U.S. patent application Ser. No. 15/535,829, filed Jun. 14, 2017, which is a national phase of International Patent Application No. PCT/EP2016/051836, filed Jan. 28, 2016, which ...

Modified saccharides, conjugates thereof, and their manufacture

Saccharide-protein conjugates having a new type of linker are described. The conjugates comprising the new linker are prepared from modified saccharides comprising a moiety of the formula (I): -A-N(R 1 )-L-M wherein: A is a bond, —C(O)— or —OC(O)—; R 1 is selected from H or C 1 -C 6 alkyl; L is a C 1 -C 12 alkylene group; and M is a masked aldehyde group. The new linker is especially useful for preparing conjugates of Neisseria meningitidis serogroup A saccharide. Conjugates having this new linker have improved immunogenicity compared to other types of conjugates.

Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of asgpr

Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.

Liposomes useful for drug delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Process for the preparation of certain triaryl rhamnose carbamates

Triaryl rhamnose carbamate insecticides are prepared from triaryl carbamates and the tetrahydropyran-2-ols in good yield without the use of a hydride base.

PROTECTED MONOMER AND METHOD OF FINAL DEPROTECTION FOR RNA SYNTHESIS

A method of deprotecting a solid support bound polynucleotide comprising at least one 2′-protected ribonucleotide in which a step of contacting the polynucleotide with a composition comprising a diamine is performed under conditions sufficient to deprotect and cleave the polynucleotide which remains retained on the solid support. 1. A method of deprotecting a polynucleotide bound to a solid support with a linker , the polynucleotide comprising at least one 2′-protected ribonucleotide having a phosphate protecting group , a 2′-protecting group , and optionally a nucleobase-protecting group; the method comprising:(a) contacting the solid support bound polynucleotide with a first composition comprising a phosphate deprotection reagent and removing the phosphate protecting group, thereby producing a first deprotected polynucleotide bound to the solid support;(b) contacting said first deprotected polynucleotide bound to the solid support with a second composition comprising a 2′-deprotection reagent and removing the 2′-protecting group, thereby producing a second deprotected polynucleotide bound to the solid support; and(c) after step (b) has been completed, contacting said second deprotected polynucleotide bound to the solid support with a third composition comprising a diamine in organic solvent, gas-phase or neat, and cleaving the linker and also removing the nucleobase protecting group, if present, and thereby producing a deprotected, cleaved polynucleotide which is retained on the solid support.2. The method of claim 1 , wherein the method further comprises:(d) washing the deprotected, cleaved polynucleotide retained on the solid support with an organic solvent; and(e) eluting the deprotected, cleaved polynucleotide from the solid support.3. The method of claim 1 , wherein said 2′-protecting group is selected from tertbutyldimethylsilyl (TBDMS) claim 1 , triisopropylsilyloxymethyl (TOM) and 2′-O-bis(2-acetoxyethoxy)methyl (ACE).4. The method of claim 1 , wherein the ...

GLYCOAMINO ACID AND USE THEREOF

An object of the present invention is to provide glycoamino acid as an amino acid precursor with improved properties (particularly water-solubility, stability in water, bitter taste etc.). The present invention relates to a compound represented by the formula (I): 2. The compound or salt according to claim 1 , wherein the sugar of said sugar residue wherein none of the hydroxyl groups are protected or modified for G is monosaccharide.3. The compound or salt according to claim 1 , wherein the sugar of said sugar residue wherein none of the hydroxyl groups are protected or modified for G is glucose claim 1 , glucosamine claim 1 , or N-acetylglucosamine.4. The compound or salt according to claim 1 , wherein the moiety represented by formula G-O— has a β-anomer structure.5. The compound or salt according to claim 1 , wherein the amino acid of said amino acid residue is an α-amino acid.6. The compound or salt according to claim 1 , wherein the amino acid of said amino acid residue is valine claim 1 , leucine claim 1 , or isoleucine.7. The compound or salt according to claim 1 , wherein the amino acid of said amino acid residue is phenylalanine claim 1 , tyrosine claim 1 , or 3 claim 1 ,4-dihydroxyphenylalanine.8. The compound or salt according to claim 1 , wherein R is a hydrogen atom.9. An aqueous composition claim 1 , comprising a compound represented by formula (I) or salt thereof according to .10. An oral preparation claim 1 , comprising a compound represented by formula (I) or salt thereof according to .11. A method of reducing a bitter taste of an amino acid claim 1 , comprising introducing a group represented by formula G-O—C(O)— claim 1 , wherein G is a sugar residue wherein none of the hydroxyl groups are protected or modified claim 1 , into an amino group of amino acid.12. The method according to claim 11 , wherein the sugar of said sugar residue wherein none of the hydroxyl groups are protected or modified for G is monosaccharide.13. The method according to ...

Neuraminidase Inhibitor Compounds, Compositions and Methods for the Use Thereof in Anti-Viral Treatments

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.

Cell-permeable probes for identification and imaging of sialidases

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.

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. 155.-. (canceled)58. The method of claim 56 , wherein the ASBTI decreases serum bile acid or hepatic bile acid levels in the patient by at least 20%.59. The method of claim 58 , wherein the ASBTI decreases serum bile acid or hepatic bile acid levels in the patient by at least 30%.60. The method of claim 58 , wherein the ASBTI decreases serum bile acid or hepatic bile acid levels in the patient by at least 40%.61. The method of claim 56 , wherein less than 10% of the ASBTI is systemically absorbed upon oral administration.62. The method of claim 56 , wherein the ASBTI is administered at a dosage between about 1 μg/kg/day and about 10 mg/kg/day.63. The method of claim 56 , wherein the ASBTI is administered at a dosage from about 5 μg/kg/day to about 1 mg/kg/day.64. The method of claim 56 , wherein the ASBTI is administered at a dosage from about 10 μg/kg/day to about 300 μg/kg/day.65. The method of claim 56 , wherein the ASBTI is administered at a dosage comprising from about 0.1 mg to about 40 mg of the ASBTI.66. The method of claim 56 , wherein the ASBTI decreases the levels of serum bile acids or hepatic bile acids claim 56 , reduces bilirubin claim 56 , reduces liver enzymes claim 56 , lowers intraenterocyte bile acids/salts claim 56 , or reduces necrosis and/or damage to hepatocellular architecture.67. The ...

Nutritional compositions with 2fl and lnnt for use in inducing a gut microbiota close to the one of breast fed infants

The present invention relates to a nutritional composition comprising at least one fucosylated oligosaccharide and at least one N-acetylated oligosaccharide for promoting or inducing a global gut microbiota that is closer to the one of infants fed exclusively with human breast milk, in comparison to infants fed with a conventional nutritional composition. The composition can be an infant formula and is in particular intended for infants between 0 and 12 months of age fed predominantly with infant formula. It promotes a healthy intestinal flora and has beneficial short and long terms effects.

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. 1. A composition for use in the treatment of hypercholemia comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of the composition comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.2. The composition for use in claim 1 , wherein the ASBTI decreases at least 20% of serum bile acid or hepatic bile acid levels in the patient.3. The composition for use in claim 1 , wherein less than 10% of the ASBTI is systemically absorbed.5. The composition for use in claim 4 , wherein:q is 1;n is 2;{'sup': 'x', 'sub': 3', '2, 'Ris N(CH);'}{'sup': 7', '8, 'Rand Rare independently H;'}{'sup': 1', '2, 'Rand Ris alkyl;'}{'sup': 3', '4, 'Ris H, and Ris OH;'}{'sup': 5', '6', '9', '9', '9', '9', '9, 'sub': 2', '3', 'z', 'z, 'Ris H, and Ris selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycle, quaternary heterocycle, quarternary heteroaryl, OR, SR, S(O)R, SOR, SOR, and -L-K;'}wherein z is 1, 2 or 3; each L is independently a substituted or unsubstituted alkyl, a substituted or unsubstituted heteroalkyl, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aminoalkyl group, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl ...

LIPOSOMES USEFUL FOR DRUG DELIVERY

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention. 1. A pharmaceutical composition comprising irinotecan sucrose octasulfate precipitated in a matrix comprising one or more phospholipids , wherein the matrix has a size of approximately 110 nm and comprises a total of 500-550 mg irinotecan base per mmol of total phospholipids.2. The liposome composition of claim 1 , wherein the matrix comprises DSPC and cholesterol.3. The liposome composition of claim 2 , wherein the matrix comprises DSPC claim 2 , cholesterol. and PEG-DSPE in a molar ratio of 3:2:0.015.4. The liposome composition of claim 1 , wherein the matrix comprises a total of 500 mg irinotecan base per mmol of total DSPC and PEG-DSPE.5. The liposome composition of claim 4 , wherein the matrix comprises DSPC claim 4 , cholesterol claim 4 , and PEG-DSPE in a molar ratio of 3:2:0.015.6. The liposome composition of claim 1 , wherein the matrix comprises a PEGylated lipid.7. A pharmaceutical composition comprising irinotecan sucrose octasulfate within a matrix comprising one or more phospholipids and having a size of approximately 110 nm claim 1 , wherein the composition comprises a total of 500-550 mg irinotecan base per mmol of total phospholipids in the matrix claim 1 , wherein at least 90% of the irinotecan in the pharmaceutical composition is in the irinotecan sucrose octasulfate within the matrix.8. The liposome composition of claim 7 , wherein the matrix comprises a PEGylated lipid.9. The composition of claim 8 , wherein the irinotecan sucrose octasulfate is precipitated within the matrix from irinotecan hydrochloride and sucrose octasulfate triethylammonium.10. The composition of claim 9 , wherein the irinotecan sucrose octasulfate is precipitated within the matrix.11. The liposome ...

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. 2. At least one chemical entity of wherein Ris phenyl substituted with{'sub': 6', '2', '11', '12', '6', '1', '6, 'a first group of the formula —Z—Rwherein Z is chosen from —O—, —S—, —S(O)—, —S(O)—, and —CRR—; and Ris chosen from hydrogen, optionally substituted C-Calkyl, optionally substituted cycloalkyl, and optionally substituted heterocycloalkyl, and'}a second group chosen from halo and lower alkyl optionally substituted with halo.3. At least one chemical entity of wherein Z is —O—.4. At least one chemical entity of wherein Z is —S—.5. At least one chemical entity of wherein Z is —S(O)—.6. At least one chemical entity of wherein Z is —CRR.7. At least one chemical entity of wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , ethyl claim 1 , 2 claim 1 ,2 claim 1 ,2-trifluoro-1-methyl-ethyl claim 1 , isopropyl claim 1 , (S)-sec-butyl claim 1 , (R)-sec-butyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , 2-morpholin-4-yl-ethyl claim 1 , 2-piperidin-1-yl-ethyl claim 1 , pyrrolidin-3-yl claim 1 , and tetrahydro-furan-3-yl.8. ...

5-ALA DERIVATIVES AND USE THEREOF

The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis. 2. The method according to claim 1 , wherein the said disorder is a malignant claim 1 , pre-malignant or non-malignant skin disorder.3. The method according to claim 1 , wherein the said disorder is an infectious diseases (e.g. viral claim 1 , bacterial claim 1 , fungal infections).4. The method according to claim 1 , wherein said compound is administered topically claim 1 , orally or systemically.5. The method according to claim 1 , wherein said method further comprises a step of administering in said subject a metal ion or a radioisotope of said metal ion before the step of exposing to light.6. The method according to claim 1 , wherein n is 1.7. The method according to claim 1 , wherein n is 0.9. The method according to claim 1 , wherein B is a biocompatible non-peptidic moiety cleavable by phosphatases or glycosidases.10. The method according to claim 1 , wherein B is a phosphate group.11. The method according to claim 1 , wherein B is at least one glucuronic acid group.13. The method according to claim 1 , wherein B is a group B1.14. The method according to claim 1 , wherein Ris H.15. The method according to claim 1 , wherein Ris an optionally substituted phenyl.16. The method according to claim 1 , wherein Ris a lipid group.17. The method according to claim 12 , wherein Ris a squalene.18. The method according to claim 1 , wherein B is a group B2.20. The method according to claim 1 , wherein the compound is selected from the following group:triethylammonium salt of hexyl 5-((hydroxy(phenoxy)phosphoryl)amino)-4-oxopentanoate;triethylammonium salt of methyl 5-((hydroxy(phenoxy) ...

LINCOMYCIN BIOSYNTHETIC INTERMEDIATES, METHOD FOR PREPARATION, AND USE THEREOF

Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation. 5. Use of the compound of claim 1 , or a pharmaceutically acceptable salt thereof as a raw material for preparing n-propyl proline claim 1 , disaccharide GlcN-Ins claim 1 , Mycothiol or ergothione.6. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and an optional carrier.7Streptomycin lincolnensis. A microbial strain claim 1 , wherein the microbial is claim 1 , and in the strain claim 1 , one or more genes selected from a group consisting of the following have been inactivated or knocked out:lmbE, lmbE3457, lmbV, mshA, mshC, lmbC, lmbD, lmbN, and lmbF.8. The strain of claim 7 , wherein in the strain claim 7 , lmbE and/or lmbE3457 genes are inactivated or knocked out; and/orthe lmbV, mshA and/or mshC genes are inactivated or knocked out; and/orthe lmbC, lmbD and/or lmbN genes are inactivated or knocked out; and/orthe lmbF gene are inactivated or knocked out.9. A preparation method of an intermediate compound claim 7 , wherein the method comprises the following steps:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'i': 'Streptomyces lincolnensis.', '(a) Using the compound of or a pharmaceutically acceptable salt thereof as a raw material for hydrolysis reaction to produce the intermediate compound, wherein the compound or a pharmaceutically acceptable salt thereof is derived from a fermentation product of'}10. The method of claim 9 , wherein in the step (a) claim 9 , one or more selected from a group consisting of the compounds of Formula I1 claim 9 , Formula I2 claim 9 , and Formula I5 are subjected to hydrolysis reaction to generate n-propyl ...

COMPOUNDS AND COMPOSITIONS FOR THE DETECTION AND TREATMENT OF ALZHEIMER'S DISEASE AND RELATED DISORDERS

One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of .4. The method of claim 3 , wherein the amyloidosis-associated pathological condition is Alzheimer's disease.5. A method for treating a subject suffering from an amyloidosis-associated pathological condition claim 3 , comprising the step of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering a therapeutically effective amount of a compound of .'}6. The method of claim 5 , wherein the amyloidosis-associated pathological condition is Alzheimer's disease. This application is a continuation of U.S. patent application Ser. No. 13/903,362, filed May 28, 2013, which is a continuation of U.S. patent application Ser. No. 12/933,139, now U.S. Pat. No. 8,450,466, issued May 28, 2013, which is the U.S. National Stage of International Patent Application No. PCT/US2009/037928, filed Mar. 23, 2009, which claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 61/038,571 filed Mar. 21, 2008, each of which is hereby incorporated by reference in its entirety.Millions of Americans suffer from dementia and other cognitive deficits as a result of Alzheimer's disease (AD), a neurodegenerative disease. Due to its occurrence in the brain, it is difficult to diagnose the condition and ...

MOENOMYCIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF

The present invention provides compounds of Formula (I): 124-. (canceled)28. The method of claim 25 , wherein G is a group of formula (a).32. The method of claim 25 , wherein G is a group of formula (b).33. The method of claim 32 , wherein at least one of X claim 32 , X claim 32 , X claim 32 , X claim 32 , X claim 32 , X claim 32 , and Xis halogen.34. The method of claim 33 , wherein Xand Xare each hydrogen claim 33 , Xand Xare each fluoro claim 33 , and X claim 33 , X claim 33 , and Xare each fluoro.37. The method of claim 25 , wherein G is a group of Formula (c).41. The method of claim 25 , wherein step (ii) comprises removing the moenocinol chain claim 25 , followed by removal of the phosphoglycerate linker.42. The method of claim 41 , wherein step (ii) comprises removing Ring A and Ring D of moenomycin A claim 41 , followed by removing the moenocinol chain claim 41 , followed by removal of the phosphoglycerate linker.43. The method of claim 25 , wherein step (ii) comprises removing the moenocinol chain using a Lewis acid.44. The method of claim 25 , wherein step (ii) comprises removing the phosphoglycerate linker using a base. The present application is a continuation of and claims priority under 35 U.S.C. §120 to U.S. patent application, U.S. Ser. No. 14/390,811, filed Oct. 6, 2014, which is a national stage filing under 35 U.S.C. §371 of international PCT application, PCT/US2013/035416, filed Apr. 5, 2013, which claims priority under 35 U.S.C. §119(e) to U.S. provisional patent application, U.S. Ser. No. 61/621,161, filed Apr. 6, 2012, which is incorporated herein by reference.This invention was made with U.S. Government support under grant GM066174 awarded by the National Institutes of Health. The U.S. Government has certain rights in the invention.Bacteria have the ability to generate resistance to antibiotics through lateral gene transfer, mutation of enzymes, or the expression of enzymes which actively pump the antibiotic out of the cell or break it down. ...

Neuraminidase Inhibitor Compounds, Compositions and Methods for the Use Thereof in Anti-Viral Treatments

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza. 3. The compound of claim 1 , wherein T is COOH or COOR claim 1 ,{'sup': '1', 'sub': '1-20', 'claim-text': {'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}, 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}4. The compound of claim 1 , wherein T is C(O)OCH claim 1 , C(O)OCHCH claim 1 , C(O)OCHCHCH claim 1 , C(O)OCHCHCHCH claim 1 , C(O)OCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCHCH claim 1 , or COOH.5. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO.6. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , C claim 1 , and OR claim 1 ,{'sup': '3', 'sub': '1-20', 'claim-text': {'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}, 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}7. The compound of claim 1 , wherein A is F or Cl.8. The compound of claim 1 , wherein A is F.9. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO claim 1 , provided A and D are not both H.10. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , and Cl claim 1 , provided A and D are not both H.11. The compound of claim ...

PROCESS FOR THE PREPARATION OF CERTAIN TRIARYL RHAMNOSE CARBAMATES

Triaryl rhamnose carbamate insecticides are prepared from triaryl acyl azides and tetrahydropyran-2-ols in good yield without the use of a hydride base. 2. The process of in which Ris a (C-C)fluoroalkoxy group.3. The process of in which Ris CHCH claim 1 , CHCHCHor CHCH═CH.4. The process of in which the isocyanate of Formula (III) is prepared and used in situ.5. The process of or in which the anhydrous aprotic solvent and the polar aprotic solvent are a mixture of an aromatic hydrocarbon and a nitrile.6. The process of in which the anhydrous aprotic solvent and the polar aprotic solvent are a mixture of toluene and acetonitrile. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/837203 filed Jun. 20, 2013, the entire disclosure of which is hereby expressly incorporated by reference.The present invention concerns an improved process for preparing certain triaryl rhamnose carbamates.U.S. Pat. No. 8,178,658 describes, inter alia, certain triaryl rhamnose carbamates and their use as insecticides. One of the methods used to prepare such triaryl compounds is by way of a the following 2 step processwhereinRrepresents (C-C)haloalkyl or (C-C)haloalkoxy, andRrepresents (C-C)alkyl, (C-C)alkenyl, or (C-C)alkynyl,in which a triaryl acyl azide is converted to an isocyanate followed by reaction with a tetrahydropyran-2-ol and a strong base to give the triaryl rhamnose carbamate pesticide. However, the reaction of the triaryl carbamate with the tetrahydropyran-2-ol requires the use of a strong hydride base, provides an anomeric mixture of alpha and beta products, and gives rise to urea and aniline by-products. It would be desirable to have a process in which the triaryl acyl azide and the tetrahydropyran-2-ol could be coupled in good yield without the use of a hydride base. It would also be desirable to reduce the amount of by-product formation and to provide a predominance of the preferred anomeric isomer.The present invention provides such ...

GLYCOSAMINOGLYCAN ESTER AND APPLICATION THEREOF

A new biomaterial is disclosed. The biomaterial is prepared by mixing glycosaminoglycan with a phosphoric acid, phosphate ester, or salt or derivative thereof under the action of a catalyst in a liquid reaction medium at a pH of 2.1 to 4.9. The obtained material is capable of enhancing the immunological resistance in human and in animals, treating diseases in human and in animals caused by viruses or bacteria, strengthening the anti-stress ability of animals, improving the appetite of animals, promoting the growth of animals, inhibiting the growth of tumor, lowering blood fat level, as well as preventing and treating viral diseases in plants. 210-. (canceled)11. A method of enhancing the immune resistance in human and animals claim 1 , treating diseases in human and in animals caused by viruses or bacteria claim 1 , strengthening the anti-stress ability of animals claim 1 , improving the appetite of animals claim 1 , promoting the growth of animals claim 1 , inhibiting the growth of tumor claim 1 , reducing blood lipid level and preventing and controlling viral diseases of plants comprising administering the ester of aminoglycan in to a human claim 1 , animal claim 1 , or plant in need thereof.12. (canceled)13. The method according to claim 11 , wherein the diseases in human or in animals comprise diseases harmful to human health claim 11 , diseases caused by viruses claim 11 , diseases caused by influenza virus claim 11 , diseases caused by hepatitis A virus claim 11 , diseases caused by hepatitis B virus claim 11 , diseases caused by hepatitis C virus claim 11 , diseases caused by HIV claim 11 , diseases caused by herpes virus; cancerous diseases; diseases harmful to animals claim 11 , viral and bacterial diseases harmful to livestock claim 11 , poultry claim 11 , aquatic product of fish claim 11 , shrimp and crab claim 11 , avian influenza claim 11 , swine influenza claim 11 , picornvirus disease claim 11 , saprolegniasis claim 11 , and streptococcusis. The ...

Liposomes Useful for Drug Delivery

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention. 1. A composition comprising a liposome in a medium , said liposome having an interior space separated from the medium by a membrane comprising one or more lipids , wherein the interior space of said liposome contains a substituted ammonium having a formula{'br': None, 'sub': 1', '2', '3', '4, 'sup': '+', 'R—(R—)N(—R)—R'}{'sub': 1', '2', '3', '4', '1', '2', '3', '4, 'wherein N is an ammonium nitrogen atom, each of R, R, R, Ris independently a hydrogen atom or an organic group having each independently not more than 8 carbon atoms, and in totality not more than 18 carbon atoms inclusive, wherein at least one of R, R, R, Ris an organic group;'}wherein the organic group is independently alkyl, alkylidene, heterocyclic alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl, or a hydroxy-substituted derivative thereof, optionally including a S, O, or N atoms forming an ether, ester, thioether, amine, or amide bond; and{'sub': 1', '2', '3', '4, 'wherein at least three of R, R, R, Rare the organic groups; or at least one of the organic groups has a secondary or tertiary carbon atom directly linked to the ammonium nitrogen atom; and'}wherein said interior space also comprises an anion.2. The composition of wherein the organic groups independently each have not more than 6 carbon atoms.3. The composition of wherein the organic groups have in totality not more than 16 carbon atoms.4. The composition of wherein the organic groups have in totality not more than 12 carbon atoms.5. The composition of wherein said substituted ammonium forms a true solution in water.6. The composition of wherein substantially all said substituted ammonium is contained within said interior space of the liposome.7. The composition of ...

COMPOUNDS AND COMPOSITIONS FOR THE DETECTION AND TREATMENT OF ALZHEIMER'S DISEASE AND RELATED DISORDERS

One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera. 12-. (canceled)4. The method of claim 3 , wherein the amyloidosis-associated pathological condition is Alzheimer's disease.57-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/903,362, filed May 28, 2013, which is a continuation of U.S. patent application Ser. No. 12/933,139, now U.S. Pat. No. 8,450,466, issued May 28, 2013, which is the U.S. National Stage of International Patent Application No. PCT/US2009/037928, filed Mar. 23, 2009, which claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 61/038,571 filed Mar. 21, 2008, each of which is hereby incorporated by reference in its entirety.Millions of Americans suffer from dementia and other cognitive deficits as a result of Alzheimer's disease (AD), a neurodegenerative disease. Due to its occurrence in the brain, it is difficult to diagnose the condition and to determine its cause without dangerous brain biopsy. Scientists believe that as many as 4.5 million Americans suffer from AD. AD usually begins after age 60 and its risk goes up with age. The cause of AD is unknown and, at present, no cure has been found.AD can only be definitely confirmed after an autopsy, which prevents early accurate diagnosis and treatment of the condition. Neuropathologically, AD is characterized by ...

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. 2. The compound of claim 1 , wherein A is selected from formula 2 wherein R-Rare independently selected from H claim 1 , F claim 1 , methyl optionally substituted with a F claim 1 , and OCHoptionally substituted with a F.3. The compound of claim 1 , wherein A is selected from formula 2 wherein Rand Rare selected from H and R-Rare selected from F or wherein R-Rare all F or wherein Rand Rare F and R claim 1 , Rand Rare H claim 1 , or wherein Rand Rare F and R claim 1 , Rand Rare H claim 1 , or wherein Ris F and R claim 1 , R-Rare H claim 1 , or wherein Rand Rare F claim 1 , Ris OCH claim 1 , and Rand Rare H.4. The compound of claim 1 , wherein A is selected from formula 3 wherein Hetis selected from a six membered heteroaromatic ring claim 1 , optionally substituted with a group selected from Br claim 1 , F claim 1 , and Cl.5. The compound of claim 1 , wherein A is selected from formula 3 wherein Hetis selected from a pyridinyl substituted with a F claim 1 , such as 3 F.6. The compound of claim 1 , wherein A is selected from formula 4 wherein Ris selected from Calkyl optionally substituted with a halogen claim 1 , and branched Calkyl claim 1 , such as CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , isopropyl and CHCF.7. The compound of claim 1 , wherein A is selected from formula 5 wherein Ris selected from phenyl optionally substituted with a group selected from Br claim 1 , F claim 1 , Cl claim 1 , methyl optionally substituted with a F claim 1 , and OCHoptionally substituted with a F.8. The compound of claim 1 , ...

Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy

A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.

Derivatives of oleandomycin class and method for their preparing

FIELD: organic chemistry, antibiotics, chemical technology, pharmacy. SUBSTANCE: invention relates to new compounds of macrolide antibiotic oleandomycin class of the general formula (I): wherein R 1 represents separately the group -CH 2 CH 3 , the group of the formula (II) that represents in common with R 2 the group of the formula (III) or in common with R 4 represents the group of the formula (IV) or the group of the formula (V) R 2 in common with R 3 represents ketone, or in common with R 1 represents the group of the formula (III); R 3 represents hydroxy-group (OH) separately or in common with R 2 represents ketone; R 4 represents methyl group separately or in common with R 1 represents group of the formula (IV) or group of the formula (V); R 5 represents hydrogen atom separately or benzyloxycarbonyl group; R 6 represents hydrogen atom, methyl group or benzyloxycarbonyl group separately, and to their pharmaceutically acceptable inorganic or organic acid salts. These compounds are intermediate substances for preparing structural analogues of chimeric oleandomycin with the simplified structure of the left part of its molecule that elicit the powerful antibacterial effect. Invention provides preparing new derivatives of oleandomycin class used in producing antibacterial agents. EFFECT: improved preparing method, valuable medicinal properties. 12 cl, 12 ex ОЕЗУЗСС ПЧ сэ (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ "” 2 234 510. (51) МПК? 13) С2 С 07Н 17/04 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 2001121147/04, 29.12.1999 (24) Дата начала действия патента: 29.12.199911.1-12 (30) Приоритет: 30.12.1998 НВ Р980646А (43) Дата публикации заявки: 10.07.2003 (46) Дата публикации: 20.08.2004 (56) Ссылки: КУ 2052263 С1 20.01.1996. 4$ 2757123 А 31.07.1956. СВ 985734 А 10.03.1965. (85) Дата перевода заявки РСТ на национальную фазу: 30.07.2001 (86) Заявка РСТ: НК 99/00035 (29.12.1999) (87) Публикация РСТ: М/О 00/40589 (13.07.2000) ...

Production of carrageenan and carrageenan products

The Methods of the present invention prepare carrageenan products from processed seaweed material using shear stress treatment are disclosed. The carrageenan products comprise at least about 65% by weight of carrageenan and at least about 2% by weight of acid insoluble material. The carrageenan products of the present invention preferably have an onset of hydration below about 40° C. and a color of greater than about 74 *L units. The carrageenan products of the present invention are useful as components in food products, such as, dairy products, meats, and dessert gels as well as non-food products, such as, toothpaste formulations, cosmetics, and paints.

Protected monomer and method of final deprotection for rna synthesis

A nucleoside monomer that is protected by a thionocarbamate protecting group is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.

Protected monomers and methods of deprotection for rna synthesis

A nucleoside monomer that is protected by a thionocarbamate protecting group is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.

Inhibitors of histone deacetylase

This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein (B), Q, J, L and Z are as defined in the specification.

Histone deacetylase inhibitors

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to compounds presented by formula (IV) or to their pharmaceutically acceptable salts: , wherein: R 140 specified in a group consisting of: H and halo; xa and xb mean the numbers each of which is independently specified in 0, 1 and 2; R 150 and R 160 are independently specified in a group consisting of H, halo, -CN, -CF 3 , -OCF 3 , -C 1 -C 6 alkyl, -C 1 -C 6 alkoxyl, -O-C 2 -C 6 alkyl-O-R 53 , -OR 53 , -C 0 -C 6 alkyl-S(O) 0-2 -R 53 , -C 0 -C 6 alkyl-C(O)NR 50 R 51 , -C 0 -C 6 alkyl-heterocyclyl wherein heterocyclyl is monocyclic and contains 6 atoms, and one or two atoms are independently specified in O and N; R 50 and R 51 and R 53 are independently specified in a group consisting of -C 1 -C 6 alkyl. EFFECT: developing a pharmaceutical composition, a method for histone deacetylase inhibition and a method of treating a polyglutamate disease wherein the polyglutamate disease is Huntington's disease. 8 cl, 332 ex, 10 tbl, 91 dwg

糖链天冬酰胺衍生物的制备方法

本发明提供糖链天冬酰胺衍生物的制备方法。按照该制备方法，与以前相比能够非常容易且大量地得到医药品开发等领域中有用的各种分离的糖链天冬酰胺衍生物。另外，本发明还提供通过上述糖链天冬酰胺衍生物的制备工序制备糖链天冬酰胺的方法以及制备糖链的方法。而且，本发明还提供新型的糖链天冬酰胺衍生物、糖链天冬酰胺和糖链。

Пестицидные композиции

Описываются новые гетероарил-N-арил-карбаматы общей формулы где: Ar 1 - фенил, возможно замещенный C 1 -C 6 галогеналкилом или C 1 -C 6 галогеналкокси; Het - триазолил; Ar 2 - фенил; X 1 представляет собой О или S; X 2 - О; R4 - Н или C 1 -C 6 алкил; n=0, 1 или 2; и R1, R2 и R3 независимо выбирают из Н, CN, C 1 -C 6 алкила, C 1 -С 6 галогеналкила, С 3 -С 6 циклоалкила, C 2 -C 6 алкенила, C 2 -C 6 алкинила, C(=O)O(C 1 -C 6 алкил)а, фенила и Het-1, где Het-1 - 5-членное ненасыщенное гетероциклическое кольцо, содержащее один гетероатом, выбранный из серы или кислорода, или 6-членное ненасыщенное гетероциклическое кольцо, содержащее один атом азота в качестве гетероатома, и Het-1 может быть замещен F, Cl, C 1 -C 6 алкилом, C 1 -C 6 галогеналкилом или C 1 -C 6 алкокси, и способ борьбы с насекомыми-вредителями Lepidoptera или Homoptera с использованием этих соединений в качестве инсектицидов и акарицидов. 3 н. и 2 з.п. ф-лы, 2 табл., 80 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 249/08 C07D 401/12 C07D 403/12 C07D 405/12 C07D 409/12 C07D 413/12 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 417/12 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A01N 43/64 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 532 470 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012108617/04, 05.08.2010 (24) Дата начала отсчета срока действия патента: 05.08.2010 (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИС ЭлЭлСи (US) 07.08.2009 US 61/232,142 (43) Дата публикации заявки: 20.09.2013 Бюл. № 26 R U Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ЛАМБЕРТ Уилльям (US), КРАУЗ Гари (US), СПАРКС Томас (US), КАДУОРТ Дениз (US) (45) Опубликовано: 10.11.2014 Бюл. № 31 2 5 3 2 4 7 0 (56) Список документов, цитированных в отчете о поиске: US 6 417 187 B2 09.07.2002 (см. прод.) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 07.03.2012 (86) Заявка PCT: US 2010/044538 (05.08.2010) (87) Публикация заявки PCT: 2 5 3 2 4 7 0 R U C 2 C 2 WO 2011/017513 (10.02.2011) ...

TIGOGENIN β-CELLOBIOSIDES

FIELD: organic chemistry. SUBSTANCE: product: tigogenin 6-b-cellobiosides of the general formula (I) (image), where R R 4 CO where R 4 -C 1 -C 4 -alkyl; R 1 and R 2 are separately taken R 1 -R 4 CO where R 4 as indicated above; R 2 a group of the formula (II) (image) or R 1 and R 2 together mean a residue of the formula (III) (image) where R 4 as indicated above. R and R 1 are preferably acetyl, and R 4 methyl. EFFECT: improved method of synthesis. 8$ ЭСУОбОсС ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) 13) ВИ” 2042 688 ' (БТ) ть С° С 074 21000 СЛ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 4830049/04, 12.06.1990 (30) Рпогйу: 13.06.1989 Ц$ 365588 (46) Рае ог рибИсаНоп: 27.08.1995 (71) АррИсапе: Р\атег К. (0$) (72) пуетог. — Ргейпк Отвоп УгБап[у$] (73) Ргорпеюг: Рарег пк. (05) (54) ПСОСЕММ В-СЕТЕОВОЗЮЕ$ (57) АБзГасЕ: НЕЕО: огдапс спетгу. ЗОВЗТАМСЕ: ргоЧис: Чдодепт 6-6-сейорюзаез о Ше депега! Гогтуа (Г) (таде), мпеге В В.СО мпеге К4-С41-Сла-аку; К ап9 КВ ае зерагаеу 1акеп К1-К4СО \мПпеге К аз паса ароуе; К2 а агоир о Ше югт\а (|1) (таде) ог К. апа В> юдейег теап а гез4ие о! {Ле Гогтша (!!!) (таде) мпеге Кл аз паса ароуе. К апя К.А аге ргаегаыу асеу|, апа К. тешу|. ЕРЕЕСТ: тргоуеа теоа ог зутПез. ОВ 2042688 С1 КО 8$ ЭСУОбОсС ПЧ ГЭ Изобретение относится к новым и благоприятным способам синтеза тигогенин В-целлобиозида и некоторым НОВЫМ промежуточным соединениям, используемым в этих способах. Тигогенин В -целлобиозид представляет собой известное соединение, имеющее пригодной при лечении (гипер) холестеринемии и атеросклероза [1 и 2] Каждый патент раскрывает различный синтез этого соединения из В -целлобиозоктаацетата; первый посредством гептаацетата гликолилбромида, который сопрягают с тигогенином в присутствии карбоната серебра последующим гидролизом; а второ посредством катализируемого четыреххлористым оловом сопряжения октаацетата с тигогенином в метиленхлориде, вновь с последующим гидролизом. В работе Малиноу и др. взаимодействие целлобиозоктаацетата с ...

Pesticidal compositions

본원에 개시된 본 발명은 살충제 및 해충 조절에서의 그들의 용도 분야에 관한 것이다. 아래의 구조를 갖는 화합물이 개시된다. The present invention disclosed herein relates to the field of pesticides and their use in pest control. Compounds having the following structure are disclosed.

Novel derivatives from class of oleandomycin

本发明涉及来自具有通式(Ⅰ)的大环内酯物抗生素竹桃霉素类的新化合物,其中R 1 单独是指－CH 2 CH 3 基团或式(Ⅱ)片段,和R 2 一起是式(III)片段,或者和R 4 一起是式(Ⅳ)片段或式(Ⅴ)片段,R 2 和R 3 一起是酮,或者和R 1 一起是式(III)片段,R 3 单独是指OH基团,或者和R 2 一起是酮,R 4 单独是指甲基,或者和R 1 一起是式(IV)片段或式(V)片段,R 5 单独是指氢或苯甲氧基羰基,R 6 单独是指氢、甲基或苯甲氧基羰基,本发明还涉及用于制备这些化合物的中间体,制备它们的方法以及它们与无机或者有机酸形成的可药用加成盐。

Liposomes used for delivery of medications

FIELD: medicine, pharmaceutics. SUBSTANCE: in claimed invention it suggested are liposome compositions, which contain substituted ammonia and/or polyanion and, optionally, desirable therapeutic agent or expressing contrast substance. EFFECT: invention provides efficient method of obtaining liposome compositions. 141 cl, 40 tbl, 74 ex, 47 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 424 792 (13) C2 (51) МПК A61K A61K A61K A61K A61K A61K A61K ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ,A61K A61K ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ A61K (12) ОПИСАНИЕ 9/00 (2006.01) 9/127 (2006.01) 45/08 (2006.01) 47/36 (2006.01) 47/30 (2006.01) 47/10 (2006.01) 9/50 (2006.01) 47/44 (2006.01) 36/24 (2006.01) 31/4375 (2006.01) A61K 31/337 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы): ХОНГ Килунг (US), ДРЮММОНД Дэрил С. (US), КИРПОТИН Дмитрий В. (US) (21)(22) Заявка: 2006142766/15, 02.05.2005 (24) Дата начала отсчета срока действия патента: 02.05.2005 (73) Патентообладатель(и): ХЕРМЕС БАЙЕСАЙЕНСИЗ, ИНК. (US) R U Приоритет(ы): (30) Конвенционный приоритет: 03.05.2004 US 60/567,921 (43) Дата публикации заявки: 20.06.2008 Бюл. № 17 2 4 2 4 7 9 2 (45) Опубликовано: 27.07.2011 Бюл. № 21 (56) Список документов, цитированных в отчете о поиске: US 5785987 А, 28.07.1998. US 6110491, 29.08.2000. RU 98116122 А, 27.06.2000. 2 4 2 4 7 9 2 R U (86) Заявка PCT: US 2005/015349 (02.05.2005) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 04.12.2006 (87) Публикация заявки РСТ: WO 2005/107712 (17.11.2005) Адрес для переписки: 119019, Москва, Гоголевский б-р, 11, 3 этаж, Московское представительство фирмы "Гоулингз Интернэшнл Инк.", В.Н.Дементьеву (54) ЛИПОСОМЫ, ИСПОЛЬЗУЕМЫЕ ДЛЯ ДОСТАВКИ ЛЕКАРСТВЕННЫХ СРЕДСТВ (57) Реферат: В настоящем изобретении предлагаются липосомные композиции, содержащие замещенный аммоний и/или полианион и, необязательно, желаемый терапевтический агент или отображающее контрастное вещество. Настоящее изобретение также обеспечивает способы получения липосомных ...

Inhibitors of histone deacetylase

本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体而言，本发明提供了式(I)化合物 其中

Single tin organic compound, preparation method and application thereof

本申请提供一种单锡有机化合物，用于合成蔗糖‑6‑羧酸酯，所述化合物为下述式(1)表示的化合物：式(1) 其中，R 1 、R 2 和R 3 分别独立地表示C1～C8的直链或支链饱和烷基、C2～C8的直链或支链不饱和烷基、C3～C8的取代或未取代的饱和环烷基、C3～C8的取代或未取代的不饱和环烷基、或C6～C12的芳基或取代芳基；R 4 表示C1～C6的直链或支链饱和烷基或C6～C12的芳基或取代芳基。本申请的单锡有机化合物，使得在合成蔗糖‑6‑羧酸酯过程中，能够准确地进行计量加料，同时提高催化剂回收率、减少后续氯化副反应的发生，且反应较快、能耗小、单位体积内收率更高。

Protein kinase c. modulators. d.

Compositions having protein kinase C-modulatory, anti-inflammatory and other activities are disclosed. The compounds are derived from aromatic heterocyclic compounds of the indole, indene, benzofuran and benzothiophene class.

Glycosaminoglycan (GAG) MIMETICS

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2006 126 718 (13) A (51) ÌÏÊ C07H 5/10 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006126718/04, 21.12.2004 (71) Çà âèòåëü(è): ÏÐÎÄÆÅÍ ÈÍÄÀÑÒÐÈÇ ËÈÌÈÒÅÄ (AU) (30) Êîíâåíöèîííûé ïðèîðèòåò: 23.12.2003 AU 2003907107 (43) Äàòà ïóáëèêàöèè çà âêè: 27.01.2008 Áþë. ¹ 3 (87) Ïóáëèêàöè PCT: WO 2005/061523 (07.07.2005) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Ã.Á. Åãîðîâîé, ðåã.¹ 513 A (54) ÌÈÌÅÒÈÊÈ ÃËÈÊÎÇÀÌÈÍÎÃËÈÊÀÍΠ(GAG) (57) Ôîðìóëà èçîáðåòåíè R U A 2 0 0 6 1 2 6 7 1 8 1. Ñîåäèíåíèå ôîðìóëû ãäå êàæäûé Õ íåçàâèñèìî îçíà÷àåò ÑÍ2, Ñ(Î), N, O, S, S(O), S(O)2 èëè ñâ çü è êàæäûé R1-R5 íåçàâèñèìî îçíà÷àåò ñâ çü èëè âûáèðàþò èç ãðóïïû, âêëþ÷àþùåé âîäîðîä; ãàëîãåí; àçèä: ãðóïïó R, îïðåäåë åìóþ êàê Ñ1-Ñ8 àëêèë èëè àëêåíèë, àðèë èëè ãåòåðîàðèë, êîòîðà äîïîëíèòåëüíî íåîá çàòåëüíî çàìåùåíà ãðóïïàìè àëêîêñè, àðèëîì, ãåòåðîàðèëîì èëè àðèëîêñè; -ÑÎÎÍ, -S(O)2OH; -S(O)2OH, -S(O)OH, -S(O)R, S(O)2R, -S(O)2NH2, -S(O)2OR, -S(O)OR; -C(O)R; ãåòåðîöèêëè÷åñêóþ ãðóïïó, êîòîðà äàëåå çàìåùåíà àëêèëîì, àðèëîì, -ÑÍ2NHC(O)R, -CH2N(C(O)R)2 èëè -CH2OR; Ñòðàíèöà: 1 RU 2 0 0 6 1 2 6 7 1 8 (86) Çà âêà PCT: AU 2004/001800 (21.12.2004) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 24.07.2006 (72) Àâòîð(û): ÄÎÍ Ðîáåðò Õüþ (AU), ÔÅÐÐÎ Âèòî (AU), ÁÈÒÂÝÉ ßí (AU), ÊÎØÐÀÍ Ñèñêà (AU), ÔÝÉÐÂÅÒÅÐ Äæîí Êðþãåð (AU), ÕÝÌÌÎÍÄ Ýäâàðä Òèìîòè (AU), ÊÀÐÎËÈ Òîìèñëàâ (AU), ËÈ Öàé Ïèí (AU), ËÈÓ Ëèãóí (AU) 2 0 0 6 1 2 6 7 1 8 R U A Ñòðàíèöà: 2 2 0 0 6 1 2 6 7 1 8 ãäå ïî êðàéíåé ìåðå îäíà, íî íå áîëåå äâóõ ãðóïï èç R7-R11 íåçàâèñèìî ïðåäñòàâë åò ñîáîé ñòðóêòóðó ôîðìóëû I; ãäå Y íåçàâèñèìî îçíà÷àåò ñâ çü, Í, R èëè -Ñ(Î)R, êàê îïðåäåëåíî âûøå; è ïî êðàéíåé ìåðå îäíà, íî íå áîëåå ãðóïïà èç R7-R11 íåçàâèñèìî ïðåäñòàâë åò ñîáîé ñòðóêòóðó ôîðìóëû II, ëèáî êàæäà ãðóïïà èç R7-R11 îòñóòñòâóåò íåçàâèñèìî îò äðóãèõ ãðóïï; èëè ...

DERIVATIVES OF 1,4-BENZOTIAZEPINE-1,1-DIOXIDE, METHOD FOR PRODUCING THEREOF, MEDICINE CONTAINING THESE COMPOUNDS AND THEIR APPLICATION AS HYPOLIPIDEMIC AGENTS

1. Соединение формулы A ! ! а также его фармацевтически приемлемые соли. ! 2. Фармацевтическая композиция, содержащая соединение по п.1 и по меньшей мере одно другое биологически активное вещество. ! 3. Композиция по п.2, отличающаяся тем, что в качестве другого биологически активного вещества оно содержит одно или несколько соединений, нормализующих липидный обмен. ! 4. Композиция по п.2 или 3, отличающаяся тем, что в качестве других биологически активных веществ она содержит одно или несколько веществ, выбранных из антидиабетических средств, гипогликемических биологически активных веществ, средств против ожирения, анорексигенных средств, ингибиторов HMGCoA-редуктазы, ингибиторов резорбции холестерина, агонистов гамма PPAR, агонистов альфа PPAR, агонистов альфа/гамма PPAR, фибратов, ингибиторов MTP, ингибиторов CETP, полимерных адсорберов желчных кислот, индукторов рецепторов LDL, ингибиторов ACAT, антиоксидантов, ингибиторов липопротеин-липазы, ингибиторов ATP(АТФ)цитрат-лиазы, ингибиторов сквален-синтетазы, антагонистов липопротеина(a), ингибиторов липазы, инсулина, сульфонилмочевины, бигуанидов, меглитинидов, тиазолидиндионов, ингибиторов α-глюкозидазы, биологически активных веществ, действующих на ATP (АТФ)-зависимый калиевый канал бета-клеток, агонистов CART, агонистов NPY, антагонистов рецептора 1 каннабиноида, антагонистов рецептора MCH, агонистов MC4, агонистов орексина, агонистов H3, агонистов TNF, агонистов CRF, антагонистов CRFBP, производных GLP1, агонистов урокортина, агонистов β3, агонистов MSH (меланоцито-стимулирующего гормона), агонистов CCKA, ингибиторов восстановления серотонина, смешанных серотонин- и норадренергических соединени (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2008 105 756 (13) A (51) МПК C07D 281/10 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2008105756/04, 13.07.2006 (71) Заявитель(и): САНОФИ-АВЕНТИС ДОЙЧЛАНД ГМБХ (DE) (30) Конвенционный приоритет: ...

Oligosaccharide heparin fragments as inhibitors of complement cascade

L'invention concerne des composés d'oligosaccharide présentant une activité anticomplément analogue à celle de l'héparine ainsi qu'une activité d'anticoagulant réduite comparée à celle de l'héparine sur une base pondérale ou molaire. Les composés d'oligosaccharide comportent au moins 5 et pas plus de 25 unités saccharide. Les oligosaccharides peuvent avoir un nombre égal d'unités saccharide avec un sucre de terminaison non réducteur, ou un nombre impair d'unités saccharide sous un sucre de terminaison non réducteur. L'invention concerne également des compositions pharmaceutiques d'anticomplément présentant une activité secondaire d'anticoagulant réduite, ainsi qu'un processus de préparation des composés d'oligosaccharide. Disclosed are oligosaccharide compounds exhibiting heparin-like anticomplement activity as well as reduced anticoagulant activity compared to heparin on a weight or molar basis. Oligosaccharide compounds have at least 5 and no more than 25 saccharide units. Oligosaccharides can have an equal number of saccharide units with a non-reducing terminating sugar, or an odd number of saccharide units under a non-reducing terminating sugar. The invention also relates to anticomplement pharmaceutical compositions having reduced anticoagulant side activity and to a process for the preparation of the oligosaccharide compounds.

Glucuronide prodrugs of Janus kinase inhibitors

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2019 142 472 A (51) МПК C07D 487/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2019142472, 22.05.2018 (71) Заявитель(и): ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи (US) Приоритет(ы): (30) Конвенционный приоритет: 23.05.2017 US 62/509,847 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.12.2019 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2018/217700 (29.11.2018) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (57) Формула изобретения 1. Соединение формулы I: A где R1 представляет собой водород или C1-3 алкил; W1 выбран из: R U 2 0 1 9 1 4 2 4 7 2 (54) ГЛЮКУРОНИДНЫЕ ПРОЛЕКАРСТВА ИНГИБИТОРОВ ЯНУС-КИНАЗЫ 2 0 1 9 1 4 2 4 7 2 US 2018/033818 (22.05.2018) R U (43) Дата публикации заявки: 24.06.2021 Бюл. № 18 (72) Автор(ы): ЛОНГ, Дэниэл Д. (US), УИЛТОН, Донна А.А. (US), ЛУ, Менди (US), ХАДСОН, Райан (US), БРЭССИЛ, Патрик Дж. (US) Стр.: 1 и и A1 выбран из: (a) группы, имеющей формулу (i): 2 0 1 9 1 4 2 4 7 2 и B1 выбран из C6-10 арила, C1-9 гетероарила, C3-10 циклоалкила и C2-9 гетероциклической группы; где гетероарильная группа содержит от 1 до 4 гетероатомов, выбранных из азота, кислорода и серы; арильная или гетероарильная группа является незамещенной или замещена 1-3 заместителями, независимо выбранными из C1-4 алкила, C1-3 алкокси, амино, циано, галогена, гидрокси, нитро и трифторметила; гетероциклическая группа содержит от 1 до 3 гетероатомов, выбранных из азота, кислорода и серы; и циклоалкильная или гетероциклическая группа является незамещенной или замещена 1-4 заместителями, независимо выбранными из C1-4 алкила, C1-3 алкокси, гидрокси и трифторметила; (c) группы, имеющей формулу (iii): где d равно 2 или 3; e равно 0 или 1; R4 представляет собой водород или C1-3 алкил; и B2 выбран из C6-10 арила, C1-9 гетероарила, C3-10 циклоалкила и C2-9 гетероциклической группы; где ...

Liposomal compositions used for drug delivery

Группа изобретений относится к области медицины, а именно к противоопухолевой иринотекановой липосомной композиции, содержащей иринотекан сахарозооктасульфат, инкапсулированный в липидные везикулы, содержащие один или более фосфолипидов, причем липосомная композиция содержит суммарное количество в диапазоне от 150 до 550 мг основания иринотекана на ммоль суммарных фосфолипидов, а также относится к противоопухолевой иринотекановой липосомной композиции, содержащей липосомы, в которых инкапсулирован иринотекан в форме соли, выбранной из пирофосфата, трифосфата и инозитгексафосфата, причем указанная композиция содержит лецитин, холестерин и амфипатический полимер, и указанная композиция имеет от около 0,15 до около 1,5 моль иринотекана на моль суммарного липида, также относится к противоопухолевой иринотекановой липосомной композиции, содержащей липидные везикулы, в виде липосомной дисперсии, где в липидных везикулах инкапсулирован иринотекан и сахарозооктасульфат, так что иринотекан и сахарозооктасульфат образуют гель или осадок в виде соли, причем указанная композиция содержит лецитин, холестерин и амфипатический полимер, и указанная композиция имеет от около 0,15 до около 1,5 моль иринотекана на моль суммарного липида, также относится к противоопухолевой иринотекановой липосомной композиции, содержащей липосому в водной среде, причем липосома содержит 1,2-дистеароил-SN-фосфатидилхолин, холестерол и N-(омега-метоксиполи(этиленгликоль)оксикарбонил)-1,2-дистеароилфосфатидилэтаноламин в мольном соотношении 3:2:0,015, и внутри липосомы захвачены иринотекан и сахарозооктасульфат. Группа изобретений обеспечивает создание липосомных композиций, которые не только обладают исключительной способностью к инкапсуляции вещества, но также обеспечивают улучшенную стабильность указанного инкапсулированного вещества, например лекарственного средства, и препятствуют его преждевременному высвобождению из липосомы в живом организме. 5 н. и 17 з.п. ф-лы, 47 ил., 40 табл., 74 пр. ...

Prodrugs, their preparation and use as medicines

Liposomes useful for drug delivery

SUGAR AMINO SULFURIC ACID ESTERS, THEIR USE, A PROCEDURE TO PREPARE THEM, AND A MEDICINAL PRODUCT CONTAINING THEM

El presente invento se refiere a nuevos ésteres de ácido sulfúrico de amino azúcares de las fórmulas generales (Ia), (Ib) y (Ic), en donde: B es alquilenoinferior o un sistema de anillo aromático opcionalmente sustituido; G1, G2 y y G3 son cada uno, independientemente, un radical de un glicopiranósido,una glicopiranosa o un derivado respectivo, estando por lo menos un grupo hidroxi del radical G1, G2 ó G3 esterificado con ácido sulfúrico, y sus salesfarmacéuticamente utilizables. Los ésteres son apropiados como sustancias terapéuticamente activas para el tratamiento de trastornos que se distinguenpor proliferación excesiva o destructiva de células del músculo liso y cambios arterioescleróticos frente a la pared vascular. Además, el presenteinvento se refiere al uso de dichos ésteres o de sus sales como medicamentos, especialmente para el tratamiento y/o profilaxis de trastornos que sedistinguen por proliferación excesiva o destructiva de células de músculo liso y cambios arterioescleróticos frente a la pared vascular y, respectivamente,para la producción de medicamentos correspondientes. Asimismo, el presente invento se refiere a un procedimiento para preparar dichos ésteres y unmedicamento que loscontiene. The present invention relates to new sulfuric acid esters of amino sugars of the general formulas (Ia), (Ib) and (Ic), wherein: B is lower alkylene or an optionally substituted aromatic ring system; G1, G2 and and G3 are each, independently, a radical of a glycopyranoside, a glycopyranose or a respective derivative, at least one hydroxy group of the radical G1, G2 or G3 being esterified with sulfuric acid, and their pharmaceutically usable salts. Esters are suitable as therapeutically active substances for the treatment of disorders distinguished by excessive or destructive proliferation of smooth muscle cells and arteriosclerotic changes against the vascular wall. Furthermore, the present invention relates to the use of said esters or their salts as medicaments, ...

Process for producing sugar chain asparagine derivative

본 발명은 당쇄 아스파라긴 유도체의 제조 방법을 제공한다. 이 제조 방법에 의하면 의약품 개발 등의 분야에서 유용한 각종 단리된 당쇄 아스파라긴 유도체를 종래에 비하여 매우 용이하고 또한 대량으로 얻을 수 있다. 또 본 발명은 상기 당쇄 아스파라긴 유도체의 제조 공정을 통하는, 당쇄 아스파라긴의 제조 방법 및 당쇄의 제조 방법을 제공한다. 또한 본 발명은 신규 당쇄 아스파라긴 유도체, 당쇄 아스파라긴 및 당쇄를 제공한다. The present invention provides a method for preparing a sugar chain asparagine derivative. According to this production method, various isolated sugar chain asparagine derivatives useful in the fields of drug development and the like can be obtained very easily and in large quantities. Moreover, this invention provides the manufacturing method of sugar chain asparagine, and the manufacturing method of sugar chain through the manufacturing process of the said sugar chain asparagine derivative. The present invention also provides novel sugar chain asparagine derivatives, sugar chain asparagine and sugar chains.

Cell-permeable probes for identification and imaging of sialidases

Provided herein are compounds for use as sialidase inhibitors, including alkynyl-3-fluorosialyl fluoride. The compounds, which include the compound DFSA, function by trapping a 3-fluorosialylenzyme intermediate (reporter-inhibitor-enzyme conjugate). These compounds can be conjugated with a detectable tagging moiety for isolation and identification of sialidases.

Chitosamine derivative, its composition and its medical usage

本发明提供式(A)化合物及其药学上可接受的盐和酯，以及其药物组合物，所述化合物及其药物组合物在用于制备预防或治疗哺乳动物关节及骨骼疾病如关节炎及骨质疏松症的药物中的用途。

Method of producing theophylline derivatives

Cell-permeable probes for sialidase identification and imaging

Photoacid generator, photoresist comprising the photoacid generator, and coated article comprising same

화학식 (I)을 갖는 화합물: 상기 식에서, R 1 은 각각 독립적으로 H 또는 인접 R 1 에 임의로 결합된, 치환되거나 미치환된 C 1 -30 지방족 그룹이고, R 2 및 R 3 는 각각 독립적으로 H, F, C 1 -10 알킬, C 1 -10 플루오로알킬, C 3 -10 사이클로알킬 또는 C 3 -10 플루오로사이클로알킬이며(여기에서 적어도 하나의 R 2 및/또는 R 3 는 F를 함유한다), L 1 , L 2 및 L 3 는 각각 독립적으로 단일 결합, 또는 임의로 락톤 그룹을 포함하는 C 1 -20 결합 그룹이며(여기에서 하나 이상의 L 1 , L 2 및 L 3 는 임의로 고리 구조를 형성하고, 하나 이상의 L 1 , L 2 및 L 3 는 폴리머화 C 2 -20 알파-베타 불포화 유기그룹으로 임의로 치환된다), X는 에테르, 에스테르, 카보네이트, 아민, 아미드, 우레아, 설페이트, 설포네이트, 또는 설폰아미드 함유 그룹이고, Z + 는 유기 또는 무기 양이온이고, a는 각각 독립적으로 0 내지 12의 정수이고, b는 0 내지 5의 정수이며, c, d, 및 r은 각각 독립적으로 0 또는 1이며, p는 0 내지 10의 정수이고, q는 1 내지 10의 정수이다. 포토레지스트는 포토애시드 발생제를 포함하고 코팅된 물품은 포토레지스트를 포함한다. 포토레지스트를 사용하여 장비를 형성할 수 있다. A compound having the formula (I): Wherein R 1 is each independently a substituted or unsubstituted C 1 -30 aliphatic group optionally bonded to H or adjacent R 1 , R 2 and R 3 are each independently H, F, C 1 -10 alkyl , (at least one of R 2 and / or R 3 here is contained F) to -10 C 1 fluoroalkyl, C 3 -10 cycloalkyl or C 3 -10 cycloalkyl, fluoroalkyl, L 1, L 2 And L < 3 > are each independently a single bond or, optionally, a C 1 -20 bond group comprising a lactone group, One or more of L 1 , L 2 and L 3 optionally form a cyclic structure and at least one of L 1 , L 2 and L 3 is optionally substituted with a polymerized C 2 -20 alpha -beta unsaturated organic group; X is an ether , ester, carbonate, amine, amide, urea, sulfate, and sulfonate, or sulfonamide-containing group, Z + is an organic or inorganic cation, and, a is each independently an integer from 0 to 12, b is from 0 to 5 C, d, and r are each independently 0 or 1, p is an integer of 0 to 10, and q is an integer of 1 to 10. The photoresist comprises a photoacid generator and the coated article comprises a photoresist. Photoresists can be used to form the equipment.

Filantstatine antitumor

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Liposomes useful for drug delivery

본 발명은 치환된 암모늄 및/또는 다중음이온을 함유하고, 경우에 따라 목적하는 치료제 또는 영상화 물질을 함유하는 리포좀 조성물을 제공한다. 본 발명은 또한 본 발명에 의해 제공되는 리포좀 조성물의 제조 방법을 제공한다. The present invention provides liposome compositions containing substituted ammonium and / or polyanions and optionally containing the desired therapeutic or imaging material. The present invention also provides a process for preparing the liposome composition provided by the present invention.

Isothiazolopyridine-2-carboxamides and their use as pharmaceuticals

본 발명은 화학식 I의 치환 이소티아졸로[5,4-b]피리딘-2-카복사미드 (화학식에서, R1, R2, R3, R10, R11 및 X는 청구범위에 정의된 것과 같음)에 관한 것이다. 화학식 I의 화합물은 트랜스글루타미나제의 억제제, 특히 트랜스글루타미나제 2(TGM2)의 억제제이며, 예를 들면, 골관절염과 같은 퇴행성 관절증 등 다양한 질환의 치료에 적합하다. 본 발명은 또한 화학식 I의 화합물의 제조 방법, 약제로서의 상기 화합물의 용도, 및 상기 화합물을 포함하는 약학적 조성물에 관한 것이다.

Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of asgpr

Thiocarbon-protecting groups for RNA synthesis

Aspects of the invention include 2'-protected nucleoside monomers that are protected at the 2'-site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.

Pesticidal compositions

FIELD: chemistry. SUBSTANCE: claimed invention relates to novel compounds, which have the following structural formula: , where radicals Ar 1 , Ar 2 , Het, J, K, L, R1-R4 have values, given in the description, which possess pesticidal action. Invention also relates to methods of applying said compounds on seeds, on locus for fighting pests such as Lepidoptera, on plants and by peroral introduction to or application on animals. EFFECT: obtaining compounds possessing pesticidal action. 21 cl, 7 tbl, 91 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07H 13/12 C07H 15/18 C07H 15/26 A01N 43/40 A01N 43/50 A01N 43/653 ФЕДЕРАЛЬНАЯ СЛУЖБА A01N 47/02 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A01N 47/18 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 513 723 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2010137808/04, 11.02.2009 (24) Дата начала отсчета срока действия патента: 11.02.2009 12.02.2008 US 61/065,475 (43) Дата публикации заявки: 20.03.2012 Бюл. № 8 (45) Опубликовано: 20.04.2014 Бюл. № 11 2336272 C1 20.10.2008. RU 2255934 C2 10.07.2005. RU 2308452 C2 20.10.2007 (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 13.09.2010 (86) Заявка PCT: 2 5 1 3 7 2 3 (56) Список документов, цитированных в отчете о поиске: WO 9847894 A1 29.10.1998. RU R U Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): КРАУЗ Гари (US), СПАРКС Томас (US), МАКЛЕД КаСандра (US), ДЕМЕТЕР Дэвид (US), БРАЙАН Кристи (US), БРАУН Аннетт (US), ДЭНТ Уилльям (US), КАДУОРТ Дениз (US), НАДЖЕНТ Джейм (US), ХАНТЕР Рики (US), САМАРИТОНИ Джек (US) WO 2009/102736 (20.08.2009) Адрес для переписки: 129090, Москва, ул. Большая Спасская, 25, стр. 3, ООО "Юридическая фирма "Городисский и Партнеры" (54) ПЕСТИЦИДНЫЕ КОМПОЗИЦИИ (57) Реферат: Данное изобретение относится к новым соединениям, имеющим следующую структурную формулу: R U 2 5 1 3 7 2 3 (87) Публикация заявки PCT: C 2 C 2 US 2009/033711 (11.02. ...

Prodrugs and methods for their preparation

본 발명은 글라이코실-스페이서-약물 화합물(선구약물), 이의 제조방법 및 약제로서의 이의 용도에 관한 것이다. The present invention relates to glycosyl-spacer-drug compounds (precursor drugs), their preparation and their use as medicaments.

Conjugated antisense compounds and their use

Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the gomeric compounds are conjugated to N -Acetylgalactosamine or to N -Acetylgalactosamine analogues.

Lipid analogs or their pharmaceutically acceptable salts

FIELD: organic chemistry. SUBSTANCE: product: lipid analogs of the general formula (I): where: R 1 - OH, ; R 2 - where: R 6 and R 7 - H, F; R 8 - H, OH or tetradecanoyloxy; - tetradecanoyl or R 9 where: R 10 - H, F; R 4 - H, OH, tetradecanoyloxy or 2,2-difluorotetradecanoyloxy; - OH, R< and at least one of groups R 4 and - group R 5 ; R 2 - OH, F at condition that exception of case when at least one of R 3 and R 2 - tetradecanoyl substituted with F or at least one substituent of the group: F, OH, tetradecanoyloxy, or at least one of R 3 and R 4 - tetradecanoyl substituted with at least one fluoro-substituted tetradecanoyloxy-group, or their pharmaceutically acceptable salts. Synthesized compounds were used as immunoregulating and immunostimulating preparations. EFFECT: improved method of synthesis. 6 cl, 4 tbl 41019140Сс ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2076 107. (51) МПК 13) Сл С 07Н 5/06 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5052656/04, 09.09.1992 (30) Приоритет: 11.12.1989 УР 1-321153 20.02.1990 УР 2-37339 (46) Дата публикации: 27.03.1997 (56) Ссылки: Сагфопуагае Кезеагсй. спет. 6 (4), 625-638 (1987). Сагропуагае Кезеагсп, 162 (1987), 127-140. (62) Первичная заявка, из которой выделена настоящая: 4830600/04 (71) Заявитель: Санкио Компани Лимитед (.Р) (72) Изобретатель: Масао Сиозаки[Р], Нобору Исида[Р], Томово Кобаяси[/Р], Тетсуо Хираока[/Р], Масами Араи[/Р], Юзуру Акаматсу[/Р], Масахиро Нисидзима[/Р] (73) Патентообладатель: Санкио Компани Лимитед (Р) (54) АНАЛОГИ ЛИПИДА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ (57) Реферат: Использование: В иммунорегулирующих и иммуностимулирующих препаратов. Сущность: продукт: аналоги липида общей формулы |: качестве 1 сн о 5 2 52 = с с 4 2 Е и в \ нк | з ОЕ 6 о Е 1 и 2 | Е -он, 0-Р-ОН к -с-с -Сн-<СН,>, -Сн, | и [3 15 он о Е Е ле Вби В’- НЕ В _Н ОН или тетрадеканоилокси, КЗ - тетрадеканоил или _-С-СН-СН -ССН —_СН и 1з 10 2 10 3 ов Е де В? - Н, Е В - Н; ОН ПРИЕМЛЕМЫЕ СОЛИ ...

Inhibitors of histone deacetylase

本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体而言，本发明提供了式(I)化合物，其中式(1)、Q、J、L及Z均如本说明书中的定义。

Liposomes useful for drug delivery

Glucosamine derivative, composition thereof and medical application thereof

本发明提供式(A)化合物及其药学上可接受的盐和酯，以及其药物组合物，所述化合物及其药物组合物在用于制备预防或治疗哺乳动物关节及骨骼疾病如关节炎及骨质疏松症的药物中的用途。

Nitrosourea derivative and its preparation

Indole and indazole compounds that activate ampk

The present invention relates to indole and indazole compounds of Formula (I) Formula (I) that activate 5' adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.

ISOTHIAZOLOPYRIDIN-2-CARBOXAMIDES AND THEIR APPLICATION AS PHARMACEUTICAL AGENTS

1. Соединение формулы I, в любой из его стереоизомерных форм или смеси стереоизомерных форм в любом отношении, или его фармацевтически приемлемая соль,в которойX выбран из ряда, состоящего из =N-и =N(O)-;R1, R2 и R3 независимо друг от друга выбраны из ряда, состоящего из водорода, галогена, (C-C)-алкила,(C-C)-алкил-O-, нитро, циано,(C-C)-алкил-O-C(O)-, R4-N(R5)-C(O)- и R6-N(R7)-S(O)-;R4 выбран из ряда, состоящего из водорода, (C-C)-алкила,(C-C)-циклоалкила,(C-C)-циклоалкил-(C-C)-алкила-, фенила, фенил-(C-C)-алкила-, Het1 и Het1-(C-C)-алкила-, причем Het1 в случае необходимости замещен одним или более одинаковыми или разными заместителями R8;R5, R6 и R7 независимо друг от друга выбраны из ряда, состоящего из водорода, (C-C)-алкила,(C-C)-циклоалкила и(C-C)-циклоалкил-(C-C)-алкила-;R8 выбран из ряда, состоящего из галогена, (C-C)-алкила, гидрокси, оксо,(C-C)-алкил-O- и циано;R10 выбран из ряда, состоящего из водорода, (C-C)-алкила,(C-C)-циклоалкила,(C-C)-циклоалкил-(C-C)-алкила- и(C-C)-алкил-O-(C-C)-алкила-, при условии, что R10 может быть только водородом, если X обозначает =N(O)-;R11 выбран из ряда, состоящего из (C-C)-алкила, который в случае необходимости замещен одним или более одинаковыми или разными заместителями R12,(C-C)-циклоалкила, который в случае необходимости замещен одним или более одинаковыми или разными заместителями R13, и Het2, который в случае необходимости замещен одним или более одинаковыми или разными заместителями R14, и причем Het2 присоединен через кольцевой атом углерода;или группы R10 и R11, вместе с атомом азота, несущим их, образуют 4-12-членный моноциклический или бициклический, насыщенный или частично ненасыщенный гетероцикл, который, в дополнение к атому азота, несущему R10 и R11, включает 0, 1 или 2 дополнительных кольцевых гетероатома, выбранных из ряда, состоящего из азота, кислорода и серы, который в случае необходимости замещен на кольцевых атомах углерода одним ил РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 513/04 (13) 2014 ...

The method of obtaining derivatives of glucose

Photoacid generator, photoresist comprising the photoacid generator, and coated article comprising same

Process for preparing nitroso urea derivatives

Nutrient compositions with 2fl and lnnt for use in inducing intestinal microbiota, which is similar to intestinal microbiota of infants in breastfeeding

FIELD: food industry. SUBSTANCE: invention relates to a nutritional composition. Nutritional composition contains 2'-fucosyllactose (2'FL) as a fucosylated oligosaccharide and N-lacto-N-neotetraose (LNnT) as the acetylated oligosaccharide for stimulation and/or induction in the infants or young children of the general intestinal microbiota, which is similar to general intestinal microbiota in infants or young children, exclusively breastfed by human milk, as compared to the general intestinal microbiota in infants or young children fed mainly or exclusively with a traditional nutrient composition without said oligosaccharides. EFFECT: invention provides healthy intestinal flora formation and has a favorable effect in the short and long term. 19 cl, 8 dwg, 5 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 724 590 C2 (51) МПК A61K 31/7028 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/7028 (2020.02) (21)(22) Заявка: 2018107583, 04.08.2016 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): СОСЬЕТЕ ДЕ ПРОДЮИ НЕСТЛЕ С.А. (CH) Дата регистрации: 25.06.2020 04.08.2015 EP 15179742.0 (43) Дата публикации заявки: 05.09.2019 Бюл. № 25 (45) Опубликовано: 25.06.2020 Бюл. № 18 (56) Список документов, цитированных в отчете о поиске: WO 2012092155 А1, 05.07.2012. US 20130251844 А1, 26.09.2013. WO 2015071402 А1, 21.05.2015. WO 2009060073 А1, 14.05.2009. WO 2012158517 А1, 22.11.2012. RU 2462252 C2, 27.09.2012. (85) Дата начала рассмотрения заявки PCT на национальной фазе: 05.03.2018 2 7 2 4 5 9 0 Приоритет(ы): (30) Конвенционный приоритет: R U 04.08.2016 (72) Автор(ы): БЕРГЕР Бернард (CH), ШПРЕНГЕР Норберт (CH) EP 2016/068597 (04.08.2016) C 2 C 2 (86) Заявка PCT: (87) Публикация заявки PCT: R U 2 7 2 4 5 9 0 WO 2017/021476 (09.02.2017) Адрес для переписки: 101000, Москва, ул. Мясницкая, д. 13, стр. 5, ООО "Союзпатент" (54) ПИТАТЕЛЬНЫЕ КОМПОЗИЦИИ С 2FL И LNNT ДЛЯ ПРИМЕНЕНИЯ ПРИ ...

Antibacterial compound nitrate salts

FIELD: medicine, pharmacy. SUBSTANCE: invention relates to nitrate salts of cefazolin, ampicillin, clindamycin, ciprofloxacin and nitroxy-derivative of metronidazole that can be used as antibacterial medicinal agents, in particular, as antiviral, antifungal and antibacterial medicinal agents. EFFECT: valuable medicinal properties of antibacterial compounds. 5 cl, 2 tbl, 21 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 288 231 (13) C2 (51) ÌÏÊ C07D 501/59 (2006.01) A61P 31/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2002120480/04, 16.01.2001 (30) Êîíâåíöèîííûé ïðèîðèòåò: 26.01.2000 IT MI 2000 A 000092 (73) Ïàòåíòîîáëàäàòåëü(è): ÍÈÊÎÊÑ Ñ.À. (FR) (43) Äàòà ïóáëèêàöèè çà âêè: 27.04.2004 R U (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 16.01.2001 (72) Àâòîð(û): ÄÅËÜ ÑÎËÄÀÒÎ Ïüåððî (IT), ÁÅÍÅÄÈÍÈ Ôðàí÷åñêà (IT), ÀÍÒÎÃÍÀÖÖÀ Ïàòðèöè (IT) (45) Îïóáëèêîâàíî: 27.11.2006 Áþë. ¹ 33 2 2 8 8 2 3 1 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: RU 2071963 C1, 20.01.1997. WO 93/20812 A, 28.10.1993. WO 90/07325 A, 12.07.1990. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 26.08.2002 Àäðåñ äë ïåðåïèñêè: 121087, Ìîñêâà, à/ 33, Â.Â.Êóðûøåâó (54) ÍÈÒÐÀÒÍÛÅ ÑÎËÈ ÀÍÒÈÌÈÊÐÎÁÍÛÕ ÑÎÅÄÈÍÅÍÈÉ (57) Ðåôåðàò: Íàñòî ùåå èçîáðåòåíèå îòíîñèòñ ê íèòðàòíûì ñîë ì öåôàçîëèíà, àìïèöèëëèíà, êëèíäàìèöèíà, öèïðîôëîêñàöèíà, ñóëüôàìåòîêñàçîëà è íèòðîêñèïðîèçâîäíîãî ìåòðîíèäàçîëà, êîòîðûå ìîãóò áûòü èñïîëüçîâàíû â êà÷åñòâå àíòèìèêðîáíûõ ëåêàðñòâåííûõ ñðåäñòâ, â îñîáåííîñòè àíòèâèðóñíûõ, ïðîòèâîãðèáêîâûõ è àíòèáàêòåðèàëüíûõ ëåêàðñòâåííûõ ñðåäñòâ. 2 í. è 3 ç.ï. ô-ëû, 2 òàáë. R U 2 2 8 8 2 3 1 (87) Ïóáëèêàöè PCT: WO 01/54691 (02.08.2001) C 2 C 2 (86) Çà âêà PCT: EP 01/00430 (16.01.2001) Страница: 1 RU RUSSIAN FEDERATION RU (19) (11) 2 288 231 (13) C2 (51) Int. Cl. C07D 501/59 (2006.01) A61P 31/04 (2006.01) FEDERAL SERVICE FOR INTELLECTUAL PROPERTY, PATENTS AND TRADEMARKS (12) ABSTRACT OF INVENTION (21 ...

New benzyl-substituted derivatives 1, 4-benzothiepin-1, 1-dioxide

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to compounds of formula I, as well as to their physiologically acceptable salts wherein: X means NH; R1 means (C 1 -C 6 )-alkyl; R2 means OH; R2' means H; R5' means (C 1 -C 6 )-alkylene-O-S(O) 2 -R6; R3, R3 ' , R4, R4' and R5 independently mean H, OH, (C 1 -C 6 )-alkylene-O-S(O) p -R6, O-(CH 2 ) m -phenyl; at least one of the radicals R3, R3', R4, R4' and R5 has the value -O-(CH 2 ) m -phenyl; R6 means OH; m=1; p=2. EFFECT: compounds can find application in medicine, eg as lipid-lowering agents. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 456 282 (13) C2 (51) МПК C07D C07H A61K A61K A61P A61P ФЕДЕРАЛЬНАЯ СЛУЖБА A61P ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P A61P (12) ОПИСАНИЕ 409/12 (2006.01) 5/06 (2006.01) 31/38 (2006.01) 31/7028 (2006.01) 3/06 (2006.01) 3/10 (2006.01) 9/10 (2006.01) 25/18 (2006.01) 25/28 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2009122470/04, 30.10.2007 (24) Дата начала отсчета срока действия патента: 30.10.2007 (56) Список документов, цитированных в отчете о поиске: US 20040087648 A1, 06.05.2004. WO 03018024 A1, 06.03.2003. US 5994391 A, 30.11.1999. RU 2220141 C2, 27.12.2003. EA 4650 В1, 24.06.2004. 2 4 5 6 2 8 2 R U (86) Заявка PCT: EP 2007/009393 (30.10.2007) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 15.06.2009 (87) Публикация заявки РСТ: WO 2008/058628 (22.05.2008) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", Е.Е.Назиной (54) НОВЫЕ БЕНЗИЛЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 1,4-БЕНЗОТИЕПИН-1,1-ДИОКСИДА (57) Реферат: Изобретение относится к соединениям формулы I, а также к их физиологически приемлемым солям Ñòð.: 1 ru 2 4 5 6 2 8 2 (43) Дата публикации заявки: 20.12.2010 Бюл. № 35 (73) Патентообладатель(и): САНОФИ-АВЕНТИС ДОЙЧЛАНД (45) Опубликовано: 20.07.2012 Бюл. № 20 ГМБХ (DE) R U Приоритет(ы): (30) Конвенционный приоритет: 14.11.2006 DE 102006053635.5 (72) Автор(ы): ФРИК Венделин ...

NEW Glycolipid Adjuvant Compositions

1. Композиция, содержащая: ! а) гликолипид формулы I ! где формула I представляет собой ! ! где R1 и R2 независимо представляют собой водород или насыщенный алкильный радикал, имеющий до 20 атомов углерода включительно; ! X представляет собой -СН2-, -О- или -NH-; ! R2 представляет собой водород или насыщенный либо ненасыщенный алкильный радикал, имеющий до 20 атомов углерода включительно; ! R3, R4 и R5 независимо представляют собой водород, -SO4 2-, -РO4 2-, -СОС1-10алкил; ! R6 представляет собой L-аланил, L-альфа-аминобутил, L-аргинил, L-аспарагинил, L-аспартил, L-цистеинил, L-глутамил, L-глицил, L-гистидил, L-гидроксипропил, L-изолейцил, L-лейцил, L-лизил, L-метионил, L-орнитинил, L-фенилаланил, L-пролил, L-серил, L-треонил, L-тирозил, L-триптофанил и L-валил или их D-изомеры; ! в форме соли, которая образована со слабой кислотой; ! б) спирт, который представляет собой HO-C1-3алкил; ! в) слабую кислоту, которая 1) присутствует в молярном избытке по отношению к содержанию гликолипида и 2) представляет собой любую кислоту, имеющую величину рКа (-log Ка) от приблизительно 1,0 до приблизительно 9,5 согласно стандартным таблицам или величинам; ! г) неионное поверхностно-активное вещество, которое представляет собой агент, уменьшающий поверхностное натяжение вещества, в котором он растворен, и содержащий компонент, который является гидрофобным, и другой компонент, который является гидрофильным. ! 2. Композиция по п.1, где гликолипид представляет собой соединение формулы II(a) ! ! а слабая кислота выбрана из следующих слабых кислот: уксусной кислоты, ! Н(С2Н3O2) (рКа 4,76); аскорбиновой кислоты(1), Н2(С6Н6O6) (рКа 4,10); ацетилсалициловой кислоты, Н8(С9O4) (рКа 3,5); бутановой кислоты Н(С4Н7O2) (рКа 4,83); угольной РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 129 203 (13) A (51) МПК A61K 39/39 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2008129203/15, 15.01.2007 (71) Заявитель(и): ...

Production of carrageenan and carrageenan products

The methods of the present invention prepare carrageenan products from processed seaweed material having a solids content ofless than 25% by weight solids, using shear stress treatment. The carrageenan products comprise at least about 60% by weight of carrageenan and at least about 2% by weight of acid insoluble material. The carrageenan products of the present invention are useful as components in food products, such as, dairy products, meats, and dessert gels as well as non-food products, such as, toothpaste formulations, cosmetics, paints, films and delivery capsules.

Process for producing n-glucofuranozid-6-yl-n -nitrosocarbamides