Abstract: Substituted propanolamine derivatives, their pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula I
in which the radicals have the abovementioned meanings, and their physiologically tolerated salts, physiologically functional derivates and processes for their preparation. The compounds are suitable as, for example, hypolipidemics.
Abstract: An inclusion compound, which comprises a cyclodextrin or a branched cyclodextrin and a vanillyl alcohol derivative represented by the following formula (I) having been included therein:
wherein, R represents a C1-6 alkyl group; and a composition containing the same. The inclusion compound exhibits remarkably reduce impure taste of VE and heightens its water solubility and stability. The inclusion compound considerably enhances and prolongs the pungent taste and warm-feeling imparting effect of VE per se and further increase and prolong the cool or refresh-feeling heightening effect of VE per se when used in combination with a refrigerant.
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
May 27, 2003
Assignee:
Takasago International Corporation
Inventors:
Kenya Ishida, Satomi Kunieda, Akira Amano
Abstract: Substituted propanolamine derivatives, their pharmaceutically tolerated salts and physiologically functional derivatives thereof are described.
Also described are compounds of formula I
in which the radicals have the abovementioned meanings, and their physiologically tolerated salts, physiologically functional derivates and processes for their preparation. The compounds are suitable as, for example, hypolipidemics.
Abstract: Oligosaccharides including those usable as anti-inflammatory agent or anti-allergy agent, represented by the following general formula (3):
wherein R10 and R11 each independently represent a hydrogen atom or —SO3M where M represents a proton or a monovalent cation, Ac represents an acetyl group, R12 represents a hydrogen atom or an anomeric substituent (a 6-O-sulfated N-acetylglucosamine residue, an alkyl group, a glycerol residue, an O-alkylglycerol residue, a cholesterol residue, a cholestanyl group, a ceramide residue, a phospholipid residue, a biotin residue, or a peptide residue), and Z represents an oxygen atom or —NHCO—.
Abstract: The invention concerns derivatives of per-(3,6-anhydro)-cyclodextrin, their preparation, and their use in separating polluting ions, for example in human decontamination. These derivatives correspond to one of the following formula:
in which at least one of the R1 groups represents the group —OCH2COOH and the other R1 groups, which may be identical or different, represent a group that corresponds to one of the following formula: OH, OR2, SH, SR2, OCOR2, NH2, NHR2, NR2R3, CONH2, CONHR2, CONR2R3, CN, COOR2, COOH and R2, in which R2 and R3, which may be identical or different, represent an aliphatic or aromatic hydrocarbon group, either saturated or unsaturated, which may include one or several hetero-atoms comprising O, S and N, and n is equal to 6, 7 or 8.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
May 6, 2003
Assignees:
Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
Abstract: A composition for enhancing immunogenicity of tumor cells or pathogen-infected cells comprising a compound having an &agr;-glycosylceramide structure or a salt or solvate thereof is provided. Tumor cells of which immunogenicity is enhanced by the compound having an &agr;-glycosylceramide structure are useful for tumor therapy (cancer vaccine therapy).
Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.
Type:
Grant
Filed:
May 15, 2001
Date of Patent:
April 22, 2003
Assignee:
Eli Lilly and Company
Inventors:
Robert M. Scarborough, Mark Smyth, Ting Su, Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffry Bernard Franciskovich
Abstract: Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V,
wherein, Ring 1 comprises a cyclic or heterocyclic ring, or aryl or heteroaryl ring, all of said rings comprising 4 to 8 carbon atoms, among which atoms are counted “X” and “Y”; R0, R1, R2, R3 and R4 comprise substituents of Ring 1; either of X or Y is optional; each of X and Y, when present comprise a carbon atom, a halogen atom or a lower alkyl; Z, R5 and R5′ are optional; when Z is present it comprises a lower alkyl having substituents R5, R5′; R6 and R6′ comprise substituents on a carbon atom linking Z with N through a single bond, or when Z is absent, linking N with Ring 1; N comprises a nitrogen atom of an amine or an amide linked with E through a single bond and having R7 as a substituent; and E comprises a saccharide.
Abstract: A method for decreasing or shortening the length of time required to complete a surgical procedure by the application of hyaluronic acid to the surgical site, and for wound management by topical application of hyaluronic acid to a wound by syringe through a thin film dressing. The method of wound management results in accelerated wound healing time. The solution of hyaluronic acid may include an effective amount of a polysulfated glycosaminoglycan for stimulating macrophage activity at the surgical wound site.
Abstract: The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.
Type:
Grant
Filed:
December 1, 1999
Date of Patent:
April 1, 2003
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Eric Swayze, Richard H. Griffey, Yili Ding, Venkatraman Mohan
Abstract: A synthetic polysaccharide including an antithrombin III binding domain consisting of a concatenation of five monosaccharides supporting a total of two carboxylic acid functions and at least four sulpho groups, said domain being directly bound at the non-reducing end by a thrombin binding domain including a concatenation of 10-25 monosaccharide units selected from hexoses, pentoses or deoxy sugars of which all the hydroxyl groups are etherified by a C1-6 alkyl group or esterified in the form of sulpho groups, as well as salts and particularly pharmaceutically acceptable salts thereof, are disclosed.
Type:
Grant
Filed:
September 7, 1999
Date of Patent:
March 18, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel
Inventors:
Pierre Alexandre Driguez, Philippe Duchaussoy, Jean Marc Herbert, Maurice Petitou, Constant Van Boeckel, Peter Grootenhuis, Johannes Basten, Cornelia Dreef-Tromp
Abstract: Glycosylated polyamines comprising of mono- or oligo-saccharides that are glycosidically linked to an aliphatic polyamine, and pharmaceutically acceptable salts, prodrugs and derivatives thereof are provided. An exemplary glycosylated polyamine has the following structure:
Glycosylated polyamines, their pharmaceutically acceptable salts, prodrugs and derivatives are useful, for example, as anticancer compounds for the treatment of a variety of cancers. Methods for synthesis of glycosylated polyamines are disclosed. In addition, metal complexes of glycosylated polyamines, the preparation of such metal complexes, analytical methods using the metal complexes are provided. Methods for detecting equatorial and axial conformation of a group other than hydrogen at the C2 position of a saccharide molecule are also provided. The compounds of the invention can be used as anti-cancer agents (e.g., against breast, ovarian, colon or renal cancers).
Type:
Grant
Filed:
September 8, 2000
Date of Patent:
March 11, 2003
Assignee:
The Regents of the University of California
Inventors:
Julie A. Leary, Sara P. Gaucher, Steven F. Pedersen
Abstract: Coagulation control compositions suitable for use in connection with PT and/or APTT assays are disclosed along with their methods of preparation and methods of use. Preferred coagulation controls comprise plasma and an anticoagulant having activity for enhancing the activity of antithrombin III (ATIII) or of heparin co-factor II (HCII) against thrombin or against a clotting factor selected from the group consisting of factors IXa, Xa and XIa. The anticoagulant is preferably a glycosaminoglycan such as heparin, a heparin derivative or a heparin analog. The anticoagulant is preferably combined with (1) an abnormal plasma (e.g. activated plasma or factor-deficient plasma) and/or (2) a primate plasma (e.g. human plasma), and a non-primate mammalian plasma (e.g. bovine plasma). In the latter case, the non-primate mammalian plasma is preferably present in the coagulation control composition in an amount of not more than about 12% by volume, relative to total volume.
Abstract: An oligosaccharide derivative, at higher homogeneity than fucose polysaccharide and rhamnose polysaccharide and with greater antiulcer effects, which is represented by the following general formula:
Y—OCH(CH2NHR)2
wherein, Y represents an oligofucose or oligorhamnose at a polymerization number of 2 to 20, where the hydroxyl groups may or may not be partially modified in the form of sulfate ester, and R represents phenyl group, a higher alkylphenyl group, a higher alkyl group or —(CH2)n—NHX wherein n is an integer of 1 to 10 and X represents a higher alkanoyl group or an alkylamino group.
Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.
Type:
Grant
Filed:
August 30, 2000
Date of Patent:
January 28, 2003
Assignees:
Ibbex, Inc., UAB Research Foundation
Inventors:
Stephen C Johnson, Ashraf Saeed, Ming Luo
Abstract: The present invention relates to a pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in vagina in which comprises sugar(s), to the use of certain sugar(s), in preparing the pharmaceutical formulation for stimulating the growth of gram-positive bacilli and increasing the acidity in vagina, in particular to a method for stimulating the growth of gram-positive bacilli and increasing the acidity in vagina, treating the reduction of gram-positive bacilli and the lowness of acidity in vagina as well as the vaginitis and the disturbance of vaginal bacterioflora accompanying the reduction of gram-positive bacili, especially bacterial vaginal disease.
Abstract: The invention relates to dendrimers comprising an initiator core with at least two functional groups and at least two saccharides, a process for preparing sch dendrimers as well as uses thereof.
Type:
Grant
Filed:
March 8, 1999
Date of Patent:
July 9, 2002
Assignee:
Deutsches Krebsforschungzentrum Stiftung des Offentlichen
Rechts
Inventors:
Manfred Wiessler, Markus Gschrey, Willi Von der Lieth, Walter Mier
Abstract: The invention relates to novel mimetics of the tetrasaccharides sialyl-Lewis-X and sialyl-Lewis-A having an improved action as inhibitors of cell adhesion, to a process for the preparation of these compounds and to their use as pharmacological active compounds and diagnostic agents.
Type:
Grant
Filed:
October 30, 1996
Date of Patent:
July 2, 2002
Assignee:
Glycorex AB
Inventors:
Wolfgang Schmidt, Ulrich Sprengard, Gerhard Kretzschmar, Robert Klein, Horst Kunz
Abstract: Novel N-acyl-lysogangliosides obtained from gangliosides by deacyation of the ceramide group, wherein the acyl group is derived from an aliphatic acid having from 2 to 24 carbon atoms, substituted by one or more polar groups. The N-acyl-lysogangliosides of the invention exhibit an inhibiting action on protein-kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system.