Abstract: Anigiogenesis is controlled by administering to a mammal an effective amount of an inhibitor of arylsulfatase. Preferably, the arylsulfatase inhibitor is administered in a pharmaceutically acceptable vehicle in combination with an angiostatic steroid and (optionally) heparin (by which term we include all forms and fragments of heparin having the desired angiostatic activity). Hydrocortisone is one specifically preferred steroid. The preferred arylsulfatase inhibitor is a carboxylic acid ester or a sulfuric acid ester of a benzylic alcohol, most preferably the esters defined more particularly below. The arylsulfatase inhibitor is preferably administered locally to the tissue experiencing undesired angiogenesis. Arylsulfatase inhibitor and an angiostatic steroid are included in a pharmaceutically acceptable vehicle, preferably also with heparin, to yield an angiostatic thereapeutic composition.
Type:
Grant
Filed:
May 27, 1988
Date of Patent:
March 17, 1992
Assignees:
The Children's Medical Center Corporation, President and Fellows of Harvard College
Inventors:
Moses J. Folkman, Neil T. Chen, Elias J. Corey
Abstract: As a new compound is now provided N-acetylbenanomicin B which is useful as an antifungal agent and also as antiviral agent for inhibiting infection of human T-cell with HIV, namely a virus causative of acquired human immunodeficiency syndrome. N-acetylbenanomicin B may be prepared by acetylation of 4"-amino group of benanomicin B which is fermentatively produced by a new microorganism, MH193-16F4 strain of actinomycetes.
Type:
Grant
Filed:
December 29, 1989
Date of Patent:
March 3, 1992
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: Pharmaceutical compositions having a formulation and form suitable for nasal administration, and containing 17.beta.-estradiol and/or progesterone. According to the invention, the composition also contains dimethyl-.beta.-cyclodextrin.
Type:
Grant
Filed:
June 28, 1989
Date of Patent:
February 18, 1992
Inventors:
Walter A. J. J. Hermens, Franciscus W. H. M. Merkus
Abstract: The process makes an oligosaccharide fraction from commerically available heparin solutions containing from 1 to 10 % heparin. This oligosaccharide fraction has antithrombotic activity, bioavailability, almost no toxic effects as well as a comparatively lower hemorrhagic risk and a reduction in bleeding time and a molecular weight range of less than 5000 D.
Type:
Grant
Filed:
April 10, 1989
Date of Patent:
January 28, 1992
Assignee:
Bioiberica, S.A.
Inventors:
Francisco J. P. Vila, Alberto D. Nusimovich, Pedro T. Gomis
Abstract: The present invention relates to antitumor 4'-demethylepipodophyllotoxin glycosides having the formula ##STR1## wherein R is a pentose selected from the group consisting of .beta.-D-ribopyranosyl, peracyl .beta.-D-ribopyranosyl, .beta.-D-xylopyranosyl, peracyl .beta.-D-xylopyranosyl, .alpha.-D-xylopyranosyl, peracyl .alpha.-D-xylopyranosyl, .alpha.-D-arabinopyranosyl, 3,4-O-(C.sub.1-4)alkylidene-D-ribopyranosyl, 2-O-acyl-3,4-O-(C.sub.1-4)alkylidene-D-ribopyranosyl, and .beta.-D-ribofuranosyl; P is hydrogen, or --PO.sub.3 H.sub.2 or a pharmaceutically acceptable salt thereof.
Abstract: Sialic acid derivative with active ester groups expressed with the formula [I] ##STR1## Where R.sup.1 denotes hydrogen or an acetyl group, R.sup.2 denotes hydrogen or a lower alkyl group, R.sup.3 denotes C.sub.2 H.sub.4, C.sub.3 H.sub.6 or C.sub.2 H.sub.2, R.sup.4 denotes an hydroxyl group, the residue left after removing hydrogen from the alcohol portion of the active ester or alkyloxycarbonyloxy group, AC denotes an acetyl group, Ph denotes an phenyl group, and X denotes oxygen or sulfur. This sialic acid derivative has high reactivity because it has active ester groups in the molecules and can be used as a raw material or intermediate for synthesis of various sialic acid derivatives.
Abstract: Novel organosoluble derivatives of chitosan, useful in coating biologically active feedstuff additives intended for ruminants, to provide coatings which are stable at a pH greater than 5 and which release the biologically active substance at a pH below 3.5, consist of a random chain of units represented by the formulae: ##STR1## in which: R.sub.1 represents an alkylcarbonyl radical (2 to 4 carbon atoms), R.sub.2 represents an alkyl radical (2 to 21 carbon atoms) or an optionally substituted phenyl radical, and R.sub.3 and R.sub.4 represent a hydrogen atom or alkylcarbonyl radicals (2 to 4 carbon atoms).
Type:
Grant
Filed:
November 29, 1989
Date of Patent:
December 31, 1991
Assignee:
Rhone-Poulenc Sante
Inventors:
Christine Franzoni, Christian Gagnieu, Hugues Porte
Abstract: A process for preparing polyol fatty acid polyesters, e.g. sucrose polyesters (SPE) is improved by(1) mixing the polyol with an alkaline catalyst such as KOH, NaOH or their carbonates, preferably in aqueous solution or dissolved in C.sub.1-5 alcohols or ketones at atmospheric pressure and 10.degree.-80.degree. C.(2) preparing a mixture of fatty acid lower alkyl esters with an emulsifier, preferably a fatty acid soap, and(3) adding the alkaline polyol solution to the mixture of (2), whereby preferably the solvent is removed during the addition of (1) to (2), e.g. at 60.degree. C. and 5 mbar.The ratio fatty acid lower alkyl esters:polyol is preferably (10-20):1.The reaction is improved so that SPE are formed at 110.degree.-145.degree. C. within 5-10 hours.
Type:
Grant
Filed:
July 21, 1987
Date of Patent:
December 10, 1991
Assignee:
Van den Bergh Foods Co., Division of Conopco Inc.
Inventors:
Pleun van der Plank, Adrianus Rozendaal
Abstract: A purified oligosaccharide consisting of a hexasaccharide with a native molecular weight of 959 which can be isolated from the cell walls of Streptococcus sanguis. The oligosaccharide is able to significantly block the interaction between the human oral plaque bacteria Streptococcus sanguis H1 and Capnocytophaga ochracea ATCC 33596. This purified oligosaccharide contains saccharide components found to inhibit many known interactions between plaque bacteria and may be effective in prevention, inhibition and reversal of dental plaque deposits. The oligosaccharide may be applied effectively when incorporated in toothpastes, mouth wash, etc.
Type:
Grant
Filed:
May 10, 1989
Date of Patent:
December 10, 1991
Assignee:
The United States of America as represented by the Secretary of the Department of Health and Human Services
Abstract: The present invention refers to a method concerning the preparation of hemo-compatible substrates by incorporation, adhesion and/or modification and embodiment of non-thrombogenic endothelial cell surface polysaccharide (HS I) in its peptide-bound or free form on and/or mixed with synthetic and biopolymers (Substrates) by way of physical distribution, adhesion to the surface and/or chemical embodiment, which can be used in medicine as blood-compatible substrates. These polymers can be presented in form of fibres, hollow fibres, membranes, organ spare parts, canulas, syringes, tubes, blood containers, or in other forms, or they can be prepared from other material.
Abstract: A for measurement of .alpha.-amylase activity uses a substrate comprising a malto-oligo saccharide represented by general formula (I) or (V) described below:A - Gn - B (I)A - Gn - I (V)wherein A represents: ##STR1## B represents a monosaccharide or a derivative thereof other than glucose; I represents inositol or a derivative thereof; G represents glucose; and n represents an integer of 3 to 15; in formula (II) or (III), R.sub.1 to R.sub.4 each represents a hydrogen atom, a lower alkyl group or (CH.sub.2)yCOOM (wherein y is 0, 1 or 2 and M represents a hydrogen atom or an alkali metal); and X.sub.1 to X.sub.4 each represents an oxygen atom or a sulfur atom. The method for measurement of .alpha.-amylase activity comprises contacting a substrate containing a malto-oligo saccharide represented by general formula (I) or (V) described above with a sample in the presence of glucosidase and measuring a liberated monosaccharide, inositol or a derivative thereof thereby to measure .alpha.
Type:
Grant
Filed:
January 3, 1991
Date of Patent:
November 26, 1991
Assignees:
Kurita Water Industries, Ltd., Zensuke Ogawa
Abstract: Disaccharide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 CO-- and R.sup.2 CO-- each represents a residue of a straight chain fatty acid having from 8 to 20 carbon atoms and having a hydroxyl group at the 3-position thereof; R.sup.3 CO-- and R.sup.4 CO-- each represents a residue of a straight chain fatty acid having from 8 to 20 carbon atoms; and m and n each represents an integer of from 8 to 12, and the salts thereof. The compounds exhibit biological activities equal to or higher than those of natural lipid A. Also, the compounds of this invention are very useful as standard reagent for determination of endotoxin in the samples to be tested.
Abstract: The present invention provides antitumor 4'-Demethylepipodophyllotoxin glycosides characterized by the fact that the glycoside moiety is altrose.
Abstract: This invention encompasses a method and compositions which inhibit pancreatic cholesterol esterase and triglyceride lipase and hence, lower cholesterol and triglycerides in the blood stream.
Type:
Grant
Filed:
October 31, 1989
Date of Patent:
November 5, 1991
Inventors:
Louis G. Lange, III, Curtis A. Spilburg
Abstract: Substantially pure saponins are disclosed. The saponins of the present invention are useful as immune adjuvants. Disclosed as well are immune response-provoking compositions comprising an antigen in admixture with the substantially pure saponins.
Abstract: An anti-AIDS virus agent comprising a sulfate of a polysaccharide having repeating units of the formula: ##STR1## and having a molecular weight of at most 1,000,000 (n.ltoreq.1544).
Type:
Grant
Filed:
May 10, 1989
Date of Patent:
October 1, 1991
Assignee:
Taito Co., Ltd.
Inventors:
Shigero Mori, Isamu Sugawara, Wataru Ito
Abstract: A process for preparing gamma inulin comprising the steps of (a) recrystallizing crude inulin from water at a temperature below 37.degree. C. to obtain a suspension, (b) heating the suspension at a temperature of from about 25.degree. to 45.degree. C. for about 1-3 days, (c) further heating the suspension at a temperature of about 40.degree. to 55.degree. C. for about 0.5 to 1.5 hours, and (d) isolating insoluble gamma inulin from the suspension. A composition comprising particles of inulin or an inulin derivative in the gamma polymorphic form is characterized in that the particles have a low rate of solution in aqueous media above 30.degree. C., particularly above 37.degree. C. The composition is effective as the active component of an immunotherapeutic preparation for activation of the alternative pathway of complement, or for antitumor treatment.
Abstract: 7-O-Glycosyl-rhodomycins which correspond to the general formula I below ##STR1## in which the radicals have the following meaning: R.sup.1 is a hydrogen atom or a hydroxyl group,R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 a hydroxyl group, an O-acyl protective group or the methyloxycarbonyl group,R.sup.4 is a hydrogen atom, an O-acyl protective group, an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group andR.sup.5 is an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group,where acyl protective group denotes an acetyl, mono-, di- or trihalogenoacetyl group with fluorine or chlorine as halogen or the p-nitrobenzoyl group, and a process for the preparation thereof and the use thereof as pharmaceuticals, are described.
Type:
Grant
Filed:
December 18, 1989
Date of Patent:
September 17, 1991
Assignee:
Behringwerke Aktiengesellschaft
Inventors:
Cenek Kolar, Hans P. Kraemer, Konrad Dehmel
Abstract: A pharmaceutical composition is provided comprising inner ester ganglioside derivatives useful for its peripheral analgesic-antiinflammatory activity in treating pain caused by pathologies of the peripheral nervous system and which can advantageously be administered orally.
Abstract: A substrate for measurement of .alpha.-amylase activity comprising a malto-oligo saccharide respresented by general formula (I) or (V) described below:A--Gn--B (I)A--Gn--I (V)wherein A represents: ##STR1## B represents a monosaccharide or a derivative thereof other than glucose; I represents inositol or a derivative thereof; G represents glucose; and n represents an integer of 3 to 15; in formula (II) or (III), R.sub.1 to R.sub.4 each represents a hydrogen atom, a lower alkyl group or (CH.sub.2)yCOOM (wherein y is 0, 1 or 2 and M represents a hydrogen atom or an alkali metal); and X.sub.1 to X.sub.4 each represents an oxygen atom or a sulfur atom.