Anticoagulation Patents (Class 514/822)
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Patent number: 5010063Abstract: New heparin derivatives having antithrombotic activity, also endowed with reduced hemorrhagic and anticoagulant activity, obtained by treating in a basic medium heparins of various origin, optionally in the presence of alkali metal salts and of a reducing agent.The heparin derivatives obtained through this treatment show peculiar chimico-physical characteristics, like new signals at about 53 and 54 p.p.m. in the .sup.13 C-NMR spectrum and an increase of the specific rotatory power, compared to that of the starting heparins, to values between +50.degree. to +90.degree..Said structural modifications produce an improvement of the biological properties of the heparin, substantially keeping the antithrombotic activity while diminishing the hemorrhagic effect in vivo and the anticoagulant activity in vitro.Type: GrantFiled: May 26, 1989Date of Patent: April 23, 1991Assignee: Alfa Wasserman S.p.A.Inventors: Silvano Piani, Gianfranco Tamagnone, Raul R. Alpino, Maria R. Milani, Marinella Fantuz
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Patent number: 5002767Abstract: The invention relates to a therapeutic composition containing, as the active principle, .alpha.-linolenic acid and an alcohol of vegetable origin, such as a tocopherol or sitosterol. Preferably, the composition contains other fatty acids and is an organic extract of plants, especially of the Resedaceae family.The invention also relates to the plant extracts as novel products.The therapeutic composition is especially useful as an antiinflammatory.Type: GrantFiled: August 24, 1988Date of Patent: March 26, 1991Assignee: Laboratories Natura MedicaInventor: Jean-Pierre Masse
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Patent number: 5002972Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.Type: GrantFiled: February 7, 1990Date of Patent: March 26, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Takaharu Matsuura
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Patent number: 4999210Abstract: An anti-infective medical article has chlorhexidine bulk distributed throughout a polyurethane base layer and may have a coating layer on the base layer. The coating layer may be chlorhexidine, an antibiotic, or an antithrombogenic agent permeated into the surface or it may be a polymeric surface layer having bulk distributed chlorhexidine laminated onto the base layer. The invention includes a method for preparing the article wherein a homogeneous melt of polymer and chlorhexidine is prepared by twin screw compounding and the melt is extruded to give a medical article having bulk distributed chlorhexidine. The article may then be laminated by dipping into a solution of chlorhexidine and a substantially hydrophilic polymer in a solvent.Type: GrantFiled: December 7, 1989Date of Patent: March 12, 1991Assignee: Becton, Dickinson and CompanyInventors: Donald D. Solomon, M. Parke Byron
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Patent number: 4992469Abstract: A quinone derivative of the formula (I): ##STR1## in which A is a group of the formula (IV): ##STR2## or a group of the formula (V): ##STR3## in which X and Y are either the same as or different from each other and each are hydroxy, methoxy or hydrogen; and n is an integer of 1 to 5,is disclosed. The compound is useful as a medicament.Type: GrantFiled: May 29, 1985Date of Patent: February 12, 1991Assignees: Eisai Co., Ltd., Nagoya UniversityInventors: Takayuki Ozawa, Morimitsu Nishikimi, Hiroshi Suzuki, Yoshiharu Shimomura, Isao Yamatsu, Shinya Abe, Kouji Yamada, Tohru Fujimori, Takanobu Takamura
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Patent number: 4987181Abstract: Copolymer film deposited on a substrate comprising covalently fixed fragments of heparin having antithrombogenic properties. The polymer further comprises free carboxylic groups intended to neutralize free amine functions which are possibly present and to improve the hemocompatibility of the film.Type: GrantFiled: September 19, 1989Date of Patent: January 22, 1991Assignee: Battelle Memorial InstituteInventors: Daniel Bichon, Christian Guillot, Michel Schneider
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Patent number: 4985245Abstract: A medical composition which contains a tissue Plasminogen Activator (tPA) in combination with meglumine or a salt thereof.Type: GrantFiled: November 3, 1989Date of Patent: January 15, 1991Assignee: Eisai Co., Ltd.Inventors: Fumio Kakimoto, Naoki Asakawa, Yasuo Ishibashi, Yasuo Miyake
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Patent number: 4973603Abstract: 6a,7,10,10a-tetrahydro-6,6-dimethyl-9-carboxyl-3-pentyl-6-H-dibenzo [b,d] pyran-1-ol is a potent antagonist to endogenous platelet activating factor (PAF). PAF is a factor in many of the pathological manifestations of disease, allergy or injury, such as inflammation, thrombosis and anaphylaxis. The actions of PAF can be inhibited in vivo by the present composition, thereby providing a safe and effective treatment for PAF-induced disorders.Type: GrantFiled: May 11, 1989Date of Patent: November 27, 1990Inventor: Sumner Burstein
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Patent number: 4954519Abstract: Substituted isocoumarins, their use in inhibiting serine proteases with trypsin-like, chymotrypsin-like and elastase-like specificity and their roles as anticoagulant agents, and anti-inflammatory agents.Type: GrantFiled: July 3, 1989Date of Patent: September 4, 1990Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Chih-Min Kam, Steven W. Oweida, David N. Ku
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Patent number: 4952675Abstract: Disclosed are methods for purifying proteins including AHF by column chromatography in the presence of additives including sugars and polyhydric alcohols which serve to increase the electrostatic forces on the surface of said proteins while decreasing the hydrophobicity of said proteins resulting in preparations of such proteins of high purity and/or resolution and/or recovery.Type: GrantFiled: December 29, 1988Date of Patent: August 28, 1990Assignee: New York UniversityInventors: Rita W. Mathews, Alan J. Johnson
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Patent number: 4952689Abstract: A 2-azetizinone derivative represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or an alkoxycarbonyl group in which the alkoxy group has 1 to 4 carbon atoms, R.sup.2 is a group represented by the formula ##STR2## a pyrrolidinyl group or a tetrahydroazepinyl group, and n is an integer of from 2 to 10, and a salt thereof are disclosed. These compounds are useful as blood platelet aggregation inhibiting agent.Type: GrantFiled: October 10, 1989Date of Patent: August 28, 1990Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Yutaka Kawashima, Masakazu Sato, Masahiro Kawase, Yoshiaki Watanabe, Katsuo Hatayama
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Patent number: 4942156Abstract: Ester derivatives of low molecular weight heparin are disclosed. These derivatives exhibit improved Anti-Xa activity in relation to global anticlotting activity.Type: GrantFiled: August 20, 1986Date of Patent: July 17, 1990Assignee: Hepar Industries, Inc.Inventors: Kevin M. Foley, Charles C. Griffin, Eduardo Amaya
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Patent number: 4935204Abstract: A process for the specific adsorption of heparin and other heparin-like substances which comprises flowing a buffered solution of whole blood, from which corpuscular blood constituents have been removed, plasma and/or solutions containing whole blood or plasma through an adsorber capsule containing a medium that adsorbs heparin and other heparin-like substances at an acid pH, preferably in the range of 4.0 to 5.5. Preferably, the process is carried out in a closed, extracorporeal circulation and the medium possesses anion exchange resin properties.Type: GrantFiled: November 14, 1988Date of Patent: June 19, 1990Assignee: B. Braun-SSC AGInventors: Dietrich Seidel, Wolfgang Feller, Gerhard Rosskopf
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Patent number: 4933326Abstract: Heparin fractions which are a mixture of oligosaccharides containing 6-12 monosaccharides are described. The oligosaccharides contain reducing end groups composed of iduronic acid 2-sulfate or glucosamine N, 6-disulfate. The end group monosaccharides contain the reducing anomeric carbons. The SO.sub.3.sup.- /COO.sup.- ratio is essentially the same as in heparin. The method of preparation is a depolymerization initiated by free radicals. One fraction is a heparin fragment with a molecular weight (MWw) of 2,100 daltons (+10%). The compound contains 6-8 monosaccharides, has the same SO.sub.3.sup.- /COO.sup.- ratio as the parent heparin and has platelet anti-aggregating activity, arterial and venous antithrombotic action, fibrinolytic and antiatherosclerotic activity. It exhibits poor anti factor Xa activity and no anticoagulant action.Type: GrantFiled: September 21, 1988Date of Patent: June 12, 1990Assignee: Opocrin S.p.A.Inventors: Pietro Bianchini, Giuseppe Mascellani
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Patent number: 4927630Abstract: Normal human colon fibroblast tissue plasminogen activator is separated by lysine-Sepharose affinity chromatography into Types I and II glycoforms and characterized with respect to the relative incidence of each type of oligosaccharide comprising the respective Types I and II glycoforms.Type: GrantFiled: March 11, 1988Date of Patent: May 22, 1990Assignee: Monsanto CompanyInventors: Joseph Feder, Susan C. Howard, Arthur J. Wittwer, Thomas W. Rademacher, Raj B. Parekh, Raymond A. Dwek
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Patent number: 4918099Abstract: A novel drug comprises as active ingredient an extract extractable from plant material of plants belonging to the genus Caesalpinia, one or several components of this extract and/or one or several substances present in this extract or derived therefrom but prepared synthetically.These substances are in particular benz(b)indeno(2.1-d)pyran derivatives, including brazilin, brazilein, hematoxylin and/or hematein. The drug is especially suited for treatment of a patient suffering from micro-circulatory disorders, diabetes mellitus, increased blood sugar values, increasing blood platelet aggregation, increased blood viscosity, decreased eryhtrocyte deformability, disorders of the lysosomal enzyme activity and/or suffering from disorders of the prostaglandin metabolism, especially increasing thromboxane A.sub.2 activity.Type: GrantFiled: March 26, 1986Date of Patent: April 17, 1990Inventor: Chang-Kiu Moon
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Patent number: 4912092Abstract: Methods for increasing extracellular concentrations of adenosine for the prophylactic or affirmative treatment of diseases of the immune, nervous, cardiac, and vascular systems involving admimistering to a patient purine nucleoside and purine nucleoside-related analogs which increase extracellular adenosine concentration, and methods for stabilizing mast cells by the suppression of mast cell activation using such compounds.Type: GrantFiled: July 29, 1987Date of Patent: March 27, 1990Assignee: The Regents of the University of CaliforniaInventor: Harry E. Gruber
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Patent number: 4909799Abstract: In order to improve the surface properties of small caliber vascular grafts or other surgical implants, Forskolin (or a derivative thereof) which is a power cAMP stimulating agent, is applied to the thrombogenic surfaces of the graft/implant. Forskolin as thus used is a potent antiplatelet agent significantly lowering platelet deposition on the implant.Type: GrantFiled: September 18, 1987Date of Patent: March 20, 1990Inventors: Olav Thulesius, Jan T. Christenson
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Patent number: 4902613Abstract: A lysing agent and a method for utilizing the lysing agent in the identification and enumeration of cells of a select subclass of leucocytes is provided. The lysing agent includes formaldehyde, an alkali or alkaline earth salt of a weak acid and a polyhydric alcohol.Type: GrantFiled: December 8, 1986Date of Patent: February 20, 1990Assignee: Becton, Dickinson and CompanyInventors: Chin-hai Chang, Alex M. Saunders
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Patent number: 4883804Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.Type: GrantFiled: November 19, 1986Date of Patent: November 28, 1989Assignee: Fisons plcInventors: Francis Ince, Brian Springthorpe, John Dixon
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Patent number: 4880788Abstract: The present invention provides a method for preventing and treating thrombosis in an individual comprising administering a compound effective to inhibit the agglutination and aggregation of blood platelets to an individual in need of said treatment. In a preferred embodiment, the compound is selected from the group consisting of aurin tricarboxylic acid, triphenyl methyl dyes, substituted naphthalene sulfonic acid moieties, the analogs and agonists of these compounds and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 30, 1987Date of Patent: November 14, 1989Assignee: Baylor College of MedicineInventors: Joel L. Moake, Martin D. Phillips, Larry V. McIntire, Jesse D. Hellums
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Patent number: 4871748Abstract: Compounds of the formula: ##STR1## wherein R represents hydroxymethyl, alkoxymethyl of 2 to 6 carbon atoms, optionally substituted phenoxymethyl, alkanoyloxymethyl of 3 to 10 carbon atoms, optionally substituted benzoyloxymethyl, alkylsulphonyloxymethyl of 2 to 9 carbon atoms, optionally substituted phenylsulphonyloxymethyl, formyl, aminomethyl optionally substituted by 1 or 2 alkyl groups of 1 to 4 carbon atoms, or hydroxyiminomethyl, and acid addition salts thereof, are useful as rodenticides.Type: GrantFiled: January 23, 1985Date of Patent: October 3, 1989Assignee: May & Baker LimitedInventor: Leslie R. Hatton
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Patent number: 4867915Abstract: Sixteen carbon atom carboxylic acids having 16-phenoxy or 16-phenylthio substituents, and 0, 1, or 4 triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors.Type: GrantFiled: May 21, 1986Date of Patent: September 19, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchwoski, Angel Guzman
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Patent number: 4861594Abstract: A method of preparing a composition capable of inhibiting platelet aggregation in mammalian blood induced by adenosine diphosphate or arachidonic acid, which comprises forming an aqueous extract of dried and powdered seeds of the plant Paullinia cupana (guarana), centrifuging the solution and filtering the supernatant. A fraction of this aqueous extract obtained by thin-layer chromatographic fractionation on silica gel plates, which is free of salicylic acid, xanthines and nicotinic acid, is capable of deaggregating platelet aggregations in mammalian blood induced by adenosine diphosphate or arachidonic acid as well as inhibiting platelet aggregation. This fraction is eluted with ethanol, and centrifuged to removed gel. The supernatant may be dried and reconstituted with distilled water.Type: GrantFiled: March 16, 1987Date of Patent: August 29, 1989Assignee: University of CincinnatiInventor: M. T. Ravi Subbiah
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Patent number: 4857326Abstract: A method for producing a stable dry composition of flax seed comprising grinding the flax seed in the presence of vitamin B-6 and zinc ion at a temperature of about 160.degree. F. to just above freezing. A stable dry composition of flax seed producted by the aforementioned method. A method for producing a stable emulsion or suspension of flax seed comprising: (1) grinding the flax seed in the presence of vitamin B-6 and zinc ion at a temperature of about 160.degree. F. to just above freezing; (2) soaking the flax seed in an aqueous solution for about 10 minutes to overnight at a temperature of about 160.degree. F. to just above freezing; and (3) blending or homogenizing said soaked, ground flax seed, with or without further additives, to form a stable emulsion or suspension; provided that the steps (1) and (2) can be conducted in any order. A stable emulsion or suspension of flax seed.Type: GrantFiled: December 29, 1986Date of Patent: August 15, 1989Inventor: Paul A. Stitt
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Patent number: 4847362Abstract: The present invention relates to a high-recovery, high-resolution method for purifying antihemophilic factor by using column chromatography techniques in the presence of sugars, polyhydric alcohols, amino acids or salts.Type: GrantFiled: November 19, 1987Date of Patent: July 11, 1989Assignee: New York UniversityInventors: Rita W. Mathews, Alan J. Johnson
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Patent number: 4842859Abstract: The new pharmaceutical compositions and processes are provided for reducing both hyperlipidemia and platelet-aggregation (PHP).The fine-PHP is composed of following ingredients: Scoparone or Aurapten, Curcumin, Ferulic Acid, Yejuhua-flavonoid and additive ingredient--fish oil. The compositions are nontoxic.Type: GrantFiled: September 8, 1986Date of Patent: June 27, 1989Inventor: Yaguang Liu
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Patent number: 4841968Abstract: The controlled first-order release of either an antithrombotic or thrombolytic agent from a sutures at an anastomosis site is disclosed which prevents postoperative thrombosis and improves vascular patency in animals. A suitable polymer, such as polycaprolactone, is blended with prostacyclin or analogues of prostacyclin to form the suture material.Type: GrantFiled: September 26, 1986Date of Patent: June 27, 1989Assignees: Southern Research Institute, Texas Health Science CenterInventors: Richard L. Dunn, John W. Gibson, Carlton A. Eddy, Leonard E. Laufe
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Patent number: 4839169Abstract: A combination of t-PA and a prostaglandin of use in removing or inhibiting the formation of a blood clot in a mammal.Type: GrantFiled: August 4, 1987Date of Patent: June 13, 1989Assignee: Burroughs Wellcome Co.Inventor: Brendan J. R. Whittle
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Patent number: 4837014Abstract: In accordance with the present invention, a method is provided that is effective in treating sickle cell anemia. The method comprises a method of treating a person with sickle cell disease comprising the step of injecting into the person with sickle cell disease a solution with an effective concentration of a surface active copolymer of the following formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000 and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.Type: GrantFiled: January 13, 1989Date of Patent: June 6, 1989Assignee: Emory UniversityInventors: Robert L. Hunter, Alexander Duncan
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Patent number: 4832849Abstract: Applicant has isolated a Factor X.sub.a inhibiting substance from the salivary gland extract of the leech H.ghilianii. The extract is subjected to separation using both DEAE-cellulose and heparin-agarose chromatography resins eluting with an increasing salt gradient. The extract is subjected to affinity chromatography using Factor X.sub.a bound to an Affi-Gel-15 resin eluting with HEPES containing benzamidine. Reverse phase chromatography yields several purified peptides or proteins having Factor X.sub.a inhibiting activity. The properties and clinical compositions of these FX.sub.a inhibitors are described.Type: GrantFiled: June 16, 1988Date of Patent: May 23, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Alan D. Cardin
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Patent number: 4833200Abstract: An antithrombogenic medical material with a remarkable antithrombogenic property and histocompatibility as well as sufficient physical strength, formed by fixing a heparinized collagen to a synthetic polymer material is provided. And a method of preparing an antithrombogenic medical material is provided, wherein a synthetic polymer material is subjected to a coating or impregnating treatment with a collagen-containing solution, followed by heparinization of the collagen, and the heparinized collagen is fixed to the synthetic polymer material. This method allows manufacturing of antithrombogenic medical material with ease.Type: GrantFiled: July 25, 1986Date of Patent: May 23, 1989Assignee: Koken Co., Ltd.Inventors: Yasuharu Noishiki, Teruo Miyata
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Patent number: 4818816Abstract: The invention relates to a process for the organic synthesis of oligosaccharides constituting or comprising fragments of acid mucopolysaccharides comprising the reaction of two compounds constituted or terminated by units of glucosamine structure and of uronic acid structure respectively, said units being specifically substituted. This process particularly enables valuable anticoagulant drugs to be obtained.Type: GrantFiled: October 26, 1987Date of Patent: April 4, 1989Assignee: Choay, S.A.Inventors: Maurice Petitou, Jean-Claude Jacquinet, Pierre Sinay, Jean Choay, Jean-Claude Lormeau, Mahmoud Nassr
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Patent number: 4816446Abstract: The invention comprises heparin derivative compounds which possess a low density lipoprotein lowering action without a significant anticoagulent effect, and are therefore useful in the treatment of disturbances of fat metabolism, especially hyperlipidemia. The heparin derivatives of the invention are derived from natural heparin, and are prepared by the hydrolysis of heparin and optionally, subsequent acylation at free amine groups of the hydrolyzed heparin.Type: GrantFiled: June 13, 1985Date of Patent: March 28, 1989Assignee: Intermedicat GmbHInventors: Wolfgang Feller, Rainer Stormer, Annemarie Muller
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Patent number: 4808570Abstract: The healing of wounds is promoted by contacting the wound surfaces with a suspension of collagen and a glycosaminoglycan that is chemotactic for fibroblasts and/or endothelial cells. Typical glycosaminoglycans that exhibit the desired chemotaxis are heparin, heparan sulfate, and alginate. Two or more glycosaminoglycans can be present in the suspensions. Collagen is present in the suspension in the order of 7-10 mg/ml; while the glycosaminoglycan is present in such lower concentrations, e.g. 250-350 .mu./ml. Application of the collagen/glycosaminoglycan suspension to open wounds greatly increases the rate of healing.Type: GrantFiled: August 15, 1986Date of Patent: February 28, 1989Assignee: University of CaliforniaInventor: Dov Michaeli
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Patent number: 4806595Abstract: In a method of preparing an antithrombogenic medical material having a heparinized collagen as an antithrombogenic component, there is provided a method comprising the steps of fixing a protamine to a collagen through a polyepoxy compound, and heparinizing the collagen by fixing heparin to the protamine.Type: GrantFiled: August 1, 1986Date of Patent: February 21, 1989Assignee: Koken Co., Ltd.Inventors: Yasuharu Noishiki, Kazuhiko Kodaira, Masayasu Furuse, Teruo Miyata
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Patent number: 4804652Abstract: Mucopolysaccharides biologically active and more specific than heparin, particularly with respect to the blood factor Xa. These mucopolysaccharides may be obtained by partial depolymerization, under controlled conditions, of heparin, by the action of a chemical agent such as nitrous acid. The conditions implemented allow the preparation of mucopolysaccharides having a USP titer lower than that of the starting heparin and a Yin-Wessler titer at least equal to that of said heparin. These products may be used particularly as antithrombotic drugs.Type: GrantFiled: February 19, 1985Date of Patent: February 14, 1989Assignee: Choay S.A.Inventors: Jean-Claude Lormeau, Maurice Petitou, Jean Choay
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Patent number: 4801576Abstract: The present invention relates to desulfatohirudins, to the preparation thereof, to pharmaceutical compositions containing these compounds, and to the use thereof. The desulfatohirudins of this invention correspond to hirudin in biological activity and are therefore particularly useful for inhibiting blood clotting.Type: GrantFiled: January 19, 1988Date of Patent: January 31, 1989Assignee: Ciba-Geigy CorporationInventors: Hans Fritz, Johannes Dodt, Ursula Seemuller, Ernst Fink
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Patent number: 4801452Abstract: In accordance with the present invention, a composition is provided that is effective in dissolving blood clots and reestablishing and maintaining blood flow through thrombosed coronary or other blood vessels. The fibrinolytic composition of the present invention comprises an enzyme, such as streptokinase, urokinase, tissue plasminogen activator or other fibrinolytic enzyme, and a surface-active copolymer. The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000, preferably approximately 1750 to 3500, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.Type: GrantFiled: May 7, 1987Date of Patent: January 31, 1989Inventors: Robert L. Hunter, Alexander Duncan
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Patent number: 4791195Abstract: Novel oligosaccharide fractions with valuable pharmacological properties are obtained from heparin. They have the same structural characteristics of heparin. The heparin fraction consists of oligosaccharides which contain end groups consisting of iduronic acid 2-sulfate, or glucosamine N, 6-disulfate. Further the oligosaccharides contain and monosaccharide endowed with reducing anomeric carbon, and are constituted by multiples of monosaccharide units.Type: GrantFiled: October 21, 1986Date of Patent: December 13, 1988Assignee: Opocrin A.P.A.Inventors: Pietro Bianchini, Giuseppe Mascellani
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Patent number: 4788307Abstract: The oligosaccharidic fractions of the invention are soluble in an hydro-alcoholic mixture 50/50 (v/v) in which is added 0.5% NaCl, at pH 3.8, are constituted by chains the majority of which have 2 to 14 sugar units, are terminated by end units with a 2,5-anhydromanno structure and are devoid or practically devoid of anti-thrombotic activity.Type: GrantFiled: January 29, 1987Date of Patent: November 29, 1988Assignee: Choay S.A.Inventors: Jean-Claude Lormeau, Jean Choay
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Patent number: 4786556Abstract: Plastic articles having enhanced antithrombogenic activity due to the presence or hydrophobic materials attached to amine compounds bonded on the surface of the plastic which repel bonded antithrombogenic agents outwardly from the plastic surface, making them more readily available to the blood for subsequent thrombus inhibition.Type: GrantFiled: July 24, 1987Date of Patent: November 22, 1988Assignee: Becton, Dickinson and CompanyInventors: Can B. Hu, Donald D. Solomon
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Patent number: 4783470Abstract: Anticoagulant is derived from hematin on standing in a slightly alkaline medium and may be isolated therefrom.Type: GrantFiled: January 14, 1986Date of Patent: November 8, 1988Assignee: The Rockefeller UniversityInventor: Robert L. Jones
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Patent number: 4783447Abstract: A process for producing natural heparan sulphate and dermatan sulphate for mixtures of proteoglycans from the aorta, myocardium and particularly vascularized organs, based on a series of precipitation and purification steps which enable the protein part of the proteoglycan to be eliminated and the two products to be obtained in substantially pure form, without any chemical or enzymatic degradation.When administered orally or parenterally, the heparan sulphate obtained exerts activation effects on antithrombin III and on the fibrinolytic process.The dermatan sulphate obtained exerts an inhibiting effect on Factor Xa and also possesses the property of activating the fibrinolytic effect of heparan sulphate.Type: GrantFiled: March 10, 1986Date of Patent: November 8, 1988Assignee: Mediolanum Farmaceutici SrlInventors: Rinaldo Del Bono, Luigi De Ambrosi, Piergiuseppe Pagella, Gianni Ferrari
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Patent number: 4777161Abstract: The medicaments of the invention contain in their active principle, oligosaccharides of low molecular weight corresponding to or including heparin fragments.Type: GrantFiled: May 29, 1985Date of Patent: October 11, 1988Assignee: Choay S.A.Inventors: Jean-Claude Lormeau, Maurice Petitou, Jean Choay, Francis Toulemonde
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Patent number: 4774241Abstract: A derivative of benzoquinonylphenyl alkanoic acid amide having the formula: ##STR1## wherein X represents an oxygen atom, sulfur atom, or methylated nitrogen atom, Me represents methyl, and n is 2 or 3. This derivative is effective as a cerebral insufficiency improver.Type: GrantFiled: March 27, 1987Date of Patent: September 27, 1988Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
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Patent number: 4766111Abstract: Plasmin inhibitory substances have been found in mammalian omental extracts. The substances all contain lipid components. In addition, related commercially available lipid containing molecules, such as mono-, di-, and trisialogangliosides are found to possess unexpected plasmin inhibitory properties. This suggests methods of therapy for diseases and conditions where blood clotting and fibrin degradation products, are implicated.Type: GrantFiled: March 23, 1987Date of Patent: August 23, 1988Assignee: Trustees of Boston UniversityInventor: Nicholas Catsimpoolas
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Patent number: 4755379Abstract: Anticoagulant products are constituted by polymers (homopolymers or copolymers) including in their chain substitutable groups on which are fixed statistically, groups X and/or Y and/or V, where X denotes the group --SO.sub.3 R.sub.1 or --R.sub.3 --SO.sub.3 R.sub.1, R.sub.1 being a hydrogen atom or a physiologically compatible metal, R.sub.3 being a --CH.sub.2 --CO--NH--R.sub.4 group in which R.sub.4 represensts an alkyl aryl or alkylaryl radical, which may or may not be substituted, or substituted or unsubstituted --CH.sub.2 --; Y denotes the group --SO.sub.2 --R.sub.2 or --R.sub.3 --SO.sub.2 --R.sub.2, R.sub.2 being the residue of an amino acid connected to the --SO.sub.2 bridge through its amine function and V denotes the group --CH.sub.2 --CO--NH--CHR--COOH, R being the side chain of an amino acid it being understood that: (a) if X is --SO.sub.3 R.sub.1 it is necessarily accompanied by Y and/or by V, and (b) V is always accompanied by X and/by Y.Type: GrantFiled: September 27, 1985Date of Patent: July 5, 1988Assignees: Jacqueline Jozefonvicz, Marcel Jozefonvicz, Christine FougnotInventors: Marcel Jozefonvicz, Jacqueline Jozefonvicz, Christine Fougnot, Monique Mauzac
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Patent number: 4755504Abstract: A pharmaceutical composition containing saponin and quercetin, derived from Tienchi, is effective in treatment of circulatory disease and as health food. Processes for producing these components are provided.Type: GrantFiled: December 22, 1986Date of Patent: July 5, 1988Inventor: Yaguang Liu
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Patent number: 4751084Abstract: Glycosylated plasminogen activator (t-PA) having a glycosylation pattern significantly different than exhibited by t-PA from Bowes melanoma cells is obtained from cultured normal human colon fibroblast cells (CCD-18Co).Type: GrantFiled: November 12, 1986Date of Patent: June 14, 1988Assignee: Monsanto CompanyInventors: Joseph Feder, William R. Tolbert, Thomas W. Rademacher, Raj B. Parekh, Raymond A. Dwek