Arteriosclerosis Patents (Class 514/824)
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Patent number: 6288250Abstract: Compounds of the general formula wherein R represents a straight or branched chain alkyl group containing from 1 to 16 carbon atoms, pharmaceutically acceptable salts thereof and/or optical isomers thereof have an immunostimulating effect, and are useful in the treatment of arteriosclerosis.Type: GrantFiled: September 30, 1999Date of Patent: September 11, 2001Assignee: Astra AktiebolagInventors: Håkan Bergstrand, Jan Dahmén, Bengt Särnstrand
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Patent number: 6264938Abstract: The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of an HMG Co-A reductase inhibitor compound. The first and second amounts together comprise a therapeutically effective amount. The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of an HMG Co-A reductase inhibitor compound. The first and second amounts comprise a therapeutically effective amount. The pharmaceutical compositions of the present invention may optionally contain a pharmaceutically acceptable carrier.Type: GrantFiled: May 13, 1999Date of Patent: July 24, 2001Assignee: GelTex Pharmaceuticals, Inc.Inventors: Chad Cori Huval, Stephen Randall Holmes-Farley, John S. Petersen, Pradeep K. Dhal
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Patent number: 6264960Abstract: The claimed invention pertains to methods for treating a patient who is at risk for a vascular (e.g., cardiovascular, cerebrovascular) event comprising administering to the patient an effective amount of a lipid-modifying drug. The claimed methods are particularly effective in patients having a lipid profile comprising a low Low Density Lipoprotein and a low High Density Lipoprotein.Type: GrantFiled: November 10, 1998Date of Patent: July 24, 2001Inventors: Sander J. Robins, Hanna Bloomfield Rubins, Dorothea Collins
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Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6262092Abstract: This invention relates to a mutual salt of amlodipine and atorvastatin, pharmaceutical compositions thereof and methods of treating angina pectoris, atherosclerosis and combined hypertension and hyperlipidemia in mammals with such a mutual salt and compositions. This invention also relates to methods of managing cardiac risk in a mammal presenting with symptoms of cardiac risk, including humans by administering such a mutual salt and compositions.Type: GrantFiled: May 24, 2000Date of Patent: July 17, 2001Assignee: Pfizer Inc.Inventors: George Chang, Ernest S. Hamanaka
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Patent number: 6262109Abstract: A method for preventing or treating high serum levels of cholesterol and lipids in a mammal, said method comprising orally administering an effective amount of natural lycopene to prevent or treat high serum levels of cholesterol or lipids to a mammal in need of such treatment. Also disclosed is an oral pharmaceutical composition in unit dosage form for oral administration for the prevention or treatment of high serum levels of cholesterol and/or lipids in a mammal, said composition comprising an effective amount of natural lycopene to prevent or treat high serum levels of cholesterol or lipids in a mammal and in a sufficient amount to achieve a level of serum cholesterol of less than 200 mg per deciliter over the course of treatment, and a pharmaceutically acceptable carrier therefor.Type: GrantFiled: August 22, 1997Date of Patent: July 17, 2001Assignee: Henkel CorporationInventors: James P. Clark, Manfred S. Dunker
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Patent number: 6255277Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.Type: GrantFiled: May 10, 1995Date of Patent: July 3, 2001Assignees: Brigham and Women's Hospital, NitroMed, Inc.Inventors: Jonathan Stamler, Joseph Loscalzo, John D. Folts
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Patent number: 6255296Abstract: A method for inhibiting the effects of cardiovascular disorders and diseases in a host susceptible to or suffering from a cardiovascular disorder or disease comprising administering to the host, a therapeutically effective amount of a first substance characterized as simulating a heparin-like effect, and a therapeutically effective amount of a second substance characterized as simulating an arginine-like effect; and a formulation for use in treating a host susceptible to or suffering from the effects of cardiovascular disorders and diseases comprising a therapeutically effective amount of a first substance characterized as simulating a heparin-like effect, and a second substance characterized an simulating an arginine-like effect, an described.Type: GrantFiled: April 30, 1999Date of Patent: July 3, 2001Assignee: EndoMatrix, Inc.Inventor: Bruce A. Daniels
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Patent number: 6251400Abstract: Compositions and methods for the prevention and treatment of neoplastic diseases and hypercholesterolemia are described. Individuals at a high risk of developing or having neoplasia or hypercholesterolemia undergoing conventional therapies may be treated with an effective dose of triterpene derivatives in citrus limonoids, polyphenolic flavonoid citrus compounds, tocotrienols or a combination of these agents.Type: GrantFiled: September 26, 1997Date of Patent: June 26, 2001Assignee: KGK Synergize INCInventors: Najla Guthrie, Elzbieta Maria Kurowska, Kenneth Kitchener Carroll
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Patent number: 6248318Abstract: A method for treating hypercholesterolemia in a patient that includes administering to the patient a therapeutically effective amount of a polydiallylamine polymer.Type: GrantFiled: March 9, 2000Date of Patent: June 19, 2001Assignee: GelTex Pharmaceuticals, Inc.Inventors: Chad Cori Huval, Stephen Randall Holmes-Farley, John S. Petersen, Pradeep K. Dhal
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Patent number: 6235767Abstract: A method to prevent or inhibit the development of arterial plaque, comprising the steps of: a. administering to a subject an amount of a green porphyrin compound effective to prevent or inhibit said development; and b. allowing the inhibition to occur in the absence of irradiation with light absorbed by the green porphyrin, or a pharmaceutical composition for preventing or inhibiting the development of arterial plaque. The composition comprises: a. an amount of a green porphyrin compound effective to prevent or inhibit the development when administered to a subject in need of such treatment, even in the absence of irradiation with light absorbed by said the green porphyrin; and b. a pharmaceutically acceptable excipient. The administration of the green porphyrin need not be accompanied by any purposeful irradiation with light.Type: GrantFiled: November 9, 1998Date of Patent: May 22, 2001Assignee: QLT, Inc.Inventors: Barbara Kelly, Julia Levy, Philippe Maria Clotaire Margaron
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Patent number: 6218403Abstract: The present invention relates to a pharmaceutical composition containing: (a) a thienopyridine derivative of formula in which R is hydrogen or a (C1-C4)alkoxycarbonyl group, or one of its pharmaceutically acceptable salts; and (b) an HMG-CoA reductase inhibitor.Type: GrantFiled: January 22, 1999Date of Patent: April 17, 2001Assignee: Sanofi-SynthelaboInventors: Georges Daste, Jean Marc Herbert
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Patent number: 6217898Abstract: A pharmaceutical compositions comprising L-carnitine or alkanoyl L-carnitine and hydroxycitric or pantothenic acid or derivatives thereof for the prevention and treatment of diseases brought about by lipid metabolism disorders, is disclosed.Type: GrantFiled: March 17, 1998Date of Patent: April 17, 2001Assignee: Sigma-Tau HealthScience S.p.A.Inventor: Claudio Cavazza
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Patent number: 6218357Abstract: A fibroin fluid obtained by adding carbon dioxide to a fibroin aqueous solution and then completely removing the carbon dioxide by pressure reduction or heating has fibroin microstructures which are dispersed in a dispersing medium, the fibroin fluid, unlike a conventional fibroin gel, having a fluidity sufficient for bringing it into the sate of a cream, having the property of excellent humidity retention and being widely usable as an agent for decreasing cholesterol or cosmetic.Type: GrantFiled: August 14, 1997Date of Patent: April 17, 2001Assignees: Hiroshi ChinzaiInventor: Seiji Terauchi
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Patent number: 6218389Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: July 31, 1998Date of Patent: April 17, 2001Assignee: The Procter & Gamble Co.Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
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Patent number: 6210686Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.Type: GrantFiled: December 18, 1998Date of Patent: April 3, 2001Assignee: Beth Israel Deaconess Medical CenterInventors: Stacey J. Bell, R. Armour Forse, Bruce R. Bistrian
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Patent number: 6203785Abstract: The present invention relates to a method for removing bile acids from a patient and certain polymers of use in the method. The method comprises the step of administering to the patient a therapeutically effective amount of a polymer composition which includes a a poly(diallylamine) polymer which is substituted with hydrophobic groups. The hydrophobic groups can be a substituted or unsubstituted, straight chain or branched C3-C24-alkyl group, an aralkyl group or an aryl group.Type: GrantFiled: December 30, 1996Date of Patent: March 20, 2001Assignee: GelTex Pharmaceuticals, Inc.Inventors: Stephen Randall Holmes-Farley, Pradeep K. Dhal, John S. Petersen
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Patent number: 6201028Abstract: Methods and compositions for the prevention and/or treatment of cardiovascular diseases, the methods comprising administering to individuals in need thereof, an effective amount of a non-steroidal anti-inflammatory drug alone or in combination with other conventional therapies to induce apoptosis, reduce proliferation, induce quiescence, inhibit cell migration, or influence cell differentiation of the cells in the vascular wall and or/induce hypolipidemia.Type: GrantFiled: December 8, 1998Date of Patent: March 13, 2001Assignees: The Rockefeller University, Mt. Sinai School of Medicine, Columbia UniversityInventors: Steven Shiff, Edward A. Fisher, I. Bernard Weinstein, Hayes M. Dansky, Urnani Reiss
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Patent number: 6187820Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for lowering lipid levels and/or increasing the HDL: LDL cholesterol ratio in humans, for example in humans having hyperlipidaemia, hypercholesterolaemia or hypertriglyceridaemia.Type: GrantFiled: March 25, 1999Date of Patent: February 13, 2001Assignee: Knoll AktiengesellschaftInventors: Peter Finian Kelly, Stephen Paul Jones
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Patent number: 6184255Abstract: The present invention has for its object to provide a medicinal composition comprising coenzyme Q10 as an active ingredient, which composition features an enhanced absorption after oral administration. The present invention is directed to a medicinal composition comprising coenzyme Q10 as an active ingredient with the reduced form of coenzyme Q10 accounting for more than 20 weight % of said coenzyme Q10.Type: GrantFiled: May 26, 1999Date of Patent: February 6, 2001Assignee: Kaneka CorporationInventors: Tatsumasa Mae, Yoshitomo Sakamoto, Souichi Morikawa, Takayoshi Hidaka
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Patent number: 6180660Abstract: Methods are described for preventing or reducing the risk of a first occurrence of a cardiovascular event using an HMG-CoA reductase inhibitor alone or in combination with another lipid altering agent. Subjects to be treated are those having an average serum total cholesterol level, an average to mildly elevated serum low-density lipoprotein cholesterol level, and a below average serum high-density lipoprotein cholesterol level, with no history of clinically evident coronary disease.Type: GrantFiled: May 13, 1998Date of Patent: January 30, 2001Assignee: Merck & Co., Inc.Inventors: Edwin J. Whitney, Geraldine Mantell
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Patent number: 6177418Abstract: The invention is directed to compounds, compositions and method of preparation of compounds of formulae I and II: wherein X, Q1, Q2, R1 and R2 are as defined by the specification. The compounds are disclosed as useful cholesterol-lowering and anti-atherosclerosis agents.Type: GrantFiled: March 16, 1998Date of Patent: January 23, 2001Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Welf von Daehne, Wagn Ole Godtfredsen
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Prevention and treatment of pathologies associated with abnormally proliferative smooth muscle cells
Patent number: 6166090Abstract: TGF-beta activators and TGF-beta production stimulators are employed to maintain or increase vessel lumen diameter in a diseased or injured vessel of a mammal. Conditions such as restenosis following angioplasty, vascular bypass grafts, transplanted organs, atherosclerosis or hypertension are characterized by a reduced vessel lumen diameter. In a preferred embodiment of the invention, TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation and/or migration of vascular smooth muscle cells over time.Type: GrantFiled: November 6, 1997Date of Patent: December 26, 2000Assignee: NeoRx CorporationInventors: David J. Grainger, James C. Metcalfe, Peter L. Weissberg -
Patent number: 6162802Abstract: A method for the treatment of a variety of cardiovascular disorders and related conditions in a mammal having at least one such disorder or condition is disclosed comprising treating the mammal with cotherapy comprising benazepril and amlodipine or pharmaceutically acceptable salts of either or both. Combination formulations of benazepril and amlodipine for use in the method are also disclosed.Type: GrantFiled: March 10, 1992Date of Patent: December 19, 2000Inventors: Joseph Papa, Marc M. J. Henis
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Patent number: 6162798Abstract: An inhibitor of atherosclerotic intimal thickening, which contains an effective amount of a compound of the formula (I): ##STR1## wherein ring X is phenyl, substituted phenyl or 5- or 6-membered heterocyclic aryl and the remaining variables are as defined herein.Type: GrantFiled: September 30, 1992Date of Patent: December 19, 2000Assignees: Nissan Chemical Industries Ltd., Kowa Company, Ltd.Inventors: Yasushi Saito, Masaki Kitahara, Mitsuaki Sakashita, Kyomi Toyoda, Toshie Shibazaki
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Patent number: 6159500Abstract: A method for the administration of glutathione orally comprising the administration of a bolus of glutathione which is pharmaceutically stabilized and encapsulated. The glutathione is administered on an empty stomach. The preferred stabilizer is ascorbic acid.Type: GrantFiled: December 31, 1997Date of Patent: December 12, 2000Assignee: Antioxidant Pharmaceuticals CorporationInventors: Harry B. Demopoulos, Myron L. Seligman
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Patent number: 6156802Abstract: The present invention has its object to provide an antihypercholesterolemic or antihyperlipidemic agent, hence a therapeutic and prophylactic drug for arteriosclerosis, which is safer and more potent in cholesterol-lowering action than the hitherto-available drugs.Type: GrantFiled: May 27, 1998Date of Patent: December 5, 2000Assignee: Kaneka CorporationInventors: Tatsumasa Mae, Takayoshi Hidaka
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Patent number: 6150336Abstract: The invention relates to certain steroidal glycoside derivatives useful as hypocholesterolemic agents and anti-atherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and use of such derivatives in treating hypercholesterolemia or atherosclerosis.Type: GrantFiled: November 21, 1997Date of Patent: November 21, 2000Assignee: Pfizer Inc.Inventors: Michael P. Deninno, Peter A. McCarthy
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Patent number: 6150332Abstract: .alpha..sub.1 -antitrypsin and peptide fragments and derivatives thereof are used to upregulate low density lipoprotein (LDL) cholesterol receptor levels in the liver, and this results in a decrease in circulating LDL cholesterol levels in the patient's circulatory system. In particular, the fragments are:Leu-Phe-Met-Gly-Lys-Val-Val-Asn (SEQ ID NO:16) - Phe-Met-Gly-Lys-Val-Val-Asn (SEQ ID NO:17).Type: GrantFiled: March 12, 1998Date of Patent: November 21, 2000Assignee: Virginia Commonwealth UniversityInventors: H. Tonie Wright, S. Janciauskiene
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Patent number: 6139871Abstract: The present invention provides compositions and methods for treating atherosclerosis. The compositions comprise unilamellar liposomes having an average diameter of 100-150 nanometers. Methods for treating atherosclerosis employing the compositions of the present invention are also provided.Type: GrantFiled: October 20, 1998Date of Patent: October 31, 2000Assignee: The University of British ColumbiaInventors: Michael J. Hope, Wendi Rodrigueza
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Patent number: 6136798Abstract: The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical compositions that contain a compound that inhibits the association of platelet-derived growth factor and phosphatidylinosital 3-kinase, and methods of treating cancer, restenosis, arthritis, dermatitis, atherosclerosis, vein graft intimal hyperplasia, neointimal hyperplasia of vascular smooth muscle and psoriasis using compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase.Type: GrantFiled: February 22, 1999Date of Patent: October 24, 2000Assignee: Warner-Lambert CompanyInventors: Wayne Livingston Cody, Annette Marian Doherty, Scott R. Eaton, Robert Lee Panek
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Patent number: 6136800Abstract: This invention describes the new 17-difluoromethylene-estratrienes of general formula I ##STR1## in which R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group,R.sup.5 is a methyl or ethyl group, andR.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group in .alpha.- or .beta.-position,R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyloxy group in .alpha.- or .beta.-position,R.sup.4 is a hydrogen atom in .alpha.- or .beta.-position, and A, B, D, E and G each is a hydrogen atom, and optionally at least one of substituent pairsG and R.sup.2, R.sup.2 and R.sup.4, R.sup.4 and A, A and R.sup.3, B and D, D and E is a double bond.Type: GrantFiled: March 8, 1999Date of Patent: October 24, 2000Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Gabor Rubayi
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Patent number: 6133311Abstract: A method for treating or preventing an elevated blood lipid level-related diseases such as hyperlipidemia, arteriosclerosis, angina pectoris, stroke and hepatic diseases in a mammal, which comprises administering thereto an effective amount of tannin, gallic acid or ellagic acid.Type: GrantFiled: September 15, 1999Date of Patent: October 17, 2000Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Song-Hae Bok, Tae-Sook Jeong, Ki-Hwan Bae, Yong-Bok Park, Myung-Sook Choi, Surk-Sik Moon, Yong-Kook Kwon, Eun-Sook Lee, Byung-Hwa Hyun, Yang-Kyu Choi, Chul-Ho Lee, Sae-Bom Lee, Young-Bae Park, Hyo-Soo Kim
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Patent number: 6129918Abstract: A method and composition are described for reducing the elevated plasma homocysteine level in mammals (humans) by oral administration of a therapeutically effective amount of Allium plants or extracts thereof, preferably garlic, with or without one or more vitamins such as B.sub.6, B.sub.12 and folic acid in an acceptable pharmaceutical carrier. Enhanced effectiveness is achieved with a combination of Allium plants or extracts thereof, preferably garlic, with vitamins such as B.sub.6, B.sub.12 and folic acid. The described method and composition are effective for prevention, treating or ameliorating cardiovascular diseases such as myocardial infarction, stroke and multiple arteriosclerosis by the reduction or prevention of high levels of plasma homocysteine, one of the major causes for such diseases. Methods and compositions are disclosed.Type: GrantFiled: August 13, 1998Date of Patent: October 10, 2000Assignee: Wakunaga of America Co., Ltd.Inventor: Harunobu Amagase
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Patent number: 6127339Abstract: Disclosed is a peptide for binding thereto a low density lipoprotein, which has an amino acid sequence represented by the formula (I) or (II) and which has an electric charge (E) satisfying the following requirement: +1.ltoreq.E.ltoreq.+4 wherein E is defined by the formula: E=(the number of positive functional groups present in the peptide)-(the number of negative functional groups present in the peptide): ##STR1## wherein each a is independently Phe or Trp; each p is independently Arg or Lys; each X.sup.1, each X.sup.2 and each X.sup.3 are individually, independently an arbitrary amino acid residue; and m, n, p, q and r satisfy the following requirement: 2.ltoreq.m+n+p+q+r.ltoreq.10, wherein m and n satisfy the following requirements: 2.ltoreq.m+n.ltoreq.10 and 1.ltoreq.m, n.ltoreq.9, and p, q and r satisfy the following requirements: 0.ltoreq.p+q+r.ltoreq.8, 0.ltoreq.p, r.ltoreq.8 and 0.ltoreq.q.ltoreq.5.Type: GrantFiled: December 18, 1997Date of Patent: October 3, 2000Assignees: Asahi Kasei Kogyo Kabushiki Kaisha, Asahi Medical Co., Ltd.Inventors: Yoshihiro Hatanaka, Masaharu Aritomi
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Patent number: 6127403Abstract: Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors.To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.Type: GrantFiled: August 12, 1999Date of Patent: October 3, 2000Assignee: Sankyo Company, Ltd.Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura, Katsuo Wada
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Patent number: 6124309Abstract: The present invention is a combination of an ACAT inhibitor, for example, sulfamic acid, [[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl) phenyl ester, and an HMG-CoA-reductase inhibitor, for example, atorvastatin, effective for lipid regulation. The combination of agents results in a greater reduction in plasma VLDL and LDL cholesterol and increases HDL cholesterol than either alone resulting in a less atherogenic lipoportein profile The combination is useful in the treatment of patents with or at risk of developing ischemic syndromes in order to restore endogenous vascular endothelium-dependent activities.Type: GrantFiled: April 7, 1998Date of Patent: September 26, 2000Assignee: Warner-Lambert CompanyInventor: Thomas M. A. Bocan
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Patent number: 6121319Abstract: This invention is a method and composition for the inhibition of VCAM-1, and in particular for the treatment of cardiovascular or inflammatory disease, including atherosclerosis, that includes the administration of an effective amount of an ester of probucol.Type: GrantFiled: May 14, 1998Date of Patent: September 19, 2000Assignee: AtheroGenics, Inc.Inventor: Patricia K. Somers
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Patent number: 6117909Abstract: The present invention is directed to new therapeutic uses of compounds of formula: ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group. The uses are cerebrovascular disease such as stroke, peripheral vascular diseases, and restenosis.Type: GrantFiled: January 26, 1998Date of Patent: September 12, 2000Assignee: Warner-Lambert CompanyInventor: Brian Robert Krause
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Patent number: 6114572Abstract: The present invention provides compounds of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Y is thio, oxy or a methylene group; Z is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;R.sub.1 is C.sub.1 -C.sub.6 alkyl; andR.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;or a stereoisomer thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as anti-oxidant chemical additives useful for preventing oxidative deterioration in organic materials.Type: GrantFiled: November 19, 1997Date of Patent: September 5, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Roger A. Parker, Paul S. Wright, Steven J. Busch, Kim S. Chen, Mark T. Yates
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Patent number: 6107346Abstract: The present application relates to a series of compounds, and pharmaceutical formulations thereof, of the formula ##STR1## which provide a method of inhibiting hyperlipidemia, especially hypercholesterolemia, and the pathological sequelae thereof, in mammals, including humans.Type: GrantFiled: August 4, 1998Date of Patent: August 22, 2000Assignee: Eli Lilly and CompanyInventor: George Joseph Cullinan
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Patent number: 6107337Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, bone resorption, loosening of artificial joint implants, atherosclerosis, multiple sclerosis, occular angiogenisis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.Type: GrantFiled: August 6, 1998Date of Patent: August 22, 2000Assignee: Pfizer Inc.Inventor: Ralph P. Robinson
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Patent number: 6103769Abstract: Disclosed are pharmaceutical composition of a sterile, injectable physiologically acceptable solution containing nitric oxide (NO), processes for preparing the compositions and a process for detecting physiologically present NO. With these NO solutions, NO in high doses can trigger locally in vessels, e.g. coronary vessels, specific local biological effects such as relaxation of the smooth vascular musculature, inhibition of thee adhesion of thrombocytes, etc., without producing systemic side-effects, such as for example, a critical drop in blood pressure, in spite of the high does. The detection process enables the presence of an endothelial dysfunction to be established from the whole blood of humans and other mammals.Type: GrantFiled: July 30, 1998Date of Patent: August 15, 2000Assignee: Schwarz Pharma AGInventor: Malte Kelm
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Patent number: 6099851Abstract: A method of decreasing atherosclerosis and its complications including but not limited to myocardial infarction, stroke and peripheral vascular disease comprising administering to a human or animal an amount of Leuprolide acetate is sufficient to decrease atherosclerosis and its complications.Type: GrantFiled: June 2, 1998Date of Patent: August 8, 2000Inventors: Kenneth M. Weisman, Michael Goldberg
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Patent number: 6090852Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.Type: GrantFiled: January 20, 1999Date of Patent: July 18, 2000Assignee: Pfizer IncInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6087353Abstract: The present invention provides a esterified and subsequently hydrogenated phytosterol composition for use alone or for incorporation into foods, beverages, pharmaceuticals, nutraceuticals, and the like. The composition has the advantage of enhanced solubility/dispersability, increased molar potency and enhanced stability over naturally isolated phytosterol compositions. Methods for the esterification and subsequent hydrogenation of the phytosterols are also provided.Type: GrantFiled: May 15, 1998Date of Patent: July 11, 2000Assignee: Forbes Medi-Tech Inc.Inventors: David John Stewart, Radka Milanova, Jerzy Zawistowski, Simon Howard Wallis
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Patent number: 6087331Abstract: Novel, substantially isolated isoforms of human platelet-endothelial cell adhesion molecule-1's, DNAs coding for transcripts that encode the novel isoforms and others, including a previously identified soluble isoform, methods of using such DNAs to make isoforms by expressing the DNA's, and promoter segments controlling transcription of human platelet-endothelial cell adhesion molecule-1 genes are provided. The novel isoforms differ from the complete human platelet-endothelial cell adhesion molecule-1's in lacking one or more segments near the C-terminus encoded by exons 10-15 of the genes for the full length molecules and arise in vivo from alternative splicing of the transcript from the genes.Type: GrantFiled: June 7, 1995Date of Patent: July 11, 2000Assignee: The Blood Center of Southeastern WisconsinInventors: Peter J. Newman, Richard J. Gumina, Nancy Kirshbaum
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Patent number: 6083497Abstract: A method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of a non-absorbable polydiallylamine polymers.Type: GrantFiled: November 5, 1997Date of Patent: July 4, 2000Assignee: GelTex Pharmaceuticals, Inc.Inventors: Chad Cori Huval, Stephen Randall Holmes-Farley, John S. Petersen, Pradeep K. Dhal
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Patent number: 6080422Abstract: The present invention provides an improved mode of operation of an apparatus for angioplasty or cardiac catheterization, apparatus for angioplasty and cardiac catheterization, and method of angioplasty or cardiac catheterization. The improvement and improved mode of operation includes the step of administering a therapeutically effective amount of a lipid acceptor during angioplasty or cardiac catheterization of a subject with the apparatus or component thereof. The lipid acceptor is selected from the group consisting of a large liposome comprised of phospholipids substantially free of sterol and small acceptors. The effective period of time is in the range of about less than 1 minute to about two years from the time of the angioplasty or cardiac catheterization. The improved angioplasty or cardiac catheterization apparatus includes means for administering a therapeutically effective amount of a lipid acceptor, and optional co-administration means for administering the lipid acceptor and a diagnostic agent.Type: GrantFiled: October 11, 1996Date of Patent: June 27, 2000Assignee: Talaria Therapeutics, Inc.Inventor: Kevin Jon Williams
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Patent number: 6066653Abstract: A method is provided for inhibiting or treating diseases associated with acid lipase deficiency by administering to a patient an MTP inhibitor, alone or optionally, in combination with another cholesterol lowering drug, such as pravastatin.Type: GrantFiled: January 10, 1998Date of Patent: May 23, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Richard E. Gregg, John R. Wetterau, II