Z Forms A Phenoxy Alkyl Or Phenoxy Alkenyl Radical Patents (Class 514/543)
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Patent number: 6548699Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.Type: GrantFiled: August 6, 1999Date of Patent: April 15, 2003Assignee: Atherogenics, Inc.Inventor: Patricia K. Somers
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Patent number: 6534546Abstract: Compounds represented by the general formula (1): (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1997Date of Patent: March 18, 2003Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toshio Honda, Toshihiko Makino, Toshiaki Nagafuji, Yasushi Kitoh, Nobuaki Kimura
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Patent number: 6534088Abstract: This invention discloses an orally administered pharmaceutical composition for the treatment of elevated levels of cholesterol and related conditions comprising a statin and fenofibrate in the form of microparticles of solid fenofibrate that are stabilized by phospholipid as a surface active substance, wherein a therapeutically effective amount of the composition provides the statin and a quantity of fenofibrate to a fasted human patient that is greater than 80% of the quantity of fenofibrate provided by the same amount of the composition when administered to the same patient who has been fed a high fat meal.Type: GrantFiled: April 20, 2001Date of Patent: March 18, 2003Assignee: SkyePharma Canada Inc.Inventors: Pol-Henri W. Guivarc'h, Indu Parikh, Robert A. Snow
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Patent number: 6521664Abstract: The present invention provides non-peptide organic compounds that have a structure analogous to or reminiscent of the TMOF structure and have pesticidal activity. Thus the present invention concerns pesticidal compounds that inhibit digestion in pests by terminating or otherwise blocking synthesis of digestive enzymes by activating a TMOF receptor (collectively referred to herein as “pesticidal compounds”). The pesticidal compounds and other compounds of the present invention are usefully employed in the control of pests, particularly insect pests such as mosquitoes, which ingest blood.Type: GrantFiled: December 8, 1999Date of Patent: February 18, 2003Assignee: North Carolina State UniversityInventor: Russell J. Linderman
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Patent number: 6511985Abstract: The present invention relates to the combination of the 3-hydroxy-3-methylglutaryl-coenzyme A inhibitor (HMG-CoA inhibitor) cerivastatin with fibrates and its use in the prophylaxis and treatment of disorders of lipid metabolism.Type: GrantFiled: June 18, 2001Date of Patent: January 28, 2003Assignee: Bayer AktiengesellschaftInventors: Joachim Ippen, Ulrike Schopen, Reiner Ziegler, Fritz Schückler
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Patent number: 6488928Abstract: The present invention concerns a product for topical application, capable of releasing a hydroxy acid on the skin, containing a lipase as enzyme and at least one precursor of the hydroxy acid. The precursor is an ester of the hydroxy acid, containing at least one ester functional group having a saturated or unsaturated, linear or branched chain and from 2 to 25 carbon atoms. According to a preferred form, the precursor and the lipase are packaged so as not to be in contact with one another until the time of application to the skin.Type: GrantFiled: October 24, 1995Date of Patent: December 3, 2002Assignee: L'OrealInventors: Emmanuelle Maurin, Daniel Sera, Gerard Guth
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Patent number: 6472421Abstract: Described are methods for treating, preventing, or reducing the risk of the onset of Alzheimer's disease by administering a therapeutically effective amount of an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (“HMG CoA reductase inhibitor”) to a patient who is at risk for a coronary or cerebrovascular event or at risk for Alzheimer's disease.Type: GrantFiled: November 13, 1998Date of Patent: October 29, 2002Assignee: Nymox CorporationInventor: Benjamin Wolozin
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Patent number: 6462064Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.Type: GrantFiled: February 4, 2000Date of Patent: October 8, 2002Assignee: Galderma Research & Development S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6448238Abstract: The invention provides novel non-&bgr;-lactam inhibitors of &bgr;-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with &bgr;-lactam antibiotics to treat &bgr;-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.Type: GrantFiled: July 19, 2000Date of Patent: September 10, 2002Assignee: Northwestern UniversityInventors: Brian K. Shoichet, Grady Scott Weston
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Publication number: 20020123524Abstract: The present 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 present methods are particularly effective in patients having a lipid profile comprising a low Low Density Lipoprotein (LDL-C) and a low High Density Lipoprotein (HDL-C). Patients having low levels of LDL-C and HDL-C include diabetics. As a result, the present invention includes methods for treating diabetics by administering a lipid-modifying drug such as a fibric acid.Type: ApplicationFiled: July 23, 2001Publication date: September 5, 2002Inventors: Sander J. Robins, Hanna Bloomfield Rubins, Dorothea Collins
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Patent number: 6436990Abstract: The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is In another embodiment, the composition is In yet another embodiment, the composition is Additional alternative embodiments are R or R″ that are therapeutic moieties.Type: GrantFiled: October 27, 2000Date of Patent: August 20, 2002Assignee: Nobex CorporationInventors: Nnochiri Nkem Ekwuribe, Jennifer A. Riggs
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Patent number: 6433012Abstract: The present invention relates to methods for effectively inhibiting inflammatory diseases, such as Crohn's disease and ulcerative colitis. In other aspects, this invention relates to methods of reducing or inhibiting granulomas.Type: GrantFiled: September 6, 2000Date of Patent: August 13, 2002Assignees: Large Scale Biology Corp., SRI InternationalInventors: Daniel Tuse, Charles Hiebert, Keith R. Laderoute, Nahid Waleh
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Patent number: 6417174Abstract: The invention provides novel non-&bgr;-lactam inhibitors of &bgr;-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with &bgr;-lactam antibiotics to treat 62 -lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.Type: GrantFiled: June 6, 2000Date of Patent: July 9, 2002Assignee: Northwestern UniversityInventors: Brian Shoichet, Scott Weston
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Patent number: 6391916Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.Type: GrantFiled: July 21, 2000Date of Patent: May 21, 2002Assignee: The Hong Kong University of Science and TechnologyInventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
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Publication number: 20020058065Abstract: This invention discloses an orally administered pharmaceutical composition comprising microparticles of solid fenofibrate that are stabilized by a phospholipid surface active substance that is present during the preparation of the microparticles, wherein a therapeutically effective amount of the composition provides a quantity of fenofibrate active species to a fasted human patient in need of treatment by fenofibrate that is greater than 80% of the quantity of fenofibrate active species provided by the same amount of the composition when administered to the same patient who has been fed a high fat meal consisting of at least 1000 calories, 50% of which are from fat.Type: ApplicationFiled: April 20, 2001Publication date: May 16, 2002Inventors: Pol-Henri Guivarc'h, Gary W. Pace, Robert A. Snow, Awadesh K. Mishra
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Patent number: 6387951Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6369071Abstract: An organic compound is provided which contains at least one nitric oxide donor group and at least one group being, or being adapted to be converted in vivo to a free sulfhydryl group. A preferred compound contains at least one sulfhydryl group, either in the reduced —SH form or in the oxidized —S—S-disulfide form.Type: GrantFiled: December 30, 1999Date of Patent: April 9, 2002Assignee: Yissum Research Development Company of The Hebrew University of JerusalemInventor: Abdullah Haj-Yehia
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Patent number: 6365610Abstract: The invention provides a urokinase production inhibitor or angiogenesis inhibitor comprising as an active component an ozonide derivative represented by the formula (1), and method of prevention or therapy using the inhibitor wherein A is an oxygen atom or N—R (wherein R is phenyl or phenyl having as a substituent lower alkyl having 1 to 6 carbon atoms, lower alkoxyl having 1 to 6 carbon atoms or a halogen atom); B is an oxo group or —R4; and (1) when A is an oxygen atom, R1 is a hydrogen atom, etc., R2 is phenyl, etc., R3 is a hydrogen atom, etc., B is an oxo group or —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.; (2) when A is N—R, R1 is a hydrogen atom, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., B is —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.Type: GrantFiled: March 28, 2000Date of Patent: April 2, 2002Assignee: Taiho Pharmaceutical Company Ltd.Inventors: Takuma Sasaki, Masatomo Nojima
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Patent number: 6346539Abstract: The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also for treating skin cancer. The piperine and analogues or derivatives thereof may also be used to cosmetically promote or enhance the natural coloration of the skin.Type: GrantFiled: January 16, 2001Date of Patent: February 12, 2002Assignee: BTG International LimitedInventors: Amala Raman, Zhixiu Lin, Charles Hider Robert, Radhakrishnan Venkatasamy
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Publication number: 20020010195Abstract: The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.Type: ApplicationFiled: December 7, 2000Publication date: January 24, 2002Inventors: Soumitra S. Ghosh, Scott W. Miller, Robert E. Davis, Walter H. Moos
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Publication number: 20020002139Abstract: The invention provides a method of modulating the immune system. Also provided is a method of treating a pathology associated with increased levels of a tumor necrosis factor. The invention further provides a method of treating a pathology resulting from infection by human immunodeficiency virus. Also provided is a method of treating chronic graft vs. host disease. Finally, the invention provides a method of promoting wound healing in a subject.Type: ApplicationFiled: December 4, 2000Publication date: January 3, 2002Applicant: Omega Pharmaceutical, Inc.Inventors: Thomas W. Hodge, David W. Boykin
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Patent number: 6319949Abstract: A method for preventing fungal diseases in crops which comprises the steps of: (a) applying to a crop an aqueous or a non-aqueous spray composition which includes a pesticide and a spray adjuvant including a solvent and an emulsifier, wherein the solvent is a mixture of aliphatic hydrocarbons having a distillation range of about 520 to 600° F. and an aromatic content of about 1% or less, or the solvent is a single or combination of C6-C18 fatty alcohol(s); and (b) applying chlorothalonil to the crop previously to, simultaneously with, or subsequently to the application of the aqueous spray composition, wherein phytotoxicity associated with the application of chlorothalonil is reduced or eliminated.Type: GrantFiled: November 4, 1996Date of Patent: November 20, 2001Assignee: Syngenta LimitedInventors: Jeffrey R. Schussler, Robert E. Moser, Kevin E. Crosby, John R. Washington
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Publication number: 20010034367Abstract: The invention is directed to novel pharmaceutical compositions comprising chemicals agents that are useful in the treatment and prevention of cystic fibrosis and the prevention of signs and symptoms of this disease. These pharmaceutical compositions are surprisingly successful in the treatment disorders related to cystic fibrosis including disorders of blood production. Many of these compositions of the invention are even more effective when administered to a patient in pulses. Pulse therapy is not a form of discontinuous administration of the same amount of a composition over time, but comprises administration of the same dose of the composition at a reduced frequency or administration of reduced doses.Type: ApplicationFiled: February 15, 2001Publication date: October 25, 2001Inventors: Douglas V. Faller, Susan P. Perrine, George Stamatoyannopoulos
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Patent number: 6303599Abstract: A fungicidal mixture comprises a.1) a carbamate of the formula I.a, in which X is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a.2) the oxime ether carboxamide of the formula I.b and b.1) 4-[2-methyl-3-(4-tert-butylphenyl)propyl]-2,6-dimethylmorpholine or b.2) 4-(C10-C13-alkyl)-2,6-dimethylmorpholine or b.3) (RS)-1-[3-(4-tert-butylphenyl)-2-methylpropyl]piperidine and c) a further active ingredient from the class of the strobilurin fungicides (III), in a synergistically effective amount.Type: GrantFiled: December 1, 1999Date of Patent: October 16, 2001Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Reinhold Saur, Hubert Sauter, Bernd Müller, Erich Birner, Joachim Leyendecker, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6303621Abstract: The present invention is directed to a method for treating cancers by administering a pharmaceutically effective amount of a diiodo thyronine analogue having no significant hormonal activity and a vinca alkaloid or biologically active analog thereof. The present invention also features novel pharmaceutical compositions comprising the same.Type: GrantFiled: April 21, 1999Date of Patent: October 16, 2001Assignee: Octamer, Inc.Inventor: Ernest Kun
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Patent number: 6284258Abstract: The present invention relates to compounds that are two-part molecules, and compositions containing such compounds, in which one part is designed to become covalently bonded to the skin (bonding agent) and the other part (a characteristic use agent) is designed to impart some characteristic use, such as emolliency, moisturizing effect, anti-acne, anti-wrinkle, anti-pain, antimicrobial, antifungal, antiviral, anti-irritation, skin tanning and skin lightening effects, extended protection of the skin (e.g., from ultraviolet light, by incorporation of a sunscreen component; from toxic and/or irritating substances; from insects and skin parasites, by incorporation of insecticides and/or insect repellants; from free radicals or other agents, as in aging, by incorporation of antioxidants), or dyeing of hair, skin nails, wool or fuir. The covalently bonded part may also be useful to impart skin strengthening effect (e.g., from shear forces) or as wound healing agents.Type: GrantFiled: September 10, 1998Date of Patent: September 4, 2001Assignee: Arizona Board of RegentsInventors: Seth D. Rose, Rosemarie F. Hartman, Carmen Chow, Cathryn M. Rose, K. Daniel Rose
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Patent number: 6277405Abstract: The invention provides a micronized fenofibrate composition. The micronized fenofibrate composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or with 0.025M sodium lauryl sulfate. The composition can further comprise hydrophilic polymers, surfactants, hydrosoluble carriers, outer phases or layers, or other pharmaceutically acceptable excipients. The immediate-release fenofibrate composition is preferably in the form of a tablet or in the form of granules inside a capsule.Type: GrantFiled: May 18, 2000Date of Patent: August 21, 2001Assignee: Labaratoires Fournier, S.A.Inventors: André Stamm, Pawan Seth
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Patent number: 6274608Abstract: Disclosed are novel compounds of formula I wherein R1, R2, R3, L, X and Y are as defined in the specification. These compounds are useful in the treatment of conditions mediated by nuclear receptors, in particular the Retinoid X Receptor (RXR) and the Peroxisome Proliferator-Activated Receptor (PPAR) families. Such conditions include diabetes and obesity.Type: GrantFiled: April 18, 2000Date of Patent: August 14, 2001Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Anthony Murray, Lone Jeppesen, Paul Stanley Bury, Ingrid Pettersson
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Patent number: 6150407Abstract: The present invention relates to methods for effectively inhibiting unwanted angiogenesis. More particularly, this invention relates to methods of treating diseases that show unwanted angiogenesis and to delivering anti-angiogenic activity to a mammal. In other aspects this invention relates to methods of reducing the level of tumor necrosis factor .alpha..Type: GrantFiled: March 22, 1999Date of Patent: November 21, 2000Assignees: Large Scale Biology Corporation, SRI InternationalInventors: Daniel Tuse, Charles Hiebert, Keith R. Laderoute, Nahid Waleh
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Patent number: 6136852Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.Type: GrantFiled: March 8, 1999Date of Patent: October 24, 2000Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
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Patent number: 6127415Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.Type: GrantFiled: April 14, 1999Date of Patent: October 3, 2000Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6121299Abstract: This invention relates to methods of modulating inflammation in mammals. Inflammation is modulated by regulating the cytochrome P-450 pathway. Inflammation is reduced by treating the subject with substances, such as bezafibrate and clofibrate, which induce the P-450 pathway. Inflammation is promoted by treating the subject with substances, such as proadifen, econazole, and clotrimazole, which inhibit the cytochrome P-450 pathway.Type: GrantFiled: March 30, 1999Date of Patent: September 19, 2000Assignee: Lovelace Respiratory Research InstituteInventors: Wieslaw Kozak, Matthew J. Kluger, Yohannes Tesfaigzi
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Patent number: 6107517Abstract: Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.Type: GrantFiled: June 30, 1999Date of Patent: August 22, 2000Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Hikari A.I. Yoshihara, Grazia Chiellini, Timothy J. Mitchison
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Patent number: 6096783Abstract: Cyclobutane analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: December 15, 1998Date of Patent: August 1, 2000Assignee: Alcon Laboratories, Inc.Inventor: Mark R. Hellberg
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Patent number: 6083982Abstract: Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.Type: GrantFiled: April 9, 1998Date of Patent: July 4, 2000Assignee: Loma Linda University MedicalInventors: William J. Wechter, David E. Murray, Darko Kantoci, Barry H. Levine, Elaine J. Benaksas
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Patent number: 6080778Abstract: Blood cholesterol levels are correlated with production of amyloid .beta. protein (A.beta.), and are predictors of populations at risk of developing AD. Methods for lowering blood cholesterol levels can be used to decrease production of A.beta., thereby decreasing the risk of developing AD. The same methods and compositions can also be used for treating individuals diagnosed with AD. Methods include administration of compounds which increase uptake of cholesterol by the liver, such as the administration of HMG CoA reductase inhibitors, administration of compounds which block endogenous cholesterol production, such as administration of HMG CoA reductase inhibitors, administration of compositions which prevent uptake of dietary cholesterol, and administration of combinations of any of these which are effective to lower blood cholesterol levels. Methods have also been developed to predict populations at risk, based on the role of cholesterol in production of A.beta..Type: GrantFiled: March 23, 1998Date of Patent: June 27, 2000Assignee: Children's Medical Center CorporationInventors: Bruce A. Yankner, Philip Nadeau
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Patent number: 6075014Abstract: The invention provides novel non-.beta.-lactam inhibitors of .beta.-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with .beta.-lactam antibiotics to treat .beta.-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.Type: GrantFiled: June 12, 1998Date of Patent: June 13, 2000Assignee: Northwestern UniversityInventors: Scott Weston, Brian Shoichet
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Patent number: 6074634Abstract: The present invention provides an composition for attracting noctuid and/or other lepidopteran species. Liquid and solid formulations are provided, along with methods for their use, for controlling or eliminating noctuid and/or other lepidopteran species, and/or protecting plants susceptible to noctuid and/or other lepidopteran species damage.Type: GrantFiled: October 5, 1998Date of Patent: June 13, 2000Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Juan D. Lopez, Jr., Ted N. Shaver, Kenneth R. Beerwinkle, Peter D. Lingren
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Patent number: 6063815Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: American Home Products CorporationInventor: Paul J. Dollings
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Patent number: 6060515Abstract: Disorders of the skin and mucous membrane that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of compounds that are either activators of the farnesoid X receptor, activators of the peroxisome proliferator-activated receptor .alpha., and oxysterol activators of the LXR.alpha. receptor. The same compounds are also effective in treating disorders of epidermal differentiation and proliferation.Type: GrantFiled: June 16, 1999Date of Patent: May 9, 2000Assignee: The Regents of the University of CaliforniaInventors: Peter M. Elias, Nathan N. Bass, Karen Hanley, Kenneth R. Feingold
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Method of treating malignant tumors with thyroxine analogues having no significant hormonal activity
Patent number: 6017958Abstract: The present invention provides methods for treating cancer, particularly malignant tumors, with thyroxine analogues having no significant hormonal activity. A thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer. Particularly preferred thyroxine analogues are those capable of causing about 35 percent or more inhibition of initial velocity of microtubule protein assembly in vitro.Type: GrantFiled: April 3, 1997Date of Patent: January 25, 2000Assignee: Octamer, Inc.Inventors: Ernest Kun, Jerome Mendeleyev -
Patent number: 6013649Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfone inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: January 11, 2000Assignee: Monsanto CompanyInventors: John N. Freskos, S. Zaheer Abbas, Gary A. DeCrescenzo, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Patent number: 5990157Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.Type: GrantFiled: July 2, 1998Date of Patent: November 23, 1999Assignee: Colgate Palmolive CompanyInventors: Germaine Zocchi, Pierre Fonsny
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Patent number: 5981586Abstract: Methods of inhibiting the proliferation of keratinocytes and inflammation of the skin comprising administering to a human in need of treatment an effective amount of a compound that modifies the activity of the peroxisome proliferator activated receptor gamma (PPAR.gamma.) in skin; and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: May 22, 1998Date of Patent: November 9, 1999Inventor: Harrihar A. Pershadsingh
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5939583Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## in which T is a pharmaceutically-acceptable substituent group; A is CH.sub.2, CH, or N; G is CH.sub.2 or CH; and R.sup.1 is any of a variety of disclosed substituent groups. The class of compounds of the invention includes ring-containing materials in which the units A and G are joined. The compounds of the invention are mixtures of diastereomers, or individual diastereomers making up these mixtures.Type: GrantFiled: October 30, 1997Date of Patent: August 17, 1999Assignee: Bayer CorporationInventors: Harold C. E. Kluender, Susan M. Bjorge, Lisa Marie Zadjura, William Frederick Brubaker
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Patent number: 5925677Abstract: A lacrimation accelerating agent containing a ligand of serotonin receptor as an active ingredient. Also provided is a method for preventive and/or therapeutic treatment of a disease caused by a deficiency of lacrimal fluid such as dry eye, which comprises the step of administering to a mammal an effective amount of a ligand of a serotonin receptor such as sarpogrelate hydrochloride.Type: GrantFiled: June 16, 1997Date of Patent: July 20, 1999Assignee: Mitsubishi Chemical CorporationInventors: Tomiya Mano, Shunji Sogo
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Patent number: 5883294Abstract: Selective thyroid hormone agonists are disclosed that are highly selective for the TR.beta. subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.Type: GrantFiled: June 18, 1997Date of Patent: March 16, 1999Assignee: The Regeants of the University of CaliforniaInventors: Thomas S. Scanlan, Grazia Chiellini, Hikari Yoshihara, James Apriletti, John D. Baxter, Ralff C. J. Ribeiro
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Patent number: RE37770Abstract: Disorders of the skin and mucous membrane that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of compounds that are either activators of the farnesoid X receptor, activators of the peroxisome proliferator-activated receptor &agr;, and oxysterol activators of the LXR&agr; receptor. The same compounds are also effective in treating disorders of epidermal differentiation and proliferation.Type: GrantFiled: January 8, 2001Date of Patent: June 25, 2002Assignee: The Regents of the University of CaliforniaInventors: Peter M. Elias, Nathan N. Bass, Karen Hanley, Kenneth R. Feingold