Abstract: This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Abstract: The invention pertains to a composition of a ketone peroxide comprising a) a peroxide derivative of the formula HOO—C(R1)(R2)—OOH wherein R1 is a branched or unbranched alkyl group with 1 to 4 carbon atoms or alkenyl group with 2 to 4 carbon atoms; and R2 is a branched or unbranched alkyl or alkenyl group with 5 to 12 carbon atoms; and b) a branched or unbranched hydrocarbon solvent; the peroxide derivative of a) having a solubility more than 40 g in 100 g of the solvent of b) at 20° C.; and comprises less than 10 wt % of a peroxide derivative of the formula HOO—C(R1)(R2)—OO—C(R1)(R2)—OOH, wherein R1 and R2have the previously given meanings.
Type:
Application
Filed:
August 10, 2004
Publication date:
December 9, 2004
Inventors:
Bernhard De Vries, Andreas Petrus Van Swieten, Ejaz Ahmed Syed
Abstract: The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I)
in which
A1 represents a single bond or represents alkanediyl (alkylene) having 1 to 3 carbon atoms,
A2 represents alkanediyl (alkylene) having 1 to 3 carbon atoms, and
R1, R2, R3, R4 and R5 are each as defined in the description,
and to novel intermediates, to processes for their preparation and to their use as herbicides.
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
November 30, 2004
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus-Helmut Müller, Hans-Georg Schwarz, Stefan Lehr, Otto Schallner, Dorothee Hoischen, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
Abstract: Insect and animal control water based concentrate and and dilute compositions and method in which a polymer and solubilizer are selected to provide a cross-linked film with matrices of sufficient capacity for trapping and being plated by an active ingredient particularly methyl nonyl ketone and other ingredients for slow degradation by environmental factors and release the active ingredient in an area to be controlled.
Abstract: The present invention provides a method capable of simply producing optically active halopropanediol derivatives useful as pharmaceutical intermediates from inexpensive raw materials.
Abstract: A substance for inducing apoptosis represented by specific formulae. A pharmaceutical composition which can be used for an anticancer agent containing said substance.
Abstract: Compositions and methods employing the compositions for attracting arthropods. The compositions comprise at least one compound of formula I and at least one compound from group II.
Type:
Grant
Filed:
May 4, 2001
Date of Patent:
October 5, 2004
Assignees:
The United States of America as represented by the Secretary
of the Agriculture, University of Florida
Inventors:
Ulrich R. Bernier, Donald R. Barnard, Matthew M. Booth, Daniel L. Kline, Kenneth H. Posey, Richard A. Yost
Abstract: A method of repelling an insect pest such as a tick, mosquito or cockroach comprises applying to a subject or substrate, in an amount effect to repel the insect pest, a compound of Formula I:
wherein R is C4-C20 linear or branched alkyl. Particularly preferred compounds of Formula (I) are 2-tridecanone and 2-undecanone.
Abstract: This present invention provides a new use of tanshinone derivatives as acetylcholinesterase inhibitors and in treating diseases associated with the depletion of acetylcholine such as cognitive impairment including Alzheimer's disease, insomnia, vascular dementia, memory loss, disorders of attention and other sleeping disorders. The active compounds commonly found in the root of Salvia genus, particularly Salvia miltiorrhiza, Danshen.
Type:
Application
Filed:
March 24, 2003
Publication date:
September 30, 2004
Inventors:
Pang-Chui Shaw, Michelle Tsz-Wan Ho, Kwok-Pui Fung, David Chi-Cheong Wan
Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.
Abstract: This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Abstract: Disclosed are methods of lowering plasma CRP levels, reducing systemic inflammation, and inhibiting proinflammatory cytokine induced CRP production by administering an effective amount of a substituted dialkyl ether, substituted alkyl, substituted aryl-alkyl, substituted dialkyl thioether, substituted dialkyl ketone, substituted-alkyl, or a pharmaceutically acceptable salt of the substituted dialkyl ether, substituted alkyl, substituted aryl-alkyl, substituted dialkyl thioether, substituted dialkyl ketone, or substituted-alkyl or a pharmaceutical composition comprising a substituted dialkyl ether, substituted alkyl, substituted aryl-alkyl, substituted dialkyl thioether, substituted dialkyl ketone, substituted-alkyl.
Type:
Application
Filed:
November 13, 2003
Publication date:
August 26, 2004
Inventors:
Rebecca Bakker-Arkema, Ok Hwang, Sotirios Karathanasis, Diane MacDougall
Abstract: Certain fatty acids and related compounds useful in the control nematodes that infest plants or the situs of plants are described. Nematodes that parasitize animals can also be controlled using the methods and compounds of this invention.
Type:
Application
Filed:
September 4, 2003
Publication date:
August 12, 2004
Inventors:
Deryck J. Williams, Andrew P. Kloek, Michelle Coutu Hresko, Barry J. Shortt, Jennifer A. Davila-Aponte, John D. Bradley, James McCarter, Merry B. McLaird
Abstract: A regenerative or protective topical skin preparation includes idebenone (6-(10-hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzochinol) or a derivative of idebenone.
Abstract: A method and composition for deterring wood damage, such as caused by woodpeckers. The method includes blending Isophorone with an epoxy resin and acrylic based sealant to form a resin composition and mixing the resin composition with a solvent resistant epoxy hardener to form a coating material. The coating material is then used to coat a wood surface to seal and coat the wood for deterring woodpecker damage to the wood. The composition may include clay and flocculated silica thickeners therein. The coating composition includes Isophorone blended with an epoxy resin and micro-capsules of acrylic and is mixed with a solvent resistant epoxy hardener. The Isophorone will not blend with the epoxy compound but blends with the acrylic resin and disperses throughout the coating composition. The solvent resistant epoxy hardener is used in connection with the epoxy compound, acrylic resin and solvent Isophorone.
Abstract: The present invention provides a method of treating neurological disorders, such as epilepsy, comprising administering an effect amount of an acetone derivative having the formula R1—C(X)—R2, to an animal in need thereof. Such acetone derivatives show higher anticonvulsant activity, higher potency and improved therapeutic indexes over acetone itself.
Type:
Application
Filed:
August 7, 2003
Publication date:
May 20, 2004
Inventors:
Serguei S. Likhodi, W. Mcintyre Burnham
Abstract: Chemical compositions are provided, for use as topical anesthetics or skin refrigerants. These compositions do not cause the depletion of the stratospheric ozone layer and are non-toxic, non-carcinogenic and less flammable than ethyl chloride. Also these chemical compositions match the skin temperature versus time profile needed in the management of myofascial pain syndromes, for effectively freezing skin prior to minor skin surgery and for effectively freezing skin prior to giving painless injections.
Abstract: The present invention is directed to novel acyloins, their derivatives, methods for their production and their use for the production of novel epothilones and their derivatives. In addition, the invention is directed to the building blocks for epothilone synthesis, methods for their production and the use of synthetic building blocks for the production of epothilones and their derivatives.
Type:
Application
Filed:
April 15, 2003
Publication date:
April 29, 2004
Inventors:
Ludger A. Wessjohann, Gunther Scheid, Uwe Bornscheuer, Erik Henke, Wouter Kuit, Romano Orru
Abstract: The present invention relates to the treatment of gastrointestinal disease and/or cancer, and a method of weight gain, via the ingestion of polymeric compositions in humans, animals or birds in need of said treatment. The invention provides methods for the treatment of cancer, the treatment and/or prevention of gastrointestinal disease and/or infection and/or diarrhea and a method for increasing weight gain in humans, animals or birds comprising administering to said humans, animals or birds an effective amount of a pharmaceutical or veterinary composition or feed additive, comprising an effective amount of a polymer and/or copolymer, having the repeating polymeric unit (I) wherein R is H or alkyl, usually C1 to C4, or this unit in hydrated, hemiacetal or acetal form, together with a pharmaceutically or veterinarally acceptable carrier, diluent, adjuvant, excipient and/or controlled release system.
Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
Type:
Application
Filed:
July 21, 2003
Publication date:
April 1, 2004
Inventors:
Thomas Arrhenius, Mi Chen, Jie Fei Cheng, Yujin Huang, Alex Michael Nadzan, Sovouthy Tith, David Mark Wallace, Bin Liu, Masahiro Nishimoto
Abstract: A method of treating a neurologic or neuropsychiatric disorder or disease in a mammal is provided. The method comprises administering a fatty acid amide hydrolase inhibitor in an amount sufficient to inhibit deamidation of a fatty acid amide. A method of identifying a fatty acid amide hydrolase inhibitor useful in the treatment of a neurologic or neuropsychiatric disorder is also provided. A method of identifying a fatty acid amide or fatty acid useful in the treatment of a neurologic or neuropsychiatric disorder is also provided.
Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Type:
Grant
Filed:
October 11, 2001
Date of Patent:
March 2, 2004
Assignee:
Esperion Therapeutics, Inc.
Inventors:
Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
Abstract: Packaging and packaged products susceptible to insect attack are afforded protective character against such attack by incorporation in the packaging an insect-combating amount of 2-undecanone or 2-tridecanone.
Abstract: The present invention provides methods of preventing, treating or ameliorating one or more symptoms of disorders in which modulation of a subject's immune system is beneficial utilizing a lymphoid tissue inducing agent and an immunomodulatory agent. In particular, the present invention provides methods of preventing, treating or ameliorating a proliferative disorder, an infectious disease, a cardiovascular disease, an autoimmune disorder, or an inflammatory disorder or one or more symptoms thereof comprising administering to a subject in need thereof one or more lymphoid tissue inducing agents and one or immunomodulatory agents. The present invention also provides compositions and articles of manufacture for use in preventing, treating or ameliorating one or more symptoms associated with disorders in which modulation of a subject's immune system is beneficial, including, but not limited to proliferative disorders, infectious diseases, cardiovascular diseases, autoimmune disorders and inflammatory disorders.
Type:
Application
Filed:
December 2, 2002
Publication date:
February 5, 2004
Inventors:
Lan Bo Chen, Stine-Kathrein Kraeft, Daniel Auclair
Abstract: Insect and animal control compositions and method in which a polymer and solvent are selected to provide a cross-linked film with matrices of sufficient capacity for trapping and being plated by an active ingredient particularly methyl nonyl ketone and other ingredients such as UV light absorber and fragrance, near transparency to UV light, flexibility, and susceptibility to slow degradation by environmental factors so to release the active ingredient, and the composition sprayed onto an area to be controlled.
Abstract: Two derivatives of nootkatone, tetrahydronootkatone and 1,10-dihydronootkatone, are surprisingly effective as repellents of termites and mosquitos. Tetrahydronootkatone and 1,10-dihydronootkatone were shown to effectively repel termites at concentrations as low as 2 &mgr;g/ml and 12.5 &mgr;g/ml, respectively. Tetrahydronootkatone was shown to repel mosquitos at a concentration of 5%. Tetrahydronootkatone is an effective repellent of termites either by itself or as an addition to other substrates, including mulches made from wood products or other cellulose-containing material. Tetrahydronootkatone or 1,10-dihydronootkatone can be used to protect construction wood from attack by Formosan subterranean termites, either alone or used in combination with other compounds known to repel termites. It is also believed that these compounds will prove effective in repelling ants, ticks, and cockroaches. These derivatives of nootkatone are non-toxic to humans and other mammals and environmentally safe.
Type:
Application
Filed:
July 3, 2002
Publication date:
January 8, 2004
Inventors:
Betty C. R. Zhu, Gregg Henderson, Roger A. Laine
Abstract: The use of specific perfume ingredients, e.g. tricyclodecenyl allyl ether, to repel insects. The perfume ingredients may be used in a composition comprising from 0.1 to 40 percent by weight of one or more of the perfume ingredients. Preferably at least one of the perfume ingredients has a hydrophobicity such that the common logarithm of the octanol-water partition coefficient, log P, of the perfume ingredient is in the range 1.0 to 6.0.
Type:
Grant
Filed:
May 29, 2001
Date of Patent:
December 9, 2003
Assignee:
Quest International B.V.
Inventors:
John Martin Behan, Richard Arthur Birch
Abstract: The present invention provides methods of preventing and treating neural inflammatory or demyelinating disease, such as multiple sclerosis, via an inhibition of the activity or expression of phospholipase A2. The invention further relates to methods of identifying phospholipase A2 inhibitors and their use thereof for the prevention and/or treatment of neural inflammatory or demyelinating disease. An observed increase in the amount of phospholipase A2 in neural lesions in the EAE animal model system indicates that elevated phospholipase A2 activity or levels correlate with neural inflammatory or demyelinating disease. Therefore, in a further aspect the invention provides methods for the diagnosis and prognostication of neural inflammatory or demyelinating disease, such as multiple sclerosis.
Abstract: Prenylating enzymes are involved in modifying oncoproteins, such as RAS, so that growth of neoplastic cells becomes uncontrolled. Inactivation of such enzymes can prevent uncontrolled growth. &agr;-Dicarbonyl compounds can be used to covalently modify and thereby inactivate prenylating enzymes such as protein farnesyltransferase and protein geranylgeranyltransferase. The compounds can be designed to enhance affinity and/or specificity for a particular protein substrate.
Type:
Application
Filed:
May 14, 2003
Publication date:
November 27, 2003
Applicant:
The Arizona Disease Control Research Commission
Inventors:
Seth D. Rose, Steven R. Ottersberg, Karl J. Okolotowicz, Dale E. Robinson, Rosemarie Hartman, Scott Lefler
Abstract: The present invention provides methods and compositions for inhibiting IKK, as well as methods and compositions for identifying compounds with activity as inhibitors of IKK, and methods and compositions for the treatment of diseases and/or conditions wherein IKK is implicated and inhibition of its activity is desired. In addition, the present invention provides methods and compositions for the improving the therapeutic activity of COX2 inhibitors, comprising administering the COX2 to a subject in combination with a compound that inhibits IKK activity. The present invention further provides compositions that comprise compounds that inhibit IKK and COX2.
Type:
Grant
Filed:
November 22, 2000
Date of Patent:
November 18, 2003
Assignee:
The Regents of the University of California
Abstract: Anticancer agents containing, as an active ingredient, at least one compound selected from the group consisting of &ohgr;-hydroxy fatty acids and salts or esters thereof, hydroxy oxo-fatty acids and salts or esters thereof, lactones, macrocyclic ketones, and macrocyclic diesters having specific chemical structures.
Abstract: This invention relates to the use of acetone as an agent to selectively destruct, neutralize, and/or inhibit cells infected by viral infections, solid tumor cancers, and carcinomas. The treatment method allows the acetone to be presented to the diseased cells in a direct manner, thereby causing the least amount of disturbance to the otherwise healthy body.
Abstract: A sunless tanning formulation is provided to impart a cosmetic coloring effect to skin. The formulation is particularly useful to camouflage the effects of vitiligo. The formulation has both makeup coloring components for instant coloring effect, and dihydroxyacetone for a lasting coloring effect. The formulation is a water-in-oil emulsion with water being the inner phase and oil being the outer phase. A method of camouflaging depigmented splotches resulting from vitiligo using dihydroxyacetone is also provided.
Type:
Grant
Filed:
July 16, 2001
Date of Patent:
October 7, 2003
Inventors:
Pearl Grimes, Irwin Palefsky, Ken Klein
Abstract: A composition for prophylaxis and therapy of dermal aging which comprises a substance having human leukocyte elastase inhibitory activity as an active ingredient.
Abstract: A method and composition for treating irritable bowel syndrome in a subject in need of such treatment, utilizing an amount of a polyamine having the formula:
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
August 12, 2003
Assignee:
MCW Research Foundation
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: &bgr;-Diketone/hydroxylated or carbonated activated cation inorganic/organic complexes are well suited for preventing, avoiding or reducing skin irritation, notably that elicited by exposure to irritant active agents/species or to the external environment.
Abstract: The invention relates to an oral formulation of methylglyoxal and/or its imino acid conjugates for human use and methods for preparing the compositions. Particularly, the invention relates to compositions comprising methylglyoxal and more particularly, imino acid conjugates of methylglyoxal. The present invention also relates to formulations of methylglyoxal and imino acid conjugates of methylglyoxal that can be used for the treatment and suppression of malignant diseases including but not limited to the cancers of Colon, Prostate, Pancreas, Lung, Oral cavity, Glioblastoma, and Leukemia.
Type:
Grant
Filed:
July 1, 2002
Date of Patent:
July 22, 2003
Assignee:
Dabur Research Foundation
Inventors:
Anand C. Burman, Rama Mukherjee, Dhiraj Khattar, Mukesh Kumar
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
July 22, 2003
Assignee:
MCW Research Foundation
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: A heat shock protein inducer is provided for purposes of preventing or treating ischemic disease or ischemia/reperfusion injury. This heat shock protein inducer has geranylgeranylacetone as an active ingredient and induces heat shock proteins in the heart.
Abstract: A method of making a coating for deterring woodpeckers from damaging wood using Isophorone and the composition made therefrom. The Isophorone is combined with heated wax and combined with a thickener, such as a clay thickener and a silica thickener, and mixed with an acrylic resin. The composition is cooled and blending with ceramic pellets under a vacuum and dried. The dried pellets are then added to a polymer resin, such as an epoxy resin to form a coating material that will deter woodpeckers.
Abstract: A method of repelling an insect pest such as a tick, mosquito or cockroach comprises applying to a subject or substrate, in an amount effect to repel the insect pest, a compound of Formula I: 1
Abstract: A method has been discovered for attracting Colorado potato beetles to an area of object or area, which method involves treating the object or area with a Colorado potato beetle attracting composition which contains a carrier material and a Colorado potato beetle attracting effective amount of (S)-3,7-dimethyl-2-oxo-oct-6-ene-1,3-diol.
Abstract: A method of reducing or preventing body malodour by topically applying to human skin perfume components capable of inhibiting the producation of odoriferous steroids by microorganisms on the skin. The perfume components are capable of inhibiting bacterial 4-ene reductase and/or 5&agr;-reductase.
Abstract: The present invention is directed to methods and compositions for use to control parasitic mites of honey bees, particularly Varroa mites. In one aspect, the invention is directed to control of parasitic mites of honey bees wherein the active ingredient is a miticidally effective amount of a selected ketone or 1-heptanol, ethyl butyrate, benzaldehyde, heptaldehyde, or d-limonene. In a second aspect, the invention is directed to control of parasitic mites of honey bees wherein the active ingredient is an effective attractant amount of 2-heptanone. The attracted mites are then trapped or otherwise removed from the locus of the bees. The present invention is also directed to methods and compositions which include 2-heptanone to control hive invading pests of honey bees.
Type:
Application
Filed:
February 27, 2002
Publication date:
March 6, 2003
Inventors:
Eric H. Erickson, Gloria De-Grandi-Hoffman, Christian G. Becker, Roy S. Whitson, Thomas A. Deeby
Abstract: &bgr;-Diketone/hydroxylated or carbonated activated cation inorganic/organic complexes are well suited for reducing skin irritation, notably that elicited by exposure to irritant active agents/species or to the external environment.
Abstract: The present invention relates generally to the fields of oligonucleotide synthesis. More particularly, it concerns the assembly of genes and genomes of completely synthetic artificial organisms. Thus, the present invention outlines a novel approach to utilizing the results of genomic sequence information by computer directed gene synthesis based on computing on the human genome database. Specifically, the present invention contemplates and describes the chemical synthesis and resynthesis of genes defined by the genome sequence in a host vector and transfer and expression of these sequences into suitable hosts.
Abstract: The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.
Type:
Application
Filed:
October 2, 2001
Publication date:
February 6, 2003
Inventors:
Susheng Wang, Dennis C. Liotta, James P. Snyder, Hariharan Venkatesan