Alicyclic Ring Patents (Class 514/683)
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Publication number: 20080125481Abstract: There are disclosed compounds of formulae (I) or (II) in which A is selected from the group consisting of (1), (2), (3) and (4); OH, and one of R1 and R2 is selected from H, OH and OCH3, and the other of R1 and R2 is selected from OH and OCH3; one of R3 and R4 is selected from H, OH and OCH3, and the other of R3 and R4 is selected from OH and OCH3; provided that at least one of the pairs R1, R2 and R3, R4 are both OH; R5 is selected from OH and OCH3; and denotes a single or double bond; and pharmaceutically acceptable salts and prodrugs thereof. The compounds of the invention are useful for the treatment of hormone-dependent conditions and cancers.Type: ApplicationFiled: January 31, 2008Publication date: May 29, 2008Inventor: George Eustace Joannou
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Patent number: 7345096Abstract: The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.Type: GrantFiled: October 14, 2003Date of Patent: March 18, 2008Assignee: WyethInventors: Darlene Coleman Deecher, Istvan Jozsef Merchenthaler, Liza Leventhal, Kimberly Jean Sipe, Lawrence Thomas O'Connor
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Patent number: 7338960Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:Type: GrantFiled: June 18, 2003Date of Patent: March 4, 2008Assignee: SmithKline Beecham CorporationInventors: Richard Bell, Paul John Beswick, Romain Luc Marie Gosmini, Richard Martin Grimes, Christopher Charles Frederick Hamlett, Nigel Paul King, Vipulkumar Kantibhai Patel
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Patent number: 7129271Abstract: Compounds, compositions, and methods that employ an eremophilane sesguiterpene are presented for controlling an arthropod pest population. The compounds have minimal adverse or toxic effects on humans, non-human animals, and the natural environment. The compounds may be isolated from natural sources, semi-synthesized from naturally occurring compounds, or completely synthesized. The compounds may be applied directly to a pest or the locus of a pest, and function as topical or ingestible toxins. Eremophilane sesguiterpenes 13-hydroxy-valencene, valencene-11,12-epoxide, valencene-13-aldehyde, and nootkatone-1,10-11,12-diepoxide are exemplary compounds.Type: GrantFiled: December 7, 2001Date of Patent: October 31, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Gary O. Maupin, Joseph Karchesy, Nicholas A. Panella, Marc C. Dolan
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Patent number: 7056950Abstract: A composition of biochemical compounds involved in bioenergy metabolism of cells and a method of use in prevention and therapy of diseases are disclosed.Type: GrantFiled: February 14, 2002Date of Patent: June 6, 2006Inventor: Matthias Rath
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Patent number: 6949585Abstract: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -DE- represents a group represented by —CH2CH2— or —CH?CH—; W represents a group represented by —CH2—, —CH2CH2—, —CH?CH— or —CH?; the partial structure >XY— represents a group represented by >CH—(CH2)n—, >C?CH—, >CH—CH2—CH(OH)—, >CH—CH2—C(?O)—, >CH—O— or >CH—O—CO—, provided that when W is —CH?, then XY— represents C—(CH2)p—; Z represents a divalent aliphatic hydrocarbon group; R1 and R2, which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1].Type: GrantFiled: April 1, 2002Date of Patent: September 27, 2005Assignee: Eisai Co., Ltd.Inventors: Yoshihito Eguchi, Ken-ichi Chiba, Masaki Goto, Hiroshi Obaishi, Yoshikazu Kuboi
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Patent number: 6887904Abstract: Substituted arylcycloalkanes, compositions containing them and use thereof. The present invention relates especially to substituted arylcycloalkanes with therapeutic activity, which may be used such as in oncology.Type: GrantFiled: December 4, 2002Date of Patent: May 3, 2005Assignee: Aventis Pharma S. A.Inventors: Patrick Mailliet, Marc Capet, Gilles Tiraboschi, Thomas Caulfield
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Patent number: 6777564Abstract: A novel compound with anthraquinone structure and having the following foluma (I): wherein R1, R2 and R3 each independently is hydrogen, hydroxy, amino or C1-6 alkyl group; R4 is hydrogen, C1-18 alkyl carbonyl, C1-6 alkyl group substituted by at least a functional group; R5 is hydrogen amino or a group of the following formula wherein R1, R2, R3 and R4 are defined as the above; and R and R′ each independently is hydrogen, hydroxyl, amino, C1-6 alkyl group or a group of the following formula wherein R1, R2, R3 and R4 are defined as the above.Type: GrantFiled: December 20, 2001Date of Patent: August 17, 2004Assignee: Industrial Technology Research InstituteInventors: Lain-Tze Lee, Jinun-Ban Yeh
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Patent number: 6706713Abstract: This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation for treating and/or diagnosing inflammatory, infectious and/or skin diseases.Type: GrantFiled: October 14, 1997Date of Patent: March 16, 2004Assignees: Deutsches Krebsforschungszentrum Stiftung des Offentlichen RechtsInventors: Hansjörg Sinn, Hans-Hermann Schrenk, Wolfgang Maier-Borst, Gerd Stehle
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Publication number: 20040048918Abstract: The disclosure concerns novel use of diterpene compound as a therapeutic agent of inlfammation, immune disease or cancer. More particularly, the present invention relates to novel use of diterpene compound that include kamebanin, kamebacetal A, kamebakaurin, and exisanin A, which would be effective for the treatnent inflammation, immune disease or cancer by inhibiting the production of nitric oxide, prostaglandin, and TNF-a, through the suppression of NF-k B activity.Type: ApplicationFiled: June 11, 2003Publication date: March 11, 2004Inventors: Jung-Joon Lee, Jeong-Hyung Lee, Hang-Sub Kim, Young-Soo Hong, Bang-Yeon Hwang
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Patent number: 6696484Abstract: Pharmaceutical compositions and methods for treating androgen related disorders. The pharmaceutical compositions may include a 5&agr;-reductase inhibitor, such as natural and synthetic flavanoids, catechols, curcumin-related substances, quinones, catechins, particularly epigallocatechin derivatives, fatty acids, and the salts, esters, analogues, pro-drugs, isomers, racemic mixtures, or derivatives of any of the foregoing. The use of testosterone (or DHT) combinations with the aforementioned 5&agr;-reductase inhibitor compounds is also contemplated.Type: GrantFiled: April 24, 2002Date of Patent: February 24, 2004Assignee: University of Chicago Office of Technology and Intellectual PropertyInventors: Shutsung Liao, Richard Hiipakka
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Publication number: 20040029918Abstract: A method for treating a microbial infection or disease in a subject, said method comprising administering to said subject an effective amount of a compound according to the formula (1). Wherein; denotes a single or double bond or an epoxidised bond, and A1 to A13 are independently selected from moieties as depicted in the description. Also claimed are methods for disinfecting surfaces using the above compound, and claims to the above compound.Type: ApplicationFiled: May 22, 2003Publication date: February 12, 2004Inventors: Rodney Warren Rickards, Chunjiu Zhao, Stephen Charles Trowell
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Publication number: 20040022778Abstract: The present invention relates to a combination of a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone and their use in treating and/or preventing disorders characterized by endothelial dysfunction, such as cardiovascular disease, strokes and myocardial infarction. According to a preferred embodiment of the invention the benzoquinone or precursor thereof is a ubiquinone or precursor thereof, more preferably, coenzyme Q10 or a precursor thereof, and the PPAR activator is a librate or a thiazolidinedionc, more preferably fenolibrate.Type: ApplicationFiled: April 17, 2003Publication date: February 5, 2004Inventors: Gerald Franus Watts, David Alan Playford
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Publication number: 20040005306Abstract: The present invention provides methods of treating or preventing vascular diseases caused by nitric oxide (NO) insufficiency. The methods encompass administering a composition comprising an antioxidant, a compound to treat cardiovascular diseases, a nitrosated compound, a compound that donates, transfers or relases NO, or is a NO synthase substrate, or endogenously stimulates NO synthesis, or stimulates levels of endothelium derived relaxing factor. In the said composition, a hydralazine compound may be an antioxidant, isosorbide mono-or dinitrate may be the compound to donate, transfer, release, or stimulate endogenous NO synthesis. The isorsorbide may also elevate endogenous levels of endotherlium-derived relaxing factor, or be a NO synthase substrate and angiotensin enzyme inhibitor may be nitrosated compound.Type: ApplicationFiled: April 25, 2003Publication date: January 8, 2004Inventors: Joseph Loscalzo, Joseph A Vita, Michael D Loberg, Manuel Morce
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Publication number: 20030206972Abstract: A novel formulation is provided that serves to synergistically inhibit the generation of free radicals and oxidative stress in warm blooded animals. The formulation comprises an effective amount of a first component of a carotenoid species, and, as a second component, a tocotrienol species and derivatives thereof, and provides for synergistic anti-oxidant activity.Type: ApplicationFiled: October 11, 2001Publication date: November 6, 2003Inventors: John G. Babish, Terrence Howell
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Patent number: 6605639Abstract: It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologues serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologues are usable in treating and/or preventing a disease or condition which can be relieved by the retinoid X receptor ligand-dependent gene transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune disease, Ca metabolic disorder, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet &bgr;-cells and, therefore, are usable in making these cells to sustain the insulin productivity.Type: GrantFiled: June 14, 2001Date of Patent: August 12, 2003Assignee: Nuclear Receptor Research, Ltd.Inventors: Gakuzo Tamura, Kunio Ando, Junji Magae, Takafumi Uchida
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Publication number: 20030147927Abstract: A eutectic-based self-nanoemulsified drug delivery system (SNEDDS) is formulated from polyoxyl 35 castor oil (Cremophor), medium chain mono- and diglycerides (capmul), essential oils, and a pharmacologically effective drug. The preferred pharmacologically effective drug is a poorly water soluble drug, such as ubiquinone (CoQ10). The SNEDDS can be further incorporated into a powder to produce a solid dosage form. The solid dosage form contains the SNEDDS, a copolymer of vinylpyrrolidone and vinyl acetate (Kollidon VA 64), maltodextrin, and microcrystalline cellulose (MCC).Type: ApplicationFiled: November 14, 2002Publication date: August 7, 2003Inventors: Mansoor A. Khan, Sami Nazzal
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Patent number: 6576660Abstract: Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.Type: GrantFiled: April 28, 2000Date of Patent: June 10, 2003Assignee: Arch Development CorporationInventors: Shutsung Liao, Richard A. Hiipakka
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Publication number: 20030092772Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.Type: ApplicationFiled: February 27, 2002Publication date: May 15, 2003Inventors: Mochammad Samhoedi Reksohadiprodjo, Henk Timmerman, Sardjiman, Supardjan Amir Margono, Sudibyo Martono, Sugiyanto, Lukman Hakim, Nurlaila, Arief Rahman Hakim, Ika Puspitasari, Arief Nurrochmad, Purwantiningsih, Oetari, Tedjo Yuwono
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Publication number: 20030073738Abstract: A combination of Vitamin C and a quinone used as a supplemental treatment for a cancer patient. The combination may be administered before, during and after the patient undergoes a conventional cancer treatment protocol. The combination may be administered orally, intravenously, or intraperitoneally. Oral administration may be in the form of capsules containing a predetermined ratio of Vitamin C to Vitamin K3. The supplemental treatment is effective to inhibit metastases of cancer cells and inhibit tumor growth. The ratio of Vitamin C to Vitamin K3 is in the range of about 50 to 1 to about 250 to 1. A method for evaluating the effectiveness of the supplemental treatment includes monitoring the patient's serum DNase activity throughout the course of treatment.Type: ApplicationFiled: June 3, 2002Publication date: April 17, 2003Inventors: Jacques Gilloteaux, Henryk S. Taper, James M. Jamison, Jack L. Summers
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Publication number: 20030039619Abstract: Cosmetic or dermatological formulations which comprise one or more active ingredients selected from phylloquinone, 2-hydroxy-5-methyllaurophenone oxime, vitamin A and its derivatives, vitamin E and its derivatives, vitamin H, allantoin, bisabolol, nicotinic acid derivatives and caffeine and in additionType: ApplicationFiled: July 26, 2002Publication date: February 27, 2003Inventors: Joachim Bunger, Jutta zur Lage, Alexandra Axt
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Publication number: 20030036565Abstract: Extracts prepared from red and high-pigment beetroots (Beta vulgaris L.) with a solvent, such as a water-containing solvent, possess antioxidant activity as demonstrated by a panel of assays. These extracts also have an ability to induce quinone reductase in Murine hepatoma cell (Hepa 1c1c7) cultured in vitro. Fractions purified from the active extracts also possess antioxidant activity and retain quinone reductase-inducing activity in the Hepa 1c1c7 cell line. The active extracts, purified by column, thin layer, and high-performance liquid chromatographic techniques, include betalains. A method of extracting a betalain includes steps of freeze-drying a source containing the betalain; grinding the freeze-dried source; and extracting the betalain from the ground source with the solvent. Additionally, the betalain extract can be isolated betalain components, such as by chromatography.Type: ApplicationFiled: June 24, 2002Publication date: February 20, 2003Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Kirk L. Parkin, Mahinda Wettasinghe
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Publication number: 20030013667Abstract: The present invention relates to a therapeutic agent for ischemia which inhibits apoptosis under ischemic condition. The therapeutic agent of present invention comprises antibacterial agents of quinolones, quinones, aminoglycosides or chlorampheni-col as an active ingredient. Since the invented therapeutic agent improved the viability of cells under hypoxic and hypoglycemic condition, it can be clinically for ischemic diseases such as applied as a potentiad drug for ischemia-associated infarction and cerebral infarction.Type: ApplicationFiled: July 12, 2002Publication date: January 16, 2003Inventors: Jongwon Lee, Kyu-Won Kim, Jong-Kyun Lee, Sang Jong Lee
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Publication number: 20020173546Abstract: A composition of biochemical compounds involved in bioenergy metabolism of cells and a method of use in prevention and therapy of diseases are disclosed.Type: ApplicationFiled: February 14, 2002Publication date: November 21, 2002Inventor: Matthias Rath
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Publication number: 20020165206Abstract: The invention is concerned in the compounds, the derivatives or those acid addition salt compounds which has the original molecular structure shown in general formula (1-a) with the following effective ingredients; antibacterial agents, antifungal agents, antiviral agents, bactericidal and/or sterilized agents, anticancer agents, blood coagulation and fibrinolysis inhibitors and/or blocking agents, inhibitory and/or blocking agents of antigen-antibody reaction, organ and/or tissue preservatives, antiseptics and preservatives for foodstuffs, spermatocidal agents and/or contraceptive agents of external use, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (proteins, lipids, sugar) improving agents, promoting agents for wound healing, epithelialization promoting agents, inhibitors and/or blocking agents which can control generation of function with bioactive substances (for example, enzymes, peptides, gene), depolymerization agents, improvType: ApplicationFiled: December 28, 2001Publication date: November 7, 2002Inventors: Shozo Koyama, Yoshihiro Yamaguchi
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Publication number: 20020156302Abstract: Processes for the stereospecific synthesis of coenzyme Q10, ubiquinone, are disclosed; a semi synthetic procedure using solanesol derived from tobacco waste as the starting material. The process of the invention results in high yields of isometrically useful compositions containing the optically pure isomers.Type: ApplicationFiled: April 19, 2001Publication date: October 24, 2002Inventor: Daniel David West
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Publication number: 20020077360Abstract: Retinoid compounds which act specifically or selectively on RAR&agr; receptor subtypes in preference over RAR&bgr; and RAR&Ggr; receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.Type: ApplicationFiled: November 29, 2001Publication date: June 20, 2002Applicant: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20020065254Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions and hydroxymethylacylfulvene analogs useful as antitumor drugs.Type: ApplicationFiled: September 18, 2001Publication date: May 30, 2002Inventor: Alvin Guttag
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Publication number: 20020052419Abstract: The present invention provides an ophthalmic composition for soft contact lenses (SCL), which contains a terpenoid as an active ingredient, an ophthalmic composition for SCL, which contains polyoxyethylene sorbitan ester, a method of enhancing the wettability of soft contact lenses, which comprises bringing terpenoid into contact with SCL and a method of inhibiting adsorption of terpenoid onto SCL, which comprises adding polyoxyethylene sorbitan ester to an ophthalmic composition containing a terpenoid. The ophthalmic composition containing a terpenoid improves, for example, the wettability of SCL, thereby to inhibit decrease in the water content of SCL. As a result, it can inhibit a dry feeling and an uncomfortable feeling during wearing SCL and is useful for enhancing the wettability of SCL. Further, addition of polyoxyethylene sorbitan ester leads to the inhibition of adsorption of terpenoid onto SCL.Type: ApplicationFiled: August 20, 2001Publication date: May 2, 2002Inventors: Koji Doi, Hisayuki Nakayama, Takuya Nakajima, Noriko Sakai
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Publication number: 20020052359Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: May 2, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020009467Abstract: This invention provides antigen substance inductors which produce highly selective and/or specific vaccine precursor, vaccine, antibody (including idiotype antibody), neutralizing antibody, antitoxin.Type: ApplicationFiled: June 18, 2001Publication date: January 24, 2002Inventors: Shozo Koyama, Satoshi Tanaka
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Publication number: 20010027216Abstract: The present invention provides a method for preventing the adverse effects which may be associated with the administration of at least one hormone to a subject without detectable cancer comprising administering to such subject at least one carotenoid. The invention further provides a method for preventing a variety of adverse effects associated with the administration of hormones, including, for example, an increased risk for developing cancer. The invention further provides a method for preventing adverse effects without inhibiting the beneficial activity of the hormone. The invention further provides a method for preventing the adverse effects associated with administration of estrogen and/or progestin in hormone replacement therapy without inhibiting the beneficial activity of such hormone. The invention further provides a method for preventing the adverse effects associated with the administration of phytoestrogens.Type: ApplicationFiled: March 5, 2001Publication date: October 4, 2001Inventors: Joseph Levy, Yoav Sharoni
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Publication number: 20010018459Abstract: The present invention relates to fuingicidally effective compositions containing at least one pentacyclic triterpene compound.Type: ApplicationFiled: April 2, 2001Publication date: August 30, 2001Inventors: Jan Glinski, Keith Branly
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Patent number: 6281250Abstract: The present invention is directed to retinyl ethers, derivatives and analogues and their use in inhibiting breast carcinogenesis or breast cancer cell growth.Type: GrantFiled: April 12, 1999Date of Patent: August 28, 2001Assignee: Southern Research InstituteInventor: Y. Fulmer Shealy
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Patent number: 6251833Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: August 31, 1999Date of Patent: June 26, 2001Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
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Patent number: 6172118Abstract: This invention relates to ketones, alcohols and amines represented by the likes of of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylethynylcyclobutan-1-one. They are useful as PDE 4 antagonists.Type: GrantFiled: April 8, 1999Date of Patent: January 9, 2001Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6159988Abstract: Compounds of formula I, ##STR1## and the physiologically tolerable salts thereof, wherein the substituents R.sub.1 -R.sub.4 have the meanings given in the specifications and show an activity against inflammatory conditions.Type: GrantFiled: June 29, 1998Date of Patent: December 12, 2000Assignee: Hoeschst AktiengesellschaftInventors: Ramachandra Ganapati Naik, Vilas Narayan Mumbaikar, Ravishankar Vasumathy, Aftab Dawoodbhai Lakdawala, Mandakini Bipin Alreja, Bansi Lal, Jurgen Blumbach, Klaus Ulrich Weithmann, Robert Ryder Bartlett, Kalpana Sanjay Joshi, Swati Bal-Tembe, Sadagopan Raghavan
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Patent number: 6150374Abstract: The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation.Type: GrantFiled: September 29, 1997Date of Patent: November 21, 2000Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6118017Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.Type: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6086857Abstract: The invention relates to cinnamylidenecamphor derivatives of the formula (1) ##STR1## where the diene system is in the Z,Z, Z,E, E,Z or E,E configuration and R.sup.1 is H, CH.sub.3,R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, NR.sup.3 H, NR.sup.3.sub.2,R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.4 is H, C.sub.1 -C.sub.6 -alkyl,n is 1, 2,and to its use.Type: GrantFiled: September 3, 1998Date of Patent: July 11, 2000Assignee: BASF AktiengesellschaftInventors: Christof Kandzia, Horst Westenfelder, Volker Schehlmann
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Patent number: 6051588Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: April 19, 1995Date of Patent: April 18, 2000Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 5880162Abstract: A pesticidal compound of formula I: ##STR1## in which formula: either R.sup.1 is hydrogen and R.sup.2 represents a cyclopropyl group or R.sup.1 and R.sup.2 each represent an alkyl group, which alkyl groups may be the same or different;Ar.sub.A represents an optionally substituted phenyl or naphthyl group;Ar.sub.B represents a phenoxy, phenyl, benzyl or benzoyl-substituted phenyl group which is optionally further substituted;the configuration of the groups Ar.sub.A --CR.sup.1 R.sup.2 and --CH.sub.2 Ar.sub.B about the double bond being mutually trans.Preferably Ar.sub.A is a substituted phenyl group; more preferably being substituted at the 4-(para) position by halogen, alkoxy or haloalkyl.Further provided is a process for the preparation of a pesticidal compound of formula I in which a compound comprising a moiety ##STR2## and a compound comprising a moiety Ar.sub.B -- are reacted together forming a link --CH.dbd.C(F)CH.sub.2 -- between ##STR3## and Ar.sub.B in the compound of formula I.Type: GrantFiled: October 21, 1996Date of Patent: March 9, 1999Assignee: British Technology Group, Ltd.Inventors: Bhupinder Pall Singh Khambay, Mu-Guang Liu
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Patent number: 5849801Abstract: 4-amino-5-oxy-2,6,6-tri methyl-2-cycloheptene compounds represented by the following general formula: ##STR1## (wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom, an alkyl group which may have a substituent, or a phenyl group which may have a hydroxyl group, lower alkoxy group, amino group, nitro group, carboxyl group, lower alkoxycarbonyl group or halogen atom, or R.sup.1, R.sup.2 and the nitrogen atom together represent a saturated nitrogen heterocyclic group; R.sup.3 represents a hydrogen atom, a lower alkyl group or a lower aliphatic acyl group); and W represents an oxo group, oxime group or oxime ether group; and their pharmacologically acceptable salts and solvates.The 4-amino-5-oxy-2,6,6-trimethyl-2-cycloheptene compounds exhibit an effect against rat peripheral arterial occlusion models, spontaneous hypertensive rats and histamine-induced airway contraction models, and are thus useful as remedy for hypertension, peripheral arterial occlusion and bronchial asthma.Type: GrantFiled: July 30, 1997Date of Patent: December 15, 1998Assignee: Tokyo Tanabe Company LimitedInventors: Susumu Yokura, Masao Yajima, Kiyokazu Murakami, Kouichi Matsunaga
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Patent number: 5840282Abstract: Photostable, cosmetic light-screening compositions for the protection of the human epidermis and the hairs against the ultraviolet rays of wavelengths between 320 and 400 nm, and between 320 and 400 nm respectively, comprising, in a cosmetically acceptable vehicle containing at least one fatty phase, about 0.75 to about 5%, in particular about 1 to about 4% by weight, of a dibenzoylmethane type UV-A screening agent and at least about 0.5% to about 2%, in particular about 0.5 to about 1% by weight, of a benzylidene type stabilizer of the general formula ##STR1## represents a bridged cyclic compound having the camphor (1,7,7-trimethyl-bicyclo?2.2.1!heptan-2-one), norcamphor (bicyclo?2.2.1!heptan-2-one), nopinone (6,6-dimethyl-bicyclo?3.1.1!heptan-2-one), pinocamphone (4,6,6-trimethyl-bicyclo?3.1.1!heptan-3-one), verbanone (4,6,6-trimethyl-bicyclo?3.1.1!heptan-2-one, thujone (1-isopropyl-4-methyl-bicyclo?3.1.0!hexan-3-one) or the 4,7-methano-octahydro-inden-5-one structure, and wherein R.sup.1, R.sup.2, R.sup.Type: GrantFiled: June 13, 1996Date of Patent: November 24, 1998Assignee: Givaudan-Roure (International) SAInventors: Hans Ulrich Gonzenbach, Peter Gygax, Bernhard Hostettler, Ulrich Huber
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Patent number: 5840661Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.Type: GrantFiled: December 31, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
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Patent number: 5807898Abstract: The invention describes a method of killing or inhibiting the growth of the malaria causing pathogen Plasmodium falciparum by exposing the pathogen to a preparation containing methylene-bis-aspidinol, desaspidin, and/or aspidin.Type: GrantFiled: August 20, 1997Date of Patent: September 15, 1998Inventor: Govind J. Kapadia
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Patent number: 5760092Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.Type: GrantFiled: March 11, 1996Date of Patent: June 2, 1998Assignee: Brandeis UniversityInventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
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Patent number: 5716995Abstract: An anti-osteopathic composition comprising as an active ingredient a compound represented by the following formula (I), (II) or (III): ##STR1## which is useful for therapeutic and prophylactic treatment of osteopathia such as osteoporosis and bone fracture.Type: GrantFiled: June 7, 1995Date of Patent: February 10, 1998Assignees: Hoechst Japan Limited, Koichi ShudoInventors: Koichi Shudo, Tatsuo Sugioka, Mizuho Inazu, Hideyuki Tanaka, Tsutomu Inoue, Kazuyuki Kitamura
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Patent number: 5677336Abstract: Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.Type: GrantFiled: October 21, 1993Date of Patent: October 14, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lawrence G. Hamann, Luc Farmer, Michael G. Johnson, Mark E. Goldman
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Patent number: 5618547Abstract: A series of 1,3-propanediones having a perfluoroalkyl group or a perfluorocycloalkyl group on one carbonyl, and a 3,5-disubstituted phenyl group on the other, are useful when administered to animals for the control of ectoparasites.Type: GrantFiled: March 10, 1994Date of Patent: April 8, 1997Assignee: British Technology Group LimitedInventors: Rudolph J. Boisvenue, Gary D. Crouse