Alicyclic Ring Patents (Class 514/683)
  • Publication number: 20080125481
    Abstract: 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: Application
    Filed: January 31, 2008
    Publication date: May 29, 2008
    Inventor: George Eustace Joannou
  • Patent number: 7345096
    Abstract: 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: Grant
    Filed: October 14, 2003
    Date of Patent: March 18, 2008
    Assignee: Wyeth
    Inventors: Darlene Coleman Deecher, Istvan Jozsef Merchenthaler, Liza Leventhal, Kimberly Jean Sipe, Lawrence Thomas O'Connor
  • Patent number: 7338960
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: March 4, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard Bell, Paul John Beswick, Romain Luc Marie Gosmini, Richard Martin Grimes, Christopher Charles Frederick Hamlett, Nigel Paul King, Vipulkumar Kantibhai Patel
  • Patent number: 7129271
    Abstract: 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: Grant
    Filed: December 7, 2001
    Date of Patent: October 31, 2006
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Gary O. Maupin, Joseph Karchesy, Nicholas A. Panella, Marc C. Dolan
  • Patent number: 7056950
    Abstract: 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: Grant
    Filed: February 14, 2002
    Date of Patent: June 6, 2006
    Inventor: Matthias Rath
  • Patent number: 6949585
    Abstract: 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: Grant
    Filed: April 1, 2002
    Date of Patent: September 27, 2005
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshihito Eguchi, Ken-ichi Chiba, Masaki Goto, Hiroshi Obaishi, Yoshikazu Kuboi
  • Patent number: 6887904
    Abstract: 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: Grant
    Filed: December 4, 2002
    Date of Patent: May 3, 2005
    Assignee: Aventis Pharma S. A.
    Inventors: Patrick Mailliet, Marc Capet, Gilles Tiraboschi, Thomas Caulfield
  • Patent number: 6777564
    Abstract: 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: Grant
    Filed: December 20, 2001
    Date of Patent: August 17, 2004
    Assignee: Industrial Technology Research Institute
    Inventors: Lain-Tze Lee, Jinun-Ban Yeh
  • Patent number: 6706713
    Abstract: 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: Grant
    Filed: October 14, 1997
    Date of Patent: March 16, 2004
    Assignees: Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
    Inventors: Hansjörg Sinn, Hans-Hermann Schrenk, Wolfgang Maier-Borst, Gerd Stehle
  • Publication number: 20040048918
    Abstract: 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: Application
    Filed: June 11, 2003
    Publication date: March 11, 2004
    Inventors: Jung-Joon Lee, Jeong-Hyung Lee, Hang-Sub Kim, Young-Soo Hong, Bang-Yeon Hwang
  • Patent number: 6696484
    Abstract: 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: Grant
    Filed: April 24, 2002
    Date of Patent: February 24, 2004
    Assignee: University of Chicago Office of Technology and Intellectual Property
    Inventors: Shutsung Liao, Richard Hiipakka
  • Publication number: 20040029918
    Abstract: 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: Application
    Filed: May 22, 2003
    Publication date: February 12, 2004
    Inventors: Rodney Warren Rickards, Chunjiu Zhao, Stephen Charles Trowell
  • Publication number: 20040022778
    Abstract: 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: Application
    Filed: April 17, 2003
    Publication date: February 5, 2004
    Inventors: Gerald Franus Watts, David Alan Playford
  • Publication number: 20040005306
    Abstract: 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: Application
    Filed: April 25, 2003
    Publication date: January 8, 2004
    Inventors: Joseph Loscalzo, Joseph A Vita, Michael D Loberg, Manuel Morce
  • Publication number: 20030206972
    Abstract: 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: Application
    Filed: October 11, 2001
    Publication date: November 6, 2003
    Inventors: John G. Babish, Terrence Howell
  • Patent number: 6605639
    Abstract: 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: Grant
    Filed: June 14, 2001
    Date of Patent: August 12, 2003
    Assignee: Nuclear Receptor Research, Ltd.
    Inventors: Gakuzo Tamura, Kunio Ando, Junji Magae, Takafumi Uchida
  • Publication number: 20030147927
    Abstract: 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: Application
    Filed: November 14, 2002
    Publication date: August 7, 2003
    Inventors: Mansoor A. Khan, Sami Nazzal
  • Patent number: 6576660
    Abstract: Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: June 10, 2003
    Assignee: Arch Development Corporation
    Inventors: Shutsung Liao, Richard A. Hiipakka
  • Publication number: 20030092772
    Abstract: 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: Application
    Filed: February 27, 2002
    Publication date: May 15, 2003
    Inventors: 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
  • Publication number: 20030073738
    Abstract: 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: Application
    Filed: June 3, 2002
    Publication date: April 17, 2003
    Inventors: Jacques Gilloteaux, Henryk S. Taper, James M. Jamison, Jack L. Summers
  • Publication number: 20030039619
    Abstract: 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 addition
    Type: Application
    Filed: July 26, 2002
    Publication date: February 27, 2003
    Inventors: Joachim Bunger, Jutta zur Lage, Alexandra Axt
  • Publication number: 20030036565
    Abstract: 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: Application
    Filed: June 24, 2002
    Publication date: February 20, 2003
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Kirk L. Parkin, Mahinda Wettasinghe
  • Publication number: 20030013667
    Abstract: 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: Application
    Filed: July 12, 2002
    Publication date: January 16, 2003
    Inventors: Jongwon Lee, Kyu-Won Kim, Jong-Kyun Lee, Sang Jong Lee
  • Publication number: 20020173546
    Abstract: 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: Application
    Filed: February 14, 2002
    Publication date: November 21, 2002
    Inventor: Matthias Rath
  • Publication number: 20020165206
    Abstract: 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, improv
    Type: Application
    Filed: December 28, 2001
    Publication date: November 7, 2002
    Inventors: Shozo Koyama, Yoshihiro Yamaguchi
  • Publication number: 20020156302
    Abstract: 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: Application
    Filed: April 19, 2001
    Publication date: October 24, 2002
    Inventor: Daniel David West
  • Publication number: 20020077360
    Abstract: 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: Application
    Filed: November 29, 2001
    Publication date: June 20, 2002
    Applicant: Allergan Sales, Inc.
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Publication number: 20020065254
    Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions and hydroxymethylacylfulvene analogs useful as antitumor drugs.
    Type: Application
    Filed: September 18, 2001
    Publication date: May 30, 2002
    Inventor: Alvin Guttag
  • Publication number: 20020052419
    Abstract: 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: Application
    Filed: August 20, 2001
    Publication date: May 2, 2002
    Inventors: Koji Doi, Hisayuki Nakayama, Takuya Nakajima, Noriko Sakai
  • Publication number: 20020052359
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: May 2, 2002
    Inventors: 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
  • Publication number: 20020009467
    Abstract: This invention provides antigen substance inductors which produce highly selective and/or specific vaccine precursor, vaccine, antibody (including idiotype antibody), neutralizing antibody, antitoxin.
    Type: Application
    Filed: June 18, 2001
    Publication date: January 24, 2002
    Inventors: Shozo Koyama, Satoshi Tanaka
  • Publication number: 20010027216
    Abstract: 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: Application
    Filed: March 5, 2001
    Publication date: October 4, 2001
    Inventors: Joseph Levy, Yoav Sharoni
  • Publication number: 20010018459
    Abstract: The present invention relates to fuingicidally effective compositions containing at least one pentacyclic triterpene compound.
    Type: Application
    Filed: April 2, 2001
    Publication date: August 30, 2001
    Inventors: Jan Glinski, Keith Branly
  • Patent number: 6281250
    Abstract: The present invention is directed to retinyl ethers, derivatives and analogues and their use in inhibiting breast carcinogenesis or breast cancer cell growth.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: August 28, 2001
    Assignee: Southern Research Institute
    Inventor: Y. Fulmer Shealy
  • Patent number: 6251833
    Abstract: 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: Grant
    Filed: August 31, 1999
    Date of Patent: June 26, 2001
    Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
  • Patent number: 6172118
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6159988
    Abstract: 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: Grant
    Filed: June 29, 1998
    Date of Patent: December 12, 2000
    Assignee: Hoeschst Aktiengesellschaft
    Inventors: 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
  • Patent number: 6150374
    Abstract: 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: Grant
    Filed: September 29, 1997
    Date of Patent: November 21, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 6118017
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: September 12, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6086857
    Abstract: 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: Grant
    Filed: September 3, 1998
    Date of Patent: July 11, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Christof Kandzia, Horst Westenfelder, Volker Schehlmann
  • Patent number: 6051588
    Abstract: 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: Grant
    Filed: April 19, 1995
    Date of Patent: April 18, 2000
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 5880162
    Abstract: 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: Grant
    Filed: October 21, 1996
    Date of Patent: March 9, 1999
    Assignee: British Technology Group, Ltd.
    Inventors: Bhupinder Pall Singh Khambay, Mu-Guang Liu
  • Patent number: 5849801
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 15, 1998
    Assignee: Tokyo Tanabe Company Limited
    Inventors: Susumu Yokura, Masao Yajima, Kiyokazu Murakami, Kouichi Matsunaga
  • Patent number: 5840282
    Abstract: 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: Grant
    Filed: June 13, 1996
    Date of Patent: November 24, 1998
    Assignee: Givaudan-Roure (International) SA
    Inventors: Hans Ulrich Gonzenbach, Peter Gygax, Bernhard Hostettler, Ulrich Huber
  • Patent number: 5840661
    Abstract: 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: Grant
    Filed: December 31, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5807898
    Abstract: 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: Grant
    Filed: August 20, 1997
    Date of Patent: September 15, 1998
    Inventor: Govind J. Kapadia
  • Patent number: 5760092
    Abstract: 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: Grant
    Filed: March 11, 1996
    Date of Patent: June 2, 1998
    Assignee: Brandeis University
    Inventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
  • Patent number: 5716995
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: February 10, 1998
    Assignees: Hoechst Japan Limited, Koichi Shudo
    Inventors: Koichi Shudo, Tatsuo Sugioka, Mizuho Inazu, Hideyuki Tanaka, Tsutomu Inoue, Kazuyuki Kitamura
  • Patent number: 5677336
    Abstract: 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: Grant
    Filed: October 21, 1993
    Date of Patent: October 14, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lawrence G. Hamann, Luc Farmer, Michael G. Johnson, Mark E. Goldman
  • Patent number: 5618547
    Abstract: 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: Grant
    Filed: March 10, 1994
    Date of Patent: April 8, 1997
    Assignee: British Technology Group Limited
    Inventors: Rudolph J. Boisvenue, Gary D. Crouse