Carbon Bonded Directly At The 17 Beta-position Of The Cyclopentanohydrophenanthrene Ring System Is A Member Of An Acyclic Chain Of Six Or More Uninterrupted Carbons (e.g., Sterols, Etc.) Patents (Class 552/540)
  • Publication number: 20040034241
    Abstract: Compositions, novel isolation sources and processes, and uses for unique policosanol containing compositions are disclosed. Seed and vegetable processing byproduct and/or “waste” streams are disclosed as containing policosanols with various relative amounts of the various long chain fatty/waxy alcohols. The policosanols are isolated and may be combined with other phytochemical/processing products, and are used in numerous food, beverage, health and/or nutraceutical applications.
    Type: Application
    Filed: May 29, 2003
    Publication date: February 19, 2004
    Applicant: Archer-Daniels-Midland Company
    Inventors: Mark W. Empie, Ahmad Hilaly, Dennis Branin Lane, Alexandra J. Sanborn
  • Publication number: 20040009199
    Abstract: Lanolin-free lanolin substitute compositions comprising:
    Type: Application
    Filed: March 20, 2003
    Publication date: January 15, 2004
    Inventors: Gary J. Dee, Norman Milstein, Barry A. Salka
  • Publication number: 20030216360
    Abstract: The process for making steroid crystals having a predetermined average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, includes subjecting a supersaturated solution containing a steroid to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.
    Type: Application
    Filed: April 17, 2003
    Publication date: November 20, 2003
    Inventors: Detlef Grawe, Hagen Gerecke, Peter Hoesel, Annette Eichardt, Sabine Gliesing, Uwe Mueller
  • Publication number: 20030195367
    Abstract: The invention concerns a method for preparing a fatty substance ester, characterised in that it consists in subjecting to an esterification reaction at least a fatty substance with at least an alcohol compound selected from the group consisting of sterols, stanols, 4-methylsterols and their hydrogenated homologous, triterpene alcohols and their hydrogenated homologues, and mixtures thereof, in the presence of at least a solid catalyst selected in the group consisting of lanthanide oxides and the mixtures of said oxides.
    Type: Application
    Filed: January 21, 2003
    Publication date: October 16, 2003
    Inventors: Joe Barrault, Mickael Boisseau, Yannick Pouilloux, Antoine Piccirilli
  • Publication number: 20030195178
    Abstract: The invention provides a kernel oil extracted from plant kernels, comprising triglyceride 90-99.9%, diglyceride 0.01-5%, monoglycerides 0.01-3%, sitosterol 0.1-2.5% and cyclolanosterol 0.01-1%. The invention also provides two methods for the extraction of said kernel oil, the pharmaceutical compositions and the uses thereof.
    Type: Application
    Filed: April 16, 2002
    Publication date: October 16, 2003
    Inventor: Dapeng Li
  • Publication number: 20030194372
    Abstract: The present invention provides novel radioimaging probes for use in combination with clinical radioimaging techniques for the visualization of specific tissues or regions of the body. These probes can be packaged into a blood-borne delivery vehicle for targeted delivery to these specific tissues or regions. This invention further provides for the use of synthetic microemulsions or chemically modified human low-density lipoprotein (LDL), such as acetylated LDL (AcLDL), as delivery vehicles to target the radioimaging probes specifically to tissues or regions that contain high concentrations of LDL receptors.
    Type: Application
    Filed: May 6, 2003
    Publication date: October 16, 2003
    Inventors: Hu Liu, Lili Wang, Wu Xiao, Ping Liu
  • Publication number: 20030191101
    Abstract: The present invention provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.
    Type: Application
    Filed: February 26, 2003
    Publication date: October 9, 2003
    Inventors: John-Claude Savoir, Juan Angeles, Aurelio De Gyves, Abraham Gomez
  • Publication number: 20030188340
    Abstract: In one aspect, the invention provides a corn fiber lipid fraction containing phytosterols and phytosterol esters obtained via solvent extraction of a proteolyzed corn fiber, wherein the concentration of phytosterols and phytosterol esters in the lipid fraction is at least about 1.4 times greater than the concentration of phytosterols and phytosterol esters in the lipid fraction of a nonproteolyzed corn fiber.
    Type: Application
    Filed: March 6, 2003
    Publication date: October 2, 2003
    Applicant: Eastman Chemical Company
    Inventors: Charles M. Buchanan, Norma L. Buchanan, John S. Debenham, Michael C. Shelton, Matthew D. Wood
  • Publication number: 20030181662
    Abstract: The invention relates to human procalcitonin and the preparation and use thereof. In particular, a process for preparing human procalcitonin is described wherein a gene coding for a polypeptide comprising the amino acid sequence of human procalcitonin is inserted into a vector; a host organism is transformed with this gene-containing vector; and the polypeptide expressed by the host organism is isolated. Furthermore the use of the polypeptides according to the invention, in particular as medicaments and diagnostic agents is described.
    Type: Application
    Filed: March 24, 2003
    Publication date: September 25, 2003
    Applicant: Dade Behring Marburg GmbH (Germany)
    Inventors: Harald Althaus, Hans-Peter Hauser
  • Patent number: 6593319
    Abstract: Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
    Type: Grant
    Filed: August 14, 2001
    Date of Patent: July 15, 2003
    Assignee: Leo Pharmaceutical Products, Ltd. A/S
    Inventors: Tore Duvold, Welf von Daehne
  • Patent number: 6589945
    Abstract: A process for treating human skin by inhibiting serine protease formation involving contacting the skin with a composition containing a sterol sulfate.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: July 8, 2003
    Assignee: Cognis Deutschland GmbH & Co. KG
    Inventors: Rolf Wachter, Holger Tesmann, Ansgar Behler, Karl-Heinz Maurer
  • Publication number: 20030120095
    Abstract: Disclosed are processes for separating valuable products, including unsaponifiable materials, from any given matrix of raw materials that is mainly composed of saponifiable components and unsaponifiable components. Preferred methods include converting sodium or potassium soaps obtained from the saponification of a starting material into metallic soaps which have a lower melting point, and when melted, have viscosity sufficiently low to enable processing such as by distillation/evaporation processes. Preferred raw materials include animal or vegetable products, as well as by-products, residues, and waste products from the processing of animal or vegetable products, such as from food processing, cellulose processing and the like. Valuable products which may be obtained by the disclosed processes include sterols, vitamins, flavonoids, and tocopherols.
    Type: Application
    Filed: February 20, 2002
    Publication date: June 26, 2003
    Inventors: Rodolfo Rohr, Raul Rohr
  • Publication number: 20030109729
    Abstract: The present invention relates to a fractionation process of the unsaponifiable material derived from black-liquor soaps of the cellulose industry. Through this procedure fractions that essentially contain free sterols, fatty alcohols, sterol esters and fatty alcohol esters respectively are separated. Fractions containing sterols or fatty alcohols can be used as such in the alimentary, cosmetic and pharmaceutical industries or they can be used as raw materials for transforming into other useful products.
    Type: Application
    Filed: January 6, 2003
    Publication date: June 12, 2003
    Inventors: Miguel Angel Fuenzalida Diaz, Alejandro Markovits Rojas, Endre Markovits Schersl
  • Patent number: 6562805
    Abstract: The present invention relates to methods, compounds and compositions for inhibiting effective binding of a chemokine to its cellular receptor. In one form of the invention, a method includes contacting a cellular population with an effective amount of cosalane or an analog thereof. The invention further relates to methods, compounds and compositions for treating inflammatory diseases. In one form, a method includes administering to a patient a therapeutically effective amount of cosalane or an analog thereof.
    Type: Grant
    Filed: January 29, 2001
    Date of Patent: May 13, 2003
    Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human Services
    Inventors: Mark S. Cushman, O. M. Zack Howard
  • Publication number: 20030087887
    Abstract: Compounds of the general formula I 1
    Type: Application
    Filed: March 21, 2002
    Publication date: May 8, 2003
    Inventor: Tore Duvold
  • Publication number: 20030087836
    Abstract: This invention relates to a group of novel sapogenins, their use in anti-cancer applications, and to a process for their production. More particularly, this invention pertains to a novel group of dammarane sapogenins, PAM-120, PBM-110 and PBM-100 (the dammarance sapogenine structure is specifically clean of any sugar moieties (glycons) at any position and hydroxyl at C-20) and PAN-20 and PAN-30 (the dammarance sapogenin structure has sugar moieties but is free of hydroxyl at C-20), obtained by chemical cleavage of dammarane saponins. The invention also includes a novel application of the said sapogenins for anti-cancer treatment by using them separately or together, and/or jointly with other drugs, as well as to the process of producing these novel sapogenins. Said novel dammarane sapogenins show surprising anti-cancer effect when applied, particularly against multi-drug resistant cancers.
    Type: Application
    Filed: October 19, 2001
    Publication date: May 8, 2003
    Inventors: Dong Huang, Dong Feng Qi
  • Publication number: 20030087835
    Abstract: This invention relates to a group of novel sapogenins, their use in anti-cancer applications, and to a process for their production. More particularly, this invention pertains to a novel group of dammarane sapogenins, PAM-120, PBM-110 and PBM-100 (the dammarance sapogenine structure is specifically clean of any sugar moieties (glycons) at any position and hydroxyl at C-20) and PAN-20 and PAN-30 (the dammarance sapogenin structure has sugar moieties but is free of hydroxyl at C-20), obtained by chemical cleavage of dammarane saponins. The invention also includes a novel application of the said sapogenins for anti-cancer treatment by using them separately or together, and/or jointly with other drugs, as well as to the process of producing these novel sapogenins. Said novel dammarane sapogenins show surprising anti-cancer effect when applied, particularly against multi-drug resistant cancers.
    Type: Application
    Filed: July 24, 2001
    Publication date: May 8, 2003
    Inventors: Dong Huang, Dong Feng Qi
  • Publication number: 20030082154
    Abstract: Novel lipid compounds are provided that may be termed “pro-cationic” in that they are neutral or negatively charged until they are either brought into contact with cellular membranes or are internalized by cells. The lipids have a hydrophobic tail group and a hydrophilic head group, the head group incorporating both a positively and negatively charged region at physiological pH. The hydrophobic tail group is stably connected to the positive region of the head group which in turn is connected to the negative region by a disulfide bond that is susceptible to cleavage by membrane-bound and intracellular factors. Cleavage of the disulfide bond removes the negatively charged region from the head group resulting in a lipid that is cationic and therefor fusogenic with negatively charged cell membranes. Consequently, lipids of the invention are useful as components of liposomes that serve as vehicles for delivering pharmaceutical agents into cells with reduced toxicity.
    Type: Application
    Filed: February 22, 2002
    Publication date: May 1, 2003
    Applicant: Isis Pharmaceuticals, Inc.
    Inventor: Christopher Paul Leamon
  • Publication number: 20030069214
    Abstract: A process for preparing compounds of formula (1): 1
    Type: Application
    Filed: August 6, 2002
    Publication date: April 10, 2003
    Inventors: Zhendong Jin, Wensheng Yu
  • Publication number: 20030032824
    Abstract: Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.
    Type: Application
    Filed: September 11, 2002
    Publication date: February 13, 2003
    Inventors: Christian Grondahl, Frederik Christian Gronvald, Peter Faarup, Anthony Murray, Jan Lund Ottesen
  • Publication number: 20030004361
    Abstract: The invention relates to a process for the preparation of stanol esters by hydrogenating a sterol blend in a hydrogenation solvent and at an elevated temperature in the presence of a hydrogenation catalyst, by removing the hydrogenation catalyst from the obtained hot reaction solution, by transesterifying the intermediate stanol blend with a fatty acid methyl ester at an elevated temperature and in the presence of a transesterification catalyst, and by finally purifying the stanol ester blend thus obtained. According to the invention, the intermediate stanol blend is neither crystallized nor removed from the reaction solution but the hydrogenation solvent is replaced therein at least in part by a transesterification reagent. Alternatively, the hydrogenation solvent may also be used as the transesterification solvent, and preferably also as the transesterification reagent.
    Type: Application
    Filed: September 5, 2002
    Publication date: January 2, 2003
    Applicant: Raisio Benecol, Ltd.
    Inventor: Jari Ekblom
  • Patent number: 6482813
    Abstract: Compounds of formula for treating osteoporosis with minimal estrogenic activity are disclosed.
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: November 19, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Publication number: 20020142998
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Application
    Filed: October 9, 2001
    Publication date: October 3, 2002
    Inventors: Kenneth C. Cundy, Mark A. Gallop
  • Publication number: 20020133032
    Abstract: This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chromatography.
    Type: Application
    Filed: February 25, 2000
    Publication date: September 19, 2002
    Inventors: Jufang Barkalow, Steven A. Chamberlin, Arthur J. Cooper, Azad Hossain, John J. Hufnagel, Denton Langridge
  • Patent number: 6441206
    Abstract: The invention concerns dietary fat compositions that contain the hydroxy acid or dicarboxylic acid or amino acid esters of a phytosterol and/or phytostanol, or the mixed esters formed with the alcohols, polyols or polyol (C2 . . . C22)-fatty acid esters of dicarboxylic acids or hydroxy acids, or the (C2 . . . C22)-fatty acid esters of hydroxy acids.
    Type: Grant
    Filed: May 12, 2000
    Date of Patent: August 27, 2002
    Assignee: Raisio Benecol Ltd.
    Inventors: Hannu Mikkonen, Elina Heikkilä, Erkki Anttila, Anneli Lindeman
  • Publication number: 20020107232
    Abstract: This invention pertains to the preparation of a sterol ester-enriched food ingredient utilizing a base-catalyzed tranesterification of free sterol with fatty acyl glyceride. Phytosterols are subject to transesterification with fatty acyl glyceride from vegetable oils in the presence of an alkali catalyst. The reaction is performed under vacuum in the range of 0.01-1 Torr. Following an initial period of transesterification, the reaction mixture is distilled to remove glycerol to enhance the formation of sterol esters. A sterol ester-rich fraction can be isolated from the reaction mixture using organic solvents in combination with aqueous washes.
    Type: Application
    Filed: January 3, 2002
    Publication date: August 8, 2002
    Inventors: Brent D. Flickinger, Richard Grabiel, George Poppe
  • Publication number: 20020098152
    Abstract: Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI)
    Type: Application
    Filed: December 14, 2001
    Publication date: July 25, 2002
    Applicant: Bracco International B.V.
    Inventors: Pier Lucio Anelli, Luciano Lattuada, Fulvio Uggeri, Giovanna Lux, Michele Serleti, Milena Gabellini, Herve Tournier
  • Publication number: 20020091278
    Abstract: A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.
    Type: Application
    Filed: August 15, 2001
    Publication date: July 11, 2002
    Inventors: Paul B. Savage, Chunhong Li
  • Publication number: 20020082237
    Abstract: Novel cationic polymers and cationic lipids, and methods of making and using the same, are provided. The cationic polymers and cationic lipids are useful for the delivery of nucleic acid polymers and oligomers to cells in vitro and in vivo.
    Type: Application
    Filed: February 28, 2002
    Publication date: June 27, 2002
    Inventors: Sean M. Sullivan, Xiao-Ying Meng
  • Patent number: 6399796
    Abstract: An improved process and composition are disclosed for isolation of steroids containing a 5,7-diene functionality from a sterol mixture that comprises formation of a Diels-Alder reaction product of the ster-5,7-dienol in the presence of at least a catalytic amount of an ethylenically unsaturated C12-C24 fatty carboxylic acid.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: June 4, 2002
    Assignee: Roche Vitamins Inc.
    Inventor: Michael M. Schwartz
  • Patent number: 6392070
    Abstract: The invention provides methods for separating outer birch bark from inner birch bark. The invention also provides methods for isolating betulin; lupeol; betulinic acid; 9,10-epoxy-18-hydroxyoctadecanoic acid; 9,10,18-trihydroxyoctadecanoic acid; polyphenolic polymers and fatty acids from birch bark.
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: May 21, 2002
    Assignee: Regents of the University of Minnesota
    Inventors: Pavel A. Krasutsky, Robert M. Carlson, Vitaliy V. Nesterenko
  • Patent number: 6388108
    Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: May 14, 2002
    Assignee: Genaera Corporation
    Inventors: Meena Rao, Binyamin Feibush, William Kinney, Michael Zasloff, Lincoln Noecker
  • Publication number: 20020025951
    Abstract: A compound having the general formula: 1
    Type: Application
    Filed: May 24, 1999
    Publication date: February 28, 2002
    Inventors: HYUN K. KIM, RICHARD P. BLYE, PEMMARAJU N. RAO, JAMES W. CESSAC, CARMIE K. ACOSTA
  • Publication number: 20020007079
    Abstract: Certain novel sterol derivatives having no hydroxy group in the 3-position can be used to regulate the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.
    Type: Application
    Filed: July 9, 1999
    Publication date: January 17, 2002
    Inventors: ANTHONY MURRAY, PETER FAARUP
  • Patent number: 6177417
    Abstract: The present invention relates to a cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives of the following formula 1, process for preparation and use thereof. The cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives of the present invention may be used as a host material in the host-guest chemistry, in detail as a material for ion sensors, optical sensors, gas sensors, biosensors, chromatographies, photostimulated ion-binding resins, ion exchange resins and organic reactions. (In the above formula 1, R, R1, R2, R3 and n are defined in the specifications).
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: January 23, 2001
    Inventors: Junho Chu, Hyung Jung Pyun, In Jun Yoon, Jae Ho Shin, Hakhyun Nam, Geun Sig Cha
  • Patent number: 6046186
    Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: April 4, 2000
    Assignee: SRI International
    Inventors: Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Kazuhiko Shigeno
  • Patent number: 6040468
    Abstract: 16.alpha., 17.alpha.-dialkylated steroids are prepared by reacting a 16.alpha.-alkyl-17(20)-enyl-20-silyl ether with an alkylating agent and an enol silyl ether cleaving agent in a suitable solvent.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: March 21, 2000
    Assignee: Alcon Laboratories, Inc.
    Inventor: Raymond E. Conrow
  • Patent number: 5948925
    Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: September 7, 1999
    Assignee: Genzyme Corporation
    Inventors: Mikaela N. Keynes, Craig S. Siegel, Edward R. Lee, David J. Harris
  • Patent number: 5942634
    Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: August 24, 1999
    Assignee: Genzyme Corporation
    Inventors: Craig S. Siegel, Edward R. Lee, David J. Harris
  • Patent number: 5925628
    Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: July 20, 1999
    Assignee: Genzyme Corporation
    Inventors: Edward R. Lee, David J. Harris, Craig S. Siegel
  • Patent number: 5760255
    Abstract: The invention is drawn to a process for the conversion of primary and secondary alcohols into the corresponding fluorine compounds in the presence of an organic solvent, 2-3 equivalents of a strong base and perfluoroalkylsulphonyl fluorides, such as perfluorobutanesulphonyl fluoride or higher homologues.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: June 2, 1998
    Assignee: Bayer AG
    Inventors: Helmut Vorbruggen, Barbel Bennua-Skalmowski
  • Patent number: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • Patent number: 5716800
    Abstract: The invention concerns the use of an organic or hydro-organic extract of Poria cocos Wolf fungi for the preparation of a cosmetic and/or pharmaceutical composition, in particular a dermatological composition, for the treatment of acne and oily skin.The preferred concentration of Poria cocos extract is in the range 0.001% to 5% by weight with respect to the total weight of the final composition.Cosmetic or pharmaceutical compositions, in particular dermatological compositions, can be prepared for the effective treatment of acne and oily skin.
    Type: Grant
    Filed: December 27, 1995
    Date of Patent: February 10, 1998
    Assignee: LVMH Recherche
    Inventors: Alain Meybeck, Frederic Bonte
  • Patent number: 5712109
    Abstract: There is disclosed a compound having the formula ##STR1## which is produced by the fungus, Arthrinium arundinis ATCC 74359, and exhibits antifungal activity.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: January 27, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Jerrold M. Liesch, Maria S. Meinz, Janet C. Onishi, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Deborah L. Zink, Angeles Cabello, Maria T. Diez, Isabella Martin, Fernando Pelaez, Francisca Vicente
  • Patent number: 5641765
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: June 24, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Alan Holt, Mark Alan Levy
  • Patent number: 5641877
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: June 24, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Alan Holt, Mark Alan Levy
  • Patent number: 5637691
    Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: June 10, 1997
    Assignee: Magainin Pharmaceuticals, Inc.
    Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty
  • Patent number: 5637722
    Abstract: "Esters" are synthesized by reacting a nucleophile with a propargyl xanthate advantageously having the formula (I):R.sub.3 --C.tbd.C--CR.sub.1 R.sub.2 --S--CS--Y--R (I)in the presence of at least one acid, Bronsted or otherwise, and at a temperature ranging from 0.degree. to 300.degree. C.; the subject reaction is particularly applicable to a wide variety of chiral organic syntheses.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: June 10, 1997
    Assignee: Rhone-Poulenc Chimie
    Inventors: Jean Boivin, Eric B. Henriet, Samir Z. Zard
  • Patent number: 5618806
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: April 8, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy
  • Patent number: RE35517
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: May 20, 1997
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan