Unsaturation Between The 7- And 8-positions (e.g., Ergosterols, 7 Dehydrocholesterols, Provitamin D, Etc.) Patents (Class 552/547)
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Patent number: 9376462Abstract: Processes for preparing lanostane triterpenes from the medicinal mushroom Ganoderma lucidum, and related compounds are described. Compounds, compositions, and methods for treating cancer are also described.Type: GrantFiled: September 29, 2011Date of Patent: June 28, 2016Assignee: Indiana University Research and Technology CorporationInventors: Robert Minto, Erin Kennedy
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Publication number: 20140378645Abstract: A problem of the present invention is to provide a liquid crystal aligning agent which never deteriorates even in a method where UV is irradiated such as a liquid crystal dropping method or the like, and is capable of forming a liquid crystal alignment film having high UV resistance.Type: ApplicationFiled: January 7, 2013Publication date: December 25, 2014Inventors: Atsushi Kozaki, Michihiko Sato
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Publication number: 20130331584Abstract: Recombinant DNA techniques are used to produce oleaginous recombinant cells that produce triglyceride oils having desired fatty acid profiles and regiospecific or stereospecific profiles. Genes manipulated include those encoding stearoyl-ACP desturase, delta 12 fatty acid desaturase, acyl-ACP thioesterase, ketoacyl-ACP synthase, and lysophosphatidic acid acyltransferase. The oil produced can have enhanced oxidative or thermal stability, or can be useful as a frying oil, shortening, roll-in shortening, tempering fat, cocoa butter replacement, as a lubricant, or as a feedstock for various chemical processes. The fatty acid profile can be enriched in midchain profiles or the oil can be enriched in triglycerides of the saturated-unsaturated-saturated type.Type: ApplicationFiled: July 12, 2013Publication date: December 12, 2013Applicant: Solazyme, Inc.Inventors: Scott Franklin, Aravind Somanchi, George Rudenko, Riyaz Bhat, Xinhua Zhao, Risha Bond, Walter Rakitsky, Alejandro Marangoni, Diza Braksmayer
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Publication number: 20130317240Abstract: Recombinant DNA techniques are used to produce oleaginous recombinant cells that produce triglyceride oils having desired fatty acid profiles and regiospecific or stereospecific profiles. Genes manipulated include those encoding stearoyl-ACP desturase, delta 12 fatty acid desaturase, acyl-ACP thioesterase, ketoacyl-ACP synthase, and lysophosphatidic acid acyltransferase. The oil produced can have enhanced oxidative or thermal stability, or can be useful as a frying oil, shortening, roll-in shortening, tempering fat, cocoa butter replacement, as a lubricant, or as a feedstock for various chemical processes. The fatty acid profile can be enriched in midchain profiles or the oil can be enriched in triglycerides of the saturated-unsaturated-saturated type.Type: ApplicationFiled: July 12, 2013Publication date: November 28, 2013Inventors: Scott Franklin, Aravind Somanchi, George Rudenko, Riyaz Bhat, Xinhua Zhao, Risha Bond, Walter Rakitsky, Alejandro Marangoni, Diza Braksmayer
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Patent number: 8586770Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.Type: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8575142Abstract: To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance or ameliorate the pathosis, the present invention provides an agent or a food or drink which contains a compound having a lophenol skeleton, or an organic solvent extract or a hot water extract of a Liliaceae plant or, a fraction thereof containing the compound as an active ingredient.Type: GrantFiled: September 22, 2006Date of Patent: November 5, 2013Assignee: Morinaga Milk Industry Co., Ltd.Inventors: Miyuki Tanaka, Eriko Misawa
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Publication number: 20130144076Abstract: Provided herein is a method of preparing a composition of a phytosterol derivative comprising a phytosterol intermediate coupled to a water-soluble carrier. The method controls the molecular structure of the product, resulting in phytosterol derivatives which are soluble in water at high concentration. The phytosterol derivatives provided herein are useful as ingredients for foods and pharmaceuticals, and have cholesterol-reducing effects.Type: ApplicationFiled: March 10, 2011Publication date: June 6, 2013Applicant: KIP BIOTECH LLCInventors: Narayana Chatla, Robert William Rambacher, Yao Yao
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Publication number: 20130053357Abstract: Provided is a skin irritation suppressant for transdermal preparations, having a sufficient reduction effect of skin irritation due to a drug. Also provided is a transdermal preparation comprising the skin irritation suppressant. One embodiment of the invention is a skin irritation suppressant for suppressing the skin irritation due to a drug and a pharmaceutical ingredient to be used in a transdermal preparation other than the drug, the skin irritation suppressant comprising a sterol compound selected from the group consisting of cholesterol, cholesterol derivatives and cholesterol analogs, and the drug is one or more basic drugs selected from the group consisting of tolterodine, asenapine, bisoprolol, risperidone, nicotine and citalopram, and their pharmaceutically acceptable salts.Type: ApplicationFiled: April 27, 2011Publication date: February 28, 2013Applicant: HISAMITSU PHARMACEUTICAL CO., INC.Inventors: Hidekazu Kuma, Kenji Atarashi, Kazuhiro Suzuki, Kazunosuke Aida
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Publication number: 20120094328Abstract: The present invention provides dendritic cells (DCs) having reduced inflammatory activity, a method for producing DCs capable of inducing regulatory T cells and regulatory T cells, and substances useful for such a method, wherein the DCs and regulatory T cells are useful for prevention and treatment of immune diseases. The present invention relates to a cereal plant-derived material fermented with a koji microorganism, which is obtained by fermentation thereof with a koji microorganism, or a processed product thereof. Preferably, the fermented product or a processed product thereof comprises 14-dehydroergosterol. According to the present invention, regulatory DCs and regulatory T cells can be induced and the proliferation of inflammatory T cells can be suppressed using plant-derived materials.Type: ApplicationFiled: June 25, 2010Publication date: April 19, 2012Applicant: KIRIN HOLDINGS KABUSHKIK KAISHAInventors: Daisuke Fujiwara, Masaru Kato, Hideki Koizumi, Kumiko Ikado, Yasuhisa Ano
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Patent number: 8101594Abstract: Compounds such as 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol which have an activity for improving pancreatic function are used as an active ingredient of a pancreas function improving drug and food or drink.Type: GrantFiled: February 28, 2006Date of Patent: January 24, 2012Assignee: Morinaga Milk Industry Co., Ltd.Inventors: Miyuki Tanaka, Eriko Misawa, Noriko Habara, Muneo Yamada
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Patent number: 7884221Abstract: The present invention provides a method of separating ergosterol from a solution containing ergosterol in water-insoluble organic solvent, comprising supplying water to the solution and precipitating ergosterol. According to the method of the present invention, ergosterol crystals can be obtained at a high yield. Moreover, controlled water supply provides granular ergosterol aggregates exhibiting good solid-liquid separation character at a high yield.Type: GrantFiled: November 7, 2003Date of Patent: February 8, 2011Assignee: Kaneka CorporationInventor: Hideo Kawachi
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Publication number: 20110009615Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.Type: ApplicationFiled: June 30, 2010Publication date: January 13, 2011Applicant: MITSUBISHI CHEMICAL GROUP SCIENCE AND TECHNOLOGY RESEARCH CENTER, INC.Inventors: Jun Takehara, Naoya Fujiwara, Junya Kawai, Kyouko Endou, Kiyoshi Ooyama
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Publication number: 20100305341Abstract: The present invention provides methods for production of one or more sterol compounds. Further provided are methods and systems for producing engineered oleaginous yeast or fungi that are capable of production of one or more sterol compounds, and compositions which utilize the produced sterol compound(s).Type: ApplicationFiled: September 28, 2007Publication date: December 2, 2010Applicant: MICROBIA PRECISION ENGINEERINGInventors: Richard Bailey, Joshua Trueheart, Kevin T. Madden
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Patent number: 7825269Abstract: Anti-nematode compounds, compositions, and methods for identifying such compounds are disclosed, where the compounds have the formula I: where Q, Q?, R1, R2, and n are defined herein.Type: GrantFiled: March 8, 2007Date of Patent: November 2, 2010Assignee: Board of Regents, University of Texas SystemInventors: David J. Mangelsdorf, Richard J. Auchus, Daniel L. Motola, Carolyn L. Cummins, Kamalesh K. Sharma
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Publication number: 20100120735Abstract: The present invention refers to a compound having anti-inflammatory and antiviral activity according to the following structural formula: wherein, R1 and R3 are selected from H, HO—, R5—O—, HCOO—, R5—COO—, —OOC—R6—COO—, p-toluene sulphonate, phosphate, tartrate, maleate, sulphate, fluorine, chlorine, bromine, iodine and methanesulphonate, R2 is selected from H, HO—, R5—O—, HCOO—, R5—COO—, —OOC—R6—COO—, p-toluene sulphonate, phosphate, tartrate, maleate, sulphate, fluorine, chlorine, bromine, and iodine, or —R1 and —R2 can be together —O—, (CH3)2—(CO)2-(ó-(CH3—CH2)2—(CO)2— R4 and R5 are selected from H and linear or branched C1-C4 alkyl, R6 is —(CH2)n equals to 1, 2 ó 3, and, can be a single bond or double bond, to the pharmaceutical compositions comprising the same, to a process for preparing the same and to the use of the same for preparing pharmaceutical compositions.Type: ApplicationFiled: July 4, 2008Publication date: May 13, 2010Applicants: Consejo Nacional de Investigaciones Cientificas Y Tecnicas (Conicet), Inis Biotech LLCInventors: Javier Alberto Ramirez, Flavia Mariana Michelini, Lydia Raquel Galagovsky, Alejandro Berra, Laura Edith Alche
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Publication number: 20100036140Abstract: The invention provides sterols modified by polyethylene glycol represented by the following formula, the preparation and the use thereof, wherein each symbol is defined as in the description.Type: ApplicationFiled: December 13, 2007Publication date: February 11, 2010Inventor: Wenfang Zhang
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Patent number: 7615546Abstract: This invention relates to certain sugar esters of phytosterols of formula (I).Type: GrantFiled: September 15, 2008Date of Patent: November 10, 2009Assignee: BioDerm ResearchInventor: Shyam K Gupta
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Publication number: 20090247497Abstract: An isolated and purified form of ergosta-7,22-dien-3?-ol and its use as a marker for identifying Coriolus versicolor (Yunzhi) are provided. A composition used for treatment of cancer and other related diseases or disorders comprising ergosta-7,22-dien-3?-ol is also provided.Type: ApplicationFiled: March 18, 2009Publication date: October 1, 2009Inventor: Hei Ling Helen CHAN
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Publication number: 20080255077Abstract: Compounds such as 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol which have an activity for improving pancreatic function are used as an active ingredient of a pancreas function improving drug and food or drink.Type: ApplicationFiled: February 28, 2006Publication date: October 16, 2008Inventors: Miyuki Tanaka, Eriko Misawa, Noriko Habara, Muneo Yamada
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Patent number: 6989456Abstract: According to the present invention, there is provided a process for enzymatically producing dietary sterol fatty acid esters having physiological activities from phytosterols and fatty acids or oils and fats using lipase as a catalyst; the synthetic reaction conditions and the purification steps are so structured that dietary sterol fatty acid esters superior in sensory qualities including color, odor and taste, and safety, which is applicable as a general food, a health food or pharmaceuticals can be produced.Type: GrantFiled: September 26, 2001Date of Patent: January 24, 2006Assignee: Ikeda Food Research Co., Ltd.Inventors: Naoko Seo, Shoji Kaneko, Fumi Sato, Seiji Norinobu, Mitsumasa Mankura
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Patent number: 6800317Abstract: This invention relates to phytosterols and phytostanols, in particular to fatty acid esters of phytosterols and phytostanols with a specified fatty acid composition. The invention further relates to methods for preparation of the phytosterol and phytostanol esters and their uses.Type: GrantFiled: May 16, 2003Date of Patent: October 5, 2004Assignee: Raisio Benecol OyInventors: Ingmar Wester, Jari Ekblom
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Patent number: 6589588Abstract: This invention relates to phytosterols and phytostanols, in particular to fatty acid esters of phytosterols and phytostanols with a specified fatty acid composition. The invention further relates to methods for preparation of the phytosterol and phytostanol esters and their uses.Type: GrantFiled: December 20, 2000Date of Patent: July 8, 2003Assignee: Raisio Benecol OyInventors: Ingmar Wester, Jari Ekblom
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Patent number: 6518262Abstract: The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03H or ═NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; R4 is hydrogen, (C1-6)alkyl or (C1-6)acyl; R5 is hydrogen; or R5 designates, together with R6, an additional bond between the carbon atoms at which R5 and R6 are placed; R6 is hydrogen, hydroxy or halogen; or R6 designates, together with R5, an additional bond between the carbon atoms at which R6 and R5 are placed; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, optionally substituted with OH, (C1-4)alkoxy, or halogen; or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.Type: GrantFiled: August 22, 2001Date of Patent: February 11, 2003Assignee: Akzo Nobel N.V.Inventors: D. Leysen, J. van der Louw, R. G. J. M. Hanssen, Anja Wiersma
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Patent number: 6429320Abstract: Processes for purifying compounds are disclosed which include reacting (i) a mixture of at least one tocopherol compound or sterol compound, and an alcohol having from about 10 to 30 carbons with (i) one or more boron-containing compounds to form a second mixture of orthoborate esters, wherein the mole ratio of tocopherol, sterol and alcohol to boron is at least about 2.5:1; heating the second mixture to form a residue containing the orthoborate esters; contacting the residue with a compound capable of solvolyzing the orthoborate esters to form a third mixture including the boron-containing compound(s), the alcohol and the tocopherol and/or sterol compound(s); and recovering the tocopherol and/or sterol compound(s).Type: GrantFiled: August 3, 2001Date of Patent: August 6, 2002Assignee: Cognis CorporationInventors: Patrick M. McCurry, Jr., Stephen W. Turner, Carl Pickens
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Patent number: 6413571Abstract: Novel sterol/stanol esters of a conjugated fatty acid are provided through the esterification or transesterification of a sterol such as beta-sitosterol or a hydrogenated form thereof (stanol). Such novel esters exhibit the combined properties normally possess by the sterol/stanol compound and the conjugated fatty acid and as such are excellent additives for dietetic foods and supplements.Type: GrantFiled: October 20, 2000Date of Patent: July 2, 2002Assignee: The Board of Regents for Oklahoma State UniversityInventor: Linsen Liu
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Patent number: 6391370Abstract: Plant sterols have been shown to be cholesterol-reducing agents in human serum. In the present invention, plant sterols, plant stanols, plant sterol esters and other non-toxic sterols are micromilled with emulsifiers in a solvent (water or edible oil) to produce dispersion which can be incorporated into full-fat, reduced-fat, low-fat, fat-free and triglyceride-free food products. Such water-based or edible oil-based dispersions can be used to incorporate relatively high levels of such sterols/stanols in food products without the adverse organoleptic effect normally associated with the use of such plant sterols and plant stanols.Type: GrantFiled: April 6, 2000Date of Patent: May 21, 2002Assignee: Kraft Foods, Inc.Inventors: Richard B. Rogers, John B. Topinka, Elizabeth Gwartney, Johnny Casanovas, Scott T. Ostergaard, Daniel G. Lis, John A. DeWalt, Anilkumar G. Gaonkar
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Patent number: 6352737Abstract: The invention relates to the use of nanoscale sterols and/or sterol esters with particle diameters of 10 to 300 nm as food additives and as active substances for the production of hypocholesterolemic agents. The particular fineness of the particles promotes more rapid absorption by the blood serum after oral ingestion by comparison with conventional sterols and sterol esters.Type: GrantFiled: June 20, 2000Date of Patent: March 5, 2002Assignee: Cognis Deutschland GmbHInventors: Hans Dolhaine, Christian Kropf, Peter Christophliemk, Bernd Fabry, Manfred Biermann, Christine Schroeder
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Patent number: 6310225Abstract: Steroid derivatives useful as intermediates for producing vitamin D derivates as well as processes for producing the steroid derivatives are provided. The steroid derivatives include halide compounds represented by the following formulae: wherein X, R1 and R2 are as defined by the specification.Type: GrantFiled: November 20, 2000Date of Patent: October 30, 2001Assignee: Kuraray Co., Ltd.Inventors: Yoshihisa Tsuji, Toshimichi Mitani
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Patent number: 6147068Abstract: A pharmaceutical composition of matter for delivering nitric oxide. The composition is an amine that was reacted with nitric oxide. The composition of matter is lipophilic and insoluble and therefore delivers nitric oxide to the specific area of the body where it is introduced. Also, a method of synthesizing an amine and reacting it with nitric oxide to form the pharmaceutical composition of matter. Finally, a method of using the pharmaceutical composition of matter to deliver nitric oxide to the body.Type: GrantFiled: September 21, 1998Date of Patent: November 14, 2000Assignee: The University of AkronInventors: Daniel J. Smith, Dominick Roselle
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Patent number: 5952516Abstract: 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: GrantFiled: May 8, 1997Date of Patent: September 14, 1999Assignee: Genzyme CorporationInventors: Craig S. Siegel, Edward R. Lee, David J. Harris
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Patent number: 5925628Abstract: 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: GrantFiled: March 31, 1997Date of Patent: July 20, 1999Assignee: Genzyme CorporationInventors: Edward R. Lee, David J. Harris, Craig S. Siegel
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Patent number: 5686435Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.Type: GrantFiled: December 7, 1995Date of Patent: November 11, 1997Assignee: Research Institute for Medicine and ChemistryInventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
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Patent number: 5591733Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.Type: GrantFiled: August 2, 1993Date of Patent: January 7, 1997Assignee: University of Southern CaliforniaInventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
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Patent number: 5496813Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.Type: GrantFiled: August 13, 1992Date of Patent: March 5, 1996Assignee: Marigen S.A.Inventors: Carl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
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Patent number: 5494905Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an 0-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile 0-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.Type: GrantFiled: May 31, 1994Date of Patent: February 27, 1996Assignee: Research Institute for Medicine and ChemistryInventors: Robert H. Hesse, Gaddam S. Reddy, Sundara K. S. Setty
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Patent number: 5359055Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.Type: GrantFiled: November 27, 1991Date of Patent: October 25, 1994Assignee: Kuraray Co., Ltd.Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
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Patent number: 5352781Abstract: The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxycarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl, and R.sub.2 is hydroxyl, lower alkoxy, or unsubstituted or substituted lower alkyl, to yield a C-25 or C-26 precursor of the formula ##STR2## which is appropriately functionalized for conversion into the corresponding steroid or secosteroid by treatment as hereinafter described.Type: GrantFiled: March 19, 1993Date of Patent: October 4, 1994Assignee: Hoffmann-La Roche Inc.Inventors: George P. Yiannikouros, Percy S. Manchand
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Patent number: 5270041Abstract: There are described antitumour sterols, their fatty acid esters and glucosides, processes for their preparation, spontaneously dispersible agents containing these sterols, their fatty acid esters and glucosides, and their use for treating tumours.Type: GrantFiled: February 15, 1991Date of Patent: December 14, 1993Assignee: Marigen S.A.Inventors: Carl Eugster, Conrad Eugster, Walter Haldemann, Giorgio Rivara
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Patent number: 5206230Abstract: Fluorine-containing vitamin D.sub.3 analogues of the formula[I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms, or an alkyl having 1 to 8 carbon atoms, X is a straight carbon chain having 4 to 6 carbon atoms which contains at least one double or triple bond, which have excellent vitamin D.sub.3 -like activities, particularly anti-tumor activity owing to differentiation-inducing activity and are useful for the prophylaxis and treatment of various tumors, and intermediates therefor.Type: GrantFiled: June 5, 1991Date of Patent: April 27, 1993Assignee: Daikin Industries, Ltd.Inventors: Nobuo Ikekawa, Yoshiro Kobayashi, Takeo Taguchi, Yoko Tanaka, Yutaka Ohira
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Patent number: 5023250Abstract: New 14.alpha.-carboxyalkyl sterols are regulators of HMG-CoA reductase and inhibitors of mammalian 14.alpha.-methyl demethylase and are useful in lowering serum cholesterol levels and treating fungal infections.Type: GrantFiled: August 24, 1989Date of Patent: June 11, 1991Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Timothy F. Gallagher, Ruth J. Mayer, Brian W. Metcalf
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Patent number: RE35517Abstract: 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: GrantFiled: November 23, 1992Date of Patent: May 20, 1997Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan