Boron, Silicon, Selenium Or Tellurium Containing Patents (Class 552/505)
  • Patent number: 9388210
    Abstract: The present disclosure is generally directed to neuroactive 17(20)-Z-vinylcyano-substituted compound of Formula (I) and (II), as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: July 12, 2016
    Assignee: WASHINGTON UNIVERSITY
    Inventors: Douglas Covey, Eva Kudova
  • Publication number: 20150140063
    Abstract: A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a C Log P value of at least 6.0, 6.25, 6.5, 7.5, 8.5, or 10.
    Type: Application
    Filed: January 22, 2015
    Publication date: May 21, 2015
    Applicant: BRIGHAM YOUNG UNIVERSITY
    Inventor: Paul B. Savage
  • Patent number: 8975310
    Abstract: A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a CLogP value of at least 6.5.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: March 10, 2015
    Assignee: Brigham Young University
    Inventor: Paul B. Savage
  • Publication number: 20150005518
    Abstract: A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17?-ethynyl-17?-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 1, 2015
    Applicants: CRYSTAL PHARMA, S.A.U., THE POPULATION COUNCIL INC.
    Inventors: Luis Gerardo Gutiérrez Fuentes, Celso Miguel Sandoval Rodríguez
  • Publication number: 20150005489
    Abstract: The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Inventors: Lung-Huang Kuo, Hsiao-Ping Fang, Ming-Feng Wu, Yu-Sheng Chang
  • Patent number: 8729257
    Abstract: This invention relates to a novel class of hybrid lipid compound based on pentaerythritol, their intermediates, preparation methods and uses thereof. Different kinds of functional groups such as alkyl chain, siloxane group, azobenzene, porphyrins, cholesterol, benzene ring and carboxyl were introduced into the four hydroxyl groups of pentaerythritol through chemical reaction to obtain the final hybrid lipid compounds based on pentaerythritol. Cerasomes prepared from such lipids have uniform size, silicate network surface, good stability and biocompatibility, and the leakage of drugs is not easy. The present liposome can be used as functional materials such as drugs or drug carriers, or used for optical storage and molecular devices, simulation, design and synthesis of artificial systems, nano-composite membrane materials and the removal of organic pollutants, etc., in addition, the preparation method of the present invention is simple, and it is easy for industrial production.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: May 20, 2014
    Assignee: Harbin Institute of Technology
    Inventors: Zhifei Dai, Xiaolong Liang, Xiuli Yue
  • Publication number: 20140107091
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of th
    Type: Application
    Filed: June 1, 2012
    Publication date: April 17, 2014
    Applicant: ESTETRA S.A.
    Inventor: Jean-Claude Pascal
  • Publication number: 20140107358
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2?Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).
    Type: Application
    Filed: June 1, 2012
    Publication date: April 17, 2014
    Applicant: ESTETRA S.A.
    Inventor: Jean-Claude Pascal
  • Publication number: 20140011992
    Abstract: The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
    Type: Application
    Filed: December 20, 2012
    Publication date: January 9, 2014
    Applicant: CRYSTAL PHARMA, S.A.U.
    Inventors: Alfonso Perez Encabo, Jose Angel Turiel Hernandez, Francisco Javier Gallo Nieto, Antonio Lorente Bonde-Larsen, Celso Miguel Sandoval Rodriguez
  • Publication number: 20130123523
    Abstract: Described herein is a process for the synthesis of etonogestrel and desogestrel and intermediates used to form etonogestrel and desogestrel.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 16, 2013
    Inventors: Klaus Nickisch, Bindu Santhamma
  • Publication number: 20130053567
    Abstract: The invention relates to a method for producing silyl enol ether compound (3) by reacting ketone or aldehyde compound (1) with allylsilane compound (2) in the presence of a base and 0.00001 to 0.5 equivalents of an acid catalyst relative to ketone or aldehyde compound (1).
    Type: Application
    Filed: March 3, 2011
    Publication date: February 28, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Kiyosei Takasu, Yoshiji Takamoto, Kei Kurahashi
  • Publication number: 20130053507
    Abstract: A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a CLogP value of at least 6.5.
    Type: Application
    Filed: July 20, 2012
    Publication date: February 28, 2013
    Inventor: Paul B. Savage
  • Publication number: 20120283217
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: July 16, 2012
    Publication date: November 8, 2012
    Applicant: SATORI PHARMACEUTICALS, INC.
    Inventors: Mark A. Findeis, Steffen P. Creaser
  • Publication number: 20120283450
    Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: July 18, 2012
    Publication date: November 8, 2012
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
  • Patent number: 8288367
    Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: October 16, 2012
    Assignee: Solvay Pharmaceuticals GmBH
    Inventors: Josef Messinger, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Mikko Unkila
  • Publication number: 20120149732
    Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.
    Type: Application
    Filed: August 22, 2011
    Publication date: June 14, 2012
    Inventors: Alexander Chucholowski, Alisher Khasanov, Gregory Parker, Tong Zhu
  • Publication number: 20120149653
    Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 14, 2012
    Inventors: Alexander Chucholowski, Alisher Khasanov, Gregory Parker, Tong Zhu
  • Publication number: 20120116064
    Abstract: This invention relates to a novel class of hybrid lipid compound based on pentaerythritol, their intermediates, preparation methods and uses thereof. Different kinds of functional groups such as alkyl chain, siloxane group, azobenzene, porphyrins, cholesterol, benzene ring and carboxyl were introduced into the four hydroxyl groups of pentaerythritol through chemical reaction to obtain the final hybrid lipid compounds based on pentaerythritol. Cerasomes prepared from such lipids have uniform size, silicate network surface, good stability and biocompatibility, and the leakage of drugs is not easy. The present liposome can be used as functional materials such as drugs or drug carriers, or used for optical storage and molecular devices, simulation, design and synthesis of artificial systems, nano-composite membrane materials and the removal of organic pollutants, etc., in addition, the preparation method of the present invention is simple, and it is easy for industrial production.
    Type: Application
    Filed: July 19, 2010
    Publication date: May 10, 2012
    Applicant: HARBIN INSTITUTE OF TECHNOLOGY
    Inventors: Zhifei Dai, Xiaolong Liang, Xiuli Yue
  • Publication number: 20120101052
    Abstract: The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5-ene-3?-yl)-?-D-glucopyranosiduronate, 16?,3?-dihydroxy-5?-androstan-17-one or 3,7,16,17-tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene, 3,7,16,17-tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.
    Type: Application
    Filed: May 13, 2011
    Publication date: April 26, 2012
    Inventor: James M. Frincke
  • Publication number: 20120077777
    Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
    Type: Application
    Filed: May 20, 2010
    Publication date: March 29, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), PIERRE FABRE MEDICAMENT
    Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
  • Publication number: 20120071570
    Abstract: Provided is a novel oily material that spreads smoothly upon application and is free from stickiness, and also gives ungreasy and moisturized feeling after application, but does not give friction feeling peculiar to silicone. The invention was completed upon finding that a specific acyl acidic amino acid monosilicone monosterol ester can solve the foregoing problems.
    Type: Application
    Filed: September 22, 2011
    Publication date: March 22, 2012
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takanori SUGIMOTO, Tatsuya Hattori, Souichirou Ootake
  • Publication number: 20110218162
    Abstract: The invention relates to the use of compounds to treat a number of conditions, such as thrombocytopenia, neutropenia or the delayed effects of radiation therapy. Compounds that can be used in the invention include methyl-2,3,4-trihydroxy-1-O-(7,17-dioxoandrost-5-ene-3?-yl)-?-D-glucopyranosiduronate, 16?,3?-dihydroxy-5?-androstan-17-one or 3,7,16,17-tetrahydroxyandrost-5-ene, 3,7,16,17-tetrahydroxyandrost-4-ene, 3,7,16,17-tetrahydroxyandrost-1-ene or 3,7,16,17-tetrahydroxyandrostane that can be used in the treatment method.
    Type: Application
    Filed: May 13, 2011
    Publication date: September 8, 2011
    Inventor: James M. Frincke
  • Publication number: 20110082306
    Abstract: Steroids are well known, medicinal relevant, chemical entities. There are numerous steroids which have fully or partially reduced ‘A’ rings. These fully or partially reduced ‘A’ rings have been reduced in the past through Birch and other dissolving metal reductions. Novel reducing conditions for steroid substrates are described which utilizes stabilized alkali metal-silica gel materials. The invention relates to a method for reducing a double bond within a steroid by contacting an unsaturated steroid having a phenyl ring with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a proton source under reaction conditions sufficient to form a reduced steroid having a diene structure.
    Type: Application
    Filed: March 24, 2009
    Publication date: April 7, 2011
    Inventors: Michael J. Costanzo, Mitul N. Patel, Paul F. Vogt
  • Publication number: 20110046402
    Abstract: The subject of the invention is a method for preparing compounds of general formula (I): in which A, Z, R3 are as defined in the description, and the intermediate compounds for carrying out this method.
    Type: Application
    Filed: October 29, 2010
    Publication date: February 24, 2011
    Applicant: Aventis Pharma S.A.
    Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
  • Publication number: 20100292184
    Abstract: The 17?-cyano-19-androst-4-ene derivatives of the present invention possess gestagenic activity.
    Type: Application
    Filed: June 12, 2008
    Publication date: November 18, 2010
    Applicant: BAYER SCHERING PHARMA AG
    Inventors: Joachim Kuhnke, Jan Huebner, Rolf Bohlmann, Thomas Frenzel, Ulrich Klar, Frederik Menges, Sven Ring, Steffen Borden, Hans Peter Muhn, Katja Prelle
  • Publication number: 20100279850
    Abstract: A coating composition comprising a Photocatalyst Composition comprising a photocatalyst and a pendent silyl ester group, wherein the photocatalyst produces singlet oxygen in the presence of light and ambient air. In certain embodiments, the coating composition further comprises a singlet oxygen scavenger.
    Type: Application
    Filed: January 5, 2010
    Publication date: November 4, 2010
    Inventors: JOHN L. LOMBARDI, CHUCHAWIN CHANGTONG
  • Publication number: 20100048887
    Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 20, 2009
    Publication date: February 25, 2010
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
  • Publication number: 20040181055
    Abstract: 6&agr;-fluorpregnanes (I), where the dotted line between positions 1 and 2 represents a single or double bond; R1 is OH, OCOR2, X, SO3R3, or an (R7)(R8)(R9)SiO— group, where X is halogen, R2 and R3 are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, and R7, R8 and R9, equal or different, are C1-6 alkyl or phenyl optionally substituted by C1-4 alkyl, can be obtained by means of a high stereoselectivity process comprising reacting a 3-(trisubstituted)silyloxy-pregna-3,5-diene (IV) with a fluorinating agent selected among N-fluorosulfonimides and N-fluorosulfonamides. The 6&agr;-fluorpregnanes (I) are intermediates for the synthesis of steroids useful as anti-inflammatory and anti-asthmatic agents.
    Type: Application
    Filed: January 26, 2004
    Publication date: September 16, 2004
    Applicant: Ragactives, S.L.
    Inventors: Jose Vicente Murillo Garrido, Luis Octavio Silva Guisasola, Jorge Martin Juarez
  • Patent number: 6767903
    Abstract: The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: July 27, 2004
    Assignee: Schering AG
    Inventors: Arwed Cleve, Gerhard Sauer, Christoph Huwe, Karsten Parczyk, Jens Hoffmann, Martin Schneider
  • Publication number: 20040097406
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Application
    Filed: June 25, 2003
    Publication date: May 20, 2004
    Inventors: Clarence Nathaniel Ahlem, James Martin Frincke, Luis Daniel dos Anjos de Carvalho, William Heggie, Patrick T. Prendergast, Christopher L. Reading, Krupakar Paul Thadikonda, Russell Neil Vernon
  • Publication number: 20040044190
    Abstract: Compositions and methods are disclosed which facilitate purification of oligomers and other compounds. The disclosed compositions are silyl compositions that can be directly coupled, or coupled through a linking group, to a compound of interest, preferably to an oligomer at the end of oligomer synthesis. The silicon atom includes between one and three sidechains that function as capture tags. In one embodiment, the capture tags are lipophilic, which allows a derivatized oligomer to be separated from failure sequences by reverse phase chromatography. In another embodiment, the capture tags are compounds with a known affinity for other compounds, which other compounds are preferably associated with a solid support to allow chromatographic separation. Examples include haptens, antibodies, and ligands. Biotin, which can bind to or interact with a streptavidin-bound solid support, is a preferred capture tag of this type.
    Type: Application
    Filed: July 25, 2003
    Publication date: March 4, 2004
    Applicants: Sirna Therapeutics, Inc., Yale University
    Inventor: Brian S. Sproat
  • Patent number: 6689768
    Abstract: The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount of a chemically modified derivative of 17&agr;-estradiol, a chemically modified derivative of 17&bgr;-estradiol and/or a chemical modified derivative of estriol. Pharmaceutical preparations containing 14&agr;, 15&agr;-methylene-1,3,5(10),8-tetraene-3,17&agr;-diol are particularly preferred.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: February 10, 2004
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Mcihael Oettel, Ludwig Wildt, Peter Licht, Joachim Neuwinger, Wolfgang Hummel, Ralph Dittrich
  • Publication number: 20040010138
    Abstract: This invention relates to a process for the production of 7&agr;-methyl steroids of general formula I, 1
    Type: Application
    Filed: March 21, 2003
    Publication date: January 15, 2004
    Applicant: Schering AG
    Inventors: Marc Willuhn, Orlin Petrov, Evelin Amoulong-Kirstein, Stephan Vettel, Agnes Matzeit
  • Publication number: 20030212045
    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: Application
    Filed: May 13, 2003
    Publication date: November 13, 2003
    Inventors: Mark S. Cushman, O. M. Zack Howard
  • Publication number: 20030109728
    Abstract: The invention is a process for the preparation of a &Dgr;4,9-steroid of formula (II) 1
    Type: Application
    Filed: December 10, 2002
    Publication date: June 12, 2003
    Inventor: Rajappa Vaidyanathan
  • 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
  • Patent number: 6448419
    Abstract: Disclosed is a method of preparing 2-hydroxy-3,17&bgr;-estradiol derivatives wherein 3,17&bgr;-estradiol is reacted with an organolithium reagent and reacted with either a boron reagent or a silicon reagent to form either a 2-boronyl or a 2-silyl modified estradiol analog represented by the corresponding structural formulae: R1 and R2 are each independently a hydroxyl protecting group. R3, R4 and R5 are selected from the group consisting of halogens, alkyl, aryl, hydroxy, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: September 10, 2002
    Assignee: Tetrionics, Inc.
    Inventors: Herbert E. Paaren, Steven R. Duff
  • Patent number: 6436917
    Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: August 20, 2002
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Peter Droescher, Bernd Menzenbach, Wolfgang Roemer, Birgitt Schneider, Walter Elger, Guenter Kaufmann
  • Patent number: 6392068
    Abstract: The present invention relates to novel carborane cholesterol analogs and their use in the treatment of tumor and cancers in humans, and in particular to the treatment of human brain tumors. Pharmaceutical compositions and methods of using these compositions in the treatment of tumors and cancer are other aspects of the present invention.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: May 21, 2002
    Assignee: The University of Georgia Research Foundation, Inc.
    Inventors: Donghao Robert Lu, Bing Qing Ji
  • Publication number: 20020038004
    Abstract: A reagent having the general formula of General Formula I: 1
    Type: Application
    Filed: June 4, 2001
    Publication date: March 28, 2002
    Inventors: Mark L. Stolowitz, Guisheng Li, Jean P. Wiley
  • Patent number: 6262042
    Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: July 17, 2001
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Gary S. Bartley
  • Patent number: 5789607
    Abstract: A process for preparing 1,25-dihydroxy-16-ene-23-yne cholecalciferol.
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: August 4, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Masami Okabe
  • Patent number: 5728826
    Abstract: The invention describes a process for the epimer enrichment of compounds of formula (I) by silation, fractionated crystallization and acid hydrolysis.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: March 17, 1998
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Patent number: 5686435
    Abstract: 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: Grant
    Filed: December 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
  • Patent number: 5591733
    Abstract: 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: Grant
    Filed: August 2, 1993
    Date of Patent: January 7, 1997
    Assignee: University of Southern California
    Inventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
  • Patent number: 5508452
    Abstract: A process for the preparation of a compound of the formula ##STR1## in which rings A and B are a remainder: ##STR2## in which the 3-ketone function is optionally protected in the form of a ketal, thioketal, hemithioketal or enol ether, or a remainder: ##STR3## wherein R is methyl or --CH.sub.2 --OR', R' is hydrogen or ether remainder or ester remainder, R.sub.1 and R.sub.2 together form a second bond, or R.sub.1 and R.sub.2 form together an epoxide in beta position, or R.sub.1 is hydrogen, ketone or .alpha.- or .beta.- hydroxy, free or protected in the form of an ether or ester and R.sub.2 is hydrogen, or R.sub.1 is hydrogen and R.sub.2 is .alpha.-hydroxy function, or R.sub.1 is .beta.-hydroxy, free or protected in the form of an ether or ester and R.sub.2 is .alpha.-fluorine or bromine and R.sub.3 is hydrogen or .alpha. or .beta. fluorine or methyl comprising reacting a compound of the formula ##STR4## in which A, B, R, R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: April 16, 1996
    Assignee: Roussel Uclaf
    Inventors: Patrick Roussel, Michel Vivat
  • Patent number: 5494905
    Abstract: 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: Grant
    Filed: May 31, 1994
    Date of Patent: February 27, 1996
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert H. Hesse, Gaddam S. Reddy, Sundara K. S. Setty
  • Patent number: 5478955
    Abstract: The invention is drawn to cholesterol derivatives in which a cyclopentane ring has been introduced onto the 25-carbon of the side chain and to 24-epimers of these compounds. The compounds are useful intermediates in the production of 26,27-dimethylene-1.alpha.,25-dihydroxyvitamin D.sub.2 and 26,27-dimethylene-24-epi-1.alpha.,25-dihydroxyvitamin D.sub.2. These vitamin D derivatives are useful for the treatment of diseases such as osteoporosis.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: December 26, 1995
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Naoshi Nakagawa
  • Patent number: 5393900
    Abstract: The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche inc.
    Inventors: Thomas I. Doran, John A. McLane, Masami Okabe, Michelangelo Scalone, Milan R. Uskokovic
  • 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