Acyclic Carbon Bonded Directly At The 17 Beta-position Of The Cyclopentanohydrophenanthrene Ring System (e.g., Etiocholanic Acids, 17 Cyanoetiocholanes, 17-aldehydrostanes, Etc.) Patents (Class 552/610)
  • Patent number: 9670246
    Abstract: A process for preparing compounds of formula [II] by esterification of the C-17 hydroxyl group of 6?,9?-difluoro-11?,17?-dihydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioic acid, the compound of formula [I] comprises treating compound [I] with a slight excess of an acyl chloride of general formula R—COCl, where R represents —CH2CH3, —CH2CH2CH3 or —CH(CH3)2, in an inert solvent, in the presence of a tertiary amine. Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5° C. to ?20° C.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: June 6, 2017
    Assignee: Hovione Inter Ltd.
    Inventors: Luis Sobral, Dionisio Martin, William Heggie, Emilia Leitäo
  • Publication number: 20140322738
    Abstract: The present invention provides haloalkane substrates, and linkers for connecting such substrates to functional elements (e.g., tags, labels, surfaces, etc.). Substrates and linkers described herein find use, for example, in labeling, detection, and immobilization of proteins, cells, and molecules. In particular, the linkers provided herein find use within substrates for dehalogenase variants that form covalent bonds with their haloalkane substrates.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 30, 2014
    Applicant: PROMEGA CORPORATION
    Inventors: Carolyn W. Hitko, Thomas Kirkland, Sergiy Levin, Poncho Meisenheimer, Rachel Friedman Ohana, Harry Tetsuo Uyeda, Ji Zhu
  • Publication number: 20140287051
    Abstract: The present invention is directed to orally administered corticosteroid compositions. The present invention also provides a method for treating a condition associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: APTALIS PHARMATECH, INC.
    Inventors: Stephen PERRETT, Fredric Jay COHEN, Gopi VENKATESH
  • Patent number: 8841442
    Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: September 23, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Kirtipalsinh Solanki, Ruchir Z Bavadia, Dhaval P Patel, Dhaval J Patel, Tejash C Shah, Manoj Kumar Singh
  • Publication number: 20140275517
    Abstract: Methods and systems for the preparation of conditioned micronized active agents. Additionally, methods and systems for in-process conditioning of micronized active agent particles and compositions comprising conditioned micronized materials.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Pearl Therapeutics, Inc.
    Inventors: Ali Kazmi, David Lechuga, Herm Snyder, James Ivey, Reinhard Vehring, Jason H. Speck, Sarvajna Dwivedi
  • Patent number: 8785425
    Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 22, 2014
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Samir Rameshchandra Shah, Sanjay Nandlal Mandhane, Trinadha Rao Chitturi, Rajamannar Thennati
  • Publication number: 20140200341
    Abstract: Described herein are processes for the preparation of monofluoromethylated organic biologically active compounds, starting from protected intermediates and/or reagents to obtain compounds such as fluticasone propionate and fluticasone furoate, in presence of decarboxylating reagents XeF2 and BrF3, or using FCH2SH as a reagent.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 17, 2014
    Applicant: HOVIONE INTER LIMITED
    Inventors: Emilia Perpetua Tavares Leitao, Maria Rita Ventura, Christopher Maycock
  • Patent number: 8765725
    Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: July 1, 2014
    Assignee: Aciex Therapeutics, Inc.
    Inventors: Thomas Cavanagh, Shikha P. Barman
  • Publication number: 20140171645
    Abstract: The present invention provides electrophilic alkylating reagents of formula II, wherein is an aryl group, R2 is an alkyl group, R3 is a substituted phenyl group, wherein the number of substituents (n) is greater than 2 and R4 is an anion, and salts thereof, methods for their preparation and methods for the preparation of alkylated biologically active compounds using such reagents.
    Type: Application
    Filed: February 23, 2012
    Publication date: June 19, 2014
    Applicant: Hovione Inter Ltd.
    Inventor: Emilia Perpetua Tavares Leitao
  • Publication number: 20140148593
    Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.
    Type: Application
    Filed: September 2, 2011
    Publication date: May 29, 2014
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Kirtipalsinh Solanki, Ruchir Z Bavadia, Dhaval P Patel, Dhaval J Patel, Tejash C Shah, Manoj Kumar Singh
  • Publication number: 20140141247
    Abstract: The invention relates to a novel crystallisation process for preparing fluticasone propionate as crystalline form 1 polymorph with controlled particle size and suitable for micronisation.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: PFIZER LIMITED
    Inventors: Martyn David Ticehurst, Ivan Marziano, Eleftherios Kougoulos
  • Publication number: 20140046061
    Abstract: Chiral salts comprising anionic cyclodextrin derivatives with particular types of non-metal cations are provided. The anionic CD derivative salts can serve as ionic liquids and can possess substantial advantages over currently commercially available ionic liquids particularly for use as chiral phase transfer catalyst, chiral reaction medium, chiral extraction medium, and/or as chiral additive to a chemical process. Methods of preparing the same are provided.
    Type: Application
    Filed: June 28, 2013
    Publication date: February 13, 2014
    Inventor: Jose R. MATOS
  • Publication number: 20130345455
    Abstract: The invention provides and describes solid state 17?-ethynyl-5?-androstane-3?,17?-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-5?-androstane-3?,17?-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17?-ethynyl-5?-androstane-3?,17?-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-5?-androstane-3?,17?-diol and uses of such formulations in treating the described conditions.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 26, 2013
    Inventors: Steven K. White, Erin E. Jansen, Keith Lorimer, Brenton Skylar Wolfe
  • Patent number: 8586770
    Abstract: 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: Grant
    Filed: February 18, 2011
    Date of Patent: November 19, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20130303502
    Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
    Type: Application
    Filed: January 7, 2013
    Publication date: November 14, 2013
    Applicant: ACIEX THERAPEUTICS, INC.
    Inventors: Thomas Cavanagh, Shikha P. Barman
  • Publication number: 20130274460
    Abstract: The invention provides electrophilic monohalomethylating reagents, methods for their preparation and methods for preparation of monohalomethylated biologically active compounds using such reagents. Typical monohalomethyl groups transferred are FH2C—, CIH2C— and others. The reagents used for transferal of the groups are described by Formulae A-D: wherein: X?F, CI, Br, I, sulfonate esters, phosphate esters or another leaving group; R11=tetrafluoroborates, inflates, halogen, perchlorate, sulfates, phosphates or carbonates The other variables are as defined in the claims.
    Type: Application
    Filed: October 27, 2011
    Publication date: October 17, 2013
    Applicant: HOVIONE INTER LIMITED
    Inventor: Emilia Perpetua Tavares Leitao
  • Publication number: 20130225844
    Abstract: Described is a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.
    Type: Application
    Filed: June 1, 2011
    Publication date: August 29, 2013
    Applicant: Hovione Inter Ltd
    Inventor: Emilia Perpetua Tavares Leitao
  • Publication number: 20130203717
    Abstract: A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.
    Type: Application
    Filed: April 21, 2011
    Publication date: August 8, 2013
    Applicant: HOVIONE INTER LTD
    Inventors: Marco Gil, Constanca Cacela, Ricardo Mendonca, Filipe Gaspar
  • Patent number: 8492570
    Abstract: The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.
    Type: Grant
    Filed: September 22, 2008
    Date of Patent: July 23, 2013
    Assignee: Sterix Limited
    Inventors: Alexander Hillisch, Olaf Peters, Christian Gege, Wilko Regenhardt, Dirk Kosemund, Gerhard Siemeister, Eberhard Unger, Ulrich Bothe
  • Publication number: 20130172587
    Abstract: The present invention relates to a process for the preparation of steroidal 17?-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17?-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 4, 2013
    Applicant: Generics [UK] Limited
    Inventor: Generics [UK] Limited
  • Publication number: 20130072698
    Abstract: Described are processes for the preparation of monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such as XeF2 and BrF3.
    Type: Application
    Filed: June 1, 2011
    Publication date: March 21, 2013
    Applicant: HOVIONE INTER LTD
    Inventors: Emilia Perpetua Tavares Leitao, William Heggie
  • Patent number: 8344168
    Abstract: The present invention relates to a process for the preparation of steroidal 17?-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17?-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.
    Type: Grant
    Filed: December 8, 2008
    Date of Patent: January 1, 2013
    Assignee: Generics (UK) Limited
    Inventors: Vinayak G. Gore, Mahesh Gadakar, K. Pokharkar, V. Wakchure
  • Publication number: 20120157421
    Abstract: The invention relates to 17?-alkyl-17?-oxy-oestratrienes of the formula (I), to processes for their preparation, to the use of the 17?-alkyl-17?-oxy-oestratrienes for preparing pharmaceuticals and to pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: May 26, 2010
    Publication date: June 21, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Rolf Bohlmann, Nikolaus Heinrich, Jan Hübner, Georg Kettschau, Hermann Künzer, Philip Lienau, Michael Gerisch, Silke Köhr, Dieter Lang, Karsten Denner, Michael Sander, Jens Hoffmann, Tim Wintermantel
  • Patent number: 8183402
    Abstract: The present invention relates to a process for the synthesis of the 17-acetoxy-11?-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II):
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: May 22, 2012
    Assignee: Richter Gedeon Nyrt.
    Inventors: József Bódi, György Visky, János Széles, Sándor Mahó, Csaba Sánta, János Csörgei, Zoltán Tuba, László Terdy, Csaba Molnár, Antal Aranyi, Zoltán Horváth, Gábor Balogh
  • Patent number: 8148353
    Abstract: Provided are polymorphs of fluticasone furoate and processes for preparation thereof.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: April 3, 2012
    Assignee: Plus Chemicals SA
    Inventors: Peter Lindsay MacDonald, Pierluigi Rossetto, Adrienne Kovacsne-Mezei, Roman Gabriel, Alexandr Jegorov, Jiri Faustmann
  • Publication number: 20120046258
    Abstract: There are provided crystalline particles of unsolvated Form 1 polymorph of the compound of formula (I): characterised in that the particles are in the form of substantially triangular plates.
    Type: Application
    Filed: November 1, 2011
    Publication date: February 23, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Wendy Isabel Cross, Matthew Lawrence Hannan, David Michael Johns, Mei-yin Lee, Christopher John Price
  • Publication number: 20120040945
    Abstract: Methods, devices and compositions for treatment of severe and uncontrolled asthma are provided by which high amounts of an inhaled corticosteroid are directed to the small airways of the lower lungs. The invention provides for a substantial decrease in the dose of concurrently administered oral corticosteroids. A particular advantage of the invention is the significant reduction in corticosteroid-related adverse effects.
    Type: Application
    Filed: February 3, 2010
    Publication date: February 16, 2012
    Applicant: ACTIVAERO GMBH RESEARCH & DEVELOPMENT
    Inventors: Bernard Muellinger, Thomas Hofmann, Gerhard Scheuch, Philipp Kroneberg
  • Publication number: 20110257142
    Abstract: The present invention relates to a method for the reliable and reproducible preparation of 4-[17?-methoxy-17?-methoxymethyl-3-oxoestra-4,9-dien-11?-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
    Type: Application
    Filed: January 10, 2011
    Publication date: October 20, 2011
    Inventors: Detlef Grawe, Sabine Gliesing, Hagen Gerecke, Peter Hoesel, Uwe Mueller, Thomas Michel, Robert Eilers, Uwe Knabe, Bernd Erhart, Michael Mosebach, David Voigtlaender, Ulf Tilstam, Jürgen Jacke, Klaus Bahl, Ulf Bohlmann, Dieter Wehmeier, Michael Sander
  • Patent number: 8012952
    Abstract: The present invention provides a novel series of cationic, lipid-based, 17?-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17?-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
    Type: Grant
    Filed: December 31, 2007
    Date of Patent: September 6, 2011
    Assignee: Council of Scientific & Industrial Research
    Inventors: Surendar Reddy Bathula, Rajkumar Banerjee
  • Publication number: 20110146678
    Abstract: This invention provides a process for increasing the crystallinity of at least one solid material which is less than 100% crystalline, comprising contacting said solid material with solvent in which the solid material is insoluble or poorly soluble (a non-solvent); and applying ultrasound to the solid material when in contact with said non-solvent.
    Type: Application
    Filed: July 20, 2009
    Publication date: June 23, 2011
    Inventors: Graham Ruecroft, Dipesh Parikh
  • Publication number: 20110144071
    Abstract: A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.
    Type: Application
    Filed: June 30, 2009
    Publication date: June 16, 2011
    Applicant: JESALIS PHARMA GMBH
    Inventors: Detlef Grawe, Sabine Gliesing, Robert Eilers
  • Patent number: 7935837
    Abstract: A process for synthesis of androstane 17-? carbothioic acid is provided. The process includes mixing an androstane 17-? carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-? carbothioic acid, wherein the androstane 17-? carbothioic acid has the formula (I): wherein R1 represents hydrogen or haloalkyl groups, R2 represents C1-8 linear alkyl groups, C1-8 branched alkyl groups, C1-6 unsaturated acyclic groups or aromatic groups, R3 represents hydrogen or hydroxyl, R4 represents hydrogen, bromine, chlorine or fluorine and R5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: May 3, 2011
    Assignee: Corum Inc.
    Inventors: Nai-Hsuan Hsu, Chu-Yi Pang, Chien-Jen Wu, Chi-Jen Huang, Chia-Jung Hsu, Peimin Lee
  • Publication number: 20110081411
    Abstract: The present invention is directed to orally administered corticosteroid compositions. The present invention also provides a method for treating a condition associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Inventors: Stephen Perrett, Fredric Jay Cohen, Gopi Venkatesh
  • Patent number: 7893284
    Abstract: The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: February 22, 2011
    Assignee: Sterix Limited
    Inventors: Matthew Leese, Atul Purohit, Michael John Reed, Simon Paul Newman, Surinder Kuman Chander, Fabrice Jourdan, Barry Victor Lloyd Potter
  • Publication number: 20100303758
    Abstract: This invention relates to novel glucocorticoid receptor agonists of formula (I): and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
    Type: Application
    Filed: May 26, 2010
    Publication date: December 2, 2010
    Inventors: Paul Alan Glossop, David Simon Millan, David Anthony Price
  • Publication number: 20100261917
    Abstract: There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is characterized by irradiating a compound represented by the formula: with UV to ring-open the compound, and then isomerizing the resulting compound; an intermediate useful for carrying out the process; and a process for producing the intermediate.
    Type: Application
    Filed: November 30, 2006
    Publication date: October 14, 2010
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Akira Kawase, Yasuharu Kato, Kazutomo Kinoshita, Yasushi Kitoh, Takuma Ikeda, Tsuyoshi Haneishi, Noriaki Maruyama, Mio Kobayashi
  • Publication number: 20100255117
    Abstract: The instant invention provides methods and compositions for the treatment of cancer.
    Type: Application
    Filed: April 6, 2008
    Publication date: October 7, 2010
    Applicant: The Johns Hopkins University
    Inventors: Shyam Biswal, Anju Singh, Deepti Malhotra
  • Publication number: 20100137622
    Abstract: The present invention relates to a process for the synthesis of the known 17-acetoxy-11-?-[4-(dimethyl amino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-ethandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones.
    Type: Application
    Filed: June 19, 2008
    Publication date: June 3, 2010
    Inventors: József Bódi, György Visky, János Széles, Sándor Mahó, Csaba Sánta, János Csörgei, Zoltán Tuba, László Terdy, Csaba Molnár, Antal Aranyi, Zoltán Horváth, Gábor Balogh
  • Publication number: 20100130458
    Abstract: Provided are polymorphs of fluticasone furoate and processes for preparation thereof.
    Type: Application
    Filed: August 6, 2009
    Publication date: May 27, 2010
    Inventors: Peter Lindsay Macdonald, Pierluigi Rossetto, Adrienne Kovacsne-Mezei, Roman Gabriel, Alexandr Jegorov, Jiri Faustmann
  • Publication number: 20100099654
    Abstract: The present invention relates to certain unsaturated fatty acid derivatives of therapeutically active glucocorticoides-fatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents and pharmaceutical formulations containing them.
    Type: Application
    Filed: March 13, 2008
    Publication date: April 22, 2010
    Applicant: CLAVIS PHARMA ASA
    Inventors: Myhren Finn, Marit Liland Sandvold, Ole Henrik Eriksen, Steinar Hagen
  • Patent number: 7638508
    Abstract: A compound of formula (I): wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the ? or ? configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and ?represents a single or a double bond; or a physiologically acceptable salt or solvate thereof, and pharmaceutical formulations and methods of use thereof.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: December 29, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Deborah Needham
  • Patent number: 7629334
    Abstract: The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred herein.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: December 8, 2009
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Kristof Chwalisz, Walter Elger, Gerd Schubert
  • Patent number: 7579335
    Abstract: The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydrogen, a methyl group, which may be in either the ? or ? configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; represents a single or a double bond; and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.
    Type: Grant
    Filed: January 9, 2006
    Date of Patent: August 25, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Deborah Needham
  • Publication number: 20090181936
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Application
    Filed: March 17, 2009
    Publication date: July 16, 2009
    Applicant: Hollis-Eden Pharmaceuticals, Inc.
    Inventors: Henry A. Lardy, Ashok Marwah, Padma Marwah
  • Publication number: 20090163458
    Abstract: The present disclosure relates generally to methods and compositions for treating symptoms of Parkinson's disease and/or other movement disorders. More particularly, the present disclosure describes a method for treating symptoms of Parkinson's disease and related disorders by administering a composition comprising one or more of the following active agents; estradiol, estriol, testosterone, and 19-nortestosterone. In addition, the compositions of the present invention can be used for enhancing or optimizing the effectiveness of neural stimulation in treating the symptoms of movement disorders such as Parkinson's disease.
    Type: Application
    Filed: November 6, 2008
    Publication date: June 25, 2009
    Inventor: Ellis L Kline
  • Publication number: 20090118495
    Abstract: A novel process for preparing a compound of formula (I) which comprises converting a compound of formula (II) to a compound of formula (I) via a compound of formula (III), or a salt thereof, without isolating any intermediates.
    Type: Application
    Filed: June 13, 2007
    Publication date: May 7, 2009
    Applicant: GLAXO GROUP LIMITED
    Inventors: Malcolm Brian Berry, Mark Jason Hughes, David Parry-Jones, Stephen John Skittrall
  • Publication number: 20090062230
    Abstract: The present invention provides a novel series of cationic, lipid-based, 17?-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17?-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), Hela (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
    Type: Application
    Filed: December 31, 2007
    Publication date: March 5, 2009
    Inventors: Surendar Reddy Bathula, Rajkumar Banerjee
  • Patent number: 7498321
    Abstract: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: March 3, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Paul Jones, Jeremy John Payne
  • Publication number: 20090054387
    Abstract: The present invention relates to a method for the reliable and reproducible preparation of 4-[17?-methoxy-17?-methoxymethyl-3-oxoestra-4,9-dien-11?-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).
    Type: Application
    Filed: April 17, 2007
    Publication date: February 26, 2009
    Inventors: Detlef Grawe, Sabine Gliesing, Hagen Gerecke, Peter Heesel, Uwe Mueller, Thomas Michel, Robert Eilers
  • Publication number: 20090054388
    Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:
    Type: Application
    Filed: July 25, 2008
    Publication date: February 26, 2009
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Samir Rameshchandra Shah, Sanjay Nandlal Mandhane, Trinadha Rao Chitturi, Rajamannar Thennati