Nitrogen Containing Hetero Ring Patents (Class 514/176)
  • Patent number: 8030298
    Abstract: The present invention relates to novel substituted steroid derivatives which represent selective inhibitors of the 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17?-estradiol concentration.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: October 4, 2011
    Assignee: Abbott Products GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
  • Patent number: 8022203
    Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: September 20, 2011
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
  • Publication number: 20110212934
    Abstract: Formulations for topical or local administration of drugs directly to the breast or chest to produce a regional or local effect with lower systemic drug levels than when an effective amount is administered systemically are disclosed herein. In a preferred embodiment, the drug is administered to the surface of the breast, areola, or directly to the nipple. The formulations provide increased patient comfort, increased bioavailability and relatively high blood levels in the region to be treated with a reduction of side effects compared to those administered systemically. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion or foam.
    Type: Application
    Filed: August 30, 2010
    Publication date: September 1, 2011
    Inventors: Gerianne Tringali DiPiano, Peter Kevin Mays, John Ziemniak
  • Publication number: 20110212935
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Application
    Filed: April 27, 2011
    Publication date: September 1, 2011
    Applicant: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 8003783
    Abstract: There is provided a compound of Formula (III) wherein R1 is a selected from an alkyloxyalkyl group, a nitrile group, alkylaryl group, alkenylaryl group, alkylheteroaryl group, alkenylheteroaryl group, ?N—O—alkyl or ?N—O—H group, branched alkenyl, alkyl-alcohol group, amide or alkylamide or —CHO so that R1 together with R3 provide the enol tautomer or R1 together with R3 form a pyrazole, wherein (a) R4 is ?N—O-alkyl or ?N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2-position is substituted with a group selected from —OH and —O-hydrocarbyl or a heteroaryl ring; R2 is selected from —OH and a sulphamate group; and R3 is selected from —OH or ?O; wherein the ring system may be further substituted with one or more hydroxyl, alkyl, alkoxy, alkinyl or halo substituents.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: August 23, 2011
    Assignee: Sterix Limited
    Inventors: Nigel Vicker, Harshani Rithma Ruchiranani Lawrence, Gillian Margaret Allan, Christian Bubert, Delphine Sophie Marion Fischer, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20110201580
    Abstract: The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 18, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora GHIDINI, Andrea RIZZI, Andrea VIRDIS, Fabio RANCATI, Anna RENCUROSI
  • Patent number: 7998935
    Abstract: The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity.
    Type: Grant
    Filed: January 8, 2007
    Date of Patent: August 16, 2011
    Assignee: Council of Scientific and Industrial Research
    Inventors: Danaboyina Ramaiah, Jyothish Kuthanapillil, Kalliat Thazhathveetil Arun
  • Publication number: 20110190246
    Abstract: The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.
    Type: Application
    Filed: July 14, 2009
    Publication date: August 4, 2011
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Thorsten Blume, Dieter Heldmann, Norbert Schmees, Christiane Otto, Tim Wintermantel, Joachim Kuhnke
  • Publication number: 20110182828
    Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
    Type: Application
    Filed: December 18, 2008
    Publication date: July 28, 2011
    Applicant: Schering Corporation
    Inventors: John C. Anthes, Kevin D. Mccormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Phillippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
  • Publication number: 20110171306
    Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.
    Type: Application
    Filed: March 25, 2011
    Publication date: July 14, 2011
    Inventor: David Bar-Or
  • Publication number: 20110171307
    Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.
    Type: Application
    Filed: March 25, 2011
    Publication date: July 14, 2011
    Inventor: DAVID BAR-OR
  • Publication number: 20110165225
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: May 26, 2009
    Publication date: July 7, 2011
    Inventors: Peter Cullis, Marcel Bally
  • Publication number: 20110160170
    Abstract: The present invention provides methods of inducing cell cycle arrest and/or cell growth inhibition, with the methods comprising administering to the cells an effective dose of the compounds of the present invention.
    Type: Application
    Filed: April 14, 2009
    Publication date: June 30, 2011
    Inventors: Vincent C. Njar, Angela Brodie, Robert Bruno
  • Publication number: 20110152212
    Abstract: A method of preparing an aqueous formulation of an active material and such a formulation per se are described, wherein the active material has a very low solubility in water. The method may involve contacting active material in solid form with an optionally cross-linked water soluble polymer. The water soluble polymer is preferably a polyvinyl polymer with polyvinylalcohol being preferred. The polymer is optionally cross-linked. The method and formulation may be of particular utility in delivery of anti-cancer drugs or drugs via a pulmonary route.
    Type: Application
    Filed: February 22, 2008
    Publication date: June 23, 2011
    Inventors: Nicholas John Crowther, Donald Eagland
  • Publication number: 20110144074
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: January 24, 2011
    Publication date: June 16, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20110144069
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
    Type: Application
    Filed: October 16, 2007
    Publication date: June 16, 2011
    Applicant: Myriad Genetics, Incorporated
    Inventors: Kraig M. Yager, Esther Arranz Plaza, Dange Vijay Kumar, In Chul Kim
  • Publication number: 20110144016
    Abstract: Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17?-hydroxylase/C17,20-lyase inhibitor, such as abiraterone acetate (i.e., 3?-acetoxy-17-(3-pyridyl) androsta-5,16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17?-hydroxylase/C17,20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.
    Type: Application
    Filed: February 24, 2011
    Publication date: June 16, 2011
    Inventors: Alan H. Auerbach, Arie S. Belldegrum
  • Publication number: 20110144075
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 16, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 7960367
    Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: June 14, 2011
    Assignee: Umecrine AB
    Inventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
  • Publication number: 20110123619
    Abstract: A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.
    Type: Application
    Filed: February 4, 2011
    Publication date: May 26, 2011
    Applicant: OZPHARMA PTY. LTD.
    Inventors: Ernest Alan Hewitt, Richard James Stenlake
  • Patent number: 7947668
    Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
    Type: Grant
    Filed: April 18, 2003
    Date of Patent: May 24, 2011
    Assignee: Institut National de la Sante et de la Recherche Medicale
    Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
  • Publication number: 20110118219
    Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles(azabenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable prodrug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.
    Type: Application
    Filed: March 19, 2009
    Publication date: May 19, 2011
    Applicant: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Vincent C.O. Njar, Angela M.H. Brodie, Lalji K. Gediya
  • Publication number: 20110118226
    Abstract: The present invention relates to transdermal danazol-containing pharmaceutical compositions, such as gels, and to methods of making and using the same.
    Type: Application
    Filed: July 24, 2009
    Publication date: May 19, 2011
    Inventor: Valerie Masini-Eteve
  • Publication number: 20110118225
    Abstract: The invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.
    Type: Application
    Filed: May 5, 2009
    Publication date: May 19, 2011
    Inventors: Petr Novak, David Sedlak, Petr Bartunek, Martin Kotora
  • Publication number: 20110105445
    Abstract: Provided are methods of inhibiting CYP17 in a mammal, such as a human, that include administering an effective amount of at least one CYP17 inhibitor, such as VN/124-1, VN/125-1, VN/85-1, VN/87-1 and/or VN/108-1 to the mammal. Also provided are methods of down regulating androgen receptor (AR) protein expression and methods of antagonizing AR in a mammal that include administering to the mammal an effective amount of at least one active ingredient selected from VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Also provided are methods of treating prostate cancer and methods of suppressing or preventing prostate tumor growth by administering such compounds to a mammal.
    Type: Application
    Filed: March 12, 2009
    Publication date: May 5, 2011
    Applicant: University of Maryland, Baltimore
    Inventors: Vincent C.O. Njar, Angela Brodie
  • Publication number: 20110098631
    Abstract: The present invention relates to implantable or insertable medical devices that treat uterine and urological conditions that cause chronic pelvic pain and other symptoms. In another aspect, the present invention relates to methods of manufacturing such implantable or insertable medical devices.
    Type: Application
    Filed: December 21, 2010
    Publication date: April 28, 2011
    Applicant: BOSTON SCIENTIFIC SCIMED, INC.
    Inventors: Jon T. McIntyre, Kenneth Daignault
  • Publication number: 20110077228
    Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: July 3, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Marc Courchesne, Lilliane Halab, Nathalie Chauret, Laval Chan Chun Kong
  • Publication number: 20110077227
    Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: July 3, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Liliane Halab, Nathalie Turcotte, Monica Bubenik, Marc Courchesne, Carl Poisson, Oswy Z. Pereira, Paul Nguyen-Ba, Bingcan Liu, Nathalie Chauret, Caroline Cadilhac, Laval Chan Chun Kong
  • Patent number: 7910571
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: March 22, 2011
    Assignee: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20110065678
    Abstract: Novel glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds.
    Type: Application
    Filed: September 9, 2010
    Publication date: March 17, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Eleonora Ghidini, IIaria Peretto, Andrea Virdis
  • Publication number: 20110059175
    Abstract: The present invention relates generally to use of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR, in the formulation of solid dispersions of low aqueous solubility and dissolution rate bioactive compound and, more particularly to a system and method for improving the solubility and dissolution rate of such low aqueous solubility and dissolution rate bioactive compound, in particular the drug of low aqueous solubility, such as a BCS Class II or Class IV drug compounds.
    Type: Application
    Filed: April 10, 2007
    Publication date: March 10, 2011
    Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENT
    Inventors: Sandrien Janssens, Guy Van Den Mooter
  • Publication number: 20110046599
    Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.
    Type: Application
    Filed: June 26, 2008
    Publication date: February 24, 2011
    Inventor: Agis Kydonieus
  • Patent number: 7893072
    Abstract: Compounds of the disclosure provide compositions, which are effective for prophylaxis and treatment of diseases or disorders, such as cell-proliferation, angiogenesis, or apoptosis mediated diseases. The disclosure encompasses compounds, analogs, prodrugs, metabolites, and pharmaceutically acceptable salts thereof, pharmaceutical compositions, and methods for prophylaxis and treatment of diseases and other maladies or conditions involving cancer, tumors, and like conditions. The disclosure also provides therapeutic methods including the administration of an effective amount of a compound of the disclosure.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: February 22, 2011
    Assignee: Genentech, Inc.
    Inventors: Mark Reynolds, Paul Polakis
  • Patent number: 7888340
    Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: February 15, 2011
    Assignee: Umecrine AB
    Inventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
  • Publication number: 20110034428
    Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. The present invention provides therapies and therapeutic regimens for the treatment of prostate cancer.
    Type: Application
    Filed: August 5, 2010
    Publication date: February 10, 2011
    Applicant: TOKAI PHARMACEUTICALS, INC.
    Inventors: Jodie Pope Morrison, Cy Aaron Stein, David Scott Casebier
  • Publication number: 20110021480
    Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.
    Type: Application
    Filed: September 28, 2010
    Publication date: January 27, 2011
    Applicant: Solvay Pharmaceuticals GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
  • Patent number: 7875599
    Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: January 25, 2011
    Assignee: University of Maryland
    Inventors: Angela Brodie, Vincent Njar
  • Publication number: 20100330148
    Abstract: Described herein are methods of inhibiting IMPDH type 1, and treating or preventing a disease or disorder (or symptoms thereof) associated with IMPDH type 1, wherein an IMPDH type 1 inhibitor compound is administered to a subject.
    Type: Application
    Filed: March 20, 2007
    Publication date: December 30, 2010
    Applicant: The Johns Hopkins University
    Inventors: Jun O. Liu, Curtis Robert Chong, David J. Sullivan
  • Publication number: 20100324005
    Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.
    Type: Application
    Filed: June 22, 2010
    Publication date: December 23, 2010
    Applicant: DMI ACQUISITION CORP.
    Inventor: David Bar-Or
  • Publication number: 20100324003
    Abstract: New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Application
    Filed: September 18, 2008
    Publication date: December 23, 2010
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Giorgio Fedrizzi, Patrizia Ferrari, Mauro Gobbini, Giuseppe Marazzi, Marco Torri, Walter Cabri
  • Publication number: 20100322997
    Abstract: A method of separating biologically ingestible microparticles is used to obtain biologically ingestible microparticles in a thin film fluid formed between two processing surfaces provided with a solution containing a first solvent in which an objective substance to be pulverized is dissolved and a solvent capable of serving as a second solvent in which the solubility of the microparticles is lower than in the first solvent, the two processing surfaces being arranged so as to be able to approach to and separate from each other, at least one of which rotates relative to the other.
    Type: Application
    Filed: July 4, 2008
    Publication date: December 23, 2010
    Applicant: M. Technique Co., Ltd.
    Inventor: Masakazu Enomura
  • Publication number: 20100324004
    Abstract: This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
    Type: Application
    Filed: September 8, 2008
    Publication date: December 23, 2010
    Inventors: Michael McLane, Inez Ruiz-White, Henry Wolfe
  • Publication number: 20100303896
    Abstract: Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of obstructive vascular lesions following vascular surgery and for the prevention and/or treatment of diseases due to organ fibrosis.
    Type: Application
    Filed: June 4, 2008
    Publication date: December 2, 2010
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Liberato Berrino, Antonio Cascino, Marilena Cipollaro, Amalia Forte, Francesco Rossi, Giuseppe Bianchi, Patrizia Ferrari
  • Patent number: 7838515
    Abstract: Muscle relaxant formulations which include one or more quaternary ammonium neuromuscular blocking agents have a reduced tendency for hydrolytic degradation, and therefore a longer shelf life stability, when combined with one or more organic anions having at least six carbon atoms and having a pKa of less than 4.0 (preferably ranging from 0.5 to 3.5). Particularly good results are achieved when using acids of very low solubility in water, such as gentisic acid which is less than 1% soluble at room temperature.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: November 23, 2010
    Assignee: Lyotropic Therapeutics, Inc.
    Inventor: David M. Anderson
  • Publication number: 20100292198
    Abstract: A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.
    Type: Application
    Filed: May 3, 2010
    Publication date: November 18, 2010
    Applicant: Wyeth LLC
    Inventors: GARY SONDERMANN GRUBB, GINGER DALE CONSTANTINE
  • Publication number: 20100292150
    Abstract: The present invention provides a method for treating menorrhagia in a premenopausal woman, which includes administering to the woman in need thereof a pharmaceutically effective amount of an aromatase inhibitor. Also within the scope of this invention is a pharmaceutical composition for the treatment.
    Type: Application
    Filed: December 10, 2008
    Publication date: November 18, 2010
    Applicant: MEDITRINA PHARMACEUTICALS, INC.
    Inventor: James Symons
  • Publication number: 20100284913
    Abstract: Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.
    Type: Application
    Filed: May 7, 2010
    Publication date: November 11, 2010
    Applicant: The Board of Trustees of the Leland Stanford Junio
    Inventors: Justin Du Bois, John Mulcahy, Brian Andresen, David C. Yeomans, Sandip Biswal
  • Publication number: 20100256105
    Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: March 30, 2010
    Publication date: October 7, 2010
    Inventors: Frank Burkamp, Peter Hansen
  • Publication number: 20100256103
    Abstract: The present invention provides named compounds of formula (I) and pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: March 30, 2010
    Publication date: October 7, 2010
    Applicant: ASTRAZENECA R&D
    Inventors: Frank Burkamp, Peter Hansen, Balint Gabos, Håkan Bladh
  • Publication number: 20100256104
    Abstract: The present invention provides compounds of formula (I) wherein n, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: March 30, 2010
    Publication date: October 7, 2010
    Applicant: ASTRAZENECA R&D
    Inventors: Frank Burkamp, Balint Gabos, Svetlana Ivanova, Alice Ingrid Annea Lisius