Unsaturation Between The 5- And 6-positions (e.g., Pregnenolones, Etc.) Patents (Class 552/606)
  • Publication number: 20140200200
    Abstract: The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.
    Type: Application
    Filed: May 18, 2012
    Publication date: July 17, 2014
    Applicants: UNIVERSITE DE BORDEAUX I, INSERM (Institut National de la Sante et de la Recherche Medicale), UNIV DE BORDEAUX II VICTOR SEGALEN
    Inventors: Pier Vincenzo Piazza, Monique Vallee, Giovanni Marsicano, Francois-Xavier Felpin, Luigi Bellocchio, Daniela Cota, Jean-Michel Revest, Sergio Vitiello, Umberto Spampinato, Rafael Maldonado
  • 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: 20130245253
    Abstract: The present disclosure provides modified neuroactive steroids. The modified neuroactive steroids may comprise, consist of, or consist essentially of a therapeutic agent and/or a modifying moiety. The modified neuroactive steroid can have modified characteristics as compared to native neuroactive steroids that do not include a modifying moiety and/or therapeutic agent. The modified neuroactive steroid may be, for example, modified pregnenolone, pregnenolone metabolites, allopregnanolone, and/or allopregnanolone metabolites. The modified neuroactive steroids can be used to treat, prevent and/or ameliorating a phenotypic state of interest in a subject.
    Type: Application
    Filed: March 28, 2011
    Publication date: September 19, 2013
    Inventors: Christine Marx, Robert Mook
  • 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
    Inventors: Mark A. Findeis, Steffen P. Creaser
  • Publication number: 20120141788
    Abstract: The present invention relates a process for the precipitation of an organic compound, wherein: (a) a solution (I) of the organic compound in a first solvent is introduced via a first inlet into a closed type mixing chamber; (b) a precipitation agent (II) is introduced, simultaneously with step (a), via a second inlet into the closed type of mixing chamber; (c) the solution (I) of the organic compound and the precipitating agent (II) are mixed thereby forming a precipitate of the organic compound and a liquid phase; and (d) discharging the precipitate of the organic compound and the liquid phase via a single outlet from the closed type mixing chamber.
    Type: Application
    Filed: September 19, 2007
    Publication date: June 7, 2012
    Inventor: Huibert Albertus Van Boxtel
  • Publication number: 20100034781
    Abstract: This invention relates, for example, to synthetic oxysterols. Also described are methods for using the compounds, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.
    Type: Application
    Filed: February 27, 2007
    Publication date: February 11, 2010
    Applicant: The Regents of the University of California
    Inventors: Farhad Parhami, Michael E. Jung, Jennifer R. Dwyer, Khanhlinh Nguyen
  • Patent number: 7495115
    Abstract: Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and haematological malignancies. Further the conjugates exhibits a synergistic action together with a cytoskeleton acting drug such as Taxol®, which enable the treatment of cancers that otherwise would be non responsive to Taxol®.
    Type: Grant
    Filed: July 14, 2003
    Date of Patent: February 24, 2009
    Assignee: Bionature E.A., Ltd.
    Inventor: Elias Castanas
  • Publication number: 20020019548
    Abstract: The invention related to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-4,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17(20)-dien-3-one, 20&xgr;-fluoropregna-4,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Application
    Filed: June 21, 2001
    Publication date: February 14, 2002
    Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
  • Patent number: 6310225
    Abstract: Steroid derivatives useful as intermediates for producing vitamin D derivates as well as processes for producing the steroid derivatives are provided. The steroid derivatives include halide compounds represented by the following formulae: wherein X, R1 and R2 are as defined by the specification.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: October 30, 2001
    Assignee: Kuraray Co., Ltd.
    Inventors: Yoshihisa Tsuji, Toshimichi Mitani
  • Patent number: 6160139
    Abstract: The invention relates to a process for the production of 16-dehydropregnenolone acetate of the formula ##STR1## comprising the oxidation of pseudodiosgenin diacetate in the presence of a phase transfer catalyst at a temperature between 0-15.degree. C. to produce diosone followed by the hydrolysis and degradation of diosone to produce 16-dehydropregnenolone acetate.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: December 12, 2000
    Assignee: Council of Scientific & Industrial Research
    Inventors: Amrit Goswami, Rumi Kataky, Ramesh Chandra Rastogi, Anil C. Ghosh
  • Patent number: 5994333
    Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
    Type: Grant
    Filed: August 3, 1995
    Date of Patent: November 30, 1999
    Assignee: Pherin Corporation
    Inventors: Clive L. Jennings-White, David L. Berliner, Nathan William Adams
  • Patent number: 5827842
    Abstract: The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are, in contrast with the disclaimed compound 14,17-ethano-19-norpregn-4-ene-3,20-dione bioavailable even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.
    Type: Grant
    Filed: December 26, 1995
    Date of Patent: October 27, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Schollkopf, Wolfgang Halfbrodt, Joachim Kuhnke, Wolfgang Schwede, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
  • Patent number: 5808117
    Abstract: The invention relates to a process for producing 16-Dehydropregnenolone acetate (16DPA) of the formula shown below ##STR1## which process comprises a) acetolysis of diosgenin of the formula shown below ##STR2## by heating in a pressure reactor in the presence of an acetylating agent and a non-polar solvent, maintaining the pressure in the reactor in the range of 4-6 kg/cm.sup.2 and at a temperature in the range of 200.degree.-250.degree. C. to produce pseudodiosgenine acetate of the formula shown below ##STR3## b) Oxidizing the so obtained pseudodiosgenin acetate to obtain diosone of the formula shown below ##STR4## and, c) Hydrolysis and degradation of the diosone so obtained to produce the said 16-Dehydropregnenolone acetate.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: September 15, 1998
    Inventors: Pritish Kumar Chowdhury, Manobjyoti Bordoloi, Nabin Chandra Baraua, Heramba Prasad Sarmah, Pradip Kumar Goswami, Ram Prakash Saharma, Ajoy Pratap Baruah, Raj Kumar Mathur, Anil Chandra Ghosh
  • Patent number: 5792759
    Abstract: Novel 17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl steroids of the general formula (I) ##STR1## where A, R.sup.1 and R.sup.2 are defined in the specification are disclosed. The compounds have cardiovascular activity. Pharmaceutical compositions containing compounds of formula (I) are also disclosed for the treatment of heart failure and hypertension.
    Type: Grant
    Filed: May 17, 1996
    Date of Patent: August 11, 1998
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Luisa Quadri, Alberto Cerri, Patrizia Ferrari, Maria Pia Zappavigna
  • Patent number: 5561124
    Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: October 1, 1996
    Inventor: Robert L. Webb
  • Patent number: 5496813
    Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Marigen S.A.
    Inventors: Carl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
  • Patent number: 5352808
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Michel Vivat
  • Patent number: 5032586
    Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: July 16, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Brian W. Metcalf, Dennis A. Holt, Mark A. Levy