The Cyclopentanohydrophenanthrene Ring System Is Fully Saturated (e.g., Pregnandiols, Pregnanolones, Etc.) Patents (Class 552/609)
  • Patent number: 10160783
    Abstract: The present disclosure is generally directed to neuroactive 13, 17-substituted steroids 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: October 25, 2016
    Date of Patent: December 25, 2018
    Assignee: Washington University
    Inventors: Douglas Covey, Xin Jiang
  • Patent number: 9512170
    Abstract: The present disclosure is generally directed to neuroactive 13,17-substituted steroids 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 27, 2014
    Date of Patent: December 6, 2016
    Assignee: Washington University
    Inventors: Douglas Covey, Xin Jiang
  • Publication number: 20140235600
    Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids 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: Application
    Filed: December 18, 2013
    Publication date: August 21, 2014
    Applicant: Washington University
    Inventors: Douglas Covey, Albert Jean Robichaud
  • Publication number: 20140058079
    Abstract: The présent invention relates to novel neurosteroids, especially derivatives of allopregnanolone and of epiallopregnanolone of formula (I) and the uses thereof as médicament for the treatment of neuropathologies, in particular neuropathies induced by the chemotherapy of a cancer. Thèse molécules according to the invention have both preventative and curative effects. The neurosteroids according to the invention may also be of use in the treatment of neurodegenerative disorders, in particular for preventing neuronal cell death. They may thus be used as neuroprotectants and/or as an agent that stimulâtes neuronal prolifération.
    Type: Application
    Filed: March 23, 2012
    Publication date: February 27, 2014
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRS, UNIVERSITE DE STRASBOURG
    Inventors: Ayikoe Guy Mensah-Nyagan, Laurence Meyer, Christine Patte-Mensah, Omar Taleb, Michel Miesch, Philippe Geoffroy, Blandine Ressault
  • Publication number: 20130203718
    Abstract: The present invention relates to a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.
    Type: Application
    Filed: May 9, 2011
    Publication date: August 8, 2013
    Inventors: Marie-Edith Rafestin-Oblin, Mouad Alami, Hugues Loosfelt, Abdallah Hamze, Ali Junaid Khan, Abdellatif Tikad, Marc Lombes, Jean-Daniel Brion
  • Publication number: 20120071453
    Abstract: A compound with general formula I for treatment of various diseases of the central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.
    Type: Application
    Filed: May 28, 2010
    Publication date: March 22, 2012
    Inventors: Hana Chodounska, Eva Stastna, Vojtech Kapras, Ladislav Kohout, Jirina Borovska, Ladislav Vyklicky, Karel Vales, Ondrej Cais, Lukas Rambousek, Ales Stuchlik, Vera Valesova
  • Publication number: 20110263553
    Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
    Type: Application
    Filed: February 26, 2009
    Publication date: October 27, 2011
    Inventors: Christopher Macnevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
  • Publication number: 20090118248
    Abstract: The invention relates to a novel multi step process of making compounds of Formula I: wherein R1 is an alkoxy group and R2 is an optionally substituted, N-attached heteroaryl. The hydrogen at the 5-position can be ? or ? isomer, preferably ?. Preferably the compound of Formula I is 17? isomer. The invention also relates to novel 3?-hydroxy-3?-substituted-17-substituted steroid compounds having GABAA receptor modulating activity, pharmaceutical compositions comprising these compounds, and the use of these compounds in a method of modulating brain excitability.
    Type: Application
    Filed: April 22, 2005
    Publication date: May 7, 2009
    Applicant: Euro-Celtique S.A.
    Inventors: Ping W. Chang, Ning Zhong, Xinping Fang, Shao-Kun Pang, Chi-Nung Hsiao, Tsung-Cheng Hu
  • Patent number: 7049305
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: May 23, 2006
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
  • Patent number: 6790970
    Abstract: The present invention provides a novel (meth)acrylic acid ester compound useful as a resin material for photosensitive compositions, which enables control of the molecular weight of a resin to be prepared. The novel (meth)acrylic acid ester compound is one represented by the following formula (I): wherein R1 and R2 each independently represent a hydrogen atom or a hydroxyl group; and R3 represents a hydrogen atom or a methyl group.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: September 14, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kenichiro Sato, Toshiaki Aoai
  • Patent number: 6395723
    Abstract: This invention provides a method of providing progestational therapy to a mammal in need thereof which comprises administering a progestationally effective amount of a pharmaceutically acceptable salt of 5&agr;-pregnan-3&bgr;-ol-20-one 3-sulfate ester to said mammal.
    Type: Grant
    Filed: October 4, 2001
    Date of Patent: May 28, 2002
    Assignee: Wyeth
    Inventors: Michael Z. Kagan, Syed M. Shah
  • Publication number: 20020002295
    Abstract: The present invention provides a novel (meth)acrylic acid ester compound useful as a resin material for photosensitive compositions, which enables control of the molecular weight of a resin to be prepared.
    Type: Application
    Filed: March 25, 1999
    Publication date: January 3, 2002
    Inventors: KENICHIRO SATO, TOSHIAKI AOAI
  • 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: 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: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • 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: 5319115
    Abstract: This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3.alpha.-hydroxy,3.beta.-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3.alpha.-hydroxy,3.beta.-substituted-20-one form, which can be further modified at the 20-keto position.Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: June 7, 1994
    Assignee: Cocensys Inc.
    Inventors: Hasan Tahir, Michael Bolger, Richard Buswell, Richard Gabriel, Jay Stearns
  • Patent number: 4946834
    Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: August 7, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf