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.
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.
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.
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
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
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
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
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
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
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.
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.
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.
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
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.
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
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
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.
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
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