The Hetero Ring Is Bonded Directly At The 3-position Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/97)
  • Publication number: 20140107089
    Abstract: Disclosed are compounds having the general formula: wherein R1-R4 and X are as defined herein, pharmaceutical compositions including such compounds, and a method of treating a patient involving antagonizing the endogenous progesterone, such as in inducing menses and treating endometriosis, dysmenorrhea, endocrine hormone-dependent tumors, meningiomas, uterine leiomyomas, or uterine fibroids, inhibiting uterine endometrial proliferation, inducing cervical ripening, inducing labor, and in contraception.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 17, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: Hyun K. Kim, Richard P. Blye, Pemmaraju N. Rao, James W. Cessac, Carmie K. Acosta, Anne Marie Simmons
  • Publication number: 20140018336
    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: September 16, 2013
    Publication date: January 16, 2014
    Applicant: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20140018337
    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: September 16, 2013
    Publication date: January 16, 2014
    Applicant: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20120190659
    Abstract: Compounds of Structural Formula I or pharmaceutically acceptable salts thereof, are effective inhibitors of angiogenesis:
    Type: Application
    Filed: April 16, 2010
    Publication date: July 26, 2012
    Applicants: Children's Medical Center Corporation, President and Fellows of Harvard College
    Inventors: Elias James Corey, Barbara Czakó, László Kürti, Akiko Mammoto, Donald E. Ingber
  • Publication number: 20120053340
    Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).
    Type: Application
    Filed: November 2, 2011
    Publication date: March 1, 2012
    Applicant: BTG International Limited
    Inventor: Neil John Hunt
  • Patent number: 7074778
    Abstract: This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: July 11, 2006
    Assignee: Genaera Corporation
    Inventors: Roy C. Levitt, Nicholas C. Nicolaides, William A. Kinney, Steve Jones
  • Patent number: 6262042
    Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: July 17, 2001
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Gary S. Bartley
  • Patent number: 5817803
    Abstract: The present invention provides new process of preparing neuromuscular blocking agents. The process include preparing neuromuscular blocking agents using the compounds of formula I: ##STR1## wherein R.sub.1 is .dbd.O and X is halo; and formula II: ##STR2## wherein R.sub.1 and X are as defined above.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 6, 1998
    Assignee: Poli Industria Chimica, S.p.A.
    Inventors: Ambrogio Magni, Paride Grisenti
  • Patent number: 5695738
    Abstract: Compositions of sterodial glycosides are described wherein the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon, or similar stable linkage, and methods of using the compositions to treat patients by binding to and/or blocking cellular receptors for a variety of diseases including cancer, inflammation, and autoimmune diseases.
    Type: Grant
    Filed: June 15, 1995
    Date of Patent: December 9, 1997
    Assignee: Glycomed Incorporated
    Inventors: Mark Anderson, John Henry Musser
  • Patent number: 5591733
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: January 7, 1997
    Assignee: University of Southern California
    Inventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
  • Patent number: 5591735
    Abstract: There is disclosed novel, therapeutically active androstane derivatives having neuromuscular blocking effect, which are substituted by a quaternary ammonium group in 16-position; pharmaceutically composition containing them; process for producing them; and novel intermediates for the production.
    Type: Grant
    Filed: October 27, 1993
    Date of Patent: January 7, 1997
    Assignee: Marvishi Pharmaceutical Co., Ltd.
    Inventors: Zoltan Tuba, E. Szilveszter Vizi, Francis F. Foldes, Sandor Maho
  • Patent number: 5565588
    Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: October 15, 1996
    Assignee: Roussel UCLAF
    Inventors: Jacobus N. M. Batist, Arthur F. Marx, Willem J. Van Zoest, Jagdish C. Kapur
  • Patent number: 5556846
    Abstract: 17-Heterocyclyl-5.alpha.-14.beta.-androstane, androstene and androstadiene of formula (I): ##STR1## wherein: Y is oxygen or guanidinoimino, when a double bond exists at position 3;Y is hydroxy, OR.sup.2 or SR.sup.2, when a single bond exists at position 3;R is a saturated or unsaturated mono- or biheterocyclic ring, containing one or more heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, unsubstituted or substituted by one or more of halogen, hydroxymethyl, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, sulfonamido, C.sub.1 -C.sub.6 lower alkyl or COR.sup.3 ; andR.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: September 17, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Piero Melloni, Luigi Bernardi, Mara Ferrandi, Marco Frigerio, Marina Mauro, Luisa Quadri
  • Patent number: 5449795
    Abstract: A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is .alpha. to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal .gamma.-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: September 12, 1995
    Assignee: CoCensys, Inc.
    Inventor: Derk J. Hogenkamp
  • Patent number: 5232917
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: August 3, 1993
    Assignee: University of Southern California
    Inventors: Michael Bolger, Kelvin W. Gee, Nancy C. Lan, Delia Belelli, Seid Mirsadeghi, Robert Purdy
  • Patent number: 5208227
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: May 4, 1993
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger, Roberta E. Brinton, Deborah J. Burke, Bruce S. McEwen
  • Patent number: 5194602
    Abstract: New 9.alpha.-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9.alpha.-hydroxyandrost-4-ene-3, 17-dione.The resulting compounds are useful starting compounds in the synthesis of corticosteroids.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 16, 1993
    Assignee: Gist-Brocades N.V.
    Inventors: Jacobus N. M. Batisi, Arthur F. Marx
  • Patent number: 5120723
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: May 10, 1990
    Date of Patent: June 9, 1992
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger
  • Patent number: 5003063
    Abstract: The invention involves a two step chemical transformation of a steroidal 17-cyanohydrin (II) ##STR1## to a 17.alpha.-hydroxy-21-halo-20-keto steroid (IV) ##STR2## intermediate which can readily be converted to pharmaceutically useful corticoids.
    Type: Grant
    Filed: January 30, 1990
    Date of Patent: March 26, 1991
    Assignee: The Upjohn Company
    Inventor: John G. Reid
  • Patent number: RE35517
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: May 20, 1997
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan