The Hetero Ring Consists Of Two Nitrogens And Three Carbons And Is Ortho Fused To The A Ring Patents (Class 540/52)
  • Patent number: 9975918
    Abstract: The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: May 22, 2018
    Assignees: VAN ANDEL RESEARCH INSTITUTE, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Huaqiang Eric Xu, Yuanzheng He, Karsten Melcher, Wei Yi, Jingjing Shi
  • Publication number: 20140045804
    Abstract: A topical cream to be applied to the clitoris and hood of the vaginal area to create an intense libido and drive for orgasm. The cream comprises a base cream having from about 9.5% to about 10%, by volume, of a steroid, based upon the total volume of the cream. Preferably, at least about 1% to about 10% by volume, of the steroid, based on the total volume of the cream. The topical cream may, also, include from about 0.1% to about 2.0%, by volume, of oxytocin. The addition of the small amount thereof enhances the efficacy of the cream.
    Type: Application
    Filed: January 21, 2013
    Publication date: February 13, 2014
    Inventor: Edward M. Lichten
  • Publication number: 20130237507
    Abstract: The present invention provides compounds of formula (1) 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: April 17, 2013
    Publication date: September 12, 2013
    Inventors: Frank Burkamp, Balint Gabos, Svetlana Ivanova, Alice Ingrid Annea Lisius
  • Patent number: 8163724
    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: Grant
    Filed: October 3, 2008
    Date of Patent: April 24, 2012
    Assignee: AstraZeneca AB
    Inventors: HÃ¥kan Bladh, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
  • Patent number: 7727976
    Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
    Type: Grant
    Filed: September 26, 2005
    Date of Patent: June 1, 2010
    Assignee: XenoPort, Inc.
    Inventors: Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
  • Publication number: 20090233274
    Abstract: The present invention provides novel target proteins and target genes for drug discovery, and the means that enable the development of novel drugs using the same. More particularly, the present invention provides NCS proteins and genes thereof; screening methods for drug (for example, anti-central nervous disease drug); agents for regulating disease (for example, central nervous disease); production methods of a drug derivative; a complex comprising a drug and NCS protein, and a method of producing the complex; a kits comprising a drug or a salt thereof; determination methods for the onset or risk of onset of a specified disease, determination methods for susceptibility to a drug, and determination kits used for the determination methods; and the like.
    Type: Application
    Filed: October 9, 2005
    Publication date: September 17, 2009
    Applicant: Reverse Proteomics Research Institute Co.
    Inventors: Tadakazu Yamauchi, Hideaki Sueoka, Koichi Tsuchiya, Katsuhisa Murayama, Ken Horiuchi, Kazuo Komiya, Morikazu Kito, Takeshi Kito, Takeshi Tsutsumi, Yuko Isono, Yorimasa Suwa
  • Publication number: 20080234242
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Application
    Filed: March 19, 2008
    Publication date: September 25, 2008
    Applicant: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7112580
    Abstract: A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: September 26, 2006
    Assignee: Inflazyme Pharmaceuticals Ltd.
    Inventors: Jeffery R Raymond, Claudia E Kasserra, Yaping Shen
  • Patent number: 7053076
    Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: May 30, 2006
    Assignee: XenoPort, Inc.
    Inventors: Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
  • Patent number: 7041839
    Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: May 9, 2006
    Assignee: Northeastern University
    Inventors: Robert N. Hanson, Carolyn Friel, Choon Young Lee
  • Publication number: 20020072510
    Abstract: A compound of the formula 1
    Type: Application
    Filed: April 30, 2001
    Publication date: June 13, 2002
    Inventors: Jeffery R. Raymond, Claudia E. Kasserra, Yaping Shen
  • Patent number: 5236912
    Abstract: [3,2-c]Pyrazole and [3,2-d]triazole steroids are useful anti-androgens.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: August 17, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Dieter Bittler, Horst Michna, Ursula Habenicht, Karl-Heinrich Fritzemeier, Yukishige Nishino
  • Patent number: 5232915
    Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: August 3, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
  • Patent number: 4605517
    Abstract: The method of preparing a 2.alpha.-cyano-4.alpha.,5.alpha.-epoxy-3-oxo steroid or a steroid fused at the 2- and 3-positions with a heterocyclic ring of controlled particle size which comprises dissolving the steroid in an organic solvent, precipitating the steroid by mixing a non-solvent for the steroid with the resulting solution, and controlling the time of mixing and the degree of agitation during mixing.
    Type: Grant
    Filed: October 11, 1984
    Date of Patent: August 12, 1986
    Assignee: Sterling Drug Inc.
    Inventors: Derek C. Riley, David Johnston