Patents Examined by Barbara P. Badio
  • 1-substituted 4-arylpiperazine as kappa opioid receptor antagonists
    Patent number: 9512105
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: December 6, 2016
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
    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
  • 3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments
    Patent number: 9512169
    Abstract: The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: December 6, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Bothe, Matthias Busemann, Oliver Martin Fischer, Naomi Barak, Andrea Rotgeri, Tobias Marquardt, Christian Stegmann
  • Extended triterpene derivatives
    Patent number: 9505800
    Abstract: The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: November 29, 2016
    Assignee: Myrexis, Inc.
    Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
  • Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments
    Patent number: 9487554
    Abstract: The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: November 8, 2016
    Assignees: Bayer Intellectual Property GmbH, Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Bothe, Naomi Barak, Matthias Busemann, Oliver Martin Fischer, Andrea Rotgeri, Isabella Gashaw, Ingo Hartung, Tobias Marquardt
  • Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
    Patent number: 9486458
    Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: November 8, 2016
    Assignee: Cassiopea SPA
    Inventors: Mauro Ajani, Luigi Moro
  • Combined synthesis route for desogestrel and etonogestrel
    Patent number: 9464108
    Abstract: The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: October 11, 2016
    Assignee: Merck Sharp & Dohme B.V.
    Inventor: Martin Ostendorf
  • Nitrate esters and their use for the treatment of muscle and muscle related diseases
    Patent number: 9452117
    Abstract: Alkyl nitrate ester compounds are provided for the delivery of nitric oxide to targeted muscle tissues, and in particular, to normal and dystrophic muscles. In one aspect, nitrate ester compounds are provided having the following formula: wherein, R1 is ONO2, CH2ONO2, CnH2n+1OH, CnH2n+1OH, CH3, CH2CH3, CH2CH2CH3, or H; R2 is ONO2, CH2ONO2, Cn?H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; R3 is ONO2, CH2ONO2, Cn??H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; and R4 is ONO2, CH2ONO2, Cn??H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; wherein n is an integer from 0 to 9, n? is an integer from 0 to 9, and n? is an integer from 0 to 9, and n+n?+n??9, and wherein at least one of R1, R2, and R3 is an ester nitrate selected from the group consisting of ONO2, CH2ONO2, and combinations thereof.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: September 27, 2016
    Assignee: The Charlotte-Mecklenburg Hospital Authority
    Inventors: Guqi Wang, Qi Long Lu
  • Cholest-4-en-3-one oxime derivatives, pharmaceutical compositions containing same, and preparation method
    Patent number: 9447140
    Abstract: The present invention relates to novel chemical compounds, in particular cholest-4-en-3-one oxime derivatives and to the use thereof as medicaments, especially as cytoprotective medicaments, in particular neuroprotective, cardioprotective and/or hepatoprotective medicaments.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: September 20, 2016
    Assignee: TROPHOS
    Inventors: Rebecca Pruss, Abdesslamc Nazih, Corinne Chaimbault, Cyrillo Drouot
  • Glycyrrhetinimidyl hydroxyproline alkyl esters and protected derivatives thereof
    Patent number: 9439845
    Abstract: The present invention is directed to glycyrrhetinimidyl hydroxyproline alkyl ester compounds and their protected derivatives and cosmetically acceptable salts thereof, methods of making the compounds, cosmetic compositions containing at least one of the compounds and methods of using the same to promote collagen production in human skin. The compounds and cosmetic compositions of the invention provide various advantageous properties to the human skin.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: September 13, 2016
    Assignee: REVLON CONSUMER PRODUCTS CORPORATION
    Inventors: Harry Cai, Dariush Hosseinpour, Alan Meyers
  • Enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives
    Patent number: 9433628
    Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: September 6, 2016
    Assignee: Cassiopea SPA
    Inventors: Mauro Ajani, Luigi Moro
  • Fatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents
    Patent number: 9428540
    Abstract: The present invention relates to certain unsaturated fatty acid derivatives of therapeutically active glucocorticoides-fatty acid esters of glucocorticoids as anti-inflammatory and anti-cancer agents and pharmaceutical formulations containing them.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: August 30, 2016
    Assignee: CLAVIS PHARMA ASA
    Inventors: Finn Myhren, Marit Liland Sandvold, Ole Henrik Eriksen, Steinar Hagen
  • Lupane triterpenoid derivatives and pharmaceutical use thereof
    Patent number: 9428542
    Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: August 30, 2016
    Assignees: JIANGXI QINGFENG PHARMACEUTICAL INC.
    Inventor: Feng Lu
  • 2?,3?,5?-trihydroxy-androst-6-one and preparation methods and use thereof
    Patent number: 9428539
    Abstract: The present invention discloses compound 2?,3?,5?-trihydroxy-androst-6-one, having the structure of formula (I). The present invention also discloses a plurality of methods for preparing the compound and a use of the compound.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: August 30, 2016
    Assignee: Guangzhou Cellprotek Pharmaceutical Co., Ltd.
    Inventors: Jingxia Zhang, Suizhen Lin, Minyu Xie
  • Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
    Patent number: 9427431
    Abstract: The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: August 30, 2016
    Assignee: Johns Hopkins University School of Medicine
    Inventors: Philip A. Beachy, Michael K. Cooper, Jefferey A. Porter
  • (22E)-2-methylene-22-dehydro-1?,24,25-trihydroxy-19-nor-vitamin Danalogs
    Patent number: 9416102
    Abstract: Disclosed are (22E)-2-methylene-22-dehydro-1,24,25-trihydroxy-19-nor-vitamin D3 compounds, their biological activities, and various pharmaceutical uses for these compounds. Particularly disclosed are (22E)-(24R)-2-methylene-22-dehydro-1?,24,25-trihydroxy-19-nor-vitamin D3 and (22E)-(24S)-2-methylene-22-dehydro-1?,24,25-trihydroxy-19-nor-vitamin D3, their biological activities, and various pharmaceutical uses for these compounds.
    Type: Grant
    Filed: November 19, 2013
    Date of Patent: August 16, 2016
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal Barycki, Margaret Clagett-Dame
  • Process for preparing delta-7,9(11) steroids from and analogs thereof
    Patent number: 9376462
    Abstract: Processes for preparing lanostane triterpenes from the medicinal mushroom Ganoderma lucidum, and related compounds are described. Compounds, compositions, and methods for treating cancer are also described.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: June 28, 2016
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Robert Minto, Erin Kennedy
  • Polycyclic tetracycline compounds
    Patent number: 9371283
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: June 21, 2016
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Xiao-Yi Xiao, Roger Clark, Diana Hunt, Magnus Rönn, Louis Plamondon, Minsheng He, Joyce Sutcliffe, Trudy Grossman
  • Photolabile caged transition metal complexes and methods of using the same
    Patent number: 9365593
    Abstract: The present invention provides compounds of Formula I: along with compositions comprising the same and methods of using the same, such as for photodynamic therapy in the treatment of cancer.
    Type: Grant
    Filed: March 21, 2013
    Date of Patent: June 14, 2016
    Assignee: Duke University
    Inventors: Katherine J. Franz, Katie L. Ciesienski
  • Synthesis of tetracyclines and analogues thereof
    Patent number: 9365493
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: June 14, 2016
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel