Patents Assigned to Alectos Therapeutics Inc.
  • Bis-acetal-based substrates for imaging exo-glycosidase activity
    Patent number: 11396522
    Abstract: The invention provides fluorescence-quenched substrates of exo-glycosidase enzymes. The invention also provides methods for imaging exo-glycosidase enzymes activity within cells.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: July 26, 2022
    Assignee: ALECTOS THERAPEUTICS INC.
    Inventors: David J. Vocadlo, Samy Cecioni, Roger Ashmus
  • Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof
    Patent number: 10913733
    Abstract: The present invention is directed to thiazolyl piperidine compounds of the general structural formula I: which are inhibitors of O-GlcNAcase. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which O-GlcNAcase is involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which O-GlcNAcase is involved.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: February 9, 2021
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Harold G. Selnick, Yuanxi Zhou
  • GLYCOSIDASE INHIBITORS AND USES THEREOF
    Publication number: 20180362517
    Abstract: The present invention is directed to thiazolyl piperidine compounds which are inhibitors of O-GlcNAcase. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which O-GlcNAcase is involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which O-GlcNAcase is involved.
    Type: Application
    Filed: December 14, 2016
    Publication date: December 20, 2018
    Applicant: Alectos Therapeutics, Inc.
    Inventors: Ernest J. McEachern, Harold G. Selnick, Yuanxi Zhou
  • Glucocerebrosidase modulators and uses thereof
    Patent number: 10081601
    Abstract: The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: September 25, 2018
    Assignee: Alectos Therapeutics Inc.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
  • Glycosidase inhibitors and uses thereof
    Patent number: 9938299
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: April 10, 2018
    Assignees: ALECTOS THERAPEUTICS, INC., MERCK SHARP & DOHME CORP.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Ramesh Kaul, Zhongyong Wei, Yaode Wang, Jiang Chang
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9815861
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: November 14, 2017
    Assignees: Alectos Therapeutics, Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou, Yongbao Zhu
  • Glycosidase inhibitors and uses thereof
    Patent number: 9809537
    Abstract: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 7, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
  • Glucocerebrosidase modulators and uses thereof
    Patent number: 9796680
    Abstract: The invention provides isofogamine analogs of structural formula (I) below that modulate and stabilize glucocerebrosidases and enhance their enzymatic activity in vivo. Such compounds, prodrugs and compositions thereof are useful in treating synucleinopathy, lysosomal storage disease and relevant neurodegenerative disease.
    Type: Grant
    Filed: December 22, 2014
    Date of Patent: October 24, 2017
    Assignee: Alectos Therapeutics Inc.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9718854
    Abstract: The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 1, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Kun Liu, Harold G. Selnick, Zhongyong Wei, Changwei Mu, Yaode Wang, Xiaona Wang
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9701693
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: July 11, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
  • Glycosidase inhibitors and uses thereof
    Patent number: 9695197
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: October 30, 2013
    Date of Patent: July 4, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Qun Dang, Harold G. Selnick
  • Glycosidase inhibitors and uses thereof
    Patent number: 9670195
    Abstract: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: June 6, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Permeable glycosidase inhibitors and uses thereof
    Patent number: 9611275
    Abstract: The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: April 4, 2017
    Assignees: ALECTOS THERAPEUTICS, INC., MERCK SHARP & DOHME CORP.
    Inventors: Harold G. Selnick, Wenping Li, Eric Hostetler, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Zhongyong Wei, Changwei Mu, Yaode Wang, Jiang Chang
  • GLUCOCEREBROSIDASE MODULATORS AND USES THEREOF
    Publication number: 20170029379
    Abstract: The invention provides isofogamine analogs of structural formula (I) below that modulate and stabilize glucocerebrosidases and enhance their enzymatic activity in vivo. Such compounds, prodrugs and compositions thereof are useful in treating synucleinopathy, lysosomal storage disease and relevant neurodegenerative disease.
    Type: Application
    Filed: December 22, 2014
    Publication date: February 2, 2017
    Applicant: Alectos Therapeutics Inc.
    Inventors: Ramesh KAUL, Ernest J. MCEACHERN, Jianyu SUN, David J. VOCADLO, Yuanxi ZHOU, Yongbao ZHU
  • Glycosidase inhibitors and uses thereof
    Patent number: 9522883
    Abstract: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-?-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-?-D-glucopyranoside (O-GlcNAc).
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: December 20, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9409924
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: August 9, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest McEachern, David Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold Selnick
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9243020
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: January 26, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Harold G. Selnick, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9199949
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: December 1, 2015
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9126957
    Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: September 8, 2015
    Assignees: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS, INC.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Yongbao Zhu
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9120781
    Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: September 1, 2015
    Assignees: Simon Fraser University, Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.
    Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Kun Liu, Harold G. Selnick