Alectos Therapeutics Inc.

Canada

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        World 31
        United States 12
        Canada 6
Date
2023 2
2022 1
2021 4
2020 3
Before 2020 39
IPC Class
C07D 513/04 - Ortho-condensed systems 21
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia 14
C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms 12
C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase 10
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine 9
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Status
Pending 6
Registered / In Force 43
Found results for  patents

1.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number 17923878
Status Pending
Filing Date 2021-05-06
First Publication Date 2023-11-02
Owner ALECTOS THERAPEUTICS lNC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings

2.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number 17923875
Status Pending
Filing Date 2021-05-06
First Publication Date 2023-06-08
Owner ALECTOS THERAPEUTICS lNC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

3.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number 17594834
Status Pending
Filing Date 2020-05-07
First Publication Date 2022-07-07
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 211/32 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

4.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Document Number 03182338
Status Pending
Filing Date 2021-05-06
Open to Public Date 2021-11-11
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 3/00 - Drugs for disorders of the metabolism
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

5.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number IB2021053864
Publication Number 2021/224865
Status In Force
Filing Date 2021-05-06
Publication Date 2021-11-11
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 3/00 - Drugs for disorders of the metabolism
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

6.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Document Number 03182334
Status Pending
Filing Date 2021-05-06
Open to Public Date 2021-11-11
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 3/00 - Drugs for disorders of the metabolism
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

7.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number IB2021053863
Publication Number 2021/224864
Status In Force
Filing Date 2021-05-06
Publication Date 2021-11-11
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 3/00 - Drugs for disorders of the metabolism
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

8.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Document Number 03138726
Status Pending
Filing Date 2020-05-07
Open to Public Date 2020-11-19
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 3/00 - Drugs for disorders of the metabolism
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

9.

NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF

      
Application Number IB2020054355
Publication Number 2020/229968
Status In Force
Filing Date 2020-05-07
Publication Date 2020-11-19
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

  • C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
  • A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 3/00 - Drugs for disorders of the metabolism
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

10.

Bis-acetal-based substrates for imaging exo-glycosidase activity

      
Application Number 16622870
Grant Number 11396522
Status In Force
Filing Date 2018-06-12
First Publication Date 2020-07-02
Grant Date 2022-07-26
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Vocadlo, David J.
  • Cecioni, Samy
  • Ashmus, Roger

Abstract

The invention provides fluorescence-quenched substrates of exo-glycosidase enzymes. The invention also provides methods for imaging exo-glycosidase enzymes activity within cells.

IPC Classes  ?

  • G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances
  • G01N 33/542 - ImmunoassayBiospecific binding assayMaterials therefor with immune complex formed in liquid phase with steric inhibition or signal modification, e.g. fluorescent quenching
  • G01N 21/64 - FluorescencePhosphorescence
  • C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings

11.

Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof

      
Application Number 16061988
Grant Number 10913733
Status In Force
Filing Date 2016-12-14
First Publication Date 2018-12-20
Grant Date 2021-02-09
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Mceachern, Ernest J.
  • Selnick, Harold G.
  • Zhou, Yuanxi

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.

IPC Classes  ?

  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

12.

BIS-ACETAL-BASED SUBSTRATES FOR IMAGING EXO-GLYCOSIDASE ACTIVITY

      
Application Number IB2018054273
Publication Number 2018/229663
Status In Force
Filing Date 2018-06-12
Publication Date 2018-12-20
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Vocadlo, David J.
  • Cecioni, Samy

Abstract

The invention provides fluorescence-quenched substrates of exo-glycosidase enzymes. The invention also provides methods for imaging exo-glycosidase enzymes activity within cells.

IPC Classes  ?

  • C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
  • A61K 49/00 - Preparations for testing in vivo
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • G01N 33/52 - Use of compounds or compositions for colorimetric, spectrophotometric or fluorometric investigation, e.g. use of reagent paper

13.

Glucocerebrosidase modulators and uses thereof

      
Application Number 15711301
Grant Number 10081601
Status In Force
Filing Date 2017-09-21
First Publication Date 2018-01-11
Grant Date 2018-09-25
Owner Alectos Therapeutics Inc. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.

IPC Classes  ?

14.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number US2016066507
Publication Number 2017/106254
Status In Force
Filing Date 2016-12-14
Publication Date 2017-06-22
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS, INC. (Canada)
Inventor
  • Mceachern, Ernest, J.
  • Selnick, Harold, G.
  • Zhou, Yuanxi

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.

IPC Classes  ?

  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • C07D 471/14 - Ortho-condensed systems

15.

Glucocerebrosidase modulators and uses thereof

      
Application Number 15107269
Grant Number 09796680
Status In Force
Filing Date 2014-12-22
First Publication Date 2017-02-02
Grant Date 2017-10-24
Owner Alectos Therapeutics Inc. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

16.

Glycosidase inhibitors and uses thereof

      
Application Number 14655222
Grant Number 09938299
Status In Force
Filing Date 2013-12-08
First Publication Date 2016-07-07
Grant Date 2018-04-10
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold G.
  • Liu, Kun
  • Mceachern, Ernest J.
  • Kaul, Ramesh
  • Wei, Zhongyong
  • Wang, Yaode
  • Chang, Jiang

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.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • B65D 71/14 - Bundles of articles held together by packaging elements for convenience of storage or transport, e.g. portable segregating carrier for plural receptacles such as beer cans or pop bottlesBales of material comprising a plurality of articles completely or mainly held together by packaging elements, e.g. under tension the packaging elements being formed by folding a single blank having the shape of a tube, without, or not being characterised by, end walls
  • B65D 71/16 - Bundles of articles held together by packaging elements for convenience of storage or transport, e.g. portable segregating carrier for plural receptacles such as beer cans or pop bottlesBales of material comprising a plurality of articles completely or mainly held together by packaging elements, e.g. under tension the packaging elements being formed by folding a single blank having the shape of a tube, without, or not being characterised by, end walls with article-locating elements
  • B65D 5/00 - Rigid or semi-rigid containers of polygonal cross-section, e.g. boxes, cartons or trays, formed by folding or erecting one or more blanks made of paper
  • B65D 5/20 - Rigid or semi-rigid containers of polygonal cross-section, e.g. boxes, cartons or trays, formed by folding or erecting one or more blanks made of paper by folding-up portions connected to a central panel from all sides to form a container body, e.g. of tray-like form

17.

Glycosidase inhibitors and uses thereof

      
Application Number 14424602
Grant Number 09522883
Status In Force
Filing Date 2013-08-29
First Publication Date 2015-08-06
Grant Date 2016-12-20
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Selnick, Harold G.

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-β-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D-glucopyranoside (O-GlcNAc).

IPC Classes  ?

  • C07D 211/56 - Nitrogen atoms
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

18.

GLUCOCEREBROSIDASE MODULATORS AND USES THEREOF

      
Application Number CA2014051252
Publication Number 2015/095963
Status In Force
Filing Date 2014-12-22
Publication Date 2015-07-02
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

  • C07D 221/20 - Spiro-condensed ring systems
  • A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/16 - Anti-Parkinson drugs

19.

Permeable glycosidase inhibitors and uses thereof

      
Application Number 14399146
Grant Number 09611275
Status In Force
Filing Date 2013-05-03
First Publication Date 2015-06-04
Grant Date 2017-04-04
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold G.
  • Li, Wenping
  • Hostetler, Eric
  • Liu, Kun
  • Mceachern, Ernest J.
  • Zhou, Yuanxi
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Chang, Jiang

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.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms

20.

PHOTOCHEMICAL PROCESS FOR THE FLUORINATION OF AN ORGANIC COMPOUND HAVING AN UNACTIVATED SP3 C-H BOND

      
Application Number CA2014050629
Publication Number 2015/000076
Status In Force
Filing Date 2014-07-02
Publication Date 2015-01-08
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Britton, Robert J.
  • Halperin, Shira

Abstract

The application provides a photochemical process for the chemoselective fluorination of an organic compound by combining a carbon-containing compound having an unactivated sp3 C-H bond with a reagent system comprised of a fluorinating agent, and a photocatalyst, in the presence of a light source. Provided as fluorinating agent is N-fluorobenzenesulfonimide (NFSI) or 1-chloromethy1-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor™), as photocatalyst is tetrabutylammonium decatungstate (TBADT), and as light source is a 365 nm UV lamp. The reactions conditions result in the C-H bond being replaced by a C-F bond, to provide a fluorinated carbon-containing compound.

IPC Classes  ?

21.

Selective glycosidase inhibitors and uses thereof

      
Application Number 14129177
Grant Number 09409924
Status In Force
Filing Date 2012-06-27
First Publication Date 2014-10-02
Grant Date 2016-08-09
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest
  • Vocadlo, David
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Selnick, Harold

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.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • C07H 13/04 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
  • C07H 13/12 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group —X—C (=X)—X—, or halides thereof, in which X means nitrogen, oxygen, sulfur, selenium, or tellurium, e.g. carbonic acid, carbamic acid
  • C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
  • C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

22.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CN2012087286
Publication Number 2014/100934
Status In Force
Filing Date 2012-12-24
Publication Date 2014-07-03
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold G.
  • Liu, Kun
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Wei, Zhongyong
  • Wang, Yaode
  • Chang, Jiang

Abstract

The compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds are provided. The methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc are also provided.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

23.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number US2013076768
Publication Number 2014/105662
Status In Force
Filing Date 2013-12-20
Publication Date 2014-07-03
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold, G.
  • Liu, Kun
  • Mceachern, Ernest, J.
  • Kaul, Ramesh
  • Wei, Zhongyong
  • Wang, Yaode
  • Chang, Jiang

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.

IPC Classes  ?

24.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2013050822
Publication Number 2014/067003
Status In Force
Filing Date 2013-10-30
Publication Date 2014-05-08
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest, J.
  • Vocadlo, David, J.
  • Zhou, Yuanxi
  • Dang, Qun
  • Selnick, Harold G.

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, accumulatio or deficiency of O-GlcNAc.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • A61P 3/00 - Drugs for disorders of the metabolism
  • C07D 498/04 - Ortho-condensed systems
  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms

25.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2013050672
Publication Number 2014/032188
Status In Force
Filing Date 2013-08-29
Publication Date 2014-03-06
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Mceachern, Ernest J.
  • Sun, Jianyu
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07D 207/12 - Oxygen or sulfur atoms
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07H 13/02 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)

26.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2013050668
Publication Number 2014/032184
Status In Force
Filing Date 2013-08-29
Publication Date 2014-03-06
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07H 5/04 - Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to nitrogen
  • C07H 7/00 - Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)

27.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2013050669
Publication Number 2014/032185
Status In Force
Filing Date 2013-08-29
Publication Date 2014-03-06
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Mceachern, Ernest, J.
  • Sun, Jianyu
  • Vocadlo, David, J.
  • Zhou, Yuanxi
  • Selnick, Harold, G.

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.

IPC Classes  ?

  • C07D 207/14 - Nitrogen atoms not forming part of a nitro radical
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07H 13/02 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)

28.

GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2013050671
Publication Number 2014/032187
Status In Force
Filing Date 2013-08-29
Publication Date 2014-03-06
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Mceachern, Ernest, J.
  • Vocadlo, David, J.
  • Zhou, Yuanxi
  • Selnick, Harold, G.

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-β-D-giucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-β-D- glucopyranoside (O-GlcNAc).

IPC Classes  ?

  • C07D 211/56 - Nitrogen atoms
  • A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
  • A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07H 13/02 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)

29.

PERMEABLE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number US2013039377
Publication Number 2013/169576
Status In Force
Filing Date 2013-05-03
Publication Date 2013-11-14
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold, G.
  • Li, Wenping
  • Hostetler, Eric
  • Liu, Kun
  • Mceachern, Ernest, J.
  • Zhou, Yuanxi
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Chang, Jiang

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.

IPC Classes  ?

30.

PERMEABLE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Document Number 02871920
Status In Force
Filing Date 2013-05-03
Open to Public Date 2013-11-14
Grant Date 2021-03-09
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold G.
  • Li, Wenping
  • Hostetler, Eric
  • Liu, Kun
  • Mceachern, Ernest J.
  • Zhou, Yuanxi
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Chang, Jiang

Abstract

The present invention is directed to a compound of Formula (I) (see formula I) or a pharmaceutically acceptable salt thereof, and pharmaceutical formulations comprising the compound 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.

IPC Classes  ?

  • C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane ringsBicyclic carbocyclic ring systems
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07H 15/02 - Acyclic radicals, not substituted by cyclic structures
  • C07H 15/20 - Carbocyclic rings
  • C07D 513/04 - Ortho-condensed systems
  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms

31.

PERMEABLE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CN2012075185
Publication Number 2013/166654
Status In Force
Filing Date 2012-05-08
Publication Date 2013-11-14
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold G.
  • Li, Wenping
  • Hostetler, Eric
  • Liu, Kun
  • Mceachern, Ernest J.
  • Zhou, Yuanxi
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Chang, Jiang

Abstract

Disclosed are compounds of Formula (I), wherein each substituent of Formula (I) is defined as in the specification, pharmaceutical formulations comprising these compounds which are useful as 0-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus are useful for the treatment of certain disorders such as Alzheimer' s disease including reducing NFTs and/or hyperphosphorylated tau. Also disclosed is the use of the compounds as O-GlcNAcase imaging agents.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 25/16 - Anti-Parkinson drugs
  • A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
  • A61P 37/08 - Antiallergic agents
  • A61P 11/06 - Antiasthmatics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/04 - Immunostimulants
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 11/02 - Nasal agents, e.g. decongestants
  • A61P 17/06 - Antipsoriatics
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

32.

Selective glycosidase inhibitors and uses thereof

      
Application Number 13883811
Grant Number 08901087
Status In Force
Filing Date 2011-11-08
First Publication Date 2013-11-07
Grant Date 2014-12-02
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Chang, Jiang
  • Liu, Kun
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Shi, Feng
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

  • C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
  • C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings
  • A61K 31/70 - CarbohydratesSugarsDerivatives thereof
  • A61K 31/425 - Thiazoles
  • C07D 513/04 - Ortho-condensed systems

33.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number US2012050225
Publication Number 2013/025452
Status In Force
Filing Date 2012-08-10
Publication Date 2013-02-21
Owner
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Selnick, Harold, G.
  • Liu, Kun
  • Mceachern, Ernest, J.
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

34.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2012050434
Publication Number 2013/000085
Status In Force
Filing Date 2012-06-27
Publication Date 2013-01-03
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest, J.
  • Vocadlo, David, J.
  • Zhou, Yuanxi
  • Selnick, Harold, G.

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.

IPC Classes  ?

  • C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings
  • C07D 277/82 - Nitrogen atoms
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

35.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2012050435
Publication Number 2013/000086
Status In Force
Filing Date 2012-06-27
Publication Date 2013-01-03
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
  • C07D 513/04 - Ortho-condensed systems

36.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Document Number 02840013
Status In Force
Filing Date 2012-06-27
Open to Public Date 2013-01-03
Grant Date 2021-02-09
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C07D 513/04 - Ortho-condensed systems
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

37.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2012050433
Publication Number 2013/000084
Status In Force
Filing Date 2012-06-27
Publication Date 2013-01-03
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
  • C07D 513/04 - Ortho-condensed systems

38.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CN2011074569
Publication Number 2012/159262
Status In Force
Filing Date 2011-05-24
Publication Date 2012-11-29
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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-Glc NAcase, accumulation or deficiency of O-Glc NAc.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07D 513/14 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase

39.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2012000267
Publication Number 2012/129651
Status In Force
Filing Date 2012-03-20
Publication Date 2012-10-04
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Liu, Kun
  • Selnick, Harold G.
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Wang, Xiaona

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.

IPC Classes  ?

  • C07H 15/12 - Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of a saccharide radical
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C07H 11/00 - Compounds containing saccharide radicals esterified by inorganic acidsMetal salts thereof
  • C07H 13/00 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
  • C07H 13/12 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group —X—C (=X)—X—, or halides thereof, in which X means nitrogen, oxygen, sulfur, selenium, or tellurium, e.g. carbonic acid, carbamic acid
  • C07H 15/18 - Acyclic radicals, substituted by carbocyclic rings
  • C07H 17/07 - Benzo[b]pyran-4-ones
  • C07H 19/04 - Heterocyclic radicals containing only nitrogen as ring hetero atom
  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase

40.

PYRANO[3,2-D]THIAZOL DERIVATIVES AND USES AS SELECTIVE GLYCOSIDASE INHIBITORS THEREOF

      
Application Number CN2011072330
Publication Number 2012/129802
Status In Force
Filing Date 2011-03-31
Publication Date 2012-10-04
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
  • SIMON FRASER UNIVERSITY (Canada)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Liu, Kun
  • Selnick, Harold G.
  • Wei, Zhongyong
  • Mu, Changwei
  • Wang, Yaode
  • Wang, Xiaona

Abstract

Pyrano[3,2-d]thiazol derivatives of formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds are provided. Methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc are also provided.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

41.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2012000247
Publication Number 2012/126091
Status In Force
Filing Date 2012-03-16
Publication Date 2012-09-27
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Coburn, Craig A.
  • Liu, Kun
  • Selnick, Harold G.

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C07H 13/02 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
  • C07D 513/04 - Ortho-condensed systems
  • C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)

42.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2011001397
Publication Number 2012/083435
Status In Force
Filing Date 2011-12-21
Publication Date 2012-06-28
Owner
  • ALECTOS THERAPEUTICS, INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Kaul, Ramesh
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C07D 513/04 - Ortho-condensed systems
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase

43.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2011001241
Publication Number 2012/061927
Status In Force
Filing Date 2011-11-08
Publication Date 2012-05-18
Owner
  • ALECTOS THERAPEUTICS, INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Coburn, Craig A.
  • Liu, Kun
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
  • C07H 13/02 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
  • C07D 513/04 - Ortho-condensed systems

44.

PYRANO[3,2-D]THIAZOL DERIVATIVES AND USES THEREOF AS SELECTIVE GLYCOSIDASE INHIBITORS

      
Application Number CN2011080691
Publication Number 2012/062157
Status In Force
Filing Date 2011-10-12
Publication Date 2012-05-18
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Chang, Jiang
  • Liu, Kun
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Shi, Feng
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

Abstract

Pyrano[3,2-d]thiazol derivatives of formula (I) for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds are disclosed. Methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc are also provided.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 37/08 - Antiallergic agents
  • A61P 9/00 - Drugs for disorders of the cardiovascular system

45.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number US2011059668
Publication Number 2012/064680
Status In Force
Filing Date 2011-11-08
Publication Date 2012-05-18
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Chang, Jiang
  • Liu, Kun
  • Mceachern, Ernest, J.
  • Mu, Changwei
  • Selnick, Harold, G.
  • Shi, Feng
  • Vocadlo, David, J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

46.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Document Number 02816798
Status In Force
Filing Date 2011-11-08
Open to Public Date 2012-05-18
Grant Date 2019-02-26
Owner ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Liu, Kun
  • Selnick, Harold G.
  • Chang, Jiang
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Shi, Feng
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

  • C07H 9/06 - Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing nitrogen as ring hetero atoms
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom

47.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CN2010078527
Publication Number 2012/061971
Status In Force
Filing Date 2010-11-08
Publication Date 2012-05-18
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Coburn, Craig A.
  • Liu, Kun
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi

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-Glc NAcase, accumulation or deficiency of O-Glc NAc.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/04 - Immunostimulants
  • A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
  • A61P 37/08 - Antiallergic agents
  • A61P 11/02 - Nasal agents, e.g. decongestants
  • A61P 11/06 - Antiasthmatics
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 25/16 - Anti-Parkinson drugs
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 17/06 - Antipsoriatics

48.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CN2010078528
Publication Number 2012/061972
Status In Force
Filing Date 2010-11-08
Publication Date 2012-05-18
Owner
  • ALECTOS THERAPEUTICS INC. (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
Inventor
  • Liu, Kun
  • Mceachern, Ernest J.
  • Mu, Changwei
  • Selnick, Harold G.
  • Vocadlo, David J.
  • Wang, Yaode
  • Wei, Zhongyong
  • Zhou, Yuanxi
  • Zhu, Yongbao

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.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/04 - Immunostimulants
  • A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
  • A61P 37/08 - Antiallergic agents
  • A61P 11/02 - Nasal agents, e.g. decongestants
  • A61P 11/06 - Antiasthmatics
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 25/16 - Anti-Parkinson drugs
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 17/06 - Antipsoriatics

49.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

      
Application Number CA2011000548
Publication Number 2011/140640
Status In Force
Filing Date 2011-05-10
Publication Date 2011-11-17
Owner
  • SIMON FRASER UNIVERSITY (Canada)
  • MERCK SHARP & DOHME CORP. (USA)
  • ALECTOS THERAPEUTICS INC. (Canada)
Inventor
  • Li, Tong-Shuang
  • Mceachern, Ernest J.
  • Vocadlo, David J.
  • Zhou, Yuanxi
  • Zhu, Yongbao
  • Liu, Kun
  • Selnick, Harold G.

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-G1cNAcase, accumulation or deficiency of O-G1cNAc.

IPC Classes  ?

  • C07D 277/60 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 263/54 - BenzoxazolesHydrogenated benzoxazoles
  • C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase