Substituted Pyridines as Inhibitors of DNMT1

N. David Adams; Andrew Benowitz; Maria  Lourdes; Karen Evans; David T Fosbenner; Bryan King; Mei Li; Juan Luengo; William Miller; Alexander Reif; Stuart Romeril; Stanley Schmidt; Roger Butlin; Kristin Goldberg; Allan Jordan; Christopher Kershaw; Ali Raoof; Bohdan Waszkowycz

Substituted Pyridines as Inhibitors of DNMT1

N. David Adams (Inventor)
, Andrew Benowitz (Inventor)
, Maria Lourdes (Inventor)
, Karen Evans (Inventor)
, David T Fosbenner (Inventor)
, Bryan King (Inventor)
, Mei Li (Inventor)
, Juan Luengo (Inventor)
, William Miller (Inventor)
, Alexander Reif (Inventor)
, Stuart Romeril (Inventor)
, Stanley Schmidt (Inventor)
, Roger Butlin (Inventor)
, Kristin Goldberg (Inventor)
, Allan Jordan (Inventor)
, Christopher Kershaw (Inventor)
, Ali Raoof (Inventor)
, Bohdan Waszkowycz (Inventor)

Cancer Research UK Manchester Institute

Research output: Patent

Abstract

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Original language	English
Patent number	WO2017216727
Priority date	21/12/17
Publication status	Published - 21 Dec 2017

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title = "Substituted Pyridines as Inhibitors of DNMT1",

abstract = "The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.",

author = "Adams, \{N. David\} and Andrew Benowitz and Maria Lourdes and Karen Evans and Fosbenner, \{David T\} and Bryan King and Mei Li and Juan Luengo and William Miller and Alexander Reif and Stuart Romeril and Stanley Schmidt and Roger Butlin and Kristin Goldberg and Allan Jordan and Christopher Kershaw and Ali Raoof and Bohdan Waszkowycz",

year = "2017",

month = dec,

day = "21",

language = "English",

type = "Patent",

note = "WO2017216727",

}

TY - PAT

T1 - Substituted Pyridines as Inhibitors of DNMT1

AU - Adams, N. David

AU - Benowitz, Andrew

AU - Lourdes, Maria

AU - Evans, Karen

AU - Fosbenner, David T

AU - King, Bryan

AU - Li, Mei

AU - Luengo, Juan

AU - Miller, William

AU - Reif, Alexander

AU - Romeril, Stuart

AU - Schmidt, Stanley

AU - Butlin, Roger

AU - Goldberg, Kristin

AU - Jordan, Allan

AU - Kershaw, Christopher

AU - Raoof, Ali

AU - Waszkowycz, Bohdan

PY - 2017/12/21

Y1 - 2017/12/21

N2 - The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

AB - The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

M3 - Patent

M1 - WO2017216727

ER -

Substituted Pyridines as Inhibitors of DNMT1

Abstract

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