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CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES SUCH AS TAUOPATHIES

a neurodegenerative disease and inhibitory technology, applied in the field of casein kinase 1 delta (ck1) inhibitors, can solve the problems of reducing the ability of tau to promote microtubule assembly and stabilize the assembled microtubules

Inactive Publication Date: 2016-12-08
ELECTROPHORETICS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0075]In one embodiment, the compound of formula (ID) is selected from any of compounds: 682, 954, 964, 978-979 and 997 as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds of this embodiment were tested in the CK1δ inhibition assay as described herein and exhibited inhibition of greater than 50%.

Problems solved by technology

However, increased phosphorylation of tau on multiple serine and threonine residues reduces the ability of tau to promote microtubule assembly and to stabilise assembled microtubules, effects that have been demonstrated both in vitro and in cells.

Method used

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  • CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES SUCH AS TAUOPATHIES
  • CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES SUCH AS TAUOPATHIES
  • CASEIN KINASE 1delta (CK 1delta) INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES SUCH AS TAUOPATHIES

Examples

Experimental program
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Embodiment Construction

[0011]According to a first aspect of the invention there is provided a pharmaceutical composition comprising a compound of formula (IA) or a pharmaceutically acceptable salt or solvate thereof:

wherein

“Het A” represents a 4 or 5 membered heterocyclic ring system containing 1 to 3 heteroatoms selected from O, N or S, wherein said ring system is optionally fused to one or more (e.g. 1-3) further rings to form a polycyclic ring system comprising up to 4 rings; X and Y independently represent a bond, —C(R7a)(R8a)—,(CH2)2, —O—, —S—, —CH2—O—, —(CH2)2—O—, NR6a, —N(R6a)—C(R7a)(R8a)—, —N(R6a)—(CH2)2—, —N(R6a)—(CH2)3—, —CH2—N(R6a)—(CH2)2—, —N(R6a)—CO—, —CH2—NH—CO—(CH2)2—, —N(R6a)—CO—CH2—, —N(R6a)—OO—(CH2)2—, —CO—N(R6a)—CH2—, ═N—, —C(H)(CN)—, —C(═N—NH—COC1-6 alkyl)-, —CH═C(R6a)—OO—, ═CH—, —CH═CH—, ═CH—CO—, —N═CH—, —N═C(Me)—, —C(R6a)═CH—, —NH—N═C(H)—, —NH—CO—C(═CH-heteroaryl)-, —C═C(Me)2—, —CH═CH—CO—N(R6a)—, —CH═C(R6a)—NH—CO—, —CH═C(R6a)—C—O—CH2—, —CS—S—CH2—, —NH—CS—NH—, —NH—CS—NH—CH2—, —NH—CS—N...

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Abstract

The invention relates to pharmaceutical compositions comprising casein kinase 1 delta (CK1δ) and to the use of said inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.

Description

CROSS-REFERENCE TO RELATED APPLICATION(S)[0001]This application is a divisional application that claims priority to U.S. application Ser. No. 13 / 993,288 filed on Sep. 19, 2013, which is the U.S. national stage entry of International Patent Application No. PCT / GB2011 / 052475 filed on Dec. 14, 2011, which claims priority to GB Application No. 1109162.6 filed on Jun. 1, 2011 and GB Application No. 1021161.3 filed on Dec. 14, 2010, the entire contents of each of which is incorporated herein by reference in their entireties.FIELD OF THE INVENTION[0002]The invention relates to pharmaceutical compositions comprising casein kinase 1 delta (CK1δ) inhibitors and to the use of said inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.BACKGROUND OF THE INVENTION[0003]Alzheimer's disease (AD; also known as senile dementia of the Alzheimer type (SDAT), primary degenerative dementia of the Alzheimer's type (PDDAT), or Alzheimer's) is the most common form of dementi...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/517A61K31/444A61K31/506
CPCA61K31/517A61K31/444A61K31/506A61K31/343A61K31/36A61K31/381A61K31/397A61K31/404A61K31/416A61K31/4184A61K31/4192A61K31/4196A61K31/42A61K31/423A61K31/4245A61K31/427A61K31/428A61K31/429A61K31/433A61K31/437A61K31/4439A61K31/4709A61K31/497A61K31/4985A61K31/502A61K31/5025A61K31/519A61K31/53A61K31/5377A61K31/538A61K31/549A61K31/55C07D209/42C07D277/68C07D401/04C07D403/06C07D405/04C07D405/12C07D407/12C07D413/06C07D413/14C07D487/04C07D487/14C07D495/14C07D401/12C07D471/04A61K31/4045A61P21/00A61P21/02A61P21/04A61P25/00A61P25/16A61P25/28A61P39/02A61P43/00
Inventor SHERIDAN, JOSEPH M.HEAL, JONATHAN R.HAMILTON, WILLIAM D.O.PIKE, IAN
Owner ELECTROPHORETICS LTD
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