Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Substituted quinazolines

A technology of drugs and compounds, applied in the field of imidazoquinazoline derivatives, can solve problems such as unawareness of anti-megakaryocyte potential

Inactive Publication Date: 2013-04-24
SHIRE PLC
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this disclosure fails to recognize a completely independent anti-megakaryocyte potential (decrease in platelet count) that may be associated with certain analogs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Substituted quinazolines
  • Substituted quinazolines
  • Substituted quinazolines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153] IC of anagrelide and certain 3-alkyl substituted analogues as PDE III inhibitors and antimegakaryocyte agents 50 Comparative data.

[0154] The table below shows the comparative activity of anagrelide and its analogs with respect to their effects on megakaryopoiesis (the process of producing platelets) and PDE III (the inhibition of which leads to adverse cardiovascular reactions).

[0155] Comparison of In Vitro Evaluation of Potential Therapeutic Effects and Adverse Effects of Anagrelide and Its Analogues

[0156] compound

IC against megakaryocytes 50

(thrombocytopenia activity)

IC for PDE III inhibition 50

(cardiovascular effects)

Benefit rate (therapeutic effect

compared with adverse effects)

Anagra

3-Hydroxyanagrelide

27nM

44nM

32nM

0.7nM

* 0.024∶1

0.016∶1

3,3-Dimethyl anagrelide

164nM

166nM

1∶1

3-Spirocyclopropyl anagrelide

547nM

797nM

1.45...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention relates to 3- and 5-substituted analogs of the selective platelet lowering agent anagrelide, which have the potential to reduce cardiovascular side effects and lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More particularly, the present invention relates to certain imidazoquinazoline derivatives that have utility as platelet lowering agents in humans. The compounds of the present invention act by inhibiting megakaryocytopoiesis and thereby inhibiting platelet formation.

Description

technical field [0001] The present invention relates to 3- and 5-substituted analogs of the selective platelet lowering agent anagrelide, which have the potential to reduce cardiovascular side effects and lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More particularly, the present invention relates to certain imidazoquinazoline derivatives that have utility as platelet lowering agents in humans. The compounds of the present invention act by inhibiting megakaryocytopoiesis and thereby inhibiting platelet formation. Background technique [0002] Anagrelide Hydrochloride is a novel orally administered imidazoquinazoline that selectively reduces platelet counts in humans and is used in the treatment of myeloproliferative disorders (MPD) such as essential thrombocythemia (ET) To this end, an elevated platelet count in said disease can place the patient at increased risk for thrombosis. The chemical structure of anagrelide, 6,7...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/505A61P43/00
CPCC07D487/04A61P43/00A61P7/02A61K31/505
Inventor 理查德·富兰克林伯纳德·戈尔丁
Owner SHIRE PLC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com