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Aminopyrimidine inhibitors of histamine receptors for the treatment of disease

A technology for diseases, alkylation, applied in the field of medicine

Inactive Publication Date: 2011-09-14
KALYPSYS INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Finally, among other side effects, H 1 Sedation by R antagonists limits many H 1 Use of R antagonists in diseases for which they would otherwise be effective

Method used

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  • Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
  • Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
  • Aminopyrimidine inhibitors of histamine receptors for the treatment of disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0302]

[0303] 4-(4-(3,4-dichlorophenyl)piperazin-1-yl)-5-methylthieno[2,3-d]pyrimidine

[0304] The title compound was obtained commercially.

Embodiment 2

[0306]

[0307] 5-methyl-4-(4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine

[0308] The title compound was obtained commercially.

Embodiment 3

[0310]

[0311] 4-(4-(2-Chlorophenyl)piperazin-1-yl)-5-methylthieno[2,3-d]pyrimidine

[0312] The title compound was obtained commercially.

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PUM

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Abstract

The present invention relates to compounds and methods which may be useful as inhibitors of HiR and / or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.

Description

[0001] This application claims the benefit of priority from US Provisional Patent Application Serial No. 61 / 095,819, filed September 10, 2008, the disclosure of which is hereby incorporated by reference as if incorporated herein in its entirety. technical field [0002] Disclosed herein are novel heterocyclic compounds and compositions, and their use as medicaments for the treatment of disease. Also provided are methods of inhibiting the activity of histamine receptors in a human or animal subject for the treatment of allergic disease, inflammation, asthma, rhinitis, chronic obstructive pulmonary disease, conjunctivitis, rheumatoid arthritis, and generalized and localized pruritus disease. Background technique [0003] Histamine, a low molecular weight biogenic amine, is a potent chemical modulator of normal and pathophysiology. Histamine functions as a secreted signal and neurotransmitter of immune and inflammatory responses. Through four different cell surface receptors ...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P29/00A61P37/08A61P27/02
CPCA61K9/0048A61K31/519A61K9/0043A61K31/4365A61K9/0073C07D495/04A61K31/5377A61K31/497A61K45/06A61P1/00A61P11/02A61P11/06A61P17/00A61P17/04A61P19/02A61P25/04A61P27/02A61P29/00A61P29/02A61P37/00A61P37/06A61P37/08A61P43/00A61K2300/00
Inventor A·J·博尔夏特C·博勒加德R·L·戴维斯D·A·加马什J·M·扬尼
Owner KALYPSYS INC
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