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8‑substituted 2‑amino‑[1,2,4]triazolo[1,5‑a]pyrazines as syk tyrosine kinase inhibitors and gcn2 serine kinase inhibitors

A technology of triazolo and C81, applied in anti-inflammatory agents, metabolic diseases, antifungal agents, etc., can solve the problems of only moderate anti-tumor efficacy and poor response

Active Publication Date: 2017-10-24
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in several tumor models, 1MT failed to induce tumor regression, suggesting only modest antitumor efficacy when IDO inhibition is administered as monotherapy
In contrast, combination treatment with 1MT and multiple cytotoxic chemotherapeutic agents induced regression of established MMTV-neu / HER2 tumors that responded poorly to any single agent treatment [Muller et al 2005a]

Method used

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  • 8‑substituted 2‑amino‑[1,2,4]triazolo[1,5‑a]pyrazines as syk tyrosine kinase inhibitors and gcn2 serine kinase inhibitors
  • 8‑substituted 2‑amino‑[1,2,4]triazolo[1,5‑a]pyrazines as syk tyrosine kinase inhibitors and gcn2 serine kinase inhibitors
  • 8‑substituted 2‑amino‑[1,2,4]triazolo[1,5‑a]pyrazines as syk tyrosine kinase inhibitors and gcn2 serine kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[1486] Example A: Injection Vials

[1487] A solution of 100 g of the active ingredient of formula I and 5 g of disodium hydrogen phosphate in 3 l of double distilled water was adjusted to pH 6.5 with 2 N hydrochloric acid, sterile filtered, transferred to injection vials, lyophilized under sterile conditions and placed in Seal under sterile conditions. Each injection vial contains 5 mg of active ingredient.

Embodiment B

[1488] Example B: Suppositories

[1489] A mixture of 20 g of the active ingredient of formula I was melted with 100 g of soy lecithin and 1400 g of cocoa butter, poured into molds and allowed to cool. Each suppository contains 20 mg of active ingredient.

Embodiment C

[1490] Example C: Solution

[1491] A solution was prepared from 1 g of active ingredient of formula I, 9.38 g NaH2PO4∙2 H2O, 28.48 g Na2HPO4∙12 H2O and 0.1 g benzalkonium chloride in 940 ml double distilled water. The pH was adjusted to 6.8 and the solution was made up to 1 l and sterilized by irradiation. This solution is available in the form of eye drops.

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PUM

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Abstract

Compounds of formula I, wherein R1 , R2 and R4 have the meanings indicated in claim 1 , are inhibitors of Syk and are especially useful in the treatment of cancer, rheumatoid arthritis and / or systemic lupus.

Description

Background of the invention [0001] The object of the present invention was to find novel compounds having valuable properties, in particular those which can be used for the preparation of medicaments. [0002] The present invention relates to compounds and uses of compounds wherein signal transduction via kinases, in particular tyrosine kinases, are inhibited, modulated and / or modulated, furthermore the invention relates to pharmaceutical compositions comprising these compounds and the use of said compounds in Use in the treatment of kinase-induced diseases. [0003] Because protein kinases regulate nearly every cellular process, including metabolism, cell proliferation, cell differentiation, and cell survival, they are attractive targets for therapeutic intervention in various disease states. For example, cell-circulation control and angiogenesis, in which protein kinases play a pivotal role, are cellular processes associated with numerous disease conditions such as, but not...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04C07D519/00A61K31/4985A61P35/00A61P29/00A61P25/00
CPCC07D487/04C07D519/00A61K31/496A61K31/519A61K31/537A61K31/5377A61K31/5386A61K31/55A61K31/5513A61P1/00A61P3/00A61P3/10A61P7/02A61P9/00A61P9/10A61P11/06A61P17/00A61P17/06A61P19/02A61P25/00A61P25/14A61P25/16A61P25/28A61P29/00A61P31/10A61P31/14A61P31/18A61P31/22A61P33/06A61P35/00A61P37/00A61P37/06A61P37/08A61P43/00Y02A50/30
Inventor C.多伊奇D.库恩T.罗斯L.布格多夫
Owner MERCK PATENT GMBH
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