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Sphingosine kinase inhibitors

A compound, R19 technology, applied in the field of sphingosine kinase inhibitors, can solve the problem of not identifying the interaction partner

Inactive Publication Date: 2014-07-23
MERCK PATENT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, no intracellular interaction partners of S1P have been identified

Method used

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Experimental program
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Embodiment Construction

[0329] I. Synthesis of Selected Compounds of the Invention

[0330] The following compounds were synthesized and identified. However, it is within the knowledge of those skilled in the art to prepare and identify these compounds in other ways.

[0331] FS101:

[0332] tert-butyl 4-[6-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)pyridin-2-yl]piperazine-1-carboxylate :

[0333]

[0334] 150 mg (0.44 mmol) of 4-(6-bromopyridin-2-yl) piperazine-1-carboxylic acid tert-butyl ester, 112 mg (0.48 mmol) of 5,5,8,8-tetramethyl-5, 6,7,8-tetrahydronaphthalen-2-ylboronic acid and 202 mg (0.88 mmol) of tripotassium phosphate monohydrate were suspended in 6 ml of ethylene glycol monomethyl ether, degassed several times, and degassed under a nitrogen atmosphere 25 mg (0.04 mmol) of bis(triphenylphosphine)palladium(II) dichloride were added. The reaction mixture was stirred at 80° C. for 16 hours, cooled to room temperature, and 20 ml of water were added. The mixture was ex...

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Abstract

The present invention relates to compounds of formula (I) and their physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers, including their Mixtures in all proportions, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in claim 1.

Description

technical field [0001] The present invention relates to sphingosine kinase inhibitors and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof for use in the treatment of diseases affected by the inhibition of Sph kinase 1, including mixtures in all their proportions. Background of the invention [0002] The object of the present invention was to discover new compounds having valuable properties, in particular those which can be used for the preparation of medicaments. [0003] The present invention relates to compounds and the use of these compounds for the treatment of diseases associated with elevated levels of sphingosine phosphate, and to pharmaceutical compositions comprising these compounds. [0004] In particular, the present invention relates to compounds of formula (I), which preferably inhibit the enzyme sphingosine kinase 1, which regulates sphingosine phosphate levels through the phosphorylation of sphingosine, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/63C07D239/42C07D251/40C07D401/14C07D403/04C07D295/145A61K31/4427A61K31/506A61K31/53A61P35/00A61P29/00
CPCC07B2200/05C07D213/61C07D403/04C07D413/14C07D251/22C07D295/096C07D239/42C07D401/14C07D241/20A61K31/444C07F5/025C07D213/74C07D295/088C07D213/65C07D295/033C07D401/04A61P1/00A61P1/04A61P1/16A61P11/00A61P11/06A61P13/00A61P13/08A61P13/10A61P13/12A61P15/00A61P17/00A61P17/06A61P17/08A61P17/10A61P19/02A61P25/00A61P27/02A61P29/00A61P35/00A61P35/02A61P37/00A61P37/06A61P37/08A61P9/00A61P9/10A61P3/10A61K31/497
Inventor F·施蒂贝尔D·维恩克
Owner MERCK PATENT GMBH
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