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Heterocyclic aspartyl protease inhibitors

A heteroaryl and solvate technology, applied in the field of heterocyclic aspartyl protease inhibitors, can solve the problems of not being able to stop the disease process and not meeting medical requirements

Inactive Publication Date: 2007-02-14
MERCK & CO INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing AD treatments are palliative, and while they improve cognitive and behavioral impairments, they do not halt disease progression
Therefore, the medical requirement for AD treatment that halts the disease process is not met

Method used

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  • Heterocyclic aspartyl protease inhibitors
  • Heterocyclic aspartyl protease inhibitors
  • Heterocyclic aspartyl protease inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0072] Compounds of formula I (wherein X, W and U are as defined above) include each of the following preferred structures:

[0073]

[0074] In compounds of formulas IA to IF, U is preferably a bond or -C(R 6 )(R 7 )-. In compounds of formula IG and IH, U is preferably -C(O)-.

[0075] It should be understood that since R 1 The definition of R 5 The definition of is the same, so when X is -N(R 5 )-, then W is a chemical bond and U is a chemical bond, -S(O)-, -S(O) 2 -, -C(O)-, -O-, -C(R 6 )(R 7 )-or-N(R 5 )-The compound of formula I is equivalent to U being a chemical bond and W being a chemical bond, -S(O)-, -S(O) 2 -, -C(O)-, -O-, -C(R 6 )(R 7 )-or-N(R 5 )- compound of formula I.

[0076] Compounds of the present invention are more preferably compounds of formula IB in which U is a chemical bond or U is -C(R 6 )(R 7 )- compound of formula IB.

[0077] Another preferred group of compounds of formula I are R 2 A compound of formula I which is H.

[0078] ...

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PUM

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Abstract

Compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

Description

field of invention [0001] The present invention relates to heterocyclic aspartyl protease inhibitors, pharmaceutical compositions containing said compounds, their use in the treatment of cardiovascular diseases, cognitive diseases and neurodegenerative diseases and their use as human immunodeficiency virus, malaria parasite Use of plasmepsin, cathepsin D and protozoan inhibitors. Background technique [0002] Eight human aspartic proteases of the Al (pepsin-like) family are known to date to be involved in various pathological conditions: pepsin A and C, renin, BACE, BACE2, Napsin A, cathepsin D. [0003] A role for the renin-angiotensin system (RAS) in the regulation of blood pressure and body fluid electrolytes has been identified (Oparil, S. et al., N Engl J Med 1974; 291:381-401 / 446-57). The octapeptide angiotensin-II, a potent vasoconstrictor and adrenal aldosterone-stimulating substance, is processed from the precursor decapeptide angiotensin-I, which in turn is derive...

Claims

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Application Information

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IPC IPC(8): A61K31/4168A61K31/4178C07D233/88C07D239/22C07D271/06C07D401/04C07D401/10C07D401/12C07D401/14C07D403/06C07D403/10C07D403/14C07D405/06C07D405/14C07D407/14C07D235/02C07D271/07C07D401/06C07D403/04C07D403/12C07D405/04C07D405/10C07D405/12C07D409/06C07D409/10C07D409/14C07D413/06C07D413/12C07D413/14C07D417/12
CPCC07D413/12C07D271/07C07D403/12C07D239/22C07D409/14C07D401/14C07D413/06C07D409/10C07D235/02C07D403/04C07D403/06C07D403/10C07D401/12C07D401/06C07D405/06C07D417/12C07D401/04C07D405/14C07D413/14C07D401/10C07D233/88C07D405/10C07D405/12C07D405/04C07D409/06A61P13/12A61P25/00A61P25/28A61P31/00A61P31/10A61P31/18A61P33/00A61P33/02A61P33/06A61P35/00A61P43/00A61P9/00A61P9/12
Inventor Z·朱B·麦基特里克Z·-Y·孙Y·C·叶J·H·沃伊特C·斯特里克兰E·M·史密斯A·斯坦福德W·J·格林利Y·吴U·艾瑟洛R·马佐拉J·考德威尔J·卡明L·王T·郭T·X·H·勒K·W·赛翁茨S·D·巴布R·C·亨特
Owner MERCK & CO INC
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