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Aspartyl protease inhibitors

A solvate and compound technology, applied in the field of aspartyl protease inhibitors, can solve problems such as unmet medical needs

Inactive Publication Date: 2010-03-10
SCHERING AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus there remains an unmet medical need for AD treatments that terminate the disease process

Method used

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  • Aspartyl protease inhibitors
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Embodiment Construction

[0069] Unless otherwise stated, it should be understood that divalent groups are read from left to right.

[0070] The present invention relates to a compound of structural formula (I) or its stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate,

[0071]

[0072] Where R 1 , R 2 , R 3 , R 4 , W, Z, Y, X, V, A, p and each R 14 Choose independently of each other, and among them:

[0073] p is an integer from 0 to 5;

[0074] The dotted line in formula (I) Represents a single bond or a double bond;

[0075] Ring A, V and X together form a monocyclic or polycyclic 4 to 12 membered cycloalkylene, cycloalkenylene, heterocycloalkylene or heterocycloalkenylene, wherein the heterocycloalkylene or heterocycloalkylene One or more heteroatoms of cycloalkenyl are independently selected from: -O-, -S-, -S(O)-, -S(O) 2 -And-N(R 5 )-;

[0076] Or ring A, V and X together form a monocyclic or polycyclic 4 to 12 membered arylene or heteroarylene group;

[0077] W is -S(O)-, -S(O) 2 -, -...

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Abstract

Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R<1>, R<2>, R<3>, R<4>, R<14>, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. 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 m1 agonist or m2 antagonist.

Description

Invention field [0001] The present invention relates to an aspartyl protease inhibitor, a pharmaceutical composition containing the compound, and its use in the treatment of cardiovascular diseases, cognitive diseases and neurodegenerative diseases, and its use as human immunodeficiency virus and plasmodium Use of plasmepsin, cathepsin D and protozoan enzyme inhibitors. Background technique [0002] Many aspartic proteases are known to be associated with pathological symptoms, including pepsin A and C, renin, BACE, BACE 2, Napsin A, and cathepsin D. The role of the renin-angiotensin system (RAS) in regulating blood pressure and fluid electrolytes has been clarified (Oparil, S, et al., N Engl J Med 1974; 291:381-401 / 446-57) . Angiotensin octapeptide II is a potent vasoconstrictor and a stimulator for the release of adrenal aldosterone. It is processed from the precursor decapeptide angiotensin I, which is It is produced by reninase processing of angiotensinogen. It has also be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/95C07D471/14A61K31/519A61P25/00
CPCC07D239/95C07D471/14A61P13/12A61P25/00A61P25/28A61P27/02A61P31/12A61P31/18A61P33/06A61P35/00A61P43/00A61P9/00A61P9/04A61P9/12A61K31/519
Inventor 朱昭宁A·史丹佛M·曼德刘小翔
Owner SCHERING AG